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Endo II: Test 2 > Pharm: Insulin and Oral Hypoglycemic Agents > Flashcards

Pharm: Insulin and Oral Hypoglycemic Agents Flashcards

1
Q

insulin receptor?

A

tyrosine kinase enzyme activity

Insulin binding to the receptor stimulates autophosphorylation of the receptor Beta subunits and activation of tyrosine kinase activity

Docking proteins bind to the receptor and recruit other mediator proteins to the plasma membrane

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2
Q

GLUT receptors

A
  • glucose transport into the cells

GLUT2 = glucose sensor in the beta cells, liver, pancreas

GLUT 4 = muscle and fat cells

GLUT 3 = brain

binding of insulin –> GLUT transport expression in order for glucose transport into the cell. When insulin signal goes away then GLUT is internalized into the cell

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3
Q

Regulation of glucose metabolism?

A
  • Insulin stimulates glucose uptake
  • Insulin stimulates glucose storage and utilization
  • Insulin inhibits glycogen breakdown (glycogenolysis)
  • Insulin inhibits glucose synthesis (gluconeogenesis)
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4
Q

recommended hemoglobin A1C?

A

6.5-7%

t1/2 of 120 days - used to measure long term exposure to elevated glucose

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5
Q

metformin**

A

Biguanide: antihyperglycemic agent (oral)

** recommended starting place for tx of type II DM

Actions:

  • NOT hypoglycemic (makes it one of the safest)
  • increases insulin action, glycolysis, uptake and utilization by muscle
  • ** turns off gluconeogenesis, and decreases hepatic glucose output

Monotherapy can be used

Advantages:

  • no weight gain
  • no hypoglycemia
  • favorable lipid profile
  • its a pill, unlike inuslin, there is no injections

Concern: lactic acidosis w/ renal or hepatic insufficeincy (rare)

SE:
GI: anorexia, nausea, abdominal discomfort, diarrhea

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6
Q

Glimepiride**

A

Sulfonylureas: Stimulates insulin secretion (oral)

MOA:

  • Block ATP-sensitive K+ channel
  • Leads to depolarization and influx of Ca++
  • Results in insulin secretion
  • causes less weight gain than other SU’s

Adverse Effects: Weight gain and Hypoglycemia

CI’s: sulfa allergy, pregnancy, type 1 DM, ketoacidosis, renal failure, hepatic failure, and major surgery

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7
Q

Glipizide**

A

Sulfonylureas: Stimulates insulin secretion (oral)

MOA:

  • Block ATP-sensitive K+ channel
  • Leads to depolarization and influx of Ca++
  • Results in insulin secretion

Adverse Effects: Weight gain and Hypoglycemia

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8
Q

Glyburide**

A

Sulfonylureas: Stimulates insulin secretion (oral)

MOA:

  • Block ATP-sensitive K+ channel
  • Leads to depolarization and influx of Ca++
  • Results in insulin secretion

Adverse Effects: Weight gain and Hypoglycemia

    • greater incidence of prolonged hypoglycemia
    • use cautiously in elderly or those predisposed to hypoglycemia
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9
Q

Repaglinide**

A

Non-sulfonylurea secretagogue (Meglitinide)- Stimulates insulin secretion (oral)

    • insulin releasing agents - act same way as sulfonylureas
    • Blocks ATP-sensitive K+ channel - Binds at different site than sulfonylureas

Biggest difference from sulfonylureas?

  • Short half-life; rapid action
  • Taken right before meals (good advantage)
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10
Q

Nateglinide**

A

Non-sulfonylurea secretagogue (Meglitinide)- Stimulates insulin secretion (oral)

    • insulin releasing agents - act same way as sulfonylureas
    • Blocks ATP-sensitive K+ channel - Binds at different site than sulfonylureas

Biggest difference from sulfonylureas?

  • Short half-life; rapid action
  • Taken right before meals (good advantage)
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11
Q

Pioglitazone**

A

Thiazolidinediones (TZD): Insulin sensitizer (oral)
** use is controversial

MOA: PPAR-gamma agonists

  • binds to nuclear txn factors involved in insulin action
  • decreased insulin resistance
  • increased peripheral action of insulin
  • increased glucose uptake via (GLUT1 and GLUT4)
  • decreased hepatic glucose output

LONG TERM RISKS!

