Drug Groups

approved

Description

A barbiturate that is metabolized to phenobarbital. It has been used for similar purposes, especially in epilepsy, but there is no evidence mephobarbital offers any advantage over phenobarbital. [PubChem]

Indication

For the relief of anxiety, tension, and apprehension, also used as an anticonvulsant for the treatment of epilepsy.

Pharmacology

Methylphenobarbital, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia.

Affected Organisms

Biotransformation

Hepatic, primarily by the hepatic microsomal enzyme system. About 75% of a single oral dose of mephobarbital is metabolized to phenobarbital in 24 hours.

Absorption

Approximately 50% of an oral dose of mephobarbital is absorbed from the gastrointestinal tract.

Half Life

34 (range 11-67) hours

Protein Binding

70-76%

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