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WELCOME
DIURETICS
C.A.I.D
Potassium
SparingDiuretics
Endinggreet
Endinggreet
DIURETICS
C.A.I.D
Potassium
SparingDiuretics
Endinggreet
Endinggreet
Diuretics are the substances which promote
the production of urine.
There are different types of diuretics on the
basis of action on different sites of nephron.
 Osmotic diuretics
 Thiazide diuretics
 Carbonic-anhydrase inhibitor
diuretics
 Loop diuretics
 Potassium sparing diuretics
about
C.A.I.D
Potassium
SparingDiuretics
Endinggreet
Endinggreet Carbonic Anhydrase Inhibitor Diuretics
Actually they are sulphonamide
derivatives. They block the activity of
carbonic anhydrase enzyme which is
responsible for formation of H+ and
HCO3- in proximal tubular cell. Thus,
they increase the watery content in urine.
Examples:
01.Acetazolamide
02.Methazolamide
03.Dorzolamide
about
MECHANISMOF
ACTION
Potassium
SparingDiuretics
Endinggreet
Endinggreet
Mechanism of action
about
STRUCTURE
Potassium
SparingDiuretics
Endinggreet
Endinggreet
The Stucture Of Acetazolamide
about
SYNTHESISOF
ACETAZOLAMIDE
Potassium
SparingDiuretics
Endinggreet
Endinggreet
Synthesis Of Acetazolamide
about
SAR
Potassium
SparingDiuretics
Endinggreet
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SAR
 Presence of sulphonamide moiety is necessary for
diuretic activity.
 N atom of sulphonamide must be unsubstituted
for its activity. This feature explain why all the
antibacterial sulphonamide exerts diuretic action.
 But the ring nitrogen can be substituted without
loss of activity. Example –Methazolamide. That
decreases the polarity and permits greater
penetration on eye fluid.More acceptable for
opthalmic preparation used in glucoma.
about
PHARMACOKINETICS
Potassium
SparingDiuretics
Endinggreet
Endinggreet PHARMACOKINETIC FACTORS
 Acetazolamide and dichlorphenamide are well
absorbed orally .Exerted by kidney .Onset of action
is 30 min to 2hours.Exist in body for 8-12 hours. That
means It can be consumed 2 or 3 times in a day.
 Brinzolamide and Dorzolamide are highly protein
binding thus prolong their half lives.
For example it is noted that brinzolamide can remain
in the body for 111 days and Dorzoalmide for 4 months.
If taken orally, can be seriously toxic for body. That’s
why only used topically for eye.
about
history
timeline
Endinggreet
Endinggreet
THANK YOUshukraan jazilaan
Drug Trade
Name
Oral
Absorption
(%)
Peak
Plasma
Half
Life
Duratio
n Of
Effect
Relative
Potency
Acetazolamide Diamox >90 1–3 h 6-9 h 8–12 h
Methazolamide Neptazane >90 NA ∼14 h 10–18 h
Ethoxzolamide Cardrase 65 2.5–5.5 h
Brinzolamide Azopt Topical use
only (eye)
NA ∼111
days
8-12 h
Dorzolamide Truspot Topical use
only (eye)
NA 4 months 8-12 h

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Diuretics