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;
131 Cards in this Set
- Front
- Back
- 3rd side (hint)
two types of cholinomimetic drugs - mode of action
|
direct-acting -bind M2,M3receptors
indirect-acting-inhibit acetylcholinesterase (anti) |
|
|
acetylcholinesterase
|
enzyme that rapidly degrades Acetylcholine in the synaptic cleft at the NMJ
|
|
|
indirect acting - mode of action
|
anti-cholinesterase
inhibit the enzyme reversibly and irreversibly |
|
|
direct acting cholinomimetics MODE OF ACTION
|
receptor agonists - bind to and activate muscarine M2,M3 receptors
|
|
|
direct acting drugs of choline esters
|
Ach (miochol)
bethanechol carbachol methacholine |
|
|
direct acting drugs -
alkaloids |
muscarine (M)
pilocarpine (M) nictotine (N) |
|
|
memory trigger for choline ester
|
beth, meth, carb and Ach all went to see cholinester
|
|
|
memory trigger for alkaloids
|
nic piled in his muscarine and vroomed away
|
|
|
indirect acting drugs cholinomimetics
|
anti-cholinesterases
antagonists |
|
|
reversible indirect-acting
|
Tensilolon (edrophonium)
|
|
|
reversible indirect-acting
carbamates (4) |
demacarium
neostigmine physiostigmine pyridostigmine |
|
|
reversible indirect-acting drugs for Alzheimers disease
|
donepezil
galantamine |
|
|
memory trigger for the AD drugs
|
she's a DONE GAL
|
|
|
IRreversible indirect-acting anticholinesterases
--Organophosphates |
echothiphate (phospholine)
Malathion parathion soman |
|
|
memory trigger
- think military call-out |
echo, mala, para, soma
|
|
|
what are the two main types of Glaucoma?
|
acute narrow angle
chronic open (wide) angle |
|
|
what issues do these glaucomas create?
|
both increase intra-occular fluid pressure
|
|
|
how is aqueous humor produced?
|
by the ciliary body behind the peripheral edge of the iris
|
|
|
where does this aqueus humor flow?
|
medially to the posterior chamber, then anteriorly to the anterior chamber
|
|
|
describe flow pattern
|
medially toward pupil in space b/t back of iris and front of the lens, then fwd thru pupil, to speace b/t front of iris and back of cornea
|
|
|
what is the function of the aqueous humor?
|
nourish the lens of the eye
|
|
|
what happens if it does not exit the anterior chamber?
|
fluid pressure builds up and causes the riris to bulge forward creating a "narrow angle"
|
|
|
what happens when the aqueous humor does exit the anterior chamber?
|
it is absorbed by a network of trabeculae and drained into a conjunctival vein
|
|
|
what is the name of the conjunctival vein?
|
the canal of schlemm
(sinus venosus sclerae) |
|
|
where is this "angle" of the eye located?
|
where the back of the cornea meets the front peripheral edge of the iris - and is usually wide and 'open'
|
|
|
what is a narrow angle?
|
when the irish bulges
|
|
|
how is a narrow angle detected?
|
by shining a penlight from the lateral side of the eye across the front
|
|
|
what is present when detecting the angle?
|
the bulging iris casts a shadow on the medial side of anterior chamber
|
|
|
what is the risk of a narrow angle?
|
rapid build up of fluid pressure if the pupil becomes significantly dilated
|
|
|
what issue is created by this risk?
|
as the iris contracts radially it can cause acute obstruction of fluid outflow and rapid increase in intra-ocular pressure
|
|
|
what causes significant eye dilation?
|
dark places (movie theater)
stress drugs used in eye exams pre-op atropine antidepressants nebulized brhochodilators (B2 agnosists) |
|
|
how does stress affect dilation?
|
increased EPI secretion and sympathetic tone
|
|
|
what drugs are used during eye exam to cause dilation?
|
mydriatic drugs - mydriacyl (topicamide)
cyclogyl (cyclopentolate) |
|
|
Mydriasis
|
dilated eyes
|
|
|
why is pre-op atropine an issue?
|
it is an anti-cholinergic drug
|
|
|
why do antidepressants affect dilation?
|
anticholinergic effects
|
|
|
how do nebulized bronchodilators dilate the eye?
|
these Beta 2 agonists cross react with Alpha1 receptors of radial muscle of iris
|
|
|
what are negative effects of long-term dilation?
