Thursday, May 27, 2010


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Ethyol is dephosphorylated to the active free thiol metabolite form which is able to bind and detoxify reactive metabolites of cisplatin and scavenge reactive oxygen species generated by exposure to either cisplatin or radiation.

Zinecard is converted intracellularly to a ring-opened chelating agent that interferes with iron-mediated free radical generation responsible for anthracycline induced cardiomyopathy.

Leucovorin counteracts the therapeutic and toxic effects of folic acid antagonists (eg, methotrexate) which act by inhibiting dihydrofolate reductase and can enhance the therapeutic and toxic effects of fluoropyrimidines (eg, 5-FU).

Mesnex reacts chemically with the urotoxic ifosfamide metabolites (acrolein and 4-hydroxy-ifosfamide) in the kidney resulting in detoxification.

ETHYOL MedImmune Rx

Amifostine 500mg/vial; pwd for IV infusion after reconstitution.

Indications: To reduce cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer. To reduce xerostomia in patients undergoing post-op radiation therapy for head and neck cancer where the radiation port includes a substantial portion of the parotid glands.

Adults: Pretreat with antiemetics. Reduction of renal toxicity: 910mg/[m.sup.2] by IV infusion over 15 minutes once daily, starting 30 minutes before chemotherapy; monitor BP every 5 minutes during infusion and thereafter, interrupt infusion if systolic BP decreases significantly; if BP returns to normal after 5 minutes, may restart; if full dose cannot be given, then give dose of 740mg/[m.sup.2] for subsequent cycles. Xerostomia: 200mg/[m.sup.2] by IV infusion over 3 minutes once daily, starting 15-30 minutes before standard fraction radiation therapy; monitor BP before and immediately after infusion.

Children: Not recommended.

Precautions: Do not use for other malignancies in which chemotherapy can produce a significant survival benefit or in patients receiving definitive radiotherapy (except in a clinical trial). Not recommended for hypotensive or dehydrated patients. Stop BP medication 24 hours before therapy when using as a chemoprotectant (do not give to patients unable to stop antihypertensives). Permanently discontinue if severe cutaneous reactions or acute allergic reactions occur. Ensure adequate hydration. Keep patient in supine position. Hypocalcemia risk (eg, nephrotic syndrome, multiple doses of Ethyol); monitor serum calcium. Cardiovascular or cerebrovascular disease (ischemic heart disease, arrhythmias, CHF, stroke or TIA). Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions: Caution with drugs that can cause hypotension.

Adverse reactions: Hypotension, hypersensitivity, nausea, vomiting, flushing, chills, fever, dizziness, somnolence; rarely: severe skin reactions, reversible loss of consciousness, hypocalcemia, cardiac arrest, renal failure, arrythmias, hypertension, seizures, syncope. How supplied: Single-use vials-3

FUSILEV Spectrum Rx

Folate analogue. Levoleucovorin (as calcium pentahydrate) 50mg/vial; pwd for IV inj after reconstitution; contains mannitol 50mg/vial.

Indications: In osteosarcoma, to reduce toxicity of high-dose methotrexate (MTX) therapy. To reduce toxicity and counteract effects of impaired MTX elimination and of inadvertent overdose of folic acid antagonists.

Adults and Children:

Precautions: Not for treating pernicious anemia and megaloblastic anemia. Monitor serum creatinine and MTX levels every 24hrs. Delayed early MTX elimination may cause reversible renal failure; provide hydration, alkalinize urine with sodium bicarbonate, closely monitor fluid and electrolytes until serum MTX

Interactions: Potentiates 5-fluorouracil toxicity. Antagonizes TMP/SMZ. Antagonizes anticonvulsants (eg, phenobarbital, primidone, phenytoin). May be affected by drugs that affect MTX elimination.

Adverse reactions: Stomatitis, vomiting, nausea.

How supplied: Single-use vial--1

Leucovorin Teva Rx

Folic acid derivative. Leucovorin calcium 100mg/vial, 350mg/vial; lyophilized pwd for IV or IM inj after reconstitution; preservative-free.

Indications: Rescue treatment after high-dose methotrexate therapy in osteosarcoma.

Adults: Max IV infusion rate: 160mg/min. Based on methotrexate dose. Normal methotrexate elimination: 15mg IM or IV every 6 hours for 10 doses starting 24 hours after the beginning of the methotrexate infusion. Delayed late or delayed early methotrexate elimination, and/or evidence of acute renal injury, impaired methotrexate elimination or inadvertent overdosage: see literature.

Children: See literature.

Contraindications: Pernicious anemia and other megaloblastic anemias due to Vit. [B.sub.12] deficiency.

Precautions: Do not administer intrathecally. Monitor serum methotrexate concentration. CNS metastases. Monitor CBCs with differential, platelets, electrolytes, liver function tests prior to each treatment, then periodically. Elderly. Debilitated. Pregnancy (Cat.C). Nursing mothers.

