Generic
Topotecan
1 brands available in the market
At a glance
Topotecan is indicated for metastatic ovarian cancer, small cell lung cancer, and cervical cancer. It is a topoisomerase I inhibitor.
Description
Topotecan is a topoisomerase I inhibitor. It binds to the topoisomerase I-DNA complex and prevents religation of single-strand breaks, leading to double-stranded DNA breaks and apoptosis.
Indications
- Metastatic ovarian cancer
- Small cell lung cancer
- Cervical cancer
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
Topoisomerase I Inhibitor
Pharmacology
Topotecan binds to the topoisomerase I-DNA complex, preventing religation of single-strand breaks. This ternary complex interferes with the replication fork, leading to double-stranded DNA breaks and apoptosis.
Mechanism of action
Binds to topoisomerase I-DNA complex, preventing DNA religation and causing apoptosis.
Dosage
Adult Dose (IV):
- Ovarian cancer: 1.5 mg/m² IV over 30 minutes daily for 5 days, every 21 days
- Small cell lung cancer: 1.5 mg/m² IV over 30 minutes daily for 5 days, every 21 days
- Cervical cancer: 0.75 mg/m² IV over 30 minutes on Days 1, 2, 3 + cisplatin 50 mg/m² on Day 1, every 21 days
- Renal impairment (CrCl 20-30): 0.75 mg/m²
Administration
- For IV infusion only
- Dose based on body surface area
- Prepare solution immediately before use
Missed dose
If you miss a dose, consult your doctor; do not double the dose.
Side effects
Common Side Effects:
- Neutropenia
- Thrombocytopenia
- Anemia
- GI upset
- Total alopecia
- Headache
- Dyspnea
- Fatigue
Precautions & warnings
- Caution in preexisting bone marrow depression
- Frequent monitoring of peripheral blood cell counts
- Do not continue subsequent courses until neutrophils >1000, platelets >100,000, and hemoglobin >9.0 g/dl
- May impair ability to drive or operate machinery
Contraindications
- Severe bone marrow depression
- Pregnancy
- Lactation
- Severe renal or hepatic impairment
Drug interactions
- Phenytoin: increased clearance
- G-CSF: may prolong neutropenia; give 24 hours after topotecan
- Other cytotoxic drugs (cisplatin): increased bone marrow suppression; dose reduction may be needed
Food interactions
Food interactions are not significant.
Use in pregnancy
Use in Pregnancy: Category D; positive evidence of human fetal risk; use only in life-threatening situations.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Contraindicated; consult your doctor.
Pediatric use
Safety and effectiveness not established in pediatric patients
Geriatric use
Caution required in elderly patients
Renal / hepatic impairment
Renal Impairment: CrCl 20-30: 0.75 mg/m²
Hepatic Impairment: Avoid
Overdose effects
Symptoms: Bone marrow suppression.
Treatment: Supportive care.
Storage conditions
Unopened vial: Store at 20-25°C; protect from light. Reconstituted solution: Stable for 24 hr at 20-25°C.