Lovastatin (Dosage)

Lovastatin, as an HMG-CoA reductase inhibitor, lowers cholesterol levels by blocking its synthesis in the liver. Its metabolism, mainly regulated by CYP3A4 enzymes and the transporter protein SLCO1B1, can vary between individuals in the presence of certain genetic changes. 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 crucial 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.

Lovastatin, a substance derived from the fungus Aspergillus terreus, was one of the first statins obtained. This drug significantly reduces LDL cholesterol levels and raises HDL cholesterol levels in most patients when they do not respond to dietary and lifestyle measures. It is currently being investigated for use in the treatment and prevention of some types of cancer.

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

Lovastatin 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), persons with a family or personal history of hereditary muscle disorders, history of statin-induced muscle toxicity, uncontrolled hypothyroidism or alcoholism.

SIDE EFFECTS

Lovastatin is generally well tolerated, with adverse reactions that are usually mild and transient. However, like all drugs, it can produce frequent side effects such as constipation and dyspepsia, and less common ones such as blurred vision, abdominal pain, diarrhea, flatulence or jaundice. Myopathy is another of the most common adverse effects, consisting of muscle pain, weakness and increased muscle enzymes. 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:

  • Advicor®
  • Aterkey®
  • Altoprev®
  • Artein®
  • Closterol®
  • Colesvir®
  • Mevacor®
  • Rodatin®
  • Sivlor®

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.

Duong H, Bajaj T. Lovastatin. 2023 Mar 20. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan–. PMID: 31082038.

Lu B, Sun L, Seraydarian M et al. Effect of SLCO1B1 T521C on Statin-Related Myotoxicity With Use of Lovastatin and Atorvastatin. Clin Pharmacol Ther. 2021 Sep;110(3):733-740.

Sizar O, Khare S, Patel P, et al. Statin Medications. 2024 Feb 29. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan–. PMID: 28613690.

Tornio A, Vakkilainen J, Neuvonen M et al. SLCO1B1 polymorphism markedly affects the pharmacokinetics of lovastatin acid. Pharmacogenet Genomics. 2015 Aug;25(8):382-7.

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