Endocrine pharm - first aid

Question 1

Insulin rapid acting

Answer 1

LAG - lispro, aspart, glulisine

Question 2

Insulin short acting

Answer 2

regular insulin

Question 3

intermediate acting insulin

Answer 3

NPH

Question 4

insulin long acting

Answer 4

determir, glargine

Question 5

Oral hypoglycemic agents

Answer 5

biguanides (metformin), sulfonylureas, glitazones/thiazolidinediones, meglitinides, GLP-analogs, DPP-4 inhibitors, amylin analogs, sodium glucose co-transporter 2 inhibitors, alpha glucosidase inhibitors.

Question 6

Biguianides (metformin) - mechanism of action

Answer 6

exact mechanism is unknown. this medication decreases gluconeogenesis, increases glycolysis, increase peripheral glucose uptake by increasing insulin sensitivity.

Question 7

Biguianides (metformin) - clinical use

Answer 7

FIRST line therapy in T2DM, can cause modest weight loss.

Question 8

Biguianides (metformin) - adverse effects

Answer 8

Gi upset, most serious is lactic acidosis (thus contraindicated in renal insufficiency).

Question 9

sulfonylureas - mechanism

Answer 9

chlorpropamide, tolbutamide, glimepiride, glipizide, glyburide

close beta cell potassium channel, cell depolarizes, calcium influx, insulin released.

Question 10

sulfonylureas - mechanism

Answer 10

Type2DM only as they stimulate endogenous insulin release. Requires some islet cell function.

Question 11

sulfonylureas - adverse effects

Answer 11

risk of hypoglycemia, weight gain,

Question 12

glitazones/thiazolidinediones - mechanism

Answer 12

pioglitazone, rosiglitazone

increase insulin sensitivity in peripheral tissue, binds to PPAR-gamma nuclear transcription regulator.

Question 13

glitazones/thiazolidinediones - clinical use

Answer 13

monotherapy in T2DM or with metformin of sulfonylurea. can be used safely in patients with renal impairment. Weight gain, edema, hepatotoxicity.

Question 14

Meglitinides - mechanism

Answer 14

nateglinide, repaglinide.

stimulate postprandial insulin release by binding to potassium channels on beta-cell membranes. NOTE that the binding site differs from sulfonylurea.

Question 15

Meglitinides - clinical use

Answer 15

montherapy or combined with metformin in T2DM.

Question 16

GLP-1 analogs - mechanism

Answer 16

exenatide, liraglutide

increase GLUCOSE DEPENDENT insulin release. decrease glucagon release, decrease gastric emptying, increase satiety.

Question 17

GLP-1 analogs - adverse effects

Answer 17

nausea, vomiting, pancreatitis

–> note can cause modest weight loss.

Question 18

DPP-4 inhibitors - mechanism

Answer 18

linagliptin, saxagliptin, sitagliptin
- INHIBITS DPP-4 enzyme that DEACTIVATES GLP-1 thereby increasing glucose dependent insulin release. decrease glucagon release, decrease gastric emptying, increase satiety.

Question 19

DPP-4 inhibitors - adverse effects

Answer 19

mild urinary or respiratory infections, weight neutral.

Question 20

SGLT-2 inhibitors - mechanism

Answer 20

canagliflozin, dapagliflozin, empagliflozin

block reabsoprtion of glucose in the PCT.

Question 21

SGLT-2 inhibitors - adverse effects

Answer 21

glucosuria, UTIs, vaginal yeast infections, hyperkalemia, dehydration

Question 22

Thionamides - mechanism

Answer 22

Propylthiouracil (PTU), methinazole

–> block thyroid peroxidase, this inhibits the oxidation of iodide and the organification (coupling), of iodine –> decreased thyroid hormone synthesis.

NOTE PTU also blocks 5-deiodinase, which blocks peripheral conversion of T4 to active T3.
PTU is also the drug of choice during pregnancy