Fenofibrate

Fenofibrate is a drug of the Abbott Labs and Lipanthyl by Solvay Pharmaceutical.

Dosage

The pharmaceutical form and the strength may change from one country from another, and from one brand to another. In the United States, Tricor was reformulated in 2005 and is available in tablets of 48 and 145 mg. This reformulation is controversial and is the subject of antitrust litigation by generic drug manufacturer Teva.^[2] In Europe, it is available in coated tablet but also in capsule, the strength range include 67, 145, 160 and 200 mg. The differences in strength belong to altered bioavailability (the fraction absorbed by the body) due to particle size. For example, 200 mg can be replaced by 160 mg micronized fenofibrate. The 145 mg strength is a new strength appeared in 2005-2006 which also replaces 200 or 160 mg as the fenofibrate is nanonised (ie the particle size is below 400 nm).

Mode of Action

Like the other fibrates, fenofibrate acts on PPARα to reduce cholesterol levels. The active ingredient in fenofibrate is fenofibric acid. Fenofibric acid inhibits the synthesis of cholesterol as well as enhancing its elimination as bile salts, while in addition both inhibiting the synthesis of triglycerides and enhancing their breakdown.

Recent Updates

A large study in 2005 of fenofibrate in patients with diabetes showed no change in total mortality or coronary artery events, but did show a significant change in overall cardiovascular events, as well as improving some microvascular complications of diabetes.^[3]

Like most fibrates, fenofibrate can cause stomach upsets and myopathy (muscle pain) and very rarely rhabdomyolysis. This risk is increased when used together with type 2 diabetes, even when nonstudy lipid-lowering medications were added. In FIELD, there were no cases of rhabdomyolysis reported in patients on combination therapy with fenofibrate and a statin. Thus, there is an increasing body of evidence that fenofibrate/statin combination therapy is safe and effective at managing dyslipidemia in patients with type 2 diabetes who are at risk for cardiovascular events. Fenofibrate increases the serum level of statins and therefore, a lower dose of statin is generally necessary. Dose of fenofibrate must also be lowered in moderate to severe renal failure and most experts recommend that fenofibrate be given in the morning and the statin at night. Fenofibrate has been shown to decrease progression of albuminuria and diabetic retinopathy.

References

1. ^ Wysocki J, Belowski D, Kalina M, Kochanski L, Okopien B, Kalina Z (2004). "Effects of micronized fenofibrate on insulin resistance in patients with metabolic syndrome". Int J Clin Pharmacol Ther 42 (4): 212–7. PMID 15124979.
2. ^ Abbott's request to dismiss antitrust charge over Tricor rejected. FDANews, Drug Daily Bulletin, (June 1, 2006) [1]
3. ^ FIELD study investigators (2005). "Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD study): randomised controlled trial". Lancet 366 (9500): 1849–61. PMID 16310551.