Peringatan Keamanan

Patients experiencing an overdose may present with headache, drowsiness, visual disturbances, cardiovascular collapse, convulsions, hypokalemia, rhythm and conduction disorders including QT prolongation, torsades de pointes, ventricular tachycardia, and ventricular fibrillation.L8072 This may progress to sudden respiratory and cardiac arrest.L8072 Overdose should be treated with immediate gastric lavage and activated charcoal at a dose of at least 5 times the hydroxychloroquine dose within 30 minutes.A183047,L8072 Parenteral diazepam may be given to treat cardiotoxicity, transfusion may reduce serum concentrations of drug, patients should be monitored for at least 6 hours, fluids should be given, and ammonium chloride should be given to acidify urine and promote urinary excretion.L8072 Patients may also be given epinephrine.A198852

Hydroxychloroquine

DB01611

small molecule approved

Deskripsi

Hydroxychloroquine is a racemic mixture consisting of an R and S enantiomer.A183047 Hydroxychloroquine is an aminoquinoline like chloroquine.L8072 It is a commonly prescribed medication in the treatment of uncomplicated malaria, rheumatoid arthritis, chronic discoid lupus erythematosus, and systemic lupus erythematosus.L8072 Hydroxychloroquine is also used for the prophylaxis of malaria in regions where chloroquine resistance is unlikely.L8072 It was developed during World War II as a derivative of quinacrine with less severe side effects.A183092 Chloroquine and hydroxychloroquine are both being investigated for the treatment of SARS-CoV-2.A192132

The FDA emergency use authorization for hydroxychloroquine and chloroquine in the treatment of COVID-19 was revoked on 15 June 2020.L14312

Hydroxychloroquine was granted FDA approval on 18 April 1955.L8072

A recent study reported a fatality in the group being treated with hydroxychloroquine for COVID-19.A192546

Struktur Molekul 2D

Berat 335.872
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) A half-life of 123.5 days in plasma was observed following a single 200 mg oral PLAQUENIL dose to healthy male volunteers. Urine hydroxychloroquine levels were still detectable after 3 months with approximately 10% of the dose excreted as the parent drug. Results following a single dose of a 200 mg tablet versus i.v. infusion (155 mg), demonstrated a half-life of about 40 days and a large volume of distribution. Following chronic oral administration of hydroxychloroquine, the absorption half-life was approximately 3 to 4 hours and the terminal half-life ranged from 40 to 50 days.[L47576]
Volume Distribusi Hydroxychloroquine is extensively distributed to tissues; it has a volume of distribution of 5522L from blood and 44,257L from plasma.[L47576,A183047]
Klirens (Clearance) The clearance of hydroxychloroquine is 96mL/min.[A183047] Renal clearance of unchanged drug was approximately 16% to 30%.[L47576]

Absorpsi

Hydroxychloroquine is 67-74% bioavailable.A183047 Bioavailability of the R and S enantiomers were not significantly different.A183047 Following a single 200 mg oral dose of hydroxychloroquine to healthy male volunteers, whole blood hydroxychloroquine Cmax was 129.6 ng/mL (plasma Cmax was 50.3 ng/mL) with Tmax of 3.3 hours (plasma Tmax 3.7 hours). Following a single oral hydroxychloroquine dose of 200 mg, the mean fraction of the dose absorbed was 0.74 (compared to the administration of 155 mg of hydroxychloroquine intravenous infusion). Peak blood concentrations of metabolites were observed at the same time as peak levels of hydroxychloroquine.L47576 After administration of single 155 mg and 310 mg intravenous doses, peak blood concentrations ranged from 1161 ng/mL to 2436 ng/mL (mean 1918 ng/mL) following the 155 mg infusion and 6 months following the 310 mg infusion. Pharmacokinetic parameters were not significantly different over the therapeutic dose range of 155 mg and 310 mg indicating linear kinetics.L47576 In patients with rheumatoid arthritis, there was large variability as to the fraction of the dose absorbed (i.e. 30 to 100%), and mean hydroxychloroquine levels were significantly higher in patients with less disease activity.L47576

