Tafenoquine Succinate
PrescriptionNoms de marque : Krintafel
About This Medication
11 DESCRIPTION KRINTAFEL contains tafenoquine succinate, an antimalarial agent for oral administration. The chemical name of tafenoquine succinate is (±) 8-[(4-amino-1-methylbutyl)amino]-2,6-dimethoxy-4‑methyl-5-[3-(trifluoromethyl)phenoxy]quinoline succinate. The molecular formula of tafenoquine succinate is C 24 H 28 F 3 N 3 O 3 •C 4 H 6 O 4 , and its molecular mass is 581.6 as the succinate salt (463.5 as free base). The structural formula is shown below. Each KRINTAFEL tablet contains 150 mg of tafenoquine (equivalent to 188.2 mg tafenoquine succinate). Inactive ingredients include magnesium stearate, mannitol, and microcrystalline cellulose. The tablet film-coating inactive ingredients include hydroxypropylmethylcellulose, polyethylene glycol, red iron oxide, and titanium dioxide. Tafenoquine succinate chemical structure
Principes Actifs
| Ingrédient | Dosage |
|---|---|
| Tafenoquine Succinate | - |
Indications et Utilisation
Comment ça marche
Posologie et Administration
Side Effects Overview
Mises en Garde et Précautions
5 WARNINGS AND PRECAUTIONS • Hemolytic Anemia : G6PD testing must be performed before prescribing KRINTAFEL due to the risk of hemolytic anemia. Monitor patients for clinical signs or symptoms of hemolysis. ( 5.1 ) • G6PD Deficiency in Pregnancy or Lactation : 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. ( 5.2 , 8.1 , 8.2 ) • Methemoglobinemia : Asymptomatic elevations in blood methemoglobin have been observed. Initiate appropriate therapy if signs or symptoms of methemoglobinemia occur. ( 5.3 ) • Psychiatric Effects : Serious psychiatric adverse reactions have been observed in patients with a previous history of psychiatric conditions at doses higher than the approved dose. The benefit of treatment with KRINTAFEL must be weighed against the potential risk for psychiatric adverse reactions in patients with a history of psychiatric illness. ( 5.4 ) • Hypersensitivity Reactions : Serious hypersensitivity reactions (e.g., angioedema) have been observed with administration of KRINTAFEL. If hypersensitivity reactions occur, institute appropriate therapy. ( 5.5 ) • Due to the long half-life of KRINTAFEL (15 days), psychiatric effects and hypersensitivity reactions may be delayed in onset and/or duration. ( 5.4 , 5.5 , 12.3 ) • Risk of P. vivax Malaria Recurrence: Lack of efficacy in reducing P. vivax malaria recurrence in patients treated with KRINTAFEL combined with dihydroartemisinin/piperaquine (not approved artemisinin-containing antimalarial) was seen in a clinical trial. Use with antimalarials other than chloroquine is not recommended. ( 1 , 5.6 ) 5.1 Hemolytic Anemia Due to the risk of hemolytic anemia in patients with G6PD deficiency, G6PD testing must be performed before prescribing KRINTAFEL [see Dosage and Administration ( 2.1 )] . Due to the limitations of G6PD tests, physicians need to be aware of residual risk of hemolysis and adequate medical support and follow-up to manage hemolytic risk should be available. Treatment with KRINTAFEL is contraindicated in patients with G6PD deficiency or unknown G6PD status [see Contraindications ( 4 )] . Patients were excluded from clinical trials of KRINTAFEL if they had a G6PD enzyme activity level <70% of the site median value for G6PD normal activity [see Clinical Studies ( 14 )]. In clinical trials, declines in hemoglobin levels were reported in some G6PD-normal patients [see Adverse Reactions ( 6.1 )] . Monitor patients for clinical signs or symptoms of hemolysis. Advise patients to seek medical attention if signs of hemolysis occur. 5.2 G6PD Deficiency in Pregnancy or Lactation Potential Harm to the Fetus The use of KRINTAFEL during pregnancy may cause hemolytic anemia in a G6PD-deficient fetus. Even if a pregnant woman has normal levels of G6PD, the fetus could be G6PD deficient. Advise females of reproductive potential that treatment with KRINTAFEL during pregnancy is not recommended and to avoid pregnancy or use effective contraception for 3 months after the dose of KRINTAFEL [see Use in Specific Populations ( 8.1 , 8.3 )] . Potential Harm to the Breastfeeding Infant A G6PD-deficient infant may be at risk for hemolytic anemia from exposure to KRINTAFEL through breast milk. Infant G6PD status should be checked before breastfeeding begins. KRINTAFEL is contraindicated in breastfeeding women when the infant is found to be G6PD deficient or the G6PD status of the infant is unknown [see Contraindications ( 4 )] . Advise the woman with a G6PD-deficient infant or if the G6PD status of the infant is unknown not to breastfeed for 3 months after the dose of KRINTAFEL [see Use in Specific Populations ( 8.2 )] . 5.3 Methemoglobinemia Asymptomatic elevations in methemoglobin have been observed in the clinical trials of KRINTAFEL [see Adverse Reactions ( 6.1 )]. Institute appropriate therapy if signs or symptoms of methemoglobinemia occur. Carefully monitor individuals with nicotinamide adenine dinucleotide (NADH)-dependent methemoglobin reductase deficiency. Advise patients to seek medical attention if signs of methemoglobinemia occur. 