amsacrine: clinical use

Prescribing considerations

• Restrict use to specialist haematology or oncology settings with facilities to manage profound myelosuppression, infection, and haemorrhage.
• Assess hepatic and renal function because impairment can increase toxicity.
• Correct hypokalaemia before administration and minimise other factors that increase arrhythmia risk.
• Consider slower elimination in older people.
• Prevent extravasation and ensure access to supportive blood products and antimicrobial treatment.

Contraindications and cautions

• Hypersensitivity to amsacrine, acridine derivatives, or product excipients
• Clear bone-marrow suppression caused by previous cytotoxic treatment or radiotherapy
• Breastfeeding

Monitoring

• Full blood count with differential and platelets
• Liver and renal function
• Electrolytes, particularly potassium
• Cardiac rhythm and clinical cardiac function
• Uric acid and renal consequences of tumour lysis
• Infusion site for phlebitis or extravasation

Clinical pharmacology

Amsacrine is an intravenously administered aminoacridine that intercalates with DNA and acts as a topoisomerase II poison. It distributes widely but has limited penetration into the brain and cerebrospinal fluid. It undergoes hepatic biotransformation with substantial biliary excretion; severe hepatic dysfunction prolongs elimination.

Formulation and product differences

• The product comprises separate concentrate and solvent vials that must be combined before further dilution.
• Only glucose solution should be used for final dilution; saline and other diluents are incompatible.
• The prepared solution reacts with plastic syringes, so specified glass equipment is required.
• Preparation requires cytotoxic-handling precautions and protection from light.

Solution for infusion

Route: Intravenous

Strengths: 75 mg/1.5 mL