Crestor

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Crestor on Prescriptsy

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Crestor is the brand name for rosuvastatin calcium, a potent HMG-CoA reductase inhibitor belonging to the statin class of medicines.

It is licensed in the United Kingdom for the treatment of primary hypercholesterolaemia (including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia, and for the reduction of cardiovascular events in adults judged to be at high risk of a first cardiovascular event.

Rosuvastatin is the most potent statin currently available on a milligram-for-milligram basis, making it particularly valuable for patients who need substantial reductions in LDL cholesterol to reach their treatment targets.

Cardiovascular disease remains the leading cause of death worldwide. In the UK, coronary heart disease causes approximately 64,000 deaths each year, and stroke accounts for a further 36,000.

Elevated LDL cholesterol is among the strongest modifiable risk factors for atherosclerotic cardiovascular disease, and decades of clinical trial evidence have established that lowering LDL cholesterol with statins significantly reduces the incidence of heart attacks, strokes, and cardiovascular death.

This page provides a comprehensive clinical overview of Crestor, including how it works, correct dosing, expected benefits, side effects, safety warnings, and how to obtain a prescription in the UK.

Important safety information about Crestor

Before reading further, note the following essential safety points. Crestor is a prescription-only medicine (POM) and must only be taken under medical supervision.

• Report any unexplained muscle pain, tenderness, or weakness to your doctor, especially if accompanied by fever, malaise, or dark brown urine. These may be signs of myopathy or rhabdomyolysis, a rare but serious condition requiring immediate medical attention.
• Crestor must not be taken during pregnancy or breastfeeding.
• The 40 mg dose should only be prescribed under specialist supervision and is not suitable for certain patient groups, including those of Asian origin and those with moderate kidney impairment.
• Tell your doctor about all medicines you take. Certain drugs, including ciclosporin and fusidic acid, must not be used with Crestor.

Understanding cholesterol and cardiovascular risk

Cholesterol is a waxy, fat-like substance that the body needs for building cell membranes, producing hormones, and synthesising vitamin D.

Most cholesterol is manufactured by the liver, with a smaller proportion absorbed from dietary sources. Cholesterol travels through the bloodstream in lipoprotein particles.

Low-density lipoprotein (LDL) carries cholesterol from the liver to the tissues and, when present in excess, deposits it in the walls of arteries.

This process, known as atherosclerosis, leads to the formation of fatty plaques that narrow and harden the arteries over time, restricting blood flow and increasing the risk of heart attack and stroke.

High-density lipoprotein (HDL) performs the opposite function, transporting cholesterol away from the arterial walls back to the liver for excretion.

A high LDL-to-HDL ratio is therefore associated with increased cardiovascular risk. Triglycerides, another type of blood fat, also contribute to atherosclerotic risk when elevated.

The goal of lipid-lowering therapy is to reduce LDL cholesterol to a level that slows or halts atherosclerotic progression and reduces the likelihood of cardiovascular events.

NICE recommends a target LDL reduction of at least 40% from baseline for primary prevention and a non-HDL cholesterol target below 2.5 mmol/L for secondary prevention.

How Crestor works: mechanism of action

Rosuvastatin inhibits HMG-CoA reductase, the enzyme that catalyses the conversion of HMG-CoA to mevalonate, the rate-limiting step in the cholesterol biosynthesis pathway.

By blocking this enzyme in hepatocytes, rosuvastatin reduces intracellular cholesterol concentration. The liver responds by upregulating the expression of LDL receptors on the hepatocyte surface.

These receptors bind and internalise circulating LDL particles, effectively clearing LDL cholesterol from the bloodstream.

Rosuvastatin also reduces the hepatic production and secretion of very-low-density lipoprotein (VLDL), the precursor to LDL, which contributes to its triglyceride-lowering effect. Additionally, it produces a modest increase in HDL cholesterol, further improving the overall lipid profile.

Compared with other statins, rosuvastatin has the highest affinity for HMG-CoA reductase and the greatest selectivity for hepatic tissue.

