Names and pronunciation
(a-pre′mi-last) Otezla
PDF page 99
Loading InternPractice…
Drug reference
(a-pre′mi-last) Otezla
PDF page 99
Func. class.: Musculoskeletal agents: disease-modifying antirheumatic drugs (DMARDs)
PDF page 99
Chem. class.: Phosphodiesterase-4 inhibitors
PDF page 99
ACTION: A phosphodiesterase-4 (PDE4) inhibitor specific for cyclic ad- enosine monophosphate (cAMP). Inhi- bition of PDE4 results in an increase in intracellular concentration of cAMP, with a partial inhibition of proinflamma- tory mediators and an increase in the production of some antiinflammatory mediators
PDF page 99
USES: Treatment of active psoriatic arthritis; severe plaque psoriasis (in those not a candidate for phototherapy)/ oral ulcers in Behcet disease
PDF page 99
CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, depression/suicidal, renal disease (CCr <30 mL/min) DOSAGES AND ROUTES Active psoriatic arthritis/severe plaque psoriasis/oral ulcers in Behcet’s disease • Adult: PO day 1: 10 mg PO AM; day 2: 10 mg AM and PM; day 3: 10 mg AM and 20 mg PM; day 4: 20 mg AM and PM; day 5: 20 mg AM and 30 mg PM; day 6 and thereafter: 30 mg bid Renal dose • Adult: PO CCr ≥30 mL/min: no change; CCr <30 mL/min: 30 mg every day. Initially, 10 mg AM days 1-3; 20 mg AM days 4 and 5; 30 mg every day for day 6 and thereafter
PDF page 100
SIDE EFFECTS CNS: Headache, depression, suicidal ideation, fatigue, insomnia GI: Diarrhea, nausea, vomiting, abdomi- nal pain, frequent bowel movements, dyspepsia, weight loss RESP: URI, pharyngitis, bronchitis SYST: Hypersensitivity reactions MS: Back pain
PDF page 100
INTERACTIONS Decrease: apremilast—CYP3A4 induc- ers (rifAMPin, isoniazid, pyrazinamide, barbiturates, phenytoin, carBAMazepine, enzalutamide); avoid concurrent use Drug/Herb Decrease: apremilast—CYP3A4 inducers (St. John’s wort); avoid concurrent use
PDF page 100
Available forms: Tablets 10, 20, 30 mg; starter pack
PDF page 100
Administer: • Give whole; do not crush, break, or chew; give without regard to meals
PDF page 100
Assess: • Psoriatic arthritis/severe plaque pso- riasis: assess for hypersensitivity reactions • For depression and suicidal ideation, mood changes • For renal failure or severe renal im- pairment (CrCl <30 mL/min), dosage re- duction is required • For significant or unexplained weight loss; report weight loss, as therapy may need to be discontinued • Pregnancy and breastfeeding: if preg- nancy is planned or suspected; use only if benefits outweigh fetal risk; if used during pregnancy, call 877-311-8972; cautious use in breastfeeding
PDF page 100
Evaluate: • Therapeutic response: resolution of symptoms of psoriatic arthritis or plaque psoriasis
PDF page 100
CLINICAL CONSIDERATIONS
PDF page 100
Patient and caregiver information: • To report new rash, hypersensitivity reactions; report change in urine output, renal disease history • To be alert for depression and suicidal ideation, mood changes; if these occur, notify prescriber immediately
PDF page 100
PHARMACOKINETICS 68% protein binding; metabolized by CYP3A4; half-life 6-9 hr; excreted urine 58%, feces 39%; peak 2.5 hr
PDF page 100