Fosaprepitant
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Dosing in kidney impairment
This label has no separate kidney-impairment dosing section. Check warnings and clinical pharmacology in the full label.
Dosing in liver impairment
Patients with Hepatic Impairment The pharmacokinetics of aprepitant in patients with mild and moderate hepatic impairment were similar to those of healthy subjects with normal hepatic function. No dosage adjustment is necessary for patients with mild to moderate hepatic impairment (Child-Pugh score 5 to 9). There are no clinical or pharmacokinetic data in patients with severe hepatic impairment (Child-Pugh score greater than 9).
Therefore, additional monitoring for adverse reactions in these patients may be warranted when NAVITRUX is administered [see Clinical Pharmacology ].
Preparation and administration
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Preparation and Administration of NAVITRUX [See table below.] Caution: Do not mix or reconstitute NAVITRUX with solutions for which physical and chemical compatibility have not been established. NAVITRUX is incompatible with any solutions containing divalent cations (e.g., Ca 2+ , Mg 2+ ), including Lactated Ringer's Solution and Hartmann's Solution.
Storage Store reconstituted product (30 mg/mL) at ambient room temperature [at or below 25°C (77°F)] for no longer than 24 hours from the time of reconstitution. Discard the vial after 24 hours. The total storage time of the reconstituted NAVITRUX and the final diluted solution should not exceed 24 hours at ambient room temperature [at or below 25°C (77°F)].
Discard the unused reconstituted or diluted solution after 24 hours from the start of reconstitution.
| Step 1 | Reconstitute NAVITRUX to achieve a concentration of 30 mg/mL as follows: Aseptically inject 5 mL 0.9% Sodium Chloride Injection into the vial. Assure that 0.9% Sodium Chloride Injection is added to the vial along the vial wall in order to prevent foaming. Swirl the vial gently. Avoid shaking and jetting 0.9% Sodium Chloride Injection into the vial. Prior to further dilution, visually inspect the reconstituted solution in the vial for particulate matter and discoloration. The solution should be clear and colorless. Discard if particulate matter is present or the solution is discolored. |
| Step 2 | Aseptically prepare an infusion bag filled with 145 mL of 0.9% Sodium Chloride Injection. |
| Step 3 | Aseptically withdraw the entire volume from the vial and transfer it into the infusion bag containing 145 mL of 0.9% Sodium Chloride Injection to yield a total volume of 150 mL and a final concentration of 1 mg/mL. |
| Step 4 | Gently invert the bag 2 to 3 times. |
| Step 5 | Determine the volume to be administered from this prepared infusion bag, based on the recommended dose [see Dosage and Administration (2.1, 2.2)] . Adults The entire volume of the prepared infusion bag (150 mL) should be administered. Pediatrics In patients 12 years and older, the volume to be administered is calculated as follows: Volume to administer (mL) equals the recommended dose (mg) In patients 6 months to less than 12 years, the volume to be administered is calculated as follows: ● Volume to administer (mL) = recommended dose (mg/kg) × weight (kg) o Note: Do not exceed the maximum dose [see Dosage and Administration (2.2)] ● In pediatric patients, the entire volume in the infusion bag may not be required. |
| Step 6 | If necessary, for volumes less than 150 mL, the calculated volume can be transferred to an appropriate size bag or syringe prior to administration by infusion. |
| Step 7 | Before administration, inspect the bag for particulate matter and discoloration. Discard the bag if particulate and/or discoloration are observed. |
Drug interactions
Check fosaprepitant against a medication listLabel text (9 paragraphs)
See Full Prescribing Information for a list of clinically significant drug interactions. ( 4 , 5.1 , 5.4 , 5.5 , 7.1 , 7.2 )
7.1 Effect of Fosaprepitant/Aprepitant on the Pharmacokinetics of Other Drugs When administered intravenously, fosaprepitant, a prodrug of aprepitant, is converted to aprepitant within 30 minutes. Therefore, drug interactions following administration of fosaprepitant are likely to occur with drugs that interact with oral aprepitant. Fosaprepitant, given as a single 150-mg dose, is a weak inhibitor of CYP3A4, and the weak inhibition of CYP3A4 continues for 2 days after single dose administration. Single dose fosaprepitant does not induce CYP3A4. Aprepitant is a substrate, an inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9 [see Clinical Pharmacology (12.3) ] .
Some substrates of CYP3A4 are contraindicated with NAVITRUX [see Contraindications (4) ] . Dosage adjustment of some CYP3A4 and CYP2C9 substrates may be warranted, as shown in Table 7. Table 7: Effects of Fosaprepitant/Aprepitant on the Pharmacokinetics of Other Drugs CYP3A4 Substrates Pimozide Clinical Impact Increased pimozide exposure Intervention NAVITRUX is contraindicated [see Contraindications (4) ]. Benzodiazepines Clinical Impact Increased exposure to midazolam or other benzodiazepines metabolized via CYP3A4 (alprazolam, triazolam) may increase the risk of adverse reactions [see Clinical Pharmacology (12.3) ]. Intervention Monitor for benzodiazepine-related adverse reactions.
