Painex

Painex

celecoxib

Manufacturer:

Millimed

Distributor:

Prosp Pharma
Full Prescribing Info
Contents
Celecoxib.
Description
Each capsule contains Celecoxib 200 mg or 400 mg.
Action
Pharmacology: Pharmacodynamics: Celecoxib inhibits prostaglandin synthesis by decreasing the activity of the enzyme, cyclooxygenase-2 (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: Prolonged due to low solubility.
Distribution: Vd (apparent): Children and Adolescents ~7-16 years (steady-state): 8.3 ± 5.8 L/kg.
Adults: ~ 400 L.
Protein binding: ~97% primarily to albumin: binds to alpha1-acid glycoprotein to a lesser extent.
Metabolism: Hepatic via CYP2C9, form inactive metabolites (a primary alcohol, corresponding carboxylic acid, and its glucuronide conjugate).
Bioavailability: Absolute: Unkonown.
Half-life elimination: Children and Adolescents ~ 7-16 years (steady-state): 6 ± 2.7 hours (range: 3-10 hours); Adults: ~11 hours (fasted).
Time to peak: Children: Median: 3 hours (range: 1-5.8 hours); Adults: ~3 hours.
Excretion: Feces (~57% as metabolites, <3% as unchanged drug).
Urine (~27% as metabolites, <3% as unchanged drug).
Primary metabolites in feces and urine: Carboxylic acid metabolite (73% of dose); low amounts of glucuronide metabolite appear in urine.
Indications/Uses
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.
Dosage/Direction for Use
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, an 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: 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.
Renal Impairment: Mild or moderate impairment: There are no dosage adjustments.
Severe impairment: Use is not recommended.
Advanced renal disease: Use is not recommended.
Abnormal renal function tests (persistent or worsening): Discontinue use.
Hepatic Impairment: Mild impairment (Child-Pugh class A): No dose adjustment necessary.
Moderate impairment (Child-Pugh class B): Reduce dose by 50%.
Severe impairment (Child-Pugh class C): Use is not recommended.
Abnormal liver function tests (persistent or worsening): Discontinue use.
Mode of Administration: Celecoxib is administered orally as a single daily dose or in 2 equally divided doses daily. May be administered without regard to meals.
Overdosage
Limited information is available on the acute toxicity of celecoxib in humans. Serious toxicity was not observed in 12 individuals who received celecoxib 2.4 g daily for 10 days.
Manifestations: Overdosage of NSAIDs (nonsteroidal anti-inflammatory agents) 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 or 1-2 g/kg in children) and/or an osmotic cathartic may be useful in symptomatic patients or in those who reportedly ingested a large overdosage. It is not known whether celecoxib is removed by hemodialysis, but the drug's extensive protein binding suggests that forced diuresis, alkalinization of urine, hemodialysis, or hemoperfusion is likely to be ineffective in removing substantial amounts of celecoxib from the body.
Contraindications
Hypersensitivity to celecoxib, sulfonamides, aspirin, other NSAIDS, or any component of the formulation; patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAJDs; use in the setting of CABG surgery.
Warnings
Do not use in patients who have hypersensitivity to celecoxib, pregnant and lactating women.
Do not use in patients who have coronary artery surgery on immediately postoperative period.
Do not use in patients with cardiovascular or cerebrovascular diseases.
If use this medication, who have rash or symptomatic like common cold, should stop taking the medication and consult the doctor immediately.
Do not use in patients who have hypersensitivity to celecoxib and have history of sulfonamides hypersensitivity.
