Each hard gelatin capsule contains:
Celecoxib …………………………………100 mg
Celecoxib, a selective cyclooxygenase-2(COX-2) inhibitor is classified as a non-steroidal anti-inflammatory drug (NSAID). Celecoxib is used to treat rheumatoid arthritis, osteoarthritis and familial adenomatous polyposis (FAP). Because of its lack of platelet effects, celecoxib is not a substitute for aspirin for cardiovascular prophylaxis. It is not known if there are any effects of celecoxib on platelets that may contribute to the increased risk of serious cardiovascular thrombotic adverse events associated with the use of celecoxib. Inhibition of PGE2 synthesis may lead to sodium and water retention through increased reabsorption in the renal medullary thick ascending loop of Henle and perhaps other segments of the distal nephron. In the collection ducts, PGE2 appears to inhibit water reabsorption by counteracting the action of antidiuretic hormone.
MECHANISM OF ACTION
The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a selective noncompetitive inhibitor of cyclooxygenase-2 (COX-2) enzyme. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region close to the active COX-2 binding site. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane.
For relief and management of osteoarthritis (OA), rheumatoid arthritis (RA), ankylosing spondylitis, acute pain, primary dysmenorrhea and oral adjunct to usual care for patients with familial adenomatous polyposis.
DOSAGE AND ADMINISTRATION
For ankylosing spondylitis
Adults: 200 mg once a day or 100 mg twice a day. Dose may be increased to 400 mg a day after 6 weeks if no effect is observed.
For familial adenomatous polyposis (polyps in the intestines)
Adults: 400 mg twice a day with food
For moderate or severe pain, such as after dental or orthopedic procedures
Adults: on the first day take 400 mg for the first dose then 200 mg as needed as a second dose. After the first day take 200 mg twice a day.
For pain during menstruation
On the first day take 400 mg for the first dose then 200 mg as needed as a second dose. After the first day take 200 mg twice a day.
For rheumatoid arthritis
100 to 200 mg twice a day
Adults: 200 mg a day as a single dose or 100 mg twice a day
Children: use and dose must be determined by the doctor
Celecoxib is contraindicated in patients with known hypersensitivity to celecoxib. Celecoxib should not be given to patients who have demonstrated allergic-type reactions to sulfonamides. Celecoxib should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Sever, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients. Celecoxib is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
Not to be given to those who have a history of:
- Stroke cerebrovascular accident. CVA
- Heart attack: myocardial infarction. MD
- Uncontrolled hypertension
- Congestive heart failure (CHF) NYHA II-IV
Cough, fever, skin rash, sneezing, sore throat, swelling of face, fingers, feet, and/or lower legs, abnormal growth in breast, arm, back or jaw pain, bloody or black tarry stools, blurred vision, burning feeling in chest or stomach, burning or stinging of skin, burning, tingling, numbness or pain in the hands, arms, feet, or legs, chest pain or discomfort, chest tightness or heaviness, chills, confusion, congestion in chest, cough, diarrhea, cramps, dry mouth, earache, fast or irregular heartbeat, fatigue, fever, heartburn, heavy bleeding, heavy nonmenstrual vaginal bleeding, high blood pressure, increased hunger, increased urination; loss of appetite, loss of consciousness, muscle aches and pains, nausea, nerve pain, painful blisters on trunk of body, painful cold sores or blisters on lips, nose, eyes, or genitals, pale skin, redness or swelling in ear, sensation of pins and needles, shortness of breath, sore throat, soreness or redness around fingernails and toenails, stiff neck, stomachache, stabbing pain, stomach pain (severe), sweating, tenderness in stomach area, troubled breathing with exertion, unexplained weight loss, unusual bleeding or bruising, unusual tiredness or weakness, unusual weight gain, vomiting of blood or material that looks like coffee grounds, wheezing, weakness.
- COX-2 inhibitors are not to be given to patients with allergy to NSAIDs and those with asthma
- Exercise caution when prescribing selective COX-2 inhibitors in patients with ischemic heart disease and those with asthma
- Considering association between cardiovascular risk and exposure to COX-2 inhibitors, doctors are advised to use the lowest effective dose for the shortest duration of treatment.
- Intake of COX-2 inhibitors should be stopped with appearance of skin rash and signs of hypersensitivity
- If not yet instituted, warning statement should include potential gastrointestinal (gastric and liver) and renal toxicities.
Taking two or more of the non-steroidal anti-inflammatory drugs together on a regular basis may increase the chance of unwanted effects. Also taking acetaminophen, aspirin or other salicylates, or ketorolac (e.g. Toradol) regularly while you are taking a non-steroidal anti-inflammatory drug may increase the chance of unwanted effects. Serious side effects can occur during treatment with this medicine. Sometimes serious side effects can occur without warning. However, possible warning signs often occur, including swelling of the face, fingers, feet, and/or lower legs, severe stomach pain, black tarry tools, and/or vomiting of blood or material that looks like coffee grounds, unusual weight gain, and/or skin rash. Also signs of serious heart problems could occur such as chest pain, tightness in chest, fast or irregular heartbeat, or unusual flushing or warmth of skin.
ACE inhibitors: Reports suggest that NSAIDs may diminish the antihypertensive effect of Angiotensin Converting Enzyme (ACE) inhibitors.
Furosemide: This response has been attributed to inhibition of renal prostaglandin synthesis.
Aspirin: Celecoxib can be used with low dose aspirin. However, concomitant administration of aspirin with celecoxib may result in an increased rate of GI ulceration or other complications.
Fluconazole: Concomitant administration of fluconazole at 200 mg QID resulted in a two-fold increase in celecoxib plasma concentration.
Lithium: In a study conducted in healthy subjects, mean steady-state lithium plasma levels increased approximately 17% in subjects receiving lithium 450 mg BID with celecoxib 200 mg BID as compared to subjects receiving lithium alone.
Methotrexate: In an interaction study of rheumatoid arthritis patients taking methotrexate, celecoxib did not have a significant effect on the pharmacokinetics of methotrexate.
Warfarin: Caution should be used when administering celecoxib with warfarin since these patients are at increased risk of bleeding complications.
Symptoms of overdose include breathing difficulties, coma, drowsiness, gastrointestinal bleeding, high blood pressure, kidney failure, nausea, sluggishness, stomach pain and vomiting.
PREGNANCY AND LACTATION
Celecoxib has not been studied in pregnant women. However, there is a chance that this medicine may cause unwanted eff3ects on the heart of blood flow of the fetus or newborn baby if it is taken regularly during the last few months of pregnancy.
It is not known whether celecoxib passes into breast milk. However, celecoxib may cause unwanted effects in nursing babies. It may be necessary for you to take another medicine or to stop breast-feeding during treatment.
Studies on this medicine have been done only in adult patients, and there is no specific information comparing the use of celecoxib in children with use in older age groups.
This medicine has been tested in a limited number of elderly patients 65 years of age and older and has not been shown to cause different side effects or problems in older people than it does in younger adults.
Alu-Pvc Blister Pack of 10’s (Box of 30’s)
Store at temperatures not exceeding 30°C. Protect from light.
KEEP OUT OF REACH OR CHILDREN.