What is rosuvastatin, and how does it work (mechanism of action)?
Rosuvastatin is an oral drug for lowering
blood cholesterol levels. It belongs to a class of drugs called HMG-CoA
reductase inhibitors, more commonly referred to as "statins." Other drugs in
this class include
- simvastatin (Zocor),
- lovastatin (Mevacor),
- pravastatin (Pravachol),
- atorvastatin (Lipitor) and
- fluvastatin (Lescol).
These drugs reduce cholesterol
levels by inhibiting HMG-CoA reductase, an enzyme that produces cholesterol in
the liver. Rosuvastatin and other statins lower blood total cholesterol as well
as blood LDL cholesterol levels. LDL cholesterol is the "bad" type of
cholesterol that increases the risk of
coronary artery disease (atherosclerosis)
and heart attacks. Lowering LDL cholesterol levels slows the progression of
coronary artery disease and may even reverse it. Statins also increase HDL
cholesterol, the "good" type of cholesterol, and reduce triglycerides.
Scientists have discovered that in addition to atherosclerosis, inflammation of
the coronary arteries may also contribute to the development of heart attacks.
The presence of inflammation can be determined by measuring a chemical in the
blood called highly sensitive, C-reactive protein (Hs-CRP). Moreover, Hs-CRP can
be used to predict the occurrence of heart attacks,
strokes and death. Hs-CRP
is, in fact, a better predictor of the risk for heart attacks than LDL
cholesterol. Scientists have found that statins reduce the level of Hs-CRP in
the body, presumably by reducing inflammation in the coronary arteries, and this
may be another mechanism through which statins prevent heart attacks, strokes,
and death. More research needs to be conducted, however, to confirm the
importance of inflammation and the mechanisms through which statins work.
Rosuvastatin was approved by the FDA in August 2003.
What brand names are available for rosuvastatin?
Crestor
Is rosuvastatin available as a generic drug?
GENERIC AVAILABLE: No
Do I need a prescription for rosuvastatin?
Yes
What are the uses for rosuvastatin?
Rosuvastatin is used for the reduction of blood total
cholesterol, HDL cholesterol and triglyceride levels, and to increase HDL
cholesterol levels. Rosuvastatin also is used for reducing the risk of heart
attacks, stroke, and arterial revascularization procedures in patients without
clinically evident coronary heart disease but with multiple risk factors for
heart disease.
What are the side effects of rosuvastatin?
The most common side effects of rosuvastatin are:
- headache,
- nausea,
- vomiting,
- diarrhea and
- muscle pain.
Other important side effects include:
- post-marketing reports of memory loss,
- forgetfulness,
- amnesia,
- confusion, and
- memory impairment.
Symptoms may start one day to years after starting treatment
and resolve within a median of three weeks after stopping the statin.
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What is the dosage for rosuvastatin?
The starting dose for most adults is 5 mg once daily. The
maximum dose is 40 mg daily, and this dose should be reserved for patients who
do not adequately respond to a 20 mg dose.
Which drugs or supplements interact with rosuvastatin?
When administered with cyclosporine, the blood
level of rosuvastatin increases seven fold, and this could increase the side
effects of rosuvastatin.
Rosuvastatin increases the action of the blood thinner
warfarin (Coumadin) and could increase the risk of bleeding from warfarin.
Antacids reduce the absorption of rosuvastatin and should be administered two
hours after rosuvastatin.
The use of rosuvastatin with nicotinic acid,
gemfibrozil
(Lopid) or other drugs that may cause liver or muscle injury may increase
the incidence of the muscle injury.
QUESTION
What is cholesterol?
See Answer
Is rosuvastatin safe to take if I’m pregnant or breastfeeding?
Statins should not be used by pregnant women because there is a high risk of harm to the fetus.
There is no information on whether rosuvastatin is excreted in human milk.
What else should I know about rosuvastatin?
What preparations of rosuvastatin are available?
Tablets: 5, 10, 20, and 40 mg
How should I keep rosuvastatin stored?
Rosuvastatin should be stored at room temperature between
2 C – 25 C (36 F – 77 F).