Brozil

Brozil

gemfibrozil

Manufacturer:

Y.S.P. Industries

Distributor:

Y.S.P. Industries
Full Prescribing Info
Contents
Gemfibrozil.
Description
Colouring agents used for Brozil capsule are brilliant blue FCF and cochineal red A.
Action
Gemfibrozil is a synthetic antihyperlipidemic agent which is structurally related to clofibrate. It has been shown to be 10 times as potent in reducing triglycerides in animal studies and 3 times more potent than active clofibrate in reducing platelet aggregation.
Preliminary studies in human volunteers indicate that gemfibrozil is a safe and effective antihyperlipidemic agent in selected cases of primary hyperlipidemia.
Pharmacology: Gemfibrozil is a lipid-regulating agent which lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total serum cholesterol. These decreases occur primarily in the very low-density lipoprotein (VLDL) fraction. It has been reported that gemfibrozil may increase levels of high-density lipoprotein (HDL) subfractions, HDL2 and HDL3 as well as apolipoproteins A-I and A-II.
The mechanism of action of gemfibrozil is not completely understood but may involve inhibition of peripheral lipolysis; reduced hepatic extraction of free fatty acids which reduces hepatic triglyceride production; inhibition of synthesis and increased clearance of VLDL carrier; apolipoprotein B, which also reduces VLDL production; and according to animal studies, reduced incorporation of long-chain fatty acids into newly formed triglycerides accelerated turnover and removal of cholesterol from the liver (stimulates incorporation of cholesterol precursors into liver sterols), and increased excretion of cholesterol in the feces.
Pharmacokinetics: Gemfibrozil is well absorbed from the intestinal tract after oral administration. Peak plasma levels occur in 1-2 hrs with a plasma half-life of 1.5 hrs following single dose and 1.3 hrs following multiple doses. Plasma levels appear proportional to dose and do not demonstrate accumulation over time following multiple doses.
Gemfibrozil mainly undergoes oxidation of a ring methyl group to successively form a hydroxymethyl and carboxyl metabolite. Approximately 70% of the human dose is excreted in the urine, mostly of the glucuronide conjugate, with <2% excreted as unchanged gemfibrozil. Six percent of the dose is accounted for in the feces.
Capsule: Unlike clofibrate, gemfibrozil has no effect on plasma fibrinogen, nor does it influence glucose tolerance.
Indications/Uses
Hyperlipidemia.
Dosage/Direction for Use
2 caps twice daily preferable 30 min before the morning and evening meals.
Contraindications
Hypersensitivity to gemfibrozil.
Alcoholism.
Patients with preexisting gallstones and primary biliary cirrhosis.
Special Precautions
Before instituting Brozil therapy, every attempt should be made to controls serum lipids with appropriate diet, exercise, weight loss in obese patients and to control other medical problems, eg diabetes mellitus and hypothyroidism.
Pre-treatment laboratory studies should be performed to ensure that patients have abnormal levels of serum lipids. Periodic determination of serum levels should be obtained during administration. Gemfibrozil should be withdrawn after 3 months if the lipid response is inadequate.
Brozil capsule should be used with caution in patients with impaired hepatic function.
Brozil capsule should be used with caution in patients with impaired severe renal function. Reduced clearance leads to increased incidence of side effects; reduced dosage is recommended.
Use in pregnancy & lactation: Safety in pregnancy and nursing mothers have not been established. Therefore, it should not be used in pregnant women unless potential benefit justifies the potential risk to the fetus.
Mothers taking gemfibrozil should not breastfeed.
Use in children: Safety and efficacy in children have not been established.
Use In Pregnancy & Lactation
Safety in pregnancy and nursing mothers have not been established. Therefore, it should not be used in pregnant women unless potential benefit justifies the potential risk to the fetus.
Mothers taking gemfibrozil should not breastfeed.
Side Effects
Gemfibrozil is well tolerated in most patients. The most frequent side effects noted in clinical trials are:
Gastrointestinal: Abdominal pain, diarrhea and occasionally nausea in 3-5% of patients.
Less common side effects include:
Skin: Rashes.
Musculoskeletal: Tenderness.
Biochemical changes are uncommon, that include eosinophilia, decreases in the plasma of alkaline phosphatase and occasionally rises in transaminases. Gemfibrozil potentiates the effects of oral anticoagulants and may increase biliary lithogenicity with a predicted long-term increase in the incidence of gallstones.
Drug Interactions
Concurrent use of anticoagulants with gemfibrozil may significantly increase the anticoagulant effect of these medications; adjustments of anticoagulant dosage based on frequent prothrombin time determinations are recommended.
Concurrent use of lovastatin with gemfibrozil may be associated with an increased risk of rhabdomyolysis, significant increases in creatine kinase concentrations and myoglobinuria that leads to acute renal failure; may be seen as early as 3 weeks or as late as several months after initiation of combined therapy; monitoring of creatine kinase has not been shown to prevent severe myopathy or renal damage.
Storage
Store at temperature between 15°C and 30°C. Keep in an airtight container. Protect from light and moisture.
Shelf-Life: 3 years.
ATC Classification
C10AB04 - gemfibrozil ; Belongs to the class of fibrates. Used in the treatment of hyperlipidemia.
Presentation/Packing
Cap 300 mg x 60 x 10's, 500's.
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