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Warnings 

Description 

Description:
The active ingredient in OTEZLA tablets is apremilast. Apremilast is a phosphodiesterase 4 (PDE4) inhibitor. Apremilast is known chemically as N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide. Its empirical formula is C22H24N2O7S and the molecular weight is 460.5.
OTEZLA tablets are supplied in 10, 20, and 30 mg strengths for oral administration. Each tablet contains apremilast as the active ingredient and the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, iron oxide red, iron oxide yellow (20 and 30 mg only) and iron oxide black (30 mg only).

Clinical pharmacology

Mechanism of Action:
Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients is not well defined.

Indications and usage 

INDICATIONS AND USAGE:
OTEZLA, an inhibitor of phosphodiesterase 4 (PDE4), is indicated for the treatment of adult patients with active psoriatic arthritis.

Contraindications

Contraindications:
Known hypersensitivity to apremilast or any excipients in formulation

Precautions

WARNINGS AND PRECAUTIONS:

  1.  Depression: Advise patients, their caregivers, and families 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. Carefully weigh risks and benefits of treatment with OTEZLA in patients with a history of depression and/or suicidal thoughts or behavior.
  2. Weight Decrease: Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of OTEZLA
  3. Drug Interactions: Use with strong cytochrome P450 enzyme inducers (e.g. rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended because loss of efficacy may occur

Adverse reactions

ADVERSE REACTIONS:
The most common adverse reactions (geq 5%) are diarrhea, nausea, and headache.

To report SUSPECTED ADVERSE REACTIONS, contact Celgene Corporation at 1-888-423-5436 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

USE IN SPECIFIC POPULATIONS
Severe Renal Impairment: Increased systemic exposure of OTEZLA has been observed, reduction in dose to 30 mg once daily is recommended

See PACKAGE INSERT for PATIENT COUNSELING INFORMATION and Medication Guide.

Dosage and administration 

DOSAGE AND ADMINISTRATION::

Dosage in Psoriatic Arthritis
The recommended initial dosage titration of OTEZLA from Day 1 to Day 5 is shown in Table 1. 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.

OTEZLA can be administered without regard to meals. Do not crush, split, or chew the tablets.
Table 1: Dosage Titration Schedule
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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
OTEZLA dosage should be reduced to 30 mg once daily in patients with severe renal impairment (creatinine clearance (CLcr) of less than 30 mL per minute estimated by the Cockroft-Gault equation). For initial dosage titration in this group, it is recommended that OTEZLA be titrated using only the AM schedule listed in Table 1 and the PM doses be skipped.

How supplied

DOSAGE FORMS AND STRENGTHS:
Tablets: 10 mg, 20 mg, 30 mg

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates.  A local search option of this data can be found here.

Disclaimer

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