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Are Sulfonylureas or Meglitinides given alone or in combo?
Both
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How is Biguanide – Metformin/Glucophage taken?
Oral
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How is Biguanide – Metformin/Glucophage metabolized ?
Not really - Little or none
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How is Biguanide – Metformin/Glucophage excreted?
Renally
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What is the MOA for Biguanide – Metformin/Glucophage?
- Stimulates AMP activated protein kinase = the master regulator of metabolism
- - Decreases hepatic glucose production
- - Enhances action of insulin in peripheral tissues
- - Decreases absorption of glucose from GI
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What are the Adverse Effects of Metformine?
- G.I. – nausea, diarrhea, anorexia
- Lactic acidosis
- CI: impaired renal function, liver dysfunction and CHF
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Is Metformin used alone or in combo?
Both
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Does Metformin cause excessive hypoglycemia?
No
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Does Metformin cause Weight loss?
Yes
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Does Metformin cause a decreases triglycerides?
Yes
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What arethe Thiacolidinediones (TZDs or Glitazones)?
Pioglitizone/actos (main) and Rosiglitazone/Avandia
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What is the MOA of TZDs?
- Activate peroxisome proliferator-activated receptor γ (PPAR γ) in the nucleus
- Transcribe genes associated with lipid steal and insulin lowering of plasma glucose
- May inhibit hepatic gluconeogenisis
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What are the adverse effects of TZDs?
- Avoid with liver dysfunction and HF (see fluid retention)
- Fluid retention, edema
- Weight gain
- Avoid with heart failure
- Risk of bladder cancer
- Bone fractures
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Should you use TZDs alone or in combo?
Both
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Do TZDs cause excessive hypoglycemia?
No
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What effect do TZDs have on lipids/cholesterol?
Increase HDL and decrease TG
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Why is Rosiglitazone not used as much as Pioglitazone?
More adverse effects
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What are the alpha glucose inhibitors/glucose absorption inhibitors?
Acarbose and Miglitol
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Are Acarbose and Miglitol/Glucose absorption inhibitors used alone or in combo?
Combo, not as effective
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What is the MOA for Acarbose and Miglitol/Glucose absorption inhibitors?
- Inhibits pancreatic alpha-amylase and intestinal alpha-glucosidase
- Slows digestion of complex carbs and decreases peak PPG
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What are the adverse effects of Acarbose and Miglitol /Glucose absorption inhibitors?
- GI effects (avoid in intestinal disease)
- Elevation of liver enzymes
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Are Acarbose and Miglitol /Glucose absorption inhibitors used alone or in combo?
Combo
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When should you take Acarbose and Miglitol /Glucose absorption inhibitors?
With meals
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Are Acarbose and Miglitol /Glucose absorption inhibitors absorbed well?
No, act in GI
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What ar eth Incretin Mimetics?
- Exenitide (Byetta)
- Liraglutide (Victoza)
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What is the MOA of Exenitide (Byetta)and Liraglutide (Victoza)/ Incretin Mimetics?
Synthetic derivatives and mimics of GLP (glucoagon like protein-1)
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How are Exenitide (Byetta)and Liraglutide (Victoza)/ Incretin Mimetics administered?
SQ
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What are the adverse effects of Exenitide (Byetta)and Liraglutide (Victoza)/ Incretin Mimetics?
N/V, diarrhea, Renal impairment, risk of thyroid C cell cancer and pancreatitis
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What are Exenitide (Byetta)and Liraglutide (Victoza)/ Incretin Mimetics used for?
Type II DM and Weight loss
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What is the MOA of Exenitide (Byetta)and Liraglutide (Victoza)/ Incretin Mimetics?
- Decreased stomach emptying
- Fullness
- Decreased appetitie
- Enhance insulin secretion w/ glucose
- Reduced Glucagon secretion
- May protect pancreas
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What are the Dipeptidyl Peptidase-IV Inhibitors (Gliptins)?
- Sitagliptin (Januvia)
- Saxagliptin (Onglyza)
- Linagliptin (Tradjenta)
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Dipeptidyl Peptidase-IV Inhibitors (Gliptins) Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta) are given by what route?
Oral
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What is the MOA for Dipeptidyl Peptidase-IV Inhibitors (Gliptins) Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta)?
Inhibits Dipeptidyl Peptidase-4 (DPP-4), increases endogenous incretins (DPP-4 breaks down endogenous incretins)
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What are the adverse effects of Dipeptidyl Peptidase-IV Inhibitors (Gliptins) Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta)?
- Naopharyngitis
- Upper respiratory infections
- HA
- Pancreatitis
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Are Dipeptidyl Peptidase-IV Inhibitors (Gliptins) Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta) used alone or in combo?
Both
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Other than Incretin mimic what drugs also act in the Incretin system?
- Dipeptidyl Peptidase-IV Inhibitors:
- (Gliptins) Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta)
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Why is Pramlinitide (Symlin) only used with insulin?
Improves effectiveness of insulin by reducing Glucagon release
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What are the adverse effects of Pramlintide?
- Excessive hypoglycemia
- Gastroparesis
- N/V
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What is the MOA of Pramlitide?
- Mimics Amylin
- Decrease postprandial glucagon
- Delay gastric emptying
- Decreases appetite/weight loss
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What is the route of administration for Pramlintide (Symlin)?
SQ (b/c it is a peptide)
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What is the Amylin analogue?
Pramlintide
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What drugs are Na-glucose co-transporter inhibitors?
Canagliflozin (Invokana), Dapagliflozin (Forxiga)
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What is the route of administration for Canagliflozin (Invokana) and Dapagliflozin (Forxiga)?
Oral
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What are the adverse effects of Canagliflozin (Invokana) and Dapagliflozin (Forxiga)?
- Vaginal yeast infections and UTIs
- Polyuria
- Caution in renal failure
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Are Canagliflozin (Invokana) and Dapagliflozin (Forxiga) use alone or in combo?
Usually in combo, but both
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What is the MOA of Canagliflozin (Invokana) and Dapagliflozin (Forxiga)?
- Inhibits Na+-glucose co-transporter 2 (SGLT2) in the renal proximal tubule
- Inhibits glucose reabsorption, increases glucose excretion, lowers plasma glucose
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