Methohexital

Methohexital

File:Methohexital2.png
Clinical data
Pregnancy category	B (USA)
Routes of administration	Intravenous, rectal
ATC code	N01AF01 (WHO) N05CA15 (WHO)
Legal status
Legal status	?
Pharmacokinetic data
Bioavailability	I.V. ~100% Rectal ~17%
Metabolism	Hepatic
Elimination half-life	5.6 ± 2.7 minutes
Excretion	?
Identifiers
IUPAC name 5-hex-3-yn-2-yl-1- methyl-5-prop-2-enyl-1, 3-diazinane-2,4,6-trione
CAS Number	151-83-7
PubChem CID	9034
DrugBank	APRD00058
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C14H18N2O3
Molar mass	262.304

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.

Pharmacology

Methohexital binds to a distinct site which is associated with Cl⁻ ionophores at GABA_A 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).

External links

• RxList.com - Methohexital
• Drugs.com - Methohexital Sodium
• DrugLib.com - Brevital (Methohexital Sodium)