apremilast (Rx)

Brand and Other Names:Otezla
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 10mg
  • 20mg
  • 30mg

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

Oral Ulcers associated with Behςet Disease

Indicated for oral ulcers associated with Behςet disease

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

Hepatic impairment: No dosage adjustment required

Renal impairment

  • Mild-to-moderate (CrCl ≥30): No dosage adjustment required
  • Severe (CrCl <30 mL/min)
    • Reduce dose to 30 mg PO qDay
    • For initial dosage titration, titrate using only the AM schedule listed above and skip the PM doses

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
Next:

Interactions

Interaction Checker

and apremilast

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% (Psoriasis and Psoriatic Arthritis)

            Diarrhea (7.7-17%)

            Nausea (7.4-17%)

            >10% (Behςet Disease)

            Diarrhea (41.3%)

            Nausea (19.2%)

            Headache (14.4%)

            Upper respiratory tract infection (11.5%)

            1-10% (Behςet Disease)

            Upper abdominal pain (8.7%)

            Vomiting (8.7%)

            Back pain (7.7%)

            Viral upper respiratory tract infection (6.7%)

            Arthralgia (5.8%)

            1-10% (Psoriasis and Psoriatic Arthritis)

            Upper respiratory tract infection (0.6-9%)

            Tension headache (8%)

            Headache (4.8-6%)

            Vomiting (0.8-4%)

            Fatigue (3%)

            Dyspepsia (3%)

            Decreased appetite (3%)

            Insomnia (2%)

            Back pain (2%)

            Migraine (2%)

            Frequent bowel movements (2%)

            Depression (1%)

            Bronchitis (1%)

            Tooth abscess (1%)

            Folliculitis (1%)

            Frequency Not Defined (Psoriasis and Psoriatic Arthritis)

            Immune system disorders: Hypersensitivity

            Investigations: Weight decrease

            Gastrointestinal disorders: Frequent bowel movement, gastroesophageal reflux disease, dyspepsia

            Metabolism and nutrition disorders: Decreased appetite

            Nervous system disorders: Migraine

            Respiratory, thoracic, and mediastinal disorders: Cough

            Skin and SC tissue disorders: Rash

            Previous
            Next:

            Warnings

            Contraindications

            Hypersensitivity to apremilast or to any of the excipients in the formulation

            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
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            Available pharmacovigilance data use in pregnant women have not established a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes, but data are extremely limited

            Based on findings from animal reproduction studies, may increase the risk for fetal loss

            Pregnancy exposure registry

            • Registry monitors pregnancy outcomes in women exposed to apremilast during pregnancyRegistry information can be obtained by calling 1-877-311-8972 or visiting https://mothertobaby.org/ongoing-study/otezla

            Animal data

            • In a pre- and postnatal study in mice, apremilast was administered to pregnant female mice at doses of 10, 80, or 300 mg/kg/day from Day 6 of gestation through Day 20 of lactation, with weaning on Day 21
            • Dystocia, reduced viability, and reduced birth weights occurred at doses corresponding to ≥4-times the MRHD (on an AUC basis at doses ≥80 mg/kg/day)
            • No adverse effects occurred at a dose 1.3- times the MRHD (10 mg/kg/day)No evidence for functional impairment of physical development, behavior, learning ability, immune competence, or fertility in the offspring at doses up to 7.5-times the MRHD (on an AUC basis at a dose of 300 mg/kg/day)
            • Apremilast distributed across the placenta into the fetal compartment in mice and monkeys
            • Advise pregnant women of the potential risk of fetal lossConsider pregnancy planning and prevention for females of reproductive potential

            Lactation

            There are no data on the presence of apremilast in human milk, the effects on the breastfed infant, or the effects on milk production

            Detected in the milk of lactating mice

            Consider developmental and health benefits of breastfeeding along with the mother’s clinical need and any potential adverse effects on the breastfed infant or from the underlying maternal condition

            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

            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

            Previous
            Next:

            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

            Storage

            Store below 30ºC (86ºF)

            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.