Deferiprone

Uses

Iron overload in patients with thalassaemia.

Deferiprone is also used to associated treatment for these conditions: Transfusional Iron Overload

How Deferiprone works

Deferiprone is an iron chelator that binds to ferric ions (iron III) and forms a 3:1 (deferiprone:iron) stable complex and is then eliminated in the urine. Deferiprone is more selective for iron in which other metals such as zinc, copper, and aluminum have a lower affinity for deferiprone.

Dosage

Deferiprone dosage

Adult: 25 mg/kg tid. Doses >100 mg/kg daily are not recommended.

Child: >6 yr: 25 mg/kg tid.

May be taken with or without food.

Side Effects

Musculoskeletal and joint pain; GI disturbances; red-brown discoloration of urine; transient liver enzyme abnormalities; zinc deficiency; neutropenia and agranulocytosis.

Toxicity

Agranulocytosis and neutropenia may occur, which can lead to fatal infections. Hepatoxicity is also possible. Most common side effects that lead to discontinuation of therapy were the gastrointestinal adverse effects (diarrhea, ulcer, nausea, gastrointestinal disturbances)

Precaution

Hepatic and renal impairment. Neutropenia, monitor neutrophil count wkly and discontinue treatment if neutropenia develops. Limited experience in children 6-10 yr.

Interaction

Avoid using deferiprone with aluminium-containing antacids as it can chelates trivalent metal ions.

Food Interaction

• Take with or without food. Food does not affect absorption.

Deferiprone multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Deferiprone has the potential to bind polyvalent cations such as aluminum, iron and zinc, which may reduce its effectiveness.

However, concurrent use with foods, mineral supplements, or antacids that contain polyvalent cations has not been studied.

A minimum 4-hour interval is recommended between the administration of deferiprone and mineral supplements or oral medications that contain antacids (e.g., didanosine buffered tablets or pediatric oral solution) or other polyvalent cations.

Deferiprone Drug Interaction

Major: tocilizumab, everolimusUnknown: aspirin, nifedipine, epinephrine, hydroxyzine, deutetrabenazine, moxifloxacin, rasagiline, sulfamethoxazole / trimethoprim, amisulpride, brolucizumab, deferoxamine, epoetin alfa, sodium ferric gluconate complex, oprelvekin, filgrastim, nivolumab, valproic acid, iron sucrose

Deferiprone Disease Interaction

Major: agranulocytosis/neutropeniaModerate: hepatic impairment

Volume of Distribution

In healthy patients, the volume of distribution is 1L/kg, and in thalassemia patients, the volume of distribution is 1.6L/kg.

Elimination Route

Deferiprone is absorbed in the upper gastrointestinal tract. Absorption is rapid with maximum plasma concentrations occurring after 1 hour in the fasted state and after 2 hours in the fed state.

Half Life

The half-life is 1.9 hours.

Elimination Route

Within 5-6 hours of administration, more than 90% of deferiprone is eliminated from the plasma. 75 to 90% of deferiprone is excreted in the urine as the metabolite.

Pregnancy & Breastfeeding use

Pregnancy Category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Contraindication

Agranulocytosis, pregnancy and lactation.

Storage Condition

Store below 30° C.

Innovators Monograph

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