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Test 2 FTM > Lecture 38 > Flashcards

Lecture 38 Flashcards

1
Q

What are the two types of cholinergic drugs?

A

cholinergic agonists and cholinergic antagonists

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2
Q

What are the two types of cholinergic agonists?

A

direct acting- bind to and activate

indirect acting- inhibit

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3
Q

What are the direct effects of ACh on the cardiovascular system?

A
  1. vasodilation (M3)
  2. decrease in cardio rate (M2)
  3. decrease in the rate of conduction by SA and AV nodes (M2)
  4. decrease force in contraction (M2)
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4
Q

How does a low dose of ACh impact the cardiovascular system?

A

A fall in blood pressure, but tachycardia occurs in response

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5
Q

How does a high does of ACh impact the cardiovascular system?

A

leads to a fall in blood pressure (M3) and bradycardia (M2)

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6
Q

How does ACh impact the vasculature?

A

release of NO and vasodilation

lower BP

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7
Q

How does ACh impact the eye?

A

miosis

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8
Q

How does ACh impact the ciliary muscle?

A

accommodation of lens to near vision

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9
Q

How does ACh impact glands?

A

increase secretion

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10
Q

how does ACh impact the bronchi?

A

constriction

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11
Q

how does ACh impact the heart?

A

decreased heart rate and conduction velocity

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12
Q

how does ACh impact the GI?

A

increased peristalic activity and relaxtion of sphincters

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13
Q

how does ACh impact the bladder?

A

Contraction of detrusor muscle; relaxation of

sphincter

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14
Q

What does atropine do?

A

a muscarinic antagonist

If muscarinic effects are blocked by a muscarinic antagonist such as atropine, large doses of acetylcholine produce nicotinic effects:

Vasoconstriction and increase in blood pressure

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15
Q

What are the two kinds of direct-acting cholinergic agonists?

A
  1. esters of choline

2. alkaloids

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16
Q

What are examples of choline esters?

A
  1. acetylcholine
  2. methacholine
  3. bethanechol
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17
Q

About choline esters?

A

they are quaternary ammoniums

poorly absorbed and distributed into the CNS

ACh is very rapid hydorlyzed

meth and beth are more resistant to hydrolysis

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18
Q

Acetylcholine

A

A muscarinic receptor and nicotinic agonist

used to produce an miosis effect during cataract surgery or other procedures where miosis is needed

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19
Q

Bethanechol

A

muscarinic agonist

uses:

  1. postoperative urinary retention
  2. atony of the bladder
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20
Q

methacholine

A

Muscarinic agonist

uses:
Diagnosis of bronchial airway hyperreactivity in
subjects who do not have clinically apparent
asthma.

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21
Q

What are the natural alkaloids (direct acting)?

A
  1. pilocarpine

2. nicotine

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22
Q

pilocarpine?

A

partial muscarinic agonist
tertiary amine
stable to hydrolysis by ACh enzyme

uses:
glaucoma
dry mouth due to radiotherapy

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23
Q

what are the adverse effects of muscarinic agonists?

A
  1. sweating
  2. salivation
  3. flushing
  4. low bp
  5. nausea
  6. abdominal pain
  7. diarrhea
  8. bronchospasm
24
Q

nicotine?

A

tertiary amine
agonist at nicotinic receptors

Depending on the dose, nicotine depolarizes
autonomic ganglia, resulting first in stimulation
and then in paralysis.

