Peringatan Keamanan

Patients experiencing an overdose may present with headache, drowsiness, visual disturbances, nausea, vomiting, cardiovascular collapse, shock, convulsions, respiratory arrest, cardiac arrest, and hypokalemia.L12051 Overdose should be managed with symptomatic and supportive treatment which may include prompt emesis, gastric lavage, and activated charcoal.L12051

Chloroquine

DB00608

small molecule approved investigational vet_approved

Deskripsi

Chloroquine is an aminoquinolone derivative first developed in the 1940s for the treatment of malaria.A191655 It was the drug of choice to treat malaria until the development of newer antimalarials such as pyrimethamine, artemisinin, and mefloquine.A191787 Chloroquine and its derivative hydroxychloroquine have since been repurposed for the treatment of a number of other conditions including HIV, systemic lupus erythematosus, and rheumatoid arthritis.A192432

The FDA emergency use authorization for hydroxychloroquine and chloroquine in the treatment of COVID-19 was revoked on 15 June 2020.L14312

Chloroquine was granted FDA Approval on 31 October 1949.L12054

Struktur Molekul 2D

Berat 319.872
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of chloroquine is 20-60 days.[A191676]
Volume Distribusi The volume of distribution of chloroquine is 200-800L/kg.[A191676]
Klirens (Clearance) Chloroquine has a total plasma clearance of 0.35-1L/h/kg.[A191676]

Absorpsi

Chloroquine oral solution has a bioavailability of 52-102% and oral tablets have a bioavailability of 67-114%.A191676 Intravenous chloroquine reaches a Cmax of 650-1300µg/L and oral chloroquine reaches a Cmax of 65-128µg/L with a Tmax of 0.5h.A191676

Metabolisme

Chloroquine is N-dealkylated primarily by CYP2C8 and CYP3A4 to N-desethylchloroquine.A38847,A191661,A39300,A191676 It is N-dealkylated to a lesser extent by CYP3A5, CYP2D6, and to an ever lesser extent by CYP1A1.A38847,A191661,A39300,A191676 N-desethylchloroquine can be further N-dealkylated to N-bidesethylchloroquine, which is further N-dealkylated to 7-chloro-4-aminoquinoline.A191676

Rute Eliminasi

Chloroquine is predominantly eliminated in the urine.A191676 50% of a dose is recovered in the urine as unchanged chloroquine, with 10% of the dose recovered in the urine as desethylchloroquine.A191676