Its long plasma half-life (approximately 19 hours) means it provides sustained enzyme inhibition throughout the day, regardless of the time of administration.

Unlike simvastatin and atorvastatin, rosuvastatin undergoes minimal metabolism by the CYP3A4 enzyme, which significantly reduces the potential for drug-drug interactions mediated by this pathway.

Clinical evidence and UK prescribing guidance

The clinical efficacy of rosuvastatin has been demonstrated in numerous large-scale trials.

The JUPITER trial enrolled nearly 18,000 apparently healthy individuals with elevated high-sensitivity C-reactive protein (hsCRP) and LDL cholesterol below 3.4 mmol/L and showed that rosuvastatin 20 mg reduced the primary composite endpoint of cardiovascular events by 44% compared with placebo.

The METEOR trial demonstrated that rosuvastatin 40 mg slowed the progression of carotid artery intima-media thickness in patients with subclinical atherosclerosis.

In the UK, NICE guideline CG181 (Cardiovascular disease: risk assessment and reduction, including lipid modification) recommends atorvastatin 20 mg as the first-line statin for primary prevention and atorvastatin 80 mg for secondary prevention.

However, rosuvastatin is a well-established alternative when atorvastatin is not tolerated, when a patient requires greater LDL reduction than atorvastatin can provide at the available dose, or when CYP3A4 drug interactions are a concern.

Rosuvastatin 5 to 10 mg produces LDL reductions broadly equivalent to atorvastatin 10 to 20 mg, while rosuvastatin 20 to 40 mg can achieve reductions comparable to the highest atorvastatin doses.

Who is Crestor suitable for?

Crestor is indicated for adults and children aged 6 years and over (for familial hypercholesterolaemia) who require lipid-lowering therapy.

In adult practice, it is suitable for patients with primary hypercholesterolaemia (Fredrickson Type IIa, including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia (Fredrickson Type IIb), and patients assessed as being at high cardiovascular risk who require effective LDL reduction.

Crestor is not suitable for patients with active liver disease, unexplained persistent transaminase elevations, severe renal impairment, myopathy, or those receiving ciclosporin. Pregnant and breastfeeding women must not take Crestor.

Dosage and administration

Take one Crestor tablet once daily, swallowed whole with water, at any time of day, with or without food.

The recommended starting dose for most adults is 5 to 10 mg.

Your prescriber will choose the starting dose based on your baseline LDL level, cardiovascular risk, and the degree of LDL reduction needed to reach your target.

The dose may be increased at intervals of 4 weeks if the target is not achieved.

The 40 mg dose should only be considered for patients with severe hypercholesterolaemia at high cardiovascular risk who have not reached their target at 20 mg.

It requires specialist supervision and is contraindicated in patients with factors predisposing to myopathy, including those of Asian origin, moderate renal impairment, hypothyroidism, or concurrent fibrate use.

Side effects of Crestor

Common side effects

The most commonly reported side effects are headache, dizziness, constipation, nausea, abdominal pain, and myalgia (muscle aches without significant creatine kinase elevation).

These effects are generally mild and do not require treatment discontinuation.

Myalgia occurs in approximately 2 to 5% of patients; in most cases, symptoms resolve with continued treatment or dose reduction.

Uncommon and rare side effects

Uncommon effects include raised liver enzymes, raised creatine kinase, rash, pruritus, and proteinuria (particularly at higher doses). Proteinuria at the 40 mg dose is usually tubular in origin and transient.

Rare and very rare effects include myopathy (unexplained muscle weakness with CK exceeding 10 times the upper limit of normal), rhabdomyolysis (severe muscle breakdown with risk of acute kidney injury), hepatitis, jaundice, pancreatitis, peripheral neuropathy, memory disturbance, gynaecomastia, and immune-mediated necrotising myopathy.

New-onset type 2 diabetes has been reported as a class effect of statins, particularly in patients with pre-existing metabolic risk factors.

