Selexa-400

White powders filled in white hard gelatin capsule.
Each capsule contains Celecoxib 400 mg.

Pharmacology: Pharmacodynamics: Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that is a selective inhibitor of cyclooxygenase-2 (COX-2). Celecoxib inhibits prostaglandin synthesis by decreasing the activity of the enzyme, COX-2, which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties. Celecoxib does not inhibit cyclooxygenase-1 (COX-1) at therapeutic concentrations.
Pharmacokinetics: Absorption: Celecoxib is well absorbed from gastrointestinal tract, peak plasma concentrations of the drug generally are attained within 3 hours after dosing in fasting individuals.
Distribution: The apparent volume of distribution of celecoxib at steady state is about 400 L (7.14 L/kg). At therapeutic plasma concentrations, celecoxib is about 97% bound to plasma protein.
Elimination: The plasma elimination half-life of celecoxib following oral administration of a single 200 mg dose under fasting conditions is about 11 hours, and the apparent clearance of the drug is about 500 mL/minute. Celecoxib is metabolized in liver to inactive metabolites principally by the cytochrome P-450 (CYP) isoenzyme 2C9. Celecoxib is excreted in urine (27%) and feces (57%); less than 3% of dose is excreted unchanged.

Symptomatic treatment of osteoarthritis (OA) and rheumatoid arthritis (RA).
Relief of signs and symptoms of ankylosing spondylitis (AS).
Management of acute pain; Treatment of primary dysmenorrhea.
Management of low back pain.

Recommended Dose: Celecoxib capsules, at doses up to 200 mg twice per day, can be taken with or without food. As the cardiovascular (CV) risks of celecoxib may increase with dose and duration of exposure, the shortest duration possible and the lowest effective daily dose should be used.
Symptomatic Treatment of Osteoarthritis (OA): The usual recommended dose of celecoxib is 200 mg administered as a single dose. In some patients, with insufficient relief from symptoms, and increased dose of 200 mg twice daily may increase efficacy. In the absence of an increase in therapeutic benefit after 2 weeks, other therapeutic options should be considered.
Symptomatic treatment of Rheumatoid Arthritis (RA): The recommended dose of celecoxib is 200 mg twice per day.
Ankylosing Spondylitis (AS): The recommended dose of celecoxib is 200 mg administered as a single dose. Some patients may benefit from a total daily dose of 400 mg.
Management of Acute Pain: The recommended dose of celecoxib is 400 mg initially, followed by an additional 200 mg dose, if needed on the first day. On subsequent days, the recommended dose is 200 mg twice daily or 400 mg once daily as needed.
Treatment of Primary Dysmenorrhea: The recommended dose of celecoxib is 400 mg, initially, followed by an additional 200 mg dose, if needed on the first day. On subsequent days, the recommended dose is 200 mg twice daily or 400 mg once daily as needed.
Low Back Pain (LBP): The recommended dose of celecoxib is 200 mg or 400 mg daily administered as a 200 mg single dose, or as 100 or 200 mg twice per day. Some patients may benefit from a total daily dose of 400 mg.
CYP2C9 Poor Metabolizers: Patients who are known, or suspected to be CYP2C9 poor metabolizers based on previous history/experience with other CYP2C9 substrates should be administered celecoxib with caution. Consider starting treatment at half the lowest recommended dose.
Elderly: No dosage adjustment is generally necessary. However, for elderly patients weighing lower than 50 kg, it is advisable to initiate therapy at the lowest recommended dose.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild hepatic impairment (Child-Pugh Class A). Introduce celecoxib at half the recommended dose in arthritis or pain patients with moderate hepatic impairment (Child-Pugh Class B).
Patients with severe hepatic impairment (Child-Pugh Class C) have not been studied.
Renal Impairment: No dosage adjustment is necessary in patients with mild or moderate renal impairment. There is no clinical experience in patients with severe renal impairment.
Co-administration with Fluconazole: Celecoxib should be introduced at half the recommended dose in patients receiving fluconazole, a CYP2C9 inhibitor. Caution is advised when co-administering celecoxib with other CYP2C9 inhibitors.
Pediatric Patients: Celecoxib has not been studied in subjects under 18 years of age.
Mode of Administration: Oral.

