antidiabetic agents II Flashcards

1
Q

List the Meglitinides

A
  1. Repaglinide
  2. Nateglinide
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2
Q

MOA of Meglitinides

A
  • bind and block ATP-sensitive K+ channel to cause membrane depolarization and increase Ca2+ influx on B cells
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3
Q

which Antidiabetic Agents can be used in sulfa allergy

A

Meglitinides

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4
Q

therapeutic effects of Meglitinides

A
  • decrease postprandial serum glucose
  • decrease HbA1c
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5
Q

route of administration and onset of action of meglitinides

A
  • oral, preprandially
  • rapid action; peak effect at 1 hour
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6
Q

MOA of Metformin (Glucophage)

A
  • increase glucost uptake (muscle and adipose tissue)
  • decrease glucose absorption from GI
  • decrease glucagon
  • decrease gluconeogenesis
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7
Q

drug of choice for Type 2 diabetics

A
  • Metformin
    • does not increase body weight
    • Reduces CV problems
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8
Q

theraputic effects of Metformin (Glucophage)? is glucose lowered in normal subjects

A
  • overall effect: decrease glucose levels
    • glucose is not lowered in normal subjects
    • decreases postprandial hyperglycemia
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9
Q

can metformin be used in children

A

safe for use in children > 10 years old

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10
Q

adverse effects of metformin

A
  • lactic acidosis
  • diarrhea
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11
Q

contraindications to taking metformin

A
  • lactic acidosis conditions
    • renal disease
    • hepatic disease
    • alcoholism
    • disease predisposing to tissue hypoxia (CHF, COPD)
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12
Q

List the Thiazolidinediones

A
  • Pioglitazone
  • Rosiglitazone
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13
Q

MOA of Thiazolidinediones

A
  • “insulin sensitizers”-> increase insulin sensitivity
  • ligands of the nuclear PPARy receptor -> post receptor insulin-mimetic action
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14
Q

theraputic effects of Thiazolidinediones

A
  • lowers insulin resistance
  • reduces the development of type 2 DM -> prophylatic use
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15
Q

adverse effects of Thiazolidinediones

A
  • weight gain
  • edema: increase in risk of heart failure in CHF patients
    • rosiglitazone black lavel warning for increased incidence of MI and angina
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16
Q

contraindications to taking Thiazolidinediones

A
  • hepatic disease
  • CHF
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17
Q

List the alpha-glucosidase inhibitors

A
  • Acarbose
  • Miglitol
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18
Q

MOA of alpha-glucosidase inhibitors

A

delayed carbohydrate digestion and absorption

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19
Q

theraputic effects of alpha-glucosidase inhibitors

A
  • Effectively lower postprandial serum glucose
  • Has minimal effects on fasting glucose
  • Modest decreases in HbA1c glycosylation
  • No significant effects on weight
20
Q

adverse effects of alpha-glucosidase inhibitors

A
  • flatulence
21
Q

oral glucose stimulates release of the incretins:

A
  • glucagon-like peptide (GLP-1)
  • glucose dependent insulinotropic peptide (GIP)
22
Q

function of GLP-1 and GIP

A
  • increase release of insulin
  • GLP-1 inhibits glucagon release -> decreased hepatic gluconeogenesis
23
Q

List the GLP-1 Incretin Mimetics

A
  • Exenatide
  • Liraglutide
  • Dulaglutide
  • Albiglutide
24
Q

incretin mimetics are resistant to enzymatic degradation by

A

DPP-IV

25
Q

route of administration of GLP-1 mimetics

A

S.C.

26
Q

theraputic effects of incretic mimetics

A
  • lowers postprandial and fasting serum glucose
  • potential increased B cell number and function
  • weight loss
27
Q

adverse effects of Incretin mimetics

A
  • acute pancreatitis
28
Q

contraindications to taking Incretin mimetics: Liraglutide

A
  • thyroid CA -> black box warning
29
Q

list the Dipeptidyl-peptidase-IV (DPP-IV) inhibitors

A
  • Sitagliptin
  • Saxagliptin
  • Linagliptin
  • Alogliptin
30
Q

MOA of Dipeptidyl-peptidase-IV (DPP-IV) inhibitors

A
  • potentiates the effects of incretin hormones, by inhibiting thier breakdown by DPP-IV
31
Q

theraputic effects of Dipeptidyl-peptidase-IV (DPP-IV) inhibitors

A
  • lowers postprandial and fasting serum glucose
  • has no significant effects on weight
32
Q

how are Dipeptidyl-peptidase-IV (DPP-IV) inhibitors administered

A

orally, once a day

33
Q

adverse effects of Dipeptidyl-peptidase-IV (DPP-IV) inhibitors

A
  • acute pancreatitis
  • pancreatic CA
34
Q

MOA and use of Pramlintide

A
  • synthetic analog of amylin, a hormone co-secreted with insulin
    • used as an adjuct to insulin therapy in type 1 and type 2 DM
    • regulates postprandial glucose by
      • decrease gastric empyting
      • centrally mediated modulation of appetite
35
Q

theraputic effects of Pramlintide

A

weight loss

36
Q

MOA of Bromocriptine

A
  • Dopamine agonist
  • reduction in postmeal plasma glucose levels due to enhanced suppression of hepatic glucose production
37
Q

therapeutic effects of Bromocriptine

A
  • no AM glucose surge
  • decrease fasting and postprandial free fatty acid and triglyceride levels
  • reduces the cardiovascular end point problems in diabetics
38
Q

MOA of Colesevelam

A
  • bile acid binding resin
  • MOA unknown
39
Q

adverse effects of Colesevelam

A
  • constipation and bloating
40
Q

List the SGLT2 inhibitors

A
  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin
41
Q

MOA of SGLT2 inhibitors

A
  • Inhibits the sodium-glucose co-transporter 2 (SGLT2) in the kidney
    • Blocks the reabsorption of glucose by the kidney, which results in increased glucose excretion and lower blood glucose concentrations in patients with type 2 diabetes mellitus
42
Q

adverse effects of SGLT2 inhibitors

A
  • female genital mycotic infections, UTIs and increased urinary frequency
43
Q

which antidiabetic drugs cause episodes of hypoglycemia

A
  • sulfonylureas
  • meglitinides
44
Q

which antidiabetic drugs cause episodes of hyperinsulinemia

A
  • sulfonylureas
  • meglitinides
45
Q

Which of the Antidiabetic drugs cause weight gain

A
  • sulfonylureas
  • thiazolidinediones
46
Q

Which of the Antidiabetic drugs causes weight loss

A
  • incretin mimetics
  • pramlintide