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Muscarinic Receptor Blocking Drugs Flashcards

1
Q

What are muscarinic receptor blocking drugs?

A

Anticholinergic drugs

Parasympatholytics

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2
Q

What is the mechanism of action of parasympatholytics?

A

They remove PSY stimulation on effector cells — SY stimulation will dominate

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3
Q

Name the tertiary tropines?

A

Atropine
Scopolamine
Homatropine
Benztropine

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4
Q

How long is the duration of effect of atropine?

A

7-10 days

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5
Q

What are the clinical uses of atropine?

A 
Antispasmodic
Anti-secretory
Antidiarrheal 
Ophthalmology (but has a long half life)
Management of AchE inhibitor OD
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6
Q

Is atropine a tertiary tropine or a quaternary?

A

Tertiary

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7
Q

Can atropine enter the CNS?

Why?

A

Yes

Because it is a tertiary tropine

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8
Q

Does atropine have central or peripheral effects?

A

Both central and peripheral effects

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9
Q

What is atropine competitive to?

A

Ach

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10
Q

What are the CNS effects of atropine?

A 
Antimimetic effect 
Restlessness
Hallucinations
Epileptiform convulsions
Coma
Death
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11
Q

What are the peripheral effects of atropine?

A 
Decreased secretions
Dry mouth
Decreased gastric secretion
Dry skin
Mydriasis (wide pupils)
Cyclopegia (blurred vision)
Hyperthermia
Bronchodilator
Tachycardia - TdP and V-fib 
Relaxation of abdominal smooth muscle which leads to decreased secretions in the intestine, urinary bladder, uterus and the Choledochus
Constipation 
Dysuria
Urinary retention
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12
Q

What is the treatment of acute intoxication with atropine?

A

Physostigmine

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13
Q

Why is physostigmine used in the treatment of atropine intoxication

A

Atropine is a competitive inhibitor of muscarinic receptors. The only way to overcome the effects of a competitive antagonist is to increase the concentration of the ligand for those receptors (Ach). Therefore we use an AchE inhibitor to increase the concentration of Ach at the synapse

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14
Q

What is mydriasis?

A

Dilation of the pupils

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15
Q

What is cyclopegia?

A

Loss of accommodation (blurred vision)

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16
Q

What are the clinical uses of parasympatholytics?

A 
Mydriasis
Bronchial asthma 
COPD (ipratropium spray)
Bradycardia
1st degree AV blocks
Peptic ulcer
Incontinence
Diarrhoea
Abdominal cramps
Parkinson’s syndrome
Organophosphate poisoning
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17
Q

Which parasympatholytic is used to treat COPD and how is it administered?

A

Ipratropium spray

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18
Q

How long is the duration of effect of scopolamine?

A

3-7 days

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19
Q

What are the clinical uses of scopolamine?

A

Motion sickness
Post-operative nausea and vomiting
To block short term memory
‘Truth serum’

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20
Q

How is scopolamine administered to treat motion sickness?

A

Topical patch

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21
Q

Can scopolamine enter the CNS?

A

Yes because it is a tertiary tropine

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22
Q

What are the clinical uses of Homatropine?

A

Ophthalmology

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23
Q

What is the duration of effect of Homatropine?

A

1-3 days

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24
Q

Is homatropine a quaternary or tertiary tropine?

25
What are the clinical uses of Benztropine?
Parkinson’s | Acute extrapyramidal symptoms induced by antipsychotics
26
Which receptor does benztropine act on?
M1 receptor
27
What type of drug is benztropine?
It is an M1 receptor antagonist
28
What are the characteristics of Benztropine?
Lipid soluble so has CNS entry M1 receptor antagonist Tertiary tropine
29
Name the quaternary tropines
Ipratropium Tiotropium Methylalatropine
30
What receptor does tiotropium act on?
M3
31
What type of tropine is tiotropium?
Quaternary tropine
32
What are the clinical uses of tiotropium?
COPD | Bronchodilator
33
How is tiotropium administered for COPD?
Inhalation, spray
34
What are the clinical uses of Methylalatropine?
Peripheral use
35
What type of tropine is methylalatropine?
Quaternary tropine.
36
What receptor does Ipratropium act on?
M3 selective
37
Which muscarinic blocking drugs selectively act on the M3 receptor?
Ipratropium | Tiotropium
38
What is Ipratropium non-selective for?
It also stimulates the negative feedback receptor in the presynaptic nerve terminal (alpha 2 receptors ???? ) CHECK THIS
39
Can Ipratropium enter the CNS? Why?
No It is a quaternary tropine
40
What are the clinical uses of Ipratropium?
Asthma and COPD Inhibition of Bronchospasm Decreased secretions
41
How is Ipratropium administered in Asthma and COPD?
Inhalation, spray
42
Name the synthetic tropines with tertiary amines
``` Procyclidin Biperiden Tropicamide Pirenzepine Tolterodine Oxybutynin Solifenacine Darifenacine ```
43
What is the duration of effect of Pirenzepine?
6h (short acting)
44
What is a characteristic of Tropicamide?
Short half-life
45
Which receptor does tolterodine, oxybutynin, solifenacine, darifenacine act on?
M3 receptor antagonists
46
What are the clinical uses tolterodine, oxybutynin, solifenacine, darifenacine act on?
Urinary incontinence
47
Which of the synthetic tropines with tertiary amines are used in urinary incontinence?
Tolterodine Oxybutynin Solifenacine Darifenacine
48
Which of the synthetic tropines with tertiary amines are used in Parkinson disease? Why?
Procyclidin Biperiden Because they inhabit tremors
49
What is the clinical use of tropicamide?
Ophthalmology- causes mydriasis and cyclopegia
50
How is tropicamide administered in ophthalmology?
Topical: eye drops
51
Which synthetic tropine with tertiary amine is used for peptic ulcers?
Pirenzepine
52
Name the synthetic tropine with quaternary amine
Propantheline
53
What is Propantheline used for?
Abdominal spasms
54
Which muscarinic blockers are used in Asthma?
Tiotropium | Ipratropium
55
Which of the muscarinic antagonists are used in Parkinson’s disease?
Benztropine Procyclidin Biperiden
56
Which muscarinic antagonists are used in COPD?
Ipratropium | Tiotropium
57
Which muscarinic antagonists are used in ophthalmology?
Atropine Homatropine Tropicamide
58
What is the duration of effect of Tropicamide?
0.25 day
59
Which muscarinic antagonists has the longest duration of effect in ophthalmology?
Atropine

Pharma (23 decks)

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