To prevent delayed nausea and vomiting associated with initial/repeat courses of emetogenic cancer chemotherapy (to be used with dexamethasone and a 5–HT3 antagonist).
Acts as a selective antagonist at substance P/neurokinin 1 (NK1 ) receptors in the brain.
Decreased nausea and vomiting associated with chemotherapy.
Augments the antiemetic effects of dexamethasone and 5-HT3 antagonists.
Absorption: Well absorbed following oral administration.
Distribution: Extensively distributed to tissues.
Protein Binding: 99.8%
Metabolism and Excretion: Mostly metabolized, primarily by CYP3A4; one metabolite, C4–pyrrolidine-hydroxylated rolapitant (M19) has antiemetic activity. Excretion is mainly via hepato/biliary elimination. 14% excreted in urine (8% as metabolites), 73% in feces (38% as unchanged drug).
Half-life: Rolapitant– 7 days; M19– 7 days.
TIME/ACTION PROFILE (blood levels)
within 30 min
Concurrent use of CYP2D6 substrates with a narrow therapeutic index.
Use Cautiously in:
Concurrent use of other CYP2D6 substrates;
Severe hepatic impairment (avoid if possible; if unavoidable, monitor carefully);
OB: Safety not established;
Lactation: Weigh maternal benefits against risks to the infant;
PO Administer 2 hr before starting chemotherapy without regard to food. Due to long action, administered no more frequently than once every 14 days. Given with dexamethasone and a 5-HT3 antagonist.
Intermittent Infusion: Administer 2 hr before starting chemotherapy. Solution is translucent white and does not need to be shaken; do not inject solutions that are discolored or contain particulate matter. Insert a vented IV set through septum of vial and use immediately; do not dilute. Infuse through a Y-site of 0.9% NaCl. D5W, D5/LR, or LR.
Rate: Infuse over 30 min.
Instruct patient to take rolapitant as directed. Direct patient to read the Patient Package Insert before starting therapy and each time Rx renewed in case of changes.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise patient and family to use general measures to decrease nausea (begin with sips of liquids and small, nongreasy meals; provide oral hygiene; remove noxious stimuli from environment).
Advise patient to notify health care professional if pregnancy is planned or suspected, or if breast feeding.
Decreased delayed nausea and vomiting associated with emetogenic chemotherapy.
rolapitant is a sample topic from the Davis's Drug Guide.
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