Diabetes Mellitus Pharmacology

Question 1

only insulin suitable for IV use

Answer 1

regular insulin

Question 2

NPH insulin: mechanism of action, duration of action

Answer 2

cloudy suspension of insulin aggregated with protamine and zinc –> time involved in breaking down these aggregates causes delayed, longer time course of this drug = intermediate

Question 3

which insulin analogs are short acting and which are long acting?

Answer 3

short acting: lispro, aspart

long acting: glargine, detemir

Question 4

insulin lispro, aspart: mechanism of action, duration of action

Answer 4

prevent hexamer formation of insulin –> more readily form monomers in solution = short acting

Question 5

insulin glargine: mechanism of action, duration of action

Answer 5

causes insulin to be poorly soluble at pH7 –> when injected forms a precipitant that requires time to be absorbed = long acting

Question 6

insulin detemir: mechanism of action, duration of action

Answer 6

fatty acid chain is added –> self association at subcutaneous injection sties and by binding to albumin in bloodstream = long acting

Question 7

rank all of the insulin types from longest to shortest acting

Answer 7

glargine > detemir > NPH > regular > lispro/aspart

Question 8

what is the hemoglobin a1C goal for glycemic control in diabetic patients?

Answer 8

less than 7%

Question 9

describe the treatment regimen used for type 1 diabetics

Answer 9

“basal-bolus” regimen: short-acting analog (aspart/lispro) before each meal and once per day insulin glargine

Question 10

sulfonylurea: mechanism of action, 3 examples

Answer 10

stimulate insulin secretion by pancreas by interacting with beta cells’ potassium transporter –> depolarization and secondary calcium influx; glipizide, glyburide, glimepride

Question 11

two classes of insulin-sensitizing drugs

Answer 11

metformin and thiazolidinediones (rosiglitazone, pioglitazone)

Question 12

metformin: mechanism of action, contraindication

Answer 12

sensitizes liver to insulin –> decreases hepatic gluconeogenesis; contraindicated in patients with renal insufficiency due to side effect of lactic acidosis

Question 13

thiazolidinediones (rosiglitazone, pioglitazone): mechanism of action, side effects

Answer 13

make peripheral tissues such as fat and muscle more sensitive to insulin by activating PPAR; hepatotoxicity, weight gain, fluid retention

Question 14

acarbose: mechanism of action, side effects

Answer 14

glucosidase inhibitor: reduces post-prandial hyperglycemia by inhibiting enteric enzymes that break down complex carbohydrates; bloating, diarrhea, flatulence (therefore not commonly used)

Question 15

exenatide: mechanism of action

Answer 15

long-acting GLP-1 analog, augments insulin secretion, increases beta cell mass, inhibits glucagon secretion

Question 16

name 2 GLP-1 analogs

Answer 16

exenatide and liraglutide

Question 17

sitagliptin: mechanism of action

Answer 17

DPP-4 inhibitor (DPP-4 usually degrades GLP-1), prolongs the action of GLP-1 in circulation

Question 18

canagliflozin: mechanism of action

Answer 18

SGLT-2 inhibitor; inhibits glucose reabsorption in proximal tubule –> loss of glucose in urine

Question 19

which 3 drug classes are potent lower-ers of HgbA1C after insulin?

Answer 19

sulfonylureas (glipizide, glyburide, glimepride), metformin, thiazolidinediones (rosiglitazone, pioglitazone)

Question 20

in treating type 2 diabetes, it common to prescribe a drug that increases insulin + a drug that improve insulin sensitivity. give two examples of both

Answer 20

drugs that increase insulin: sulfonylureas (glipizide, glyburide, glimepride), insulin
drugs that improve insulin sensitivity: metformin, thiazolidinediones (rosiglitazone, pioglitazone)