Tafenoquine

Tafenoquine is a prescription medication used for the prevention of malaria.

• Tafenoquine is available under the following different brand names: Krintafel, Arakoda

Common side effects of Tafenoquine include:

• Nausea,
• Vomiting,
• Abnormal hemoglobin tests,
• Dizziness, and
• Headache

Serious side effects of Tafenoquine include:

• Hives,
• Difficulty breathing,
• Swelling of the face, lips, tongue, or throat,
• Dizziness,
• Pale or yellowed skin,
• Dark-colored urine,
• Darkening of the mouth, lips, or fingernails,
• Fast heartbeats,
• Shortness of breath,
• Headache,
• Lightheadedness,
• Confusion,
• Tiredness,
• Anxiety,
• Strange dreams, and
• Trouble sleeping

Rare side effects of Tafenoquine 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 include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because 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 dosage

Tablet

• 100 mg (Arakoda)
• 150 mg (Krintafel)

Malaria

Adult dosage

• Prevention of relapse following treatment of acute P vivax infection

Krintafel only

• 300 mg orally as a single dose
• Coadminister tafenoquine on the first or second day of chloroquine therapy for acute P vivax malaria
• Prophylaxis when traveling to a malarious area.

Arakoda only

• Loading regimen
  • For each of the 3 days before travel to a malarious area: 200 mg orally once a day for 3 days
• Maintenance regimen
  • While in the malarious area: 200 mg orally once weekly starting 7 days after the last loading regimen dose.
• Terminal prophylaxis regimen
  • In the week following exit from the malarious area: 200 mg orally as a single, one-time dose, taken 7 days after the last maintenance dose.

Pediatric dosage

• Prevention of relapse following treatment of acute P vivax infection
• Below 16 years: Safety and efficacy not established.
• Above 16 years
  • Krintafel only
    • 300 mg orally as a single dose
    • Coadminister tafenoquine on the first or second day of chloroquine therapy for acute P vivax malaria

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.

• Tafenoquine has severe interactions with no other drugs.
• Tafenoquine has serious interactions with the following drugs:
  • amantadine
  • amiloride
  • cimetidine
  • cisplatin
  • dapsone topical
  • dofetilide
  • dopamine
  • famotidine
  • lamivudine
  • memantine
  • metformin
  • pindolol
  • pramipexole
  • procainamide
  • trimethoprim
  • varenicline
• Tafenoquine has moderate interactions with the following drug:
  • bupivacaine implant
• Tafenoquine 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 healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Krintafel or Arakoda
  • G6PD deficiency or unknown G6PD status
  • Breastfeeding by a lactating female when the infant is G6PD deficient or if G6PD status is unknown.
  • Hypersensitivity reactions to tafenoquine, other 8-aminoquinolines, or any component of tafenoquine
• Arakoda
  • History of psychotic disorders or current psychotic symptoms (ie, hallucinations, delusions, and/or grossly disorganized behavior)

Effects of drug abuse

• None

Short-Term Effects

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

Long-Term Effects

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

Cautions

• Owing to the risk of hemolytic anemia in patients with G6PD deficiency, G6PD testing must be performed before prescribing; advise patients to seek medical attention if signs of hemolysis occur.
• Use during pregnancy or in breastfeeding women may cause hemolytic anemia in a G6PD-deficient fetus or infant, respectively (
• Asymptomatic methemoglobin elevations observed; initiate appropriate therapy if signs or symptoms of methemoglobinemia occur; carefully monitor individuals with nicotinamide adenine dinucleotide (NADH)-dependent methemoglobin reductase deficiency.
• Psychiatric adverse reactions (. g, anxiety, abnormal dreams, insomnia) reported in clinical trials; a benefit of treatment must be weighed against the potential risk for psychiatric adverse reactions in patients with a history of psychiatric illness; owing to long half-life (approximately 15 days [Krintafel] or approximately 17 days [Arakoda]), signs or symptoms of psychiatric adverse reactions that may occur could be delayed in onset and/or duration.
• Serious hypersensitivity reactions (. g, angioedema, urticaria) reported; initiate appropriate therapy and do not readminister tafenoquine; owing to long half-life (approximately 15 days [Krintafel] or approximately 17 days [Arakoda), hypersensitivity signs or symptoms may be delayed in onset and/or duration (see Contraindications)
• Drug interaction overview
  • Tafenoquine inhibits organic cation transporter-2 (OCT2) and multidrug and toxin extrusion (MATE) transporters in vitro.
  • Avoid coadministration with OCT2 or MATE substrates.
  • If coadministration cannot be avoided, monitor for substrate-related toxicities, and consider dosage reduction if needed based on prescribing information.
  • Lack of efficacy in reducing P. vivax malaria recurrence in treated patients when combined with an artemisinin-containing antimalarial was seen in a clinical trial; coadministration with antimalarials other than chloroquine is not recommended.

Pregnancy and Lactation

• Available data on pregnant women are insufficient to establish a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes; however, it is recommended to avoid use during pregnancy.
• Use during pregnancy may cause hemolytic anemia in a G6PD-deficient fetus.
• Also see Contraindications and Cautions
• Clinical considerations
  • Malaria during pregnancy increases the risk for adverse pregnancy outcomes, including maternal anemia, prematurity, spontaneous abortion, and stillbirth.