oral hypoglycemic drugs

about hypoglycemic drugs

1. Oral Hypo- glycemic drugs By Rinku meena

2. INTRODUCTION An oral antidiabetics agents commonly used in the treatment of type 2 diabetes mellitus. An oral hypoglycemic agents cannot be used as monotherapy in pt. With type 1 diabetes mellitus since these pt. Lack sufficent insulin.

3. COMBINATIONS What are Antidiabetic combnations ? Antidiabetic combinations are medicines with two or more classes of antidiabetic agent in one pill or dose . just having one pill may improve glycemic control .

4. SULFONYLUREASE INTRODUCTION A Sulfonamide derivative used for its antibacterial effects in typhoid patients produced hypo - glycemia . This observation led to the development of sulfonylureas .

5. MECHANISM OF ACTION Sulfonylurease reduce the blood glucose level by: Stimulating the release of insulin from the pancreatic B-cells. Increasing the sensitivity of peripheral tissues to insulin. Increasing the no. Of insulin receptors. Suppressing gluconeogenesis in the liver.

6. Adverse reactions Hypoglycemia Weight gain[1-3] Nausea and vomiting Cholestatic jaundice, agranulocytosis , aplastic and hemolytic anemias Generalized hypersensitivity reactions CONTRA INDICATIONS Pregnancy, lactation Renal and hepatic impairment

7. DRUG INTERACTIONS 1. Drugs that increase hypo- glycemic effects. NSAIDs, warfarin , sulfonamides - displace sulfonylureas from protein bindingmsites . Alcohol, chloramphenicol,cimetidine - inhibit metabolism of sulfonylureas . 2. Druges that decrease the action of sulfonylureas Diuretics and corticosteroids increase blood glucose level

8. FIRST – GENERATION SULFONYLUREAS Tolbutamide Its half- life is relatively short [6 hours] Is the safest sulfoylureas for use in elderly Chlorpropamide Has a long half- life [32hr] Contraindicated in elderly patients Tolazamide Comparable to chlorpropamide in potency but shorter acting [half life 7 hr.]

9. Second GENERATION SULFONYLUREAS Glyburide Has few adverse effects other than hypoglycemia . Contraindicated in the presence of hepatic and renal insufficiency. Glipizide Has the shortest half-life[3hr] Taken 30 min. Before meals Glimepiride Has the lowest dose of any sulfonylurea [a single daily dose of 1 mg]

10. Meglitinide INTRODUCTION A class of agents includes repaglinide and nateglinide . Although they are not sulfonylureas , they have common action.

11. Mechanism of action ; Their action is dependent on functioning pancreatic B-cells. The meglitinides have a rapid onset and a short duration of action.

12. Adverse Effects Hypo - glycemia hypersensitivity reactions

13. Biguanides METFORMIN the only currently available biguanide It increases glucose uptake and utilization by target tissues, thereby decreasing insulin resistance.

14. Mechanism of action Suppresses hepatic gluconeogenesis Inhibit glucose absorption from the intestines Stimulate peripheral uptake of glucose in tissues in the presence of insulin.

15. Biguanides Adverse effects ; These are largely gastrointestinal. LONG TERM use may interfere eith vita. B12 absorption. Nausea diarrhea

16. Biguanides Pharmacokinetics; metformin is well absorbed orally, is not bound to serum proteins it is not metabolized Excretion is via the urine.

17. Thiazlidenediones Also knows as; 1- PPRAs [ peroxisome prolifelator activated receptores ] 2- Glitazones

18. Mechanism of action Increase insulin sensetivity in liver and muscle Do not increase insulin secretion Reduce hepatic glucose output improve lipid profile May induce weight gain

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