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Biomedical Pharmacology > Lecture 13 - Respiratory Pharmacology > Flashcards

Lecture 13 - Respiratory Pharmacology Flashcards

1
Q

What phases does asthma have?

A

Early and late phases

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2
Q

What is asthma characterised by?

A

Airway Inflammation
Bronchial hyper-reactivity
Reversible airway obstruction

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3
Q

When is asthma observed as reversible?

A

Once allergens that are responsible for reaction has been removed

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4
Q

What can degree of obstruction be monitored by?

A

Spirometry (lung function)

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5
Q

What is FEV1?

A

Forced expiratory volume in 1 second

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6
Q

What is FVC?

A

Forced vital capacity

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7
Q

What is the equation for spirometry?

A

FEV1/FVC

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8
Q

What is PEFR?

A

Peak expiratory flow rate

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9
Q

What is bronchospasm?

A

Smooth muscle constriction

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10
Q

When does late phase occur?

A

After immediate phase because of certain mediators that are generated and released during the immediate phase

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11
Q

Immediate phase of asthmatic attack

A

Occurs abruptly
Caused by spasm of bronchial smooth muscle
Allergen interaction with mast cell-fixed IgE cause release of histamine, leukotriene B4 and prostaglandin

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12
Q

What are other mediators of immediate phase?

A 
IL-4
IL-5
IL-13
Macrophage inflammatory protein-1alpha 
Tumour necrosis factor TNA-alpha
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13
Q

When the allergens are inhaled what does it cause?

A

Mast cell degranulation

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14
Q

How do you relieve smooth muscle constriction?

A

Beta-2 adrenoceptor agonist

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15
Q

What does inflammatory cell include?

A

Activated eosinophils

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16
Q

What does activated eosinophils release?

A 
Cysteinyl leukotrienes 
Interleukin IL-3
IL-5
IL-8
Toxic proteins (eosinophil cationic protein)
Major basic protein 
Eosinophil derived neurotoxin
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17
Q

What can late phase be inhibited by?

A

Glucocorticoids

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18
Q

What is Glucocorticoid and what does it do?

A

Steroid hormone

Interrupt the link between T helper cells and accumulation of eosinophils

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19
Q

What is the long term effect of changes occurring in the bronchioles?

A

Hypertrophied smooth muscle

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20
Q

What is hypertrophied smooth muscle?

A

Changes in the smooth muscles which make it more reactive/liable to reduce the diameter of the bronchioles

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21
Q

What is an example of changes to be lining of bronchioles?

A

Thickened basement membrane

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22
Q

What formation is seen during asthma attack?

A

Formation of mucus plug with eosinophils and desquamated epithelial cells
Further restrict the flow of air through the bronchioles

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23
Q

What are the main drugs used for bronchodilators?

A

B2-adrenoceptor agonist

Theophylline

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24
Q

What are examples of bronchodilators?

A

Cysteinyl leukotriene receptor antagonist

Muscarinic receptor antagonist

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25
Q

What does bronchodilators do?

A

Reverse the bronchospasm of the immediate phase

26
Q

What are anti-inflammatories and what do they do?

A

Steroids

Inhibit or prevent the inflammatory components of both phases

27
Q

What is step 1 of the stepwise approach ?

A

Mild intermittent asthma

Inhaled short-acting B2 agonist as required

28
Q

What is step 2 of stepwise approach?

A

Regulator preventer therapy
Add inhAled corticosteroid 200-800 micrograms/day
400 micrograms are an appropriate starting dose for many patients
Start at dose of inhaled corticosteroid appropriate to severity of disease

29
Q

What is step 3 of step wise approach?

A

Add inhaled long-acting B2 agonist (LABA)

30
Q

What is step 4 of step wise approach?

A

Persistent poor control
Increase inhaled corticosteroid up to 2,000 micrograms/day
Addition of 4th drug e.g. leukotriene receptor antagonist
SA theophylline, B2 agonist tablet

31
Q

What is step 5 of stepwise approach?

