VALDECOXIB

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DRUGS
VALDECOXIB

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.

Introduction

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)

Indications

  • Osteoarthritis

  • Rheumatoid arthritis

  • Primary dysmenorrhea

Pharamcological Action

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.

Dosage

  • Osteoarthritis or rheumatoid arthritis: 10 mg, once daily

  • Dysmenorrhea: 20 mg, twice daily

Pharmacokinetics

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.

Contraindications

  • Contraindicated in patients who have allergic-type reactions to sulfonamides.

  • Contraindicated in patients with known hypersensitivity to valdecoxib.

  • Contraindicated in patients who have experienced asthma, utricaria, or allergic reactions after taking aspirin or NSAIDs.

  • Contraindicated for the treatment of post-operative pain immediately, following coronary artery bypass graft (CABG) surgery and should not be used in this setting.

Drug Interactions

  • Concomitant administration of aspirin with valdecoxib may result in an increased risk of GI ulceration and complications compared to valdecoxib alone.

  • NSAIDs may diminish the antihypertensive effect of ACE-inhibitors.

  • NSAIDs can reduce the natriuretic effect of furosemide and thiazides in some patients.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Acid or sour stomach

  • Belching

  • Cough

  • Diarrhea

  • Ear congestion

  • Headache

  • Heartburn

  • Indigestion

  • Sore throat

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Abdominal fullness

  • Accidental injury

  • Back pain

  • Bloating

  • Excess gas

  • Rash

  • Stuffy or runny nose

Very rare (affecting less than 1 in 10,000)

  • Tightness in chest and/or wheezing

  • Troubled breathing

  • Unusual tiredness or weakness

  • Vomiting of blood or material that looks like coffee grounds

Precautions

  • Caution should be taken in patients with history of ulcer, GI bleeding; dehydration, high blood pressure, heart failure, fluid retention, liver or kidney disease, any allergy, during pregnancy and breastfeeding.

  • Monitor hemoglobin level regularly while taking this medication.

  • Avoid co-administration with ketoconazole or fluconazole.

  • Avoid excess dosage.

Clinic Evidence

  • 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

References

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