Overview
11 DESCRIPTION ARAKODA contains tafenoquine succinate, an antimalarial agent for oral administration. The structural formula of tafenoquine succinate is: Figure 1: Tafenoquine Succinate Structure The chemical name of tafenoquine succinate is (±)-8-[(4-amino-1-methylbutyl) amino]-2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl) phenoxy]quinoline succinate.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Tafenoquine is an 8-aminoquinoline antimalarial drug [see Microbiology ( 12.4 )] . 12.2 Pharmacodynamics Cardiac Electrophysiology The effect of tafenoquine on the QT interval was evaluated in a study of healthy adult subjects. In this study, subjects received once daily 400 mg (2 times the approved recommended dosage) doses of tafenoquine for 3 days. The results suggest that the mean increase in the QTcF interval for tafenoquine is less than 20 msec. 12.3 Pharmacokinetics Absorption A food effect study was not conducted with the 100 mg ARAKODA tablet. In majority of the clinical trials, tafenoquine was administered under fed conditions.
Indications
- 1 INDICATIONS AND USAGE ARAKODA is indicated for the prophylaxis of malaria in patients aged 18 years and older. ARAKODA is an antimalarial indicated for the prophylaxis of malaria in patients aged 18 years and older. ( 1 )
Common Doses
- 200 mg
- 100 mg
Dosage
2 DOSAGE AND ADMINISTRATION • All patients must be tested for glucose-6-phosphate dehydrogenase (G6PD) deficiency prior to prescribing ARAKODA. ( 2.1 ) • Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with ARAKODA. ( 2.1 ) Regimen Name Timing Dosage Loading regimen For each of the 3 days before travel to a malarious area 200 mg (2 of the 100 mg tablets) once daily for 3 days Maintenance regimen While in the malarious area 200 mg (2 of the 100 mg tablets) once weekly – start 7 days after the last loading regimen dose Terminal prophylaxis...
Contraindications
- 4 CONTRAINDICATIONS ARAKODA is contraindicated in: • patients with G6PD deficiency or unknown G6PD status due to the risk of hemolytic anemia [see Warnings and Precautions ( 5.2 )] . • 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 Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.2 )] . • patients with a history of psychotic disorders or current psychotic symptoms (i.e., hallucinations, delusions, and/or grossly disorganized behavior) [see Warnings and Precautions ( 5.
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions observed with ARAKODA are discussed in detail in the Warnings and Precautions section: • Hemolytic Anemia [see Warnings and Precautions ( 5.2 )] • Methemoglobinemia [see Warnings and Precautions ( 5.3 )] • Psychiatric Effects [see Warnings and Precautions ( 5.4 )] • Hypersensitivity Reactions [see Warnings and Precautions ( 5.5 )] The most common adverse reactions (incidence ≥1%) were: headache, dizziness, back pain, diarrhea, nausea, vomiting, increased alanine aminotransferase (ALT), motion sickness, insomnia,...
Interactions
- 7 DRUG INTERACTIONS Avoid co-administration with drugs that are substrates of organic cation transporter-2 (OCT2) or multidrug and toxin extrusion (MATE) transporters ( 7.1 ) 7.1 Effect of ARAKODA on Organic Cation Transporter-2 (OCT2) and Multidrug and Toxin Extrusion (MATE) Substrates The effect of coadministration of tafenoquine on the pharmacokinetics of OCT2 and MATE substrates in humans is unknown. However, in vitro observations suggest the potential for increased concentrations of these substrates [see Clinical Pharmacology ( 12.