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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
Q

low nicotine dose?

A

ganglionic stimulation by depolarization

26
Q

high nicotine dose?

A

ganglionic and neuromuscular blockade

27
Q

nicotine uses?

A

to stop smoking

28
Q

indirect-acting cholinergic agents?

A
  1. edrophonium
  2. carbamates
  3. organophosphates
29
Q

mechanism of edrophonium?

A

binds reversibly to the active site
of the enzyme. The inhibition is short-lived.

anticholinesterase

30
Q

mechanism of carbamates?

A

form a covalent bond with the enzyme

anticholinesterase

31
Q

mechanism of organophosphates?

A

phosphorylate the enzyme.

The covalent bond formed is extremely stable
and hydrolyzes very slowly

32
Q

explain anticholinesterases

A

they increase the concentration of ACh since acetylcholinesterase is inhibited

effects are similar to direct acting cholinergic agonists

33
Q

how do anticholinesterases impact the cardiovascular system?

A

In the vascular smooth muscle cholinesterase
inhibitors have minimal effects because most
vascular beds lack cholinergic innervation.

34
Q

how do anticholinesterases impact the neuromuscular junction

A

increase the strength of the contraction

Useful to reverse action of nondepolarizing
neuromuscular blockers.

Useful in myasthenia gravis.

35
Q

edrophonium uses?

A

does not enter CNS
quaternary ammonium

uses:
diagnosis of myasthenia gravis

Used to reverse the neuromuscular block produced by non-depolarizing muscular blockers

36
Q

physostigmine uses?

A

tertiary amine
can enter the CNS

uses:
treatment of anticholinergic drug overdose

37
Q

neostigmine uses?

A

quaternary ammonium
does not enter CNS

uses:
urinary retention

Reversal of effects of non-depolarizing
neuromuscular blockers after surgery.

Treatment of myasthenia gravis

38
Q

pyridostigmine uses?

A

quaternary ammonium
does not enter CNS

uses:

treatment of myasthenia gravis

39
Q

types of organophosphates?

A

malathion (insecticide)

sarin (nerve agent)

40
Q

Types of cholinergic antagonists?

A
  1. muscarinic
  2. nicotinic
  3. drugs that act presynaptically
41
Q

types of nicotinic receptor antagonists?

A
  1. ganglion blockers

2. NMJ blockers

42
Q

what drugs are muscarinic receptor antagonists?

A

atropine and scopolamine

43
Q

Atropine characteristics?

A

Reversible competitive antagonist at muscarinic
receptors.

Tertiary amine: both central and peripheral
muscarinic blocker

44
Q

Atropine actions?

A

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
Q

Atropine uses?

A

antidote for cholinergic agonists

to block respiratory secretions prior to surgery

46
Q

adverse effects of atropine?

A

Dry mouth, blurred vision, sandy eyes,
tachycardia, constipation, urinary retention.

Effects on CNS: restlessness, confusion,
hallucinations, delirium.

47
Q

uses of scopolamine?

A

motion sickness

48
Q

Ipratropium use?

A

used for the treatment of COPD and asthma

muscarinic antagonist

49
Q

tropicamide use?

A

used as a mydriatic for fundoscopy

produces mydriasis with cycloplegia

muscarinic antagonist

50
Q

What are the contraindications of using antimuscarinic agents?

A

Contraindicated in patients with angle-closure
glaucoma.

Should be used with caution in patients with
prostatic hypertrophy and in the elderly.

51
Q

examples of ganglion blockers?

A

nicotinic antagonists
remove dominant control

  1. nicotine = prolonged depolarization
  2. hexamethonium = antagonism of nicotinic receptors
52
Q

hexamethonium use?

A

was used for hypertension in the past

no longer used due to adverse effects

53
Q

Tubocurarine?

A

nondepolarizing blocker

mechanism: competitive antagonist

use: As adjuvant drugs in anaesthesia during surgery
to relax skeletal muscle.

54
Q

Succinylcholine?

A

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
Q

Botulinum toxin?

A

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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