Rosuvastatin

Indications
 Oral
Hyperlipidaemias
Adult: Initially, 5-10 mg daily, may increase dose at 4-wkly intervals to 20 mg daily if necessary. Max: 40 mg daily. In patients receiving gemfibrozil, max: 10 mg once daily. For those receiving ciclosporin, max: 5 mg once daily.
CrCl (ml/min)Dosage Recommendation
<60Initially, 5 mg/day. Max: 20 mg/day.
<30Avoid use.
Contraindications
 Severe renal impairment, active liver disease, unexplained persistent elevations of serum transaminases; hypersensitivity. Pregnancy, lactation.
Warnings / Precautions
 Not to be used in patient with acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis e.g. sepsis, hypotension, major surgery, trauma, severe metabolic, endocrine and electrolyte disorders or uncontrolled seizures. History of liver disease and alcoholism. Discontinue treatment if there is marked or persistent increase in serum aminotransferase concentrations, significant increase in creatinine phosphokinase or evidence of myopathy.
Adverse Reactions
 Headache, dizziness, constipation, nausea, vomiting, abdominal pain, myalgia, chest pain, peripheral oedema, depression, insomnia, rash, paraesthesia, proteinuria and asthenia.
Potentially Fatal: Rhabdomyolysis with acute renal failure.
Overdose Reactions
 Symptomatic and supportive treatment should be instituted as required.
Drug Interactions
 Increased risk of myopathy when used with gemfibrozil. May increase serum levels of warfarin and oral contraceptives. Concurrent admin with aluminium/magnesium hydroxide may lead to decreased bioavailability of rosuvastatin. Serum levels may be increased by fluconazole.
Potentially Fatal: Increased risk of serious myopathy and renal failure when used with ciclosporin.
See Below for More rosuvastatin Drug Interactions
Mechanism of Actions
 Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. It increases the number of hepatic LDL receptors on the cell surface, enhancing uptake and catabolism of LDL. It also decreases apolipoprotein B, triglycerides and increases HDL.
Onset: 1 wk.
Absorption: Incompletely absorbed in the GI tract. Bioavailability: about 20%. Plasma concentrations peak 5 hr after oral admin.
Distribution: Protein-binding: 90%. Extensively taken up by the liver.
Metabolism: Limited metabolism by CYP2C9.
Excretion: Faeces (90% of an oral dose); 19 hr (elimination half-life).
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 20-25°C.
ATC Classification
 C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Storage
 Oral: Store at 20-25°C.
Available As
  • Rosuvastatin 10 mg
  • Rosuvastatin 2.5 mg
  • Rosuvastatin 20 mg
  • Rosuvastatin 40 mg
  • Rosuvastatin 5 mg

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