If use this medication, who have following signs and symptoms: fever, erythema rash, bullous, exfoliation of skin and mucous membranes e.g. oral cavity, throat, nasal, genital organ and conjunctivitis, should stop taking the medication and consult the doctor immediately because it can be drug allergy of Stevens-Johnson syndrome.
Do not use in patients who have myocardial infarction or congestive heart failure (NYHA II-IV).
Do not use in patents who have had ischemic heart disease or paresis, paralysis due to cerebrovascular accident.
Use with caution in patients with risk factors for developing coronary heart disease such as hypertension, hyperlipidemia, diabetes, smoking, elderly, etc.
Use with caution in patients with hepatic and renal disorder.
Special Precautions
NSAIDs cause an increased risk of serious (and potentially fatal) adverse cardiovascular thrombotic events, including MI and stroke. Risk may occur early during treatment and may increase with duration of use.
NSAIDs cause an increased risk of serious gastrointestinal inflammatory, ulceration, bleeding, and perforation (may be fatal); elderly patients and patients with history of peptic ulcer disease GI events. The events may occur at any time during therapy and with warning.
Use with caution in patients with decreased hepatic (dosage adjustments are recommended for moderate hepatic impairment; not recommended for patients with severe hepatic impairment) or renal function.
Patients with impaired renal function, dehydration, hypovolemia, heart failure, liver dysfunction, those taking diuretics, ACE inhibitors, angiotensin II receptor blockers, and the elderly are at greater risk for renal toxicity. Rehydrate patient before starting therapy; monitor renal function closely. Avoid use in patients with advanced renal disease; discontinue use with persistent or worsening abnormal renal function test. Long-term NSAID use may result in renal papillary necrosis.
Anemia may occur with use; monitor hemoglobin or hematocrit in patients on long-term treatment. Celecoxib does not affect PT, PTT or platelet count; does not inhibit platelet aggregation at approved doses. Potentially significant drug-drug interaction may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy.
Use In Pregnancy & Lactation
Pregnancy: Category C (less than 30 weeks' gestation).
Category D (starting at 30 weeks' gestation).
NSAIDs may cause premature closure of the ductus arteriosus, celecoxib should be avoided starting at 30-weeks gestation.
Celecoxib is a NSAID that primarily inhibits COX-2 whereas other available NSAIDs are nonselective for COX-1 and COX-2. The effects of this selective inhibition to the fetus have not been well studied and limited information is available specific to celecoxib.
Lactation: Celecoxib is present in breast milk. Most NSAIDs are excreted in breast milk. In general, do not use in breast-feeding mothers because of the possible adverse effects of prostaglandin-inhibiting drugs on neonates.
Adverse Reactions
Cardiovascular: Aggravated hypertension, coronary artery disorder (less than 2%); aortic valve incompetence, cerebral infarction, deep vein thrombosis, sinus bradycardia, ventricular hypertrophy (less than 1%); peripheral gangrene, thrombophlebitis, ventricular fibrillation (less than 0.1%).
CNS: Ataxia, suicide (less than 0.1%); fetal intracranial hemorrhage.
Dermatologic: Cellulitis, contact dermatitis, dermatitis, dry skin, rash erythematous, rash maculopapular, skin disorder, skin nodule (less than 2%).
GI: Upper Abdominal pain (8%); gastroesophageal reflux disease (4.7%); diverticulitis, dysphagia, hemorrhoids, hepatic function abnormal, hiatal hernia, tenesmus (less than 2%); cholelithiasis, colitis with bleeding, esophageal perforation, ileus, intestinal obstruction, intestinal perforation (less than 0.1%).
GU: Ovarian cyst (less than 1%).
Lab Test Abnormalities: Alkaline phosphatase increased, creatine phosphokinase increased (less than 2%); blood potassium increased, blood sodium increased, blood testosterone decreased (less than 1%).
