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

Stem definition	Drug id	CAS RN
	2302	2078-54-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: propofol ampofol diprivan disoprofol pofol	An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS. Molecular weight: 178.28 Formula: C12H18O CLOGP: 3.93 LIPINSKI: 0 HAC: 1 HDO: 1 TPSA: 20.23 ALOGS: -3.05 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

propofol
ampofol
diprivan
disoprofol
pofol

An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.

Molecular weight: 178.28
Formula: C12H18O
CLOGP: 3.93
LIPINSKI: 0
HAC: 1
HDO: 1
TPSA: 20.23
ALOGS: -3.05
ROTB: 2

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	4.70 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	36 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.20 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	14.02 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.16 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Oct. 2, 1989	FDA	FRESENIUS KABI USA

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
Anaphylactic shock	2837.85	15.90	910	39973	22723	63425416
Anaphylactic reaction	1182.70	15.90	655	40228	65445	63382694
Hypotension	964.59	15.90	1023	39860	271581	63176558
Cardiac arrest	853.47	15.90	602	40281	91943	63356196
Bronchospasm	773.89	15.90	322	40561	16958	63431181
Propofol infusion syndrome	753.90	15.90	165	40718	818	63447321
Serotonin syndrome	465.42	15.90	267	40616	28415	63419724
Tachycardia	418.73	15.90	445	40438	117711	63330428
Circulatory collapse	404.18	15.90	222	40661	21716	63426423
Bradycardia	401.88	15.90	351	40532	72876	63375263

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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
Anaphylactic shock	1921.37	15.95	708	38455	15233	34902535
Propofol infusion syndrome	1327.90	15.95	289	38874	677	34917091
Anaphylactic reaction	851.90	15.95	500	38663	31801	34885967
Hyperthermia malignant	684.29	15.95	200	38963	1977	34915791
Hypotension	598.49	15.95	964	38199	220685	34697083
Cardiac arrest	597.44	15.95	632	38531	95527	34822241
Bronchospasm	491.22	15.95	240	38923	10491	34907277
Bradycardia	484.65	15.95	505	38658	74913	34842855
Rhabdomyolysis	348.44	15.95	405	38758	67758	34850010
Delayed recovery from anaesthesia	344.26	15.95	94	39069	707	34917061

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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
Anaphylactic shock	4489.03	14.06	1566	73384	34430	79635008
Anaphylactic reaction	1955.99	14.06	1126	73824	82617	79586821
Propofol infusion syndrome	1907.35	14.06	429	74521	1554	79667884
Hypotension	1435.41	14.06	1907	73043	438410	79231028
Cardiac arrest	1337.64	14.06	1182	73768	170914	79498524
Bronchospasm	1187.24	14.06	542	74408	24317	79645121
Hyperthermia malignant	949.56	14.06	265	74685	2652	79666786
Bradycardia	815.03	14.06	808	74142	134749	79534689
Delayed recovery from anaesthesia	670.31	14.06	179	74771	1494	79667944
Serotonin syndrome	664.35	14.06	453	74497	44574	79624864

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N01AX10	NERVOUS SYSTEM ANESTHETICS ANESTHETICS, GENERAL Other general anesthetics
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:38877	intravenous anesthetics
CHEBI has role	CHEBI:48578	free radical scavengers
CHEBI has role	CHEBI:50919	antiemetico
FDA EPC	N0000175681	General Anesthetic
FDA PE	N0000175975	General Anesthesia
MeSH PA	D000777	Anesthetics
MeSH PA	D018686	Anesthetics, Intravenous

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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
Sedation in Intubated Patients	indication
Sedation as Adjunct to Anesthesia	indication
Apnea	contraindication	1023001
Asthenia	contraindication	13791008
Hypovolemia	contraindication	28560003
Low blood pressure	contraindication	45007003
Cerebral arteriosclerosis	contraindication	65312002
Decreased respiratory function	contraindication	80954004
Epilepsy	contraindication	84757009	DOID:1826

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🐶 Veterinary Drug Use

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Species	Use	Relation
Cats	Anesthesia	Indication
Cats	General anesthesia for short procedures	Indication
Cats	Induction and maintenance of general anesthesia	Indication
Cats	General anesthesia	Indication
Dogs	Anesthesia	Indication
Dogs	General anesthesia for short procedures	Indication
Dogs	Induction and maintenance of general anesthesia	Indication
Dogs	General anesthesia	Indication

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🐶 Veterinary products

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Product	Applicant	Ingredients
PropoClear	Zoetis Inc.	1
PropoFlo, PropoFlo 28	Zoetis Inc.	1
Rapanofal	iVaoes Animal Health	1

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.8	acidic

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 alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	5.70	CHEMBL	CHEMBL
GABA A receptor alpha-2/beta-2/gamma-2	Ion channel	P18507 P47869 P47870	GBRG2_HUMAN GBRA2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	4.95	CHEMBL	CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRG2_HUMAN GBRB3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	5.39	CHEMBL	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.46	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.22	DRUG MATRIX
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		IC50	4.01	WOMBAT-PK
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		IC50	4.71	WOMBAT-PK
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	4.91	WOMBAT-PK
Transient receptor potential cation channel subfamily V member 4	Ion channel	Q9HBA0	TRPV4_HUMAN	INHIBITOR	IC50	4.41	IUPHAR
Fatty-acid amide hydrolase 1	Enzyme	O00519	FAAH1_HUMAN		IC50	4.28	WOMBAT-PK

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External reference:

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ID	Source
PFL	PDB_CHEM_ID
003528	NDDF
14179	MMSL
196459	RXNORM
387423006	SNOMEDCT_US
4019500	VUID
4019500	VANDF
4943	PUBCHEM_CID
5073	INN_ID
5372	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fresenius Propoven 2%	HUMAN PRESCRIPTION DRUG LABEL	1	18124-027	EMULSION	20 mg	INTRAVENOUS	unapproved drug other	2 sections
Propofol	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0209	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	36 sections
Propofol	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0209	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	36 sections
Propofol	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0234	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	36 sections
Propofol	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0234	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	36 sections
Propofol	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0248	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	36 sections
Propofol	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0248	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	36 sections
PROPOFOL	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9943	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	14 sections
PROPOFOL	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4699	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	34 sections
PROPOFOL	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4699	INJECTION, EMULSION	10 mg	INTRAVENOUS	ANDA	34 sections

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