The disposition of captopril, an angiotensin-converting enzyme inhibitor with antihypertensive properties, was studied in 10 normal male subjects after a single 100-mg tablet of 35S-labeled drug. Average absorption parameters for unchanged captopril in blood were Tmax 0.93 +/- 0.08 hr and Cmax 800 +/- 76 ng/ml. For total radioactivity in blood the values were Tmax 1.05 +/- 0.08 hr and Cmax 1,580 +/- 90 ng/ml (as captopril equivalents). Because of the curvilinearity of the semilogarithmic plots of blood concentrations of captopril:time, elimination half-life (t1/2) of unchanged drug could not be determined. At 1 hr unchanged captopril accounted for about 52% of total radioactivity in blood, and the dimeric disulfide metabolite of captopril accounted for about 10%. In the first 5 days after dosing, an average of about 68% of the radioactive dose was recovered in urine and 18% in feces. The distribution of radioactivity in the first 24-hr urine sample (66% of the dose) was 58% captopril (38% of dose), 2% captopril disulfide (1.5% of dose), and 40% unidentified polar metabolites (26% of dose).
Captopril modifies the hemodynamic and neuroendocrine responses to sodium nitroprusside in hypertensive patients
Sustained haemodynamic and clinical effects of captopril in long-term treatment of severe chronic congestive heart failure
Influence of chronic renal failure on captopril pharmacokinetics and clinical and biological effects in hypertensive patients
Captopril: clinical pharmacology and benefit-to-risk ratio in hypertension and congestive heart failure
Cardiovascular drugs in children. II. Angiotensin-converting enzyme inhibitors in pediatric patients
Impact of disease states on the pharmacokinetics and pharmacodynamics of angiotensin-converting enzyme inhibitors
Interactions between carnosine and captopril on free radical scavenging activity and angiotensin-converting enzyme activity in vitro
Visualized absorption of anti-atherosclerotic dipeptide, Trp-His, in Sprague-Dawley rats by LC-MS and MALDI-MS imaging analyses
Evaluation of captopril versus reserpine and frusemide in treating hypertensive children with acute post-streptococcal glomerulonephritis
Preferential biliary elimination of FPL 63547, a novel inhibitor of angiotensin-converting enzyme, in the rat
Maintenance of the antihypertensive efficacy of captopril despite consistent reduction in daily dosage
What is the objective of the mass balance study? A retrospective analysis of data in animal and human excretion studies employing radiolabeled drugs
The efficacy of a coordinated pharmacological blockade in glioblastoma stem cells with nine repurposed drugs using the CUSP9 strategy
Sustained Captopril-Induced Reduction in Blood Pressure Is Associated With Alterations in Gut-Brain Axis in the Spontaneously Hypertensive Rat
Pharmacokinetics and biological effects of captopril and hydrochlorothiazide after acute and chronic administration either alone or in combination in hypertensive patients
Blood concentration and urinary excretion of captopril (SQ 14,225) in patients with chronic renal failure
Development and evaluation of physiologically based pharmacokinetic drug-disease models for predicting captopril pharmacokinetics in chronic diseases.
Determination of total captopril in dog plasma by HPLC after prelabelling with ammonium 7-fluorobenzo-2-oxa-1,3-diazole-4-sulphonate (SBD-F)
Determination of captopril and its mixed disulphides in plasma and urine by high-performance liquid chromatography
Antihypertensive Agents: Mechanisms of Action
Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.