Rosuvastatin Oral

Rosuvastatin is also known under US brand name Crestor and it works by reducing the levels of "bad" cholesterol and triglycerides in the blood, whilst increasing the levels of "good" cholesterol in the body.

Overview

Rosuvastatin is used in combination with a proper diet to help reduce the number of triglycerides (fats) in the blood and lower cholesterol. This medication can help slow down or prevent medical problems, such as atherosclerosis (hardening of the arteries), that are caused by the blood vessels becoming clogged with fats. It can also be used to prevent certain types of blood vessels and heart problems in those who present risk factors for heart problems.

This drug belongs to a group of medicines known as HMG-CoA reductase inhibitors or statins. They work by blocking the enzyme that is needed by the body to make cholesterol, which therefore reduces the amount of cholesterol in the blood. This medication is only available via prescription from your doctor and is available in the dosage form of tablet for oral consumption.

Conditions Treated

  • Modify levels of lipids (fats) in the blood
  • Treating abnormal blood cholesterol or triglyceride levels in conjunction with diet
  • For patients who have a type of inherited and severe hypercholesterolemia
  • Prevention of heart attack and stroke

Type of Medicine

  • Oral tablet

Side Effects

Along with it's intended effects, rosuvastatin can produce some unwanted side effects. Not all of these side effects may occur, but if any of them do, they may require medical attention.

Inform your doctor immediately if you suffer from any of the following side effects whilst taking rosuvastatin:

Rare:

  • Unusual weakness or tiredness
  • Dark-colored urine
  • Muscle spasms or cramps
  • Fever
  • Muscle pain, tenderness, stiffness, weakness or waisting

Incidence unknown:

  • Clay-colored stools
  • Stomach or abdominal pain
  • Skin rash
  • Vomiting of blood
  • Unpleasant breath odour
  • Yellow skin or eyes

Some side effects may occur that do not need urgent medical attention. You usually find that these side effects begin to reduce or disappear once your body adjusts to the medication. However, if you find the following side effects are bothering your day-to-day life, then contact your doctor or a local pharmacist for advice on ways to reduce or prevent the side effects. If your side effects worsen, seek medical attention. The following side effects are ranked in terms of more common and less common.

More common:

  • Congestion
  • Body pain or aches
  • Cough
  • Difficulty with moving
  • Headache
  • Sore or dry throat
  • Hoarseness
  • Runny nose
  • Pain in the joints
  • Changes in voice
  • Swollen, tender, glands in the neck
  • Difficulty swallowing

Less common:

  • Accumulation of swollen, pus, red, or tender area of infection near a tooth
  • Back, arm, or jaw pain
  • Accidental injury
  • Sour or acid stomach
  • Belching
  • Feeling full or bloated
  • Bladder pain
  • Cloudy or bloody urine
  • Burning feeling in the stomach or chest
  • Blurred vision
  • Crawling, burning, itching, numbness, prickling, tingling or "pins and needles" feelings
  • Chest discomfort or pain
  • Depression
  • Chest heaviness or tightness
  • Chills
  • Constipation
  • Diarrhea
  • Dizziness
  • Difficult or labored breathing
  • Burning, difficult or painful urination
  • Discouragement
  • Dry mouth
  • Excessive muscle tone
  • Excess gas or air in the stomach or intestines
  • Fast, irregular, racing, or pounding pulse or heartbeat
  • Feeling faint
  • Fear
  • Feeling of heat or warmth
  • Feeling of constant movement of self or surroundings
  • Feeling empty or sad
  • Redness or flushing of the skin especially on the face and neck
  • Dry, flushed skin
  • Fruit-like breath odour
  • Heartburn
  • General feeling of discomfort or illness
  • Increased hunger
  • Increased urination
  • Increased thirst
  • Irritability
  • Lack of appetite
  • Itching skin
  • Loss or lack of strength
  • Loss of appetite
  • Lightheadedness
  • Loss of consciousness
  • Muscle tension or tightness
  • Loss of pleasure or interest
  • Nausea
  • Nerve pain
  • Neck pain
  • Nervousness
  • Tenderness or pain around the eyes and cheekbones
  • Swelling or pain in the legs or arms without any injury
  • Swelling, pain or redness in the joints
  • Pale skin
  • Pounding in the ears
  • Passing gas
  • A sensation of spinning
  • Slow heartbeat
  • Shivering
  • Sneezing
  • Stomach discomfort, pain, tenderness, or upset
  • Sweating
  • Stuffy nose
  • Swelling of the hands, ankles, feet, or lower legs
  • Trouble sleeping
  • Trouble concentrating
  • Unexplained weight loss
  • Vomiting
  • Unusual bruising or bleeding

