Dosing & Uses
Dosage Forms & Strengths
tablet
- 10mg
- 20mg
- 30mg
Psoriatic Arthritis
Indicated for active psoriatic arthritis
Day 1: 10 mg in AM
Day 2: 10 mg AM and PM
Day 3: 10 mg AM and 20 mg PM
Day 4: 20 mg AM and PM
Day 5: 20 mg AM and 30 mg PM
Day 6 and thereafter: 30 mg PO BID
Psoriasis
Indicated for moderate-to-severe plaque psoriasis in adults who are candidates for phototherapy or systemic therapy
Day 1: 10 mg in AM
Day 2: 10 mg AM and PM
Day 3: 10 mg AM and 20 mg PM
Day 4: 20 mg AM and PM
Day 5: 20 mg AM and 30 mg PM
Day 6 and thereafter: 30 mg PO BID
Oral Ulcers associated with Behςet Disease
Indicated for oral ulcers associated with Behςet disease
Day 1: 10 mg in AM
Day 2: 10 mg AM and PM
Day 3: 10 mg AM and 20 mg PM
Day 4: 20 mg AM and PM
Day 5: 20 mg AM and 30 mg PM
Day 6 and thereafter: 30 mg PO BID
Dosage Modifications
Hepatic impairment: No dosage adjustment required
Renal impairment
- Mild-to-moderate (CrCl ≥30): No dosage adjustment required
- Severe (CrCl <30 mL/min)
- Reduce dose to 30 mg PO qDay
- For initial dosage titration, titrate using only the AM schedule listed above and skip the PM doses
Safety and efficacy not established
Ulcerative Colitis (Orphan)
Orphan designation for treatment of pediatric patients with ulcerative colitis
Sponsor
- Celgene Corporation; 86 Morris Avenue Summit, New Jersey 07901
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10% (Psoriasis and Psoriatic Arthritis)
Diarrhea (7.7-17%)
Nausea (7.4-17%)
>10% (Behςet Disease)
Diarrhea (41.3%)
Nausea (19.2%)
Headache (14.4%)
Upper respiratory tract infection (11.5%)
1-10% (Behςet Disease)
Upper abdominal pain (8.7%)
Vomiting (8.7%)
Back pain (7.7%)
Viral upper respiratory tract infection (6.7%)
Arthralgia (5.8%)
1-10% (Psoriasis and Psoriatic Arthritis)
Upper respiratory tract infection (0.6-9%)
Tension headache (8%)
Headache (4.8-6%)
Vomiting (0.8-4%)
Fatigue (3%)
Dyspepsia (3%)
Decreased appetite (3%)
Insomnia (2%)
Back pain (2%)
Migraine (2%)
Frequent bowel movements (2%)
Depression (1%)
Bronchitis (1%)
Tooth abscess (1%)
Folliculitis (1%)
Frequency Not Defined (Psoriasis and Psoriatic Arthritis)
Immune system disorders: Hypersensitivity
Investigations: Weight decrease
Gastrointestinal disorders: Frequent bowel movement, gastroesophageal reflux disease, dyspepsia
Metabolism and nutrition disorders: Decreased appetite
Nervous system disorders: Migraine
Respiratory, thoracic, and mediastinal disorders: Cough
Skin and SC tissue disorders: Rash
Warnings
Contraindications
Hypersensitivity to apremilast or to any of the excipients in the formulation
Cautions
Associated with an increase in adverse reactions of depression; before using, evaluate patient for history of depression and/or suicidal thoughts or behavior
Weight decrease of 5-10% of body weight reported in 10-12% of patients
Severe GI adverse effects
- Severe diarrhea, nausea, and vomiting reported; mostly occurred within the first few weeks of treatment
- In some cases, patients were hospitalized
- Patients aged ≥65 yr and patients taking medications that cause volume depletion or hypotension may be at a higher risk of these complications; monitor those who are more susceptible to complications of diarrhea or vomiting
- Quick improvement observed with dosage reduction or discontinuation; consider dose reduction or suspension if patients develop severe diarrhea, nausea, or vomiting
Drug interaction overview
- Coadministration with strong CYP inducers (eg, rifampin, carbamazepine, phenobarbital phenytoin) may occur and result in a loss of efficacy of apremilast; therefore, coadministration is not recommended
Pregnancy & Lactation
Pregnancy
Available pharmacovigilance data use in pregnant women have not established a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes, but data are extremely limited
Based on findings from animal reproduction studies, may increase the risk for fetal loss
Pregnancy exposure registry
- Registry monitors pregnancy outcomes in women exposed to apremilast during pregnancyRegistry information can be obtained by calling 1-877-311-8972 or visiting https://mothertobaby.org/ongoing-study/otezla
Animal data
- In a pre- and postnatal study in mice, apremilast was administered to pregnant female mice at doses of 10, 80, or 300 mg/kg/day from Day 6 of gestation through Day 20 of lactation, with weaning on Day 21
- Dystocia, reduced viability, and reduced birth weights occurred at doses corresponding to ≥4-times the MRHD (on an AUC basis at doses ≥80 mg/kg/day)
- No adverse effects occurred at a dose 1.3- times the MRHD (10 mg/kg/day)No evidence for functional impairment of physical development, behavior, learning ability, immune competence, or fertility in the offspring at doses up to 7.5-times the MRHD (on an AUC basis at a dose of 300 mg/kg/day)
- Apremilast distributed across the placenta into the fetal compartment in mice and monkeys
- Advise pregnant women of the potential risk of fetal lossConsider pregnancy planning and prevention for females of reproductive potential
Lactation
There are no data on the presence of apremilast in human milk, the effects on the breastfed infant, or the effects on milk production
Detected in the milk of lactating mice
Consider developmental and health benefits of breastfeeding along with the mother’s clinical need and any potential adverse effects on the breastfed infant or from the underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Oral small molecule inhibitor of phosphodiesterase-4 specific for cAMP, resulting in increased intracellular cAMP levels
The specific mechanism by which apremilast exerts it therapeutic action in psoriatic arthritis is not well defined
Absorption
Absolute bioavailability: 73%
Peak plasma time: 2.5 hr
Coadministration with food does not alter absorption
Distribution
Protein bound: 68%
Vd: 87 L
Metabolism
Apremilast is a major circulating component (45%) followed by inactive metabolite M12 (39%), a glucuronide conjugate of O-demethylated apremilast
Metabolized by both CYP oxidative metabolism with subsequent glucuronidation and non-CYP mediated hydrolysis
In vitro CYP metabolism primarily by CYP3A4, with minor contribution from CYP1A2 and CYP2A6
Elimination
Half-life: 6-9 hr
Clearance: 10 L/hr
Excretion: 58% urine; 39% feces
Administration
Oral Administration
To reduce risk of GI symptoms associated with initial therapy, titrate to recommended dose (30 mg PO BID) according to the dosage schedules listed above
Can be administered without regard to meals
Swallow tablet whole; do not crush, split, or chew
Storage
Store below 30ºC (86ºF)
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Patient Handout
Formulary
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