Coxsafe
Generic Name
Celecoxib
Manufacturer
Various manufacturers (e.g., Square Pharmaceuticals Ltd. in Bangladesh)
Country
Global, specific to manufacturing country
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Description
Overview of the medicine
Coxsafe (Celecoxib) is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits cyclooxygenase-2 (COX-2) enzyme. It is used to relieve pain, swelling, and inflammation associated with various conditions like arthritis.
Uses & Indications
Dosage
Adults
Osteoarthritis: 200 mg once daily or 100 mg twice daily. Rheumatoid Arthritis: 100 mg or 200 mg twice daily. Ankylosing Spondylitis: 200 mg once daily or 100 mg twice daily, may increase to 400 mg daily. Acute Pain & Primary Dysmenorrhea: 400 mg initially, followed by 200 mg if needed on the first day, then 200 mg twice daily thereafter.
Elderly
No specific dose adjustment is generally required, but caution is advised, and starting with the lowest effective dose is recommended.
Renal_impairment
No specific studies in severe renal impairment. Use with caution in patients with mild to moderate renal impairment; not recommended in severe renal impairment.
How to Take
Take orally with or without food. Taking with food may help reduce gastrointestinal upset. Swallow the capsule whole with water.
Mechanism of Action
Celecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, which is primarily responsible for the synthesis of prostaglandins involved in inflammation, pain, and fever. By inhibiting COX-2, celecoxib reduces the production of these inflammatory mediators, thereby exerting its analgesic, anti-inflammatory, and antipyretic effects, while preserving the COX-1 enzyme which is responsible for gastric protection and platelet function.
Pharmacokinetics
Onset
Significant pain relief may occur within 30 minutes for acute pain, but full anti-inflammatory effects for chronic conditions may take 24-48 hours.
Excretion
Excreted predominantly in the feces (about 57%) and urine (about 27%) as metabolites; less than 3% is excreted as unchanged drug.
Half life
Approximately 8-12 hours.
Absorption
Well absorbed from the gastrointestinal tract, reaching peak plasma concentrations in approximately 2-3 hours after oral administration. Bioavailability is about 99%.
Metabolism
Extensively metabolized in the liver, primarily by cytochrome P450 2C9 (CYP2C9) to inactive metabolites. Individuals with poor CYP2C9 metabolism may have higher plasma levels.
Side Effects
Contraindications
- Hypersensitivity to celecoxib, sulfonamides, or any component of the formulation.
- History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs.
- Active peptic ulceration or gastrointestinal bleeding.
- Severe heart failure (NYHA Class IV).
- Advanced renal disease.
- Severe hepatic impairment.
- Third trimester of pregnancy.
- Peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
Drug Interactions
Lithium
May increase plasma lithium levels; monitor lithium levels.
Warfarin
Increased risk of bleeding, monitor INR.
Diuretics
May reduce the natriuretic effect of loop and thiazide diuretics.
Fluconazole
Potent CYP2C9 inhibitor, may significantly increase celecoxib plasma concentrations; reduce celecoxib dose by half.
Methotrexate
May increase methotrexate toxicity; caution advised.
ACE Inhibitors / Angiotensin Receptor Blockers (ARBs)
May diminish the antihypertensive effect; concurrent use may lead to renal impairment.
Storage
Store below 30°C in a dry place, away from light and moisture. Keep out of reach of children.
Overdose
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression, and coma may occur rarely. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs and may occur following an overdose. Treatment is symptomatic and supportive. There is no specific antidote. Forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion are unlikely to be useful due to high protein binding.
Pregnancy & Lactation
Pregnancy Category C in first and second trimesters, D in third trimester. Avoid celecoxib in late pregnancy due to potential for premature closure of the fetal ductus arteriosus. Use with caution early in pregnancy only if potential benefits outweigh risks. It is excreted into breast milk; use with caution in nursing mothers or consider alternative treatment.
Side Effects
Contraindications
- Hypersensitivity to celecoxib, sulfonamides, or any component of the formulation.
- History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs.
- Active peptic ulceration or gastrointestinal bleeding.
- Severe heart failure (NYHA Class IV).
- Advanced renal disease.
- Severe hepatic impairment.
- Third trimester of pregnancy.
- Peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
Drug Interactions
Lithium
May increase plasma lithium levels; monitor lithium levels.
Warfarin
Increased risk of bleeding, monitor INR.
Diuretics
May reduce the natriuretic effect of loop and thiazide diuretics.
Fluconazole
Potent CYP2C9 inhibitor, may significantly increase celecoxib plasma concentrations; reduce celecoxib dose by half.
Methotrexate
May increase methotrexate toxicity; caution advised.
ACE Inhibitors / Angiotensin Receptor Blockers (ARBs)
May diminish the antihypertensive effect; concurrent use may lead to renal impairment.
Storage
Store below 30°C in a dry place, away from light and moisture. Keep out of reach of children.
Overdose
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression, and coma may occur rarely. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs and may occur following an overdose. Treatment is symptomatic and supportive. There is no specific antidote. Forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion are unlikely to be useful due to high protein binding.
Pregnancy & Lactation
Pregnancy Category C in first and second trimesters, D in third trimester. Avoid celecoxib in late pregnancy due to potential for premature closure of the fetal ductus arteriosus. Use with caution early in pregnancy only if potential benefits outweigh risks. It is excreted into breast milk; use with caution in nursing mothers or consider alternative treatment.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 2-3 years, as indicated on the packaging.
Availability
Available in pharmacies and hospitals
Approval Status
Approved by regulatory bodies
Patent Status
Generic available
Clinical Trials
Numerous clinical trials have evaluated the efficacy and safety of celecoxib in various inflammatory conditions. The CLASS (Celecoxib Long-term Arthritis Safety Study) trial compared celecoxib with non-selective NSAIDs regarding gastrointestinal safety.
Lab Monitoring
- Renal function (BUN, creatinine) periodically, especially in patients with risk factors or on long-term therapy.
- Liver function (ALT, AST) periodically, especially with signs/symptoms of liver dysfunction.
- Complete blood count (CBC) if signs of GI bleeding or anemia are present.
- Blood pressure monitoring regularly, especially at initiation of treatment and during long-term therapy.
Doctor Notes
- Prescribe the lowest effective dose for the shortest possible duration consistent with individual patient treatment goals.
- Monitor patients for signs and symptoms of cardiovascular events, gastrointestinal bleeding, and renal dysfunction, especially during long-term therapy.
- Consider alternative pain management strategies or co-administration of gastroprotective agents for patients at high GI risk.
Patient Guidelines
- Take Coxsafe exactly as prescribed by your doctor. Do not exceed the recommended dose.
- Report any signs of stomach pain, black stools, or severe stomach upset to your doctor immediately.
- Be aware of the potential for cardiovascular events (heart attack, stroke) and discuss any risk factors with your doctor.
- Do not take other NSAIDs or aspirin concurrently without consulting your doctor.
- Inform your doctor about all other medications you are taking, including over-the-counter drugs and herbal supplements.
Missed Dose Advice
If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at once to make up for a missed dose.
Driving Precautions
Coxsafe may cause dizziness, drowsiness, or visual disturbances in some patients. If you experience these effects, avoid driving or operating machinery until you know how the medicine affects you.
Lifestyle Advice
- Avoid alcohol consumption and smoking, as these can increase the risk of gastrointestinal side effects.
- Maintain a healthy lifestyle with a balanced diet and regular exercise, as advised by your doctor.
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Global Brand Names
International brand names for this medicine. Click a brand to search for detailed information.
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