Metabolisme

Hydroxychloroquine is N-dealkylated by CYP3A4 to the active metabolite desethylhydroxychloroquine, as well as the inactive metabolites desethylchloroquine and bidesethylchloroquine.A183056,A183059 Desethylhydroxychloroquine is the major metabolite.L8072

Rute Eliminasi

40-50% of hydroxychloroquine is excreted renally, while only 16-21% of a dose is excreted in the urine as unchanged drug.A183047 5% of a dose is sloughed off in skin and 24-25% is eliminated through the feces.T671

Interaksi Makanan

1 Data
  • 1. Take with food. Take with a meal or glass of milk.

Interaksi Obat

1379 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Hydroxychloroquine.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Hydroxychloroquine.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Hydroxychloroquine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Hydroxychloroquine.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Hydroxychloroquine.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Hydroxychloroquine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Hydroxychloroquine.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Hydroxychloroquine.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Hydroxychloroquine.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Hydroxychloroquine.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Hydroxychloroquine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Hydroxychloroquine.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Hydroxychloroquine.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Hydroxychloroquine.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Hydroxychloroquine.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Hydroxychloroquine.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Hydroxychloroquine.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Hydroxychloroquine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Hydroxychloroquine.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Hydroxychloroquine.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Hydroxychloroquine.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Hydroxychloroquine.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Hydroxychloroquine.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Hydroxychloroquine.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Hydroxychloroquine.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Hydroxychloroquine.
Cladribine Hydroxychloroquine may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Hydroxychloroquine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Hydroxychloroquine.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Hydroxychloroquine.
Chlorambucil The risk or severity of seizure can be increased when Hydroxychloroquine is combined with Chlorambucil.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Hydroxychloroquine.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Hydroxychloroquine.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Hydroxychloroquine.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Hydroxychloroquine.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Hydroxychloroquine.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Hydroxychloroquine.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Hydroxychloroquine.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Hydroxychloroquine.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Hydroxychloroquine.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Hydroxychloroquine.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Hydroxychloroquine.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Hydroxychloroquine.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Hydroxychloroquine.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Hydroxychloroquine.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Hydroxychloroquine.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Hydroxychloroquine.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Hydroxychloroquine.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Hydroxychloroquine.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Hydroxychloroquine.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Hydroxychloroquine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Hydroxychloroquine.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Hydroxychloroquine.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Hydroxychloroquine.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Hydroxychloroquine.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Hydroxychloroquine.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Hydroxychloroquine.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Hydroxychloroquine.
Linezolid The risk or severity of seizure can be increased when Hydroxychloroquine is combined with Linezolid.
Imatinib The serum concentration of Hydroxychloroquine can be increased when it is combined with Imatinib.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Hydroxychloroquine.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Hydroxychloroquine.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Hydroxychloroquine.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Hydroxychloroquine.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Hydroxychloroquine.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Hydroxychloroquine.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Hydroxychloroquine.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Hydroxychloroquine.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Hydroxychloroquine.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Hydroxychloroquine.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Hydroxychloroquine.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Hydroxychloroquine.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Hydroxychloroquine.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Hydroxychloroquine.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Hydroxychloroquine.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Hydroxychloroquine.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Hydroxychloroquine.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Hydroxychloroquine.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Hydroxychloroquine.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Hydroxychloroquine.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Hydroxychloroquine.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Hydroxychloroquine.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Hydroxychloroquine.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Hydroxychloroquine.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Hydroxychloroquine.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Hydroxychloroquine.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Hydroxychloroquine.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Hydroxychloroquine.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Hydroxychloroquine.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Hydroxychloroquine.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Hydroxychloroquine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Hydroxychloroquine.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Hydroxychloroquine.
Ifosfamide The risk or severity of adverse effects can be increased when Ifosfamide is combined with Hydroxychloroquine.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Hydroxychloroquine.
Mitoxantrone The risk or severity of adverse effects can be increased when Mitoxantrone is combined with Hydroxychloroquine.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Hydroxychloroquine.
Budesonide The risk or severity of adverse effects can be increased when Budesonide is combined with Hydroxychloroquine.
Dexamethasone The risk or severity of adverse effects can be increased when Dexamethasone is combined with Hydroxychloroquine.
Docetaxel The risk or severity of adverse effects can be increased when Docetaxel is combined with Hydroxychloroquine.

