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Diuretics PCM

Diuretics work by increasing urine production and electrolyte excretion in the kidneys. They are used to treat hypertension, edema, heart failure, and kidney disease. There are several classes of diuretics that act on different parts of the nephron, including loop diuretics, thiazide diuretics, potassium-sparing diuretics, and carbonic anhydrase inhibitors. Furosemide and chlorthalidone are examples of loop and thiazide diuretics, respectively, that are commonly used to treat fluid overload and reduce blood pressure.

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92 views8 pages

Diuretics PCM

Diuretics work by increasing urine production and electrolyte excretion in the kidneys. They are used to treat hypertension, edema, heart failure, and kidney disease. There are several classes of diuretics that act on different parts of the nephron, including loop diuretics, thiazide diuretics, potassium-sparing diuretics, and carbonic anhydrase inhibitors. Furosemide and chlorthalidone are examples of loop and thiazide diuretics, respectively, that are commonly used to treat fluid overload and reduce blood pressure.

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Anuj pandit
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DIURETICS

Diuretics are a class of drugs that increase the production of urine by the kidneys, resulting
in increased elimination of water and electrolytes from the body.
Or
Diuretics (natriuretics) are drugs that cause a net loss of Na+ and water in urine.
They are used to treat various conditions such as hypertension, edema (swelling caused by
excess fluid), heart failure, and kidney disease.
1. Diuretic agents are ingested orally or administered intravenously.
2. The drug is absorbed into the bloodstream and transported to the kidneys.
3. The specific type of diuretic agent binds to its target site in the kidneys, such as the
sodium-chloride symporter in the distal convoluted tubule or the Na-K-2Cl cotransporter in
the loop of Henle.
4. The diuretic agent inhibits the reabsorption of sodium, chloride, and/or potassium ions,
depending on the type of diuretic agent used.
5. As a result, the concentration of these ions in the filtrate increases and more water is
retained in the urine.
6. The increased excretion of water and electrolytes results in a decrease in blood volume
and a reduction in fluid accumulation in tissues such as the lungs, legs, or abdomen.
7. The net effect of diuretic agents is a reduction in blood pressure, a decrease in edema and
fluid overload, and an improvement in renal function in some cases.
CLASSIFICATION OF DIURETICS
Diuretics can be classified based on their mechanism of action, chemical structure, and site
of action in the kidneys. Here are the most common classifications of diuretics:
A. High efficacy diuretics (Inhibitors of Na+- K+-2Cl¯ cotransport)- Sulphamoyl
derivatives: (@BTF)
Loop Diuretics
 Furosemide
 Bumetanide
 Torasemide.

B. Medium efficacy diuretics (Inhibitors of Na+-Cl¯ symport)


Thiazide diuretics
 Hydrochlorothiazide
 Benzthiazide
 Chlorthalidone
 Metolazone
 Xipamide
 Indapamide.

C. Weak or adjunctive diuretics


Carbonic anhydrase inhibitors:
 Acetazolamide
Potassium-sparing diuretics:
 Spironolactone
 Amiloride.\

Chemical Structures

Acetazolamide
Bumetanide

Xipamide
Diuretic Example Site of
Mechanism of Action
Type Diuretics Action

Hydrochlorothiazide
(HCTZ) Distal Inhibits the sodium-chloride symporter,
Thiazide
Convoluted leading to increased excretion of sodium,
Diuretics Chlorthalidone
Tubule chloride, and water
xipamide

Furosemide (Lasix) Ascending Inhibits the Na+/K+/2Cl- symporter,


Loop
Loop of leading to increased excretion of sodium,
Diuretics bumetanide Henle chloride, and water

Blocks the aldosterone receptor, leading to


Collecting
Spironolactone decreased reabsorption of sodium and
Duct
increased excretion of sodium and water

Potassium-
Sparing
Diuretics Blocks the epithelial sodium channel
Collecting (ENaC), leading to decreased reabsorption
Amiloride
Duct of sodium and increased excretion of
sodium and water

