Proguanil

DB01131

small molecule approved

Deskripsi

Proguanil is a prophylactic antimalarial drug, which works by stopping the malaria parasite, Plasmodium falciparum and Plasmodium vivax, from reproducing once it is in the red blood cells. It does this by inhibiting the enzyme, dihydrofolate reductase, which is involved in the reproduction of the parasite.

Struktur Molekul 2D

Berat 253.731
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 20 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly and well absorbed in humans following oral doses ranging from 50 to 500 mg.

Metabolisme

Variably metabolized in the liver by cytochrome P450 isoenzymes to the active triazine metabolite, cycloguanil. This variable metabolism of proguanil may have profound clinical importance in poor metabolizers such as the Asian and African populations at risk for malaria infection. Prophylaxis with proguanil may not be effective in these persons because they may not achieve adequate therapeutic levels of the active compound, cycloguanil, even after multiple doses.

Rute Eliminasi

Data eliminasi belum tersedia.

Farmakogenomik

2 Varian
CYP2C19 (rs4244285)

Patients with this genotype have reduced metabolism of proguanil.

CYP2C19 (rs4986893)

Patients with this genotype have reduced metabolism of proguanil.

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

610 Data
Dabrafenib The serum concentration of Proguanil can be decreased when it is combined with Dabrafenib.
Artemether The risk or severity of QTc prolongation can be increased when Proguanil is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Lumefantrine.
Luliconazole The serum concentration of Proguanil can be increased when it is combined with Luliconazole.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Proguanil.
Ritonavir The serum concentration of Proguanil can be decreased when it is combined with Ritonavir.
Efavirenz The serum concentration of Cycloguanil, an active metabolite of Proguanil, can be decreased when used in combination with Efavirenz.
Tetrahydrofolic acid The therapeutic efficacy of Proguanil can be decreased when used in combination with Tetrahydrofolic acid.
Folic acid The therapeutic efficacy of Proguanil can be decreased when used in combination with Folic acid.
Leucovorin The therapeutic efficacy of Proguanil can be decreased when used in combination with Leucovorin.
(6S)-5,6,7,8-tetrahydrofolic acid The therapeutic efficacy of Proguanil can be decreased when used in combination with (6S)-5,6,7,8-tetrahydrofolic acid.
Triglu-5-formyl-tetrahydrofolate The therapeutic efficacy of Proguanil can be decreased when used in combination with Triglu-5-formyl-tetrahydrofolate.
Levoleucovorin The therapeutic efficacy of Proguanil can be decreased when used in combination with Levoleucovorin.
5-methyltetrahydrofolic acid The therapeutic efficacy of Proguanil can be decreased when used in combination with 5-methyltetrahydrofolic acid.
Warfarin Proguanil may increase the anticoagulant activities of Warfarin.
Acenocoumarol Proguanil may increase the anticoagulant activities of Acenocoumarol.
(R)-warfarin Proguanil may increase the anticoagulant activities of (R)-warfarin.
R,S-Warfarin alcohol Proguanil may increase the anticoagulant activities of R,S-Warfarin alcohol.
S,R-Warfarin alcohol Proguanil may increase the anticoagulant activities of S,R-Warfarin alcohol.
(S)-Warfarin Proguanil may increase the anticoagulant activities of (S)-Warfarin.
Thiethylperazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Thiethylperazine.
Promazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Prochlorperazine.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Chlorpromazine.
Triflupromazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Triflupromazine.
Fluphenazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Fluphenazine.
Thioridazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Thioridazine.
Moricizine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Moricizine.
Trifluoperazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Trifluoperazine.
Perphenazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Perphenazine.
Mesoridazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Mesoridazine.
Acetophenazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Acetophenazine.
Promethazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Promethazine.
Alimemazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Alimemazine.
Methotrimeprazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Methotrimeprazine.
Periciazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Periciazine.
Acepromazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Acepromazine.
Aceprometazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Aceprometazine.
Pipotiazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Pipotiazine.
Thioproperazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Thioproperazine.
BL-1020 The risk or severity of QTc prolongation can be increased when Proguanil is combined with BL-1020.
Cyamemazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Cyamemazine.
Methylene blue The risk or severity of QTc prolongation can be increased when Proguanil is combined with Methylene blue.
Propiopromazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Propiopromazine.
Perazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Perazine.
Butaperazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Butaperazine.
Chlorproethazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Chlorproethazine.
Thiazinam The risk or severity of QTc prolongation can be increased when Proguanil is combined with Thiazinam.
