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isoflurane 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
halogenated compounds used as general inhalation anaesthetics	1493	26675-46-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: isoflurane 1-Chloro-2,2,2-trifluoroethyl difluoromethyl ether forane forene isoforine isorrane	A stable, non-explosive inhalation anesthetic, relatively free from significant side effects. Molecular weight: 184.49 Formula: C3H2ClF5O CLOGP: 1.95 LIPINSKI: 0 HAC: 1 HDO: 0 TPSA: 9.23 ALOGS: -1.72 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

isoflurane
1-Chloro-2,2,2-trifluoroethyl difluoromethyl ether
forane
forene
isoforine
isorrane

A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.

Molecular weight: 184.49
Formula: C3H2ClF5O
CLOGP: 1.95
LIPINSKI: 0
HAC: 1
HDO: 0
TPSA: 9.23
ALOGS: -1.72
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Dec. 18, 1979	FDA	BAXTER HLTHCARE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Propofol infusion syndrome	127.94	55.58	23	2137	743	50602221
Intra-abdominal pressure increased	125.82	55.58	19	2141	200	50602764
Mitochondrial DNA mutation	123.30	55.58	19	2141	231	50602733
Pneumatosis	119.94	55.58	20	2140	411	50602553
Intestinal ischaemia	105.19	55.58	29	2131	6728	50596236
Necrosis ischaemic	101.25	55.58	19	2141	780	50602184
Apnoea	95.20	55.58	27	2133	6939	50596025
Gene mutation	92.45	55.58	19	2141	1252	50601712
Hyperthermia malignant	90.02	55.58	17	2143	722	50602242
Blood gases abnormal	86.08	55.58	16	2144	623	50602341
Delayed recovery from anaesthesia	83.54	55.58	16	2144	733	50602231
Systemic inflammatory response syndrome	80.09	55.58	22	2138	5027	50597937
Exposure during pregnancy	78.46	55.58	54	2106	120961	50482003
Post procedural complication	70.92	55.58	26	2134	15078	50587886
Metabolic acidosis	64.61	55.58	32	2128	38793	50564171
Perforation	61.90	55.58	13	2147	951	50602013
Ultrasound ovary abnormal	60.27	55.58	9	2151	87	50602877
Hypotension	59.66	55.58	61	2099	235408	50367556
Blood lactic acid increased	55.84	55.58	17	2143	5568	50597396

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyperthermia malignant	232.31	52.39	47	2027	1737	29570716
Apnoea	111.08	52.39	33	2041	6069	29566384
Post procedural complication	101.54	52.39	35	2039	10354	29562099
Hypotension	96.88	52.39	91	1983	194263	29378190
Intestinal ischaemia	91.26	52.39	29	2045	6663	29565790
Necrosis ischaemic	87.09	52.39	15	2059	223	29572230
Fear	81.28	52.39	29	2045	9475	29562978
Anhedonia	77.14	52.39	26	2048	7174	29565279
Superinfection	74.48	52.39	19	2055	1982	29570471
Injury	74.41	52.39	33	2041	19013	29553440
Renal injury	68.29	52.39	26	2048	10176	29562277
Mucosal ulceration	67.38	52.39	15	2059	873	29571580
Systemic inflammatory response syndrome	65.65	52.39	22	2052	5959	29566494
Emotional distress	60.51	52.39	26	2048	13869	29558584

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyperthermia malignant	301.51	42.19	61	4180	2398	64492093
Intestinal ischaemia	207.74	42.19	61	4180	11488	64483003
Necrosis ischaemic	179.22	42.19	34	4207	949	64493542
Hypotension	149.04	42.19	152	4089	380822	64113669
Systemic inflammatory response syndrome	140.83	42.19	44	4197	10191	64484300
Propofol infusion syndrome	122.69	42.19	27	4214	1590	64492901
Intra-abdominal pressure increased	115.29	42.19	19	4222	228	64494263
Mitochondrial DNA mutation	114.39	42.19	19	4222	240	64494251
Fear	111.62	42.19	44	4197	20127	64474364
Renal injury	108.17	42.19	40	4201	15389	64479102
Delayed recovery from anaesthesia	107.59	42.19	24	4217	1504	64492987
Anhedonia	105.25	42.19	38	4203	13668	64480823
Pneumatosis	98.52	42.19	20	4221	796	64493695
Blood lactic acid increased	95.73	42.19	33	4208	10368	64484123
Metabolic acidosis	95.72	42.19	59	4182	70899	64423592
Gene mutation	79.87	42.19	20	4221	2062	64492429
Injury	79.17	42.19	48	4193	55944	64438547
Emotional distress	75.58	42.19	40	4201	35998	64458493
Blood gases abnormal	72.28	42.19	16	4225	967	64493524
Unevaluable event	68.08	42.19	42	4199	50447	64444044
Respiratory acidosis	67.04	42.19	25	4216	9830	64484661
Superinfection	63.17	42.19	19	4222	3867	64490624
Anaesthetic complication	61.53	42.19	17	4224	2562	64491929
Mucosal ulceration	58.39	42.19	15	4226	1712	64492779
Procedural hypotension	57.08	42.19	15	4226	1871	64492620
Ultrasound ovary abnormal	56.38	42.19	9	4232	87	64494404
Procedural complication	55.21	42.19	20	4221	7245	64487246
Perforation	54.03	42.19	13	4228	1135	64493356
Left ventricular hypertrophy	53.48	42.19	21	4220	9485	64485006
Renal failure	52.34	42.19	62	4179	181626	64312865
Multiple organ dysfunction syndrome	51.64	42.19	47	4194	101366	64393125
Bradycardia	49.19	42.19	49	4192	118170	64376321
Exposure during pregnancy	47.58	42.19	40	4201	77635	64416856
Blood creatine phosphokinase increased	46.22	42.19	35	4206	58523	64435968
Myotonia	42.26	42.19	8	4233	220	64494271

