Clinical pharmacokinetics and metabolism of chloroquine

Discussion in 'Canadian Drugs' started by naspor, 19-Mar-2020.

  1. seodigest Well-Known 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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    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. 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. For the past 300 years antimalarial dosage regimens have not been based on pharmacokinetk information. However, now that this information is available, it is appropriate to examine current.

    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

    Clinical pharmacokinetics Pharmacology Education Project, Hydroxychloroquine - Wikipedia

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  7. Hydroxychloroquine has pharmacokinetics similar to that of chloroquine, with rapid gastrointestinal absorption and renal elimination. However, the clinical indications and toxic doses of these drugs slightly differ.

    • New insights on the antiviral effects of chloroquine..
    • Clinical Pharmacokinetics of Antimalarial Drugs SpringerLink.
    • Clinical Pharmacokinetics, Volume 31, Issue 4 - Springer.

    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' Jan 19, 2010 Pharmacokinetics of chloroquine in Thais plasma and red-cell concentrations following an intravenous infusion to healthy subjects and patients with Plasmodium vivax malaria. Br. J. 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.

     
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  9. nmarinin Moderator

    Hydroxychloroquine is widely used in the treatment of post-Lyme arthritis. Efficacy and Safety of Hydroxychloroquine for Treatment of. Hydroxychloroquine Oral Uses, Side Effects, Interactions. Hydroxychloroquine Indications, Side Effects, Warnings.
     
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    Plaquenil Hydroxychloroquine - Side Effects, Dosage.
     
  11. rewo New Member

    Plaquenil Oral Uses, Side Effects, Interactions, Pictures. How to use Plaquenil. Hydroxychloroquine is usually taken with food or milk to prevent stomach upset. The dosage and length of treatment are based on your medical condition and response to therapy. In children, dosage is also based on weight.

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