Each film-coated tablet contains: Gemfibrozil, USP 600 mg.
Pharmacology: Mechanism of Action: Gemfibrozil reduces total cholesterol, (low-density lipoprotein) LDL cholesterol, (very low density lipoprotein) VLDL, and triglycerides and increases (high density lipoprotein) HDL cholesterol. Gemfibrozil's mechanism of action has not been definitely established. In man, Gemfibrozil inhibits peripheral lipolysis and decreases the hepatic extraction of free fatty acids. It also inhibits synthesis and increases clearance of apolipoprotein B which is a carrier of VLDL leading to a decrease in VLDL production.
Gemfibrozil is readily absorbed from the gastrointestinal tract, peak concentration in plasma occur within 1 to 2 hours; the half life is about 1.5 hours. About 70% of a dose is excreted in the urine; little is excreted in the faeces. Plasma protein binding is about 98%.
Gemfibrozil is used to reduce total cholesterol and triglycerides in the management of hyperlipidaemias, including type Ila, type Ilb, type III, type IV and type V hyperlipoproteinaemias. It is also indicated for the primary prevention of ischaemic heart disease in hyperlipidaemic middle-aged men who have not responded to dietary and other measures.
The usual adult dose is 600 mg twice a day to be taken 30 minutes before the morning and evening meals. The dosage range may vary from 900 mg to 1500 mg a day or as prescribed by the physician.
Symptoms reported with overdosage were abdominal cramps, abnormal LFT's, diarrhea, increased CPK, joint and muscle pain, nausea and vomiting. Symptomatic supportive measure should be taken of overdose occurs.
Gemfibrozil is contraindicated in patients with hepatic or severe renal dysfunction, pre-existing gall bladder disease and patients who are hypersensitive to gemfibrozil.
Gemfibrozil should not be given to patients with severe hepatic impairment or significant liver disease, gallstones or gallbladder disorders, or hypoalbuminaemic states such as nephrotic syndrome. It should be used with caution in renal impairment and is contra-indicated if creatinine clearance is below 15 mL/minute unless the patient is on dialysis.
Pregnancy: There are no adequate data on use of Gemfibrozil in pregnant women. Animal studies are insufficiently clear to allow conclusions to be drawn on pregnancy and foetal development. The potential risk for humans is unknown. Gemfibrozil should not be used during pregnancy unless it is clearly necessary.
Breastfeeding: There are no data on excretion of gemfibrozil in milk. Gemfibrozil should not be used when breastfeeding.
Fertility: Reversible decreases in male fertility have been observed in reproductive toxicity studies in rats.
The most frequently adverse effect are abdominal pain, epigastric pain, diarrhea, nausea, vomiting and flatulence. Headache, dizziness, fatigue or drowsiness, skin rashes, pruritus, alopecia, and anaemia or leukopenia may occur.
Gemfibrozil is an inhibitor of a number of cytochrome P450 isoenzymes, including CYP2C8, CYP2C9, CYP2C19, and CYP1A2 and may increase the plasma concentration of drugs metabolised by these isoenzymes; it also inhibits some UDP-glucuronosyltransferases. Increased plasma concentration of bexarotene, pioglitazone, and rosiglitazone have been reported with gemfibrozil, and use of gemfibrozil in patients receiving repaglinide is contra-indicated due the risk of serious hypoglycaemia.
Store at temperatures not exceeding 30°C. Protect from light.
C10AB04 - gemfibrozil ; Belongs to the class of fibrates. Used in the treatment of hyperlipidemia.
FC tab 600 mg (white to off-white capsule, plain on one side and bisected on the other side) x 100's.