Pharma 5

Question 1

Biguanides include

Answer 1

Metformin

Question 2

Mechanism of action of metformin

Answer 2

Liver (Major): Inhibits Gluconeogenesis & Glycogenolysis.
Muscle: Increases insulin sensitivity & Glucose uptake.
Gut: Delays glucose absorption.

Question 3

Result of the effects of metformin

Answer 3

Lowers fasting glucose without causing hypoglycemia (Euglycemic)

Question 4

Theraputic uses of Metformin

Answer 4

▪ As the initial drug of choice for type 2 diabetes (may be used alone or in combination with other oral agents or insulin).
▪ Used in the treatment of polycystic ovary syndrome, as it reduces insulin resistance

Question 5

Adverse effects of Metformin

Answer 5

1) GI upset: metallic taste, anorexia, diarrhoea
2) Vitamin B12 deficiency: Interferes with absorption in ileum
3) Lactic Acidosis: Rare but fatal. (Risk in renal failure)

Question 6

First-line therapy for Type 2 DM worldwide

Answer 6

Metformin

Question 7

Key feature of metformin

Answer 7

Antihyperglycemic (Euglycemic). Does not cause hypoglycemia when used alone.

Question 8

Thiazolidinediones (TZDs) include

Answer 8

Pioglitazone

Question 9

Mechanism of action of pioglitazone

Answer 9

Selective agonists of PPAR-γ (Peroxisome ProliferatorActivated Receptor-gamma) regulates the transcription of
genes involved in CHO and lipid metabolism, synthesis of
GLUT-4 and other genes involved in insulin sensitivity.

Question 10

“Insulin Sensitizers” enhance insulin sensitivity in muscle & fat

Answer 10

Thiazolidinediones (TZDs)

Question 11

Onset of pioglitazone

Answer 11

slow(gene transcription)

Question 12

Theraputic uses of pioglitazone

Answer 12

Used as a second- or third line agent for type 2 diabetes

Question 13

Adverse effects of pioglitazone

Answer 13

▪ Fluid retention/edema( congestive heart failure risk)
▪ Weight gain
▪ Bone fracture risk
▪ Bladder Cancer: Potential link with long-term Pioglitazone.

Question 14

Sulfonylureas include

Answer 14

Glipizide & Glimepiride

Question 15

Primary action of Sulfonylureas

Answer 15

Increase insulin secretion from pancreatic β-cells
(independent of glucose)

Question 16

An active metabolite of sulfonylureas

Answer 16

Glibenclamide

Question 17

Mechanism of action of sulfonylureas

Answer 17

Bind to the SUR1 subunit on ATP-sensitive K+ channels on
pancreatic β-cells → membrane depolarization → Ca2+ influx →
insulin release irrespective of glucose level

Question 18

Adverse effects of sulfonylureas

Answer 18

▪ Hypoglycemia (especially with Elderly, Renal Failure, Skipped
meals, Long-acting agents)
▪ Weight gain
▪ Secondary Failure: Initial response is good, but efficacy declines as
β-cell mass fails over time (5-10% fail/year)

Question 19

Salicylates (Aspirin), Sulfonamides given alongside sulfonylureas can result in

Answer 19

Displacement from ablumin = increase in free drug = hypoglycemia

Question 20

Cimetidine, Ketoconazole, Warfarin given alonside sulfonylureas can result in

Answer 20

CYP enzyme inhibition= increase plasma levels = hypoglycemia

Question 21

Rifampicin, Phenytoin given alongside sulfonylureas can result in

Answer 21

CYP enzyme induction= decrease efficacy = hyperglycemia

Question 22

Steroids, thiazides given alonside sulfonylureas can result in

Answer 22

Physiological antagonism = increase glucose = hyperglycemia

Question 23

Meglitinides include

Answer 23

Repaglinide

Question 24

Repaglinide is metabolized and excereted

Answer 24

They are metabolized in the liver and are excreted through the bile

Question 25

Mehcanism of action & benefits of repaglinide

Answer 25

Same as SUs (Block K+ channel) but different binding site. ▪ have faster onset and shorter duration. "Skip the meal, skip the pill." Lower risk of hypo than SUs.

Question 26

"Prandial Regulators". Taken immediately before meals

Answer 26

Meglitinides (Repaglinide)

Question 27

α-Glucosidase Inhibitors include

Answer 27

Acarbose

Question 28

Mechanism of action of acarbose

Answer 28

Inhibits enzyme in gut lining that breaks down complex carbs → Delays glucose absorption → Lowers postprandial glucose level

Question 29

Administration of acarbose

Answer 29

Taken just before meal

Question 30

Adverse effects of Acarbose

Answer 30

Severe Flatulence/GI upset (fermentation)

Question 31

Contraindications of Acarbose

Answer 31

Patients with inflammatory bowel disease

Question 32

Clinical key of α-Glucosidase Inhibitors (Acarbose)

Answer 32

If patient becomes hypoglycemic, Sucrose will NOT work because the drug blocks its breakdown. You MUST use Glucose tablets/gel or milk