Clinical pharmacokinetics and metabolism of chloroquine

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  1. elek7 New Member

    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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    Excretion of Chloroquine is quite slow,but is increased by acidification of the urine. Chloroquine is deposited in the tissues in considerable amounts. In animals, from 200 to 700 times the plasma concentration may be found in the liver,spleen, kidney, and lung; leukocytes also concentrate the drug. The pharmacokinetics of chloroquine and its main metabolite desethylchloroquine have been carried out in volunteers with and without chloroquine‐induced pruritus. It was shown that the volunteers with pruritus tended to metabolize chloroquine slower than the volunteers without pruritus because the metabolic ratio was lower in the volunteers with pruritus than that in the volunteers without pruritus. Ducharme J, Farinotti R Clinical pharmacokinetics and metabolism of chloroquine. Focus on recent advancements. Clin Pharmacokinet. 1996 Oct;314257-74. doi 10.2165/00003088-199631040-00003.

    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

    Pharmacokinetics of hydroxychloroquine and chloroquine during., The disposition of chloroquine and its main metabolite.

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  4. 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.

    • Pharmacokinetics of Chloroquine and Some of Its..
    • Reaction Chloroquine to 1 product - DrugBank.
    • Pharmacokinetics/pharmacodynamics of chloroquine and..

    Recent reports have highlighted that chloroquine CQ is capable of inhibiting ZIKV endocytosis in brain cells. We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an optimal maternal/fetal dosing regimen to prevent ZIKV endocytosis in brain cells. A recent case report showed that treatment with remdesivir improved the clinical condition of the first patient infected by SARS-CoV-2 in the United States 2, and a phase III clinical trial of. This paper presents the current state of knowledge on chloroquine disposition, with special emphasis on stereoselectivity and microsomal metabolism. In addition, the impact of the patient’s physiopathological status and ethnic origin on chloroquine pharmacokinetics is discussed. In humans, chloroquine concentrations decline multiexponentially.

     
  5. DeALZ Well-Known Member

    This article focuses upon hydroxychloroquine retinopathy. Chloroquine was originally used as an anti-malarial therapeutic. Hydroxychloroquine toxicity - EyeWiki Plaquenil Toxicity - Symptoms, Treatment, Risk Factors. Chloroquine and Hydroxychloroquine Toxicity - emedicine.qa01.
     
  6. D-Ark-M User

    Chloroquine has long been used in the treatment or prevention of malaria from Plasmodium vivax, P. malariae, excluding the malaria parasite Plasmodium falciparum, for it started to develop widespread resistance to it. Chloroquine triggers Epstein-Barr virus replication through. The return of chloroquine-susceptible Plasmodium falciparum. Chloroquine & Hydroxychloroquine supporting chemo.
     
  7. violetgorman Guest

    Plaquenil Hydroxychloroquine - Side Effects, Dosage. Plaquenil is the brand name for the prescription drug hydroxychloroquine. It's used to treat and prevent malaria infection, and to reduce symptoms and progression of autoimmune diseases such as.

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  8. Taboo XenForo Moderator

    Hydroxychloroquine Dosage Guide with Precautions - Side effects may require reduction in the initial dose for 5 to 10 days; the dose may then gradually be increased to the optimum response level.-The compound is cumulative in action and will require several weeks to exert its beneficial therapeutic effects, whereas minor side effects may occur relatively early.

    Plaquenil Dosage. Am I starting with too much.