A

Continuous or frequent use of oral steroids
Use daily steroid tablet in lowest dose providing adequate control
Maintain high dose inhaled corticosteroid at 2,000 micrograms/day
Refer patients for specialist care

32
Q

What are examples of short-acting (5 hours) of B2-Adrenoceptor agonist?

A

Salbutamol
Terbutaline
Given as needed

33
Q

What are examples of long-acting (12 hours) of B2-adrenoceptor agonist?

A

Salmeterol
Formoterol
Given as adjunct to other treatment/prophylactically

34
Q

What is the administration for B2-adrenoceptor agonist?

A

Inhalation
Metered dose inhalers
Spacers
Nebulisers

35
Q

How is the duration of action for B2-adrenoceptor agonist prolonged?

A

Incorporation of lipophilic side-chain which bonds to area adjacent to receptor active site

36
Q

What does formoterol enter?

A

Lipid bilayer

37
Q

How are short acting compounds administered (B2-adrenoceptor agonist)?

A

Orally
Subcutaneously
IntrVenously

38
Q

What can B-adrenoceptor stimulation lead to?

A 
Tremor 
Tachycardia, arrythmia 
Acute metabolic response 
Paradoxical bronchospam 
Headache
39
Q

Membrane phospholipid

A

Generation of inflammatory mediators through action of enzyme: phospholipase A2 and cyclo-oxygenase

40
Q

PGE2

A

Potent vasodilator

41
Q

LTBB4

A

Potent chemotaxin

42
Q

When is corticosteroid introduced?

A

Using bronchodilator more than once daily

43
Q

What is corticosteroid skewed to?

A 
Glucocorticoid action 
Beclometasone
Budesonide 
Fluticasone
Mometasone
Cuclesonide 
Prednisone
44
Q

What are the actions of corticosteroid?

A 
Decrease cytokines formation 
Inhibit production of leukotriene 
Inhibit allergen-induces influx of eosinophils into lung 
Upregulate B2-adrenoceptors
Decrease microvascular permeability 
Reduce mast cell number
45
Q

What are unwanted effects of corticosteroid?

A

Limited by route of administration
Oropharyngeal thrush
Sore throat
Adrenal suppression

46
Q

What are 3 types of Muscarinic receptor associated with airway function?

47
Q

M1

A

Facilitate parasympathetic Ganglia transmission

48
Q

M2

A

Presynaptic inhibitory auto receptors

49
Q

M3

A

Postsynaptic
Mediate bronchoconstriction
Mucus secretion - generation of CGMP

50
Q

How are antimuscarinic compound administered?

A

Inhalational route

51
Q

Ipratropium

A

Short acting

52
Q

Tiotropium

53
Q

What are antimuscarinic compound use for?

A

Reduced secretion

Increase clearance

54
Q

What are side effects of antimuscarinic compounds?

A

Dry mouth
Constipation
Contribute to glaucoma

55
Q

Methylxanthenes

A

Theophylline and related derogate aminophylline

56
Q

What are multiple actions of methylxanthene?

A

Phosphodiesterase inhibition
Increased contraction of diaphragm
Adenosine receptor antagonism
Activation of histone deacetylsse

57
Q

What are unwanted effect of methylxanthene

A

Hypotension

CNS and GI disturbance

58
Q

Metyhlxanthene

A

Metabolised by CYP3A4

Low TI

59
Q

Leukotriene receptor antagonist

A

Monteluklast
Oral agents with additive affect when given with corticosteroid
Inhibit early and late stage bronchoconstriction

60
Q

Status asthmaticus

A 
Medical emergency - prompt attention 
High conc oxygen 
Use of nebuliser to deliver salbutamol 
IV corticosteroid, e.g hydrocortisone 
Oral prednisolone
61
Q

How is status asthmaticus monitored by?

A

Spirometry

Blood gas

Biomedical Pharmacology (19 decks)

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