Drug reference

Apremilast

Inhaled Corticosteroid · Disease-Modifying Antirheumatic Drug (DMARD); Anti-psoriatic

Inhaled CorticosteroidDisease-Modifying Antirheumatic Drug (DMARD); Anti-psoriatic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

10 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 10 →

ApalutamideSevereDatabaseDDInter
CarbamazepineSevereDatabaseDDInter
EnzalutamideSevereDatabaseDDInter
FosphenytoinSevereDatabaseDDInter

Mechanism

Apremilast is a selective small molecule inhibitor of the enzyme phosphodiesterase 4 (PDE4), hindering the conversion of cyclic AMP to AMP. The inhibition of PDE4 leads to increased intracellular cAMP and decreased production of proinflammatory cytokines including CXCL9 and CXCL10, IFN-γ, TNF-α, and IL-2, -8, -12, and -23.

Indications

Plaque psoriasis (in candidates for phototherapy or systemic therapy)Psoriatic arthritis (active and progressive, with peripheral arthritis having 3 or more tender joints and 3 or more swollen joints, and unresponsive to at least 2 standard DMARDs given alone or in combination)Oral ulcers associated with Behçet diseasepsoriasisdecreased alcohol drinking (in a human laboratory study, repurposing potential for AUD)Psoriatic Arthritis (PsA)

Dosing

Adult: Orally, gradually increasing the dose over the first 5 days until the recommended dose of 30 mg bid is reached.
Renal adjustment: Recommended if creatinine clearance (CrCl) is ≤30 mL/min.

Pharmacokinetics

Half-life

Approximately 6–9 hours.

Bioavailability

73%

Metabolism

70% metabolized by CYP3A4.

Excretion

58% by the kidneys and 39% by the feces.

Side effects

Common

DiarrheaNauseaUpper abdominal painVomitingUpper respiratory tract infectionsArthralgiaWeight lossHeadachesdyspepsiaheadachefatigue

Serious

Mood disorders
Suicidal ideation
hypersensitivity reaction
depression