Clinical pharmacokinetics and metabolism of chloroquine

Discussion in 'Hydroxychloroquine Plaquenil' started by Pavelcreative, 29-Feb-2020.

  1. Nariman 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 .

    Aralen dosage malaria prevention What part of the malaria life cycle does chloroquine target Aralen price

    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. 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%. 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.

    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 and Metabolism of Chloroquine., Pharmacokinetics and Metabolism of the Antimalarial.

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  6. 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.

    • Chloroquine - FDA prescribing information, side effects..
    • Clinical Pharmacokinetics, Volume 31, Issue 4 - Springer.
    • Chloroquine, Past and Present In the Pipeline.

    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. Metabolism Chloroquine undergoes metabolism by hepatic mechanisms. The main active metabolite is desethylchloroquine. Plasma half-life of desethylchloroquine is similar to chloroquine. The main processes involved in pharmacokinetics are absorption, distribution, and the two routes of drug elimination, metabolism and excretion. Together they are sometimes known by the acronym ‘ADME’. Distribution, metabolism and excretion are sometimes referred to collectively as drug disposition.

     
  7. andre111 New Member

    Hydroxychloroquine is widely used in the treatment of post-Lyme arthritis. Sildenafil brands in India DrugsUpdate India Medicine India Hydroxy-chloroquine brands in India DrugsUpdate India
     
  8. Karl_Gray Well-Known Member

    Chloroquine - In the US, Chloroquine chloroquine systemic is a member of the following drug classes amebicides, antimalarial quinolines and is used to treat Amebiasis, Malaria, Malaria Prevention and Sarcoidosis.

    Chloroquine Oral Uses, Side Effects, Interactions.