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35 Cards in this Set

  • Front
  • Back
cholinergic agonists are divided into two groups which are:
esters of chline (ACh, methacholine, bethanecol, carbachol)

Alkoloids (muscarine, nicotine, pilocarpine,)
Muscarinic effects on the eye and cardiovascular system include
decrease IOP

vasodilation, dec HR and reduced contractility
Muscarinic effects on the respiratory and GI tract include
bronchoconstriction, increased secretion (contraindicated in asthma)

increased secretory and motorof gut activity..digestion
Nicotine effects on PNS in cardiovascular system, GI, respiratory, and genitourinary
-will activate both through post ganglionic neurons

cardiovascular effects are sympathetic

all the rest are parasympathetic

MATCH (muscle weakness, fasciculations, Adrenal medula inc, tachycardia, cramping of skeletal muscle, hypertension)
organophosphates are
nonselective ACHe inhibitors- inhibits both nicotinic and muscarinic
All esters of choline cross the bbb T/F
false
esters of choline are contraindicated for
hyperthyroidism, asthma, coronary disease (hypotension), acid peptic disorders, obstructive urinary retention
ACH
ester of choline
-need high IV doses to detect effects- used to dec IOP post operatively and sweat spot test
Methacholine
ester of choline

more resistant to cholinesterase and longer lasting-

-used to diagnose bronchial airway hypersensitivity
carbachol
-ester of choline
significant nicotinic activity at ganglia, skeletal muscle and adrenal medulla

used for intracameral instillation to produce miosis in ocular surgery and to reduce postoperative rises in IOP. Ophthalmic drops to reduce IOP in glaucoma or hypertension

limited to ophtalmic applications
bethanechol
ester of choline
-not nicotinic, inc GI motility,
-only ester of choline given systemically
used for empying bladder in postpartum nonobstructive urinary retention
alkaloids-
muscarine, pilocarpine, nicotine, varenecline
pilocarpine
-alkaloid-
crosses BBB
-active on eye and sweat glands
-miosis, accomodation
-initial tx of open angle glaucoma- red IOP (not use if IOP is >45mmHg.
-if taken orally causes Xerostomia assoc with Sjogren's syndrome
Nicotine
cholinomimetic-> alkaloid
All autonomic ganglia including skeletal muscles and cns.
-can activate and inhibit nicotinic ACH receptors
-used as smoking cessasion agent
-rapid activation of receptor followed by desensitized state.
Varenecline
-Alkaloid-
partial agonist
ACHe inhibitor groups
-simple alcohols - quarternary ammonium (edrophonium) 5-15 min
-Carbamic acid esters (carbamates, neostigmine) 30min-6hrs
-organic derivatives of phosphoric acid (organophosphates) (irreversible 2 step process)
hundreds of hours
pralidoxime
PAM- if used before aging in organophosphate (ACHe inhibitor) occurs, then enzyme can be restored.
ACHe inhibitors effects on organ systems
mostly parasymphathetic-
CV-reduced CO, no VSM effect,

CNS- coma, convulsions, respiratory failure

NMJ- can be beneficial for someone with myasthenia gravis or someone given curare
edrophonium
-reversible ACHe
5-15 min
-dx for myasthenia gravis and evaluating efficacy of myasthenia therapies

-give 2mg followed by 8ngm if muscle weakness occurs -> cholinergic crisis- need atropine

-used to assess efficacy of long term tx- pyridostigmine- if patient is stronger, dosage not enough
physostigmine salicylate
reversible ACHe
30m to 6hrs-
-local application causes miosis, accomodation, decrease in IOP. Pilocarpine is more effective.
neostigmine
reversible cholinesterase inhibitor
.5-2hrs
myasthenia gravis,
alleviate postoperative urinary retention and paralytic ileus
-reverse neuromuscular blockade,
-lower IOP in glaucoma or post ophthalmic surgery
donepezil
-reversible anticholinesterase
long duration, for symptomatic tx of AD
-no hepatic toxicity
tacrine
like donepezil but with hepatic toxicity
galantamine
mild to moderate tx of AD
reversible ACHe inhibitor
pyridostigmine
long term ACHe inhibitor
3-6hrs
myasthenia gravis
ambenonium
reversible anticholinesterase
4-8hrs
demarcium
reversible ACHe
glaucoma
carbaryl
reversible ACHe
lice
Pralidoxime 2-PAM
irreversible ACHe
-regenerate enzyme if given before aging for organophosphates
echothiopate
irreversible ACHe inhibitor
-low lipid solubility- not absorbed systemically
-glaucoma
-100 hrs
malathion and parathion
-irreversible ACHe inhibitor
-rapidly metabolized by birds and mammals to non-toxic metabolites but not by insects or fish
-parathion is not detoxified in vertebrates, more dangerous
nerve agents
sarin, soman, tabun and vx
-chemical warfare
-flaccid paralysis, respiratory failure
-pyridostigmine given prophylactically to block binding of irreversible agents so more time for tx with atropine or 2-PAM
toxicity of cholinomimetics-direct acting stimulants
tx is atropine
o
toxicity of cholinomimetics- direct acting nicotinic stimulants
-toxic dose = 40mg - 2 cigarettes but it is an emetic

-tx with atropine or diazepam for cns effects
toxicity of cholinomimetics: cholinesterase inhibitors
-home pesticides = source
-tx- maintain vital signs, decontaminate, parenteral atropine in large doses and PAM to regenerate, benzodiazepines to prevent seizures