A-Z Drug Facts > Celecoxib

Celecoxib

Pronouncation: (SEL-e-KOX-ib)
Class: Selective COX-2 inhibitor

Trade Names:
Celebrex
- Capsules 50 mg
- Capsules 100 mg
- Capsules 200 mg
- Capsules 400 mg

Pharmacology

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Reduces inflammation, fever, and pain by inhibiting prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2) isoenzyme.

Pharmacokinetics

Absorption

T _max is about 3 h.

Food

T _max increased about 1 to 2 h and AUC increased 10% to 20% when taken with a high-fat meal.

Distribution

97% protein bound. Vd is about 400 L.

Metabolism

Metabolized in the liver; primarily mediated via CYP2C9 to inactive metabolites.

Elimination

Less than 3% is excreted unchanged in the urine and feces. About 57% is excreted in feces and 27% in urine. The t _½ is about 11 h. Cl is about 500 mL/min.

Special Populations

Renal Function Impairment

AUC is about 40% lower in those with Ccr 35 to 60 mL/min.

Hepatic Function Impairment

AUC is increased about 40% in mild impairment and 180% in moderate impairment. Reduce dosage.

Elderly

C _max is 40% higher and AUC is 50% higher.

Race

AUC is about 40% higher in blacks vs whites.

Indications and Usage

Relief of signs and symptoms of osteoarthritis (OA), rheumatoid arthritis (RA) in adults, and ankylosing spondylitis; management of acute pain in adults; treatment of primary dysmenorrhea; reduction of the number of adenomatous colorectal polyps in familial adenomatous polyposis (FAP), as an adjunct to usual care; relief of signs and symptoms of juvenile RA in patients 2 yr of age and older.

Unlabeled Uses

Adjunctive therapy in the treatment of schizophrenia (inconclusive data).

Contraindications

Hypersensitivity to celecoxib; allergy to sulfonamides; previous allergic reactions following aspirin or other NSAID use (eg, asthma, hives, rash); treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

Dosage and Administration

OA
Adults

PO 200 mg/day administered as a single dose or as 100 mg twice daily.

RA
Adults

PO 100 to 200 mg twice daily.

Juvenile RA
Children 2 yr of age and older

PO Children weighing 10 kg (22 lb) to 25 kg (55 lb), administer 50 mg twice daily. Children weighing more than 25 kg (55 lb), administer 100 mg twice daily.

Ankylosing Spondylitis
Adults

PO 200 mg/day administered as a single dose or as 100 mg twice daily. If no response after 6 wk, attempt dose increase to 400 mg/day; if no response after 6 wk at 400 mg/day, discontinue and consider alternate treatment.

Acute Pain, Primary Dysmenorrhea
Adults

PO 400 mg initially followed by an additional 200 mg dose on day 1, if needed, then 200 mg twice daily as needed.

FAP
Adults

PO 400 mg twice daily.

Hepatic Function Impairment

Reduce dose 50% in patients with moderate hepatic function impairment. Not recommended in patients with severe hepatic function impairment.

Advanced Renal Function Impairment

Not recommended.

Patients Weighing 50 kg or less

Initiate at the lowest recommended dose.

General Advice

• Dosages up to 200 mg twice daily can be given without regard to meals. Administer high doses (400 mg twice daily) with food.
• To minimize potential GI events, use lowest effective dose for the shortest duration.
• Capsules may be opened and sprinkled on soft food.

Storage/Stability

Store at controlled room temperature (59° to 86°F).

Drug Interactions

ACE inhibitors

NSAIDs may diminish the antihypertensive effect of ACE inhibitors.

Alcohol, corticosteroids

May increase risk of GI bleeding.

Aspirin

Coadministration may result in an increased rate of GI ulceration or other complications.

Clopidogrel

Risk of hemorrhage may be increased.

CYP-450 2C9 and 2D6 inhibitors

There is a potential for drug interaction when coadministered with celecoxib.

Diuretics

Patients taking thiazides or loop diuretics may have an impaired response to therapy.

Fluconazole

Increase in celecoxib plasma concentration may occur.

Lithium

Mean steady-state lithium plasma levels increased about 17% when coadministered.

Warfarin

Monitor anticoagulant activity, particularly in the first few days, after initiating or changing celecoxib therapy in patients receiving warfarin or similar agents.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Aggravated hypertension, angina pectoris, coronary artery disorder, MI, palpitations, tachycardia (less than 2%).

CNS

Headache (16%); dizziness, insomnia (2%); anorexia, anxiety, depression, fatigue, migraine, nervousness, neuralgia, neuropathy, pain, paresthesia, somnolence, vertigo (less than 2%).

Children

Headache (13%); pyrexia (9%); dizziness (1%).

Dermatologic

Rash (2%); alopecia, cellulitis, contact dermatitis, dermatitis, dry skin, erythematous rash, increased sweating, injection-site reaction, maculopapular rash, nail disorder, photosensitivity, pruritus, skin disorder, skin nodule, urticaria (less than 2%).

EENT

Sinusitis (5%); rhinitis (2%); blurred vision, cataracts, conjunctivitis, deafness, ear abnormality, earache, eye pain, glaucoma, laryngitis, otitis media, taste perversion, tinnitus (less than 2%).

Children

Nasopharyngitis (6%); eye disorders (5%).

GI

Dyspepsia (9%); diarrhea (6%); abdominal pain, nausea (4%); flatulence (2%); constipation, diverticulitis, dry mouth, dysphagia, eructation, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux, hemorrhoids, hiatal hernia, increased appetite, melena, stomatitis, tenesmus, tooth disorder, vomiting (less than 2%).

