Drug information of Deferiprone

Mechanism of effect

Chelates iron by binding ferric ions and forming a stable complex. Has a high binding affinity for iron in a 3:1 ratio (3 deferiprone molecules binding 1 iron atom) and a lower binding affinity for other metals, including copper, aluminum, and zinc.

Pharmacodynamic

 Iron-chelating agent with affinity for ferric ion (iron III); binds to ferric ion and forms a 3:1 (deferiprone:iron) complex which is excreted in the urine. Has a lower affinity for other metals such as copper, aluminum, and zinc

Pharmacokinetics

Absorption: Rapidly absorbed from upper GI within 5-10 minutes of PO administration, with peak plasma concentration 20 mcg/ml that usually attained within 1 hour after a single dose in fasting state and up to 2 hours after a single dose in fed state.

AUC: 53 mcg hr/mL. Vd: 1.6 L/kg (in patients with thalassemia); 1 L/kg (in healthy subjects).

 Plasma Protein Binding is <10%. Extensively metabolized, primarily by UGT1A6 to the 3-O-glucuronide (lacks iron binding capability).

 Excreted in urine (75–90% within 24 hours following oral administration) mainly as metabolite. Half-life is 1.9 hours.

Dosage

Note: Round dose to the nearest 250 mg (or ¹/₂ tablet) or 2.5 mL (oral solution). If serum ferritin falls consistently below 500 mcg/L, consider temporary treatment interruption.

Transfusional iron overload: Oral: Initial: 25 mg/kg 3 times/day (75 mg/kg/day); individualize dose based on response and therapeutic goal; maximum dose: 33 mg/kg 3 times/day (99 mg/kg/day).

Drug contraindications

Hypersensitivity to this drug or components

Side effects

nausea , vomiting , Increased ALT , Abdominal pain , Abdominal discomfort

Interactions

Dacarbazine , Allopurinol , Anti-thymocyte , Everolimus , Dapsone , Penicillamine , Diclofenac , Phenylbutazone , Chloroquine , Chloramphenicol , Colchicine , Ganciclovir , probenecid , Linezolid , Adalimumab , Rituximab , valganciclovir , Levamisole , Mycophenolate mofetil , Methotrexate , Hydroxychloroquine , Sucralfate , Lomustine , Melphalan , Carbamazepine , Chlorambucil , Zidovudine , Pentamidine , Aldesleukin , Lenalidomide , Teniposide , thiotepa , Idelalisib , Iron , Clofarabine , Pemetrexed , Tositumomab , Ibritumomab tiuxetan , Acalabrutinib , Bendamustine , Aflibercept , Axicabtagene ciloleucel , Pazopanib , Pralatrexate , trabectedine , dinutuximab , Duvelisib , Floxuridine , Ferrous Gluconate , upadacitinib , Nelarabine , Edetate Calcium Disodium , Alemtuzumab , Ofatumumab , Carmustine , Temsirolimus , Rucaparib , Abemaciclib , Blinatumomab , Romidepsin , Ruxolitinib , Biolectra Magnesium , Dasatinib , stiripentol , Famtrastuzumab

Alerts

• Agranulocytosis//Neutropenia :May cause agranulocytosis, which could lead to serious infections (some fatal). Agranulocytosis may be preceded by neutropenia; monitor absolute neutrophil count (ANC) prior to treatment initiation and weekly during therapy. If infection develops, interrupt treatment and monitor ANC more frequently. Patients should promptly report any symptoms which may indicate infection.
• Hepatotoxicity : Elevations in ALT values have been observed; monitor ALT and consider treatment interruption for persistent elevations.
• Hypersensitivity : Hypersensitivity reactions have been reported [immunoglobulin A vasculitis], urticaria, and periorbital edema with skin rash).
• Zinc deficiency : Lower plasma zinc concentrations have been observed; monitor zinc levels and supplement if necessary.
• Monitor serum ferritin concentration every 2-3 months to assess the effects on body iron stores

Points of recommendation

Do not use deferiprone if you are pregnant. It could harm the unborn baby.

Stop using this medicine and call your doctor right away if you have signs of infection such as: fever, chills, body aches, flu symptoms, or sores in your mouth and throat.

You should not use deferiprone if you are allergic to it.

To make sure deferiprone is safe for you, tell your doctor if you have:

• liver disease; or
• a weak immune system.

Deferiprone is not approved for use by anyone younger than 18 years old.

 

It is not known whether deferiprone passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are taking deferiprone.

Deferiprone is usually taken 3 times per day. Take the first daily dose each morning, the second dose at mid-day, and the third dose in the evening.

Take with food if deferiprone upsets your stomach. You may also take the medicine without food.

Tell your doctor if you have any changes in weight. Deferiprone doses are based on weight, and any changes may affect the dose.

Deferiprone may cause your urine to turn a reddish-brown color. This side effect is usually not harmful. Call your doctor if you also have upper stomach pain, clay-colored stools, or jaundice (yellowing of your skin or the whites of your eyes).

Deferiprone can lower blood cells that help your body fight infections. Your blood will need to be tested weekly while you are taking deferiprone . Your treatments may be delayed based on the results of these tests. Visit your doctor regularly.

Store at room temperature, away from moisture and heat.

Administer after at least a 4-hour interval with medications or supplements containing polyvalent cations (iron, aluminum, zinc).

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Pregnancy level

D

Related drugs

Deferasirox , Deferoxamine , Succimer