Apemilast10 mg

Apemilast 10 mg is indicated for the treatment of adult patients with active psoriatic arthritis and moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.

Disease-modifying antirheumatic drugs (DMARDs)

Apemilast 10 mg is a novel, orally available small molecule inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4). PDE-4 is a cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase that is predominantly located in inflammatory cells. By inhibiting PDE-4, Apemilast 10 mg increases intracellular levels of cAMP and thereby inhibits the production of multiple proinflammatory mediators including PDE-4, TNF-alpha, interleukin-2 (IL-2), interferon-gamma, leukotrienes, and nitric oxide synthase. By targeting a central component of the inflammatory signaling cascade rather than a single inflammatory marker, PDE-4 inhibition may restore the homeostatic balance between pro- and anti-inflammatory signalling.

The recommended initial dosage titration of Apemilast 10 mg 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. Apemilast 10 mg can be administered without regard to meals.Day 1: 10 mg in morningDay 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 dailyDosage adjustment in patients with severe renal impairment. Apemilast 10 mg dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Apemilast 10 mg be titrated using only the morning schedule and the evening doses be skipped.

The recommended initial dosage titration of Apemilast 10 mg 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. Apemilast 10 mg can be administered without regard to meals.Day 1: 10 mg in morningDay 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 dailyDosage adjustment in patients with severe renal impairment. Apemilast 10 mg dosage should be reduced to 30 mg once daily in patients with severe renal impairment. For initial dosage titration, it is recommended that Apemilast 10 mg be titrated using only the morning schedule and the evening doses be skipped.

Co-administration of strong cytochrome P450 enzyme inducer Rifampin resulted in a reduction of systemic exposure of Apemilast 10 mg.Therefore.the use of cytochrome P450 enzyme inducers (e.g. Rifampin, Phenobarbital,Carbamazepine, Phenytoin) with Apemilast 10 mg is not recommended.

Apemilast 10 mg is contraindicated in patients with a known hypersensitivity to Apemilast 10 mg or to any of the excipients in the formulation.

The most frequently occurring side effects of Apemilast 10 mg are nausea, diarrhea and headache. Other less frequent side effects are upper respiratory tract infection, vomiting, naospharyngitis, abdominal pain, hypersensitivity, gastroesophageal reflux disease, dyspepsia, fatigue, decrease appetite, cough, rash, insomnia.

Pregnancy Category C. It is not known whether Apemilast 10 mg or its metabolites are present in human milk; however, Apemilast 10 mg was detected in milk of lactating mice. Caution should be exercised when Apemilast 10 mg is administered to a nursing woman.

Treatment with Apemilast 10 mg 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 Apemilast 10 mg 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 Apemilast 10 mg 30 mg twice daily compared to 3.3% treated with placebo.

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

Use in Paediatric patient: The safety and effectiveness of Apemilast 10 mg in paediatric patients less than 18 years of age have not been established.

Disease-modifying antirheumatic drugs (DMARDs)

Apemilast 10 mg is a novel, orally available small molecule inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4). PDE-4 is a cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase that is predominantly located in inflammatory cells. By inhibiting PDE-4, Apemilast 10 mg increases intracellular levels of cAMP and thereby inhibits the production of multiple proinflammatory mediators including PDE-4, TNF-alpha, interleukin-2 (IL-2), interferon-gamma, leukotrienes, and nitric oxide synthase. By targeting a central component of the inflammatory signaling cascade rather than a single inflammatory marker, PDE-4 inhibition may restore the homeostatic balance between pro- and anti-inflammatory signalling.

Pregnancy Category C. It is not known whether Apemilast 10 mg or its metabolites are present in human milk; however, Apemilast 10 mg was detected in milk of lactating mice. Caution should be exercised when Apemilast 10 mg is administered to a nursing woman.

Use in Paediatric patient: The safety and effectiveness of Apemilast 10 mg in paediatric patients less than 18 years of age have not been established.