Intravenous Prophylaxis of chemotherapy-induced nausea and vomiting
Adult: For HEC: 130 mg via IV inj over 2 minutes given approx 30 minutes prior to chemotherapy on day 1. Doses are given in combination with a 5-HT3 antagonist antiemetic on day 1 and an oral corticosteroid on days 1-4. For MEC: As single-dose regimen: 130 mg via IV inj over 2 minutes given approx 30 minutes prior to chemotherapy on day 1. Doses are given in combination with a 5-HT3 antagonist antiemetic and an oral corticosteroid on day 1. As 3-day regimen: 100 mg via IV inj over 2 minutes given approx 30 minutes prior to chemotherapy on day 1, followed by oral doses on days 2 and 3. Doses are given in combination with a 5-HT3 antagonist antiemetic and an oral Corticosteroid on day 1. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Intravenous Prophylaxis of postoperative nausea and vomiting
Adult: 32 mg via IV inj over 30 seconds given 30 minutes prior to induction of anaesthesia. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Oral Prophylaxis of chemotherapy-induced nausea and vomiting
Adult: For highly emetogenic chemotherapy (HEC): As cap: 125 mg once daily given one hour prior to chemotherapy on day 1 followed by 80 mg in the morning on days 2 and 3. Doses are given in combination with a type 3 serotonin (5-HT3) antagonist on day 1 and a corticosteroid on days 1-4 (refer to specific product guidelines). For moderately emetogenic chemotherapy (MEC): As cap: 125 mg once daily given one hour prior to chemotherapy on day 1 followed by 80 mg in the morning on days 2 and 3. Doses are given in combination with a 5-HT3 antagonist and corticosteroid on day 1 (refer to specific product guidelines). Child: For HEC or MEC in combination with 5-HT3 antagonist with or without corticosteroid: 6 months to <12 years weighing >6 kg: As oral susp: 3 mg/kg (Max: 125 mg) given 1 hour prior to chemotherapy on day 1 followed by 2 mg/kg (Max: 80 mg) once daily on days 2-3; ≥12 years Same as adult dose. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
Oral Prophylaxis of postoperative nausea and vomiting
Adult: As cap: 40 mg given within 3 hours prior to induction of anaesthesia. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
What are the brands available for Aprepitant in Hong Kong?
Solution for IV infusion: Dilute a 130 mg or 100 mg dose into a 100 mL non-PVC infusion bag containing NaCl 0.9 % or dextrose 5% in water. Invert the bag gently for 4 to 5 times. Avoid shaking.
Concomitant use with pimozide, astemizole, cisapride, or terfenadine.
Special Precautions
Concomitant use with warfarin and orally active agents that are metabolised by CYP3A4 with narrow therapeutic index (e.g. alfentanil, ciclosporin, everolimus, sirolimus, tacrolimus, ergotamine, fentanyl, quinidine, irinotecan). Moderate to severe hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions, anaphylactic reactions.
Blood and lymphatic system disorders: Anaemia, febrile neutropenia. Cardiac disorders: Palpitations, hypotension. Ear and labyrinth disorders: Rarely, tinnitus. Eye disorders: Rarely, conjunctivitis. Gastrointestinal disorders: Nausea, vomiting, constipation, diarrhoea, dyspepsia, flatulence, eructation, abdominal pain, dry mouth, GERD. General disorders and administration site conditions: Fatigue, asthenia, malaise, peripheral oedema. Infections and infestations: Rarely, candidiasis, staphylococcal infection. Investigations: Increased ALT, AST, blood alkaline phosphatase. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Rarely, muscular weakness, muscle spasms. Nervous system disorders: Headache, dizziness, somnolence. Psychiatric disorders: Anxiety. Renal and urinary disorders: Dysuria. Respiratory, thoracic and mediastinal disorders: Hiccups, cough, dyspnoea, pharyngitis. Skin and subcutaneous tissue disorders: Rash, acne, pruritus, urticaria, alopecia, hyperhidrosis. Rarely, Stevens-Johnson syndrome, toxic epidermal necrolysis. Vascular disorders: Flushing.
Patient Counseling Information
This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery. Women of childbearing potential and their male partners must use effective alternative non-hormonal methods of contraception during treatment and for 1 or 2 months after stopping the treatment.
Monitoring Parameters
Monitor INR or prothrombin time (individuals taking warfarin) for 2 weeks (specifically at 7-10 days) after treatment initiation. Assess for signs or symptoms of hypersensitivity reaction or adverse reactions for individuals with severe hepatic impairment.
