Rosuvastatin

1. Introduction

Rosuvastatin is a lipid-lowering medication in the statin class. It is used to reduce elevated cholesterol and triglycerides and to prevent cardiovascular events such as heart attack and stroke. Rosuvastatin inhibits the enzyme HMG-CoA reductase, which plays a key role in cholesterol synthesis, effectively reducing low-density lipoprotein (LDL) cholesterol and raising high-density lipoprotein (HDL) cholesterol.

2. Indications

  • Hyperlipidaemia and Mixed Dyslipidaemia: To reduce elevated LDL cholesterol, total cholesterol, and triglycerides while increasing HDL cholesterol.
  • Familial Hypercholesterolaemia: Treatment of heterozygous or homozygous familial hypercholesterolaemia.
  • Prevention of Cardiovascular Disease: Primary prevention in patients at high risk of cardiovascular events.
  • Hypertriglyceridaemia: To reduce elevated triglycerides.
  • Atherosclerosis: To slow the progression of atherosclerosis.

3. Dosage

Adults:

  • Hyperlipidaemia and Cardiovascular Prevention: Start with 10 mg or 20 mg once daily.
    • Adjust based on response after 4 weeks.
    • Maximum dose: 40 mg once daily (reserved for patients with severe hypercholesterolaemia who are not achieving goals on lower doses).

Elderly (>70 years):

  • Start with 5 mg once daily. Titrate based on response.

Children (10–17 years):

  • Heterozygous Familial Hypercholesterolaemia: 5–20 mg once daily.
  • Homozygous Familial Hypercholesterolaemia: 20 mg once daily.

Patients with Renal Impairment:

  • Start with 5 mg once daily in moderate renal impairment (eGFR <60 mL/min).
  • Avoid 40 mg dose in severe renal impairment (eGFR <30 mL/min).

4. Administration

  • Take orally, once daily, at the same time each day.
  • Can be taken with or without food.
  • Avoid consuming large amounts of alcohol or grapefruit juice while on rosuvastatin.

5. Forms Available

  • Tablets: 5 mg, 10 mg, 20 mg, 40 mg

6. Side Effects

6.1 Common Side Effects:

  • Headache
  • Muscle pain (myalgia)
  • Abdominal pain
  • Nausea
  • Weakness

6.2 Less Common Side Effects:

  • Constipation
  • Dizziness
  • Joint pain (arthralgia)

6.3 Rare but Serious Side Effects:

  • Rhabdomyolysis (severe muscle breakdown)
  • Hepatotoxicity (liver enzyme elevations)
  • Proteinuria (protein in urine)
  • Severe allergic reactions (e.g., angioedema)

7. Warnings

  • Rhabdomyolysis: Monitor for muscle pain, tenderness, or weakness, particularly if accompanied by fever or dark-coloured urine.
  • Liver Dysfunction: Discontinue if significant liver enzyme elevations occur.
  • Diabetes Risk: May slightly increase blood glucose levels; monitor in patients at risk of diabetes.
  • Renal Impairment: Use cautiously in patients with impaired renal function, as rosuvastatin can cause proteinuria.

8. Precautions

  • Use cautiously in patients with a history of liver disease or heavy alcohol consumption.
  • Avoid use in pregnant or breastfeeding women due to potential harm to the foetus or infant.
  • Monitor for symptoms of memory loss or confusion, although rare.

9. Interactions

  • Cyclosporine: Increases rosuvastatin levels; avoid doses higher than 5 mg.
  • Gemfibrozil: Increases the risk of rhabdomyolysis; avoid concurrent use if possible.
  • Warfarin: Increases INR; monitor closely.
  • Antacids: May reduce rosuvastatin absorption; take antacids at least 2 hours after rosuvastatin.
  • HIV/Hepatitis C Protease Inhibitors: Can increase rosuvastatin levels; dose adjustments may be required.