Creates an osmotic gradient in the lumen


Osmotic Proximal of the nephron, preventing reabsorption of
Mannitol
Diuretics Tubule water and leading to increased excretion of
water and solutes
1. Carbonic anhydrase inhibitors: Carbonic anhydrase inhibitors (CAIs) are a class of
medications that inhibit the action of the enzyme carbonic anhydrase, which is found in
the proximal tubule of the nephron.
Carbonic anhydrase plays a role in the reabsorption of bicarbonate and the excretion of
hydrogen ions in the kidneys. By inhibiting carbonic anhydrase, CAIs reduce the
reabsorption of bicarbonate, leading to increased excretion of bicarbonate, sodium, and
water.
CAIs are less commonly used as diuretics compared to thiazide diuretics or loop
diuretics. However, they may be prescribed for specific conditions, such as glaucoma,
Examples include acetazolamide and dorzolamide.
2. Osmotic diuretics: These diuretics work by creating an osmotic gradient in the proximal
tubule of the nephron, preventing reabsorption of water and leading to increased excretion
of water and solutes. They are particularly useful in reducing intracranial pressure, as they
decrease the amount of water in brain tissue.
Examples include mannitol and urea.
3. Loop diuretics: These diuretics work by inhibiting the Na+/K+/2Cl- symporter in the
ascending limb of the loop of Henle. This leads to increased excretion of sodium,
chloride, and water, and can be particularly effective in reducing edema associated with
heart failure, liver disease, and kidney disease.
Examples include furosemide, bumetanide, and torsemide.
4. Thiazide diuretics: These are the most commonly prescribed diuretics and work by
blocking the sodium-chloride symporter in the distal convoluted tubule of the nephron.
This results in increased excretion of sodium, chloride, and water, leading to decreased
blood volume and blood pressure.
Examples include Hydrochlorothiazide, chlorthalidone, Benzthiazide, indapamide and
Xipamide
5. Potassium-sparing diuretics: These diuretics work by blocking the action of aldosterone
in the collecting duct of the nephron. This results in decreased reabsorption of sodium and
increased excretion of sodium and water, without causing excessive loss of potassium.
Examples include spironolactone, eplerenone, and amiloride.
FUROSEMIDE
Introduction:
Frusemide, also known as furosemide, is a loop diuretic medication that is primarily used to
treat conditions such as hypertension, edema, and heart failure. It works by inhibiting the Na-
K-2Cl cotransporter in the loop of Henle of the kidney, leading to increased excretion of
sodium, potassium, and water.
Mechanism of Action:
Frusemide acts on the thick ascending limb of the loop of Henle in the kidney to inhibit the
Na-K-2Cl cotransporter. This leads to increased excretion of sodium, potassium, and water.
Frusemide also has vasodilatory effects that can help to lower blood pressure.
Chemistry:
Frusemide is a sulfonamide-based compound that has a chemical formula of
C12H11ClN2O5S. It is a white to slightly yellow crystalline powder that is practically
insoluble in water and has a melting point of approximately 206-208 °C. Frusemide is
usually administered orally or intravenously.
Uses:
Frusemide is primarily used to treat hypertension, edema, and heart failure. It is also used in
the treatment of acute pulmonary edema, hypercalcemia, and hyperkalemia. Frusemide can
be used alone or in combination with other medications, such as ACE inhibitors and beta-
blockers, to treat hypertension.
Storage and Stability Conditions:
Frusemide should be stored at room temperature, away from moisture and heat. It should be
kept in a tightly closed container and protected from light. The stability of frusemide
depends on the specific formulation and the storage conditions. Generally, frusemide tablets
have a shelf life of two to three years when stored at room temperature.

Types of Formulations and Marketed Products:


Frusemide is available in various formulations, including tablets, oral solutions, and
injectable solutions. Some of the commonly marketed products of frusemide include Lasix,
Furosemide, and Frudix. These products may have different dosages, strengths, and
formulations depending on the manufacturer and the country of origin.

CHLORTHALIDONE
Chlorthalidone is a thiazide-like diuretic medication that is primarily used to treat
hypertension and edema. It works by inhibiting the reabsorption of sodium, chloride, and
water in the distal tubules of the kidney, leading to increased excretion of these substances.
Mechanism of Action:
Chlorthalidone works by inhibiting the Na-Cl cotransporter in the distal tubules of the
kidney. This leads to increased excretion of sodium, chloride, and water, and ultimately to
reduced blood volume and lower blood pressure. Chlorthalidone also has vasodilatory effects
that can help to lower blood pressure.
Chemistry:
Chlorthalidone is a sulfonamide-based compound that has a chemical formula of
C14H11ClN2O4S. It is a white or almost white crystalline powder that is practically
insoluble in water and has a melting point of approximately 280-284 °C. Chlorthalidone is
usually administered orally.
Uses:
Chlorthalidone is primarily used to treat hypertension and edema. It is often used as a first-
line treatment for hypertension, either alone or in combination with other medications.
Chlorthalidone can also be used in the treatment of heart failure, kidney stones, and diabetes
insipidus.
Storage and Stability Conditions:
Chlorthalidone should be stored at room temperature, away from moisture and heat. It should
be kept in a tightly closed container and protected from light. The stability of chlorthalidone
depends on the specific formulation and the storage conditions. Generally, chlorthalidone
tablets have a shelf life of two to three years when stored at room temperature.
Types of Formulations and Marketed Products:
Chlorthalidone is available in tablet form and is often marketed under the brand name
Thalitone. The tablet is typically available in strengths of 15 mg or 25 mg, and is usually
taken once daily. It is also available in combination with other medications, such as ACE
inhibitors and beta-blockers, to treat hypertension.

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