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Cholinergic Activiating Agents
Pete
83
Medical
Graduate
07/21/2012

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Cards

Term
7 transmembrane domains
Definition
Muscarinic
Term
Only found in CNS
Definition
M4, M5
Term
Responsible for increased gland secretion (Salivary, gastric)
Definition
M1
Term
Responsible for Ganglionic potnetiation, slow EPSP
Definition
M1
Term
Stimulatory muscarinic receptors (Gq)
Definition
M1, M3, M5
Term
Inhibitory muscarinic receptors (Gi)
Definition
M2, M4
Term
Pertussis sensitive muscarinic receptor (inhibitory)
Definition
M2
Term
muscarinic receptor

increases secretion and contraction of smooth muscle
Definition
M3
Term
hyperpolarization through opening of K channels is important for which receptors (muscarinic)?
Definition
M2, M4
Term
PENTAMERIC
Definition
nicotinic
Term
ACH, Methacholine, bethanecol, carbachol
Definition
esters of choline
Term
muscarine, nicotine, pilocarpine
Definition
alkaloids
Term
All of these have a longer effect than Ach because they are not hydrolyzed as rapdily or at all
Definition
cholinergic agonists
Term
causes vasodilation and drop in BP
leads to reflex w/ tachycardia
Definition
low dose of Ach
Term
causes vasodilation and drop in BP
reflex tachycardia is over come: bradycardia
Definition
high dose of Ach
Term
no parasympathetic innervation of blood vessels, however circulating muscarinic agents can cause vasodilation due to what receptors on endothelial cells that stimulates production of EDRF (NO)
Definition
M3
Term
disease can remove endothelium from BV leading to what when muscarinic agonists hit em
Definition
vasoconstriction
Term
lungs: bronchoconstriction, increased seretion
Definition
M3
Term
contradicted in asthma patients
Definition
cholinergic agonists
Term
myenteric plexus receptor (^ activity)
Definition
M1
Term
increased peristalsis
smooth mm relaxation of sphincter
increases secretion
Definition
M3
Term
eccrine (thermogregulatory) are only sweat glands controlled by muscarinic what are receptors for em
Definition
M3, M2
Term
in cns involved in controlling voluntary movements
Definition
muscarinic
Term
in cns involved in regulating actions of other nT like dopamine
Definition
nicotinic
Term
eser of choline, slightly sensitive to achesterase
Definition
methacholine
Term
ester of choline; resistant to Acetylcholine esteras
Definition
Bethanecol, Carbachol
Term
contraindication my cause hypotension w/ choline ester
Definition
Coronary Artery disease
Term
contraindication may cuase increased gastric secretions w/ choline ester
Definition
Acid peptic disorders
Term
Contraindications to choline esters
Definition
Hyperthryoidism (atrial fib), asthma, CAD (hypotension), acid-peptic disorders (increases gastric secretions), obstructive urinary retention
Term
Only high IV doses lead to short term effects
Definition
Ach
Term
Ocular surgery: distilled to anterior chamber lasts 20 min
Definition
Ach
Term
Sweat spot test for autonomic neuropathy in diabetic patients (subdermal injection w/. iodine -> black spots)
Definition
Ach
Term
Inhalation to diagnose bronchial airway hypersensitivity
Definition
Methacholine
Term
Significant nicotinic activity (seen in prsence of atropine) Ester of choline
Definition
Carbachol
Term
limited to opthalmic applications (reduction in IOP) but severe side effects CV and GI (due to nicotinic activity also)
Definition
Carbachol
Term
No nicotinic acitivyt ester
Definition
Bethanechol
Term
emptying of bladder in cases of acute postoperative and postpartum NONOBSTRUCTIVE urinary retension
also hypotonic, myotonic, neurogenic bladder
Definition
Bethanechol
Term
orally or Subq injection ester
(only one given systemically!!!)
Definition
Bethanechol
Term
Which ester is most likely to produce systemic side effects
Definition
Bethanechol
Term
crosses BBB
longer acting than choline esters but less potent
Definition
Pilocarpine
Term
Very active on eye and sweat glands:
miosis and acommodation last 4-8 hrs
Definition
Pilocarpine
Term
Initial treatment for open angle glaucoma (contracts ciliar mm )

