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At a glance

Apremilast is a phosphodiesterase 4 (PDE4) inhibitor used for the treatment of moderate to severe plaque psoriasis and active psoriatic arthritis in adult patients who are candidates for phototherapy or systemic therapy.

Indications
  • Active psoriatic arthritis
  • Moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy
Pharmacology

Apremilast is a novel, orally available small molecule inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4). PDE-4 is a cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase that is predominantly located in inflammatory cells.

By inhibiting PDE-4, apremilast increases intracellular levels of cAMP and thereby inhibits the production of multiple proinflammatory mediators including TNF-alpha, interleukin-2 (IL-2), interferon-gamma, leukotrienes, and nitric oxide synthase.

Dosage

Recommended Dose Titration (to reduce GI symptoms):

DayMorningEvening
Day 110 mg—
Day 210 mg10 mg
Day 310 mg20 mg
Day 420 mg20 mg
Day 520 mg30 mg
Day 6 and onwards30 mg30 mg

Maintenance Dose: 30 mg twice daily from Day 6

Severe Renal Impairment (CrCl <30 mL/min): Reduce dose to 30 mg once daily. Use only morning schedule; skip evening doses.

Hepatic Impairment: No dosage adjustment required.

Side effects

Common (>10%):

  • Nausea
  • Diarrhea
  • Headache

Other (1-10%):

  • Upper respiratory tract infection
  • Vomiting
  • Nasopharyngitis
  • Abdominal pain
  • Hypersensitivity
  • Gastroesophageal reflux disease
  • Dyspepsia
  • Fatigue
  • Decreased appetite
  • Cough
  • Rash
  • Insomnia

Weight Loss: 5-10% body weight loss reported during treatment.

Use in pregnancy

[CONSULT YOUR DOCTOR] Apremilast may be unsafe to use during pregnancy (Pregnancy Category C). Animal studies have shown harmful effects on the developing baby. Your doctor will weigh the benefits and potential risks before prescribing.

Pregnancy Category: C — always consult a doctor before taking during pregnancy.

Precautions & warnings

Serious Precautions:

  • Inform your doctor immediately if you experience new or worsened depression, suicidal thoughts, or other mood changes
  • Monitor weight regularly - apremilast may cause weight loss
  • Caution during pregnancy - animal studies have shown harmful effects on the developing baby
  • Caution during breastfeeding - apremilast was detected in milk of lactating mice
  • Dose adjustment needed in severe renal impairment
  • Mild stomach upset may occur early during treatment but usually resolves
Overdose effects

There is no known specific antidote for apremilast overdose. In the event of an overdose, undertake general supportive measures.

Storage conditions

Store at cool & dry place below 30°C, protected from light & moisture. Keep out of reach of children.

Apremilast — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.