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Pharmacology > Anticholinergics > Flashcards

Anticholinergics Flashcards

1
Q

Cholinergic receptors are broadly divided into _______ and ______ receptors

A

Nicotinic

Muscarinic

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2
Q

Where are Nn receptors present❓

A

Ganglia
Adrenal medulla

Nn blockers are referred to as ganglion blockers

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3
Q

Where are Nm receptors found❓

A

Neuromuscular junctions

Nm antagonists are therefore referred to as neuromuscular blockers

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4
Q

Where are M1 receptors found❓

A

Gastric ganglia

CNS

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5
Q

Where are M2 receptors found❓

A

Heart

CNS

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6
Q

Where are M3 receptors found❓

A 
Eye 
GI 
Bladder
Bronchus 
Glands 
CNS
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7
Q

M3 and M4 receptors are found in the CNS

True or false

A

True

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8
Q

How are antimuscarinics classified❓

A

Natural alkaloids

Semisynthetic derivatives

Synthetic compounds

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9
Q

Give a few examples of antimuscarinic natural alkaloids

A

Atropine

Hyosine/Scopalamine

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10
Q

Atropine is…

  1. Rapidly absorbed from❓
  2. Distributed❓
  3. Metabolized in the❓
  4. Half life❓
A
  1. Upper small intestine
  2. Throughout the body
    Crosses BBB
    Crosses placenta
  3. Liver, 50%, by hydrolysis

3-4hrs

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11
Q

Hycosine is more metabolized and has a better BBB penetration than atropine

True or false

A

True

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12
Q

List the antimuscarinic spasmolytics you know

A

Atropine

Hyosine butyl bromide/Buscolysin®️

Oxyphenonium (GI)

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13
Q

What is the mechanism of action of antimuscarinics❓

A

🚫Action of Ach on autonomic receptors innervated by parasympathetic postganglionic neurons

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14
Q

Atropine stimulates the CNS but higher doses are required than for peripheral nerve stimulation

True or false
Why❓

A

True

Some level of restriction to BBB crossing

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15
Q

Highlight the effects of atropine

A

CNS stimulation

🚫Cholinergic overactivity in basal ganglia
⬇️tremor and rigidity in parkinsonism

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16
Q

What drugs would you combine in the treatment of Parkinsonism❓

Why❓

A

Antimuscarinic+Dopamine precursor drug

May provide more effective therapy than either drug alone

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17
Q

List a few examples of antimuscarinic semisynthetic derivatives

A

Homatropine

Hyoscine butyl bromide/Buscolysin®️

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18
Q

List a few examples of antimuscarinic synthetic compounds

A

Oxyphenonium

Pirenzepine

Ipratropium, Tiotropium

Flavoxate, Oxybutynynine, trospium

Tropicamide

Benztropine, Biperiden, Trihexyphenidyl

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19
Q

Which antimuscarinic semisynthetic derivative is a…

  1. Mydriatic
  2. Spasmolytic ❓
A
  1. Homatropine

2. Hyosine butyl bromide/Buscolysin®️

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20
Q

Which antimuscarinic natural alkaloid is a…

  1. Mydriatic
  2. Spasmolytic
  3. Antiemetic ❓
    What is it’s significance❓
A
  1. Atropine
  2. Atropine
  3. Hyosine
    It can be used to treat nausea/vomiting/motion sickness
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21
Q

Which antimuscarinic synthetic compound is a…

  1. Mydriatic
  2. Spasmolytic
  3. Antiulcer
  4. Antiasthmatic
  5. Antidysuric
  6. Antiparkinsonian
A
  1. Tropicamide
  2. Oxyphenonium (GI spasmolytic)
  3. Pirenzepine
  4. Ipratropium, Tiotropium
  5. Flavoxate, Oxybutynynine, trospium
  6. Benztropine, Biperiden, Trihexyphenidyl
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22
Q

List the antimuscarinic mydriatic you know

A

Atropine

Homatropine

Tropicamide

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23
Q

Which antimuscarinic would you use to treat a patient with dysuria❓

A

Flavoxate

Oxybutynynine

Trospium

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24
Q

Which antimuscarinic would you use to treat a patient with Parkinsonism❓

A

Benztropine

Biperiden

Trihexyphenidyl

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25
Q

There are drugs that aren’t antimuscarinics with antimuscarinic properties.