25
low nicotine dose?
ganglionic stimulation by depolarization
26
high nicotine dose?
ganglionic and neuromuscular blockade
27
nicotine uses?
to stop smoking
28
indirect-acting cholinergic agents?
1. edrophonium 2. carbamates 3. organophosphates
29
mechanism of edrophonium?
binds reversibly to the active site of the enzyme. The inhibition is short-lived. anticholinesterase
30
mechanism of carbamates?
form a covalent bond with the enzyme anticholinesterase
31
mechanism of organophosphates?
phosphorylate the enzyme. The covalent bond formed is extremely stable and hydrolyzes very slowly
32
explain anticholinesterases
they increase the concentration of ACh since acetylcholinesterase is inhibited effects are similar to direct acting cholinergic agonists
33
how do anticholinesterases impact the cardiovascular system?
In the vascular smooth muscle cholinesterase inhibitors have minimal effects because most vascular beds lack cholinergic innervation.
34
how do anticholinesterases impact the neuromuscular junction
increase the strength of the contraction Useful to reverse action of nondepolarizing neuromuscular blockers. Useful in myasthenia gravis.
35
edrophonium uses?
does not enter CNS quaternary ammonium uses: diagnosis of myasthenia gravis Used to reverse the neuromuscular block produced by non-depolarizing muscular blockers
36
physostigmine uses?
tertiary amine can enter the CNS uses: treatment of anticholinergic drug overdose
37
neostigmine uses?
quaternary ammonium does not enter CNS uses: urinary retention Reversal of effects of non-depolarizing neuromuscular blockers after surgery. Treatment of myasthenia gravis
38
pyridostigmine uses?
quaternary ammonium does not enter CNS uses: treatment of myasthenia gravis
39
types of organophosphates?
malathion (insecticide) sarin (nerve agent)
40
Types of cholinergic antagonists?
1. muscarinic 2. nicotinic 3. drugs that act presynaptically
41
types of nicotinic receptor antagonists?
1. ganglion blockers | 2. NMJ blockers
42
what drugs are muscarinic receptor antagonists?
atropine and scopolamine
43
Atropine characteristics?
Reversible competitive antagonist at muscarinic receptors. Tertiary amine: both central and peripheral muscarinic blocker
44
Atropine actions?
Eye: Mydriasis & cycloplegia (M3 blockade). GI: Reduces gastric motility (M3 blockade). ``` Urinary system: Decreases hypermotility of urinary bladder (M3 blockade). ``` ``` CV system: Moderate to high therapeutic doses cause tachycardia (Atrial M2 blockade). ``` Secretions: Salivary, sweat and lachrymal glands are blocked. Inhibition of sweat glands may cause high body temperature (M3 blockade).
45
Atropine uses?
antidote for cholinergic agonists to block respiratory secretions prior to surgery
46
adverse effects of atropine?
Dry mouth, blurred vision, sandy eyes, tachycardia, constipation, urinary retention. Effects on CNS: restlessness, confusion, hallucinations, delirium.
47
uses of scopolamine?
motion sickness
48
Ipratropium use?
used for the treatment of COPD and asthma muscarinic antagonist
49
tropicamide use?
used as a mydriatic for fundoscopy produces mydriasis with cycloplegia muscarinic antagonist
50
What are the contraindications of using antimuscarinic agents?
Contraindicated in patients with angle-closure glaucoma. Should be used with caution in patients with prostatic hypertrophy and in the elderly.
51
examples of ganglion blockers?
nicotinic antagonists remove dominant control 1. nicotine = prolonged depolarization 2. hexamethonium = antagonism of nicotinic receptors
52
hexamethonium use?
was used for hypertension in the past no longer used due to adverse effects
53
Tubocurarine?
nondepolarizing blocker mechanism: competitive antagonist use: As adjuvant drugs in anaesthesia during surgery to relax skeletal muscle.
54
Succinylcholine?
depolarizing blocker mechanism: binds to the nicotinic receptor and depolarizes the junction. Persists in the synaptic cleft, stimulating the receptor: receptor desensitizes. This leads to flaccid paralysis. use: Rapid endotracheal intubation. ECT
55
Botulinum toxin?
inhibitor of ACh release Injected locally into muscles for treatment of several diseases involving muscle spasms. Also approved for cosmetic treatment of facial wrinkles.

Test 2 FTM (28 decks)

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