MedWorm: Carbamazepine

Anticonvulsants for alcohol withdrawal.

Cochrane Database of Systematic Reviews — Sat, 20 Mar 2010 06:22:03 +0100

CONCLUSIONS: Results of this review do not provide sufficient evidence in favour of anticonvulsants for the treatment of AWS. There are some suggestions that carbamazepine may actually be more effective in treating some aspects of alcohol withdrawal when compared to benzodiazepines, the current first-line regimen for alcohol withdrawal syndrome. Anticonvulsants seem to have limited side effects, although adverse effects are not rigorously reported in the analysed trials. PMID: 20238337 [PubMed - in process] (Source: Cochrane Database of Systematic Reviews)

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Association between HLA-B*1502 and carbamazepine-induced severe cutaneous adverse drug reactions in a Thai population

Epilepsia — Fri, 19 Mar 2010 00:00:00 +0100

Carbamazepine (CBZ) has been reported as the most common culprit drug for Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) in several Asian countries including Thailand. A strong association between HLA-B*1502 and CBZ-induced SJS/TEN has been reported in Han Chinese but not in Caucasian and Japanese populations. A case[ndash]control study was conducted to determine whether HLA-B*1502 is a valid pharmacogenetic test for SJS/TEN caused by CBZ in a Thai population. Among 42 CBZ-induced patients with SJS/TEN, 37 (88.10%) patients carried the HLA-B*1502 while only 5 (11.90%) of the CBZ-tolerant controls had this allele. The risk of CBZ-induced SJS/TEN was significantly higher in the patients with HLA-B*1502, with an odds ratio (OR) of 54.76 [95% confidence interval (CI) 14.62...

Development of a New Method to Get a Reliable Powder Flow Characteristics Using Only 1 to 2 g of Powder.

AAPS PharmSciTech — Thu, 18 Mar 2010 00:00:00 +0100

Authors: Seppälä K, Heinämäki J, Hatara J, Seppälä L, Yliruusi J In powder technology, it is often important to directly measure real powder flow rate from a small amount of powder. For example, in pharmaceutical industry, a frequent problem is to determine powder flow properties of new active pharmaceutical ingredient (API) in an early stage of the development when the amount of API is limited. The purpose of this paper is to introduce a new direct method to measure powder flow when the material is poorly flowing (cohesive) and the amount of material is about 1 to 2 g. The measuring system was simple, consisting of a flow chamber and electronic balance and an automated optical detection system, and for each measurement, only 1 to 2 g of sample was require...

Effects of oxcarbazepine and carbamazepine on driving ability: a double-blind, randomized crossover trial with healthy volunteers

Psychopharmacology — Tue, 16 Mar 2010 14:48:41 +0100

Conclusions Under both drugs, driving performance was worse than at baseline. Even though deterioration of driving performance was only slightly less pronounced under OXC than under CBZ, it might be recommended as more appropriate than CBZ for epileptic patients who need to drive a car. Content Type Journal ArticleCategory Original InvestigationDOI 10.1007/s00213-010-1814-yAuthors Yvonne Kaussner, University of Würzburg Center for Traffic Sciences, Department of Psychology Würzburg GermanyRamona Kenntner-Mabiala, Würzburg Institute for Traffic Sciences Raiffeisenstraße 17 97209 Veitshöchheim GermanySonja Hoffmann, Würzburg Institute for Traffic Sciences Raiffeisenstraße 17 97209 Veitshöchheim GermanyJan Klatt, Novartis Pharma GmbH Nürnberg GermanyFerenc Tra...

[Review] Voltage-gated sodium channels as therapeutic targets in epilepsy and other neurological disorders

Lancet Neurology — Mon, 15 Mar 2010 00:00:00 +0100

Voltage-gated sodium channels (VGSCs) are key mediators of intrinsic neuronal and muscle excitability. Abnormal VGSC activity is central to the pathophysiology of epileptic seizures, and many of the most widely used antiepileptic drugs, including phenytoin, carbamazepine, and lamotrigine, are inhibitors of VGSC function. These antiepileptic drugs might also be efficacious in the treatment of other nervous system disorders, such as migraine, multiple sclerosis, neurodegenerative diseases, and neuropathic pain. In this Review, we summarise the structure and function of VGSCs and their involvement in the pathophysiology of several neurological disorders. We also describe the biophysical and molecular bases for the mechanisms of action of antiepileptic VGSC blockers and discuss the efficacy of...

HLA-B*15 subtypes distribution in Han population in Beijing, China, as compared with those of other populations

International Journal of Immunogenetics — Sun, 14 Mar 2010 00:00:00 +0100

To identify HLA-B*15 subtypes distribution in Han population in Beijing, People's Republic of China, 826 unrelated healthy individuals were typed using the polymerase chain reaction-sequence-based typing method. Within the 246 HLA-B*15 positive individuals, 29 HLA-B*15 alleles were identified, the most predominant of which is B*1501 (40.07%), followed by B*1502 (12.87%), B*1511 (12.87%), B*1518 (9.19%) and B*1532 (3.31%). The distribution of HLA-B*15 subtype frequencies was compared between the Beijing Han, eight other Chinese ethnic minorities and six Chinese populations covering the mainland of China, Taiwan, Hong Kong and Singapore. A neighbor-joining phylogenetic tree was constructed and revealed that the Beijing Han population clustered into the northern populations group and had a cl...

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Growth hormone levels in children and adolescents with epilepsy.

European Journal of Paediatric Neurology — Fri, 12 Mar 2010 00:00:00 +0100

In conclusion, physical growth seems to be affected in patients with epilepsy. This may be due to hormonal imbalance as evident by reduced post provocation GH levels and IGF-1 levels in the included group of patients. PMID: 20227898 [PubMed - as supplied by publisher] (Source: European Journal of Paediatric Neurology)

Stevens Johnson syndrome after carbamazepine and SJS/TEN overlap syndrome after amoxicillin: case reports and a review

Articles of Archives of Medical Science - TERMEDIA publishing house — Tue, 09 Mar 2010 16:16:09 +0100

We present a case of Stevens Johnson syndrome in a child after carbamazepine application and Stevens Johnson/TEN overlap syndrome in an adult after amoxicillin application. On the basis of two reported cases we review the most commonly associated drugs, the postulated pathogenesis, clinical manifestation and management in these severe life-threatening diseases. We especially discuss the controversial systemic corticosteroid therapy. Topical care is also discussed. (Source: Articles of Archives of Medical Science - TERMEDIA publishing house)

49. Paroxysmal dystonia and epilepsy – one differential diagnostic aspect

Clinical Neurophysiology — Mon, 08 Mar 2010 18:13:09 +0100

We present 19 year-old boy who has been suffering from paroxysmal nocturnal attacks of painful dystonic postures involving one hand, neck and eyes, for several years. The consciousness is always preserved, standard day-time EEG examinations are normal. Initial therapeutical response to carbamazepine was effective. During the clinical course, and disease aggravation, ictal sleep EEG suggested epileptic frontal lobe discharges. Although PND and ADNFLE are very similar diseases, their electrophysiological differences suggest the most important role of EEG in establishing the final, correct diagnosis of some neurological diseases. (Source: Clinical Neurophysiology)

In ovo nanoinjection of triclosan, diclofenac and carbamazepine affects embryonic development of medaka fish (Oryzias latipes).

Chemosphere — Fri, 05 Mar 2010 00:00:00 +0100

We examined the toxicity of three pharmaceuticals and personal care products (PPCPs) - triclosan (TCS), diclofenac (DCF), and carbamazepine (CBMZ) - on embryonic development of Japanese medaka (Oryzias latipes) using in ovo nanoinjection. Medaka eggs (8h post-fertilization; late blastula stage) were injected with 0.5nL of triolein (vehicle control) or 0.5nL of PPCPs, using different doses of TCS (1, 5, or 9ng), DCF (1, 5, or 12ng), or CBMZ (1, 5, or 12ng) per egg in triolein, in addition to uninjected control. Following injection, we recorded survival, embryonic lesions, delay in embryonic development (eye, embryonic body and internal organs), heart beat rate, hatchability, and hatching time of embryos and upward swimming of larvae. As a result, injected PPCPs caused toxic responses to med...

Synthesis and Anticonvulsant Activity of Some 7-Alkoxy-2H-1,4-benzothiazin-3(4H)-ones and 7-Alkoxy-4H-[1,2,4]triazolo[4,3-d]benzo[b][1,4]thiazines.

Chemical and Pharmaceutical Bulletin — Wed, 03 Mar 2010 05:56:03 +0100

Authors: Zhang LQ, Guan LP, Wei CX, Deng XQ, Quan ZS A series of 7-alkoxy-2H-1,4-benzothiazin-3(4H)-ones and a new series of 7-alkoxy-4H-[1,2,4]triazolo[4,3-d]benzo[b][1,4]thiazine derivatives were synthesized using 5-methoxybenzo[d]thiazol-2-amine as starting material. The structures of the compounds were elucidated by IR, (1)H-NMR spectroscopic data and microanalyses. The anticonvulsant activity of these compounds was evaluated by maximal electroshock (MES) test and rotarod test following intraperitoneal injection in KunMing mice. Among the synthesized compounds 3a-v, 7-(hexyloxy)-2H-benzo[b][1,4]thiazin-3(4H)-one (3f) could be considered potentially the most useful and safe therapeutic compound. Among the synthesized compounds 4a-u, compound 7-(2-fluorobenzyloxy)-4H-[1,2,4]triazolo[...

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Does the Long Plasma Half-Life of 4{beta}-Hydroxycholesterol Impact Its Utility as a Cytochrome P450 3A (CYP3A) Metric?

The Journal of Clinical Pharmacology — Tue, 02 Mar 2010 00:00:00 +0100

Authors: Yang Z, Rodrigues AD Plasma 4beta-hydroxycholesterol (4betaHC) has been proposed as an endogenous marker of cytochrome P450 3A (CYP3A). To assess its utility as a CYP3A metric, a pharmacokinetic model, assuming no alteration in cholesterol plasma concentrations, was developed to simulate the effect of CYP3A induction and inhibition on 4betaHC plasma levels under different treatment durations. By incorporating the long plasma half-life of 4betaHC (~17 days) into the model, the inductive effect of 2 known inducers (carbamazepine and rifampicin) reported in the literature was adequately described. Furthermore, the simulations showed that it was possible to resolve none, weak, moderate, and potent inducers within 2 weeks of dosing. On the other hand, simulations indicated that at ...

Injection of botulinum toxin type A (BOTOX) into trigger zone of trigeminal neuralgia as a means to control pain

Oral Surgery, Oral Medicine, Oral Pathology, Oral Radiology, and Endodontics — Mon, 01 Mar 2010 00:00:00 +0100

This article illustrates a case of persistent trigeminal neuralgia in a medically compromised 65-year-old female who did not respond to pharmacotherapy. She had undergone several peripheral neurectomies as well as a failed right posterior fossa exploration that resulted in a cerebrospinal fluid leak. Persistent pain over the right external nasal area and right mental region was relieved for several hours after daily injections of bupivacaine. A trial of a single dose of 100 units of botulinum toxin type A (BOTOX) diluted in 2.5 mL saline was injected into the external nasal trigger zone (60 units) and to the mental nerve region (40 units). She achieved complete pain relief in the external nasal region for 5 months. Pain recurred and the site was again injected with 100 units of botulinum t...

The Role of Topiramate and other Anticonvulsants in the Treatment of Alcohol Dependence: a Clinical Review.

CNS and Neurological Disorders Drug Targets — Mon, 01 Mar 2010 00:00:00 +0100

Authors: De Sousa A Alcohol dependence is a major health problem worldwide. Various pharmacological agents have been used in the management of alcohol dependence. This review looks at the role of topiramate and other anticonvulsants in the management of alcohol dependence. Topiramate is the most widely used anticonvulsant in the treatment of alcohol dependence. The literature on topiramate is reviewed and critically analyzed, along with its proposed mechanism of action in alcohol dependence. A review of data available on other anticonvulsants like carbamazepine, oxcarbazepine, sodium valproate, gabapentin and levetiracetam are presented and their potential in the treatment of alcohol dependence is considered, together with future research directions. PMID: 20201814 [PubMed - in pro...