Do you know any❓

A

Antihistamines

Tricyclic antidepressants

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26
Q

What effects will pharmacological doses of atropine cause❓

What effects will high doses of atropine cause❓

A

✅
CNS excitation

⬆️
Restlessness
Hallucinations
Delirium

Respiratory depression
Coma

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27
Q

What effects will pharmacological doses of hyoscine cause❓

What effects will high doses of hyoscine cause❓

A 
✅
CNS depression:
Drowsiness
Amnesia 
Fatigue 
Dreamless sleep
⬆️
CNS excitation:
Restlessness
Hallucinations
Delirium

Used in preventing motion sickness

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28
Q

“Twilight sleep” is induced by ______

What is it’s application❓

A

Hyoscine

Truth serum for crime suspects

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29
Q

How would you apply the antiemetic properties of hyosine❓

A

Used to preventing motion sickness: transdermal patch placed behind pinna

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30
Q

What are the effects of anticholinergic drugs on the eye❓

A

Mydriasis (relaxation of cilliary muscle)

Photophobia

Cycloplegia

⬆️Intraocular tension

⬇️Lacrimal secretion (dry/sandy eyes)

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31
Q

How do antimuscarinics cause cycloplegia?

A 
Paralysis of cilliary eye muscles 
⬇️
🚫of accommodation
⬇️
Focused for far vision
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32
Q

Which antimuscarinic would you use to treat iritis, choroiditis, keratitis and corneal ulcers❓

Why❓

A

Atropine

It has a long lasting mydriatic-cycloplegic and local anodyne action on the cornea

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33
Q

Antimuscarinics should be carefully administered in patients with glaucoma.

Why❓
Why is this significant❓

A
  1. Antimuscarinics
    ⬇️

Relaxation of ciliary muscle
⬇️

Obstruction of drainage of aqueous humor
⬇️

⬆️IOP

  1. Contraindication in pts with narrow arrow angle glaucoma b/c of likelihood of complete obstruction of flow of aqueous humor

Refer to photos*
OR
http://tmedweb.tulane.edu/pharmwiki/doku.php/antimuscarinics

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34
Q

Tropicamide is a short acting antimuscarinic commonly used in eye exams

True or false

A

True

35
Q

What are the effects of anticholinergic drugs on the CVS❓

What CVS conditions are they useful in treating❓

A

1.
⬆️HR/Tachycardia

2.
Digitalis-induced bradycardia
Arrhythmias due to AV node

36
Q

What are the effects of anticholinergic drugs on the respiratory system❓

What conditions are they useful in treating❓

A 
1. 
Inhibition of M3 receptors
⬇️secretion 
⬇️ reflex bronchspasm
⬇️Bronchoconstriction
  1. Tx of bronchial asthma
    Tx of COPD
    Pre-anaesthetic mdx
37
Q

What anticholinergic drugs would you administer to threat bronchial asthma or COPD❓

A

Ipratropium (non selective)

Tiotropium (M1 and M3 receptors)

38
Q

Which anticholinergic drug is most suitable for pre-anaesthetic mdx to ⬇️secretions and reflex bronchospasm ❓

A

Glycopyrolate

39
Q

What are the effects of anticholinergic drugs on the GIT❓

What conditions are they useful in treating❓

A

1.
⬇️Motility
⬇️Secretions

2.
Peptic ulcer disease

Intestinal colic (anti-spasmodic agents)

