| TOPOTECAN HYDROCHLORIDE
Classifications: antineoplastic; camptothecin agent; topoisomerase i inhibitor; Therapeutic: antineoplastic; topoisomerase i inhibitor
Pregnancy Category: D
4 mg injection
Antitumor mechanism is related to inhibition of the activity of topoisomerase I, an enzyme required for DNA replication.
Topoisomerase I is essential for the relaxation of supercoiled double-stranded DNA that enables replication and transcription
Topotecan binds to the DNA-topoisomerase I complex. This permits uncoiling but prevents recoiling of the two strands of
DNA, resulting in a permanent break in the DNA strands.
Metastatic ovarian cancer, small cell lung cancer.
Previous hypersensitivity to topotecan, irinotecan, or other camptothecin analogs; acute infection; severe bone marrow depression;
severe thrombocytopenia; pregnancy (category D), lactation.
Myelosuppression; severe renal impairment or renal failure; history of bleeding disorders; previous cytotoxic or radiation
Route & Dosage
|Metastatic Ovarian Cancer and Small Cell Lung Cancer
Adult: IV 1.5 mg/m2 daily for 5 d starting on day 1 of a 21 d course. Four courses of therapy recommended. Subsequent doses can be adjusted
by 0.25 mg/m2 depending on toxicity.
Clcr 2039 mL/min: use 0.75 mg/m2
Hemodialysis: Supplementation not needed
- Initiate therapy only if baseline neutrophil count ≥1500/mm3 and platelet count ≥100,000/mm3. Do not give subsequent doses until neutrophils ≥1000/mm3, platelets ≥100,000/mm3, and Hgb >9.0 mg/dL.
- Note: Dosage adjustments to 0.75 mg/m2 are recommended with moderate renal impairment.
PREPARE: IV Infusion: Reconstitute each 4-mg vial with 4 mL sterile water for injection to yield 1 mg/mL. Withdraw the required dose and inject
into 50100 mL of NS or D5W. If skin contacts drug during preparation, wash immediately with soap and water.
ADMINISTER: IV Infusion: Give over 30 min immediately after preparation.
INCOMPATIBILITIES Y-site: Dexamethasone, fluorouracil, mitomycin.
- Store vials at 20°25° C (68°77° F); protect from light. Reconstituted vials are stable for
Adverse Effects (≥1%) Body as a Whole: Asthenia, fever, fatigue. GI: Nausea, vomiting, diarrhea, constipation, abdominal pain, stomatitis, anorexia,
transient elevations in liver function tests. Hematologic: Leukopenia, neutropenia, anemia, thrombocytopenia. Respiratory: Dyspnea. Skin: Alopecia.
Increased risk of bleeding with anticoagulants
, antiplatelet agents
35% bound to plasma proteins
Undergoes pH-dependent hydrolysis. Elimination:
30% in urine. Half-Life:
Assessment & Drug Effects
- Lab tests: Obtain CBC counts with differential frequently; periodically monitor ALT.
- Assess for GI distress, respiratory distress, neurosensory symptoms, and S&S of infection throughout therapy.
Patient & Family Education
- Learn common adverse effects and measures to control or minimize when possible. Immediately report any distressing adverse
effects to physician.
- Avoid pregnancy during therapy.