celecoxib (Rx)

Brand and Other Names:Celebrex, Elyxyb
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule (Celebrex)

  • 50mg
  • 100mg
  • 200mg
  • 400mg

oral solution (Elyxyb)

  • 25mg/mL (120mg/4.8mL)

Acute Pain or Primary Dysmenorrhea

400 mg PO initially, then 200 mg PRN on first day; 200 mg q12hr PRN on subsequent days

Ankylosing Spondylitis

200 mg PO once daily or divided q12hr; if no effect after 6 weeks, may increase to 400 mg/day; if inadequate response observed after 6 weeks of taking 400 mg/day consider discontinuing therapy

Osteoarthritis

200 mg PO once daily or divided q12hr

Rheumatoid Arthritis

100-200 mg PO q12hr

Migraine

Elyxyb only

Indicated for the acute treatment of migraine with or without aura in adults

120 mg (4.8 mL) PO

Not to exceed 120 mg/24 hr; safety and efficacy of a second dose within 24 hr not established

Use for the fewest number of days per month, as needed

Familial Adenomatous Polyposis (Off-label)

400 mg PO q12hr, taken with food

Usual medical care should be continued during celecoxib therapy

Dosage Modifications

Hepatic impairment

  • Moderate (Child-Pugh class B): Decrease dose by 50%
  • Severe (Child-Pugh class C): Not recommended

Renal impairment

  • Relative contraindication to use

Dosage Forms & Strengths

capsule

  • 50mg
  • 100mg
  • 200mg
  • 400mg

Juvenile Rheumatoid Arthritis

<2 years: Safety and efficacy not established

≥2 years and 10-25 kg: 50 mg PO q12hr

≥2 years and >25 kg: 100 mg PO q12hr

Consider alternative management in patients who are poor CYP2C9 metabolizers

Pediatric Juvenile Idiopathic Arthritis (Orphan)

Oral liquid suspension: Orphan designation for juvenile idiopathic arthritis

Sponsor

  • NuBioPharma, LLC; 111 Dennis Drive, Suite 121; Sanford, North Carolina 27330

Dosage Modifications

Poor CYP2C9 Metabolizers

  • May consider reducing the initial dose by 50%; consider alternative therapy in patients that are poor CYP2C9 metabolizers
Next:

Interactions

Interaction Checker

and celecoxib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            >10%

            Headache (10-16%)

            Hypertension (13%)

            1-10%

            Fever (9%)

            Dyspepsia (8.8%)

            Upper respiratory tract infection (8.1%)

            Arthralgia (7%)

            Cough (7%)

            Vomiting (6%)

            Diarrhea (5.6%)

            Gastroesophageal reflux (5%)

            Sinusitis (5%)

            Abdominal pain (4.1%)

            Nausea (3.5%)

            Back pain (2.8%)

            Insomnia (2.3%)

            Pharyngitis (2.3%)

            Flatulence (2.2%)

            Rash (2.2%)

            Dizziness (2%)

            Peripheral edema (2%)

            <1%

            Anemia

            Erythema multiforme

            Exfoliative dermatitis

            Hepatitis

            Jaundice

            Stevens-Johnson syndrome

            Toxic epidermal necrolysis

            Frequency Not Defined

            Increased serum asparate aminotransferase concentration

            Previous
            Next:

            Warnings

            Black Box Warnings

            Cardiovascular risk

            • Nonsteroidal anti-inflammatory drugs (NSAIDs) may increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), and stroke, which can be fatal
            • Risk may increase with duration of use
            • Patients with existing cardiovascular disease or risk factors for such disease may be at greater risk
            • NSAIDs are contraindicated for perioperative pain in setting of coronary artery bypass graft (CABG) surgery

            Gastrointestinal risk

            • NSAIDs increase risk of serious gastrointestinal (GI) adverse events, including bleeding, ulceration, and gastric or intestinal perforation, which can be fatal
            • GI adverse events may occur at any time during use and without warning symptoms
            • Elderly patients are at greater risk for serious GI events