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N01AB06	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Halogenated hydrocarbons
MeSH PA	D000777	Anesthetics
MeSH PA	D018685	Anesthetics, Inhalation
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
CHEBI has role	CHEBI:38870	inhalation anesthetics
FDA EPC	N0000175681	General Anesthetic
FDA PE	N0000175975	General Anesthesia

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
General anesthesia	indication	50697003
Hyperkalemia	contraindication	14140009
Low blood pressure	contraindication	45007003
Duchenne muscular dystrophy	contraindication	76670001	DOID:11723
Disease of liver	contraindication	235856003	DOID:409
Malignant hyperthermia	contraindication	405501007

🐶 Veterinary Drug Use

Species	Use	Relation
Dogs	Induction and maintenance of general anesthesia	Indication
Horses	Induction and maintenance of general anesthesia	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
IsoFlo	Zoetis Inc.	1
Isoflurane, USP	Dechra Veterinary Products LLC	1
ATTANE	Piramal Critical Care Inc.	1
Isoflurane, USP	Piramal Enterprises Ltd.	1

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
GABA-A receptor; anion channel	Ion channel	O00591 O14764 P14867 P18505 P18507 P28472 P31644 P34903 P47869 P47870 P48169 P78334 Q16445 Q8N1C3 Q99928 Q9UN88	GBRP_HUMAN GBRD_HUMAN GBRA1_HUMAN GBRB1_HUMAN GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN GBRA3_HUMAN GBRA2_HUMAN GBRB2_HUMAN GBRA4_HUMAN GBRE_HUMAN GBRA6_HUMAN GBRG1_HUMAN GBRG3_HUMAN GBRT_HUMAN	POSITIVE ALLOSTERIC MODULATOR			CHEMBL	CHEMBL
Potassium channel subfamily K member 2	Ion channel	O95069	KCNK2_HUMAN	OPENER			CHEMBL	CHEMBL
Potassium channel subfamily K member 3	Ion channel	O14649	KCNK3_HUMAN	OPENER			CHEMBL	CHEMBL
Potassium channel subfamily K member 9	Ion channel	Q9NPC2	KCNK9_HUMAN	OPENER			CHEMBL	CHEMBL
Potassium channel subfamily K member 10	Ion channel	P57789	KCNKA_HUMAN	OPENER			CHEMBL	CHEMBL
Potassium channel subfamily K member 18	Ion channel	Q7Z418	KCNKI_HUMAN	OPENER			CHEMBL	CHEMBL
Glycine receptor (alpha-1/beta)	Ion channel	P23415 P48167	GLRA1_HUMAN GLRB_HUMAN	POSITIVE MODULATOR			CHEMBL	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.11	PDSP

External reference:

ID	Source
4019107	VUID
N0000147364	NUI
D00545	KEGG_DRUG
4019107	VANDF
C0022180	UMLSCUI
CHEBI:6015	CHEBI
ICF	PDB_CHEM_ID
CHEMBL1256	ChEMBL_ID
DB00753	DRUGBANK_ID
D007530	MESH_DESCRIPTOR_UI
3763	PUBCHEM_CID
3286	INN_ID
2505	IUPHAR_LIGAND_ID
CYS9AKD70P	UNII
6026	RXNORM
284	MMSL
4326	MMSL
4926	MMSL
d00267	MMSL
001391	NDDF
387368002	SNOMEDCT_US
66492008	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
FORANE	HUMAN PRESCRIPTION DRUG LABEL	1	10019-360	INHALANT	1 mL	RESPIRATORY (INHALATION)	NDA	22 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	12164-012	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	22 sections
Terrell	HUMAN PRESCRIPTION DRUG LABEL	1	66794-011	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	13 sections
Terrell	HUMAN PRESCRIPTION DRUG LABEL	1	66794-011	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	13 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-017	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	21 sections
Terrell	HUMAN PRESCRIPTION DRUG LABEL	1	66794-019	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	21 sections
Terrell	HUMAN PRESCRIPTION DRUG LABEL	1	66794-019	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	21 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-020	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	13 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-020	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	13 sections