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Tafenoquine Succinate

Prescription

商品名: Krintafel

剤形
Tablet
投与経路
ORAL
製造会社
GlaxoSmithKline LLC

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

有効成分

成分 含有量
Tafenoquine Succinate -

適応症と用法

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. vivax malaria [see Warnings and Precautions ( 5.6 )] . KRINTAFEL is an antimalarial 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. ( 1 ) Limitations of Use • KRINTAFEL is NOT indicated for the treatment of acute P. vivax malaria. ( 1 ) • The concomitant use of KRINTAFEL with antimalarials other than chloroquine is not recommended because of the risk of recurrence of P. vivax malaria. ( 1 , 5.6 )

作用のしくみ

12.1 Mechanism of Action Tafenoquine is an 8-aminoquinoline antimalarial drug [see Microbiology ( 12.4 )].

用量と投与方法

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 day of chloroquine therapy for the acute P. vivax malaria. ( 2.2 ) • Administer KRINTAFEL with food. ( 2.2 ) 2.1 Tests to be Performed Prior to Treatment with KRINTAFEL All patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency prior to prescribing KRINTAFEL [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 )] . Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with KRINTAFEL [see Use in Specific Populations ( 8.1 , 8.3 )] . 2.2 Recommended Dosage and Administration The recommended dose of KRINTAFEL in patients aged 16 years and older is a single dose of 300 mg administered as two 150-mg tablets taken together. Coadminister KRINTAFEL on the first or second day of chloroquine therapy for acute P. vivax malaria [see Clinical Studies ( 14 )] . Administer KRINTAFEL with food to increase systemic absorption [see Clinical Pharmacology ( 12.3 )] . Swallow tablets whole. Do not break, crush, or chew the tablets. In the event of vomiting within 1 hour after dosing, a repeat dose should be given. Re-dosing should not be attempted more than once.

Side Effects Overview

6 ADVERSE REACTIONS The following clinically significant adverse reactions have been observed with KRINTAFEL and are discussed in detail in the Warnings and Precautions section: • Hemolytic anemia [see Warnings and Precautions ( 5.1 )] • Methemoglobinemia [see Warnings and Precautions ( 5.3 )] • Psychiatric effects [see Warnings and Precautions ( 5.4 )] • Hypersensitivity reactions [see Warnings and Precautions ( 5.5 )] Common adverse reactions (≥5%) were dizziness, nausea, vomiting, headache, and decreased hemoglobin. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact GlaxoSmithKline at 1-888-825-5249 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety data described below reflect exposure to 4,129 subjects, of whom 810 received a 300-mg single dose of KRINTAFEL. KRINTAFEL was evaluated in patients with P. vivax malaria (n = 483) in 3 randomized, double-blind trials including a placebo-controlled trial comparing KRINTAFEL plus chloroquine (n = 260) with chloroquine alone (Trial 1), a placebo-controlled dose-ranging trial (Trial 2) (n = 57) [see Clinical Studies ( 14 )] , and a hematologic safety trial (Trial 3, NCT02216123) (n = 166). In Trial 1, in patients with P. vivax malaria, the most common adverse reactions reported in ≥5% of patients treated with KRINTAFEL are listed in Table 1 . Patients included in the trial had a mean age of 35 (range: 16 to 79 years), were 75% male and from the following regions: 70% Latin America (Brazil and Peru), 19% Southeast (SE) Asia (Thailand, Cambodia, and the Philippines), and 11% Africa (Ethiopia). Table 1. Selected Adverse Reactions a Reported in ≥5% of Patients with P. vivax Malaria Receiving KRINTAFEL in a Randomized, Active-Controlled Trial (Trial 1) a Adverse reactions reported prior to Day 29 as subsequent adverse reactions can be confounded by recurrence of malaria or retreatment with another agent from the quinoline class. Adverse Reaction Chloroquine KRINTAFEL + Chloroquine (n = 133) (n = 260) % % Dizziness 3 8 Nausea 7 6 Vomiting 5 6 Decreased Hemoglobin 2 5 Headache 7 5 Other Adverse Reactions Reported with KRINTAFEL Clinically significant adverse reactions with KRINTAFEL 300-mg single dose in clinical trials (n = 810) in ≤3% of subjects are listed below: Psychiatric Disorders: Anxiety, insomnia, abnormal dreams. Nervous System Disorders: Somnolence. Laboratory Investigations: Increased blood creatinine, increased blood methemoglobin, increased alanine aminotransferase. Immune System Disorders: Hypersensitivity reactions (e.g., angioedema, urticaria) [see Contraindications ( 4 ), Warnings and Precautions ( 5.5 )] . Eye Disorders: Vortex keratopathy, photophobia.

警告と注意事項

禁忌

薬物動態

12.3 Pharmacokinetics Absorption Maximum plasma concentrations were generally observed 12 to 15 hours following oral administration. Food Effect: Plasma tafenoquine AUC increased by 41% and C max increased by 31% when administered as an investigational capsule formulation with a high-calorie, high-fat meal (approximately 1,000 calories with 15% protein, 25% carbohydrate, and 60% fat) compared with the fasted state. Distribution Protein binding of tafenoquine is >99.5%. The apparent oral volume of distribution is ~1,600 L. Following single- and multiple-oral-dose administration, tafenoquine whole blood concentrations were on average 67% higher than corresponding plasma values. Elimination The apparent oral clearance of tafenoquine is approximately 3 L/h. The average terminal half-life is approximately 15 days. Metabolism: Tafenoquine undergoes slow metabolism. Unchanged tafenoquine represented the only notable drug-related component in human plasma after a single oral dose of tafenoquine. Excretion: The full excretion profile of tafenoquine in humans is unknown. Over a 6-day collection period, renal elimination of unchanged tafenoquine was low. Specific Populations Pharmacokinetics of tafenoquine were not significantly impacted by age, sex, ethnicity, and body weight. The effect of renal or hepatic impairment on tafenoquine pharmacokinetics is unknown. Drug Interaction Studies Clinical Studies: No clinically significant effects on tafenoquine pharmacokinetics were observed following coadministration with chloroquine, dihydroartemisinin-piperaquine, or artemether-lumefantrine in healthy subjects. No clinically significant effects on the pharmacokinetics of dihydroartemisinin, piperaquine, artemether, lumefantrine, or substrates of cytochrome P450 isoenzymes (CYP)1A2 (caffeine), CYP2D6 (desipramine), CYP2C8 (chloroquine), CYP2C9 (flurbiprofen), or CYP3A4 (midazolam, chloroquine) were observed following coadministration of tafenoquine in healthy subjects. In Vitro Studies Where Drug Interaction Potential Was Not Further Evaluated Clinically: Tafenoquine inhibited metformin transport via human OCT2, MATE-1, and MATE2-K transporters. Clinical drug interaction studies with tafenoquine and OCT2 and MATE substrates have not been conducted [see Drug Interactions ( 7 )] . The effect of tafenoquine on substrates of P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and organic anion transporting polypeptides 1B1/1B3 (OATP1B1/OATP1B3) is unknown.

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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References & Data Sources

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データソース: DailyMed (NLM), openFDA, MFDS

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Data sources: ChEMBL, PubChem, DailyMed.