Oral Hypoglycemic Drugs - Sulphonylureas

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Oral Hypoglycemic Drugs - Sulphonylureas

  1. 1. ORAL HYPOGLYCEMIC DRUGS PgBlazer.com
  2. 2. CLASSIFICATION α glucosidase Sulphonylureas Biguanides Meglitinide Thiazolidinediones inhibitors I generation Metformin Repaglinide Rosiglitazone Acarbose •Tolbutamide •Chlorpromamide Nateglinide Pioglitazone Miglitol II generation •Glibenclamide •Glipizide •Gliclazide •Glimepiride PgBlazer.com
  3. 3. Sulphonylureas • Lower blood glucose in normal persons and type 2 diabetics • Not effective in type 1 diabetics PgBlazer.com
  4. 4. Mechanism of action – Sulphonylureas SUR1 receptors on pancreatic β cell membrane Binding to receptor Reduced conductance of ATP sensitive K+ channels Depolarization of membrane Enhanced Ca2+ influx Degranulation of insulin vesicles PgBlazer.com
  5. 5. Mechanism of action – Sulphonylureas • Augment 2nd phase of insulin secretion • At least 30% functional β cells required PgBlazer.com
  6. 6. Extrapancreatic action – Sulphonylureas • Chronic administration – downregulation of sulphonylurea receptors – Insulin release decreased • But control of blood sugar is maintained • Tissues are sensitized to insulin – By Increase in insulin receptors and/or postreceptor action PgBlazer.com
  7. 7. Pharmacokinetics – Sulphonylureas • Well absorbed orally • High plasma protein binding – 90% • Low volume of distribution – 0.2-0.4 L/kg PgBlazer.com
  8. 8. Interactions – Sulphonylureas • Increasing sulphonylurea action – Displacement from plasma proteins – Decrease metabolism – Synergistic action • Decreasing sulphonylurea action – Increase metabolism – Antagonistic action PgBlazer.com
  9. 9. Interactions – Sulphonylureas • Increasing sulphonylurea action – Displacement from plasma proteins • Phenylbutazone • Sulphinpyrazone • Salicylates • Sulfonamides • PAS – Decrease metabolism – Synergistic action • Decreasing sulphonylurea action – Increase metabolism – Antagonistic action PgBlazer.com
  10. 10. Interactions – Sulphonylureas • Increasing sulphonylurea action – Displacement from plasma proteins – Decrease metabolism • Cimetidine • Sulfonamides • Warfarin • Chloramphenicol • Acute alcohol intake – Synergistic action • Decreasing sulphonylurea action – Increase metabolism – Antagonistic action PgBlazer.com
  11. 11. Interactions – Sulphonylureas • Increasing sulphonylurea action – Displacement from plasma proteins – Decrease metabolism – Synergistic action • Salicylates • Propranolol • Sympatholytic antihypertensives • Lithium • Theophylline • Alcohol (inhibits gluconeogenesis) • Decreasing sulphonylurea action – Increase metabolism – Antagonistic action PgBlazer.com
  12. 12. Interactions – Sulphonylureas • Increasing sulphonylurea action – Displacement from plasma proteins – Decrease metabolism – Synergistic action • Decreasing sulphonylurea action – Increase metabolism • Phenobarbitone • Phenytoin • Rifampicin • Chronic alcoholism – Antagonistic action PgBlazer.com
  13. 13. Interactions – Sulphonylureas • Increasing sulphonylurea action – Displacement from plasma proteins – Decrease metabolism – Synergistic action • Decreasing sulphonylurea action – Increase metabolism – Antagonistic action • Corticosteroids • Diazoxide • Thiazides • Furosemide • Oral contraceptives PgBlazer.com
  14. 14. Adverse Effects – Sulphonylureas • Hypoglycemia – Commonest – More in elderly, liver+kidney disease – More with Chlorpropamide – long action – Least with Tolbutamide – low potency, short action • Non specific side effects • Hypersensitivity PgBlazer.com
  15. 15. Adverse Effects – Sulphonylureas • Hypoglycemia • Non specific side effects – Nausea – Vomiting – Flatulence – Diarrhoea/constipation – Headache – Paresthesias – Weight gain • Hypersensitivity PgBlazer.com
  16. 16. Adverse Effects – Sulphonylureas • Hypoglycemia • Non specific side effects • Hypersensitivity – Rashes – Photosensitivity – Prupura – Transient leukopenia – Agranulocytosis (rare) PgBlazer.com
  17. 17. Adverse Effects – Sulphonylureas • Chlorpropamide – Cholestatic jaundice – Dilutional hyponatremia (sensitise kidney to ADH) – Disulfuram like reactions • Tolbutamide – Reduce iodine uptake by thyroid • Does not cause hypothyroidism • Should changeover to insulin during pregnancy PgBlazer.com

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