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noscapine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| quinoline derivatives | 1973 | 128-62-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A naturally occurring opium alkaloid that is a centrally acting antitussive agent.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.13 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 30 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 2.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 16.88 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.13 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.853 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.461 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 60.814 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 44.463 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 6.840 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 17.850 | % | High | 1 |
| herg | hERG pIC50 | 4.607 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 80.724 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 306.902 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 6.860 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK | 45 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,EPHB4,GRK2,PDK4,TTK | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.406 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 165.577 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 7.660 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.824 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 20.110 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 308.319 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 61.150 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 5.490 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 27.733 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 484.70 | 123.71 | 164 | 514 | 228972 | 42391685 |
| Drug abuse | 212.38 | 123.71 | 74 | 604 | 104697 | 42515960 |
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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 401.25 | 91.85 | 156 | 959 | 480399 | 110107785 |
| Drug abuse | 248.18 | 91.85 | 85 | 1030 | 177326 | 110410858 |
| Asphyxia | 109.67 | 91.85 | 26 | 1089 | 14189 | 110573995 |
| Sinobronchitis | 97.62 | 91.85 | 14 | 1101 | 468 | 110587716 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R05DA07 | RESPIRATORY SYSTEM COUGH AND COLD PREPARATIONS COUGH SUPPRESSANTS, EXCL. COMBINATIONS WITH EXPECTORANTS Opium alkaloids and derivatives |
| MeSH PA | D000996 | Antitussive Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:51177 | anti-tussive |
| CHEBI has role | CHEBI:68495 | Type I cell-death inducers |
| CHEBI has role | CHEBI:76924 | plant metabolites |
Related Drugs by ATC class:
R05DA Opium alkaloids and derivatives 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Tachyarrhythmia | contraindication | 6285003 | |
| Alcoholism | contraindication | 7200002 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Pulmonary edema | contraindication | 19242006 | DOID:11396 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Shock | contraindication | 27942005 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Acute hepatitis | contraindication | 37871000 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Third trimester pregnancy | contraindication | 41587001 | |
| Chronic heart failure | contraindication | 48447003 | |
| Multiple organ failure | contraindication | 57653000 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Cor pulmonale | contraindication | 83291003 | DOID:8515 |
| Seizure disorder | contraindication | 128613002 | |
| Cystic fibrosis | contraindication | 190905008 | DOID:1485 |
| Angina pectoris | contraindication | 194828000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Sepsis syndrome | contraindication | 238150007 | |
| Continuous fever | contraindication | 271751000 | |
| Smoking cessation assistance | contraindication | 384742004 | |
| Smokes tobacco daily | contraindication | 449868002 | |
| Theophylline Toxicity | contraindication | ||
| Severe Hypoxemia | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.51 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 2C9 | Enzyme | IC50 | 5.09 | DRUG MATRIX | |||||
| Cytochrome P450 2C19 | Enzyme | IC50 | 6.40 | DRUG MATRIX | |||||
| Solute carrier family 22 member 2 | Transporter | IC50 | 5.59 | CHEMBL | |||||
| Multidrug and toxin extrusion protein 1 | Transporter | IC50 | 4.46 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166975 | NUI |
| D01036 | KEGG_DRUG |
| C0028426 | UMLSCUI |
| CHEBI:73237 | CHEBI |
| 08N | PDB_CHEM_ID |
| CHEMBL364713 | ChEMBL_ID |
| D009665 | MESH_DESCRIPTOR_UI |
| DB06174 | DRUGBANK_ID |
| 275196 | PUBCHEM_CID |
| 10212 | IUPHAR_LIGAND_ID |
| 632 | INN_ID |
| 8V32U4AOQU | UNII |
| 7533 | RXNORM |
| 001654 | NDDF |
| 006427 | NDDF |
| 387437002 | SNOMEDCT_US |
| 76696004 | SNOMEDCT_US |
| CHEMBL2106732 | ChEMBL_ID |
| 912-60-7 | SECONDARY_CAS_RN |
| 8V32U4AOQU | INXIGHT DRUGS |
Pharmaceutical products:
None