Overdose: Overdosage of NSAIDs can cause lethargy, drowsiness, nausea, vomiting and epigastric pain; these manifestations generally are reversible with supportive care. GI bleeding also has been reported. Rarely, hypertension, acute renal failure, respiratory depression and coma may occur. Anaphylactoid reactions have been reported with therapeutic use of NSAIDs and may occur following an overdosage.
Treatment: Treatment of NSAIDs overdosage involves symptomatic and supportive care; there is no specific antidote for NSAIDs overdosage. During the first 4 hours after overdosage, emesis and/or administration of activated charcoal (60-100 g in adults) and/or osmotic cathartic may be useful in symptomatic patients or in those who reportedly ingested a large overdosage.

Hypersensitivity to celecoxib, sulfonamides, or any component of the formulation.
Patients with asthma, urticarial, or other sensitivity reactions are precipitated by aspirin or other NSAIDs.
Celecoxib is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

Statement according to Announcement of Ministry of Public Health: Contraindicated in patients who are sensitive to this drug, pregnancy and lactating women.
Contraindicated in patients who have undergone immediate post-operative from CABG surgery.
Contraindicated in patients with cardiovascular or cerebrovascular diseases.
Contraindicated in patients with history of sulfonamides hypersensitivity due to the risk of severe skin adverse reactions.
Contraindicated in patients with myocardial infarction or congestive heart failure class NYHA II-IV.
Contraindicated in patients with history of coronary artery disease or paresis/paralysis from stroke.
Use with caution in patients with risk factors for cardiovascular disease such as hypertension, hyperlipidemia, diabetes mellitus, smoking, elderly etc.
Use with caution in patients with hepatic and renal impairment.
Cardiovascular: NSAIDs are associated with an increased risk of serious adverse cardiovascular thrombotic events, including Ml and stroke. Risk of cardiovascular events may be increased with duration of use or pre-existing cardiovascular risk factors or disease. Carefully evaluate individual cardiovascular risk profile prior to prescribing. New onset or exacerbation of hypertension may occur; may contribute to cardiovascular event. Celecoxib should be used with caution in patients with hypertension. Celecoxib may cause sodium and fluid retention. Celecoxib should be used with caution in patients with edema, cerebrovascular disease or ischemic heart disease.
GI: NSAIDs may increase risk of serious gastrointestinal ulceration, bleeding and perforation. Use caution with history of GI disease (bleeding or ulcer), concurrent therapy with aspirin, anticoagulants and/or corticosteroids, smoking.
Hepatic: Severe reactions, including jaundice and fatal fulminant hepatitis, liver necrosis and hepatic failure have been reported rarely in patients receiving NSAIDs. Celecoxib should be discontinued if clinical sign and symptoms consistent with liver disease develop.
Other: Use of corticosteroids during NSAIDs therapy may increase the risk of GI ulceration, the drugs should be used concomitantly with caution.
Anaphylactoid reactions may occur in patients receiving celecoxib, even without prior exposure.
Serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis) can occur in patients receiving celecoxib. These serious skin reactions can occur without warning and in patients without history of sulfonamide sensitivity reactions. Celecoxib should be discontinued at the first appearance of rash or any other sign of hypersensitivity.
Patient with asthma may have aspirin-sensitivity asthma; celecoxib should be used with caution in patient with asthma.

Pregnancy: Pregnancy category: C (prior to 30 weeks gestation)/D (≥30 weeks gestation).
The use of celecoxib is not recommended ≥30 weeks gestation.
Lactation: Celecoxib enters breast milk, use with caution.

At usual dosages, celecoxib generally is well tolerated. Adverse effects of celecoxib usually are mild and mainly involve the GI tract.
Adverse effects occurring in 2% or more of patients receiving celecoxib include peripheral edema, dizziness, fever, headache, insomnia, rash, abdominal pain, diarrhea, dyspepsia, flatulence, nausea, vomiting, arthralgia, back pain, cough, nasopharyngitis, pharyngitis, rhinitis, sinusitis and upper respiratory tract infection.

Fluconazole: Increase plasma concentrations of celecoxib.
Warfarin: Increased prothrombin time (mainly geriatric).
Antacid: Antacid containing magnesium or aluminium decreases peak plasma concentrations of celecoxib and area under the plasma-concentration-time curve (AUC).
May reduce the blood pressure response to ACE inhibitors or angiotensin II receptor antagonists.
Lithium: Celecoxib and other NSAIDs can decrease renal clearance of lithium, which may lead to increased serum or plasma lithium concentrations.
Nonsteroidal anti-inflammatory drugs: Concomitant use of 2 nonsteroidal anti-inflammatory agents may increase the incidence of GI-ulceration or other complications.

Store below 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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