DESCRIPTION
An antilipemic agent which reduces both cholesterol and triglycerides in the blood.
CATEGORIES
Hypolipidemic Agents
CHEMICAL FORMULA
C20H21ClO4
COMPOSITION
Fenofibrate 160mg
INDICATION
For use as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb).
PHARMACODYNAMICS
Fenofibrate is a lipid regulating agent indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb). Fenofibrate is also indicated as adjunctive therapy to diet for treatment of adult patients with hypertriglyceridemia (Fredrickson Types IV and V hyperlipidemia). Fenofibric acid, the active metabolite of Fenofibrate, produces reductions in total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) in treated patients. In addition, treatment with fenofibrate results in increases in high density lipoprotein (HDL) and apoproteins apoAI and apoAII.
MECHANISM
Fenofibrate exerts its therapeutic effects through activation of peroxisome proliferator activated receptor a (PPARa). This increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III. The resulting fall in triglycerides produces an alteration in the size and
COMPOSITION
of LDL from small, dense particles, to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly.
ABSORPTION
Fenofibrate is well absorbed from the gastrointestinal tract. After absorption, fenofibrate is mainly excreted in the urine in the form of metabolites, primarily fenofibric acid and fenofibric acid glucuronide.
VOLUME DISTRIBUTION
95 L [moderate renal impairment (creatinine clearance of 50 to 90 mL/min)], 30 L [healthy adults].
ELIMINATION
Fenofibric acid is primarily conjugated with glucuronic acid and then excreted in urine. Following oral administration in healthy volunteers, approximately 60% of a single dose of radiolabelled fenofibrate appeared in urine, primarily as fenofibric acid and its glucuronate conjugate and 25% was excreted in the feces.
HALF LIFE
20 hours
TOXICITY
LD50=1600 mg/kg (Oral, in mice); Investigated as a teratogen and reproductive hazard.
FOOD INTERACTIONS
Increased absorption- take with meals.
SIDE EFFECTS
Headache, Back pain ,Nasopharyngitis, Nausea, Myalgia Joint pain or arthralgia ,Diarrhea ,Upper respiratory tract infection.