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Rosuvastatin


A hydrophilic statin with fewer side effects.

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Introduction to Rosuvastatin

Rosuvastatin is a unique member of the statin family. It is a hydrophilic statin, meaning it has an affinity for water and tends to stay in the bloodstream rather than deeply penetrating muscle and other tissues. This property is thought to contribute to a lower risk of side effects, especially muscle-related symptoms, compared to some other statins (3).

Rosuvastatin

Considerations for Patients Taking Rosuvastatin

When prescribing or taking rosuvastatin, it’s important to consider not only its cholesterol-lowering properties but also its broader impact on cardiovascular health—and the timing of when it’s taken. Like other statins, rosuvastatin has effects that go far beyond lowering cholesterol. Many of these additional benefits help reduce overall cardiovascular risk (2, 3, 4, 7).

Statins Do Much More Than Just Lower Cholesterol

A growing body of evidence shows that statins reduce mortality across a wide range of heart conditions—including heart failure—and can even lessen the extent of damage after a heart attack. Remarkably, many of these benefits occur independently of their cholesterol-lowering effects, thanks to the pleiotropic actions of statins. These additional benefits include (2, 3, 4, 7):

  • Stabilising cholesterol deposits (atherosclerotic plaques), making them less likely to rupture and cause blood clots. This involves reducing inflammation, oxidative stress (from free radicals), and overactivity in the immune system.

  • Improving blood vessel function by helping them dilate more effectively and reducing blood viscosity, which supports smoother, more efficient circulation.


The Body Synthesises Cholesterol in the Evening

Cholesterol production in the liver follows a natural daily rhythm, peaking between 8 p.m. and midnight—with activity up to four times higher than in the morning (12). As a result, taking statins at night—especially shorter-acting ones—can help maximise their cholesterol-lowering effects.

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Why Have I Been Prescribed Statins?

Statins like rosuvastatin may be prescribed for several reasons (5):

Statins like rosuvastatin may be prescribed for several reasons (5):


  • Elevated cholesterol levels that haven’t responded sufficiently to lifestyle changes such as a healthy diet and regular physical activity.

  • Primary prevention of cardiovascular events in people at high risk of heart disease or stroke.

  • Secondary prevention after a heart attack or stroke. This is a common use of rosuvastatin, although it may be considered off-label in some regions. It is, however, strongly supported by clinical evidence.

Rosuvastatin Doses

How and when to take it

How and when to take it


Rosuvastatin is typically taken once a day, with or without food. Your starting dose and how it increases depends on your age, ethnicity, and reason for treatment. Adjustments are usually made at 4-week intervals (5).

For High Cholesterol Not Responding to Lifestyle Changes:

  • General population: Start with 5–10 mg once daily, increasing if needed to 20 mg

  • Patients of Asian origin: Start with 5 mg once daily, increasing up to 20 mg

  • Adults aged 70 and over: Start with 5 mg once daily, increasing up to 20 mg

For Preventing Cardiovascular Events:

  • Adults aged 18–69 years: Start with 20 mg once daily

  • Patients of Asian origin: Start with 5 mg once daily, with increases to 20 mg over time

Rosuvastatin Side Effects

While rosuvastatin is generally well tolerated and widely prescribed, like all medications, it can cause side effects in some individuals. Understanding the most common and less common reactions can help you monitor your response and know when to seek advice.

Muscle-Related Side Effects

Rosuvastatin is a hydrophilic statin, meaning it doesn’t penetrate body tissues—including muscle and brain—as deeply as some other statins. This doesn’t reduce its ability to lower cholesterol or inflammation, but it does lower the risk of side effects, especially muscle-related ones (3, 6).

That said, muscle symptoms are still the most common side effects of statin therapy (5, 6, 7), including:

  • Pain, soreness, or tenderness not linked to exercise or illness

  • Typically affecting both thighs, calves, or hip flexors

  • Occurring in an estimated 10–29% of patients (6)

  • Leading to statin discontinuation in many cases


Observe the Condition of Your Muscles

If you notice muscle discomfort that isn’t related to physical activity or a viral infection, speak with your GP or pharmacist. These may be early signs of statin-related muscle symptoms—and early support can help.


