Rosuvastatin

Boxed warning

Rosuvastatin has boxed warnings. Rosuvastatin use is associated with the development of neuromuscular disorders characterized by muscle weakness. The risk is especially high in people 65 or older and those with poorly-controlled hypothyroidism or kidney impairment.¹

Rosuvastatin may cause liver enzyme abnormalities, and any person taking the drug should be routinely monitored to prevent complications.¹

What is rosuvastatin?

Rosuvastatin is a medicine prescribed by doctors, alongside a healthy diet and exercise, to help patients achieve lower blood levels of low-density lipoprotein or LDL, otherwise known as bad cholesterol. It also increases high-density lipoprotein or HDL, known as good cholesterol, and lowers triglycerides, a type of fat in the blood. It’s used to treat various conditions marked by lipid imbalances and may be prescribed to slow the progression of atherosclerosis or prevent certain types of heart disease.

Rosuvastatin is the generic name of the well-known brands Crestor and Ezallor Sprinkle. 

Rosuvastatin belongs to a drug class known as statins. Statins work by blocking a specific enzyme in the liver that plays an essential role in the cholesterol production pathway; this, in turn, hinders cholesterol synthesis.²

The drug’s effectiveness in lowering LDL and triglycerides while increasing HDL reduces the likelihood of developing atherosclerosis, which is the narrowing and stiffening of the arteries resulting from the buildup of fats and cholesterol. This can help reduce the risk of cardiovascular disease, heart attack, and stroke.

What is rosuvastatin used to treat?

Rosuvastatin is used to treat a number of conditions characterized by abnormally high or poorly-balanced blood lipid concentrations, including:¹

• Hyperlipidemia, where it aims to reduce high blood lipids

• Mixed dyslipidemia, to achieve balanced lipid concentrations

• Heterozygous familial hypercholesterolemia in children aged 8–17, where its goal is to reduce high cholesterol

• Hypertriglyceridemia, with the intent to lower blood triglycerides

• Primary dysbetalipoproteinemia, where it works to achieve target levels of triglycerides and cholesterol

• Homozygous familial hypercholesterolemia in adults and children aged 7–17, where it helps in the elimination of excess LDL

• Atherosclerosis, with the goal of slowing the condition’s progression

• Cardiovascular (heart) disease, with the goal of preventing heart disease and cardiovascular events in high-risk individuals

Dosage forms and strengths

Rosuvastatin is available in two forms:

Tablet³

Generic rosuvastatin and Crestor are available in tablet form in strengths of 5mg, 10mg, 20mg, and 40mg. 

Capsule⁴

Ezallor Sprinkle is available in capsules, with doses of 5mg, 10mg, 20mg, and 40mg.

How do you take rosuvastatin?

How you take rosuvastatin (and how much you take) will depend on individual factors, including your age and ethnicity, your condition, and the form you’re prescribed.

If you take the drug in tablet form, you’ll need to swallow it whole without crushing or chewing it. People who are able to swallow capsules will take the capsule form the same way; however, if a person is unable to swallow capsules or tablets, they can break open the rosuvastatin capsule and carefully mix its contents into a spoonful of water or applesauce and consume the mixture (completely) immediately after mixing.

As with any medication, you should take rosuvastatin precisely as your doctor recommends. You may take the medication with or without food, but taking it with food may alleviate stomach upset.

Dosage for adults¹

• The dosage in adults may range from 5mg to 40mg, taken orally once daily. Typically, the starting dosage is 10mg or 20mg taken orally, once daily, except in the case of Asian patients, where the initial dose is lower, 5mg daily, due to increased rosuvastatin plasma concentrations.

• The doctor may adjust your dosage based on your age, medical history, ethnicity, and predisposition to side effects.

• The maximum dosage should not exceed 40mg taken orally each day. This dose is reserved for those who cannot meet their target cholesterol levels with 20mg. 

• For those who have difficulty swallowing tablets, capsules are available. 

• The brand Ezallor is indicated exclusively for adults.⁵

What You Need To Know About Cholesterol

Dosage for children with heterozygous hypercholesterolemia¹

For this condition, rosuvastatin is only suitable for children eight years and older.

• Dosage varies by age group:

  • 8 to 10 years old: 5–10mg taken orally once daily

  • 10 to 17 years old: 5–20mg taken orally once daily, with adjustments by the prescribing doctor every four weeks, if necessary, up to a maximum daily dose of 20mg

Dosage for children with homozygous hypercholesterolemia¹

For this condition, rosuvastatin should not be given to children younger than seven years.

Children aged 7 to 17 years with homozygous hypercholesterolemia will take 20mg orally once daily.

