Muscarinic receptor agonists - direct agonists of muscarinic receptors - produce effects similar to those obsered during the stimulation of post-ganglionic PS nerves

Reversible competitive AcHE inhibitor - rapid onset and short duration of action - not orally active: IV admistration Uses - diagnosis of myasthenia gravis - distinguish cholinergic crisis from myasthenic crisis - reversal of paralysis by competitive neuromuscular blocking drugs

Reversible non-substrate AcHE inhibitor - alkaloid - slowly reversible - tertiary amine--> CNS effects Uses: - treatment of wide-angle glaucoma - treat toxicity by anti-muscarinic drug poisoning ( IV penetrates into CNS)

Reversible non-substrate AcHE inhibitor - slow reversible - quaternary amine: no CNS effects Use: - treat myasthenia gravis (oral) - prevention and treatment of post-operatirve atony of gut and bladder - reversal of anesthesia

muscarinic receptor antagonist - treat AcHE or muscarinic toxicity - treat bradyarrhythmia (acute MI) - produce mydriasis (dilation) and cycloplegia (paralysis of accomodation) - long duration of action (7-10 days) - treat acute iritis or choroiditis - use as anethesia to block vagal reflex

Muscarinic Antagonist - CNS penetration - used as a transdermal patch - used to treat motion sickness

Derivative of alkaloids - muscarinic receptor antagonist - used to treat COPD - administered by inhalation - no CNS penetration - reduce brochosecretions and constriction

Cholinergics Flashcards by jacky c

Parasympathomimetic

Muscarinic receptor agonists

direct agonists of muscarinic receptors
produce effects similar to those obsered during the stimulation of post-ganglionic PS nerves

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parasympatholytic

Muscarinic receptor antagonists

Interfere with responses that result from PS stimulation

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Cholinergic

Receptors types

Acetyl CoA +Choline–> AcH
AcH acts on
- muscarinic R (PS)
- nicotinic R

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Muscarinic R effects

Eye
Heart
Lung
GI
Sweat glands
BV

Eye: contraction of ciliary m.= accomodation, contraction of iris= miosis

Decrease HR
Bronchoconstriction
bladder voiding
Salivation, increase gastric secretion, intestinal tone and motility
generalized sweating
Vasodilation

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anti-muscarinic

parasympatholytics

muscarinic receptor antagonists

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nicotinic

Nicotinic (muscle m)
Nicotinic (neural)

skeletal m: end plate depolarization

Autonomic ganglia: depolarization of post-ganglionic neurons

Adrenal Medulla: depolarization and secretion of catecholamines

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Bethanechol

choline ester- muscarinic receptor agonist
Quaternary amine
- primary effect of GI/GU tracts
- orally or SQ injection for urinary retention in absence of obstruction

Not administered thru IV- cause hypotension

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Pilocarpine

Alkaloid- muscarinic receptor agonist
Tertiary amine 
muscarinic effects
Uses:
- orally to treat xerostomia
- miotic agent ophthalmically to treat wide- angle glaucoma & emergency treatment for narrow angle glaucoma

not administered thru IV- will cause hypotension

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Edrophonium

Reversible competitive AcHE inhibitor

rapid onset and short duration of action
not orally active: IV admistration

Uses

diagnosis of myasthenia gravis
distinguish cholinergic crisis from myasthenic crisis
reversal of paralysis by competitive neuromuscular blocking drugs

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Physostigmine

Reversible non-substrate AcHE inhibitor

alkaloid
slowly reversible
tertiary amine–> CNS effects

Uses:

treatment of wide-angle glaucoma
treat toxicity by anti-muscarinic drug poisoning ( IV penetrates into CNS)

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Neostigmine

Reversible non-substrate AcHE inhibitor

slow reversible
quaternary amine: no CNS effects

Use:

treat myasthenia gravis (oral)
prevention and treatment of post-operatirve atony of gut and bladder
reversal of anesthesia

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Sarin

Irreversible Organophosphate inhibitors of AcHE

irreversibly phosphorylate the serine in the substrate binding domain of AcHE
regeneration of enzyme is slow
return of activity depends on synthesis of new enzyme

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Atropine

muscarinic receptor antagonist

treat AcHE or muscarinic toxicity
treat bradyarrhythmia (acute MI)
produce mydriasis (dilation) and cycloplegia (paralysis of accomodation)
long duration of action (7-10 days)
treat acute iritis or choroiditis
use as anethesia to block vagal reflex

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Scopolamine

Muscarinic Antagonist

CNS penetration
used as a transdermal patch
used to treat motion sickness

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Ipratropium

Derivative of alkaloids

muscarinic receptor antagonist
used to treat COPD
administered by inhalation
no CNS penetration
reduce brochosecretions and constriction

