Metabolism of chloroquine

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  1. Metabolism of chloroquine


    Please review the following URL and make sure that it is spelled correctly. The administration of chloroquine or hydroxychloroquine to albino and pigmented (hooded) rats at a daily dosage of 40 mg/kg produces a rapid rise in tissue concentrations of the drugs during the first month of medication, but comparatively little further rise when the medications are continued for two additional months.

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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. The drug is extensively distributed, with a. Chloroquine also is taken up into the acidic food vacuoles of the parasite in the erythrocyte. It increases the pH of the acid vesicles, interfering with vesicle functions and possibly inhibiting phospholipid metabolism. In suppressive treatment, chloroquine inhibits the erythrocytic stage of development of plasmodia. Cimetidine can inhibit the metabolism of chloroquine, increasing its plasma level. Concomitant use of cimetidine should be avoided. Ampicillin. In a study of healthy volunteers, chloroquine significantly reduced the bioavailability of ampicillin. An interval of at least two hours between intake of this agent and chloroquine should be observed.

    However, rats degrade the latter compound more extensively, so that their total mean tissue content of 4-aminoquinoline bases is greater than 30 mg/kg at that time. The mean tissue concentration of chloroquine at 1 month is about 100 mg/kg, compared to about 30 mg/kg for hydroxychloroquine.

    Metabolism of chloroquine

    Recommendations on Screening for Chloroquine and., Chloroquine phosphate C18H32ClN3O8P2 - PubChem

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  5. The rapid and direct analysis of the amount and spatial distribution of exogenous chloroquine CHQ and CHQ metabolites from tissue sections by liquid extraction surface sampling analysis coupled wit.

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    Oct 20, 2012 Chloroquine is extensively distributed with an enormous total apparent volume of distribution Vd more than 100 L/kg, and a terminal elimination half-life of 1 to 2 months. As a consequence, distribution rather than elimination processes determine the blood concentration profile of chloroquine in patients with acute malaria. Chloroquine undergoes appreciable degradation in the body. The main metabolite is desethylchloroquine, which accounts for one fourth of the total material appearing in the urine; bisdesethylchloroquine, a carboxylic acid derivative, and other metabolic products as yet uncharacterized are found in small amounts. In order to determine the pharmacokinetic disposition of chloroquine CQ and its active metabolite, desethylchloroquine DECQ, when administered as intermittent presumptive treatment in pregnancy IPTp for malaria, 30 Papua New Guinean women in the second or third trimester of pregnancy and 30 age-matched nonpregnant women were administered three daily doses of 450 mg CQ 8.5 mg/kg of body.

     
  6. Chloroquine is the generic form of the brand-name prescription medicine Aralen, which is used to prevent and treat malaria — a mosquito-borne disease caused by a parasite — and to treat amebiasis, an infection of the intestines caused by a parasite. Chloroquine overdose Request PDF Chloroquine Michigan Medicine Chloroquine PeaceHealth
     
  7. akronimus Guest

    PLAQUENIL HYDROXYCHLOROQUINE SULFATE TABLETS, USP DESCRIPTION Mechanism of action The precise mechanism by which hydroxychloroquine exhibits activity against. Plasmodium. is not known. Hydroxychloroquine, like chloroquine, is a weak base and may exert its effect by concentrating in the acid vesicles of the parasite and by inhibiting polymerization of heme.

    Hydroxychloroquine-Induced Retinal Toxicity - American.