Nonsteroidal anti-inflammatory drugs (NSAIDs or NSAID) - a group of drugs with analgesic, antipyretic and anti-inflammatory effects. Their action is based on blocking the production of prostaglandins, which are excreted at the site of any tissue damage. Currently, non-steroidal anti-inflammatory drugs are rightfully considered one of the most popular drugs used in clinical practice.
The most famous NSAID is aspirin (acetylsalicylic acid). By non-steroidal anti-inflammatory drugs also include diflunisal, lizinmonoatsetilsalitsilat, phenylbutazone, indomethacin, sulindac, etodolac, diclofenac, piroxicam, tenoxicam, lornoxicam, meloxicam, ibuprofen, naproxen, flurbiprofen, ketoprofen, tiaprofenic acid, nabumetone, nimesulide, celecoxib, rofecoxib, mesalazine and a lot others.
The main problem of the use of nonsteroidal anti-inflammatory drugs is that, being the most effective drugs in the treatment of many diseases, they also damaging act on the mucous membrane of the stomach and duodenum, and as a therapeutic, naproxen-Akritak and damaging effects of NSAIDs are consequences of inhibition NSAIDs prostaglandin production.
The main physiological functions of prostaglandins in the digestive tract are stimulated secretion of protective mucus and bicarbonates, activation of cell proliferation in normal recovery processes and increased local blood flow in the mucous membrane. The anti-inflammatory and analgesic effects of nonsteroidal anti-inflammatory drugs are due to inhibition of the enzyme cyclooxygenase (COX). There are two isoforms of COX: COX-1 and COX-2. The first of them is present in most tissues, including the gastrointestinal mucosa, controls the production of prostaglandins that regulate the integrity of the mucosa of the gastrointestinal tract, platelet function and renal blood flow. COX-2 plays a role of "structural" enzyme only in some organs (brain, kidney, bone, etc.)., And normally is not found in other tissues. Its expression significantly increases under the influence of "pro-inflammatory" stimuli and, on the contrary, it decreases under the action of endogenous substances with anti-inflammatory activity. It is believed that the anti-inflammatory effect of NSAIDs depends on the blocking of COX-2, and their side effects are associated with the suppression of COX-1.
Diclofenac One of the most important problems of gastroenterology is the treatment and prevention of NSAIDs-gastropathies - diseases of the gastrointestinal tract associated with the use of non-steroidal anti-inflammatory drugs and acetylsalicylic acid. In the late 1970s it was found that patients with rheumatic diseases receiving NSAIDs die from gastrointestinal bleeding and perforation of ulcers more often than those who do not take NSAIDs.
Despite significant progress in the study of NSAIDs and the creation of safer drugs, modern statistics indicate that the risk of gastrointestinal bleeding when taking NSAIDs increases by 3-5 times, perforations at 6, the risk of death from complications associated with gastrointestinal tract damage - 8 times. In 40-50% of patients hospitalized with a diagnosis of acute gastrointestinal bleeding, it is due to the intake of this class of drugs. In the United Kingdom, of these complications, up to 2,000 patients die each year, in the US, NSAIDs are responsible for 100,000 hospitalizations and 16,000 deaths per year.