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methylnaltrexone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4616 | 83387-25-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 6 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 52.75 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.34 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 2.60 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 22 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.87 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.50 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 0 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIM2,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 29 | |||
| kinase-selectivity-class | EIF2AK3,MAP2K6 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 2, 2008 | EMA | ||
| April 24, 2008 | FDA | SALIX PHARMS |
FDA Adverse Event Reporting System (Female)
| 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 | 71.10 | 30.27 | 43 | 725 | 395678 | 90232001 |
| Death | 40.00 | 30.27 | 32 | 736 | 456519 | 90171160 |
FDA Adverse Event Reporting System (Male)
| 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 | 50.07 | 30.86 | 41 | 432 | 471144 | 42149718 |
| Pneumatosis intestinalis | 42.61 | 30.86 | 10 | 463 | 4742 | 42616120 |
| Therapeutic product effect prolonged | 31.31 | 30.86 | 5 | 468 | 313 | 42620549 |
| Large intestine perforation | 31.18 | 30.86 | 9 | 464 | 9527 | 42611335 |
FDA Adverse Event Reporting System (Geriatric)
| 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 | 91.49 | 29.02 | 64 | 948 | 698805 | 109889482 |
| Abdominal pain | 55.43 | 29.02 | 42 | 970 | 512947 | 110075340 |
| Pneumatosis intestinalis | 43.57 | 29.02 | 11 | 1001 | 8518 | 110579769 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| 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 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 |
| FDA EPC | N0000175691 | Opioid Antagonist |
| CHEBI has role | CHEBI:50503 | laxative |
| CHEBI has role | CHEBI:55324 | gastrointestinal drug |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
A06AH Peripheral opioid receptor antagonists 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
🐶 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)
| 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 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 12303592 | Aug. 3, 2027 | TREATMENT OF OIC IN ADULTS WITH ADVANCED ILLNESS OR PAIN CAUSED BY ACTIVE CANCER WHO REQUIRE OPIOID DOSAGE ESCALATION FOR PALLIATIVE CARE |
| 12MG/0.6ML (12MG/0.6ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 12303592 | Aug. 3, 2027 | TREATMENT OF OPIOID-INDUCED CONSTIPATION (OIC) IN ADULTS WITH CHRONIC NON-CANCER PAIN, INCLUDING PATIENTS WITH CHRONIC PAIN RELATED TO PRIOR CANCER OR ITS TREATMENT WHO DO NOT REQUIRE FREQUENT (E.G., WEEKLY) OPIOID DOSAGE ESCALATION |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 12303592 | Aug. 3, 2027 | TREATMENT OF OIC IN ADULTS WITH ADVANCED ILLNESS OR PAIN CAUSED BY ACTIVE CANCER WHO REQUIRE OPIOID DOSAGE ESCALATION FOR PALLIATIVE CARE |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 12303592 | Aug. 3, 2027 | TREATMENT OF OPIOID-INDUCED CONSTIPATION (OIC) IN ADULTS WITH CHRONIC NON-CANCER PAIN, INCLUDING PATIENTS WITH CHRONIC PAIN RELATED TO PRIOR CANCER OR ITS TREATMENT WHO DO NOT REQUIRE FREQUENT (E.G., WEEKLY) OPIOID DOSAGE ESCALATION |
| 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 | April 24, 2008 | 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 | April 24, 2008 | RX | SOLUTION | SUBCUTANEOUS | 9492445 | Sept. 30, 2029 | TREATMENT OF OPIOID-INDUCED CONSTIPATION |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 8420663 | Sept. 30, 2029 | TREATMENT OF OPIOID-INDUCED CONSTIPATION |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 8822490 | Sept. 30, 2029 | TREATMENT OF OPIOID-INDUCED CONSTIPATION |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 9180125 | Sept. 30, 2029 | TREATMENT OF OPIOID-INDUCED CONSTIPATION |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 9492445 | Sept. 30, 2029 | 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 |
| 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 |
| 8MG/0.4ML (8MG/0.4ML) | RELISTOR | SALIX PHARMS | N021964 | Sept. 27, 2010 | RX | SOLUTION | SUBCUTANEOUS | 8247425 | Dec. 31, 2030 | TREATMENT OF OPIOID-INDUCED CONSTIPATION |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | ANTAGONIST | Ki | 7.55 | WOMBAT-PK | CHEMBL | |||
| Cytochrome P450 2D6 | Enzyme | Ki | 5.10 | WOMBAT-PK | |||||
| Kappa-type opioid receptor | GPCR | Ki | 6.65 | WOMBAT-PK | |||||
| Delta-type opioid receptor | GPCR | Ki | 6.05 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 7.70 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D06618 | KEGG_DRUG |
| 916055-93-1 | SECONDARY_CAS_RN |
| 916055-92-0 | SECONDARY_CAS_RN |
| 4027431 | VANDF |
| 4027432 | VANDF |
| CHEBI:136007 | CHEBI |
| CHEMBL1186579 | ChEMBL_ID |
| CHEMBL1201770 | ChEMBL_ID |
| C032257 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7563 | IUPHAR_LIGAND_ID |
| DB06800 | DRUGBANK_ID |
| 0RK7M7IABE | UNII |
| 29899 | RXNORM |
| 136491 | MMSL |
| 25289 | MMSL |
| d07135 | MMSL |
| 012677 | NDDF |
| 012678 | NDDF |
| 429838001 | SNOMEDCT_US |
| 431072004 | SNOMEDCT_US |
| 433519000 | SNOMEDCT_US |
| C0066411 | UMLSCUI |
| 5361918 | PUBCHEM_CID |
| 8728 | INN_ID |
| 0RK7M7IABE | INXIGHT DRUGS |
Pharmaceutical products:
| 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 |