PMSC | 213Faisal A. Al Moaiqel 30 05 03 008Abdulaziz Alenazi COX 1,2 30 05 01 007Mohammed Al-Sherbrain Inhibitors 30 05 02 013Meshal A. Almaghrabi 30 05 02 008Khalid N. Al Dalbahi 28 05 03 016
Objectives Overview. Mechanism of Action. Medical Uses. Side Effects.
Overviewwhat’s COXs and their roles? Cyclooxygenase is an enzyme responsible about formation prostanoids . Ex: prostaglandins - fatty-acid derivatives located all over body. The role of COX is mediates the conversion of arachidonic acid into PGH2,which is then converted to various PGs by specific syntheses COX 1,2 .
OverviewHow NSAIDs work ? RegularNon-steroidal anti-inflammatory drugs (NSAIDs) work by inhibit the production of prostaglandins (PGs) , which will inhabit their inflammation and immune response effects.
OverviewCOX-1 COX-1 is expressed in many tissues (including the gastrointestinal tract, platelets, and kidney) And its responsible for producing prostanoids that regulate normal physiologic functions.
OverviewCOX-2 COX-2 is the inducible form responsible for the production of prostanoids in response to a variety of evoking stimuli (including cytokines, growth factors, mitogens, and tumor promoters) in different tissues and for the mediation of inflammation and pain in certain diseases.
Mechanism of Action Most NSAIDs act as non-selective inhibitors of the enzyme cyclooxygenase, inhibiting both the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes.
Mechanism of Action Cyclooxygenase catalyzes the formation of prostaglandins and thromboxane from arachidonic acid . Prostaglandins act (among other things) as messenger molecules in the process of inflammation.
Medical Uses NSAIDs are usually indicated for the treatment of acute or chronic conditions where pain and inflammation are present. Research continues into their potential for prevention of colorectal cancer, and treatment of other conditions, such as cancer and cardiovascular disease.
Medical Uses NSAIDs are generally indicated for the symptomatic relief of the following conditions: Rheumatoid arthritis. Inflammatory arthropathies. Dysmenorrhea. Headache and migraine.
Medical Uses Aspirin, the only NSAID able to irreversibly inhibit COX-1, is also indicated for inhibition of platelet aggregation. This is useful in the management of arterial thrombosis and prevention of adverse cardiovascular events. Aspirin inhibits platelet aggregation by inhibiting the action of thromboxane A2
Side EffectsThe Main Side Effect of NSAIDsIs: Cardiovascular. The link between COX-2 inhibitors and increased risk of heart attack is now well established.Others: Gastrointestinal. Inflammatory bowel disease. Renal Disorders.