Peringatan Keamanan

Tafenoquine can cause hemolysis in people with glucose-6-phosphate dehydrogenase deficiency.A35671 In preclinical studies, renal cell adenomas and carcinomas are increased in male rats with an overdose administration. However, this drug does not seem to be carcinogenic in humans and it was shown to lack mutagenic potential. In fertility studies, tafenoquine resulted in a reduced number of viable fetuses, implantation sites and corpora lutea.FDA label

Tafenoquine

DB06608

small molecule approved investigational

Deskripsi

Tafenoquine is an 8-aminoquinoline analogue of primaquine which varies only on the presence of a 5-phenoxy group.A35671, A35690 It was discovered by the scientists at the Walter Reed Army Institute of Research in 1978 as a substitute for primaquine that would be more effective against relapsing vivax malaria.A35690 Tafenoquine was further developed collaboratively between GlaxoSmithKline and Medicines for Malaria Venture.A35677 It was FDA approved on July 20, 2018.L3770

Struktur Molekul 2D

Berat 463.501
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Tafenoquine presents a long half-life of approximately 14 days.[A35693]
Volume Distribusi Tafenoquine presents a high volume of distribution of approximately 2 560 L.[A35677]
Klirens (Clearance) Tafenoquine presents a low clearance of approximately 6 L/h.[A35677]

Absorpsi

The first-in-human pharmacokinetic study showed a tmax of 13.8 hours and this study suggested that the prolonged absorption from the gut can be due to absorption in the distal gastrointestinal tract combined with a slow clearance. The AUC and Cmax demonstrated an intersubject variability. The bioavailability of tafenoquine is increased in the presence of a high-fat meal by modifying the amount of drug absorbed rather than the rate of absorption. Once absorbed, the concentration of tafenoquine in the whole body is two-fold higher than the corresponding concentration in plasma and it seems to be highly distributed in the liver showing an AUC of approximately 80 times more than what is found in the plasma.A35677

Metabolisme

The activation of tafenoquine needs the activity of CYP 2D6 liver microsomal enzyme. This activation step produces the metabolite 5,6 ortho quinone tafenoquine. This metabolite is internalized by the parasite and reduced to radicals by ferredoxin-NADP+ reductase and diflavin reductase enzymes.A35677 In the human, tafenoquine is metabolized by several metabolic pathways including O-demethylation, N-dealkylation, N-oxidation and oxidative deamination as well as C-hydroxylation of the 8-aminoalkylamino side chain.T304

Rute Eliminasi

After degradation by different metabolic pathways, tafenoquine is slowly excreted from the body primarily in the feces and renal elimination of the unchanged form is very low.T304

