Ferriprox (deferiprone)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Deferiprone is a chelating agent with affinity for ferric ions.
Deferiprone chelates iron by binding ferric ions (iron III) and forming a stable complex. The drug has a high binding affinity for iron in a 3:1 ratio (3 deferiprone molecules binding 1 iron atom). Deferiprone has a lower binding affinity for other metals, including aluminum and zinc.
No pharmacodynamic studies have assessed the relationship between deferiprone oral tablet doses and the amount of iron eliminated from the body. Relationships between deferiprone oral solution exposure and pharmacodynamic response (including the time course of the response) are also unknown. Deferiprone does not prolong the QT interval to any clinically relevant extent at the maximum approved recommended dosage.
After administration of a single dose of the oral tablet (2 times a day 1000 mg tablet formulation), peak serum concentrations of deferiprone occur in approximately 2 hours in fasted, healthy subjects. Administration of food has no effect on absorption (peak serum concentration and AUC remain unchanged after a high-fat meal compared to fasted conditions). Consumption of alcohol has been found to result in more rapid release of deferiprone tablet (2 times a day formulation).
The mean elimination half-life of deferiprone oral tablets (2 times a day formulation) is approximately 1.8 hours.
After administration of a single dose of the oral tablet (3 times a day 1000 mg tablet formulation or 500 mg tablet) or oral solution, peak serum concentrations of deferiprone occur in approximately 1-2 hours. Administration of food with these formulations does not result in clinically significant differences in the pharmacokinetics of deferiprone. The elimination half-life of deferiprone oral tablets (3 times a day formulation) or solution is approximately 2 hours.
Deferiprone is extensively metabolized, mainly by UGT1A6. The major metabolite of deferiprone (the 3-O-glucuronide) lacks iron-binding capability. Approximately 75-90% of an orally administered dose of deferiprone is recovered in urine within 24 hours, mainly as metabolite.
No clinically significant differences in the pharmacokinetics of deferiprone were observed based on sex, race/ethnicity, body weight, mild to severe renal impairment, or mild to moderate hepatic impairment; the effects of age, end stage renal disease, or severe hepatic impairment on the pharmacokinetics of deferiprone are unknown.
USES: This medication is used by people with certain blood disorders (such as thalassemia, sickle cell anemia) who have too much iron in the body, caused by repeated blood transfusions. Blood transfusions help people with blood disorders but they also bring extra iron into the body. It is important to get rid of the extra iron because high levels of iron can cause health problems (such as heart failure, liver disease, diabetes, delayed growth in children).
Deferiprone is used if you have trouble taking other traditional iron-removal medications or you continue to have high iron levels after taking other iron-removal medications. Deferiprone belongs to a class of drugs known as iron chelators. It works by attaching to iron which helps your body pass the extra iron out in the urine.
Generic name: deferiprone
Pronunciation: (de-FER-i-prone)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Ferriprox:
- Chronic Iron Overload Due To Repeated Blood Transfusions
Also known as: Secondary Iron Overload From Multiple Blood Transfusions, Transfusion Hemosiderosis, Transfusion-Induced Iron Overload, Transfusional Hemosiderosis, Transfusional Iron Overload.
Dosing
Dosing of deferiprone is based on actual body weight.
Deferiprone is administered orally as tablets or oral solution.
Deferiprone oral tablets are administered orally 2 or 3 times daily depending on the formulation. For the 2-times-daily formulation (1000 mg twice-a-day tablet), administer the first dose in the morning and second dose in the evening, approximately 12 hours apart. For the 3-times-daily formulations (1000 mg three-times-a-day tablet or 500 mg tablet), administer the first dose in the morning, second dose at mid-day, and third dose in the evening.
Deferiprone oral solution is administered 3 times daily with the first dose in the morning, second dose at mid-day, and third dose in the evening. Use the provided measuring cup to measure the prescribed dose. For specific instructions on use of the oral solution, consult the manufacturer's labeling.
Administration with meals may help reduce nausea associated with the drug.
Store deferiprone tablets and oral solution at 20-25oC (excursions permitted to 15-30oC). Store the 3-times-daily 1000-mg tablet formulation in the original bottle, closed tightly to protect from moisture. Store the oral solution in the original bottle and carton to protect from light; after first opening the bottle, discard any unused portion after 35 days.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Deferiprone is metabolized primarily by uridine diphosphate-glucuronosyltransferase (UGT) 1A6. Deferiprone is a chelating agent with an affinity for ferric ions (iron III). Deferiprone binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable at physiological pH.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to the drug or any ingredient in the formulation. Hypersensitivity reactions (Henoch-Schonlein purpura, urticaria, and periorbital edema with skin rash) have been reported.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in >6% of patients with thalassemia receiving deferiprone include nausea, vomiting, abdominal pain, arthralgia, increased ALT concentrations, and neutropenia.
Adverse effects reported in >6% of patients with sickle cell disease or other anemias receiving deferiprone include pyrexia, abdominal pain, bone pain, headache, vomiting, pain in extremity, sickle cell anemia with crisis, back pain, increased ALT concentrations, increased AST concentrations, arthralgia, oropharyngeal pain, nasopharyngitis, decreased neutrophil count, cough, and nausea.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of deferiprone for the treatment of transfusional iron overload due to thalassemia syndromes have been established in pediatric patients. Evidence of efficacy and safety for this indication are derived from clinical trials in adult patients with thalassemia and pediatric patients with sickle cell disease, respectively.
Safety and efficacy of deferiprone for the treatment of transfusional iron overload due to sickle cell disease or other anemias have been established in 86 pediatric patients 3-16 years of age in an adequate and well-controlled study.
A US registry established from December 2011-2019 includes 125 patients 4 to <17 years of age with sickle cell disease who received deferiprone. The adverse reactions (including agranulocytosis) observed in the registry are similar to those reported in recent clinical studies.
Safety and efficacy of deferiprone tablets have not been established in pediatric patients <8 years of age. Safety and efficacy of deferiprone oral solution have not been established in pediatric patients <3 years of age.
There are limited data regarding use of deferiprone in pregnant women to inform a drug-associated risk of major birth defects and miscarriage. However, based on evidence of genotoxicity and findings from animal reproduction studies, deferiprone can cause fetal harm. Animal studies showed embryo-fetal mortality, structural malformations, and alterations to growth after administration of oral deferiprone to pregnant rabbits and rats during the period of organogenesis at doses 49% and 33%, respectively, of the maximum recommended human dose. Pregnant women and females of reproductive potential should be apprised of the potential drug-associated risk to the fetus.
It is not known whether deferiprone is distributed into human milk; the effects of the drug on the breast-fed infant or on the production of milk are also unknown. Animal studies of deferiprone have found potential for tumorigenicity in the breast-fed child. Because of the potential for adverse reactions in breast-fed infants, women should be advised not to breast-feed while receiving deferiprone and for >=2 weeks after the last dose.
The manufacturer makes no specific dosage recommendations for geriatric patients.
Clinical studies of deferiprone did not include sufficient numbers of patients >65 years of age to determine whether or not geriatric subjects respond differently than younger subjects. Other reported clinical experience has not identified differences in responses between elderly and younger patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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