topotecan

High Alert

IV: Metastatic ovarian cancer that has not responded to previous chemotherapy.
Small cell lung cancer unresponsive to first line therapy.
Stage IV-B persistent or recurrent cervical cancer not amenable to treatment with surgery or radiation (with cisplatin).
PO: Relapsed small cell lung cancer in patients with a complete or partial prior response and who are ≥45 days from the end of first-line chemotherapy.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Renal impairment (↓ dose if CCr <40 mL/min);
Platelet count <25,000 cells/mm³ (↓ dose);
History of interstitial lung disease (ILD), pulmonary fibrosis, lung cancer, thoracic radiation, or use of pneumotoxic drugs or colony stimulating factors;
Rep: Women of reproductive potential;
Geri: Older adults may require dose ↓ due to age-related ↓ in renal function.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia

GI: abdominal pain, diarrhea, nausea, vomiting, ↑liver enzymes, anorexia, constipation, stomatitis

Hemat: anemia, neutropenia, thrombocytopenia

MS: arthralgia

Neuro: headache, fatigue, weakness

Resp: dyspnea, ILD

Interactions ⬆ ⬇

Drug-drug:

P-glycoprotein inhibitors, including amiodarone, azithromycin, captopril, carvedilol, clarithromycin, conivaptan, cyclosporine, diltiazem, dronedarone, erythromycin, felodipine, itraconazole, ketoconazole, lopinavir, ritonavir, quinidine, ranolazine, ticagrelor, or verapamil, may ↑ levels and risk of toxicity; avoid concurrent use.
Neutropenia is prolonged by concurrent use of filgrastim; do not use filgrastim until day 6, 24 hr following completion of topotecan.
↑myelosuppression with other antineoplastics (especially cisplatin) or radiation therapy.
May ↓ antibody response to and ↑ risk of adverse reactions from live-virus vaccines.

Availability ⬆ ⬇

(Generic available)

Capsules: 0.25 mg; 1 mg
Powder for injection: 4 mg/vial
Solution for injection: 1 mg/mL

Route/Dosage ⬆ ⬇

PO (Adults ): 2.3 mg/m²/day for 5 days starting on Day 1 of a 21-day course (round calculated oral dose to nearest 0.25 mg and prescribe the minimum number of 1 mg and 0.25 mg capsules with the same number of capsules prescribed for each of the 5 days).
IV (Adults ): Ovarian and Small Cell Lung Cancer: 1.5 mg/m²/day for 5 days starting on Day 1 of a 21-day course; Cervical Cancer: 75 mg/m² on Days 1, 2, and 3 followed by cisplatin on Day 1 and repeated every 21 days.

Renal Impairment

PO (Adults ): CCr 30–49 mL/min: 1.5 mg/m²/day for 5 days starting on Day 1 of a 21-day course; may ↑ dose after 1st course by 0.4 mg/m²/day if no severe hematologic or GI toxicities occur; CCr <30 mL/min: 0.6 mg/m²/day for 5 days starting on Day 1 of a 21-day course; may ↑ dose after 1st course by 0.4 mg/m²/day if no severe hematologic or GI toxicities occur.

Renal Impairment

IV (Adults ): CCr 20–39 mL/min: 0.75 mg/m²/day for 5 days starting on Day 1 of a 21-day course; Cervical Cancer: Administer at standard doses only if serum creatinine ≤1.5 mg/dL; do not administer if serum creatinine >1.5 mg/dL.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Interferes with DNA synthesis by inhibiting the enzyme topoisomerase.

Therapeutic effects:

Death of rapidly replicating cells, particularly malignant ones.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: enzyme inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability. 40% absorbed following oral administration.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Small amounts metabolized by the liver. 18–33% excreted in feces; 20–50% excreted in urine (primarily as metabolites).

Half-Life: PO: 3–6 hr; IV: 2–3 hr.