|
*acute eye pain
*blurred vision *see halos around light *nausea/abd pain *conjunctivitis *stamy cornea *dilated pupil that is unreactive to light *permanent vision loss 2-5 days |
|
|
T/F acute narrow angle glaucoma is a medical emergency?
|
TRUE - must treat immediately by reducing the pressure - by re-constricting the puil and reopening the angle
|
|
|
what drug treatment is used to treat narrow angle glaucoma?
|
muscarinic agonist combined with anticholinesterases
|
|
|
what is the effect of the general treatment?
|
cause ciliary muscle contraction, stretching the trabeculae, allowing for draining of fluid
|
|
|
what muscarinic agonists are used?
|
pilocarpine drops or carbachol drops
|
|
|
what anticholinesterases are used to treat narrow angle?
|
physostigmine - opth. ointmnt
echothiophate drops demecarium drops |
|
|
what other drugs are used to decrease fluid pressure?
|
carbonic anhydrase inhibitors
Acetazolamide brinzolamide |
|
|
why are carbonic anhydrase inhibitors used?
|
to decrease the fluid production
|
|
|
what is the effect of prostaglandins?
|
increase drainage of aqueous humor
|
|
|
what prostaglandins are used?
|
Lumigen (bimatroprost)
rescula (unoprostone) |
|
|
does surgical treatment work?
|
Yes - laser peripheral iridotomy is a permanent cure
|
|
|
describe Chronic open angle glaucoma
|
simple, wide angle glaucoma - with increased intra-ocular pressure doe to inadequate drainage of trabeculae
|
|
|
is this a true angle problem>
|
no, it is an issue of inadequate drainage
|
|
|
what is the etiology?
|
unknown - idiopathic, could be familial or cx by diabetes
|
|
|
what secondary events could cause chronic open glaucoma?
|
uveitis or trauma
|
|
|
which glaucoma is considered to be bilateral?
|
chronic open angle
|
|
|
is surgical treatment a viable option for chronic open angle?
|
typically no, but laser trabeculopplasty may come into play on some
|
|
|
what is the recommendation for drug treatment for chronic glaucoma? (timeframe)
|
long term is required using alpha-agonists, beta-blockers, caronic anyhdrase inhibitors and prostaglandins
|
|
|
how do cholinomimetics work to treat COG?
|
enhance drainage of fluid by contracting ciliary muscles and stretching trabeculae
|
|
|
what cholinomimetic drugs are used?
|
muscarinic agonists
*pilocarpine, carbachol anti-cholinesterase -physostigmine |
|
|
what carbonic anhydrase inhibitors are used?
|
acetazolamide
brinzolamide |
|
|
what alpha agonists are used?
|
nonselective =EPI, and propine
alpha2 = iopidine & alphagan |
|
|
what affect do the alpha agonists have?
|
non-selective
**INCREASE DRAINAGE selective alpha 2 **DECREASE humor PRODUCTION |
|
|
What beta blockers are used?
|
betaxolol (betoptic)
timolol(timoptic, betomil) |
|
|
what is the function of beta blockers for this?
|
DEcrease humor production
|
|
|
what drugs decrease humor production?
|
*beta blockers betoptic, betomil, timoptic
*aplha2 agonists-iopidine, brimonidine |
iopen my brim , and tim and beto bet-om-il at the casino
|
|
what cholinomimetics are used to counteract GI and UT smooth muscle activity depression?
|
muscarinic agonist
*bethanechol (uricholine) indrect-acting (anti-cholins.) *neostigmine |
|
|
what is Post-Op Ileus?
|
atony or paralysis of stomach or bowel after surgery
|
|
|
depressed muslce activity causing urinary retention occurs from?
|
*post-op
*postpartum *after spinal cord injury/disease "neurogenic bladder" |
|
|
reflux esophagitis (GERD) is treated with?
|
H2 blockers, bethanechol, neostigmine
|
|
|
What is used to treat DRY MOUTH cx by sjorgren's syndrom or other sicca syndromes?
|
muscarinic agonist -
cevimiline (Evoxac) |
|
|
what is the relationship b/t Myesthenias gravis and receptors?
|
Ab-mediated reduction in the # of FX nicotinic Nm receptors of NMJ
|
|
|
what is used to treat MG for this?
|
ONLY indirect-acting anticholinesterases
-pyridostigmine -neostigmine -ambenomium demercarium LONG TERM |
|
|
how is MG diagnosed?
|
by giving Tensilon to pt - will see decreased fatigue w/in 5 min,
|
|
|
how is Tensilon used regarding MG?
