Apremilast

Indications

Apremilast is used for: Adult patients with active psoriatic arthritis, moderate to severe plaque psoriasis for whom phototherapy or systemic therapy is appropriate.

Adult Dose

To reduce risk of gastrointestinal symptoms, titrate to recommended dose of 30 mg twice daily according to the following schedule: Day 1: 10 mg in morning Day 2: 10 mg in morning and 10 mg in evening Day 3: 10 mg in morning and 20 mg in evening Day 4: 20 mg in morning and 20 mg in evening Day 5: 20 mg in morning and 30 mg in evening Day 6 and thereafter: 30 mg twice daily Hepatic impairment: No dosage adjustment required

Child Dose

Renal Dose

Severe renal impairment (CrCl <30 mL/min): Reduce dose to 30 mg PO qDay Mild-to-moderate renal impairment: No dosage adjustment required

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

Contra Indications

Known hypersensitivity to apremilast.

Precautions

Apremilast is 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. Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of Apremilast. Lactation: Unknown if distributed in human breast milk; caution required

Pregnancy-Lactation

Interactions

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.

Adverse Effects

Side effects of Apremilast : 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%)

Mechanism of Action

Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.