What is the use of Pitavastatin (Nicotinic acid receptor antagonist)?

From the Guidelines

Pitavastatin should be considered as a first-line treatment option for patients with established atherosclerotic cardiovascular disease, particularly those with metabolic disturbances, diabetes, or pre-diabetes, due to its potent LDL-C lowering effects and favorable pleiotropic effects, as recommended by the international lipid expert panel (ILEP) in 2024 1.

Key Benefits of Pitavastatin

• Pitavastatin is a potent inhibitor of HMG-coenzyme A reductase, reducing LDL-C effectively by a mean of 43-47% 1.
• It has pleiotropic effects, including inhibiting phosphatidylinositol 3-kinase (PI3K), which may be beneficial in specific patient groups, such as those with metabolic disturbances or diabetes 1.
• Pitavastatin does not increase the risk of new-onset diabetes (NOD) and may even have a slight optimizing effect on fasting blood glucose (FBG) and HbA1c levels 1.
• It has been shown to reduce subsequent and total CVD events in sub-analyses 1.

Clinical Use of Pitavastatin

• The recommended dose of pitavastatin is 4 mg once daily, which has been shown to be effective in reducing LDL-C and CVD risk in clinical trials, such as the REPRIVE trial 1.
• Pitavastatin can be used in monotherapy or as part of a combination therapy with ezetimibe in patients with metabolic disturbances to increase the chance of achieving LDL-C targets and improving adherence 1.
• It is also recommended for patients with statin intolerance, HIV, or elevated Lp(a) levels, as it has been shown to be well-tolerated and effective in these patient populations 1.

Safety and Monitoring

• Common side effects of pitavastatin include muscle pain, headache, and mild digestive issues 1.
• Liver function tests should be performed before starting treatment and periodically thereafter to monitor for potential liver damage 1.
• Patients should report unexplained muscle pain, tenderness, or weakness immediately, as these could indicate rare but serious muscle damage 1.

From the Research

Overview of Pitavastatin

• Pitavastatin is a synthetic member of the statin class of lipid-lowering drugs, approved for the reduction of elevated total cholesterol and low-density lipoprotein cholesterol (LDL-C) levels in adults with primary hypercholesterolemia and mixed dyslipidemia 2, 3, 4.
• It has a unique cyclopropyl group on its base structure, which increases 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition and significantly increases the transcription and activity of LDL receptors 5.

Efficacy of Pitavastatin

• Pitavastatin has been shown to be effective in reducing LDL-C levels, with median reductions of 30-45% in clinical trials 2, 6.
• It has also been shown to increase high-density lipoprotein (HDL) cholesterol levels by 3-10% 2, 4.
• Pitavastatin is comparable to atorvastatin and simvastatin in improving lipid measures, and more potent than pravastatin 2, 3, 6.

Safety and Tolerability of Pitavastatin

• Pitavastatin is generally well tolerated, with a safety profile similar to that of other available statins 2, 3, 4.
• The most common treatment-related adverse events are musculoskeletal or gastrointestinal in nature 2, 6.
• Pitavastatin has a low propensity for drug-drug interactions due to its minimal metabolism by cytochrome P450 enzymes 2, 3.

Clinical Use of Pitavastatin

• Pitavastatin is an attractive alternative for the treatment of patients with primary hyperlipidemia or mixed dyslipidemia who have not responded adequately to diet and other non-pharmacological measures 3, 4.
• It may be particularly beneficial in treating patients with mixed dyslipidemia due to its effectiveness in reducing triglycerides and increasing HDL-cholesterol 5.