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piretanide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| diuretics, piretanide derivatives | 2201 | 55837-27-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
potent inhibitor of chloride transport; structure
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.55 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 92 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.17 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.06 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.30 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 | -0.390 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 7.015 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 3.467 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.309 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 3.390 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 4.990 | % | High | 1 |
| herg | hERG pIC50 | 4.362 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.161 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.162 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 2.340 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,JAK2,MAP2K6,MAP3K7,MAPK14,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,TTK | 33 | |||
| kinase-selectivity-class | ACVR2B,AXL,CDK9,DYRK1B,GRK2,MAP2K6,MAPK7,SIK2,STK10,STK33,SYK,TEK,TTK | 13 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.596 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 25.645 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.520 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.531 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 6.390 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 14.997 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 78.600 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.850 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 935.406 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1980 | YEAR INTRODUCED |
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 |
|---|---|---|---|---|---|---|
| Stevens-Johnson syndrome | 64.50 | 63.60 | 17 | 326 | 46884 | 110542072 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C03CA03 | CARDIOVASCULAR SYSTEM DIURETICS HIGH-CEILING DIURETICS Sulfonamides, plain |
| MeSH PA | D004232 | Diuretics |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D049994 | Sodium Potassium Chloride Symporter Inhibitors |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C03CA Sulfonamides, plain 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Edema | indication | 267038008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.58 | acidic |
| pKa2 | 9.66 | acidic |
| pKa3 | 3.92 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Solute carrier family 12 member 1 | Transporter | INHIBITOR | Kd | 8.30 | WOMBAT-PK | KEGG DRUG | |||
| Solute carrier family 12 member 2 | Transporter | INHIBITOR | IC50 | 5.62 | IUPHAR | KEGG DRUG |
External reference:
| ID | Source |
|---|---|
| D01634 | KEGG_DRUG |
| C0071132 | UMLSCUI |
| CHEBI:32015 | CHEBI |
| CHEMBL349803 | ChEMBL_ID |
| DB02925 | DRUGBANK_ID |
| C015451 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4849 | PUBCHEM_CID |
| 4742 | IUPHAR_LIGAND_ID |
| 3741 | INN_ID |
| DQ6KK6GV93 | UNII |
| 151370 | RXNORM |
| 23252 | MMSL |
| 004024 | NDDF |
| 318031002 | SNOMEDCT_US |
| 419451002 | SNOMEDCT_US |
| DQ6KK6GV93 | INXIGHT DRUGS |
Pharmaceutical products:
None