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

Stem definition	Drug id	CAS RN
opioid receptor antagonists/agonists, morphinan derivates	4412	561-27-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: diamorphine hydrochloride diacetylmorphine hydrochloride heroin diamorphine acetomorphin acetomorphine diacetylmorphine diamorphine HCl diacetylmorphine HCl	A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed) Molecular weight: 369.42 Formula: C21H23NO5 CLOGP: 1.57 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 65.07 ALOGS: -3.14 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

diamorphine hydrochloride
diacetylmorphine hydrochloride
heroin
diamorphine
acetomorphin
acetomorphine
diacetylmorphine
diamorphine HCl
diacetylmorphine HCl

A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed)

Molecular weight: 369.42
Formula: C21H23NO5
CLOGP: 1.57
LIPINSKI: 0
HAC: 6
HDO: 0
TPSA: 65.07
ALOGS: -3.14
ROTB: 4

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
CL (Clearance)	212.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.31 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	1 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	0.06 hours	Lombardo F, Berellini G, Obach RS

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Approvals:

None

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 abuse	3879.52	83.59	875	2930	71643	63413574
Toxicity to various agents	1046.21	83.59	427	3378	246823	63238394
Cardio-respiratory arrest	604.47	83.59	198	3607	59761	63425456
Respiratory arrest	449.47	83.59	137	3668	32508	63452709
Cardiac arrest	336.36	83.59	145	3660	92400	63392817
Completed suicide	285.09	83.59	149	3656	145524	63339693
Death	185.32	83.59	163	3642	374218	63110999
Overdose	170.08	83.59	98	3707	114980	63370237
Drug dependence	157.16	83.59	58	3747	24425	63460792
Myocardial stunning	131.36	83.59	20	3785	153	63485064

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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
Drug abuse	8020.53	59.87	2243	7126	96853	34850709
Toxicity to various agents	2273.84	59.87	1080	8289	199282	34748280
Drug dependence	535.85	59.87	212	9157	24005	34923557
Respiratory arrest	475.70	59.87	203	9166	27840	34919722
Cardio-respiratory arrest	471.42	59.87	249	9120	55024	34892538
Overdose	428.67	59.87	279	9090	90780	34856782
Intentional product misuse	392.93	59.87	207	9162	45404	34902158
Substance abuse	283.62	59.87	98	9271	7543	34940019
Asphyxia	274.51	59.87	93	9276	6742	34940820
Cardiac arrest	226.94	59.87	195	9174	95964	34851598

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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
Drug abuse	11824.89	60.20	2993	8986	159698	79572711
Toxicity to various agents	3256.94	60.20	1456	10523	420084	79312325
Cardio-respiratory arrest	1017.33	60.20	435	11544	108075	79624334
Respiratory arrest	884.89	60.20	330	11649	57220	79675189
Cardiac arrest	529.90	60.20	326	11653	171770	79560639
Intentional product misuse	525.69	60.20	265	11714	94900	79637509
Drug dependence	490.95	60.20	196	11783	40573	79691836
Overdose	438.61	60.20	297	11682	183909	79548500
Asphyxia	347.09	60.20	110	11869	11610	79720799
Death	316.26	60.20	405	11574	566109	79166300

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FDA Adverse Event Reporting System (Pediatric)

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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
Sudden infant death syndrome	24.74	19.18	4	3	52	89733

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Pharmacologic Action:

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Source	Code	Description
ATC	N07BC06	NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS DRUGS USED IN ADDICTIVE DISORDERS Drugs used in opioid dependence
CHEBI has role	CHEBI:35482	narcotic analgesic
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:38867	anaesthetic
CHEBI has role	CHEBI:55322	mu-opioid agonists
CHEBI has role	CHEBI:76924	plant metabolites
CHEBI has role	CHEBI:78298	environmental contaminants
CHEBI has role	CHEBI:88188	allergenic drug
CHEBI has role	CHEBI:176497	geroprotectors

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

Disease	Relation	SNOMED_ID	DOID
Severe pain	indication	76948002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.18	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	UniProt	Type	Activity value (-log[M])	Bioact source
D(2) dopamine receptor	GPCR	DRD2_RAT	Ki	7.96	CHEMBL
D(1A) dopamine receptor	GPCR	DRD1_RAT	Ki	6.62	CHEMBL
D(3) dopamine receptor	GPCR	DRD3_RAT	Ki	7.44	CHEMBL

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External reference:

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ID	Source
MOI	PDB_CHEM_ID
001545	NDDF
003843	NDDF
003844	NDDF
3304	RXNORM
373529000	SNOMEDCT_US
387341002	SNOMEDCT_US
396019002	SNOMEDCT_US
4017530	VANDF
5288826	PUBCHEM_CID

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Pharmaceutical products:

None