Interaction of azoles with rifampin, phenytoin, and carbamazepine: in vitro and clinical observations

The Aspergillus Website - articles — Fri, 26 Feb 2010 00:00:00 +0100

Tucker RM, Denning DW, Hanson LH, Rinaldi MG, Graybill JR, Sharkey PK, Pappagianis D, Stevens DA (Source: The Aspergillus Website - articles)

Trigeminal trophic syndrome treated with thermoplastic occlusion

Australasian Journal of Dermatology — Mon, 22 Feb 2010 00:00:00 +0100

A 72-year-old man with a history of thrombotic CVA causing lateral medullary infarction presented with non-healing ulcers of the right side of the face of 5 months' duration. After extensive investigations, a diagnosis of trigeminal trophic syndrome was made. The ulcers progressed relentlessly despite amitriptyline and gabapentin, and he was treated with a combination of carbamazepine and thermoplastic mask occlusion of the right side of his face. Over the next 10 weeks the shallower facial ulcers began to diminish in depth and diameter, and the deeper ulcers stopped progressing. Although the patient showed early signs of healing, he died because of complications from the CVA. (Source: Australasian Journal of Dermatology)

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New Medicines Profile: Eslicarbazepine

NeLM - Drug Specific Reviews — Mon, 22 Feb 2010 00:00:00 +0100

Source: North West Medicines Information Centre Area: Evidence > Drug Specific Reviews Eslicarbazepine acetate is a new antiepileptic drug (AED) which is licensed as add-on therapy in adults with partial-onset seizures with or without secondary generalisation. In three 12-week clinical trials eslicarbazepine has been shown to be more effective than placebo at a dose of 800mg or 1,200mg once daily as add-on treatment in patients receiving one or more AEDs in the management of simple and complex partial seizures with or without secondary generalisation. There are no active-comparator trials. Data from open-label extension studies of one year duration suggest that the efficacy of eslicarbazepine is maintained. Eslicarbazepine has similar adverse effects to oxcarbazepine. The most com...

Antiepileptics for aggression and associated impulsivity.

Cochrane Database of Systematic Reviews — Sat, 20 Feb 2010 04:58:05 +0100

CONCLUSIONS: The authors consider that the body of evidence summarised in this review is insufficient to allow any firm conclusion to be drawn about the use of antiepileptic medication in the treatment of aggression and associated impulsivity. Four antiepileptics (valproate/divalproex, carbamazepine, oxcarbazepine and phenytoin) were effective, compared to placebo, in reducing aggression in at least one study, although for three drugs (valproate, carbamazepine and phenytoin) at least one other study showed no statistically significant difference between treatment and control conditions. Side effects were more commonly noted for the intervention group although adverse effects were not well reported. Absence of information does not necessarily mean that the treatment is safe, nor that the po...

A Prospective Open-Label Trial of Extended-Release Carbamazepine Monotherapy in Children with Bipolar Disorder

Journal of Child and Adolescent Psychopharmacology — Thu, 18 Feb 2010 13:07:32 +0100

Journal of Child and Adolescent Psychopharmacology Feb 2010, Vol. 20, No. 1: 7-14. (Source: Journal of Child and Adolescent Psychopharmacology)

FSRH statement on antiepileptic drugs and contraception

NeLM - News — Thu, 18 Feb 2010 00:00:00 +0100

Source: Faculty of Sexual and Reproductive Healthcare Area: News The Clinical Effectiveness Unit (CEU) of the Faculty of Sexual & Reproductive Healthcare (FSRH) has issued a statement on the concomitant use of antiepileptic drugs (AEDs) and contraception. The statement summarises the following points in relation to new information (direct from source): . There is evidence that progestogen-only methods do not affect lamotrigine levels. . Lamotrigine levels are not reduced by combined hormonal contraception (CHC) when lamotrigine is given in conjunction with sodium valproate. . CHC may increase the clearance of sodium valproate. The clinical significance of this interaction is unknown. . Long-term treatment with carbamazepine, phenytoin, primidone and sodi...

Cross-species comparison of fluoxetine metabolism with fish liver microsomes.

Chemosphere — Thu, 18 Feb 2010 00:00:00 +0100

In this study, in vitro hepaticfluoxetine metabolism was determined in several model fish species: rainbow trout, goldfish, zebrafish and killifish. Incubation of fluoxetine with hepatic microsomes from trout pre-treated with carbamazepine showed a time-dependant loss of fluoxetine, concomitant with an increase in norfluoxetine, the major mammalian demethylated metabolite. However, fluoxetine was not well metabolized in reactions with hepatic microsomes from untreated fish. Fluoxetine loss was greater than norfluoxetine production, indicating that norfluoxetine is not the predominant fluoxetine biotransformation product in fish. Furthermore, norfluoxetine was often undetected, possibly indicating that fluoxetine demethylation is a minor metabolic pathway in fish. Inter-species differences ...

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Carbamazepine/lamotrigine: DRESS syndrome: case report

Reactions — Mon, 15 Feb 2010 14:06:03 +0100

(Source: Reactions)

Best Practice Guide for the Treatment of REM Sleep Behavior Disorder (RBD)

Journal of Clinical Sleep Medicine : JCSM — Sat, 13 Feb 2010 16:23:47 +0100

Summary of Recommendations: Modifying the sleep environment is recommended for the treatment of patients with RBD who have sleep-related injury. Level A Clonazepam is suggested for the treatment of RBD but should be used with caution in patients with dementia, gait disorders, or concomitant OSA. Its use should be monitored carefully over time as RBD appears to be a precursor to neurodegenerative disorders with dementia in some patients. Level B Clonazepam is suggested to decrease the occurrence of sleep-related injury caused by RBD in patients for whom pharmacologic therapy is deemed necessary. It should be used in caution in patients with dementia, gait disorders, or concomitant OSA, and its use should be monitored carefully over time. Level B Melatonin is suggested for the treatment o...

Effect of magnesium oxide on the activity of standard anti-epileptic drugs against experimental seizures in rats

Indian Journal of Pharmacology — Fri, 12 Feb 2010 14:06:53 +0100

Conclusion</b> : The dose of oral MgO appears to have an inverse relation with the protective effect in MES-induced seizure model. High doses of MgO supplementation given orally appear to enhance the activity of standard anti-epileptic drugs in the MES-induced seizure model. (Source: Indian Journal of Pharmacology)

Human health risk assessment of pharmaceuticals in water: An uncertainty analysis for meprobamate, carbamazepine, and phenytoin.

Regulatory Toxicology and Pharmacology : RTP — Tue, 09 Feb 2010 00:00:00 +0100

This study presents a step-wise development of a quantitative pharmaceutical risk assessment (QPhRA, hereafter) framework, including Monte Carlo uncertainty analysis for meprobamate, carbamazepine, and phenytoin during (1) accidental exposures of stream water and fish consumption and (2) direct ingestion of finished drinking water for children and adults. Average hazard quotients of these pharmaceuticals (i.e., the ratio of values of chronic daily intake to acceptable daily intake) were found to lie between 1x10(-10) and 3x10(-5) and 99(th) percentile values of hazard quotients were found to be less than 1x10(-4) for both subpopulations, indicating no potential risks of adverse effects due to pharmaceuticals exposures. In addition, pharmaceutical concentrations were also observed to be low...

Antiepileptic drugs and quality of life in the elderly: Results from a randomized double-blind trial of carbamazepine and lamotrigine in patients with onset of epilepsy in old age.

Epilepsy and Behaviour — Mon, 08 Feb 2010 00:00:00 +0100

Authors: Saetre E, Abdelnoor M, Perucca E, Taubøll E, Isojärvi J, Gjerstad L During an international double-blind trial evaluating the efficacy and tolerability of lamotrigine and carbamazepine in patients aged 65 with newly diagnosed epilepsy, the comparative effects of the drugs on health-related quality of life were investigated based on screening and 12-, 28-, and 40-week data, using the modified Side Effect and Life Satisfaction (SEALS) Inventory and the Liverpool Adverse Event Profile. Of 167 patients, 29 discontinued before first follow-up, and data were incomplete for 13. In 125 eligible subjects (62 taking carbamazepine, 63 taking lamotrigine), comparable baseline data did not change significantly during medication, within or across treatments. A borderline differenc...

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Detecting retinal vigabatrin toxicity in patients with partial symptomatic or cryptogenic epilepsy.

European Journal of Ophthalmology — Mon, 08 Feb 2010 00:00:00 +0100

Conclusions. RNFLT measurement with OCT can efficiently identify vigabatrin toxicity in patients with partial symptomatic and cryptogenic epilepsy. Perimetry, contrast sensitivity, and color discrimination assessment might be inconclusive in these particular subgroups of epileptic patients. PMID: 20155709 [PubMed - as supplied by publisher] (Source: European Journal of Ophthalmology)

Potential physiological effects of pharmaceutical compounds in Atlantic salmon (Salmo salar) implied by transcriptomic analysis.

Environmental Science and Pollution Research International — Sat, 06 Feb 2010 00:00:00 +0100

CONCLUSIONS: The continuously growing number of annotations of representative species relevant for environmental quality testing is facilitating pathway analysis processes for not completely annotated organisms. KEGG has shown to be a useful tool for the analysis of induced pathways from data generated by microarray techniques with the selected pharmaceutical contaminants acetaminophen, carbamazepine, and atenolol, but further studies have to be carried out in order to determine if a similar expression pattern in terms of fold change quantity and pathways is observed after long-term exposure. Together with the information obtained in this study, it will then be possible to evaluate the potential risk that the continuous release of these compounds may have on the environment and ecosystem f...

Carbamazepine but not pregabalin impairs eye control: A study on acute objective CNS side effects in healthy volunteers

Epilepsy Research — Mon, 01 Feb 2010 00:00:00 +0100

Discussion: CBZ causes more commonly dizziness after intake than PGB, when given in single doses, which is reflected in objective measurements; CBZ but not PGB impaired saccadic eye movements. Electrooculography and posturography serve as an objective measure of AED CNS side effects and could be used at an early stage of drug development. (Source: Epilepsy Research)

Management of a severe carbamazepine overdose with continuous venovenous hemodiafiltration

The American Journal of Emergency Medicine — Mon, 01 Feb 2010 00:00:00 +0100

Carbamazepine (CBZ) is a commonly used antiepileptic agent. Common toxic effects include neurological abnormalities; ataxia, seizures, coma, cardiorespiratory problems; dysrhythmias; conduction disorders; respiratory depression; and eye abnormalities, such as nystagmus and ophthalmoplegia. Carbamazepine is highly protein bound. There is no antidote for the medication. Carbamazepine is not removed effectively through conventional hemodialysis. Supportive measures and charcoal hemoperfusion have been regarded as efficient treatment methods. We herein report a 17-year-old girl to whom continuous venovenous hemodiafiltration lacking the albumin-enhance after suicidal overdose of CBZ was performed. We suggest continuous venovenous hemodiafiltration lacking the albumin-enhance as an alternative ...

A review of the effect of anticonvulsant medications on bone mineral density and fracture risk.

The American Journal of Geriatric Pharmacotherapy — Mon, 01 Feb 2010 00:00:00 +0100

Conclusions: Observational studies suggest an association between use of anticonvulsant medications, reduced bone mineral density, and increased fracture risk. Randomized clinical trials are needed to guide the management of bone disease among those who use anticonvulsants. PMID: 20226391 [PubMed - as supplied by publisher] (Source: The American Journal of Geriatric Pharmacotherapy)

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[Which factors have an impact on levetiracetam serum concentrations? : An analysis in 163 patients with epilepsy.]

Der Nervenarzt — Sat, 30 Jan 2010 00:00:00 +0100

Authors: Bauer J, Pfeiffer C, Burr W We evaluated factors possibly influencing serum concentrations of levetiracetam (LEV-SC). The study included 163 patients with epilepsy (91 men, 72 women; mean age 39.6 years). The duration of treatment on first analysis was 226 days; the mean daily dose amounted to 2,434 mg. In each patient between one and seven measurements were carried out (mean 2.2). LEV-SC significantly depended on daily dosage and the interval between the time the medication was taken and the time of blood extraction. A marked drop in LEV-SC was observed 4-5 h following ingestion. Carbamazepine, oxcarbazepine and clobazam reduced LEV-SC, whereas valproate elevated LEV-SC significantly. When assessing evaluation of compliance these factors have to be taken into consideration wh...

Single and combined toxicity of pharmaceuticals at environmentally relevant concentrations in Daphnia magna - A multigenerational study.