Dixyrazine The risk or severity of QTc prolongation can be increased when Proguanil is combined with Dixyrazine.
Perphenazine enanthate The risk or severity of QTc prolongation can be increased when Proguanil is combined with Perphenazine enanthate.
Dapsone The risk or severity of adverse effects can be increased when Proguanil is combined with Dapsone.
Lumacaftor The serum concentration of Proguanil can be decreased when it is combined with Lumacaftor.
Fluvoxamine The metabolism of Proguanil can be decreased when combined with Fluvoxamine.
Ticlopidine The metabolism of Proguanil can be decreased when combined with Ticlopidine.
Chloramphenicol The metabolism of Proguanil can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Proguanil can be decreased when combined with Lansoprazole.
Fluoxetine The metabolism of Proguanil can be decreased when combined with Fluoxetine.
Zafirlukast The metabolism of Proguanil can be decreased when combined with Zafirlukast.
Isoniazid The metabolism of Proguanil can be decreased when combined with Isoniazid.
Stiripentol The metabolism of Proguanil can be decreased when combined with Stiripentol.
Eslicarbazepine acetate The metabolism of Proguanil can be decreased when combined with Eslicarbazepine acetate.
Troglitazone The metabolism of Proguanil can be decreased when combined with Troglitazone.
Nabilone The metabolism of Proguanil can be decreased when combined with Nabilone.
Imatinib The metabolism of Proguanil can be decreased when combined with Imatinib.
Mifepristone The metabolism of Proguanil can be decreased when combined with Mifepristone.
Felbamate The metabolism of Proguanil can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Proguanil can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Proguanil can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Proguanil can be decreased when combined with Medical Cannabis.
Amiodarone The metabolism of Proguanil can be decreased when combined with Amiodarone.
Valproic acid The metabolism of Proguanil can be decreased when combined with Valproic acid.
Quinidine The metabolism of Proguanil can be decreased when combined with Quinidine.
Fluconazole The metabolism of Proguanil can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Proguanil can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Proguanil can be decreased when combined with Nicardipine.
Delavirdine The metabolism of Proguanil can be decreased when combined with Delavirdine.
Miconazole The metabolism of Proguanil can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Proguanil can be decreased when combined with Gemfibrozil.
Sulfaphenazole The metabolism of Proguanil can be decreased when combined with Sulfaphenazole.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Proguanil.
Vemurafenib The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Proguanil.
Apalutamide The serum concentration of Proguanil can be increased when it is combined with Apalutamide.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Proguanil.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Proguanil.
Bortezomib The metabolism of Proguanil can be decreased when combined with Bortezomib.
Pantoprazole The metabolism of Proguanil can be decreased when combined with Pantoprazole.
Citalopram The metabolism of Proguanil can be decreased when combined with Citalopram.
Olanzapine The metabolism of Proguanil can be decreased when combined with Olanzapine.
Omeprazole The metabolism of Proguanil can be decreased when combined with Omeprazole.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Proguanil.
Nilutamide The metabolism of Proguanil can be decreased when combined with Nilutamide.
Esomeprazole The metabolism of Proguanil can be decreased when combined with Esomeprazole.
Ethanol The metabolism of Proguanil can be decreased when combined with Ethanol.
Zonisamide The metabolism of Proguanil can be decreased when combined with Zonisamide.
Memantine The metabolism of Proguanil can be decreased when combined with Memantine.
Etoricoxib The metabolism of Proguanil can be decreased when combined with Etoricoxib.
Oritavancin The metabolism of Proguanil can be decreased when combined with Oritavancin.
Dexlansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Proguanil.
Dovitinib The metabolism of Proguanil can be decreased when combined with Dovitinib.
Sitaxentan The metabolism of Proguanil can be decreased when combined with Sitaxentan.

Target Protein

Dihydrofolate reductase DHFR
Peptide deformylase, mitochondrial PDF
Bifunctional dihydrofolate reductase-thymidylate synthase

Referensi & Sumber

Synthesis reference: Dhananjay Govind Sathe, Harish Kashinath Mondkar, Tanaji Shamrao Jadhav, Nitin Nivrutti Hagavane, "Process of Preparation of Proguanil." U.S. Patent US20110263901, issued October 27, 2011.

Contoh Produk & Brand

Produk: 39 • International brands: 1
Produk
  • Atovaquone and Proguanil HCl
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil HCl
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil HCl
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil HCl
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil Hydrochloride
    Tablet • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil Hydrochloride
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil Hydrochloride
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Atovaquone and Proguanil Hydrochloride
    Tablet, film coated • - • Oral • US • Generic • Approved
Menampilkan 8 dari 39 produk.
International Brands
  • Paludrine

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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