Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
52 Cards in this Set
- Front
- Back
|
physostigmine
|
reversible ACHE inhibitor
|
|
|
pyridostigmine
|
reversible ACHE inhibitor
|
|
|
neostigmine
|
reversible ACHE inhibitor
|
|
|
what is unique about physostigmine
|
activity is pH dependent
because it requires a change in pH to protonate one of its nitrogens thereby allowing it to bind to the enzyme (anionic site) can cross BBB |
|
|
what is unique about pyridostigmine and neostigmine
|
they are not pH dependent because they already have a positive charge
they can't cross the BBB and are poorly absorbed in GI because they are quartenary ammonium salts |
|
|
what are the properties of Edrophonium
|
non classical ACHE inhibitor
short duration because it only binds to the anionic site of the enzyme |
|
|
what is edrophonium mainly used for
|
diagnostic purposes not treatment
|
|
|
tacrine
|
reversible AChE for treatment of alzheimers
|
|
|
donepezil
|
reversible AChE for treatment of alzheimers
non classical |
|
|
rivastigmine
|
reversible AChE for treatment of alzheimers
carbomylated reversible inhibitor |
|
|
galantamine
|
reversible AChE for treatment of alzheimers
non classical |
|
|
what are the organophosphates for chem war fare
|
sarin
tabun soman vx |
|
|
malathion
|
organophosphates used as insecticides
|
|
|
parathion
|
organophosphates used as insecticides
|
|
|
paraoxon
|
organophosphates used as insecticides
|
|
|
schradon
|
organophosphates used as insecticides
|
|
|
dichlorfenthion
|
organophosphates used as insecticides
|
|
|
chlorpyrifos
|
organophosphates used as insecticides
|
|
|
what can be used to reactivate phosphorylated AChE
|
hydroxylamine
oxime hydroxamic acid can't be used clinically cause doses required to hydrolyze the phosphate esters are toxic |
|
|
what is the agent of choice for reactivation of AChE
|
2 PAM
|
|
|
how is 2 PAM GIVEN
|
usually given w/ atropine which blocks the symptoms while 2 PAM reactivates the AChE
|
|
|
what does atropine do
|
competes w/ ACh to bind to the same Rc
since its bulky it will bind to other parts of the enzyme that ACh won't carbonyl same distance away from nitrogen as in ACh muscarinic antagonist soluble only as salt selective for M1,2,3, |
|
|
what forms of calcium are water soluble
|
lactate, acetate, chloride, gluconate
|
|
|
what does 1,25 D3 do
|
it is inactive and suppresses PTH secretions
|
|
|
what does teripeptide do
|
functions as PTH
|
|
|
under what conditions do osteoclast break down hydroxyapetite
|
acidic
|
|
|
what do osteocytes do
|
calcium mobilization
found in bone |
|
|
what does estrogen do
|
increase ca absorption
inhibit osteoclast increase Vit D Rc on osteoclast promote calcitonin biosynthesis |
|
|
why is estrogen replacement therapy not used
|
because those drugs are non selective binding for estrogen Rc in breast and uterus and can increase risk of cancer
|
|
|
why is estradiol more potent than estrone
|
b/c estrone is in a oxidized state
|
|
|
what are the serms
|
raloxifine
tamoxifine |
|
|
what are the properties of raloxifine
|
similar structure to estradiol
agonist in bone antagonist in breast mimics estrogen except for uterus and breast growth |
|
|
what do bisphosphonates do
|
don't help build new bone just fill in holes that have been eaten by osteoclast
decrease osteoclast activity decrease osteoclast life span (promote apoptosis) decrease bone resorption |
|
|
why was the O replaced in pyrophosphate to make bisphosphate
|
this was done because the O in pyrophosphate gets hydrolized causing the compound to break up and become inactive
|
|
|
what are the properties of etidronate
|
1st gen bisphosphonate
treats pagets disease only |
|
|
what are the properties of Zoledronic acid
|
not water soluble therefore given in basic media so it forms a salt which is water soluble
|
|
|
what is the order of potency of the bisphosphonates
|
etidronate < adendronate < risedronate < ibandronate <zoladronic acid
|
|
|
what does risdronate treat
|
pagets or osteoporosis
|
|
|
what may decrease cancer metastasis in bone
|
zoledronic acid
|
|
|
what drugs can be given to treat hypercalcemia of malignancy
|
zoledronic acid and pamidronate disodium
|
|
|
what kind of calcitonin is used and why
|
salmon because 50x more potent than human and has longer halflife and duration of action
|
|
|
what does calcitonin do
|
inhibits osteoclast
|
|
|
what are the drug therapy choices for osteoporosis
|
SERM (raloxifine, tamoxifine)
estrogen replacement therapy (ERT) bisphosphonates (etidronate, adendronate, risedronate, ibandronate, zoledromic acid) calcitonin |
|
|
what are the bone forming agents
|
teripeptide
calcium salts sodium fluoride |
|
|
what does teriparatide do and how is it administered
|
increase osteoblast
administered w/ calcium and vit d |
|
|
what does sodium fluoride do
|
increase osteoblast
increase osteoblast activity inhibit osteoclast activity |
|
|
what all inhibits osteoclast activity
|
sodium fluoride
bisphosphonates calcitonin estrogen |
|
|
what does RankL do
|
transmembrane protein that normally:
improves formation of osteoclasts improves function of osteoclasts improves survival of osteoclasts |
|
|
what are the RankL inhibitors
|
Demosumab
Osteoprotegrin |
|
|
how does Demosumab work
|
decrease bone resorption
increase bone mass strength inhibits Rank L |
|
|
what has human IgG2 monoclonal activity
|
demosumab
|
|
|
what does osteoprotegrin do
|
inhibits Rank L but can also be inhibited by OSTEOCLAST
|
