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]]