What is Fosaprepitant pimozide?
Fosaprepitant pimozide blocks the actions of chemicals in the body that trigger nausea and vomiting.
Fosaprepitant pimozide is used together with other medications to prevent nausea and vomiting that may be caused by chemotherapy.
Fosaprepitant pimozide will only prevent nausea and vomiting. It will not treat nausea or vomiting that you already have.
Fosaprepitant pimozide may also be used for purposes not listed in this medication guide.
Fosaprepitant pimozide indications
Fosaprepitant pimozide for Injection, in combination with other antiemetic agents, is indicated in adults for the prevention of:
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- acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin.
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- delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC).
Limitations of Use
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- Fosaprepitant pimozide for Injection has not been studied for the treatment of established nausea and vomiting.
Pediatric use information is approved for Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.’s Emend (Fosaprepitant pimozide) for injection. However, due to Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.’s marketing exclusivity rights, this drug product is not labeled with that pediatric information.
How should I use Fosaprepitant pimozide?
Use Fosaprepitant pimozide as directed by your doctor. Check the label on the medicine for exact dosing instructions.
- An extra patient leaflet is available with Fosaprepitant pimozide. Talk to your pharmacist if you have questions about this information.
- Tell your doctor if you already have nausea or vomiting before you receive Fosaprepitant pimozide.
- Fosaprepitant pimozide is usually given as an injection at your doctor's office, hospital, or clinic 30 minutes before chemotherapy treatment.
- If you miss a dose of Fosaprepitant pimozide, contact your doctor immediately.
Ask your health care provider any questions you may have about how to use Fosaprepitant pimozide.
Uses of Fosaprepitant pimozide in details
Use: Labeled Indications
Prevention of chemotherapy-induced nausea and vomiting:
Prevention of acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy, including high-dose cisplatin (initial and repeat courses; in combination with other antiemetics) in patients ≥6 months of age
Prevention of delayed nausea and vomiting associated with moderately emetogenic chemotherapy (initial and repeat courses; in combination with other antiemetics) in patients ≥6 months of age
Limitations of use: Fosaprepitant pimozide has not been studied for the management of existing nausea and vomiting.
Fosaprepitant pimozide description
Fosaprepitant pimozide is an intravenously administered antiemetic drug. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment.
Fosaprepitant pimozide dosage
Usual Adult Dose for Nausea/Vomiting -- Chemotherapy Induced:
HIGHLY EMETOGENIC CHEMOTHERAPY (HEC):
Fosaprepitant pimozide 150 mg (single dose regimen):
Day 1: 150 mg intravenously as an infusion over 20 to 30 minutes approximately 30 minutes prior to chemotherapy.
Comments:
-Fosaprepitant pimozide should be administered in conjunction with a corticosteroid and a 5-HT3 antagonist.
-The recommended dosage of dexamethasone is 12 mg orally on day 1 administered 30 minutes prior to chemotherapy, 8 mg orally in the morning on day 2, and 8 mg twice daily on days 3 and 4.
- The 5-HT3 antagonist is administered on day 1 only. Consult the package insert for the 5-HT3 antagonist dosing prior to initiation of treatment.
Fosaprepitant pimozide 115 MG (3 DAY DOSING REGIMEN):
Day 1: 115 mg intravenously as an infusion over 15 minutes approximately 30 minutes prior to chemotherapy.
Comments:
-Aprepitant 80 mg should be administered orally in the mornings of days 2 and 3.
-Fosaprepitant pimozide should be administered in conjunction with a corticosteroid and a 5-HT3 antagonist.
-The recommended dosage of dexamethasone is 12 mg orally on day 1 administered 30 minutes prior to chemotherapy and 8 mg in the mornings on days 2 through 4.
-A 5-HT3 antagonist is administered on day 1 only. Consult the package insert for the 5-HT3 antagonist dosing prior to initiation of treatment.
-Aprepitant may be taken with or without food.
MODERATELY EMETOGENIC CHEMOTHERAPY (MEC) 3 DAY DOSING REGIMEN:
Day 1: 115 mg intravenously as an infusion over 15 minutes approximately 30 minutes prior to chemotherapy.
Comments:
-Aprepitant 80 mg should be administered orally in the mornings of days 2 and 3.
-Fosaprepitant pimozide should be administered in conjunction with a corticosteroid and a 5-HT3 antagonist.
-The recommended dosage of dexamethasone is 12 mg orally on day 1 administered 30 minutes prior to chemotherapy.
-A 5-HT3 antagonist is administered on day 1 only. Consult the package insert for the 5-HT3 antagonist dosing prior to initiation of treatment.
