Drug Guide
Tafenoquine succinate
Classification
Therapeutic: Antimalarial agent
Pharmacological: Aminoquinoline compound
FDA Approved Indications
- Prevention of malaria caused by Plasmodium falciparum in areas with chloroquine-resistant malaria (Arakoda)
- Prevention of malaria caused by Plasmodium vivax (Arakoda)
- Treatment of Plasmodium vivax malaria (Krintafel)
Mechanism of Action
Tafenoquine disrupts the mitochondrial electron transport chain of the malaria parasite, leading to their death. It is active against dormant hypnozoites of P. vivax and P. ovale, preventing relapse.
Dosage and Administration
Adult: For prophylaxis: 200 mg once weekly, starting 1-2 days before travel and continuing during travel and for 1 week after leaving endemic area. For radical cure: 300 mg as a single dose.
Pediatric: Use is not well established; doses should be determined based on weight and clinical judgment.
Geriatric: No specific dosage adjustment provided; caution advised due to potential comorbidities.
Renal Impairment: Use with caution. No specific dose adjustment recommended; monitor renal function.
Hepatic Impairment: Contraindicated in patients with G6PD deficiency and caution advised in those with hepatic impairment.
Pharmacokinetics
Absorption: Rapidly absorbed from the gastrointestinal tract.
Distribution: Widely distributed in the body including tissues and plasma.
Metabolism: Metabolized minimally in the liver, primarily via CYP enzymes.
Excretion: Excreted mainly in the urine.
Half Life: Approximately 14 days, supporting weekly dosing.
Contraindications
- G6PD deficiency
- History of psychiatric disorders
- Known hypersensitivity to tafenoquine
Precautions
- Screen for G6PD deficiency before use to prevent hemolysis.
- Caution in patients with liver impairment.
- Monitor for neuropsychiatric symptoms during therapy.
Adverse Reactions - Common
- Gastrointestinal symptoms (nausea, abdominal pain) (Common)
- Dizziness (Common)
- Headache (Common)
Adverse Reactions - Serious
- Hemolytic anemia in G6PD-deficient patients (Serious and potentially life-threatening)
- Psychiatric disturbances (depression, anxiety, hallucinations) (Serious but rare)
- Leukopenia, thrombocytopenia (Rare)
Drug-Drug Interactions
- CYP450 inhibitors or inducers may alter tafenoquine levels.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Assess G6PD status prior to initiation. Monitor for neuropsychiatric symptoms, hemolysis, hepatic function.
Diagnoses:
- Risk for hemolytic anemia
- Risk for neuropsychiatric effects
Implementation: Administer with food to reduce gastrointestinal upset. Educate patient on importance of adherence and monitoring.
Evaluation: Evaluate for side effects, adherence, and effectiveness in preventing malaria.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report any signs of hemolysis (fatigue, pallor, dark urine).
- Avoid alcohol and hepatotoxic substances.
- Inform about potential neuropsychiatric effects.
Special Considerations
Black Box Warnings:
- G6PD deficiency screening is mandatory prior to use due to risk of hemolytic anemia.
- Neuropsychiatric reactions including hallucinations, paranoia, psychosis have been reported.
Genetic Factors: G6PD deficiency status is critical to determine before starting therapy.
Lab Test Interference: May interfere with certain blood tests but not specifically known for tafenoquine.
Overdose Management
Signs/Symptoms: Hemolytic anemia, neuropsychiatric symptoms, nausea, vomiting.
Treatment: Supportive care; consider hospitalization for monitoring and management of hemolysis.
Storage and Handling
Storage: Store at room temperature, 20-25°C (68-77°F).
Stability: Stable under recommended storage conditions.