Clinical pharmacokinetics and metabolism of chloroquine

Discussion in 'Chloroquine' started by maxаndr, 17-Mar-2020.

  1. yuori XenForo Moderator

    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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    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. Plasma and cerebrospinal fluid pharmacokinetics of hydroxysafflor yellow A in patients with traumatic brain injury after intravenous administration of Xuebijing using LC-MS/MS method. Xenobiotica Vol. 50, No. 5, pp. 545-551. There is differential binding and metabolism of the R and S stereoisomers. Both drugs bind strongly to pigmented tissues but also bind to mononuclear cells, muscles, etc. Clinical Pharmacokinetics of Antimalerial Drugs. Pharmacokinetics of chloroquine saliva and plasma levels relationship. Eur J Drug Metab Pharmacokin 1986; 11.

    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/pharmacodynamics of chloroquine and., Plasma and cerebrospinal fluid pharmacokinetics of.

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  7. 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.

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    Metabolism Chloroquine undergoes metabolism by hepatic mechanisms. The main active metabolite is desethylchloroquine. Plasma half-life of desethylchloroquine is similar to chloroquine. 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. 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.

  8. Evol Well-Known Member

    This is not a list of all drugs or health problems that interact with chloroquine. G. I.s’ Drug Use in Vietnam Soared—With Their Commanders’ Help - HISTORY What was the malaria pills mainly for in the Vietnam War - Answers A Nightmare Drug, Military Suicides and Killings -
  9. lykov Guest

    Chloroquine Phosphate chloroquine phosphate dose. Use of chloroquine for indications other than acute malaria is contraindicated in patients with ocular disease, specifically those who have retinal or visual field changes of any etiology. Irreversible retinal damage has been observed in some patients who received chloroquine.

    Chloroquine Oral Route Precautions - Mayo Clinic