How Vioxx Works
Non-steroidal anti-inflammatory drugs (NSAIDs) are prescribed to patients who suffer from arthritis and pain. The most common adverse side effect from taking these medicines is gastrointestinal toxicity. Non-selective NSAIDs decrease pain and inflammation through halting the activity of both COX-1 and COX-2 enzymes.
Vioxx is apart of a new class of NSAIDs, 'super aspirins' or COX 2 selective inhibitors. COX 2 selective drugs, also including Bextra and Celebrex were created as an alternative to non-selective NSAIDs to decrease stomach, kidney and gastrointestinal problems commonly associated with these drugs. The mechanism of action of Vioxx and other drugs in the same class is believed to be through strictly inhibiting cyclooxygenase 2, the enzyme that is primarily responsible for inflammation and pain. Inhibiting strictly COX 2 enzymes creates an imbalance in favor of COX 1 enzymes resulting in a greater likelihood for platelet aggregation and endothelial constriction. Although COX-2 enzyme activity is notorious for inducing symptoms of inflammation and pain, these enzymes also act as natural blood thinners and vasodialators preventing cardiovascular adverse such as heart attacks and strokes. Patients taking COX-2 selective inhibitors (Vioxx, Celebrex and Bextra) may be trading GI risks for cardiovascular risks.
Although COX-2 selective drugs differ structurally from non-selective NSAIDs, they virtually have the same gastrointestinal toxicity risks. COX-2 selective inhibitors in addition to non-selective NSAIDs also creates increased cardiovascular risk and with the drugs Bextra and Celebrex (in some patients) severe skin disorders.
After ingesting the drug Vioxx (rofecoxib), it stays within your body (regardless of gender) for a maximum of 9 days at steady-state levels and the maximum concentrations are reached generally after 2-3 hours. Rofecoxib has low solubility in aqueous pathways.
Cyclooxygenase activates arachidonic acid that then creates the synthesis of prostaglandins. Prostaglandins are the mediators for many functions throughout the body, but the drug Vioxx specifically stops the enzymic activity of COX-2 that mediates the production of prostaglandin that causes inflammation, pain and fever. However when inhibiting specifically COX-2 it also inhibits Prostaglandin I2 (PGI2) that was found by Dr. Garret A. FitzGerald to vasodilate smooth muscle and prevents aggregation of platelets.
The VIGOR study, conducted by Vioxx’s manufacturer, Merck, confirmed serious cardiovascular adverse events may occur as soon as four months after chronic use.
Vioxx prescription labeling was changed in April 2002 to include the mention of dangerous cardiovascular side effects and to also expand its prescribing indication to patients who suffer from rheumatoid arthritis.
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