Chemosphere — Thu, 28 Jan 2010 00:00:00 +0100

Authors: Dietrich S, Ploessl F, Bracher F, Laforsch C Pharmaceuticals are continuously discharged into the environment, resulting in the chronic exposure of aquatic organisms to these compounds. In this multigenerational study, we examined the influence of four pharmaceuticals (carbamazepine (CBZ), diclofenac (DIC), 17alpha-ethinylestradiol (EE2) and metoprolol (MET)) as single substances and as a drug mixture at environmentally relevant concentrations on life-history and morphological parameters over six generations of the cladoceran Daphnia magna. Detectable effects of the used pharmaceuticals occured in the first observed generation, followed by an acclimation period and a recurrence of drug effects in later generations: daphnids exposed to MET were affected by the pharmaceutical, r...

Immediate-release versus controlled-release carbamazepine in the treatment of epilepsy

Neurological Conditions Specialist Library — Wed, 27 Jan 2010 16:26:34 +0100

Cochrane systematic review. Authors' conclusions: At present, data from trials do not confirm or refute an advantage for CR CBZ over IR CBZ for seizure frequency or adverse events in patients with newly diagnosed epilepsy. For trials involving epilepsy patients already prescribed IR CBZ, no conclusions can be drawn concerning superiority of CR CBZ with respect to seizure frequency. There is a trend for CR CBZ to be associated with fewer adverse events when compared to IR CBZ. A change to CR CBZ may therefore be a worthwhile strategy in patients with acceptable seizure control on IR CBZ but experiencing unacceptable adverse events. The included trials were of small size, poor methodological quality and possessed a high risk of bias, limiting the validity of this conclusion. Randomised ...

Carbamazepine/opioid analgesics: Interaction leading to fatal carbamazepine poisoning, and fatal hydromorphone overdose, due to medication errors: 2 case reports

Reactions — Wed, 27 Jan 2010 14:05:47 +0100

(Source: Reactions)

Carbamazepine: DRESS syndrome: case report

Reactions — Wed, 27 Jan 2010 14:05:47 +0100

(Source: Reactions)

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Immediate-release versus controlled-release carbamazepine in the treatment of epilepsy

NeLM - Drug Specific Reviews — Tue, 26 Jan 2010 00:00:00 +0100

Source: Cochrane Library Area: Evidence > Drug Specific Reviews Background Epilepsy is defined as the tendency to spontaneous, excessive neuronal discharge, manifesting as seizures. It is a common disorder with an incidence of 50 per 100,000 per year and a prevalence of 0.5% to 1% (Hauser 1993) in the developed world. Carbamazepine is a commonly used antiepileptic drug that is associated with a number of troublesome adverse events including dizziness, double vision and unsteadiness. These often occur during peaks in plasma concentration. The occurrence of such adverse events may limit the daily dose that can be tolerated and reduce the chances of seizure control for patients requiring higher doses (Vojvodic 2002). A controlled-release formulation of carbamazepine delivers the same do...

Uptake of human pharmaceuticals by plants grown under hydroponic conditions.

Chemosphere — Thu, 21 Jan 2010 00:00:00 +0100

Authors: Herklotz PA, Gurung P, Vanden Heuvel B, Kinney CA Cabbage (Brassica rapa var. pekinensis) and Wisconsin Fast Plants (Brassica rapa) were chosen for a proof of concept study to determine the potential uptake and accumulation of human pharmaceuticals by plants. These plants were grown hydroponically under high-pressure sodium lamps in one of two groups including a control and test group exposed to pharmaceuticals. The control plants were irrigated with a recirculating Hoagland's nutrient solution while the test plants were irrigated with a Hoagland's nutrient solution fortified with the pharmaceuticals carbamazepine, salbutamol, sulfamethoxazole, and trimethoprim at 232.5mugL(-1). When plants reached maturity, nine entire plants of each species were separated into components suc...

Epicrania Fugax: Ten New Cases and Therapeutic Results

Headache: The Journal of Head and Face Pain — Wed, 20 Jan 2010 00:00:00 +0100

Conclusions.[mdash] This description reinforces the proposal of EF as a new headache variant or a new headache syndrome. Anesthetic blockades, carbamazepine, gabapentin, and lamotrigine have been apparently effective in individual patients. Further observations and therapeutic trials are needed. (Source: Headache: The Journal of Head and Face Pain)

Epicrania Fugax: Ten New Cases and Therapeutic Results.

Headache — Wed, 20 Jan 2010 00:00:00 +0100

Conclusions.- This description reinforces the proposal of EF as a new headache variant or a new headache syndrome. Anesthetic blockades, carbamazepine, gabapentin, and lamotrigine have been apparently effective in individual patients. Further observations and therapeutic trials are needed. PMID: 20100299 [PubMed - as supplied by publisher] (Source: Headache)

CARBAMAZEPINE ( Carbamazepine ) Tablet CARBAMAZEPINE ( Carbamazepine ) Tablet, Chewable [Torrent Pharmaceuticals Limited]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Tue, 19 Jan 2010 05:00:00 +0100

Updated Date: Jan 19, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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Micropollutant removal during biological wastewater treatment and a subsequent ozonation step.

Environmental Pollution — Mon, 18 Jan 2010 00:00:00 +0100

Authors: Schaar H, Clara M, Gans O, Kreuzinger N The design criteria for wastewater treatment plants (WWTP) and the sludge retention time, respectively, have a significant impact on micropollutant removal. The upgrade of an Austrian municipal WWTP to nitrogen removal (best available technology, BAT) resulted in increased elimination of most of the analyzed micropollutants. Substances, such as bisphenol-A, 17alpha-ethinylestradiol and the antibiotics erythromycin and roxithromycin were only removed after the upgrade of the WWTP. Nevertheless, the BAT was not sufficient to completely eliminate these compounds. Thus, a pilot scale ozonation plant was installed for additional treatment of the effluent. The application of 0.6 g O(3) g DOC(-1) increased the removal of most of the micropollut...

Exploring differential prescribing between anti-epileptic drugs in epilepsy patients with a history of mood disorders

Pharmacoepidemiology and Drug Safety — Fri, 15 Jan 2010 00:00:00 +0100

To explore differential prescribing of anti-epileptic drugs (AEDs) to patients with epilepsy by history of mood disorder.Epilepsy was defined as at least one diagnosis code and one AED prescription, and all patients must have been on the database 182 days before and after their first AED prescription. The Integrated HealthCare Information Services (IHCIS) insurance claims database included 44 557 patients with epilepsy between January 1997 and March 2007. The General Practice Research Database (GPRD) included 16 904 patients with epilepsy up to March 2007. Patients were categorized by their first use of specified AEDs. Mood disorders were defined as diagnosis codes for depression and bipolar disorder, or anti-depressant use. The unadjusted odds ratios and 95% confidence intervals for a his...

Pattern of P450 expression at the human blood–brain barrier: Roles of epileptic condition and laminar flow

Epilepsia — Fri, 15 Jan 2010 00:00:00 +0100

Discussion: These results support the hypothesis of local drug metabolism at the diseased BBB. The direct association between BBB CYP enzymes and the drug-resistant phenotype needs to be further investigated. (Source: Epilepsia)

Evaluation of transport of common antiepileptic drugs by human multidrug resistance-associated proteins (MRP1, 2 and 5) that are overexpressed in pharmacoresistant epilepsy.

Neuropharmacology — Thu, 14 Jan 2010 00:00:00 +0100

Authors: Luna-Tortós C, Fedrowitz M, Löscher W Resistance to antiepileptic drugs (AEDs) is one of the most serious problems in the treatment of epilepsy. Accumulating experimental evidence suggests that increased expression of the drug efflux transporter P-glycoprotein (Pgp) at the blood-brain barrier may be involved in the mechanisms leading to AED resistance. In addition to Pgp, increased expression of several multidrug resistance-associated proteins (MRPs) has been determined in epileptogenic brain regions of patients with pharmacoresistant epilepsy. However, it is not known whether AEDs are substrates for MRPs. In the present experiments, we evaluated whether common AEDs are transported by human MRPs (MRP1, 2 and 5) that are overexpressed in AED resistant epilepsy. For th...

A case of rheumatoid arthritis presenting with postherpetic neuralgia and abdominal-wall pseudohernia

Rheumatology International — Mon, 11 Jan 2010 18:19:50 +0100

We report a patient >45 years of age with a history of rheumatoid arthritis (RA) who presented with two chronic HZ complications. A 75-year-old woman was admitted with neuralgia following cutaneous herpes zoster 6 weeks before. She was on long-term glucocorticoid, antimalarial and non-steroidal anti-inflammatory treatment. Confluent ulcers began to fill with granulation tissue, crusts, scars and skin discoloration in the area of the left T12-L2 dermatomes and reducible, painless swelling of the left flank, 20 × 20 cm, without palpable defect in abdominal-wall. There were typical joint deformity and positive rheumatoid factor. On neurological examination superficial abdominal reflexes were diminished in the left side, with hypesthesia of the overlying skin...

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Fatal carbamazepine induced fulminant eosinophilic (hypersensitivity) myocarditis: Emphasis on anatomical and histological characteristics, mechanisms and genetics of drug hypersensitivity and differential diagnosis

Journal of Forensic and Legal Medicine — Mon, 11 Jan 2010 16:43:37 +0100

We report a case of hypersensitivity myocarditis secondary to administration of carbamazepine. Acute hypersensitivity myocarditis was not suspected clinically, and the diagnosis was made post-mortem. Histology revealed diffuse infiltration of the myocardium by eosinophils and lymphocytes with myocyte damage. Clinically, death was due to cardiogenic shock. To best of our knowledge this is the second case of fatal carbamazepine induced myocarditis reported in English literature. (Source: Journal of Forensic and Legal Medicine)

Carbamazepine: DRESS syndrome: case report

Reactions — Mon, 11 Jan 2010 14:23:59 +0100

(Source: Reactions)

Relationship between Antiepileptic Drugs and Biological Markers Affecting Long-Term Cardiovascular Function in Children and Adolescents.

The Canadian Journal of Clinical Pharmacology — Fri, 08 Jan 2010 01:48:02 +0100

ConclusionsPersistent elevation in these biochemical markers has shown to be associated with the development of long-term sequelae such as cardiovascular diseases, prompting concerns about the long-term implications of chronic AED use in children and cardiovascular risk. Further research is needed to assess the relationship between specific chronic AED use, homocysteine and lipoprotein concentrations, the influence of genotype, as well as the risk of long-term sequelae in the paediatric population. PMID: 20051609 [PubMed - in process] (Source: The Canadian Journal of Clinical Pharmacology)

Eslicarbazepine Acetate: A Well-Kept Secret?

Epilepsy Currents — Fri, 08 Jan 2010 00:00:00 +0100

DISCUSSION: ESL, 800 and 1,200 mg once-daily, was well tolerated and more effective than placebo in patients who were refractory to treatment with one or two concomitant AEDs. (Source: Epilepsy Currents)

Transient improvement after brief antiepileptic drug withdrawal in the epilepsy monitoring unit—possible relationship to AED tolerance

Epilepsia — Thu, 07 Jan 2010 00:00:00 +0100

Discussion: SIP does occur after brief AED withdrawal. This effect is greater in patients on monotherapy and tends to be larger in patients with a history of AED tolerance. The SIP effect may be related to the phenomenon of tolerance, clinically seen as resistance to AED therapeutic effect. (Source: Epilepsia)

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Effect of sildenafil on the anticonvulsant action of classical and second-generation antiepileptic drugs in maximal electroshock-induced seizures in mice

Epilepsia — Thu, 07 Jan 2010 00:00:00 +0100

Conclusions: Sildenafil significantly raised the threshold for electroconvulsions in mice without any impairment of motor performance and long-term memory, but it enhanced muscle strength. Treatment of patients on CBZ or VPA with sildenafil may not be recommended due to pharmacokinetic interactions. Coadministration of sildenafil with other AEDs, especially with TPM, seems to be a reasonable choice. (Source: Epilepsia)

CARBATROL (Carbamazepine) Capsule, Extended Release [Shire US Manufacturing Inc.]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Wed, 06 Jan 2010 05:00:00 +0100

Updated Date: Jan 6, 2010 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Evaluation and performance of desorption electrospray ionization using a triple quadrupole mass spectrometer for quantitation of pharmaceuticals in plasma.

Rapid Communications in Mass Spectrometry : RCM — Mon, 04 Jan 2010 00:00:00 +0100

Authors: Kennedy JH, Wiseman JM The present work describes the methodology and investigates the performance of desorption electrospray ionization (DESI) combined with a triple quadrupole mass spectrometer for the quantitation of small drug molecules in human plasma. Amoxepine, atenolol, carbamazepine, clozapine, prazosin, propranolol and verapamil were selected as target analytes while terfenadine was selected as the internal standard common to each of the analytes. Protein precipitation of human plasma using acetonitrile was utilized for all samples. Limits of detection were determined for all analytes in plasma and shown to be in the range 0.2-40 ng/mL. Quantitative analysis of amoxepine, prazosin and verapamil was performed over the range 20-7400 ng/mL and shown to be linear in all ...