Acute treatment of angle closure glacoma
Definition
Pilocarpine
Term
Do not use if IOP higher htan 45mmHg can reduce angle further
Definition
Pilocarpine
Term
Can overcome mydriatic actions of atropine
used alternatively to break up lesions
Definition
Pilocarpine
Term
Orally causes increase in salivation (xerostomia treatment ) from radiation/ Sjogrens
Definition
Pilocarpine
Term
M3 and M1 selective muscarinic agonist
Definition
Cevimeline
Term
can be used for Xerstomia in Sjogrens syndrome works M3 and m1 only
Definition
Cevimeline
Term
can both activate and inhibit nicotinic receptors
Definition
Nicotine
Term
acutely: increases HR and BP from symnpathetic ganglia stimulation and secretion of epi at adrenal medulla
Definition
Nicotine
Term
partial agonist at neuronal nicotinic receptors
stimulates receptors while blocking at same time
Definition
Varenecline
Term
functionally similar to acetylcholinesterase but found in plasma
Definition
Butyrylcholinesterase
Term
simple alcohol w/ quaternary ammonium group
(less solubility in CNS)
reversible
short acting
Definition
edrophonium
Term
Carbanic acid esters of alcohols w/ quaternary ammonium
Definition
cargbamates, eg neostigmine
Term
In addition to the muscarinic effects of over activation (DUMBELS) you may see vasodilation w/ systemic agent such as this
Definition
Bethanechol
Term
treatment for cholinergic overactivation
Definition
atropine
Term
treatment for nicotinic overactivation
Definition
maintenance of vitals
Term
200x more potent than morphine for pain
from frog(alkaloid)
Definition
Epibatidine
Term
carbamic acid esters and simple alcohols are cholinesterase inhibitors (indirect agents) that are
Definition
reversible
Term
organic derivatives of phosphoric acid are
_____ inihbitors of cholinesterase

(phosphorylate serine residue)
Definition
irreversible
Term
used to treat patients of organophosphate poisoining. PRevents "aging" by displacing phosphorus group
Definition
PAM (pralidoxime)
Term
low doses lipophilic agents: increase alertness in CNS
high :
convulsions followed by respiratory failure
Definition
acetylcholinesterase inhibitors
Term
moderate doses REDUCE CO
INCREASE BP

might be bad for alzheimers pts that are hypertensive
Definition
acetylcholinesterase inhibitors
Term
large/toxic doses can result in
marked bradycardia
decrease in CO (large)
hypotension
Definition
acetylcholinesterase inhibitors
Term
10% of MG patients will not beneifit from anticholinesterase inhibitor because it is not autoimmune disease it is
Definition
congential
Term
DOC for anticholinergic drug poisoning (scopolamine etc)
Definition
Physostigmine
Term
Carbamate w/ intermediate duration 30 min- 6 hrs
Definition
Physostigmine
Term
Decreases IOP for 2 hrs pilocarpine more effective
Definition
Physostigmine
Term
synthetic carbamate that cant go through CNS

postoperative urinary retention/paralytic ileus
Definition
Neostigmine
Term
Used to reverse NM blockade by copetative neuromuscular blocers like tubocurarine

sometimes used to lower IOP in management of glaucoma or after opthalmic surgery though others are usually used
Definition
Neostigmine
Term
Neostigmine analog used for MG (longer duration of action) 3-6 hrs
Definition
Pyridostigmine
Term
Used for Mg duration of action 4-8 hrs (no cns effects)
Definition
Ambenonium
Term
quaternary ammonium, no CNS
used for glaucoma
Definition
Demecarium (Humorsol)
Term
high lipid solubility
used exclusively as insecticide (Lice)

carbamate
Definition
Carbaryl (Sevin, Carbacide)
Term
first piperidine type reversible anticholesterase used
Definition
Donepezil
Term
selective for AChE low for butyrylcholinesterase
Definition
Donepezil
Term
Similar to donepezil but also approved for parkinsons w/ dementia
transdermal patch
Definition
Rivastigmine
Term
derived from daffodils (AChE inhibitor) no hepatotoxicity
mild ot moderate Alzheimer disease
Definition
Galantamine
Term
Rarely used due to hepato toxicity
Definition
Tacrine
Term
Irreversible inhibitor of AChE but low lipid solubility so can be topical only used for glaucoma that doesnt work with other stuff 100 hr duration***
Definition
Echothiophate
Term
nerve agents
Definition
Sarin, Soman, Tabun, VX
Term
administered at low concentrations prophalaxis to nerve agents
reversible and can lock irreversible nerve agents from binding

gives them time to get treated w/ atropine (cholinergic antagonist) or Pralidoxime (2-PAM)
also get benzo as anticonvuslant
Definition
Pyridostigmine
Term
toxic dose of nicotine
Definition
40mg
Term
toxic dose of nicotine found in
Definition
2 cigarettes
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