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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
esters of choline are contraindicated for
hyperthyroidism, asthma, coronary disease (hypotension), acid peptic disorders, obstructive urinary retention
ester of choline
-need high IV doses to detect effects- used to dec IOP post operatively and sweat spot test
ester of choline

more resistant to cholinesterase and longer lasting-

-used to diagnose bronchial airway hypersensitivity
-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
ester of choline
-not nicotinic, inc GI motility,
-only ester of choline given systemically
used for empying bladder in postpartum nonobstructive urinary retention
muscarine, pilocarpine, nicotine, varenecline
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
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.
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
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
-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.
reversible cholinesterase inhibitor
myasthenia gravis,
alleviate postoperative urinary retention and paralytic ileus
-reverse neuromuscular blockade,
-lower IOP in glaucoma or post ophthalmic surgery
-reversible anticholinesterase
long duration, for symptomatic tx of AD
-no hepatic toxicity
like donepezil but with hepatic toxicity
mild to moderate tx of AD
reversible ACHe inhibitor
long term ACHe inhibitor
myasthenia gravis
reversible anticholinesterase
reversible ACHe
reversible ACHe
Pralidoxime 2-PAM
irreversible ACHe
-regenerate enzyme if given before aging for organophosphates
irreversible ACHe inhibitor
-low lipid solubility- not absorbed systemically
-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
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