Metabolism of chloroquine

Discussion in 'Chloroquine Drug' started by Spunky, 01-Mar-2020.

  1. MITROFAN Well-Known Member

    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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    Both chloroquine and hydroxychloroquine are substrates for cytochrome P450 CYP enzymes enzymes responsible for the metabolism of multiple drugs and hence can interfere with other drugs 38,46,47. 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. Abstract. In humans, the antimalarial drug chloroquine CQ is metabolized into one major metabolite, N-desethylchloroquine DCQ. Using human liver microsomes HLM and recombinant human cytochrome P450 P450, we performed studies to identify the P450 isoforms involved in the N-desethylation of CQ.

    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

    Chloroquine - an overview ScienceDirect Topics, CHLOROQUINE PHOSPHATE TABLETS, USP 250 MG and 500 MG

  2. Chloroquine-resistant malaria is now widespread in africa
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  4. 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.

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    During model development and validation step 1, model performance depends largely on the certainty of the model input parameters describing CQ absorption, distribution, and metabolism and elimination. 58 When using literature-reported PK parameters for absorption ka, distribution Vss, and elimination clearance, the model performance was. 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. 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.

     
  5. HabaHaba Moderator

    Plaquenil (hydroxychloroquine) belongs to a group of medicines called quinolines. Day Or Night—When Is The Best Time To Take Your Blood. NHS advice on the best time to take blood pressure tablets Hydroxychloroquine Uses, Dosage & Side Effects -
     
  6. m.maslov Moderator

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