Download as PDF, PPTX
Oral hypoglycemic agent.pdf
- 1.
- 2. Classification • Sulfonyl ureas:Tolbutamide, Chlorpropamide, Glipizide, Glimepiride. • Biguanides: Metformin. • Thiazolidinediones: Pioglitazone, Rosiglitazone. • Meglitinides: Repaglinide, Nateglinide. • Glucosidase inhibitors: Acrabose, Voglibos
- 3. Sulfonyl ureas • Theseoral hypoglycemic medications are the first class used to treat diabetes. • Mechanism of action? These drugs bind to the sulfonyl urea receptors present in pancreatic β- cells. It leads to closure of ATP-sensitive K+ channels. Then it opens voltage gated Ca+2 channels and stimulates β-cells to secrete more insulin.
- 4. • 1 stgeneration- Chlorpropamide, Tolbutamide • 2 nd generation- Glipizide • 3 rd generation- Glimepiride
- 5.
- 6.
- 7.
- 8.
- 9.
- 10. • A substitutent,ideally in the para position, must be present in the benzene ring. The antihyperglycaemic efficacy was found to be enhanced by substituents such as methyl, acetyl, amino, chloro, bromo, trifluoromethyl. • It was discovered that the activity is further increased when the para position of benzene is substituted with an aryl carboxamidoalkyl group (second-generation sulphonylureas, such as glibenclamide). •
- 11. • For activity,the size of the group linked to the terminal nitrogen is essential. The N-propyl and higher homologues were found to be active, and the activity is lost when the N-substituent comprises 12 or more carbons. The group should also confer lipophilicity to the compound's N-methyl and ethyl substituents, which show no activity.