A - 13 + 14. Pancreatic hormones and parenterally applied antidiabetic drugs. Pharmacotherapy of IDDM + Oral antidiabetics. Pharmacotherapy of non-insulin dependent diabetes mellitus

Question 1

Which pancreatic cells produce what hormone?

Answer 1

A-cells - glucagon
B-cells - insulin
D-cells - somatostatin
F-cells - pancreatic polypeptide

Question 2

DM1 and DM2 main difference

Answer 2

DM1 - elevated glucagon, needs exogenous insulin

DM2 - spectrum of insulin problems, both production and resistance

• lowered B-cell sensitivity to glucose
• circulating insulin is usually enough to prevent ketoacidosis

Question 3

B-cell stimulants

Answer 3

glucose
mannose
arginine
leucine
vagus

Question 4

Insulin structure

Answer 4

A and B chain held together by c-peptide

Question 5

Insulin action tissues

Answer 5

Liver
Muscle
Adipose

Question 6

Insulin receptor

Answer 6

Tyr-kinase

Question 7

Elimination of insulin

Answer 7

Breakage of disulfide bridges -> excretion through liver and kidneys

Question 8

Insulin glucose transporter effects

Answer 8

GLUT4 translocation in muscle and adipose

Question 9

Insulin muscle effect

Answer 9

Increased glucose uptake -> glycogen synthase -> increased glycogenolysis

Protein uptake increase

Question 10

Insulin adipose effect

Answer 10

LPL increase (reduces circulating FA)
Glucose uptake increase
Lipolysis decrease

Question 11

Insulin liver effect

Answer 11

Glycogenesis and triglyceride synthesis increase

Gluconeogenesis, glycogenolysis , ketogenesis decrease (indirect effect of decreased lipolysis in adipose)

Question 12

Ultra short acting insulin preps

Answer 12

Lispro insulin

Given subcutanously to DM1 around 5 min before meals

Active for 3-4 hours regardless of dosage

Question 13

Short acting insulin preps

Answer 13

Regular insulin

30 min after admin, works for 5-7 hours

Question 14

Intermediate/long acting insulin preps

Answer 14

Isophane

Insulin + protamine (10:1) ratio
Given subcutanously
Onset 90 min, lasts 24 hours

Question 15

Ultra long acting insulin preps

Answer 15

Glargine

Precipitates subcutanously, slow dissolving
Lasts >24 hours

Question 16

Complications of insulin preps

Answer 16

Lipodystrophy at injection site
Hypoglycemia
Allergy
Development of insulin resistance

Question 17

Oral antidiabetics: insulin secretagogues action

Answer 17

Closes K+ channels on B-cells -> depol -> insulin release

Question 18

Oral antidiabetics: insulin secretagogues - sulfonyrureas

Answer 18

Glipizide

Glimpiride

Question 19

Oral antidiabetics: insulin secretagogues - meglitinides

Answer 19

Repaglinide

Rapid onset, short duration - taken before meals

Question 20

Oral antidiabetics: insulin secretagogues - SE

Answer 20

Hypoglycemia (less than insulin preps)
Rashes, allergies
Weight gain

Question 21

Oral antidiabetics: Biguanides action

Answer 21

Inhibits gluconeogenesis in liver and kidneys
Stimulation of glucose uptake and glycolysis
Activates AMP-stimulated protein kinase

Question 22

Oral antidiabetics: Biguanides names

Answer 22

Metformin

Modern drug choice for DM2;

• Reduces glucose levels after meals and fasting
• Reduces endogenous insulin in patients with insulin resistance (insulin sparing)
• No weight gain

Question 23

Oral antidiabetics: Biguanides SE

Answer 23

• GI problems

- Lactic acidosis

Question 24

Oral antidiabetics: Thiazolidinediones action

Answer 24

Increases tissue sensitivity to insulin by activating PPAR-gamma receptor

Question 25

Oral antidiabetics: a-glucosidase inhibitors action

Answer 25

Inhibits a-glucosidase within intestines, inhibiting breakdown of polysaccharides, slowing absorption of glucose

Question 26

Oral antidiabetics: a-glucosidase inhibitors name

Answer 26

Acarbose

Question 27

Oral antidiabetics: DPP-4 inhibitor

Answer 27

Vildagliptin

GLP-1 degredation

Question 28

Oral antidiabetics: SGLT-2 inhibitor

Answer 28

dapagliflozin

Inhibits SGLT-2, responsible for 90% of glucose reuptake in kidneys

SE: rapid weightloss from glucosuria, dehydration