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Pharmacology > Bisphosphonates and Diabetic Agents > Flashcards

Bisphosphonates and Diabetic Agents Flashcards

1
Q

what are bisphosphonates used for

A

used for osteoporosis

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2
Q

pharmacology of bisphosphonates

  • what is it used for
A

strongly bind bone and inhibit osteoclast activity (bone resorption) and in doing so increase bone mineral density

to prevent fracture

will begin using these when ppl have osteopenia as preventative measure
or paget’s disease

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3
Q

what is the absorption / distribution/ metabolism/ excretion of bisphosphonates

A
  • low % absorbed - take on empty stomach first thing in morning with large glass water and no laying down fr 30 mins (toxic to esophagus)!!!
  • nearly half absorbed accumulated in bone
  • excreted in urine

because it binds strongly to bone, TERMINAL HALF LIFE IS ABOUT 10 YEARS

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4
Q

what are the medications that fall under bisphosphonates class

A
  1. alendronate (fosamax)
  2. risedronate (actonel)
  3. boniva - may not ask about this one
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5
Q

alendronate (fosamax)

A

bisphosphonate drug

  • most commonly used for treatment of osteoporosis
  • daily/weekly dosing
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6
Q

risedronate (actonel)

A

bisphosphonate drug

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7
Q

what are the bisphosphonates side effects

A
  1. GI !!!!!
    - nausea
    - reflux
    - lower GI
  2. osteonecrosis-
    ex: dental procedure that breaks into bone can get osteonecrosis of jaw- tissue dies

-cancer/ fractures???
want someone on these for 5 years, after 5 years may not need to be continued
-this may prevent?

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8
Q

forms of dispensing of diabetic agents

A
  • injecting pen
  • injecting syringe
  • insulin pump
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9
Q

normal control of glucose

A

increased glucose levels= increase insulin to bring glucose in cells

natural spikes of insulin 3 times a day for healthy peopl

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10
Q

type 2 diabetes control of glucose

A

they start at healthy levels

overtime they develop glucose intolerance

  • fasting blood sugar increases
  • insulin production increases (more insulin needed to perform same duty as before)
  • aka insulin resistance increases

pre-diabetic= insulin resistance/glucose intolerance

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11
Q

what secretes insulin and what type of receptor does insulin bind

what does it cause

A

beta cells in pancreas secrete

binds to extracellular receptor

causes autophosphorylation of intracellular proteins= glucose uptake into cell

without insulin= cells are starving, blood sugar high

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12
Q

what are the effects of insulin

A
  1. help glucose enter muscle, adipose and other tissue
  2. stimulate liver to store glucose as glycogen- glycogenesis
  3. decrease blood glucose levels (blood sugar)
  4. promote syn of fatty acids in liver
  5. inhibit intracellular lipase !!!
    - too much insulin = cant break down fat= not losing weight
    - this with too much insulin
  6. increase aa entry into cells
  7. activate Na/K ATPases
    - aka can be used in hyperkalemia
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13
Q

how is insulin divided/categorized

A

based on its pharmacokinetics

  • rapid (type 1 diabetes person about to eat ice cream)
  • intermediate -(takes longer, but lasts longer)
  • long acting (can simulate basal metabolic rate of insulin secretion)
  • prolonged action if add zinc or protamine or fat molecules
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14
Q

where is insulin metabolized if we eat it

A

gut

aka we dont have oral insulin

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15
Q

how long does it take for rapid acting insulins to work

A

10-30 mins to work

3-5 hours lasts

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16
Q

what are the rapid acting insulins

A

humalog (insulin lispro)
novolog (insulin aspart)

commonly put in insulin pump

can be mixed with NPH (intermed)

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17
Q

what are the short acting insulins (regular insulins)

how long does it take them to work
how long do they last

A

short acting

  • Humulin R (regular) - stands for human insulin
  • novolin R (regular)

work in 30-60 mins
last 6-8 hours

available directly from pharmacist with out prescription (OTC) !!!!!!!!

  • good to educate pt on this for emergency use
  • commonly used in ED
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18
Q

what are the intermediate acting insulins

how long to work/last

A 
Humulin N (NPH)
Novolin N (NPH)

take 2-4 hours to work
last: 20 hours

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19
Q

what are the long acting insulins

how long to work / last

A

Lantus (insulin glargine)
levemir (insulin detemir)

take hours to work and 24 hours it lasts

mimic the basal rate of normal insulin secretion !!!

