Drug information of Rofecoxib

Rofecoxib


Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks.

Mechanism of effect

The anti-inflammatory, analgesic, and antipyretic effects of NSAIDs appear to result from the inhibition of prostaglandin synthesis. Although the exact mechanism of action has not been determined, these effects appear to be mediated through the inhibition of the COX-2 isoenzyme at the sites of inflammation with subsequent reduction in the synthesis of certain prostaglandins from their arachidonic acid precursors. Rofecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, which is important for the mediation of inflammation and pain

Pharmacodynamic

Rofecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Unlike celecoxib, rofecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism. Like other NSAIDs, rofecoxib exhibits anti-inflammatory, analgesic, and antipyretic activity. NSAIDs appear to inhibit prostaglandin synthesis via the inhibition of cyclooxygenase (COX), which are responsible for catalyzing the formation of prostaglandins in the arachidonic acid pathyway. There are at least two isoenzymes, COX-1 and COX-2, that have been identified. Although the exact mechanisms have not been clearly established, NSAIDs exert their anti-inflammatory, analgesic, and antipyretic primarily through the inhibition of COX-2. The inhibition of COX-1 is principally

Pharmacokinetics

metabolism: hepatic

Drug indications

artirit rhomatoid , Pain , Migraine , Dysmenorrhea

For the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras.

Dosage

Usual Adult Dose for Osteoarthritis
12.5 mg orally once daily. May increase to a maximum of 25 mg orally once daily.
Usual Adult Dose for Rheumatoid Arthritis
25 to 50 mg orally once daily
Usual Adult Dose for Dysmenorrhea
50 mg orally once daily for no more than 5 days
Usual Adult Dose for Pain
50 mg orally once daily for no more than 5 days
Usual Adult Dose for Migraine
25 mg orally once daily. May increase to a maximum of 50 mg orally once daily.
Usual Pediatric Dose for Pain
3 to 11 years: 1 mg/kg oral suspension administered 45 minutes before induction of anesthesia.
Usual Pediatric Dose for Rheumatoid Arthritis
=>2 years to <=17 years:

>=10 to 42 kg; 0.6 mg /kg to a maximum of 25 mg oral suspension daily

>=42 kg: 25 mg orally daily

Drug contraindications

Allergies:

  • Salicylates
  • NSAIDS (Non-Steroidal Anti-Inflammatory Drug)

Side effects

Gastrointestinal
Gastrointestinal side effects have included diarrhea,

Alerts

RISK OF SERIOUS CARDIOVASCULAR AND GASTROINTESTINAL EVENTS
Cardiovascular Thrombotic Events
  • Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal.
  • VIOXX is contraindicated in the setting of coronary artery bypass graft (CABG) surgery
Gastrointestinal Bleeding, Ulceration, and Perforation

Points of recommendation

  • NSAIDs cause an increased risk of serious gastrointestinal (GI) adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients and patients with a prior history of peptic ulcer disease and/or GI bleeding are at greater risk for serious GI events

Pregnancy level

Group c - Not adequate studies in pregnant women

 

C

Breast feeding warning

There is no data on the excretion of rofecoxib into human milk

Related drugs

Celecoxib , Parecoxib

celecoxib

Drug forms

vioxx

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