phosphodiesterase type 4 inhibitors
- Active psoriatic arthritis.
- Moderate to severe plaque psoriasis in patients who are candidates for phototherapy or systemic therapy.
Acts as an inhibitor of phosphodiesterase type 4 (PDE4). Inhibition of PDE4 results in ↑ intracellular levels of cyclic adenosine monophosphate (cAMP).
- Decreased severity of psoriatic arthritis with improved joint function.
- Reduced severity of plaques.
Absorption: 73% absorbed following oral administration.
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†)
|PO||unknown||2.5 hr||12–24 hr|
- Concurrent use of P450 enzyme inducers.
Use Cautiously in:
- History of depression or suicidal ideation
- Severe renal impairment (dose ↓ required for CCr <30 mL/min)
- OB: Use during pregnancy only if potential benefits justify potential fetal risks;
- Lactation:Use caution if breastfeeding;
- Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
CNS: depression, headache
GI: diarrhea, nausea, upper abdominal pain, vomiting
Metabolic: weight loss
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
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.
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.
Tablets: 10 mg, 20 mg, 30 mg
- 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.
- Follow titration guidelines when beginning therapy to minimize GI side effects.
- PO: Administer without regard for meals. Swallow tablet whole; do not crush, break, or chew.
- Instruct patient to take apremilast as directed.
- 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 need to monitor weight regularly. Notify health care professional if unexplained or clinically significant weight loss occurs.
- 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.
- Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
- Improvement in pain and function in patients with psoriatic arthritis.
- Increased healing of lesions in plaque psoriasis.
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