Mechanism of effect
They inhibit the synthesis of cholesterol and bile acid , and inhance the secretion of cholesterol in bile . the main effect is to reduce triglycerides by reducing the concentration of (VLDL) , they also increase HDL-cholesterol and have variable effect on LDL- cholesterol .
Pharmacodynamic
Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL.
Pharmacokinetics
Absorption : Completely but slowly absorbed from the intestine.
Distribution : Highly protein-bound (95% to 97%).
Metabolism : Chlofibrate is hydrolyzed by serum enzymes to the clotophyllic acid, and the metabolism of clotophyllic acid is metabolized in the liver.
Eliminations: half –life elimination is 18 to 22 hours by urine in form of a glucuronideconjucate .
Dosage
Adults—1.5 to 2 grams a day. This is divided into two to four doses.
Usual dose for neonatal jaundice is 100to 150mg/kg.
Side effects
nausea , Hematuria , vomiting , Diarrhea , cardiac arrhythmias , impotence , ProteinuriaInteractions
insulin , Prostatan , Gemfibrozil , Simvastatin , Lovastatin , Warfarin , Tolbutamide , glyburide , Tolazamide , Phenindione , MitiglinideAlerts
Do not take clofibrate if you have liver disease, kidney disease, biliary cirrhosis ,hypothyroidism, diabetes, and ulcer in your stomach or intestines.
Do not take clofibrate without first talking to your doctor if you are pregnantand breast-feeding.
Points of recommendation
Take clofibrate exactly as directed by your doctor.
Take each dose with a full glass of water.
Clofibrate can be taken with food to lessen stomach upset.
Do not crush, chew, or break the capsules. Swallow them whole.
Clofibrate is usually taken several times a day. Follow the directions your doctor has given to you.
Store clofibrate at room temperature away from moisture and heat.
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