Amsacrine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Acute leukaemia
Adult: Induction of remission: 90 mg/m2 daily for 5-8 days. Courses may be repeated at 2- to 4-week intervals according to response, and may be increased to 120 mg/m2 daily in subsequent courses if tolerated. Maintenance: 150 mg/m2 as a single dose or divided over 3 consecutive days. Doses are given every 3-4 weeks, adjusted as necessary according to response. All doses are given via infusion over 60-90 minutes.
Renal Impairment
Reduce dose by 20-30%.
Hepatic Impairment
Reduce dose by 20-30%.
Hướng dẫn pha thuốc
Add 1.5 mL of amsacrine to 13.5 mL of diluent providing a solution containing in a 5 mg/mL; further dilute with 500 mL of 5% glucose inj.
Tương kỵ
Incompatible with Na chloride 0.9%, chloride containing solution.
Chống chỉ định
Pre-existing drug-induced or radiation therapy-induced bone marrow suppression. Pregnancy and lactation. Concomitant administration with live vaccines.
Thận trọng
Renal and hepatic impairment.
Phản ứng phụ
Significant: Bone marrow suppression, cardiovascular effects (e.g. acute arrhythmia, heart failure, bradycardia, tachycardia), extravasation, tumour lysis syndrome.
Blood and lymphatic system disorders: Thrombocytopenia, pancytopenia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain.
General disorders and administration site conditions: Pyrexia, infusion site phlebitis; injection site irritation, necrosis, skin inflammation.
Hepatobiliary disorders: Hepatitis, jaundice, hepatic insufficiency.
Investigations: Increased hepatic enzymes.
Metabolism and nutrition disorders: Hypokalaemia.
Nervous system disorders: Grand mal seizure, headache, hypoesthesia, dizziness, peripheral neuropathy
Psychiatric disorders: Affect lability.
Renal and urinary disorders: Hematuria.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Purpura, alopecia, urticaria, rash.
Vascular disorders: Hypotension.
Potentially Fatal: Infection, haemorrhage, stomatitis.
MonitoringParameters
Monitor LFT, kidney function prior to and during treatment. Monitor CBC with differential frequently during induction and for 2-3 weeks after, electrolytes prior to each dose, bone marrow studies periodically; ECG during and after administration. Monitor for signs and symptoms of infection, tumour lysis syndrome, bleeding, and fluid status during therapy. Monitor infusion site during infusion.
Quá liều
Symptoms: Haemorrhage, infection, severe mucositis, vomiting or diarrhoea. Management: symptomatic and supportive treatment. Bone marrow hypoplasia or aplasia may require treatment with red cell, granulocyte or platelet transfusions and appropriate antibiotics.
Tương tác
May increase risk of cardiotoxicity with diuretics or nephrotoxic drugs (e.g. aminoglycosides). May diminish therapeutic effects of vaccines. May potentiate adverse effects with other cytotoxic agents.
Tác dụng
Description: Amsacrine, an antineoplastic agent, intercalates with DNA and inhibits nucleic acid synthesis, causing breakage of double-strand DNA and cell cycle arrest at the G2 or S phase.
Pharmacokinetics:
Distribution: Plasma protein binding: Approx 98%.
Metabolism: Metabolised in the liver.
Excretion: Mainly via bile as metabolites; urine (35%; 20% as unchanged drug). Elimination half-life: 5-8 hours.
Đặc tính

Chemical Structure Image
Amsacrine

Source: National Center for Biotechnology Information. PubChem Database. Amsacrine, CID=2179, https://pubchem.ncbi.nlm.nih.gov/compound/2179 (accessed on July 27, 2020)

Bảo quản
Store below 25°C. Protect from light.
Phân loại MIMS
Phân loại ATC
L01XX01 - amsacrine ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Amsidine 75 mg/1.5 mL Concentrate and Solvent for Concentrate for Solution for Infusion (Eurocept International BV) . MHRA. https://products.mhra.gov.uk/. Accessed 07/07/2020.

Anon. Amsacrine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/07/2020.

Buckingham R (ed). Amsacrine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2020.

Joint Formulary Committee. Amsacrine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2020.

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