Apremilast
Indications
Apremilast 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.
Pharmacology
Apremilast 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, apremilast 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.
Dosage & Administration
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.
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.
Interaction
Co-administration of strong cytochrome P450
enzyme inducer Rifampin resulted in a reduction of systemic exposure of
Apremilast.Therefore.the use of cytochrome P450 enzyme inducers (e.g.
Rifampin, Phenobarbital,Carbamazepine, Phenytoin) with Apremilast is not
recommended.
Contraindications
Apremilast is contraindicated in patients
with a known hypersensitivity to Apremilast or to any of the excipients
in the formulation.
Side Effects
The most frequently occurring side effects
of Apremilast 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 & Lactation
Pregnancy Category C. It is not known
whether Apremilast or its metabolites are present in human milk;
however, Apremilast was detected in milk of lactating mice. Caution
should be exercised when Apremilast is administered to a nursing woman.
Precautions & Warnings
Treatment with Apremilast 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 Apremilast 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 Apremilast 30 mg twice daily compared to 3.3% treated with placebo.
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 Apremilast 30 mg twice daily compared to 3.3% treated with placebo.
Use in Special Populations
Use in Paediatric patient: The safety and effectiveness of Apremilast in paediatric patients less than 18 years of age have not been established.
Therapeutic Class
Disease-modifying antirheumatic drugs (DMARDs)
Storage Conditions
Store at cool & dry place, protected from light & moisture. Keep the medicine out of the reach of children.
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