Mean daily plasma concentrations of beta-endorphin, leu-enkephalin, ACTH, cortisol, and DHEAS in epileptic patients with complex partial seizures evolving to generalized tonic-clonic seizures.

Endokrynologia Polska — Fri, 01 Jan 2010 00:00:00 +0100

Conclusions: 1. Pituitary-adrenal axis hyperactivity is observed in patients with clinically active epilepsy, independently of the frequency of seizures and duration of the disease. 2. Changes in endogenous opioid system activity are related to the clinical activity of epilepsy - beta-endorphin concentrations are connected with frequency of seizures and duration of the disease and leu-enkephalin concentrations with duration of the disease. 3. Endogenous opioid peptides might take part in the neurochemical mechanism of human epilepsy. (Pol J Endocrinol 2010; 61 (1): 103-110). PMID: 20205112 [PubMed - in process] (Source: Endokrynologia Polska)

Antiepileptic drug utilisation and seizure outcome among paediatric patients in a Malaysian public hospital.

Singapore Medical Journal — Fri, 01 Jan 2010 00:00:00 +0100

Conclusion: Monotherapy was the most frequently used remedy in all forms of epilepsy. Overall, sodium valproate was the most commonly used drug, while carbamazepine was found to be more frequently used as monotherapy. There was a significant difference found between the older and newer antiepileptic drugs, with 87.5 percent of seizure-free patients on older antiepileptic drugs. PMID: 20200771 [PubMed - in process] (Source: Singapore Medical Journal)

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Amelioration of Oxaliplatin Neurotoxicity by Drugs in Humans and Experimental Animals: A MiniReview of Recent Literature

Basic and Clinical Pharmacology and Toxicology — Wed, 30 Dec 2009 00:00:00 +0100

Abstract: The broad spectrum anti-neoplastic drug oxaliplatin is a third-generation platinum compound that inhibits DNA synthesis, mainly by causing intrastrandal cross-links in DNA. The drug is particularly useful alone and in combination with flurouracil and leucovorin in colorectal cancer, but it is also used for other cancers such as those of the ovary, lung, breast and liver, as well as non-Hodgkin's lymphoma. The drug is known to cause neurological, gastrointestinal and haematological toxicities. Neurotoxicity occurs in most of the treated patients and is considered to be a serious limitation for the use of the drug. The mechanism of the neurotoxicity is not known with certainty but may involve prolongation of sodium channels opening. Strategies to ameliorate oxaliplatin neurotoxicit...

Acute Pharmaceutical Toxicity killed Brittany Murphy - Could it be killing millions more?

NaturalNews.com — Mon, 28 Dec 2009 07:00:00 +0100

(NaturalNews) The entire pharmaceutical industry is based on the idea that for whatever's wrong with you, there's a patented chemical pill that can make it better. Feeling some anxiety? There's a pill for that. Have high blood pressure? There's a pill for that, too. Suffering from sleepless nights? There's yet another pill for that, too.Importantly, modern medicine and the pharmaceutical industry both believe there is no limit to how many prescription medications you can simultaneously take. If you have ten health problems, they've got ten different pills for you. And when those pills cause twenty different dangerous side effects, they're ready for twenty more prescriptions for you to dutifully swallow.This idea that health is achieved by taking prescription chemicals is ludicrous from the...

Pregnancy with epilepsy: Obstetric and neonatal outcome of a controlled study

Seizure: European Journal of Epilepsy — Fri, 25 Dec 2009 00:00:00 +0100

Conclusion: MCM were more prevalent in the babies of WWTE particularly amongst those receiving sodium valproate. (Source: Seizure: European Journal of Epilepsy)

Valproate in Pregnancy Problematic, Carbamazepine Another Concern

Medscape Today Headlines — Fri, 18 Dec 2009 15:07:59 +0100

New data confirm the dose-related effect of fetal valproate exposure on cognitive development. The work also points to carbamazepine affecting verbal abilities. Medscape Medical News (Source: Medscape Today Headlines)

Hypertrophic scars from surgical staples mimicking folliculitis

Journal of the American Academy of Dermatology — Thu, 17 Dec 2009 14:02:46 +0100

We report an unusual presentation of multiple hypertrophic scars resulting from surgical staples. A 23-year-old Vietnamese man developed toxic epidermal necrolysis to carbamazepine and was treated with porcine skin allograft sheets, which were secured with surgical staples, and continued supportive care in our burn unit with complete recovery. Four to 5 weeks after discharge, he developed widespread pruritic red papules. He denied fevers or other systemic complaints. His medical history included anxiety, which was treated with alprazolam, and allergic rhinitis, which was controlled with cetirizine. A physical examination revealed dozens of paired 4-mm dome-shaped, firm, red papules on all four extremities and the lateral trunk, sparing the back. On the arms and trunk, the pairs were reprod...

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Acquired erythroderma in adults: a clinical and prognostic study

Journal of the European Academy of Dermatology and Venereology — Thu, 17 Dec 2009 00:00:00 +0100

Conclusions Our study illustrates the severity of erythroderma. It alters heavily the quality of life of patients which is initially altered by the pre-existent dermatosis. It may be life threatening as mortality rate is high. (Source: Journal of the European Academy of Dermatology and Venereology)

Bone and calcium metabolism and antiepileptic drugs

Clinical Neurology and Neurosurgery — Wed, 16 Dec 2009 16:10:19 +0100

Abstract: There is increasing evidence suggesting that epilepsy and its treatment can affect bone mineralization and calcium metabolism. Many studies have shown a significant reduction in bone mineral density in patients treated with classic (phenobarbital, carbamazepine, valproate, etc.) and with new (oxcarbazepine, gabapentin) antiepileptic drugs. In spite of data about the possible effects of the antiepileptic drugs on calcium metabolism, the mechanisms of this important side effect remain to be defined. The abnormalities of calcium metabolism were thought to result from the cytochrome P450 enzyme-inducing properties of some antiepileptic drugs and the resultant reduction in vitamin D levels, but the effect of many medications (e.g., valproate) cannot be readily explained by vitamin D m...

Changing patterns of antiepileptic drug use in pregnant Australian women

Acta Neurologica Scandinavica — Wed, 16 Dec 2009 00:00:00 +0100

Conclusions [ndash] While otherwise following national AED prescribing trends, Australian prescribers are reducing the use and dose of valproate in pregnant women, likely in recognition of the teratogenic hazards of this drug. (Source: Acta Neurologica Scandinavica)

Is Anticonvulsant Treatment of Mania a Class Effect? Data from Randomized Clinical Trials.

CNS Neuroscience and Therapeutics — Tue, 15 Dec 2009 00:00:00 +0100

Authors: Rosa AR, Fountoulakis K, Siamouli M, Gonda X, Vieta E Our aim was to evaluate the efficacy and tolerability of anticonvulsant agents for the treatment of acute bipolar mania and ascertain if their effects on mania are a "class" effect. We conducted a systematic review of randomized controlled trials (RCTs) with placebo or active comparator, in acute bipolar mania in order to summarize available data on anticonvulsant treatment of mania/mixed episodes. We searched (PubMed/MEDLINE) with the combination of the words "acute mania" and "clinical trials" with each one of the following words: "anticonvulsants/antiepileptics,""valproic/valproate/divalproex,""carbamazepine,""oxcarbazepine,""lamotrigine,""gabapentin,""topiramate,""phenytoin,""zonisamide,""retigabine,""pregabalin,""tiaga...

EPITOL (Carbamazepine) Tablet [TEVA Pharmaceuticals USA Inc]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Fri, 11 Dec 2009 05:00:00 +0100

Updated Date: Dec 11, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

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Modulatory effects of neuropsychopharmaca on intracellular pH of hippocampal neurones in vitro

British Journal of Pharmacology — Thu, 10 Dec 2009 00:00:00 +0100

Conclusion and implications: These data substantiate the view that clinically relevant concentrations of neuroleptics and antidepressants can mediate changes in neuronal pHi, which may contribute to their pharmacological mode of action. Effects on pHi should be taken into account when therapeutic or even harmful effects of these drugs are evaluated. (Source: British Journal of Pharmacology)

Tegretol Tablets 100mg, 200mg, 400mg (carbamazepine) - Revised SPC

NeLM - Neurology — Thu, 10 Dec 2009 00:00:00 +0100

Source: eMC (electronic Medicines Compendium) Area: Other Library Updates > SPC Changes Revised SPC included updates to: Section 4.5 (Interaction with other medicinal products and other forms of interaction) - to include buprenorphine, mianserin and sertraline Section 4.8 (Undesirable Effects) - to include vanishing bile duct syndrome (Source: NeLM - Neurology)

CARBAMAZEPINE (CHEWABLE) (Carbmazepine (Chewable)) Tablet, Chewable [American Health Packaging]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Wed, 09 Dec 2009 05:00:00 +0100

Updated Date: Dec 9, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Effect of Carbamazepine and Lamotrigine on Cognitive Function and Oxidative Stress in Brain during Chemical Epileptogenesis in Rats

Basic and Clinical Pharmacology and Toxicology — Mon, 07 Dec 2009 00:00:00 +0100

Abstract: The present study assessed the effect of carbamazepine and lamotrigine on cognitive function and oxidative stress in brain during chemically induced epileptogenesis in rats. Epileptogenesis was induced by administration of pentylenetetrazole (30 mg/kg, s.c.) on alternate days (three times/week) for 9[ndash]11 weeks or until stage 4 of seizure score was achieved. The neurobehavioural parameters used for cognitive assessment were step-down latency in continuous avoidance apparatus and transfer latency in elevated plus maze test paradigm. Carbamazepine and lamotrigine were administered intraperitoneally in doses of 60 mg/kg and 25 mg/kg, respectively, according to the groups, once a day for 11 weeks. Oxidative stress was assessed in isolated homogenized whole brain samples and estim...

Analysis of potential genotoxic impurities in pharmaceuticals by two-dimensional gas chromatography with Deans switching and independent column temperature control using a low-thermal-mass oven module.

Analytical and Bioanalytical Chemistry — Tue, 01 Dec 2009 00:00:00 +0100

Authors: David F, Jacq K, Sandra P, Baker A, Klee MS The analysis of potential genotoxic impurities (PGIs) in active pharmaceutical ingredients (APIs) is a challenging task. The target limit of detection for a PGI in an API is typically 1 ppm (1 microg/g API). This is about 500 times lower than for classical impurity analysis. Consequently, analytical methods for trace analysis, mostly in combination with MS detection, need to be applied for the qualitative and quantitative determination of these impurities. A two-dimensional capillary GC method is presented that can be used for the determination of some target PGIs. A concentrated solution of the API sample is directly introduced in the GC-MS system, using an apolar column for first-dimension separation. The fraction (heart-cut) conta...

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Long-term Effectiveness and Tolerability of Topiramate in Children with Epilepsy under the Age of 2 Years: 4-Year Follow-up.

J Korean Med Sci — Tue, 01 Dec 2009 00:00:00 +0100

Authors: Kim JM, Kwon S, Seo HE, Choe BH, Cho MH, Park SP This is a long-term, open label, observational study aimed to broaden our clinical experiences in managing infants and toddlers with epilepsy. The long-term retention rate and side effects of topiramate (TPM) in them were evaluated and compared with carbamazepine (CBZ). A total of 146 children were involved in the study (TPM=41, CBZ=105). The retention rates at 24 , 36, and 48 months were 46.3%, 34.1%, 26.8% for TPM and 36.2%, 23.8%, 13.3% for CBZ, respectively. At 6 months after starting antiepileptic drugs (AED), the seizure freedom or clinical efficacy (seizure reduction rate more than 50 percent) were 73.2% for TPM and 62.9% for CBZ. The major side effects led to discontinuation included psychomotor slowing, poor oral intake...

Exposure to antiepileptic drugs does not alter the functionality of P-glycoprotein in brain capillary endothelial and kidney cell lines.

