Gliclazide - DrugBank
independent of its hypoglycaemic activity, may make gliclazide useful in .. of the dose/effect relationship at the time defined in phase 1 (t = 24 h) and using the. The quantitative structure – activity relationship in antidiabetic oral drugs . by 50 % and HbAlc by 33%, whereas glibenclamide and gliclazide. The effects of ingestion time of gliclazide in relationship to meals on plasma glucose, . Part I, pharmacological and hypoglycaemic activity studies in different animal species .. Diabetes and fibrin network structure: studies with gliclazide and.
Stimulating insulin secretion and thus reducing plasma glucose concentration. Basal insulin secretion and the secretory response to various stimuli are enhanced in the first few days of treatment with sulphonylurea drugs. With longer treatment, insulin secretion continues to be augmented and tissue sensitivity to insulin also improves, by an unknown mechanism.
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Absorption, Fate, and Excretion The sulfonylureas have similar spectra of activities; thus, their pharmacokinetic properties are their most distinctive characteristics. Although there are differences in the rates of absorption of the different sulfonylureas, all are effectively absorbed from the gastrointestinal tract.
However, food and hyperglycemia can reduce the absorption of sulfonylureas.
Hyperglycemia per se inhibits gastric and intestinal motility and thus can retard the absorption of many drugs. In view of the time required to reach an optimal concentration in plasma, sulfonylureas with short half lives may be more effective when given 30 minutes before eating. The volumes of distribution of most of the sulfonylureas are about 0. The first-generation sulfonylureas vary considerably in their half-lives and extents of metabolism.
Chlorpropamide has a long half-life 24 to 48 hours.
The second-generation agents are approximately times more potent than are those in the first group Lebovitz and Feinglos, Although their half-lives are short 1. The reason for the discrepancy between the half-life and duration of action of these drugs is not clear.
All of the sulfonylureas are metabolized by the liver, and the metabolites are excreted in the urine.
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Thus, sulfonylureas should be administered with caution to patients with either renal or hepatic insufficiency. Not unexpectedly, sulfonylureas may cause hypoglycemic reactions, including coma Ferner and Neil, ; Seltzer, This is a particular problem in elderly patients with impaired hepatic or renal function who are taking longer-acting sulfonylureas. Sulfonylureas can be ranked in order of decreasing risk of causing hypoglycemia based on their half-lives.
The N-methyl are inactive, N-ethyl have low activity, while N-propyl to N-hexyl are most active. Activity is lost if N-substituent contains 12 or more carbons 17 Cont. Structure activity relationship There must be a reasonable bulk group on the urea nitrogen; methyl and ethyl compound are not active. There is only one normally para substituent on the sulfonyl aromatic ring.
used in treatment of diabetes
The spatial relationship between the amide nitrogen of the substituent and the sulfonamide nitrogen is important. The blood sugar level reaches a minimum after h. It is oxidized rapidly in vivo to derivative with hydroxyl group I or derivative with carboxyl group IIwhich are inactive.
Because these processes are slow, chloropropamide is a long lasting drug. Second-generation oral hypoglycemic agent.
The drug has a half-life elimination of 10h, but its hypoglycemic effect remains for up to 24h. The third-generation oral hypoglycemic agent. Instead of the benzene ring found in Glibenclamide, Glimepiride contains a pyrrolidine system. According to its substitutes, literature divides sulfonamide derivatives to antibacterial sulfonamides and non-anti-bacterial sulfonamides.
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Gliclazide | C15H21N3O3S - PubChem
We presented these differences from these compounds changes in their chemical structure, in a way to build a solid base that can be depended on for developing new drugs from these compounds that interact with different receptors. Competing interests The authors have declared that no competing interests exist. In-vitro In-vivo In-silico Journal - 1 1: They have in common the same main core but they differ in their bioactivities; 12 The common core structure of sulfonamide is illustrated in Figure 1.
Literature used to divide sulfonamides into anti-bacterial sulfonamides; with an aromatic amine, and non-anti-bacterial sulfonamides; without an aromatic amine.SAR of acetylcholine / structural activity relationship of acetylcholine/ SAR of parasympathomimetic