Apremilast is indicated for the treatment of adult patients with active psoriatic arthritis and moderate to severe plaque psoriasis, particularly in those who are eligible for phototherapy or systemic treatment.

Apremilast is an orally active, selective inhibitor of phosphodiesterase-4 (PDE-4). This enzyme is primarily found in inflammatory cells and is responsible for the breakdown of cyclic adenosine monophosphate (cAMP). By inhibiting PDE-4, Apremilast increases intracellular cAMP levels, leading to a reduction in the production of pro-inflammatory mediators such as TNF-alpha, interleukins, interferon-gamma, leukotrienes, and nitric oxide synthase. Through this mechanism, it helps restore the balance between pro-inflammatory and anti-inflammatory signals in the body.

The recommended initial dosage titration of Apremilast from Day 1 to Day 5 is shown below. Following the 5-day titration, the recommended maintenance dosage is 30 mg twice daily taken orally starting on Day 6. This titration is intended to reduce the gastrointestinal symptoms associated with initial therapy. Apremilast can be administered without regard to meals.

Day 1: 10 mg in morning
Day 2: 10 mg in morning and 10 mg in evening
Day 3: 10 mg in morning and 20 mg in evening
Day 4: 20 mg in morning and 20 mg in evening
Day 5: 20 mg in morning and 30 mg in evening
Day 6: 30 mg twice daily

Dosage adjustment in patients with severe renal impairment. Apremilast dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Apremilast be titrated using only the morning schedule and the evening doses be skipped.

Co-administration of Apremilast with strong cytochrome P450 enzyme inducers such as rifampin significantly reduces its systemic exposure. Therefore, concurrent use with potent CYP450 inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended.

Apremilast is contraindicated in patients with known hypersensitivity to Apremilast or any component of the formulation.

The most commonly reported side effects include nausea, diarrhea, and headache. Other less frequent effects include upper respiratory tract infections, vomiting, nasopharyngitis, abdominal pain, hypersensitivity reactions, gastroesophageal reflux disease, indigestion, fatigue, decreased appetite, cough, rash, and insomnia.

Pregnancy Category C. It is unknown whether Apremilast or its metabolites are excreted in human breast milk, although animal studies have shown its presence in milk. Use with caution in breastfeeding women.

Apremilast treatment has been associated with an increased risk of depression and mood changes. Patients and caregivers should monitor for signs of depression or suicidal thoughts and seek medical advice if such symptoms occur.

Weight loss (5–10% of body weight) has also been observed in some patients during treatment. Careful evaluation of risks and benefits is required if these effects develop.

The safety and effectiveness of Apremilast in pediatric patients under 18 years of age have not been established.

Disease-modifying antirheumatic drug (DMARD).

Store in a cool, dry place, protected from light and moisture. Keep out of reach of children.