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Goodman & Gilman's The Pharmacological Basis of Therapeutics, 11e
| IV. Autacoids: Drug Therapy of Inflammation > |
Enolic Acids (Oxicams)
Sections: Enolic Acids
(Oxicams), Piroxicam, Pharmacological
Properties, Pharmacokinetics
and Metabolism, Therapeutic
Uses, Meloxicam, Other Oxicams, Nabumetone, Pharmacological
Properties, Pharmacokinetics
and Metabolism, Side Effects.
Topics Discussed: anti-inflammatory agents, non-steroidal; enolic acids; meloxicam; nabumetone; piroxicam.
Excerpt:
"The oxicam derivatives are enolic acids that inhibit COX-1 and
COX-2 and have antiinflammatory, analgesic, and antipyretic activity.
In general, they are nonselective COX inhibitors, although one member
(meloxicam) shows modest COX-2 selectivity comparable to celecoxib
in human blood in vitro and was approved
as a selective COX-2 inhibitor in some countries (see below). They are similar in efficacy
to aspirin, indomethacin, or naproxen for the long-term treatment
of rheumatoid arthritis or osteoarthritis. Controlled trials comparing
gastrointestinal tolerability with aspirin have not been performed.
The main advantage suggested for these compounds is their long half-life,
which permits once-a-day dosing.The pharmacological properties and therapeutic uses of piroxicam
have been reviewed (Guttadauria, 1986).Piroxicam is effective as an antiinflammatory agent.
It can inhibit activation of neutrophils, apparently independently
of its ability to inhibit cyclooxygenase; hence, additional modes
of antiinflammatory action have been proposed, including inhibition
of proteoglycanase and collagenase in cartilage. Approximately 20% of
patients experience side effects..."
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