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

Stem definition	Drug id	CAS RN
	4616	83387-25-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: relistor methylnaltrexone methylnaltrexonium methylnaltrexone bromide	a selective antagonist of opioid binding at the mu-opioid receptor with restricted ability to cross the blood-brain barrier, function as a peripherally-acting mu‑opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system Molecular weight: 356.44 Formula: C21H26NO4 CLOGP: -2.64 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 66.76 ALOGS: -4.73 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

relistor
methylnaltrexone
methylnaltrexonium
methylnaltrexone bromide

a selective antagonist of opioid binding at the mu-opioid receptor with restricted ability to cross the blood-brain barrier, function as a peripherally-acting mu‑opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system

Molecular weight: 356.44
Formula: C21H26NO4
CLOGP: -2.64
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 66.76
ALOGS: -4.73
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
6	mg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	52.75 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	22 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	2.60 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.50 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.87 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.34 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
April 24, 2008	FDA	SALIX PHARMS
July 2, 2008	EMA

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
Abdominal pain	72.93	29.20	43	652	293413	63194914
Death	34.31	29.20	30	665	374351	63113976

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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
Death	45.05	32.92	38	405	398011	34558477
Pneumatosis intestinalis	43.20	32.92	10	433	3913	34952575

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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
Death	78.89	30.80	58	824	566456	79177050
Abdominal pain	51.92	30.80	39	843	389530	79353976
Pneumatosis intestinalis	44.65	30.80	11	871	6386	79737120

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A06AH01	ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Peripheral opioid receptor antagonists
FDA CS	M0474216	Quaternary Ammonium Compounds
FDA EPC	N0000175691	Opioid Antagonist
FDA MoA	N0000000154	Opioid Antagonists
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D009292	Narcotic Antagonists
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory 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
Therapeutic opioid induced constipation	indication	136801000119102
Gastrointestinal ulcer	contraindication	40845000
Gastrointestinal perforation	contraindication	51875005
Acute nephropathy	contraindication	58574008
Gastrointestinal obstruction	contraindication	126765001
Chronic diarrhea	contraindication	236071009
Primary malignant neoplasm of gastrointestinal tract	contraindication	363745004
Macrocolon	contraindication	367495003
Severe diarrhea	contraindication	409587002

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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	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
12MG/0.6ML (12MG/0.6ML)	RELISTOR	SALIX PHARMS	N021964	April 24, 2008	RX	SOLUTION	SUBCUTANEOUS	10376584	April 8, 2024	TREATMENT OF OPIOID-INDUCED CONSTIPATION
12MG/0.6ML (12MG/0.6ML)	RELISTOR	SALIX PHARMS	N021964	Sept. 27, 2010	RX	SOLUTION	SUBCUTANEOUS	8420663	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
12MG/0.6ML (12MG/0.6ML)	RELISTOR	SALIX PHARMS	N021964	Sept. 27, 2010	RX	SOLUTION	SUBCUTANEOUS	8822490	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
12MG/0.6ML (12MG/0.6ML)	RELISTOR	SALIX PHARMS	N021964	April 24, 2008	RX	SOLUTION	SUBCUTANEOUS	9180125	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
12MG/0.6ML (12MG/0.6ML)	RELISTOR	SALIX PHARMS	N021964	Sept. 27, 2010	RX	SOLUTION	SUBCUTANEOUS	9492445	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
12MG/0.6ML (12MG/0.6ML)	RELISTOR	SALIX PHARMS	N021964	Sept. 27, 2010	RX	SOLUTION	SUBCUTANEOUS	8247425	Dec. 31, 2030	TREATMENT OF OPIOID-INDUCED CONSTIPATION
150MG	RELISTOR	SALIX	N208271	July 19, 2016	RX	TABLET	ORAL	8420663	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
150MG	RELISTOR	SALIX	N208271	July 19, 2016	RX	TABLET	ORAL	9180125	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
150MG	RELISTOR	SALIX	N208271	July 19, 2016	RX	TABLET	ORAL	9492445	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION
150MG	RELISTOR	SALIX	N208271	July 19, 2016	RX	TABLET	ORAL	9724343	Sept. 30, 2029	TREATMENT OF OPIOID-INDUCED CONSTIPATION

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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	ANTAGONIST	Ki	7.55	WOMBAT-PK	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	6.65	WOMBAT-PK
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		Ki	5.10	WOMBAT-PK
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		Ki	6.05	CHEMBL
Kappa-type opioid receptor	GPCR		OPRK_CAVPO		Ki	7.70	CHEMBL

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External reference:

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ID	Source
012677	NDDF
012678	NDDF
0RK7M7IABE	UNII
136491	MMSL
25289	MMSL
29899	RXNORM
4027431	VANDF
4027432	VANDF
429838001	SNOMEDCT_US
431072004	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Relistor	HUMAN PRESCRIPTION DRUG LABEL	1	65649-150	TABLET	150 mg	ORAL	NDA	28 sections
Relistor	HUMAN PRESCRIPTION DRUG LABEL	1	65649-551	INJECTION, SOLUTION	12 mg	SUBCUTANEOUS	NDA	28 sections
Relistor	HUMAN PRESCRIPTION DRUG LABEL	1	65649-552	INJECTION, SOLUTION	8 mg	SUBCUTANEOUS	NDA	28 sections

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