Asthma Pharmacology - Detailed Flashcards

1
Q

What is the initial management for anyone presenting with asthma?

A

ICS and SABA

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2
Q

What is the indication to move from step 1 to step 2 of asthma management?

A

If the SABA is being used more than 3 times a week

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3
Q

What is the 2nd step of asthma management?

A

Add a LABA

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4
Q

Normally, how is the LABA administered?

A

In combination with an ICS

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5
Q

If a patient shows no responce to a LABA, what should be done?

A

Stop it and increase the ICS to medium dose

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6
Q

If a patient shows a responce to the LABA, what should be done if they still require further treatment?

A

Continue the LABA and increase the ICS dose to medium

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7
Q

What is another option in asthma management if a patient does have a responce to LABAs?
(but you dont want to increase the ICS dose)

A

Trail of a leukotriene receptor antagonist, SR theophylline or a LAMA

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8
Q

What are the 3 components of Step 4 asthma management?

A

High dose ICS
Add a 4th drug
Refferal

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9
Q

What are the 4 options of alternative asthma drugs that can be added as a 4th drug?

A

Leukotriene receptor antagonist
SR theophylline
Beta agonist tablet
LAMA

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10
Q

What is the final step of asthma management?

A

Daily oral prednisolone and refer

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11
Q

In the general management of asthma, any extrinsic causes/triggers should be ___ ____ __ _____ __ ____

A

Rapidly identified and removed if possible

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12
Q

Passive, and active _____ should always be avoided in asthma

A

Smoking

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13
Q

What are the 3 advantages of administering asthma meds through inhalation?

A

Direct delivery to the lungs
Avoids first-pass metabolism via the liver
Lowers dose needed and systemic effects

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14
Q

What is the general indication of asthma deterioration and therefore the need for more intensive management?

A

Increased reliever/bronchodilator usage

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15
Q

What should be done if asthma has been well controlled for 2/3 months?

A

The treatment reviewed and the steroid dose reduced

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16
Q

What beta agonists are selective to the resp tract?

A

Beta 2

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17
Q

Where are Beta 1 adrenoceptors?

A

The myocardium

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18
Q

What is the general effect of beta-agonists and what do they not do?

A

Relaxation of bronchial smooth muscle

Dont help with underlying airway inflammation

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19
Q

What kind of drug is Salbutamol?

A

SABA

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20
Q

What is the normal dose of SABA?

A

2 puffs when required

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21
Q

What are the 4 side effects of SABAs?

A

Fine tremor
Tachycardia
Arrhythmias
Hypokalaemia

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22
Q

What type of drug is terbutaline?

A

SABA

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23
Q

What time frame does a SABA work within, peak at and then last for?

A

5 mins
Peak - 30 mins
Lasts - 3-5 hrs

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24
Q

What type of drug is salmeterol?

A

LABA

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25
Q

When are LABAs taken?

A

Everyday, regardless of symptoms

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26
Q

What type of drug is formoterol?

A

LABA

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27
Q

What is a fundamental to remember about LABA administration?

A

Should never be administered alone, always with an ICS

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28
Q

What are the 2 LABA/ICS combination inhalers

A

Salmeterol & fluticasone

Formoterol & budesonide

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29
Q

What is seratide composed of?

A

Salmeterol and fluticasone

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30
Q

What type of drug is useful in noctural asthma?

A

LABAs

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31
Q

What type of muscarinic receptors are in the large airways?

A

M3

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32
Q

What type of muscarinic receptors are in the peripheral lung tissue?

A

M1 and M3

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33
Q

What type of drug is Ipratropium?

A

Anti-muscarinic bronchodilator

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34
Q

When are anti-muscarinic bronchodilators useful?

A

In exacerabtions

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35
Q

What are the 2 anti-muscarinics that are useful in severe exacerabtions?

A

Tiotropium or adidium

36
Q

What type of drug is oxitropium bromide?

A

Antimuscarinic bronchodilators

37
Q

What type of drug is sodium cromoglicate?

A

Mast cell stabliser

38
Q

What type of drugs are sodium cromoglicate and nedocromil sodium?

A

Anti-inflammatories

39
Q

What is the mechanism of action of asthma anti-inflammatory drugs?

A

Prevent activation of immune cells by blocking Ca2+ influx

40
Q

What are the 3 immune cells that are blocked by asthma anti-inflammatories?

A

Mast cells
Eosinophils
Epithelial cells

41
Q

When are anti-inflammatories used in asthma?

