Peringatan Keamanan

The acute toxicity of praziquantel is relatively low, as demonstrated by oral LD50 values ranging between 200 - 2976 mg/kg in various species.L40268

Published studies have not identified an association between praziquantel use during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies conducted in pregnant rats and rabbits no adverse developmental outcomes were observed with oral administration of praziquantel during organogenesis at approximately 0.65 times (rats) or 1.3 times (rabbits) the highest recommended human daily dose of 75 mg/kg/day, based on body surface area.L50021

Mutagenicity studies of praziquantel published in the scientific literature are inconclusive. Long-term oral carcinogenicity studies in rats and golden hamsters did not reveal any carcinogenic effect at doses up to 250 mg/kg/day (about half of the human daily dose based on body surface area). Praziquantel had no effect on fertility and general reproductive performance of male and female rats when given at oral doses ranging from 30 to 300 mg/kg body weight (up to 0.65 times the human daily dose based on body surface area).L50021

Praziquantel

DB01058

small molecule approved investigational vet_approved

Deskripsi

Praziquantel is a pyrazino-isoquinolein derivative from the thioxantonic group used as a broad anthelmintic spectrum. Specifically, it is known as a treatment of trematodes and cestodes infections such as schistosomiasis, taeniasis, and cysticercosis.A263201 The efficacy of praziquantel in treating parasitic flatworms infection with low cost (~US$0.20 drug cost to treat a child) makes it an integral to WHO's plan to eliminate schistosomiasis by 2030.A263206,A263211 Despite being approved since 1980, the exact mechanism of action is yet to be elucidated.A263211

Struktur Molekul 2D

Berat 312.4061
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration, the elimination half-life of praziquantel in serum ranges between 0.8 to 1.5 hours.[L50021]
Volume Distribusi Following a single oral dose of 40 mg/kg of praziquantel in healthy volunteers, the volume of distribution was estimated to be 7695 ± 2716 L.[A263181]
Klirens (Clearance) Following a single oral dose of 40 mg/kg of praziquantel in healthy volunteers, the clearance was estimated to be 11.4 ± 2.8 L/kg/h.[A263181]

Absorpsi

After oral administration of praziquantel, about 80% of the dose is absorbed. In subjects with normal hepatic function who received 40 mg/kg of praziquantel under fasting conditions, the mean ± SD Cmax and AUC were 0.83 ± 0.52 µg/mL and 3.02 ± 0.59 µg/mL x hr. The Tmax was 1.48 ± 0.74 hours.L50021

Metabolisme

Praziquantel is rapidly metabolized by the cytochrome P450 enzyme system and undergoes a first-pass effect after oral administration.L50021

Rute Eliminasi

Approximately 80% of an oral dose of praziquantel is excreted in the kidneys, almost exclusively (greater than 99%) in the form of praziquantel metabolites.L50021

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Praziquantel is metabolized by CYP450 enzymes.
  • 2. Take with food. Take tablets with water during meals.

