What question did this study set out to answer?

To review the pharmacological mechanisms, metabolic pathways, and pharmacokinetic disposition of the angiotensin-converting enzyme inhibitor captopril.

January 1, 1984Drug Metabolism Reviews

Captopril: Pharmacology, Metabolism, and Disposition

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Why the study?

What are the pharmacological, metabolic, and dispositional properties of captopril in animals and humans?

Population

Animals and humans with essential hypertension, renovascular hypertension, and hypertension associated with…

Design

Review

Authors

BMBruce H. MigdalofBristol-Myers Squibb (Germany)MAMichael J. AntonaccioUniversity of Dundee DKDoris N. Mc Kinstry

Discussion

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Implication

Captopril's pharmacokinetics aid dosing in hypertension; leaves open comparative efficacy versus newer agents in contemporary populations.

Key Points

To review the pharmacological mechanisms, metabolic pathways, and pharmacokinetic disposition of the angiotensin-converting enzyme inhibitor captopril.
Assessed blood pressure and hemodynamic changes following oral captopril administration across renal hypertensive animal models (rats, dogs, monkeys), spontaneously hypertensive rats, and human hypertensive cohorts.
Evaluated the impact of co-interventions, including diuretic co-administration and dietary salt depletion, on antihypertensive efficacy.
Characterized drug absorption, tissue distribution, protein binding, and in vivo and in vitro metabolic transformation.
Oral captopril lowered blood pressure across all species by reducing total peripheral resistance while leaving cardiac output unchanged or elevated.
Antihypertensive effects occurred via renin-dependent ACE inhibition in high-renin states, whereas blood pressure reduction in low- or normal-renin states operated through non-renin-dependent pathways.
The drug demonstrated rapid oral absorption, widespread distribution into all major tissues except the brain, and reversible disulfide conjugation with plasma albumin, cysteine, and glutathione.

Structured PICO

What are the pharmacological, metabolic, and dispositional properties of captopril in animals and humans?

Population

Animals (rats, dogs, monkeys, spontaneously hypertensive rats) and humans with essential hypertension, renovascular hypertension, and hypertension associated with chronic renal failure

Intervention

Captopril

Outcome

Blood pressure reduction and pharmacokinetic/metabolic profilesurrogate

This review summarizes the foundational pharmacology, metabolism, and antihypertensive efficacy of captopril across various animal models and human hypertensive populations.

Cite This Study

Migdalof et al. (1984) studied this question.

synapsesocial.com/papers/6a8e6b26fc1ff9db3528de3e https://doi.org/10.3109/03602538409041080

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Implication

Captopril's pharmacokinetics aid dosing in hypertension; leaves open comparative efficacy versus newer agents in contemporary populations.

Captopril: Pharmacology, Metabolism, and Disposition

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

Captopril: Pharmacology, Metabolism, and Disposition

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

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