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Clinical Pharmacology > 9.2.1 Asthma Drugs > Flashcards

9.2.1 Asthma Drugs Flashcards

1
Q

What is asthma?

A

Chronic inflammatory airway disease
Intermittent airway obstruction
Hyper-reactivity of small airways
Reversible inflammation with drugs and spontaneously

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2
Q

How do airways look in asthma?

A

Mucosal oedema and plugging
More eosinophils than COPD

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3
Q

What symptoms are present in asthma exacerbation?

A

Coughing
Wheezing
SOB
Caused by bronchospasm

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4
Q

What features are considered good asthma control?

(5)

A
  • Minimal symptoms during day and night
  • Minimal need for reliever medication
  • No exacerbations
  • No limitation to physical activity
  • Normal lung function - FEV1/PEFR >80% predicted)
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5
Q

What is the aim for asthma control overall?

A

Early control with steeping up or down as needed

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6
Q

What must be checked before stepping up or down the treatment ladder?

A
  • Adherence
  • Inhaler technique
  • Trigger removal- eg animal hair
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7
Q

What are the features of uncontrolled asthma?

A
  • 3 or more days a week with symptoms or:
  • 3 or more days a week with required use of SABA for symptomatic relief or:
  • 1 or more nights a week with awakening due to asthma
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8
Q

Outline the asthma treatment ladder

A

1) Start with (short acting beta 2 agonists) to use when needed

2) Add preventer if needed - low dose ICS

3) LABA - long acting beta agonist

4) LTRA - leukotrine receptor antagonist

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9
Q

Why do NICE recommend leukotrine receptor antagonist before long acting beta agonists?

A

LTRAs are cheaper
Evidence shows most patients end up on LABA eventually anyway

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10
Q

When do you give inhaled corticosteroids?

A

When SABA alone is not enough

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11
Q

Give some examples of inhaled corticosteroids

A

Beclometasone
Budesonide
Fluticasone

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12
Q

How are ICS absorbed and how do they work?

A

ICS pass through plasma membrane
Activate cytoplasmic receptors
Activated receptor then passes into nucleus to modify transcription

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13
Q

What do ICS do?

A
  • Reduced mucosal inflammation, widens airways
  • Reduces mucus
  • Reduces symptoms, exacerbations and prevents death
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14
Q

What are the adverse effects of ICS?

A

Local immunosupression causing
- Candidiasis
- Hoarse voice

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15
Q

What can ICS possibly cause in COPD patients?

A

Pneumonia risk possible at high doses

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16
Q

What are some important drug to drug interactions with ICS?

A

If taken correctly very few DDIs and adverse effects

17
Q

How do steroids work?

A

Gene Activation:
- Increase B2 receptors
- Increase anti-inflammatory mediators
- Inhibit release of arachidonic acid

Gene Repression:
- Inflammatory mediators- interleukins, chemokines

18
Q

What are the pharmacokinetics of ICS?

A
  • Poor oral bioavailability
  • Have lipophilic side chain added causing slow dissolution in aqueous bronchial fluid
  • High affinity for glucocorticoid receptor
19
Q

What happens if steroid is absorbed p.o?

A

Transported from stomach to liver by hepatic portal system
Almost complete first pass metabolism - litte gets to systemic circulation
But at high doses all ICS have potential to produce systemic side effects

20
Q

When do you use SABAs?

A

Symptom relief through reversal of bronchoconstriction - only to be used when needed

21
Q

When do you use LABAs?

A
  • Add on therapy to ICS and SABA and in MART (maintenance and reliever)
  • LABA and ICS together - as LABA cannot be taken without ICS
22
Q

What effect do beta 2 agonists SABA and LABA have?

A

Major action on airway smooth muscle - bronchorelaxation
Also increase mucus clearance action by cilia

Normal B2 binding mechanism

23
Q

Why can SABAs only be used when required?

A

When SABA is used regularly it can reduce asthma control, if not well managed, patient at high risk

24
Q

What are the different B2 agonists and their onset speeds?

A

Fast onset:
Salbutamol and terbutaline (turbo-speedy)- short acting
Formoterol - long acting

Slow onset:
Salmeterol - long acting

25
Q

What are the adverse effects of Beta 2 agonists?

A

Adrenergic - fight or flight effects:
- Tachycardia
- Palpitations
- Anxiety
- Tremor
- Increased glycogenolysis in liver
- Increase renin release from kidney
- SVT - increases SAN activity, increases HR, decreases refractory period at AVN

26
Q

What are the warnings/contraindications for beta 2 agonists?

A
  • LABA should only be prescribed alongside ICS if alone can mask airway inflammation and near fatal and fatal attacks can occur
  • CVD - tachycardia may provoke angina
27
Q

What is a combined fixed dose inhaler?

A
  • ICS and LABA together
  • Improves adherance as only 1 inhaler
  • Improved safety - LABA needs to be taken with ICS
28
Q

What are some important drug interactions for beta 2 agonists?

A

Beta blockers - reduce effects of beta 2 agonists

29
Q

Why are LABA and ICS used together?

A

Synergistic - using at same time better than using alone

30
Q

When are leukotrine receptor antagonists used and how are they taken?

A

Used as add on therapy to SABA and ICS
Orally

31
Q

What is an example of a leukotrine receptor antagonist?

A

Montelukast

32
Q

How do leukotrine receptor antagonists work?

A

Leukotrines are usually released by mast cells/eosinophils causing:
- Bronchoconstriction
- Increased mucus
- Increased oedema

Through CysLT1acting on a GPCR

Leukotriene receptor antagonists block CysLT1 from binding to CYSLTR1

33
Q

How useful are LRTAs?

A

Most move on to LABA

Useful in 15% of asthmatics

34
Q

What are some adverse effects of LTRAs?

A

Headache
GI disturbance
Dry mouth
Hyperactivity

35
Q

What warnings andcontraindications are there for LTRAs?

A

Neuropsychiatric reactions can happen

36
Q

What important drug interactions are there with LTRAs?

A

None reported

Clinical Pharmacology (45 decks)

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