Drug intelligence / Profile preview

rosuvastatin + furosemide

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Rosuvastatin + furosemide is a combination of two pharmaceutical drugs, each with distinct mechanisms of action. Rosuvastatin is a statin medication that acts as a competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase), the enzyme responsible for catalyzing the conversion of HMG-CoA to mevalonate in cholesterol biosynthesis. This results in decreased hepatic cholesterol concentrations, upregulation of hepatic LDL receptors, increased uptake and clearance of LDL from plasma, and reduced synthesis of VLDL[3]. Furosemide is a loop diuretic that inhibits the Na-K-2Cl cotransporter in the thick ascending limb of the loop of Henle in the kidney, leading to increased excretion of sodium, chloride, potassium, and water[6]. It also has direct vasodilatory effects and may open potassium channels in resistance arteries[5][6]. The combination may be used when both lipid-lowering (rosuvastatin) and diuretic (furosemide) effects are desired. There are no significant pharmacokinetic interactions between these drugs at standard doses; however, high doses may slightly increase systemic exposure to rosuvastatin[2][4].

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)CA2 (Carbonic Anhydrase 2)GPR35 (G-protein Coupled Receptor 35)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)SLCO1B3 (Organic anion transporting polypeptide 1B3)NKCC2 (Sodium-potassium-chloride cotransporter 2)

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