This document provides information on the loop diuretic furosemide, including its chemical and pharmacological classification, dosing, pharmacokinetics, mechanism of action, indications, adverse effects, contraindications, and drug interactions. Furosemide is a loop diuretic that works by inhibiting sodium reabsorption in the loop of Henle, promoting increased excretion of sodium, chloride, potassium, and water. It is indicated for conditions like edema, hypertension, and hyperkalemia. Adverse effects include ototoxicity and electrolyte disturbances. It can interact with other diuretics or drugs that affect electrolyte levels.

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
StorageTemperature: 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.

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

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

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

14. DRUG INTERACTIONS:
• Acebutalol
• Cisapride
• Ethacrynic Acid
• Avanafil

15. 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

16. 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

17. 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

18. 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

19. 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

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