Names and pronunciation
(toh-poh-tee′kan) Hycamtin
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Drug reference
(toh-poh-tee′kan) Hycamtin
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Func. class.: Antineoplastic, natural; topoisomerase inhibitor
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Chem. class.: Camptothecin analog
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ACTION: Antitumor product with topoisomerase-I–inhibitory activity; topoisomerase I relieves torsional strain in DNA by causing single-strand breaks; also causes double-strand DNA damage
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USES: Metastatic ovarian cancer after failure of traditional chemotherapy; relapsed small-cell lung cancer; cervical cancer
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, hypersensitivity, severe bone marrow depression
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Black Box Warning: Neutropenia, bone marrow suppression Precautions: Children, renal disease, gelatin hypersensitivity, anemia, contra- ceptive requirements, dehydration, diar- rhea, extravasation, herpes, infertility, neutropenia, pulmonary fibrosis, varicella Black Box Warning: Bone marrow suppression: CBC, differential, plate- let count weekly; withhold product if WBC is <3500/mm3 or platelet count is <100,000/mm3; notify prescriber of re- sults; product should be discontinued • Pregnancy/breastfeeding: do not use in pregnancy or breastfeeding, can cause fetal harm; use contraception during and for ≥1 mo after final dose (female), during and for 3 mo after final dose (males); may cause infertility in both males/females • Oral status: Buccal cavity for dry- ness, sores or ulcerations, white patches, oral pain, bleeding, dysphagia • Interstitial lung disease (ILD): fever, cough, dyspnea, hypoxia; may be fatal • Fluid balance: Increased fluid intake to 2-3 L/day to prevent dehydration un- less contraindicated Black Box Warning: To report signs of anemia: fatigue, headache, faintness, SOB, irritability • Rinsing of mouth tid-qid with water, club soda; brushing of teeth bid-tid with soft brush or cotton-tipped applicator for stomatitis; to use unwaxed dental floss • To use effective contraception during treatment and for 6 mo after; that males should use contraception during and for 3 mo after final dose; not to breastfeed • To avoid OTC products without ap- proval of prescriber • To avoid driving or other activities re- quiring alertness • To avoid vaccines, toxoids • Not to crush, chew capsules • Not to retake dose if vomiting occurs; to notify prescriber
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SIDE EFFECTS CNS: Arthralgia, asthenia, headache, myalgia, pain, weakness GI: Abdominal pain, constipation, diarrhea, obstruction, nausea, stoma- titis, vomiting; increased ALT, AST; anorexia HEMA: Neutropenia, leukopenia, throm bocytopenia, anemia, sepsis INTEG: Total alopecia RESP: Dyspnea, cough, interstitial lung disease
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INTERACTIONS • Avoid use with P-glycoprotein, breast cancer resistance protein inhibitors (amiodarone, clarithromycin, diltiaZEM, erythromycin, indinavir), quiNIDine, tes- tosterone, verapamil, tamoxifen, itracon- azole, mefloquine, RU-486, niCARdipine, vaccines, toxoids Increase: myelosuppression when used with CISplatin Increase: bleeding risk—NSAIDs, antico- agulants, thrombolytics, platelet inhibitors Drug/Food • Avoid use with grapefruit juice
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DOSAGE AND ROUTES Metastatic carcinoma of the ovary • Adult: IV INFUSION 1.5 mg/m2 over 30 min daily × 5 days starting on day 1 of 21-day course × 4 courses Persistent cervical cancer • Adult: IV INFUSION 0.75 mg/m2 on days 1, 2, 3 then 50 mg/m2 cisplatin IV on day 1 then repeat q21days; adjust for toxicity Relapsed small-cell lung cancer • Adult: PO 2.3 mg/m2/day × 5 days then repeat q21days Renal dose • Adult: PO CCr ≥50 mL/min: No change; CCr 30-49 mL/min: Reduce dose to 1.5 mg/m2/day; dose may be increased by 0.4 mg/m2/day after the first course if no severe hematologic or gastrointestinal toxicities occur; CCr <30 mL/min: Reduce dose to 0.6 mg/m2/day; dose may be in creased by 0.4 mg/m2/day after the first course if no severe hematologic or gas trointestinal toxicities occur • Adult: IV CCr 40-60 mL/min: No change; CCr 20-39 mL/min: Reduce dose to 0.75 mg/m2; CCr <20 mL/min: unknown Available forms Lyophilized powder for inj 4 mg; caps 0.25, 1 mg
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Administer: • Store caps in refrigerator; IV INFU- SION unopened at room temperature; protect both from light PO route • Do not break, crush, chew, or open caps; protect from light • Take without regard to food Intermittent IV INFUSION route • Visually inspect for particulate matter and discoloration before use • Reconstitute each 4-mg vial with 4 mL sterile water for injection; use immedi- ately; no preservative • Withdraw the appropriate volume of the reconstituted solution; dilute further; dilute in 0.9% NaCl or D5W before ad- ministration • The reconstituted solution is yellow or yellow-green • Topotecan injection diluted for infu- sion is stable at room temperature with normal light for 24 hr • Infuse over 30 min
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Assess: • Hepatic studies: AST, ALT, alk phos, which may be elevated; creatinine, BUN
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Evaluate: • Therapeutic response: decreased tu- mor size, spread of malignancy
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That total alopecia may occur; that hair grows back but is different in color and texture • To avoid foods with citric acid, hot temperature, or rough texture if stomati- tis is present; to drink adequate fluids • To report stomatitis and any bleeding, white spots, ulcerations in mouth; to ex- amine mouth daily; to report symptoms
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PHARMACOKINETICS Rapidly and completely absorbed, excreted in urine and feces as metabolites, half-life 2.8 hr, 7%-35% bound to plasma proteins, PO peak 1-2 hr
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• Adult: IV INFUSION 1.5 mg/m2 over 30 min daily × 5 days starting on day 1 of 21-day course × 4 courses Persistent cervical cancer
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• Adult: IV INFUSION 0.75 mg/m2 on days 1, 2, 3 then 50 mg/m2 cisplatin IV on day 1 then repeat q21days; adjust for toxicity Relapsed small-cell lung cancer
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• Adult: PO 2.3 mg/m2/day × 5 days then repeat q21days Renal dose
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• Adult: PO CCr ≥50 mL/min: No change; CCr 30-49 mL/min: Reduce dose to 1.5 mg/m2/day; dose may be increased by 0.4 mg/m2/day after the first course if no severe hematologic or gastrointestinal toxicities occur; CCr <30 mL/min: Reduce dose to 0.6 mg/m2/day; dose may be in creased by 0.4 mg/m2/day after the first course if no severe hematologic or gas trointestinal toxicities occur
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• Adult: IV CCr 40-60 mL/min: No change; CCr 20-39 mL/min: Reduce dose to 0.75 mg/m2; CCr <20 mL/min: unknown Available forms Lyophilized powder for inj 4 mg; caps 0.25, 1 mg
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