5.4 Psychiatric Effects Psychiatric adverse reactions including anxiety (<1%), abnormal dreams (<1%), and insomnia (3%) have been reported in clinical trials of KRINTAFEL [see Adverse Reactions ( 6.1 )] . Two cases of depression and 2 cases of psychosis have occurred primarily in patients with a history of psychiatric disorders following receipt of single doses of tafenoquine that were higher than the approved 300-mg dose (350 mg to 600 mg). Safety and effectiveness of KRINTAFEL have not been established at doses or regimens other than the approved regimen; use of KRINTAFEL at doses or regimens other than a 300-mg single dose is not approved by FDA. The benefit of treatment with KRINTAFEL must be weighed against the potential risk for psychiatric adverse reactions in patients with a history of psychiatric illness. Due to the long half-life of KRINTAFEL (approximately 15 days), signs or symptoms of psychiatric adverse reactions that may occur could be delayed in onset and/or duration [see Clinical Pharmacology ( 12.3 )] . 5.5 Hypersensitivity Reactions Serious hypersensitivity reactions (e.g., angioedema, urticaria) have been observed with administration of KRINTAFEL [see Adverse Reactions ( 6.1 )] . Institute appropriate therapy if hypersensitivity reactions occur. Do not re-administer KRINTAFEL. KRINTAFEL is contraindicated in patients who develop hypersensitivity to tafenoquine or any component of KRINTAFEL or other 8-aminoquinolines [see Contraindications ( 4 )] . Due to the long half-life of KRINTAFEL (approximately 15 days), signs or symptoms of hypersensitivity adverse reactions that may occur could be delayed in onset and/or duration [see Clinical Pharmacology ( 12.3 )] . Advise patients to seek medical attention if signs of hypersensitivity occur. 5.6 Risk of P. vivax Malaria Recurrence Lack of efficacy in reducing P. vivax malaria recurrence in patients treated with KRINTAFEL combined with an artemisinin-containing antimalarial was seen in a clinical trial (NCT02802501). In this double-blind, randomized, placebo-controlled trial in which all patients with P. vivax malaria were treated with dihydroartemisinin/piperaquine (not approved artemisinin-containing antimalarial) and were coadministered KRINTAFEL, primaquine, or placebo, lack of efficacy (recurrence rates at 6 months following treatment) was seen in patients treated with KRINTAFEL. Concomitant administration of KRINTAFEL with antimalarials other than chloroquine is not recommended.
Contre-indications
4 CONTRAINDICATIONS KRINTAFEL is contraindicated in: • Patients with G6PD deficiency or unknown G6PD status due to the risk of hemolytic anemia [see Warnings and Precautions ( 5.1 )] . • Breastfeeding by a lactating woman when the infant is found to be G6PD deficient or if the G6PD status of the infant is unknown [see Use in Specific Populations ( 8.2 )]. • Patients with known hypersensitivity to tafenoquine, other 8-aminoquinolines, or any component of KRINTAFEL [see Warnings and Precautions ( 5.5 )] . • G6PD deficiency or unknown G6PD status. ( 4 ) • Breastfeeding by a lactating woman when the infant is found to be G6PD deficient or if G6PD status is unknown. ( 4 , 8.2 ) • Known hypersensitivity reactions to tafenoquine, other 8-aminoquinolines, or any component of KRINTAFEL. ( 4 )
Pharmacocinétique
Frequently Asked Questions
1 INDICATIONS AND USAGE KRINTAFEL is indicated 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 [see Dosage and Administration ( 2.2 )] . Limitations of Use • KRINTAFEL is NOT indicated for the treatment of acute P. vivax malaria. • Concomitant use of KRINTAFEL with antimalarials other than chloroquine is not recommended because of the risk of recurrence of P. …
2 DOSAGE AND ADMINISTRATION • All patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency prior to prescribing KRINTAFEL. ( 2.1 ) • Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with KRINTAFEL. ( 2.1 ) • 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. ( 2.2 ) • Coadminister KRINTAFEL on the first or second …
5 WARNINGS AND PRECAUTIONS • Hemolytic Anemia : G6PD testing must be performed before prescribing KRINTAFEL due to the risk of hemolytic anemia. Monitor patients for clinical signs or symptoms of hemolysis. ( 5.1 ) • G6PD Deficiency in Pregnancy or Lactation : 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 …
4 CONTRAINDICATIONS KRINTAFEL is contraindicated in: • Patients with G6PD deficiency or unknown G6PD status due to the risk of hemolytic anemia [see Warnings and Precautions ( 5.1 )] . • Breastfeeding by a lactating woman when the infant is found to be G6PD deficient or if the G6PD status of the infant is unknown [see Use in Specific Populations ( 8.2 )]. • Patients with known hypersensitivity to tafenoquine, other 8-aminoquinolines, or any component of KRINTAFEL [see Warnings and …
Tafenoquine Succinate is a prescription medication. You will need a valid prescription from a licensed healthcare provider.
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Browse all Tablet products →References & Data Sources
- • DailyMed — Tafenoquine Succinate drug label (National Library of Medicine)
- • openFDA — Tafenoquine Succinate label data (U.S. Food & Drug Administration)
- • RxNorm — RXCUI 2109233 (NLM Normalized Drug Names)
- • NDC Directory — Tafenoquine Succinate (FDA National Drug Code)
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Sources des données : DailyMed (NLM), openFDA, MFDS