Diabetes Medications Flashcards
Metformin is the most common used drug in what class?
biguanides
WHat is metformin derived from?
french lilac
What does metformin do?
- inhibits the enzymes used for gluconeogenesis
- inhibits hepatic uptake of gluconeogenic substrates
- suppresses the mitochondrial repsiratory chain, increases insulin receptor tyrosine kinase activity and stimualtes GLUT4 transporters —– all increasing insulin sensitivity
What are the side effects of metformin?
about 50% complain of diarrhea with the initial dose
lactic acidosis is the most serious side effect
Why does the lactic acidosis happen?
the circulating lactate isn’t used as a substrate for gluconeogenesis, but those enzymes are inhibited
this means the lactate just builds up in the blood causing an acidosis
What are sufonylureas in general?
insulin secretagogues (meaning they promote insulin secretion)
What is the most commonly used sulfonylurea?
Glimepiride
How does Glimepiride work?
by binding to the SUR1 subunit of the ATP=sensitive potassium channel
it makes the channel close (essentially acting like glucose does)
This activates the Ca channels increasing intracellular Ca and thus triggering insulin release
What are the primary side effects of glimepiride?
hypoglyecmia
weight gain
Glimepiride is the most common, but what are some otherse?
First gen: tolbutamide, chlorporpamide
second gen: Glimepiride, glyburide, Glipizide
What made the second generations better than the first generations?
the first generations has half lives that were too long
How do they alter the pharmacokinetics of synthetic insulin preparations?
they use different amino acid substitutions in the alpha and beta chains
What insulin preparations are rapid acting?
Lispro
Aspart
Glulisine
What is the time of onset for the rapid acting? Peak effect? Duration?
15 minute to onset
max at .5-1.5 hours
Duration about 3-4 hours
What is the short acting insulin?
regular insulin!
What is the time of onset for insulin? Maximum effect? Duration?
30 minutes to onset
max at 2-3 hours
4-8 hr duration
What is the intermediate acting insulin?
NPH insulin
How long to onset? Maximum? Duration?
2-4 hours to onset
4-12 hours maximum effect
10-20 hour duration
What are the two long acting insulins?
Glargine
Detemir
How long does it take for the long acting to start having effect? WHen’s their max effect? Duration?
1-2 hours to onset
there’s no peak!!!
duration of 18-24 hours
What are the main side effects of insulin?
hypoglycemia (duh) weight gain allergic reaction to the preparation atrophy or hypertrophy of subcutaneous fat at injection site insulin resistance
Which incretin do we make analogs of to promote insulin secretion and inhbit glucagon secretion?
GLP-1 analogs
What is the main example of a GLP-1 analog?
Exenatide
How is exenatide administered?
administered subq before a meal
