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
esomeprazole, omeprazole, lansoprazole - class
proton pump inhibitors
esomeprazole, omeprazole, lansoprazole - target
irreversible inhibition of the H+/K+ ATPase
esomeprazole, omeprazole, lansoprazole - biochemical, physiological
inability of parietal cells to release H+ ions into the lumen due to H+/K+ ATPase activity loss
decrease in stomach acid production
esomeprazole, omeprazole, lansoprazole - treatment
peptic ulcers, GERD - increase in pH (decrease in acid concentration) allows the stomach/esophagus to heal
esomeprazole, omeprazole, lansoprazole - adverse effects
none predictable
esomeprazole, omeprazole, lansoprazole - interactions
may alter the absorption of other drugs through the GI tract (those that rely on acidic environment for absorption)
CYP2C19 inhibitor
antacids - target
NaHCO3, CaCO3, Al(OH)3/Mg(OH)2
antacids - biochemical, physiological
neutralizes stomach acid
decrease in stomach acid/increase in stomach pH
antacids - treatment
acute GERD
antacids - adverse effects
rebound hyperacidity upon discontinuation of therapy
antacids - interactions
aluminum antacids - avoid with aluminum containing agents (nephrotoxic)
may alter the absorption of other drugs through the GI tract (those that rely on acidic environment for absorption)
ondansetron, granisetron, palonosetron, dolasetron - class
5-HT3 receptor antagonists
ondansetron, granisetron, palonosetron, dolasetron - target
inhibition of the 5-HT3 receptor
ondansetron, granisetron, palonosetron, dolasetron - biochemical/physiological
inhibition of electrochemical/neurochemical signal from the CTZ and the vagus nerve (from the GI tract) to the Vomiting Center
emesis inhibition, relief of nausea
ondansetron, granisetron, palonosetron, dolasetron - treatment
very effective in treating chemo-induced, pregnancy related, and post-op nausea and emesis
ondansetron, granisetron, palonosetron, dolasetron - adverse effects
CNS (headache, lightheadedness), cardiovascular (EKG abnormalities)
ondansetron, granisetron, palonosetron, dolasetron - interactions
causes prolongation of QT interval
promethazine, cyclizine, meclizine, dimenhydrinate - class
anti-histamines
promethazine, cyclizine, meclizine, dimenhydrinate - target
inverse agonist of the H1 receptor
promethazine, cyclizine, meclizine, dimenhydrinate - biochemical/physiological
inhibition of electrochemical/neurochemical signal from inner ear to vestibular nuclei
emesis inhibition, relief of nausea
promethazine, cyclizine, meclizine, dimenhydrinate - treatment
motion sickness
promethazine, cyclizine, meclizine, dimenhydrinate - adverse effects
CNS (sedation), antimuscarinic (urinary retention, constipation, dry eyes)
promethazine, cyclizine, meclizine, dimenhydrinate - interactions
CNS depressants, CYP2D6 inhibitor, bupropion, contrast agents, tramadol (increased incidence of seizures)
scopolamine - target
antagonist for the H1 and muscarinic receptors of the inner ear
scopolamine - biochemical, physiological
inhibition of electrochemical/neurochemical signal from the inner ear to the vestibular nuclei
emesis inhibition, relief of nausea
scopolamine - treatment
motion sickness
scopolamine - adverse effects
generally well-tolerated
scopolamine - interactions
bupropion, contrast agents, tramadol (increased incidence of seizures)
aprepitant - target
NK1 receptor (in the STN and CTZ) antagonista
aprepitant - biochemical, physiological
inhibition of electrochemical/neurochemical signal from the STN and CTZ
reduces drug-induced inflammation and emesis/nausea
aprepitant - treatment
delayed phase drug-induced emesis (platinum associated complexes, chemotherapy), postoperative nausea and emesis
aprepitant - adverse effects
CNS (fatigue, dizziness, headache), dehydration
aprepitant - interactions
CYP3A4 inhibitor
nabilone, dronabinol - class
cannabinoids
nabilone, dronabinol - target
CB1 receptor agonist
nabilone, dronabinol - biochemical/physiological
stimulation of the CB1 cannabinoid receptors in and around vomiting center
emesis inhibition, relief of nausea
nabilone, dronabinol - treatment
prophylaxis for cancer chemotherapy-induced emesis when other treatments are ineffective, appetite stimulation/emesis suppression in AIDS and anorexic patients
nabilone, dronabinol - adverse effects
cardiovascular, abstinence syndrome (withdrawal)
nabilone, dronabinol - interactions
CNS/respiratory depressants
droperidol, prochlorperazine - class
dopamine receptor antagonists
droperidol, prochlorperazine - target
D2 receptor antagonist
droperidol, prochlorperazine - biochemical, physiological
inhibition of electrochemical/neurochemical signal from the CTZ to the vomiting center
emesis inhibition, relief of nausea
droperidol, prochlorperazine - treatment
effective in treating nausea as a result of an infection or unknown cause, postoperative nausea
droperidol, prochlorperazine - adverse effects
CNS (restlessness, anxiety), cardiovascular (hypotension, tachycardia)
droperidol, prochlorperazine - interactions
causes prolongation of QT interval
erythromycin - target
motilin analog - agonist for the motilin receptor
erythromycin - biochemical, physiological
motilin receptor agonist - stimulation of motilin receptor
increase in GI motility
erythromycin - treatment
emesis, constipation, GI irregularity
sincalide - target
cholecystokinin analog - agonist for the cholecystokinin receptor
sincalide - biochemical, physiological
stimulation of the cholecystokinin receptor
increase in GI motility, increase in digestion secretions
sincalide - treatment
emesis, constipation, GI irregularity, malnutrition
sincalide - adverse effects
cardiovascular (hypo or hypertension), CNS (headache, dizziness)
sincalide - interactions
none reported
loperamide - target
mu opioid receptor agonist
loperamide - biochemical, physiological
inhibition of contraction/relaxation of smooth muscle
inhibition of intestinal motility (increases small intestine transit time), allows for reabsorption of water and electrolytes
loperamide - treatment
available OTC for treatment of mild diarrhea
loperamide - adverse effects
CNS (sedation/drowsiness, headache, depression, euphoria)
loperamide - interactions
none reported, may interfere with absorption of some drugs
octreotide - class
somatostatin analogs
octreotide - target
inhibition of hormone-secreting tumors of the pancreas and GI tract
octreotide - biochemical, physiological
decreased secretion of 5-HT, gastrin, secretin, pancreatic polypeptide, and GLP-2
fluid retention, inhibition of motility
octreotide - treatment
severe secretory diarrhea
octreotide - adverse effects
gallbladder abnormalities, cardiovascular, hypo/hyperglycemia, hypothyroidism
octreotide - interactions
none reported, may interfere with absorption of some drugs
colestipol, cholestyramine - class
bile acid sequestrants
colestipol, cholestyramine - target
increases the amount of bile that reaches the colon
colestipol, cholestyramine - biochemical, physiological
increased fat absorption from intestine, decreased water/electrolyte secretion into the lumen of the GI tract
inhibition of GI motility
colestipol, cholestyramine - treatment
exudation (fluid loss), secretory diarrhea
colestipol, cholestyramine - adverse effects
anorexia, intestinal obstruction
colestipol, cholestyramine - interactions
none reported, may interfere with absorption of some drugs