Amifostine

Also known as: Ethiofos, Gammaphos

Drug #1604

Amifostine is a phosphorylated sulfhydryl-containing prodrug developed by the military for use in the event of nuclear warfare. Once activated by alkaline phosphatase, it protects bone marrow stem cells as well as other normal cells from the damaging effects of cytotoxic therapy. Unlike other thiols, such as sodium thiosulfate and diethyldithiocarbamate, which protect both normal and tumor cells, it has cytoprotective effects only for normal tissues. Amifostine is used for the prevention of cisplatin-induced nephrotoxicity in ovarian and lung cancer patients.

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Primary Characteristics

Amifostine is also known as Ethiofos, Gammaphos.

It is of Synthetic origin and belongs to Amifostine Momohydrate.

Molecular Weight: 214.2 · pK_a: <2.0 · Solubility in Water: Freely Soluble · Non-proprietary name: Amifostine.

Pharmacokinetics

Distribution: Amifostine has a volume of distribution is 3.5L.

Elimination: it is metabolised via Hepatic dephosphorylation, plasma half-life is Less than 8 minutes, renal excretion is 6% or less.

Indications

Amifostine is primarily indicated in conditions like Ovarian cancer, Prevention of xerostomia, Solid tumor.

Contraindications

Amifostine is contraindicated in conditions like Cardiac arrhythmia, Heart failure, Hypocalcaemia, Hypotension, Cerebrovascular disease, Dehydration.

Dosage

Amifostine's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
200 mg/m.sq	200 mg/m.sq	Every 24h	IV	For prevention of xerotamine infuse over 3 minutes started 15-30 minutes before Radiotherapy.
740 mg/m.sq	740 mg/m.sq	—	IV	To reduce cisplatin induced renal toxicity if doses of cisplatin of less tgan 100 mg/m.sq are used. Give as IV infussion over 15 minutes starting no more than 30 minutes before the antineoplastic therapy.
910 mg/m.sq	910 mg/m.sq	Every 24h	IV	Subsequent doses should be reduced to 740 mg/m.sq in patient unable tolerate the full dose.
Paediatric Dosage (20kg)
740 – 740 mg/m2	—	—	IV	To reduce cisplatin induced renal toxicity, if doses of cisplatin of less than 100mg/m2 are used. Gi
200 – 200 mg/m2/day	—	—	IV-Inf
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown1 interaction

1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Amifostine in overdosage may give rise to further complications which include Hypotension , Hypotension , Hypocalcemia .

Amifostine is known to cause more or less tolerable side effects which are usually transient. These include Chills, Dizziness, Drowsiness, Flushing, Hiccups, Nausea and vomiting, Rashes , Sedation , Sneezing, Somnolence , Stevens Johnson syndrome, Toxic epidermal necrolysis.

Warnings / Precautions

" Tell your doctor and pharmacist if you are allergic to amifostine. Women who are pregnant or breast-feeding should tell their doctors before they begin taking this drug. You should know that the most common side effect of amifostine is a decrease in blood pressure, which may start while the drug is being given and lasts about 6 minutes. Do not breast feed while taking this medication. For both men and women: Do not conceive a child (get pregnant) while taking amifostine. Barrier methods of contraception, such as condoms, are recommendedDiscontinue Antihypertensive drugs 24 hours before starting amifostine.

Available Brands

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Single Ingredient

Inj

500 mg

Drug Classification

1.4.2.11 — Miscellaneous

Manufacturers

Manufacturers of Amifostine in Pakistan:

Pharmedic