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levorphanol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists, morphinan derivates | 1574 | 77-07-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.58 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 11.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 15.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.60 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 13.50 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.17 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-selectivity-class | EIF2AK3,GRK2 | 2 | |||
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,ZAP70 | 39 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 8, 1953 | FDA | VALEANT PHARM INTL |
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 |
|---|---|---|---|---|---|---|
| Product dose omission issue | 73.93 | 49.46 | 29 | 252 | 291658 | 90336508 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Product dose omission issue | 100.94 | 45.85 | 38 | 327 | 321744 | 110267190 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000701 | Analgesics, Opioid |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009294 | Narcotics |
| MeSH PA | D018689 | Sensory System Agents |
| FDA MoA | N0000175684 | Full Opioid Agonists |
| FDA EPC | N0000175690 | Opioid Agonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pain | indication | 22253000 | |
| General anesthesia | indication | 50697003 | |
| Local anesthesia | indication | 386761002 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Dependent drug abuse | contraindication | 6525002 | |
| Alcohol withdrawal delirium | contraindication | 8635005 | |
| Asthenia | contraindication | 13791008 | |
| Constipation | contraindication | 14760008 | DOID:2089 |
| Mood swings | contraindication | 18963009 | |
| Inflammatory bowel disease | contraindication | 24526004 | DOID:0050589 |
| Alcohol intoxication | contraindication | 25702006 | |
| Shock | contraindication | 27942005 | |
| Hypercapnia | contraindication | 29596007 | |
| Dehydration | contraindication | 34095006 | |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Bradycardia | contraindication | 48867003 | |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
| Substance abuse | contraindication | 66214007 | |
| Benign intracranial hypertension | contraindication | 68267002 | DOID:11459 |
| Urethral stricture | contraindication | 76618002 | |
| Decreased respiratory function | contraindication | 80954004 | |
| Injury of head | contraindication | 82271004 | |
| Cor pulmonale | contraindication | 83291003 | DOID:8515 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Acute abdominal pain | contraindication | 116290004 | |
| Neoplasm of brain | contraindication | 126952004 | DOID:1319 |
| Seizure disorder | contraindication | 128613002 | |
| Drug-induced psychosis | contraindication | 191483003 | DOID:1742 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Morbid obesity | contraindication | 238136002 | DOID:11981 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Exacerbation of asthma | contraindication | 281239006 | |
| Lesion of brain | contraindication | 301766008 | |
| Coma | contraindication | 371632003 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Operation on gastrointestinal tract | contraindication | 386621005 | |
| Hypoxia | contraindication | 389086002 | |
| Central nervous system depression | contraindication | 418072004 | |
| Dysfunction of sphincter of Oddi | contraindication | 430887001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.05 | acidic |
| pKa2 | 9.55 | Basic |
Orange Book patent data (new drug applications)
None
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 | AGONIST | Ki | 9.68 | CHEMBL | CHEMBL | |||
| Kappa-type opioid receptor | GPCR | Ki | 8.64 | CHEMBL | |||||
| Delta-type opioid receptor | GPCR | Ki | 8.38 | CHEMBL | |||||
| Solute carrier family 22 member 1 | Transporter | IC50 | 5.10 | CHEMBL | |||||
| Glutamate [NMDA] receptor | Ion channel | IC50 | 5.60 | CHEMBL | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 4.60 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | Ki | 9.52 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | Ki | 9.68 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 8.64 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | Ki | 4.60 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 8 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 8.72 | CHEMBL | |||||
| Glutamate NMDA receptor | Ion channel | IC50 | 5.92 | CHEMBL | |||||
| Opioid receptor | GPCR | EC50 | 9.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019801 | VUID |
| N0000147890 | NUI |
| D00841 | KEGG_DRUG |
| 297-90-5 | SECONDARY_CAS_RN |
| 5985-38-6 | SECONDARY_CAS_RN |
| 4017787 | VANDF |
| 4019801 | VANDF |
| C0023586 | UMLSCUI |
| CHEBI:6444 | CHEBI |
| CHEMBL592 | ChEMBL_ID |
| CHEMBL20803 | ChEMBL_ID |
| DB00854 | DRUGBANK_ID |
| CHEMBL3989768 | ChEMBL_ID |
| D007981 | MESH_DESCRIPTOR_UI |
| 5359272 | PUBCHEM_CID |
| 7595 | IUPHAR_LIGAND_ID |
| 91 | INN_ID |
| 27618J1N2X | UNII |
| 153973 | RXNORM |
| 1811 | MMSL |
| 1836 | MMSL |
| 4975 | MMSL |
| d00825 | MMSL |
| 001563 | NDDF |
| 004625 | NDDF |
| 387275004 | SNOMEDCT_US |
| 50335004 | SNOMEDCT_US |
| 67347006 | SNOMEDCT_US |
| 28 | INN_ID |
| 27618J1N2X | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| LEVORPHANOL TARTRATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0438 | TABLET | 2 mg | ORAL | ANDA | 22 sections |
| LEVORPHANOL TARTRATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0438 | TABLET | 2 mg | ORAL | ANDA | 22 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-2224 | TABLET | 2 mg | ORAL | ANDA | 30 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-3236 | TABLET | 2 mg | ORAL | ANDA | 24 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-3237 | TABLET | 3 mg | ORAL | ANDA | 24 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57664-058 | TABLET | 3 mg | ORAL | ANDA | 25 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 57664-762 | TABLET | 2 mg | ORAL | ANDA | 25 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2093 | TABLET | 2 mg | ORAL | ANDA | 26 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69543-417 | TABLET | 2 mg | ORAL | ANDA | 29 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2309 | TABLET | 2 mg | ORAL | ANDA | 29 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2309 | TABLET | 2 mg | ORAL | ANDA | 29 sections |
| Levorphanol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72989-417 | TABLET | 2 mg | ORAL | ANDA | 29 sections |