  • risk of MI and weight gain!!
  • causes fluid retention –> CHF
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12
Q

Acarbose**

A

alpha-Glucosidase inhibitor: prevents complex carbohydrates hydrolysis and delays carb abosorption (oral)

MOA:

  • inhibits digestion of complex sugars
  • Decrease sugar uptake after a meal
  • Cause flatulence and GI upset: poor compliance
  • Watch out for hypoglycemia when used with insulin or sulfonylurea
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13
Q

Miglitol**

A

alpha-Glucosidase inhibitor: prevents complex carbohydrates hydrolysis and delays carb abosorption (oral)

MOA:

  • inhibits digestion of complex sugars
  • Decrease sugar uptake after a meal
  • Cause flatulence and GI upset: poor compliance
  • Watch out for hypoglycemia when used with insulin or sulfonylurea
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14
Q

Exenatide**

A

Glucagon-Like Peptide-1 (GLP-1) Agonist: potentiates glucose-dependent insulin secretion, suppress glucagon secretion, slow gastric emptying, promotes satiety

dose: SC injection 1x/week

MOA:

  • enhances insulin secretion
  • inhibits glucagon secretion
  • appetite suppression/satiety
  • reduces gastric emptying
  • stimulates islet cell growth, differentiation, regeneration
  • ** decreased HbA1c, postprandial glucose and weight loss

Advantages: satiety and little hypoglycemia

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15
Q

ddx of diabetes?

A

Classic signs and symptoms

Unequivocally high FPG >126 mg/dL

Random glucose of >200 mg/dL

FPG of >126 mg/dL on two or more occasions

Failure on Oral Glucose Tolerance Test

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16
Q

Rapidly acting insulin?

A
  • shows one fast rapid peak
Insulin lispro (human)
insulin aspart (human)
insulin glulisine (human)
17
Q

short acting insulin

A

Regular insulin

18
Q

Intermediate-acting insulin?

A

NPH (Isophane Insulin Suspension)

19
Q

Long acting insulin?

A

Insulin Glargine

Insulin Detemir

20
Q

Fixed-mix insulin preparation?

A

NPH/Regular mixture

NPH/Humalog mixture

NPA/aspart

  • NPA/NPH are intermediate acting - these are used to sustain insulin, esp. at nighttime
  • regular/humalog/aspart are more rapidly acting and will result in short peaks throughout the day
21
Q

how does metformin differ from sulfonylurea agents?

A

-

22
Q

DDP-4 inhibitors

A
  • gliptin
  • potentiate glucose-dependent insulin secretion and suppress glucagon secretion (oral)

ex. Alogliptin, linagliptin, saxagliptin, stiagliptin phosphate

MOA: enzyme breaks peptide bonds
- increases insulin secretion, decreases glucagon, decreases hepatic glucose production, increases peripheral glucose uptake and utilization

Advantages: Little hypoglycemia

23
Q

Amylin analogs

A
  • mimics amylin (SC injection before meals)
  • ex: pramlintide acetate
  • third of fourth line tx: reqs. SQ injections prior to meals that can’t be mixed with inuslin

MOA:
- synthetic analog of amyln: results in decreased endogenous glucagon production, decreased gastric emptying time, decreased prostprandial glucose levels

** used esp. in pts w/ insulin resistance

24
Q

SGLT2 inhibitors

A
  • gliflozin
  • sodium-glucose co-transporter 2 inhibitors: decreases renal glucose reabsorption and increases urinary glucose excretion
  • ex: canagliflozin, dapagliflozin, empagliflozin

MOA:

  • oral tx once per day
  • SGLT2 is a membrane protein expressed on kidney: it transports filtered glucose from the proximal renal tubule into tubular epithelial cells.
  • By inhibiting SGLT2, canagliflozin decreases glucose reabsorption, increases urinary glucose excretion, and lowers blood glucose levels
  • Flozins are modestly effective in reducing HbA1c, systolic blood pressure and weight, with a low risk of hypoglycemia.

AE’s:
Genital mycotic infections can occur in both men and women; long-term safety still unknown.

