Topotecan

Indications
 Intravenous
Small cell lung cancer
Adult: 1.5 mg/m2/day by IV infusion over 30 min on days 1-5 of a 21-day course. Min: 4 courses to be given (provided blood counts and haemoglobin have adequately recovered). In the event of severe neutropenia or platelet count falls below 25,000 cells/mm3, reduce dose to 1.25 mg/m2. Alternatively, in the event of severe neutropenia, granulocyte colony-stimulating factor (G-CSF) to be given following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hr after topotecan treatment completion).
CrCl (ml/min)Dosage Recommendation
20-30Initial dose 0.75 mg/m2.
Hepatic impairment: Severe: Avoid.
Intravenous
Ovarian carcinoma
Adult: 1.5 mg/m2/day by IV infusion over 30 min on days 1-5 of a 21-day course. Min: 4 courses to be given (provided blood counts and haemoglobin have adequately recovered). In the event of severe neutropenia or platelet count falls below 25,000 cells/mm3, reduce dose to 1.25 mg/m2. Alternatively, in the event of severe neutropenia, granulocyte colony-stimulating factor (G-CSF) to be given following the subsequent course (before resorting to dose reduction) starting from day 6 of the course (24 hr after topotecan treatment completion).
CrCl (ml/min)Dosage Recommendation
20-30Initial dose 0.75 mg/m2.
Hepatic impairment: Severe: Avoid.
Intravenous
Cervical cancer
Adult: As combination therapy with cisplatin: 0.75 mg/m2, by IV infusion over 30 min on days 1, 2 and 3 of a 21-day course; cisplatin 50 mg/m2 as IV infusion after topotecan on day 1. Dosage adjustments for subsequent courses are specific for each drug. If severe febrile neutropenia or if the platelet count drops below 10,000 cells/mm3, topotecan dose to be reduced to 0.6 mg/m2. Alternatively, in severe febrile neutropenia, granulocyte colony-stimulating factor (G-CSF) to be given from day 4 of the subsequent course (before resorting to dose reduction), 24 hr after topotecan treatment completion; if febrile neutropenia recurs despite G-CSF , topotecan dosage to be further reduced to 0.45 mg/m2 for subsequent courses.
Renal impairment: Treatment to be initiated only if serum creatinine ≤1.5 mg/dl.
Hepatic impairment: Severe: avoid.

Special Populations: Dosage should be reduced after severe thrombocytopaenia and in patients with impaired renal function; CrCl between 20-39 mL/min: 1/2 of the recommended dose.

Reconstitution: Add 4 ml of sterile water for inj to the vial containing 4 mg of topotecan in order to obtain a solution with 1 mg/ml of topotecan. The required daily dose is further diluted in a suitable volume (e.g. 50-250 ml) of 5% dextrose or 0.9% sodium chloride inj and infused IV over a period of 30 min. Solution should be prepared immediately before use.
Incompatibility: Incompatible with ticarcillin sodium, potassium clavulanate, dexamethasone sodium phosphate, fluorouracil and mitomycin.
Contraindications
 Severe bone marrow depression (e.g. baseline neutrophil count of <1500 cells/mm3 and platelet count <100,000/mm3). Pregnancy, lactation, severe renal or hepatic impairment.
Warnings / Precautions
 Preexisting bone marrow depression. Frequent monitoring of peripheral blood cell counts during treatment. Do not continue subsequent courses until neutrophils recover to >1000 cells/mm3, platelets recover to >100,000 cells/mm3 and haemoglobin levels recover to 9.0 g/dl (with transfusion if needed). May impair ability to drive or operate machinery.
Adverse Reactions
 Neutropenia (nadir of white cell count occurs about 9-12 days after admin), thrombocytopenia and anaemia. GI upset, total alopecia, headache, dyspnoea. Fatigue, weakness, malaise, pruritus and hyperbilirubinaemia.
Overdose Reactions
 Symptoms: Bone marrow supression.
Drug Interactions
 Increased clearance with phenytoin. G-CGF to be given 24 hr after completion of treatment with topotecan as concurrent admin may prolong duration of neutropenia. Increased bone marrow supression with other cytotoxic drugs (e.g. cisplatin) so dose reduction may be needed.
See Below for More topotecan Drug Interactions
Food Interactions
 Possible decrease in activity with St John's wort.
Mechanism of Actions
 Topotecan, an alkaloid, is a semi-synthetic derivative of camptothecin which inhibits topoisomerase I, preventing DNA replication and translocation. It acts in the S phase of DNA synthesis.
Distribution: Widely distributed. Protein-binding: 35%. Terminal half-life: 2-3 hr.
Metabolism: Undergoes reversible hydrolysis to inactive hydroxy acid form; small amounts demethylated in the liver.
Excretion: Excreted in urine.
Administration
 Cap: May be taken with or without food. (Swallow whole, do not open/chew/crush.)
Storage Conditions
 Intravenous: Unopened vial: Store at 20-25°C; protect from light. Reconstituted solution: Stable for 24 hr at 20-25°C in ambient light.
ATC Classification
 L01XX17 - topotecan ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
Storage
 Intravenous: Unopened vial: Store at 20-25°C; protect from light. Reconstituted solution: Stable for 24 hr at 20-25°C in ambient light.
Available As
  • Topotecan 2.5 mg
  • Topotecan 4 mg

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