Celecoxib
Celecoxib (Celebrex)
Celecoxib
( sell-ah- KOX-ihb)
Pregnancy Category: C Celebrex (Rx)

Classification: NSAID, COX-2 inhibitor

See Also: See also Nonsteroidal Anti-Inflammatory Drugs.

Action/Kinetics: Inhibits prostaglandin synthesis, primarily by inhibiting cyclooxygenase-2 (COX-2); it does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme. Does not affect platelet aggregation; renal effects similar to other NSAIDs. Causes fewer GI complications, such as bleeding and perforation, compared with other NSAIDs. Peak plasma levels: 3 hr. About 97% protein bound. t 1/2, terminal: 11 hr when fasting; low solubility prolongs absorption. Metabolized in the liver to inactive compounds; excreted in the urine and feces. Blacks show a 40% increase in the total amount absorbed compared with Caucasians.

Uses: Relief of signs and symptoms of rheumatoid arthritis in adults and of osteoarthritis.

Contraindications: Use in severe hepatic impairment, in those who have shown an allergic reaction to sulfonamides, or in those who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Use in late pregnancy (may cause premature closure of ductus arteriosus). Lactation.

Special Concerns: Use with caution in pre-existing asthma, with drugs that are known to inhibit P450 2C9 in the liver, or when initiating the drug in significant dehydration. Use with extreme caution in those with a prior history of ulcer disease or GI bleeding. Safety and efficacy have not been determined in clients less than 18 years of age. Use caution not to confuse Celebrex with Celexa (an antidepressant) or Cerebyx (injectable fosphenytoin to treat seizures).

Side Effects: Listed are side effects with a frequency of 0.1% or greater. GI: Dyspepsia, diarrhea, abdominal pain, N&V;, dry mouth, flatulence, constipation, GI bleeding, GI ulceration, GI hemorrhage, diverticulitis, dysphagia, eructation, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux, hemorrhoids, hiatal hernia, melena, stomatitis, tooth disorder, abnormal hepatic function. CNS: Headache, dizziness, insomnia, anorexia, anxiety, depression, nervousness, somnolence, hypertonia, hypoesthesia, migraine, neuropathy, paresthesia, vertigo, increased appetite. CV: Aggravated hypertension, angina pectoris, coronary artery disorder, MI palpitation, tachycardia, thrombocythemia. Respiratory: URI, sinusitis, pharyngitis, rhinitis, bronchitis, bronchospasm, coughing, dyspnea, laryngitis, pneumonia. Dermatologic: Rash, ecchymosis, alopecia, dermatitis, nail disorder, photosensitivity, pruritus, erythematous rash, maculopapular rash, skin disorder, dry skin, increased sweating, urticara. Body as a whole: Accidental injury, back pain, peripheral edema, aggravated allergy, allergic reaction, asthenia, chest pain, fluid retention, generalized edema, fatigue, fever, hot flushes, flu-like symptoms, pain, peripheral pain, weight increase. Musculoskeletal: Arthralgia, arthrosis, bone disorder, accidental fracture, myalgia, stiff neck, synovitis, tendinitis. Infections: Bacterial, fungal, or viral infection; herpes simplex, herpes zoster, soft tissue infection, moniliasis, genital moniliasis, otitis media. GU: Cystitis, dysuria, frequent urination, renal calculus, urinary incontinence, UTI, breast fibroadenosis, breast neoplasm, breast pain, dysmenorrhea, menstrual disorder, vaginal hemorrhage, vaginitis, prostatic disorder. Ophthalmic: Glaucoma, blurred vision, cataract, conjunctivitis, eye pain. Otic: Deafness, ear abnormality, earache, tinnitus. Miscellaneous: Tenesmus, facial edema, leg cramps, diabetes mellitus, epistaxis, anemia, taste perversion.

Laboratory Test Alterations: ALT, AST, BUN, CPK, NPN, creatinine, alkaline phosphatase. Hypercholesterolemia, hyperglycemia, hypokalemia, albuminuria, hematuria.

Drug Interactions: ACE Inhibitors / Antihypertensive effect Antacids, aluminum- and magnesium-containing / Absorption of celecoxib Aspirin / Risk of GI ulceration Fluconazole / Plasma levels of celecoxib Furosemide / Natriuretic drug effect Lithium / Plasma lithium levels Thiazide diuretics / Natriuretic drug effects Warfarin / Possible prothrombin time, especially in the elderly

How Supplied: Capsules: 100 mg, 200 mg

Dosage
?Capsules Osteoarthritis.
Adults: 100 mg b.i.d. or 200 mg as a single dose.
Rheumatoid arthritis.
Adults: 100-200 mg b.i.d.