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pancuronium 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neuromuscular blocking agents with rigid structure | 2052 | 15500-66-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 67 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.17 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.20 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.09 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.90 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.097 | High | 0.83 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.556 | High | 0.83 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 2.234 | 10^-6 cm/s | High | 0.83 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.639 | uL/min/10^6 cells | High | 0.83 |
| dppb | Dog plasma protein binding (% unbound) | 62.830 | % | High | 0.83 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 42.680 | % | High | 0.83 |
| herg | hERG pIC50 | 4.283 | pIC50 | High | 0.83 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.702 | uL/min/10^6 cells | High | 0.83 |
| hlm-clint | Human liver microsomal intrinsic clearance | 6.546 | uL/min/mg protein | High | 0.83 |
| hppb | Human plasma protein binding (% unbound) | 54.480 | % | High | 0.83 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 | 20 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,ZAP70 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.054 | High | 0.83 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 21.135 | High | 0.83 | |
| mppb | Mouse plasma protein binding (% unbound) | 49.830 | High | 0.83 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.887 | High | 0.83 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 51.840 | % | High | 0.83 |
| rh-clint | Rat hepatocyte intrinsic clearance | 47.534 | uL/min/10^6 cells | High | 0.83 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 86.050 | % | High | 0.83 |
| rppb | Rat plasma protein binding (% unbound) | 48.560 | % | High | 0.83 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 883.080 | uM | High | 0.83 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 24, 1972 | FDA |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Labile blood pressure | 242.45 | 104.45 | 36 | 687 | 2435 | 110586141 |
| Hepatic ischaemia | 144.18 | 104.45 | 21 | 702 | 1230 | 110587346 |
| Haematemesis | 123.94 | 104.45 | 35 | 688 | 59073 | 110529503 |
| Hepatorenal syndrome | 116.87 | 104.45 | 21 | 702 | 4576 | 110584000 |
| Renal failure | 104.54 | 104.45 | 43 | 680 | 226531 | 110362045 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M03AC01 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS Other quaternary ammonium compounds |
| MeSH PA | D003473 | Neuromuscular Nondepolarizing Agents |
| MeSH PA | D009465 | Neuromuscular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D018733 | Nicotinic Antagonists |
| FDA EPC | N0000175720 | Nondepolarizing Neuromuscular Blocker |
| FDA PE | N0000175732 | Neuromuscular Nondepolarizing Blockade |
| CHEBI has role | CHEBI:48873 | cholinergic antagonist |
| CHEBI has role | CHEBI:48878 | nicotinic antagonist |
| CHEBI has role | CHEBI:51371 | muscle relaxant |
Related Drugs by ATC class:
M03AC Other quaternary ammonium compounds 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Muscle relaxation, function | indication | 11977004 | |
| General anesthesia | indication | 50697003 | |
| Skeletal Muscle Relaxation for Endotracheal Intubation | indication | ||
| Asthenia | contraindication | 13791008 | |
| Disorder of lung | contraindication | 19829001 | DOID:850 |
| Renal failure syndrome | contraindication | 42399005 | DOID:1074 |
| Body fluid retention | contraindication | 43498006 | |
| Decreased cardiac function | contraindication | 43650005 | |
| Acidosis | contraindication | 51387008 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Disorder of electrolytes | contraindication | 237840007 | |
| Carcinomatosis | contraindication | 307593001 | |
| Hypoxia | contraindication | 389086002 | |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Complete Biliary Obstruction | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Acetylcholine receptor | Ion channel | ANTAGONIST | IC50 | 8.20 | WOMBAT-PK | CHEMBL | |||
| Neuronal acetylcholine receptor; alpha4/beta2 | Ion channel | IC50 | 8.26 | WOMBAT-PK | |||||
| Acetylcholine receptor; alpha1/beta1/delta/gamma | Ion channel | IC50 | 7.09 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018513 | VUID |
| N0000178946 | NUI |
| D00492 | KEGG_DRUG |
| 16974-53-1 | SECONDARY_CAS_RN |
| 4018513 | VANDF |
| 4019874 | VANDF |
| C0030310 | UMLSCUI |
| CHEBI:7907 | CHEBI |
| CHEMBL185073 | ChEMBL_ID |
| CHEMBL1200757 | ChEMBL_ID |
| DB01337 | DRUGBANK_ID |
| 4001 | IUPHAR_LIGAND_ID |
| J76UF062FS | UNII |
| 441289 | PUBCHEM_CID |
| 7883 | RXNORM |
| 4541 | MMSL |
| 5228 | MMSL |
| d00330 | MMSL |
| 002405 | NDDF |
| 013421 | NDDF |
| 350064000 | SNOMEDCT_US |
| 373738000 | SNOMEDCT_US |
| 373764006 | SNOMEDCT_US |
| D010197 | MESH_DESCRIPTOR_UI |
| 2489 | INN_ID |
Pharmaceutical products:
None