LASIX - Furosemide(loop diuretics)

Furosemide is an loop diuretic.

1. FUROSEMIDE KHAWAR JAVED 16-PD-47

2. TABLE OF CONTENTS: Chemical class pharmacological class therapeutic class pregnancy category Chemistry Physio-chemical Properties Solubility storage temperature

3. Dose Pharmacokinetics Pharmacodynamics Indications adverse effects contraindications drug interactions brands

4. CHEMICAL CLASS : 2-Furfurylamino-4-chloro-5-sulfamoylbenzoic acid PHARMACOLOGICAL CLASS: loop Diuretics/high ceiling diuretics THERAPEUTIC CLASS: Edematous agent Anti-hypertensive

5. Pregnancy category: C Chemistry: Molcecular weight: 330.744g/mol Chemical formula: C12H11ClN2O5S Chemical structure:

6. Physico-Chemical properties: Color : colourless Odour: characteristic odour Taste: Bitter Solubility: Soluble in ether and polar solvents Storage Temperature : less than 35 celcius

7. DOSING FORMS AVAILABLE: IV : 10mg/ml ORAL : 10mg/ml, 8mg/ml TABLET : 20mg, 40 mg, 80mg DOSE: Edema: 20-80mg PO/daily Anti-hypertensive: 20-80mg PO/ BD HyperKalemia: 0.5-1mg /kg /day

8. PHARMACOKINETICS: ROUTE: ORAL ,IV,IM BIOAVAILABILITY: 47-64% ONSET: 30-60min (ORAL) ,30min(IM),5min(IV) PROTEIN BINDING: 91-99% Vd: 0.2L/Kg DURATION : 2 Hrs (IV) ,6-8 Hrs(Oral) METABOLISM: Liver (Glucoronidation) HALF LIFE: 30-120 mins EXCRETION: Urine( 2ml/min/kg)

9. Pharmacodynamics: Mechanism of action: Furosemide, a loop diuretic, inhibits water reabsorption in the nephron by blocking the sodium-potassium-chloride cotransporter( Na + /K + /2CL- ) in the thick ascending limb of the loop of Henle. This is achieved through competitive inhibition at the chloride binding site on the cotransporter, thus preventing the transport of sodium from the lumen of the loop of Henle into the basolateral interstitium. Consequently, the lumen becomes more hypertonic while the interstitium becomes less hypertonic, which in turn diminishes the osmotic gradient for water reabsorption throughout the nephron. Because the thick ascending limb is responsible for 25% of sodium reabsorption in the nephron, furosemide is a very potent diuretic.

10. INDICATIONS: Acute pulmonary edema in congestive heart failure acute hypercalcemia Hypertension Hyperkalemia Acute Renal Failure Anion overdose

11. ADVERSE EFFECTS: Ototoxicity Hyperuricemia Acute hypovolemia Potassium depletion Hypomagnesemia Hypokalemic Metabolic Alkalosis Allergies

12. CONTRAINDICATIONS Diuretics hypersensitivity Electrolyte Imbalance Hyperglycemia Ventricular arrhythmias acute myocardial Infarction hypovolemia Hypotension

13. DRUG INTERACTIONS: Acebutalol Cisapride Ethacrynic Acid Avanafil

14. INTERACTION WITH ACEBUTALOL: It is a beta1-blocker TYPE : Pharmacodynamic Interaction Mechanism : Acebutalol increases serum potassium while furosemide decrease serum potassium Severity :moderate Management : Monitor serum potassium closely

15. INTERACTION WITH CISAPRIDE: It is a prokinetic agent TYPE: Pharmacodynamic Interaction Mechanism :Pharmacodynamic synergism(Both reduce calcium level ,so may cause prolonging of QTc intervals) Severity : Severe Management: Contraindicated

16. INTERACTION WITH ETHACRYNIC ACID: It is a loop diuretic Type: Pharmacodynamic interaction Mechanism :Pharmacodynamic synergism(both are diuretics,so ethacrynic acid potentiate ototoxicity of Furosemide ) Severity: severe management : contraindicated

17. INTERACTION WITH AVANAFIL: It is a phosphodiesterase-5 enzyme Inhibitor Type: Pharmacodynamic interaction Mechanism :Pharmacodynamic synergism(avanafil is phosphodiestrase-5 inhibitor, causes vasodilation ,causes hypotension, so BP may reduce below normal) Severity: moderate management : change in time of administration

18. BRANDS: LASIX 40mg (sanofi aventis Pharmaceuticals (PVT) LTD) FRUMID 40mg/80mg (Goodmann Laboratories) LOSAMIDE (Pharmadic (PVT) LTD) OREX(Rex Pharmaceuticals Pakistan) FRUSINOX (Abbott Laboratories (Pakistan) LTD

19. REFERENCES: Katzung 13E Basic & Clinical Pharmacology KD Tripathi - Essentials of Medical Pharmacology, 6th Edition Lippincott Illustrated Reviews, Pharmacology - Whalen, Karen MEDSCAPE PHARMAGUIDE PAKISTAN