Interactions: Potentiates toxicity of 5-fluorouracil; use lower 5-fluorouracil dose. May antagonize phenobarbital, phenytoin, and primidone. Caution with trimethoprim sulfamethoxazole.

Adverse reactions: Leukopenia, thrombocytopenia, infection, GI upset, stomatitis, constipation, lethargy, malaise, fatigue, alopecia, dermatitis, anorexia; seizures, syncope.

How supplied: Single-use vials--1

MESNEX TABLETS Bristol-Myers Squibb Rx

Cytoprotective agent. Mesna 400mg; tabs.


Mesna 100mg/mL; soln for IV inj after dilution; contains benzyl alcohol.

Indications: Prophylactic agent in reducing the incidence of ifosfamide-induced hemorrhagic cystitis.

Adults: See literature. IV Schedule: Give as IV bolus injection in a dosage equal to 20% of the ifosfamide dose at the time of ifosfamide administration and 4 and 8 hours after each dose of ifosfamide; total daily dose is 60[degrees]% the ifosfamide dose. IV and oral dosing: Give as IV bolus injection in a dosage equal to 20% of the ifosfamide dose at the time of ifosfamide administration, followed by the tablets given orally in a dosage equal to 40% of the ifosfamide dose 2 and 6 hours after each dose of ifosfamide; total daily dose is 100% of the ifosfamide dose. Repeat schedule on each day ifosfamide is given. If vomiting occurs within 2hrs of oral mesna, repeat dose or give IV mesna.

Children: Not recommended.

Contraindications: Hypersensitivity to thiol compounds.

Precautions: Monitor morning specimen of urine for the presence of hematuria each day prior to ifosfamide therapy; consider dose reduction or discontinue if hematuria occurs. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.

Adverse reactions: GI upset, fever, anorexia, flatulence, constipation, rhinitis, rigors, back pain, rash, conjunctivitis, arthralgia, headache, inj site reactions, flushing, dizziness, pharyngitis, hyperaesthesia, flu-like symptoms, coughing; hypersensitivity reactions.

Note: Patients taking mesna should drink at least a quart of liquid a day.

How supplied: Tabs--10 Multidose vials-1, 10

TOTECT TopoTarget Rx

Detoxifying agent. Dexrazoxane 500mg; per vial; pwd for IV infusion after reconstitution and dilution; preservative-free.

Indications: To treat extravasation resulting from IV anthracycline chemotherapy.

Adults: Give once daily for 3 consecutive days by IV infusion over 1-2 hours. Initiate 1st dose as soon as possible and within 1st 6 hours after extravasation. Days 1 and 2: 1000mg/[m.sup.2]; max 2000mg. Day 3: 500mg/[m.sup.2]; max 1000mg. Renal impairment (CrCl

Children: Not recommended.

Precautions: Renal or hepatic impairment (monitor liver enzymes). Monitor for myelosuppression; obtain blood counts periodically. Elderly. Labor & delivery. Pregnancy (Cat.D); avoid use. Nursing mothers: not recommended.

Interactions: Avoid dimethylsulfoxide (DMSO). Caution with concurrent cytotoxic chemotherapy (additive cytotoxicity).

Adverse reactions: Inj site reactions, GI upset, stomatitis, leukopenia, neutropenia, thrombocytopenia, elevated liver enzymes, pyrexia, infections.

How supplied: Kit--10 single-use vials (w. diluent)


Chelating agent. Dexrazoxane 250mg, 500mg; per vial; pwd for IV infusion after reconstitution and dilution.

Indications: To reduce the incidence and severity of cardiomyopathy associated with doxorubicin administration in women with metastatic breast cancer who have received a cumulative doxorubicin dose of 300mg/[m.sup.2] and will continue to receive doxorubicin therapy to maintain tumor control.

Adults: Give by slow IV push or rapid drip IV infusion. Doxorubicin should be administered within 30 minutes after starting Zinecard infusion. Administer in 10:1 ratio (eg, 500mg/[m.sup.2] Zinecard: 50mg/[m.sup.2] doxorubicin). Renal impairment (CrCl

Children: Not recommended.

Contraindications: Chemotherapy regimens that do not contain an anthracycline.

Precautions: Not recommended for use with initiation of doxorubicin. Renal or hepatic impairment. Monitor cardiac function and for myelosuppression; obtain CBCs frequently. Pregnancy (Cat.C). Nursing mothers: not recommended.

Adverse reactions: Inj site pain, myelosuppression, possible secondary malignancies (see literature).

How supplied: Single-use vial--1 (w. diluent)

Source Citation
"12L Cytoprotective agents." MPR [Hematology and Oncology Edition] Summer 2010: 206+. Academic OneFile. Web. 27 May 2010.
Document URL

Gale Document Number:A226475392

Disclaimer:This information is not a tool for self-diagnosis or a substitute for professional care.

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