Rosuvastatin; Uses, Dosage, Side Effects, Drug Interactions

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

Side Effects of Rosuvastatin

The most common

• back pain
• constipation
• muscle aches
• Nausea and vomiting
• Severe stomach ache
• diarrhoea,
• anorexia,
• flatulence,
• headache,
• dizziness,
• heartburn
• joint pain

 Common

• Nausea and vomiting
• Severe stomach ache
• Severe diarrhea
• Mouth sores
• Vaginal thrush
• Skin rash
• Headache

Less common

• Difficulty with moving
• joint pain
• muscle aching or cramping
• muscle pains or stiffness
• pain in the arms and legs
• swollen joints
• Back pain
• difficulty having a bowel movement
• Burning, numbness, tingling, or painful sensations
• decreased interest in sexual intercourse
•  discouragement

Drug Interactions of Rosuvastatin

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

• antacids (if taken within 2 hours of taking rosuvastatin)
• clopidogrel
• colchicines
• cyclosporine
• daptomycin
• dronedarone
• eltrombopag
• fenofibrate
• gemfibrozil
• hepatitis? C virus protease inhibitors (e.g., boceprevir, simeprevir, telaprevir)
• itraconazole
• proton pump inhibitors (PPIs; e.g., lansoprazole, omeprazole, pantoprazole)
• other “statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
• trabectedin
• warfarin

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