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Y1 RESPIRATORY > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Sympathetic adrenergic innervation of the airways is the dominant neuronal control of bronchial smooth muscle. True/False?

A

False

Parasympathetic cholinergic innervation dominates the airways

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2
Q

Stimulation of parasympathetic division causes bronchial smooth muscle _____, mediated by __ acting on __ receptors

A

Contraction, ACh, M3

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3
Q

Mucus secretion is increased when parasympathetic division is active. True/False?

A

True

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4
Q

There is no sympathetic innervation of bronchial smooth muscle. True/False?

A

True

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5
Q

What do postganglionic sympathetic fibres supply with regards to airways?

A

Submucosal glands

Smooth muscle of blood vessels

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6
Q

Stimulation of sympathetic division causes bronchial smooth muscle _____, mediated by __ released from the ___ ___ acting on __ receptors

A

Relaxation, adrenaline, adrenal gland, B2

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7
Q

Mucus secretion is increased when sympathetic division is active. True/False?

A

False

Mucus secretion decreases; mucociliary elevator activity increases

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8
Q

Asthma is irreversible obstruction of small airways. True/False?

A

False

It is reversible

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9
Q

What are the pathological changes that may occur in chronic asthma?

A

Increased mass of smooth muscle
Accumulation of interstitial fluid
Increased mucus secretion
Epithelial damage

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10
Q

FEV1 and PEFR increase in asthma sufferers. True/False?

A

False

They both decrease

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11
Q

What causes hypersensitivity of airways in asthma?

A

Epithelial damage, exposing sensory nerve endings

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12
Q

What are the 2 components of an asthma attack?

A

Initial bronchospasm followed by late inflammation

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13
Q

In non-atopic individuals, THo cells mature into TH_ cells

A

TH1

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14
Q

TH1 suppresses the production of which TH cell?

A

TH2

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15
Q

In atopic individuals, THo cells mature into TH_ cells

A

TH2

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16
Q

TH2 suppresses the production of which TH cell?

A

TH1

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17
Q

Which interleukin helps/allows TH2 cells to activate B cells?

A

IL-4

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18
Q

Activated B cells can mature into plasma cells which secrete __ in the allergic response

A

IgE

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19
Q

IgE binds to eosinophils and mast cells via which receptor?

A

FcE

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20
Q

Which interleukin causes eosinophils to differentiate and activate?

A

IL-5

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21
Q

Which interleukins cause mast cells to express IgE receptors?

A

IL-4 and IL-13

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22
Q

When mast cells are activated, which substances do they release?

A

Histamine
Chemokines
Leukotrienes

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23
Q

Relievers act as anti-inflammatory agents. True/False?

A

False

They are bronchodilators used for acute attacks

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24
Q

Name the 3 main types of relievers used in asthma

A

SABAs, LABAs, CysLT antagonists

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25
Q

Name controllers/preventers used in asthma

A

Glucocorticoids, chromoglicate

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26
Q

What does PKA do in bronchial smooth muscle?

A

Phosphorylates MLCK and B2 receptors

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27
Q

MLCK’s action is to cause relaxation of bronchial smooth muscle. True/False?

A

False

Action is to cause contraction; phosphorylation by PKA inhibits this action to cause relaxation

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28
Q

How does PKA cause desensitisation of B2 receptors?

A

Phosphorylates the receptor, causing reduced G-protein coupling

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29
Q

B2 receptor can be phosphorylated by PKA when no agonist is bound. True/False?

A

True

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30
Q

B2 receptor can be phosphorylated by GRK when no agonist is bound. True/False?

A

FalseAgonist must be bound

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31
Q

Give an example of a SABA

A

Salbutamol

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32
Q

SABAs are usally administered via the _____ route. Why?

A

Inhalational

Reduces systemic effects

33
Q

Give an example of a LABA

A

Salmeterol

34
Q

LABAs are recommended for acute relief of bronchospasm. True/False

A

False

They are slow to act

35
Q

LABAs can be used as a monotherapy. True/False?

A

False

They would desensitise receptors

36
Q

CysLT1 receptor activation causes bronchodilation. True/False?

A

False

Causes bronchoconstriction and inflammation

37
Q

Give an example of a CysLT antagonist?

A

Montelukast

38
Q

CysLT antagonists are less potent than salbutamol in acute asthma. True/False?

A

True

39
Q

How are CysLT antagonists administered (which route)?

A

Oral

40
Q

How do Xanthines work? Give an example of a Xanthine?

A

Inhibit PDE3 allowing action of cAMP in ASM

Theophylline
Aminophylline

41
Q

Xanthines have little adverse effects. True/False?

A

False

Nausea, vomiting, headache are some of the side effects

42
Q

What are the 2 main classes of corticosteroid released by the adrenal cortex?

A

Glucocorticoids

Mineralocorticoids

43
Q

What is the effect of cortisol on inflammatory responses?

A

Decreases them

44
Q

What is the effect of cortisol on gluconeogenesis?

