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109 Cards in this Set

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where is nicotinic-g receptor
ACh receptor at parasympathetic/sympathetic ganglia
type of receptor at parasympathetic organ?
muscarinic
neurotransmitter at alpha/beta receptors
NE
neurotransmitter at muscarinic receptors
ACh
for the most part, nicotic actions create _____ :(
side-effects
For the most part, indirect acting cholinomimetic drugs inhibit ______
Ach-esterase
examples of direct acting cholinomimetic drugs
Ach
Bethanechol
Pilocarpine
examples of indirect acting cholinomimetic drugs
Physostigmine
Neostigmine
Edrophonium
Acetylcholine is
a) specific
b)nonspecific
nonspecific (muscarinic/nicotinic)
Why does ACh have a short duration of action?
ACh-esterase
ACh has nicotinic action: describe its side-effect profile.
a) poor
b) rich
c) no side-effects
poor = side-effect prone
initial effect of IV Ach on Heart rate and BP
increase both initially

(subsequent decrease in both)
Direct acting cholinergic drugs
Ach (Miochol-E)
Bethanechol (Urecholine)
Carbachol
Cevimeline (Evoxac)
Pilocarpine
Side effect of Pilocarpine
diarrhea

Pile o' crap-ine
cholinergic agonists are more resistant to _______
ACh-esterase
Cholinergic Agonist directly stimulate ___________receptor
muscarinic
Cholinergic Agonist effect on the eye
miosis
improved near vision
Cholinergic Agonist effect on the heart
decreased HR
decreased CF
decreased conduction
Cholinergic Agonist effect on the lung
bronchoconstriction
increased secretion
Cholinergic Agonist effect on GI
increased motility
relaxed sphincters
increased secretion
Cholinergic Agonist effect on urinary bladder
contraction
relaxed spinchters
Cholinergic Agonist effect on glands
secretion
Cholinergic agonist used as a test for asthma
methanacol (provocholine)
Bethanechol is selective for ________and _______
GI and urinary tracts
Bethanechol is the DOC for postoperative, postpartum, neurogenic _____________
urinary retention
Bethanechol is used for reflux_________
esophagitis
Bethanechol is used for postoperative abdominal ________
distension
Carbachol has a poor side effect profile b/c ________
has muscarinic and NICOTINIC actions
main usage for carbachol
1- treatment of glaucoma

2- for cataract surgery: to reduce intraocular pressure and produc miosis
pilocarpine is specific for _______ receptors
muscarinic
pilocarpine has minimal ________ actions
nicotinic
Pilocarpine is used to reverse _________
mydriasis
and
effects of cyclopegic agents
pilocarpine is most commonly used cholinergic agonist to treat _________
glaucoma
pilocarpine used to treat dry mouth by increasing _______
salivation
Muscarine is specific for _______ receptors
muscarinic
side effects of direct acting cholinergic agonists
sweating, salivation,
cutaneous vasodilation with flushing,
nausea, vomiting, diarrhea,
HR changes, hypotension
contraindication of cholinergic agonists
asthma,
peptic ulcer,
Parkinsonism,
Pregnancy,
Severe cardiac disease,
hyperthyroidism (arrhythmias),
mechanical obstruction or impairment of GI or urinary tract
Indirect acting drugs potentiate the effects of ACh by inhibiting ________
hydrolysis
Indirect acting drug effects are due to ACh stimulating __________
muscarinic and nicotinic receptors
Reversible Anticholinesterases
Physostigmine, Pyridostigmine, Neostigmine,
Demecarium, Ambenoenium, Edrophonium
Irreversible Anticholinesterases
Isoflurophate, Echothiophate,
Malathion, Parathion,
Tabun,
Paraoxon
Physostigmine can be used to treat _______, but pilocarpine is preferred
glaucoma
Physostigmine is used for treatment of ___________, but be careful to avoid seizures, bradycardia
anticholinergic intoxication (ex. curare overdose)
Neostigmine has ACh-esterase action and direct _____-like action
ACh
Neostigmine has muscarinic effects due to ___________ inhibition
cholinesterase
Neostigmine has nicotinic effects at neuromuscular sites due to _____________
direct stimulation
Neostigmine's muscarinic action are used to treat ________
postoperative distension and urinary retention
Neostigmine' nicotinic actions can be used to reverse ________
paralysis induced by neuromuscular blocking agents
Side effects of neostigmine
Elevation of skin temperature,
Sweating,
Salivation,
Bradycardia with hypotension
Skeletal muscle fasciculations
Neostigmine Substitutes
Pyridostigmine
Ambenonium
Demecarium
Pyridostigmine used for _____
-used for chronic management of myasthenia gravis
Ambenonium used for______
- used also for management of myasthenia
Demecarium used for _______
-used for glaucoma
Edrophonium has a _____ duration of action
short
Edrophonium is Used as a diagnostic tool for ______
myasthenia
Edrophonium produces ________ in untreated myasthenia patient
rapid, transient increase in muscular strength

