Analgesics-Antipyretics and Anti-Inflammatory Agents

The development of aspirin was a significant landmark in the history of medicine because it stimulated the development of a family of medicines, collectively known as the nonsteroidal antiinflammatory drugs (NSAIDs). NSAIDs such as ibuprofen, naproxen, and sulindac are valuable drugs used for the alleviation of pain, inflammation, and fever, and they are commonly prescribed for the treatment of rheumatoid disorders such as arthritis. The world market for NSAIDs now exceeds 6 billion (Vainio and Morgan, 1997). 

Salicylates and allied compounds have analgesic, antipyretic, uricosuric, and anti-inflammatory properties. Their mechanisms of action differ from those of the anti-inflammatory steroids and the opioid analgesics. They are classified into the following categories  

Drugs used in the treatment of gout Colchicine Allopurinol Uricosuric agents 

The pharmacology of acetylsalicylic acid (aspirin) is discussed in detail as a prototype drug, and all the other drugs are compared to it. 

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Aspirin is an analgesic, antipyretic, and anti-inflammatory agent. 

ANALGESIC-ANTIPYRETIC AND ANTI-INFLAMMATORY AGENTS PHARMACOTHERAPY OF GOUT... 

CHAPTER 26 Analgesic-Antipyretic and Anti-inflammatory Agents Pharmacotherapy of Gout 429... 

Aspirin is the most widely consumed analgesic, antipyretic, and anti-inflammatory agent and is the standard for the comparison and evaluation of the others. Because aspirin is so available, the possibility of misuse and serious toxicity probably is underappreciated. 

Flower, R. J. Moncada, S. and Vane, J. R. Analgesic-Antipyretics and Anti-inflammatory Agents Drugs Employed in the Treatment of Gout. In The Pharmacological Basis ofTherapeutics, 7th ed. Gilman, A. G., Goodman, L. S., Rail, T. W., and Mmad, E, Eds. Macmillan New York 1985. 

Aspirin, non-acetylated salicylates, and other NSAIDs have analgesic, antipyretic, and anti-inflammatory actions. These agents inhibit cyclooxygenase (COX-1 and COX-2) enzymes, thereby preventing prostaglandin synthesis, which results in reduced nociceptor sensitization and an increased pain threshold. NSAIDs are the preferred agents for mild to moderate pain in situations that are mediated by prostaglandins (e.g., rheumatoid... 

Reversible inhibitors of COX 1 and COX 2, with analgesic, antipyretic, and anti-inflammatory actions, include ibuprofen, naproxen, indomethacin, ketorolac, and sulindac. When used as antiinflammatory agents, they are usually no more effective than ASA, but they may be better tolerated. All have antiplatelet actions (reversible) at moderate (not low) doses and cause bleeding tendencies. 

In 1899, the Bayer chemical company in Germany produced an ester of salicylic acid and acetic acid, called acetylsalicylic acid (aspirin), which is less irritating. Today, aspirin is used as an analgesic (pain reliever), antipyretic (fever reducer), and anti-inflammatory agent. Many people take a daily low-dose aspirin, which has been found to lower the risk of heart attack and stroke. 

The separation of nonsteroidal anti-inflammatory drugs (NSAIDs) has recently attracted considerable interest. Nonsteroidal anti-inflammatory drugs are agents that, in addition to having anti-inflammatory action, also have analgesic, antipyretic, and platelet-inhibitory properties. They are used primarily in the treatment of chronic arthritic conditions and certain soft tissue disorders associated with pain and inflammation. 

Thiazolyl and benzothiazolyl derivatives are known for their anti-inflammatory, analgesic, and antipyretic activities [72-77], for example Meloxicam (Fig. 3) is a known non-steroidal anti-inflammatory agent with a thiazolyl... 

Aspirin, or acetylsalicylic acid, is the most well known member of a group of compounds called salicylates. Although aspirin was first used in medicine for its analgesic (pain-relieving), antipyretic (fever-reducing), and anti-inflammatory properties, today it is commonly used as an antiplatelet agent in the treatment and prevention of heart attacks and strokes. Aspirin is a synthetic compound it does not occur in nature, though some related salicylates are found in willow bark and meadowsweet blossoms. 

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