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DEN 2026 - Pharmacology > Pharmacology of the Airways > Flashcards

Pharmacology of the Airways Flashcards

1
Q

What nervous system predominates in the control of airway smooth muscle?

A

Parasympathetic

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2
Q

How does the parasympathetic nervous system cause bronchoconstriction?

A

Acetylcholine acting on muscarinic M3 receptor

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3
Q

Describe how the sympathetic nerves affect the control of airway smooth muscle tone

A
  • Innervate blood vessels and glands
  • Can inhibit parasympathetic ganglia to prevent acetylcholine release
  • Adrenaline inhibits release of mediators from mast and mucocilliary cells
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4
Q

Name 2 chemicals which relax airway smooth muscle

A
  1. VIP

2. Nitrous oxide

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5
Q

Name 2 chemicals which constrict airway smooth muscle

A
  1. Substance P

2. Neurokinin

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6
Q

What is bronchial asthma?

A

Chronic inflammatory disease of airways that causes acute bronchospasm

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7
Q

Describe the events in asthma from chronic inflammation to acute bronchospasm

A
  • Chronic inflammatory response
  • Mast cell and eosinophil mediator release
  • Damage to epithelial layer / increased irritability
  • Acute bronchospasm
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8
Q

Name 2 symptoms of asthma which accompany bronchospasm

A
  1. Mucous secretion

2. Blood vessel leak

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9
Q

What are 2 influences leading to an asthma attack asthma?

A
  1. Genetic predisposition (hyper-reactive airways)

2. Environmental exposure (trigger)

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10
Q

Name 5 examples of asthma attack triggers

A
  1. Upper RTIs
  2. Allergens (dust, fur)
  3. Irritants (smoke)
  4. Medication
  5. Exercise
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11
Q

Name a medicine which can cause asthma attacks

A

Aspirin

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12
Q

How can aspirin cause an asthma attack?

A
  • Inhibits prostaglandin synthesis from leukotriene
  • Increases leukotriene levels in body
  • Leukotriene can act as an irritant
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13
Q

Name 2 phases of an asthma attack

A
  1. Immediate phase (response to triggers)

2. Delayed phase

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14
Q

Name 2 chemicals released during the immediate phase of an asthma attack

A
  1. Spasmogens

2. Chemotaxins

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15
Q

Name 4 spasmogens released during an asthma attack

A
  1. Acetylcholine
  2. Histamine
  3. LTC₄
  4. D₄
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16
Q

Name 3 physiological symptoms of the release of spasmogens

A
  1. Wheezing
  2. Coughing
  3. Bronchospasm
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17
Q

Name 2 chemotaxins released during an asthma attack

A
  1. LTB₄

2. Cytokines

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18
Q

What is the physiological outcome of the release of chemotaxins during an asthma attack?

A

Influx of inflammatory cells

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19
Q

What 2 physiological processes occur during the delayed phase of an asthma attack?

A
  1. Activation of inflammatory cells

2. Mediator release

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20
Q

Name 2 main classes of drug which are used to treat asthma

A
  1. Bronchodilators (treat wheezing)

2. Anti-Inflammatory drugs (prophylactic drugs)

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21
Q

Name 4 types of bronchodilators

A
  1. β₂ adrenoceptor agonists
  2. Muscarinic antagonists
  3. Leukotriene antagonists
  4. Xanthines
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22
Q

Name 2 examples of short acting β₂ adrenoceptor agonists

A
  1. Salbutamol

2. Terbutaline

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23
Q

Name an example of a long acting β₂ adrenoceptor agonist

A

Salmeterol

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24
Q

What is the mode of action of β₂ adrenoceptor agonists

A
  • Agonises β₂ adrenoceptor
  • G protein produces cAMP as a second messenger
  • cAMP-dependent protein kinase becomes activated
  • Proteins phosphorylation causes bronchodilation
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25
Q

Describe how β₂ adrenoceptor agonists are usually administered?

A

Inhalation as reduces systemic dose (side-effects) but retains effectiveness

26
Q

Name 3 additional benefits of β₂ adrenoceptor agonists other than bronchodilation

A
  1. Reduce mast cell mediator release
  2. Inhibit vagal tone
  3. Promote mucous clearance
27
Q

Name 5 adverse effects of β₂ adrenoceptor agonists

A
  1. Muscle tremor
  2. Hypokalaemia
  3. Tachycardia
  4. Arrhythmias
  5. Tolerance
28
Q

Why does tolerance develop for β₂ adrenoceptor agonists?

A

Excessive use causes downregulation of β₂ adrenoceptors in the airway so there is a less marked dilatory effect

29
Q

How does muscarinic antagonists function?

A

Block bronchoconstrictor and mucus-secreting effects of parasympathetic neurotransmitter acetylcholine mediated via muscarinic M3 receptors

30
Q

What types of bronchospasm are muscarinic antagonists particularly effective for?

