What is important about NSAID-s?

Answer 1

Nonsteroidal anti-inflammatory drugs,, are drugs with analgesic and antipyretic effects and which have, in higher doses, anti-inflammatory effects. The term "nonsteroidal" is used to distinguish these drugs from steroids, which have a similar eicosanoid-depressing, anti-inflammatory action.

Most nonsteroidal anti-inflammatory drugs are weak acids, with a pKa of 3-5. They are absorbed well from the stomach and intestinal mucosa. They are highly protein-bound in plasma (typically >95%), usually to albumin, so that their volume of distribution typically approximates to plasma volume. Most NSAIDs are metabolised in the liver by oxidation and conjugation to inactive metabolites which are typically excreted in the urine, although some drugs are partially excreted in bile. Metabolism may be abnormal in certain disease states, and accumulation may occur even with normal dosage.

Uses

a. Antipyretic, analgesic and antiinflammatory; especially good for pain of headaches, muscles and joints

b. Aspirin also has antiplatelet activity since it causes irreversible inhibition of both cyclooxygenases and platelets are not able to synthesize cyclooxygenase. Thus, until the next generation of platelets develops, which takes 8-11 days, platelet function is disturbed. This enables aspirin to be used for prophylactic treatment of coronary artery disease, thrombotic CVA Cardiovascular Accident and hypercoaguable states.

c. Topical use of salicylic acid irritates skin and mucus membranes and so is used in the treatment of warts, corns and some fungi.

d. Rectal suspensions and suppositories of mesalamine are useful in the treatment of inflammatory bowel disease. Sulfasalazine is ingested and in the colon breaks down to mesalamine.