Metabolic/Nutritional: Hypercholesterolemia, nonprotein nitrogen increase (less than 2%); hypoglycemia, hyponatremia.
Musculoskeletal: Arthrosis, leg cramps, synovitis, tendinitis (less than 2%); epicondylitis, tendon rupture (less than 1%).
Respiratory: Nasopharyngitis (6%); bronchospasm aggravated, laryngitis (less than 2%).
Special Senses: Deafness (less than 2%); conjunctival hemorrhage, labyrinthitis, vitreous floaters (less than 1%).
Miscellaneous: Injury and poisoning (6%); allergy aggravated, cyst NOS, hot flushes, peripheral pain (less than 2%); sepsis, sudden death (less than 0.1%).
Drug Interactions
Metabolism/Transport Effects Substrate of CYP2C9 (major), CYP3A4 (minor).
Inhibits CYP2C8 (moderate), CYP2D6 (weak).
Avoid Concomitant Use: Avoid concomitant use of Celecoxib with any of the following: Acemetacin; Aminolevulinic Acid (Systemic); Amodiaquine; Dexibuprofen; Dexketoprofen; Floctafenine; Ketorolac (Nasal); Ketorolac (Systemic); Macimorelin; Mecamylamine; Mifamurtide; Morniflumate; Nonsteroidal Anti-inflammatory Agents; Nonsteroidal Anti-inflammatory Agents (COX-2 Selective); Omacetaxine; Pelubiprofen; Phenylbutazone; Talniflumate; Tenoxicam; Zaltoprofen.
Increased Effect/Toxicity: Celecoxib may increase the levels/effects of: 5-Aminosalicylic Acid Derivatives; Ajmaline; Aliskiren; Aminoglycosides; Aminolevulinic Acid (Systemic); Aminolevulinic Acid (Topical); Amodiaquine; Anticoagulants; Aripiprazole; Bisphosphonate Derivatives; Cyclosporine (Systemic); CYP2C8 substrates (high risk with inhibitors); Deferasirox; Desmopressin; Dexibuprofen; Digoxin; Drospirenone; Eplerenone; Estrogen Derivatives; Haloperidol; Lithium; Mecamylamine; Methotrexate; Nonsteroidal Anti-inflammatory Agents (COX-2 Selective); Omacetaxine; Perhexiline; Porfimer; Potassium-Sparing Diuretics; Pralatrexate; Prilocaine; Quinolones; Selexipag; Sodium nitrate; Tacrolimus (Systemic); Tenofovir Products; Tolperisone; Triflusal; Vancomycin; Verteporfin; Vitamin K Antagonists.
The levels/effects of celecoxib may be increased by: Acemetacin; Alcohol (Ethyl);  Angiotensin II Receptor Blockers; Angiotensin-Converting Enzyme Inhibitors; Aspirin; Ceritinib; Corticosteroids (Systemic); Cyclosporine (Systemic); CYP2C9 inhibitors (Moderate); CYP2C9 inhibitors (Strong); Dapsone (Topical); Dexketoprofen; Felbinac; Floctafenine; Herbs (Anticoaguiant/Antiplatelet Properties); Ketorolac (Nasal); Ketorolac (Systemic); Loop Diuretics; Lumacaftor; Mifepristone; Morniflumate; Naftazone; Nitric Oxide; Nonsteroidal Anti-inflammatory Agents; Pelubiprofen; Phenylbutazone; Probenecid; Selective Serotonin Reuptake Inhibitors; Sodium Phosphates; Talniflumate; Tenoxicam; Tetracaine (Topical); Thiazide and Thiazide-Like Diuretics; Tolperisone; Tricyclic Antidepressants (Tertiary Amine); Triflusal; Zaltoprofen.
Decreased Effect: Celecoxib may decrease the levels/effects of: Aliskiren; Angiotensin II Receptor Blockers; Angiotensin­-Converting Enzyme Inhibitors; Beta-Blockers; Eplerenone; Hydralazine; Loop Diuretics; Macimorelin; Mifamurtide; Potassium-Sparing Diuretics; Prostaglandins (Ophthalmic); Selective Serotonin Reuptake Inhibitors; Thiazide and Thiazide-Like Diuretics.
The levels/effects of Celecoxib may be decreased by: Bile Acid Sequestrants; CYP2C9 Inducers (Moderate); Dabrafenib; Enzalutamide; Lumacaftor; Rifapentine.
Food Interactions: Peak concentrations are delayed and AUC is increased by 10% to 20% when taken with a high fat meal.
Storage
Store below 30°C.
ATC Classification
M01AH01 - celecoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Presentation/Packing
Cap 200 mg (opaque, white, no. 2 filled with white granular powder) x 3 x 10's. 400 mg (opaque, white, no. 0 filled with white granular powder) x 3 x 10's.
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