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CPR Exam 1 > cholinergic receptors > Flashcards

cholinergic receptors Flashcards

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

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)

A 
sweating 
salivation
bronchoconstriction 
miosis 
cutaneous vasodilation with flushing 
nausea, vomiting and diarrhea 
changes in HR 
hypotension
25
Q

Contraindications of Cholinergic agonists

A

Asthma
Peptic ulcer
Parkinsonism
obstruction of GI or urinary tract

26
Q

Reversible Anticholinesterases

A 
Prolong the action of Ach and nonspecific 
Physostigmine
Pyridostigmine 
Demecarium 
Neostigmine 
Ambenonium 
Edrophonium
27
Q

Irreversible Anticholinesterases

A 
Malathion - lice 
Parathion
sarin/tabun/soman 
paraoxon 
echothiophate/ isoflurophate = glaucoma but obsolete now
28
Q

Physostigmine

A

tx gluacoma but Pilocarpine is still preferred
tx anticholinergic intoxication*
side effect of too much = seizure and bradycardia

29
Q

Neostigmine

A

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
Q

Neostigmine substitutes

A

Pyridostigmine - for chronic Myasthenia gravis
Ambenonium - to manage Myasthenia
Demecarium - glaucoma

31
Q

Edrophonium

A

short duration of action
*diagnostic tool and for therapy adjustment in Myasthenia Gravis
Antidote to curare

32
Q

How would you check the severity of organophosphorus anticholinesterase intoxication?

A

measure RBC AChase

33
Q

Therapeutic uses of Organophosphates

A

Glaucoma - must minimize drainage through lacrimal ducts and ciliary spasm can cause discomfort, risk of cataracts with prolonged use
insecticides, chem warfare

34
Q

Organophosphate Toxicity

A

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
Q

Muscarinic manifestations of Organophosphate tox

A

bronchoconstriction, increased bronchial secretions, sweating, salivation, lacrimation, bradycardia, miosis, blurred vision, urinary incontinence

36
Q

Nicotinic manifestations of organophosphate tox

A

depolarizing neuromuscular blockade

CNS - restlessness, insomnia, tremors, confusion, ataxia, convulsions, respiratory depression, CVS collapse

37
Q

Pralidoxime

A

used to regenerate AChase after inhibited by irreversible anticholinesterase, given before aging of the phosphate bond
has its own anticholinesterase activity

38
Q

Tx of organophosphorus toxicity

A

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
Q

Cholinergic antagonists

A

competitive antagonists
prototype agents - atropine and scopolamine
scopolamine is more effective in the eye and has more prominent CNS actions

40
Q

sensitivity of tissues to atropine

A

salivary glands>sweat glands>eye and heart>GI and urinary tract

41
Q

Cholinergic antagonists: CVS

A

moderate to high therapeutic dosages produce tachycardia (blocks muscarinic receptors which mediate bradycardia)
large doses of atropine may cause flushing

42
Q

Cholinergic anatagonists: GI and urinary

A

require large doses
reduces motility and tone more than secretion
*Favors urinary retention by promoting sphincter contraction

43
Q

Cholinergic antagonists: Eye

A

prolonged (up to 2 wks) mydriasis and cycloplegia

contraindiated for narrow angle glaucoma

44
Q

Cholinergic antagonists: CNS

A

high doses - excitation, hallucinations, delirium
Scopolamine - motion sickness, sedation
can produce amnesia

45
Q

Uses for Cholinergic Antagonists

A

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
Q

Homatropine, cyclpentolate, tropicamide

A

atropine substitues

Mydriatics - short acting

47
Q

Anticholinergic SM relaxants

A

selective action on GI
less lipid soluble
does NOT cross BBB

48
Q

Irritable bowel syndrome

A

Dicyclomine

more bowel selective anticholinergic

49
Q

Anticholinergic for Overactive bladder

A

uroselective drugs

darifenacin, solifenacin, tolterodine, trospium

50
Q

Neuromuscular blocking agents act on

A

Nicotinic recetors
nondepolarizing compete with ACh for receptors
depolarizing agents initially stimulate NMJ and block

51
Q

Nondepolaring NM agents

A

competitive blockade

includes: tubocurare, metocurine, pancuronium, gallamine, atracurium, vecuronium

52
Q

Effective antagonists for nondepolarizing agents

A

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
Q

depolarizing neuromuscular blocking agent

A

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
Q

Botulinum toxin

A

enters cholinergic nerve endings and inhibits exocytosis
used for tx of strabismus and blepharospasm of eye
side effects: excessive tearing and unilateral ptosis

55
Q

Ganglionic blocking drugs

A

used as antihypertensives
Hexmethonium
Trimethaphan
rarely used due to toxicity

CPR Exam 1 (2 decks)

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