Deferiprone

Deferiprone is a prescription medication used to treat people with thalassemia syndromes who have iron overload from blood transfusions when current iron removal (chelation) therapy does not work well enough. 

• Deferiprone is available under the following different brand names: Ferriprox

Common side effects of Deferiprone include:

• nausea,
• vomiting,
• stomach/abdominal pain,
• diarrhea,
• joint pain,
• back pain,
• increased appetite,
• headache,
• reddish-brown urine discoloration (this is not harmful),
• a decrease in the number of white blood cells (neutropenia), and
• an increase in the level of a liver enzyme that may be indicative of tissue or liver damage at unsafe amounts

Serious side effects of Deferiprone include:

• reddish-purple spots or rash, especially on the lower half of the body; swollen and sore joints; stomach pain, or bloody urine
• hives
• swelling around the eyes
• fast or pounding heartbeat
• dizziness
• light-headedness
• fainting
• seizures

Rare side effects of Deferiprone include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms such as fast, irregular, or pounding heartbeats; fluttering in your chest; shortness of breath; sudden dizziness, lightheartedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

  Adult and pediatric dosage

Tablet

• 500 mg
• 1000 mg tablets
  • Note: Two different formulations with different dosage frequencies
  • 1000 mg (twice a day); imprinted with FPX DR on one side and APO 1000 on the other
  • 1000 mg (three times a day); imprinted with APO 1000 on one side and plain on the other

Oral solution

• 80 mg/mL (40 g/400 mL; 20 g/250 mL)
• 100 mg/mL (50 g/500 mL)

Transfusional Iron Overload

• Adult dosage
• 500 mg tablet
  • Initial: 25 mg/kg (actual body weight) orally three times a day
  • Maximum dose: 99 mg/kg/day
  • Round dose to nearest 250 mg (half-tablet)

Pediatric dosage

• Children below 3 years: Safety and efficacy not established
• 500 mg tablet (children above 8 years)
  • Initial: 25 mg/kg (actual body weight) orally three times a day
  • Maximum dose: 99 mg/kg/day
  • Round dose to nearest 250 mg (half-tablet)

1000 mg tablets

Adult dosage

• 75 mg/kg/day (actual body weight) orally initially; maximum dose is 99 mg/kg/day
• Divide the total daily dose (e.g., two times a day or three times a day) based on a particular 1000-mg tablet
• Round dose to nearest 500 mg (half-tablet)

Pediatric dosage

• 1000 mg tablets (children above 8 years)
  • 75 mg/kg/day (actual body weight) orally initially; maximum dose is 99 mg/kg/day
  • Divide the total daily dose (.g, two times a day or three times a day) based on a  particular 1000-mg tablet
  • Round dose to nearest 500 mg (half-tablet)

Oral solution

• Adult dosage
  • Initial: 25 mg/kg/day (actual body weight) orally three times a day
  • Maximum dose: 99 mg/kg/day
  • Round to nearest 2.5 mL (i.e., 200 mg for 80 mg/mL; 250 mg for 100 mg/mL)

Pediatric dosage

• Oral solution (aged children above 3 years)
  • Initial: 25 mg/kg/day (actual body weight) orally three times a day
  • Maximum dose: 99 mg/kg/day
  • Round to nearest 2.5 mL (i.e., 200 mg for 80 mg/mL; 250 mg for 100 mg/mL)

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

• Deferiprone has severe interactions with no other drugs.
• Deferiprone has serious interactions with at least 81 other drugs.
• Deferiprone has moderate interactions with at least 42 other drugs.
• Deferiprone has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity of Henoch-SchÖnlein purpura, urticaria, and periorbital edema with skin rash have been reported 

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Deferiprone?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Deferiprone?”

Cautions

• May cause fetal harm; women should be advised of the potential hazard to the fetus and to avoid pregnancy while on this drug
• Monitor serum ferritin concentration every 2-3 months to assess the effects on body iron stores
• Thorough QT interval studies have not been conducted
• In clinical studies, subjects treated developed increased ALT values; monitor
• Decreased plasma zinc concentrations; monitor plasma zinc, and supplement in the event of a deficiency

Agranulocytosis and neutropenia

• Fatal agranulocytosis can occur
• It may also cause neutropenia, which may foreshadow agranulocytosis
• Obtain absolute neutrophil count (ANC) before starting therapy and monitor weekly during therapy
• Reduction in frequency of ANC monitoring should be considered on an individual patient basis, according to the health care provider’s assessment of the patient’s understanding of risk minimization measures required during therapy
• If neutropenia develops (ANC below 1.5 x 109/L) or if an infection develops: Interrupt therapy and closely monitor ANC
• For agranulocytosis (ANC below 0.5 x 109/L): Consider hospitalization and other management as clinically appropriate; do not resume if agranulocytosis develops unless potential benefits outweigh potential risks; do not rechallenge if neutropenia develops unless potential benefits outweigh potential risks
• For neutropenia (ANC above 0.5 to less than 1.5 x 109/L): Instruct patients to immediately discontinue treatment and all other medications with a potential to cause neutropenia; obtain a complete blood cell (CBC) count, including a white blood cell (WBC) count corrected for the presence of nucleated red blood cells, an ANC, and a platelet count daily until recovery (ANC above1.5 x 109/L)
• Advise patients to immediately interrupt therapy and report to their physician if they experience any symptoms indicative of infection
• The mechanism of drug-associated agranulocytosis is unknown
• Agranulocytosis and neutropenia usually resolve upon discontinuation, but there have been reports of agranulocytosis leading to death

Drug interactions overview

• Avoid coadministration with other drugs known to cause neutropenia or agranulocytosis; however, if this is not possible, closely monitor the absolute neutrophil count
• Allow at least a 4-hour interval between deferiprone and mineral supplements, and antacids that contain polyvalent cations (e.g., iron, aluminum, zinc) to avoid binding and malabsorption of supplements
• Avoid the use of UGT1A6 inhibitors (e.g., diclofenac, probenecid, or silymarin [milk thistle]) with deferiprone

Pregnancy and Lactation

• Limited available data on use in pregnant women are insufficient to inform a drug-associated risk of major birth defects and miscarriage
• Verify the pregnancy status of females of reproductive potential before initiating therapy
• Contraception
• Females: Advise females of reproductive potential to avoid pregnancy during treatment and 6 months of contraception is recommended after cessation of therapy; advise females to immediately report pregnancy
• Males: Advise males with female sexual partners of reproductive potential to use effective contraception during treatment and 3 months of contraception is recommended after cessation of therapy

Lactation

• There is no information regarding the presence of deferiprone in human milk, the effects on the breastfed child, or the effects on milk production
• Because of the potential for serious adverse reactions, including the potential for tumorigenicity shown for deferiprone in animal studies, advise not to breastfeed during treatment and for 2 weeks after the last dose