DIURETIC AGENT, STRUCTURE, SAR, MOA AND USES
- 1. By- Dr. Prerana B. Jadhav M. Pharm, Ph.D. Pharmaceutical Chemistry Assistant Professor, Sanjivani College of Pharmaceutical Education and Research, Kopargaon. DIURETICS
- 2. Introduction • Kidneys remove waste products from the blood and produce urine. Kidneys control the levels of many substances in the blood. Kidneys help to control the blood pressure.
- 3. DIURETICS
- 4. • Diuretics results in decrease in body fluids (extracellular fluids) • Four major sites of Nephron that are responsible for reabsorption • 1. Proximal Convoluted Tubule • 2. Ascending Loop of Henle • 3. Distal Convoluted Tubule • 4. Collecting Duct
- 7. Functions of Diuretics • Used to prevent and alleviate edema and ascitis (build of fluid in space between the lining of abdomen and abdominal organs) • Used in hypertension and diabetes insipidus (caused by problem with hormone arginine vasopressin which plays key role in regulating the amount of fluid in the body) • Acute renal failure • Pulmonary edema. • Nephritic syndrome • Glaucoma • High intracranial pressure
- 8. Classification of Diuretics • Carbonic anhydrase inhibitors: Acetazolamide, Methazolamide, Dichlorphenamide. • Thiazides: Chlorthiazide, Hydrochlorothiazide, Hydroflumethiazide, Cyclothiazide • Loop diuretics: Furosemide, Bumetanide, Ethacrynic acid. • Potassium sparing Diuretics: Spironolactone, Triamterene, Amiloride. • Osmotic Diuretics: Mannitol
- 18. Osmotic Diuretics • Inhibits water reabsorption in the proximal convoluted tubule, loop of henle & collecting duct, where membrane is most permeable to water. • Ex. Mannitol: It hinders tubular reabsorption of water and enhances excretion of sodium & chloride by elevating the osmolarity of glomerular filtrate.
- 19. Uses: • Management of cerebral edema • Diagnostic agent for kidney function • To increase urine volume in patients with acute renal failure.
- 20. LOOP DIURETIC
- 24. • MOA: Competitive inhibition of sodium-potassium-chloride cotransporters (NKCC2) expressed along these tubules in the nephron, preventing the transport of sodium ions from the lumenal side reabsorption. This inhibition results in increased excretion of water along with sodium, chloride, magnesium, calcium, hydrogen, and potassium ions • USES: Loop diuretics are medications used in the management and treatment of fluid overload conditions such as heart failure, nephrotic syndrome or cirrhosis, and hypertension