Metabolism And Inactivation

Degradation of insulin takes place in liver, muscles and kidney. In the liver, about 50 of the insulin is extracted, therefore insulin undergoes a strong first-pass effect when released from the pancreas. The capacity of hepatic degradation is maximal under normal conditions but may be reduced after oral administration of glucose, possibly because of the effect of gastrointestinal hormones (Kahn and Schechter, 1990). In the kidney, insulin is filtered via the glomerula and reabsorbed in the...

Initiation of Insulin Secretion

Initiators of insulin secretion switch on the secretory machinery. Thereafter modulators derived from nutrient metabolism, hormones peptides and neurotransmitters determine how fast or slow the machine will run. 3.1 MEMBRANE POTENTIAL AND PERMEABILITY TO K + It is now well accepted that initiation of insulin release in response to glucose and other nutrients is caused by depolarization of the B-cell as a first step followed by subsequent Ca2+ influx. The resting potential of mouse pancreatic...

Compounds Acting on Insulin Secretion Sulphonylureas

1 Chemical Structure 2 Actions 2.1 Pancreatic 2.1.1 Action on Insulin 2.1.2 Binding to and Uptake to Islet Cells 110 2.1.3 Binding to Other Tissues Ill 2.1.4 Membrane Potential and Ion Fluxes 112 2.1.5 Modulating 2.2 Extrapancreatic 2.2.2 Increase of Insulin Actions and Insulin-like Effects 115 2.2.3 Critical 2.2.4 Indirect Effects 117 3.1 Dosage and Application 117 3.2 Pharmacokinetic 3.3 Pathological Changes in Pharmacokinetics of Sulfonylureas 120 4 Toxic 4.1 5 Side 5.1 While Driving 5.2...

Compounds Acting on Glucose Absorption

1.2.1 Uses and 1.2.2 Glucose 1.2.3 Lipid 1.2.4 Blood 1.3.1 Dosage and 1.3.2 Pharmacokinetic 1.4 Toxic and Side 1.5 Interactions with Other 1.6 Clinical 1.6.1 Healthy 1.6.2 Type-I Diabetes 1.6.3 Type-II Diabetes 2.2.1 Glycogen Metabolism 160 2.2.2 Lipid 2.3 Uses and 2.4.2 Plasma 2.5 Toxic and Side 2.6 Interaction with Other 2.7 Clinical 2.7.1 Healthy 2.7.2 Type-I Diabetes 2.7.3 Type-II Diabetes Guar is derived from the endosperm of the seed Cyamopsis psoraloides (C. tetragonoloba). It contains...

S

Mean plasma glucose and plasma insulin responses to oral glucose before ( ) and after (O) 1 week of metformin treatment in NIDDM patients. Plasma glucose concentrations decreased significantly. (Source Fantus and Brosseau, 1986.) diabetics. Despite the controversy about hyperinsulinaemia as an independent risk factor for coronary heart disease, there is no doubt of its relationship to other risk factors (Campbell, 1990). In contrast to sulphonylureas, the non-insulinotropic biguanides...

Info

Source Hanefeld el al. (1990). markedly reduced, making acarbose the drug of choice for treating the metabolic syndrome after dietary failure (Hanefeld et al., 1990). In long-term trials, acarbose also lowered serum triglycerides and VLDL significantly, while cholesterol levels were not affected (Leonhardt et al., 1991). The therapeutic effects of acarbose and biguanides have been compared in Type-II diabetics (Pagano and Cavallo-Perin, 1990) and found to be...

Pharmacokinetics

The development of aldose reductase inhibitors as useful drugs is actually at the stage of evaluation of their pharmacodynamic benefit. Data on the pharmacokinetic properties of these drugs are therefore rather scarce. In addition, owing to their chemical heterogeneity, no common principles can be established. Tolrestat is absorbed after oral administration to the extent of about 70 in man. Data on different animal models give higher values (Dvornik et al., 1988). The maximal plasma level after...