Final Exam - Individual Flashcards
rapid and short-acting, mimics spikes of physiologic secretion insulin after eating
bolus insulin
intermediate/long-acting, mimics normal pancreatic insulin secretion with constant levels, suppresses glucose production in the fasting and post-absorptive period
basal insulin
mixture of short-acting and intermediate/long-acting insulin derivatives
combination therapy
insulin - target
insulin receptor agonist
insulin - biochemical, physiological, stage/type
activates the insulin receptor tyrosine kinase - activates PI3K/Akt enzyme cascade
movement of GLUT4 transporters to surface of cell - uptake of glucose from systemic circulation into cells
stage 3 type 2 DM
insulin - adverse effects
hypoglycemia, lipodystrophy
insulin - interactions
none serious
glipizide, glimepiride, glyburide - class
2nd generation sulfonylureas
glipizide, glimepiride, glyburide - target
inhibition of the K+ channel in beta cells
glipizide, glimepiride, glyburide - biochemical, physiological, stage/type
mimics rise in intracellular ATP - causes beta cell depolarization
depolarization results in migration of insulin granules to cell surface and release of insulin into systemic circulation
stage 2 type 2
glipizide, glimepiride, glyburide - adverse effects
hypoglycemia, cardiovascular (myocardial damage/infarction)
glipizide, glimepiride, glyburide - interactions
none serious
metformin - target
activation of AMPK
metformin - biochemical, physiological, stage/type
initiation of insulin-independent migration of glucose transporters to cell surface
movement of GLUT4 transporters to surface of cell - uptake of glucose from systemic circulation into cells
stage 1/2 type 2 (doesn’t rely on insulin receptors or beta cells to work)
metformin - adverse effects
hypoglycemia, lactic/ketoacidosis, cardiovascular (tachycardia)
metformin - interactions
contrast agents induce ketoacidosis, substrate and inhibitor for the P-gp membrane efflux protein
pioglitazone, rosiglitazone - class
thiazolidinediones
pioglitazone, rosiglitazone - target
peroxisome proliferation activating receptor gamma (PPAR gamma) agonists
pioglitazone, rosiglitazone - biochemical, physiological, stage/type
increased expression of genes under the control of the PPAR gamma receptor
an increase in glucose uptake and fatty acid oxidation/metabolism
stage 2 type 2
pioglitazone, rosiglitazone - adverse effects
cardiovascular (congestive heart failure, myocardial ischemia), increased percent of bone fractures in women, hepatotoxicity, hematological (anemia)
pioglitazone, rosiglitazone - interactions
none serious
semaglutide, exenatide, liraglutide - class
GLP-1 agonists
semaglutide, exenatide, liraglutide - target
agonist for the glucagon-like peptide receptor
semaglutide, exenatide, liraglutide - biochemical, physiological, stage/type
stimulation of the GLP receptor and subsequent activation of the cellular enzyme cascade
stimulates insulin secretion, inhibits glucagon release, delays gastric emptying, decreases appetite
stage 2 type 2
semaglutide, exenatide, liraglutide - adverse effects
hypoglycemia, pancreatitis
semaglutide, exenatide, liraglutide - interactions
delayed gastric emptying - can affect the pharmacokinetic profile of other therapeutics (oral contraceptives and some antibiotics)
saxagliptin, sitagliptin - class
DPP-4 inhibitors
saxagliptin, sitagliptin - target
inhibition of dipeptidyl peptidase (DPP-4)
saxagliptin, sitagliptin - biochemical, physiological, stage/type
decreased metabolism/deactivation of GLP-1
increased GLP-1 - stimulates insulin secretion, inhibits glucagon release, delays gastric emptying, decreases appetite
stage 2 type 2
saxagliptin, sitagliptin - adverse effects
these compounds inhibit CD26 on lymphocytes - concern regarding immune function but nothing has been reported as of yet
saxagliptin, sitagliptin - interactions
delayed gastric emptying - can affect pharmacokinetic profile of other therapeutics (oral contraceptives and some antibiotics)
dapagliflozin, empagliflozin, canagliflozin - class
SGLT-2 inhibitors
dapagliflozin, empagliflozin, canagliflozin - target
inhibition of the sodium-glucose cotransporter 2 (SGLT-2)
dapagliflozin, empagliflozin, canagliflozin - biochemical, physiological
prevents reabsorption of glucose from kidneys into systemic circulation
decrease in sugar reabsorption from lumen of kidney into systemic circulation - lowering blood glucose levels
dapagliflozin, empagliflozin, canagliflozin - adverse effects
cardiovascular (hypotension), lactic/ketoacidosis, hyperkalemia, hypoglycemia, increased risk of bone fractures, increased risk of UTIs
dapagliflozin, empagliflozin, canagliflozin - interactions
diuretic drugs - increased risk of severe dehydration
glucagon - target
glucagon receptor agonist
glucagon - biochemical, physiological
stimulation of glucagon receptor
stimulates the production of glucose - glycogen breakdown and gluconeogenesis
glucagon - adverse effects
cardiovascular (hypotension, tachycardia, hypertension)
glucagon - interactions
none severe
cimetidine, famotidine, ranitidine - class
H2 receptor antagonists
cimetidine, famotidine, ranitidine - target
inhibits the activation of the H2 receptor
cimetidine, famotidine, ranitidine - biochemical, physiological
inability of parietal cells to release H+ into the lumen due to H+/K+ ATPase loss
decrease in stomach acid production
cimetidine, famotidine, ranitidine - treatment
peptic ulcers, GERD - increase in pH (decrease in acid concentration) allows the stomach/esophagus to heal
cimetidine, famotidine, ranitidine - adverse effects
generally well tolerated
cimetidine, famotidine, ranitidine - interactions
may alter the absorption of other drugs through the GI tract (those that rely on acidic environment for absorption)
CYP1A2/2D6 inhibitor