Rosuvastatin

Introduction


Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, also known as a "statin." 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.

Indication

  • Rosuvastatin is used for Lowering high cholesterol and triglycerides in certain patients.
  • It also increases high-density lipoprotein (HDL) ("good") cholesterol levels.
  • It is used to slow atherosclerosis (narrowing of the arteries) in patients with high blood cholesterol levels.
  • It is used in certain patients to reduce the risk of heart attack or stroke.
  • It is also used in certain patients to reduce the need for medical procedures to open blocked heart vessels. It is used along with an appropriate diet.
  • In summary rosuvastatin may used for Atherosclerosis, Atherosclerotic Cardiovascular Diseases, Cardiovascular Diseases, Dysbetalipoproteinemia, Familial hyperlipidemia, Heterozygous Familial Hypercholesterolemia, Homozygous Familial Hypercholesterolemia, Hypertriglyceridemias and Mixed hypercholesterolemia

Pharmacokinetics



Pharmacodynamics

Contra-indications:

  • allergy to any ingredient in rosuvastatin
  • active liver disease or unexplained abnormal liver function tests
  • pregnancy or breast-feeding

Cautions:

  • This product should be used with caution if the patients are planning to become pregnant
  • Also should be used with caution in patients with kidney disease
  • Grapefruit or grapefruit juice has been known to interact with this medication, leading to serious problems.
  • Safety and efficacy have been not established in patients younger than 7 years.
  • This drug should be used in addition to a diet restricted in saturated fat and cholesterol when response to diet and nonpharmacologic interventions alone has been inadequate.

Drug interactions:


  • The following drugs might increase the risk of muscle problems if take them with rosuvastatin: Cyclosporine (Gengraf, Neoral, or Sandimmune), Gemfibrozil (Lopid) should not be combined, Fenofibric acid (Fibricor or Trilipix), Fenofibrate (Antara, Fenoglide, Lipofen, Lofibra, Tricor, or Triglide)
  • Other medications that might increase the negative effects are HIV drugs, including: Atazanavir (Reyataz), Ritonavir (Norvir), Lopinavir/ritonavir (Kaletra), Saquinavir (Invirase)
  • Rosuvastatin should not take with any other statin such as atorvastatin (Lipitor), lovastatin (Mevacor), pravastatin (Pravachol), or simvastatin (Zocor or Vytorin).
  • Some other drugs should be combined with caution such as warfarin (Coumadin or Jantoven) cimetidine (Tagamet), ketoconazole (Nizoral), and birth control pills.
  • It’s also important to refrain from taking aluminum and magnesium hydroxide antacids, such as Mylanta and Maalox, within two hours of using this drug.

Side-effects:

The most frequently reported side effects included:
  • Headache and dizziness
  • Muscle and joint pain
  • Abdominal pain
  • Asthenia
  • Nausea
  • Elevated sugar levels
  • Memory loss
  • Confusion

Dosage:

F.C tablet: 10,20mg


Following initiation or upon titration of this drug, lipid levels should be analyzed within 2 to 4 weeks and the dosage adjusted accordingly.
• Renal Dose Adjustments
Severe renal dysfunction (not on hemodialysis [CrCl less than 30 mL/min]):
-Initial dose: 5 mg orally once a day
-Maximum dose: 10 mg orally once a day
• Liver Dose Adjustments
Chronic alcohol liver disease: Caution recommended.
Active liver disease or persistent elevations of hepatic transaminase levels: Contraindicated