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    Kartik Reddy
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    This document summarizes several anti-malarial drugs including chloroquine, quinine, primaquine, mefloquine, and artemisinin derivatives. Chloroquine is commonly used to suppress the erythrocytic phase of malaria parasites and works by inhibiting heme polymerization. Quinine is effective against chloroquine-resistant strains and concentrates in the acidic environment of parasites. Primaquine is used for radical cure by targeting exo-erythrocytic and gametocyte forms. Mefloquine is a rapidly-acting schizontocide effective against chloroquine-resistant malaria. Artemisinin derivatives are potent blood schizontoc

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    concepts over drugs used in malaria

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    This document summarizes several anti-malarial drugs including chloroquine, quinine, primaquine, mefloquine, and artemisinin derivatives. Chloroquine is commonly used to suppress the erythrocytic phase of malaria parasites and works by inhibiting heme polymerization. Quinine is effective against chloroquine-resistant strains and concentrates in the acidic environment of parasites. Primaquine is used for radical cure by targeting exo-erythrocytic and gametocyte forms. Mefloquine is a rapidly-acting schizontocide effective against chloroquine-resistant malaria. Artemisinin derivatives are potent blood schizontoc

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    41 views3 pages

    AntiMalarial Pharm

    Uploaded by

    Kartik Reddy
    This document summarizes several anti-malarial drugs including chloroquine, quinine, primaquine, mefloquine, and artemisinin derivatives. Chloroquine is commonly used to suppress the erythrocytic phase of malaria parasites and works by inhibiting heme polymerization. Quinine is effective against chloroquine-resistant strains and concentrates in the acidic environment of parasites. Primaquine is used for radical cure by targeting exo-erythrocytic and gametocyte forms. Mefloquine is a rapidly-acting schizontocide effective against chloroquine-resistant malaria. Artemisinin derivatives are potent blood schizontoc

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    of 3

    [Type text]

    Anti-Malarial Drugs

    Drugs for the Exo-erythrocytic


    phase (liver) and gametocytes :
    Malaria is caused by the four species of protozoa Plasmodium
    Primaquine

    Plasmodium . vivax
    Plasmodium . falciparum
    Plasmodium . malariae
    Plasmodium . ovale

    Drugs to suppress erythrocytic


    phase / Schizontocides / Clinical
    cure:
    Chloroquine, Quinine,
    Pyrimethamine, Mefloquine,
    Artemisinin

    Anti-malarial drugs:
    Chloroquine most common
    Quinine Chloroquine resistant

    Radical cure : Exoerythrocytic


    phase
    (hypnozoites)
    with the clinical cure thus achieve
    total eradication of parasite

    Pyrimethamine / Sulfonamides
    Primaquine Radical cure
    Mefloquine, Artimisinin , Halofantrine New drugPharmokinetics:
    Oral absorption is excellent
    It has high affinity for melanin
    (retina) and concentrated in
    liver, spleen, kidney

    MOA:
    rapidly acting
    erythrocytic schizontocide
    against all species of
    plasmodium

    Chloroquine

    No effect on exoerythrocytic phase


    It is concentrated by
    intraerythrocytic plasmodia
    Conversion of toxic
    heme to non-toxic hemozoin
    is inhibited. Heme damages
    plasmodia.

    Metabolized by liver and


    excreted in urine
    Half-life ~ 3-10 days

    Adverse Effects:
    Nausea , vomiting and
    epigastric pain
    Parenteral administration
    hypotension and
    cardiac arrhythmia,
    convulsions
    Prolonged treatment ( as
    in RA) retinal damage
    Loss of hearing, mental
    disturbances, rashes

    Uses:
    Pharmokinetics:
    Clinical cure and
    suppressive
    It is orally well
    absorbed
    prophylaxis
    in malaria
    It has local irritant
    action and has
    Extra-intestinal
    antipyretic action,
    ameobiasis
    affects hearing and
    Rheumatoid
    arthritis
    vision at high
    dose
    Lepra
    Highreactions
    intravenous dose
    can cause hypotension
    and cardiac depression

    MOA:

    [Type text]

    It is basic and gets


    concentrated in
    acidic schizonts
    and kills by
    inhibiting heme
    polymerase

    Quinine

    It is a levo-rotatory
    alkaloid from
    cinchona bark
    ( dextro isomer
    Quinidine)
    It is an erythrocytic

    Adverse Effects:
    Cinchonism ringing in
    ears, nausea , difficulty
    in hearing, visual
    defects

    Uses / Treatment:
    Babesiosis,
    Falciparum malaria

    Hypersensitivity
    reactions
    Hemolysis can result
    Pharmakinetics:
    Oral absorption is good
    Concentrated in liver,
    lungs and intestine

    Uses:

    Metabolized in liver and


    excreted in bile

    Primary indication is
    radical cure of malaria.
    It is more active against
    exo-erythrocytic phase
    of Pl.ovale and vivax
    It is highly active
    against non-growing
    forms - gametocytes
    and hypnozoites.
    MOA:
    It appears to
    damage the
    plasmodia
    membranes

    Primaquin

    QT interval prolongation
    (arrhythmia) when given
    Pharmokinetics:
    with halofantrine or
    quinine
    Oral absorption is good
    Concentrated in liver,
    lungs and intestine
    Metabolized in liver and
    excreted in bile
    QT interval prolongation
    (arrhythmia) when given
    with Halofantrine or
    quinine

    [Type text]

    Mefloquine

    Use:
    It is rapidly acting
    erythrocytic
    schizontocide
    Effective against
    even chloroquine
    resistant strains of
    plasmodia
    Pharm kinetics:

    Obtained from Chinese herb


    Artemisia annua

    No resistance to Pl
    .falciparum

    MOA:
    It is a potent and
    rapidly acting
    blood
    schizontocide
    and have
    peroxide
    configuration
    responsible for its
    action.

    Artemisinin derivatives :
    Artemether / Arteether /
    Artesunate

    Adverse Effects:
    ST segment and QT
    prolongation
    conduction defects

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