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Valdecoxib is a
sulfonamide derivative and non-steroidal anti-inflammatory drug (NSAID) with
anti-inflammatory, analgesic, and antipyretic activities.
Valdecoxib is a sulfonamide derivative and non-steroidal
anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and
antipyretic activities. Valdecoxib is used to reduce pain, inflammation, and
stiffness caused by osteoarthritis and adult rheumatoid arthritis. It is also
used to treat painful menstruation.
Pharmacological
class: NSAID (COX-2 Inhibitor)
Both COX-1 and COX-2 catalyze the conversion of arachidonic
acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib
selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the
mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does
not inhibit platelet aggregation.
Valdecoxib achieves maximal plasma concentrations in
approximately 3 hours. The absolute bioavailability of valdecoxib is 83%,
following oral administration. Plasma protein binding for valdecoxib is about
98% over the concentration range (21–2384 ng/mL). It undergoes extensive
hepatic metabolism involving both P450 isoenzymes (3A4 and 2C9) and non-P450 dependent
pathways (i.e., glucuronidation). Valdecoxib is eliminated predominantly via
hepatic metabolism with less than 5% of the dose excreted unchanged in the
urine and feces.
Common (affecting between 1
in 10 to 1 in 100):
Uncommon (affecting 1 in 100 to 1 in 1000):
Very rare (affecting less than 1 in 10,000):
In 10 large, well-controlled, randomized trials (n = 203 to 1089), valdecoxib was significantly more effective than placebo in treating osteoarthritis, rheumatoid arthritis and pain associated with primary dysmenorrhea, and for postsurgical analgesia. Valdecoxib, 1.25 to 10 mg twice daily and valdecoxib 10 mg once daily were more effective than placebo for the relief of pain in patients with osteoarthritis of knee, and dosages above 5 mg twice daily were similar in efficacy to naproxen 500 mg twice daily. Similarly, valdecoxib 5 and 10 mg/day were as effective for osteoarthritis of the hip as naproxen 500 mg twice daily. In patients with rheumatoid arthritis, valdecoxib 10, 20 or 40 mg/day was significantly more effective than placebo, and similar in efficacy to naproxen 500 mg twice daily.1
Total 14 clinical studies involving > 4000 patients have
been conducted. Valdecoxib was significantly more effective than placebo in
treating adult rheumatoid arthritis, osteoarthritis, pain associated with
primary dysmenorrhea, and postoperative pain. Valdecoxib was comparable to naproxen
for treating rheumatoid arthritis in 1 study and equivalent to naproxen for
treating osteoarthritis in other studies. Three studies found valdecoxib
comparable to naproxen sodium for the relief of moderate to severe pain due to
primary dysmenorrhea, and others found valdecoxib comparable to oxycodone plus
acetaminophen and significantly more effective than rofecoxib for the relief of
pain associated with dental surgery (P < 0.05).2
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