Children

Upper abdominal pain (8%); abdominal pain, nausea (7%); vomiting (6%); diarrhea (5%).

Genitourinary

Albuminuria, breast fibroadenosis, breast neoplasm, breast pain, cystitis, dysmenorrhea, dysuria, hematuria, menstrual disorder, micturition frequency, prostatic disorder, renal calculus, urinary incontinence, UTI, vaginal hemorrhage, vaginitis (less than 2%).

Hematologic

Anemia, ecchymosis, epistaxis, thrombocythemia (less than 2%).

Hepatic

Abnormal hepatic function, elevated AST and ALT (less than 2%).

Metabolic

Diabetes mellitus, hypercholesterolemia, hyperglycemia, hypokalemia, increased alkaline phosphatase, BUN, CPK, creatinine, and nonprotein nitrogen, weight gain (less than 2%).

Musculoskeletal

Arthralgia, arthrosis, bone disorder, hypertonia, hypesthesia, leg cramps, myalgia, neck stiffness, synovitis, tendonitis (less than 2%).

Children

Arthralgia (7%).

Respiratory

Upper respiratory tract infection (8%); pharyngitis (2%); aggravated bronchospasm, bronchitis, bronchospasm, coughing, dyspnea, pneumonia (less than 2%).

Miscellaneous

Accidental injury, back pain (3%); peripheral edema (2%); accidental fracture, allergic reaction, asthenia, bacterial infection, chest pain, cyst not otherwise specified, facial edema, fever, flu-like symptoms, generalized edema, genital moniliasis, herpes simplex, herpes zoster, hot flushes, moniliasis, peripheral pain, soft tissue infection, viral infection (less than 2%).

Children

Injury and poisoning (6%).

Precautions

Warnings CV risk May cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with duration of use. Patients with CV disease or risk factors for CV disease may be at higher risk. Celebrex is contraindicated for the treatment of perioperative pain in the setting of CABG surgery. GI risk NSAIDs, including celecoxib, caused an increase in serious GI adverse reactions, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These reactions can occur at any time during use and without warning symptoms. Elderly patients are at higher risk for serious GI events.

Monitor Monitor BP closely during initiation and throughout therapy. Monitor CBC and chemistry profile periodically during long-term use. Monitor for signs and symptoms of GI bleeding. Monitor renal function in patients with advanced renal disease. Monitor liver function in patients with signs and symptoms of liver dysfunction.

Pregnancy

Category C . Avoid use in late pregnancy.

Lactation

Excreted.

Children

Safety and efficacy not established in children younger than 2 yr of age or less than 10 kg (22 lb) with juvenile RA. For other indications, safety and efficacy not established in patients younger than 18 yr of age.

Elderly

Initiate therapy with lowest recommended dose.

Hypersensitivity

Anaphylactoid reactions have occurred.

Anemia

May occur.

Aspirin triad

Use not recommended.

Asthma

Use with caution in patients with preexisting asthma.

CHF and edema

Fluid retention and edema have been observed. Use with caution.

Debilitated patients

Use with caution. Most spontaneous reports of fatal GI events are in debilitated patients.

Dermatologic

Can cause serious skin reactions, which can be fatal.

GI effects

Use with extreme caution in patients with prior history of ulcer disease or GI bleeding.

Hepatic effects

Elevated liver enzymes may occur. Rare cases of severe hepatic reactions (eg, jaundice, hepatic failure) have occurred. Discontinue use if liver disease develops or if systematic manifestations occur (eg, eosinophilia, rash).

Hypertension

Use with caution. Can lead to onset of new hypertension or worsening of preexisting hypertension.

Renal effects

Long-term use of NSAIDs has resulted in renal papillary necrosis and other renal injury. Those at great risk are patients with impaired renal function, heart failure, or liver dysfunction; those taking diuretics or ACE inhibitors; and elderly patients.

Sulfa allergy

Do not use in patients with a sulfa allergy.

Systemic onset juvenile RA

Use with caution because of risk of serious adverse reactions, including DIC.

Overdosage

Symptoms

Acute renal failure, coma, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.

Patient Information

• Instruct patient to take medication as prescribed.
• Advise patient to inform health care provider if taking or planning to take any OTC medications, as there is potential for drug interactions.
• Advise patient with sensitive stomach to take medication with food to help avoid GI distress.
• Instruct patient to promptly report signs or symptoms of GI ulceration or bleeding, unexplained weight gain, or edema to health care provider.
• Inform patient of the warning signs and symptoms of hepatotoxicity (eg, fatigue, flu-like symptoms, jaundice, lethargy, nausea, pruritus, right upper quadrant tenderness) and to stop therapy and contact health care provider if any of these occur.
• Instruct patient to seek immediate emergency help in case of an anaphylactoid reaction.
• Warn women with childbearing potential to avoid becoming pregnant and apprise them of the potential hazard to the fetus, especially in the third trimester.
• Warn breast-feeding mothers of the danger of transferring drug to the baby through breast milk; a decision will need to be made in collaboration with health care provider to discontinue the drug or breast-feeding.
• Instruct patient to report chest pain, shortness of breath, weakness, slurring of speech, or any unusual reaction or concern to health care provider.
• Instruct patient to discontinue treatment immediately and contact health care provider if rash develops.
• Advise patient with sulfa allergy not to take celecoxib.
• Advise patient with FAP to continue regular care while receiving celecoxib.

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