Pharmacology Book

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Rofecoxib

Aka: Rofecoxib, Vioxx
  1. See Also
    1. COX2 Inhibitor
    2. Celecoxib
  2. Precaution
    1. Vioxx voluntarily withdrawn from market October 2004
      1. Withdrawal due to increased risk of MI and CVA
  3. Class
    1. NSAID: COX2 Inhibitor
    2. Similar to Celecoxib (Celebrex)
  4. Advantages
    1. Less gastrointestinal adverse effects than other NSAIDs
      1. See NSAID Gastrointestinal Adverse Effects
    2. Appears safe in Aspirin and NSAID-induced Asthma
      1. Martin-Garcia (2002) Chest 121:1812-7 [PubMed]
  5. Dosing
    1. Osteoarthritis: 12.5 to 25 mg PO qd
    2. Acute pain or Dysmenorrhea: 50 mg PO qd
  6. Pharmacokinetics
    1. Oral Bioavailability: 92%
    2. Peaks: 2-3 hours (delayed by food intake)
    3. Half life: 17 hours
    4. Metabolized by hepatic reduction
    5. Factors increasing serum concentrations
      1. Age over 65 years old
      2. Hepatic insufficiency
  7. Efficacy: Equivalent analgesia to 50 mg Vioxx
    1. Ibuprofen 400 mg
    2. NaproxenSodium (e.g. Anaprox) 550 mg
  8. Drug Interactions
    1. Decreased Vioxx serum concentrations
      1. Antacids (decrease Vioxx serum concentrations 20%)
      2. Rifampin (decrease Vioxx serum concentrations 50%)
    2. Increased concentrations of other medications
      1. Raises serum Methotrexate levels 23%
      2. Raises Warfarin levels - increases ProTime 10%
  9. Adverse Effects
    1. See COX-2 Inhibitor for Nonfatal MI risk
      1. Confirmed in larger trial and withdrawn from market
    2. Diarrhea
    3. Nausea
    4. Dyspepsia
    5. Abdominal Pain
    6. Lower extremity edema
    7. Increased Blood Pressure
  10. References
    1. Daniels (1999) Clin Pharmacol Ther 65:118 [PubMed]
    2. Ehrich (1999) Clin Pharmacol Ther 65:336 [PubMed]
    3. Fricke (1999) Clin Pharmacol Ther 65:119 [PubMed]
    4. (1999) Med Lett Drugs Ther 41(1056): 59-61 [PubMed]

rofecoxib (C0762662)

Definition (NCI_NCI-GLOSS) A drug that was being used for pain relief and was being studied for its ability to prevent cancer and to prevent the growth of new blood vessels that tumors need to grow. It is a type of nonsteroidal anti-inflammatory drug and a type of antiangiogenesis agent. Rofecoxib was taken off the market in the U.S. because of safety concerns.
Definition (NCI) A synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2. (NCI04)
Definition (PDQ) A synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=38568&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=38568&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1832" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C116926
SnomedCT 363596000, 116095002, 387008005
LNC LP171636-6
English 4-[4'-(Methylsulfonyl)phenyl]-3-phenyl-2(5H)-furanone, rofecoxib (medication), rofecoxib, rofecoxib [Chemical/Ingredient], Rofecoxib product (substance), Rofecoxib product, Rofecoxib (product), Rofecoxib (substance), Rofecoxib, 4-(4-methylsulfonylphenyl)-3-phenyl-5H-furan-2-one, ROFECOXIB
Spanish rofecoxib (producto), rofecoxib (sustancia), rofecoxib
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Vioxx (C0876768)

Definition (CHV) a kind of nonsteroidal anti-inflammatory drugs
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C116926
English Vioxx, vioxx, Cahill May Roberts brand of rofecoxib, MSD brand of rofecoxib, Merck Frosst brand of rofecoxib, Merck Sharp & Dhome brand of rofecoxib, Merck brand of rofecoxib, Vioxx Dolor
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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