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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)

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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	166.34	59.77	26	2385	396	63486215
Propofol infusion syndrome	150.95	59.77	27	2384	956	63485655
Intra-abdominal pressure increased	125.59	59.77	19	2392	230	63486381
Pneumatosis	122.08	59.77	20	2391	415	63486196
Gene mutation	118.72	59.77	24	2387	1641	63484970
Blood gases abnormal	116.51	59.77	21	2390	776	63485835
Intestinal ischaemia	105.65	59.77	29	2382	7439	63479172
Necrosis ischaemic	102.06	59.77	19	2392	841	63485770
CSF oligoclonal band present	95.42	59.77	16	2395	384	63486227
Apnoea	94.53	59.77	27	2384	7995	63478616

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FDA Adverse Event Reporting System (Male)

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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	269.17	53.48	54	2161	2123	34952593
Apnoea	111.50	53.48	33	2182	6631	34948085
Hypotension	104.11	53.48	96	2119	221553	34733163
Intestinal ischaemia	102.20	53.48	32	2183	7762	34946954
Post procedural complication	101.85	53.48	35	2180	11353	34943363
Necrosis ischaemic	99.08	53.48	17	2198	275	34954441
Superinfection	86.64	53.48	22	2193	2497	34952219
Fear	81.38	53.48	29	2186	10447	34944269
Anhedonia	78.39	53.48	26	2189	7559	34947157
Mucosal ulceration	78.28	53.48	17	2198	978	34953738

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FDA Adverse Event Reporting System (Geriatric)

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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	340.45	48.16	68	4555	2849	79736916
Intestinal ischaemia	220.16	48.16	64	4559	13206	79726559
Necrosis ischaemic	192.63	48.16	36	4587	1054	79738711
Hypotension	157.47	48.16	158	4465	440159	79299606
Mitochondrial DNA mutation	154.61	48.16	26	4597	407	79739358
Systemic inflammatory response syndrome	154.05	48.16	47	4576	11418	79728347
Propofol infusion syndrome	142.73	48.16	31	4592	1952	79737813
Blood lactic acid increased	120.57	48.16	40	4583	12704	79727061
Intra-abdominal pressure increased	115.29	48.16	19	4604	261	79739504
Fear	113.30	48.16	44	4579	21942	79717823

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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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

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🐶 Veterinary Drug Use

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

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🐶 Veterinary products

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

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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:

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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

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External reference:

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ID	Source
ICF	PDB_CHEM_ID
001391	NDDF
2505	IUPHAR_LIGAND_ID
284	MMSL
3286	INN_ID
3763	PUBCHEM_CID
387368002	SNOMEDCT_US
4019107	VUID
4019107	VANDF
4326	MMSL

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Pharmaceutical products:

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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
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
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
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-017	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	21 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-020	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	14 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-020	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	14 sections
Isoflurane	HUMAN PRESCRIPTION DRUG LABEL	1	66794-020	LIQUID	1 mL	RESPIRATORY (INHALATION)	ANDA	14 sections

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