Names and pronunciation
(ta fen′oh-kwin) Krintafel, Arakoda
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Drug reference
(ta fen′oh-kwin) Krintafel, Arakoda
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Func. class.: Antimalarial
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Chem. class.: 8-aminoquinoline
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ACTION: Activity against the pre- erythrocytic liver stages of the parasite prevents the development of the erythro- cytic forms, which are responsible for malarial relapse; may inhibit hematin polymerization, inducing apoptotic-like death of the parasite
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USES: Prevention of relapse of Plasmodium vivax malaria in those receiving antimalarial therapy for acute P. vivax infection (Krintafel); for malaria prophylaxis (Arakoda)
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CONTRAINDICATIONS: Hypersensitivity to this product or iodo- quinol or primaquine, G6PD deficiency, psychosis Precautions: Breastfeeding, contracep- tion requirements, hepatic disease, met- hemoglobin reductase deficiency, preg- nancy, pregnancy testing, psychiatric events, renal disease, reproductive risk
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SIDE EFFECTS CNS: Dizziness, headache, anxiety, abnor- mal dreams, insomnia, somnolence EENT: Vortex keratopathy, photophobia GI: Nausea, vomiting HEMA: Decreased HB INTEG: Angioedema, urticaria
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INTERACTIONS • Avoid use with MATE (multidrug and toxin extrusion substrates) and OCT2 (organic cation transporter-2) (dofetilide, metformin); if these products must be given, monitor for toxicity Drug/Lab: Increase: methemoglobin, ALT, creatinine
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DOSAGE AND ROUTES Prevention of relapse of Plasmodium vivax malaria (Krintafel) • Adult/adolescent ≥16 yr: PO 300 mg as a single dose on the first or second day of the antimalarial therapy (chloroquine) For malaria prophylaxis (Arakoda) • Adult: PO 200 mg daily for 3 days be- fore travel as loading dose, then 200 mg weekly starting 7 days after the last load- ing dose, continue during travel to area as maintenance, then 200 mg once at 7 days after the last maintenance dose in the wk after exit from area; may be given for ≤6 mo of continuous dosing
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Administer: • Give with food • Swallow tablets whole. Do not break, crush, or chew • If vomiting occurs within 1 hr after dosing, repeat the dose; do not attempt to redose more than once (prevention of relapse single-dose therapy) • Storage: At room temperature in orig- inal container, protect from moisture
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Evaluate: • Therapeutic response: prevention of relapse or prevention of malaria
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CLINICAL CONSIDERATIONS Assess • Malaria symptoms: anemia, jaundice, diarrhea, sweating, vomiting, fast heart rate, low B/P; report symptoms to health care provider • Methemoglobinemia: monitor for in creased methemoglobin; report immedi ately shortness of breath, cyanosis, men tal status changes; O2 and methylene blue may be given • Psychiatric effects: serious psychiat- ric adverse reactions have been observed in patients with a previous history of psychiatric conditions at doses higher than the approved dose; the effects may occur during or after treatment. • Hypersensitivity reactions: serious hypersensitivity reactions (angioedema) may occur; these reactions may occur during or after conclusion of therapy • Pregnancy/breastfeeding: avoid use in pregnancy, a pregnancy test is required in all females of reproductive potential, adequate contraception is re quired during and for 3 mo after last dose; infant should be tested for G6PD deficiency before breastfeeding
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Patient and caregiver information: • Pregnancy/breastfeeding: not to use during pregnancy; adequate contra ception should be used during and for 3 mo after last dose; infant should have a lab test performed before breast feeding • To swallow tablets whole, not to split or cut; to take with food • To report immediately dark urine or lips as these may be symptoms of hemolytic anemia • To use sunglasses in bright light to prevent photophobia
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PHARMACOKINETICS Protein binding 99.5%, peak 12-15 hr, half-life 12-15 days (Krintafel). Affected cytochrome P450 isoenzymes and drug transporters: OCT2, MATE-1, MATE2-K
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• Adult/adolescent ≥16 yr: PO 300 mg as a single dose on the first or second day of the antimalarial therapy (chloroquine) For malaria prophylaxis (Arakoda)
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• Adult: PO 200 mg daily for 3 days be- fore travel as loading dose, then 200 mg weekly starting 7 days after the last load- ing dose, continue during travel to area as maintenance, then 200 mg once at 7 days after the last maintenance dose in the wk after exit from area; may be given for ≤6 mo of continuous dosing
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