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

Stem definition	Drug id	CAS RN
	844	469-62-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: dextropropoxyphene propoxyphene hydrochloride dextropropoxyphen propoxyphene d-Propoxyphene propoxyphene napsylate propoxyphene HCl destropropoxifene	A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect. Molecular weight: 339.48 Formula: C22H29NO2 CLOGP: 5.21 LIPINSKI: 1 HAC: 3 HDO: 0 TPSA: 29.54 ALOGS: -4.91 ROTB: 9 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

dextropropoxyphene
propoxyphene hydrochloride
dextropropoxyphen
propoxyphene
d-Propoxyphene
propoxyphene napsylate
propoxyphene HCl
destropropoxifene

A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.

Molecular weight: 339.48
Formula: C22H29NO2
CLOGP: 5.21
LIPINSKI: 1
HAC: 3
HDO: 0
TPSA: 29.54
ALOGS: -4.91
ROTB: 9

Status: OFM

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

Drug dosage:

Dose	Unit	Route
0.20	g	O
0.30	g	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	19.15 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	18 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	15 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	12 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.24 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.02 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 16, 1957	FDA

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
Drug hypersensitivity	721.70	44.41	236	731	310451	63177604
Toxicity to various agents	111.54	44.41	60	907	247190	63240865
Completed suicide	61.55	44.41	34	933	145639	63342416

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FDA Adverse Event Reporting System (Male)

None

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
Drug hypersensitivity	578.47	46.13	196	927	298720	79444545
Toxicity to various agents	169.48	46.13	92	1031	421448	79321817
Completed suicide	57.05	46.13	38	1085	245729	79497536

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02AC04	NERVOUS SYSTEM ANALGESICS OPIOIDS Diphenylpropylamine derivatives
ATC	N02AC54	NERVOUS SYSTEM ANALGESICS OPIOIDS Diphenylpropylamine derivatives
ATC	N02AC74	NERVOUS SYSTEM ANALGESICS OPIOIDS Diphenylpropylamine derivatives
CHEBI has role	CHEBI:35482	narcotic analgesic
CHEBI has role	CHEBI:55322	mu-opioid agonists
FDA EPC	N0000175690	Opioid Agonist
FDA MoA	N0000175684	Full Opioid Agonists
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid
MeSH PA	D002491	Central Nervous System Agents

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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
Pain	indication	22253000
Necrotizing enterocolitis in fetus OR newborn	contraindication	2707005
Suicidal thoughts	contraindication	6471006
Alcoholism	contraindication	7200002
Peptic ulcer	contraindication	13200003	DOID:750
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Alcohol intoxication	contraindication	25702006
Shock	contraindication	27942005
Hypovolemia	contraindication	28560003
Orthostatic hypotension	contraindication	28651003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.26	Basic

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
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST			WOMBAT-PK	CHEMBL
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN				WOMBAT-PK
Glutamate receptor ionotropic, NMDA 3A	Ion channel	Q8TCU5	NMD3A_HUMAN		IC50	5.30	WOMBAT-PK

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External reference:

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ID	Source
001574	NDDF
001575	NDDF
001576	NDDF
10100	PUBCHEM_CID
117005003	SNOMEDCT_US
1639-60-7	SECONDARY_CAS_RN
2224	MMSL
26570-10-5	SECONDARY_CAS_RN
387042001	SNOMEDCT_US
4017511	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Darvon-N	HUMAN PRESCRIPTION DRUG LABEL	1	16590-874	TABLET, FILM COATED	100 mg	ORAL	NDA	14 sections
Propoxyphene	HUMAN PRESCRIPTION DRUG LABEL	1	16590-198	CAPSULE	65 mg	ORAL	ANDA	13 sections
Propoxyphene and Acetaminophen	HUMAN PRESCRIPTION DRUG LABEL	2	63874-201	TABLET, FILM COATED	100 mg	ORAL	ANDA	29 sections
Propoxyphene and Acetaminophen	HUMAN PRESCRIPTION DRUG LABEL	2	68387-100	TABLET, FILM COATED	100 mg	ORAL	ANDA	29 sections
PROPOXYPHENE NAPSYLATE AND ACETAMINOPHEN	HUMAN PRESCRIPTION DRUG LABEL	2	12634-537	TABLET, FILM COATED	100 mg	ORAL	ANDA	16 sections
Propoxyphene Napsylate and Acetaminophen	HUMAN PRESCRIPTION DRUG LABEL	2	21695-280	TABLET, FILM COATED	100 mg	ORAL	ANDA	23 sections
PROPOXYPHENE NAPSYLATE AND ACETAMINOPHEN	HUMAN PRESCRIPTION DRUG LABEL	2	67296-0104	TABLET	100 mg	ORAL	ANDA	19 sections
PROPOXYPHENE NAPSYLATE AND ACETAMINOPHEN	HUMAN PRESCRIPTION DRUG LABEL	2	67296-0105	TABLET	100 mg	ORAL	ANDA	19 sections
Propoxyphene Napsylate and Acetaminophen	HUMAN PRESCRIPTION DRUG LABEL	2	67296-0378	TABLET, FILM COATED	100 mg	ORAL	ANDA	23 sections

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