Fluvastatin (Dosage)

Fluvastatin is a drug of the statin family used to lower blood cholesterol levels and prevent cardiovascular disease. The efficacy and safety of fluvastatin may be influenced by genetic variants in the SLCO1B1 gene and in the cytochrome CYP2C9. These variants may affect the pharmacokinetics of the drug and increase the risk of developing musculoskeletal symptoms associated with its use.

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. In addition, they help to maintain the stability of arterial plaques and prevent platelet aggregation. Fluvastatin is primarily used to treat hypercholesterolemia and, when combined with proper diet and exercise, may reduce the risk of heart attack or stroke in people at risk for heart disease.

Fluvastatin was the first fully synthetic statin, patented in 1982. It is on the World Health Organization's list of essential medicines. It is a widely used drug because of its safety profile in both adults and children.

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

Flavastatin 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, pregnancy or together with cyclosporine. Furthermore, its use is not recommended in pregnant women.

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.

Unlike other statins, its metabolism involves several liver enzymes (mainly CYP2C9, but also others), which makes it less susceptible to interactions than other drugs of the same family.

SIDE EFFECTS

The use of fluvastatin shares adverse effects with other drugs of the same family. It can cause headaches, constipation, diarrhea, dyspepsia or nausea. Other infrequent and rare adverse effects are anemia, insomnia, dizziness, abdominal pain, urticaria, fatigue or edema. 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 drug withdrawal.

A rare but significant side effect is rhabdomyolysis, a potentially serious condition that tends to occur more frequently when combined with other drugs, especially fibrates.

BRAND NAMES

Drugs containing lovastatin as an active ingredient include:

  • Lescol®
  • Fluindostatin®
  • Canef®
  • Cranoc®
  • Vastin®

Genes analyzed

CYP2C9 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.

Toda T. et al. Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):327-32.

Ramsamooj H, Preuss CV. Fluvastatin. 2023 May 29. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan–. PMID: 28613474.

Scripture CD, Pieper JA. Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81.

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.

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