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Indications and Dosage
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.
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Renal Impairment
Reduce dose by 20-30%.
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Hepatic Impairment
Reduce dose by 20-30%.
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Reconstitution
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.
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Incompatibility
Incompatible with Na chloride 0.9%, chloride containing solution.
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Contraindications
Pre-existing drug-induced or radiation therapy-induced bone marrow suppression. Pregnancy and lactation. Concomitant administration with live vaccines.
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Special Precautions
Renal and hepatic impairment.
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Adverse Reactions
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. |
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Monitoring Parameters
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.
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Overdosage
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.
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Drug Interactions
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.
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Action
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. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Amsacrine, CID=2179, https://pubchem.ncbi.nlm.nih.gov/compound/2179 (accessed on July 27, 2020) |
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Storage
Store below 25°C. Protect from light.
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MIMS Class
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ATC Classification
L01XX01 - amsacrine ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
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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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