European Journal of Pharmacology — Mon, 30 Nov 2009 00:00:00 +0100

Authors: Ambroziak K, Kuteykin-Teplyakov K, Luna-Tórtos C, Al-Falah M, Fedrowitz M, Löscher W Several major antiepileptic drugs, including carbamazepine, phenytoin and phenobarbital, induce xenobiotic metabolizing enzymes via activation of nuclear receptors, including pregnane X receptor (NR1I2) and constitutive androstane receptor (NR1I3). Via activation of these xenobiotic sensors, antiepileptic drugs may also induce the expression of efflux transporters such as P-glycoprotein (Pgp) in different tissues, including intestine, liver, kidney and brain. Increased expression of Pgp in brain capillary endothelial cells, which form the blood-brain barrier, could limit the penetration of antiepileptic drugs into the brain and therefore decrease their therapeutic efficacy. As a cons...

Reversible parkinsonism with oxcarbazepine use

Parkinsonism and Related Disorders — Sat, 28 Nov 2009 14:36:31 +0100

Oxcarbazepine (OXC) is an effective anti-epileptic drug useful in the treatment of both generalized and partial epilepsies, and trigeminal neuralgia. The mechanism of action of OXC primarily involves blockage of sodium currents. It differs from carbamazepine in modulating a different type of calcium channel expressed in the central nervous system. OXC is considered to have a good safety profile. The most frequently observed adverse effects associated with OXC are somnolence or sedation, headache, dizziness, nausea, vomiting, fatigue, abnormal vision, diplopia and hyponatremia. (Source: Parkinsonism and Related Disorders)

Psychoactive drugs in the road traffic in the legal and consultative aspects—Experience gained by the Forensic Medicine Department, Silesian University of Medicine, Katowice

Forensic Science International Supplement Series — Fri, 27 Nov 2009 16:16:37 +0100

Conclusion: The obtained results showed cannabinoids and amphetamine derivatives to be the most frequent whereas opium alkaloids, barbiturates and benzodiazepines rather rare psychoactive drugs found in the tested blood samples of the drivers involved in the road accidents. The authors suggest screening psychoactive drugs not only in drivers involved in road accidents but also those put through the routine road check procedures. While giving opinions on the influence of the above mentioned drugs on the psychophysical efficiency of road traffic users, drugs and compounds which are not subject to legal control but have an effect on the human psychomotor efficiency and thus, enhance the risk of the road accident should be also taken into account. (Source: Forensic Science International Supple...

Reply to discussion by Reinhard Länge et al. on "Degradation of the endocrine disrupting chemicals (EDCs) carbamazepine, clofibric acid, and iopromide by corona discharge over water" [Chemosphere 75(2) (2009) 163-168].

Chemosphere — Wed, 25 Nov 2009 00:00:00 +0100

Reply to discussion by Reinhard Länge et al. on "Degradation of the endocrine disrupting chemicals (EDCs) carbamazepine, clofibric acid, and iopromide by corona discharge over water" [Chemosphere 75(2) (2009) 163-168]. Chemosphere. 2009 Nov 25; Authors: Krause H, Schuhmacher J, Scholl S, Schweiger B, Steinfeld U PMID: 19944447 [PubMed - as supplied by publisher] (Source: Chemosphere)

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Carbamazepine/methylphenobarbital: Congenital disorders following in utero exposure: 2 case reports

Reactions — Sun, 22 Nov 2009 14:04:51 +0100

(Source: Reactions)

Carbamazepine: Toxic epidermal necrolysis in a child: case report

Reactions — Sun, 22 Nov 2009 14:04:51 +0100

(Source: Reactions)

[A prospective, open, controlled and randomised study of clobazam versus carbamazepine in patients with frequent episodes of rolandic epilepsy.]

Revista de Neurologia — Sat, 21 Nov 2009 02:18:30 +0100

CONCLUSIONS. CBZ is an effective drug in rolandic epilepsy, but it may be associated with exacerbation of seizures as well as with cognitive-behavioural impairment. CLB in monotherapy seems to be an effective and better tolerated drug in this kind of epilepsy. PMID: 19921623 [PubMed - as supplied by publisher] (Source: Revista de Neurologia)

Transient lower limb pain following accidental thoracic subarachnoid insertion of an epidural catheter

Journal of Anesthesia — Tue, 17 Nov 2009 23:59:16 +0100

We report a case of transient lower limb pain following the accidental placement of an epidural catheter into the thoracic subarachnoid space. A 31-year-old woman was scheduled to undergo laparoscopic myomectomy. An epidural catheter was accidentally inserted subarachnoid at the T12–L1 intervertebral space with a 2-ml test dose of 2% lidocaine, and was promptly removed. Fulgurant pain and allodynia extending over the L2–5 areas of the left lower limb and buttock started immediately postoperatively. We treated the persistent pain in our patient with epidural infusion of local anesthetics and steroids during her hospital stay, and with carbamazepine and a tricyclic antidepressant after her discharge from the hospital. All signs of allodynia had disappeared on postoperative day 25. ...

Discussion by Reinhard Länge et al. on "Degradation of the endocrine disrupting chemicals (EDCs) carbamazepine, clofibric acid, and iopromide by corona discharge over water" by Krause et al. [Chemosphere 75(2) (2009) 163-168].

Chemosphere — Tue, 17 Nov 2009 00:00:00 +0100

Discussion by Reinhard Länge et al. on "Degradation of the endocrine disrupting chemicals (EDCs) carbamazepine, clofibric acid, and iopromide by corona discharge over water" by Krause et al. [Chemosphere 75(2) (2009) 163-168]. Chemosphere. 2009 Nov 17; Authors: Länge R, Steger-Hartmann T, Borden SA, Pietsch H PMID: 19926112 [PubMed - as supplied by publisher] (Source: Chemosphere)

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Carbamazepine: Exacerbation of idiopathic generalised epilepsy: case report

Reactions — Mon, 16 Nov 2009 14:06:44 +0100

(Source: Reactions)

Carbamazepine: Hyperammonaemia: case report

Reactions — Mon, 16 Nov 2009 14:06:44 +0100

(Source: Reactions)

Inhibition of specific adenylyl cyclase isoforms by lithium and carbamazepine, but not valproate, may be related to their antidepressant effect

Bipolar Disorders — Mon, 16 Nov 2009 00:00:00 +0100

Conclusions: Lithium and carbamazepine preferentially inhibit AC5, albeit via different mechanisms. Lithium competes with Mg2+, which is essential for AC activity; carbamazepine competes for AC's catechol-estrogen site. Antidepressant-like behavior of AC5 knockout mice in the forced-swim test supports the notion that AC5 inhibition is involved in the antidepressant effect of lithium and carbamazepine. The effect of lithium and carbamazepine to lower cAMP formation in AC5-rich dopaminergic brain regions suggests that D1-dopamine receptors in these regions are involved in the antidepressant effect of mood stabilizers. (Source: Bipolar Disorders)

High concentrations of commonly used drugs can inhibit the in vitro glucuronidation of bisphenol A and nonylphenol in rats.

Xenobiotica — Mon, 16 Nov 2009 00:00:00 +0100

This study aimed to identify and characterize the potential metabolic interactions between 14 drugs and these two endocrine disruptors. Nonylphenol and bisphenol A were co-incubated in freshly isolated rat hepatocytes with, drugs at a high concentration. Statistically significant metabolic inhibition of bisphenol A and nonylphenol biotransformation was observed with nine drugs (>50% inhibition by naproxen, salicylic acid, carbamazepine and mefenamic acid). Inhibition assays of UGT activity in rat liver microsomes revealed: 1) competitive inhibition by naproxen (K(i)(app) = 848.3 muM) and carbamazepine (K(i)(app) = 1023.1 muM), 2) no inhibition by salicylic acid suggesting another mechanism of inhibition. Detoxification of nonylphenol and bisphenol A was shown to be impaired by excessive...

[Music as an uninvited guest: the auditive variant of the Charles Bonnet syndrome.]

Tijdschrift voor Psychiatrie — Fri, 13 Nov 2009 05:34:03 +0100

Authors: Tuerlings JH, Wijnen H, Boerman R, Verwey B Visually handicapped patients can be tormented by complex visual hallucinations (Charles Bonnet syndrome). Likewise, deaf patients and patients with impaired hearing can be plagued by auditory hallucinations, mostly involving music. Our article focuses on three female patients who suffered from musical hallucinations. In one of these patients the hallucinations ceased when her hearing was restored. In the second patient the hallucinations ceased when carbamazepine was prescribed. Quetiapine reduced the musical hallucinations in the third patient. The differential diagnoses and therapeutic options are discussed. PMID: 19904711 [PubMed - in process] (Source: Tijdschrift voor Psychiatrie)

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Association of HLA-B*1502 allele and carbamazepine-induced <i>Stevens-Johnson syndrome</i> among Indians

Indian Journal of Dermatology, Venereology and Leprology — Thu, 12 Nov 2009 14:01:24 +0100

Conclusion:</b> This study suggests an association between HLA-B*1502 and carbamazepine-induced SJS in Indian patients. (Source: Indian Journal of Dermatology, Venereology and Leprology)

Occurrence and fate of pharmaceuticals in wastewater treatment plants and rivers in Korea.

Environmental Pollution — Thu, 12 Nov 2009 00:00:00 +0100

Authors: Sim WJ, Lee JW, Oh JE We measured 25 pharmaceuticals in ten municipal wastewater treatment plants (WWTPs), one hospital WWTP and five rivers in Korea. In the municipal WWTP influents, acetaminophen, acetylsalicylic acid and caffeine showed relatively high concentrations. The occurrence of pharmaceuticals in the wastewater seems to be influenced by production and consumption of pharmaceuticals. The hospital WWTP influent showed higher total concentrations of pharmaceuticals than the municipal WWTPs, and caffeine, ciprofloxacin and acetaminophen were dominant. In the rivers, caffeine was dominant, and the distribution of pharmaceuticals was related to the inflow of the wastewater. In the municipal WWTPs, the concentrations of acetaminophen, caffeine, acetylsalicylic acid, ibupro...

Carbamazepine: Drug-induced hypersensitivity syndrome and granulomatous dermatitis: case report

Reactions — Wed, 11 Nov 2009 14:08:04 +0100

(Source: Reactions)

To enhance dissolution rate of poorly water-soluble drugs: Glucosamine hydrochloride as a potential carrier in solid dispersion formulations.

Colloids and Surfaces — Wed, 11 Nov 2009 00:00:00 +0100

Authors: Al-Hamidi H, Edwards AA, Mohammad MA, Nokhodchi A The solid dispersion technique is the most effective method for improving the dissolution rate of poorly water-soluble drugs, however this is reliant on a suitable carrier and solvent being selected. The work presented explores d-glucosamine HCl (G-HCl) as a potential hydrophilic carrier to improve dissolution rate of a poorly water-soluble drug, carbamazepine (CBZ), from physical mixtures and solid dispersion formulations. The effect of different solvents in the preparation of solid dispersion formulations was also investigated. Solid dispersions of the drug and G-HCl were prepared using different ratios by the conventional solvent evaporation method. Different solvents (ethanol, acetone and water) were used as second variable...

Role of Ventral Hippocampal GABA A and NMDA Receptors in the Anxiolytic Effect of Carbamazepine in Rats Using the Elevated Plus Maze Test

Pharmacology — Tue, 10 Nov 2009 23:00:00 +0100

Pharmacology 2009;84:356-366 (DOI:10.1159/000256666) (Source: Pharmacology)

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Antieplipetic treatment eslicarbazepine acetate (Zebinix®) launched in UK

NeLM - News — Tue, 10 Nov 2009 00:00:00 +0100

Source: PharmaTimes Area: News Eisai has launched eslicarbazepine acetate (Zebinix®) in the UK as adjunctive therapy in adults with partial-onset seizures, with or without secondary generalisation. The drug, which is chemically related to carbamazepine and oxcarbazepine, is administered as a once daily regimen. The recommended starting dose is 400mg/d, increased to 800mg/d once daily after one or two weeks, and based on individual response, it may be increased to 1200mg/d. The cost of 30 x 800mg tablets is £154.20. (Source: NeLM - News)

Carbamazepine for serotonin reuptake inhibitor nonresponder case of obsessive compulsive disorder

Indian Journal of Medical Sciences — Sat, 07 Nov 2009 14:26:17 +0100

Aggarwal Ashish, Jain Manish, Garg Amit, Jiloha R CIndian Journal of Medical Sciences 2009 63(10):468-469 (Source: Indian Journal of Medical Sciences)

Positive interference of the analgesic nefopam in the urine immunoassay for benzodiazepines in a secure setting

Journal of Psychopharmacology — Thu, 05 Nov 2009 16:24:40 +0100

An inpatient on a secure unit with a history of bipolar affective disorder and physical complaints including pain was prescribed carbamazepine, quetiapine, dihydrocodeine, nefopam, paracetamol and various aperients. A benzodiazepine urine test by immunoassay was positive. Initial literature searches did not suggest a candidate drug for positive interference. Other explanations were excluded. Positive results continued, despite room searches and other disruptive security measures. Further literature searches revealed one experimental series demonstrating positive interference of nefopam in the relevant assay. Benzodiazepine assays were negative after cessation of nefopam. This is the first such clinical case to our knowledge. (Source: Journal of Psychopharmacology)

A prospective study of cognitive fluency and originality in children exposed in utero to carbamazepine, lamotrigine, or valproate monotherapy.

