Celecoxib

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Celecoxib.jpg

[edit] MECHANISM OF ACTION

Celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a noncompetitive inhibitor of cyclooxygenase-2 (COX-2) enzyme. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane.

Celecoxib metabolism is predominantly mediated via CYP2C9 in the liver

[edit] INDICATIONS

  • Osteoarthritis
  • Rheumatoid arthritis
  • Juvenile rheumatoid arthritis in patients 2 years and older
  • Ankylosing spondylitis
  • Acute Pain
  • Primary dysmenorrhea

[edit] DOSAGE

  • Osteoarthritis: 200 mg once daily or 100 mg twice daily
  • Rheumatoid arthritis: 100-200 mg twice daily
  • Juvenile rheumatoid arthritis in patients 2 years and older: 50 mg twice daily in patients 10-25 kg. 100 mg twice daily in patients more than 25 kg
  • Ankylosing spondylitis: 200 mg once daily or 100 mg twice daily. Max: 400 mg/day
  • Acute Pain and Primary dysmenorrhea: 400 mg initially, followed by 200 mg dose if needed on first day. On subsequent days, 200 mg twice daily as needed

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to celecoxib or sulfonamides
  • History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs
  • Use during the perioperative period in the setting of coronary artery bypass graft (CABG) surgery
  • Active gastrointestinal bleeding

[edit] WARNINGS AND PRECAUTIONS

  • Cardiovascular Thrombotic Events: Celecoxib may cause an increased risk of cardiovascular thrombotic events, myocardial infarction, and stroke. All nonsteroidal anti-inflammatory drugs (NSAIDs) may have a similar risk. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. To minimize the potential risk for an adverse cardiovascular event, the lowest effective dose should be used for the shortest duration consistent with individual patient treatment goals.
  • Hypertension: NSAIDs can lead to onset of new hypertension or worsening of preexisting hypertension, either of which may contribute to the increased incidence of cardiovascular events. Patients taking thiazides (Hydrochlorothiazide) or loop diuretics (Bumetanide, Etacrynic acid, Furosemide, Torasemide) may have impaired response to these therapies when taking NSAIDs. NSAIDs, including diclofenac, should be used with caution in patients with hypertension. Blood pressure (BP) should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.
  • Heart failure and edema: Fluid retention and edema have been observed in some patients taking NSAIDs, including Celecoxib, therefore caution is advised in patients with fluid retention or heart failure.
  • Gastrointestinal effects: NSAIDs, including Celecoxib, can cause serious gastrointestinal events including bleeding, ulceration, and perforation of the stomach, small intestine or large intestine, which can be fatal. The risk is greater in patients with a prior history of ulcer disease or GI bleeding, and in patients at high risk for GI events, especially the elderly. Celecoxib should be used with caution in these patients.
  • Hepatic Effects: Elevated liver enzymes and, rarely, severe hepatic reactions have been reported with celecoxib. Discontinue use of Celecoxib immediately if abnormal liver enzymes persist or worsen.
  • Renal Effects: Long-term administration of NSAIDs has resulted in renal papillary necrosis and other renal injury. Use Celecoxib with caution in the elderly, those with impaired renal function, heart failure, liver dysfunction, and those taking diuretics, ACE-inhibitors, or angiotensin II antagonists.
  • Anaphylactoid Reactions: Do not use Celecoxib in patients with the aspirin triad (nasal polyps, asthma and aspirin intolerance).
  • Skin Reactions: Rare cases of serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN), which can be fatal and can occur without warning even without known prior sulfa allergy, have been reported in patients receiving Celecoxib. Discontinue Celecoxib at first appearance of rash or skin reactions.

[edit] INTERACTIONS

  • Warfarin: increased risk of bleeding complications.
  • Lithium carbonate: Celecoxib increases lithium plasma levels
  • ACE Inhibitors and Angiotensin II antagonists: Celecoxib may reduce the antihypertensive effect. Concomitant use of Celecoxib with ACE Inhibitors in elderly or volume depleted or renally compromised patients may result in deterioration of renal function, including acute renal failure.
  • CYP2C9 inhibitors: concomitant use of CYP2C9 inhibitors, such as fluconazole, which can greatly elevate celecoxib serum levels. 200 mg of Fluconazole once daily resulted in a two-fold increase in celecoxib plasma concentration.
  • CYP2D6 sustrates: Celecoxib increases their plasma levels (Celecoxib is an inhibitor of CYP2D6)
  • The concurrent use of aspirin and Celecoxib increase the risk of serious GI events

[edit] PREGNANCY AND LACTATION

Celecoxib should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

In nursing mothers a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

  • Gastrointestinal symptoms (Abdominal pain, diarrhea, dyspepsia), lower incidence of GI ulcers than other NSAIDs

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib