Difference between revisions of "Methohexital"
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Latest revision as of 20:01, 24 September 2010
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Systematic (IUPAC) name | |
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5-hex-3-yn-2-yl-1- methyl-5-prop-2-enyl-1, 3-diazinane-2,4,6-trione | |
Clinical data | |
Pregnancy category |
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Routes of administration | Intravenous, rectal |
Legal status | |
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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 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.[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
- RxList.com - Methohexital
- Drugs.com - Methohexital Sodium
- DrugLib.com - Brevital (Methohexital Sodium)
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- 2Fix
- Barbiturates
- General anesthetics
- Alkenes
- Alkynes