Pharmacological effects of gemfibrozil on some isolated smooth muscle preparations of experimental animals

Background: Gemfibrozil is a member of fibrates (gemfibrozil, fenofibrate, ceprofibrate, and benzafibrate) which is employed for treatment of dyslipidemia particularly hypertriglyceridemiae through its action on peroxisome proliflator activated receptors (PPAR-). Objective: The aim of this work was to study the site of action and pharmacololgical effects of different doses of gemfibrozil on some isolated smooth muscles preparations of experimental animals. Materials and Methods: The experiments were conducted on isolated jejunum of rabbits, isolated spiral tracheal and urinary bladder strips of guinea pigs. Results: I- On isolated rabbit jejunum, gemfibrozil produced a dose-dependent reduction on the amplitude of jejunal contractions. The inhibitory effect of gemfibrozil was not abolished after complete blockade of alpha and beta adrenergic receptors, while it was completely abolished after inhibition of nitric oxide synthase by N-methyl L-arginine. On the other hand the stimulatory effects of nicotine small dose, acetylcholine, calcium gluconate, histamine and serotonin were not abolished after administration of gemfibrozil. II- On isolated tracheal spiral strips of ginea pigs, gemfibrozil produced a dose- dependent relaxation on the basal tone and a dose-dependent reduction on the amplitude of acetylcholine-induced tracheal contractions of the tracheal strips. The inhibitory effect of gemfibrozil was completely abolished after inhibition of nitric oxide synthase by N-methyl L-arginine. Gemfibrozil completely abolished also serotonin-induced contraction, while it has no effect on histamine or calcium-induced tracheal contractions. III- On isolated urinary bladder strips of guinea pigs, gemfibrozil produced a dose-dependent reduction on the amplitude of urinary bladder contractions. The inhibitory effect of gemfibrozil was not abolished after complete blockade of beta adrenergic receptors, while it was completely abolished after inhibition of nitric oxide synthase by N-methyl L-arginine. On the other hand the stimulatory effects of acetylcholine and serotonin were not abolished after administration of gemfibrozil. Conclusion: Gemfibrozil (antidyslipidemic, PPAR- agonist) reduced jejunal and urinary bladder contractions and has a relaxant effect on tracheal basal tone. So it has a beneficial effect in obstructive airway diseases and cases of urgency and frequency of micturation and urinary incontinence. However, it may be used cauciously in cases of ,GIT disturbances as constipation and prostatic hypertrophy

Comparison between duration dependent effects of Simvastatin and Gemfibrozil on dyslipidemia in patients with type 2 diabetes

To observe the duration dependent effects of two important classes of lipid lowering drugs i.e. simvastatin and gemfibrozil in type 2 diabetic patients with dyslipidemia in Pakistani population. Seventy type 2 diabetic patients with newly diagnosed dyslipidemia were enrolled and were divided randomly into two groups each, with 35 patients. Group I patients was given tablets Simvastatin 20 mg once daily and group II patients received tablet Gemfibrozil 600 mg twice daily. The study period comprised of 12 weeks. Fasting lipid profile and fasting blood sugar was analyzed on week 0 [day of inclusion], week 6 and week 12. At week 12 simvastatin decreased serum LDL cholesterol by 36.97% [P<0.001]. In contrast gemfibrozil did not reduce it significantly with a reduction of only 1.33% [P=N.S]. Simvastatin reduced serum total cholesterol and serum triglyceride by 29.88% [P<0.001] and 21.78% [P<0.001] respectively and increased serum HDL cholesterol by 16.67% [P<0.001]. While gemfibrozil decreased serum total cholesterol by 9.14% [P<0.001] and serum triglyceride by 30.84% [P<0.001]. Gemfibrozil raised serum HDL cholesterol levels by 18.08% [P<0.001]. Significant changes were observed in all lipid parameters with both simvastatin and gemfibrozil with regard to duration of treatment. Simvastatin was found to be more effective in lowering serum total cholesterol and LDL cholesterol levels in comparison to gemfibrozil, which was found to be more effective in lowering serum triglyceride and elevating serum HDL cholesterol levels. Both of these drugs were well tolerated and none of the patients exhibited any significant adverse effects. Both can be given as monotherapy in patients with type 2 diabetes mellitus and abnormal lipid profile

role of garlic powder and gemfibrozil in lowering lipid levels in patients of diabetes mellitus

To study the effects of powdered garlic [Allium sativum] on the lipid profile of patients of diabetes mellitus with hyperlipedemia. DESIGN: Controlled trial. PATIENTS AND METHODS: Ten patients fasting serum cholesterol levels of 280 mg/ 100 ml or more and /or triglyceride 180 mg / 100 ml or more were treated with powdered garlic at a dose of 6 grams/ day for four weeks. Gemfibrozil 1200 mg/day was used on seven patients for 4 weeks as standard drug for comparison. The data obtained showed a marked reduction in total serum lipids, cholesterol, triglycerides and LDL- Cholesterol levels while mean serum HDL - Cholesterol levels were significantly raised which was more marked with garlic as compared to gemfibrozil, CONCLUSIONS: Garlic power has got significant effect on lowering most of the serum lipids. HDL- C levels were raised with its use. In diabetic patients the beneficial effects of garlic powder are significant and economical

Effect of garlic [Allium Sativum] powder on lipid profile in patients of ischemic heart disease [IHD]

The effects of garlic [Allium Sativum] powder were studied on the lipid profile in patients of ischemic heart disease [I.H.D] and compared with gemfibrozil [Lopid], a standard lipid lowering agent. Twenty one patients of I.H.D. with raised lipid levels were administered 6 grams of garlic powder, in three divided doses, orally for four weeks. Seven patients of I.H.D. with raised lipid levels were given 1200 mg gemfibrozil orally per day in two doses for four weeks. Garlic powder reduced serum total lipids, cholesterol, triglycerides and LDL-C more than gemfibrozil but the differences were non-significant [P>0.05]. Garlic powder increased the level of HDL-C more than gemfibrozil and the difference was significant [p<0.01]. No side effect specifically comparing with gemfibrozil was detected in the patients treated with garlic