Pharmacology > Anticholinergics > Flashcards

Anticholinergics Flashcards

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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
There are drugs that aren’t antimuscarinics with antimuscarinic properties. Do you know any❓
Antihistamines Tricyclic antidepressants
26
What effects will pharmacological doses of atropine cause❓ What effects will high doses of atropine cause❓
✅ CNS excitation ⬆️ Restlessness Hallucinations Delirium Respiratory depression Coma
27
What effects will pharmacological doses of hyoscine cause❓ What effects will high doses of hyoscine cause❓
``` ✅ CNS depression: Drowsiness Amnesia Fatigue Dreamless sleep ``` ``` ⬆️ CNS excitation: Restlessness Hallucinations Delirium ``` Used in preventing motion sickness
28
“Twilight sleep” is induced by ______ What is it’s application❓
Hyoscine Truth serum for crime suspects
29
How would you apply the antiemetic properties of hyosine❓
Used to preventing motion sickness: transdermal patch placed behind pinna
30
What are the effects of anticholinergic drugs on the eye❓
Mydriasis (relaxation of cilliary muscle) Photophobia Cycloplegia ⬆️Intraocular tension ⬇️Lacrimal secretion (dry/sandy eyes)
31
How do antimuscarinics cause cycloplegia?
``` Paralysis of cilliary eye muscles ⬇️ 🚫of accommodation ⬇️ Focused for far vision ```
32
Which antimuscarinic would you use to treat iritis, choroiditis, keratitis and corneal ulcers❓ Why❓
Atropine It has a long lasting mydriatic-cycloplegic and local anodyne action on the cornea
33
Antimuscarinics should be carefully administered in patients with glaucoma. Why❓ Why is this significant❓
1. Antimuscarinics ⬇️ Relaxation of ciliary muscle ⬇️ Obstruction of drainage of aqueous humor ⬇️ ⬆️IOP 2. 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
34
Tropicamide is a short acting antimuscarinic commonly used in eye exams True or false
True
35
What are the effects of anticholinergic drugs on the CVS❓ What CVS conditions are they useful in treating❓
1. ⬆️HR/Tachycardia 2. Digitalis-induced bradycardia Arrhythmias due to AV node
36
What are the effects of anticholinergic drugs on the respiratory system❓ What conditions are they useful in treating❓
``` 1. Inhibition of M3 receptors ⬇️secretion ⬇️ reflex bronchspasm ⬇️Bronchoconstriction ``` 2. Tx of bronchial asthma Tx of COPD Pre-anaesthetic mdx
37
What anticholinergic drugs would you administer to threat bronchial asthma or COPD❓
Ipratropium (non selective) Tiotropium (M1 and M3 receptors)
38
Which anticholinergic drug is most suitable for pre-anaesthetic mdx to ⬇️secretions and reflex bronchospasm ❓
Glycopyrolate
39
What are the effects of anticholinergic drugs on the GIT❓ What conditions are they useful in treating❓
1. ⬇️Motility ⬇️Secretions 2. Peptic ulcer disease Intestinal colic (anti-spasmodic agents) Irritable bowel syndrome Urinary incontinence/Overactive bladder
40
What antimuscarinic drugs would you use in treating peptic ulcer disease❓ Why❓
Pirenzepine Telenzepine Selective M1 blockers
41
What anticholinergic drugs would you use in treating intestinal colic❓
Hyoscine Dicyclomine Propantheline Oxyphenonium Clidinium
42
What antimuscarinic drugs would you use in treating irritable bowel syndrome❓ Why❓
Darifenacin Solefenacin Selective M3 blockers
43
If you had to manage a case of an overactive bladder or urinary incontinence, what drugs would you prescribe to your pt❓
Solefenacin Oxybutynin Flavoxate, Fesoterodine Tolterodine, Trospium Darifenacin SOFT blad-DER
44
Anticholinergic drugs: ⬇️secretions Cause dry mouth ⬇️sweating ⬇️salivation What is the significance on this in terms of pediatrics❓
Atropine is contraindicated in children b/c of the risk of hyperthermia (due to ⬇️sweating)
45
Is there any anticholinergic that may be useful in poisoning cases❓
Atropine for early mushroom poisoning from Inocybe species
46
List a few adverse effects of anticholinergic drugs you know
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
What are the clinical presentations in atropine overdose❓
Palpitation Weak, rapid pulse CVS collapse Respiratory depression ``` Excitement Psychotic behavior Ataxia Delirium Hallucinations Convulsions Coma ```
48
How would you make a confirmatory diagnosis if you’re suspecting a case of atropine overdose❓
1mg neostigmine 🚫typical muscarinic effects
49
How would you treat atropine overdose❓
Put pt in dark, quiet room Tannic acid for gastric lavage 1-3mg Galantamine/Physostigmine (SC or IV) Diazepam against convulsion
50
What effect will anticholinergics (atropine) have on absorption of some drugs❓ Will drug doses ⬆️/⬇️
Slowness of absorbtion b/c of slow gastric emptying ⬆️Drug doses in circulation
