apremilast

(redirected from Otezla)

apremilast

(a-pre-mil-ast),

Otezla

(trade name)

Classification

Therapeutic: antirheumatics
Pharmacologic: temporary class
Pregnancy Category: C

Indications

Treatment of active psoriatic arthritis.

Action

Acts as an inhibitor of phosphodiesterase type 4 (PDE4). Inhibition of PDE4 results in ↑ intracellular levels of cyclic adenosine monophosphate (cAMP).

Therapeutic effects

Decreased severity of psoriatic arthritis with improved joint function.

Pharmacokinetics

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†)

ROUTEONSETPEAKDURATION
POunknown2.5 hr 12–24 hr
† Improvement in joint symptoms make take up to 4 mos.

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Concurrent use of P450 enzyme inducers.
Use Cautiously in: History of depression or suicidal ideation; Severe renal impairment (dose reduction required for CCr <30 mL/min); Obstetric: Use during pregnancy only if potential benefits justify potential fetal risks; Lactation: Use caution if breastfeeding; Pediatric: Safe and effective use in children <18 yr has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • depression
  • headache

Gastrointestinal

  • diarrhea
  • nausea
  • upper abdominal pain
  • vomiting

Metabolic

  • weight loss

Interactions

Drug-Drug interaction

Concurrent use of P450 enzyme inducers including carbamazepine, phenobarbital, phenytoin and rifampin may ↓ blood levels and effectiveness; concurrent use should be avoided.

Route/Dosage

Oral (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

Oral (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.

Availability

Tablets: 10 mg, 20 mg, 30 mg

Nursing implications

Nursing assessment

  • 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.

Potential Nursing Diagnoses

Chronic pain (Indications)
Impaired skin integrity (Indications)
Deficient knowledge, related to medication regimen (Patient/Family Teaching)

Implementation

  • Follow titration guidelines when beginning therapy to minimize GI side effects.
  • Oral: Administer without regard for meals. Swallow tablet whole; do not crush, break, or chew.

Patient/Family Teaching

  • 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 if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

  • Improvement in pain and function in patients with psoriatic arthritis.
References in periodicals archive ?
According to Robbie McCarthy, Vice President of Rare Insights and Patient Portfolio at Spherix, "With an increasing number of biologic and novel treatment options such as Celgene's Otezla and Pfizer's Xeljanz now available, the competition for second and third line positioning is fierce.
Behcet's Disease Approval For Otezla Would Boost Celgene's Developing Autoimmune Presence - Corporate Activity 19.
Otezla, recently approved as a treatment for psoriasis, could eclipse the billion-dollar sales mark by 2017.
Celgene Corporation said the US Food and Drug Administration (FDA) has approved Otezla (apremilast), the company's oral, selective inhibitor of phosphodiesterase 4 (PDE4), for the treatment of adult patients with active psoriatic arthritis.
Food and Drug Administration today approved Otezla (apremilast) to treat adults with active psoriatic arthritis (PsA).
Its cancer drugs Abraxane and Revlimid have been helping drive double-digit revenue growth, and the company expects its newest product, psoriasis drug Otezla, to generate sales topping $1 billion within the next three years.
These findings, along with physician and payer views on the two new oral therapies: the recently launched Otezla (Celgene's apremelast), and Pfizer's emerging therapy Xeljanz (tofacitinib), shed light on the many changes that will occur in psoriasis treatment over the next three years.
TNF share expected to erode as Otezla sees greater adoption, according to Spherix Global Insights, GmbH
25, 2015 /PRNewswire/ -- Celgene Corporation (NASDAQ: CELG), the maker of OTEZLA (apremilast)-the first and only oral U.
The authorization of OTEZLA is a significant new option for the treatment of patients who are not experiencing satisfactory relief for their conditions.
Most recently, Celgene received FDA approval for its new oral treatment for psoriasis and psoriatic arthritis, Otezla.
The FDA also said yes to BioMarin's Vimizim for the treatment of Morquio A syndrome, Celgene's blockbuster hopeful Otezla and Amgen's leukemia drug, Blincyto.