Clinical pharmacokinetics and metabolism of chloroquine

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  1. BARTONUA 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 .

    Plaquenil side effects teeth Chloroquine lysosome acidification

    Metabolism Chloroquine undergoes metabolism by hepatic mechanisms. The main active metabolite is desethylchloroquine. Plasma half-life of desethylchloroquine is similar to chloroquine. The cytochrome P450 enzymes CYP2D6 17, 19 and CYP2C8 are known to participate in the metabolism of the primaquine and chloroquine, respectively. Two SNPs G416Ars11572080 and A805T rs11572103 were genotyped in the CYP2C8 gene. 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.

    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

    Hydroxychloroquine, a less toxic derivative of chloroquine., Pharmacokinetics/pharmacodynamics of chloroquine and.

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  6. Chloroquine is a medication used to prevent and to treat malaria in areas where malaria is known to be sensitive to its effects. Certain types of malaria, resistant strains, and complicated cases typically require different or additional medication. Occasionally it is used for amebiasis that is occurring outside the intestines, rheumatoid arthritis, and lupus erythematosus.

    • Chloroquine - Wikipedia.
    • The disposition of chloroquine and its main metabolite..
    • Clinical pharmacokinetics Pharmacology Education Project.

    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. 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.

     
  7. ivo_ivan Guest

    Lupus symptoms vary widely from one person to another; therefore, the best treatment is decided individually by your physician according to your specific condition. New Plaquenil Guidelines - Plaquenil Toxicity - Symptoms, Treatment, Risk Factors. Recommendations on Screening for Chloroquine and.
     
  8. fortress Moderator

    Aralen Side Effects - Drugs Home Page An Introduction to Aralen Side Effects Just like any medicine, Aralen ® chloroquine phosphate can cause side effects. However, not everyone who takes the medication will have problems. In fact, most people tolerate it quite well. If side effects do occur, in many cases, they are minor and either require no treatment or are treated easily by.

    Chloroquine MedlinePlus Drug Information
     
  9. wastemaster Guest

    Hydroxychloroquine Plaquenil Side Effects & Dosage for. Side effects include irritability, headache, weakness, hair lightening or loss, stomach upset, nausea, dizziness, muscle pain, rash and itching. Rarely, hydroxychloroquine can affect the bone marrow leading to reduced white blood cells leukopenia or platelets thrombocytopenia and abnormal red blood cells anemia.

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