methohexital sodium

Trade name: brevital sodium

Small moleculeapproved

Approved

Jun 27, 1960

Methohexital is an ultrashort-acting barbiturate widely used in dentistry because of its rapid onset, predictable effects, and short duration of action. It was marked under the name brevital sodium for the intravenous anaesthesia. It has also been commonly used to induce deep sedation. Like other barbiturates, methohexital exerts its effects through the gamma-aminobutyric acid (GABA) receptor complex. By binding to its own receptor on the complex, methohexital augments the inhibitory effect of GABA on neurons and additionally can exert a similar effect independent of GABA. — NCATS

Clinical trial activity

10 trials · 12 clinical orgs · 5 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started May 1, 2008 (NCT01907217)

Timeline

1960s

Jun 27, 1960
Par Pharmaceuticals — Earliest FDA Approval
Jun 27, 1960
Par Pharmaceuticals — NDA Organization
Jun 27, 1960
Par Pharmaceuticals — NDA Secondary Org
Jun 27, 1960
Endo Pharmaceuticals — Marketing Organization
Jun 27, 1960
PH HEALTH — Marketing Organization

2010s

Jan 1, 2019
Earliest Phase 1 Sponsor(trial)

2020s

Oct 3, 2024
STERISCIENCE — Marketing Organization
Oct 3, 2024
ONESOURCE SPECIALTY — Marketing Organization

Indications

Approved for

Pain (approved 1960)

Studied for

Mechanism of action

GABA-A receptor; anion channelPOSITIVE ALLOSTERIC MODULATOR
GABA-A receptor; anion channel positive allosteric modulator
Barbiturate site

Approval history

approvedJun 27, 1960

Chemistry & pharmacology

Loading structure…

SMILES

C=CCC1(C(C)C#CCC)C(=O)NC(=O)N(C)C1=O

Mol. weight: 262.31 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Racemic Mixture
Inorganic: No
Polymer: No
Delivery: Parenteral
Availability: Prescription Only

Oral

Parenteral

Yes

Topical

Black box warning

Sources

Also known as

5-allyl-1-methyl-5-(1-methyl-2-pentynyl)-2,4,6(1h,3h,5h)-pyrimidinetrione
5-allyl-1-methyl-5-(1-methyl-2-pentynyl)-2,4,6(1h,3h,5h)-pyrimidinetrione
(+-)-5-allyl-1-methyl-5-(1-methyl-2-pentynyl)barbituric acid
(+-)-5-allyl-1-methyl-5-(1-methyl-2-pentynyl)barbituric acid
5-allyl-1-methyl-5-(1-methyl-pent-2-ynyl)-pyrimidine-2,4,6-trione
5-allyl-1-methyl-5-(1-methyl-pent-2-ynyl)-pyrimidine-2,4,6-trione
5-allyl-5-(3-hexyn-2-yl)-1-methylbarbituric acid
5-allyl-5-(3-hexyn-2-yl)-1-methylbarbituric acid
alpha-dl-1-methyl-5-allyl-5-(1'-methylpentyn-2-yl)barbituric acid
alpha-dl-1-methyl-5-allyl-5-(1'-methylpentyn-2-yl)barbituric acid
brevimytal
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enallynymall
enallynymal sodium
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methohexitone
metoesital
metohexital
metohexital

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT05655754	Phase 4	Nov 1, 2022	Medical University of Vienna
NCT04187196	Phase 4	Dec 31, 2019	Wake Forest University
NCT04022226	Early Phase 1 (Phase 1)	Oct 1, 2019	University of New Mexico
NCT02624050	N/A	Jul 1, 2016	Pennsylvania State University
NCT02752724	N/A	Mar 1, 2016	Department of Veteran Affairs
NCT01567852	N/A	Aug 1, 2011	University of New Mexico
NCT01367119	N/A	May 1, 2011	Mayo Clinic
NCT01881763	Phase 4	Jun 1, 2010	Brain & Behavior Research Foundation, Northwell Health, The Zucker Hillside Hospital
NCT01309581	N/A	Apr 1, 2010	Icahn School of Medicine at Mount Sinai
NCT01907217	Phase 4	May 1, 2008	Health Research Board, Ireland, Trinity College Dublin

Showing 10 of 10 trials

Page 1 / 1

Organizations

Research & Development (12)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
University of New Mexico	Academic/Hospital	2	2	2	2011
Brain & Behavior Research Foundation	Academic/Hospital	1	0	1	2010
Department of Veteran Affairs	Government	1	1	1	2016
Health Research Board, Ireland	Academic/Hospital	1	0	1	2008
Icahn School of Medicine at Mount Sinai	Academic/Hospital	1	1	1	2010
Mayo Clinic	Academic/Hospital	1	1	1	2011
Medical University of Vienna	Academic/Hospital	1	1	1	2022
Northwell Health	Academic/Hospital	1	1	1	2010
Pennsylvania State University	Academic/Hospital	1	1	1	2016
The Zucker Hillside Hospital	Academic/Hospital	1	0	1	2010
Trinity College Dublin	Academic/Hospital	1	1	1	2008
Wake Forest University	Academic/Hospital	1	1	1	2019

12 organizations

Page 1 / 1

Marketing (6)

Organization	Org type	Relationship	Date
Endo Pharmaceuticals	For profit	MKTG	Jun 27, 1960
ONESOURCE SPECIALTY	For profit	MKTG	Oct 3, 2024
PH HEALTH	For profit	MKTG	Jun 27, 1960
Par Pharmaceuticals	For profit	NDA	Jun 27, 1960
Par Pharmaceuticals	For profit	NDA2	Jun 27, 1960
STERISCIENCE	For profit	MKTG	Oct 3, 2024