Halothane

N01A - Anesthetics, general ATC N01AB01 Small molecule approved 1958 Topical

JFDA label: Anestane

Mechanism of Action

Positive Modulator of Glycine receptor (alpha-1/beta) — Glycine receptor (alpha-1/beta) positive modulator; Positive Allosteric Modulator of GABA-A receptor; anion channel — GABA-A receptor; anion channel positive allosteric modulator; Opener of Potassium channel subfamily K member 10 — Potassium channel subfamily K member 10 opener; Opener of Potassium channel subfamily K member 18 — Potassium channel subfamily K member 18 opener; Opener of Potassium channel subfamily K member 3 — Potassium channel subfamily K member 3 opener; Opener of Potassium channel subfamily K member 9 — Potassium channel subfamily K member 9 opener; Opener of Potassium channel subfamily K member 2 — Potassium channel subfamily K member 2 opener

Target	Action	Gene / class
GABA-A receptor; anion channel efficacy	POSITIVE ALLOSTERIC MODULATOR
Glycine receptor (alpha-1/beta) efficacy	POSITIVE MODULATOR
Potassium channel subfamily K member 10 efficacy	OPENER	KCNK10
Potassium channel subfamily K member 18 efficacy	OPENER	KCNK18
Potassium channel subfamily K member 2 efficacy	OPENER	KCNK2
Potassium channel subfamily K member 3 efficacy	OPENER	KCNK3
Potassium channel subfamily K member 9 efficacy	OPENER	KCNK9

Pregnancy & Lactation

Lactation

Caution Hale L3

Halothane is no longer available in the United States.

Chemistry & Properties

Formula	C2HBrClF3
Molecular weight	197.38 g/mol
IUPAC name	2-bromo-2-chloro-1,1,1-trifluoroethane
CAS	151-67-7
PubChem CID	3562
InChIKey	`BCQZXOMGPXTTIC-UHFFFAOYSA-N`
logP	2.51 (XLogP 2.3)
Polar surface area	0.0 Å²
H-bond acceptors / donors	0 / 0
Drug-likeness (QED)	0.52
Lipinski violations	0

SMILES

FC(F)(F)C(Cl)Br

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes (logBB 0.3)

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Inhibitor	—
CYP1A2	Substrate	—
CYP2B6	Inhibitor	—
CYP2B6	Substrate	—
CYP2C19	Inhibitor	—
CYP2C19	Substrate	—
CYP2C8	Inhibitor	—
CYP2C9	Inhibitor	—
CYP2C9	Substrate	—
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Aminophylline	major
Anagrelide	major
Arsenic trioxide	major
Cabozantinib	major
Ceritinib	major
Chloroquine	major
Cisapride	major
Crizotinib	major
Dolasetron	major
Dyphylline	major
Epinephrine	major
Fingolimod	major
Halofantrine	major
Hydroxychloroquine	major
Ivosidenib	major
Lumefantrine	major
Macimorelin	major
Nilotinib	major
Osimertinib	major
Oxtriphylline	major
Ozanimod	major
Panobinostat	major
Papaverine	major
Pasireotide	major
Phenylephrine	major
Phenylephrine (nasal)	major
Phenylephrine (ophthalmic)	major
Ribociclib	major
Siponimod	major
Theophylline	major
Toremifene	major
Vandetanib	major
Vemurafenib	major
Abarelix	moderate
Abiraterone	moderate
Alimemazine	moderate
Alpelisib	moderate
Apalutamide	moderate
Astemizole	moderate
Bicalutamide	moderate

Showing 40 of 100+.

Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Anestane	Solution 100 %	250 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	—