apremilast (Rx)

Brand and Other Names:Otezla
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 10mg
  • 20mg
  • 30mg
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Psoriatic Arthritis

Indicated for active psoriatic arthritis

Day 1: 10 mg in AM

Day 2: 10 mg AM and PM

Day 3: 10 mg AM and 20 mg PM

Day 4: 20 mg AM and PM

Day 5: 20 mg AM and 30 mg PM

Day 6 and thereafter: 30 mg PO BID

Psoriasis

Indicated for moderate-to-severe plaque psoriasis in adults who are candidates for phototherapy or systemic therapy

Day 1: 10 mg in AM

Day 2: 10 mg AM and PM

Day 3: 10 mg AM and 20 mg PM

Day 4: 20 mg AM and PM

Day 5: 20 mg AM and 30 mg PM

Day 6 and thereafter: 30 mg PO BID

Dosage Modifications

Severe renal impairment (CrCl <30 mL/min): Reduce dose to 30 mg PO qDay

Mild-to-moderate renal impairment: No dosage adjustment required

Hepatic impairment: No dosage adjustment required

Safety and efficacy not established

Ulcerative Colitis (Orphan)

Orphan designation for treatment of pediatric patients with ulcerative colitis

Sponsor

  • Celgene Corporation; 86 Morris Avenue Summit, New Jersey 07901
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Interactions

Interaction Checker

and apremilast

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Diarrhea (7.7-9.3%)

            Nausea (7.4-8.9%)

            Headache (4.8-5.9%)

            Upper respiratory tract infection (0.6-3.9%)

            Vomiting (0.8-3.2%)

            Nasopharyngitis (0.2-2.6%)

            Upper abdominal pain (0.6-2%)

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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            Associated with an increase in adverse reactions of depression; before using, evaluate patient for history of depression and/or suicidal thoughts or behavior

            Weight decrease of 5-10% of body weight reported in 10-12% of patients

            Severe GI adverse effects

            • Severe diarrhea, nausea, and vomiting reported; mostly occurred within the first few weeks of treatment
            • In some cases, patients were hospitalized
            • Patients aged ≥65 yr and patients taking medications that cause volume depletion or hypotension may be at a higher risk of these complications; monitor those who are more susceptible to complications of diarrhea or vomiting
            • Quick improvement observed with dosage reduction or discontinuation; consider dose reduction or suspension if patients develop severe diarrhea, nausea, or vomiting

            Drug interaction overview

            • Coadministration with strong CYP inducers (eg, rifampin, carbamazepine, phenobarbital phenytoin) may occur and result in a loss of efficacy of apremilast; therefore, coadministration is not recommended
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            Pregnancy & Lactation

            Pregnancy Category: C; Pregnancy registry 1-877-311-8972

            Lactation: Unknown if distributed in human breast milk; caution required

            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.

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            Pharmacology

            Mechanism of Action

            Oral small molecule inhibitor of phosphodiesterase-4 specific for cAMP, resulting in increased intracellular cAMP levels

            The specific mechanism by which apremilast exerts it therapeutic action in psoriatic arthritis is not well defined

            Absorption

            Absolute bioavailability: 73%

            Peak plasma time: 2.5 hr

            Coadministration with food does not alter absorption

            Distribution

            Protein bound: 68%

            Vd: 87 L

            Metabolism

            Apremilast is a major circulating component (45%) followed by inactive metabolite M12 (39%), a glucuronide conjugate of O-demethylated apremilast

            Metabolized by both CYP oxidative metabolism with subsequent glucuronidation and non-CYP mediated hydrolysis

            In vitro CYP metabolism primarily by CYP3A4, with minor contribution from CYP1A2 and CYP2A6

            Elimination

            Half-life: 6-9 hr

            Clearance: 10 L/hr

            Excretion: 58% urine; 39% feces

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            Administration

            Oral Administration

            To reduce risk of GI symptoms associated with initial therapy, titrate to recommended dose (30 mg PO BID) according to the dosage schedules listed above

            Can be administered without regard to meals

            Swallow tablet whole; do not crush, split, or chew

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            Images

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            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:

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