Mechanisms of Action of Nimesulide: Current Understanding

For citation: Knorring G.Yu., Pakhomova I.G. Mechanisms of Action of Nimesulide: Current Understanding. Doctor.Ru. 2020; 19(4): 18–22. (in Russian) DOI: 10.31550/1727-2378-2020-19-4-18-22
13 july 2020

Objective of the Review: To discuss the current understanding of the mechanisms of action of nimesulide and describe the results of studies of this drug, particularly the pharmacokinetics of nimesulide with improved disintegration parameters, which significantly contribute to its therapeutic effect, and new studies of COX-independent effects of this medication.

Key Points: The high bioavailability of nimesulide, effective pain relief, and a marked anti-inflammatory effect should be viewed as its advantages. The rapid onset of Nise’s analgesic action is explained by its 3D-effect, which is related to a high rate of tablet disintegration. The rapid and prolonged pain relief and anti-inflammatory effect provided by nimesulide are due to a wide range of effects not related to cyclooxygenase-2 inhibition.

Conclusion: These properties of nimesulide make it the analgesic and anti-inflammatory medication of choice in clinical practice.

Contributions: Knorring, G.Yu. — developed the concept of the article, studied sources in the literature, and prepared the manuscript; Pakhomova, I.G. — checked critically important content and approved the final version of the manuscript submitted for publication.

Conflict of interest: The authors declare that they do not have any conflict of interests.

G.Yu. Knorring (Corresponding author) — A.I. Yevdokimov Moscow State University of Medicine and Dentistry (a Federal Government-funded Educational Institution of Higher Education), Russian Federation Ministry of Health; 20 Delegatskaya St., Bldg. 1, Moscow, Russian Federation 127473. eLIBRARY.RU SPIN: 1674-4747. ORCID: https://orcid.org/0000-0003-4391-2889. E-mail: knorring@mail.ru

I.G. Pakhomova — V.A. Almazov National Medical Research Center (a Federal Government-funded Institution), Russian Federation Ministry of Health; 2 Akkuratov St., St. Petersburg, Russian Federation 197341. eLIBRARY.RU SPIN: 7798-9476. ORCID: https://orcid.org/0000-0002-3125-6282. E-mail: pakhomova-inna@yandex.ru


Fig. 1. Differences in the mechanisms of action of superdisintegrants: sodium starch glycolate and croscarmellose [12]


Fig. 2. Increase in the volume (swelling) of sodium starch glycolate (Explosol), croscarmellose and other superdisintegrants in contact with fluids with a pH similar to that of the gastric (pH = 1.0) or intestinal (pH = 6.8) contents [14]


Fig 3. Changes in pain level within the first hour after taking non-steroidal anti-inflammatory drugs [15]

Received: 26.05.2020
Accepted: 16.06.2020

13 July 11:33
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