|
diagnosis
assess level of longterm tx with anitcholinesterases |
|
|
what is the result of overmedicating the pt?
|
depolarizing blockade and excessive stimulation of muscarinic receptors
|
|
|
what are the signs of an overmedicated pt?
|
miosis
bradycardia excessive salivation and bronchial secretions abd pain cramps and diarrhea |
|
|
how do you know if pt is over or under medicated?
|
by giving Tensilon -
if weakness does not improve - overmedicatd if weakness does improve - undermedicated |
|
|
are cholinomimetics useful in treating Alzheimer's Disease?
|
NO - but people use as a last hope and some results have been positive SHORT TERM
|
|
|
What cholinomimetics are prescribed for AD?
|
anticholinesterases
-donepezil -galantamine |
|
|
T/F AD is the result of too little Ach due to a reduction of brain neurons?
|
TRUE
|
|
|
what is the action of anesthetics during surgery?
|
neuromuscular blockade - imposing dysfunction of the motor endplate - cx muscle paralysis via NT dysfunction at NMJ
|
|
|
what drugs are used to impose this skeletal muscle paralysis? (general class)
|
anti-cholinergics
deoplarizing and nonpolarizing |
|
|
what depolarizing drugs are used?
|
succinylcholine
|
|
|
what nonpolarizing drugs are used?
|
curare
attracurium pipecuronium pancuronium vecuronium (remember 3 curoniums) |
|
|
trigger- who are the 3 curonium brothers and their sister?
|
pipe, panc, vec and sister curare
|
|
|
which anti-cholinergic class is used most frequently and what is its action?
|
non-depolarizing - they block the Nm receptors by competing w/ Ach, thereby preventing depolarization of muscle fiber membrane
|
|
|
T/F the muscle paralysis induced by these drugs is caused by upper/lower motor neuron dysfunction?
|
FALSE - it is from neurotransmitter dysfunction at the NMJ
|
|
|
what drug class is used to reverse this process?
|
anti-cholinesterases- aimed at increasing amount of Ach (and icreasing half-life) at the motor end plate
|
|
|
what are these drugs?
|
neostigmine
pyridostigmine Tensilon |
|
|
what ailments are cholinomimetics used for?
|
acute narrow angle glaucoma
chronic wide angle glaucoma GI and UT activity depression Alzheimer's Disease Dry mouth Myasthenias Gravis reversal of surgical NM block antidotes for insecticides and humanocides |
|
|
What does DUMBELS represent?
( OR...DUMB3ELS) |
Diarrhea
Urination Miosis Bronchorrhea Bronchospasm Bradycardia Excitation (anxiety, fasciculation, seizures) Lacrimation Salivation |
|
|
what is the other name for cholinomimetics?
|
parasympathomimetics
or cholinoreceptor activating drugs |
|
|
what is the action of insecticides?
|
organophosphates kill via irreversible anticholinesterase activity-causing excessive parasympathetic activity-
|
|
|
what parasympathetic activity is induced from ingestion of insecticides?
|
vegetative manifestations:
miosis salivation hyperactive bowel sounds lethargy bradycardia (muscarinic axn) or tachycardia (nicotinic axn) |
|
|
death can occur from?
|
respiratory depression - you can NOT take IN another breath
|
|
|
what is the mnemonic used to describe the effects of insecticides?
|
DUMBELS
|
|
|
what does DUMBELS stand for?
|
Diarrhea
Urination Miosis Bronchorrhea Bronchospasm Bradycardia Excitation: anx,fasciulations, seizures Lacrimation Salivation |
|
|
what are the antidotes for DUMBELS?
|
Atropine
pralidoxime(Protopam 2-PAM) |
|
|
what is the action of Atropine?