Remember you can report all side effects to the FDA on 1-800-FDA-1088

Dosage

The final dosage you will receive of rosuvastatin will depend upon a number of factors. This includes your age, weight and height, what condition you are being treated for, your past medical history, how severe your condition is and how you react to the first dosage. Below are guidelines for the typical doses that are given for various treatments. Do not stop, start or change your dose if it is different than what is given below. Doses should not be altered unless your doctor has given permission to do so.

These guidelines apply to the following strength(s): 5, 10, 20 and 40 mg.

Typical Adult Dose for Hyperlipidemia

An initial dose of 10-20mg is given once a day orally and a maintenance dose of around 5-40 mg is given once daily, taken orally.

This dose is to be used as an adjunct to diet in the following situations:

  • To slow the progression of atherosclerosis
  • To reduce elevated total cholesterol, apolipoprotein B (ApoB), low-density lipoprotein cholesterol (LDL-C), non-high density lipoprotein cholesterol) and triglycerides
  • To increase HDL-C levels in mixed dyslipidemia or primary hyperlipidemia or mixed dyslipidemia
  • To treat hypertriglyceridemia
  • To treat primary Type III Hyperlipoproteinemia (dysbetalipoproteinemia)

Typical Adult Dose for Hyperlipoproteinemia Type III

An initial dose of 10-20mg is given once a day orally. Then a maintenance dose of around 5-40mg is given once daily, taken orally.

This dose is to be used as an adjunct to diet in the following situations:

  • To slow the progression of atherosclerosis
  • To reduce elevated total cholesterol, apolipoprotein B (ApoB), low-density lipoprotein cholesterol (LDL-C), non-high density lipoprotein cholesterol) and triglycerides
  • To increase HDL-C levels in mixed dyslipidemia or primary hyperlipidemia or mixed dyslipidemia
  • To treat primary Type III Hyperlipoproteinemia (dysbetalipoproteinemia)

Typical Adult Dose for Hypertriglyceridemia

An initial dose of 10-20mg is given once a day orally. Following that is a maintenance dose of around 5-40mg once daily taken orally.

This dose is to be used as an adjunct to diet in the following situations:

  • To slow the progression of atherosclerosis
  • To reduce elevated total cholesterol, apolipoprotein B (ApoB), low-density lipoprotein cholesterol (LDL-C), non-high density lipoprotein cholesterol) and triglycerides
  • To increase HDL-C levels in mixed dyslipidemia or primary hyperlipidemia or mixed dyslipidemia
  • To treat primary Type III Hyperlipoproteinemia (dysbetalipoproteinemia)

Usual Adult Dose for Atherosclerosis

An initial dose of 10-20mg is given once a day orally. Following that is a maintenance dose of around 5-40mg once daily taken orally.

This dose is to be used as an adjunct to diet in the following situations:

  • To slow the progression of atherosclerosis
  • To reduce elevated total cholesterol, apolipoprotein B (ApoB), low-density lipoprotein cholesterol (LDL-C), non-high density lipoprotein cholesterol) and triglycerides
  • To increase HDL-C levels in mixed dyslipidemia or primary hyperlipidemia or mixed dyslipidemia
  • To treat primary Type III Hyperlipoproteinemia (dysbetalipoproteinemia)

Typical Adult Dose for Prevention of Cardiovascular Disease

An initial dose of 10-20mg is given once a day orally. Following that is a maintenance dose of around 5-40mg once daily taken orally.

  • For individuals who show an increased risk of cardiovascular disease (CVD) but who don't show evident coronary heart disease
  • To reduce the risk of myocardial infarction and stroke
  • To reduce the risk of arterial revascularization procedures

Typical Pediatric Dose for Heterozygous Familial Hypercholesterolemia

For those aged eight to less than 10 years old: 5-10mg is given once daily via oral consumption. Note that efficacy and safety have not been studied for doses great than 10 mg/day.

