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Methohexital



Methohexital
Systematic (IUPAC) name
5-hex-3-yn-2-yl-1- methyl-5-prop-2-enyl-1, 3-diazinane-2,4,6-trione
Identifiers
CAS number 151-83-7
ATC code N01AF01 N05CA15
PubChem 9034
DrugBank APRD00058
Chemical data
Formula C14H18N2O3 
Mol. mass 262.304
Pharmacokinetic data
Bioavailability I.V. ~100%
Rectal ~17%
Metabolism Hepatic
Half life 5.6 ± 2.7 minutes
Excretion  ?
Therapeutic considerations
Pregnancy cat.

B (USA)

Legal status

?

Routes Intravenous, rectal

Methohexital (marketed under the brand name Brevital) is a drug which is a barbiturate derivative. It is classified as short-acting, and has a rapid onset of action. It is similar in its effects to sodium thiopental, a drug with which it competed in the market for anaesthetics.

Additional recommended knowledge

Pharmacology

Methohexital binds to a distinct site which is associated with Cl ionophores at GABAA receptors. This increases the length of time which the Cl ionopores are open, thus causing an inhibitory effect.

Metabolism of methohexital is primarily hepatic (i.e. taking place in the liver), via demethylation and oxidation. Side-chain oxidation is the primary means of metabolism involved in the termination of the drug's biological activity.

Protein binding is approximately 73% for methohexital.

Indications

Methohexital is primarily used to induce anesthesia, and is generally provided as a sodium salt (i.e. methohexital sodium). It is only used in hospital or ambulatory care (i.e. in an ambulance) settings, under strict supervision. It has been commonly used to induce deep sedation, "twilight sleep" or general anesthesia for oral surgery and dentistry. It is also used to induce anesthesia prior to ECT(electroconvulsive therapy).

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Methohexital". A list of authors is available in Wikipedia.
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