            Contraindications

            Known hypersensitivity (eg, anaphylactic reactions, serious skin reactions) to celecoxib or its components

            History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs; severe, sometimes fata, anaphylactic reactions reported

            In the setting of coronary artery bypass graft

            Demonstrated allergic-type reactions to sulfonamides

            Cautions

            Congestive heart failure, hypertension

            Increased risk of adverse cardiovascular events and skin reactions

            Caution in asthma (bronchial), bleeding disorder, bronchospasm, duodenal/gastric/peptic ulcer, renal impairment

            Risk of GI bleeding, ulceration, and perforation; factors that increase risk of GI bleeding in patients treated with NSAIDs include longer duration of NSAID therapy; concomitant use of oral corticosteroids, antiplatelet drugs (such as aspirin), anticoagulants; or selective serotonin reuptake inhibitors (SSRIs); smoking; use of alcohol; older age; and poor general health status

            Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include elderly individuals; those with impaired renal function, hypovolemia, heart failure, liver dysfunction, or salt depletion, and those taking diuretics, angiotensin-converting enzyme inhibitors, or angiotensin-receptor blockers

            Anemia may occur; monitor hemoglobin or hematorcrit in long term treatment patients

            Use caution in pediatrics with systemic-onset juvenile idiopathic arthritis; serious adverse reactions, including disseminated intravascular coagulation reported

            NSAIDs may cause serious skin reacitons including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, may occur without warning or without prior known sulfa allergy; discontinue at first sign of rash

            Drug interaction overview

            • CYP2C9 inhibitors
              • Celecoxib is a CYP2C9 substrate
              • Coadministration with CYP2C9 inhibitors may increase celecoxib plasma levels owing to reduced metabolic clearance
              • Coadministration with CYP2C9 inducers may decrease celecoxib efficacy
            • CYP2D6 substrates
              • Celecoxib inhibits CYP2D6
              • If coadministered, may increase levels of CYP2D6 substrates
            • Drugs that interfere with hemostasis
              • Monitor if coadministered with anticoagulants (eg, warfarin), antiplatelet agents (eg, aspirin), selective serotonin reuptake inhibitors (SSRIs), and serotonin norepinephrine reuptake inhibitors (SNRIs) for signs of bleeding
              • Coadministration with analgesic doses of aspirin is not recommended owing to increased risk of bleeding
              • If coadministration with low-dose aspirin for cardiac prophylaxis, monitor closely for evidence of GI bleeding
            • ACE inhibitors, ARBs, beta-blockers
              • NSAIDs may diminish antihypertensive effect of ACE inhibitors, angiotensin receptor blockers (ARBs), or beta blockers
              • In patients who are elderly, volume-depleted (including those on diuretic therapy), or have renal impairment, coadministration of an NSAID with ACE inhibitors or ARBs may result in deterioration of renal function, including possible acute renal failure; these effects are usually reversible
              • If coadministered, patients should be well hydrated; monitor for signs of worsening renal function
            • Diuretics
              • NSAIDs may reduce the natriuretic effect of loop and thiazide diuretics
              • This effect is attributed to the NSAID inhibition of renal prostaglandin synthesis
            • Digoxin
              • Coadministration increases digoxin serum concentration and prolongs digoxin half-life
            • Lithium
              • NSAIDs elevate plasma lithium levels and reduce renal lithium clearance
              • Mean minimum lithium concentration increased 15%; renal clearance decreased by ~20%
              • Effect attributed to NSAID inhibition of renal prostaglandin synthesis
              • Monitor for lithium toxicity
            • Methotrexate
              • Coadministration of NSAIDs and methotrexate may increase risk for methotrexate toxicity (eg, neutropenia, thrombocytopenia, renal dysfunction)
            • Cyclosporine
              • Coadministration may increase nephrotoxicity
              • If coadministered, monitor for worsening renal function
            • Pemetrexed
              • Coadministration may increase risk of pemetrexed-associated myelosuppression, renal, and GI toxicity
              • CrCl 45-79 mL/min: Monitor for myelosuppression, renal, and GI toxicity
              • CrCl <30 mL/min: Coadministration not recommended
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            Use of NSAIDs during the 3rd trimester of pregnancy increases risk of premature closure of the fetal ductus arteriosus

