Coxid

Coxid

celecoxib

Manufacturer:

Westmont

Distributor:

United Lab
Full Prescribing Info
Contents
Celecoxib.
Action
Pharmacology: Celecoxib exhibits anti-inflammatory, analgesic, and antipyretic activities by selectively inhibiting cyclooxygenase-2 (COX-2) isoenzymes resulting in inhibition of prostaglandin synthesis. Traditional non-steroidal anti-inflammatory drugs (NSAIDs) appear to inhibit prostaglandin synthesis through inhibition of both COX-1 and COX-2 isoenzymes.
At therapeutic doses, celecoxib does not inhibit COX-1 isoenzyme, thus, it does not interfere with the normal COX-1 related physiological processes in tissues, such as the stomach, intestine and platelets.
Pharmacokinetics: Bioavailability: Celecoxib is well absorbed from the GI tract. Peak plasma levels occur approximately 2 to 3 hours after the drug is given orally under fasting conditions. After oral administration of a single 200 mg dose of celecoxib in healthy fasting adults, peak plasma concentrations (Cmax) of the drug averaged 705 ng/mL. When celecoxib was taken with a high fat meal (24 g fat), bioavailability (AUC) was increased by 10 to 20% and time to reach peak plasma levels (tmax) was delayed by 1 to 2 hours compared with administration with a medium-fat meal (8 g fat) or under fasting conditions. The AUC and plasma concentration 12 hours after a celecoxib dose were slightly higher when the drug was given in the evening versus in the morning. Under fasting conditions, at doses above 200 mg, there is less than a proportional increase in Cmax and AUC, which is thought to be due to the low solubility of the drug in aqueous media. After oral administration of celecoxib at recommended doses of 200 to 400 mg/day, steady-state plasma concentrations are reached within five days. Celecoxib doses up to 200 mg twice a day can be administered without regard to timing of meals. Higher doses (400 mg twice a day) should be given with food to improve absorption. Celecoxib's protein binding is 97%. The apparent volume of distribution at steady state is about 400 L (about 7.14 L/kg), suggestive of extensive tissue distribution. Celecoxib is not bound to erythrocytes. It is not known whether celecoxib crosses human placenta.
Celecoxib is extensively metabolized in the liver; metabolism is primarily mediated via cytochrome P450 2C9. Three metabolites have been identified in human plasma: a primary alcohol, the corresponding carboxylic acid and its glucuronide conjugate.
Celecoxib's metabolites do not have pharmacologic activity as COX-1 and 2 inhibitors. (See Interactions).
Celecoxib is excreted in urine and feces principally as metabolites; less than 3% of the dose is excreted unchanged. Under fasted condition, the effective half-life is approximately 11 hours. The apparent plasma clearance (CL/F) is about 500 mL/min.
Indications/Uses
Relief of the signs and symptoms of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
Relief of the signs and symptoms of juvenile rheumatoid arthritis (JRA) in patients 2 years and older.
Management of acute pain, including postoperative dental or orthopedic pain, and treatment of primary dysmenorrheal.
Carefully consider the potential benefits and risks of celecoxib and other treatment options before deciding to use celecoxib.
Dosage/Direction for Use
Celecoxib dosages up to 200 mg twice a day may be taken with or without food; higher doses, i.e., 400 mg twice a day, should be given with food to improve absorption.
As with other NSAIDs, the lowest effective dose of celecoxib should be used for the shortest possible time. (See Table 1 and Table 2.)

