Category: Antineoplastic
Composition- : Each vial contains: Topotecan HCl equivalent to Topotecan 2.5mg/2.5ml, 4mg/4ml.
Topotecan is believed to exert its cytotoxic effects during the S-phase of DNA synthesis. Topoisomerase I relieves torsional strain in DNA by inducing reversible single strand breaks. Topotecan binds to the topoisomerase I-DNA complex and prevents religation of these single strand breaks. This ternary complex interferes with the moving replication fork, which leads to the induction of replication arrest and lethal double-stranded breaks in DNA. As mammalian cells cannot efficiently repair these double strand breaks, the formation of this ternary complex eventually leads to apoptosis (programmed cell death). Topotecan mimics a DNA base pair and binds at the site of DNA cleavage by intercalating between the upstream (−1) and downstream (+1) base pairs. Intercalation displaces the downstream DNA, thus preventing religation of the cleaved strand. By specifically binding to the enzyme–substrate complex, Topotecan acts as an uncompetitive inhibitor.
| Specification- | Light Greenish color powder filled in glass vials.
pH------------ 2.5 to 4.5 | | Indication : | Metastatic carcinoma of the ovary after failure of initial or subsequent chemo therapy. Small cell lung cancer disease after failure of first line chemotherapy | | Dosage :- | The recommended starting dose is 1.5mg/m2 body surface area by IV infusion over 30 minutes daily for 5 consecutive days In absence of tumor progression, a minimum of four courses are recommended, as tumour response may be delayed. | | Contraindications:- | Severe hypersensitivity reactions (e.g., anaphylactoid reactions)
Pregnant or Breastfeeding,
Severe bone marrow depression. | | Precautions:- | Bone Marrow Suppression, Thrombocytopenia, Diarrhea, Interstitial Lung Disease, Pregnancy Neutropenia, Thrombocytopenia, Anemia. | | Drug interaction: | Cyclosporine A (inhibitor of ABCB1, ABCC1 [MRP-1], and CYP3A4) with hycamtin capsules increased topotecan exposure to 2- to 3-fold of control. The pharmacokinetics of topotecan were generally unchanged when coadministered with ranitidine. | | Adverse Effect-: | Bone marrow suppression. Primarily neutropenia, thrombocytopenic anaemia, abdominal discomfort. | | Storage: | Store between 2-80C | | Purity:- | Not less than 99.5%. |
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