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Pharmacology Exam 3
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Acetylcholine site of action
cholinergic agonist
muscarinic receptors
nicotinic receptors
Properties of Acetylcholine
rapidly hydrolized
for surgical use only to constrict iris
Physiological effect of ACH at lower doses
muscarinic action
Blood pressure
Physiological effect of acetylcholine at higher doses
ganglionic
primarily nicotinic
parasympathetic effects
Respiratory effects of acetylcholine
bronchoconstricion
increased mucous
GI effects of acetylcholine
digestion and motility
Methacholine
ACH-CH
3
cholinergic agonist
muscarinic specific
little nicotinic effect
uses of methacholine
diagnosis of asthma
use a B
2
agonist to overcome the effect
Bethanechol
cholinergic agonist
little nicotinic effect
highly resistant to AChE and Pseudocholinesterase
used for systemic effects
Uses of Bethanechol
urinary retention
abdominal distention
gastric atony (no movement)
Avoid used of bethanechol with
GI obstruction
leads to ischemia and tissue necrosis
Adverse reactions that occur with muscarinic cholinergic agonists
salivation
nausea
GI cramping
warm, sweating
faintness
Nicotine
cholinergic agonist
activates neuromuscular junction
leads to depolarization block (overstimulation)
activates chemoreceptors
stimulates respiration
Carbachol
cholinergic agonist
little hydrolysis at AChE and PSChE
high nicotinic effect
some muscarinic effect (GI/Bladder)
Use for carbachol
glaucoma
causes miosis
enhances aqueous humor outflow (muscarinic)
muscarine
cholinergic agonist
mushrooms
hypotention
decreased HR
increased gland secretions
Pilocarpine & Cevimeline
cholinergic agonist
tertiary amines that cross BBB
Pilocarpine use
glaucoma treatment
xerostomia
side effects of pilocarpine and cevimeline
sweating
cevelemine
cholinergic agonist
m1 and m3 selective
fewer side effects
less toxicity
Reversible AChE inhibitors
cations
competitively bind to the anionic site of AChE
Edrophonium
reversible AChE inhibitor
quaternary alcohol (cannot cross BBB)
differential diagnosis of myasthenia gravis
Physostigmine
reversible AChE inhibitor
freely crosses BBB
glaucoma
myasthenia gravis
reverse mydriasis or NMJ blockade
Neostigmine
reversible AChE inhibitor
quaternary amine (can't cross BBB)
nicotinic agonist (NMJ)
reversible AChE inhibitor
Neostigmine uses
myasthenia gravis
glaucoma
NMJ blockade reversal (curariform toxicity)
GI and Urinary atony
Antimuscarinic drug overdose (Atropine)
Donepezil & Rivastigmine
treat alzheimer's disease
reversable AchE inhibitors
Direct acting cholinergic agonists
acetylcholine
Metacholine
Bethanechol
Muscarine
Pilocarpine
Cevimeline
Nicotine
Carbachol
Reversible AChE inhibitors
Edrophonium
Physostigmine
Neostigmine
Donepezil
Rivastigmine
Irreversible AChE inhibitors
Organophosphates
covalently bind to the esteratic side of AChE
insecticide
sarin gas
Use of irreversible AChE inhibitors leads to:
overstimulation of parasympathetics leading to paralysis of respiratory muscles
Treatments for exposure to irreversible AChE inhibitors
vital sign maintenance
atropine
pralidoxime
bzd's
Toxicology of AChE Inhibitors 1st symptoms
Muscarinic effects
miosis
tightness of chest
salivation/sweating
bradycardia
Toxicology of AChE inhibitors 2nd effect
Nicotinic effects
skeletal muscle fasciculations
weakness
paralysis
Toxicology of AChE inhibitors (3rd phase)
CNS
restless/anxiety
confusion
convulsion
4th toxicological effect of AChE inhibitors
respiratory arrest
paralysis of muscles
central depression of respiration
airway obstruction (increased secretions)
Used for Glaucoma
pilocarpine
physostigmine
used for paralytic ileus and bladder atony
bethanechol
neostigmine
used for xerostomia
pilocarpine
cevimeline
used for myasthenia gravis
edrophonium (diagnosis and dose check)
neostigmine
antidote for atropine poisoning or TCA overdose
physostigmine
Used for alzheimer's/dementia
donepezil
rivastigmine
galantamine
other uses for cholinergic agonsits
paroxysmal supraventricular tachycardia
edrophonium for specific arrhythmias
Toxicity of direct actin muscarinic stimulants
N/V
Diarrhea
Urination/Salivation/Sweating
cutaneous vasodilation
bronchial constriction
Acute toxicity of direct acting nicotinic stimulants
central stimulant
depolarization blockade => respiratory paralysis
HTN and arrhythmias
Chronic toxicity of direct acting nicotinic stimulants
vascular disease risk
sudden coronary death
ulcer recurrences
varenicline (partial agonist)
Major pharmacologic effects of muscarinic receptors
SLUDGE
Salivation
Lacrimation
Urination
Defication
GI motility
Emesis
Myasthenia gravis
autoantibodies against alpha 1 subunit of the nicotinic receptor
results in weakness of commonly used voluntary muscles
Makes Myasthenia gravis worse
activity
aminoglycosides
Myasthenia gravis vs. cholinergic crisis
myasthenia needs more AChE inhibition
Crisis needs less AChE inhibition
edrophonium used to distinguish
Author
Rx2013
ID
44039
Card Set
Pharmacology Exam 3
Description
Cholinergic Agonists
Updated
2010-10-21T19:57:13Z
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