Characteristics of triglyceride drugs and lipid management strategies

What are the characteristics of triglyceride (TG) drugs?

Fibrates lower serum TG levels and raise HDL-C levels by activating peroxisome proliferator-activated receptor α (PPARα) and lipoprotein lipase (LPL). Meta-analyses of clinical trials suggest that fibrates can reduce the risk of cardiovascular events by approximately 10% in individuals with high TG and low HDL-C, primarily by reducing non-fatal myocardial infarction and the need for coronary revascularization, with no significant effect on cardiovascular death, fatal myocardial infarction, or stroke.

Commonly used fibrates include: fenofibrate tablets 0.1 g three times daily; micronized fenofibrate 0.2 g once daily; gemfibrozil 0.6 g twice daily; and bezafibrate 0.2 g three times daily.

Common adverse reactions of fibrates are similar to those of statins, including hepatotoxicity, muscle toxicity, and nephrotoxicity. The incidence of elevated serum creatine kinase and liver transaminase (ALT) levels was less than 1%.

Niacin, a B vitamin, can have a significant lipid-lowering effect when used in doses exceeding its vitamin function. The mechanism of niacin's lipid-lowering effect is not fully understood, but it may be related to inhibiting lipolysis in adipose tissue and reducing VLDL synthesis and secretion in the liver.

A meta-analysis of early clinical trial results found that niacin, whether used alone or in combination with other lipid-lowering drugs, improved cardiovascular outcomes, reducing cardiovascular events by 34% and coronary events by 25%. Clinical studies combining niacin with statins suggest no cardiovascular protective effect compared to statin monotherapy, and many European and American countries have phased out niacin-based drugs from the lipid-lowering drug market.

The most common adverse reaction to niacin is facial flushing. Other adverse reactions include liver damage, hyperuricemia, hyperglycemia, acanthosis pilaris, and gastrointestinal discomfort. It is contraindicated in patients with chronic active liver disease, active peptic ulcers, and severe gout.

Niacin is available in two dosage forms: immediate-release and sustained-release. Immediate-release niacin has significant adverse reactions and is generally difficult to tolerate; it is no longer commonly used. Sustained-release niacin tablets have significantly fewer adverse reactions and are more easily tolerated.

High-purity fish oil preparations: The main component of fish oil is n-3 fatty acids, also known as ω-3 fatty acids. Early clinical studies showed that high-purity fish oil preparations could reduce cardiovascular events, but this has not been confirmed by subsequent clinical trials.

The commonly used dosage of fish oil is 0.5–1.0 g three times a day, primarily used to treat hypertriglyceridemia (TG). Adverse reactions are rare, occurring in 2%–3% of cases, including gastrointestinal symptoms. A few cases show mild elevations in transaminases or creatine kinase, and bleeding tendency is occasionally observed.