Chloroquine endosome

Discussion in 'Canadian Drug' started by sh12q, 18-Mar-2020.

  1. azavorin2 User

    Chloroquine endosome


    -Suppressive therapy should continue for 8 weeks after leaving the endemic area. Approved indication: For the suppressive treatment of malaria due to Plasmodium vivax, P malariae, P ovale, and susceptible strains of P falciparum CDC Recommendations: 300 mg base (500 mg salt) orally once a week Comments: -For prophylaxis only in areas with chloroquine-sensitive malaria -Prophylaxis should start 1 to 2 weeks before travel to malarious areas; should continue weekly (same day each week) while in malarious areas and for 4 weeks after leaving such areas.

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    Chloroquine is a lysosomotropic agent that prevents endosomal acidification 1. It accumulates inside the acidic parts of the cell, including endosomes and lysosomes. This accumulation leads to inhibition of lysosomal enzymes that require an acidic pH, and prevents fusion of endosomes and lysosomes. EDITORIAL Chloroquine a brand-new scenario for an old drug Reza Baradaran Eftekhari, Niloufar Maghsoudnia and Farid Abedin Dorkoosh Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Medical Biomaterial Research Center Chloroquine is a weak base that can rapidly penetrate the plasma membrane, accumulate in acidic vesicles and increase the pH of the acidic compartment Maxfield 1982; Mellman, Fuchs et al. 1986. Preventing endosome acidification may subsequently inhibit hydrolytic enzymes such as proteases and nucleases Cotten, Längle-Rouault et al. 1990.

    Approved indication: For acute attacks of malaria due to P vivax, P malariae, P ovale, and susceptible strains of P falciparum CDC Recommendations: Chloroquine-sensitive uncomplicated malaria (Plasmodium species or species not identified): 600 mg base (1 g salt) orally at once, followed by 300 mg base (500 mg salt) orally at 6, 24, and 48 hours Total dose: 1.5 g base (2.5 g salt) Comments: -For the treatment of uncomplicated malaria due to chloroquine-sensitive P vivax or P ovale, concomitant treatment with primaquine phosphate is recommended. 60 kg or more: 1 g chloroquine phosphate (600 mg base) orally as an initial dose, followed by 500 mg chloroquine phosphate (300 mg base) orally after 6 to 8 hours, then 500 mg chloroquine phosphate (300 mg base) orally once a day on the next 2 consecutive days Total dose: 2.5 g chloroquine phosphate (1.5 g base) in 3 days Less than 60 kg: First dose: 16.7 mg chloroquine phosphate/kg (10 mg base/kg) orally Second dose (6 hours after first dose): 8.3 mg chloroquine phosphate/kg (5 mg base/kg) orally Third dose (24 hours after first dose): 8.3 mg chloroquine phosphate/kg (5 mg base/kg) orally Fourth dose (36 hours after first dose): 8.3 mg chloroquine phosphate/kg (5 mg base/kg) orally Total dose: 41.7 mg chloroquine phosphate/kg (25 mg base/kg) in 3 days Comments: -Concomitant therapy with an 8-aminoquinoline compound is necessary for radical cure of malaria due to P vivax and P malariae.

    Chloroquine endosome

    The lysosomal inhibitor, chloroquine, increases cell surface BMPR-II., Chloroquine a brand-new scenario for an old drug

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  6. The importance of preventing the degradation of therapeutics in the endosomes/lysosomes has been exemplified by the use of lysosomotrophic agents such as chloroquine which prevents the activity of lysosomal enzymes. In this review, several mechanisms which have been proposed for endosomal escape as well as the agents which are known to have.

    • Endosomal escape pathways for delivery of biologicals..
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    Unfortunately, Chloroquine, as well as other endosomal escape or endolytic agents, are often too toxic for use in preclinical models or eventual clinical trials of macromolecular therapeutics. Chemical treatment of cells with an endosomal trafficking inhibitor that blocks endosome progression, bafilomycin A1, resulted in a significant decrease in eTE. However, treatment of cells with lysosomotropic agents chloroquine and ammonium chloride had little effects on eTE. Mar 11, 2002 Chloroquine is one of the drugs commonly used to treat malaria in parts of sub-Saharan Africa, where HIV infection is endemic 3, 27, 31, 47. Our initial observation that chloroquine increased the infectivity of HIV suggested that administration of chloroquine to HIV-infected patients could potentially exacerbate the course of HIV infection.

     
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  9. DeN69 New Member

    Plaquenil Hydroxychloroquine Side Effects and Adverse Reactions Plaquenil Adverse Reactions with Treating Lupus and Rheumatoid Arthritis; Ocular Reactions. The goal with ocular screening for the side effects of Plaquenil is to find the damage at the earliest stage to reduce the amount of vision loss.

    Taking Plaquenil for Rheumatoid Arthritis
     
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