What ion regulates the two forming steps of insulin?
Stimulating what receptors will inhibit insulin release?
alpha 2 adrenergic
Stimulating what receptors will cause in a release of insulin?
beta 2 adrenergic receptors and vagal nerves
What is the primary stimulatory factor that releases insulin?
What neurotransmitter is found in beta cells in pancreas and is released along with insulin?
What type of impairment has a more detrimental effect on insulin levels-- kidney or liver?
what is the most commonly used clinical marker utilized to screen for diabetes?
This is a yellow fluorescent AGE that is formed when arginine groups in proteins react with methylglyoxal that has built up inside cells during hyperglycemia?
____ insulin differs from human by substitution of 1 different AA?
_____ insulin differs from human by substitution of 2 different AAs?
What is the normal range of glucose when fasted?
What drugs can cause hypoglycemia?
beta adrenergic receptor antagonists
What drugs can cause hyperglycemia?
calcium channel blockers
These drugs stimulate the release of insulin from beta cells by binding to and blocking an ATP-ase sensitive K+ channel, which causes depolarization and an increase in intracellular calcium which leads to release of insulin?
These drugs may also decrease the hepatic clearance of insulin?
Are first gen or second gen sulfonylureas 100 times more potent?
The dosage must be individualized for these oral hypoglycemic agents?
Name the four first gen sulfonylureas.
Which first gen sulfonylurea has no active metabolites?
Which first gen sulfonylurea has the longest serum half life of 36 hours and is therefore the longest acting?
List first gen sulfonylureas in order of increasing half lives starting with the shortest half life.
Name the two second gen sulfonylureas.
Which second gen sulfonylurea has no active metabolites?
Name the third gen sulfonylurea.
What is the half life of glimepiride?
What are the addtl MOAs of glimepiride?
appears to translocate GLUT4 to the cell surface -- insulin like activity
may bind to a different protein than the usual sulfonylurea receptor on the beta cell
What is the indication for sulfonylureas?
control glucose in Type 2 when diet and exercise do not work
What is the pKa of sulfonylureas?
What is the most common side effect of the sulfonylureas?
lots of DIs
What is the indication for the thiazolidinediones?
for Type 2
alone or in combo with sulfonylurea or insulin
These drugs could cause hepatic failure?
Monitor transaminase levels before and after starting therapy with these drugs?
Name the two thiazolidinediones.
Which thiazolid is metabolized by 2C8 (and to a lesser extent by 2C9)?
Which thiazolid is metabolized by 3A4?
These drugs increase the activity of nuclear receptor PPAR gamma that regulates genes responsible for the control of glucose and insulin metabolism in adipose, liver and skeletal muscle tissues, which increases tissue sensitivity?
These drugs need to be taken with additional BC other than OCs?
thiazolids (mainly pioglitazone)
These drugs are contraindicated in patients at risk for heart failure?
What is a common side effect when taking thiazolids?
This drug is a non-sulfonylurea analog of glyburide?
What enzyme metabolizes Prandin?
this drug is for Type 2 w/ diet and exercise and can be used in combo with a thiazolid?
This drug stimulates the release of insulin in beta cells by binding to and blocking an ATPase sensitive K+ channel, which causes depolarization and an increase in intracellular calcium, which leads to release of insulin? May also decrease hepatic clearance of insulin and is a miscellaneous non-sulf?
This drug can decrease vit B12 and folate absorption?
This drug's half life is only 1.3-4.5 hours?
This drug has no protein binding and no metabolism with rapid renal excretion?
You should STOP taking this drug if you have an MI or septicemia?
T/F: metformin causes insulin release in the pancreas.
This drug is for Type 2 with diet and exercise and can be used in combo with a sulfonylurea?
This drug decreases hepatic gluconeogenesis and intestinal glucose absorption, increases peripheral tissue insulin sensititivity, and does NOT cause insulin release in the pancreas?
This drug is a D-phenylglycine and is unrelated to the sulfonylureas?
What enzymes metabolize Starlix?
2C9 = 70%
3A4 = 30%
This drug is highly selective with low affinity for heart and skeletal muscle potassium channels and has 98% albumin binding?
Which drug should you take w/ the first bite of every meal TID?
This drug decreases carb absorption by competitively inhibiting teh intestinal enzyme alpha glucosidase? Also prevents protonation of glycosidic bond in the saccharides.
