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Y1 RESPIRATORY > Pharmacology > Flashcards

Pharmacology Flashcards

(78 cards)

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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
Name controllers/preventers used in asthma
Glucocorticoids, chromoglicate
26
What does PKA do in bronchial smooth muscle?
Phosphorylates MLCK and B2 receptors
27
MLCK's action is to cause relaxation of bronchial smooth muscle. True/False?
False | Action is to cause contraction; phosphorylation by PKA inhibits this action to cause relaxation
28
How does PKA cause desensitisation of B2 receptors?
Phosphorylates the receptor, causing reduced G-protein coupling
29
B2 receptor can be phosphorylated by PKA when no agonist is bound. True/False?
True
30
B2 receptor can be phosphorylated by GRK when no agonist is bound. True/False?
FalseAgonist must be bound
31
Give an example of a SABA
Salbutamol
32
SABAs are usally administered via the _____ route. Why?
Inhalational | Reduces systemic effects
33
Give an example of a LABA
Salmeterol
34
LABAs are recommended for acute relief of bronchospasm. True/False
False | They are slow to act
35
LABAs can be used as a monotherapy. True/False?
False | They would desensitise receptors
36
CysLT1 receptor activation causes bronchodilation. True/False?
False | Causes bronchoconstriction and inflammation
37
Give an example of a CysLT antagonist?
Montelukast
38
CysLT antagonists are less potent than salbutamol in acute asthma. True/False?
True
39
How are CysLT antagonists administered (which route)?
Oral
40
How do Xanthines work? Give an example of a Xanthine?
Inhibit PDE3 allowing action of cAMP in ASM Theophylline Aminophylline
41
Xanthines have little adverse effects. True/False?
False | Nausea, vomiting, headache are some of the side effects
42
What are the 2 main classes of corticosteroid released by the adrenal cortex?
Glucocorticoids | Mineralocorticoids
43
What is the effect of cortisol on inflammatory responses?
Decreases them
44
What is the effect of cortisol on gluconeogenesis?
Increases it
45
What is the function of mineralocorticoids?
Regulate salt and water retention by the kidney
46
Glucocorticoids have good bronchodilator action. True/False?
False
47
How do glucocorticoids enter cells?
Diffusion - they are lipophilic
48
Glucocorticoids combine with GRa which causes dissociation of which class of proteins?
HSP (heat shock proteins)
49
Glucocorticoids stimulate production of proteins which suppress inflammation. True/False?
True | Also decrease production of proteins which stimulate inflammation
50
Expression of inflammatory genes is associated with the acetylation of histones by which enzyme?
Histone Acetyltransferases (HATs)
51
What does acetylation do to DNA?
Unwinds it, enabling transcription to occur
52
What are some cellular effects of glucocorticoids in asthma?
Decrease numbers of eosinophils, mast cells, T cells, macrophages Increase expression of B2 receptors
53
Give an example of a glucocorticoid used in asthma and its adverse effects
Inhaled beclomethasone Hoarse voice + oral thrush Also oral prednisolone in combination for severe asthma
54
COPD can be divided into which 2 disease states?
Chronic bronchitis | Emphysema
55
Describe chronic bronchitis and its symptoms
Inflammation of bronchi + bronchioles | Causes cough + purulent sputum
56
Describe emphysema and its symptoms
Collapse of alveoli, decreasing SA available for gas exchange Breathlessness
57
What is the function of M1 receptors at ganglia?
Facilitate neurotransmission mediated by ACh acting on nicotinic receptors
58
What is the function of M2 receptors on the post-ganglionic neurone?
Inhibit further release of ACh
59
What is the function of M3 receptors in smooth muscle? What drug are they blocked by?
Mediate contraction + increased mucous secretion in response to ACh stimulation Muscarinic antagonists
60
Give an example of a SAMA
Ipratropium
61
Give an example of a LAMA
Tiotropium
62
Ipratropium is a selective blocker of M3 receptors. True/False?
False | Tiotropium is a selective blocker of M3; ipratropium is non-selective
63
Why is block of M2 receptors undesirable?
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
What is Indacaterol?
An "ultra-LABA" which has rapid onset of action (vs salmeterol)
65
A combination of LABA + LAMA is not recommended. True/False?
False | This combination is superior to using each drug alone in increasing FEV1
66
What is the function of a PDE4 antagonist? Give an example of one
Inhibits inflammation caused by PDE4 released by neutrophils | Rofumilast - oral for severe COPD
67
What is rhinitis and its symptoms?
Inflammation of nasal mucosa - divided into allergic, non-allergic and mixed Typically rhinorrhoea, sneezing, itching, nasal congestion
68
What is non-allergic rhinitis and its causes?
Rhinitis not involving IgE | Infection, drug-induced, hormonal e.g. pregnancy, idiopathic
69
List drug classes that can be used for rhinitis
Glucocorticoids H1 and cysLT1 receptor antagonists Sodium chromoglicate
70
Mechanism of action of H1 receptor antagonistsExamples
Reduce effects of histamine released from mast cellsGiven orally or nasal sprayLoratidine, fexofenadine, cetirizine
71
Mechanism of action of sodium chromoglicate
Mast cell stabilisation (2nd line to CCS) | Nasal spray, usually better for children, used in asthma
72
Describe the transduction pathway that regulates SM tone
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
Dephosphorylation of MLC occurs via...
Myosin phosphatase
74
List the main side effects of SABAs
Fine tremor Tachycardia Cardiac dysrhythmia Hypokalaemia
75
Give two examples of monoclonal anti-inflammatory drugs
Anti-IgE e.g. omalizumab | Anti-IL5 e.g. mepolizumab
76
Explain the mechanism of action of bronchodilators
Stimulate bronchial SM B2 receptors to increase cAMP (SABA/ LABA)
77
What class of drugs is used to reduce sputum viscosity and aid sputum expectoration? Give an example
Mucolytics | Carbocistein
78
What class of drugs used in rhinitis activate a1 receptors? Give an example
Vasoconstrictors | Oxymetazoline

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