Irritable bowel syndrome

Urinary incontinence/Overactive bladder

40
Q

What antimuscarinic drugs would you use in treating peptic ulcer disease❓

Why❓

A

Pirenzepine
Telenzepine

Selective M1 blockers

41
Q

What anticholinergic drugs would you use in treating intestinal colic❓

A

Hyoscine

Dicyclomine

Propantheline

Oxyphenonium

Clidinium

42
Q

What antimuscarinic drugs would you use in treating irritable bowel syndrome❓

Why❓

A

Darifenacin
Solefenacin

Selective M3 blockers

43
Q

If you had to manage a case of an overactive bladder or urinary incontinence, what drugs would you prescribe to your pt❓

A

Solefenacin

Oxybutynin

Flavoxate, Fesoterodine

Tolterodine, Trospium

Darifenacin

SOFT blad-DER

44
Q

Anticholinergic drugs:

⬇️secretions
Cause dry mouth
⬇️sweating
⬇️salivation

What is the significance on this in terms of pediatrics❓

A

Atropine is contraindicated in children b/c of the risk of hyperthermia (due to ⬇️sweating)

45
Q

Is there any anticholinergic that may be useful in poisoning cases❓

A

Atropine for early mushroom poisoning from Inocybe species

46
Q

List a few adverse effects of anticholinergic drugs you know

A

Difficulty swallowing or talking

Dry, flushes and hot skin (esp head and neck)

Fever

Difficulty in micturition

Scarlet rash

Dilated pupils; photophobia

Blurring of near vision

47
Q

What are the clinical presentations in atropine overdose❓

A

Palpitation
Weak, rapid pulse
CVS collapse
Respiratory depression

Excitement 
Psychotic behavior 
Ataxia
Delirium 
Hallucinations 
Convulsions
Coma
48
Q

How would you make a confirmatory diagnosis if you’re suspecting a case of atropine overdose❓

A

1mg neostigmine 🚫typical muscarinic effects

49
Q

How would you treat atropine overdose❓

A

Put pt in dark, quiet room

Tannic acid for gastric lavage

1-3mg Galantamine/Physostigmine (SC or IV)

Diazepam against convulsion

50
Q

What effect will anticholinergics (atropine) have on absorption of some drugs❓

Will drug doses ⬆️/⬇️

A

Slowness of absorbtion b/c of slow gastric emptying

⬆️Drug doses in circulation

51
Q

Anticholinergics will cause slow absorption of most

List some drugs that will be well absorbed

A

Digoxin

Tetracyclines (⬆️absorption)

52
Q

Antacids interfere with absorption of cholinergics

True or false

A

True

53
Q

Would an administration of antihistamines/tricyclic antidepressants or phenothiazine with anticholinergics increase or reduce the risk of additives side effects❓

A

⬆️risk of side effects b/c antihistamines/tricyclic antidepressants/phenothiazines have anticholinergic properties

54
Q

MAO inhibitors will interfere with the metabolism of antiparkinsonian drugs

True or false
Give an example

A

True

Biperiden; derilium may occur

55
Q

If you had to undergo a dental prodecure and you needed to give an antisialogogue, what drug would you administer❓

A

Atropine sulphate tablet, 1hr before appointment

56
Q

Conditions like xerostomia may increase incidence of caries glossitis if atropine is administered

True or false

A

True

57
Q

Ganglion blockers have many side effects and their clinical use is out of date

Give a few examples

A

Hexamethonium

Trimethaphan

Mecamylamine

58
Q

Neuromuscular blocking agents can be divided into

A

Nondepolarizing/Competitive blockers/Curare-like drugs

Depolarising/Hyperpolarizing agents

59
Q

List some short-acting, non-depolarizing, neuromuscular agents

A

Mivacurium

60
Q

List some intermediate-acting, non-depolarizing, neuromuscular agents

A

Atracurium

Vecuronium

61
Q

List some long-acting, non-depolarizing, neuromuscular agents

A

d-tubocurarine
Pancuronium
Doxacurium
Pipecuronium

62
Q

List some depolarizing, neuromuscular agents

A

Suxamethonium (Succinylcholine)