Seeing results

Rosuvastatin will start taking effect within one to two weeks. It will take at least a month to achieve the full impact or your target cholesterol level. Cholesterol levels should drop within four weeks of starting treatment.

Who should not take rosuvastatin?

Rosuvastatin is generally safe when taken as directed. However, some people should not take rosuvastatin, including:¹

• Children who have not reached the age for which the drug has been deemed safe

• People with known sensitivities to the medication

• Individuals with liver disease or elevated liver enzymes

• Women who are pregnant, trying to become pregnant, or breastfeeding

Potential side effects of rosuvastatin

In most cases, the side effects of rosuvastatin are mild and improve over time, but rarely, a person taking the drug may experience severe and persistent side effects.²

Among the more common side effects of rosuvastatin are:

• Muscle and joint pains

• Sore throat

• Headache

• Dizziness

• Nausea 

• Abdominal pain

• Increase in creatine phosphokinase

• Urinary tract infections

• Allergic reactions 

• Flu-like symptoms

• Weakness, tiredness, or fatigue

• Constipation

The more severe side effects of rosuvastatin include: 

• Pancreatitis

• New onset of diabetes or worsening of pre-existing diabetes

• Memory problems and confusion

• Foamy urine

• Muscle problems that might lead to rhabdomyolysis and autoimmune myopathy

• Liver problems

• Chest pain

• Fever

• Severe allergic reactions (rash, hives, swelling of the face, tongue, or throat)

Among the most serious side effects are those relating to skeletal muscle and liver enzymes.¹

Rosuvastatin may cause skeletal muscle disorders, including myopathy and rhabdomyolysis. Myopathy is a neuromuscular disorder characterized by the weakening of the muscles due to muscle fiber dysfunctions. It’s a disabling condition and could lead to early death. Rhabdomyolysis is a life-threatening condition characterized by muscle breakdown and muscular cell death, leading to the release of muscle cell contents (proteins and electrolytes) into the blood, which may result in organ failure and death.

People taking rosuvastatin are also at an increased risk for developing liver enzyme abnormalities. While levels typically return to normal when the medication is stopped, it’s essential to monitor enzyme levels to prevent complications.

Some groups of people are more likely to experience severe side effects, including people 65 and older, those who consume alcohol daily, people with liver, kidney, or thyroid diseases, and those taking other anti-cholesterol medications or any medications that interact with rosuvastatin. 

Overdose

If you think you might have overdosed on rosuvastatin, seek immediate medical attention. You can call the poison control helpline or 911 in a medical emergency. 

Possible signs of an overdose include:

• Nausea

• Vomiting

• Muscle pain

• Weakness

• Jaundice (yellowing of the skin or eyes)

• Dark urine

• Difficulty breathing

Missed doses

If you miss a dose of rosuvastatin, take one as soon as you remember unless you were supposed to take it 12 or more hours ago. If you’re 12 or more hours overdue, skip the dose and resume your usual dosing schedule.

Allergy information

Some people may be mildly or severely allergic to rosuvastatin. Hypersensitivity reactions, such as itching, rashes, and hives, are among the possible side effects of the drug. 

In severe cases, a person may experience swelling in the face, lips, tongue, and throat, accompanied by difficulty breathing or swallowing. 

If you suspect you may be having an allergic reaction, call 911 immediately. 

Long-term use of rosuvastatin

Having high cholesterol levels or other cardiovascular risk factors could be a long-term health issue, in which case you’ll need to take rosuvastatin on a long-term basis or as a maintenance drug. Taking it as prescribed and following your doctor’s instructions will help keep your cholesterol levels in check.

In the majority of cases, rosuvastatin is safe and effective when used long-term.⁶

Pregnancy category

Rosuvastatin falls into pregnancy category X, according to the US FDA. Blood cholesterol and triglycerides increase during pregnancy to support fetal development. Using drugs like rosuvastatin to lower these levels may negatively affect development.¹

Rosuvastatin in pregnancy and breastfeeding

Rosuvastatin is contraindicated in pregnancy as it may harm your baby. Human trials did not establish safety in pregnant women, and there is no apparent benefit to rosuvastatin therapy during pregnancy. Potential risks to the fetus could include congenital abnormalities, low birth weight, or miscarriage. Do not take rosuvastatin if you are pregnant or planning to become pregnant.

Those breastfeeding must not take rosuvastatin because the drug may pass from mother to baby through breast milk, potentially harming the nursing infant.