When to seek urgent medical advice

Stop taking Crestor and seek emergency care (call 999 or attend A&E) if you develop severe unexplained muscle pain, tenderness, or weakness, particularly with fever, malaise, or dark brown urine.

Contact your GP or NHS 111 for persistent muscle aches, jaundice, unexplained fatigue, or any new symptoms that concern you.

Report suspected adverse reactions via the MHRA Yellow Card scheme at yellowcard.mhra.gov.uk .

Warnings and precautions

Muscle effects

All statins carry a risk of myopathy and, rarely, rhabdomyolysis.

The risk is dose-dependent and increased by drug interactions, renal impairment, hypothyroidism, advanced age, female sex, small body frame, and genetic factors.

Patients should be counselled to report unexplained muscle symptoms promptly. If myopathy is confirmed (CK exceeding 10 times normal with symptoms), Crestor must be stopped.

If CK is markedly elevated but the patient is asymptomatic, clinical judgement is required regarding continuation.

Liver effects

Liver function tests should be checked before starting Crestor. If transaminases exceed 3 times the upper limit of normal, treatment should not be initiated. Recurrence of significant transaminase elevation during treatment warrants dose reduction or discontinuation.

Renal effects

Proteinuria has been observed at higher doses, particularly 40 mg. In most cases this is transient and does not indicate renal damage. Renal function should be monitored in patients with pre-existing kidney disease.

Diabetes risk

Patients with risk factors for diabetes (fasting glucose 5.6 to 6.9 mmol/L, BMI above 30, elevated triglycerides, hypertension) should be monitored for glycaemic changes during statin therapy. The cardiovascular benefit of treatment generally outweighs the modest diabetes risk.

Drug interactions

Ciclosporin is contraindicated with rosuvastatin. Concurrent use with gemfibrozil, other fibrates, fusidic acid, certain HIV protease inhibitors, and regorafenib increases myopathy risk and requires dose restriction or avoidance.

Warfarin INR should be monitored when initiating or adjusting rosuvastatin. Antacids containing aluminium and magnesium hydroxide reduce rosuvastatin absorption; take antacids at least 2 hours after Crestor.

Lifestyle measures alongside statin therapy

Crestor is most effective as part of a comprehensive cardiovascular risk reduction strategy.

Dietary changes, including reducing saturated fat intake, increasing soluble fibre, and incorporating plant stanols and sterols, complement pharmacological cholesterol lowering.

Regular physical activity (at least 150 minutes of moderate-intensity exercise per week), smoking cessation, maintaining a healthy weight, and limiting alcohol intake all contribute to improved cardiovascular outcomes.

These measures do not replace statin therapy in patients at elevated risk but work synergistically with it.

How to get a Crestor prescription in the UK

Crestor and generic rosuvastatin are prescription-only medicines available through the NHS.

Your GP can prescribe rosuvastatin following a cardiovascular risk assessment (using the QRISK3 tool for primary prevention) and baseline blood tests including a fasting lipid profile, liver function, renal function, HbA1c, and thyroid function.

Specialist lipid clinic referral may be appropriate for familial hypercholesterolaemia or statin intolerance.

Authorised online prescribers registered with the GPhC may also issue prescriptions following a structured clinical assessment. The standard NHS prescription charge in England is currently 9.90 pounds per item; prescriptions are free in Scotland, Wales, and Northern Ireland.

When to seek medical advice

Contact your GP or NHS 111 if you experience persistent muscle aches, unexplained fatigue, yellowing of the skin or eyes, or any new symptoms while taking Crestor.

Seek emergency care (call 999 or attend A&E) if you develop severe muscle pain with dark urine, chest pain, or symptoms of stroke.

Report any adverse reactions via the MHRA Yellow Card scheme at yellowcard.mhra.gov.uk .

Sources

• Crestor Film-Coated Tablets, Summary of Product Characteristics (EMC)
• Rosuvastatin, British National Formulary (BNF)
• NICE CG181: Cardiovascular disease: risk assessment and reduction
• High cholesterol, NHS
• MHRA Yellow Card Scheme