A

Bronchospasm induced by irritant stimuli

31
Q

Describe 2 second messengers present in PLC-β signalling pathway

A
  • PR3 causes increased calcium release from sarcoplasmic reticulum
  • DAG activates protein kinase C which phosphorylates proteins which modifies calcium handling
32
Q

Name a short acting muscarinic antagonist

A

Ipratropium bromide

33
Q

Name an established long acting muscarinic antagonist

A

Tiotropium bromide

34
Q

Name 3 newer long acting muscarinic antagonist

A
  1. Umeclidinium
  2. Aclidinium
  3. Glycopyrronium
35
Q

How are muscarinic antagonists usually administered?

A

Inhalation as reduces systemic dose (side-effects) but retains effectiveness

36
Q

Name 4 side effects of muscarinic antagonists

A
  1. Dry mouth
  2. Constipation
  3. Urinary retention
  4. Blurred vision
37
Q

Name a drug which is a leukotriene synthesis inhibitor

A

Zileuton

38
Q

Name 3 targets of zileuton

A
  1. LTB₄
  2. LTC₄
  3. D₄
39
Q

Name a drug which acts as cysLT₁ receptor antagonist

A

Montelukast

40
Q

Name 3 specific types of asthma drugs targeting leukotrienes are useful

A
  1. Exercise induced asthma
  2. Aspirin induced asthma
  3. Responses to inhaled allergens
41
Q

Name 3 side effects of drugs targeting leukotrienes

A
  1. Headache
  2. GI upset
  3. Abdominal pain
  4. Churg-Strauss syndrome (rare)
42
Q

Name an example of a xanthine drug

A

Theophylline

43
Q

What is theophylline used for?

A

Reserve drug for difficult to control patients who do not respond adequately to β₂ agonists

44
Q

Name 2 ways which theophylline may be administered

A
  1. Orally

2. Slow IV infusion

45
Q

Describe the mode of action of theophylline

A
  • Inhibits cyclic nucleotide phosphodiesterase
  • Prevents hydrolysis of cyclic ring in cAMP
  • Higher levels of cAMP persist for longer in cytoplasm
  • Prolongation of cAMP-dependent signalling
46
Q

Name 4 useful effects of theophylline

A
  1. Relaxes bronchial smooth muscle
  2. Some anti-inflammatory effects
  3. Stimulates respiratory centre in brain
  4. Prevents diaphragm fatigue
47
Q

What is a major consideration for a person prescribed theophylline?

A

Narrow therapeutic window means plasma concentrations must be monitored

48
Q

What 3 types of drugs regularly used to prevent inflammation during prophylactic treatment for asthma?

A
  1. Glucocorticosteroids
  2. Xanthines
  3. Drugs targeting leukotrienes
49
Q

Name 2 drugs used rarely in to prevent inflammation during prophylactic treatment for asthma?

A
  1. Cromolyn sodium

2. Nedocromil sodium

50
Q

Name a type of drug used to resolve established inflammation during anti-inflammatory treatment for asthma?

A

Glucocorticosteroids

51
Q

Name 3 inhaled glucocorticosteroids

A
  1. Beclometasone
  2. Budasonide
  3. Fluticasone
52
Q

Name an oral glucocorticosteroid

A

Prednisolone

53
Q

Name an intravenous glucocorticosteroid

A

Hydrocortisone

54
Q

How do glucocorticosteroid function?

A

Increase β₂ receptor expression / response

55
Q

Name 4 types of molecules inhibited by inhaled corticosteroids leading to the reduction of inflammation

A
  1. Cytokines
  2. Enzymes
  3. Peptides
  4. Adhesion molecules
56
Q

Name 3 ways corticosteroids reduce inflammation

A
  1. Reduce chemotaxins
  2. Reduce synthesis of spasmogenic mediators
  3. Reduce endothelium prostaglandin release
57
Q

Name 2 side effects of corticosteriods

A
  1. Oropharyngeal candidiasis

2. Sore throat

58
Q

Name 4 possible systemic side effects on prolonged exposure to excessive levels of glucocorticosteroids

A
  1. Hyperglycaemia
  2. Hypertension
  3. Cushing’s like syndrome
  4. Tanning of skin
59
Q

Describe the weak anti-inflammatory action of cromolyn sodium and nedocromil sodium

A
  • Mast cell stabilisation
  • Reduce inflammatory cell recruitment
  • Blunted neuronal irritant reflexes
60
Q

Name 3 side effects of cromolyn sodium and nedocromil sodium

A
  1. Cough
  2. Throat irritation
  3. Paradoxical bronchospasm
61
Q

What can be given to a person suffering severe exacerbation?

A

Bronchodilators administered by oxygen-driven nebuliser

DEN 2026 - Pharmacology (22 decks)

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