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QuickView for Methohexital (compound)


PubChem
Name: Methohexital
PubChem Compound ID: 9034
Description: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.
Molecular formula: C14H18N2O3
Molecular weight: 262.304 g/mol
Synonyms:
Methohexital; 5-Allyl-5-(3-hexyn-2-yl)-1-methylbarbituric acid; DEA No. 2264; Metohexital [INN-Spanish]; 2,4,6(1H,3H,5H)-Pyrimidinetrione, 1-methyl-5-(1-methyl-2-pentynyl)-5-(2-propenyl)-, (.+/-.)-; Compound 25398; Enallynymalum; 151-83-7; Barbituric acid, 5-allyl-1-methyl-5-(1-methyl-2-pentynyl)-; EINECS 205-798-6.
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DrugBank
Identification
Name: Methohexital
Name (isomeric): DB00474
Drug Type: small molecule
Description: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.
Synonyms:
Methohexitone; Methodrexitone
Brand: Brevital sodium, Brietal, Brevital
Category: Anesthetics, Intravenous, Anesthetics, Barbiturates
CAS number: 151-83-7
Pharmacology
Indication: Methohexital is indicated for use as an intravenous anaesthetic. It has also been commonly used to induce deep sedation.
Pharmacology:
Methohexital, a barbiturate, is used for the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in exc...
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Mechanism of Action: Methohexital 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: The absolute bioavailability following rectal administration of methohexital is 17%.
Protein binding: 73%
Biotransformation: Metabolism occurs in the liver through demethylation and oxidation. Side-chain oxidation is the most important biotransformation involved in termination of biologic activity.
Route of elimination: Excretion occurs via the kidneys through glomerular filtration.
Half Life: 5.6 ± 2.7 minutes
Toxicity: The onset of toxicity following an overdose of intravenously administered methohexital will be within seconds of the infusion. If methohexital is administered rectally or is ingested, the onset of toxicity may be delayed. The manifestations of an ultrashort-acting barbiturate in overdose include central nervous system depression, respiratory depression, hypotension, loss of peripheral vascular resistance, and muscular hyperactivity ranging from twitching to convulsive-like movements. Other findings may include convulsions and allergic reactions. Following massive exposure to any barbiturate, pulmonary edema, circulatory collapse with loss of peripheral vascular tone, and cardiac arrest may occur.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
BetamethasoneThe barbiturate, methohexital, may decrease the effect of the corticosteroid, betamethasone.
Ethinyl EstradiolThis product may cause a slight decrease of contraceptive effect
GriseofulvinThe barbiturate, methohexital, decreases the effect of griseofulvin.
PrednisoloneThe barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisolone.
DiethylstilbestrolThe enzyme inducer, methohexital, decreases the effect of the hormone agent, diethylstilbestrol.
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Targets