Epilepsy and Behaviour — Tue, 03 Nov 2009 00:00:00 +0100

CONCLUSION: Children prenatally exposed to valproate demonstrate impaired fluency and originality compared with children exposed to lamotrigine and carbamazepine. PMID: 19892603 [PubMed - as supplied by publisher] (Source: Epilepsy and Behaviour)

Responses of antioxidant status and Na(+)-K(+)-ATPase activity in gill of rainbow trout, Oncorhynchus mykiss, chronically treated with carbamazepine.

Chemosphere — Mon, 02 Nov 2009 00:00:00 +0100

Authors: Li ZH, Zlabek V, Velisek J, Grabic R, Machova J, Randak T In recent years, chemical pollution by the residual pharmaceuticals has been increasingly important issue due to its widely present in the aquatic environment. However, the toxicological effects of residual pharmaceuticals on fish have not been adequately researched. The aim of this work is to investigate the toxic effect of CBZ, an anticonvulsant drug commonly present in aquatic environment, on antioxidant status and Na(+)-K(+)-ATPase in gill of rainbow trout exposed to sublethal CBZ (1.0mugL(-1), 0.2mgL(-1) and 2.0mgL(-1)) for 7, 21 and 42d. After prolonged exposure of CBZ at higher test concentration (0.2 or 2.0mgL(-1)), oxidative stress was apparent as reflected by the significant higher LPO and CP levels in fish gi...

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Modeling the influence of cyclodextrins on oral absorption of low solubility drugs: II. Experimental validation

Biotechnology and Bioengineering — Sun, 01 Nov 2009 00:00:00 +0100

A model was developed for predicting the influence of cyclodextrins (CDs) delivered as a physical mixture with drug on oral absorption. CDs are cyclic oligosaccharides which form inclusion complexes with many drugs and are often used as solubilizing agents. The purpose of this work is to compare the simulation predictions with in vitro as well as in vivo experimental results to test the model's ability to capture the influence of CD on key processes in the gastrointestinal (GI) tract environment. Dissolution and absorption kinetics of low solubility drugs (Naproxen and Nifedipine) were tested in the presence and absence of CD in a simulated gastrointestinal environment. Model predictions were also compared with in vivo experimental results (Glibenclamide and Carbamazepine) from the literat...

Is asymmetric dimethylarginine responsible for the vascular events in patients under antiepileptic drug treatment?

Epilepsy Research — Sun, 01 Nov 2009 00:00:00 +0100

In conclusion our data suggest that elevated ADMA levels may be responsible for the increased cardiovascular risk in patients with epilepsy under AED therapy. (Source: Epilepsy Research)

The clinical challenge of SIADH-three cases.

NDT Plus — Sun, 01 Nov 2009 00:00:00 +0100

Authors: van der Lubbe N, Thompson CJ, Zietse R, Hoorn EJ The syndrome of inappropriate antidiuretic hormone secretion (SIADH) remains a challenging disorder to diagnose and treat. Three cases are presented to illustrate these challenges. The first two cases had drug-induced SIADH secondary to a selective serotonin reuptake inhibitor (for depression) or carbamazepine (for trigeminal neuralgia). The third case had SIADH possibly secondary to bronchiectasis. The lowest serum sodium concentrations ranged between 118 and 124 mmol/L in the three cases. Hyponatraemia was not acute and severe symptoms were absent. However, several mild neurological symptoms were present. In the first case, hyponatraemia likely contributed to a fall, which resulted in a fracture of the odontoid process of the ...

Prescriber compliance with black box warnings in older adult patients.

The American Journal of Managed Care — Sun, 01 Nov 2009 00:00:00 +0100

CONCLUSIONS: Administrative claims analysis identified low rates of prescriber compliance with BBWs in managing patients age >or=65 years. Claims analysis may be a cost-effective strategy to monitor prescriber compliance with BBWs in older patients at higher risk. PMID: 19895180 [PubMed - in process] (Source: The American Journal of Managed Care)

[Co-analgesics--today and tomorrow--a receptor-based overview of therapeutical options]

Anasthesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie : AINS — Sun, 01 Nov 2009 00:00:00 +0100

We describe the peripheral action sites of co-analgesics, such as cannabinoids, capsaicin, bisphosphonates, steroids and somatostatin. We also summarise the effect of peripherally and centrally acting ion-channel blockers, e.g. local anaesthetics, carbamazepine and tolperisone working on sodium channels and gabapentin and pregabalin working on calcium channels. Finally, central analgesic mechanisms are discussed, for instance the inhibition of NMDA-receptors by ketamine or magnesium, the stimulation of alpha2-receptors by clonidine, tizanidine or antidepressants, the activation of GABA-receptors through baclofen and other analgesic mechanisms of i.e. ondansetron and neostigmine. PMID: 19918705 [PubMed - in process] (Source: Anasthesiologie, Intensivmedizin, Notfallmedizin, Schmerzthera...

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Extended-release formulations of antiepileptic drugs: rationale and comparative value.

Epilepsy Curr — Sun, 01 Nov 2009 00:00:00 +0100

Authors: Perucca E Extended-release products are designed to prolong the absorption of drugs with short half-lives, thereby allowing longer dosing intervals while minimizing fluctuations in serum drug levels. The relationship between serum drug concentration and clinical effects of antiepileptic drugs (AEDs) can be complex and reducing fluctuations in serum drug levels is not equally advantageous for all AEDs. Extended-release formulations have been shown to be particularly valuable for carbamazepine, whereas for other AEDs advantages, other than prolongation of the dosing interval, have not been clearly demonstrated. Differences in bioavailability may exist between extended-release and immediate-release formulations and among different brands of extended-release products. Therefore, w...

Bipolar disorder and tuberous sclerosis complex: is it a mere coincidence?

CNS Spectrums — Sun, 01 Nov 2009 00:00:00 +0100

Authors: Haq MZ, Dubey I, Khess CR, Das U, Kumar R Tuberous sclerosis complex (TSC) is associated with significant psychiatric comorbidity mainly in the form of autistic disorders, hyperkinetic disorders, depression, and anxiety disorders. There are very few reports of bipolar disorder in TSC. The authors present the case of a patient with TSC having bipolar disorder manifesting as manic as well as depressive episodes. The diagnosis of TSC was based on the presence of facial angiofibromas, enamel pits, and shagreen patches on clinical examination, and the presence of cortical tubers and calcified subependymal nodules on neuroimaging. The patient presented during the manic phase of the illness and responded well to treatment with carbamazepine and haloperidol and became symptom free wit...

Carbamazepine/risperidone: Lichenoid drug eruptions: case report

Reactions — Sat, 31 Oct 2009 14:02:00 +0100

(Source: Reactions)

CARBATROL (Carbamazepine) Capsule [Physicians Total Care, Inc.]

DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST) — Fri, 30 Oct 2009 05:00:00 +0100

Updated Date: Oct 30, 2009 EST (Source: DailyMed Drug Label Updates for the last seven days (since May 20, 2007 EST))

Human health risk assessment of carbamazepine in surface waters of North America and Europe.

Regulatory Toxicology and Pharmacology : RTP — Fri, 30 Oct 2009 00:00:00 +0100

Authors: Cunningham VL, Perino C, D'Aco VJ, Hartmann A, Bechter R A human health risk assessment was carried out for environmental exposures to carbamazepine (CBZ) and its major human metabolites, carbamazepine diol (CBZ-DiOH) and carbamazepine N-glucuronide (CBZ-N-Glu). Carbamazepine is an active pharmaceutical ingredient (API) used worldwide as a medicine for treating epileptic seizures and trigeminal neuralgia. Carbamazepine tends to be detected in surface water more frequently and at relatively higher concentrations, than most other APIs. Predicted no effect levels (PNECs) for CBZ and its major human metabolites were developed for surface waters to be protective of human health from environmental exposures from drinking water and fish consumption. These PNECs were compared to both ...

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Treatment of febrile seizures: Historical perspective, current opinions, and potential future directions

Brain & Development — Mon, 26 Oct 2009 00:00:00 +0100

Abstract: Although most febrile seizures do no harm and two-thirds of initial cases have no witnessed recurrence, the seizures cause much family anxiety, and are sometimes prolonged. In rare cases they are the first evidence of important epilepsy syndromes or are implicated in the development of epilepsy with mesial temporal sclerosis in later life. There have been trials of prophylactic treatment with antiepileptic drugs including carbamazepine, diazepam, phenobarbital, phenytoin, and sodium valproate. Several strategies have been employed with these drugs, including continuous secondary prophylaxis, intermittent secondary prophylaxis in response to later episodes of fever, and rescue medication early in the course of further seizures. Another treatment strategy has been using one or more...

Teratogenic Effects of Antiepileptic Medications

Neurologic Clinics — Sat, 24 Oct 2009 13:25:56 +0100

During the last few years epilepsy and pregnancy registries and other large scale observational studies have provided new information on the teratogenic effects of the most frequently used antiepileptic drugs (AEDs). The prevalence of major congenital malformations associated with exposure to carbamazepine or lamotrigine appears to be only marginally increased from the expected, while malformation rates with valproate have been reported to be 2 to 4 times higher. Recent studies also suggest that compared with carbamazepine, lamotrigine and phenytoin, exposure to valproate in utero may be associated with poorer postnatal cognitive development. However, adverse outcomes with valproate appear to be dose-related, and doses below 800-1,000 mg/day might not be associated with worse outcome than ...

Eslicarbazepine Acetate Evaluated for Partial-Onset Seizures

Medscape Today Headlines — Fri, 23 Oct 2009 16:58:26 +0100

The experimental drug, similar to carbamazepine, may reduce seizure frequency in refractory patients. Medscape Medical News (Source: Medscape Today Headlines)

Effect of acute and chronic treatment with milnacipran potentiates the anticonvulsant activity of conventional antiepileptic drugs in the maximal electroshock-induced seizures in mice

Psychopharmacology — Tue, 20 Oct 2009 16:31:24 +0100

Conclusions Acute, but not chronic, treatment with MLN can increase the effectiveness of some AEDs against MES-induced seizures in mice. It seems that MLN may also be considered as a candidate drug for clinical trials in patients with epilepsy and depressive disorders. Content Type Journal ArticleCategory Original InvestigationDOI 10.1007/s00213-009-1698-xAuthors Kinga K. Borowicz, Lublin Medical University Experimental Neuropathophysiology Unit, Department of Pathophysiology Jaczewskiego 8 Lublin PolandKamila Furmanek-Karwowska, Lublin Medical University Experimental Neuropathophysiology Unit, Department of Pathophysiology Jaczewskiego 8 Lublin PolandMarta Morawska, Lublin Medical University Experimental Neuropathophysiology Unit, Department of Pathophysiology Jaczew...

The usefulness of olfactory bulb kindling as a model for evaluation of antiepileptics

Epilepsia — Mon, 19 Oct 2009 23:00:00 +0100

Discussion: OB kindling can be used as a new valuable model to evaluate antiepileptic drugs, with the advantage of its rapid development and the efficacy of antiepileptics. (Source: Epilepsia)

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Levodopa/tolcapone: Hypersexuality treated with carbamazepine in an elderly patient: case report

Reactions — Mon, 19 Oct 2009 13:04:56 +0100

(Source: Reactions)

No Pharmacokinetic Interaction Between Lacosamide and Carbamazepine in Healthy Volunteers.

The Journal of Clinical Pharmacology — Sun, 18 Oct 2009 23:00:00 +0100

Authors: Cawello W, Nickel B, Eggert-Formella A Lacosamide is a new antiepileptic drug for adjunctive treatment of adult partial-onset seizures. Two open-label, multiple-dose clinical trials were conducted to evaluate the potential for pharmacokinetic interaction between lacos amide and carbamazepine. The influence of carbamazepine on lacosamide pharmacokinetics (trial A) and lacosamide on carbamazepine pharmacokinetics (trial B) was investi gated in 19 (trial A) and 18 (trial B) healthy male partici pants. Trial A participants received lacosamide 200 mg bid alone and with carbamazepine 200 mg bid. Trial B partici pants received carbamazepine 200 mg bid alone and with lacosamide 200 mg bid. Pharmacokinetic parameters, area under the concentration-time curve during a dosage interval at ...

