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Thread: Pharmacodynamics and Pharmacokinetics of Long Half-Life ACEIs

  1. #1
    PharmD Year 1 TomHsiung's Avatar
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    Default Pharmacodynamics and Pharmacokinetics of Long Half-Life ACEIs

    Benazepril
    • Systemic, parent drug Tmax: 0.5-1 hr, prodrug (active metabolite: benazeprilat), food does not reduce the extent of absorption, half-life of benazeprilate: 10-11 hrs, excretion: predominantly renal
    • Peak plasma concentrations of benazeprilat are reached 1-2 hours after drug intake in the fasting state and 2-4 hours after drug intake in the nonfasting state


    Enalapril
    • Systemic, parent drug Tmax: 1 hr, prodrug (active metabolite: enalaprilat), food does not impact absorption, half-life of enalaprilat: 35-38 hrs, excretion: primarily renal
    • Peak serum concentrations of enalaprilat occur three to four hours after an oral dose of enalapril maleate


    Fosinopril
    • Systemic, parent drug Tmax: 3 hr, prodrug (active metabolite: fosinoprilat), food delays absorption, half-life of fosinoprilat: 12 hrs, excretion: equally by the liver and kidney
    • The time to peak plasma concentrations of fosinoprilat is about 3 hours, independent of the administered dose of fosinopril


    Lisinopril
    • Systemic, Tmax: within 7 hrs, no metabolism, food does not alter absorption, half-life: 12 hrs, excretion: principally renal


    Ramipril
    • Systemic, Tmax: 1 hr, prodrug (active metabolite: ramiprilat), food delays absorption, half-life of ramirilat: 13-17 hrs, excretion: urine 60% and feces 40%
    • Peak plasma concentrations of ramiprilat are reached 2 to 4 hours after drug intake


    Trandolapril
    • Systemic, Tmax: 1 hr, prodrug (active metabolite: trandolaprilat), food delays absorption, half-life of trandolaprilate: 22.5 hrs, excretion: urine 33%, feces 66%
    • After oral trandolapril under fasting conditions, peak trandolapril levels occur at about one hour and peak trandolaprilat levels occur between 4 and 10 hours
    Last edited by TomHsiung; Wed 15th June '16 at 5:22pm.
    B.S. Pharm, West China School of Pharmacy, Class of 2007, Health System Pharmacist, RPh. Hematology, Infectious Disease.

  2. #2
    PharmD Year 1 TomHsiung's Avatar
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    Default Re: Pharmacodynamics and Pharmacokinetics of Long Half-Life ACEIs

    Benazepril
    The label maintenance dosage is 20 mg/qDay. So according to the Css min of the regimen 20 mg/qDay, and the teff of 24 hours, the loading dose should be 25 mg.

    Enalapril
    The label maintenance dosage is 10 mg/qDay. So according to the Css min of the regimen 10 mg/qDay, and the teff of 24 hours, the loading dose should be 28 mg.
    Last edited by TomHsiung; Wed 15th June '16 at 5:17pm.
    B.S. Pharm, West China School of Pharmacy, Class of 2007, Health System Pharmacist, RPh. Hematology, Infectious Disease.

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