pinacidil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasodilators | 2173 | 60560-33-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.91 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 57 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.68 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.60 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.50 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.04 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | LEO PHARM |
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 | C02DG01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON Guanidine derivatives |
| ATC | C02LX01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Other antihypertensives and diuretics |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D014665 | Vasodilator Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.09 | Basic |
| pKa2 | 0.0 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sulfonylurea receptor 2, Kir6.2 | Ion channel | OPENER | Ki | 6.49 | CHEMBL | CHEMBL | |||
| ATP-binding cassette sub-family C member 9 | Ion channel | EC50 | 5.45 | CHEMBL | |||||
| Calcium-activated potassium channel subunit alpha-1 | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4025256 | VUID |
| N0000171786 | NUI |
| D05482 | KEGG_DRUG |
| 4025256 | VANDF |
| C0071074 | UMLSCUI |
| CHEBI:34923 | CHEBI |
| CHEMBL1159 | ChEMBL_ID |
| CHEMBL251647 | ChEMBL_ID |
| CHEMBL1200338 | ChEMBL_ID |
| CHEMBL398879 | ChEMBL_ID |
| DB06762 | DRUGBANK_ID |
| D020110 | MESH_DESCRIPTOR_UI |
| 4826 | PUBCHEM_CID |
| 2412 | IUPHAR_LIGAND_ID |
| 7B0ZZH8P2W | UNII |
| 33717 | RXNORM |
| 003753 | NDDF |
| 003777 | NDDF |
| 85371-64-8 | SECONDARY_CAS_RN |
Pharmaceutical products:
None