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TABLE OF CONTENTS:
• Chemical class
• pharmacological class
• therapeutic class
• pregnancy category
• Chemistry
• Physio-chemical Properties
• Solubility
• storage temperature
• Dose
• Pharmacokinetics
• Pharmacodynamics
• Indications
• adverse effects
• contraindications
• drug interactions
• brands
CHEMICAL CLASS:
2-Furfurylamino-4-chloro-5-sulfamoylbenzoic acid
PHARMACOLOGICAL CLASS:
loop Diuretics/high ceiling diuretics
THERAPEUTIC CLASS:
Edematous agent
Anti-hypertensive
Pregnancy category: C
Chemistry:
Molcecular weight: 330.744g/mol
Chemical formula: C12H11ClN2O5S
Chemical structure:
Physico-Chemical properties:
Color: colourless
Odour: characteristic odour
Taste:Bitter
Solubility:Soluble in ether and polar solvents
StorageTemperature: less than 35 celcius
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
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)
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.
INDICATIONS:
• Acute pulmonary edema in congestive heart failure
• acute hypercalcemia
• Hypertension
• Hyperkalemia
• Acute Renal Failure
• Anion overdose
ADVERSE EFFECTS:
• Ototoxicity
• Hyperuricemia
• Acute hypovolemia
• Potassium depletion
• Hypomagnesemia
• Hypokalemic Metabolic Alkalosis
• Allergies
CONTRAINDICATIONS
• Diuretics hypersensitivity
• Electrolyte Imbalance
• Hyperglycemia
• Ventricular arrhythmias
• acute myocardial Infarction
• hypovolemia
• Hypotension
DRUG INTERACTIONS:
• Acebutalol
• Cisapride
• Ethacrynic Acid
• Avanafil
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
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
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
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
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
REFERENCES:
• Katzung 13E Basic & Clinical Pharmacology
• KD Tripathi - Essentials of Medical Pharmacology, 6th
Edition
• Lippincott Illustrated Reviews, Pharmacology - Whalen,
Karen
• MEDSCAPE
• PHARMAGUIDE PAKISTAN

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LASIX - Furosemide(loop diuretics)

  • 1.
  • 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.
  • 10.
  • 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