Diabetes Mellitus Drugs Flashcards
Name the rapid-acting insulins
Lispro
Aspart
Glulisine
Name the long-acting insulins
Glargine
Detemir
Do longer-acting insulins have higher or lower risk of hypoglycemia compared to shorter-acting insulins?
Higher
Mechanism of action of metformin
- Decreases hepatic glucose production
- Increases density of insulin receptors
- Decreases intestinal glucose absorption
- Increases muscular glucose absorption
- Improves glucose tolerance, lowers both basal and postprandial plasma glucose
AE of metformin
- GIT
- Increased risk of Vitamin B12 malabsorption to cause deficiency
Mechanism of action of thiazolidinediones
- Increases insulin-dependent glucosal disposal
- Decreases insulin resistance in periphery and liver without increasing insulin production
- Activates nuclear transcription near PPAR-gamma to increase GLUT1 and GLUT4 production and enhance tissue sensitivity to insulin
AE of pioglitazone
- Weight gain, peripheral edema
- Increased risk of heart failure and bone fractures
- Induces CYP450 to cause DDI
List the sulfonylureas
Tolbutamide Gibenclamide Glipizide Glicazide Glimepiride
Mechanism of action of sulfonylureas
Lowers blood glucose by stimulating insulin release from pancreas
Targets b cell ATP-sensitive K+ channel by binding to SU receptor, inhibiting K+ efflux and triggering Ca2+ dependent exocytosis of insulin
AE of SU
Weight gain
Hypoglycemia risk especially in elderly and those with renal impairments
Contraindicated in people with sulfa allergy
List the meglitinides
Repaglinide
Nateglinide
Mechanism of action of meglitinides
Binds to and closes the ATP-dependent K+ channels by binding to SUR1 site of b cell, inhibiting K+ efflux in glucose-dependent manner to stimulate insulin increase
Mechanism of action of acarbose and miglitol
Reversibly inhibits membrane-bound alpha-glucosidase in intestinal brush borders to slow down rise in glucose levels after meals
Why are a-glucosidase inhibitors unpopular 2nd line treatments?
Lower efficacy (rapid metabolisation via intestinal bacteria) and poorer tolerance by patients due to flatulence
List the DDP4 inhibitors
Sitagliptin Vildagliptin Alogliptin Saxagliptin Linagliptin
Mechanism of action of DDP4 inhibitors
- Prevents degradation of incretin hormones glucagon-like peptide-1 (GLP1) and glucose-dependent insulinotropic polypeptide (GIP) by DDP4
- Prolonging incretin action to stimulate b cells to increase glucose-stimulated insulin release
- Suppress a cell mediated glucagon release and hepatic glucose production
List the GLP-1 receptor agonists
Exenatide
Liraglutide
Mechanism of action of GLP-1 receptor agonists
- Activates GLP-1 receptors in b cells to increase insulin release in presence of elevated glucose concentrations
- Suppresses glucagon release
- Delays gastric emptying, reducing appetite hence lowering glucose intake
Why is exenatide and canagliflozin so expensive?
GLP-1 receptor agonists have been shown to reduce major adverse CV events, all-cause mortality and hopsitalisation for heart failure
List the SGLT2 inhibitors
Empagliflozin
Canagliflozin
Dapagliflozin
Mechanism of action of SGLT2 inhibitors
Reduces filtered glucose reabsorption in proximal renal tubules and lowers renal threshold for glucose to increase urinary excretion
Which kind of patients should be careful of using incretin-based therapy?
Patients with pancreatitis
AE of SGLT2 inhibitors
- UTI
- Female genital mycotic infections
- Increased risk of lower limb amputations by canagliflozin
- Diabetic ketoacidosis
