WordNet

a silvery soft waxy metallic element of the alkali metal group; occurs abundantly in natural compounds (especially in salt water); burns with a yellow flame and reacts violently in water; occurs in sea water and in the mineral halite (rock salt) (同)Na, atomic number 11

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ソジウム,ナトリウム(金属元素;化学記号はNa)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/21 23:36:23」(JST)

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Methohexital or 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 GABA_A 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 involved in the termination 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 or general anesthesia for surgery and dental procedures. Unlike many other barbiturates, Methohexital actually lowers the seizure threshold, a property that make it particularly useful when anesthesia is provided for a electroconvulsive therapy (ECT). And rapid recovery rate with consciousness being gained within three to seven minutes after induction and full recovery within 30 minutes is a major advantage over other ECT barbiturates (Schulgasser and Borowitz 1963).

Synthesis

Methohexital, 5-allyl-1-methyl-5-(1-methyl-2-pentinyl barbituric acid, is synthesized in the classic manner of making barbituric acid derivatives, in particular by the reaction of malonic ester derivatives with derivatives of urea.

Methohexital synthesis: W.J. Doran, U.S. Patent 2,872,448 (1959).

The resulting allyl-(1-methyl-2-pentynyl) malonic ester is synthesized by subsequent alkylation of the malonic ester itself, beginning with 2-bromo-3-hexyne, which gives (1-methyl-2-pentynyl)malonic ester, and then by allylbromide. In the final step, reaction of the disubstituted malonic ester with N-methylurea gives desired methohexital.

References

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

^[1]

External links

RxList.com - Methohexital
Drugs.com - Methohexital Sodium
DrugLib.com - Brevital (Methohexital Sodium)

^ SCHULGASSER, H; BOROWITZ, A (1963). "Methohexital anaesthesia in electroconvulsive therapy". South African Medical Journal 37: 870.

UpToDate Contents

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English Journal

Effect of Atropine Dose on Heart Rate During Electroconvulsive Therapy.

Anastasian ZH1, Khan N, Heyer EJ, Berman MF, Ornstein E, Prudic J, Brady JE, Berman JA.Author information 1From the *Department of Anesthesiology, Columbia University, New York, NY; †Department of Anesthesiology, Beth Israel Deaconess Medical Center, Boston, MA; ‡Departments of Neurology, §Psychiatry and ∥Epidemiology, Columbia University, New York, NY.AbstractINTRODUCTION: Transient bradycardia during the stimulation phase of electroconvulsive therapy (ECT) is a well-known clinical observation. The optimal dose of atropine needed to prevent bradycardia has not been determined. This study was designed to investigate the effect of low doses of atropine on heart rate during ECT.
The journal of ECT.J ECT.2014 Apr 21. [Epub ahead of print]
INTRODUCTION: Transient bradycardia during the stimulation phase of electroconvulsive therapy (ECT) is a well-known clinical observation. The optimal dose of atropine needed to prevent bradycardia has not been determined. This study was designed to investigate the effect of low doses of atropine on
PMID 24755728

Post-Electroconvulsive Therapy Recovery and Reorientation Time With Methohexital and Ketamine: A Randomized, Longitudinal, Crossover Design Trial.

Yen T1, Khafaja M, Lam N, Crumbacher J, Schrader R, Rask J, Billstrand M, Rothfork J, Abbott CC.Author information 1From the *Departments of Anesthesiology and †Psychiatry, University of New Mexico School of Medicine, Albuquerque, NM; ‡University of New Mexico School of Medicine, Albuquerque, NM and §Clinical and Translational Science Center, University of New Mexico School of Medicine, Albuquerque, NM.AbstractOBJECTIVES: Methohexital, a barbiturate anesthetic commonly used for electroconvulsive therapy (ECT), possesses dose-dependent anticonvulsant properties, and its use can interfere with effective seizure therapy in patients with high seizure thresholds. Ketamine, an N-methyl-D-aspartate antagonist with epileptogenic properties not broadly used for ECT inductions, is a commonly used induction agent for general anesthesia. Recent studies suggest that the use of ketamine is effective in allowing successful ECT treatment in patients with high seizure thresholds without an increase in adverse effects. In this preliminary study, we directly compared the recovery and reorientation times of subjects receiving ketamine and methohexital for ECTs.
The journal of ECT.J ECT.2014 Apr 21. [Epub ahead of print]
OBJECTIVES: Methohexital, a barbiturate anesthetic commonly used for electroconvulsive therapy (ECT), possesses dose-dependent anticonvulsant properties, and its use can interfere with effective seizure therapy in patients with high seizure thresholds. Ketamine, an N-methyl-D-aspartate antagonist wi
PMID 24755722