The Far-Reaching Influence of Hepatic Enzyme-Inducing Antiepileptic Drugs

Epilepsy Currents — Thu, 15 Oct 2009 23:00:00 +0100

Effects of Antiepileptic Drugs on Lipids, Homocysteine, and C-Reactive Protein. Mintzer S, Skidmore CT, Abidin CJ, Morales MC, Chervoneva I, Capuzzi DM, Sperling MR. Ann Neurol 2009;65:448[ndash]456. OBJECTIVE: The widely prescribed anticonvulsants phenytoin and carbamazepine are potent inducers of cytochrome P450 enzymes, which are involved in cholesterol synthesis. We sought to determine whether these drugs have an effect on cholesterol and other serological markers of vascular risk. METHODS: We recruited 34 epilepsy patients taking carbamazepine or phenytoin in monotherapy whose physicians had elected to change treatment to one of the noninducing anticonvulsants lamotrigine or levetiracetam. Fasting blood samples were obtained both before and 6 weeks after the switch to measure serum li...

Oxcarbazepine for refractory epilepsy: systematic review of the literature.

Sao Paulo Medical Journal — Thu, 15 Oct 2009 04:02:02 +0100

CONCLUSIONS: There is moderate evidence indicating that oxcarbazepine is effective as an alternative treatment for partial or generalized epilepsy in children and adults who were refractory to previous treatment. PMID: 19820875 [PubMed - in process] (Source: Sao Paulo Medical Journal)

Population-based study of antiepileptic drug exposure in utero—Influence on head circumference in newborns

Seizure: European Journal of Epilepsy — Thu, 15 Oct 2009 00:00:00 +0100

Abstract: Purpose: To study the effect of AED exposure on head circumference in the newborn.Methods: Data on all Swedish singletons births between 1995 and 2005, over 900,000 births, were obtained from the Swedish Medical Birth Registry. The effects of AEDs on birth-weight-adjusted mean head circumference (bw-adj-HC) were estimated by comparison with data from all births in an analysis which was adjusted for year of birth, maternal age, parity, maternal smoking, and maternal body mass index.Results: A significant reduction of mean bw-adj-HC was seen after both carbamazepine (CBZ) (standard deviation scores (SDS)=0.15, p (Source: Seizure: European Journal of Epilepsy)

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[Teratogenic effects of lamotrigine in women with bipolar disorder.]

Tijdschrift voor Psychiatrie — Wed, 14 Oct 2009 15:10:02 +0100

CONCLUSION: There are no strong indications that the use of lmt during pregnancy results in an increased number of major congenital malformations. PMID: 19821242 [PubMed - in process] (Source: Tijdschrift voor Psychiatrie)

Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles as potential anticonvulsant agents

Medicinal Chemistry Research — Wed, 14 Oct 2009 06:11:55 +0100

Abstract A series of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (Sc-PTZ), and rotarod tests in intraperitoneally injected mice. Among the synthesized compounds, compound 2-phenyl-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3a) could be considered the potentially most useful and safe therapeutic compound, with ED50 = 29.6 mg/kg, TD50 = 285 mg/kg, and PI = 9.7. Its neurotoxicity was the lowest of all the synthesized compounds and was also markedly lower than that of the reference drug carbamazepine with PI value of 6.4. Content Type Journal ArticleCategor...

Oxcarbazepine versus carbamazepine monotherapy for partial onset seizures

Neurological Conditions Specialist Library — Tue, 13 Oct 2009 16:30:09 +0100

Cochrane systematic review. Summary: Carbamazepine is the most commonly used drug to treat partial epileptic seizures. Oxcarbazepine is a newer drug that was developed with the intention to be as effective as carbamazepine but to cause fewer side effects. In this systematic review, we summarise three studies in which oxcarbazepine and carbamazepine treatment were compared directly. We found that both drugs appear to be equally effective and to cause side effects equally often. Significantly fewer patients on carbamazepine developed nausea or vomiting during treatment. (Source: Neurological Conditions Specialist Library)

Outpatient utilization of drugs acting on nervous system: a study from the Republic of Srpska, Bosnia & Herzegovina

European Journal of Clinical Pharmacology — Fri, 09 Oct 2009 06:06:13 +0100

Conclusions The observed tendency toward increased total drug utilization observed in our study is comparable to worldwide trends. Implementation of new clinical guidelines for nervous diseases and updating of the list of reimbursable drugs with the addition of new ones contributed to the observed improvement in prescribing patterns in primary healthcare during the study period. The DU90% is shown to be a simple rough method for assessing prescribing quality. More stratified analyses should be performed on a routine basis to ensure a rational use of medicines and a cost-efficient use of limited healthcare resources. Content Type Journal ArticleCategory Pharmacoepidemiology and PrescriptionDOI 10.1007/s00228-009-0732-6Authors Vanda Marković-Peković, Health Insuranc...

Updated MTRAC Verdict/Summary on levetiracetam (Keppra®)

NeLM - Drug Specific Reviews — Thu, 08 Oct 2009 23:00:00 +0100

Source: MTRAC Area: Evidence > Drug Specific Reviews The updated verdict on levetiracetam (Keppra®) for the treatment of partial onset seizures from the Midlands Therapeutics Review and Advisory Committee (MTRAC) is that it should be initiated and stabilised within secondary care, after which it is then appropriate for GPs to prescribe this treatment over the longer term, but patients are expected to receive continuing follow-up in secondary care. As a well established second line therapy, it is considered to have a relatively high place in therapy. The evidence was considered relatively strong for adults and children over the age of 4 years but was much weaker for children aged from 1 month to 4 years. A large comparative RCT found that levetiracetam monotherapy was not inferior to carb...

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Solvent Effects on the Crystallization and Preferential Nucleation of Carbamazepine Anhydrous Polymorphs: A Molecular Recognition Perspective

Organic Process Research — Wed, 07 Oct 2009 17:52:51 +0100

Organic Process Research & Development, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable). (Source: Organic Process Research)

Surprise Finding at Endoscopic Retrograde Cholangiopancreatography

Clinical Gastroenterology and Hepatology — Mon, 05 Oct 2009 00:00:00 +0100

A 47-year-old woman was admitted with right upper-quadrant pain, radiating to her back, with nausea and fever. She was known to have had gallstones and had undergone open cholecystectomy 9 years earlier. She developed epilepsy after an intracerebral hemorrhage at the age of 22, for which she was on treatment with phenytoin and carbamazepine, and had mild asthma. (Source: Clinical Gastroenterology and Hepatology)

Opinion of Belgian neurologists on antiepileptic drug treatment in 2006: Belgian study on epilepsy treatment (BESET-2)

Acta Neurologica Scandinavica — Sun, 04 Oct 2009 23:00:00 +0100

Conclusions [ndash] In end 2006, carbamazepine, valproate and oxcarbazepine were considered to be first choice drugs, whereas other newer drugs, like lamotrigine, levetiracetam and topiramate were predominantly prescribed in second line. (Source: Acta Neurologica Scandinavica)

Antiepileptic drugs in Australia: 2002-2007

Pharmacoepidemiology and Drug Safety — Thu, 01 Oct 2009 23:00:00 +0100

We examined the trends in the prescribing of subsidised AEDs in the Australian population from 2002 to 2007.We analysed the Medicare Australia and Drug Utilisation Sub-Committee databases for script data for AEDs from 2002 to 2007 in 5-year age groups by gender and by class of prescriber. Scripts were converted to defined daily doses (DDDs)/1000/day using Australian Bureau of Statistics population data.Overall AED use (mainly valproate, lamotrigine and levetiracetam) increased progressively in 2002-2007 from 9.33 to 10.12 DDD/1000 population/day. Sodium valproate was the most widely used agent followed by carbamazepine then phenytoin. Amount of AED used increased in those aged in their 20s and 30s to plateau between 40 and 90 years. Use peaked in those aged 80-84 years and was slightly hig...

The Influence of Drug-Drug Interaction and Patients' Characteristics on Valproic Acid's Clearance in Adults with Epilepsy using Nonlinear Mixed Effects Modeling.

European Journal of Pharmaceutical Sciences — Thu, 01 Oct 2009 23:00:00 +0100

This study confirms the interaction of VPA with TPR, which is presumably dependent on VPA dose. PMID: 19804822 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)

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Simultaneous determination of venlafaxine and its main active metabolite O-desmethyl venlafaxine in rat plasma by LC-MS/MS.

Wed, 30 Sep 2009 23:00:00 +0100

Authors: Shah GR, Thaker BT, Surati KR, Parabia MH A simple, sensitive and selective liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed and validated for the analysis of venlafaxine (VX) and its major active metabolite O-desmethyl venlafaxine (ODV) in rat plasma using carbamazepine as an internal standard (IS). The analytes from the biological matrix were extracted by liquid-liquid extraction using tert-butyl methyl ether (TBME). The HPLC separation of the analytes was performed on a water symmetry C18 (150 x 4.6 mm i.d., 5 microm) column, using a 10 mM ammonium formate:methanol (20:80 v/v) as mobile phase. The calibration curve concentration range was 10.10 to 8000.00 ng/mL for VX and ODV with coefficient of determination above 0.9970. The lower limit of qu...

Argatroban/carbamazepine/heparin: TEN, coagulation failure and fatal HIT: case report

Reactions — Wed, 30 Sep 2009 16:32:33 +0100

(Source: Reactions)

Predicting physical properties of emerging compounds with limited physical and chemical data: QSAR model uncertainty and applicability to military munitions.

Chemosphere — Sun, 27 Sep 2009 23:00:00 +0100

Authors: Bennett ER, Clausen J, Linkov E, Linkov I Reliable, up-front information on physical and biological properties of emerging materials is essential before making a decision and investment to formulate, synthesize, scale-up, test, and manufacture a new material for use in both military and civilian applications. Multiple quantitative structure-activity relationships (QSARs) software tools are available for predicting a material's physical/chemical properties and environmental effects. Even though information on emerging materials is often limited, QSAR software output is treated without sufficient uncertainty analysis. We hypothesize that uncertainty and variability in material properties and uncertainty in model prediction can be too large to provide meaningful results. To test ...

[Aetiology of epileptic seizures in a rehabilitation centre.]

Revista de Neurologia — Thu, 24 Sep 2009 15:34:33 +0100

CONCLUSIONS. Epilepsy can limit rehabilitation therapy in patients with stroke or traumatic injury, due to the risk of developing difficult-to-treat epilepsy. Caregivers often have to take responsibility for the pharmacological treatment in disabled patients with brain damage. PMID: 19774528 [PubMed - in process] (Source: Revista de Neurologia)

Disinhibition Due to Disruption of the Orbitofrontal Circuit Treated Successfully With Carbamazepine: A Case Series [CLINICAL AND RESEARCH REPORTS]

J Neuropsychiatry Clin Neurosci — Tue, 22 Sep 2009 23:00:00 +0100

The frontal-subcortical pathways play a role in governing behavior. Injury may disrupt their functioning and produce neuropsychiatric symptoms. The authors discuss the kindling theory in the possible production of these symptoms, which significantly improved with the potent antikindling agent, carbamazepine. (Source: J Neuropsychiatry Clin Neurosci)

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Ghrelin levels are reduced in prepubertal epileptic children under treatment with carbamazepine or valproic acid

Epilepsia — Mon, 21 Sep 2009 23:00:00 +0100

A relationship between ghrelin and epilepsy has been already shown in humans, although the results are controversial. Ghrelin levels are reduced in obesity. Epileptic patients progressively develop a therapy-linked weight gain; however, the mechanisms for this have not been fully explained. The aim of our study is to evaluate if ghrelin secretion is modulated by treatment with carbamazepine or valproic acid in young prepubertal epileptic children. Ghrelin levels were reduced in normal-weight young epileptic prepubertal children under treatment with carbamazepine (p < 0.0001) or valproic acid (p < 0.006) compared to healthy age- and weight-matched subjects. Ghrelin was also lower in children under carbamazepine when compared to those under valproic acid (p < 0.01). A derangement in ghrelin ...