For those aged 10 to 17 years old: 5-20mg is given once daily via oral consumption. Note that efficacy and safety have not been studied in doses great than 20 mg/day.

  • Dose adjustments should be made at four-week intervals or more.
  • Doses should be based on each individual patient and their recommended goal of therapy.

Typical Pediatric Dose for Homozygous Familial Hypercholesterolemia

For ages seven to 17 years old, 20mg is given once daily via oral consumption.

Administration advice

  • This drug may be taken via oral consumption once daily at any time. It can be swallowed whole with or without food.
  • No more than two doses within 12 hours of each other should be taken.
  • If antacids are needed whilst taking this drug they should be taken at least two hours after consumption of this drug.
  • Rosuvastatin should be used in addition to a diet that is restricted in cholesterol and saturated fat when the response to nonpharmacologic interventions and diet alone has been inadequate.

General dosage advice

  • When switching from another HMG-CoA reductase inhibitor or initiating this drug, the dose, to begin with, should be used appropriately in response to the patient's response and individual goals of the therapy.
  • Upon titration or following initiation lipid levels need to be analyzed within two to four weeks and the dose should be adjusted accordingly.
  • The 40mg dose should be reserved only for those patients who have not been successful in achieving their LDL-C goal utilizing the 20mg dose.
  • This drug has not been studied in those who suffer from V dyslipidemias and Fredrickson Type I.

Interactions

Different drugs used in combination can cause interactions. These interactions can produce harmful side effects, it is therefore important that you inform your doctor or healthcare professional of all the medications you are currently taking and have taken in the past. This includes all prescription and nonprescription drugs, all vitamins and herbal remedies. You should also give your doctor a history of past illnesses and any illnesses that run in the family history.

There are 36 major drugs that interact with rosuvastatin and these drugs should not be taken together.

  • Atazanavir
  • Clofibrate
  • Amprenavir
  • Atazanavir / cobicistat
  • Cobicistat / darunavir
  • Colchicine
  • Cyclosporine
  • Colchicine / probenecid
  • Darunavir
  • Elbasvir / grazoprevir
  • Dasabuvir / paritaprevir / ombitasvir / ritonavir
  • Emtricitabine / ritonavir / lopinavir / tenofovir
  • Fenofibrate
  • Emtricitabine / tenofovir / nelfinavir
  • Fenofibric acid
  • Gemfibrozil
  • Fosamprenavir
  • Glecaprevir / pibrentasvir
  • Indinavir
  • Lenalidomide
  • Leflunomide
  • Lomitapide
  • Lovastatin / niacin
  • Lopinavir / ritonavir
  • Mipomersen
  • Nelfinavir
  • Ombitasvir / ritonavir / paritaprevir
  • Ritonavir
  • Niacin
  • Niacin / simvastatin
  • Simeprevir
  • Saquinavir
  • Sofosbuvir / velpatasvir
  • Tipranavir
  • Sofosbuvir / voxilaprevir / velpatasvir
  • Teriflunomide

There are over 190 drugs that have a moderate interaction with rosuvastatin. If you are taking one of the following drugs whilst taking rosuvastatin, your doctor may alter your medication or keep a close eye on things. Some of these are listed below, however, this list is not complete, so it's important to give your doctor a full list of the medications you are currently taking.

