Dosing and uses of Bezafibrate
Adult dosage forms and strengths
Investigational in the United States
Barth Syndrome (Orphan)
Orphan designation for Barth syndrome
Orphan sponsor
- Barth Sydrome Foundation, Inc.; P. O. Box 618; Larchmont, NY 10538
Pediatric dosage forms and strengths
Safety and efficacy not established
Interactions
1-10%
Allergic reaction
Anorexia
Anemia
Constipation
CPK increased
Creatinine increased
Diarrhea
Dizziness
Dyspepsia
Eczema
Flatulence
Gastritis
Insomnia
Migraine
Nausea
Pain
Pruritus
Rash
Transaminases increased
<1%
Cholelithiasis
Myopathy
Rhabdomyolysis
Warnings
Contraindications
Hypersensitivity to bezafibrate, fibrates
Primary biliary cirrhosis
Pre-existing gallbladder disease
Concurrent use of MAO inhibitors
Pregnancy or breast-feeding
Cautions
History of jaundice or hepatic disorder
Concurrent use of HMG-CoA reductase inhibitors
Hepatic/renal impairment
Hypoalbuminemia or nephrotic syndrome
Pregnancy and lactation
Pregnancy category: Not available. Not recommended.
Lactation: excretion in milk unknown/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Bezafibrate
Mechanism of action
Increases VLDL catabolism by increasing lipoprotein and hepatic triglyceride lipase activities
Decreases triglyceride biosynthesis by inhibiting acetyl-CoA carboxylase
Decreases cholesterol biosynthesis by inhibiting 3-hydroxyl-3-methyglutaryl coenzyme A reductase
Absorption
Bioavailability: Almost complete (immediate-release); 70% (sustained-release)
Peak plasma time: 1-2 hr (immediate-release); 3-4 hr (sustained-release)
Distribution
Vd: 17 L
Protein bound: 94-96%
Elimination
Half-life: 1-2 hr
Excretion: 95% urine; 3% feces