Interaksi Obat

616 Data
Deferasirox The serum concentration of Praziquantel can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Praziquantel can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Praziquantel can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Praziquantel can be decreased when it is combined with Teriflunomide.
Dabrafenib The serum concentration of Praziquantel can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Praziquantel can be increased when it is combined with Luliconazole.
Abiraterone The serum concentration of Praziquantel can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Praziquantel can be increased when combined with Cyproterone acetate.
Albendazole The metabolism of Praziquantel can be increased when combined with Albendazole.
Caffeine The metabolism of Praziquantel can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Praziquantel can be decreased when combined with Moxifloxacin.
Lidocaine The metabolism of Praziquantel can be decreased when combined with Lidocaine.
Mexiletine The metabolism of Praziquantel can be decreased when combined with Mexiletine.
Alosetron The metabolism of Praziquantel can be decreased when combined with Alosetron.
Gatifloxacin The metabolism of Praziquantel can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Praziquantel can be decreased when combined with Simeprevir.
Dosulepin The metabolism of Praziquantel can be decreased when combined with Dosulepin.
Lobeglitazone The metabolism of Praziquantel can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Praziquantel can be decreased when combined with Pazufloxacin.
Osilodrostat The metabolism of Praziquantel can be decreased when combined with Osilodrostat.
Fluvoxamine The metabolism of Praziquantel can be decreased when combined with Fluvoxamine.
Ticlopidine The metabolism of Praziquantel can be decreased when combined with Ticlopidine.
Chloramphenicol The metabolism of Praziquantel can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Praziquantel can be decreased when combined with Lansoprazole.
Fluoxetine The metabolism of Praziquantel can be decreased when combined with Fluoxetine.
Zafirlukast The metabolism of Praziquantel can be decreased when combined with Zafirlukast.
Isoniazid The metabolism of Praziquantel can be decreased when combined with Isoniazid.
Miconazole The metabolism of Praziquantel can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Praziquantel can be decreased when combined with Gemfibrozil.
Clomipramine The metabolism of Praziquantel can be decreased when combined with Clomipramine.
Imipramine The metabolism of Praziquantel can be decreased when combined with Imipramine.
Eslicarbazepine acetate The metabolism of Praziquantel can be decreased when combined with Eslicarbazepine acetate.
Osimertinib The serum concentration of Praziquantel can be decreased when it is combined with Osimertinib.
Vemurafenib The serum concentration of Praziquantel can be increased when it is combined with Vemurafenib.
Pitolisant The serum concentration of Praziquantel can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Praziquantel can be increased when combined with Metreleptin.
Cimetidine The metabolism of Praziquantel can be decreased when combined with Cimetidine.
Isavuconazole The metabolism of Praziquantel can be decreased when combined with Isavuconazole.
Erythromycin The serum concentration of Praziquantel can be increased when it is combined with Erythromycin.
Nabiximols The metabolism of Praziquantel can be decreased when combined with Nabiximols.
Troglitazone The metabolism of Praziquantel can be decreased when combined with Troglitazone.
Fluticasone propionate The metabolism of Praziquantel can be decreased when combined with Fluticasone propionate.
Aprepitant The metabolism of Praziquantel can be decreased when combined with Aprepitant.
Fluticasone furoate The metabolism of Fluticasone furoate can be decreased when combined with Praziquantel.
Fluticasone The metabolism of Praziquantel can be decreased when combined with Fluticasone.
Medical Cannabis The metabolism of Praziquantel can be decreased when combined with Medical Cannabis.
Curcumin sulfate The metabolism of Praziquantel can be decreased when combined with Curcumin sulfate.
Methylene blue The metabolism of Praziquantel can be decreased when combined with Methylene blue.
Clofazimine The metabolism of Praziquantel can be decreased when combined with Clofazimine.
Pralsetinib The metabolism of Praziquantel can be decreased when combined with Pralsetinib.
Levoketoconazole The metabolism of Praziquantel can be decreased when combined with Levoketoconazole.
Acalabrutinib The metabolism of Praziquantel can be decreased when combined with Acalabrutinib.
Icotinib The metabolism of Praziquantel can be increased when combined with Icotinib.
Budesonide The metabolism of Praziquantel can be increased when combined with Budesonide.
Dexamethasone acetate The metabolism of Praziquantel can be increased when combined with Dexamethasone acetate.
Reserpine The metabolism of Praziquantel can be increased when combined with Reserpine.
Beclomethasone dipropionate The metabolism of Praziquantel can be increased when combined with Beclomethasone dipropionate.
Daunorubicin The metabolism of Praziquantel can be increased when combined with Daunorubicin.
Thalidomide The metabolism of Praziquantel can be increased when combined with Thalidomide.
Oxcarbazepine The metabolism of Praziquantel can be increased when combined with Oxcarbazepine.
Triamcinolone The metabolism of Praziquantel can be increased when combined with Triamcinolone.
Cortisone acetate The metabolism of Praziquantel can be increased when combined with Cortisone acetate.
Paramethasone The metabolism of Praziquantel can be increased when combined with Paramethasone.
Fluprednidene The metabolism of Praziquantel can be increased when combined with Fluprednidene.
Meprednisone The metabolism of Praziquantel can be increased when combined with Meprednisone.
Dexamethasone isonicotinate The metabolism of Praziquantel can be increased when combined with Dexamethasone isonicotinate.
Cortivazol The metabolism of Praziquantel can be increased when combined with Cortivazol.
Prednylidene The metabolism of Praziquantel can be increased when combined with Prednylidene.
Cloprednol The metabolism of Praziquantel can be increased when combined with Cloprednol.
Mometasone furoate The metabolism of Praziquantel can be increased when combined with Mometasone furoate.
Prednisolone phosphate The metabolism of Praziquantel can be increased when combined with Prednisolone phosphate.
Prednisolone hemisuccinate The metabolism of Praziquantel can be increased when combined with Prednisolone hemisuccinate.
Prednisone acetate The metabolism of Praziquantel can be increased when combined with Prednisone acetate.
Clocortolone acetate The metabolism of Praziquantel can be increased when combined with Clocortolone acetate.
Melengestrol acetate The metabolism of Praziquantel can be increased when combined with Melengestrol acetate.
Betamethasone phosphate The metabolism of Praziquantel can be increased when combined with Betamethasone phosphate.
Cortisone The metabolism of Praziquantel can be increased when combined with Cortisone.
Clobetasol propionate The metabolism of Praziquantel can be increased when combined with Clobetasol propionate.
Fluocinonide The metabolism of Praziquantel can be increased when combined with Fluocinonide.
Mometasone The metabolism of Praziquantel can be increased when combined with Mometasone.
Fluocortolone The metabolism of Praziquantel can be increased when combined with Fluocortolone.
Difluocortolone The metabolism of Praziquantel can be increased when combined with Difluocortolone.
Betamethasone The metabolism of Praziquantel can be increased when combined with Betamethasone.
Dutasteride The metabolism of Dutasteride can be decreased when combined with Praziquantel.
Dexloxiglumide The metabolism of Dexloxiglumide can be decreased when combined with Praziquantel.
Azimilide The metabolism of Azimilide can be decreased when combined with Praziquantel.
Nevirapine The metabolism of Praziquantel can be decreased when combined with Nevirapine.
Dapsone The metabolism of Praziquantel can be decreased when combined with Dapsone.
Levonorgestrel The metabolism of Praziquantel can be decreased when combined with Levonorgestrel.
Nisoldipine The metabolism of Praziquantel can be decreased when combined with Nisoldipine.
Alprazolam The metabolism of Praziquantel can be decreased when combined with Alprazolam.
Cerivastatin The metabolism of Praziquantel can be decreased when combined with Cerivastatin.
Buspirone The metabolism of Praziquantel can be decreased when combined with Buspirone.
Oxycodone The metabolism of Praziquantel can be decreased when combined with Oxycodone.
Dextromethorphan The metabolism of Praziquantel can be decreased when combined with Dextromethorphan.
Lercanidipine The metabolism of Praziquantel can be decreased when combined with Lercanidipine.
Cisapride The metabolism of Praziquantel can be decreased when combined with Cisapride.
Chloroquine The metabolism of Praziquantel can be decreased when combined with Chloroquine.
Simvastatin The metabolism of Praziquantel can be decreased when combined with Simvastatin.
Trazodone The metabolism of Praziquantel can be decreased when combined with Trazodone.

