Methohexital

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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.^{[citation needed]} 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.

[edit] Pharmacology

Methohexital binds to a distinct site which is associated with Cl^−ionophores at GABA_A receptors.^{[citation needed]} 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.^{[citation needed]} 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.^{[citation needed]}

[edit] 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.^{[citation needed]} 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).

[edit] External links