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Pharmacology Part 2 > Antidiabetic Drugs > Flashcards

Antidiabetic Drugs Flashcards

1
Q

Insulin’s MOA

A

Insulin binds to receptor on cell and GLUT 4 transported moves to cell surface and brings glucose into the cell
* without insulin, glucose cannot enter the cell

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2
Q

Insulin actions

A 
⬆️ glucose, aa, fatty acid and K uptake 
⬆️ glycogenolysis
⬆️ protein synthesis 
⬆️ TG synthesis 
Gluconeogenolysis
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3
Q

How much do insulins lower HBa1c levels?

A

2% decrease

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4
Q

Adverse effects of all insulins

A

Hypoglycemia
Lipodystrophies
Hypokalemia

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5
Q

Hypoglycemia and hyperglycemia cause problems for diabetics?

A

Hypoglycemia: can kill you
Hyperglycemia: DKA, increase fluid loss, dehydration

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6
Q

Rapid acting and long acting insulins have a Lower risk of hypoglycemia versus what?

A

Regular human insulin and NPH

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7
Q

Slow acting/long duration insulin

A

Modified chain of amino acids of human insulin

  • huddle after SQ for a long time and are released slowly over time into blood
  • onset slow
  • duration: up to 24hrs
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8
Q

Lispro (humalog)
Aspart (novalog)
Glusine (apidra)

A

Rapid acting short duration insulin

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9
Q

Detemir (levimir)

Glargine (lantus)

A

Slow acting long duration insulin

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10
Q

NPH

A

Suspension in injected liquid- NO IV only SQ

  • available for aspart and lispro
  • 2% ⬇️ in Hba1c levels with insulin
  • ⬆️ risk of hypoglycemia
  • must be gently mixed
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11
Q

What kind of insulin can be given IV or mixed with other insulin?

A

Short duration/rapid acting

  • when mixing draw short duration first
  • lispro, aspart, glusine
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12
Q

Insulin: rapid acting/short duration

A

Modified chain of amino acids of human insulin

  • rapid onset shirt duration (3-5 HR)
  • no huddle after SQ-straight to blood stream
  • preferred over regular/human insulin bc of fast onset and lower risk of hypoglycemia
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13
Q

Non insulin drug therapy

A

-1% Hba1c levels
All similiar in effectiveness
Duration varies by drug
*none of these are shown to have positive effects on macrovascular outcomes

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14
Q 
Metformin (glucophage) 
Sulfonylures
Meitinides
Thiazolineadiones TZDs 
Alpha-glucoside inhibitors 
SGLT2 inhibitors 
GLP analogs
DPP-IV inhibitors 
Pramlintide (symlin)
A

Non-insulin diabetic therapy

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15
Q

Metformin (glucophage)

MOA

A

⬇️ hepatic glucose production, ⬇️ intestinal glucose absorption: sensitizes target cells to insulin
*stops gluconeogenesis and glycogenolysis

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16
Q

Metformin (glucophage)

MOA

A

⬇️ hepatic glucose production, ⬇️ intestinal glucose absorption: sensitizes target cells to insulin

  • stops gluconeogenesis and glycogenolysis
  • superior to sulfonylureas: low risk of heart attack, no weight gain, improved lipids
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17
Q

Metformin (glucophage)

Adverse effects

A 
Stinky 
Lactic acidosis- lower risk: high with phenformin-low with metformin 
* renal dysfunction- do not give!!
Diarrhea 
Anorexia 
Dyspepsia 
*B12 folate deficiency
-GI low absorption
18
Q

Metformin (glucophage)

Inx

A

*Cimetidine: H2 receptor antagonist

19
Q

Sulfonylureas -“ide”

MOA

A

Indirectly ⬆️ insulin release/levels
Long duration
-two generations (1 old, 2 new)

20
Q

Sulfonylureas

Adverse effects

A 
* hypoglycemia 
Impaired B-cell fxn 
* cardiovascular toxicity- ⬆️ heart attack risk 
Weight gain 
Increase BP
* risk of disulfiram rxn
21
Q

Sulfonylureas

Disulfiram rxn

A

Disulfiram (anabuse): anti alcoholic drug
Makes body intolerant to alcohol
*mimic disulfiram with OLD sulfonylureas
-N/V
-sweating
-severely sick

22
Q 
Tolbutamide (orinase) 
Acetohexamide (dymelor)
Tolazamide (tolinase) 
Chlorpropamide (diabinese) 
* old- 1st generation 
Glipizide (glucotrol, glucotrol XL) 
Glyburide 
-nonmicronized (diabeta, micronase)
-micronized (glynase prestab) 
Glimepride (amaryl) 
* second generation-new
A

Sulfonylureas

23
Q

Meglitinides (new)