Hyperhomocysteinemia in epileptic patients on new antiepileptic drugs

Epilepsia — Mon, 21 Sep 2009 23:00:00 +0100

Discussion: Oxcarbazepine and topiramate might cause hyper-tHcy, most likely because of the capacity of these agents to induce the hepatic enzymes. Because literature data suggest that hyper-tHcy may contribute to the development of cerebrovascular diseases and brain atrophy, a supplement of folate can be considered in these patients to normalize plasma tHcy. (Source: Epilepsia)

Neurological and Cardiovascular Adverse Events Associated with Antimanic Treatment in Children and Adolescents.

CNS Neuroscience and Therapeutics — Sun, 20 Sep 2009 23:00:00 +0100

Authors: Jerrell JM To identify the factors associated with incident neurological and cardiovascular adverse events in children and adolescents treated with antimanic agents, a retrospective, longitudinal study was conducted. Medicaid medical and pharmacy claims between January 1996 and December 2005 were used to identify 3657 children and adolescents prescribed antimanic medications, and a random sample of 4500 children not treated with psychotropic medications. All adverse events examined (sedation/drowsiness, headaches, involuntary movements/extrapyramidal symptoms (EPS), cardiovascular events, hypertension, and orthostatic hypotension) were more prevalent in the antimanic-treated cohort. The odds of developing incident sedation/drowsiness and headaches were significantly higher for...

Modulation of antioxidant defence system in brain of rainbow trout (Oncorhynchus mykiss) after chronic carbamazepine treatment.

Comparative biochemistry and physiology. Toxicology and pharmacology : CBP — Sun, 20 Sep 2009 23:00:00 +0100

Authors: Li ZH, Zlabek V, Velisek J, Grabic R, Machova J, Randak T We investigated the effect of long-term exposure to CBZ on the antioxidant system in brain tissue of rainbow trout. Fish were exposed to sublethal concentrations of CBZ (1.0mug/L, 0.2mg/L or 2.0mg/L) for 7, 21, and 42days. Oxidative stress indices (LPO and CP) and activities of antioxidant enzymes (SOD, CAT, GPx and GR) in fish brain were measured. In addition, non-enzymatic antioxidant (GSH) was determined after 42days exposure. Carbamazepine exposure at 0.2mg/L led to significant increases (p<0.05) of LPO and CP after 42days and, at 2.0mg/L, after 21days. Activities of the antioxidant enzymes SOD, CAT, and GPx in CBZ-treated groups slightly increased during the first period (7days). However, activities of all measu...

Catastrophic antiphospholipid syndrome in a patient with Down syndrome.

Lupus — Sat, 19 Sep 2009 13:34:03 +0100

We report a patient with Down syndrome, under treatment with carbamazepine, levopromazine and clonazepam. After urinary infection he developed glans necrosis requiring excision of prepuce. Six hours post surgery he presented right-hand ischemia followed by arterial and venous thrombosis of the right thoracic extremity. Later, he progressed to a compartment syndrome and presented ischemia of toes. All the clinical manifestations developed over a week. Anticardiolipin (aCL) antibodies, lupus anticoagulant and perinuclear antineutrophil antibodies were positive. Anticoagulant and immunosuppressive treatment were initiated. Owing to the failure of both treatments, the patient underwent amputation of right hand and a toe. Histopathology revealed recent and old thrombosis of medium- and small-si...

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Is the brain arachidonic acid cascade a common target of drugs used to manage bipolar disorder?

Biochemical Society Transactions — Fri, 18 Sep 2009 02:26:20 +0100

Authors: Bazinet RP Although lithium has been used therapeutically to treat patients with bipolar disorder for over 50 years, its mechanism of action, as well as that of other drugs used to treat bipolar disorder, is not agreed upon. In the present paper, I review studies in unanaesthetized rats using a neuropharmacological approach, combined with kinetic, biochemical and molecular biology techniques, demonstrating that chronic administration of three commonly used mood stabilizers (lithium, valproic acid and carbamazepine), at therapeutically relevant doses, selectively target the brain arachidonic acid cascade. Upon chronic administration, lithium and carbamazepine decrease the binding activity of activator protein-2 and, in turn, the transcription, translation and activity of its ar...

PtdIns(3,4,5)P(3) and inositol depletion as a cellular target of mood stabilizers.

Biochemical Society Transactions — Fri, 18 Sep 2009 02:26:18 +0100

Authors: Teo R, King J, Dalton E, Ryves J, Williams RS, Harwood AJ Lithium (Li(+)) is the mood stabilizer most frequently used in the treatment of bipolar mood disorder; however, its therapeutic mechanism is unknown. In the 1980s, Berridge and colleagues proposed that Li(+) treatment acts via inhibition of IMPase (inositol monophosphatase) to deplete the cellular concentration of myo-inositol. Inositol depletion is also seen with the alternative mood stabilizers VPA (valproic acid) and CBZ (carbamazepine), suggesting a common therapeutic action. All three drugs cause changes in neuronal cell morphology and cell chemotaxis; however, it is unclear how reduced cellular inositol modulates these changes in cell behaviour. It is often assumed that reduced inositol suppresses Ins(1,4,5)P(3), ...

Synthetic and Natural Compounds that Interact with Human Cytochrome P450 1A2 and Implications in Drug Development.

Current Medicinal Chemistry — Tue, 15 Sep 2009 23:00:00 +0100

Authors: Wang B, Zhou SF Human cytochrome P450 1A2 (CYP1A2) is one of the major CYPs in the liver ( approximately 13%) and metabolizes about 20% of clinically used drugs. CYP1A2 is a 515-residue protein with a molecular mass of 58,294 Dal. The recently published crystal structure of CYP1A2 in complex with alpha-naphthoflavone has showed a rather compact active site with a relatively small volume of the cavity of 375 A(3), which is 44.2% and 49.3% larger than that of CYP2A6 (260 A(3)) and CYP2E1 (190 A(3)), respectively. A series of residues in the substrate recognition regions of CYP1A2 (e.g. Arg108, Thr124, Thr223, Glu225, Phe226, Lys250, Arg251, Lys253, Asn312, Asp313, Glu318, Thr319, Asp320, Thr321, Val322, Leu382, Thr385, and Ile386) have been shown to play important roles in ligan...

Early effects of drugs responsible for DRESS on HHV-6 replication in vitro

Journal of Clinical Virology — Tue, 15 Sep 2009 23:00:00 +0100

In this study we determined the early effects of therapeutical plasma levels of VPA, carbamazepine, phenytoin and sulfazalasine on replication of HHV-6B strain HST in MT4 cells. (Source: Journal of Clinical Virology)

Carbamazepine/lamotrigine: Anticonvulsant hypersensitivity syndrome: case report

Reactions — Mon, 14 Sep 2009 16:26:44 +0100

(Source: Reactions)

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Carbamazepine/lamotrigine/valproate: Aggravation of seizures, and elevation of ALT, in an infant with SCN1A mutation: case report

Reactions — Mon, 14 Sep 2009 16:26:44 +0100

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Impact of antiepileptic drugs on cognition, behavior, and motor skills in children with new-onset, idiopathic epilepsy.

Epilepsy and Behaviour — Fri, 11 Sep 2009 23:00:00 +0100

CONCLUSIONS: There were few adverse effects of antiepileptic drug treatment in the group followed over 12 months. Carbamazepine may have been responsible for persistent impairment of reaction time and reaction time variability. PMID: 19751992 [PubMed - as supplied by publisher] (Source: Epilepsy and Behaviour)

Carbamazepine/haloperidol/phenothiazines: Intussusception (first report with carbamazepine and haloperidol): case report

Reactions — Mon, 07 Sep 2009 16:24:50 +0100

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Oxcarbazepine in Combination with Tiaprid in Inpatient Alcohol-withdrawal – a RCT

Pharmacopsychiatry — Wed, 02 Sep 2009 18:17:55 +0100

Pharmacopsychiatry 2009; 42: 175-181DOI: 10.1055/s-0029-1202264Abstract Oxcarbazepine (OXC), a derivative of Carbamazepine (CBZ), may represent a solution to metabolic and side effects of CBZ treatment due to the fact that renal excretion is its major route of elimination. The goal of the study is to compare the efficacy and tolerability of OXC/Tiaprid (TIA) combination therapy to the well established Clomethiazole (CLO) therapy in an inpatient setting.[...]© Georg Thieme Verlag KG Stuttgart · New YorkGet connected:Table of contents | Abstract | Full text (Source: Pharmacopsychiatry)

Association between consistent purchase of anticonvulsants or lithium and suicide risk: A longitudinal cohort study from Denmark, 1995–2001

Journal of Affective Disorders — Wed, 02 Sep 2009 16:52:08 +0100

Abstract: Background: Prior studies suggest anticonvulsants purchasers may be at greater risk of suicide than lithium purchasers.Methods: Longitudinal, retrospective cohort study of all individuals in Denmark purchasing anticonvulsants (valproic acid, carbamazepine, oxcarbazepine or lamotrigine) (n=9952) or lithium (n=6693) from 1995–2001 who also purchased antipsychotics at least once (to select out nonpsychiatric anticonvulsant use). Poisson regression of suicides by medication purchased (anticonvulsants or lithium) was conducted, controlling for age, sex, and calendar year. Confounding by indication was addressed by restricting the comparison to individuals prescribed the same medication: individuals with minimal medication exposure (e.g., who purchased only a single prescription of a...

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Effect of caffeine on the anticonvulsant effects of oxcarbazepine, lamotrigine and tiagabine in a mouse model of generalized tonic-clonic seizures.

Pharmacological Reports — Tue, 01 Sep 2009 00:00:00 +0100

In conclusion, caffeine did not impair the anticonvulsant effects of lamotrigine, oxcarbazepine, or tiagabine as assessed by electroconvulsions in mice. Also, caffeine was without effect upon the adverse potential of the studied antiepileptic drugs. Thus caffeine may not necessarily adversely affect the efficacy of all antiepileptic drugs and this is an important observation. PMID: 19904004 [PubMed - in process] (Source: Pharmacological Reports)

Clinical risk management of Stevens–Johnson syndrome/toxic epidermal necrolysis spectrum

Dermatologic Therapy — Mon, 31 Aug 2009 23:00:00 +0100

Clinical risk management concedes that risk is inherent to all health-care processes. Stevens[ndash]Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) are rare but potentially life-threatening reactions to medications. Risk management should be considered prior to starting, during, and after therapy. Prior to starting therapy, risks that need to be assessed include any specific patient groups that may be at greater risk for the development of SJS/TEN. Gene testing is in place for Chinese and Thai patients who are going to be exposed to carbamazepine. During therapy, it is important to recognize SJS/TEN as a possible adverse drug reaction. Diagnostic criteria have changed, and more data exist on drugs with an increased risk. Although there is no standardized treatment for all patie...

Hypersensitivity Syndrome Induced by Anticonvulsants: Possible Cross-Reactivity Between Carbamazepine and Lamotrigine.

The Journal of Clinical Pharmacology — Mon, 31 Aug 2009 23:00:00 +0100

Authors: Aouam K, Ben Romdhane F, Loussaief C, Salem R, Toumi A, Belhadjali H, Chaabane A, Boughattas NA, Chakroun M A 14-year-old male presents with erythroderma and fever 44 days after carbamazepine intake. Laboratory exams show eosinophilia and elevated liver enzymes, and thoracic imaging reveals interstitial pneumonitis. All symptoms disappear after carbamazepine withdrawal. A patch test to carbamazepine performed 6 weeks after recovery is positive. About 8 months later, the patient exhibits the same clinical and biological picture 52 days after lamotrigine intake. Lamotrigine is stopped and all symptoms disappear. A patch test to LMG is positive. This case illustrates a possible cross-reactivity between carbamazepine and lamotrigine, which are aromatic and nonaromatic anticonvulsa...

Extended-Release Formulations of Antiepileptic Drugs: Rationale and Comparative Value

Epilepsy Currents — Mon, 31 Aug 2009 23:00:00 +0100

Extended-release products are designed to prolong the absorption of drugs with short half-lives, thereby allowing longer dosing intervals while minimizing fluctuations in serum drug levels. The relationship between serum drug concentration and clinical effects of antiepileptic drugs (AEDs) can be complex and reducing fluctuations in serum drug levels is not equally advantageous for all AEDs. Extended-release formulations have been shown to be particularly valuable for carbamazepine, whereas for other AEDs advantages, other than prolongation of the dosing interval, have not been clearly demonstrated. Differences in bioavailability may exist between extended-release and immediate-release formulations and among different brands of extended-release products. Therefore, when switching from one ...