Bisphosphonates and Diabetic Agents Flashcards by Abby Davis

what are bisphosphonates used for

used for osteoporosis

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pharmacology of bisphosphonates

what is it used for

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

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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what are the medications that fall under bisphosphonates class

alendronate (fosamax)
risedronate (actonel)
boniva - may not ask about this one

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alendronate (fosamax)

bisphosphonate drug

most commonly used for treatment of osteoporosis
daily/weekly dosing

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risedronate (actonel)

bisphosphonate drug

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what are the bisphosphonates side effects

GI !!!!!
- nausea
- reflux
- lower GI
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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forms of dispensing of diabetic agents

injecting pen
injecting syringe
insulin pump

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normal control of glucose

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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type 2 diabetes control of glucose

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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what secretes insulin and what type of receptor does insulin bind

what does it cause

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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what are the effects of insulin

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

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how is insulin divided/categorized

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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where is insulin metabolized if we eat it

gut

aka we dont have oral insulin

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how long does it take for rapid acting insulins to work

10-30 mins to work

3-5 hours lasts

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what are the rapid acting insulins

humalog (insulin lispro)
novolog (insulin aspart)

commonly put in insulin pump

can be mixed with NPH (intermed)

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what are the short acting insulins (regular insulins)

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

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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what are the intermediate acting insulins

how long to work/last

Humulin N (NPH)
Novolin N (NPH)

take 2-4 hours to work
last: 20 hours

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what are the long acting insulins

how long to work / last

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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what are the mixed insulin products

normally mixed with NPH

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

fraction= NPH % / other %

insulin is dosed in ___________ not ___________

insulin dosed in UNITS

not mg

insulin can be used in BOTH

type 1 and type 2 diabetes

what are analog insulins

mimic release of insulin seen after meals

fast acting short lasting

aka rapid acting one= insulin lispro= humalog

what are insulin pumps

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

what are oral sulfonylureas used for

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

what is the MOA of sulfonylureas

bind to extracellular receptors on beta cells in pancreas bind leads to intracellular change= expel insulin into blood stream NEVER USED IN TYPE I

what are sulfonylureas never used in but can be used to treat

type one diabetes can be used to treat type two

what are the oral sulfonylureas

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

what is a common side effect of oral sulfonylureas

they can cause hypoglycemia because can release too much insulin

what are biguanides

used to treat type two diabetes

MOA of biguanides

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

what is a common side effect of biguanides

diarrhea !!!!

how well are biguanides absorbed how are they excreted

absorbed - 50-60% = pretty well excreted unchanged in urine CANNOT BE USED IN PTS WITH IMPAIRED CREATININE CLEARANCE !!!!!!!!!!!!!! aka someone with impaired renal funciton

what is the only biguanide used in US

metformin (glucophage, XR) REMEBER GI SIDE EFFECTS common in combination prods

what are thiazolidinediones used for

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

what is the MOA of thiazolidinediones

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

what is the biggest benefit of thiazolidinediones and metformin

does not cause hypoglycemia

what are the two thiazolidinediones used in type 2 diabetes

pioglitazone (actos) | rosiglitazone (avandia)

what is a side effect of thiazolidinediones

can be hepatotoxic

glucagon like peptides (incretin mimetics) what are the drugs in this class

``` "tides" exenatide (byetta, byureon) dulaglutide (trulicitiy) liraglutide (victoza) lixisenatide ``` reduces appetite and increases insulin release

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

exenatide

what are glucagon like peptides (GLPs) good for

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

what are the side effects of GLPs

GI (5-10%- discontinue med) - nausea - vomit - diarrhea hypoglycemia - if with mixture with insulin CHF worsening possible pancreatitis

What are DPP4 inhibitors

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

what is the suffix common to DPP-4 inhibitors

"gliptin" ex: alogliptin the name helps remember what it does GLiPtIN = GLP INhibitor

what does SGLT2 stand for where is it found what does it do

sodium dependent glucose transporter kidney naturally helps reabsorb sugar

what are SGLT2 inhibitors/ what do they do

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

what are the drugs within SGLT2 inhibitors class

"Flozin" ex: canagliflozin

what are side effects of SGLT2 inhibitors

UTI because sugar allows bacteria to grow candidiasis - yeast infection diabetic ketoacidosis in some ppl - when lose too much sugar - not huge concern