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Loop diuretics are a class of diuretics that act on the ascending limb of the loop of Henle in the kidney to inhibit sodium and chloride reabsorption. This results in increased urine production, which helps to reduce fluid buildup in the body. They are commonly used to treat conditions such as edema associated with heart failure, liver disease, and kidney disease, as well as hypertension.
Historical
Historical
The development of loop diuretics is a fascinating story that reflects advancements in medicinal chemistry and a deeper understanding of renal physiology. Here’s a concise history:
Discovery and Development:
1. Early Diuretics:
- Before loop diuretics, mercurial diuretics were widely used in the early 20th century despite their toxicity.
- The search for safer and more effective diuretics led to the development of thiazide diuretics in the 1950s.
2. Discovery of Furosemide:
- In the late 1950s and early 1960s, chemists at Hoechst Pharmaceuticals (now part of Sanofi) in Germany were exploring new compounds for diuretic effects.
- Furosemide, also known as frusemide, was discovered in 1962 by chemist Leo Sternbach. It was found to have a potent diuretic effect, significantly more powerful than thiazides.
Development of Other Loop Diuretics:
- Following the success of furosemide, other loop diuretics were developed:
- Bumetanide: Introduced in the 1970s, known
Mechanism
Mechanism
Mechanism of Action:
Loop diuretics inhibit the sodium-potassium-chloride cotransporter (NKCC2) in the thick ascending limb of the loop of Henle. By blocking this transporter, they prevent sodium, chloride, and potassium from being reabsorbed into the bloodstream. This leads to:
- Increased excretion of sodium, chloride, and water.
- Increased excretion of potassium and calcium due to the loss of the positive voltage gradient.
- Increased urine output (diuresis).
Example of drug in the Egyptian market
Example of drug in the Egyptian market
1.furosemide
2.bumetanide
3.Torsemide
Common Loop Diuretics:
Common Loop Diuretics:
1. Furosemide (Lasix):
- The most commonly used loop diuretic.
- Available in both oral and intravenous forms.
2. Bumetanide (Bumex):
- More potent than furosemide but with a shorter duration of action.
3. Torsemide (Demadex):
- Longer duration of action compared to furosemide.
4. Ethacrynic Acid (Edecrin):
- Used less frequently due to its higher risk of ototoxicity (hearing damage).
Indications:
Indications:
- Edema: Due to heart failure, liver cirrhosis, or kidney disease.
- Hypertension: Often used when patients have resistant hypertension or require rapid blood pressure reduction.
- Hypercalcemia: By increasing calcium excretion.
- Acute pulmonary edema: To rapidly reduce fluid overload in the lungs.
How Does Furosemide Work? Understanding Loop Diuretics
How Does Furosemide Work? Understanding Loop Diuretics
Structures
Structures
Interested video for more information about Structures of loop Diuretics:
Side Effects
Side Effects
- Electrolyte Imbalances: Hypokalemia (low potassium), hyponatremia (low sodium), hypocalcemia (low calcium), and hypomagnesemia (low magnesium).
- Dehydration: Due to excessive fluid loss.
- Ototoxicity: Hearing loss or ringing in the ears, particularly with high doses or rapid intravenous administration.
- Hyperuricemia: Increased uric acid levels, which can exacerbate gout.
- Hypotension: Low blood pressure, especially when initiating therapy or increasing the dose.
Monographs:
Monographs:
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