Etoposide
Pronouncation: (EH-toe-POE-side)Class: Podophyllotoxin derivative
Trade Names:
VePesid
- Concentrate for injection 20 mg/mL
- Liquid-filled capsules for oral use 50 mg
Trade Names:
Toposar
- Concentrate for injection 20 mg/mL
- Liquid-filled capsules for oral use 50 mg
Trade Names:
Etopophos
- Powder for injection 100 mg vial
Pharmacology
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Feedback for Etoposide
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Etoposide's main effect appears to be at the G 2 portion of the cell cycle. At high concentrations (10 mcg/mL or more), lysis of cells entering mitosis is seen; at low concentrations (0.3 to 10 mcg/mL), cells are inhibited from entering prophase. Predominant macromolecular effect appears to be DNA synthesis inhibition.
Pharmacokinetics
Absorption
Bioavailability is approximately 50% (oral).
Distribution
Distribution t ½ is approximately 1.5 h. Vd is approximately 18 to 29 L (at steady state). 97% is protein bound.
Metabolism
Etoposide phosphate is rapidly dephosphonylate to etoposide in the plasma. Etoposide is extensively metabolized in the liver (including CYP3A4).
Elimination
The t ½ is approximately 4 to 11ߙh. Cl is 33 to 48ߙmL/min. 42 to 67% is excreted in the urine and 0 to 16% is excreted in the feces. Less than 50% is excreted in the urine and less than 6% is excreted in bile as etoposide.
Special Populations
Renal Function ImpairmentTotal body clearance is reduced, AUC is increased, and Vd is lower.
Indications and Usage
Refractory testicular tumors, small-cell lung cancer.
Unlabeled Uses
Bladder carcinoma, lymphomas, leukemias, Ewing sarcoma, Kaposi sarcoma, brain tumors, gestational trophoblastic tumors, ovarian germ cell tumors, refractory breast tumors, rhabdomyosarcomas, Wilms tumor, bone marrow transplantation.
Contraindications
Standard considerations.
Dosage and Administration
Testicular CancerAdults
IV 50 to 100ߙmg/m 2 /day for 3 to 5ߙdays every 3 to 4ߙwk.
Small-Cell Lung CancerAdults
IV 35 to 50 mg/m 2 /day IV for 4 to 5ߙdays every 3 to 4 wk. PO 2 times the IV dose, rounded to nearest 50 mg, given orally for 21ߙdays. Alternately, 50ߙmg/m 2 /day orally for 21ߙdays has been given. Repeat regimen after a 1- to 2-wk rest period. Oral bioavailability of the capsules is erratic, averaging 50% (range, 25% to 75%).
Dosage AdjustmentAdults
Hold etoposide if the platelet count is less than 50,000/mm 3 or the absolute neutrophil count is less than 500/mm 3 .
Adjustment in Hepatic InsufficiencyAdults
Dosage reduction may be warranted; specific guidelines are not available.
Adjustment in Renal InsufficiencyAdults
For patients with Ccr of 16ߙto 50ߙmL/min, give 75% of the usual dose. Consider further dose reduction for those with Ccr 15ߙmL/min or less.
General Advice
IV- Dilute prior to use with 5% Dextrose or 0.9% Sodium Chloride to final concentration of 0.2ߙor 0.4 mg/mL. Concentrations less than 0.4ߙmg/mL may precipitate.
- Infuse over 30 to 60 min. Do not give by rapid IV injection because of the risk of hypotension.
- Etoposide solution for injection can be mixed to a final concentration 0.4ߙmg/mL or less with orange juice, apple juice, or lemonade for oral administration.
- Stable for 3 h at room temperature.
Storage/Stability
VialsStore at room temperature. At room temperature, 0.2ߙmg/mL solution is stable for 96 h, 0.4 mg/mL solution is stable for 48ߙh.
CapsulesRefrigerate; can be stored at room temperature for 3 mo.
Drug Interactions
WarfarinEtoposide may increase the hypoprothrombinemic effects of warfarin.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Hypotension.
Dermatologic
Alopecia; radiation recall.
GI
Nausea and vomiting; abdominal pain; anorexia; diarrhea; mucositis with high doses or prior radiation to head and neck; elevation of LFTs; hepatocellular necrosis.
Genitourinary
Amenorrhea.
Hematologic
Bone marrow suppression, granulocyte nadir at 7ߙto 14ߙdays, platelet nadir at 9ߙto 16ߙdays.
Hypersensitivity
Acute anaphylactoid reaction.
Miscellaneous
Increased risk of acute nonlymphocytic leukemia.
Precautions
WarningsMyelosuppressionSevere cases with resulting infection or bleeding may occur. Dose-limiting bone marrow suppression is the most significant toxicity. |
MonitorBPMonitor BP before and after infusion. |
Pregnancy
Category D .
Lactation
Undetermined.
Children
Safety and efficacy in children not established.
Anaphylaxis
Anaphylaxis manifested by chills, fever, tachycardia, bronchospasm, dyspnea, facial flushing, hypertension, or hypotension may occur.
Hypotension
Administer by slow IV infusion because hypotension may occur with rapid IV injection.
Extravasation
Can cause local irritation or phlebitis. Refer to your institution-specific protocol.
Overdosage
Symptoms
Bone marrow suppression.
Patient Information
- Contraceptive measures are recommended during treatment.
- Notify health care provider of any of the following: fever; chills; rapid heartbeat; difficult breathing.
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More Etoposide resources:
Etoposide - Includes detailed dosage instructions.
Ovarian Cancer, Cancer, Hodgkin's Lymphoma, Testicular Cancer, Small Cell Lung Cancer