Dexamethasone Clinical Impact Increased dexamethasone exposure [see Clinical Pharmacology (12.3) ]. Intervention Reduce the dose of oral dexamethasone by approximately 50% [see Dosage and Administration (2.1) ]. Methylprednisolone Clinical Impact Increased methylprednisolone exposure [see Clinical Pharmacology (12.3) ]. Intervention Reduce the dose of oral methylprednisolone by approximately 50% on Days 1 and 2 for patients receiving HEC and on Day 1 for patients receiving MEC. Reduce the dose of intravenous methylprednisolone by 25% on Days 1 and 2 for patients receiving HEC and on Day 1 for patients receiving MEC.
Chemotherapeutic agents that are metabolized by CYP3A4 Clinical Impact Increased exposure of the chemotherapeutic agent may increase the risk of adverse reactions [see Clinical Pharmacology (12.3) ]. Intervention Vinblastine, vincristine, or ifosfamide or other chemotherapeutic agents ● Monitor for chemotherapeutic-related adverse reactions. Etoposide, vinorelbine, paclitaxel, and docetaxel ● No dosage adjustment needed. Hormonal Contraceptives Clinical Impact Decreased hormonal exposure during administration of and for 28 days after administration of the last dose of fosaprepitant [see Warnings and Precautions (5.5), Use in Specific Populations (8.3), and Clinical Pharmacology (12.3) ].
Intervention Effective alternative or back-up methods of contraception (such as condoms and spermicides) should be used during treatment with NAVITRUX and for 1 month following administration of the last dose of NAVITRUX or oral aprepitant. Examples birth control pills, transdermal systems, implants CYP2C9 Substrates Warfarin Clinical Impact Decreased warfarin exposure and prolongation of prothrombin time (INR) [see Warnings and Precautions (5.4) , Clinical Pharmacology (12.3) ]. Intervention In patients on chronic warfarin therapy, monitor the prothrombin time (INR) in the 2-week period, particularly at 7 to 10 days, following administration of NAVITRUX with each chemotherapy cycle.
Other 5-HT 3 Antagonists Clinical Impact No change in the exposure of the 5-HT 3 antagonist [see Clinical Pharmacology (12.3) ]. Intervention No dosage adjustment needed Examples ondansetron, granisetron, dolasetron
7.2 Effect of Other Drugs on the Pharmacokinetics of Fosaprepitant/Aprepitant Aprepitant is a CYP3A4 substrate [see Clinical Pharmacology (12.3) ]. Co-administration of NAVITRUX with drugs that are inhibitors or inducers of CYP3A4 may result in increased or decreased plasma concentrations of aprepitant, respectively, as shown in Table 8. Table 8: Effects of Other Drugs on Pharmacokinetics of Fosaprepitant/Aprepitant Moderate to Strong CYP3A4 Inhibitors Clinical Impact Significantly increased exposure of aprepitant may increase the risk of adverse reactions associated with NAVITRUX [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) ].
Intervention Avoid concomitant use of NAVITRUX Examples Moderate inhibitor: diltiazem Strong inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir Strong CYP3A4 Inducers Clinical Impact Substantially decreased exposure of aprepitant in patients chronically taking a strong CYP3A4 inducer may decrease the efficacy of NAVITRUX [see Clinical Pharmacology (12.3) ]. Intervention Avoid concomitant use of NAVITRUX Examples rifampin, carbamazepine, phenytoin
Contraindications
4 CONTRAINDICATIONS NAVITRUX is contraindicated in patients: who are hypersensitive to any component of the product. Hypersensitivity reactions including anaphylactic reactions, flushing, erythema, and dyspnea have been reported [see Warnings and Precautions (5.2) , Adverse Reactions (6.2) ] . taking pimozide. Inhibition of CYP3A4 by aprepitant, the active moiety, could result in elevated plasma concentrations of this drug, which is a CYP3A4 substrate, potentially causing serious or life-threatening reactions, such as QT prolongation, a known adverse reaction of pimozide [see Warnings and Precautions (5.1) ]. Known hypersensitivity to any component of this drug.
( 4 , 5.2 ) Concurrent use with pimozide. ( 4 )
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary There are insufficient data on use of fosaprepitant in pregnant women to inform a drug associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal reproduction studies, no adverse developmental effects were observed in rats or rabbits exposed during the period of organogenesis to systemic drug levels (AUC) approximately equivalent to the exposure at the recommended human dose (RHD) of 150 mg (see Data) . The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. In the U.S.
general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In embryofetal development studies in rats and rabbits, aprepitant was administered during the period of organogenesis at oral doses up to 1000 mg/kg twice daily (rats) and up to the maximum tolerated dose of 25 mg/kg/day (rabbits). No embryofetal lethality or malformations were observed at any dose level in either species. The exposures (AUC) in pregnant rats at 1000 mg/kg twice daily and in pregnant rabbits at 25 mg/kg/day were approximately equivalent to the exposure at the RHD of 150 mg.
Aprepitant crosses the placenta in rats and rabbits.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
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