Who Is at Greatest Risk of Muscle Side Effects?

Certain factors increase the likelihood of developing muscle symptoms while taking statins (11):

  • Age over 60

  • Diabetes

  • Hypothyroidism

  • Multisystem diseases

  • Vitamin D deficiency

  • Strenuous physical activity

  • Alcohol consumption

  • Major surgery

  • Higher statin doses — the strongest known risk factor, increasing risk sixfold


Memory Issues

There have also been increasing reports of memory problems, especially at higher statin doses. Although research findings are mixed, if you notice memory lapses, low mood, or trouble concentrating after starting or changing your dose, speak to your GP (8, 9).


Myasthenia Gravis – A Caution

If you have myasthenia gravis and experience worsening symptoms while on rosuvastatin, inform your doctor. Although rare, statins have been reported to aggravate this condition, and any changes should be reviewed promptly.


Other Possible Side Effects

While less common, rosuvastatin may also cause:

  • Painful joints

  • Fatigue or lack of strength

  • Dizziness

  • Sleep disturbances

  • Liver enzyme changes

  • Memory problems

Rosuvastatin is considered the most hydrophilic statin, meaning it tends to stay in the bloodstream and penetrates less into tissues like muscle, liver, and brain. This property is believed to contribute to its lower risk of side effects, especially muscle-related symptoms, compared to more lipophilic statins (3, 6).

However, understanding your individual risk of side effects from statins can still be challenging. A pharmacogenomics (PGx) test in the UK can reveal how your genes influence your response to medications like rosuvastatin, enabling safer, more personalised medicine through genetic testing for medication response.

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How Your Body and Genes Process Rosuvastatin

Rosuvastatin’s journey through the body—how it’s absorbed, distributed, metabolised, and eliminated—is shaped by both biological processes and your genetic makeup. These areas of study are known as pharmacokinetics and pharmacogenetics, and they help explain why the same medication can affect different people in different ways (10).

AbsorptionAbsorption

Rosuvastatin has unique properties compared to other statins. It is the most hydrophilic statin, meaning it has a strong affinity for water and exists in a water-soluble salt form. This contributes to its targeted action and limited tissue penetration. Its oral bioavailability is approximately 20%—comparable to atorvastatin, pravastatin, and fluvastatin, and higher than simvastatin and lovastatin.

MetabolismMetabolism

Rosuvastatin undergoes minimal liver metabolism. It is taken up into liver cells (hepatocytes) via several transporters, including:

  • OATP1B1 (encoded by the SLCO1B1 gene)

  • OATP1B3

  • OATP2B1

Once in the liver, it is processed by enzymes such as UGT1A1 and UGT1A3, primarily through a process called lactonization. Two transport proteins, BCRP (Breast Cancer Resistance Protein) and P-glycoprotein (P-gp), are mainly responsible for moving rosuvastatin into the bile for excretion.

EliminationElimination

Rosuvastatin has the longest half-life of any statin—about 19 hours. Around 90% of the drug is eliminated in the faeces, making it efficient and long-lasting in effect.

Personalising Rosuvastatin with Pharmacogenetics

Genetic variation can significantly affect how well rosuvastatin works—and your likelihood of experiencing side effects. Key genes involved:

SLCO1B1 (encodes OATP1B1 transporter)

  • Critical for moving rosuvastatin into liver cells.

  • Reduced function variants (such as the c.521T>C polymorphism) can lead to higher statin levels in the blood and increase the risk of muscle-related side effects.

ABCG2 (Breast Cancer Resistance Protein / BCRP)

  • Expressed in tissues like the liver, intestine, and blood-brain barrier.

  • Helps transport rosuvastatin out of cells.

  • The minor A allele is associated with 30–40% lower protein expression and higher plasma levels of rosuvastatin, increasing the risk of side effects.

Related Medications:

These pharmacogenetic insights are also relevant for other statins, particularly:

  • Atorvastatin

  • Simvastatin

  • Pravastatin

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References