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Tropicamide

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Synthetic muscarinic antagonist

used to produce mydriasis and cycloplegia
fast onset (20-40 min) and short duration (4-6 hrs)

Oxybutynin

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Synthetic muscarinic antagonist

Use to treat overactive bladder and incontinence
high incidence of anti-muscarinic side effects
treat xerostomia mainly but also blurred vision, GI and antimuscarinic effects

Darifenacin

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Synthetic muscarinic antagonist

used to treat overactive bladder and incontinence
selective for M3 receptors

Glycopyrrolate

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Synthetic muscarinic antagonist

used to block PS effects during reversal of anesthesia with ACHE
no CNS penetration

Rocuronium

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Competitive Neuromuscular blocking agent

aminosteroid
intermediate duration (30-60 min)
rapid onset of action (intubation)
liver metabolism

Atracurium

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Competitive Neuromuscular blocking agent

benzylioquinoline
intermediate duration (30-60 min)
spontaneously degrades ( inactive)
minimal CV effects

Vecuronium

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Competitive Neuromuscular blocking agent

aminosteroid
intermediate duration of action (30-60 min)
onset 2-4 min
liver metabolism
no CV effects

Pancuronium

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Competitive Neuromuscular blocking agent

aminosteroid
onset 2-4 min
long duration of action (120-180 min)
liver metabolism
no CV effects

Succinylcholine

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Depolarizing Neuromuscular blocking agent
agonist of nicotinic receptors at NMJ–> opening of cation channels
- activate nicotinic receptors at NMJ maintains motor end plate depolarization ( prevent transmission of another AP)
- muscle fasciculations followed by flaccid paralysis
- metabolized by pseudocholinesterase
- ultra short duration of action (5-8 min): tracheal intubation
-genetic variation in pseudocholinesterase activity

Pralidoxime

``` Reactivates AcHE ( need to treat quickly 2-3 hours) - used for poisoning ```

Anti-cholinesterase

agents that enhance the effects of endogenously released AcH by blocking natural breakdown of ACH by AcHE

Ganglionic blocking agents

neural nicotinic receptor antagonists - competitive antagonists for Nn at autonomic ganglia - interferes with ganglionic transmission of both PS and S nerves

Side effects of choline esters what blocks toxicity? Use with caution in which groups?

``` SLUDGE Salivation Lacrimation Urination Defecation GI upset Emesis ``` Atropine blocks toxicity Use w/ caution: - Asthma & COPD - Urinary or GI obstruction - CV disease (bradycardia, hypotension)

Malathion

Irreversible Organophosphate inhibitors of AcHE - irreversibly phosphorylate the serine in the substrate binding domain of AcHE - regeneration of enzyme is slow - return of activity depends on synthesis of new enzyme -insecticide

Side effects of AcHE inhibitors Treatment

SLUDGE - death due to respiratory failure Treatment - atropine: muscarinic receptor antagonist- blocks muscarinic effects - pralidoxime- reactivates AcHE ( need to treat quickly 2-3 hours)

Muscarinic R antagonists Effects

competitively block muscarinic receptors Effects: - relax iris sphincter and ciliary muscles - relax non-vascular smooth muscle - inhibit exocrine gland secretion - increase HR - CNS effects - low dose: sedation - high dose: excitement, delirium, agitation

Side effects of muscarinic antagonist Use with caution

``` Hot as a hare (no sweating) Dry as a bone (dry mouth) Red as beet ( excessive heat) Blind as a bat (mydriasis, cycloplegia, blurred vision) Drowsiness- CNS ``` Toxic: mad as a hatter- hallucinations, delirium, coma Use with caution - Glaucoma: increase intraocular pressure - Prostatic Hypertrophy - tachycardia Poisoning: Treat with physostigmine

Neuromuscular blocking agent

block neurotransmission at NMJ producing muscle paralysis - use as adjuvant in anesthesia to obtain relaxation - use to facilitate intubation with tracheal tube - 2 classes ( non-depolarizing/ competitive or depolarizing)

Adverse effects/ Toxicity of neuromuscular blocking agents

Competitive: prolonged apnea and analphylaxis - toxicity can be reversed with neostigmine or edrophonium - if treating with ACHE for reversal, co-administer with muscarinic antagonist (glycopyrrolate) to reduce muscarinic actions Depolarizing: - prolonged apnea - not treatable with ACHE - Malignant hyperthermia: triggered by administration of depolarizing agents--> cause uncontrolled Ca release (due to mutation in ryanodine receptor) --> treat with ca release blocker - post- operative muscle pain due to muscle fasciculation - hyperkalemia: release potassium from intracellular sites

Cholinergics Flashcards

(34 cards)