  • Auranofin
  • Bedaquiline
  • Aurothioglucose
  • Benznidazole
  • Bortezomib
  • Black cohosh
  • Brentuximab
  • Ceritinib
  • Certolizumab
  • Cerivastatin
  • Chloramphenicol
  • Cisplatin
  • Chloroquine
  • Carboplatin
  • Dabrafenib
  • Carfilzomib
  • Daclatasvir
  • Daptomycin
  • Dapsone
  • Dicumarol
  • Dihydroxyaluminum sodium carbonate
  • Didanosine
  • Disulfiram
  • Etanercept
  • Docetaxel
  • Ethambutol
  • Etravirine
  • Ethionamide
  • Etoposide
  • Ezetimibe
  • Elotuzumab
  • Eluxadoline
  • Eltrombopag
  • Epirubicin
  • Eslicarbazepine
  • Eribulin
  • Fludarabine
  • Ixabepilone
  • Fluvastatin
  • Ixazomib
  • Lovastatin
  • Linezolid
  • Magnesium oxide
  • Metronidazole
  • Methotrexate
  • Nelarabine
  • Osimertinib
  • Nitrofurantoin
  • Oxaliplatin
  • Red yeast rice
  • Pomalidomide
  • Ponatinib
  • Regorafenib
  • Rolapitant
  • Ribociclib
  • Ruxolitinib
  • Stavudine
  • Sodium citrate
  • Telbivudine
  • Teniposide
  • Temsirolimus
  • Thalidomide
  • Vinblastine
  • Vemurafenib
  • Vincristine
  • Vinorelbine
  • Vincristine liposome
  • Tinidazole
  • Thioguanine
  • Tocilizumab
  • Warfarin
  • Trabectedin
  • Zidovudine
  • Zafirlukast
  • Zalcitabine

Other medical conditions

The presence of other illnesses or medical issues can affect the effectiveness of rosuvastatin. Ensure that you inform your doctor or a healthcare professional if you suffer from any other medical conditions, especially:

  • Liver disease, or a history of liver disease. Use of rosuvastatin needs to be used with caution as it can cause side effects that may worsen.
  • A history of alcohol abuse or current alcohol abuse
  • If a patient is of Asian descent, they may require a lower dose of rosuvastatin.
  • Convulsions (seizures)
  • Dehydration
  • Electrolyte deficiency or disorder
  • Hypotension (low blood pressure)
  • Severe endocrine disorder
  • Hypothyroidism (underactive thyroid)
  • Major trauma or surgery or trauma, recent or otherwise
  • Metabolic enzyme deficiency or disorder
  • Sepsis (severe infection) - Patients who suffer from this condition may be at risk for kidney or muscle problems.
  • Severe kidney disease
  • Those who suffer from diabetes should use with caution
  • Should not be used in patients with these liver enzymes

Warnings

Allergies

Before taking rosuvastatin, inform your pharmacist or doctor if you are allergic to it or any other similar drugs such as statins. You should inform them of all allergies including to, animals, dyes, preservatives, foods etc

Use in pregnancy and breastfeeding

  • Studies in women breastfeeding have shown harmful infant effects. Therefore you should stop breastfeeding whilst using this medicine or an alternative medication should be prescribed.
  • Rosuvastatin is not safe to take if you are pregnant, or planning on becoming pregnant. Use adequate contraception to limit your risk of falling pregnant whilst taking this drug.
  • It is therefore sensible to limit the use of medication during pregnancy and use an alternative medication when possible. In unique cases, your doctor may decide that the benefits outweigh the risks and after a careful assessment of your health situation.

If you have any concerns or doubts, you should contact your pharmacist, doctor or a local healthcare professional.

Use in pediatric patients

Studies that have been performed to date have not indicated any pediatric-specific problems that could limit the usefulness of this medication in children. However, efficacy and safety have not been established in children under the age of seven years old.

Use in geriatric patients

Studies that have been performed to date have not indicated any geriatric-specific problems that could limit the benefits of rosuvastatin in the older population. However, elderly patients are more likely to suffer from age-related muscle problems, which could require a degree of caution in those receiving this drug.

Storage

This medication should be stored at 68° to 77°F (20° to 25°C) and it should be protected from moisture.

Summary

When used correctly, rosuvastatin is effective at lowering cholesterol. However, its use can be limited by side effects such as muscle pain. Those who are pregnant or breastfeeding should not use this drug and seek alternative medication. If you fall pregnant whilst taking this drug, you must inform your doctor urgently. People of Asian descent can be more sensitive to the effects of this drug.

Peak levels of this drug are witnessed within 3-5 hours of consumption of the tablet. However, it can take up to 1-2 weeks of regular dosing before improvements can be seen in cholesterol levels. It can take up to four weeks before you can see the maximal cholesterol-lowering effects of rosuvastatin. To help limit side effects and interactions, it's important that you inform your doctor of everything you are currently taking and have taken in the past. You should also make a list of any illness you have suffered from or any medical complications that run in the family.

 

Resources
Last Reviewed:
January 29, 2018
Last Updated:
January 27, 2018