Arsenor

Arsenor Tablet

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.

Uses

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

Arsenor

Trade Name Arsenor
Generic Apremilast
Apremilast Other Names Aprémilast, Apremilast, Apremilastum
Weight 10mg, 30mg
Type Tablet
Formula C22H24N2O7S
Weight Average: 460.5
Monoisotopic: 460.130422295
Protein binding

The plasma protein binding of apremilast is about 68%.

Therapeutic Class Disease-modifying antirheumatic drugs (DMARDs)
Manufacturer Beacon Pharmaceuticals Ltd
Available Country Bangladesh
Last Updated: June 23, 2021 at 11:16 am

Structure

Arsenor
Apremilast Structure

Dosage

Arsenor dosage

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.

Side Effects

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.

Precaution

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.

Interaction

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.

Food Interaction

  • 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.

Half Life

The average elimination half-life of this drug ranges from 6-9 hours.

Clearance

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.

Contraindication

Arsenor is contraindicated in patients with a known hypersensitivity to Arsenor or to any of the excipients in the formulation.

Special Warning

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.

Storage Condition

Store at cool & dry place, protected from light & moisture. Keep the medicine out of the reach of children.

Innovators Monograph

Arsenor contains Apremilast see full prescribing information from innovator Monograph