Target Protein

Hematopoietic prostaglandin D synthase HPGDS
Schistosome calcium ion (Ca2+) channels

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18978535
    Doenhoff MJ, Cioli D, Utzinger J: Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis. Curr Opin Infect Dis. 2008 Dec;21(6):659-67. doi: 10.1097/QCO.0b013e328318978f.
  • PMID: 18202444
    McManus DP, Loukas A: Current status of vaccines for schistosomiasis. Clin Microbiol Rev. 2008 Jan;21(1):225-42. doi: 10.1128/CMR.00046-07.
  • PMID: 24390933
    Olliaro P, Delgado-Romero P, Keiser J: The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer). J Antimicrob Chemother. 2014 Apr;69(4):863-70. doi: 10.1093/jac/dkt491. Epub 2014 Jan 2.
  • PMID: 2124391
    Mandour ME, el Turabi H, Homeida MM, el Sadig T, Ali HM, Bennett JL, Leahey WJ, Harron DW: Pharmacokinetics of praziquantel in healthy volunteers and patients with schistosomiasis. Trans R Soc Trop Med Hyg. 1990 May-Jun;84(3):389-93. doi: 10.1016/0035-9203(90)90333-a.
  • PMID: 36375598
    Nogueira RA, Lira MGS, Lica ICL, Frazao GCCG, Dos Santos VAF, Filho ACCM, Rodrigues JGM, Miranda GS, Carvalho RC, Nascimento FRF: Praziquantel: An update on the mechanism of its action against schistosomiasis and new therapeutic perspectives. Mol Biochem Parasitol. 2022 Nov;252:111531. doi: 10.1016/j.molbiopara.2022.111531. Epub 2022 Nov 11.
  • PMID: 34936384
    Park SK, Friedrich L, Yahya NA, Rohr CM, Chulkov EG, Maillard D, Rippmann F, Spangenberg T, Marchant JS: Mechanism of praziquantel action at a parasitic flatworm ion channel. Sci Transl Med. 2021 Dec 22;13(625):eabj5832. doi: 10.1126/scitranslmed.abj5832. Epub 2021 Dec 22.
  • PMID: 31787521
    Park SK, Marchant JS: The Journey to Discovering a Flatworm Target of Praziquantel: A Long TRP. Trends Parasitol. 2020 Feb;36(2):182-194. doi: 10.1016/j.pt.2019.11.002. Epub 2019 Nov 29.

Contoh Produk & Brand

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