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Drugs reference index «Celecoxib»

Celecoxib
Celecoxib


Celecoxib

Pronunciation: (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

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

Pharmacokinetics

Absorption

C max is 705 ng/mL and T max is about 3 h after a single dose. Steady state is reached on or before day 5 with multiple dosing.

Food

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

Distribution

Approximately 97% protein bound. Vd is about 400 L.

Metabolism

Metabolized in the liver 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 half-life is about 11 h. Cl is about 500 mL/min.

Special Populations

Renal Function Impairment

AUC is about 40% lower in patients with a CrCl of 35 to 60 mL/min.

Hepatic Function Impairment

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

Elderly

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

Children

10 and 25 kg children are predicted to have 40% and 24% lower Cl, respectively, compared with a 70 kg adult.

Race

AUC is about 40% higher in black vs white patients.

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 (JRA) in patients 2 yr of age and older.

Unlabeled Uses

Adjunctive therapy in the treatment of schizophrenia (inconclusive data); prevention of colorectal cancer; preterm labor.

Contraindications

Hypersensitivity to celecoxib, aspirin, or other NSAIDs; 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

Acute Pain, Primary DysmenorrheaAdults

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

Ankylosing SpondylitisAdults

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

FAPAdults

PO 400 mg twice daily with food.

JRAChildren 2 yr of age and older

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

OAAdults

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

RAAdults

PO 100 to 200 mg twice daily.

Hepatic Function Impairment

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

Advanced Renal Function Impairment

Not recommended.

Poor Metabolizers of CYP2C9 Substrates

Use with caution. Consider starting treatment at half the lowest recommended dose. In patients with JRA who are poor metabolizers, consider using alternative treatment.

General Advice

  • Dosages of 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 added to 1 level tablespoon of cool or room temperature applesauce; ingest immediately with water.

Storage/Stability

Store at 59° to 86°F. The sprinkled capsule contents on applesauce are stable for up to 6 h in the refrigerator.

Drug Interactions

ACE inhibitors, angiotensin II antagonists

NSAIDs may diminish the antihypertensive effect of these drugs.

Alcohol, corticosteroids, SSRIs (eg, fluoxetine)

May increase risk of GI bleeding.

Antacids (containing aluminum or magnesium)

Coadministration may decrease celecoxib plasma levels.

Aspirin

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

Clopidogrel

Risk of hemorrhage may be increased.

CYP2C9 and CYP2D6 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. Risk of renal impairment may be increased.

Fluconazole, voriconazole

Increase in celecoxib plasma concentration may occur.

Heparin, low molecular weight heparin (eg, enoxaparin)

Risk of hemorrhagic adverse reactions may be increased. Monitor closely.

Lithium

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

Nonaspirin NSAIDs

Avoid concomitant use because of the potential for increased risk of adverse reactions.

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

Hypertension (13%); aggravated hypertension, angina pectoris, coronary artery disorder, MI, palpitations, tachycardia (less than 2%); deep venous thrombosis, vasculitis (postmarketing).

CNS

Headache (16%); dizziness, insomnia (2%); anorexia, anxiety, depression, fatigue, migraine, nervousness, paresthesia, somnolence, vertigo (less than 2%); ageusia, anosmia, aseptic meningitis, fatal intracranial hemorrhage (postmarketing).

Dermatologic

Rash (2%); alopecia, cellulitis, contact dermatitis, dermatitis, dry skin, erythematous rash, increased sweating, maculopapular rash, photosensitivity, pruritus, skin disorder, urticaria (less than 2%); erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, TEN (postmarketing).

EENT

Nasopharyngitis (6%); eye disorders, sinusitis (5%); rhinitis (2%); deafness, laryngitis, tinnitus (less than 2%).

GI

Diarrhea (11%); dyspepsia (9%); upper abdominal pain (8%); abdominal pain, nausea (7%); vomiting (6%); gastroesophageal reflux (5%); flatulence (2%); constipation, diverticulitis, dry mouth, dysphagia, eructation, esophagitis, gastritis, gastroenteritis, hemorrhoids, hiatal hernia, increased appetite, melena, stomatitis, tenesmus (less than 2%).

