Rosuvastatin; Uses, Dosage, Side Effects, Drug Interactions

Rosuvastatin
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Rosuvastatin is a statin with antilipidemic and potential antineoplastic activities. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. In addition, rosuvastatin, like other statins, exhibits pro-apoptotic, growth inhibitory, and pro-differentiation activities in a variety of tumor cell types; these antineoplastic activities may be due, in part, to inhibition of the isoprenylation of Ras and Rho GTPases and related signaling cascades.

Rosuvastatin is a member of the drug class of statins, used in combination with exercise, diet, and weight-loss to treat high cholesterol and related conditions and to prevent cardiovascular disease. that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.

Mechanism of Action of Rosuvastatin

Rosuvastatin is a competitive inhibitor of HMG-CoA reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Rosuvastatin acts primarily in the liver. Decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low density lipoprotein (LDL) receptors which increases hepatic uptake of LDL. Rosuvastatin also inhibits hepatic synthesis of very low density lipoprotein (VLDL). The overall effect is a decrease in plasma LDL and VLDL. In vitro and in vivo animal studies also demonstrate that rosuvastatin exerts vasculoprotective effects independent of its lipid-lowering properties. Rosuvastatin exerts an anti-inflammatory effect on rat mesenteric microvascular endothelium by attenuating leukocyte rolling, adherence and transmigration . The drug also modulates nitric oxide synthase (NOS) expression and reduces ischemic-reperfusion injuries in rat hearts . Rosuvastatin increases the bioavailability of nitric oxide by upregulating NOS  and by increasing the stability of NOS through post-transcriptional polyadenylation . It is unclear as to how rosuvastatin brings about these effects though they may be due to decreased concentrations of mevalonic acid.

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Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol. In vivo studies in animals, and in vitro studies in cultured animal and human cells have shown rosuvastatin to have a high uptake into, and selectivity for, action in the liver, the target organ for cholesterol lowering. In in vivo and in vitro studies, rosuvastatin produces its lipid-modifying effects in two ways. First, it increases the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL. Second, rosuvastatin inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.

Indications of Rosuvastatin

  • High Cholesterol
  • High Cholesterol, Familial Homozygous
  • High Cholesterol, Familial Heterozygous
  • Atherosclerosis
  • Prevention of Cardiovascular Disease
  • Atherosclerotic Cardiovascular Diseases
  • Cardiovascular Disease
  • Dysbetalipoproteinemia
  • Hyperlipoproteinemia
  • Hyperlipoproteinemia Type III, Elevated beta-VLDL IDL
  • Hyperlipoproteinemia Type IIa, Elevated LDL
  • Hyperlipoproteinemia Type IIb, Elevated LDL VLDL
  • Hyperlipoproteinemia Type IV, Elevated VLDL
  • Fredrickson type IIb hyperlipidemia
  • Heterozygous Familial Hypercholesterolemia
  • Homozygous Familial Hypercholesterolemia
  • Hypertriglyceridemias
  • Mixed hypercholesterolemia
  • Used as an adjunct to dietary therapy to treat primary hyperlipidemia (heterozygous familial and nonfamilial), mixed dyslipidemia and hypertriglyceridemia. Also indicated for homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering therapies or when other such therapies are not available. Furthermore, it is used to slow the progression of atherosclerosis and for primary prevention of cardiovascular disease.

Contra Indications of Rosuvastatin

  • Untreated Decreased Level of Thyroid Hormones
  • Extreme Loss of Body Water
  • alcoholism
  • hemorrhage in the brain
  • Liver Failure
  • liver problems
  • severe renal impairment
  • Bloody Urine
  • rhabdomyolysis
  • recent operation
  • Loss of Memory
  • High Blood Sugar
  • Proteinuria
  • trauma
  • pregnancy
  • a mother who is producing milk and breastfeeding
  • Muscle Pain or Tenderness with Increase Creatine Kinase
  • Metabolic Syndrome X
  • Muscle Damage Due to Auotimmunity
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Side Effects of Rosuvastatin

The most common

 Common

Less common

Drug Interactions of Rosuvastatin

Rosuvastatin may interact with following drugs, suppliments & may change the efficasy of drug

Pregnancy & Lactation of Rosuvastatin

FDA Pregnancy Catagory X

Pregnancy

This medication should not be taken during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

It is not known if rosuvastatin passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

References

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