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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 C 14H18N2O3  
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 Schedule IV
Routes Intravenous, rectal
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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.

Contents

Pharmacology

Methohexital binds to a distinct site which is associated with Cl ionophores at GABAA 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. Side-chain oxidation is the primary means of metabolism involvedtermination 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 similar 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).

References

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

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