What is celecoxib? How does it work (mechanism of action)?
Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID), for example, ibuprofen (Motrin), aspirin, and naproxen (Naprosyn) used to treat arthritis, pain, menstrual cramps, and colonic polyps. Prostaglandins are chemicals that are important contributors to the inflammation of arthritis that causes pain, 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 other NSAIDs in 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 the genetic disease, familial adenomatous polyposis (FAP). In FAP, patients develop large numbers of polyps in their colons, and the polyps invariably become malignant. The only cure of FAP is removal of the entire colon. Celecoxib is approved as an adjunctive (secondary) treatment among patients with FAP. The cramping and pain during menstrual periods is due to prostaglandins, and blocking the production of prostaglandins with celecoxib reduces the cramps and pain.
The FDA approved celecoxib in December 1998.
What are the uses for celecoxib?
Celecoxib is used for the relief of pain, fever, swelling, and tenderness caused by osteoarthritis, juvenile arthritis, rheumatoid arthritis, and ankylosing 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. Celebrex also is also used for the relief of acute pain and the pain of menstrual cramps (primary dysmenorrhea).
What are the side effects of celecoxib?
The most common side effects of celecoxib include:
Other and more serious side effects of celecoxib include:
- Kidney failure
- Heart failure
- Aggravation of hypertension
- Chest pain
- Ringing in the ears
- Stomach and intestinal ulcers
- Blurred vision
- Weight gain
- Water retention
- Flu-like symptoms
- GERD (gastrointestinal reflux disease)
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 lead to increased bleeding time like other NSAIDs.
Allergic reactions can occur with celecoxib. Individuals who have developed allergic reactions (rash, itching, difficulty breathing) from sulfonamides (for example, sulfamethoxazole and trimethoprim [Bactrim]), aspirin or other NSAIDs may experience an allergic reaction to celecoxib and should not take celecoxib.
NSAIDs (except for low-dose aspirin) may increase the risk of heart attacks, stroke, and related conditions, which can be fatal. This risk may increase with duration of use and in patients who have underlying risk factors for heart and blood vessel conditions. NSAIDs should not be used for the treatment of pain resulting from coronary artery bypass graft (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.
What joints are most often affected by osteoarthritis?
What is the dosage for celecoxib?
The lowest effective dose should be used for each patient.
- For the management of osteoarthritis, the dose usually is 100 mg twice daily or 200 mg as a single dose.
- For rheumatoid 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.
Which drugs or supplements interact with celecoxib?
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 the liver. Therefore, treatment with celecoxib should be initiated at the lowest recommended doses in patients who are taking fluconazole.
Celecoxib increases the concentration of lithium (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 the anticoagulant (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.
Persons who drink more than three alcoholic beverages per day may be at increased risk of developing stomach ulcers when taking NSAIDs, and this also may be true with celecoxib.
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Is celecoxib safe to take if I’m pregnant or breastfeeding?
Celecoxib has not been studied in pregnant women. In animal studies, doses that were twice the maximally recommended dose were harmful to the fetus. It should not be used in late pregnancy because there is a risk of heart defects in the newborn. Celecoxib should only be used in pregnant women when the benefits outweigh the potential risk to the fetus.
What else should I know about celecoxib?
- Celecoxib is available as capsules: 50, 100, 200, and 400 mg. Capsules should be stored between 15 C and 30 C (59 F and 86 F).
- Celecoxib is available in generic form. You need a prescription to obtain this drug.
- The brand name for celecoxib available in the US is Celebrex.