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CPR Exam 1 > cholinergic receptors > Flashcards

cholinergic receptors Flashcards

(55 cards)

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1
Q

muscarinic receptors

A

mAChR located on parasympathetic neuroeffector sites

mAChR’s mediate parasympathetic responses

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2
Q

M1

A

nerve cells

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3
Q

M2

A

heart and SM

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4
Q

M3

A

heart and SM

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5
Q

M4

A

SM and glands

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6
Q

M5

A

?

probably central NS

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7
Q

Blocks mAchR?

A

Atropine

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8
Q

Nicotinic receptors

A

nAchR located on autonomic ganglia
nAchR’s are also involved in neuromuscular transmission

Nm
Nn

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9
Q

Nm

A

nicotinic receptor

Neuromuscular

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10
Q

Blocks Nm receptors?

A

Tubocurarine

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11
Q

Nn

A

nicotinic receptor

autonomic ganglia, adrenal medulla and CNS

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12
Q

Blocks Nn receptors?

A

Trimethaphan

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13
Q

Cholinomimetic Direct acting drugs

A

interact with receptor

ACh, bethanechol, pilocarpine, carbachol, cevimeline, methacholine

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14
Q

Cholinomimetic Indirect acting drugs

A

Potentiate effect of ACh, inhibit AChase, nonspecific
Physostigmine
Neostigmine
edrophonium

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15
Q

Ach

A

non-specific = Muscarinic and Nicotinic
Poor side effect profile
IV small dose - transient fall in BP (generalized vasodilation) accompanied by reflex Tachycardia
Large dose = bradycardia or block of AV nodal conduction (direct action on heart)

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16
Q

Cholinergic agonists: Eye

A

Miosis

improved near vision

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17
Q

Cholinergic agonists: Heart and vasculature

A

Decreased HR, CF, conduction

Vasodilation

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18
Q

Cholinergic agonists: Lung

A

Bronchoconstriction

increased secretion

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19
Q

Cholinergic agonists: GI and glands

A

increased motility
relaxation of sphincters
increased secretion

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20
Q

Cholinergic agoinsts: Urinary bladder

A

contraction

relaxation of sphincters

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21
Q

Bethanechol

A

selective for GI and urinary tracts
Urinary retention*
reflux esophagitis

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22
Q

Carbachol

A

muscarinic and nicotinic
Mainly Glaucoma
cataract surgery
Reduces intraocular pressure and produces miosis

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23
Q

Pilocarpine

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A

specific for muscarinic receptors
reverses mydriatic and cycloplegic agents
Most common drug given for Glaucoma*
promotes salivation

24
Q

Side effects of direct acting Cholinergic agonists (parasympathetic overstimulation)

