Rosuvastatin (Dosage)

Rosuvastatin is a drug of the statin family used to lower blood cholesterol levels and prevent cardiovascular disease. Muscle myopathy is one of the main adverse effects of statin treatment, and genomic variants have been described that increase the predisposition to suffer it.

Statins are drugs that act as inhibitors of the enzyme hydroxymethylglutaryl-CoA (HMG-CoA) reductase, which plays a key role in cholesterol synthesis. These drugs have a wide range of beneficial effects, including anti-inflammatory, antioxidant, antiproliferative and immunomodulatory properties. They also help to maintain the stability of arterial plaques and prevent platelet aggregation.

Rosuvastatin has been approved by the FDA to treat homozygous familial hypercholesterolemia, hyperlipidemia, mixed dyslipidemia, primary dysbetalipoproteinemia, hypertriglyceridemia and prevention of cardiovascular disease.

Rosuvastatin is of synthetic origin, patented in 1991. In 2021, it was among the 30 most prescribed drugs. Its safety profile allows its use both in adults and in children over 8 years of age with hypercholesterolemia of genetic origin.

MECHANISM OF ACTION

Statins are inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, a key enzyme in cholesterol biosynthesis. As a consequence, SREBP(sterol regulatory elements-binding proteins) regulatory proteins are activated, which increase the number of LDL cell receptors, decreasing circulating cholesterol levels.

CONTRAINDICATIONS

Rosuvastatin is contraindicated in patients with a history of hypersensitivity to this drug or to any of its excipients. In addition, it should not be prescribed in people with hepatic problems, with renal insufficiency, concomitant to treatment with cyclosporines or during pregnancy.

In addition, it should be used with caution in elderly patients (>70 years), people with family or personal history of muscular disorders, hypothyroidism, alcoholism or renal insufficiency.

It is important to bear in mind that the simultaneous use of rosuvastatin with other drugs can alter the bioavailability of this statin, increasing the risk of undesirable adverse effects. Among the drugs that have shown interaction are cyclosporine, protease inhibitors (ritornavir/atazanavir), regorafenib, some antibiotics such as erythromycin or antacids, among others. Therefore, it is important to inform the physician of any prescription or non-prescription treatment taken simultaneously with rosuvastatin.

SIDE EFFECTS

The use of rosuvastatin shares adverse effects with other drugs of the same family. It may cause headaches, constipation, diarrhea, dyspepsia, nausea or asthenia. Other infrequent and rare adverse effects are urticaria, increased transaminases, jaundice or edema. Myopathy is another of the most common adverse effects, consisting of muscle pain, weakness and increased muscle enzymes. The identification of this statin-induced myopathy is not easy and resolves after withdrawal of the drug.

BRAND NAMES

Drugs containing lovastatin as an active ingredient include:

  • Crestor®
  • Ezallor®
  • Roszet®
  • Rosumed®
  • Rosvel®

Genes analyzed

ABCG2 SLCO1B1

Bibliography

Tuteja S, Rader DJ. SLCO1B1 and Statin Therapy. Circ Genom Precis Med. 2018 Sep;11(9):e002320.

Cooper-DeHoff RM. The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 genotypes and Statin-Associated Musculoskeletal Symptoms. Clin Pharmacol Ther. 2022 May;111(5):1007-1021.

Bajaj T, Giwa AO. Rosuvastatin. 2023 May 23. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan–. PMID: 30969705.

Luvai A, Mbagaya W, Hall AS, et al. Rosuvastatin: a review of the pharmacology and clinical effectiveness in cardiovascular disease. Clin Med Insights Cardiol. 2012;6:17-33.

Zhang D, Ding Y, Wang X, et al. Effects of ABCG2 and SLCO1B1 gene variants on inflammation markers in patients with hypercholesterolemia and diabetes mellitus treated with rosuvastatin. Eur J Clin Pharmacol. 2020 Jul;76(7):939-946.

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