Absorption: 73% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: Extensively metabolized (mostly by CYP3A4); metabolites are not pharmacologically active. Excreted in urine (58%) and feces (39%) as inactive metabolites; 3% excreted unchanged in urine, 7% in feces.
Half-life: 6–9 hr.
TIME/ACTION PROFILE (blood levels†)
ROUTE
ONSET
PEAK
DURATION
PO
unknown
2.5 hr
12–24 hr
† Improvement in joint symptoms make take up to 4 mos.
PO (Adults): Day 1: 10 mg in the morning; Day 2: 10 mg in the morning and 10 mg in the evening; Day 3: 10 mg in the morning and 20 mg in the evening; Day 4: 20 mg in the morning and 20 mg in the evening; Day 5: 20 mg in the morning and 30 mg in the evening; Day 6 and thereafter: 30 mg in the morning and 30 mg in the evening.
Renal Impairment PO (Adults CCr <30 mL/min): Days 1–3: 10 in the morning; days 4–5: 20 mg in the morning; day 6 and thereafter: 30 mg in the morning.
Assess pain and range of motion before and periodically during therapy.
Monitor mental status for signs and symptoms of depression (orientation, mood behavior) frequently. Assess for suicidal tendencies, especially during early therapy.
Obtain weight and BMI initially and periodically during treatment. If clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of therapy.
Advise patient, family and caregivers to look for suicidality, especially during early therapy or dose changes. Notify health care professional immediately if thoughts about suicide or dying, attempts to commit suicide, new or worse depression or anxiety, agitation or restlessness, panic attacks, insomnia, new or worse irritability, aggressiveness, acting on dangerous impulses, mania, or other changes in mood or behavior occur.
Inform patient of risk of nausea, vomiting, and diarrhea. Instruct patient to notify health care professional if severe nausea, vomiting or diarrhea occur; may need to consider dose reduction or interruption of therapy.
Inform patient of need to monitor weight regularly. Notify health care professional if unexplained or clinically significant weight loss occurs: may need to discontinue therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Encourage patients to enroll in pregnancy registry for women who have taken apremilast during pregnancy 1-877-311-8972 to enroll or visit https://mothertobaby.org/ongoing-study/otezla/