Study These Flashcards
A 
sweating 
salivation
bronchoconstriction 
miosis 
cutaneous vasodilation with flushing 
nausea, vomiting and diarrhea 
changes in HR 
hypotension
25
Contraindications of Cholinergic agonists
Asthma Peptic ulcer Parkinsonism obstruction of GI or urinary tract
26
Reversible Anticholinesterases
``` Prolong the action of Ach and nonspecific Physostigmine Pyridostigmine Demecarium Neostigmine Ambenonium Edrophonium ```
27
Irreversible Anticholinesterases
``` Malathion - lice Parathion sarin/tabun/soman paraoxon echothiophate/ isoflurophate = glaucoma but obsolete now ```
28
Physostigmine
tx gluacoma but Pilocarpine is still preferred tx anticholinergic intoxication* side effect of too much = seizure and bradycardia
29
Neostigmine
Muscarinic action - tx distention and urinary retention Nicotinic actions - reverse paralysis induced by NMJ blocking agents elevate skin temp, sweating, salivation, brady w/ hypotension, skeletal muscle fasciculations
30
Neostigmine substitutes
Pyridostigmine - for chronic Myasthenia gravis Ambenonium - to manage Myasthenia Demecarium - glaucoma
31
Edrophonium
short duration of action *diagnostic tool and for therapy adjustment in Myasthenia Gravis Antidote to curare
32
How would you check the severity of organophosphorus anticholinesterase intoxication?
measure RBC AChase
33
Therapeutic uses of Organophosphates
Glaucoma - must minimize drainage through lacrimal ducts and ciliary spasm can cause discomfort, risk of cataracts with prolonged use insecticides, chem warfare
34
Organophosphate Toxicity
plasma cholinesterase regen. in 2 wks Neural cholinesterase may require 1 to 3 months Death second to respiratory complications N/V/D, abdominal pain, weakness, blurred vision, dizzy, HA
35
Muscarinic manifestations of Organophosphate tox
bronchoconstriction, increased bronchial secretions, sweating, salivation, lacrimation, bradycardia, miosis, blurred vision, urinary incontinence
36
Nicotinic manifestations of organophosphate tox
depolarizing neuromuscular blockade | CNS - restlessness, insomnia, tremors, confusion, ataxia, convulsions, respiratory depression, CVS collapse
37
Pralidoxime
used to regenerate AChase after inhibited by irreversible anticholinesterase, given before aging of the phosphate bond has its own anticholinesterase activity
38
Tx of organophosphorus toxicity
tx symptoms - support respiration and CVS Pralidoxime reverses neuromuscular effects Atropine for muscarinic and CNS effects scopolamine may be more effective for CNS effects
39
Cholinergic antagonists
competitive antagonists prototype agents - atropine and scopolamine scopolamine is more effective in the eye and has more prominent CNS actions
40
sensitivity of tissues to atropine
salivary glands>sweat glands>eye and heart>GI and urinary tract
41
Cholinergic antagonists: CVS
moderate to high therapeutic dosages produce tachycardia (blocks muscarinic receptors which mediate bradycardia) large doses of atropine may cause flushing
42
Cholinergic anatagonists: GI and urinary
require large doses reduces motility and tone more than secretion *Favors urinary retention by promoting sphincter contraction
43
Cholinergic antagonists: Eye
prolonged (up to 2 wks) mydriasis and cycloplegia | contraindiated for narrow angle glaucoma
44
Cholinergic antagonists: CNS
high doses - excitation, hallucinations, delirium Scopolamine - motion sickness, sedation can produce amnesia
45
Uses for Cholinergic Antagonists
tx Mydriasis, break adhesions (alternate agonists and antagonists) perioperative uses: dry secretion, prevent vagal bradycardia, reduce dose of anesthetic, scopolamine -sedative and amnesic tx - peptic ulcer by decreasing vagal mediated secretion, relieve spasm and slow gastric emptying antimuscarinic therapy asthma
46
Homatropine, cyclpentolate, tropicamide
atropine substitues | Mydriatics - short acting
47
Anticholinergic SM relaxants
selective action on GI less lipid soluble does NOT cross BBB
48
Irritable bowel syndrome
Dicyclomine | more bowel selective anticholinergic
49
Anticholinergic for Overactive bladder
uroselective drugs | darifenacin, solifenacin, tolterodine, trospium
50
Neuromuscular blocking agents act on
Nicotinic recetors nondepolarizing compete with ACh for receptors depolarizing agents initially stimulate NMJ and block
51
Nondepolaring NM agents
competitive blockade | includes: tubocurare, metocurine, pancuronium, gallamine, atracurium, vecuronium
52
Effective antagonists for nondepolarizing agents
Reversible Anticholinesterases b/c blocks break down of Ach prolonging it and increasing Ach concentration to better compete with the nondepolarizing (these block nicotinic receptors) agent for receptors
53
depolarizing neuromuscular blocking agent
Succinylcholine (depolarizing muscle relaxant)- produces 2 phase response 1. stim receptors, associated with muscle contraction 2. follows rapidly desensitizes receptors, making them refractory to stimulation. half life is 8 minutes GOOD FOR INTUBATION
54
Botulinum toxin
enters cholinergic nerve endings and inhibits exocytosis used for tx of strabismus and blepharospasm of eye side effects: excessive tearing and unilateral ptosis
55
Ganglionic blocking drugs
used as antihypertensives Hexmethonium Trimethaphan rarely used due to toxicity

CPR Exam 1 (2 decks)

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