Interactions with other drugs

There are known interactions between rosuvastatin and other drugs. Speak with your doctor before taking rosuvastatin if you’re taking any of the following:¹

• Cyclosporine (an immunosuppressant medication), which may increase the risk of myopathy when taken with statins (including rosuvastatin)

• Fibrates (drugs used to treat high cholesterol and triglycerides), which may increase the risk of muscle problems when taken alongside rosuvastatin

• Some antivirals (including those used to treat hepatitis and HIV), which might interact with rosuvastatin, increasing the risk of muscle problems

• Other medicines (such as niacin, colchicine, and regorafenib), which might increase the risk of muscle issues

• Blood thinners (including warfarin), which may increase the risk of bleeding when taken with rosuvastatin

Can I drink alcohol while taking rosuvastatin?

Both alcohol and rosuvastatin can affect liver function. Consuming alcohol, especially in large quantities, while taking rosuvastatin may increase your risk for harmful side effects. Speak with your doctor before taking rosuvastatin if you consume alcohol regularly.

What to discuss with your doctor before starting rosuvastatin

Some personal factors may influence how your body reacts to rosuvastatin. Speak with your doctor about your condition if you:

• Have (or have a family history of) liver, kidney, or thyroid disease

• Have respiratory issues

• Struggle with unexplained muscle aches

• Are pregnant, planning to become pregnant, or breastfeeding

• Have had or plan to have surgery, including dental

• Consume alcohol regularly

• Are of Asian descent, as you may need a lower dose

• Are allergic to any medications, especially statins

Be sure to bring a list of all medications, vitamins, and supplements you’re taking. Your doctor may ask about your lifestyle to minimize the risk of rosuvastatin affecting your daily life. If you’re inquiring about treatment for a child with a disorder treatable with rosuvastatin, the doctor will ensure the dose is appropriate for the child’s age.

Stopping rosuvastatin

Some patients may need to take rosuvastatin long-term as a maintenance drug to prevent cholesterol levels from rising.

Since this drug controls cholesterol levels, suddenly stopping it may trigger a spike in cholesterol levels, increasing the risk of cardiovascular issues, including heart attack or stroke.

If you need to stop taking rosuvastatin due to disruptive side effects, consult your doctor first, as they will switch you to a different medication.

Drug approval history

Rosuvastatin received FDA approval in 2003. The generic version and Ezallor Sprinkle have been available since 2016 and 2019, respectively.⁷

In a double-blind clinical trial of participants with hyperlipidemia and mixed dyslipidemia, researchers found that rosuvastatin significantly reduced undesirably high levels of total cholesterol, LDL, and non-HDL cholesterol, within the six-week study period at all doses (5mg, 10mg, 20mg, and 40mg daily).¹

In adult and pediatric patients with heterozygous familial hypercholesterolemia, rosuvastatin effectively reduced LDL cholesterol in a 12-week period, starting with a 20mg dose and increasing the dose to 40mg after six weeks.¹

In an assessment of people with atherosclerosis, 52.1% of participants saw halted disease progression while taking rosuvastatin compared to 37.7% who weren’t taking the treatment.¹

Finally, in a large-scale study focusing on the drug’s value in preventing cardiovascular disease in 17,802 men and women, researchers found that rosuvastatin significantly decreased the risk of experiencing a major cardiovascular event, with 142 cardiovascular events reported in the rosuvastatin group compared to 252 in the non-treatment group.⁸

Tips for taking rosuvastatin

Rosuvastatin is generally well-tolerated, but there are steps you can take to reduce your risk of side effects. Here are some tips for taking rosuvastatin: 

• Take rosuvastatin with a full glass of water

• Never chew the tablet or capsule

• If you have difficulty swallowing, you can sprinkle the capsule contents onto a teaspoon of soft food and mix it in

• If you take an antacid containing magnesium, you must take it at least two hours after taking rosuvastatin

• Healthy diet and lifestyle choices will improve rosuvastatin’s effectiveness

• Limiting alcohol intake will reduce the risk of possible liver damage

• Always follow your doctor’s instructions, and if there’s something you’re unsure about, don’t hesitate to ask for clarification

Frequently asked questions

What time of day is best to take rosuvastatin?

You can take rosuvastatin anytime, but it’s best to take it around the same time every day. If you take antacids containing magnesium, plan your dosage schedule, so you take them no sooner than two hours after you’ve taken rosuvastatin.

Does rosuvastatin cause weight gain?

Weight gain is not a known side effect of rosuvastatin. Likewise, there’s no evidence the drug causes weight loss.

Can rosuvastatin affect sleep?

There is some evidence that taking statins may impact sleep quality, with sleep disorders being reported post-marketing as one of the adverse effects of taking rosuvastatin. However, more studies are needed to confirm the association.