51
Anticholinergics will cause slow absorption of most List some drugs that will be well absorbed
Digoxin | Tetracyclines (⬆️absorption)
52
Antacids interfere with absorption of cholinergics True or false
True
53
Would an administration of antihistamines/tricyclic antidepressants or phenothiazine with anticholinergics increase or reduce the risk of additives side effects❓
⬆️risk of side effects b/c antihistamines/tricyclic antidepressants/phenothiazines have anticholinergic properties
54
MAO inhibitors will interfere with the metabolism of antiparkinsonian drugs True or false Give an example
True Biperiden; derilium may occur
55
If you had to undergo a dental prodecure and you needed to give an antisialogogue, what drug would you administer❓
Atropine sulphate tablet, 1hr before appointment
56
Conditions like xerostomia may increase incidence of caries glossitis if atropine is administered True or false
True
57
Ganglion blockers have many side effects and their clinical use is out of date Give a few examples
Hexamethonium Trimethaphan Mecamylamine
58
Neuromuscular blocking agents can be divided into
Nondepolarizing/Competitive blockers/Curare-like drugs Depolarising/Hyperpolarizing agents
59
List some short-acting, non-depolarizing, neuromuscular agents
Mivacurium
60
List some intermediate-acting, non-depolarizing, neuromuscular agents
Atracurium | Vecuronium
61
List some long-acting, non-depolarizing, neuromuscular agents
d-tubocurarine Pancuronium Doxacurium Pipecuronium
62
List some depolarizing, neuromuscular agents
Suxamethonium (Succinylcholine) Decamethonium (C-10)
63
What is the structural configuration of the Nm receptor❓ How do the antagonists function❓
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 2. Competitive blockers have 2 or more quaternary N+ atoms which are attracted to same site as Ach 🚫intrinsic activity
64
Succinylcholine and decamethonium have affinity and intrinsic activity at the Nm Ach receptors True or false❓ How do they function❓
True Prolonged depolarization of muscle end plates by opening Na+ channels
65
The Phase I block of depolarizing Nm agents involves❓
Persistent depolarization of muscular end plate Rapid onset
66
The Phase II block of depolarizing Nm agents involves❓
Desensitization of Nm receptor to Ach Slow onset
67
What are the actions of Nm blockers on skeletal muscles❓
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
Tubocurarine, a Nm blocker, may significantly ⬇️BP and sometimes, tachycardia True or false
True
69
SCh may initially produce bradycardia due to activation of vagal ganglia, followed by tachycardia and rise in BP True or false
True
70
How are Nm competitive blockers applied in GI surgeries❓
Ganglion blocking action of competitive agents may enhance postoperative paralytic ileus after abdominal operations
71
Nm blockers are quaternary hydrophilic and ionized compounds True or false
True
72
Nm blockers are not well absorbed in GIT, do not cross placenta and BBB True or false
True
73
What would you consider the most important use Nm blockers❓
Adjuvant drugs in general anaesthesia
74
SCh is employed for brief procedures True or false Give a few examples
True ``` Endotracheal intubation Laryngoscopy Bronchoscopy Esophagoscopy Reduction of fractures/dislocations ```
75
Using atropine to treat early mushroom poisoning can be contraindicated in which species❓ Why❓
Amanita muscarina
76
Atropine is a plant extract from❓ Hyosine is a plant extract from❓ Curare is a plant extract from❓
Atropa belladona/Deadly night shade Datura stramonium/Jimson weed Hyoscyamus niger/ Henbane Chondrodendron tomentosum Strychnos toxifera
77
How is SCh metabolized❓
SCh ⬇️plasma pseudocholinestase Succinymonocholine ⬇️ Succinic acid + choline
78
List a few uses of competitive Nm blockers
General anesthesia Abdominal and thoracic surgery intubations Endoscopies Orthopedic procedures 🚫Convulsions and trauma from electroconvulsive therapy Severe tetanus and status epileptucs
79
You should expect competitive drug interactions when you administer Nm blockers with what drugs❓
Aminoglycosides Hypokalemic diuretics
80
List some drugs that can reverse the action of competitive Nm blockers
Neostigmine Galantamine Aminopyridine (Pymadine®️)
81
What drugs will potentiate the action of both depolarizing and nondepolarizing Nm agents❓
Calcium channel blockers
82
Sympathomimetics (adrenaline etc) ⬇️competitive block by ⬆️Ach release True or false
True
83
What are the clinical features you’ll observe in SCh toxicity❓
Cardiac arrhythmias Prolonged apnoea Malignant hyperthermia
Pharmacology
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