Arsenor 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 Arsenor exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.
Arsenor 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.
Arsenor is also used to associated treatment for these conditions: Psoriatic arthritis aggravated, Severe Plaque psoriasis, Moderate Plaque psoriasis, Ulceration of the mouth
|Apremilast Other Names||Aprémilast, Apremilast, Apremilastum|
The plasma protein binding of apremilast is about 68%.
|Therapeutic Class||Disease-modifying antirheumatic drugs (DMARDs)|
|Manufacturer||Beacon Pharmaceuticals Ltd|
|Last Updated:||June 23, 2021 at 11:16 am|
The recommended initial dosage titration of Arsenor 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. Arsenor 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
Arsenor dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Arsenor be titrated using only the morning schedule and the evening doses be skipped.
The most frequently occurring side effects of Arsenor 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 Arsenor 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 Arsenor 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 Arsenor 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 Arsenor.Therefore.the use of cytochrome P450 enzyme inducers (e.g. Rifampin, Phenobarbital,Carbamazepine, Phenytoin) with Arsenor is not recommended.
- Avoid St. John's Wort. Arsenor 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 Arsenor or its metabolites are present in human milk; however Arsenor was detected in milk of lactating mice. Caution should be exercised when Arsenor is administered to a nursing woman.
Usage in Pediatric Patients
The safety and effectiveness of Arsenor in pediatric patients less than18 years of age have not been established.
Arsenor is contraindicated in patients with a known hypersensitivity to Arsenor or to any of the excipients in the formulation.
Use in Paediatric patient: The safety and effectiveness of Arsenor 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 Arsenor. Therefore, the use of cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) with Arsenor is not recommended.
Store at cool & dry place, protected from light & moisture. Keep the medicine out of the reach of children.