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It is rapidly absorbed in the stomach and upper small intestine and reaches 80% of its peak plasma concentration in 1 hour. Gastrointestinal symptoms are encountered in 20% of patients. Other adverse reactions include dizziness, tinnitus, headache, and rash.

Mefenamic acid, another fenamate, possesses analgesic properties but is probably less effective than aspirin as an anti-inflammatory agent and is clearly more toxic.

Sulindac is a prodrug. Its active metabolite is, like diclofenac, an acetic acid derivative. The drug is effective only after it is converted by liver enzymes to a sulfide, which is excreted in bile and then reabsorbed from the intestine. The enterohepatic cycling prolongs the duration of action to 12-16 hours. The indications and adverse…

Diclofenac is a potent cyclooxygenase inhibitor with antiinflammatory, analgesic, and antipyretic properties. The drug is rapidly absorbed following oral administration and has a half-life of 1-2 hours. It accumulates in the synovial fluid. The potency of diclofenac as a cyclooxygenase inhibitor is greater than that of naproxen. The drug is recommended for chronic inflammatory conditions…

Ibuprofen is extensively metabolized in the liver, and little is excreted unchanged. Gastrointestinal irritation and bleeding occur, though less frequently than with aspirin. In addition to the gastrointestinal symptoms, rash, pruritus, tinnitus, dizziness, headache, and fluid retention have been reported. Rare hematologic effects include agranulocytosis and aplastic anemia. Effects on the kidney include acute renal…

The newer NSAIDs inhibit of biosynthesis of prostaglandins. In addition they inhibit chemotaxis, down-regulate interleukin-1 production, and interfere with calcium-mediated intracellular events. These drugs are reversible inhibitors of cyclooxygenase. Most of these drugs are well absorbed. Most of the NSAIDs are highly metabolized, some by phase I and phase II mechanisms and others by direct…

Aspirin Aspirin and other nonsteroidal anti-inflammatory drugs are weak organic acids. They all inhibit prostaglandin biosynthesis. They decrease the production of free radicals and of superoxide and may interact with adenylyl cyclase to alter the cellular concentration of cAMP. Aspirin is the drug of choice for treating the majority of articular and musculoskeletal disorders. It…

Thromoboxane A2 is an arachidonate product that causes platelet to change shape, to release their granules and to aggregate. Drugs that antagonize this pathway interfere with platelet aggregation and prolong bleeding time. Asprin at low dose is the prototype of this class of drugs. It inhibits the synthesis of thromboxane A2 by irreversible acetylation of…

Platelet function is regulated by three categories of substances Agents    outside    the   platelet    that    interact   with        platelet    membrane      receptors,                   e.g. catecholamines, prostacyclin. Agents generated within the platelets and interact with the membrane receptors, e.g. prostaglandin E2 and serotonin. Agents generated within the platelet and act within the platelet, e.g. thromboxane A2 and calcium ions. Antiplatelets…

Fibrinolytic agents rapidly lyse thrombi by catalyzing the formation of plasmin from plasminogen. All thrombolytic agents currently in use act directly or indirectly as plasminogen activators. The presently used plasminogen activators are: Streptokinase- a protein synthesized by streptococci, combines with plasminogen to convert it to active plasmin. Urokinase-human enzyme synthesized by the kidneys that directly…