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Apremilast

  • PDE4 inhibitorsPDE4 inhibitors

An oral PDE4 inhibitor that calms immune cells, used in psoriatic arthritis, plaque psoriasis and the mouth ulcers of Behçet disease.

Updated

Quick facts

Group
PDE4 inhibitors
Target
Phosphodiesterase 4 (cAMP-specific)
Used for
Active psoriatic arthritis · Plaque psoriasis
Key effects
Diarrhoea and nausea · Headache
Monitor
Weight · Mood · Diarrhoea
ATC
L04AA32

No doses: the clinician sets them by the current guideline.

Mechanism of action

The figure shows apremilast in the catalytic site of human PDE4D (crystal structure).

Target in 3D: Phosphodiesterase 4 (cAMP-specific). PDB structure 7CBQ (RCSB PDB, public domain). View the structure at RCSB PDB

Apremilast is a small-molecule inhibitor of phosphodiesterase 4, the main enzyme that breaks down cyclic AMP in immune cells. Higher intracellular cAMP lowers the expression of pro-inflammatory cytokines such as TNF, interferon-gamma, IL-17 and IL-23. This damps the immune pathway that drives psoriasis and psoriatic arthritis. Exactly how this produces the clinical effect is not fully defined.

  1. Apremilast blocks PDE4 inside immune cells
  2. Cyclic AMP is no longer broken down and rises
  3. Pro-inflammatory cytokines (TNF, IL-17, IL-23) fall
  4. Skin plaques, joint inflammation and oral ulcers improve

Indications

Adverse effects

Common

  • Diarrhoea and nausea (most common)
  • Headache
  • Abdominal pain and vomiting
  • Upper respiratory infections, sore throat and nasal congestion

Contraindications

  • Hypersensitivity to apremilast
  • Caution with a history of depression or suicidal thoughts
  • Caution in older adults prone to dehydration or low blood pressure

Key interactions

St John's wort and other strong enzyme inducers
May lower apremilast levels and its effect

What is monitored

  • Weight, regularly
  • Mood, depression and suicidal thoughts
  • Diarrhoea, vomiting and hydration
  • Kidney disease, noted before starting

Administration and safety

  • Oral tablets swallowed whole, not split, chewed or crushed
  • The dose is built up gradually over the first days to lessen stomach upset

Pregnancy and breastfeeding

Human data are very limited; animal studies suggested a possible higher risk of fetal loss, so the potential risk is explained.

Nursing care

  • Ask about depression or suicidal thoughts before starting and at each visit
  • Weigh the patient regularly
  • Teach to report severe diarrhoea or vomiting
  • Review the medicine list and supplements, including St John's wort

Pharmacokinetics

Absorption
Oral tablet, with or without food

Test yourself

Think of the answer, then tap the question to see it.

Which enzyme does apremilast inhibit, and which messenger rises?

Phosphodiesterase 4; cyclic AMP rises.

What are three indications of apremilast?

Psoriatic arthritis, plaque psoriasis and the oral ulcers of Behçet disease.

Which psychiatric adverse effect is checked during apremilast treatment?

Depression and suicidal thoughts.

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Connections

← Back to the class: PDE4 inhibitors

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Apremilast: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); RCSB PDB - 7CBQ: Crystal structure of PDE4D catalytic domain in complex with Apremilast (RCSB Protein Data Bank, 2021); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.