tafenoquine

Absorption: Well absorbed following oral administration (↑ with high-calorie, high-fat meals).

Distribution: Widely distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Minimally metabolized; route of excretion unknown.

Half-Life: 15–16.5 days.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	12–15 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to tafenoquine, chloroquine, hydroxychloroquine, or primaquine;
Glucose-6-phosphate dehydrogenase (G6PD) deficiency or unknown G6PD status (↑ risk of hemolytic anemia);
History of psychotic disorders or current psychotic symptoms (e.g., hallucinations, delusions, grossly disorganized behavior) (Arakoda only);
OB: Pregnancy (may cause hemolytic anemia in fetus if G6PD deficient);
Lactation: Avoid breastfeeding if infant has G6PD deficiency or if G6PD status unknown.

Use Cautiously in:

Hepatic or renal impairment;
Rep: Women of reproductive potential;
Pedi: Children <18 yr (Arakoda) or <16 yr (Krintafel) (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

EENT: keratopathy, motion sickness, retinal disorders

GI: diarrhea, ↑liver enzymes, nausea, vomiting

Hemat: methemoglobinemia, anemia, HEMOLYTIC ANEMIA

MS: back pain

Neuro: headache, anxiety, delusions, depression, dizziness, hallucinations, insomnia, nightmares

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA AND URTICARIA)

Interactions ⬆ ⬇

Drug-drug:

May ↑ levels and risk of toxicity of dofetilide and metformin; avoid concurrent use.

Route/Dosage ⬆ ⬇

Arakoda

PO (Adults ): Loading regimen (given prior to travel): 200 mg once daily for 3 days prior to traveling to a malarious area; Maintenance regimen (while in the malarious area): 200 mg once weekly, starting 7 days after the final dose of the loading regimen; Terminal prophylaxis regimen (after leaving malarious area): 200 mg single dose taken 7 days after the last dose of the maintenance regimen.

Krintafel

PO (Adults and Children ≥16 yr): 300 mg single dose taken on first or second day of the appropriate antimalarial therapy for acute Plasmodium vivax infection.

Availability ⬆ ⬇

Tablets (Arakoda): 100 mg
Tablets (Krintafel): 150 mg

Assessment ⬆ ⬇

Monitor for signs or symptoms of hemolytic anemia (darkening of urine, dizziness, confusion, feeling tired, light-headedness, shortness of breath, pale skin or yellowing of the skin and whites of eyes). If hemolytic anemia occurs, permanently discontinue tafenoquine .
Monitor for signs and symptoms of methemoglobinemia (bluish coloring of the lips or skin, headache, fatigue, shortness of breath, lack of energy). Monitor patients with nicotinamide adenine dinucleotide-dependent methemoglobin reductase deficiency. If methemoglobinemia occurs, discontinue tafenoquine.
Monitor for psychotic symptoms (hallucinations, delusions, grossly disorganized thinking or behavior) during therapy. Other psychiatric symptoms, such as changes in mood, anxiety, insomnia, and nightmares, should be promptly evaluated by a medical professional if they are moderate and last >3 days or are severe. If psychotic symptoms occur, consider discontinuation of tafenoquine and prompt evaluation by a mental health professional as soon as possible.
Monitor for signs and symptoms of hypersensitivity reactions (angioedema, urticaria) during therapy. If hypersensitivity reactions occur, discontinue tafenoquine and institute appropriate therapy.

Lab Test Considerations:

All patients must be tested for G6PD deficiency before prescribing tafenoquine.
Verify negative pregnancy test before starting therapy.

Implementation ⬆ ⬇

PO: Administer with food. DNC: Swallow tablets whole; do not crush, break, or chew.Complete full course of therapy including loading and terminal doses.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct to take as directed. If vomiting occurs within 1 hr after dosing, a repeat dose should be given. Do not attempt to redose more than once. Arakoda: If a dose is missed during loading dose, take one dose of 200 mg (2 of the 100-mg tablets) for a total of three daily loading doses taken. Begin maintenance dose 1 wk after last loading dose. If two doses of loading dose are missed, take two doses of 200 mg (two 100-mg tablets) on 2 consecutive days so that a total of three daily loading doses have been taken. Begin maintenance dose 1 wk after the last loading dose. If one dose of maintenance dose is missed, take one dose of 200 mg (two 100-mg tablets) on any day up to the time of the next scheduled weekly dose. If two doses of maintenance dose are missed, take one dose of 200 mg (two 100-mg tablets) on any day up to the time of the next scheduled weekly dose. If at least three doses of maintenance dose are missed, take two doses of 200 mg (two 100-mg tablets), taken as 200 mg (two 100-mg tablets) once daily for 2 days up to the time of next weekly dose. If a dose of terminal prophylaxis dose is missed, take one dose of 200 mg (two 100-mg tablets) as soon as remembered.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise patient to notify health care professional if symptoms of hemolytic anemia, methemoglobinemia, or hypersensitivity (swelling of face, lips, tongue or throat; itching; trouble breathing or wheezing; vomiting; fainting; light-headedness; rash; hives) occur. Seek immediate medical attention if necessary.
Rep: Malaria during pregnancy causes ↑ risk for adverse pregnancy outcomes, including maternal anemia, prematurity, spontaneous abortion, and stillbirth. Advise women of reproductive potential that treatment with tafenoquine during pregnancy is not recommended and to avoid pregnancy or use effective contraception during treatment and for 3 mo after the last dose of tafenoquine. If a pregnancy is detected during tafenoquine use, discontinue tafenoquine as soon as possible and switch to an alternative prophylactic drug for malaria during pregnancy. Check infant G6PD status before starting breastfeeding. Advise patient with a G6PD-deficient infant or if the G6PD status of the infant is unknown not to breastfeed during treatment with tafenoquine and for 3 mo after final dose.

Evaluation/Desired Outcomes ⬆ ⬇

Prevention of initial episode and relapses of malaria.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

0173- GlaxoSmithKline LLC
- 0173-0889- Krintafel
  - 0173-0889-39- 2 TABLET, FILM COATED in 1 BOTTLE (0173-0889-39)

65085- Piramal Pharma Limited
- 65085-0061-
  - 65085-0061-1- 5 kg in 1 DRUM (65085-0061-1)

65085- Piramal Pharma Limited
- 65085-0061-
  - 65085-0061-2- 10 kg in 1 DRUM (65085-0061-2)

65085- Piramal Pharma Limited
- 65085-0061-
  - 65085-0061-3- 15 kg in 1 DRUM (65085-0061-3)

65085- Piramal Pharma Limited
- 65085-0061-
  65085-0061-4- 20 kg in 1 DRUM (65085-0061-4)

65085- Piramal Pharma Limited
- 65085-0061-
  65085-0061-5- 25 kg in 1 DRUM (65085-0061-5)

69766- MSN Life Sciences Private Limited
- 69766-079-
  69766-079-01- 50 kg in 1 DRUM (69766-079-01)

71475- 60 Degrees Pharmaceuticals, INC.
- 71475-257- Arakoda
  71475-257-01- 2 BLISTER PACK in 1 CARTON (71475-257-01) / 8 TABLET, FILM COATED in 1 BLISTER PACK

71475- 60 Degrees Pharmaceuticals, INC.
- 71475-257- Arakoda
  - 71475-257-02- 8 TABLET, FILM COATED in 1 BOTTLE (71475-257-02)

71475- 60 Degrees Pharmaceuticals, INC
- 71475-258- Kodatef
  - 71475-258-03- 1 TABLET, FILM COATED in 1 CARTON (71475-258-03)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