Which one has minimal systemic absorption -- acarbose or miglitol?
Which one has rapid and complete systemic absorption -- acarbose or miglitol?
At what dose of acarbose can we see an elevated serum transaminase?
Name two alpha-glucosidase inhibitors.
What is a common adverse side effect of using alpha glucosidase inhibitors to treat Type 2 diabetes?
pneumatosis cystoides intestinalis
Which drug could reduce Hemoglobin A1C that Sreejayan is studying?
glipizide + metformin
rosiglitazone + metformin
glyburide + metformin
rosiglitazone + glimepiride
ACTOplus met combo
pioglitazone + metformin
Prandin (repag) + metformin
What are the two long acting insulins?
This insulin product is developed in saccharomyces cerevisiae and is followed by chemical modification with a fatty acid?
This long acting insulin forms microprecipitates in subQ tissue which prolongs its duration from 18 to 26 hours?
This insulin product is produced in E. coli?
Take this rapid acting insulin 5-10 min before a meal?
Take this rapid acting insulin 15 min before meals or immediately after eating?
What is the duration for both humalog and novolog?
Name the recombinant/chemically modified insulins.
This NME recombinant/synthetic insulin is an incretin mimetic or glucagon-like peptide -1 receptor agonist that binds the GLP1 receptor on beta cells causing insulin synthesis and excretion?
This NME recombinant/synthetic insulin is a synthetic analog of human amylin (which is a neuroendocrine hormone made by beta cells that contribute to post prandial glucose control)?
Pioglitazone + Glimepiride
This is a rapid acting insulin product for inhalation that failed?
What are incretins?
peptide hormones released from the gut in response to ingestion of carbs
What are the 2 MOAs of incretins?
regulate rate of nutrient transit in the GI tract (esp stomach emptying)
enhance glucose, stimulate insulin secretion from the pancreas when glucose levels are high
T/F: IV insulin causes the release of incretins
This drug could cause acute pancreatitis and the FDA also warns of acute renal failure and insufficiency?
This drug was originally identified in the Heloderm suspectum lizard (Gila monster) and has 39 amino acids?
Why is the action of incretins so short (short half life)?
because of rapid metabolism by DPP-IV
This drug has a black box warning for risk of thyroid C-cell tumors?
Inject this drug SubQ every day any time of the day independent of meals?
What is the MOA of Victoza?
mimics incretin or GLP-1 as an adjunct to diet and exercise
This drug is a DPP-IV inhibitor so it prolongs the biological levels of natural incretins GLP-1 and GIP, thereby increasing insulin release and decreasing glucagon release?
Does Januvia inhibit any CYP enzymes?
T/F: Januvia is a substrate for PGP
You need to modify the dosage of this drug if patient has moderate to end-stage renal failure b/c it is excreted via active tubular secretion as unchanged drug via organic cation transporters (OCT)?
Januvia + metformin
Januvia + simvastatin
What is the MOA of Onglyza?
How is Onglyza metabolized?
3A4 and 3A5 to an active metabolite
What is an adverse effect of Januvia?
cleaving other peptides like neuropeptides, cytokines, chemokines
What is an adverse effect of Onglyza?
decreased Lymphocyte countsd = UTI and URI
What is the newest DPP-IV inhibitor (2011)?
Do not use this new drug in Type 1 patients or patients with diabetic ketoacidosis or with insulin?
This drug is a mild inducer and mild inhibitor of 3A4, and a substrate for PGP? (new)
Old drug but new indication?
This drug is a dopamine receptor agonist, so it can increase dopamine levels early in the day and improve metabolism problems related to diabetes Type 2?
This drug was also marketed as Parlodel for Parkinson's and hyperprolactinemia?
this drug comes from human derived platelet growth factor?
Use this drug with extreme caution in patients with any known malignancy?
This is a 0.1% topical gel used to treat lower extremity diabetic neuropathic ulcers assuming that adequate blood supply is present?
Who cannot use Regranex?
anyone with a known neoplasm at the site of administration
How do you calculate the dose for Regranex?
length of gel in inches- (ulcer length) x (ulcer width) x 0.6
This is a bile acid sequesterant used as an adjunct to diet and exercise to improve glycemic control in adults with Type 2 DM?