If strength improves, increase therapy
If response is unfavorable, decrease therapy
Edrophonium Used as an antidote to
curare
Irreversible organophosphorus anticholinesterases Bind _____
irreversibly with the enzyme - enzyme becomes permanently phosphorylated
Irreversible organophosphorus anticholinesterases Effects remain until ________
new enzyme is regenerated
Irreversible organophosphorus anticholinesterases Effects may persist for ______
weeks or months
Measurement of RBC Achase can be used to assess _______
severity of intoxication of Irreversible organophosphorus anticholinesterases
Isoflurophate and echothiophate are used for ______ therapeutically
glaucoma
Malathion can be used to treat _________
head lice
Organophosphates Most commonly used as ____________
insecticides
Organophosphates Developed as _________
chemical warfare agents
Organophosphates Toxicology is significant due to___________
High lipid solubility
Absorbed through skin, ingestion or inhalation
Readily enter CNS
Most common symptoms of Organophosphate Toxicity include __________________
nausea, dizziness, vomiting, abdominal pain, weakness, blurred vision and headache
Plasma cholinesterase is regenerated in _______
2 weeks
Neural cholinesterase may require _____ months to completely restore the enzyme
1-3
Organophosphate Toxicity Vision disturbances and headache can persist for ________
more than a month
Muscarinic manifestations of Organophosphate Toxicity
bronchoconstriction, increased bronchial secretions, sweating, salivation, lacrimation, bradycardia, miosis, blurred vision, urinary incontinence
Nicotinic manifestations of Organophosphate Toxicity
muscular fasciculations, tachycardia, hypertension
CNS manifestations of Organophosphate Toxicity
restlessness, insomnia, tremors, confusion, ataxia, convulsions, respiratory depression, CVS collapse
Used to regenerate Achase after it has been phosphorylated by irreversible anticholinesterase
Pralidoxime
Pralidoxime is Not used in intoxication by reversible anticholinesterase due to __________
its own anticholinesterase activity
Treatment of Organophosphorus Toxicity
Treat symptomatically - support respiration and CVS
___________ reverses neuromuscular effects of Organophosphorus Toxicity
Pralidoxime
_________used for muscarinic and CNS effects but scopolamine may be more effective for CNS effects of Organophosphorus Toxicity
Atropine
Prototype Cholinergic Antagonists are _______
atropine and scopolamine
Sensitivity of tissues to atropine:
Salivary glands>sweat glands>eye and heart>GI and urinary tract
________ is more effective in the eye and has more prominent CNS actions
Scopolamine
Cholinergic Antagonists Effects on CVS:
High therapeutic dosages produce _______
tachycardia
Cholinergic Antagonists Effects on CVS:
Small doses may decrease ____ due to central stimulation of vagus
HR
Cholinergic Antagonists effects on blood pressure
Minimal
Large doses of atropine may cause ________
flushing (atropine flush)
Cholinergic Antagonists Effects on GI and urinary tract
Requires large doses
Reduces motility and tone more than secretion
Favors urinary retention by promoting contraction of sphincter
Cholinergic Antagonists Effects on eye
Produce prolonged (up to 2 weeks) mydriasis and cycloplegia
Cholinergic Antagonists Contraindicated in
narrow angle glaucoma patients
Cholinergic Antagonists Effects on CNS
High doses produce excitation, hallucinations, delirium
Scopolamine used for motion sickness, preanesthetic, sedation
Can produce amnesia
Opthalmologic Uses of Cholinergic Antagonists
Mydriatic
Break adhesions
Perioperative uses of Cholinergic Antagonists
Dry secretions
Prevent vagal bradycardia
Reduce dose of anesthetic
Scopolamine used for sedative and amnesic effects
Prevent muscarinic effects of neuromuscular blocking agent
Cardiac uses of Cholinergic Antagonists
Prevent bradycardia after MI
GI disease uses of Cholinergic Antagonists
Once used to treat peptic ulcer by decreasing vagal mediated secretion, relieve spasm, and slowing gastric emptying
Side effects limited use
Uses of Cholinergic Antagonists
Motion sickness
Antimuscarinic intoxication
Asthma
Atropine Substitutes: Mydriatics (short acting)
Homatropine Cyclopentolate
Tropicamide
Atropine Substitutes: Anticholinergic smooth muscle relaxants
Methscopolamine Propantheline
Dicyclomine
Use for GI problems has been replaced by antihistamines
Used for urinary incontinence
Neuromuscular Blocking Agents Act on ________
nicotinic receptors
Nondepolarizing Agents compete with ____ for receptors
Ach
Depolarizing agents initially stimulate the neuromuscular junction and then _______
block it.
Nondepolarizing Agents
Tubocurare Metocurine
Pancuronium Gallamine
Atracurium Vercuronium
Botulinum Toxin Enters cholinergic nerve endings and inhibit ________
exocytosis
Botulinum Toxin Used for treatment of __________ of eye
strabismus and blepharospasm
Botulinum Toxin Used for smoothing _______
wrinkles
Side effects of Botulinum Toxin include excessive tearing and _________
unilateral ptosis
Ganglionic Blocking Drugs
Hexamethonium
Trimethaphan
Ganglionic Blocking Drugs In past, used as antihypertensives. Now, Rarely used due to _______
toxicity
The majority of therapeutic actions of cholinergic drugs are focused on an interaction at the __________ receptor
muscarinic
Side effects of cholinergic drugs are predictable, dose related
Excessive action on the muscarinic receptor
Interaction with ________ receptor
nicotinic
A
B