Fosaprepitant


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Prophylaxis of chemotherapy-induced nausea and vomiting
Adult: In combination therapy w/ a corticosteroid (e.g. dexamethasone) and 5-HT3 antagonist: 150 mg given via IV infusion over 20-30 min approx 30 min prior to chemotherapy on day 1 of cycle only.
Hướng dẫn pha thuốc
IV infusion: Add 5 mL of NaCl 0.9% soln to a vial labelled as containing 150 mg. Swirl gently to avoid foaming. Dilute further w/ 145 mL of NaCl 0.9% to a total volume of 150 mL, w/ a final concentration of 1 mg/mL.
Tương kỵ
Incompatible w/ soln containing divalent cations (e.g. Ca, Mg, Hartmann’s soln, lactated Ringer’s inj).
Chống chỉ định
Hypersensitivity. Concomitant use w/ pimozide, cisapride, terfenadine.
Thận trọng
Moderate to severe hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Nervous: Asthenia, fatigue, malaise, dizziness, somnolence, peripheral neuropathy, headache, weakness, anxiety.
CV: Palpitations, hot flush.
GI: Nausea, anorexia, constipation, diarrhoea, abdominal pain, GERD, dry mouth, flatulence, eructation, dyspepsia.
Resp: Hiccups.
Hepatic: Increased ALT/AST, alkaline phosphatase.
Genitourinary: UTI, dysuria.
Haematologic: Neutropenia, anaemia, leucopenia.
Musculoskeletal: Limb pain.
Dermatologic: Pruritus, acne, urticaria.
Others: Infusion site reactions (e.g. pain, induration).
Potentially Fatal: Hypersensitivity reactions (e.g. Steven-Johnson syndrome/toxic epidermal necrolysis, anaphylaxis and anaphylactic shock).
IV/Parenteral: B
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor INR (in patients taking warfarin) for 2 wk (particularly at 7-10 days) following admin; signs or symptoms of hypersensitivity reaction.
Tương tác
Decreased INR of prothrombin time w/ warfarin. Increased plasma concentration of midazolam or other benzodiazepines (e.g. alprazolam, triazolam). May decrease efficacy of OC. May decrease plasma concentration of CYP2C9 substrates (e.g. tolbutamide). Increased exposure w/ CYP3A4 inhibitors (e.g. clarithromycin, ketoconazole, protease inhibitors, nefazodone). Decreased serum concentration w/ phenytoin. Decreased exposure w/ CYP3A4 inducers (e.g. rifampicin, carbamazepine). May increase serum concentration of corticosteroids.
Potentially Fatal: Increased serum concentration and risk of QT interval prolongation w/ pimozide, cisapride, terfenadine.
Food Interaction
Increased serum concentration w/ grapefruit and grapefruit juice. Decreased serum concentration w/ St John’s wort.
Tác dụng
Description: Fosaprepitant is a prodrug of aprepitant. It prevents acute and delayed emesis by inhibiting a substance P/neurokin-1 (NK1) receptor. It also augments antiemetic effect of 5HT3 receptor antagonist and corticosteroids.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: W/in 30 min.
Distribution: Aprepitant: Crosses blood brain barrier. Volume of distribution: Approx 70 L. Plasma protein binding: >95%.
Metabolism: Rapidly converted in hepatic and extrahepatic tissues into aprepitant which undergoes extensive metabolism via oxidation primarily by CYP3A4 enzyme and some by CYP1A2 and CYP2C19 enzymes into 7 weakly-active metabolites.
Excretion: Mainly via urine (57% as metabolites); faeces (45% as metabolites). Elimination half-life: Approx 9-13 hr.
Đặc tính

Chemical Structure Image
Fosaprepitant

Source: National Center for Biotechnology Information. PubChem Database. Fosaprepitant, CID=135413538, https://pubchem.ncbi.nlm.nih.gov/compound/Fosaprepitant (accessed on Jan. 21, 2020)

Bảo quản
Store between 2-8°C.
Phân loại MIMS
References
Anon. Fosaprepitant. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/09/2017.

Buckingham R (ed). Fosaprepitant. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2017.

Emend Injection Powder, Lyophilized for Solution (Merck Sharp and Dohme Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/09/2017.

Joint Formulary Committee. Fosaprepitant. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Aprepitant/Fosaprepitant Dimeglumine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 08/09/2017.

Preston CL (ed). Interactions Search Results for Fosaprepitant Pimozide. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/09/2017.

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