|
competitive muscarinic receptor blocker
M1,2,3 etc. _reduces symptoms, may need repeated doses |
|
|
what is the action of Pralidoxime? (protopam, 2pam)
|
competitively INHIBIT binding of organophosphates to acetylcholinesterase
(2-PAM carried by military personnel) |
|
|
carbachol
|
cholinomimetic direct acting choline ester
Tx: narrow angle glaucoma fx: M + N, resistant to AchE, |
|
|
Acetylcholine
|
cholinomimetic direct-acting
M+N shortest duration |
|
|
Bethanechol
|
cholinomimetic direct-acting
Fx: Muscarinic resistant to AchE, TX: stimulates post op bladder and GI |
|
|
Pilocarpine
|
Cholinomimetic direct-acting alkyloid
Fx: M Tx: glaucoma, narrow angle and chronic wide |
|
|
cevimeline (Evoxac)
|
cholinomimetic direct-acting
fx: M tx: dry mouth from Sjogrens or sicca syndrome |
|
|
nicotine
|
cholinomimetic direct-acting
Alkaloid Fx: nicotinic receptor |
|
|
endrophonium (Tensilon)
|
anticholinesterase
indirect-acting -reversible FX: M+N Tx: diagnostic test for myasthnia gravis reversal of surgical NM blockade |
|
|
demecarium (Humorsol)
|
Indirect-anticholinesterase
a carbamate Fx: inhibit, reversible Tx: Myastehnias Gravis wide angle glaucoma |
|
|
neostigmine
|
indirect-anticholinesterase - carbamate
Fx: inhibit, reversible tx: myasthenias gravis GI, GERD, UT post-op reversal of surgical blockade |
|
|
physostigmine
|
cholinomimetic indirect-acting
Fx: M+N carbamate=reversible Tx: glaucoma |
|
|
echothiophate
|
indirect-acting M+N organophosphate
=irreversible Tx: glaucoma |
|
|
parathion
|
indirect-acting M+N irreversible organophosphate
longest lasting=most toxic |
|
|
atropine
|
antidote for organophosphate insecticides
Fx: blocks M1,2,3 etc no effect on nicotinic |
|
|
curare,atracurium,pipecuronium,pancuronium, vecuronium
|
non-polarizing anti-cholinergic drugs used for surgical NM blockade
|
block Nm on muscle fibers by competing with Ach and prevent depolarization
|
|
succinylcholine
|
depolarizing anti-cholinergic drug used for reversal of surgical NM blockade
|
|
|
what anticholinesterases are used for reversal of NM blockade post surgery?
|
neostigmine
pyridostigmine Tensilon "PEN" |
I will wave my magic "PEN" to wake you up
|
|
pralidoxime (Protopam, 2PAM)
|
used by military and in hospitals to counteract DUMBELS poisoning
Fx: inhibitrs binding of organophosphates to acetylcholinesterase |
|
|
what drugs decrease aqueous humor production?
|
alpha 2 agonists
aproclinidine (Iopidine) brimonidine (Alphagan) |
|
|
what drugs increase drainage of aqueous fluid to trabeculae?
|
non-selective alpha agonists=
EPI, Propine Prostaglandins = Lumigan, Rescula |
|
|
what drugs decrease aqueous humor production?
|
beta blockers=
Betoptic, Timoptic,Betimol carbonic anyhdrase inhibitors = Diamox, Azopt |
|
|
memory trigger for beta blockers
|
Tim and Beto Bet-im-ol at the casino, and you beta their wives blocked their receptors
|
|
|
treatment of myasthenias Gravis can include one of the following
|
indirect -anticholinesterases
reversible pyridostigmine neostigmine ambenonium(Mytelase) demercarium (Humorsol) |
|
|
Donepezil (Aricpet)
|
anticholinesterase -indirect, reversible
Tx: alzheimer disease |
|
|
neurogenic bladder tx
|
treat with cholinomimetic
M =bethanechol (urecholine) anti-ChE=neostigmine (prostigmin) |
|
|
memory trigger
neurogenic bladder and urecholine |
when you 'gotta go'
ur-e-choline for the drugs to help you out |
|
|
Mytelase
|
generic for ambenonium for tx of MG
|
|
|
Humorsol
|
generic for demecarium
tx for MG, wide angle glaucoma (drops) |
|
|
trigger for increased draining of aqueous humor
|
ED, please RESCULA my LUMIGAN, I AZOPT it in the DIAMOX drain and it is full o PCP's
p=pilocarpine, C-carbachol p=physostigmine ED = epi, diivefrin |
|
|
trigger for decreased humor production (tx for glaucoma)
|
no humor until you do your ABC's
alpha 2 agonists, beta blockers, carbonic anhydrase inhibitors |
|
|
memory trigger ro decreased humor productionn - specific drug names used
|
IOPIDINE THE BRIMONIDINE, BETA clean my diamox beore I azopt for the night.
|
|
|
CAIs
|
acetazolamide (diamox)
brinzolamide (Azopt) |
|
|
memory trigger for GI, UT, GERD
|
when those go crazy - some people smell like "P U" .
|
|
|
my mouth is dry, bring me some
|
cevimiline
|
|