Methohexital 3250677 209765851 2008-05-02T20:07:39Z 71.204.15.239 {{Drugbox| |IUPAC_name = 5-hex-3-yn-2-yl-1- methyl-5-prop-2-enyl-1, 3-diazinane-2,4,6-trione | image=methohexital2.png | width=100 | CAS_number=151-83-7 | ATC_prefix=N01 | ATC_suffix=AF01 | ATC_supplemental={{ATC|N05|CA15}} | PubChem=9034 | DrugBank=APRD00058 | C=14 | H=18 | N=2 | O=3 | molecular_weight = 262.304 | bioavailability= I.V. ~100%<br>Rectal ~17% | metabolism = [[Hepatic]] | elimination_half-life= 5.6 ± 2.7 minutes | excretion = ? | pregnancy_category = B ([[United States|USA]]) | legal_status = ? | routes_of_administration= Intravenous, rectal }} '''Methohexital''' (marketed under the brand name '''Brevital''') is a drug which is a [[barbiturate]] derivative.<sup>[''[[citation needed]]'']</sup> 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<sup>−</sup> [[ionophore]]s at GABA<sub>A</sub> receptors.<sup>[''[[citation needed]]'']</sup> This increases the length of time which the Cl<sup>−</sup> ionopores are open, thus causing an [[Inhibitory postsynaptic potential|inhibitory]] effect. Metabolism of methohexital is primarily hepatic (i.e., taking place in the liver) via demethylation and oxidation.<sup>[''[[citation needed]]'']</sup> 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.<sup>[''[[citation needed]]'']</sup> ==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.<sup>[''[[citation needed]]'']</sup> 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== * [http://www.rxlist.com/cgi/generic3/methohexital.htm RxList.com - Methohexital] * [http://www.drugs.com/pdr/methohexital_sodium.html Drugs.com - Methohexital Sodium] * [http://druglib.com/druginfo/brevital/ DrugLib.com - Brevital (Methohexital Sodium) ] {{Barbiturates}} {{General anesthetics}} {{Hypnotics and sedatives}} [[Category:Barbiturates]] [[Category:Anesthetics]] [[sv:Metohexital]]