Pharmacokinetics of enalapril in patients with arterial hypertension depending on the glomerular filtration rate

Abstract


Aim. To study the pharmacokinetics of enalapril in patients with arterial hypertension, depending on the value of the prescribed dose of enalapril and the state of renal function to improve the efficiency and safety of treatment. Materials and methods. The study was performed in a group of 328 patients (107 men and 221 women aged 43 to 88 years) who received treatment for hypertension of 1-2 degrees. As the main antihypertensive drug was prescribed enalapril in doses of 2.5 to 20 mg twice a day. Patients underwent therapeutic drug monitoring to determine the concentration of enalapril and its metabolite - enalaprilat. Results. Among the examined patients in 31% of cases there was a decrease in GFR less than 60 ml/min, and in 9 (3%) patients GFR was less than 30 ml/min. This indicates a high prevalence of chronic kidney disease among patients with hypertension. During therapeutic drug monitoring enalapril in patients with hypertension and reduced GFR (less than 60 ml/min) serum concentration of the main metabolite was 1.5-2 times higher than in patients with GFR more than 60 ml/min. Conclusion. It is advisable to carry out therapeutic drug monitoring to determine the concentrations of enalapril and enalaprilat in the serum of patients receiving the drug in high doses and having impaired renal function. In the appointment of enalapril in high doses to patients with reduced GFR, the concentration of enalaprilat significantly exceeds similar indicators in patients with normal GFR and in some cases goes beyond the therapeutic range, indicating the need to consider the correction of the treatment regimen.

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About the authors

Marina V. Zhuravleva

Scientific Center for Expertise of Pharmaceuticals for Medical Use; Sechenov First Moscow State Medical University (Sechenov University)

Moscow, Russia
D. Sci. (Med.), Prof

Aleksei B. Prokofiev

Scientific Center for Expertise of Pharmaceuticals for Medical Use; Sechenov First Moscow State Medical University (Sechenov University)

Moscow, Russia
D. Sci. (Med.), Prof.

Artem I. Dmitriev

Scientific Center for Expertise of Pharmaceuticals for Medical Use

Email: dmitriev-doc@mail.ru
Moscow, Russia
Research Officer

Sergei A. Belkov

Scientific Center for Expertise of Pharmaceuticals for Medical Use

Moscow, Russia
D. Sci. (Med.), Prof.

Evgenii S. Melnikov

Scientific Center for Expertise of Pharmaceuticals for Medical Use; Sechenov First Moscow State Medical University (Sechenov University)

Moscow, Russia
Cand. Sci. (Pharmaceut.)

Tatiana A. Rodina

Scientific Center for Expertise of Pharmaceuticals for Medical Use

Moscow, Russia
Cand. Sci. (Chemical)

Andrei A. Danko

Scientific Center for Expertise of Pharmaceuticals for Medical Use

Moscow, Russia
Cand. Sci. (Med.)

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