Details
Stereochemistry | ACHIRAL |
Molecular Formula | C7H8ClN3O4S2 |
Molecular Weight | 297.739 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NS(=O)(=O)C1=C(Cl)C=C2NCNS(=O)(=O)C2=C1
InChI
InChIKey=JZUFKLXOESDKRF-UHFFFAOYSA-N
InChI=1S/C7H8ClN3O4S2/c8-4-1-5-7(2-6(4)16(9,12)13)17(14,15)11-3-10-5/h1-2,10-11H,3H2,(H2,9,12,13)
Molecular Formula | C7H8ClN3O4S2 |
Molecular Weight | 297.739 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including:
https://www.drugs.com/cdi/capozide.html
http://www.rxlist.com/capozide-drug.htm
Curator's Comment: Description was created based on several sources, including:
https://www.drugs.com/cdi/capozide.html
http://www.rxlist.com/capozide-drug.htm
CAPOZIDE (captopril and hydrochlorothiazide tablets, USP) for oral administration combines two antihypertensive agents: captopril and hydrochlorothiazide. The mechanism of action of captopril has not yet been fully elucidated. Captopril prevents the conversion of angiotensin I to angiotensin II by inhibition of ACE, a peptidyldipeptide carboxy hydrolase. Hydrochlorothiazide belongs to thiazide class of diuretics. It reduces blood volume by acting on the kidneys to reduce sodium (Na+) reabsorption in the distal convoluted tubule. CAPOZIDE (captopril and hydrochlorothiazide tablets, USP) is indicated for the treatment of hypertension. The blood pressure lowering effects of captopril and thiazides are approximately additive. Major side effects are: Black, tarry stools; chest pain; chills; cough; fever; painful or difficult urination; shortness of breath; sore throat; sores, ulcers, or white spots on lips or in mouth; swollen glands; unusual bleeding or bruising; unusual tiredness or weakness. It has been reported that indomethacin may reduce the antihypertensive effect of captopril, especially in cases of low renin hypertension. Captopril’s effect will be augmented by antihypertensive agents that cause renin release. For example, diuretics (e.g., thiazides) may activate the renin-angiotensin-aldosterone system.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
16.7 µM [IC50] | |||
Target ID: CHEMBL1876 |
70.0 µM [IC50] | ||
Target ID: CHEMBL5742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3037074 |
117.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CAPOZIDE Approved UseCAPOZIDE® (captopril and hydrochlorothiazide tablets, USP) is indicated for the treatment of hypertension. The blood pressure lowering effects of captopril and thiazides are approximately additive. Launch Date1984 |
PubMed
Title | Date | PubMed |
---|---|---|
Captopril versus captopril plus hydrochlorothiazide for essential hypertension in Koreans. | 1991 Jan 1 |
|
Captopril and hydrochlorothiazide (Capozide) combine to enhance the reduction in voluntary alcohol intake in rats. | 1993 Oct |
|
[Capozide-50 alone and in combination with melatonin in therapy of hypertension]. | 2000 |
Patents
Sample Use Guides
therapy may be instituted with a single tablet of CAPOZIDE (captopril/hydrochlorothiazide) 25 mg/15 mg taken once daily. For patients insufficiently responsive to the initial dose, additional captopril or hydrochlorothiazide may be added as individual components or by using CAPOZIDE (captopril/hydrochlorothiazide) 50 mg/15 mg, 25 mg/25 mg or 50 mg/25 mg, or divided doses may be used. Daily doses of captopril should not exceed 150 mg and of hydrochlorothiazide should not exceed 50 mg.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7037633
Curator's Comment: The present study shows that 1-100 microM hydrochlorothiazide (HCTZ) dose dependently inhibits bone resorption by isolated rat osteoclasts in the bone slice assay with an IC50 of approximately 20 microM.
