Methohexital

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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 N05 CA15
PubChem	9034
DrugBank	APRD00058
Chemical data
Formula	C₁₄H₁₈N₂O₃
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	?
Routes	Intravenous, rectal

Methohexital (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.

[edit] Pharmacology

Methohexital binds to a distinct site which is associated with Cl⁻ ionophores at GABA_A receptors. 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 involved in the termination of the drug's biological activity.

Protein binding is approximately 73% for methohexital.

[edit] 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. It has been commonly used to induce deep sedation, "twilight sleep" or general anesthesia for oral surgery and dentistry.

[edit] External links

v • d • e

Barbiturates

Allobarbital, Amobarbital, Aprobarbital, Alphenal, Barbexaclone, Barbital, Butabarbital, Butalbital, Butobarbital, Butallylonal, Cyclobarbital, Cyclopal, Ethallobarbital, Hexethal, Heptabarbital, Hexobarbital, Mephobarbital, Metharbital, Methohexital, Methylphenobarbital, Pentobarbital, Probarbital, Proxibarbital, Propallylonal, Reposal, Secobarbital, Talbutal, Thialbarbital, Thiamylal, Thiobarbital, Thiobutabarbital Thiopental, Vinbarbital, Vinylbital

v • d • e General anesthetics (N01A)
Barbiturates	Hexobarbital, Methohexital, Narcobarbital, Thiopental
Ethers	Diethyl ether,Desflurane, Enflurane, Isoflurane, Methoxyflurane, Methoxypropane, Sevoflurane, Vinyl ether
Haloalkanes	Chloroform, Halothane, Trichloroethylene
Opioids	Alfentanil, Anileridine, Fentanyl, Phenoperidine, Remifentanil, Sufentanil
Others	Alfaxalone, Droperidol, Esketamine, Etomidate, Hydroxybutyric acid, Ketamine, Minaxolone, Nitrous oxide, Propanidid, Propofol, Xenon