Decamethonium (C-10)

63
Q

What is the structural configuration of the Nm receptor❓

How do the antagonists function❓

A

1.
Macroprotein

5 subunits arranged like a rosette around Na+ channel

2alpha subunits carry 2Ach binding sites w -ve charged groups which combine w cationic group of Ach and open Na+ channel

  1. Competitive blockers have 2 or more quaternary N+ atoms which are attracted to same site as Ach

🚫intrinsic activity

64
Q

Succinylcholine and decamethonium have affinity and intrinsic activity at the Nm Ach receptors

True or false❓
How do they function❓

A

True

Prolonged depolarization of muscle end plates by opening Na+ channels

65
Q

The Phase I block of depolarizing Nm agents involves❓

A

Persistent depolarization of muscular end plate

Rapid onset

66
Q

The Phase II block of depolarizing Nm agents involves❓

A

Desensitization of Nm receptor to Ach

Slow onset

67
Q

What are the actions of Nm blockers on skeletal muscles❓

A

Weak muscles
Flaccid paralysis

In order of:
Fingers, intraocular muscles 
⬇️
Hands, feet, arm, leg 
⬇️
Neck, face
⬇️
Trunk, intercoastal muscles
⬇️
Diaphragm, respiration stops

Recovery in reverse direction

68
Q

Tubocurarine, a Nm blocker, may significantly ⬇️BP and sometimes, tachycardia

True or false

A

True

69
Q

SCh may initially produce bradycardia due to activation of vagal ganglia, followed by tachycardia and rise in BP

True or false

A

True

70
Q

How are Nm competitive blockers applied in GI surgeries❓

A

Ganglion blocking action of competitive agents may enhance postoperative paralytic ileus after abdominal operations

71
Q

Nm blockers are quaternary hydrophilic and ionized compounds

True or false

A

True

72
Q

Nm blockers are not well absorbed in GIT, do not cross placenta and BBB

True or false

A

True

73
Q

What would you consider the most important use Nm blockers❓

A

Adjuvant drugs in general anaesthesia

74
Q

SCh is employed for brief procedures

True or false

Give a few examples

A

True

Endotracheal intubation 
Laryngoscopy 
Bronchoscopy 
Esophagoscopy
Reduction of fractures/dislocations
75
Q

Using atropine to treat early mushroom poisoning can be contraindicated in which species❓

Why❓

A

Amanita muscarina

76
Q

Atropine is a plant extract from❓

Hyosine is a plant extract from❓

Curare is a plant extract from❓

A

Atropa belladona/Deadly night shade
Datura stramonium/Jimson weed

Hyoscyamus niger/ Henbane

Chondrodendron tomentosum
Strychnos toxifera

77
Q

How is SCh metabolized❓

A

SCh

⬇️plasma pseudocholinestase

Succinymonocholine

⬇️

Succinic acid + choline

78
Q

List a few uses of competitive Nm blockers

A

General anesthesia

Abdominal and thoracic surgery intubations

Endoscopies

Orthopedic procedures

🚫Convulsions and trauma from electroconvulsive therapy

Severe tetanus and status epileptucs

79
Q

You should expect competitive drug interactions when you administer Nm blockers with what drugs❓

A

Aminoglycosides

Hypokalemic diuretics

80
Q

List some drugs that can reverse the action of competitive Nm blockers

A

Neostigmine
Galantamine

Aminopyridine (Pymadine®️)

81
Q

What drugs will potentiate the action of both depolarizing and nondepolarizing Nm agents❓

A

Calcium channel blockers

82
Q

Sympathomimetics (adrenaline etc) ⬇️competitive block by ⬆️Ach release

True or false

A

True

83
Q

What are the clinical features you’ll observe in SCh toxicity❓

A

Cardiac arrhythmias

Prolonged apnoea

Malignant hyperthermia

Pharmacology (10 decks)

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