Medications

Question 1

For sulphonylureas to be used, there should be some

Answer 1

residual number of β-cells

Question 2

Which generation of sulphonylurea is preferred in diabetes ?

Answer 2

2nd generation

Question 3

1st generation sulphonylureas

Answer 3

Chlorpropamide,
Tolbutamide,
Tolazamide,
Acetohexamide.

Question 4

2nd generation sulphonylureas include

Answer 4

Glipizide,
Glibenclamide,
Glimepiride, and
Gliclazide.

Question 5

MOA of sulphonylureas

Answer 5

They Inhibit K+-ATPase and hence closes K+channels in the β-cells. This leads to an influx of Ca2+ into the β-cells and this causes the release of insulin.

Question 6

All sulphonylureas are metabolized in the

Answer 6

liver

Question 7

Sulphonylureas have different excretion profiles

Answer 7

different excretion profiles

Question 8

Which Sulphonylureas undergo Hepatic excretion

Answer 8

Glipizide and Gliclazide

Question 9

Glibenclamide undergoes

Answer 9

40% hepatic excretion and 60% biliary excretion

Question 10

SE of Sulphunlyureas

Answer 10

Weight gain
• Hypoglycemia
• Hyponatremia
• GI upset

Question 11

How does Hyponatremia in Sulphunlyureas come about?

Answer 11

There is an increased sensitivity of ADH which dilutes the
system

Question 12

INSULIN concentration in the plasma is higher WHEN GIVEN

Answer 12

Oral than when glucose is given through the IV route. Due to incretin hormones

Question 13

Dpp4 inhibitors are also called

Answer 13

Incretins

Question 14

The types of incretin hormones

Answer 14

Glucagon-like peptide-1 (GLP-1) and Gastric inhibitory polypeptide/Glucose-dependent insulinotropic peptide (GIP)

Question 15

MOA of DPP4 INHIBITORS

Answer 15

DPP4 (Dipeptidyl peptidase 4) are enzymes that break down incretins, thereby, inhibition of DPP4 prolongs or preserves incretins.

Question 16

Examples of DPP4 INHIBITORS

Answer 16

Vildagliptin,
Sitagliptin
Saxagliptin

Question 17

Gliptins or DPP4 inhibitors are metabolised by

Answer 17

Liver - CYP3A4 and CYP3A5.

Question 18

CYP3A4 and CYP3A5 are used in the metabolism of DPP4 inhibitors

Answer 18

Such medications include enzyme
inhibitors (e.g. Ketoconazole, Itraconazole, Voriconazole, Fluoxetine, Cimetidine, Clarithromycin, Erythromycin, etc.) and enzyme inducers (Phenytoin, Rifampicin, Carbamazepine, Phenobarbital, Barbiturates, Glucocorticoids, etc.)

Question 19

Galvus Met

Answer 19

(Vildagliptin + Metformin

Question 20

Contraindications of gliptins

Answer 20

•History of pancreatitis
• Type 1 diabetes or DKA
• Severe renal impairment
• Heart failure
• Hepatic impairment
• Hypersensitivity to the drug

Question 21

SE OF DPP4 INHIBITORS

Answer 21

GI disturbances
• Upper respiratory infections
• Acute pancreatitis
• Sitagliptin causes weight loss
• Nasopharyngitis
• Diarrhea
• Peripheral edema

Question 22

Sitagliptin causes

Answer 22

weight loss

Question 23

MOA of incretins

Answer 23

These medications mimic the incretins. They bind and activate incretin receptors and aid in insulin secretion. They activate the GLP-1.

Question 24

Examples of Incretin mimetics GLP-1

Answer 24

Exenatide
Liraglutide.

Question 25

Action of the mimetics is more

Answer 25

prolonged than that of the endogenous incretins

Question 26

Between DPP4 and incretin Mimetics which is more effective?

Answer 26

DPP4 inhibitors will tend to be more effective than incretin mimetics. This is because DPP4 inhibitors stop the action of DPP4 enzymes hence preventing the breakdown of incretins. However, when incretin mimetics are taken, there would still be DPP4 enzymes in the system to break them down

Question 27

Contraindications of incretin mimetics

Answer 27

•Diabetic ketoacidosis • Severe gastrointestinal disease • Inflammatory bowel disease • Diabetic gastroparesis

Question 28

Thiazolidinediones are agonists at the PPAR-γ receptor.

Answer 28

Peroxisome proliferator-activated receptor gamma (PPAR-γ or PPARG) found in adipose tissues, pancreatic β-cells, vascular endothelium, and macrophages.

Question 29

when PPAR-γ is stimulated,

Answer 29

fat is utilized in the periphery and this increases insulin sensitivity.

Question 30

The anaemia caused by this Pioglitazone is termed

Answer 30

Dilutional anaemia

Question 31

Contraindications of Pioglitazone

Answer 31

History of heart failure • Previous or active bladder cancer • Uninvestigated macroscopic haematuria