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    8 - Diuretics

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    JericSalcedo
    The document discusses different classes of diuretics including carbonic anhydrase inhibitors, loop diuretics, thiazide and thiazide-like diuretics, potassium sparing diuretics, and miscellaneous classes. It provides details on their mechanisms of action and structural requirements for activity.

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    8 - Diuretics

    Uploaded by

    JericSalcedo
    34 views9 pages
    The document discusses different classes of diuretics including carbonic anhydrase inhibitors, loop diuretics, thiazide and thiazide-like diuretics, potassium sparing diuretics, and miscellaneous classes. It provides details on their mechanisms of action and structural requirements for activity.

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    Diuretics

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    8.-Diuretics

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    The document discusses different classes of diuretics including carbonic anhydrase inhibitors, loop diuretics, thiazide and thiazide-like diuretics, potassium sparing diuretics, and miscellaneous classes. It provides details on their mechanisms of action and structural requirements for activity.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    34 views9 pages

    8 - Diuretics

    Uploaded by

    JericSalcedo
    The document discusses different classes of diuretics including carbonic anhydrase inhibitors, loop diuretics, thiazide and thiazide-like diuretics, potassium sparing diuretics, and miscellaneous classes. It provides details on their mechanisms of action and structural requirements for activity.

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    DIURETICS

    SITE 1:
    CARBONIC ANHYDRASE INHIBITORS
     They inhibit the enzyme carbonic
    anhydrase which is found in the
    proximal convoluted tubule.
     They suppress the activity of carbonic
    anhydrase.
     Carbonic anhydrase is an enzyme that
    catalyzes the rapid interconversion of
    carbon dioxide and water to
    bicarbonate and protons(or vice versa) SAR:
    The free sulfamoyl nitrogen is essential for
    diuretic activity.
     The net result of carbonic anhydrase
    inhibition is increased excretion of Na+, Attachment of the sulfamoyl group to
    K+, HCO3-. aromatic system
    SITE 2:
    LOOP DIURETICS
     High ceiling diuretics
     Inhibit Co-transport System
     Onset of action in about 30 minutes and lasts for 6 hours.
     They cause hypokalemia.
    Subclasses:
    1. 2-Aminobenzoic acid derivatives. (Furosemideand
    Azosemide)
    2. Phenoxyaceticacid derivatives (Ethacrynicacid).
    SITE 2:
    LOOP DIURETICS
    5-Sulfamoyl-2-aminobenzoic
    Acids

    1. Position-1 must be acidic


    (optimal activity with COOH)
    2. SO2NH2 group at position 5 is
    prerequisite for activity, Furosemide
    3. must be free.
    4. Activating group at position
    4- as Cl or CF3.
    SITE 2:
    LOOP DIURETICS

    Phenoxyacetic acid

    Ethacrynic acid
    -Obsolete
    SITE 3:
    THIAZIDE AND THIAZIDE LIKE ACTIVITY
     Lossof Double bond
    between 3 and 4 position
    increases potency
     Position 6 must be –Cl, -Br,
    -CF3, –NO2 or a phenoxy
    group
     Sulfamoyl group in position MOA:
    7 is required
     inhibits reabsorption of Na+ and
     4,
    5, and 8 substitution Cl-
    destroys activity  Inhibits electroneutral Na+/Cl-
    co-transport system
    SITE 4:
    POTASSIUM SPARING DIURETICS

    Aldosterone antagonist:
     Spironolactone
     Inhibits Aldosterone
     Resembles progesterone
     Eplerinone,Amiloride and
    Triamterene (Resembles
    vitamin B9)
     Na+ Channel Blockers
    MISCELLANEOUS CLASS

    Xanthine Alkaloids
    Osmotic Diuretics
     Dextrose
     Mannose

    Mercurial Diuretics
     Mercaptomerin

     Meralluride

     Merthoxyline

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