Time/Action Profile ⬆ ⬇

(effects on WBCs)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1–2 hr	24 hr
IV	within days	11 days	7 days

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise to read Patient Information before starting therapy. Instruct patient to take as directed. If vomiting occurs after taking, do not replace dose; notify health care provider. Do not take missed doses; take next scheduled dose and notify health care provider. If any capsules are broken or leaking, do not touch with bare hands; dispose of capsules and wash hands with soap and water.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
May cause drowsiness or sleepiness during and for several days after therapy. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
Advise patient to notify health care provider if fever; chills; sore throat; signs of infection; bleeding gums; bruising; petechiae; blood in urine, stool, or emesis; or signs and symptoms of interstitial lung disease occur. Caution patient to avoid crowds and persons with known infections. Instruct patient to use soft toothbrush and electric razor. Patient should be cautioned not to drink alcoholic beverages or take products containing aspirin or NSAIDs.
May cause diarrhea. Advise patient to notify health care provider if diarrhea with fever, stomach pain, or cramps or for diarrhea that occurs >3 times/day.
Discuss with patient the possibility of hair loss. Explore methods of coping.
Instruct patient not to receive any vaccinations without advice of health care provider.
Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception during therapy and for 6 mo after last dose and to avoid breastfeeding during therapy and for 1 wk after last dose. Advise men with female partners of reproductive potential to use effective contraception during therapy and for 3 mo after last dose. May impair fertility in men and women.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

0078- Novartis Pharmaceuticals Corporation
- 0078-0672- HYCAMTIN
  - 0078-0672-01- 10 CAPSULE in 1 BOTTLE (0078-0672-01)

0078- Novartis Pharmaceuticals Corporation
- 0078-0673- HYCAMTIN
  - 0078-0673-01- 10 CAPSULE in 1 BOTTLE (0078-0673-01)

0078- Novartis Pharmaceuticals Corporation
- 0078-0674- HYCAMTIN
  - 0078-0674-61- 1 VIAL, SINGLE-DOSE in 1 CARTON (0078-0674-61) / 4 mL in 1 VIAL, SINGLE-DOSE

0409- Hospira, Inc.
- 0409-0302- Topotecan
  - 0409-0302-01- 1 VIAL, SINGLE-DOSE in 1 CARTON (0409-0302-01) / 4 mL in 1 VIAL, SINGLE-DOSE

16729- Accord Healthcare, Inc.
- 16729-151- topotecan hydrochloride
  - 16729-151-31- 1 VIAL in 1 PACKAGE (16729-151-31) / 4 mL in 1 VIAL

16729- Accord Healthcare Inc.
- 16729-243- Topotecan
  - 16729-243-31- 1 VIAL, MULTI-DOSE in 1 CARTON (16729-243-31) / 4 mL in 1 VIAL, MULTI-DOSE

45963- Actavis Pharma, Inc.
- 45963-615- Topotecan hydrochloride
  - 45963-615-56- 1 VIAL in 1 CARTON (45963-615-56) / 4 mL in 1 VIAL

61187- ThermoFisher Scientific Cork
- 61187-001-
  - 61187-001-00- 10 kg in 1 DRUM (61187-001-00)

63323- Fresenius Kabi USA, LLC
- 63323-762- Topotecan Hydrochloride
  - 63323-762-10- 1 VIAL in 1 BOX (63323-762-10) / 4 mL in 1 VIAL

63323- Fresenius Kabi USA, LLC
- 63323-762- Topotecan Hydrochloride
  - 63323-762-94- 1 VIAL in 1 BOX (63323-762-94) / 4 mL in 1 VIAL

65129- ScinoPharm Taiwan Ltd.
- 65129-1131-
  - 65129-1131-0- 1 kg in 1 BAG (65129-1131-0)

65129- ScinoPharm Taiwan Ltd.
- 65129-1131-
  - 65129-1131-1- 1 kg in 1 BAG (65129-1131-1)

66758- Sandoz Inc
- 66758-101- HYCAMTIN
  66758-101-11- 10 CAPSULE in 1 BOTTLE (66758-101-11)

66758- Sandoz Inc
- 66758-102- HYCAMTIN
  - 66758-102-11- 10 CAPSULE in 1 BOTTLE (66758-102-11)

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Indications ⬇