1what is the rate limiting step of PNS neurotransmission
uptake of choline into nerve terminal
2what makes ACh
choline acetyltransferase
3what degrades ACh
acetylcholinesterase
4muscarinic cholinergic recep subtypes
m1 - cns
m2 - heart
m3 - sm m, glands
5direct muscarinic recep agonists: tx uses
glaucoma
diagnostic
urinary retention or bladder atony
reverse GIT depression/paralytic ileus
xerostomia
6direct muscarinic recep agonist: sfx
bradycardia
hypotension
sweating
dizzy
headache
if poisoning, DUMBBELS/full cholinergic poisoning
7direct musc agonist: ach
has muscarinic/nicotinic action
musc at low dose
8direct musc agonist: methacholine
musc >> nico
relatively resistant to ACh-esterase, so last longer
tx: diagnostic for bronchial asthma; if pt has hyper reactive airway, will have bronchial sm m contr
sfx: bradycardia, hypotension
9direct musc agonist: bethanechol
no nico action
completely resistant to AChE
tx: urinary retention, activation of AChM in bladder > sm m contr > urination
off label > tx xerostomia by stim salivate
oral or sc only! IM/IV=bradycardia
sfx: bradycardia, hypotension
contraind: asthma pt
10direct musc agonist: carbachol
musc > nico
complete resist to AChE
tx: topical use reduces intraocular pressure in wide angle glaucoma (sm m contr lining schlemm canals, more aq humor)
11direct musc agonist: cevimiline
muscarinic receptor subtype selective
can dec adverse cardiac fx
tx: xerostomia
contraind: complete loss of gland func
12glaucoma can be tx in what ways
muscarinic agonist: inc outflow (carbachol)
beta blocker: dec secretion (timolol)
prostaglandin
13amanita mushroom contains what that is deadly
muscarine
14cholinergic toxicity
xs stim of muscarinic receps
happens with mushrooms or OD
15cholinergic toxicity symptoms
SLUDGE
salivation
lacrimation
urination
diarrhea
GI upset
emesis(vomit)
can also get Bronchoconstriction/Bronchorrea (↑mucus), bradycardia
16reversible AChE inhibitors (indirect muscarinic agonist)
physostigmine
neostigmine
donepezil
17physostigmine
reversible AChE inhibitor
cross BBB > CNS activity
tx: WAglaucoma, anticholinergic poisoning
18neostigmine
reversible AChE inhibitor
no CNS activity
tx: post op urinary retention, myasthenia gravis
19donepezil
reversible AChE inhibitor
CNS activity
tx: alzheimers
20reversible AChE inhibitor toxicity
same as muscarine; tx with atropine
21irreversible AChE inhibitors
very toxic!
organophosphates insecticides
organophosphates nerve agents
sfx: DUMBBELS and hyper/hypotension, NMJ paralysis (nicotinic sfx too since ACh presence too much)
22irreversible AChE inhibitor examples
DFP, Isoflurophate, Malathion, Parathion, Nerve gases
23tx irreversible AChE toxicity
atropine
mechanical ventilation if NMJ paralysis
2-PAM