DIURETIC DRUGS Clarise Elefante Shirley Garay Daniel Alexei Garcia
Diuretic Drugs• Medications that augments “Diuresis”• Commonly known as Water Pills• Homeopathic remedies or foods that help to prevent or treat fluid retention• Used to treat heart failure, liver cirrhosis, hypertension and certain kidney diseases.
Diuresis • Process involved in the administration of the drugs • Condition in which body loses water through excess urination • Leads advantage and disadvantage of taking diuretic drugs.
Why the need to lose fluids?• Failure to excrete excess fluid from the body.• If there are renal, cardiovascular, or metabolic disorders• Congestive Heart Failure Patients- reduction of fluid in blood, reduces pressure on the heart, so that its efficiency of pumping blood is increased.
Why the need to lose fluids?• Hypertensive Patients- the loss of sodium, chlorine and water which helps in lowering of blood pressure.• To ease the discomfort of patients suffering from edema• Get rid of the body’s excess salts• May reduce blood volume.
Side Effects• Frequent urination • Blurred vision• Dehydration • Unusual bleeding or• Severe potassium bruisingdeficiencies • Loss of appetite• Electrolyte imbalance • Weight loss• Extreme weakness • May induce breast• Fatigue enlargement in men (Pot. Sparing Diuretics)
Mechanism of action• Most diuretics produce diuresis by inhibiting the reabsorption of sodium at different segments of the renal tubular system• This is accomplished by altering how the kidney handles sodium.• If the kidney excretes more sodium, then water excretion will also increase
• passes into glomerular capillaries located within the cortex (outer zone of the kidney)• 20% of the plasma that enters the glomerular capillaries is filtered• 65-70% of the filtered sodium is removed from the urine found within the proximal convoluting tubule (PCT)• thick ascending limb has a cotransport system that reabsorbs sodium, potassium and chloride at a ratio of 1:1:2• more sodium is reabsorbed and more potassium and hydrogen ion are excreted• water is reabsorbed in the collected duct through special pores• sodium originally filtered is reabsorbed by the kidney, so that less than 1% of originally filtered sodium remains in the final urine.
Osmotic Diuretics• Helps to prevent the reabsorption of water and sodium in the body• Increase the amount of blood flowing into the kidneys• Prevent the urine to get concentrated• Used during heart problems
• used to treat patients with oliguric renal failure• increases water and sodium excretion, thereby decreasing extracellular fluid volume• used clinically in osmotherapy to reduce acutely raised intracranial pressure• first drug of choice for the treatment of acute glaucoma in veterinary medicine
BRAND NAMES MANUFACTUREROsmitrol BaxterResectisol B. BraunAridol Pharmaxis
Ammonium Chloride- used as a mild diuretic,an expectorant, a weight-reducing agent and aurine acidifying Azanium chlorideagent.- combination: used tocontrol a coughassociated with a cold orother respiratory illnesses
Brand Name ManufacturerSummer’s Eve Feminine Blooming FieldsPowder, Feminine Wash,Feminine Bath andFeminine Cleansing Cloth
Carbonic Anhydrase Inhibitor• decrease bicarbonate (HCO3-) reabsorption in the proximal tubule by decreasing the amount of H+ secreted into the lumen.• inhibitors are established as hypotensive agents, diuretics and antiepileptics, with additional use in the management of gastric and duodenal ulcers, neurological disorders and osteoporosis.
• used to treat glaucoma• used with other medicines to reduce edema (excess water retention) and to help control seizures in certain types of epilepsy• also used to reduce the severity and duration of symptoms Brand names Manufacturer Cetamid Sea Pharmacom Zolmide Vista Pharma (Dist.)
Benzothiazide• Frequently are first line drugs for treating mild to moderate hypertension• Mainly inhibit reabsorption of Na+ and Cl- via action at the Na+-Cl- symporter• Used extensively to treat edema associated with congestive heart failure (CHF) and cirrhosis of the liver.• Very often combined with other antihypertensive agents• Usually given orally• Most thiazides are excreted unchanged.
Structure Activity Relationship• C-7 MUST have an unsubstituted sulfonamide and it must be directly attached to the aromatic ring• N-2 can be substituted with a small alkyl group• C-6 electron withdrawing group here increases activity electron donating groups at C-6 will cause a decrease in activity (Most clinically-used thiazides have a Cl at C-6 and a few have a CF3• 3,4-dihydro derivatives (hydrothiazides) this reduction usually results in a ~10x increase in potency compared to the oxidized thiazide ring• The lipophilicity of the C-3 substituent governs potency and duration
• used to treat high blood pressure• can lessen symptoms such as shortness of breath or swelling in your ankles and feet.• Weakness, dizziness, or a spinning sensation• Increased blood sugar (hyperglycemia) Brand Names Manufacturer Blopress Plus Zuellig CoAprovel Metro Drug Combizar United Lab Hytaz United Lab Hytzaar Zuellig Micardis Plus Metro Drug Pritor Plus Zuellig
• used to treat fluid retention (edema) that is caused by congestive heart failure, severe liver disease (cirrhosis), kidney disease, or from treatment with a steroid or hormone medicine.• also used alone or together with other medicines to treat high blood pressure (hypertension) Brand Names Manufacturer Diuril Lundbeck Inc.
LOOP DIURETICS A T Y P E O F D I U R E T I C T H AT A C T S IN THE LOOP OF HENLE. M O S T L Y U S E D F O R HYPERTENSION AND EDEMA. M A I N F U N C T I O N S : INHIBITION OF NKCC2 AND NKCC1
Loop Diuretics• Adverse Effect:• Hypokalemia• Metabolic alkalosis• Hypomagnesemia• Hyperuricemia• Dehydration (hypovolemia), leading to hypotension• Dose-related hearing loss (ototoxicity)• Drug Interaction Effects:• Hypokalemia potentiates digitalis toxicity• Non-steroidal Anti-inflammatory Drugs: reduced diuretic efficacy• Corticosteroids: Enhance Hypokalemia• Aminoglycosides: enhance ototoxicity, nephrotoxicity
FUROSEMIDE Also known as frusemide Most popular brand is Lasix® by Sanofi-Aventis Banned by the World’s Anti-doping Agency in sports due to being a masking agent. It has also been used to prevent Thoroughbred and Standard bred race horses from bleeding through the nose during races.
MECHANISM OF ACTION• It acts by inhibiting NKCC2, the luminal Na-K-2Cl symporter in the thick ascending limb of the loop of Henle
USES: For the treatment of:• Edema associated with heart failure, hepatic cirrhosis, renal impairment, nephrotic syndrome• Hypertension• Adjunct in cerebral/pulmonary edema where rapid diuresis is required (IV injection)ADVERSE EFFECTS:• Ototoxicity• Gout• Hypokalemia• In large amounts, dehydration• Sulfa allergy
ETHACRYNIC ACID• - Etacrynic acid is a phenoxyacetic acid derivative containing a ketone and a methylene group• - Known under the tradename Edecrin™• - Not a sulfonamide
USES: For the treatment of:• Edema associated with heart failure, hepatic cirrhosis, renal• impairment, nephrotic syndrome• Hypertension• Potent inhibitors of glutathione S-transferase family membersADVERSE EFFECTS:• Ototoxicity• Hypokalemia• In large amounts, dehydration• Diarrhea• In high doses, causes intestinal bleeding