Names and pronunciation
Emend
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Drug reference
Emend
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Func. class.: Antiemetic
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Chem. class.: Substance P/neurokinin antagonist
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Do not confuse: aprepitant/fosaprepitant
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ACTION: Selective antagonist of human substance P/neurokinin 1 (NK1) receptors that decreases emetic reflex
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USES: Prevention of nausea/vomiting associated with cancer chemotherapy (highly emetogenic/moderately emeto- genic), including high-dose CISplatin; used in combination with other antiemet- ics; postoperative nausea/vomiting
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CONTRAINDICATIONS: Hyper- sensitivity to this product, polysorbate 80, pimozide Precautions: Pregnancy, breastfeeding, children, geriatric patients, hepatic disease
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SIDE EFFECTS CNS: Headache, dizziness, insomnia, weakness, headache, fever CV: Bradycardia, hypo/hypertension GI: Diarrhea, constipation, abdominal pain, nausea, vomiting, heartburn HEMA: Anemia INTEG: Pruritus, rash, urticaria, injec- tion reaction MISC: Fatigue, dehydration, fever, alopecia
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INTERACTIONS Increase: levels of each product— ALPRAZolam, midazolam, triazolam; de- crease benzodiazepine dose Increase: aprepitant action—CYP3A4 inhibitors (ketoconazole, itraconazole, nefazodone, troleandomycin, clarithro- mycin, ritonavir, nelfinavir, diltiaZEM) Increase: action of CYP3A4 substrates (pimozide, dexamethasone, methylPRED- NISolone, midazolam, ALPRAZolam, tri- azolam, DOCEtaxel, PACLitaxel, etoposide, irinotecan, imatinib, ifosfamide, vinorel- bine, vinBLAStine, vinCRIStine), avoid con- current use Decrease: aprepitant action—CYP3A4 inducers (rifAMPin, carBAMazepine, phenytoin) Decrease: action of CYP2C9 substrates (warfarin, phenytoin), hormonal contra ceptives Decrease: action of both products— PARoxetine Drug/Food Decrease: effect—grapefruit juice Drug/Lab Increase: AST/ALT, alkaline phosphatase Decrease: HB,WBC
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DOSAGE AND ROUTES Prevention of nausea/vomiting after chemotherapy • Adult: PO Day 1 (1 hr before chemo- therapy) aprepitant 125 mg with 12 mg dexamethasone PO, with 32 mg ondanse- tron IV; day 2 aprepitant 80 mg with 8 mg dexamethasone PO; day 3 aprepitant 80 mg with 8 mg dexamethasone PO; day 4 only dexamethasone 8 mg PO; Adult: IV (Cin- vanti): (HEC) On day 1 130 mg over 30 min before chemotherapy; 3-day regimen (MEC) on day 1 100 mg over 30 min, given 30 min before chemotherapy, on day 2 and 3 80 mg PO 1 hr before chemotherapy, given in AM if no chemotherapy is given Child ⬧12 yr: PO capsules 125 mg 1 hr prior to chemotherapy; suspension 3 mg/ kg 1 hr prior to chemotherapy, max 125 mg IV INFUSION 150 mg fosaprepitant over 15 min, 30 min prior to chemotherapy Prevention of postoperative nausea/vomiting • Adult: PO 40 mg within 3 hr of induc- tion of anesthesia
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Available forms: Capsules 40, 80, 125 mg; lyophilized powder for injection, 150 mg; combo pack capsules 80-125 mg; powder for oral suspension 125 mg/pouch
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Administer: • Give with dexamethasone and a 5-HT3 antagonist PO route • Do not break, crush, or chew • PO on 3-day schedule, give with full glass of water 1 hr before chemotherapy, with or without food, given with other antiemetics • Do not open or break capsules • Suspension: Use for children unable to swallow capsules, administer slowly, store at room temperature • Store at room temperature; keep in original bottles, blisters Intermittent IV INFUSION route (Fosaprepitant-Emend) • Use IV on day 1 of 3-day regimen • Reconstitution: use aseptic technique; inject 5 mL 0.9% NaCl into the vial, directing stream to wall of vial to prevent A foam; swirl (do not shake) • Prepare infusion bag 145 mL/150 mg; do not dilute, reconstitute with calcium, magnesium, including LR, Hartmann’s solution • Withdraw entire volume from vial, transfer to infusion bag; total volume 115 mL (1 mg/1 mL) • Gently invert bag; reconstituted solu- tion stable for 24 hr at lower room tem- perature or (<77°F/<25°C) • Visually inspect for particulates, dis- coloration • Infuse over 30 min, stable for 24 hr at room temperature, 30 min prior to che- motherapy, pediatrics use CVAD • Monitor for IV site reactions Aprepitant (Cinvanti) • Withdraw 18 mL for the 130-mg dose or 14 mL for the 100-mg dose from the vial and transfer it into an infusion bag filled with 100 mL of 0.9% NaCl or D5W • Gently invert the bag 4 to 5 times. Avoid shaking • Before using, inspect the bag for par- ticulate matter and discoloration. Dis- card if present
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Assess: • For hypersensitivity reactions: pruri- tus, rash, urticaria, anaphylaxis • CV status: hypo/hypertension, brady- cardia, tachycardia, DVT • For absence of nausea, vomiting dur- ing chemotherapy • For drug/herb/supplement interactions, as there are many • CBC, LFTs, creatinine baseline and pe- riodically
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Evaluate: • Therapeutic response: absence of nausea, vomiting during cancer chemotherapy, or post-op
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take only as prescribed; to take first dose 1 hr prior to chemotherapy or within 3 hr of surgery to prevent nausea, vomiting • To report all medications and herbals to prescriber before taking this medica- tion • That those patients also taking warfa- rin should have clotting monitored closely during 2-wk period after adminis- tration of aprepitant • Pregnancy/breastfeeding: to use nonhormonal form of contraception while taking this agent and for 1 mo thereafter; oral contraceptive effect may be de- creased; to avoid breastfeeding
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PHARMACOKINETICS Absorption 60%-65%, peak 4 hr (PO) infusion’s end (IV), metabolized in liver by CYP3A4 enzymes to active metabolite, half-life 9-12 hr, 95% protein bound, not excreted in kidneys, crosses blood-brain barrier
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• Adult: PO Day 1 (1 hr before chemo- therapy) aprepitant 125 mg with 12 mg dexamethasone PO, with 32 mg ondanse- tron IV; day 2 aprepitant 80 mg with 8 mg dexamethasone PO; day 3 aprepitant 80 mg with 8 mg dexamethasone PO; day 4 only dexamethasone 8 mg PO; Adult: IV (Cin- vanti): (HEC) On day 1 130 mg over 30 min before chemotherapy; 3-day regimen (MEC) on day 1 100 mg over 30 min, given 30 min before chemotherapy, on day 2 and 3 80 mg PO 1 hr before chemotherapy, given in AM if no chemotherapy is given Child ⬧12 yr: PO capsules 125 mg 1 hr prior to chemotherapy; suspension 3 mg/ kg 1 hr prior to chemotherapy, max 125 mg IV INFUSION 150 mg fosaprepitant over 15 min, 30 min prior to chemotherapy Prevention of postoperative nausea/vomiting
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• Adult: PO 40 mg within 3 hr of induc- tion of anesthesia
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