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20
Q

what are the mixed insulin products

A

normally mixed with NPH

  • Humalog mix 75/25, 50/50
  • humulin 70/30
  • novolin 70/30

fraction= NPH % / other %

21
Q

insulin is dosed in ___________ not ___________

A

insulin dosed in UNITS

not mg

22
Q

insulin can be used in BOTH

A

type 1 and type 2 diabetes

23
Q

what are analog insulins

A

mimic release of insulin seen after meals

fast acting short lasting

aka rapid acting one= insulin lispro= humalog

24
Q

what are insulin pumps

A

electronic devices about size of pager

have insulin cartridge release constant basal rate of insulin

pt can give self bolus based on amount of carbs going to eat

25
Q

what are oral sulfonylureas used for

A

used to treat type II diabetes by increasing insulin secreted by pancreas

26
Q

what is the MOA of sulfonylureas

A

bind to extracellular receptors on beta cells in pancreas

bind leads to intracellular change= expel insulin into blood stream

NEVER USED IN TYPE I

27
Q

what are sulfonylureas never used in

but can be used to treat

A

type one diabetes

can be used to treat type two

28
Q

what are the oral sulfonylureas

A

glipizide (glucotrol, and XL)
glyburide (diabeta, micronase)
glimepiride (amaryl)

29
Q

what is a common side effect of oral sulfonylureas

A

they can cause hypoglycemia because can release too much insulin

30
Q

what are biguanides

A

used to treat type two diabetes

31
Q

MOA of biguanides

A

decrease liver production of glucose

improves insulin sensitivity at receptor
(in type 2 diabetes they are still producing insulin, but not having the same affect so this helps with hyperglycemia)

can inhibit some glucose absorption at the gut by changing the gut flora

32
Q

what is a common side effect of biguanides

A

diarrhea !!!!

33
Q

how well are biguanides absorbed

how are they excreted

A

absorbed - 50-60% = pretty well

excreted unchanged in urine

CANNOT BE USED IN PTS WITH IMPAIRED CREATININE CLEARANCE !!!!!!!!!!!!!! aka someone with impaired renal funciton

34
Q

what is the only biguanide used in US

A

metformin (glucophage, XR)

REMEBER GI SIDE EFFECTS

common in combination prods

35
Q

what are thiazolidinediones used for

A

used to treat type 2 diabetes by improving insulin sensitivity in skeletal muscle/fat and inhibit hepatic gluconeogensis

36
Q

what is the MOA of thiazolidinediones

A

highly selective/potent agonist for intracellular peroxisome proliferators acivated receptor (PPAR-gamma)

activation regulates prod of insulin responsive genes involved in glucose prod, transport, utilization

IMPROVES GLYCEMIC CONTROL BY IMPROVING INSULIN SENSITIVITY IN SKELETAL MUSCLE/FAT AND INHIBITING HEPATIC GLUCONEOGENESIS
- liver no longer makes as much glucose= decrease blood sugar and increase insulin sens

37
Q

what is the biggest benefit of thiazolidinediones and metformin

A

does not cause hypoglycemia

38
Q

what are the two thiazolidinediones used in type 2 diabetes

A

pioglitazone (actos)

rosiglitazone (avandia)

39
Q

what is a side effect of thiazolidinediones

A

can be hepatotoxic

40
Q

glucagon like peptides (incretin mimetics)

what are the drugs in this class

A 
"tides" 
exenatide (byetta, byureon)
dulaglutide (trulicitiy)
liraglutide (victoza)
lixisenatide

reduces appetite and increases insulin release

41
Q

what drug came from saliva of the gila monster (lizard in arizona)

A

exenatide

42
Q

what are glucagon like peptides (GLPs) good for

A

good for diabetes- most potent- first line in replacing GLP bc GLP agonist

well spread effect around body

  • help prevent cardiovascular disease
  • help stop inflammation
  • help lose weight
  • increase insulin release
43
Q

what are the side effects of GLPs

A

GI (5-10%- discontinue med)

  • nausea
  • vomit
  • diarrhea

hypoglycemia - if with mixture with insulin

CHF worsening

possible pancreatitis

44
Q

What are DPP4 inhibitors

A

class of oral diabetes drugs

inhibit DPP-4 enzyme

DPP-4 enzyme breaks down glucagon like peptides (GLP-1)

inhibit this= increase natural GLP

  • aka the GLP agonsists replace GLP
  • these save the GLP

not as potent

45
Q

what is the suffix common to DPP-4 inhibitors

A

“gliptin”

ex: alogliptin

the name helps remember what it does
GLiPtIN = GLP INhibitor

46
Q

what does SGLT2 stand for

where is it found

what does it do

A

sodium dependent glucose transporter

kidney

naturally helps reabsorb sugar

47
Q

what are SGLT2 inhibitors/ what do they do

A

block reuptake of sugar, glucose urinated out

helps take strain OFF of kidney
-renal protective

also a diuretic (Water follows sugar)

good for type 2 diabetes and CHF
can help ppl lose weight

48
Q

what are the drugs within SGLT2 inhibitors class

A

“Flozin”

ex: canagliflozin

49
Q

what are side effects of SGLT2 inhibitors

A

UTI because sugar allows bacteria to grow

candidiasis - yeast infection

diabetic ketoacidosis in some ppl

  • when lose too much sugar
  • not huge concern

Pharmacology (13 decks)

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