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hydroquinidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 889 | 1435-55-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
urinary quinine metabolite; RN given refers to (9S)-isomer; structure in Merck Index, 9th ed, #4703
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 11.10 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 18 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 30.82 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 2.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 4.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.22 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.70 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 | 1.952 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.618 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 18.030 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.112 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 28.570 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 50.690 | % | High | 1 |
| herg | hERG pIC50 | 5.388 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.570 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 24.266 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 31.520 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,EIF2AK3,ERBB2,GRK2,ITK,PDK1,PDK2,PDK4,PIK3CA,PRKDC | 13 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK9,EIF2AK3,MAP2K6 | 5 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 5.572 | Moderate | 0.74 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.556 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 56.885 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 27.640 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 13.804 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.74 | |
| pppb | Pig plasma protein binding (% unbound) | 45.980 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.126 | % | Moderate | 0.74 |
| rh-clint | Rat hepatocyte intrinsic clearance | 52.240 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 68.480 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 33.690 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 887.156 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C01BA13 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ia |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D010276 | Parasympatholytics |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
Related Drugs by ATC class:
C01BA Antiarrhythmics, class Ia 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.89 | acidic |
| pKa2 | 8.86 | Basic |
| pKa3 | 4.1 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 5 subunit alpha | Ion channel | WOMBAT-PK | |||||||
| Sodium channel subunit beta-1 | Ion channel | WOMBAT-PK | |||||||
| Sodium channel subunit beta-2 | Ion channel | WOMBAT-PK | |||||||
| Sodium channel subunit beta-3 | Ion channel | WOMBAT-PK | |||||||
| Sodium channel subunit beta-4 | Ion channel | WOMBAT-PK | |||||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D08048 | KEGG_DRUG |
| 236160 | RXNORM |
| CHEBI:5792 | CHEBI |
| CHEMBL531472 | ChEMBL_ID |
| CHEMBL2092739 | ChEMBL_ID |
| C014486 | MESH_SUPPLEMENTAL_RECORD_UI |
| 1476-98-8 | SECONDARY_CAS_RN |
| DB15300 | DRUGBANK_ID |
| 005252 | NDDF |
| 005253 | NDDF |
| 765387007 | SNOMEDCT_US |
| 765388002 | SNOMEDCT_US |
| C0063103 | UMLSCUI |
| 91503 | PUBCHEM_CID |
| 8P68XPY4HG | UNII |
Pharmaceutical products:
None