Oral Hypoglycaemic Agents (OHA): MOA and Drugs.pptx

This is a compact slide on Oral Hypoglycaemic Agents (drugs acting against diabetes, both type 1 and type 2) including its mechanism of action and drug examples.

1. Oral Hypoglycaemic Agents: MOA & Drugs Anirban Kumar Bora 17.11.2022 Assistant Professor Gitanjali College of Pharmacy Lohapur, Birbhum, West Bengal.

2. C ontents Sulphonylureas 01 Biguanides 02 Glinides 03 4 Thiazolidinediones Gliptins 5 6 α- Glucosidase Inhibitors Glucose Transport Inhibitors 7

3. 01 Sulphonylureas

4. Drugs Tolbutamide Glyburide Gliclazide Glipizide Glimepiride 1st Generation: 2nd Generation:

5. 1 Binds to specific receptors on β- cells of islets of Langerhans Mechanism of Action Stimulation of insulin release from β-cells of pancreas 2 Blocks ATP sensitive K + Channels 3 Depolarisation and influx of Ca 2+ ions into β-cells 4 Degranulation and exocytosis of stored insulin from β- cells

6. 2 Biguanides

7. 1 Directly or indirectly ↓ hepatic glucose production by inhibiting the mitochondrial respiratory chain complex I Drugs 2 ↑ in AMP which in turn activates AMP activated protein kinase (AMPK) 3 Triggers release of GLP-I 4 Stimulates gut- brain- liver vagal network (that regulates hepatic glucose production) Mechanism of Action Metformin

8. Ancillary Mechanism of Action ↑ G lucose uptake and utilisation in skeletal muscle ↓ C arbohydrate absorption from intestine ↓ C irculating low- density (LDL) and very low density lipoproteins (VLDL)

9. 03 Gli nides

10. Repaglinide Nateglinide Stimulation of insulin release from β-cells of pancreas [Insulin secretagogue] Drugs Type of Mechanism

11. 1 Binds to specific receptors on β- cells of islets of Langerhans Mechanism of Action 2 Closure of ATP sensitive K + Channels (known as SUR1 channel) 3 Depolarisation and influx of Ca 2+ ions into β-cells 4 Degranulation and exocytosis of stored insulin from β- cells Note Administered shortly before a meal to reduce postprandial rise in blood glucose in type 2 diabetes patients

12. 04 Thiazolidinediones

13. Selective agonist for peroxisome proliferator- activated receptor γ (PPAR γ ) [a nuclear hormone receptor] Regulates transcription of several insulin responsive genes ↑ Sensitivity of insulin in peripheral tissue (including adipose tissue, liver, skeletal muscle) Drugs Pioglitazone Mechanism of Action

14. 05 Gliptins

15. Sitagliptin Vildagliptin Drugs Saxagliptin Linagliptin Alogliptin

16. Inhibits enzyme DPP-4 (dipeptidyl peptidase 4) Stimulates insulin secretion Prevents inactivation of incretin hormones such as GLP-1 Mechanism of Action

17. 06 α- Glucosidase Inhibitors

18. Acarbose Miglitol Drugs Voglibose

19. Reversibly inhibit α- glucosidase enzyme [ α- glucosidase enzymes break down carbohydrates into glucose and other simple sugars that can be absorbed] Delays digestion of carbohydrates, resulting in lower postprandial glucose Mechanism of Action

20. 07 Glucose Transport Inhibitors

21. Canagliflozin Dapagliflozin Drugs Empagliflozin

22. Inhibits sodium- glucose cotransporter 2 (SGLT2) [SGLT2 is responsible for reabsorbing filtered glucose in the tubular lumen of the kidney] Promoting glucose excretion into the urine, thereby reducing the concentration of circulating glucose Mechanism of Action

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