Medicinal of diuretics

1. THIAZIDES
Raj K. Prasad, SIP

2. Hydrochlorothiazide
Raj K. Prasad, SIP

3. Hydrochlorothiazide
 Furosemide, triamterene, and hydrochlorothiazide
are the most commonly used diuretics for sport
doping since they are eliminated rapidly and are
therefore more difficult to detect in urine samples
taken at later time points after use.
Raj K. Prasad, SIP

4. USES:
 Hydrochlorothiazide is one of the most widely used
drugs of thiazides series.
 Hydrochlorothiazide causes less inhibition of
carbonic anhydrase, but causes 5–10 times more
diuresis of sodium ions than chlorothiazide using the
same dose.
Raj K. Prasad, SIP

5. HYDROFLUMETHIAZIDE
Raj K. Prasad, SIP

6. USES
 Hydroflumethiazide is a potent diuretic
employed in the management of edema
associated with cardiac failure, steroid
administration, and hepatic cirrhosis.
Raj K. Prasad, SIP

7. CYCLOTHIAZIDE
(3-bicyclo[2.2.1]hept-5-en-2-yl-6-chloro-3,4-dihydro-, 1,1-
dioxide)
Raj K. Prasad, SIP

8. USES:
 It possesses both diuretic and antihypertensive
actions.
 It is often used as an adjunct to other
antihypertensive drugs, such as reserpine and
the ganglionic blocking agents.
Raj K. Prasad, SIP

9. CHLORTHIAZIDE
(1,1-dioxide 6-chloro-2H-1,2,4-benzothiadiazin-7-sulfonamide)
Raj K. Prasad, SIP

10. USES
• It is used for arterial hypertension, in edematous
syndromes of various genesis, congestive effects in
cardiovascular insufficiency, nephrosis and
nephritis, and toxicosis.
• It is especially recommended for hypertonic
illnesses.
• It lowers intraocular pressure in a number of cases.
Raj K. Prasad, SIP

11. LOOP DIURETICS (high-ceiling diuretics)
 The most powerful diuretic effect is provided by
loop diuretics, which severely inhibit the absorption
of sodium and chloride ions from renal tubules in
cortical and cerebral regions and the ascending
region of Henle’s loop.
Raj K. Prasad, SIP

12. GENERAL MECHANISM OF ACTION
 Their main site of action is believed to be on the thick
ascending limb of the loop of Henle, where they
inhibit the luminal Na+/ K+/2Cl− symporter.
 High-ceiling diuretics are characterized by a quick
onset and short duration of activity.
Raj K. Prasad, SIP

13. STRUCTURE–
ACTIVITY
RELATIONSHIPS
Raj K. Prasad, SIP

14.  The chlorine and sulfonamide substitutions are
features also seen in diuretics.
 Because the molecule possesses a free carboxyl group,
furosemide is a stronger acid than thiazide diuretics
(pKa = 3.9).
Raj K. Prasad, SIP

15. FUROSEMIDE
(4-chloro-N-furfuryl-5-sulfamoyl anthranilic acid)
 Furosemide is a highly effective and quick-acting diuretic
whose action is associated with blocking the reabsorption
of ions in the ascending bend of Henle’s loop.
Raj K. Prasad, SIP

16. SYNTHESIS
Raj K. Prasad, SIP

17. USES
 Furosemide has proven more effective than
other diuretics.
 Besides a diuretic effect, it also dilates
peripheral vessels.
 It is frequently used in combination with other
anti-hypertensive drugs.
Raj K. Prasad, SIP

18. BUMETANIDE
Raj K. Prasad, SIP

19. BUMETANIDE
 Bumetanide, a phenoxy group has replaced the customary chloro
or trifluoromethyl substitutions in other diuretic molecules.
 The phenoxy group is an electron-withdrawing group similar to
the chloro or trifluoromethyl substitutions.
 The amine group at position 6 has been moved to position 5.
 The short duration of activity is similar, but the compound is
approximately 50-fold more potent.
Raj K. Prasad, SIP

20. USES
 Bumetanide is used for relieving edema
associated with cardiac insufficiency, for liver
and kidney diseases, and hypertension.
Raj K. Prasad, SIP

21. ETHACRYNIC ACID
 Ethacrynic acid is the only loop diuretic that is not a
sulfonamide derivative and may be useful in patients allergic
to sulfonamides.
Raj K. Prasad, SIP

22. USES
 Ethacrynic acid is a powerful diuretic
prescribed for edema associated with cardiac
insufficiency, renal edema that does not
respond to other diuretics, and edema of the
brain and lungs.
Raj K. Prasad, SIP

23. POTASSIUM SPARING DIURETICS
 Potassium sparing diuretics differ from other
diuretics in that they increase excretion of
sodium ions from the body while simultaneously
reducing excretion of potassium ions.
Raj K. Prasad, SIP

24. SPIRONOLACTONE
(7-acetate of the γ-lactone of 17-hydroxy-7-mercapto-3-oxo-17-α-pregn-4-ene-21-carboxylic acid)
Raj K. Prasad, SIP

25. Mechanism of action
 It is a competitive antagonist of aldosterone, spironolactone
blocks aldosterone receptors, thus increasing excretion of
sodium, chloride, and corresponding equivalents of water
with urine, thus retaining the amount of potassium ions in the
organism.
 Antagonist activity is dependent on the presence of γ-lactone
ring on C-17 and a substituent on C-7 in spironolactone.
Raj K. Prasad, SIP

26. USES
 It is used for edema syndrome caused by chronic
cardiac insufficiency, liver cirrhosis,
hyperaldosteronism, and hypokalemia caused by other
diuretics.
 However, it should not be combined with potassium-
sparing diuretics(e.g., triamterene or amiloride).
Raj K. Prasad, SIP

27. Triamterene
(2,4,7-triamino-6-phenylpteridine)
Raj K. Prasad, SIP

28. Triamterene
 Triamterene is a pyrazine derivative that inhibits the
reabsorption of sodium ions without increasing the
excretion of potassium ions.
 It has little effect on urine volume.
Raj K. Prasad, SIP

29. USES
 This drug is recommended in combination with
other diuretics for treating edema, cirrhosis of
the liver, and nephrotic syndrome.
Raj K. Prasad, SIP

30. AMILORIDE
(N-amidino-3,5-diamino-6-chloropirazincarboxamide)
Raj K. Prasad, SIP

31. USES
 Amyloride is rarely used individually—as a rule it is used in combination with thiazides or loop diuretics.
It is mainly used in combination with thiazide diuretics for cardiac insufficiency and hypertension,
Raj K. Prasad, SIP

32. Raj K. Prasad, SIP