Methohexital

Methohexital
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Systematic (IUPAC) name
	5-hex-3-yn-2-yl-1- methyl-5-prop-2-enyl-1, 3-diazinane-2,4,6-trione
Clinical data
Pregnancy; category	B (USA);
Routes of; administration	Intravenous, rectal
Legal status
Legal status	Schedule IV;
Pharmacokinetic data
Bioavailability	I.V. ~100%; Rectal ~17%
Metabolism	Hepatic
Biological half-life	5.6 ± 2.7 minutes
Excretion	?
Identifiers
CAS Number	151-83-7
ATC code	N01AF01 (WHO) N05CA15
PubChem	CID 9034
DrugBank	APRD00058
Chemical data
Formula	C14H18N2O3
Molar mass	262.304[[Script error: No such module "String".]]
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Methohexital, also called methohexitone, (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.^[1] 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 involvedtermination of the drug's biological activity.

Protein binding is approximately 73% for methohexital.^{[citation needed]}

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 similar 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).

References

↑ Katzung, Bertram G., Basic and Clinical Pharmacology, 10th ed., p. 406-407

External links

sv:Metohexital

[1] Katzung, Bertram G., Basic and Clinical Pharmacology, 10th ed., p. 406-407

[1]

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Carbamates	Carisbamate • Carisoprodol • Emylcamate • Ethinamate • Febarbamate • Felbamate • Hexapropymate • Mebutamate • Meprobamate • Methocarbamol • Phenprobamate • Procymate • Styramate • Tybamate
Neuroactive steroids	Acebrochol • Allopregnanolone • Alphadolone • Alphaxolone • Ganaxolone • Hydroxydione • Minaxolone • Org 20599 • THDOC
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Methohexital

Contents

Pharmacology

Indications

References

External links

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