Interaksi Makanan

1 Data
  • 1. Take with food. Food reduces irritation and increases bioavailability.

Interaksi Obat

1627 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Chloroquine.
Agalsidase beta The therapeutic efficacy of Agalsidase beta can be decreased when used in combination with Chloroquine.
Succinylcholine The therapeutic efficacy of Succinylcholine can be increased when used in combination with Chloroquine.
Metocurine iodide The therapeutic efficacy of Metocurine iodide can be increased when used in combination with Chloroquine.
Gallamine triethiodide The therapeutic efficacy of Gallamine triethiodide can be increased when used in combination with Chloroquine.
Cisatracurium The therapeutic efficacy of Cisatracurium can be increased when used in combination with Chloroquine.
Rocuronium The therapeutic efficacy of Rocuronium can be increased when used in combination with Chloroquine.
Atracurium besylate The therapeutic efficacy of Atracurium besylate can be increased when used in combination with Chloroquine.
Doxacurium The therapeutic efficacy of Doxacurium can be increased when used in combination with Chloroquine.
Mivacurium The therapeutic efficacy of Mivacurium can be increased when used in combination with Chloroquine.
Decamethonium The therapeutic efficacy of Decamethonium can be increased when used in combination with Chloroquine.
Metocurine The therapeutic efficacy of Metocurine can be increased when used in combination with Chloroquine.
Pancuronium The therapeutic efficacy of Pancuronium can be increased when used in combination with Chloroquine.
Pipecuronium The therapeutic efficacy of Pipecuronium can be increased when used in combination with Chloroquine.
Vecuronium The therapeutic efficacy of Vecuronium can be increased when used in combination with Chloroquine.
Rapacuronium The therapeutic efficacy of Rapacuronium can be increased when used in combination with Chloroquine.
Pyrantel The therapeutic efficacy of Pyrantel can be increased when used in combination with Chloroquine.
Neosaxitoxin The therapeutic efficacy of Neosaxitoxin can be increased when used in combination with Chloroquine.
Atracurium The therapeutic efficacy of Atracurium can be increased when used in combination with Chloroquine.
Gallamine The therapeutic efficacy of Gallamine can be increased when used in combination with Chloroquine.
Alcuronium The therapeutic efficacy of Alcuronium can be increased when used in combination with Chloroquine.
Tubocurarine The therapeutic efficacy of Tubocurarine can be increased when used in combination with Chloroquine.
Artemether The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Lumefantrine.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Chloroquine.
Eliglustat The metabolism of Chloroquine can be decreased when combined with Eliglustat.
Prilocaine The risk or severity of methemoglobinemia can be increased when Chloroquine is combined with Prilocaine.
Mifepristone The serum concentration of Chloroquine can be increased when it is combined with Mifepristone.
Ampicillin The bioavailability of Ampicillin can be decreased when combined with Chloroquine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Chloroquine.
Kaolin Kaolin can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mefloquine The risk or severity of adverse effects can be increased when Chloroquine is combined with Mefloquine.
Mirabegron The serum concentration of Chloroquine can be increased when it is combined with Mirabegron.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum carbonate Lanthanum carbonate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabies virus inactivated antigen, B The therapeutic efficacy of Rabies virus inactivated antigen, B can be decreased when used in combination with Chloroquine.
Rabies virus inactivated antigen, A The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Chloroquine.
Thiethylperazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Thiethylperazine.
Triflupromazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Triflupromazine.
Fluphenazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Fluphenazine.
Moricizine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Moricizine.
Trifluoperazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Trifluoperazine.
Acetophenazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Acetophenazine.
Alimemazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Alimemazine.
Periciazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Periciazine.
Acepromazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Acepromazine.
Aceprometazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Aceprometazine.
Thioproperazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Thioproperazine.
BL-1020 The risk or severity of QTc prolongation can be increased when Chloroquine is combined with BL-1020.
Cyamemazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Cyamemazine.
Propiopromazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Propiopromazine.
Perazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Perazine.
Butaperazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Butaperazine.
Chlorproethazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Chlorproethazine.
Thiazinam The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Thiazinam.
Dixyrazine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Dixyrazine.
Perphenazine enanthate The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Perphenazine enanthate.
Dapsone The risk or severity of methemoglobinemia can be increased when Dapsone is combined with Chloroquine.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Chloroquine.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Chloroquine.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Chloroquine.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Chloroquine.
Cymarin The serum concentration of Cymarin can be increased when it is combined with Chloroquine.
Proscillaridin The serum concentration of Proscillaridin can be increased when it is combined with Chloroquine.
Lanatoside C The serum concentration of Lanatoside C can be increased when it is combined with Chloroquine.
Gitoformate The serum concentration of Gitoformate can be increased when it is combined with Chloroquine.
Peruvoside The serum concentration of Peruvoside can be increased when it is combined with Chloroquine.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Chloroquine.
Anagrelide The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Valproic acid.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Grepafloxacin.
Toremifene The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Toremifene.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Trovafloxacin.
Cocaine The risk or severity of methemoglobinemia can be increased when Chloroquine is combined with Cocaine.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Arsenic trioxide.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Sparfloxacin.
Lithium cation The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Temafloxacin.
Vandetanib The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Vandetanib.
Romidepsin The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Romidepsin.

