This document provides an overview of diuretics, which are drugs that increase urine production by the kidneys, and are used to treat conditions like hypertension and fluid retention. It covers various classes of diuretics, including carbonic anhydrase inhibitors, thiazides, potassium-sparing diuretics, and loop diuretics, detailing their mechanisms, uses, properties, and specific examples. Each diuretic class is discussed with information on common medications, formulations, dosage, and storage recommendations.

1. DIURETICS
PRESENTATION ON DIURETICS FOR
DIPLOMA 1ST YEAR STUDENTS
GURU GOBIND SINGH COLLEGE OF
PHARMACY, YAMUNA NAGAR
SHIKHA KAMBOJ
ASSISTANT PROFESSOR

2. DIURETICS
 A diuretic is a drug that increases the secretion of urine (i.e, water, electrolytes, and
waste products) by the kidneys or diuretics are the chemical agents which increase
the excretion of urine by kidneys.
 They lead to the secretion of excess water and salt that accumulates in tissues and
urine, results in decrease in body fluids especially the extracellular fluid.
 Many conditions or diseases, such as hypertension, congestive heart failure,
endocrine disturbances, and kidney and liver diseases can cause retention of excess
fluid (edema).
 Adiuretic is used when the patient shows signs of excess fluid retention.
 Reabsorption of Na in the kidney results in the reabsorption of water. It follows
that inhibition of Na reabsorption will result in diuresis. Because of this, the term
diuretic has come to mean any agent that will inhibit the tubular reabsorption of
sodium.

3. Different sites for diuretics

4. Classification of drugs

6. 1. CARBONIC ANHYDRASE (CA)
Thecarbonicanhydrases formafamilyofenzymes thatcatalyzethe rapid inter-
conversionofcarbondioxide (CO2)andwatertobicarbonate(HCO3) and protons (or
viceversa).

7. Uses: 1. It is used in treatment of glaucoma and drug induced edema.
2. It is also used as anticonvulsant for the treatment of epilepsy.
3. It is also used in the treatment of Menieres disease (disorder of inner ear) and neuromuscular disorders.
4. It is used in the treatment of moderate congestive heart failure, and in the treatment of glaucoma.
Acetazolamide
Chemical name: N-(5-sulphomoyl-1, 3, 4 thiadiazole-2-yl) acetamide.
Properties: It is a sulfonamide derivative. It occurs as white to yellowish white crystalline powder, slightly
soluble in water and alcohol. It is preserved in tight light-resistant containers. It is rapidly absorbed by the
stomach, reaches peak level within 2 hours and is eliminated unchanged.
Formulations: Actazolamide Tablets B.P, L.P, Actetazolamide CapsulesIt is used in the form of tablets, usual
dose is 250 mg daily. Its sodium salt is official in U.S.P. and used parenterally. Intravenous or intramuscular dose
is 250 mg of acetazolamide base.
Storage: Store in air tight light resistant container.

8. Formulations: Actazolamide Tablets B.P, L.P, Actetazolamide CapsulesIt is used in the form of
tablets, usual dose is 250 mg daily. Its sodium salt is official in U.S.P. and used parenterally.
Intravenous or intramuscular dose is 250 mg of acetazolamide base.
Brand name: Zolamide
Diamos

9. Thiazides
Thiazide diuretics are a type of diuretic (a drug that increases urine flow). They act directly on the kidneys and
promote diuresis (urine flow) by inhibiting the sodium/chloride cotransporter located in the distal convoluted
tubule of a nephron (the functional unit of a kidney). Thiazides decrease sodium reabsorption which increases
fluid loss in urine, which in turn decreases extracellular fluid and plasma volume. This reduces cardiac output
(how hard the heart has to work to pump blood around the body) and lowers blood pressure. Thiazides also work
in other ways to lower blood pressure. Thiazides also cause potassium loss while retaining calcium.

10. Metolazone
Common name: 7-chloro-2-methyl-4-oxo-3-o-tolyl-1,2,3,4-
tetrahydroquinazoline-6-sulfonamide.
It is a long action quinazolone based sulphonamide thiazide like
diuretic.
Properties: - It occurs as a crystalline powder. It is tasteless and
odourless, insoluble in water and alcohol. It is light sensitive. It is
polymorphic.
Storage:- Store in a air tight. Light resistant container.
Uses -(i) It is used to reduce the swelling and fluid retention caused by
heart failure or kidney diseases.
(ii) It is also used alone with other medications to treat high B.P

11. Formulations:
Metolazone is a thiazide-like diuretic marketed under the brand names Zytanix, Metoz, Zaroxolyn, and Mykrox.
Metolazone tablets, USP, for oral administration contain 2½, 5, or 10 mg of metolazone, USP, a diuretic
XIPEMIDE (DIUREXAN, AQNAPHOR)
•Common name:
•4-chloro-N-(2,6-dimethylphenyl)-2-hydroxy-5-sulfamoylbenzamide
•Diurexan
•Xipamid
•Aquaphor
•Diurex (lacer)
•Aquaphor (diuretic)
•Aquaphoril
•Zipix
It is a sulphonamide diuretic
Properties:- It occurs as white to beige colored crystalline powder. It is lipophilic poorly soluble in
water and highly soluble in polar organic solvents.

