Ramipril pharmacokinetics and molecular data

Pharmacokinetics and molecular data
Absorption Distribution Metabolism Elimination

Absorption
Extent of absorption in GI tract is at least 50% to 60%. T max is 1 h (parent compound) or 2 to 4 h (metabolite, ramiprilat). Bioavailability is 28% (ramipril) or 44% (ramiprilat).

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Distribution
Protein binding is about 73% (parent) or about 56% (metabolite). Plasma concentrations of ramiprilat decline in a triphasic manner: initial rapid decline (representing distribution into peripheral compartment), apparent elimination phase, and terminal elimination phase.

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Metabolism
In liver to active metabolite ramiprilat, which had 6 times the ACE inhibitory activity.

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Elimination
Eliminated in urine (60% of parent and metabolites) and feces (40%). Less than 2% of drug recovered in urine is unchanged. The t ½ is less than 50 h (ramiprilat).

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