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

455 Data
Artemether The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Lumefantrine.
Mefloquine The risk or severity of adverse effects can be increased when Tafenoquine is combined with Mefloquine.
Mirabegron The serum concentration of Tafenoquine can be increased when it is combined with Mirabegron.
Thiethylperazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Thiethylperazine.
Promazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Prochlorperazine.
Triflupromazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Triflupromazine.
Fluphenazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Fluphenazine.
Thioridazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Thioridazine.
Moricizine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Moricizine.
Trifluoperazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Trifluoperazine.
Perphenazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Perphenazine.
Mesoridazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Mesoridazine.
Acetophenazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Acetophenazine.
Promethazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Promethazine.
Alimemazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Alimemazine.
Methotrimeprazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Methotrimeprazine.
Periciazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Periciazine.
Acepromazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Acepromazine.
Aceprometazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Aceprometazine.
Pipotiazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Pipotiazine.
Thioproperazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Thioproperazine.
BL-1020 The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with BL-1020.
Cyamemazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Cyamemazine.
Methylene blue The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Methylene blue.
Propiopromazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Propiopromazine.
Perazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Perazine.
Butaperazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Butaperazine.
Chlorproethazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Chlorproethazine.
Thiazinam The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Thiazinam.
Dixyrazine The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Dixyrazine.
Perphenazine enanthate The risk or severity of QTc prolongation can be increased when Tafenoquine is combined with Perphenazine enanthate.
Dapsone The risk or severity of adverse effects can be increased when Tafenoquine is combined with Dapsone.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Tafenoquine.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Tafenoquine.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Tafenoquine.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Tafenoquine.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Tafenoquine.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Tafenoquine.
Cymarin The serum concentration of Cymarin can be increased when it is combined with Tafenoquine.
Proscillaridin The serum concentration of Proscillaridin can be increased when it is combined with Tafenoquine.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Tafenoquine.
Lanatoside C The serum concentration of Lanatoside C can be increased when it is combined with Tafenoquine.
Gitoformate The serum concentration of Gitoformate can be increased when it is combined with Tafenoquine.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Tafenoquine.
Peruvoside The serum concentration of Peruvoside can be increased when it is combined with Tafenoquine.
Chlorpromazine The metabolism of Tafenoquine can be decreased when combined with Chlorpromazine.
Cimetidine The metabolism of Tafenoquine can be decreased when combined with Cimetidine.
Cyclosporine The metabolism of Tafenoquine can be decreased when combined with Cyclosporine.
Cholecalciferol The metabolism of Tafenoquine can be decreased when combined with Cholecalciferol.
Fluvoxamine The metabolism of Tafenoquine can be decreased when combined with Fluvoxamine.
Metoprolol The metabolism of Tafenoquine can be decreased when combined with Metoprolol.
Venlafaxine The metabolism of Tafenoquine can be decreased when combined with Venlafaxine.
Terfenadine The metabolism of Tafenoquine can be decreased when combined with Terfenadine.
Clobazam The serum concentration of Tafenoquine can be increased when it is combined with Clobazam.
Clozapine The serum concentration of Tafenoquine can be increased when it is combined with Clozapine.
Quinine The metabolism of Tafenoquine can be decreased when combined with Quinine.
Duloxetine The metabolism of Tafenoquine can be decreased when combined with Duloxetine.
Celecoxib The metabolism of Tafenoquine can be decreased when combined with Celecoxib.
Darifenacin The metabolism of Tafenoquine can be decreased when combined with Darifenacin.
Ritonavir The metabolism of Tafenoquine can be decreased when combined with Ritonavir.
Chloroquine The metabolism of Tafenoquine can be decreased when combined with Chloroquine.
Delavirdine The metabolism of Tafenoquine can be decreased when combined with Delavirdine.
Tranylcypromine The metabolism of Tafenoquine can be decreased when combined with Tranylcypromine.
Terbinafine The metabolism of Tafenoquine can be decreased when combined with Terbinafine.
Tipranavir The metabolism of Tafenoquine can be decreased when combined with Tipranavir.
Ketoconazole The metabolism of Tafenoquine can be decreased when combined with Ketoconazole.
Perhexiline The metabolism of Tafenoquine can be decreased when combined with Perhexiline.
Tegaserod The metabolism of Tafenoquine can be decreased when combined with Tegaserod.
Fusidic acid The metabolism of Tafenoquine can be decreased when combined with Fusidic acid.
Abiraterone The metabolism of Tafenoquine can be decreased when combined with Abiraterone.
Panobinostat The metabolism of Tafenoquine can be decreased when combined with Panobinostat.
Vilazodone The metabolism of Tafenoquine can be decreased when combined with Vilazodone.
Sulfaphenazole The metabolism of Tafenoquine can be decreased when combined with Sulfaphenazole.
Phenylbutyric acid The metabolism of Tafenoquine can be decreased when combined with Phenylbutyric acid.
Manidipine The metabolism of Tafenoquine can be decreased when combined with Manidipine.
Rolapitant The metabolism of Tafenoquine can be decreased when combined with Rolapitant.
Asunaprevir The metabolism of Tafenoquine can be decreased when combined with Asunaprevir.
Pitolisant The metabolism of Tafenoquine can be decreased when combined with Pitolisant.
Rucaparib The metabolism of Tafenoquine can be decreased when combined with Rucaparib.
Ritanserin The metabolism of Tafenoquine can be decreased when combined with Ritanserin.
Rhein The metabolism of Tafenoquine can be decreased when combined with Rhein.
Primaquine The metabolism of Tafenoquine can be decreased when combined with Primaquine.
Imipramine The metabolism of Tafenoquine can be decreased when combined with Imipramine.
Desipramine The metabolism of Tafenoquine can be decreased when combined with Desipramine.
Dosulepin The metabolism of Tafenoquine can be decreased when combined with Dosulepin.
Lorcaserin The metabolism of Tafenoquine can be decreased when combined with Lorcaserin.
Nicardipine The metabolism of Tafenoquine can be decreased when combined with Nicardipine.
Berotralstat The metabolism of Tafenoquine can be decreased when combined with Berotralstat.
Cisapride The metabolism of Tafenoquine can be decreased when combined with Cisapride.
Paroxetine The metabolism of Tafenoquine can be decreased when combined with Paroxetine.
Quinidine The metabolism of Tafenoquine can be decreased when combined with Quinidine.
Cinacalcet The metabolism of Tafenoquine can be decreased when combined with Cinacalcet.
Bupropion The metabolism of Tafenoquine can be decreased when combined with Bupropion.
Orphenadrine The metabolism of Tafenoquine can be decreased when combined with Orphenadrine.
Propafenone The metabolism of Tafenoquine can be decreased when combined with Propafenone.
Halofantrine The metabolism of Tafenoquine can be decreased when combined with Halofantrine.
Glycerol phenylbutyrate The metabolism of Tafenoquine can be decreased when combined with Glycerol phenylbutyrate.
Tipiracil The excretion of Tipiracil can be decreased when combined with Tafenoquine.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25921416
    Rajapakse S, Rodrigo C, Fernando SD: Tafenoquine for preventing relapse in people with Plasmodium vivax malaria. Cochrane Database Syst Rev. 2015 Apr 29;(4):CD010458. doi: 10.1002/14651858.CD010458.pub2.
  • PMID: 27528800
    Ebstie YA, Abay SM, Tadesse WT, Ejigu DA: Tafenoquine and its potential in the treatment and relapse prevention of Plasmodium vivax malaria: the evidence to date. Drug Des Devel Ther. 2016 Jul 26;10:2387-99. doi: 10.2147/DDDT.S61443. eCollection 2016.
  • PMID: 10615272
    Peters W: The evolution of tafenoquine--antimalarial for a new millennium? J R Soc Med. 1999 Jul;92(7):345-52.
  • PMID: 25759576
    Melariri P, Kalombo L, Nkuna P, Dube A, Hayeshi R, Ogutu B, Gibhard L, deKock C, Smith P, Wiesner L, Swai H: Oral lipid-based nanoformulation of tafenoquine enhanced bioavailability and blood stage antimalarial efficacy and led to a reduction in human red blood cell loss in mice. Int J Nanomedicine. 2015 Feb 20;10:1493-503. doi: 10.2147/IJN.S76317. eCollection 2015.
Textbook
  • Grayson L., Cosgrove S., Crowe S., Hope W., McCarthy J., Mills J., Mouton J., Paterson D. (2017). Kucer's the use of antibiotics (7th ed.). CRC Press LLc.

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