MOA

A

Promote insulin release- control postprandial hyperglycemia

  • short duration (1-4 HR)
  • dosed 30 min prior to meal (few times a day)
  • cannot skip meals!!!!
24
Q

Meglitinides

Adverse effects

A
  • hypoglycemia

- many drug inx risks

25
Q

Repaglinide (prandin)

Nateglinide ( starlix)

A

Meglitinides

26
Q

Thiazolidinediones-2

A

MOA- decrease insulin sensitivity
-almost never used
AE: fluid retention, edema, weight gain

27
Q

1) Pioglitazone (actos)

2) Rosiglitazone (arandia)

A

Thiazolidinediones

1) worsens HF, 2012 bladder cancer
2) MI, cardiovascular related deaths, DC in 2010

28
Q

Alpha Glucosidase inhibitors-2

MOA

A

Reduce post prandial rise in glucose
Delays carb absorbtion
* prevent gut from breaking down big sugars into small Sugars
Absorb sugar slowly-delayed
-given at start of a meal
* do not use oral sucrose for treatment of hypoglycemia-use glucose

29
Q

Alpha Glucoside inhibitors

AE

A 
Flatulence 
Cramps 
Bloating 
Constipation 
* hepatic dysfunction with long term use
30
Q

Acarbose (precose)

Miglitol (glyset)

A

Alpha Glucoside inhibitors

31
Q

Sodium glucose cotransporter 2 inhibitors
(SGLT2)
-“flozin”
MOA

A

Increase urinary excretion of glucose; blocks kidneys ability to reabsorb filtered glucose
* blocks SGLT2 pump= pee out glucose = lower blood sugar

  • newest class
  • favorable on wt and BP
  • BS of 150-180= kidney cannot filter anymore sugar conc too high
32
Q

SGLT2 inhibitors

AE

A 
High risk of UTI
High risk of vaginal yeast infections 
Hypotension 
Orthostatic hypotension 
Low BP 
Dehydration 
* will not work if renal fxn is impaired 
-not reccomeneded for PTs with renal dysfunction
33
Q

Drugs working via incretins

1) GLP-1 analogs
2) DPP-IV inhibitors

A

Hormones that are released from the GI tract for gastric emptying, glucose absorbtion, tells pancreas how quickly to make insulin

34
Q

GLP-1 analogs
Incretins
MOA

A

Stimulate insulin release in a glucose dependent manner
Act like GLP
* injectable
-⬆️ satiety and ⬇️ food intake: weight loss or neutral effect on WT
Preserve B cell fxn
* control post prandial glucose concentration: ⬇️ glucagon ⬆️ insulin

35
Q

DPP-IV inhibitors -“gliptin”
Incretins
MOA

A

Stimulate insulin release in a glucose dependent manner
* slows down the breakdown of GLP1 and GIP
* effectiveness is half of GLP analogs (less potent)
* PO 1x a day
-well tolerated
-⬆️ satiety and ⬇️ food intake: weight loss or neutral effect on WT
Preserve B cell fxn
* control post prandial glucose concentration: ⬇️ glucagon ⬆️ insulin

36
Q

GLP-1 analogs

AE

A 
N/V 
Diarrhea 
Caution with some orally admin drugs 
* acute pancreatitis 
Low risk of hypoglycemia when used with a sulfonylureas
37
Q

DPP-IV inhibitors

AE

A

Low risk of hypoglycemia
Low risk of GI effects
Low risk regarding pancreatitis
-theoretical concerns regarding cancer

38
Q

Exenatide (byetta): avoid in severe renal dysfunction

Liraglutide (victoza)
Albiglutide (tanzem)
Dulaglutide (triulicity)

A

GLP-1 analogs

Incretins

39
Q

Sitagliptin (januvia)
Saxagliptin (anglyza): high drug inx risk
Linagliptin (trajenta): not sensitive to renal fxn
Alogliptin (nesina)
* all available in combo with metformin

A

DPP-IV inhibitors

Incretins

40
Q

GLP1 analogs and DPP-IV inhibitors

A 
Low risk of hypoglycemia 
Slows the rate of gastric emptying 
Increase satiety 
N/V 
Impairs body ability to absorb other drugs
41
Q

Pramlintide (symlin)

A

An amylin mimetic- pancreas

  • lowers postprandial glucagon
  • slows gastric emptying- increase satiety
  • can be used for type 1 and type 2 DM
  • dosed prior to meals
  • SQ injection
  • acts like a GLP-1: decreases GI absorbtion of glucose
  • may increase insulin related hypoglycemia
  • caution with drugs that slows down gastric emptying
42
Q

Canagliglozin (invokana)
Dapagliflozin (farxiga)
Empagliflozin (jardiance)

A

SLGT2 inhibitors

Pharmacology Part 2 (16 decks)

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