Diabetes Mellitus Drugs

Question 1

Name the rapid-acting insulins

Answer 1

Lispro
Aspart
Glulisine

Question 2

Name the long-acting insulins

Answer 2

Glargine

Detemir

Question 3

Do longer-acting insulins have higher or lower risk of hypoglycemia compared to shorter-acting insulins?

Answer 3

Higher

Question 4

Mechanism of action of metformin

Answer 4

• 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

Question 5

AE of metformin

Answer 5

• GIT

- Increased risk of Vitamin B12 malabsorption to cause deficiency

Question 6

Mechanism of action of thiazolidinediones

Answer 6

• 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

Question 7

AE of pioglitazone

Answer 7

• Weight gain, peripheral edema
• Increased risk of heart failure and bone fractures
• Induces CYP450 to cause DDI

Question 8

List the sulfonylureas

Answer 8

Tolbutamide
Gibenclamide
Glipizide
Glicazide
Glimepiride

Question 9

Mechanism of action of sulfonylureas

Answer 9

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

Question 10

AE of SU

Answer 10

Weight gain
Hypoglycemia risk especially in elderly and those with renal impairments
Contraindicated in people with sulfa allergy

Question 11

List the meglitinides

Answer 11

Repaglinide

Nateglinide

Question 12

Mechanism of action of meglitinides

Answer 12

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

Question 13

Mechanism of action of acarbose and miglitol

Answer 13

Reversibly inhibits membrane-bound alpha-glucosidase in intestinal brush borders to slow down rise in glucose levels after meals

Question 14

Why are a-glucosidase inhibitors unpopular 2nd line treatments?

Answer 14

Lower efficacy (rapid metabolisation via intestinal bacteria) and poorer tolerance by patients due to flatulence

Question 15

List the DDP4 inhibitors

Answer 15

Sitagliptin
Vildagliptin
Alogliptin
Saxagliptin
Linagliptin

Question 16

Mechanism of action of DDP4 inhibitors

Answer 16

• 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

Question 17

List the GLP-1 receptor agonists

Answer 17

Exenatide

Liraglutide

Question 18

Mechanism of action of GLP-1 receptor agonists

Answer 18

• 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

Question 19

Why is exenatide and canagliflozin so expensive?

Answer 19

GLP-1 receptor agonists have been shown to reduce major adverse CV events, all-cause mortality and hopsitalisation for heart failure

Question 20

List the SGLT2 inhibitors

Answer 20

Empagliflozin
Canagliflozin
Dapagliflozin

Question 21

Mechanism of action of SGLT2 inhibitors

Answer 21

Reduces filtered glucose reabsorption in proximal renal tubules and lowers renal threshold for glucose to increase urinary excretion

Question 22

Which kind of patients should be careful of using incretin-based therapy?

Answer 22

Patients with pancreatitis

Question 23

AE of SGLT2 inhibitors

Answer 23

• UTI
• Female genital mycotic infections
• Increased risk of lower limb amputations by canagliflozin
• Diabetic ketoacidosis