Chloroquine mechanism of resistance

Discussion in 'Canadian Pharcharmy Online' started by titanik-korolev, 28-Feb-2020.

  1. Karuneshka XenForo Moderator

    Chloroquine mechanism of resistance


    However, the reason for the lower accumulation of chloroquine was unknown. The resistant parasite has now been found to release chloroquine 40 to 50 times more rapidly than the susceptible parasite, although their initial rates of chloroquine accumulation are the same.

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    Resistance to chloroquine has, however, steadily spread since the 1960s from two foci, one in South America and one in South East Asia. Throughout the 1980s, chloroquine resistance spread through Africa, the global heartland of malaria mortality and morbidity, and there are very few effective and affordable drugs to take its place. Chloroquine is a 4-aminoquinoline with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the mechanism is not well understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. The clinical usefulness of chloroquine, and in some recent cases of quinine as well, has been much reduced by the evolution and spread of chloroquine resistant malaria parasites. The mechanism of resistance involves a reduced accumulation of the drug, although again the mechanism involved is controversial.

    These results suggest that a higher rate of chloroquine release explains the lower chloroquine accumulation, and thus the resistance observed in resistant Plasmodium falciparum. Verapamil and two other calcium channel blockers, as well as vinblastine and daunomycin, each slowed the release and increased the accumulation of chloroquine by resistant (but not susceptible) Plasmodium falciparum.

    Chloroquine mechanism of resistance

    Chloroquine - FDA prescribing information, side effects and uses, Chloroquine C18H26ClN3 - PubChem

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  6. Effects of chloroquine? Chloroquine is a relatively well-tolerated. medicine. The most common adverse reactions reported are stomach pain, nausea, vomiting, and headache. These side effects can often be lessened by taking chloroquine with food. Chloroquine may also cause itching in some people. All medicines may have some side effects.

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    Mechanism of Action Chloroquine, a 4-aminoquinoline, is an anti-protozoal agent. The precise mechanism by which chloroquine exhibits activity is not known. Chloroquine, may exert its effect against Plasmodium species by concentrating in the acid vesicles of the parasite and by inhibiting polymerization of heme. Causes of resistance 12 3.1 Definition of antimalarial drug resistance 12 3.2 Malaria treatment failure 12 3.3 Mechanisms of antimalarial resistance 12 3.3.1 Chloroquine resistance 12 3.3.2 Antifolate combination drugs 13 3.3.3 Atovaquone 13 3.4 Factors contributing to the spread of resistance 13 3.4.1 Biological influences on resistance 13 Mechanisms of Drug Action and Resistance Focus on Antimalarials Chemotherapy is the primary means of treating protozoan infections. Successful chemotherapy depends in a large part on the ability to exploit metabolic differences between the pathogen and the host.

     
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