《药理学》课程PPT教学课件（Endocrine Sys）35 insullin

Antidiabetic Drugs

Antidiabetic Drugs

InsulinInsulin is a small protein containing51 amino acids and is secreted from β cellsof pancreas.The main factor controlling thesynthesis and secretion of insulin is theblood glucose concen-tration

Insulin Insulin is a small protein containing 51 amino acids and is secreted from β cells of pancreas. The main factor controlling the synthesis and secretion of insulin is the blood glucose concen-tration

Pharmacological Effects.Carbohydrate metabolism·Increase glucose utilization·Decrease glucose synthesisFatmetabolismIncreaselipogenesis·Decease lipolysisProteinmetabolismIncreaseproteinsynthesis·Decrease protein breakdown

Pharmacological Effects • Carbohydrate metabolism • Increase glucose utilization • Decrease glucose synthesis • Fat metabolism • Increase lipogenesis • Decease lipolysis • Protein metabolism • Increase protein synthesis • Decrease protein breakdown

PharmacologicalEffects.Potassiumtransportation.PromoteKtinfluxofcell·Growth-promotingactionPromote protein,fatand ribonucleoside synthesis

Pharmacological Effects • Potassium transportation • Promote K+ influx of cell • Growth-promoting action • Promote protein, fat and ribonucleoside synthesis

PharmacokineticsThe liver and kidney are the principalsites of insulin uptake and degradationEach is capable of destroying 40% of theinsulin produced per day.Some of thepharmacokinetic properties of differentcommercially available insulin preparationaredepicted inTable31-2

Pharmacokinetics • The liver and kidney are the principal sites of insulin uptake and degradation. Each is capable of destroying 40% of the insulin produced per day. Some of the pharmacokinetic properties of different commercially available insulin preparation are depicted in Table 31-2

Clinical UsesDiabetesmellitusTypeI diabetes(IDDM)Type diabetes（NIDDM）·Diabetes complicated withinfection,operationpregnancy or ketoacidosisIntracellularpotassiumdeficiency.GlKsolution

Clinical Uses • Diabetes mellitus • Type Ⅰ diabetes (IDDM) • Type Ⅱ diabetes (NIDDM) • Diabetes complicated with infection, operation, pregnancy or ketoacidosis • Intracellular potassium deficiency • GIK solution

Untoward Effects·HypoglycemiaResponsivehyperglycemiaAllergicreactionInsulinresistanceLocalreactions

Untoward Effects • Hypoglycemia • Responsive hyperglycemia • Allergic reaction • Insulin resistance • Local reactions

Oral Hypoglycemic Agents.Sulfonylureas·Biguanides·α-glucosidase inhibitors

Oral Hypoglycemic Agents • Sulfonylureas • Biguanides • α-glucosidase inhibitors

SulfonylureasMechanism of action.Directstimulationofinsulinreleasefrom β cellsReduced glucagonsecretionImproved tissuesensitivity to insulin

Sulfonylureas Mechanism of action • Direct stimulation of insulin release from β cells • Reduced glucagon secretion • Improved tissue sensitivity to insulin

SulfonylureasPharmacokineticsAll sulfonylurea agents are readilyabsorbedfromthesmallandintestine福areavidly bound by plasmaproteinsTheironsetofactionalsovariesfromagent to agent(Table 3l-3)

Sulfonylureas Pharmacokinetics All sulfonylurea agents are readily absorbed from the small intestine and are avidly bound by plasma proteins. Their onset of action also varies from agent to agent (Table 31-3)