Canonical Question
Endo Pharm – OHGAs
Master answer
| Drug class | Mechanism | Side effects |
|---|---|---|
| Biguanides (Metformin) | – Stimulates the movement of GLUT-4 receptors to the membrane of skeletal muscle and adipose tissue cells, increasing glucose uptake by those cells. – Also inhibits gluconeogenesis and glycogenolysis in the liver, and delays intestinal glucose absorption. | – Life threatening lactic acidosis may occur in the presence of renal impairment – Diarrhoea, n/v, abdominal discomfort common – Must be withheld prior to administration of iodinated IV contrast |
| Sulfonylureas (Gliclazide) | – Combine with KATP receptors on pancreatic ß cells, closing the ATP-dependent potassium channels to depolarize the cell, resulting in an influx of calcium which stimulates insulin secretion. | – Risk of hypoglycaemia – GIT disturbance – Stimulate appetite and may cause weight gain |
| Meglitinides (Repaglinide) | – Act by stimulating the same receptor as the sulfonylurea drugs but at a different side. | – Risk of hypoglycaemia – Repaglinide is a major substrate of CYP3A4 and caution should be used when administering with clarithromycin or antifungals, as may result in high plasma levels of repaglinide and consequent severe hypoglycaemia |
| Thiazolidinediones (Rosiglitazone) | – Act on the PPARg in fat cells to induce insulin sensitivity | – Associated with increased risk of peripheral limb fracture in post-menopausal women, and also some cases of diabetic maculopathy. – prone to cause severe fluid retention and precipitate heart failure, contraindicated in CCF – Contraindicated in people with known IHD. |
| Alpha- glucosidase inhibitors (Acarbose) | – Act by inhibit the enzyme that breaks down dietary complex carbs to sugar, reducing the quantity of glucose available for absorption | – Abdominal discomfort & distention, Flatulence – Elevates serum transaminases – Shouldn’t produce hypoglycaemia itself as does not promote insulin release |
| DPP-IV inhibitors (Sitagliptin) | – Inhibit the activity of the enzyme DPP-IV, which normally breaks down the gut hormones GLP-1 (glucagon-like peptide 1) and the protein GIP (gastric inhibitor peptide). GLP-1 and GIP stimulate glucose-mediated insulin release from the pancreas following an oral load of glucose. | – Monitor in renal insufficiency – May cause hypoglycaemia |
| SGLT2 inhibitors (Dapagliflozin) | – Inhibit Sodium-glucose transport protein 2 (SGLT2, which is responsible for reabsorbing glucose in kidney). – Decreased kidney reabsorption of glucose, glucosuria effect (Insulin and pancreatic b cell independent) | – May cause Hypoglycemia – May cause Severe Euglycemic Ketoacidosis, esp in post-op period – UTIs, Candidal Vulvovaginits |
JC 2019
Click to Open CICMWrecks Pharmacopeia Table: Hypoglycaemic Agents
Exam appearances
| Exam | Exact wording | Relationship | Success |
|---|---|---|---|
| 2013A Q06 | Classify the oral hypoglycaemic drugs; include their mechanism of action, and their most significant side effects. | historical_member | — |
| 2020B Q06 | Classify the oral hypoglycaemic drugs (20% marks); include their mechanism of action (40% marks) and their most significant side effects (40% marks). | historical_member | — |