Pitavastatin (Dosage)

Pitavastatin 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.

Pitavastatin has been marketed since 2005 and has been shown to have the highest bioavailability rate of all the statins marketed to date, which allows it to be used at lower doses. In addition, it has few drug-drug interactions, minimizing the risk of adverse effects in polymedicated patients. It is approved by the FDA to treat heterozygous familial hypercholesterolemia in patients over 8 years of age and as adjunctive therapy for primary and mixed dyslipidemia. Unlike other statins, it has not been clearly established whether pitavastatin offers additional benefits in reducing cardiovascular problems.

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

Pitavastatin 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. In addition, its use is not recommended in pregnant women.

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

SIDE EFFECTS

Adverse effects of pitavastatin are generally similar to those of other statins and include headaches, constipation, diarrhea, dyspepsia or nausea. Other infrequent and rare adverse effects include 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 withdrawal of the drug.

BRAND NAMES

Drugs containing lovastatin as an active ingredient include:

  • Livalo®
  • Zypitamag®
  • Nikita®

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.

Bhatti H, Tadi P. Pitavastatin. 2023 Jul 4. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan–. PMID: 32491334.

Chung JY, Cho JY, Yu KS et al. Effect of OATP1B1 (SLCO1B1) variant alleles on the pharmacokinetics of pitavastatin in healthy volunteers. Clin Pharmacol Ther. 2005 Oct;78(4):342-50.

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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