Clinical pharmacokinetics and metabolism of chloroquine

Discussion in 'Chloroquine Pills' started by COH, 15-Mar-2020.

  1. webivwebo Guest

    Clinical pharmacokinetics and metabolism of chloroquine


    Tablet, Oral, as phosphate: Generic: 250 mg [equivalent to chloroquine base 150 mg], 500 mg [equivalent to chloroquine base 300 mg] Binds to and inhibits DNA and RNA polymerase; interferes with metabolism and hemoglobin utilization by parasites; inhibits prostaglandin effects; chloroquine concentrates within parasite acid vesicles and raises internal p H resulting in inhibition of parasite growth; may involve aggregates of ferriprotoporphyrin IX acting as chloroquine receptors causing membrane damage; may also interfere with nucleoprotein synthesis Rapid and almost complete Widely in body tissues including eyes, heart, kidneys, liver, leukocytes, and lungs where retention is prolonged Partially hepatic to main metabolite, desethylchloroquine Urine (~70%; ~35% as unchanged drug); acidification of urine increases elimination; small amounts of drug may be present in urine months following discontinuation of therapy Serum: Oral: Within 1-2 hours 3 to 5 days ~55% Malaria: Treatment of uncomplicated malaria due to susceptible strains of Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, and Plasmodium falciparum; prophylaxis of malaria (in geographic areas where chloroquine resistance is not present). Limitations of use: Chloroquine does not prevent relapses in patients with vivax or ovale malaria (not effective against exoerythrocytic forms). Extraintestinal amebiasis: Treatment of extraintestinal amebiasis. Data from a prospective, randomized, controlled, double-blind clinical trial supports the use of chloroquine in the treatment of discoid lupus erythematosus .

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    Clinical Pharmacokinetics and Metabolism of Chloroquine. Julie Ducharme, Dr Robert Farinotti Pages 257-274. Erratum. Erratum to Pharmacokinetics, metabolism amd interactions of acid pump inhibitors focus on omeprazoie, iansoprazoie and pantoprazoie. Clinical Pharmacokinetics of Alfentanil, Fentanyl and Sufentanil. Dr Jens Scholz, Markus. Hydroxychloroquine HCQ and chloroquine CQ are well absorbed 0.7-0.8 bioavailability when given orally. Severe malnutrition such as kwashiorkor effects absorption but diahrrea does not. Both HCQ and CQ have prolonged half-lives, between 40 and 50 days, and low blood clearance e.g. hydroxychloroquine's blood clearance is 96 ml/min. Data from a prospective, randomized, controlled, double-blind clinical trial supports the use of chloroquine in the treatment of discoid lupus erythematosus Bezerra 2005. Chloroquine also demonstrated a reduction in epidermal vascular endothelial growth factor VEGF expression resulting in a significant reduction in the median number of CD34+ dermal blood vessels Lesiak 2009.

    Hypersensitivity to chloroquine, 4-aminoquinoline compounds, or any component of the formulation; the presence of retinal or visual field changes of any etiology (when used for indications other than acute malaria) Note: Chloroquine is currently under investigation for use in the treatment of COVID-19. Do not use for the treatment of complicated malaria (high-grade parasitemia and/or complications [eg, cerebral malaria, acute renal failure]) or for malaria prophylaxis in areas where chloroquine resistance occurs (resistance to chloroquine is widespread in P. Additional data may be necessary to further define the role of chloroquine in the treatment of this condition.

    Clinical pharmacokinetics and metabolism of chloroquine

    Chloroquine C18H26ClN3 - PubChem, Pharmacokinetics of hydroxychloroquine and chloroquine during.

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  7. The pharmacokinetics of piperaquine was characterized by a low clearance, a large volume of distribution and a long terminal half-life. Piperaquine displayed a low biliary clearance and less than 1% of the total dose was recovered in urine. The absolute oral bioavailability was approximately 50%.

    • Pharmacokinetics and Metabolism of the Antimalarial..
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    Pharmacokinetics Hydroxychloroquine has similar pharmacokinetics to chloroquine, with rapid gastrointestinal absorption and elimination by the kidneys. Cytochrome P450 enzymes CYP2D6, 2C8, 3A4 and 3A5 metabolize hydroxychloroquine to N -desethylhydroxychloroquine. Studies on the pharmacokinetics of Primaquine Article PDF Available in Bulletin of the World Health Organisation 593407-12 February 1981 with 89 Reads How we measure 'reads' Eight healthy volunteers who had not taken chloroquine 2 to 12 months previously participated in a single dose study designed to evaluate the pharmacokinetics of chloroquine and some of its metabolites. Each subject received two tablets of chloroquine sulfate 300 mg base only.

     
  8. qdprocomua Moderator

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  9. OLEGz New Member

    Chloroquine Resistance in Plasmodium falciparum Malaria. Plasmodium falciparum chloroquine resistance is a major cause of worldwide increases in malaria mortality and morbidity. Recent laboratory and clinical studies have associated chloroquine resistance with point mutations in the gene pfcrt. However, direct proof of a causal relationship has remained elusive and most models have posited a multigenic basis of resistance.

    Malaria - Chapter 4 - 2020 Yellow Book Travelers' Health.
     
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