Fenofibrate in the treatment of dyslipidemia: a review of the data as they relate to the new suprabioavailable tablet formulation.
Abstract | BACKGROUND: OBJECTIVE: This paper reviews the pharmacologic properties, clinical usefulness, and safety profile of fenofibrate in the management of dyslipidemias. METHODS: RESULTS:
Fenofibrate is well absorbed after oral administration, with peak plasma levels attained in 6 to 8 hours. The absolute bioavailability of fenofibrate cannot be determined due to its being virtually insoluble in aqueous media suitable for injection; however, after oral administration of a single dose of radiolabeled fenofibrate, approximately 60% of the dose appeared in urine, primarily as fenofibric acid and its glucuronated conjugate, and approximately 25% was excreted in the feces. The apparent volume of distribution is 0.89 L/kg in healthy volunteers, and protein binding is approximately 99% in healthy and hyperlipidemic patients. Neither fenofibrate nor fenofibric acid appears to undergo significant oxidative metabolism in vivo. Fenofibric acid has a half-life of 20 hours. Fenofibrate is effective in lowering TG levels and increasing HDL-C levels. Its LDL-C-lowering effect is greater than that of gemfibrozil. Adverse effects of fenofibrate appear to be similar to those of other fibrates, including gastrointestinal symptoms, cholelithiasis, hepatitis, myositis, and rash. Fenofibrate therapy has been associated with increases in serum aminotransferase levels, and clinical monitoring of these markers of liver function should be performed regularly. CONCLUSIONS:
Fenofibrate is effective in reducing levels of TG, TC, and LDL-C, and increasing levels of HDL-C in patients with dyslipidemias. Its efficacy and tolerability in the treatment of hypertriglyceridemia and combined hyperlipidemia have been demonstrated in numerous clinical trials. Its use is accompanied by a low incidence of adverse effects and laboratory abnormalities. Fenofibrate protects against coronary heart disease not only through its effects on lipid parameters but also by producing alterations in LDL structure and, possibly, alterations in the various hemostatic parameters. Its uricosuric property may prove to be a useful adjunctive attribute.
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Authors | Jadwiga Najib |
Journal | Clinical therapeutics
(Clin Ther)
Vol. 24
Issue 12
Pg. 2022-50
(Dec 2002)
ISSN: 0149-2918 [Print] United States |
PMID | 12581543
(Publication Type: Journal Article, Review)
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Chemical References |
- Anticholesteremic Agents
- Hypolipidemic Agents
- Fenofibrate
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Topics |
- Adult
- Anticholesteremic Agents
(therapeutic use)
- Biological Availability
- Chemistry, Pharmaceutical
- Clinical Trials as Topic
- Drug Interactions
- Fenofibrate
(adverse effects, economics, pharmacokinetics, therapeutic use)
- Humans
- Hyperlipidemias
(drug therapy, economics)
- Hypolipidemic Agents
(adverse effects, economics, pharmacokinetics, therapeutic use)
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