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QuickView for Methylphenobarbital (compound)


PubChem
Name: Mephobarbital
PubChem Compound ID: 6451435
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.
Molecular formula: C13H14N2O3
Molecular weight: 246.262 g/mol
Synonyms:
2671-99-0; (S)-5-Ethyl-1-methyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione; 2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-ethyl-1-methyl-5-phenyl-, (S)-; (+)-Mephobarbitol; ZINC03831033
DrugBank
Identification
Name: Mephobarbital
Name (isomeric): DB00849
Drug Type: small molecule
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.
Synonyms:
Methylphenylbarbituric acid; Metilfenobarbitale [Dcit]; N-Ethylmethylphenylbarbituric acid; Methylphenobarbitonum; N-Methylphenobarbital; Mephobarbitone; Methylphenolbarbital; Methyl Phenobarbitone; Methylphenobarbitalum [INN-Latin]; N-Methylethylphenylbarbituric acid.
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Brand: Prominal, Mebroin, Isonal, Metylfenemal, Enphenemal, Menta-Bal, Metyna, Mebaral, Morbusan, Phemitone, Phemetone, Methyl-Calminal, Enphenemalum, Phenmiton, Phemiton, Enfenemal, Meberal, Mephytal
Category: GABA Modulators, Hypnotics and Sedatives, Anticonvulsants
CAS number: 115-38-8
Pharmacology
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 excitati...
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Mechanism of Action: Methylphenobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Absorption: Approximately 50% of an oral dose of mephobarbital is absorbed from the gastrointestinal tract.
Protein binding: 70-76%
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.
Half Life: 34 (range 11-67) hours
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
DelavirdineThe anticonvulsant, methylphenobarbital, decreases the effect of delavirdine.
DoxycyclineThe anticonvulsant, methylphenobarbital, decreases the effect of doxycycline.
MetronidazoleThe barbiturate, methylphenobarbital, decreases the effect of metronidazole.
ClomifeneThe enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, clomifene.
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Targets


Enzymes