Different regimens of intravenous sedatives or hypnotics for electroconvulsive therapy (ECT) in adult patients with depression.

Lihua P1, Su M, Ke W, Ziemann-Gimmel P.Author information 1Department of Anaesthesia and Pain Medicine, The First Affiliated Hospital, Chongqing Medical University, No 1 Youyi Road, Yuan-jia-gang, Yu-zhong District, Chongqing Municipality, China, 40016.AbstractBACKGROUND: Depression is a common mental disorder. It affects millions of people worldwide and is considered by the World Health Organization (WHO) to be one of the leading causes of disability. Electroconvulsive therapy (ECT) is a well-established treatment for severe depression. Intravenous anaesthetic medication is used to minimize subjective unpleasantness and adverse side effects of the induced tonic-clonic seizure. The influence of different anaesthetic medications on the successful reduction of depressive symptoms and adverse effects is unclear.
The Cochrane database of systematic reviews.Cochrane Database Syst Rev.2014 Apr 11;4:CD009763. [Epub ahead of print]
BACKGROUND: Depression is a common mental disorder. It affects millions of people worldwide and is considered by the World Health Organization (WHO) to be one of the leading causes of disability. Electroconvulsive therapy (ECT) is a well-established treatment for severe depression. Intravenous anaes
PMID 24723301

Japanese Journal

Sodium Methohexital (Brevital) as an Anesthetic in the Wada Test

BUCHTEL Henry A.,PASSARO Erasmo A.,SELWA Linda M.,DEVEIKIS John,GOMEZ-HASSAN Diana
Epilepsia : journal of the International League against Epilepsy 43(9), 1056-1061, 2002-09-01
NAID 10010878133

Preliminary observations on the effects of hydrocortisone and sodium methohexital on development of Sarcophaga (Curranea) tibialis Macquart (Diptera : Sarcophagidae), and implications for estimating post mortem interval

MUSVASVA E.
Forensic Science International 120, 37-41, 2001
NAID 30004308061

「メトヘキシタール」

Methohexital
Systematic (IUPAC) name
	5-hex-3-yn-2-yl-1- methyl-5-prop-2-enyl-1, 3-diazinane-2,4,6-trione
Clinical data
AHFS/Drugs.com	Consumer Drug Information
Pregnancy; category	B (USA);
Legal status	AU: S4 (Prescription only); Schedule IV;
Routes of; administration	Intravenous, rectal
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 N05CA15
PubChem	CID: 9034
IUPHAR/BPS	7233
DrugBank	DB00474
ChemSpider	8683
UNII	E5B8ND5IPE
KEGG	D04985
ChEBI	CHEBI:102216
ChEMBL	CHEMBL7413
Chemical data
Formula	C14H18N2O3
Molecular mass	262.304
	SMILES O=C1N(C(=O)NC(=O)C1(C\C=C)C(C#CCC)C)C ;
	InChI InChI=1S/C14H18N2O3/c1-5-7-8-10(3)14(9-6-2)11(17)15-13(19)16(4)12(14)18/h6,10H,2,5,9H2,1,3-4H3,(H,15,17,19) ; Key:NZXKDOXHBHYTKP-UHFFFAOYSA-N ;
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