541
Volume 5, Issue 10: Special Issue
(EJAR)
ISSN: 2181-2020
MPHAPP
THE 6TH INTERNATIONAL SCIENTIFIC AND PRACTICAL
CONFERENCE
“
MODERN PHARMACEUTICS: ACTUAL
PROBLEMS AND PROSPECTS
”
TASHKENT, OCTOBER 17, 2025
in-academy.uz
IMMUNOSUPPRESSANTS IN MODERN PHARMACOLOGY: MECHANISMS OF
ACTION AND CLINICAL APPLICATION
Ismatova.Sh.A.
Sultanova.R.X.
Tashkent Pharmaceutical Institute, Tashkent, Republic of Uzbekistan
e-mail:ismatovas342@gmail.com (90)-193-01-10
https://doi.org/10.5281/zenodo.17344101
Relevance:
The immune system is a complex network of cells and mediators designed to
protect the div from pathogens. However, in some cases (organ transplantation, autoimmune and
allergic diseases) this protective reaction becomes excessive or directed against one's own tissues,
which requires pharmacological correction. Immunosuppressants are a heterogeneous group of drugs
that specifically inhibit the immune response. Their introduction revolutionized transplantology and
significantly improved the prognosis for many autoimmune pathologies. However, their use is
associated with serious side effects, primarily with an increased risk of infections and cancer, which
dictates the need to search for new, more selective targets and drugs.
Objective:
to conduct a systematic review and analysis of current scientific data on the
classification, mechanisms of action, main indications for use and side effects of immunosuppressive
drugs.
Materials and methods:
to write this review, we conducted a search and analysis of scientific
publications for the last 10 years (2014-2024) published in peer-reviewed domestic and foreign
journals. Materials were searched in the electronic databases "PubMed, Google Scholar,
CyberLeninka, eLibrary".
Results.
1)
Detailed analysis of the mechanisms of action and evolution of approaches:
Ингибиторы Calcineurin inhibitors (IC) (Cyclosporine, Tacrolimus): The mechanism consists
in blocking calcineurin, which prevents the activation of the nuclear factor of activated T cells (NF-
AT) and, as a result, the transcription of interleukin-2 (IL-2) genes. Tacrolimus was shown in meta-
analyses to be more effective in preventing acute renal transplant rejection than cyclosporine, but
with a comparable risk of nephrotoxicity and a higher incidence of diabetogenic effects; 2) Trends in
combination therapy:
Current protocols are based on the principle of synergy to reduce the doses and toxicity of each
component. Standard triple regimen after transplantation: IR (tacrolimus) + antimetabolite (MMF) +
low-dose glucocorticoid. There is a trend towards early reduction or elimination of glucocorticoids
and the use of induction therapy with biological agents (for example, basiliximab) to minimize the
nephrotoxicity of IC. 3) Safety profile analysis: The main class-effect of all immunosuppressants is
a dose-dependent increase in the risk of opportunistic infections (cytomegalovirus, Epstein-Barr
virus) and cancer (skin cancer, lymphoproliferative disorders). IC-based regimens carry the greatest
risk of nephrotoxicity and cardiovascular complications, while biologics require vigilance for
reactivation of tuberculosis and hepatitis B.
Conclusions.
Modern pharmacotherapy is based on the principles of combined use of drugs
with different mechanisms of action to achieve maximum effectiveness while minimizing doses and,
accordingly, toxicity. The mainchallenge for long-term treatment with immunosuppressants remains
the management of their side effects, which requires careful monitoring of patients and an individual
approach to the choice of treatment regimen.
