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Acridine Derivative Cytotoxic (Specialist Oncology Drug) Pregnancy: Pregnancy: data on the use of amsacrine during pregnancy in patients are not available to judge possible harmfulness, but based on its pharmacological activity harmfulness of treatment during pregnancy is possible, and teratogenicity and other reproductive toxicity have been observed in animal studies. Use during pregnancy is discouraged, especially during the first trimester; in every individual case the advantages of treatment should be weighed against the risks to the foetus. Contraception: because of the mechanism of action and possible adverse effects on the foetus, females should use effective contraception for 3 months after treatment and males for 6 months after treatment. Fertility: reversible azoospermia in humans has been described. Lactation: it is not clear whether amsacrine is excreted in breast milk, so lactation is contraindicated.

Amsacrine

Brand names: Amsidine

Amsacrine is an intravenous cytotoxic agent (an acridine derivative) used in the treatment of acute leukaemias, generally in relapsed or refractory disease.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: SPECIALIST ONCOLOGY USE, ADULTS — INDUCTION OF REMISSION PHASE: the usual dosage of Amsidine is 90 mg/m2 per day for five consecutive days, giving a total dose of 450 mg/m2 per course of treatment. If a bone marrow biopsy performed on day six displays over 50% cellularity and a blast count over 30%, treatment may be extended for an additional three days, bringing the total to 720 mg/m2 per course. More than one course may be required to achieve induction; depending on the effectiveness of the first course in producing myelosuppression, subsequent courses are given at two-week intervals (if not effective) to four-week intervals (if effective). Where a hypocellular marrow has not been achieved after the first course, the daily dose may be escalated to 120 mg/m2 per day for subsequent courses, provided this is not contraindicated for reasons of non-myelosuppressive toxicity. MAINTENANCE PHASE: the maintenance dose is about one third of the induction dose, given either as a single IV infusion or divided into three daily doses — for example 150 mg/m2 once every 3-4 weeks, or 50 mg/m2 per day for three consecutive days repeated every 3-4 weeks.
Route: Intravenous infusion — Amsidine must be diluted in 500 ml of 5% Dextrose Injection BP and infused over 60 to 90 minutes. DO NOT USE OTHER DILUENTS: AMSIDINE IS INCOMPATIBLE WITH SALINE. Care must be taken that no extravasation occurs, which might produce severe irritation or necrosis. Phlebitis or pain at the injection site may occur at doses greater than 70 mg/m2; injection site irritation can be prevented by diluting in a greater volume of 5% glucose and spreading the infusion over a longer period (minimum 1 hour). Caution should be exercised in handling and preparing the solution and the use of polyethylene gloves is recommended; if the solution contacts skin or mucosae, wash thoroughly with soap and water immediately.
Frequency: Induction: once daily for five consecutive days (extendable to eight days — see dose), with subsequent courses at two-week to four-week intervals. Maintenance: once every 3-4 weeks as a single infusion, or daily for three consecutive days repeated every 3-4 weeks.
Max: 120 mg/m2 per day — the highest daily induction dose stated in the SPC posology (escalation for subsequent courses where a hypocellular marrow has not been achieved after the first course, provided this is not contraindicated for non-myelosuppressive toxicity). The highest total per induction course stated is 720 mg/m2 (the eight-day extended course). In hepatic or renal impairment the daily dose must instead be reduced by 20-30%, to 60-75 mg/m2 per day.
THIS DRAFT REPLACES AN EARLIER HOLD. The previous hold reason (no UK SPC in the bundle) is now STALE — the UK SPC for Amsidine 75mg/1.5 ml, concentrate and solvent for concentrate for solution for infusion (eMC product 13279) has been recovered and matches this page exactly on brand, active substance (amsacrine) and route (IV infusion). INDICATION SCOPE: section 4.1 (therapeutic indications) was NOT fetched into this bundle, so the licensed indication is not quoted here; the posology describes an 'induction of remission phase' guided by bone marrow biopsy cellularity and blast count, with a maintenance phase. Verify the licensed indication against the SPC before use. SPECIALIST SUPERVISION: amsacrine should only be used under strict control of a specialised oncologist, preferably in institutions experienced with this kind of therapy. HEPATIC OR RENAL IMPAIRMENT: toxicity at recommended doses is enhanced by hepatic or renal impairment — the dose of Amsidine should be DECREASED BY 20-30% (to 60-75 mg/m2 per day), and laboratory evaluation of hepatic and renal function is necessary prior to and during administration. ELDERLY: elimination may be slower in this group, which should be considered when designing dose schedules. MAINTENANCE TITRATION: each maintenance course should bring the granulocyte count down to 1,000-1,500/microlitre and the platelet count to 50,000-100,000/microlitre; if this is not accomplished the maintenance dose may be escalated by 20% every second course. Granulocyte and platelet counts should be allowed to recover between courses to over 1,500/microlitre and 100,000/microlitre respectively, otherwise the subsequent course should be delayed. DOSE INTERRUPTION: if too strong a decrease in white blood cells or platelets occurs, interruption of treatment or a decrease of dosage can be necessary; red blood cells and platelets should be available for transfusion, along with other facilities for treating bone marrow depression. SOURCE COMPLETENESS: all five captured sections (4.2, 4.3, 4.4, 4.6, 4.8) are complete and untruncated in this bundle. Sections 4.1 and 4.5 (interactions) were not fetched. No openFDA or WHO source was present in this bundle.