-Aprepitant may be taken with or without food.
Fosaprepitant pimozide interactions
See also:
What other drugs will affect Fosaprepitant pimozide?
ARIPiprazole: CYP3A4 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations. Monitor therapy
Astemizole: Fosaprepitant pimozide may increase the serum concentration of Astemizole. The active metabolite aprepitant is likely responsible for this effect. Avoid combination
Bosentan: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination
Corticosteroids (Systemic): Fosaprepitant pimozide may increase the serum concentration of Corticosteroids (Systemic). The active metabolite aprepitant is likely responsible for this effect. Management: Decrease oral dexamethasone or methylprednisolone dose by 50% during coadministration with Fosaprepitant pimozide/aprepitant. Reduce intravenous methylprednisolone dose by 25% during coadministration with Fosaprepitant pimozide/aprepitant. Consider therapy modification
CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Fosaprepitant pimozide. Specifically, CYP3A4 Inducers (Strong) may decrease serum concentrations of the active metabolite aprepitant. Avoid combination
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Fosaprepitant pimozide. Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Fosaprepitant pimozide. Avoid combination
CYP3A4 Substrates (High risk with Inhibitors): Fosaprepitant pimozide may increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Monitor therapy
Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Estrogen Derivatives (Contraceptive): Fosaprepitant pimozide may decrease the serum concentration of Estrogen Derivatives (Contraceptive). The active metabolite aprepitant is likely responsible for this effect. Management: Alternative or additional methods of contraception should be used both during treatment with Fosaprepitant pimozide or aprepitant and for at least one month following the last Fosaprepitant pimozide/aprepitant dose. Consider therapy modification
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination
Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination
Ifosfamide: Fosaprepitant pimozide may increase the serum concentration of Ifosfamide. Specifically, concentrations of the toxic metabolites of ifosfamide may increase. Monitor therapy
Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Lemborexant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Consider therapy modification
Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Consider therapy modification
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Monitor therapy
Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
PARoxetine: May decrease serum concentrations of the active metabolite(s) of Fosaprepitant pimozide. Fosaprepitant pimozide may decrease the serum concentration of PARoxetine. Monitor therapy
Pimozide: Fosaprepitant pimozide may increase the serum concentration of Pimozide. The active metabolite aprepitant is likely responsible for this effect. Avoid combination
Progestins (Contraceptive): Fosaprepitant pimozide may decrease the serum concentration of Progestins (Contraceptive). The active metabolite aprepitant is likely responsible for this effect. Management: Alternative or additional methods of contraception should be used both during treatment with aprepitant or Fosaprepitant pimozide and for at least one month following the last aprepitant/Fosaprepitant pimozide dose. Consider therapy modification
Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification
Terfenadine: Fosaprepitant pimozide may increase the serum concentration of Terfenadine. The active metabolite aprepitant is likely responsible for this effect. Avoid combination
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy
TOLBUTamide: Fosaprepitant pimozide may decrease the serum concentration of TOLBUTamide. Monitor therapy
Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Management: Consider triazolam dose reduction in patients receiving concomitant weak CYP3A4 inhibitors. Consider therapy modification
Ubrogepant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (if needed) of ubrogepant should be limited to 50 mg. Consider therapy modification
Warfarin: Fosaprepitant pimozide may decrease the serum concentration of Warfarin. The active metabolite aprepitant is likely responsible for this effect. Monitor therapy
Fosaprepitant pimozide side effects
See also:
What are the possible side effects of Fosaprepitant pimozide?
The following clinically significant adverse reactions are described elsewhere in the labeling:
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- Hypersensitivity Reactions
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- Infusion Site Reactions
Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
The overall safety of Fosaprepitant pimozide for Injection was evaluated in approximately 1600 adult patients.
Adverse Reactions in Adults for the Prevention of Nausea and Vomiting Associated with MEC
In an active-controlled clinical trial in patients receiving MEC, safety was evaluated in 504 patients receiving a single dose of Fosaprepitant pimozide for Injection in combination with ondansetron and dexamethasone (Fosaprepitant pimozide for Injection regimen) compared to 497 patients receiving ondansetron and dexamethasone alone (standard therapy). The most common adverse reactions are listed in Table 6.
