Exam 1 Drug Categories

Question 1

Natural Insulin

Answer 1

• half life 6 mins
• injected
• hexamer to monomer rate limiting step

Question 2

Ultra-Rapid Insulin Agents (3)

Answer 2

• Lispro, Aspart, Glulisine

- stay in monomeric form, do not aggregate to hexamers

Question 3

Intermediate Insulin Agent

Answer 3

• NPH

- has protamine (protein from fish sperm), delays absorption

Question 4

Long Acting Insulin Agent (3)

Answer 4

• Glargine, Degludec, Determir

- mimic basal levels of insulin secretion, no peak

Question 5

Biguanides

Answer 5

• Meformin
• increase insulin sensitivity by increasing AMPPK levels which increase AMP which decreases lipolysis, gluconeogenesis, and glycongenolysis
• lactic acidosis side effects
• hypoglycemia not risk, DECREASE WEIGHT
• can treat hyperinsulinemia in PCOS
• half life 1.5-3 hrs
• taken orally
• excreted unchanged by kidney
• GI distress common

Question 6

Sulfonylureas (what they do)

Answer 6

• increase insulin production by beta cells
• does so by binding to Mg-ADP on K-ATP channel on SUR1 subunit
• keeps channel closed which allows influx of Ca, which stimulates vesicle release
• oral delivery
• metabolized by LIVER
• hypoglycemia and weight gain risks

Question 7

Sulfonylureas (how to identify)

Answer 7

• 2nd gen: gly, glip, glime

- 1st gen: amide

Question 8

Which 2nd gen Sulfonylurea is longest duration?

Which 1st gen Sulfonylrea is shortest duration?

Answer 8

• Glyburide (2nd gen longest duration)

- Tolbutamide (1st gen shortest duration)

Question 9

Meglitinide (what is and how to identify)

Answer 9

• identify: -inide
• also increase insulin production by beta cells
• binds to different site on K-ATP channel than sulfonylureas, but same idea that keeps channel closed and allows influx of Ca
• oral delivery, rapidly absorbed by intestine
• metabolism by LIVER
• t 1/2 less than 2 hrs
• less risk for hypoglycemia than sulfonylureas, weight gain still common

Question 10

TZDs (what is and how to identify)

Answer 10

• identify: -azone
• sensitize the adipose tissue to glc by agonizing PPARy which activates transcription of genes in glc and lipid metabolism
• indirect effect on liver and muscle but also sensitize them
• oral delivery
• treats PCOS
• adverse effects: weight gain common, edema, heart failure, hepatotoxicity
• NO RISK hypoglycemia

Question 11

DPP-IV inhibitor (what is and how to identify)

Answer 11

• identify: gliptin
• elevates circulating GLP-1 by inhibiting DPP-IV
• increases insulin secretion, decreases glucagon concentration
• given orally
• clearance by kidney
• adverse effects: upper resp. tract infections, nasopharyngitis, & headaches
• no significant risk hypoglycemia

Question 12

GLP-1 Analogs (what is and how to identify)

Answer 12

• identify: -atide and -utide
• longer acting than endogenous GLP-1
• injected 2x/day
• silght increase in insulin secretion, inhibits glucagon, decreases appetite
• taken in combo with other drugs
• adverse: nausea (40%) and hypoglycemia

Question 13

Abliglutide

Answer 13

• GLP-1 analog

- half life 3-7 days

Question 14

Exenatide

Answer 14

• GLP-1 analog

- based on gila monster hormone

Question 15

Liraglutide

Answer 15

• GLP-1 analog

- 13 hr half-life

Question 16

Synthetic analog of Amylin

Answer 16

• Pramlinitide
• injected before meals AND WITH insulin
• binds to receptors in CNS, affects neuroendocrine pathways
• decrease appetite, suppress postprandial release of glucagon
• adverse: nausea (50%) and hypoglycemia (need lower dose of insulin than if taken alone)

Question 17

SGLT2 inhibitors (what is and how to identify)

Answer 17

• identify: gliflozin
• inhibits SGLT2’s which causes excretement of excess glc into urine
• adverse: thirst and dehydration
• increased incidence of lower UTIs

Question 18

alpha-glucosidase inhibitor (2)

Answer 18

• acarbose and miglitol
• Not common in US
• carbohydrate analogue that binds to a-glucosidase which normally cleaves complex carbs to simple sugars
• by inhibiting, increase time of absorption
• no peak in blood sugar after meal
• given orally
• adverse: flatulence, bloating, abdomen discomfort, diarrhea
• NO RISK HYPOGLYCEMIA or weight gain

Question 19

difference between acarbose and miglitol

Answer 19

• acarbose is not absorbable

- miglitol is absorbable (similar structure to glc)

Question 20

Treatment of excess insulin and hypoglycemia (2)

Answer 20

• Diazoxide: b cell K/ATP channel binding drug that keeps channel open and reduces secretion (generally by a tumor)
• Octreotide: synthetic form of somatostatin that reduces hormone release from glucagon and insulin tumors as well as thyrotropin-secreting pituitary adenomas