Paediatric dose

Route: N/A
Frequency: N/A
Max: Not established
UK SPC section 4.2, verbatim: 'Children under 12 Years: Not recommended.' The SPC gives no dose for children under 12, and it also gives no separate figure for adolescents aged 12 to under 18 — the adult BSA-based regimen above is the only regimen published in the label. No paediatric dose is published here and none may be derived by scaling the adult dose. Verify any use under 18 years against a children's formulary and specialist paediatric oncology advice. Note section 4.4 warns that epileptic seizures (grand mal) are a recognised adverse reaction of amsacrine.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to amsacrine or acridine derivatives
  • Hypersensitivity to one of the other ingredients of the product
  • Clear bone-marrow-suppression as a result of treatment with cytostatics or radiotherapy
  • Lactation (breast-feeding is contraindicated, as it is not clear whether amsacrine is excreted in breast milk)

Side effects

  • Most common adverse reactions — nausea and/or vomiting, anaemia, fever and infection; pain or phlebitis on infusion has been reported
  • Bone marrow depression occurs in ALL patients treated with a therapeutic dosage; main complications are infections and haemorrhages. Minimal white blood cell counts occur on day 5-12, usually followed by complete recovery on day 25; the pattern for platelets is similar to that of leucocytes
  • Common blood and lymphatic — thrombocytopenia, pancytopenia, haemorrhage; Rare — anaemia, granulocytopenia, leukopenia
  • Common infections — infection
  • Rare immune — hypersensitivity, anaphylactic reaction, oedema
  • Common metabolism — hypokalaemia; Rare — weight decreased, weight increased; Not known — hyperuricaemia (secondary to rapid lysis of neoplastic cells)
  • Common psychiatric — affect lability; Rare — lethargy, confusion
  • Common nervous system — grand mal seizure; Rare — headache, hypoaesthesia, dizziness, peripheral neuropathy
  • Rare eye — visual disturbances
  • Common cardiac — cardiotoxicity, arrhythmia, congestive heart failure; Rare — atrial fibrillation, sinus tachycardia, ventricular fibrillation, ventricular arrhythmias, cardiomyopathy, bradycardia, abnormal ECG, decreased ejection fraction
  • Very common vascular — hypotension; Common — haemorrhage
  • Common respiratory — dyspnoea
  • Very common gastrointestinal — nausea, vomiting (mild to moderate), diarrhoea, abdominal pain, stomatitis
  • Common hepatobiliary — hepatitis, jaundice, hepatic insufficiency
  • Very common skin — purpura; Common — alopecia, urticaria and rash
  • Common renal and urinary — haematuria; Rare — anuria, proteinuria, acute renal insufficiency
  • Very common general — infusion site phlebitis/reactions; local necrosis can occur with extravasation

Monitoring

  • Frequent blood counts are necessary — amsacrine can cause severe bone marrow depression, and infections and haemorrhages can be fatal. Administer cautiously and with extra controls where bone marrow depression already exists from other drugs
  • Ensure red blood cells and platelets are available for transfusion, together with other facilities for the treatment of bone marrow depression
  • Blood uric acid levels — careful monitoring is recommended because of hyperuricaemia secondary to rapid lysis of neoplastic cells, in particular for possible consequences for renal function; consider reducing uric acid levels prophylactically prior to or concurrent with treatment
  • Laboratory evaluation of hepatic and renal function prior to and during administration — toxicity at recommended doses is enhanced by hepatic or renal impairment, and a dose reduction might be considered
  • Careful monitoring of cardiac rhythm is recommended for detection of cardiotoxicity
  • Serum potassium — ensure a normal serum potassium level immediately prior to and during administration; patients with hypokalaemia are at increased risk of ventricular fibrillation
  • Watch for allergic reactions (anaphylaxis, oedema, skin reactions), gastrointestinal problems and epileptic seizures; seizures related to amsacrine can be treated according to standard regimen
  • Inspect the infusion site — care must be taken that no extravasation occurs, which might produce severe irritation or necrosis
  • During maintenance, check that each course brings granulocytes down to 1,000-1,500/microlitre and platelets to 50,000-100,000/microlitre, and confirm recovery above 1,500/microlitre and 100,000/microlitre before the next course

Clinical monograph

How it works

It intercalates into DNA and inhibits topoisomerase II, causing DNA strand breaks and inhibition of cell replication in dividing cells.

Prescribing in practice

  • Profound myelosuppression and cardiotoxicity (including arrhythmias, exacerbated by hypokalaemia) are major risks, so correct potassium before dosing and monitor cardiac status.
  • Administered as an intravenous infusion by clinicians experienced in cytotoxic chemotherapy.
  • It is a vesicant/irritant and requires careful intravenous administration to avoid extravasation.

Monitoring

Monitor full blood count, serum potassium and magnesium, cardiac rhythm, and liver function during treatment.

Counselling the patient

  • Report fever, bleeding, bruising, or signs of infection promptly as blood counts can fall.
  • Report palpitations, chest pain, or fainting.
  • Treatment is given in a specialist haematology setting.

Evidence & guidelines

Amsacrine has an established role in acute leukaemia regimens; consult the SPC and current prescribing references for administration and monitoring.

Reference: SACT database; SmPC Amsidine; British Committee for Standards in Haematology (BCSH) acute leukaemia guidelines; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.

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