| ||
| Fosaprepitant pimozide for Injection, ondansetron, and dexamethasone† (N=504) | Ondansetron and dexamethasone‡ (N=497) | |
| fatigue | 15% | 13% |
| diarrhea | 13% | 11% |
| neutropenia | 8% | 7% |
| asthenia | 4% | 3% |
| anemia | 3% | 2% |
| peripheral neuropathy | 3% | 2% |
| leukopenia | 2% | 1% |
| dyspepsia | 2% | 1% |
| urinary tract infection | 2% | 1% |
| pain in extremity | 2% | 1% |
Infusion-site reactions were reported in 2.2% of patients treated with the Fosaprepitant pimozide for Injection regimen compared to 0.6% of patients treated with standard therapy. The infusion-site reactions included: infusion-site pain (1.2%, 0.4%), injection-site irritation (0.2%, 0.0%), vessel puncture-site pain (0.2%, 0.0%), and infusion-site thrombophlebitis (0.6%, 0.0%), reported in the Fosaprepitant pimozide for Injection regimen compared to standard therapy, respectively.
Adverse Reactions in Adults for the Prevention of Nausea and Vomiting Associated with HEC
In an active-controlled clinical study in patients receiving HEC, safety was evaluated for 1143 patients receiving a single dose of Fosaprepitant pimozide for Injection compared to 1169 patients receiving the 3-day regimen of oral Fosaprepitant pimozide (aprepitant). The safety profile was generally similar to that seen in the MEC study with Fosaprepitant pimozide and prior HEC studies with aprepitant. However, infusion-site reactions occurred at a higher incidence in patients in the Fosaprepitant pimozide group (3.0%) compared to those in the aprepitant group (0.5%). The following additional infusion-site reactions occurred in the HEC study and were not reported in the MEC study described above: infusion-site erythema (0.5%, 0.1%), infusion-site pruritus (0.3%, 0.0%), and infusion-site induration (0.2%, 0.1%), reported in the Fosaprepitant pimozide group compared to the aprepitant group, respectively.
Because Fosaprepitant pimozide is converted to aprepitant, those adverse reactions associated with aprepitant might also be expected to occur with Fosaprepitant pimozide for Injection. See the full prescribing information for Fosaprepitant pimozide capsules for complete safety information regarding studies performed with oral aprepitant.
Pediatric use information is approved for Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.’s Emend (Fosaprepitant pimozide) for injection. However, due to Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.’s marketing exclusivity rights, this drug product is not labeled with that pediatric information.
Postmarketing Experience
The following adverse reactions have been identified during post-approval use of Fosaprepitant pimozide for Injection. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Skin and subcutaneous tissue disorders: pruritus, rash, urticaria, Stevens-Johnson syndrome/toxic epidermal necrolysis.
Immune system disorders: hypersensitivity reactions including anaphylaxis and anaphylactic shock.
Nervous system disorders: ifosfamide-induced neurotoxicity reported after Fosaprepitant pimozide for Injection and ifosfamide coadministration.
Fosaprepitant pimozide contraindications
See also:
What is the most important information I should know about Fosaprepitant pimozide?
Fosaprepitant pimozide for Injection 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.
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- 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.
Active ingredient matches for Fosaprepitant pimozide:
List of Fosaprepitant pimozide substitutes (brand and generic names) | Sort by popularity |
| Unit description / dosage (Manufacturer) | Price, USD |
| Emend for Injection pimozide | |
| Emend Injection | |
| Emend Intravenous | |
| Emend IV (Canada) | |
| Emend IV 150mg (Israel) | |
| FOSAPORT | |
| FOSAPORT 150MG INJECTION 1 vial / 1 injection each (Biocon) | $ 25.20 |
| FOSAPREPIT | |
| FOSAPREPIT 150MG INJECTION 1 vial / 1 ML injection each (Cipla Ltd) | $ 27.41 |
| Fosaprepitant (Austria, Croatia (Hrvatska), Denmark, Finland, Germany, Greece, Latvia, Lithuania, Portugal, Romania, Serbia, Slovenia, Spain, Sweden, Switzerland, United Kingdom) | |
| FOSARAN | |
| FOSARAN 150MG INJECTION 1 vial / 1 ML injection each (Ranbaxy Laboratories Ltd) | $ 26.65 |
| Ivemend (Austria, Croatia (Hrvatska), Denmark, Finland, Germany, Greece, Latvia, Lithuania, Portugal, Romania, Serbia, Slovenia, Spain, Sweden, Switzerland, United Kingdom) | |
| Injectable; Injection; Fosaprepitant Dimeglumine 115 mg (MSD) | |
| Ivemend 150mg (Austria, Luxembourg, Switzerland) | |
| Proemend (Japan) | |
References
- DailyMed. "FOSAPREPITANT DIMEGLUMINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- PubChem. "Fosaprepitant". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
- DrugBank. "Fosaprepitant". http://www.drugbank.ca/drugs/DB06717 (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
