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Effects of felbamate on the pharmacokinetics of phenobarbital. 1995

P Reidenberg, and P Glue, and C R Banfield, and R D Colucci, and J W Meehan, and E Radwanski, and P Mojavarian, and C C Lin, and J Nezamis, and M Guillaume
Department of Clinical Pharmacology, Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.

The effects of felbamate on the pharmacokinetics of phenobarbital and one of its main metabolites, parahydroxyphenobarbital, were assessed in a parallel-group, placebo-controlled, double-blind study, in 24 healthy volunteers. Pharmacokinetic parameters of phenobarbital and parahydroxyphenobarbital were determined from plasma and urine samples obtained after 28 days of daily administration of 100 mg phenobarbital and after a further 9 days of phenobarbital plus 2400 mg/day felbamate or placebo. Felbamate increased phenobarbital values for area under the plasma concentration-time curve from 0 to 24 hours and maximum concentration by 22% and 24%, respectively, whereas placebo had no effect. This increase was caused by a reduction in parahydroxylation of phenobarbital and possibly through effects on other metabolic pathways. Because felbamate inhibits the S-mephenytoin hydroxylase (CYP2C19) isozyme in vitro, it appears that phenobarbital hydroxylation is mediated in part by this isozyme.

UI MeSH Term Description Entries
D008297 Male Males
D010634 Phenobarbital A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. Phenemal,Phenobarbitone,Phenylbarbital,Gardenal,Hysteps,Luminal,Phenobarbital Sodium,Phenobarbital, Monosodium Salt,Phenylethylbarbituric Acid,Acid, Phenylethylbarbituric,Monosodium Salt Phenobarbital,Sodium, Phenobarbital
D010919 Placebos Any dummy medication or treatment. Although placebos originally were medicinal preparations having no specific pharmacological activity against a targeted condition, the concept has been extended to include treatments or procedures, especially those administered to control groups in clinical trials in order to provide baseline measurements for the experimental protocol. Sham Treatment
D011409 Propylene Glycols Derivatives of propylene glycol (1,2-propanediol). They are used as humectants and solvents in pharmaceutical preparations. Propanediols,Glycols, Propylene
D004311 Double-Blind Method A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment. Double-Masked Study,Double-Blind Study,Double-Masked Method,Double Blind Method,Double Blind Study,Double Masked Method,Double Masked Study,Double-Blind Methods,Double-Blind Studies,Double-Masked Methods,Double-Masked Studies,Method, Double-Blind,Method, Double-Masked,Methods, Double-Blind,Methods, Double-Masked,Studies, Double-Blind,Studies, Double-Masked,Study, Double-Blind,Study, Double-Masked
D004334 Drug Administration Schedule Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience. Administration Schedule, Drug,Administration Schedules, Drug,Drug Administration Schedules,Schedule, Drug Administration,Schedules, Drug Administration
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D005937 Glucaric Acid A sugar acid derived from D-glucose in which both the aldehydic carbon atom and the carbon atom bearing the primary hydroxyl group are oxidized to carboxylic acid groups. Glucosaccharic Acid,L-Gularic Acid,Levo-Gularic Acid,Tetrahydroxyadipic Acid,Calcium Glucarate,Calcium Glucarate, Anhydrous,Calcium Saccharate,Calcium Saccharate Anhydrous,Calcium Saccharate Tetrahydrate,Calcium Saccharate, Anhydrous,D-Glucaric Acid,D-Saccharic Acid,Saccharic Acid,Acid, Saccharic,Anhydrous Calcium Glucarate,Anhydrous Calcium Saccharate,D Glucaric Acid,D Saccharic Acid,Glucarate, Anhydrous Calcium,Glucarate, Calcium,L Gularic Acid,Levo Gularic Acid,Saccharate Tetrahydrate, Calcium,Saccharate, Anhydrous Calcium,Saccharate, Calcium,Tetrahydrate, Calcium Saccharate
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000078328 Felbamate A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY. (3-Carbamoyloxy-2-phenyl-propyl) carbamate,2-Phenyl-1,3-propanediol dicarbamate,ADD-03055,Felbamyl,Felbatol,Taloxa,W-554,2 Phenyl 1,3 propanediol dicarbamate,ADD 03055,ADD03055,W 554,W554

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