Details

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Amifostine 375mg, 500mg injection is a cytoprotective agent used with chemotherapy and radiation therapy.

It is an organic thiophosphate prodrug that forms active thiol metabolite after dephosphorylation in tissue, which protects normal cells from cytotoxic metabolites.

Mechanism of action: it gets dephosphorylated by alkaline phosphatase enzyme inside tissues to active thiol metabolite. This thiol metabolite has more affinity for normal tissues because of high vascularity, higher alkaline phosphatase activity and higher pH. This metabolite binds to toxic metabolites of cytotoxic agents and radiation therapy resulting in protection from cytotoxicity. It also reduces the levels of reactive oxygen species produced during radiation therapy.

It is available as Ethyol in both International and Indian markets.

Uses

• Amifostine 375mg, 500mg injection is used to reduce the cumulative renal toxicity due to repeated administration of cisplatin in ovarian cancer and non-small cell lung cancer.
• It is also used to decrease neutropenia-related fever and infection caused by DNA-binding cytotoxic agents like mitomycin-C, cyclophosphamide and platinum-containing drugs .
• Ethyol is also used to decrease moderate to severe dry mouth (xerostomia) caused by radiation therapy of head and neck cancer involving salivary glands.

 

Dosage

• Amifostine 375mg, 500mg injection comes as a single use vial containing sterile lyophilized powder for reconstitution.
• Ethyol is given intravenously by healthcare professionals only, 15 minutes before the chemotherapy and 3 minutes before the radiation therapy.
• Final doses are determined by the doctor on the basis of pre existing medical condition, ongoing medications, age, weight and any allergy.
• Doses and infusion rate are also modified according to dose related side effects.
• It is stored at room temperature.

 

Side effects

• Headache
• Chills
• Fever
• Flushing
• Nausea and vomiting
• Hypocalcemia
• Hiccups
• Sneezing
• Hypotension
• Allergic reactions- skin rashes and urticaria.
• Dizziness
• Rarely seizures

 

Precautions

• Amifostine 375mg, 500mg injection is contraindicated in case of allergy to amifostine.
• Close monitoring is required for signs and symptoms of hypotension,heart disease and kidney dysfunction.
• Blood tests must be done to monitor serum calcium levels.
• Ethyol interacts with anti hypertensive drugs or drugs that cause hypotension.
• Proper hydration and antiemetic treatment is required prior to infusion.
• Proper setup is required to treat hypotension after infusion.
• Always tell the doctor about pre-existing medical conditions, ongoing medications, any history of allergic reaction, pregnancy, future plan of pregnancy and pregnancy.
• It must be used in pregnancy only if benefits are more than the risks.

It is not recommended in breastfeeding mothers.