How is apremilast supplied and used in the treatment of rheumatic diseases?
- • FDA-approved indications: psoriasis and PsA. Also effective for Behçet’s disease (oral and genital ulcers).
- • Available formulation: starter therapy pack (10-, 20-, 30-mg tablets); 30-mg tablets.
- • Dosage: use starter pack to start with 10 mg one per day (QD) and escalate up to 30 mg BID over 1 to 2 weeks. Decrease dose by 50% if severe renal insufficiency (CrCl <30 mL/minute).
- • Cost (30 mg BID): $3500/month.
- • Monitoring: no specific blood tests required.
- • Adverse effects: most common side effects are diarrhea (15%–20%), weight loss, and headache.
- • Precautions: monitor for depression. Dexamethasone and rifampin decrease effectiveness of apremilast by increasing its metabolism. Ketoconazole/fluconazole decreases its metabolism.
- • MOA: apremilast is an immune modulator rather than an immunosuppressant. It is an inhibitor of phosphodiesterase 4, which results in an elevation of cAMP intracellularly in multiple cell types (T cells, mononuclear cells, others). The increase in intracellular cAMP decreases the production of several proinflammatory mediators (tumor necrosis factor [TNF]-α, IL-12, IL-23, interferon [IFN]γ , and inducible nitric oxide synthase) and increases the production of antiinflammatory cytokines (IL-10).
