Crestor

Crestor - Use | Dose | Side Effects

Crestor, also known as "super statin" is a drug from the group of the HMG CoA reductase inhibitors (also known as statins). Crestor is a selective competitive inhibitor of this enzyme and its primary site of action is the liver (most important organ for the metabolism of cholesterol). It increases the number of hepatic LDL receptors on the cell surface and directly increases the degradation of so-called "bad" (LDL) cholesterol. Researches also showed that this drug reduces the liver production of VLDL cholesterol. In this way, Crestor lowers the concentration of cholesterol in the blood.

Crestor is used to treat hypercholesterolemia and for the prevention of cardiovascular diseases.

It is called "super statin", because it demonstrates the stronger effect than other cholesterol-lowering drugs. In fact, researches have shown that lowest dose of Crestor (5 mg) reduces LDL-cholesterol by 38%, which is more than with usual recommended doses of all other statins.1 A meta-analysis showed that Crestor exerts the same effect on lowering cholesterol than four times higher dose of Atorvastatin, while on the other hand risk for side effects is the same with both drugs.2

Precautions

Contraindications to the use of this drug are the same as for other statins, and include following:

  • Myopathy and other muscle diseases. The incidence of myopathy caused by this drug in doses up to 40 mg per day is less than 0.01%, meaning this side effect occurs very rare. However, if you're experiencing unexplained muscle ache or muscle inflammation, immediately contact your doctor.
  • Renal insufficiency. There have been reports of acute interstitial nephritis induced by using this medicine3, therefore the use of Crestor in patients with kidney diseases is not recommended.
  • Hepatic insufficiency. Crestor may exhibit hepatotoxicity4, and should not be used in patients who already have impaired liver function.
  • Pregnancy and lactation. Crestor can cause malformations of the central nervous system and limbs in newborns, which is why its use during pregnancy is strictly prohibited!
  • Hypothyroidism. Crestor is contraindicated in patients who suffer from this disease, as it may lead to symptoms exacerbation.

Crestor, pregnancy and breastfeeding

FDA has classified this drug group in the group X - there is sufficient evidence of its embryotoxicity and its use during pregnancy almost inevitably leads to birth defects. Therefore, use of Crestor is contraindicated during pregnancy.

Crestor is probably excreted into breast milk, therefore breastfeeding should be avoided while taking this drug.

Dosage

The usual starting dose for the treatment of hypercholesterolemia in adult patients is 5-10 mg per day (preferably at bedtime). Maintenance dose ranges from 5mg to 40 mg per day.

Doses greater than 40 mg are not recommended because high doses increase the risk of myopathy, hepatotoxicity and nephrotoxicity.

It can be used in children aged 10-18 years to treat familial (inherited) hypercholesterolemia at a dose of 5-10 mg per day.

Use in children younger than 10 years is not recommended.

Recommended dose for the prevention of cardiovascular diseases is 20 mg once a day.

Take the tablet with little water, regardless of meals.

Interactions

Crestor should not be used in combination with the following drugs:

  • Cyclosporin (immunosuppressive drug). Cyclosporin cause 7-fold increase in Crestor levels in the blood, which significantly increases the risk of hepatotoxicity, nephrotoxicity and myopathy!
  • Atazanavir-cobicistat (drug used to treat HIV). There have been reported cases of concomitant use of Crestor with this drug and three times higher concentration of Crestor in the blood was observed, which also significantly increases the risk of adverse reactions.
  • Other drugs used in the treatment of hypercholesterolemia and hypertriglyceridemia (e.g. fenofibrate, gemfibrozil, niacin, nicotinic acid, and other statins). Concomitant use significantly increases the risk of nephrotoxicity, hepatotoxicity and rhabdomyolysis.
  • Antacids containing aluminum hydroxide, sodium hydrogencarbonate and magnesium hydroxide. These drugs reduce the concentration of Crestor in the blood by 50% which reduces its efficiency.
  • Erythromycin (antibiotic). Erythromycin increases intestinal motility, which reduces intestinal absorption of Crestor by about 30%. This leads to reduced effectiveness of the Crestor.

Side effects

Immediately stop taking Crestor and go to your doctor if the following side effects occur:

  • Pain in the muscles or inflammation of the muscles
  • Liver damage (pain in the right upper abdomen, loss of appetite and jaundice)
  • Persistent itching accompanied by facial swelling, swelling of the tongue or swelling of the throat
  • Difficulty breathing

Other adverse effects of Crestor are:

  • Headache
  • Dizziness
  • Weakness
  • Pancreatitis
  • Blood in the urine
  • Arthralgia
  • Sexual disorders
  • Depression
  • Memory loss
  • Polyneuropathy
  • Stevens-Johnson syndrome
  • Gynecomastia

References

  1. NCBI link 1
  2. NCBI link 2
  3. NCBI link 3
  4. NCBI link 4