Scroll

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
Mitochondrial DNA mutation	153.36	61.26	24	2294	338	56289411
Propofol infusion syndrome	139.31	61.26	25	2293	830	56288919
Intra-abdominal pressure increased	126.49	61.26	19	2299	200	56289549
Pneumatosis	120.65	61.26	20	2298	411	56289338
Status epilepticus	115.00	61.26	37	2281	15104	56274645
Gene mutation	108.18	61.26	22	2296	1427	56288322
Intestinal ischaemia	105.38	61.26	29	2289	6926	56282823
Blood gases abnormal	103.67	61.26	19	2299	710	56289039
Necrosis ischaemic	101.46	61.26	19	2299	800	56288949
Apnoea	95.11	61.26	27	2291	7215	56282534
Hyperthermia malignant	90.35	61.26	17	2301	734	56289015
Delayed recovery from anaesthesia	83.92	61.26	16	2302	742	56289007
Systemic inflammatory response syndrome	79.90	61.26	22	2296	5256	56284493
Exposure during pregnancy	76.66	61.26	55	2263	136287	56153462
Metabolic acidosis	73.48	61.26	35	2283	40419	56249330
Post procedural complication	70.89	61.26	26	2292	15640	56274109
Blood lactic acid increased	68.00	61.26	20	2298	6044	56283705
Perforation	61.31	61.26	13	2305	1033	56288716

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	234.83	54.51	48	2099	1936	31693261
Apnoea	111.26	54.51	33	2114	6249	31688948
Post procedural complication	102.01	54.51	35	2112	10571	31684626
Hypotension	99.38	54.51	93	2054	204525	31490672
Intestinal ischaemia	90.78	54.51	29	2118	7016	31688181
Necrosis ischaemic	87.48	54.51	15	2132	225	31694972
Fear	80.89	54.51	29	2118	9945	31685252
Anhedonia	77.18	54.51	26	2121	7416	31687781
Injury	74.42	54.51	33	2114	19676	31675521
Superinfection	73.19	54.51	19	2128	2199	31692998
Renal injury	68.04	54.51	26	2121	10639	31684558
Mucosal ulceration	67.08	54.51	15	2132	923	31694274
Systemic inflammatory response syndrome	65.53	54.51	22	2125	6203	31688994
Emotional distress	60.56	54.51	26	2121	14330	31680867

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	305.31	44.99	62	4399	2599	70921384
Intestinal ischaemia	207.77	44.99	61	4400	12003	70911980
Necrosis ischaemic	180.01	44.99	34	4427	970	70923013
Hypotension	152.49	44.99	155	4306	404226	70519757
Mitochondrial DNA mutation	142.68	44.99	24	4437	345	70923638
Systemic inflammatory response syndrome	140.77	44.99	44	4417	10668	70913315
Propofol infusion syndrome	133.20	44.99	29	4432	1700	70922283
Intra-abdominal pressure increased	116.13	44.99	19	4442	228	70923755
Fear	112.17	44.99	44	4417	20767	70903216
Metabolic acidosis	108.53	44.99	64	4397	74282	70849701
Renal injury	108.25	44.99	40	4421	16054	70907929
Delayed recovery from anaesthesia	108.20	44.99	24	4437	1533	70922450
Blood lactic acid increased	106.55	44.99	36	4425	11137	70912846
Anhedonia	105.54	44.99	38	4423	14175	70909808
Pneumatosis	99.16	44.99	20	4441	806	70923177
Gene mutation	93.88	44.99	23	4438	2268	70921715
Blood gases abnormal	87.91	44.99	19	4442	1075	70922908
Emotional distress	76.07	44.99	40	4421	37148	70886835
Status epilepticus	75.94	44.99	35	4426	24491	70899492
Respiratory acidosis	74.48	44.99	27	4434	10254	70913729
Injury	74.37	44.99	48	4413	65197	70858786
Unevaluable event	68.61	44.99	42	4419	52021	70871962
Anaesthetic complication	66.58	44.99	18	4443	2618	70921365
Superinfection	62.51	44.99	19	4442	4187	70919796
Mucosal ulceration	58.43	44.99	15	4446	1786	70922197
Procedural hypotension	57.12	44.99	15	4446	1951	70922032
Ultrasound ovary abnormal	56.78	44.99	9	4452	87	70923896
Procedural complication	55.42	44.99	20	4441	7494	70916489
Perforation	53.35	44.99	13	4448	1252	70922731
Blood creatine phosphokinase increased	52.96	44.99	38	4423	61225	70862758
Left ventricular hypertrophy	52.94	44.99	21	4440	10181	70913802
Bradycardia	52.57	44.99	51	4410	124564	70799419
Renal failure	52.56	44.99	62	4399	189008	70734975
Multiple organ dysfunction syndrome	50.70	44.99	47	4414	108468	70815515
Shock	49.16	44.99	31	4430	40394	70883589
Exposure during pregnancy	46.90	44.99	41	4420	87676	70836307
CSF oligoclonal band present	46.69	44.99	9	4452	286	70923697

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	23 sections
FORANE	HUMAN PRESCRIPTION DRUG LABEL	1	10019-360	INHALANT	1 mL	RESPIRATORY (INHALATION)	NDA	23 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
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
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
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-020	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	13 sections