Target Protein

Atypical chemokine receptor 1 ACKR1
Glutathione S-transferase A2 GSTA2
Tumor necrosis factor TNF
Toll-like receptor 9 TLR9
Glutathione S-transferase GST
High mobility group protein B1 HMGB1
Glutathione S-transferase Mu 1 GSTM1
Angiotensin-converting enzyme 2 ACE2

Referensi & Sumber

Synthesis reference: Andersag, H., Breitner, S.and Jung, H.; U S . Patent 2,233,970; March 4,1941; assigned to Winthrop Chemical Company, Inc.
Artikel (PubMed)
  • PMID: 29033372
    Li C, Zhu X, Ji X, Quanquin N, Deng YQ, Tian M, Aliyari R, Zuo X, Yuan L, Afridi SK, Li XF, Jung JU, Nielsen-Saines K, Qin FX, Qin CF, Xu Z, Cheng G: Chloroquine, a FDA-approved Drug, Prevents Zika Virus Infection and its Associated Congenital Microcephaly in Mice. EBioMedicine. 2017 Oct;24:189-194. doi: 10.1016/j.ebiom.2017.09.034. Epub 2017 Sep 28.
  • PMID: 29150641
    Shiryaev SA, Mesci P, Pinto A, Fernandes I, Sheets N, Shresta S, Farhy C, Huang CT, Strongin AY, Muotri AR, Terskikh AV: Repurposing of the anti-malaria drug chloroquine for Zika Virus treatment and prophylaxis. Sci Rep. 2017 Nov 17;7(1):15771. doi: 10.1038/s41598-017-15467-6.
  • PMID: 32074550
    Gao J, Tian Z, Yang X: Breakthrough: Chloroquine phosphate has shown apparent efficacy in treatment of COVID-19 associated pneumonia in clinical studies. Biosci Trends. 2020 Feb 19. doi: 10.5582/bst.2020.01047.
  • PMID: 31643549
    Authors unspecified: Chloroquine .
  • PMID: 12967198
    Kim KA, Park JY, Lee JS, Lim S: Cytochrome P450 2C8 and CYP3A4/5 are involved in chloroquine metabolism in human liver microsomes. Arch Pharm Res. 2003 Aug;26(8):631-7.
  • PMID: 30873854
    Kaewkhao K, Chotivanich K, Winterberg M, Day NP, Tarning J, Blessborn D: High sensitivity methods to quantify chloroquine and its metabolite in human blood samples using LC-MS/MS. Bioanalysis. 2019 Mar;11(5):333-347. doi: 10.4155/bio-2018-0202. Epub 2019 Mar 15.
  • PMID: 12756207
    Projean D, Baune B, Farinotti R, Flinois JP, Beaune P, Taburet AM, Ducharme J: In vitro metabolism of chloroquine: identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-desethylchloroquine formation. Drug Metab Dispos. 2003 Jun;31(6):748-54.
  • PMID: 3768249
    Ofori-Adjei D, Ericsson O, Lindstrom B, Sjoqvist F: Protein binding of chloroquine enantiomers and desethylchloroquine. Br J Clin Pharmacol. 1986 Sep;22(3):356-8. doi: 10.1111/j.1365-2125.1986.tb02900.x.
Menampilkan 8 dari 18 artikel.

Contoh Produk & Brand

Produk: 26 • International brands: 8
Produk
  • Aralen
    Tablet, film coated • 500 mg/1 • Oral • US • Approved
  • Aralen
    Tablet • 250 mg • Oral • Canada • Approved
  • Chloroquine
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Chloroquine
    Tablet, coated • 500 mg/1 • Oral • US • Generic • Approved
  • Chloroquine
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Chloroquine
    Tablet, coated • 500 mg/1 • Oral • US • Generic • Approved
  • Chloroquine
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Chloroquine
    Tablet, coated • 500 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 26 produk.
International Brands
  • Artrichin
  • Bemaphate
  • Capquin
  • Malarex — Actavis
  • Nivaquine B — Sanofi
  • Resoquine
  • Reumachlor
  • Sanoquin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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