Tafenoquine succinate

What is Tafenoquine succinate?

• Tafenoquine succinate (KRINTAFEL) is an antimalarial used to treat malaria.

What are the uses of this medicine?

• This medicine is used for the radical cure (prevention of relapse) of Plasmodium vivax malaria in patients aged 16 years and older who are receiving chloroquine therapy for acute P. vivax infection.

Limitations of Useː

• KRINTAFEL is NOT indicated for the treatment of acute P. vivax malaria.
• The concomitant use of KRINTAFEL with antimalarials other than chloroquine is not recommended because of the risk of recurrence of P. vivax malaria.

How does this medicine work?

Tafenoquine, an 8-aminoquinoline antimalarial, is active against the liver stages including the hypnozoite (dormant stage) of P. vivax. In addition to its effect on the parasite, tafenoquine causes red blood cell shrinkage in vitro. The molecular target of tafenoquine is not known. The activity of tafenoquine against the pre-erythrocytic liver stages of the parasite prevents the development of the erythrocytic forms of the parasite, which are responsible for relapses in P. vivax malaria.

Who Should Not Use this medicine ?

This medicine cannot be used in patients if:

• have a blood problem called glucose-6-phosphate dehydrogenase (G6PD) deficiency (sometimes known as favism) or you have not been tested for G6PD deficiency.
• KRINTAFEL can cause a breakdown of red blood cells (hemolysis) in people with G6PD deficiency. Your healthcare provider will test you for G6PD deficiency before you start taking KRINTAFEL.
• are breastfeeding a child known to have G6PD deficiency or breastfeeding a child that has not been tested for G6PD deficiency.
• are allergic to tafenoquine or any of the ingredients in KRINTAFEL or if you have had an allergic reaction to similar medicines containing 8-aminoquinolines. See the end of this Patient Information leaflet for a complete list of ingredients in KRINTAFEL.

What drug interactions can this medicine cause?

Avoid coadministration of KRINTAFEL with OCT2 and MATE substrates (e.g., dofetilide, metformin). If coadministration cannot be avoided, monitor for drug-related toxicities and consider dosage reduction if needed.

Is this medicine FDA approved?

• It was approved for use in the United States in 2018.

How should this medicine be used?

• All patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency prior to prescribing KRINTAFEL.
• Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with KRINTAFEL.

Recommended Dosage

• The recommended dose of KRINTAFEL in patients aged 16 years and older is a single dose of 300 mg administered as two 150-mg KRINTAFEL tablets taken together.
• Coadminister KRINTAFEL on the first or second day of chloroquine therapy for the acute P. vivax malaria.

Administration

• Your healthcare provider will test you for G6PD deficiency before you start taking KRINTAFEL.
• KRINTAFEL is given as 2 tablets that you take together as a single dose.
• You will take KRINTAFEL on the first or second day of your treatment with chloroquine.
• Take KRINTAFEL with food to make sure the right amount of medicine is absorbed into your body.
• Swallow KRINTAFEL tablets whole. Do not break, crush, or chew the tablets.
• If you vomit within 1 hour of taking KRINTAFEL, call your healthcare provider as you may need to take a second dose of KRINTAFEL.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 150 mg of tafenoquine

This medicine is available in fallowing brand namesː

• KRINTAFEL

What side effects can this medication cause?

The most common side effects of this medicine include:

• dizziness
• nausea
• vomiting
• headache
• changes in laboratory tests for hemoglobin

KRINTAFEL can cause serious side effects, including:

• Breakdown of red blood cells (hemolytic anemia)
• Hemolytic anemia in an unborn baby who has G6PD deficiency
• Decrease of oxygen in your blood caused by a certain type of abnormal red blood cell (methemoglobinemia)
• Allergic (hypersensitivity) reactions
• Mental health (psychiatric) symptoms

What special precautions should I follow?

G6PD testing must be performed before prescribing KRINTAFEL due to the risk of hemolytic anemia. Monitor patients for clinical signs or symptoms of hemolysis. KRINTAFEL may cause hemolytic anemia when administered to a pregnant woman with a G6PD-deficient fetus. KRINTAFEL is not recommended during pregnancy. A G6PD-deficient infant may be at risk for hemolytic anemia from exposure to KRINTAFEL through breast milk. Check infant’s G6PD status before breastfeeding begins. Asymptomatic elevations in blood methemoglobin have been observed. Initiate appropriate therapy if signs or symptoms of methemoglobinemia occur. Serious psychiatric adverse reactions have been observed in patients with a previous history of psychiatric conditions at doses higher than the approved dose. Serious hypersensitivity reactions (e.g., angioedema) have been observed with administration of KRINTAFEL. If hypersensitivity reactions occur, institute appropriate therapy. Lack of efficacy in reducing P. vivax malaria recurrence in patients treated with KRINTAFEL combined with dihydroartemisinin/piperaquine. Use with antimalarials other than chloroquine is not recommended.

What to do in case of emergency/overdose?

Hemoglobin decline and methemoglobinemia may be encountered in an overdose with KRINTAFEL.

Management for overdosage:

• Treatment of overdosage consists of institution of appropriate symptomatic and/or supportive therapy.

Can this medicine be used in pregnancy?

The use of KRINTAFEL during pregnancy may cause hemolytic anemia in a fetus who is G6PD deficient. Treatment with KRINTAFEL during pregnancy is not recommended.

Can this medicine be used in children?

• The safety and effectiveness of KRINTAFEL have been established in pediatric patients aged 16 years and older.
• Safety and effectiveness of KRINTAFEL in pediatric patients younger than 16 years have not been established.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: tafenoquine succinate.
• Inactive Ingredients: magnesium stearate, mannitol, and microcrystalline cellulose.

Who manufactures and distributes this medicine?

Manufactured by: GlaxoSmithKline Research Triangle Park, NC 27709 Made in India

What should I know about storage and disposal of this medication?

• Store at 20°C to 25°C (68°F to 77°F). Temperature excursions are permitted to 15°C to 30°C (59°F to 86°F) .
• Store in the original package to protect from moisture. Keep the bottle tightly closed and do not remove the desiccant.

• Dailymed label info on Tafenoquine succinate
• FDA Tafenoquine succinate

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