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Rosuvastatin and Pharmacogenomics

Published 02/05/2025

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A Smarter, Safer Approach to Cholesterol Management

Rosuvastatin is a commonly prescribed statin used to lower cholesterol and reduce the risk of cardiovascular events. Unlike other statins, it’s hydrophilic, meaning it tends to stay in the bloodstream and has minimal penetration into muscle and brain tissue—making it less likely to cause certain side effects. However, not everyone responds to rosuvastatin in the same way.

With the rise of pharmacogenomics in the UK, it’s now possible to use genetic testing for medication response to understand how your genes influence your reaction to medications like rosuvastatin. This personalised medicine approach doesn’t just improve safety and effectiveness for individuals—it also has the potential to lower NHS costs by reducing trial-and-error prescribing, preventing avoidable side effects, and helping patients stay on treatment.

Introduction to Rosuvastatin

Rosuvastatin is a unique member of the statin family. As a hydrophilic statin, it remains primarily in the bloodstream, penetrating body tissues—such as muscle, liver, and brain—to a lesser extent. This property contributes to its lower risk of muscle-related side effects (3, 6).

Considerations for Patients Taking Rosuvastatin

When prescribing or taking rosuvastatin, it’s important to consider not only its cholesterol-lowering effects but also its broader impact on heart health. Like other statins, rosuvastatin has pleiotropic effects—benefits that go beyond cholesterol reduction (2, 3, 4, 7).

Statins Do More Than Just Lower Cholesterol

Evidence shows that statins reduce mortality across a wide range of cardiovascular conditions—including heart failure—and even reduce damage after a heart attack. These effects occur partly due to:

Stabilising cholesterol plaques, making them less likely to rupture
Improving blood vessel function and reducing blood viscosity
Reducing inflammation and oxidative stress

The Body Makes More Cholesterol at Night

Cholesterol synthesis peaks between 8 p.m. and midnight (12). Taking statins in the evening—particularly short-acting ones—can enhance their cholesterol-lowering effects. While rosuvastatin has a longer half-life than many statins, evening dosing is still often recommended.

Why Rosuvastatin May Be Prescribed

Rosuvastatin may be prescribed for several reasons (5):

Elevated cholesterol that hasn’t responded to lifestyle changes
Primary prevention of heart disease or stroke in high-risk individuals
Secondary prevention after a cardiovascular event (e.g. heart attack)—though this may be off-label in some regions, it is widely supported by clinical evidence

Rosuvastatin Doses: How and When to Take It

Rosuvastatin is typically taken once daily, with or without food. Dose adjustments are made at 4-week intervals.

For high cholesterol:

General population: Start with 5–10 mg daily; increase to 20 mg if needed
Asian patients: Start with 5 mg daily; increase gradually to 20 mg
Patients over 70: Start with 5 mg daily; increase gradually to 20 mg

For cardiovascular prevention:

Adults aged 18–69: 20 mg daily
Asian patients: Start with 5 mg daily, increasing to 20 mg as needed

Rosuvastatin Side Effects

Rosuvastatin is generally well tolerated, but as with any medication, side effects can occur.

Muscle-Related Side Effects

Because it is hydrophilic, rosuvastatin enters muscle tissue less than other statins—reducing the risk of muscle pain or weakness (3, 6). Still, muscle symptoms remain the most common side effect and include:

Pain, soreness, or tenderness (especially if unrelated to exercise)
Often affects both thighs, calves, or hip flexors
Occurs in 10–29% of statin users (6)

Other Side Effects May Include:

Joint pain
Tiredness or weakness
Dizziness
Sleep issues
Liver enzyme changes
Memory concerns, especially at higher doses

If you experience any of these symptoms, pharmacogenetic testing for statins may help uncover if your genes are part of the cause.

Who Is at Higher Risk of Side Effects?

Statin-related side effects are more likely in people with:

Age over 60
Diabetes
Hypothyroidism
Vitamin D deficiency
High physical activity levels
Alcohol use
Major surgery
Higher statin doses (strongest risk factor)

Myasthenia Gravis – A Special Warning

If you have myasthenia gravis and notice worsening symptoms while taking rosuvastatin, speak to your GP. Though rare, statins have been reported to aggravate this condition.

How Genetics and Your Body Handle Rosuvastatin

Rosuvastatin’s absorption, metabolism, and elimination involve several genes that can affect how the drug works in your body (10).

Absorption:

20% oral bioavailability
Most hydrophilic of all statins—exists as a water-soluble salt

Metabolism:

Minimal liver metabolism
Transported into liver cells via OATP1B1, OATP1B3, and OATP2B1
Lactonised via UGT1A1 and UGT1A3
Excreted via BCRP (Breast Cancer Resistance Protein) and P-glycoprotein (P-gp)

Elimination:

Longest statin half-life: 19 hours
Eliminated mostly through faeces (90%)

Personalising Rosuvastatin with Pharmacogenetics

Several genes influence how well rosuvastatin works and your risk of side effects:

SLCO1B1

Encodes the OATP1B1 transporter, which moves rosuvastatin into the liver
Reduced function variants (like c.521T>C) can raise statin levels in the blood and increase muscle side effect risk

ABCG2 (BCRP)

Involved in drug transport across tissues
The minor A allele leads to 30–40% lower protein expression and higher rosuvastatin levels, increasing side effect risk

Rosuvastatin is considered the most hydrophilic statin, meaning it remains mostly in the bloodstream and minimally penetrates tissues like muscle, liver, and brain. This helps explain why it’s associated with fewer side effects than more lipophilic statins (3, 6).

Still, understanding your individual risk of side effects can be difficult. A pharmacogenomics (PGx) test in the UK can help identify how your genes influence your response to medications like rosuvastatin, supporting safer, more personalised medicine through genetic testing for medication response.

References:

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