nalbuphine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists related to normorphine | 1874 | 20594-83-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 80 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 35.50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 4 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.80 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 16 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 4.60 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) | 0.50 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.70 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 15, 1979 | FDA |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 256.96 | 44.76 | 93 | 405 | 310594 | 63177930 |
| Antithrombin III | 88.52 | 44.76 | 11 | 487 | 156 | 63488368 |
| Hypoalbuminaemia | 46.61 | 44.76 | 12 | 486 | 11793 | 63476731 |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 173.76 | 36.01 | 76 | 749 | 298840 | 79444723 |
| Febrile bone marrow aplasia | 46.64 | 36.01 | 13 | 812 | 13007 | 79730556 |
| Antithrombin III | 46.45 | 36.01 | 6 | 819 | 87 | 79743476 |
| Transverse sinus thrombosis | 41.51 | 36.01 | 7 | 818 | 658 | 79742905 |
| Superior sagittal sinus thrombosis | 38.23 | 36.01 | 7 | 818 | 1056 | 79742507 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02AF02 | NERVOUS SYSTEM ANALGESICS OPIOIDS Morphinan derivatives |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D000701 | Analgesics, Opioid |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D009294 | Narcotics |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| CHEBI has role | CHEBI:35482 | narcotic analgesic |
| CHEBI has role | CHEBI:50137 | mu-opioid receptor antagonists |
| FDA MoA | N0000175685 | Partial Opioid Agonists |
| FDA MoA | N0000175686 | Competitive Opioid Antagonists |
| FDA EPC | N0000175692 | Opioid Agonist/Antagonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pain | indication | 22253000 | |
| General anesthesia | indication | 50697003 | |
| Labor pain | indication | 247412007 | |
| 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 | 9.93 | acidic |
| pKa2 | 8.23 | 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 | 8.80 | WOMBAT-PK | CHEMBL | |||
| Kappa-type opioid receptor | GPCR | AGONIST | Ki | 8 | WOMBAT-PK | CHEMBL | |||
| Delta-type opioid receptor | GPCR | AGONIST | Ki | 6 | WOMBAT-PK | CHEMBL | |||
| Kappa-type opioid receptor | GPCR | AGONIST | IC50 | 7.40 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4019851 | VUID |
| N0000147937 | NUI |
| D00843 | KEGG_DRUG |
| 23277-43-2 | SECONDARY_CAS_RN |
| 4019046 | VANDF |
| 4019851 | VANDF |
| C0027348 | UMLSCUI |
| CHEBI:7454 | CHEBI |
| CHEMBL1201132 | ChEMBL_ID |
| CHEMBL895 | ChEMBL_ID |
| DB00844 | DRUGBANK_ID |
| D009266 | MESH_DESCRIPTOR_UI |
| 5311304 | PUBCHEM_CID |
| 1663 | IUPHAR_LIGAND_ID |
| 2623 | INN_ID |
| L2T84IQI2K | UNII |
| 154985 | RXNORM |
| 2038 | MMSL |
| 5147 | MMSL |
| d00839 | MMSL |
| 001565 | NDDF |
| 004627 | NDDF |
| 111123003 | SNOMEDCT_US |
| 373539006 | SNOMEDCT_US |
| 83085007 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9917 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 14 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9917 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 14 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9918 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 13 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9918 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 13 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9919 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 13 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9919 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 13 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1463 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1463 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1463 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1463 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1464 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1464 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1465 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1465 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1467 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 28 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-1467 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 28 sections |
| NALBUPHINE HCI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1418 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 14 sections |
| NALBUPHINE HCI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1420 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 14 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-083 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 14 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-463 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 14 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52584-464 | INJECTION, SOLUTION | 10 mg | INTRAVENOUS | ANDA | 14 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7114 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 29 sections |
| Nalbuphine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71872-7114 | INJECTION, SOLUTION | 10 mg | INTRAMUSCULAR | ANDA | 29 sections |