Apremilast

What is Apremilast?

• Apremilast (OTEZLA), an inhibitor of phosphodiesterase 4 (PDE4) used for the treatment of certain types of psoriasis and psoriatic arthritis.

What are the uses of this medicine?

This medicine is used for the treatment of:

• Adult patients with active psoriatic arthritis.
• Patients with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.
• Adult patients with oral ulcers associated with Behçet's Disease.

How does this medicine work?

• Apremilast (a pre' mi last) is a small molecule inhibitor of the enzyme phosphodiesterase-4 (PDE-4) that is responsible for the degradation of cyclic adenosine monophosphate (cAMP), thereby blocking an important step in the inflammatory signaling of immune effector cells including T lymphocytes, monocytes and macrophages.
• Apremilast therapy has been shown to decrease the level of circulating proinflammatory cytokines and to improve symptoms in cases of psoriatic arthritis that have not responded to conventional therapies.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• a known hypersensitivity to apremilast or to any of the excipients in the formulation.

What drug interactions can this medicine cause?

• Use with strong cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended because loss of efficacy may occur.

Is this medicine FDA approved?

• Apremilast was approved as oral therapy of active psoriatic arthritis and for moderate-to-severe plaque psoriasis in the United States in 2014.

How should this medicine be used?

Recommended Dosage:

Dosage in Psoriatic Arthritis, Psoriasis, and Behçet's Disease To reduce risk of gastrointestinal symptoms, titrate to recommended dose of 30 mg twice daily according to the following schedule

• 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 in Severe Renal Impairment:

• Recommended dose is 30 mg once daily
• For initial dosage titration, titrate using only morning schedule listed in TABLE 1 and skip afternoon doses

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 10 mg, 20 mg, 30 mg

This medicine is available in fallowing brand namesː

• OTEZLA

What side effects can this medication cause?

The most common side effects of this medicine include: Psoriatic Arthritis:

• diarrhea
• nausea
• headache

Psoriasis:

• diarrhea
• nausea
• upper respiratory tract infection
• headache
• tension headache

Behçet's Disease:

• diarrhea
• nausea
• headache
• upper respiratory tract infection

What special precautions should I follow?

• There have been postmarketing reports of severe diarrhea, nausea, and vomiting associated with the use of OTEZLA. Consider OTEZLA dose reduction or suspension if patients develop severe diarrhea, nausea, or vomiting.
• Treatment with OTEZLA is associated with an increase in adverse reactions of 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.
• During the controlled period of the studies in psoriatic arthritis (PsA), weight decrease between 5%-10% of body weight was reported in patients treated with OTEZLA. Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of OTEZLA.
• Use with strong cytochrome P450 enzyme inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended because loss of efficacy may occur.

What to do in case of emergency/overdose?

Management of overdosage:

• In case of overdose, patients should seek immediate medical help.
• Patients should be managed by symptomatic and supportive care should there be an overdose.

Can this medicine be used in pregnancy?

• OTEZLA use in pregnant women have not established a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes, but these data are extremely limited.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to OTEZLA during pregnancy. Information about the registry can be obtained by calling 1-877-311-8972 or visiting https://mothertobaby.org/ongoing-study/otezla/.

Can this medicine be used in children?

• The safety and effectiveness of OTEZLA in pediatric patients less than 18 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• APREMILAST

Inactive ingredients:

• MICROCRYSTALLINE CELLULOSE
• LACTOSE MONOHYDRATE
• CROSCARMELLOSE SODIUM
• MAGNESIUM STEARATE

Who manufactures and distributes this medicine?

Packager: Celgene Corporation

What should I know about storage and disposal of this medication?

• Store tablets below 30°C (86°F).

• Dailymed label info on Apremilast
• FDA Apremilast