PhclD
Terms
undefined, object
copy deck
- 4 sulfonylureas
- 1. Glyburide 2. Glipizide 3. Gliclazide 4. Glimeperide
- Where are the potent sulfonylureas metabolized and how are they excreted? (the 4 G's)
- Metabolized in liver and excreted in urine
- Which of the sulfonylureas should not be used in renal impairment?
- Glyburide
- Which of the sulfonylureas can now be used in pregnant women after 11 wks gestation?
- Glyburide
- MOA of sulfonylureas (start with how things normally work)
- 1. Normally glu gets metabolized in B-cell and ATP increases blocking of ATP/K channel 2. K unable to leave and there is a decrease conductance resulting in influx of Ca 3. Increase Ca causes insulin vesicles to fuse with membrane and secrete insulin 4. Sulfonylureas work by binding to ATP/K channel and blocking it. Thus like ATP, it will cause insulin vesicles to fuse with membrane and insulin to secrete
- 5 drug interaction mechanisms of sulfonylureas
- 1. Displacement from plasma binding proteins by other drugs 2. inhibition of hepatic metabolism of sulfonylureas by other drugs 3. Reduction of renal excretion of sulfonylureas 4. Drugs with intrinsic hypoglycemic activity 5. Drugs w/intrinsic hyperglycemic activity
- MOA of meglinitides
- same as sulfonylureas so can't be taken together
- Which is a better regulator of post prandial, sulfonylureas or mglinitides?
- Meglinitides
- Name 2 meglinitides
- 1. repaglinide 2. nateglidide
- Name a biguanide
- Metformin
- 2 side effects that metformin DOES NOT cause
- 1. hypoglycemia 2. weight gain
- General MOA of metformin
- insulin sensitizer by 2 awys: 1. lowers blood sugar by improving resposne to insulin w/o increasing insulin secretion 2. Activates AMP-dependent protein kinase
- 2 SE of metformin
- 1. GI upset (diarrhea, nausea, anorexia) 2. Lactic acidosis (rare)
- Who are contraindicated for biguanides (3)
- liver and renal failure or conditions associated with hypotension
- 1st line drug for DM2
- Metformin
- There are 3 glitazones but 2 have been taken off market, there is one still available but what is the problem?
- Pioglitazone (actos)- issue with bladder caner
- 2 oral alpha-glucosidase inhibitors
- 1. acarbose (precose 2. Miglitol (glyset)
- MOA of oral alpha-glucosidase inhibtors
- Inhibits glucosidases in gut, which normally the enzyme will convert carbs to free glucose. By blocking this breakdown of complex sugars to glucose, it stops the post prandial increase of glucose
- Main SE of acarbose and why?
- Flatuelence and diarrhea because sugars that aren't absorbed get into large intestine and bacteria interacts with it causing GI symptoms
- Where is amylin made?
- Made in Beta cells and packaged and release with insulin
- There are 5 new tx for DM2, what are they?
- 1. human amylin analog AC137 (pramlintide) 2. GLP-1-incretin mimetics 3. DDPIV inhibitor 4. Bromocriptine (D2 agonist) 5. BARS (colesevalam)
- MOA of AC137
- slows gastic emptying and GI absorption of nutrients; also decrease glucagon secretion
- 2 GLP-1 -incretin mimetics
- 1. Exenatide 2. Liraglutide
- 6 MOA of GLP-1-incretin mimetics
- 1. Increase glu-dependent insulin secretion 2. enhance betacell function 3. slows gastric emptying 4. decrease appetite 5. inhibits glucagon secretion 6. decrease hepatic glucose output
- How is GLP-1 approved for tx of DM2
- In combination with metformin and/or sulfonylurea, no evidence that it can't be used as monotherapy
- 3 DPP IV inhibitors
- 1. sitagliptin phosphate 2. saxagliptin 3. linagliptin
- What is DPP IV?
- It is involved in the degradation of incretins like GLP-1
- MOA of DPP IV inhibitors
- increase GLP-1 by slowing degradation and increasing halflife
- What is the function of Bromocriptane
- Dopamine levels are low in diabetics during early mornings leading to increase SNS activity, to reverse this, bromocriptaine (D2 agonist) is given 2 hrs after waking to increase dopamine levels
- MOA of colesevalam
- indirectly reduce hepatic glu production by increaing secretion of GLP-1 and other incretins
- 3 class agents that causes weight gain
- 1. insulin 2. sulfonylureas 3. meglinitidees
- 2 class agents that decrease weight
- 1. amylin mimetics 2. GLP-IR agonist
- Side effect: Metformin
- 1. Gi disturbance 2. lactic acidosis
- Side effect: Insulin
- 1. hypoglycemia 2. weight gain
- Side effect: Sulfonylureas
- 1. hypoglycemia 2. weight gain
- Side effect: Meglinitides
- 1. hypoglycemia 2. weight gain
- Side effect: alphaglucosidase inhibitors
- 1. flatulence 2. diarrhea
- Side effect: Amylin mimetics
- nausea
- Side effect: GLP-1R agonist
- 1. nausea 2. weight loss
- Side effect: DPPIV inhibitors
- 1. URTI 2. HA
- Side effect: Bromocriptine
- 1. nausea 2. dizziness 3. fatigue
- Side effect: Celesevelam
- 1. GI upset 2. constipation