Crestor

$ 119.48$ 486.75

Category: Heart & Cholesterol
Commercial name: Crestor
Active ingredient: Rosuvastatin
Production form: Pills
Available dosage: 5 mg, 10 mg, 20 mg

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Description

Crestor (Rosuvastatin). Dosage, Side Effects, Interactions

The active ingredient of Crestor –  Rosuvastatin belongs to the statin group of drugs and is used to treat high cholesterol levels in the blood. Rosuvastatin lowers elevated LDL cholesterol, total cholesterol and triglycerides and increases HDL cholesterol.

Crestor (Rosuvastatin) is used to treat

  • Hypercholesterolaemia in adults, adolescents and children over 6 years of age
  • Prevention of cardiovascular events in patients at high risk for new cardiovascular events

Rosuvastatin can be taken at any time of the day, regardless of meals.

Application type

The active ingredient rosuvastatin is available on the market in the form of tablets and hard capsules. In addition, the active ingredient is available as a combination preparation with ezetimibe and amlodipine

How Crestor (Rosuvastatin) works

Like all statins, rosuvastatin interferes with the metabolism of cholesterol and inhibits the enzyme HMG-CoA reductase, which catalyses the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, a precursor of cholesterol. As a result, cholesterol biosynthesis is interrupted at an early stage and the cholesterol level in the cells drops.

Rosuvastatin lowers elevated LDL cholesterol, total cholesterol and triglycerides and increases HDL cholesterol.

Pharmacokinetics

Rosuvastatin reaches peak plasma levels approximately 5 hours after oral administration. The absolute bioavailability is about 20 percent. Rosuvastatin is primarily taken up by the liver and only about 10 percent is metabolised by enzymes in the cytochrome P450 system. Approximately 90 percent of the rosuvastatin dose is excreted unchanged in the stool and approximately 5 percent is excreted unchanged in the urine. The plasma elimination half-life is approximately 19 hours and does not increase with higher doses.

Dosage of Crestor (Rosuvastatin)

  • Starting dose : 5 mg or 10 mg Rosuvastatin once daily.
  • If necessary, the dose can be adjusted after 4 weeks to the next higher dose.
  • Maximum dose : 40 mg rosuvastatin once daily.

Side effects of Crestor (Rosuvastatin)

The following side effects have occurred frequently (≥ 1/100 to < 1/10) during therapy with rosuvastatin:

  • diabetes mellitus
  • headache, dizziness
  • Constipation, nausea, abdominal pain
  • myalgia
  • asthenia

As with other HMG-CoA reductase inhibitors, the frequency of side effects is often dose-dependent.

interactions

The following interactions exist for the use of rosuvastatin:

  • Transport protein inhibitors: Rosuvastatin is a substrate of certain transport proteins including the hepatic uptake transporter OATP1B1 and the efflux transporter BCRP. Co-administration of rosuvastatin and medicinal products that inhibit these transporters may result in increased rosuvastatin plasma concentrations and an increased risk of myopathy.
  • Ciclosporin : During concomitant treatment with rosuvastatin and ciclosporin, the AUC values ​​for rosuvastatin were on average 7-fold higher than the values ​​observed in healthy subjects.
  • Protease Inhibitors: Concomitant use of protease inhibitors with rosuvastatin may greatly increase the bioavailability of rosuvastatin.
  • Gemfibrozil and other lipid-lowering medicinal products: Co-administration of rosuvastatin and gemfibrozil resulted in a 2-fold increase in rosuvastatin Cmax and AUC.
  • Ezetimibe : Co-administration of rosuvastatin 10 mg and ezetimibe 10 mg resulted in a 1.2-fold increase in rosuvastatin AUC in patients with hypercholesterolaemia.
  • Antacids: Co-administration of rosuvastatin and an antacid suspension containing aluminum and magnesium hydroxide resulted in a decrease in rosuvastatin plasma levels of approximately 50%. This effect was attenuated when the antacid dose was administered 2 hours after rosuvastatin.
  • Erythromycin : Co-administration of rosuvastatin and erythromycin resulted in a 20% decrease in rosuvastatin AUC(0-t) and a 30% decrease in Cmax. This interaction is thought to be caused by an increase in gut motility induced by erythromycin.
  • Fusidic acid : The risk of myopathy including rhabdomyolysis may be increased when fusidic acid and statins are administered systemically . There have been reports of rhabdomyolysis (including some fatalities) in patients receiving this combination.
  • Cytochrome P450 enzymes: Results from in vitro and in vivo studies indicate that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450 isoenzymes. In addition, rosuvastatin is a poor substrate for these isoenzymes. Therefore, no drug-drug interactions based on cytochrome P-450 mediated metabolism are expected.
  • Vitamin K antagonists: There may be an increase in the International Normalized Ratio (INR) at the start of treatment. Discontinuation or dose reduction of rosuvastatin may result in a decrease in INR.
  • Oral contraceptives/hormone replacement therapy: Co-administration of rosuvastatin and an oral contraceptive resulted in a 26% and 34% increase in ethinyl estradiol and norgestrel AUC, respectively . There are no pharmacokinetic data in patients receiving concomitant rosuvastatin and hormone replacement therapy. Therefore, a similar effect cannot be ruled out.

Contraindication

Rosuvastatin has the following contraindications:

  • Known hypersensitivity to rosuvastatin
  • Active liver disease, including unexplained and persistent elevations in serum transaminases, and any elevation in serum transaminases greater than 3 times the upper limit of normal
  • severe renal impairment (creatinine clearance < 30 ml/min)
  • myopathy
  • Simultaneous treatment with ciclosporin
  • Pregnancy and lactation and in women of childbearing potential who are not using appropriate contraceptive measures.

The 30 mg and 40 mg doses are contraindicated in patients with predisposing factors for myopathy/rhabdomyolysis. Such factors include:

  • moderate renal impairment (creatinine clearance < 60 ml/min)
  • hypothyroidism
  • hereditary muscle disorders in personal or family history
  • muscle-damaging effects from previous use of a fibrate or other HMG-CoA reductase inhibitor
  • alcohol abuse
  • Situations where increased plasma concentrations may occur
  • Asian descent
  • simultaneous use of fibrates

Pregnancy

Rosuvastatin is contraindicated during pregnancy and lactation. Women of childbearing potential must use appropriate contraceptive measures. Cholesterol and other products of cholesterol biosynthesis are necessary for fetal development, therefore the potential risk from inhibition of HMG-CoA reductase outweighs the benefit of treatment during pregnancy.

Lactation

Rosuvastatin is excreted in the milk of rats. There are no data on the excretion of rosuvastatin in human milk.

Driving ability

When driving vehicles or using machines it should be taken into account that dizziness may occur during treatment with rosuvastatin.

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Additional information

Dosage

5 mg, 10 mg, 20 mg

Quantity

30, 60, 90, 120, 180

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