12. Combinations requiring special precautions
The product information requests special precautions for these combinations:
•The antihypertensive effect can be increased by ACE
inhibitors, barbiturates, phenothiazines, tricyclic antidepressants, alcohol, etc. (Classified
as minor.)
•NSAIDs can reduce the antihypertensive and diuretic effects. Xipamide increases the
neurotoxicity of high doses of salicylates. (Classified as minor.)
•Toxicity of cardiac glycosides is increased due to hypokalemia
and hypomagnesemia.(Classified as minor.)
•Antiarrhythmic agents (classes Ia and III), phenothiazines and other antipsychotics increase
the risk of torsades de pointes due to hypokalemia.

13. Chlorthalidone
Storage: Store in air tight, light resistant containers
Uses: (i) It is used to treat mild hypertension
(ii) It is used as diuretic in patient with renal failure
(3) cardiac oedema caused by decompensation of heart failure
(4) hypertension in combination with chronic renal disease
Formulations: Xipamide is a sulfonamide diuretic drug marketed by Eli Lilly under the trade names Aquaphor (in
Germany) and Aquaphoril (in Austria). It is used for the treatment of oedema and hypertension.
Common name: 2-Chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzene-1-sulfonamide
•chlorthalidone
Chlorothalidone
It is thiazide diuretic. It occurs as white to yellowish white crystalline powder. It is practically insoluble in water,
ether and chloroform and soluble in methanol.
Storage: It should be stored in airtight container

14. Uses: It is used to treat high blood pressure and fluid retension
Formulations: Chorthalidone tablets USP
Potassium sparing diuretics
Potassium-sparing diuretics are medicines that increase diuresis (urination) without the loss
of potassium. They are generally weak diuretics and work by interfering with the sodium-
potassium exchange in the distal convoluted tubule of the kidneys or as an antagonist at the
aldosterone receptor. Aldosterone promotes the retention of sodium and water, so if
potassium-sparing diuretics are used to block this effect, more sodium and water can pass
into the collecting ducts of the kidneys, increasing diuresis.
Because potassium-sparing diuretics do not promote the secretion of potassium during
diuresis they do not cause hypokalemia (low potassium levels). However, there is a risk
of hyperkalemia (high potassium levels) if they are used with other agents that also retain
potassium, such as ACE inhibitors.
Potassium-sparing diuretics may be used alone or in conjunction with loop or thiazide
diuretics.

15. SPIRONOLACTONE
It is aldosterone antagonist.
Properties: It occurs as a buff coloured powder. It is odourless or has a slight odour of thioacetic acid. It is very
slightly soluble in water.
Storage: Protect from light
Uses: It acts as a potassium sparing diuretic for the management of hypertension. It is used to control edema
associated with hepatic cirrhosis and nephrotic syndrome off. It is used in conjugation with other diuretics to
prevent excessive loss of potassium ions.
Formulations: Spironolactone tablets B.P, I.P
Brand name: (ALDECTONE®, LACTONE®, SPIROMIDE®)

16. Loop diuretics
Diuretics are medicines that increase urine flow (cause diuresis). Loop diuretics are a powerful type of diuretic that
work by inhibiting the sodium-potassium-chloride (Na+/K+/2Cl) co-transporter in the thick ascending loop of Henle
(hence the name loop diuretic), which is located in the kidneys. This reduces or abolishes sodium, chloride, and
potassium reabsorption, leading to increased loss of sodium, chloride, and potassium into the nephron (the functional
unit of a kidney). As a result, water is also drawn into the nephron and urine volume increases. Loop diuretics also
reduce the reabsorption of calcium and magnesium.

18. Bumetanide
Bumetanide is used to treat edema (fluid retention; excess fluid held in body tissues) caused by various medical
problems, including heart, kidney, and liver disease. Bumetanide is in a class of medications called diuretics ('water
pills'). It works by causing the kidneys to get rid of unneeded water and salt from the body into the urine.
Common name: 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid.
Properties: - Bumetanide is a diuretic. It is a potent sulfamoylanthranilic acid derivative. It belongs to the class of
loop diuretics. It occurs as a white crystalline powder. It has a bitter taste. It is relatively stable in light and at room
temperature. It is very slightly soluble in water.
Storage: Store in an airtight container.
Uses: It is used for the treatment of oedema associated with CH, hepatic and renal disease.
Formulations: Bumetanide Tablets B.P, Bumetanide Oral Solution B.P, Bumetanide Injection B.I
Brand name: The brand name of this medication is Bumex, BUMET, BURINEX.

19. BENZTHIAZIDE
Properties: It occurs as a white crystalline powder with characteristic odour and a bitter taste. It is practically
insoluble in water. It is stable in light and air.
Storage: It should be stored in air tight container.
Uses: (1) It is used in the treatment of oedema associated with CHF
(ii) Hypokelaemia and other electrolyte imbalances may occur on prolonged use. It is used in the treatment of high
blood pressure.
Brand name: aquatag, fovane, exosalt, Dihydrex, Diucen, Edemax, Exna, Foven.