https://www.ncbi.nlm.nih.gov/pubmed/7820777
In the presence of captopril (2 X 10^4 M), contractile responses to angiotensln I (5 X 10^10 to 5 X 10^8 M) were attenuated significantly.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:17:35 GMT 2023
by
admin
on
Fri Dec 15 15:17:35 GMT 2023
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Record UNII |
0J48LPH2TH
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
---|---|---|---|---|
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EMA ASSESSMENT REPORTS |
RASITRIO (WITHDRAWN: HYPERTENSION)
Created by
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EMA ASSESSMENT REPORTS |
TOLUCOMBI (AUTHORIZED: HYPERTENSION)
Created by
admin on Fri Dec 15 15:17:35 GMT 2023 , Edited by admin on Fri Dec 15 15:17:35 GMT 2023
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EMA ASSESSMENT REPORTS |
IBERSARTAN/HYDROCHLOROTHIAZIDE ZENTIVA (AUTHORIZED: HYPERTENSION)
Created by
admin on Fri Dec 15 15:17:35 GMT 2023 , Edited by admin on Fri Dec 15 15:17:35 GMT 2023
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WHO-ATC |
C03AB03
Created by
admin on Fri Dec 15 15:17:35 GMT 2023 , Edited by admin on Fri Dec 15 15:17:35 GMT 2023
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EMA ASSESSMENT REPORTS |
IBERSARTAN/HYDROCHLOROTHIAZIDE-BMS (WITHDRAWN: HYPERTENSION)
Created by
admin on Fri Dec 15 15:17:35 GMT 2023 , Edited by admin on Fri Dec 15 15:17:35 GMT 2023
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NDF-RT |
N0000166469
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WHO-VATC |
QC09DX01
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EMA ASSESSMENT REPORTS |
SPRIMEO-HCT (WITHDRAWN: HYPERTENSION)
Created by
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EMA ASSESSMENT REPORTS |
EXFORGE-HCT (AUTHORIZED: HYPERTENSION)
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WHO-VATC |
QC09DX03
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EMA ASSESSMENT REPORTS |
KINZALKOMB (AUTHORIZED: HYPERTENSION)
Created by
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EMA ASSESSMENT REPORTS |
KARVEZIDE (AUTHORIZED: HYPERTENSION)
Created by
admin on Fri Dec 15 15:17:35 GMT 2023 , Edited by admin on Fri Dec 15 15:17:35 GMT 2023
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WHO-ATC |
C09XA52
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EMA ASSESSMENT REPORTS |
RASILEZ-HCT (AUTHORIZED: HYPERTENSION)
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WHO-ESSENTIAL MEDICINES LIST |
12.3
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IARC | Hydrochlorothiazide | ||
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EMA ASSESSMENT REPORTS |
IMPRIDA-HCT (WITHDRAWN: HYPERTENSION)
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EMA ASSESSMENT REPORTS |
MICARDISPLUS (AUTHORIZED: HYPERTENSION)
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WHO-ATC |
C03AA03
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WHO-VATC |
QC03EA01
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EMA ASSESSMENT REPORTS |
PRITORPLUS (AUTHORIZED: HYPERTENSION0
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WHO-ATC |
C09XA54
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WHO-VATC |
QC03AA03
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WHO-ATC |
C03EA01
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WHO-ATC |
C09DX01
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WHO-ATC |
C09BX03
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NDF-RT |
N0000175419
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WHO-VATC |
QC09XA52
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EMA ASSESSMENT REPORTS |
RIPRAZO-HCT (WITHDRAWN: HYPERTENSION)
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WHO-ESSENTIAL MEDICINES LIST |
12.4
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WHO-VATC |
QC03AX01
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LIVERTOX |
483
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EMA ASSESSMENT REPORTS |
IBERSARTAN/HYDROCHLOROTHIAZIDE TEVA (AUTHORIZED: HYPERTENSION)
Created by
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WHO-ESSENTIAL MEDICINES LIST |
16
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NDF-RT |
N0000175359
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EMA ASSESSMENT REPORTS |
COPALIA-HCT (AUTHORIZED: HYPERTENSION)
Created by
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WHO-VATC |
QC09XA54
Created by
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EMA ASSESSMENT REPORTS |
IFIRMACOMBI (AUTHORIZED: HYPERTENSION)
Created by
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WHO-VATC |
QC03AB03
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CFR |
21 CFR 522.1150
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WHO-ATC |
C09DX03
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NDF-RT |
N0000166469
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NCI_THESAURUS |
C49185
Created by
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EMA ASSESSMENT REPORTS |
DAFIRO-HCT (AUTHORIZED: HYPERTENSION)
Created by
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WHO-ATC |
C09DX06
Created by
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WHO-ATC |
C03AX01
Created by
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Code System | Code | Type | Description | ||
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8049-49-8
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SUPERSEDED | |||
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DB00999
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PRIMARY | |||
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HYDROCHLOROTHIAZIDE
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PRIMARY | |||
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5487
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PRIMARY | RxNorm | ||
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DTXSID2020713
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PRIMARY | |||
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HYDROCHLOROTHIAZIDE
Created by
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PRIMARY | Description: A white or almost white, crystalline powder; odourless or almost odourless. Solubility: Very slightly soluble in water; practically insoluble in ether R; soluble in 200 parts of ethanol (~750 g/l) TS and in 20 parts of acetone R. Category: Diuretic. Storage: Hydrochlorothiazide should be kept in a well-closed container. Definition: Hydrochlorothiazide contains not less than 98.0% and not more than 102.0% of C7H8ClN3O4S2, calculated with reference to the dried substance. | ||
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3096
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PRIMARY | |||
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58-93-5
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PRIMARY | |||
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1314009
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PRIMARY | |||
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100000091737
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PRIMARY | |||
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C29098
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PRIMARY | |||
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0J48LPH2TH
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PRIMARY | |||
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53477
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PRIMARY | |||
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D006852
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PRIMARY | |||
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m6089
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PRIMARY | Merck Index | ||
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841
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PRIMARY | |||
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SUB08062MIG
Created by
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PRIMARY | |||
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Hydrochlorothiazide
Created by
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PRIMARY | |||
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3639
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PRIMARY | |||
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0J48LPH2TH
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PRIMARY | |||
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200-403-3
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PRIMARY | |||
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CHEMBL435
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PRIMARY | |||
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1385
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PRIMARY | |||
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4836
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PRIMARY | |||
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5778
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PRIMARY |
Related Record | Type | Details | ||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
EP
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TRANSPORTER -> INHIBITOR | |||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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EXCRETED UNCHANGED |
URINE
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> INHIBITOR |
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TRANSPORTER -> INHIBITOR |
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DERIVATIVE -> PARENT |
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
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Related Record | Type | Details | ||
---|---|---|---|---|
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Biological Half-life | PHARMACOKINETIC |
|
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