apremilast

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 ?
The market is witnessing a strong presence of late-stage pipeline drugs such as tocilizumab, baricitinib, olokizumab, apremilast, abatacept, PF-06438179, golimumab, ustekinumab, etrolizumab, tofacitinib, and others.
The targeted synthetic DMARD apremilast, a small-molecule inhibitor that modulates inflammatory cytokine production via the inhibition of phosphodiesterase 4, has also been approved for the treatment of PsA.
(NASDAQ: CELG) to acquire rights to Otezla (apremilast), an oral, non-biologic treatment for psoriasis and psoriatic arthritis for USD 13.4bn in cash, the company said.
Release date- 26082019 - THOUSAND OAKS - Amgen (NASDAQ: AMGN) announced today that it has entered into an agreement with Celgene Corporation (NASDAQ: CELG) in connection with its previously announced merger with Bristol-Myers Squibb Company (NYSE: BMY) to acquire worldwide rights to Otezla(apremilast), the only oral, non-biologic treatment for psoriasis and psoriatic arthritis, and certain related assets and liabilities, for $13.4 billion in cash, or approximately $11.2 billion, net of the present value of $2.2 billion in anticipated future cash tax benefits.
US-based biotechnology company, Amgen (NASDAQ: AMGN), announced yesterday that it has entered into an agreement with Celgene Corporation (NASDAQ: CELG) in connection with its previously announced merger with Bristol-Myers Squibb Company (NYSE: BMY) to acquire worldwide rights to Otezla(R) (apremilast), a non-biologic treatment for psoriasis and psoriatic arthritis, and certain related assets and liabilities.
Under the terms of the agreement and subject to the closing conditions, Amgen (AMGN) will acquire OTEZLA and related intellectual property, including any patents that primarily cover apremilast, as well as other assets and liabilities related to OTEZLA.
In June, Bristol-Myers Squibb announced the planned divestiture of OTEZLA[R] (apremilast) in light of concerns raised by the U.S.
In conjunction, Bristol-Myers Squibb Company is planning the sale of OTEZLA (apremilast) to allow the transaction to close on a timely basis in light of concerns expressed by the FTC.
Otezla[R](apremilast) is an oral, nonbiologic phosphodiesterase-4 (PDE4) inhibitor indicated for moderate to severe plaque psoriasis.
Clinical review report: apremilast (Otezla) for treatment of adult patients with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy [Internet].
For the autoimmune diseases, the drugs and trade names are abatacept (Orencia), adalimumab (Humira), certolizumab pegol (Cimzia), etanercept (Enbrel), infliximab (Remicade), leflunomide (Arava), otezla (Apremilast), teriflunomide (Aubagio), tocilizumab (Actemra), tofacitinib (Xeljanz), and ustekinumab (Stelara).