Overdosage
Symptoms: Dizziness, drowsiness, headache and fatigue. Management: Supportive treatment.
Drug Interactions
May increase the plasma concentration of agents that are metabolised by CYP3A4 (e.g. alfentanil, ciclosporin, everolimus, sirolimus, tacrolimus, ergotamine, fentanyl, quinidine, irinotecan, ifosfamide, midazolam, alprazolam, triazolam). May reduce the plasma concentration of drugs metabolised by CYP2C9 isoenzyme (e.g. warfarin, acenocoumarol, phenytoin, tolbutamide). May reduce the efficacy of hormonal contraceptives. Increased plasma concentration with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, voriconazole, clarithromycin, troleandomycin, nefazodone, protease inhibitors, diltiazem). Reduced plasma concentration with strong CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenobarbital). May increase the exposure to corticosteroids (e.g. dexamethasone, methylprednisolone). Potentially Fatal: Increased plasma level and increased risk of QT prolongation with pimozide, astemizole, cisapride, terfenadine.
Food Interaction
Decreased plasma levels with St. John's wort. Serum concentration may be increased with grapefruit juice.
Action
Description: Mechanism of Action: Aprepitant, an antiemetic, is a selective and high-affinity antagonist of substance P/neurokinin 1 (NK1) receptors that are found in the medulla which regulates emetic reflex. It also enhances the antiemetic activity of type 3 serotonin (5-HT3) receptor antagonists and corticosteroids resulting in the inhibition of acute or delayed phases of chemotherapy-induced emesis. Pharmacokinetics: Absorption: Absorbed in the gastrointestinal tract. Bioavailability: Approx 60-65% (oral). Time to peak plasma concentration: Approx 4 hours. Distribution: Crosses the blood-brain barrier. Volume of distribution: Approx 70 L. Plasma protein binding: >95% (oral); >99% (IV). Metabolism: Extensively metabolised in the liver mainly via oxidation by the CYP3A4 isoenzyme and with minor contribution by CYP1A2 and CYP2C19 into weak active metabolites. Excretion: Via urine and faeces (as metabolites). Terminal elimination half-life: Approx 9-13 hours.
Chemical Structure
Aprepitant Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 135413536, Aprepitant. https://pubchem.ncbi.nlm.nih.gov/compound/Aprepitant. Accessed Nov. 26, 2024.
Storage
Cap: Store between 20-25°C. Oral susp: Store between 15-30°C. Reconstituted oral susp: Store between 2-8°C for up to 72 hours or between 20-25°C for up to 3 hours. Intact vials: Store between 2-8°C or between 20-25°C for up to 6 months. Do not freeze. Solution for IV infusion: Store solutions at room temperature for up to 6 hours (solution diluted in NaCl 0.9 %) or for 12 hours (solution diluted in dextrose 5% in water). Alternatively, solutions for IV infusion may be stored in the refrigerator for up to 72 hours (solution diluted in NaCl 0.9 % or dextrose 5% in water).
A04AD12 - aprepitant ; Belongs to the class of other antiemetics.
References
Anon. Aprepitant. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 27/10/2023.Anon. Aprepitant. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/10/2023.Aponvie Injection Emulsion (Heron Therapeutics, Inc.). U.S. FDA. https://www.fda.gov. Accessed 27/10/2023.Aprepitant Accord 125 mg/80 mg Hard Capsules (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 27/10/2023.Aprepitant Capsule and Powder for Suspension (Torrent Pharmaceuticals Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 27/10/2023.Aprepitant, Fosaprepitant. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 27/10/2023.Buckingham R (ed). Aprepitant. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/10/2023.Cinvanti Injection Emulsion (Heron Therapeutics, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 27/10/2023.Emend 125 mg and 80 mg Hard Capsules (Merck Sharp & Dohme [UK] Limited). MHRA. https://products.mhra.gov.uk. Accessed 27/10/2023.Emend 125 mg Powder for Oral Suspension (Merck Sharp & Dohme [UK] Limited). MHRA. https://products.mhra.gov.uk. Accessed 27/10/2023.Emend 80 mg Capsule (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 27/10/2023.Emend Capsule and Powder for Suspension (Merck Sharp & Dohme LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 27/10/2023.Joint Formulary Committee. Aprepitant. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/10/2023.Merck Sharp & Dohme (New Zealand) Limited. Emend 80 mg and 125 mg and Capsule data sheet 9 October 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 27/10/2023.
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