Topotecan


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Small cell lung cancer 2.3 mg/m2 once daily for 5 consecutive days, repeat every 21 days. If neutropenia, or if platelet count drops below 25,000 cells/mm3 or for patient w/ severe diarrhoea, reduce dose to 400 mcg/m2 (to 1.9 mg/m2/day, and subsequently to 1.5 mg/m2/day). IV Ovarian carcinoma; Small cell lung cancer 1.5 mg/m2/day on days 1-5 of a 21-day course. Min: 4 courses to be given (provided blood counts and Hb 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. Cervical cancer W/ cisplatin: 0.75 mg/m2 on days 1, 2 and 3 of a 21-day course. 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, reduce topotecan dose to 0.6 mg/m2.
Dosage Details
Intravenous
Ovarian carcinoma, 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).

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.

Oral
Small cell lung cancer
Adult: 2.3 mg/m2 once daily for 5 consecutive days, repeat every 21 days. If neutropenia, or if platelet count drops below 25,000 cells/mm3 or for patient w/ severe diarrhoea, reduce dose to 400 mcg/m2 (to 1.9 mg/m2 daily, and subsequently to 1.5 mg/m2 daily).
Renal Impairment
Oral:
CrCl Dosage
30-49 1.8 mg/m2 once daily for 5 consecutive days.
50-80 No dosage adjustment.
Intravenous:
Ovarian carcinoma,Small cell lung cancer:
CrCl Dosage
20-30 Initial dose 0.75 mg/m2.
Cervical cancer: Treatment to be initiated only if serum creatinine ≤1.5 mg/dl.
Hepatic Impairment
Intravenous:
Ovarian carcinoma,Small cell lung cancer: Severe: Avoid.
Cervical cancer: Severe: avoid.
Administration
Cap: May be taken with or without food. Swallow whole, do not open/chew/crush.
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.
Special 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.
IV/Parenteral/PO: D
Overdosage
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.
Food Interaction
Possible decrease in activity with St John's wort.
Action
Description: 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.
Pharmacokinetics:
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.
Storage
Cap: Store between 2-8°C. Do not freeze. Unopened vial: Store at 20-25°C; protect from light. Reconstituted solution: Stable for 24 hr at 20-25°C in ambient light.
Disclaimer: This information is independently developed by MIMS based on Topotecan from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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