Coxbitor 200

Celecoxib (Coxbitor 200) 200 mg Capsule: Each hard gelatin capsule with pink cap and light gray body contains 200 mg of Celecoxib 200 mg.

Pharmacotherapeutic group: M01AH Coxibs.
Pharmacology: Pharmacodynamics: The mechanism of action of celecoxib is via inhibition of prostaglandin synthesis primarily by inhibition of cyclooxygenase 2 (COX-2). At therapeutic concentrations in humans, celecoxib does not inhibit cyclooxygenase 1 (COX-1). COX-2 is induced in response to inflammatory stimuli. This leads to the synthesis and accumulation of inflammatory prostanoids, in particular prostaglandin E2, causing inflammation, edema and pain. Celecoxib acts as an anti-inflammatory, analgesic, and antipyretic agent in animal models by blocking the production of inflammatory prostanoids via COX-2 inhibition. In animal colon tumor models, celecoxib reduced the incidence and multiplicity of tumors.
In vivo and ex vivo studies show that celecoxib has a very low affinity for the constitutively expressed cyclooxygenase 1 enzyme (COX-1). Consequently, at therapeutic doses, celecoxib has no effect on prostanoids synthesized by activation of COX-1 thereby not interfering with normal COX-1 related physiological processes in tissues, particularly stomach, intestine and platelets.
Pharmacokinetics: Celecoxib is absorbed from the gastrointestinal tract; peak plasma concentrations being achieved after about 3 hours. Protein binding is about 97%. Celecoxib is metabolized in the liver mainly by the cytochrome P450 isoenzyme CYP2C9; the three identified metabolites are inactive as inhibitors of COX-1 or COX-2 enzymes. It is eliminated mainly as metabolites in the feces and urine; less than 3% is recovered as unchanged drug. The effective terminal half-life is about 11 hours. Celecoxib is distributed into breast milk. The pharmacokinetics of celecoxib may vary in different ethnic groups; it has been stated that the area under the curve is elevated in patients of Afro-Caribbean origin, although any clinical significance is unclear.

Celecoxib is an NSAID reported to be a selective inhibitor of cyclooxygenase-2 (COX-2). It is used in the treatment of rheumatoid arthritis including juvenile idiopathic arthritis, osteoarthritis, and ankylosing spondylitis, and in the adjunctive treatment of adenomatous colorectal polyps. Celecoxib is also used in the management of acute pain and dysmenorrhea.

For osteoarthritis: Adult: 200 mg daily given as a single dose or in 2 divided doses. If necessary, a dose of 200 mg twice daily may be used.
For rheumatoid arthritis: Adult: 100 to 200 mg given twice daily.
For ankylosing spondylitis: Adult: an initial dose of 200 mg daily, as a single dose or in 2 divided doses.
In the treatment of pain and dysmenorrhea: Adult: an initial dose of 400 mg followed by an additional dose of 200 mg, if necessary, is recommended on the first day; thereafter the dose is 200 mg twice daily.
As an adjunctive treatment of adenomatous colorectal polyps: Adult: may be given in doses of 400 mg twice daily with food.
Reduced doses are recommended in patients with hepatic impairments. Or as prescribed by a physician.

Clinical experience of overdose is limited. Single doses up to 1200 mg and multiple doses up to 1200 mg twice daily have been administered to healthy subjects without clinically significant adverse effects. In the event of suspected overdose, appropriate supportive medical care should be provided. Dialysis is unlikely to be an efficient method of drug removal because of high protein binding of the drug.

Absolute contraindications: Not to be given to those patients who have history of: Stroke: cerebrovascular accident, CVA.
Heart attack: Myocardial infarction, MI.
Coronary artery bypass graft: CABG.
Uncontrolled hypertension.
Congestive heart failure (CHF) NYHA II-IV.
Therapy is contraindicated in patients with moderate to severe heart failure (NYHA class II to IV), inflammatory bowel disease, and renal impairment associated with a creatinine clearance of less than 30 mL/minute. Celecoxib should also not be used in patients with severe hepatic impairment (Child-Pugh category C). Caution is recommended when using celecoxib in dehydrated patients; rehydration may be advisable before giving celecoxib. Celecoxib treatment may need to be stopped if signs or symptoms of organ toxicity develop.

Celecoxib should not be used after coronary artery bypass surgery as there may be an increased risk of adverse effects such as myocardial infarction and stroke. It should be used with caution, if at all, in patients with a history of ischemic heart disease, peripheral arterial disease, or cerebrovascular disease; it should also be used with caution in patients with significant risk factors for cardiovascular disease such as hypertension, hyperlipidemia, and diabetes mellitus. Celecoxib is not given to patients with allergy to NSAIDs and those with asthma. Use the lowest effective dose for the shortest duration of treatment. Intake of celecoxib should be stopped with appearance of skin rash and signs of hypersensitivity.
Use in the Elderly (> 65 years of age): In the elderly, frail and debilitated, the dosage should be reduced to the lowest level providing control of symptoms and adjusted when necessary.

There are no studies in pregnant women. Studies in animals have shown reproductive toxicity. The relevance of these data for humans is unknown. Celecoxib, as with other drugs inhibiting prostaglandin synthesis, may cause uterine inertia and premature closure of the ductus arteriosus and should be avoided during the third trimester of pregnancy. Celecoxib should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.
Studies in rats show that celecoxib is excreted in milk at concentrations similar to those in plasma. Administration of celecoxib to lactating women has shown very low transfer of celecoxib into breast milk. Because of the potential for adverse reactions in nursing infants from celecoxib, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the expected benefit of the drug to the mother.

Serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis have been reported with celecoxib. Other hypersensitivity reactions, including anaphylaxis and angioedema, have also occurred. Celecoxib should be stopped at the first signs of hypersensitivity. Some of these reactions have been seen in patients with a history of allergic reactions to sulfonamides and the use of celecoxib is contraindicated in such patients.

The metabolism of celecoxib is mediated mainly by the cytochrome P450 isoenzyme CYP2C9. Use with other drugs that inhibit or induce or are metabolized by this isoenzyme may result in changes in plasma concentration of celecoxib; fluconazole has increased plasma concentrations of celecoxib and it is recommended that the dose of celecoxib should be halved when given with fluconazole. Celecoxib is an inhibitor of the isoenzyme CYP2D6 and the potential therefore exists for an effect on drugs metabolized by this enzyme.

Store at temperatures not exceeding 30°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AH01 - celecoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.

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