Class 11 Deck 2 Flashcards
When are oral hypoglycemics used?
-Control glucose in type 2
What are sulfonylureas MOA?
- Act at pancreas to release insulin
- Decreases insulin resistance
What are the failure rates of sulfonylureas?
- 20% primary
- 10-15% secondary
When should sulfonylureas be avoided?
-With a patient with a sulfa allergy
What are the pharmocokinetics of sulfonylureas?
- Metabolized by liver
- Excreted by kidneys
- Active and inactive metabolites
Sulfonylureas most severe side effect? and what drugs have the greatest risk?
- Hypoglycemia
- One’s w/ longest half life (glyburide and chlorproamide)
can Sulfonylureas cross the placenta?
yes
besides hypoglycemia, What are the other Sulfonylureas side effects?
- Increase CV mortality by inhibiting ischemic preconditioning and less effect on lipids
- GI disturbances (N/V, abnormal LFT’s, cholestasis)
Sulfonylureas should be avoided in patients with liver disease except for what drug?
acetohexamide
Tolbutamide (orinase) tidbits. {1st gen}
- Shortest acting and least potent
- Fewest side effects (less potent metabolites)
Acetohexamide tidbits {1st gen}
- hypoglycemic action from its metabolite
- Uricosuric
Chlorpropamide (diabinese) tidbits {1st gen}
- Longest acting
- Prolonged w/ impaired kidneys
- Disulfiram reactions
- Hyponatremia
Glyburide {2nd gen} tidbits
- Single daily dose for 24 hour effects
- Increase sensitivity to insulin
- Decrease hepatic glucose production
Glipizide {2nd gen} tidbits
- Stimulates insulin secretion for 12 hrs
- increase peripheral glucose uptake
- Suppress hepatic glucose output
- no metabolite
Glimepiride {2nd gen} tidbits
- Stimulate insulin secretion
- decrease hepatic glucose production
Name the 2 meglitinides.
- Repaglinide
- Nateglinide
What do meglitinides do?
-Increase insulin secretion from islet cells
When should meglitinides be administered? and when should they not be administered?
- 15-30 mins before meals
- While fasting
how do meglitinides compare to sulfonylureas?
-Faster onset, shorter duraton
When are meglitinides active?
-When in presence of glucose
How do Alpha-Glucosidase Inhibitors work?
- Decrease carbohydrate digestion
- slows absorption of glucose from GI tract
When are Alpha-Glucosidase Inhibitors useful as monotherapy?
-when postprandial hyperglycemia is problem
Name 2 Alpha-Glucosidase Inhibitors.
- Acarbose
- Miglitol
What are the benefits of Biguanides?
- Inhibit glucose production by liver
- Positive effect on lipids
- Mild weight loss
- Low risk of hypoglycemia
What is the drawback of biguanides?
-Lactic acidosis
Metformin is a _______ while sulfonylureas are _______.
- Antihyperglycemic
- Hypoglycemic
_____________ produces satisfactory results in 50% of the sulfonylurea failures
Metformin
What are the intraop metformin considerations?
- Lactic acidosis
- Increased nephrotoxicity (IV contrast)
How is metformin eliminated?
- Not plasma bound or metabolized
- Excreted by kidneys (cautious in renal patients)
What is metformins MOA?
- Inhibits gluconeogenisis in kidney and liver
- Requires insulin (does not stimulate insulin secretion)
- Decreases triglycerides and cholesterol
What are the metfromin side effects?
- Anorexia
- Nausea
- Diarrhea
- Lactic acidosis (rare)
Name 2 Thiazolidinediones.
- Pioglitazone (actos)
- Rosiglitazone (avandia)
how do Thiazolidinediones work?
- decrease insulin resistance in skeletal muscle and adipose tissue (more glucose to tissue and out of blood)
- Requires insulin
- Decrease hepatic glucose output
- Decrease triglycerides and increase HDL and LDL
- Effective in the obese
side effects of Thiazolidinediones
- Weight gain
- Liver dysfunction
name the 3 Dipeptidyl Peptidase 4 (DPP-4) Inhibitors
-The gliptins
what are the Dipeptidyl Peptidase 4 (DPP-4) Inhibitors MOA
- Increase pancreas insulin secretion
- Limit glucagon
- Slow gastric emptying
- Promote satiety
side effects of Dipeptidyl Peptidase 4 (DPP-4) Inhibitors
- URI ad UTI
- Headache
- Pancreatitis
- angioedema
- Stevens johnson
- anaphylaxis
Name the 2 types of incretin mimetics
- GLP-1 (byetta and victoza)
- Amylin analogs (Symlin)
What do GLP1 do?
- Prolong gastric emptying
- Reduce postprandial glucagon secretion
What do amylin analogs do?
- Increase insulin
- slow gastric emptying
- increase beta cell growth
- appetite suppression
name the Sodium-Glucose co-Transporter 2 (SGLT2) Inhibitor. and what does it do?
- Invokana
- Increase urinary glucose secretion
when is invokana contraindicated?
- CrCl < 30
- ESRD
- dialysis
When should Byetta be avoided? Victoza?
- Renal failure
- Thyroid carcinoma
