Atorvastatin (Dosage)

Atorvastatin 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 therapy, and genomic variants have been described that increase the predisposition to suffer it. Adjusting the dosage of atorvastatin according to the genetic variants of the SLCO1B1 gene can optimize treatment and reduce the risk of musculoskeletal symptoms.

Statins are drugs that act as inhibitors of the enzyme hydroxymethylglutaryl-CoA (HMG-CoA) reductase involved in cholesterol synthesis. Statins have a variety of beneficial effects including anti-inflammatory, antioxidant, antiproliferative and immunomodulatory properties. In addition, they participate in maintaining the stability of arterial plaques and prevent platelet aggregation.

Atorvastatin, unlike other statins, is of synthetic origin and was first described in 1985. It has proven to be more effective than other statins such as simvastatin in reducing lipid parameters in the short term.

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

Atorvastatin 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 liver problems, pregnancy or together with potent CYP3A4 inhibitors (itraconazole, ketoconazole, erythromycin, ritornavir, carbamazepine, rifampicin, miconazole, diclofenac, among many others).

In addition, it should be used with caution in elderly patients (>70 years), people with family or personal history of hereditary muscle disorders, history of statin-induced muscle toxicity or alcoholism.

SIDE EFFECTS

The use of atorvastatin can cause frequent side effects such as constipation, flatulence, dyspepsia, headache, skin rash, insomnia, asthenia or fatigue, among others. Myopathy is another of the most common adverse effects, consisting of muscle pain, weakness and increased muscle enzymes. It is important to monitor those severe cases that develop rhabdomyolysis, since this condition involves the breakdown of muscle tissue. Identification of this statin-induced myopathy is not easy and resolves after withdrawal of the drug.

BRAND NAMES

Drugs containing atorvastatin include:

  • Atorvaliq®
  • Caduet®
  • Lipitor®
  • Lypqozet®
  • Cardyl®
  • Colator®
  • Prevencor®
  • Thervan®
  • Zarator®

Genes analyzed

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.

McIver LA, Siddique MS. Atorvastatin. 2024 May 8. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan–. PMID: 28613530.

Mykkänen AJH, Tarkiainen EK, Taskinen S, et al. Genome-Wide Association Study of Atorvastatin Pharmacokinetics: Associations With SLCO1B1, UGT1A3, and LPP. Clin Pharmacol Ther. 2024 Jun;115(6):1428-1440.

Romaine SP, Bailey KM, Hall AS, Balmforth AJ. The influence of SLCO1B1 (OATP1B1) gene polymorphisms on response to statin therapy. Pharmacogenomics J. 2010 Feb;10(1):1-11.

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