Names and pronunciation
(a′puh-loo′tuh-mide) Erleada
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Drug reference
(a′puh-loo′tuh-mide) Erleada
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Func. class.: Antineoplastic
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Chem. class.: Anti-androgen receptor inhibitor
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ACTION: An androgen receptor inhi bitor that binds directly to the ligand- binding domain of the androgen receptor. It inhibits androgen receptor translocation and DNA binding and impedes androgen receptor–mediated transcription
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USES: For the treatment of non- metastatic castration-resistant prostate cancer
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CONTRAINDICATIONS: Preg nancy Precautions: Bone fractures, breast- feeding, contraception requirements, driving or operating machinery, geriatric patients, infertility, male-mediated terato- genicity, reproductive risk, seizure disor- der, seizures
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SIDE EFFECTS CNS: Fatigue CV: Hypertension, peripheral edema, heart failure, MI GI: Diarrhea, anorexia, nausea, weight loss GU: Hot flashes HEMA: Anemia, leukopenia, lymphopenia INTEG: Rash META: Hypercholesterolemia, hypertri- glyceridemia, hyperkalemia MS: Arthralgia, bone fractures
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INTERACTIONS Decrease: effects of CYP3A4 substrates— abemaciclib, cycloSPORINE, tacrolimus, sirolimus, DOCEtaxel, tamoxifen, PACLitaxel, cyclophosphamide, DOXOru bicin, erlotinib, etoposide, ifosfamide, teniposide, vinBLAStine, vinCRIStine, vindesine, imatinib, irinotecan, sorafenib, sunitinib, vemurafenib, temsirolimus, anastrozole, gefitinib, azole antifungals, macrolides, clarithromycin, erythromy- cin, telithromycin, dapsone, tricyclic an- tidepressants, SSRIs, some miscellaneous antidepressants, antipsychotics, opioids, benzodiazepines, some hypnotics, busPIRone, statins, calcium channel blockers, class I/III antidysrhythmics, PDE5 inhibitors, sex hormone agonists/ antagonists, H1-receptor antagonists, protease inhibitors, non-nucleoside re- verse transcriptase inhibitors; avoid con- current use
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DOSAGE AND ROUTES Nonmetastatic, castration-resistant prostate cancer • Adults: PO 240 mg daily until disease progression or toxicity; a gonadotropin- releasing hormone (GnRH) analog should be given concurrently or a bilateral orchi- ectomy should have been performed
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Available forms: Tablet 60 mg
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Evaluate: • Therapeutic response: decrease in prostatic size, decrease in spread of cancer Teach patient/family • Male-mediated teratogenicity: that product is not indicated for use in fe- males; that males with female partners of reproductive potential should avoid pregnancy and use effective contracep- tion during and for at least 3 mo after treatment; that product may impair male fertility • Seizures: about an increase in the risk of seizure and the risk of engaging in any activity where sudden loss of consciousness could cause harm to themselves or others (driving or operat- ing machinery). It is unknown whether antiepileptic medications will prevent seizures HIGH ALERT
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CLINICAL CONSIDERATIONS Assess • Possible bone fractures: monitor and manage patients at risk for bone frac- tures; consider the use of bone-targeted agents. Falls and fractures are possible • Seizures: use with caution in those with pre-existing seizure disorders; per- manently discontinue if seizure occurs • Geriatric patients: may be at increased risk for related adverse reactions; moni- tor closely for adverse reactions • Pregnancy/breastfeeding: contraindi- A cated in pregnancy, male infertility is a possibility
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PHARMACOKINETICS 96% plasma protein binding, primarily metabolized by CYP2C8 and CYP3A4 to its active metabolite, half-life 3 days, excreted 65% urine (unchanged), 24% feces (unchanged)
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• Adults: PO 240 mg daily until disease progression or toxicity; a gonadotropin- releasing hormone (GnRH) analog should be given concurrently or a bilateral orchi- ectomy should have been performed
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