Genitourinary

Albuminuria, cystitis, dysuria, hematuria, micturition frequency, renal calculus (less than 2%); interstitial nephritis (postmarketing).

Hematologic

Anemia, ecchymosis, epistaxis, thrombocythemia (less than 2%); agranulocytosis, aplastic anemia, leukopenia, pancytopenia (postmarketing).

Hepatic

Abnormal hepatic function, elevated AST and ALT (less than 2%); hepatitis, jaundice, liver failure (postmarketing).

Metabolic

Hypercholesterolemia; hyperglycemia; hypokalemia; increased alkaline phosphatase, BUN, CPK, creatinine, and nonprotein nitrogen; weight gain (less than 2%); hypoglycemia, hyponatremia (postmarketing).

Musculoskeletal

Arthralgia (7%); arthrosis, hypertonia, hypesthesia, leg cramps, myalgia, synovitis, tendonitis (less than 2%).

Respiratory

Upper respiratory tract infection (8%); cough (7%); dyspnea (3%); pharyngitis (2%); aggravated bronchospasm, bronchitis, bronchospasm, coughing, pneumonia (less than 2%).

Miscellaneous

Pyrexia (9%); injury and poisoning (6%); accidental injury, back pain (3%); peripheral edema (2%); aggravated allergy, allergic reaction, chest pain, cyst not otherwise specified, facial edema, flu-like symptoms, generalized edema, hot flushes, pain, peripheral pain (less than 2%); anaphylactoid reaction, angioedema (postmarketing).

Precautions

Warnings

CV risk

May cause an increased risk of serious CV thrombotic events, MI, and stroke, which may 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. Celecoxib 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. Monitor for the development of abnormal coagulation tests in patients with JRA.

Pregnancy

Category C . Category D from 30 weeks' gestation onward. Because celecoxib may cause premature closure of the patent ductus arteriosus, avoid use in late pregnancy.

Lactation

Excreted in breast milk.

Children

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

Elderly

There have been more spontaneous reports of fatal GI events and acute renal failure in elderly patients.

Hypersensitivity

Severe anaphylactoid reactions and angioedema have occurred.

Renal Function

Not recommended in patients with advanced renal disease.

Hepatic Function

Not recommended in patients with severe hepatic impairment.

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 may be fatal (eg, Stevens-Johnson syndrome, TEN).

FAP

Celecoxib has not been shown to reduce the risk of GI cancer or the need for prophylactic colectomy or other FAP-related surgeries. Therefore, usual care of FAP patients should not be altered.

GI effects

Use with extreme caution in patients with 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 greater risk are patients with impaired renal function, heart failure, or liver dysfunction; those taking diuretics, angiotensin II receptor antagonists, or ACE inhibitors; and elderly patients.

Sulfa allergy

Do not use in patients with a sulfa allergy.

Systemic-onset JRA

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

Overdosage

Symptoms

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

Patient Information

  • Advise patient that Medication Guide is available for celecoxib and to read the Medication Guide before starting therapy and with each refill.
  • Instruct patient to take medication as prescribed.
  • Advise patient to inform health care provider if taking or planning to take any OTC medications, because 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 (eg, difficulty breathing, swelling of the face or throat).
  • Warn women of 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; decide whether to discontinue the drug or breast-feeding.
  • Instruct patient to report chest pain, shortness of breath, slurring of speech, weakness, 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.

Copyright © 2009 Wolters Kluwer Health.

  • Celecoxib MedFacts Consumer Leaflet (Wolters Kluwer)
  • Celecoxib Detailed Consumer Information (PDR)
  • celecoxib Advanced Consumer (Micromedex) - Includes Dosage Information
  • Celebrex Prescribing Information (FDA)
  • Celebrex Consumer Overview

See Also...

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