Kessobamate - General Information
A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Kessobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of anxiety disorders, and also for the short-term management of insomnia but has largely been superseded by the benzodiazepines. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) Kessobamate is a controlled substance in the U.S.
Pharmacology of Kessobamate
Kessobamate is an anxiolytic drug. It was the best selling minor tranquilizer for a time but has largely been replaced by benzodiazepines. Kessobamate has most of the pharmacological effects and dangers of the barbiturates (though it was marketed as being safer). However, it is less sedating at effective doses. It is reported to have some anticonvulsant properties against absence seizures, but can exacerbate generalized tonic-clonic seizures. It has also been used as a hypnotic (sleeping pill). However, its is currently only licensed as an anxiolytic and it is a third or fourth-order choice.
Kessobamate for patients
No Information Provided.
Acute intermittent porphyria as well as allergic or idiosyncratic reactions to meprobamate or related compounds such as carisoprodol, mebutamate, tybamate or carbromal.
Additional information about Kessobamate
Kessobamate Indication: For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety.
Mechanism Of Action: Kessobamate's mechanism of action is not known. It has been shown in animal studies to have effects at multiple sites in the central nervous system, including the thalamus and limbic system. Kessobamate binds to GABAA receptors which interrupt neuronal communication in the reticular formation and spinal cord, causing sedation and altered perception of pain.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Meprobamate
Synonyms: Meprobamat [German]; Meprobamatum [INN-Latin]; Meprobamato [Italian]; Meprobamato [INN-Spanish]; Meprobamic acid; DEA No. 2820; Procarbamide
Drug Category: Anti-anxiety Agents; Anticonvulsants; Hypnotics and Sedatives; Muscle Relaxants, Central
Drug Type: Small Molecule; Illicit; Approved
Absorption: Well absorbed from the gastrointestinal tract.
Toxicity (Overdose): Symptoms of overdose include coma, drowsiness, loss of muscle control, severely impaired breathing, shock, sluggishness, and unresponsiveness. Death has been reported with ingestion of as little as 12 g meprobamate and survival with as much as 40 g.
Protein Binding: Not Available
Half Life: Plasma half-life is about 10 hours.
Dosage Forms of Kessobamate: Tablet Oral
Chemical IUPAC Name: [2-(carbamoyloxymethyl)-2-methylpentyl] carbamate
Chemical Formula: C9H18N2O4
Meprobamate on Wikipedia: https://en.wikipedia.org/wiki/Meprobamate
Organisms Affected: Humans and other mammals