Diabetic medications Flashcards
Sulfonyl ureas _____ insulin secretion
stimulate
_____ is the only insulin preparation that can be injected IV.
Regular insulin (short-actin)
What is NPH insulin?
Intermediated acting insulin
What is lente insulin?
Mixture of 30% semilente (short acting) and 70% ultralente (long acting) zinc insulin crystals–> intermediate acting insulin
How many times is insulin measured a day? How often will insulin be injected?
4- before each meal
2- one before breakfast one before dinner
What is humulin?
recombinant human insulin made in bacteria/yeast
What is novolin?
made by switching the aa that is different in pork insulin
T or F. Insulin in circulation forms hexamers with Zn, but hexamers dont bind the insulin receptor until dissoc.
T
Structure of insulin lispro
proline B28 and lysine B29 of humulin are switched— doesnt form hexamers
MOA of insulin lispro
doesn’t form hexamers, faster onset of action and shorter half-life than regular insulin
Describe insulin glulisine
rapid acting-insulin analogue that differs from human insulin in that the amino acid Asp at B3 is replaced by lysine and the lysine in B29 is replaced by glutamic acid. Does not form hexamers
Describe nsulin aspart
rapid acting insulin analog that exists only as a monomer
___, ____, and ____ all have the same pharmacokinetic properties - faster onset of action and shorter duration than regular insulin- because they exist in monomer form.
Insulin lispro, insulin aspart, insulin glulisine
What insulin therapies have an altered isoelectric point?
Insulin glargine, insulin detemir
What is insulin glargine?
recombinant human insulin analogue used for injection. Differs in a few amino acids, Long duration of action. Can be injected once a day.
What is insulin detemir?
Long acting human insulin recombinant analogue
Explain why insulin glargin and determir are long-acting.
When injected, the acidic solution is neutralized causing crystals to precipitate=slow absorption=long acting. The low peak insulin concentration decreases chances of nocturnal hypoglycemia.
____ is the treatment for DKA.
Insulin
____ is the treatment for hypoglycemic coma.
glucagon
Normal HbA1C is ___. Over __ is not good. ___ is dangerous
6,8,10
What are the sulfonylureas
glyburide, glipizide, gliclazide, glimepiride
MOA of sulfonylureas
Oral hypoglycemics. Act on insulin. Initially may increase insulin release. Long term treatment may decrease insulin metabolism and increase insulin sensitivity.
ADME of sulfonyureas
Rapidly absorbed from GI. extensively protein bound, metabolized in liver, excreted by kidney
What are the meglitinides
repaglinide and nateglinide
MOA of meglitinides
Oral hypoglycemics. Benzoic acid derivatives that increase insulin secretion.
ADME of meglitinides
Oral, GI rapid absoprtion, short half-life, take before each meal to control post-prandial glucose, metabolized by liver
AD of meglitinides
hypoglycema
What are the biguanides
metformin, metformin+glyburide
MOA and ADME of biguanides
oral hypoglycemics, does not affect insulin secretion, no hypoglycemia. Decreases hepatic glucose production
Absorbed from GI; little metabolism
What are the thiazolidinediones?
rosi-, pio-, rosi- + metformin …-glitazone
MOA and ADME of thiazolidinediones?
Bind PPARy, increase insulin sensitivity, increase glucose transport, absorb GI tract, little metabolism
What are the a-glucosidase inhibitors?
acarbose, miglitol
MOA, ADME of a-glucosidase inhibitors
reduce intestinal absorption of starch at brush border, reduce uptake of carbs to reduce post-prandial glucose rise, used in combination with other hypoglycemic drugs/insulin
Which oral hypoglycemic drugs act on hepatic glucose secretion?
Biguanides: metformin +/- glyburide
Which oral hypoglycemic drugs act on the brush border?
a-glucosidase inhibitors, acarbose and miglitol
Which oral hypoglycemic drugs act on insulin secretion?
meglitinides: regalinide, nateglinide
Which oral hypoglycemic drugs act on insulin sensitivity and increase glucose transport?
Thiazolidinediones- rosi, pio glitazone
Which oral hypoglycemic drugs decrease insulin metabolism, increase insulin sensitivity, and increase insulin uptake?
Sulfonylureas: glyburide, glipizide, gliclazide, glimepiride
_____ enhance the hypoglycemic actions of sulfonyureas.
NSAIDs
Therapeutic uses of somatostatins
insulinomas, glucagonomas, acromegaly
_____ is an antihypertensive antidiuretic that has potent hyperglycemic actions
Diazoxide
MOA of diazoxide
inhibits insulin secretion but NOT synthesis. So there is a build up in B cells.
Therapeutic uses of diazoxide
various forms of hypoglycemia including inoperable insulinomas
GLP-1 ____ glucose-dependent insulin secretion.
Increases
MOA for GLP1
increase glucose dependent insulin secretion, inhibits glucagon stimulated glycogenolysis, slow gastric emptying, decrease appetite, decrease glucagon, decrease postprandial glucose
What are incretins?
hormones that increase insulin secretion
What are the GLP1 receptor agonists?
Exenatide, liraglutide
What are the DPP4 inhibitors?
sitagliptin, saxagliptin, linagliptin
What are the amylin analogues
Pramlintide symlin
MOA of amylin analogues
aids glucose absorption, promote satiety, inhibits inappropriate secretion of glucagon, weight loss
MOA of colesevelam hydrochloride
bile acid sequesterant, lowers blood cholesterol, lowers HbA1C by .5%, LDL by 15%, interrupts enterohepatic cycling
