Antidiabetic Drugs 2 Flashcards
chlorpropamide is a ___ generation sulfonylureas; what are some AE’s?
1st; has a long half life: hypoglycemia, hyperemic flush when dirt k alcohol and can potentiate action of vasopressin leading to SIADH
what are the effects of glucagon on:
cardiac ionotropy and chronotropy
intestine
- ↑ cardiac ionotropy and chronotropy
- relaxes the intestine (in large doses)
a typical regiment for managing diabetes in a pregnant patient tarot with a single dose of bedtime _______
NPH insulin
meglitindies are _____ (time) glucose regulators
postprandial; because these have a rapid onset and short duration of action so take them before each meal
both sufonuylureas and meglitinides have the same MOA. what is the difference and which one is more effective?
- meglitinides (repaglinide and nateglinide) hae sorter half life but are NOT AS EFFECTIVE in reducing fasting plasma glucose and HBA1c
meglitinides do not have sulfur and thus can be indicated in patients with sulfur allergy
colesevelam is a bile acid sequestrant used to lower ______
LDL cholesterol; give to type 2 DM patients
what are some scenarios you would give a diabetic patient statins?
should be given REGARDLESS OF LIPID LEVELS:
- patients with CVD
- younger than 40 with CVD risk factors
- older than 40 w/ or w/o CVD risk factors
a patient with type 2 DM tried to change lifestyle but his HBA1c levels did not improve. Doctor prescribes metformin but the levels did not lower by 1%. so he starts a dual combination therapy. What drugs would he prescribe?
oral agent, exenatide (injectable) or insulin
what type of patient is metformin contraindicated in?
those that are more prone to lactic acidosis:
- renal disease
- hepatic disease
- hypoxia
- alcoholism
what is the MOA of canagliflozin to treat diabetes?
- inhibits SGLT-2 and thus ↓ the reabsorption of glucose BUT because there is more glucose in the urinary tract, users of this drug are at more risk for UTI’s
pramlintide is an analog of _______
amylin;
amylin is a peptide that is co-secreted with insulin from β cells and it inhibits food intake, gastric emptying and glucagon secretion
what are two drugs that can cause pancreatitis?
- exenatide
- sitagliptin
what is the MOA and effect of acarbose?
- it reduces post prandial digestion of starch and carbohydrates in the upper intestine (↓ post prandial hyperglycemia and hyperinsulinemia)
- acarbose is a competitive inhibitor to the enzyme α glucosidase with converts disaccharides and trisaccharides to glucose
a diabetic patient presents with albuminuria. what drug would you give them in addition to what they are taking
ACEI or ARB’s
______ therapy should be given as a primary prevention statregy in patient with diebaes and an ↑ cardiovascular risk
low dose aspirin because it is an anti platelet agent
of the 2nd generation sulfonylreuas, which one is most likely to cause hypoglycemia? which one is least likely?
most likely to see hypoglycemia: glyburide
least likely to see hypoglycemia: glipizide (short half life)
any patient placed on ______ (diabetic drug) MUST be placed on liver function monitoring
TZD (glitazones) specifically troglitazone because it can cause severe hepatic toxicity (not seen with pioglitazone or rosiglitazone)
also with acarbose
when is a good time to use metformin?
insulin resistant patients because metformin does not cause secretion of insulin but rather ↓ gene expression of gluconoegenic enzymes
_______ is a drug that affects gene expression as part of its MOA in treating diabetes via activation of AMP activated protein kinase
metformin
weight loss/gain is an AE of metformin
weight loss;
with drugs that cause insulin secretion, the AE would be weight gain because insulin is anabolic
glucose is filtered by the glomerulus and reabsorbed in the proximal tubule by which transporters?
SGLT’s (sodium glucose linked transporter)
thiazolidinediones (TZDs) are used to ________ by ________
TZD’s: pioglitazone and rosiglitazone
↓ insulin resistance (help promote glucose uptake and utilization in adipose tissue) by acting as agonists for PPAR - gamma (peroxisome proliferator activated receptor)
which of the TZD’s have more favorable effects on lipids
- pioglitazone > rosigliazone
significant improvements on HDL, TG, LDL particle size and concentration
2nd generation sulfonylureas drugs that have replaced the 1st generation
2nd generation: glyburide, glipizide, glimepiride
1st generation: chlorpropamide
how long does it take to see the effects of TZD’s (-glitazones)
weeks or even months (mechanism of action involves gene expression)
long term use of metformin ay interfere with ____ (vitamin) absorption
B12
what is the major AE’s of exenatide?
- acute pancreatitis (exenatide can cause β cell proliferation)
- should NOT be use din patients with gastroparesis because the drug already slows down gastric emptying
how to sulfonylrureas stimulate insulin release from β cells?
bind to the SUR1 subunit and block the ATP sensitive K channel in the β cell membrane ultimately leading to exocytosis of insulin
_______ is the preferred agent for managing diabetes in pregnant patents
human insulin which are the short acting and NPH because they are the least immunogenic; (does not cross placenta unlike other drugs)
what are some contraindications of acarbose?
- IBS or any intestinal condition worsened with gas/distention
______ (transporter) is responsible for most of glucose reabsorption
SGLT-2
what is the MOA and effect of metformin?
- it has equal effectiveness of surlfonylureas at ↓ the fasting plasma glucose and HBA1c WITHOUT secreting insulin
- inhibits gluconoegenesis by reducing gene expression of gluconogeinc enzymes by activation of AMP activated protein kinase
- AND ↑ insulin mediated glucose utilization in the muscle and liver
the decision to transition to insulin in treating type 2 DM should be favorable when HBA1 levels are:
> or equal to 8.5%
typically insulin is not the intimal therapy in patients with type 2 DM.
what are some scenarios where it can be the initial therapy
patients with:
- significant hyperglycemic symptoms
- ketonuria
- HBA1c > 10%
- random glucose > 300 mg/dL
glucagon is used in ______ poisoning
β blocker
_____ (molecule) stimulates incretin secretion
glucose; incretin enhances glucose stimulated insulin secretion but it does NOT enhance insulin secretion on its own (requires glucose in the gut)
enhances glucose dependent insulin secretion
in severe hypoglemic patients who have lost consciousness and you cant find an IV line, you can give _____ via ____ (method of administration)
glucagon via subcutaneous or IM
______ and ______ (drugs) should not be used in patients with gastroparesis
- pramlintide (amylin analog)
- exenatide (incretin analog)
glitazones should NOT be use what type of patients?
those with Class III/IV HF because it can cause fluid retention and edema and exacerbate CHF
________ is the preferred first line drug in treating type 2 DM
metformin
_______ is given to treat the erectile dysfunction seen in the neuropathy caused by DM
sildenalphil (inhibits PDE 5)
what drugs would you give to improve the gastroparesis symptoms which can be a complication of diabetes
- metoclopramide
- erythromycin
boh are pro kinetic agents
______ (drug) is an incretin analog
exenatide (glucagon-like polypeptide 1 analog)
what is the enzyme that degrades human incretin?
DPP-4 (dipeptiduyy peptidase IV) and exenatide is resistant to it
________ can be given to ↑ the circulating GLP-1 and insulin levels by selectively inhibiting DPP-4
sitagliptin
DPP 4 breaks down incretin
patents with diabetes and HTN should be given _____
ACE inhibitor or ARB
sulfonylureas are effective at reducing _____ and _____
fasting plasma glucose and HBA1c