Target Protein

Toll-like receptor 7 TLR7
Toll-like receptor 9 TLR9
DNA
Angiotensin-converting enzyme 2 ACE2

Referensi & Sumber

Synthesis reference: U.S. Patent 2,546,658.
Artikel (PubMed)
  • PMID: 19188392
    Lim HS, Im JS, Cho JY, Bae KS, Klein TA, Yeom JS, Kim TS, Choi JS, Jang IJ, Park JW: Pharmacokinetics of hydroxychloroquine and its clinical implications in chemoprophylaxis against malaria caused by Plasmodium vivax. Antimicrob Agents Chemother. 2009 Apr;53(4):1468-75. doi: 10.1128/AAC.00339-08. Epub 2009 Feb 2.
  • PMID: 8803904
    Furst DE: Pharmacokinetics of hydroxychloroquine and chloroquine during treatment of rheumatic diseases. Lupus. 1996 Jun;5 Suppl 1:S11-5.
  • PMID: 29438998
    Collins KP, Jackson KM, Gustafson DL: Hydroxychloroquine: A Physiologically-Based Pharmacokinetic Model in the Context of Cancer-Related Autophagy Modulation. J Pharmacol Exp Ther. 2018 Jun;365(3):447-459. doi: 10.1124/jpet.117.245639. Epub 2018 Feb 8.
  • PMID: 8278823
    Fox RI: Mechanism of action of hydroxychloroquine as an antirheumatic drug. Semin Arthritis Rheum. 1993 Oct;23(2 Suppl 1):82-91.
  • PMID: 1474861
    Chou AC, Fitch CD: Heme polymerase: modulation by chloroquine treatment of a rodent malaria. Life Sci. 1992;51(26):2073-8. doi: 10.1016/0024-3205(92)90158-l.
  • PMID: 29883308
    Shippey EA, Wagler VD, Collamer AN: Hydroxychloroquine: An old drug with new relevance. Cleve Clin J Med. 2018 Jun;85(6):459-467. doi: 10.3949/ccjm.85a.17034.
  • PMID: 32171740
    Devaux CA, Rolain JM, Colson P, Raoult D: New insights on the antiviral effects of chloroquine against coronavirus: what to expect for COVID-19? Int J Antimicrob Agents. 2020 Mar 11:105938. doi: 10.1016/j.ijantimicag.2020.105938.
  • PMID: 16115318
    Vincent MJ, Bergeron E, Benjannet S, Erickson BR, Rollin PE, Ksiazek TG, Seidah NG, Nichol ST: Chloroquine is a potent inhibitor of SARS coronavirus infection and spread. Virol J. 2005 Aug 22;2:69. doi: 10.1186/1743-422X-2-69.
Menampilkan 8 dari 11 artikel.
Textbook
  • ISBN: 9781493905973
    Browning, David J. (2014). Hydroxychloroquine and chloroquine retinopathy. Springer.

Contoh Produk & Brand

Produk: 132 • International brands: 4
Produk
  • Ach-hydroxychloroquine Sulfate
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Ag-hydroxychloroquine
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Apo-hydroxyquine
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Hydroxychloroquine
    Tablet • 200 mg • Oral • Canada • Approved
  • Hydroxychloroquine
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Hydroxychloroquine Sulfate
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Hydroxychloroquine Sulfate
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
  • Hydroxychloroquine Sulfate
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 132 produk.
International Brands
  • Dolquine — Inmunosyn
  • HCQS — Medigroup
  • Polirreumin — TRB
  • Quensyl — Sanofi

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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