Ethyol (Lyophilisate) Instructions for Use

ATC Code

V03AF05 (Amifostine)

Active Substance

Amifostine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Drug for the prevention of toxic side effects of alkylating anticancer agents

Pharmacotherapeutic Group

Chelating agent

Pharmacological Action

Cytoprotective agent. It is a thiophosphate and exerts a protective effect on cells not involved in tumor growth against the cytotoxic effects of DNA-binding chemotherapeutic agents (classical alkylating agents such as cyclophosphamide, as well as mitomycin C, platinum drugs).

The use of amifostine reduces the likelihood of hematotoxic, nephrotoxic, neurotoxic, and ototoxic reactions observed during chemotherapy.

Pharmacokinetics

After intravenous administration, Amifostine is rapidly cleared from plasma and dephosphorylated under the action of alkaline phosphatase to form an active metabolite, an unbound thiol compound.

After a 15-minute infusion, the T_1/2 of amifostine is less than 10 minutes. Urinary excretion is 6% or less.

Indications

Prevention of hematotoxic effects caused by DNA-binding chemotherapeutic agents; prevention of nephrotoxic, neurotoxic, and ototoxic effects associated with baseline therapy with platinum drugs.

ICD codes

Dosage Regimen

Administer Ethyol intravenously as a 15-minute infusion once daily.

Calculate the dose based on patient body surface area. The standard dose for reducing cumulative renal toxicity associated with repeated administration of cisplatin is 910 mg/m².

Initiate the infusion 30 minutes before starting cisplatin chemotherapy.

For reducing the incidence of moderate to severe xerostomia in patients undergoing postoperative radiation treatment for head and neck cancer, where the radiation port includes a substantial portion of the parotid glands, the dose is 200 mg/m² administered once daily as a 3-minute infusion.

Initiate the infusion 15-30 minutes before each fraction of radiation therapy.

Ensure adequate hydration prior to administration. Monitor blood pressure before the infusion, and at least every 5 minutes during the infusion.

Interrupt the infusion if a significant decrease in systolic blood pressure occurs. Do not exceed a single dose of 910 mg/m².

Reconstitute the lyophilisate strictly according to manufacturer instructions using 9.7 mL of Sodium Chloride 0.9% Injection. Further dilute the reconstituted solution in Sodium Chloride 0.9% Injection to a final concentration ranging from 5 mg/mL to 40 mg/mL.

Administer antiemetic medication, including a dexamethasone dose and a serotonin 5HT3 receptor antagonist, before the amifostine infusion.

Adverse Reactions

From the cardiovascular system: transient decrease in systolic BP, facial flushing, feeling of warmth, dizziness; rarely – increase in diastolic BP; very rarely – short-term loss of consciousness (as a consequence of a pronounced decrease in systolic BP).

From the digestive system: nausea, vomiting, hiccups.

Allergic reactions: skin rash, eosinophilia, chills.

Other: decrease in serum calcium concentration, drowsiness, sneezing.

Contraindications

Arterial hypotension, dehydration, pregnancy, lactation, hypersensitivity to aminothiol compounds and mannitol.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

It is not recommended to use Amifostine in severe liver function disorders.

Use in Renal Impairment

It is not recommended to use Amifostine in severe renal function disorders.

Pediatric Use

It is not recommended to use Amifostine in children, as experience in these patient groups is insufficient.

Geriatric Use

It is not recommended to use Amifostine in patients over 70 years of age, as experience in these patient groups is insufficient.

Special Precautions

It is recommended to take antiemetic drugs immediately before or together with the administration of amifostine, especially when using chemotherapeutic agents with a pronounced emetogenic effect.

In patients at risk of developing hypocalcemia (e.g., with nephrotic syndrome), serum calcium levels should be monitored.

Antihypertensive therapy should be discontinued 24 hours before the administration of amifostine.

When using amifostine with chemotherapeutic agents that have a pronounced emetogenic effect, the patient’s fluid balance should be carefully monitored.

Amifostine can be used to prevent side effects of radiation therapy.

It is not recommended to use Amifostine in severe liver and/or kidney dysfunction, in children and patients over 70 years of age, as experience in these patient groups is insufficient.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.