Contribution of lipophilicity to the clinical effects of drugs
https://doi.org/10.15829/1560-4071-2024-5829
EDN: GJICGY
Abstract
The article is devoted to a detailed analysis of the action of various drugs used in the treatment of hypertension and atherogenic dyslipidemia, depending on their ability to dissolve in fatty media (lipophilicity). The authors analyze connection between the lipophilicity level of drugs and their pharmacokinetics, drug-drug interactions, the manifestations of clinical effects and organ protection, as well as their ability to influence the prognosis of comorbid patients. Using angiotensin-converting enzyme inhibitors, calcium channel blockers, and statins as examples, the authors explain the practical significance of pharmacological parameters such as plasma protein binding and distribution volume, and also develop an understanding of the importance of its routine use in order to obtain clinical benefits for patients.
Supporting agencies: This article was supported by the Servier Company
About the Authors
A. S. Skotnikov
I.M. Sechenov First Moscow State Medical University; Russian State Social University; Research Center for Comorbid Pathology "Rational Medicine"
Russian Federation
Competing Interests:
Russian Federation
Moscow
Competing Interests:
none
M. V. Melnik
I.M. Sechenov First Moscow State Medical University
Russian Federation
Competing Interests:
Russian Federation
Moscow
Competing Interests:
none
E. A. Zinina
Russian State Social University
Russian Federation
Competing Interests:
Russian Federation
Moscow
Competing Interests:
none
I. V. Sivertseva
Russian State Social University; Research Center for Comorbid Pathology "Rational Medicine"
Russian Federation
Competing Interests:
Russian Federation
Moscow
Competing Interests:
none
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- Fat-soluble (lipophilic) medications are quickly absorbed, widely distributed in the body, and also have material and functional accumulation in tissues, providing longer-lasting and more pronounced organ protective effects than hydrophilic medications.
- An excessive lipophilicity of medications affects not only its positive properties, but also the severity of its undesirable effects and toxicity.
- Modern drugs with moderate lipophilicity and prescribed in average therapeutic doses are most effective in terms of long-term benefits and organ protective properties, while having an adequate safety profile.
- Combining lipophilic ingredients in multi-purpose drugs potentiates the severity of the beneficial properties of each of them.
Review
For citations:
Skotnikov A.S., Melnik M.V., Zinina E.A., Sivertseva I.V. Contribution of lipophilicity to the clinical effects of drugs. Russian Journal of Cardiology. 2024;29(3):5829. (In Russ.) https://doi.org/10.15829/1560-4071-2024-5829. EDN: GJICGY
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