June 26, 2014

Safe use of NSAIDs

Non-steroidal anti-inflammatory drugs (NSAIDs) are of value in the treatment of many types of diseases or diseases with pain stemming from their inflammatory.

NSAIDsNSAIDs are today among the most commonly used class of drugs for analgesic therapy. The discovery of the mechanism of action of non-steroidal anti-inflammatory drugs was a result of research mins. Sir John Vane. They enabled not only to understand the mechanism of action of one of the most popular and most frequently used drugs – aspirin, but also become the basis for the synthesis of new drugs – inhibitors, arachidonic acid cyclooxygenase (COX-1 and COX-2).

This mechanism relies on the ability to inhibit cyclooxygenase activity on the central and peripheral, and consequently to inhibit prostaglandin synthesis. NSAIDs, inhibiting both isoforms – both COX-1 and COX-2 – exhibit severe toxic effects on the gastrointestinal mucosa. Thus there is a need for a drug to inhibit COX-2 more than COX-1. As a result, the drugs appeared to be equally well characterized efficiency of operation, while minimal adverse reactions compared to the gastrointestinal tract, that preferential and selective COX-2 inhibitors (coxibs). As selective inhibitors of COX-2 showed a profile of adverse side effects on the cardiovascular system, it appears that the optimum solution becomes preferential COX-2 inhibitors.

The group Preferential inhibitors include etodolac, meloxicam and nimesulide. At therapeutic dosages of these drugs inhibit mainly OOX-2, and COX-1 to a much lesser extent than the first generation of NSAIDs. COX-1 is responsible for the synthesis of PGE2 and prostacyclin, which have a protective effect on the mucous membrane of the stomach and duodenum. Due to the preferential inhibition of COX-2 over COX-1, these drugs have very favorable safety profile towards the gastrointestinal tract.

Meloxicam is widely used in the treatment of osteoarthritis, including rheumatoid arthritis and ankylosing spondylitis nimesulide advantage is that it is rapidly and completely absorbed from the gastrointestinal tract (80-100 percent). And almost completely bound to protein plasma (in ok.98 percent), providing optimal analgesia. Therefore, it is recommended to treat acute pain, osteoarthritis and primary dysmenorrhoea. Both are on the list of reimbursed drugs, with 50-percent level of payment.

Category : NSAIDs