A

In milder asthma as a preventer (not a reliever)

42
Q

What is the mechanism of action of ICS? (3)

A

Work by modifying genes - increase the transcription of anti-inflammatory genes, and decrease the inflammatory protein gene transcription

43
Q

ICS’s prevent the formation of Ig _

A

IgE

44
Q

ICS’s decrease ___ cytokine formation and cause ___

A

Th2

Apoptosis

45
Q

ICS’s prevent allergen induced ___ influx into the lungs and cause __

A

Eosinophil

apoptosis

46
Q

ICS’s decrease the number of ___ __ and their IgE receptor expression

A

Mast cells

47
Q

What are the 2 very general effects of ICSs?

A

Prevent inflammation

Reduce established inflammation

48
Q

When are ICS’s most effective?

A

In the long term - at preventing attacks

49
Q

Why is the dose of ICSs metered?

A

To prevent unwanted, systemic side effects

50
Q

How long does it take for ICSs to become active?

A

A few days

51
Q

What are the 4 unwanted effects of ICSs?

A

Dysphonia (hoarse voice)
Oral candidiasis
Sup-capsular cataract formation (rare, but can occur in elderly)
Stunted growth in children (final height not affected)

52
Q

What 3 things must be included in good ICS technique?

A

Use of a spacer
Mouth rinsing post-use
Teeth cleaning post-use

53
Q

What makes ICSs less effective?

A

Smoking

54
Q

What are the 3 situations in which oral corticosteroids are used?

A

Chronic asthma
Severe asthma
Deteriorating asthma

55
Q

What type of drug is methotrexate?

A

Oral corticosteroid

56
Q

What type of drug is beclometasone dipropionate?

A

ICS

57
Q

What type of drug is budesonide?

A

ICS

58
Q

What type of drug is cicrolosporin?

A

Oral corticosteroid

59
Q

What type of drug is fluticasone propionate and fluticasone furoate?

A

ICS

60
Q

What type of drug is prednisolone?

A

Oral corticosteroid

61
Q

What type of drug is montelukast?

A

Leukotriene receptor antagonist

62
Q

Where are cysteinyl LT1 receptors?

A

Bronchial smooth muscle

63
Q

What are the 3 effects of cysteinyl LT1 receptors?

A

Bronchial smooth muscle contraction
Mucus secretion
Oedema

64
Q

What type of drug is zarfirlukast?

A

Leukotriene receptor antagonist

65
Q

How are Leukotrine antagonists administered?

A

orally

66
Q

What are leukotriene antagonists effective against?

A

The early and late bronchospasm in mild, persistent asthma

67
Q

What are the 2 types of asthma are leukotriene antagonists used in?

A

Antigen-induced

Exersize-induced

68
Q

Overall, leukotriene antagonists are well tolerated.

What are the 2 potential adverse effects?

A

Headache

GI upset

69
Q

What type of drug is theophylline?

A

Methylxanthine

70
Q

What is the assumed mechanism of action of methylxanthines?

A

Inhibition of PDE (phosphodiesterase) stops cAMP break down, which therefore relaxes bronchial smooth muscle

71
Q

What are the 2 general effects of methylxanthines?

A

Bronchodilatory

Anti-inflammatory

72
Q

Methylxanthines increase ____ motility and reduce ___

A

Diaphragmatic

Fatigue

73
Q

What drugs should methylxanthines be used in combination with?

A

Beta-agonists

Glucocorticosteroids

74
Q

Methylxanthines have a __ __ therapeutic window

A

very narrow

75
Q

What 4 things are affected in the side effects of methylxanthines?

A

CNS
CVS
GI tract
Kidneys

76
Q

What are the 3 main side effects of methylxanthines when dose is too great?

A

Arrhythmias
seizures
hypotension

77
Q

In the theraputic range of methylxanthines, what are the 4 side effects that can occur?

A

Nausea
Vomiting
Abdo discomfort
Headache

78
Q

What kind of drugs can have adverse interactions with methylxanthines?

A

CYP450 drugs, especially antibiotics that inhibit CYP450 enzymes

79
Q

What type of drug is omalizumab?

A

IgE monoclonal antibody

80
Q

Describe the mechanism of action of omalizumab

A

They bind to IgE via the Fc receptor, preventing their attachment to mast cells, and therefore suppressing the allergen responce

81
Q

When is omalizumab cost effective?

A

In patients that require frequent hospital admissions

82
Q

Describe the administration of omalizumab

A

IV every 2-4 weeks

83
Q

What 2 things does the dose of omalizumab depend on?

A

Body weight and total serum IgE

84
Q

What type of drugs are mepolizumab and reslizumab?

A

Monoclonal antibodies against IL-5

85
Q

When are IL-5 antibodies used in asthma?

A

Asthma associated with severe eosinophillia (steroid refractory)