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

Stem definition	Drug id	CAS RN
	1728	76-99-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: metadone methadone methadone hydrochloride methadone HCl	A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3) Molecular weight: 309.45 Formula: C21H27NO CLOGP: 4.17 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 20.31 ALOGS: -4.72 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

metadone
methadone
methadone hydrochloride
methadone HCl

A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)

Molecular weight: 309.45
Formula: C21H27NO
CLOGP: 4.17
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 20.31
ALOGS: -4.72
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
25	mg	O
25	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	92 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	4.40 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	31 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	24 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	120 mg/mL	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	1.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.62 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.21 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 13, 1947	FDA	ROXANE

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	2783.06	13.01	1106	29093	71412	63387411
Toxicity to various agents	1962.32	13.01	1299	28900	245951	63212872
Exposure during pregnancy	667.78	13.01	568	29631	154979	63303844
Completed suicide	635.55	13.01	537	29662	145136	63313687
Death	522.19	13.01	757	29442	373624	63085199
Cardio-respiratory arrest	503.12	13.01	328	29871	59631	63399192
Respiratory arrest	469.53	13.01	253	29946	32392	63426431
Respiratory depression	437.52	13.01	184	30015	13531	63445292
Cardiac arrest	370.07	13.01	325	29874	92220	63366603
Premature delivery	335.88	13.01	198	30001	30083	63428740

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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	4608.03	13.99	2225	37053	96871	34820782
Toxicity to various agents	3376.48	13.99	2321	36957	198041	34719612
Respiratory depression	1006.42	13.99	448	38830	15797	34901856
Intentional product misuse	640.67	13.99	477	38801	45134	34872519
Respiratory arrest	566.96	13.99	367	38911	27676	34889977
Drug dependence	562.33	13.99	346	38932	23871	34893782
Overdose	522.81	13.99	575	38703	90484	34827169
Coma	518.05	13.99	421	38857	45257	34872396
Poisoning	498.53	13.99	253	39025	11973	34905680
Miosis	447.08	13.99	217	39061	9318	34908335

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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	7627.01	12.53	3276	58074	159415	79523623
Toxicity to various agents	5200.31	12.53	3486	57864	418054	79264984
Respiratory depression	1488.72	12.53	618	60732	27012	79656026
Respiratory arrest	1327.58	12.53	717	60633	56833	79626205
Completed suicide	1131.95	12.53	1155	60195	244612	79438426
Death	1039.53	12.53	1683	59667	564831	79118207
Cardio-respiratory arrest	1014.74	12.53	764	60586	107746	79575292
Overdose	989.29	12.53	942	60408	183264	79499774
Cardiac arrest	927.61	12.53	882	60468	171214	79511824
Intentional product misuse	925.21	12.53	686	60664	94479	79588559

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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
Drug withdrawal syndrome neonatal	1033.48	86.42	509	839	1610	86834
Foetal exposure during pregnancy	144.46	86.42	440	908	12401	76043

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Pharmacologic Action:

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Source	Code	Description
ATC	N02AC52	NERVOUS SYSTEM ANALGESICS OPIOIDS Diphenylpropylamine derivatives
ATC	N07BC02	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:35703	Xenobiotic
CHEBI has role	CHEBI:50949	SSRI
CHEBI has role	CHEBI:55322	mu-opioid agonists
CHEBI has role	CHEBI:60643	N-methyl-D-aspartate receptor antagonists
CHEBI has role	CHEBI:78298	environmental contaminants
FDA EPC	N0000175690	Opioid Agonist
FDA MoA	N0000175684	Full Opioid Agonists

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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
Severe pain	indication	76948002
Opioid withdrawal	indication	87132004
Chronic disease of respiratory system	contraindication	17097001
Mood swings	contraindication	18963009
Inflammatory bowel disease	contraindication	24526004	DOID:0050589
Hypercapnia	contraindication	29596007
Torsades de pointes	contraindication	31722008
Disorder of gallbladder	contraindication	39621005	DOID:0060262
Hypothyroidism	contraindication	40930008	DOID:1459
Conduction disorder of the heart	contraindication	44808001

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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	8.55	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	Ki	8.78	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.01	CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	5.68	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	4.58	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		IC50	6.29	CHEMBL
Glutamate receptor ionotropic, NMDA 3A	Ion channel	Q8TCU5	NMD3A_HUMAN				WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-10	Ion channel	Q9GZZ6	ACH10_HUMAN				WOMBAT-PK
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		IC50	5.96	CHEMBL
Opioid receptor	GPCR		OPRD_RAT OPRM_RAT OPRK_RAT SGMR1_RAT		IC50	7.29	CHEMBL

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External reference:

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ID	Source
001566	NDDF
004628	NDDF
1095-90-5	SECONDARY_CAS_RN
1981	MMSL
218337	RXNORM
23883005	SNOMEDCT_US
387286002	SNOMEDCT_US
4017431	VANDF
4019820	VUID
4019820	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
DISKETS	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4538	TABLET	40 mg	ORAL	NDA	31 sections
DOLOPHINE	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4218	TABLET	5 mg	ORAL	NDA	32 sections
DOLOPHINE	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4219	TABLET	10 mg	ORAL	NDA	32 sections
Methadone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0391	CONCENTRATE	10 mg	ORAL	ANDA	39 sections
Methadone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0391	CONCENTRATE	10 mg	ORAL	ANDA	39 sections
Methadone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0392	CONCENTRATE	10 mg	ORAL	ANDA	39 sections
Methadone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0392	CONCENTRATE	10 mg	ORAL	ANDA	39 sections
METHADONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0709	TABLET	5 mg	ORAL	ANDA	32 sections
METHADONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0709	TABLET	5 mg	ORAL	ANDA	32 sections
METHADONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0710	TABLET	10 mg	ORAL	ANDA	32 sections

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