Intravenous Prophylaxis of chemotherapy-induced nausea and vomiting
Adult: For highly emetogenic chemotherapy (HEC): 150 mg via IV infusion over 20-30 minutes on day 1, completing the infusion approx 30 minutes before chemotherapy; doses are given in combination with a 5-HT3 antagonist on day 1 and an oral corticosteroid (e.g. dexamethasone) on days 1-4. For moderately emetogenic chemotherapy (MEC): 150 mg via IV infusion over 20-30 minutes on day 1, completing the infusion approx 30 minutes before chemotherapy; doses are given in combination with a 5-HT3 antagonist and an oral corticosteroid (e.g. dexamethasone) on day 1. Refer to the specific product information of the selected 5-HT3 antagonist and oral corticosteroid for dosage recommendations. Child: For single or multi-day chemotherapy regimens of HEC or MEC: 6 months to <12 years weighing ≥6 kg: 3 mg/kg (Max: 115 mg) on day 1, followed by 2 mg/kg (Max: 80 mg) on days 2-3; ≥12 years 115 mg on day 1, followed by 80 mg on days 2-3. Alternative dosage recommendation for single-day chemotherapy regimens of HEC or MEC: 6 months to <2 years weighing ≥6 kg: 5 mg/kg (Max: 150 mg) on day 1; 2-<12 years 4 mg/kg (Max: 150 mg) on day 1; ≥12 years 150 mg on day 1. Administer doses via IV infusion over 60 minutes (for those aged 6 months to <12 years) or over 30 minutes (for those aged ≥12 years), completing the infusion approx 30 minutes before chemotherapy. All doses are given in combination with 5-HT3 antagonist with or without corticosteroid. Refer to the specific product information of the selected 5-HT3 antagonist and corticosteroid for dosage recommendations. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
What are the brands available for Fosaprepitant in Malaysia?
Powder for solution for IV infusion: Reconstitute the vial with 5 mL of NaCl 0.9% solution for inj. Swirl gently; avoid shaking. Further dilute the reconstituted solution in an infusion bag with 145 mL of NaCl 0.9% solution for inj to make a total volume of 150 mL with a final concentration of 1 mg/mL. Gently invert the bag 2-3 times to mix. If necessary, calculated doses with volume of <150 mL may be transferred to an appropriate size bag or syringe before infusion.
Incompatibility
Incompatible with solutions containing divalent cations (e.g. magnesium, calcium), including lactated Ringer's solution or Hartmann's solution.
Contraindications
Hypersensitivity. Concomitant use with astemizole, cisapride, pimozide, or terfenadine.
Special Precautions
Avoid infusion into small veins or through a butterfly catheter. Moderate to severe hepatic impairment. Children. Pregnancy and lactation. Concomitant use with warfarin and agents that are known to be metabolised by CYP3A4 (e.g. alfentanil, ciclosporin, everolimus, sirolimus, tacrolimus, docetaxel, paclitaxel, ergotamine, fentanyl, quinidine, irinotecan, ifosfamide, vincristine, vinblastine).
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. dyspnoea, flushing, hypotension, syncope, anaphylaxis or anaphylactic shock); severe infusion-site reactions including vasculitis, necrosis and thrombophlebitis (particularly when concomitantly given with vesicant chemotherapy); other infusion-site reactions (e.g. erythema, pain, oedema, pruritus, inj site induration). Blood and lymphatic system disorders: Anaemia, febrile neutropenia. Cardiac disorders: Palpitations. Gastrointestinal disorders: Diarrhoea, constipation, dyspepsia, eructation, nausea, vomiting, GERD, abdominal pain, dry mouth, flatulence. General disorders and administration site conditions: Fatigue, asthenia, malaise. Investigations: Increased AST, ALT and blood alkaline phosphatase. Metabolism and nutrition disorders: Decreased appetite. Nervous system disorders: Headache, dizziness, somnolence. Psychiatric disorders: Anxiety. Renal and urinary disorders: Dysuria. Respiratory, thoracic and mediastinal disorders: Hiccups. Skin and subcutaneous tissue disorders: Rash, acne.
Women of childbearing potential must use alternative non-hormonal methods of contraception during treatment and for at least 1 month after the last dose.
Monitoring Parameters
Monitor INR in patients on chronic warfarin therapy for 2 weeks (particularly at 7-10 days) after treatment initiation. Closely monitor for immediate hypersensitivity reactions (e.g. dyspnoea, erythema, flushing). Assess for signs and symptoms of infusion site reactions.
Drug Interactions
May increase the plasma levels of corticosteroids (e.g. dexamethasone, methylprednisolone) or other agents (e.g. ciclosporin, everolimus, sirolimus, tacrolimus, alfentanil, fentanyl, ergotamine, quinidine, irinotecan, midazolam, alprazolam, triazolam) that are metabolised by CYP3A4. Decreased plasma concentration and efficacy with strong CYP3A4 inducers (e.g. carbamazepine, rifampicin, phenytoin, phenobarbital). Increased plasma concentration and risk of adverse effects with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, nefazodone, diltiazem, ritonavir, nelfinavir). May induce the metabolism of drugs metabolised by CYP2C9 isoenzyme (e.g. warfarin, tolbutamide), resulting in reduced plasma levels. May reduce the serum levels and efficacy of hormonal contraceptives. Potentially Fatal: May increase the plasma concentrations of astemizole, cisapride, pimozide, and terfenadine.
Food Interaction
Reduced plasma concentration with St. John's wort. May increase serum concentration with grapefruit juice.
Action
Description: Overview: Fosaprepitant is an antiemetic agent and a prodrug of aprepitant, a selective high-affinity antagonist at human substance P neurokinin 1 (NK1) receptors. Mechanism of Action: Fosaprepitant is rapidly converted to aprepitant, which inhibits the NK1 receptors, thereby preventing acute and delayed vomiting. It also enhances the antiemetic effects of 5-HT3 receptor antagonists and corticosteroids, providing additive protection against chemotherapy-induced nausea and vomiting. Pharmacokinetics: Distribution: Crosses the blood-brain barrier (aprepitant). Plasma protein binding: >95% (aprepitant). Metabolism: Rapidly converted in the hepatic and extrahepatic tissues into aprepitant (active form), which undergoes extensive metabolism via oxidation primarily by CYP3A4 with minor contribution by the CYP1A2 and CYP2C19, forming 7 weakly-active metabolites. Excretion: Via urine (57%); faeces (45%). Elimination half-life: Approx 9-13 minutes (aprepitant).
Chemical Structure
Fosaprepitant Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 135413538, Fosaprepitant. https://pubchem.ncbi.nlm.nih.gov/compound/Fosaprepitant. Accessed Oct. 28, 2025.
Storage
Intact vial: Store between 2-8°C. Diluted solution for IV infusion: Stable for 24 hours at ambient room temperature (≤25°C). Storage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Aprepitant, Fosaprepitant Dimeglumine. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/10/2025.Aprepitant, Fosaprepitant. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 23/10/2025.Brayfield A, Cadart C (eds). Fosaprepitant. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/10/2025.Focinvez Injection (Amneal Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/10/2025.Fosaprepitant 150 mg Powder for Solution for Infusion (Hikma Farmaceutica [Portugal], S.A.). MHRA. https://products.mhra.gov.uk. Accessed 07/10/2025.Fosaprepitant. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/10/2025.Fosemred Powder for Solution for Infusion 150 mg/vial (Dr. Reddy's Laboratories Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/10/2025.Joint Formulary Committee. Fosaprepitant. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/10/2025.Paediatric Formulary Committee. Fosaprepitant. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 23/10/2025.
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