Aprila is an inhibitor of phosphodiesterase 4 (PDE4) enzyme specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism by which Aprila exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.
Aprila is used for the treatment of adult patients with active psoriatic arthritis and moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.
Aprila is also used to associated treatment for these conditions: Psoriatic arthritis aggravated, Severe Plaque psoriasis, Moderate Plaque psoriasis, Ulceration of the mouth
|Other Names||Aprémilast, Apremilast, Apremilastum|
The plasma protein binding of apremilast is about 68%.
|Therapeutic Class||Disease-modifying antirheumatic drugs (DMARDs)|
|Manufacturer||Drug International Ltd|
|Last Updated:||June 23, 2021 at 11:16 am|
Table Of contents
The recommended initial dosage titration of Aprila 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. Aprila 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 and thereafter: 30 mg twice daily
Dosage adjustment in patients with severe renal impairment
Aprila dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Aprila be titrated using only the morning schedule and the evening doses be skipped.
The most frequently occurring side effects of Aprila are nausea, diarrhea, and headache.
Other less frequent side effects are upper respiratory tract infection, vomiting, nasopharyngitis, abdominal pain, hypersensitivity, gastroesophageal reflux disease, dyspepsia, fatigue, decrease appetite, cough, rash, insomnia.
Treatment with Aprila is associated with an increase in adverse reactions of depression. Patients, their caregivers and families should be advised of the need to be alert for the emergence or worsening of depression, suicidal thoughts or other mood changes and if such changes occur to contact their healthcare provider. Prescribers should carefully evaluate the risks and benefits of continuing treatment with Aprila if such events occur.
During the controlled period of the studies in psoriatic arthritis, weight decrease between 5%-10% of body weight was reported in 10% of subjects treated with Aprila 30 mg twice daily compared to 3.3% treated with placebo.
Co-administration of strong cytochrome P450 enzyme inducer Rifampin resulted in a reduction of systemic exposure of Aprila.Therefore.the use of cytochrome P450 enzyme inducers (e.g. Rifampin, Phenobarbital,Carbamazepine, Phenytoin) with Aprila is not recommended.
- Avoid St. John's Wort. Aprila is a CYP3A substrate; therefore, co-administration with St. John's wort, a CYP3A inducer, may reduce the serum level of apremilast.
- Take with or without food.
Volume of Distribution
The average apparent volume of distribution (Vd) is about 87 L, suggesting that apremilast is distributed in the extravascular compartment.
The average elimination half-life of this drug ranges from 6-9 hours.
In healthy patients, the plasma clearance of apremilast is about 10 L/hour.
Pregnancy & Breastfeeding use
Pregnancy: Pregnancy Category C.
Nursing mothers: It is not known whether Aprila or its metabolites are present in human milk; however Aprila was detected in milk of lactating mice. Caution should be exercised when Aprila is administered to a nursing woman.
Usage in Pediatric Patients
The safety and effectiveness of Aprila in pediatric patients less than18 years of age have not been established.
Aprila is contraindicated in patients with a known hypersensitivity to Aprila or to any of the excipients in the formulation.
Use in Paediatric patient: The safety and effectiveness of Aprila in paediatric patients less than 18 years of age have not been established.
Interaction with other Medicine
Co-administration of strong cytochrome P450 enzyme inducer, rifampin, resulted in a reduction of systemic exposure of Aprila. Therefore, the use of cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) with Aprila is not recommended.
Store at cool & dry place, protected from light & moisture. Keep the medicine out of the reach of children.