Furosemide

Furosemide

Cat Number
API0232827
CAS Number
54-31-9

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CAS Number
54-31-9
EINECS
200-203-6
Synonyms
Frusemide, Lasix, Furanthril
Molecular Formula
C12H11ClN2O5S
Molecular Weight
330.74
Smiles
C1=COC(=C1)CNC2=CC(=C(C=C2C(=O)O)S(=O)(=O)N)Cl
Appearance
White to off-white powder
Melting Point
220℃
Boiling Point
582.1℃
General Description
Furosemide is a potent, loop diuretic belonging to the sulfonamide class, widely used to manage fluid overload. FDA-approved since the early 1980s, it is characterized by rapid onset and short duration of action.
Mechanism of Action
Furosemide inhibits the Na+/2Cl-/K+ cotransport system located in the thick ascending limb of the loop of Henle. This action blocks the reabsorption of sodium, chloride, and potassium, leading to excretion of water and electrolytes.
Application
Furosemide is indicated for edema associated with congestive heart failure, hepatic cirrhosis, and renal disease, including nephrotic syndrome. It is also used as adjunctive therapy for acute pulmonary edema and for management of hypertension. Therapy is contraindicated in anuria and in patients with hypersensitivity to sulfonamides.

McMahon BA, et al. summarized the pharmacology and evolving clinical utility of the furosemide stress test (FST) in the management of acute kidney injury (AKI). Loop diuretics, including furosemide, exert their effects through unique renal pharmacology that is significantly altered in AKI. The FST—which involves administering a standardized furosemide dose and measuring urine output over the subsequent hours—has emerged as a valuable functional assessment tool. Evidence demonstrates that the FST effectively identifies patients with AKI who are at higher risk for disease progression and need for renal replacement therapy, outperforming static biomarkers. Additionally, the test shows promise in predicting successful discontinuation of continuous renal replacement therapy in established AKI.

Fig. 1 Schematic diagram showing the 12 transmembrane domain Na-K-2Cl (NKCC) transporter in the thick ascending limb of the loop of Henle. (McMahon BA, Chawla LS, 2021) Fig. 1 Schematic diagram showing the 12 transmembrane domain Na-K-2Cl (NKCC) transporter in the thick ascending limb of the loop of Henle. (McMahon BA, Chawla LS, 2021)

References

  1. McMahon BA, Chawla LS. The furosemide stress test: current use and future potential. Ren Fail. 2021;43(1):830-839.

Mentz RJ, et al. compared torsemide versus furosemide in 2,859 patients discharged after hospitalization for heart failure, regardless of ejection fraction. Over a median follow-up of 17.4 months, all-cause mortality occurred in 26.1% of torsemide-treated patients and 26.2% of furosemide-treated patients (hazard ratio, 1.02; 95% CI, 0.89–1.18). Secondary outcomes, including all-cause mortality or hospitalization and total hospitalizations, also showed no significant differences between groups, with consistent findings across subgroups, including categories of ejection fraction.

Fig. 2 Participant flow in the TRANSFORM-HF randomized clinical trial. (Mentz RJ, <i>et al</i>, 2023) Fig. 2 Participant flow in the TRANSFORM-HF randomized clinical trial. (Mentz RJ, et al, 2023)

References

  1. Mentz RJ, et al. Effect of Torsemide vs Furosemide After Discharge on All-Cause Mortality in Patients Hospitalized With Heart Failure: The TRANSFORM-HF Randomized Clinical Trial. JAMA. 2023;329(3):214-223.

Is Furosemide sensitive to light, and what happens upon exposure?

Yes, Furosemide is highly photosensitive. Exposure to light can lead to photodegradation, causing the solution to discolor to yellow or amber. It must be stored in light-resistant containers.

What is the recommended storage temperature for Furosemide?

Store at controlled room temperature, between 15°C and 30°C. Avoid elevated temperatures, as they can accelerate degradation, especially in the presence of moisture.

Is Furosemide stable in alkaline conditions during formulation?

It is soluble in alkaline solutions but can hydrolyze over time. For bulk storage, the solid form is stable, but formulated solutions require pH control (ideally pH 8-9) and protection from light.

How is the impurity 4-chloro-5-sulfamoylanthranilic acid monitored?

This primary degradation product is specifically quantified using a stability-indicating HPLC method to ensure it remains well below pharmacopoeial limits throughout the shelf life.
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