25
Q

Sulfonylureas

A

“insulin releasers” (oral)
- glimepiride, glipizide, glyburide

MOA: Lower blood glucose

  • Block ATP-sensitive K+ channel
  • Leads to depolarization and influx of Ca++
  • Results in insulin secretion***

Key points:

  • stimulates insulin release –> lowers blood glucose
  • indirectly increase tissue sensitivity to insulin
  • helps suppress hepatic glucose output

** success depends on functionality of Beta cells!

26
Q

non-sulfonylurea secreatagogues

A
  • stimulates insulin secretion
  • Repaglinide, nateglinide
    • insulin releasing agents - act same way as sulfonylureas
    • Blocks ATP-sensitive K+ channel - Binds at different site than sulfonylureas

Biggest difference from sulfonylureas?

  • Short half-life; rapid action
  • Taken right before meals (good advantage)
27
Q

Thiazolidinediones (TZDs)

A 
Insulin sensitizers (oral)
ex. pioglitazone, rosiglitazone
  • use is controversial

MOA: PPAR-gamma agonists

  • binds to nuclear txn factors involved in insulin action
  • decreased insulin resistance
  • increased peripheral action of insulin
  • increased glucose uptake via (GLUT1 and GLUT4)
  • decreased hepatic glucose output

LONG TERM RISKS!

  • risk of MI and weight gain!!
  • causes fluid retention –> CHF
28
Q

signs of hypoglycemia?

A
  • need increased glucose - too much insulin (this is a common AE of tx of diabetes)

Signs and Symptoms

  • Sweating, hunger, paresthesias, palpitations, tremor, anxiety
  • confusion, weakness, drowsiness, blurred vision, loss of consciousness

Treatment:
Glucose
Glucagon

29
Q

alpha-glucosidase inhibitors

A

prevents complex carbs hydrolysis and delays carb absorption (oral)
ex. acarbose, miglitol

MOA:

  • inhibits digestion of complex sugars
  • Decrease sugar uptake after a meal
  • Cause flatulence and GI upset: poor compliance
  • Watch out for hypoglycemia when used with insulin or sulfonylurea
30
Q

Glucagon-like peptide-1 analog (GLP-1) agonists

A

potentiate glucose-dependent insulin secretion, suppress glucagon secretion, slows gastric emptying, and promotes satiety

ex: Exenatide, liraglutide
dose: SC injection 1x/week

MOA:

  • enhances insulin secretion
  • inhibits glucagon secretion
  • appetite suppression/satiety
  • reduces gastric emptying
  • stimulates islet cell growth, differentiation, regeneration
  • ** decreased HbA1c, postprandial (postmeal) glucose and weight loss

Advantages: satiety and little hypoglycemia

SE: not many, just GI

31
Q

advantages of metformin?

A

its first choice! and can be used as monotherapy

Advantages:

  • no weight gain
  • no hypoglycemia
  • favorable lipid profile
  • its a pill, unlike inuslin, there is no injections
32
Q

concern for metformin?

A

its considered quite safe, but lactic acidosis can rarely occur with

  • renal or hepatic insufficiency
  • CV disease
33
Q

SE for sulfonylureas?

A

Adverse Effects: Weight gain and Hypoglycemia

34
Q

which SU causes most hypoglycemia?

A

glyburide!

35
Q

benefits of GLP-1 agonists?

A

*** decreased HbA1c, postprandial (postmeal) glucose and weight loss

36
Q

whats big problem with GLP-1 agonist?

A

its a peptide, has to be injected! (no pill form :/) - though can now be once per week injections

37
Q

recommended HbA1c target?

A

below 6.5% for diabetics

38
Q

signs of hypoglycemia?

A

autonomic: sweating, hunger, paresthesias, palpitations, tremor anxiety
neuro: difficulty concentrating, confusion, weakness, drowsiness, feeling of warmth, dizziness, blurred vision, loss of consciousness

can be drug induced by: ethanol. beta adrenergic antagonists, salicylates

  • ethanol inhibits gluconeogensis
    • Beta agonists inhibit the effects of catecholamines on gluconeogensis and can mask the sympathetically mediated sx associated with low blood glucose (tremors, palpitations)

Endo II: Test 2 (10 decks)

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