A

Increases it

45
Q

What is the function of mineralocorticoids?

A

Regulate salt and water retention by the kidney

46
Q

Glucocorticoids have good bronchodilator action. True/False?

A

False

47
Q

How do glucocorticoids enter cells?

A

Diffusion - they are lipophilic

48
Q

Glucocorticoids combine with GRa which causes dissociation of which class of proteins?

A

HSP (heat shock proteins)

49
Q

Glucocorticoids stimulate production of proteins which suppress inflammation. True/False?

A

True

Also decrease production of proteins which stimulate inflammation

50
Q

Expression of inflammatory genes is associated with the acetylation of histones by which enzyme?

A

Histone Acetyltransferases (HATs)

51
Q

What does acetylation do to DNA?

A

Unwinds it, enabling transcription to occur

52
Q

What are some cellular effects of glucocorticoids in asthma?

A

Decrease numbers of eosinophils, mast cells, T cells, macrophages
Increase expression of B2 receptors

53
Q

Give an example of a glucocorticoid used in asthma and its adverse effects

A

Inhaled beclomethasone
Hoarse voice + oral thrush
Also oral prednisolone in combination for severe asthma

54
Q

COPD can be divided into which 2 disease states?

A

Chronic bronchitis

Emphysema

55
Q

Describe chronic bronchitis and its symptoms

A

Inflammation of bronchi + bronchioles

Causes cough + purulent sputum

56
Q

Describe emphysema and its symptoms

A

Collapse of alveoli, decreasing SA available for gas exchange
Breathlessness

57
Q

What is the function of M1 receptors at ganglia?

A

Facilitate neurotransmission mediated by ACh acting on nicotinic receptors

58
Q

What is the function of M2 receptors on the post-ganglionic neurone?

A

Inhibit further release of ACh

59
Q

What is the function of M3 receptors in smooth muscle? What drug are they blocked by?

A

Mediate contraction + increased mucous secretion in response to ACh stimulation
Muscarinic antagonists

60
Q

Give an example of a SAMA

A

Ipratropium

61
Q

Give an example of a LAMA

A

Tiotropium

62
Q

Ipratropium is a selective blocker of M3 receptors. True/False?

A

False

Tiotropium is a selective blocker of M3; ipratropium is non-selective

63
Q

Why is block of M2 receptors undesirable?

A

M2 receptor normal function is to inhibit ACh release. If this is blocked, more ACh will be released which will ultimately cause more contraction

64
Q

What is Indacaterol?

A

An “ultra-LABA” which has rapid onset of action (vs salmeterol)

65
Q

A combination of LABA + LAMA is not recommended. True/False?

A

False

This combination is superior to using each drug alone in increasing FEV1

66
Q

What is the function of a PDE4 antagonist? Give an example of one

A

Inhibits inflammation caused by PDE4 released by neutrophils

Rofumilast - oral for severe COPD

67
Q

What is rhinitis and its symptoms?

A

Inflammation of nasal mucosa - divided into allergic, non-allergic and mixed
Typically rhinorrhoea, sneezing, itching, nasal congestion

68
Q

What is non-allergic rhinitis and its causes?

A

Rhinitis not involving IgE

Infection, drug-induced, hormonal e.g. pregnancy, idiopathic

69
Q

List drug classes that can be used for rhinitis

A

Glucocorticoids
H1 and cysLT1 receptor antagonists
Sodium chromoglicate

70
Q

Mechanism of action of H1 receptor antagonistsExamples

A

Reduce effects of histamine released from mast cellsGiven orally or nasal sprayLoratidine, fexofenadine, cetirizine

71
Q

Mechanism of action of sodium chromoglicate

A

Mast cell stabilisation (2nd line to CCS)

Nasal spray, usually better for children, used in asthma

72
Q

Describe the transduction pathway that regulates SM tone

A

Harmone activates GPCR. Ca moves out of SR and binds to voltage gated channel causing depolarisation. Activated MLCK phosphorylation myosin cross bridge which binds to actin. This generates a sliding force causing contraction.

73
Q

Dephosphorylation of MLC occurs via…

A

Myosin phosphatase

74
Q

List the main side effects of SABAs

A

Fine tremor
Tachycardia
Cardiac dysrhythmia
Hypokalaemia

75
Q

Give two examples of monoclonal anti-inflammatory drugs

A

Anti-IgE e.g. omalizumab

Anti-IL5 e.g. mepolizumab

76
Q

Explain the mechanism of action of bronchodilators

A

Stimulate bronchial SM B2 receptors to increase cAMP (SABA/ LABA)

77
Q

What class of drugs is used to reduce sputum viscosity and aid sputum expectoration? Give an example

A

Mucolytics

Carbocistein

78
Q

What class of drugs used in rhinitis activate a1 receptors? Give an example

A

Vasoconstrictors

Oxymetazoline

Y1 RESPIRATORY (12 decks)

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