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Apremilast

Medically reviewed by Drugs.com. Last updated on Jul 14, 2020.

Pronunciation

(a PRE mi last)

Index Terms

  • CC-10004

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Otezla: 30 mg

Tablet Therapy Pack, Oral:

Otezla: 10 & 20 & 30 mg (55 ea)

Brand Names: U.S.

  • Otezla

Pharmacologic Category

  • Phosphodiesterase-4 Enzyme Inhibitor

Pharmacology

Apremilast inhibits phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP) which results in increased intracellular cAMP levels and regulation of numerous inflammatory mediators (eg, decreased expression of nitric oxide synthase, TNF-α, and interleukin [IL]-23, as well as increased IL-10) (Schafer, 2012).

Absorption

Well absorbed

Distribution

Vd: 87 L

Metabolism

Hepatic, primarily via CYP3A4: minor pathways include CYP1A2 and CYP2A6

Excretion

Urine (58%; 3% unchanged drug); feces (39%; 7% unchanged drug)

Time to Peak

~2.5 hours

Half-Life Elimination

~6 to 9 hours

Protein Binding

~68%

Special Populations: Renal Function Impairment

The AUC and Cmax of apremilast increased by ~88% and 42%, respectively, in patients with severe renal impairment.

Special Populations: Elderly

The apremilast exposure in elderly subjects (65 to 85 years of age) was about 13% higher in AUC and about 6% higher in Cmax than in younger subjects (18 to 55 years of age).

Special Populations: Gender

The extent of exposure in females was about 31% higher and Cmax was about 8% higher than that in male subjects.

Use: Labeled Indications

Behçet disease: Treatment of oral ulcers associated with Behçet disease.

Psoriasis: Treatment of patients with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.

Psoriatic arthritis: Treatment of patients with active psoriatic arthritis.

Contraindications

Hypersensitivity to apremilast or any component of the formulation.

Canadian labeling: Additional contraindications (not in US labeling): Pregnancy; breastfeeding.

Dosing: Adult

Behçet disease, psoriasis, or psoriatic arthritis: Oral: Initial: 10 mg in the morning on day 1. Titrate upward by additional 10 mg per day on days 2 to 5 as follows: Day 2: 10 mg twice daily; Day 3: 10 mg in the morning and 20 mg in the evening; Day 4: 20 mg twice daily; Day 5: 20 mg in the morning and 30 mg in the evening. Maintenance dose: 30 mg twice daily starting on day 6.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Administration

Oral: Administer without regard to food. Do not crush, chew, or split tablets.

Storage

Store below 30°C (86°F).

Drug Interactions

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Apremilast. Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Apremilast. Avoid combination

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to concomitant therapy when possible. If concomitant therapy cannot be avoided, monitor for reduced clinical effects of the CYP3A4 substrate. Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Riociguat: Apremilast may enhance the hypotensive effect of Riociguat. Management: Riociguat is contraindicated with nonselective phosphodiesterase (PDE) inhibitors and PDE type 5 inhibitors. Other types of PDE inhibitors are not contraindicated, but caution is advised and patients should be monitored for hypotension. Monitor therapy

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Endocrine & metabolic: Weight loss (>5% of body weight: 5%; 5% to 10% of body weight: 10% to 12%; ≥10% of body weight: 2%)

Gastrointestinal: Diarrhea (8% to 41%; severe diarrhea: <1%), nausea (7% to 22%; severe nausea: <1%)

Nervous system: Headache (5% to 14%; severe headache: <1%)

Respiratory: Upper respiratory tract infection (4% to 12%; viral upper respiratory tract infection: 7%)

1% to 10%:

Dermatologic: Folliculitis (1%)

Gastrointestinal: Abdominal pain (4%; upper abdominal pain: ≤9%; severe abdominal pain: <1%), decreased appetite (3%), dyspepsia (3%), frequent bowel movements (2%), vomiting (≤9%; severe vomiting: <1%)

Infection: Tooth abscess (1%)

Nervous system: Depressed mood (≤1%), depression (≤1%; severe depression: <1%), fatigue (3%), insomnia (2%), migraine (2%), tension headache (8%)

Neuromuscular & skeletal: Arthralgia (6%), back pain (2% to 8%)

Respiratory: Bronchitis (1%), nasopharyngitis (3%), sinus headache (1%)

<1%:

Dermatologic: Exacerbation of psoriasis (rebound following discontinuation)

Nervous system: Suicidal ideation, suicidal tendencies

Frequency not defined:

Dermatologic: Skin rash

Gastrointestinal: Gastroesophageal reflux disease

Hypersensitivity: Hypersensitivity reaction

Respiratory: Cough

Warnings/Precautions

Concerns related to adverse effects:

• GI effects: Severe diarrhea, nausea, and vomiting have been reported, usually observed within the first few weeks of initiating therapy. Monitor patients who are more susceptible to complications of diarrhea or vomiting; use with caution in elderly patients (≥65 years) and patients taking medications that may lead to volume depletion or hypotension. Symptom improvement observed with dose reduction or discontinuation of therapy; consider dose reduction or suspension of therapy if severe symptoms occur.

• Neuropsychiatric effects: Neuropsychiatric effects (eg, depression, suicidal ideation, mood changes) have been reported. Use with caution in patients with a history of depression and/or suicidal thoughts /behavior. Instruct patients/caregivers to report worsening psychiatric symptoms and consider risks/benefits of continuation of therapy in such patients.

• Weight loss: May cause weight loss; monitor weight regularly. Discontinuation of therapy should be considered with unexplained or significant weight loss.

Disease-related concerns:

• Renal impairment: Use with caution in renal impairment. Systemic exposure is increased in patients with severe renal impairment (CrCl <30 mL/minute); dosage reduction is recommended.

Monitoring Parameters

Monitor weight regularly during therapy; renal function; signs or symptoms of mood changes, depression, or suicidal thoughts

Reproductive Considerations

Due to potential toxicity, discontinue use ≥2 days prior to a planned pregnancy (Rademaker 2018).

Pregnancy Considerations

Due to potential toxicity and limited information related to use in pregnancy, use is not currently recommended in pregnant females (Rademaker 2018).

A registry is available for women exposed to apremilast during pregnancy (877-311-8972).

Patient Education

What is this drug used for?

• It is used to treat psoriatic arthritis.

• It is used to treat plaque psoriasis.

• It is used to treat oral ulcers caused by Behçet disease.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache

• Weight loss

• Abdominal pain

• Back pain

• Joint pain

• Common cold symptoms

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Depression like thoughts of suicide, anxiety, emotional instability, agitation, irritability, panic attacks, mood changes, behavioral changes, or confusion

• Severe diarrhea

• Nausea

• Severe or persistent vomiting

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Frequently Asked Questions