            Avoid use of NSAIDs in pregnant women starting at 30 weeks of gestation

            There are no adequate and well-controlled studies in pregnant women

            Data from observational studies regarding potential embryofetal risks of NSAIDs during the 1st or 2nd trimesters are inconclusive

            Animal studies

            • Administration during pregnancy resulted in adverse effects on development, including increases in embryonic death and fetal malformations, at doses or maternal plasma drug exposures greater than those used clinically
            • Prostaglandins have shown an important role in endometrial vascular permeability, blastocyst implantation, and decidualization; in animal studies, administration of prostaglandin synthesis inhibitors resulted in increased pre- and postimplantation loss

            Labor and delivery

            • There are no studies on the effects of celecoxib during labor or delivery
            • In animal studies, NSAIDs inhibit prostaglandin synthesis, cause delayed parturition, and increase the incidence of stillbirth

            Infertility

            • Published animal studies have shown that administration of prostaglandin synthesis inhibitors has the potential to disrupt prostaglandin mediated follicular rupture required for ovulation
            • Consider withdrawal of NSAIDs in women who have difficulties conceiving or who are undergoing investigation of infertility

            Lactation

            Limited data from 12 breastfeeding women showed low levels of celecoxib in breast milk

            Calculated average daily infant dose was 10-40 mcg/kg/day, <1% of the weight-based therapeutic dose for a 2-year old child

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Inhibits cyclooxygenase (COX)-2; does not affect COX-1 (at therapeutic concentrations), thereby decreasing formation of prostaglandin synthesis

            Absorption

            Bioavailability: Undetermined

            Peak plasma time: ≤3 hr (capsule); 1 hr (oral solution)

            Peak plasma concentration: 705 ng/mL

            Distribution

            Protein bound: 97% (principally to albumin; to a lesser extent, to alpha1-acid glycoprotein)

            Vd: 400 L

            Metabolism

            Metabolized in liver by CYP2C9

            Metabolites: Carboxylic acid (SC-62807), glucuronide

            Enzymes inhibited: COX-2

            Elimination

            Half-life: Mild hepatic impairment, 11 hr; chronic renal insufficiency or moderate hepatic impairment, 13.1 hr

            Dialyzable: Undetermined

            Clearance: 500 mL/min

            Excretion: Feces (57%), urine (27%)

            Pharmacogenomics

            CYP2C9 activity is reduced in individuals with genetic polymorphisms that lead to reduced enzyme activity (eg, individuals who are homozygous for the CYP2C9*2 and CYP2C9*3 polymorphisms)

            Limited data from 4 published reports that included a total of 8 subjects with the homozygous CYP2C9*3/*3 genotype showed celecoxib systemic levels that were 3- to 7-fold higher in these subjects compared with subjects with CYP2C9*1/*1 or *I/*3 genotypes

            Pharmacokinetics of celecoxib have not been evaluated in subjects with other CYP2C9 polymorphisms (eg, *2, *5, *6, *9 and *11)

            Estimated frequency of the homozygous *3/*3 genotype is 0.3-1% in various ethnic groups

            Previous
            Next:

            Administration

            Oral Administration

            May take with or without food

            Oral solution

            • Use a calibrated measuring device (eg, oral syringe) to measure dose accurately
            • A household teaspoon or tablespoon is not an adequate measuring device

            Storage

            Capsules or oral solution: Store at room temperature 20-25ºC (68-77ºF); excursions permitted between 15-30ºC (59--86ºF)

            Do not refrigerate or freeze

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.