What is the mechanism of action of chloroquine and primaquine

Discussion in 'Chloroquin' started by mdi, 14-Mar-2020.

  1. Grek's Guest

    What is the mechanism of action of chloroquine and primaquine


    Chloroquine has been extensively used in mass drug administrations, which may have contributed to the emergence and spread of resistance. It is recommended to check if chloroquine is still effective in the region prior to using it.

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    Chloroquine binds to heme or FP to form the FP-chloroquine complex; this complex is highly toxic to the cell and disrupts membrane function. Action of the toxic FP-chloroquine and FP results in cell lysis and ultimately parasite cell autodigestion. In essence, the parasite cell drowns in its own metabolic products. Cautions. Since anemia, methemoglobinemia, and leukopenia may occur following administration of large doses of primaquine, do not exceed adult dosage of 1 tablet = 15 mg base daily for fourteen days; make routine blood examinations particularly blood cell counts and hemoglobin determinations during therapy; drug should be discontinued immediately. Chloroquine is thought to exert its antimalarial effect by preventing the polymerization of toxic heme released during proteolysis of hemoglobin in the Plasmodium digestive vacuole. The mechanism of this blockade has not been established. We incubated cultured parasites with subinhibitory doses of 3Hchloroquine and 3H quinidine.

    The Centers for Disease Control and Prevention recommend against treatment of malaria with chloroquine alone due to more effective combinations. In areas where resistance is present, other antimalarials, such as mefloquine or atovaquone, may be used instead.

    What is the mechanism of action of chloroquine and primaquine

    Primaquine Phosphate Indications, Pharmacology, Dosage, Side Effects., Primaquine dosing, indications, interactions, adverse.

  2. Recommandation surveillance ophtalmologique plaquenil
  3. Malaria caused by P. vivax or P. ovale is treated with chloroquine in Brazil at a dose of 30 mg/kg divided into three days and primaquine in the 30 mg dose/day for 7 days or 15 mg/day for 14 days. Also, low doses of chloroquine can be used for the prevention of vivax malaria.

    • Side Effects of Chloroquine and Primaquine and Symptom Reduction in..
    • On the molecular mechanism of chloroquine's antimalarial action PNAS.
    • Chloroquine + Primaquine Pharmacology & Usage Details Medicine India.

    Chloroquine is one of the oldest anti-malarial agent, effectively used in malarial infections. P. falciparum and vivax are the sensitive types. It is a rapidly acting drug, targeting the asexual stage. It is an effective blood schizonticidal agent. It is gametocidal, except for P. falciparum. Mechanism of action Quinine is theorized to be toxic to the malarial pathogen, Plasmodium falciparum, by interfering with the parasite's ability to dissolve and metabolize hemoglobin. 32 As with other quinoline antimalarial drugs, the mechanism of action of quinine has not been fully resolved. The inhibitory effect of chloroquine and quinine on the formation and time-course of the PQ 5,6-orthoquinone generated from racemic PQ a and its individual enantiomers b, c by CYP2D6; and on the formation of primaquine alcohol from CYP2D6-catalyzed metabolism of racemic PQ d and its enantiomers e, f.

     
  4. JollyRodger New Member

    Dosing schedules not well established in children Case reports describe dosage regimens that are effective yet tolerated, such as 12.5 mg PO twice weekly over 2 yr in a child aged 4-6 yr, and 100 mg PO twice weekly over 5 months in a child aged 12 yr; mg/kg dosing not reported Hypersensitivity to chloroquine, 4-aminoquinolones Psoriasis, porphyria, retinal or visual field changes For prevention, may use proguanil concomitantly Shown to cause severe hypoglycemia including loss of consciousness that could be life-threatening in patients treated with or without antidiabetic medications; patients should be warned about risk of hypoglycemia and associated clinical signs and symptoms; patients presenting with clinical symptoms suggestive of hypoglycemia during treatment with chloroquine should have blood glucose level checked and treatment reviewed as necessary Not effective in most areas; CDC recommends mefloquine or atovaquone/proguanil - check CDC traveler information for specific recommendations for region May cause hemolysis in glucose-6 phosphate dehydrogenase (G-6-PD) deficiency; blood monitoring may be needed as hemolytic anemia may occur, in particular in association with other drugs that cause hemolysis Monitor CBC periodically with prolonged therapy Caution with history of auditory damage Caution with hepatic disease, alcoholism, and coadministration with other hepatotoxic drugs May provoke seizures in patients with history of epilepsy Antacids and kaolin reduce chloroquine absorption; separate administration by at least 4 hr Irreversible retinal damage observed in some patients; significant risk factors for retinal damage include daily doses of chloroquine phosphate 2.3 mg/kg of actual body weight, durations of use greater than five years, subnormal glomerular filtration, use of some concomitant drug products such as tamoxifen citrate, and concurrent macular disease A baseline ophthalmological examination should be performed within the first year of initiating therapy; for individuals with significant risk factors, monitoring should include annual examinations; discontinue if ocular toxicity is suspected; patient should be closely observed given that retinal changes (and visual disturbances) may progress even after cessation of therapy In individuals of Asian descent, retinal toxicity may first be noticed outside macula; it is recommended that visual field testing be performed in visual field of central 24 degrees instead of central 10 degrees May exacerbate heart failure Not effective against chloroquine- or hydroxychloroquine-resistant strains of Plasmodium species; information regarding geographic areas where resistance to chloroquine occurs, is available at the Centers for Disease Control and Prevention (gov/malaria) Does not treat hypnozoite liver stage forms of Plasmodium and will therefore not prevent relapses of malaria due to P. ovale; additional treatment with an anti-malarial agent active against these forms, such as an 8-aminoquinoline, is required for the treatment of infections with P. ovale Cases of cardiomyopathy resulting in cardiac failure, in some cases with fatal outcome, reported during long term therapy at high doses; monitor for signs and symptoms of cardiomyopathy and discontinue chloroquine if cardiomyopathy develops; chronic toxicity should be considered when conduction disorders (bundle branch block / atrio-ventricular heart block) diagnosed; if cardiotoxicity suspected, prompt therapy discontinuation may prevent life-threatening complications QT interval prolongation, torsades de pointes, and ventricular arrhythmias reported; risk is greater if chloroquine is administered at high doses; fatal cases reported; use with caution in patients with cardiac disease, a history of ventricular arrhythmias, uncorrected hypokalemia and/or hypomagnesemia, or bradycardia ( There are no adequate and well-controlled studies evaluating the safety and efficacy of chloroquine in pregnant women; usage during pregnancy should be avoided except in prophylaxis or treatment of malaria when benefit outweighs potential risk to fetus Because of the potential for serious adverse reactions in nursing infants from chloroquine, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account potential clinical benefit of drug to mother A: Generally acceptable. Individual plans may vary and formulary information changes. Aralen chloroquine Malaria Drug Side Effects & Dosage Aralen side effects - Things You Didn’t Know Aralen Chloroquine myRAteam
     
  5. redgray User

    Hydroxychloroquine Plaquenil Hydroxychloroquine Plaquenil is considered a disease-modifying anti-rheumatic drug DMARD. It can decrease the pain and swelling of arthritis. It may prevent joint damage and reduce the risk of long-term disability. Hydroxychloroquine is in a class of medications that was first used to prevent and treat malaria.

    Hydroxychloroquine Plaquenil -