What question did this study set out to answer?

To evaluate and compare the pharmacokinetic disposition, absorption, and bioactivation of enalapril maleate and its lysine analogue MK-521 in healthy human volunteers.

September 1, 1982British Journal of Clinical PharmacologyOpen Access

Enalapril maleate and a lysine analogue (MK‐521): disposition in man.

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Authors

EUE H UlmMerck & Co., Inc., Rahway, NJ, USA (United States)MHM HichensUnited States Military Academy HGHJ GomezMerck & Co., Inc., Rahway, NJ, USA (United States)

Discussion

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Implication

Pharmacokinetic study reveals rapid absorption and bioactivation of enalapril versus slower uptake of MK-521 in healthy volunteers, indicating minimal non-bioactivating metabolism.

Key Points

To evaluate and compare the pharmacokinetic disposition, absorption, and bioactivation of enalapril maleate and its lysine analogue MK-521 in healthy human volunteers.
Administered oral 10 mg doses of enalapril maleate (a prodrug requiring bioactivation to MK-422) and MK-521 (a lysine analogue requiring no bioactivation) to normal volunteers.
Quantified parent drugs and active metabolites in serum, urine, and feces to calculate absorption rates, bioactivation extent, and total excretion.
Enalapril maleate was rapidly absorbed (peak serum concentrations at 0.5–1.5 h, ≥61% absorption based on urinary recovery) and underwent at least 70% post-absorptive bioactivation to MK-422.
MK-521 was absorbed more slowly (peak serum concentrations at 6–8 h, ≥29% absorption based on urinary recovery), with both compounds displaying polyphasic serum profiles and prolonged terminal phases.
Total recovery across urine and feces reached 94% for enalapril maleate (intact and MK-422) and 97% for MK-521, confirming the lack of significant metabolism other than enalapril bioactivation.

Cite This Study

Ulm et al. (1982) studied this question.

synapsesocial.com/papers/6a70390d26a7f98052dcba35 https://doi.org/10.1111/j.1365-2125.1982.tb01991.x

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Implication

Pharmacokinetic study reveals rapid absorption and bioactivation of enalapril versus slower uptake of MK-521 in healthy volunteers, indicating minimal non-bioactivating metabolism.

Enalapril maleate and a lysine analogue (MK‐521): disposition in man.

Discussion

Member takes

Implication

Key Points

Cite This Study

Enalapril maleate and a lysine analogue (MK‐521): disposition in man.

Discussion

Member takes

Implication

Key Points

Cite This Study

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