celecoxib (Celebrex)

Brand name: Celebrex
Generic name: celecoxib
Dosage forms: capsules (50, 100, 200, and 400 mg)
Drug Class: NSAIDs

Celecoxib is anonsteroidal anti-inflammatory drug(NSAID), for example,ibuprofen(Motrin),aspirin, andnaproxen(Naprosyn) used to treatarthritis,pain,menstrual cramps,结肠息肉。

Prostaglandins are chemicals that are important contributors to the inflammation ofarthritisthat causespain,fever, swelling, and tenderness. Celecoxib blocks the enzyme that makes prostaglandins (cyclooxygenase 2), resulting in lower concentrations of prostaglandins. As a consequence, inflammation and its accompanying pain,fever, swelling, and tenderness are reduced. Celecoxib differs from otherNSAIDsin that it causes less inflammation and ulceration of the stomach and intestine (at least with short-term use) and does not interfere with the clotting of blood.

NSAIDs have been found to prevent the formation and reduce the size of polyps in patients with thegenetic disease,familial adenomatous polyposis(FAP). In FAP, patients develop large numbers of polyps in their colons, and the polyps invariably becomemalignant.

The only cure for FAP is the removal of the entire colon. Celecoxib is approved as an adjunctive (secondary) treatment among patients with FAP. The cramping and pain during menstrual periods are due to prostaglandins, and blocking the production of prostaglandins with celecoxib reduces thecrampsand pain.

Celecoxib uses and conditions it treats

• Celecoxib is used for the relief of pain, fever, swelling, and tenderness caused byosteoarthritis, juvenile arthritis,rheumatoid arthritis, andankylosing spondylitis.
• Celecoxib does not prevent the progression of either type of arthritis. It reduces only the symptoms and signs of arthritis.
• Celecoxib is also approved for patients with familial FAP who have not had their colons removed.
• 西乐葆还也用于缓解急性pain and the pain ofmenstrual cramps(primarydysmenorrhea).

WARNING

RISK OF SERIOUS CARDIOVASCULAR AND GASTROINTESTINAL EVENTS

Cardiovascular Thrombotic Events

• Nonsteroidal anti-inflammatorydrugs(NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, includingmyocardial infarction, andstroke, which can be fatal. This risk may occur early in the treatment and may increase with the duration of use.
• Celecoxib is contraindicated in the setting ofcoronary artery bypass graft(CABG) surgery.

Gastrointestinal Bleeding, Ulceration, and Perforation

• NSAIDs cause an increased risk of serious gastrointestinal (GI) adverse events including bleeding, ulceration, and perforation of the stomach orintestines, 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 ofpeptic ulcerdisease and/orGI bleedingare at greater risk for serious (GI) events.

The most common side effects of celecoxib include:

• Headache
• Abdominal pain
• Indigestion(dyspepsia)
• Diarrhea
• Nausea
• Flatulence(gas)
• Insomnia

Other and more serious side effects of celecoxib include:

• Fainting
• Vomiting
• Kidney failure
• 心failure
• Aggravation ofhypertension
• Chest pain
• Ringing in the ears
• Deafness
• Stomach and intestinal ulcers
• Bleeding
• Blurred vision
• Anxiety
• Photosensitivity
• Weight gain
• Water retention
• Flu-like symptoms
• Fever
• Cough
• GERD(gastrointestinal reflux disease)
• Rash
• Drowsiness
• Weakness

Other adverse reactions

Celecoxib, like other NSAIDs, may cause serious stomach and intestinal ulcers that may occur at any time during treatment. Celecoxib does not interfere with the function of the blood platelets and, as a result, does not reduce clotting and leads to increased bleeding time like other NSAIDs.

Allergicreactions can occur with celecoxib. Individuals who have developed allergic reactions (rash,itching, difficultybreathing) fromsulfonamides(for example,sulfamethoxazole and trimethoprim[Bactrim]), aspirin, or other NSAIDs may experience anallergic reactionto celecoxib and should not take celecoxib.

NSAIDs (except for low-dose aspirin) may increase the risk ofheart attacks,stroke, and related conditions, which can be fatal. This risk may increase with the duration of use and in patients who have underlying risk factors forheartand blood vessel conditions. NSAIDs should not be used for the treatment of pain resulting fromcoronary artery bypassgraft (CABG) surgery.

NSAIDs cause an increased risk of serious, even fatal, stomach and intestinal adverse reactions such as bleeding, ulcers, and perforation of the stomach or intestines. These events can occur at any time during treatment and without warning symptoms. Elderly patients are at greater risk for these types of reactions.

The lowest effective dose should be used for each patient.

• For the management ofosteoarthritis, the dose usually is 100 mg twice daily or 200 mg as a single dose.
• Forrheumatoid arthritis, the dose usually is 200 mg twice daily.
• For acute pain or menstrual cramps, the dose is 400 mg as a single dose on the first day followed by an additional 200 mg if needed, then 200 mg twice daily as needed.
• For FAP, the recommended dose is 400 mg twice daily.

• Concomitant use of celecoxib with aspirin or other NSAIDs (for example, ibuprofen, naproxen, etc.) may increase the occurrence of stomach and intestinal ulcers. It may be used with low-dose aspirin.
• Fluconazole(Diflucan) increases the concentration of celecoxib in the body by preventing the elimination of celecoxib in theliver. Therefore, treatment with celecoxib should be initiated at the lowest recommended doses in patients who are taking fluconazole.
• Celecoxib increases the concentration oflithium(Eskalith,Lithobid) in the blood by 17% and may promote lithium toxicity. Therefore, lithium therapy should be closely monitored during and after therapy with celecoxib.
• Persons taking theanticoagulant(blood thinner)warfarin(Coumadin) should have their blood tested when initiating or changing celecoxib treatment, particularly in the first few days, for any changes in the effects of the anticoagulant.
• NSAIDs may reduce the官网地址bwin-lowering effects of drugs that are given to reduce blood pressure. This may occur because prostaglandins play a role in the regulation of blood pressure.
• Persons who drink more than three alcoholicbeveragesper day may be at increased risk of developing stomach ulcers when taking NSAIDs, and this also may be true with celecoxib.

• Celecoxib has not been studied inpregnantwomen. In animal studies, doses that were twice the maximally recommended dose were harmful to the fetus.
• It should not be used in latepregnancybecause there is a risk of heart defects in thenewborn.
• Celecoxib should only be used inpregnantwomen when the benefits outweigh the potential risk to the fetus.
• Available evidence suggests that celecoxib is secreted inbreast milk.
• Nursingmothers should avoid celecoxib or discontinuebreastfeeding.