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 ?
NASDAQ: CELG) has presented data from the phase III RELIEF clinical trial of Otezla (apremilast) in patients with active Behcet's Disease with oral ulcers at the 2018 American Academy of Dermatology annual meeting, the company said.
OTEZLA is Celgene's oral selective inhibitor of phosphodiesterase 4.
However, it was found to be less effective when it was indirectly compared with systemic biological therapies and Celgene's (NASDAQ: CELG) Otezla (apremilast).
The nine drugs listed are Entresto ( for heart conditions), Erivedge ( for basal cell carcinoma), Brintellix ( for depression), Otezla ( for psoriasis & psoriatic arthritis), Lynparza ( for ovarian cancer), Gazyvaro (for follicular lymphoma), Entyvio (for Crohn's & ulcerative colitis), Opdivo ( for renal cell carcinoma), Opdivo ( for Hodgkin's lymphoma).
Curran joined Celgene in 2013, and since April she has served as president of worldwide markets, I&I, leading the global launch of Otezla, a medication for the treatment of certain types of psoriasis and psoriatic arthritis.
In a U-turn by the National Institute for Health and Care Excellence (NICE), patients will now be able to access Otezla on the NHS in Wales and England, bringing availability in line with Scotland.
This growth will be driven primarily by the highly anticipated arrivals of promising systemic therapies- interleukin-17 (IL-17) inhibitors (Cosentyx, guselkumab and tildrakizumab), interleukin-23 (IL-23) inhibitors (ixekizumab and brodalumab) as well as phsophodiesterase (PDE4) inhibitor- Otezla (apremilast).
Additionally, the recent launch of products like Otezla and Stelara is also expected to boost market growth during the forecast period, resulting in its moderate CAGR of nearly 5% by 2019.
This is anchored by the successful global launch of Otezla (apremilast) in psoriasis and psoriatic arthritis, and new opportunities for expansion as a result of the addition of the Receptos programmes.
Otezla, recently approved as a treatment for psoriasis, could eclipse the billion-dollar sales mark by 2017.
Apremilast is approved as Otezla for the treatment of adults with psoriatic arthritis and is under study for other chronic inflammatory diseases, including rheumatoid arthritis and ankylosing spondylitis.
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.