Apremilast

Generic Details

Generic Name

Apremilast

Other Names

  • Otezla

Drug Class

  • Phosphodiesterase-4 (PDE-4) Inhibitor

Chemical Formula

C22H24N2O7

Molecular Weight

460.436 g/mol

Mechanism of Action

  • Inhibits the enzyme phosphodiesterase-4 (PDE-4), leading to decreased production of pro-inflammatory mediators

Indications

  • Treatment of psoriasis
  • Treatment of psoriatic arthritis

Common Dosage Forms

  • Oral tablet

Typical Dosage

  • 30 mg twice daily

Pediatric Dosage

  • Not established

Geriatric Dosage

  • Adjust dosage based on renal function

Side Effects

  • Nausea
  • Diarrhea
  • Headache
  • Upper respiratory tract infection

Contraindications

  • Hypersensitivity to apremilast

Pregnancy Category

  • Category C

Lactation Safety

  • Not recommended

Drug Interactions

  • Strong CYP3A4 inducers/inhibitors may alter apremilast levels

Overdose Symptoms

  • Nausea
  • Vomiting
  • Diarrhea

Antidote for Overdose

  • Symptomatic treatment

Storage Conditions

  • Store at room temperature (20-25°C)

Pharmacokinetics

  • Absorption: Rapidly absorbed after oral administration
  • Distribution: Highly distributed in tissues
  • Metabolism: Primarily metabolized in the liver to inactive metabolites
  • Excretion: Mainly excreted in urine

Precautions

  • Monitor for mood changes and depression

Warnings

  • Increase in depression and suicidal thoughts reported

Others