10. Monitoring Parameters

  • Lipid profile (total cholesterol, LDL, HDL, triglycerides) at baseline and periodically.
  • Liver function tests (ALT, AST) at baseline and during therapy.
  • Creatine kinase (CK) levels if muscle symptoms occur.
  • Blood glucose and HbA1c in patients at risk of diabetes.

11. Use in Children

  • Approved for use in children aged 10 years and older with familial hypercholesterolaemia.
  • Start with lower doses and adjust based on response.

12. Use in Pregnancy

  • Category X: Contraindicated in pregnancy. Discontinue immediately if pregnancy occurs.
  • Cholesterol and triglycerides are necessary for foetal development, so statins should not be used during pregnancy.

13. Use in Elderly

  • Safe for use in elderly patients, but start with the lowest effective dose (e.g., 5 mg). Monitor for muscle and liver-related side effects.

14. Use in Kidney Disease

  • Dose adjustment is required in patients with moderate to severe renal impairment. Avoid the 40 mg dose in severe renal impairment.

15. Use in Liver Disease

  • Contraindicated in patients with active liver disease or unexplained persistent elevations in liver enzymes.

16. Patient Counselling Points

  • Take rosuvastatin at the same time daily, with or without food.
  • Inform your doctor if you experience unexplained muscle pain, weakness, or dark-coloured urine.
  • Avoid alcohol and grapefruit juice while taking rosuvastatin.
  • Women of childbearing potential should use effective contraception while on rosuvastatin.
  • Do not stop taking rosuvastatin without consulting your doctor, even if you feel well.

17. Table of Brand Names, Manufacturer, and Prices in USD

Brand NameManufacturerStrength/Dosage FormPrice (USD)
CrestorAstraZeneca20 mg Tablet$150 (30 tablets)
RosuvasCipla10 mg Tablet$30 (30 tablets)
Generic RosuvastatinVarious10 mg Tablet$20 (30 tablets)

18. 15 FAQs (Frequently Asked Questions)

1. What is Rosuvastatin used for?
Rosuvastatin is used to lower cholesterol and triglycerides and to reduce the risk of heart attacks, strokes, and other cardiovascular events.

2. How does Rosuvastatin work?
It inhibits the HMG-CoA reductase enzyme, reducing cholesterol synthesis in the liver.

3. Can Rosuvastatin cause muscle pain?
Yes, muscle pain or weakness is a possible side effect. Contact your doctor if it occurs.

4. Is Rosuvastatin safe during pregnancy?
No, it is contraindicated during pregnancy due to potential harm to the foetus.

5. Can Rosuvastatin be taken at night?
Yes, but it can be taken at any time of day, unlike some other statins.

6. Does Rosuvastatin require regular monitoring?
Yes, regular lipid profile and liver enzyme tests are recommended during therapy.

7. Can Rosuvastatin cause liver damage?
Rarely, it can cause liver enzyme elevations. Discontinue if significant liver injury occurs.

8. Can Rosuvastatin interact with other medications?
Yes, it interacts with cyclosporine, gemfibrozil, and warfarin, among others.

9. Does Rosuvastatin cause weight gain?
Weight gain is not a typical side effect of rosuvastatin.

10. Can alcohol be consumed while taking Rosuvastatin?
Alcohol should be limited as it increases the risk of liver damage.

11. How long does it take for Rosuvastatin to work?
Cholesterol levels may start improving within 2–4 weeks of therapy.

12. Can Rosuvastatin cause diabetes?
It may slightly increase the risk of developing diabetes, particularly in patients already at risk.

13. Can I stop Rosuvastatin if my cholesterol is normal?
No, continue taking rosuvastatin as directed to maintain cholesterol control.

14. Can Rosuvastatin be taken with other cholesterol-lowering drugs?
Yes, but consult your doctor to avoid drug interactions.

15. How should Rosuvastatin be stored?
Store at room temperature, away from moisture and heat.