Details
Stereochemistry | RACEMIC |
Molecular Formula | C13H19N5.H2O |
Molecular Weight | 263.3387 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CC(NC(NC1=CC=NC=C1)=NC#N)C(C)(C)C
InChI
InChIKey=AFJCNBBHEVLGCZ-UHFFFAOYSA-N
InChI=1S/C13H19N5.H2O/c1-10(13(2,3)4)17-12(16-9-14)18-11-5-7-15-8-6-11;/h5-8,10H,1-4H3,(H2,15,16,17,18);1H2
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/2434746
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2434746
Pinacidil is a clinically effective vasodilator used for the treatment of hypertension.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2434746
Curator's Comment: Pinacidil does not have a high propensity for crossing the blood/brain barrier
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
69.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10028374 |
12.5 mg 2 times / day multiple, oral dose: 12.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PINACIDIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
365.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10028374 |
12.5 mg 2 times / day multiple, oral dose: 12.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PINACIDIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10028374 |
12.5 mg 2 times / day multiple, oral dose: 12.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PINACIDIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Other AEs: Headache, Edema... Other AEs: Headache (9.7%) Sources: Edema (29%) Dizziness (9.7%) Asthenia (3.2%) Tachycardia (12.9%) Palpitation (3.2%) |
25 mg 2 times / day multiple, oral Dose: 25 mg, 2 times / day Route: oral Route: multiple Dose: 25 mg, 2 times / day Sources: |
unhealthy, 53.6 ± 11.0 years Health Status: unhealthy Age Group: 53.6 ± 11.0 years Sex: M+F Sources: |
Disc. AE: Edema, Tachycardia... AEs leading to discontinuation/dose reduction: Edema (5.9%) Sources: Tachycardia (3.4%) |
37.5 mg 2 times / day multiple, oral Dose: 37.5 mg, 2 times / day Route: oral Route: multiple Dose: 37.5 mg, 2 times / day Sources: |
unhealthy, 53.6 ± 11.0 years Health Status: unhealthy Age Group: 53.6 ± 11.0 years Sex: M+F Sources: |
Disc. AE: Edema... AEs leading to discontinuation/dose reduction: Edema (18.8%) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Tachycardia | 12.9% | 75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Edema | 29% | 75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Asthenia | 3.2% | 75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Palpitation | 3.2% | 75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Dizziness | 9.7% | 75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Headache | 9.7% | 75 mg 2 times / day multiple, oral Highest studied dose Dose: 75 mg, 2 times / day Route: oral Route: multiple Dose: 75 mg, 2 times / day Sources: |
unhealthy, 53.1 years n = 31 Health Status: unhealthy Age Group: 53.1 years Sex: M+F Population Size: 31 Sources: |
Tachycardia | 3.4% Disc. AE |
25 mg 2 times / day multiple, oral Dose: 25 mg, 2 times / day Route: oral Route: multiple Dose: 25 mg, 2 times / day Sources: |
unhealthy, 53.6 ± 11.0 years Health Status: unhealthy Age Group: 53.6 ± 11.0 years Sex: M+F Sources: |
Edema | 5.9% Disc. AE |
25 mg 2 times / day multiple, oral Dose: 25 mg, 2 times / day Route: oral Route: multiple Dose: 25 mg, 2 times / day Sources: |
unhealthy, 53.6 ± 11.0 years Health Status: unhealthy Age Group: 53.6 ± 11.0 years Sex: M+F Sources: |
Edema | 18.8% Disc. AE |
37.5 mg 2 times / day multiple, oral Dose: 37.5 mg, 2 times / day Route: oral Route: multiple Dose: 37.5 mg, 2 times / day Sources: |
unhealthy, 53.6 ± 11.0 years Health Status: unhealthy Age Group: 53.6 ± 11.0 years Sex: M+F Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
major | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
no | |||
Sources: https://pubmed.ncbi.nlm.nih.gov/11851418/ Page: 5.0 |
yes |
Sample Use Guides
Adults: Oral: 12.5 mg twice daily, may increase at intervals of 1-2 weeks; maximum dose: 100-150 mg/day in divided doses
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11282890
In murine WT ventricular cells, pinacidil (1-100uM) concentration-dependently induced an outward current and action potential shortening, effects that were blocked by glibenclamide, a K(ATP) channel blocker.
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QC02LX01
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WHO-ATC |
C02DG01
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WHO-VATC |
QC02DG01
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WHO-ATC |
C02LX01
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NCI_THESAURUS |
C270
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7B0ZZH8P2W
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2412
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DTXSID4045682
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55329
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85371-64-8
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759588
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D020110
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m8819
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33717
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100000081956
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C66387
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DB06762
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PINACIDIL
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2173
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CHEMBL1159
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U-14
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ACTIVE MOIETY
SUBSTANCE RECORD