Click on icon to see table/diagram/image


Click on icon to see table/diagram/image
Special Precautions
Hepatic Impairment: The daily dose of celecoxib should be reduced by approximately 50% in patients with moderate hepatic impairment. The use of celecoxib in patients with severe hepatic impairment is not recommended.
Renal Insufficiency: There is no clinical experience in patients with severe renal impairment thus the use of celecoxib is not advised.
Poor Metabolizers of CYP2C9 Substrates: Celecoxib should be administered with caution in patients who are poor CYP2C9 metabolizers based on genotype or previous history with other CYP2C9 substrates such as warfarin or phenytoin. Consider starting treatment at half of the lowest recommended dose in poor metabolizers and consider using alternative management in JRA patients who are poor metabolizers.
Adverse Reactions
At usual dosages, celecoxib is generally well tolerated. Adverse effects are usually mild and mainly involve the GI tract.
Cardiovascular: peripheral edema, angina pectoris, chest pain, coronary artery disorder, myocardial infarction, palpitation, tachycardia, aggravated hypertension, syncope, congestive heart failure, ventricular fibrillation, pulmonary embolism, cerebrovascular accident, peripheral gangrene, thrombophlebitis, deep-vein thrombosis, vasculitis.
Gastrointestinal: dyspepsia, diarrhea, constipation, abdominal pain, nausea, vomiting, flatulence, anorexia, diverticulitis, dry mouth, dysphagia, eructation, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux, hemorrhoids, hiatal hernia, increased appetite, melena, stomatitis, taste perversion, tenesmus, tooth disorder, dry socket, intestinal obstruction, intestinal perforation, GI bleeding, colitis with bleeding, esophageal perforation, pancreatitis, cholelithiasis, ileus, intestinal anastomotic ulceration.
Nervous System: headache, migraine, dizziness, insomnia, somnolence, anxiety, asthenia, depression, hypertonia, hypoesthesia, nervousness, neuralgia, neuropathy, paresthesia, vertigo, aseptic meningitis, ataxia, ageusia, anosmia, fatal intracranial hemorrhage, suicide.
Respiratory: upper respiratory tract infection, sinusitis, pharyngitis, rhinitis, bronchitis, bronchospasm (including aggravated bronchospasm), coughing, dyspnea, laryngitis, pneumonia, nasopharyngitis.
Dermatologic and Sensitivity Reactions: rash, alopecia, dermatitis, dry skin, erythematous rash, maculopapular rash, nail disorder, photosensitivity reaction, pruritus, skin disorder, increased sweating, urticaria.
Allergic Reactions: aggravated allergy, bronchospasm, generalized or facial edema, angioedema, anaphylactoid reactions, erythema multiforme, exfoliative dermatitis, Sweet's syndrome, Stevens-Johnson Syndrome, toxic epidermal necrolysis.
Hematologic: anemia, ecchymosis, epistaxis, thrombocythemia, agranulocytosis, aplastic anemia, pancytopenia, leukopenia, thrombocytopenia.
Renal and Genitourinary: albuminuria, cystitis, dysuria, hematuria, frequent micturition, renal calculus, urinary incontinence, urinary tract infection, dysmenorrhea, genital moniliasis, menstrual disorder, vaginal hemorrhage, vaginitis, prostatic disorder, acute renal failure, interstitial nephritis, renal papillary necrosis, renal injury.
Hepatic: Borderline elevations in serum ALT (SGPT) or AST (SGOT), jaundice, hepatitis, fatal fulminant hepatitis, liver necrosis, liver failure.
Musculoskeletal: back pain, arthralgia, arthrosis, bone disorder, leg cramps, myalgia, neck stiffness, synovitis, tendinitis, accidental fracture.
Special Senses: blurred vision, cataract, conjunctivitis, ocular pain, glaucoma, deafness, ear abnormality, earache, otitis media, tinnitus.
Metabolic: increases in: blood urea nitrogen (BUN), creatinine phosphokinase (CPK), nonprotein nitrogen (NPN), creatinine, alkaline phosphatase; diabetes mellitus, hyperglycemia, hypoglycemia, hypercholesterolemia, hypokalemia, hyponatremia, weight gain.
General: hot flushes, influenza-like symptoms, accidental injury, cysts, fatigue, fever, flu-like symptoms, soft tissue infection, bacterial infections, fungal infections (including moniliasis), viral infections (including herpes simplex or herpes zoster), pain and peripheral pain, sepsis, sudden death.
ATC Classification
M01AH01 - celecoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Presentation/Packing
Cap 200 mg (size "1" hard-gelatin with a violet cap and white body containing a white to off-white powder) x 30's. 400 mg (size "00" hard-gelatin with a dark yellow cap and white body containing a white to off-white powder) x 30's.
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