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BRS2 Pharmacology and Therapeutics > Pharmacology of Asthma - Core Drugs & Case Study > Flashcards

Pharmacology of Asthma - Core Drugs & Case Study Flashcards

1
Q

What are the 5 core drugs used in the treatment of asthma?

From Phase 1b

A
  1. Salbutamol
  2. Fluticasone
  3. Mometasone
  4. Budesonide
  5. Montelukast
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2
Q

What class are drugs with the suffix -sone or -ione?

A

Corticosteroids

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3
Q

What is the primary mechanism of action of salbutamol?

A

Agonist at the B2-receptor on airway smooth muscle cells

Activation reduces Ca2+ influx

This prevents smooth muscle contraction

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4
Q

What is the drug target for salbutamol?

A

Beta-2 (B2) adrenergic receptor

aka B2 adrenoreceptor

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5
Q

What is the primary site of action for salbutamol?

A

Airway (bronchial) smooth muscle

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6
Q

What are the main side effects associated with use of salbutamol?

A

Palpitations/agitation
Tachycardia/arrythmias
Hypokalaemia (at higher doses)

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7
Q

What is the half life of salbutamol?

A

2.5-5hrs

Salbutamol is a short acting beta agonist (SABA)

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8
Q

Why can cardiac effects be seen with use of salbutamol?

A

Beta-2 selectivity is not absolute so cardiac (beta-1) effects can be seen

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9
Q

What can cause hypokalaemia with use of salbutamol?

A

Hypokalaemia can be caused via an effect on sodium/potassium ATPase

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10
Q

Hypokalaemia is a side effect associated with use of salbutamol.

Use of what type of medication can exacerbate this effect?

A

Co-administration with corticosteroids can exacerbate this hypokalaemia

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11
Q

What is the primary mechanism of action of Fluticasone?

A

Very powerful drug that has multiple actions on many different cell types

Fluticasone directly decreases inflammatory cells, e.g. eosinophils, monocytes, mast cells, macrophages, and dendritic cells

It reduces the (n) of these cells and also the (n) of cytokines they produce

E.G.

Binds glucocorticoid receptor on eosinophils

Action - stimulates GR

GR - promotes anti-inflammatory response, reduced IL-5 production

This reduces (n) of eosinophils + their produced cytokines, promotes eosinophil apoptosis etc.

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12
Q

What is the drug target for Fluticasone?

A

Glucocorticoid receptor

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13
Q

What are the main local side effects of Fluticasone?

A

Sore throat
Hoarse voice
Opportunistic oral infections

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14
Q

What are the main systemic side effects of Fluticasone?

A 
Growth retardation in children
Hyperglycaemia 
Decreased bone mineral density
Immunosuppression
Effects on mood

(Many others)

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15
Q

How do Fluticasone and Cortisol differ in affinity for the glucocorticoid receptor?

A

Fluticasone has greater affinity for the glucocorticoid receptor compared to cortisol

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16
Q

What is the oral bioavailability of Fluticasone?

A

Oral bioavailability <1%

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17
Q

Any systemic delivery of Fluticasone via the inhaled route is predominantly through the pulmonary vasculature.

Why is this?

A

Oral bioavailability <1%

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18
Q

What is the primary mechanism of action of Mometasone?

A

Very powerful drug that has multiple actions on many different cell types

Mometasone directly decreases inflammatory cells, e.g. eosinophils, monocytes, mast cells, macrophages, and dendritic cells

It reduces the (n) of these cells and also the (n) of cytokines they produce

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19
Q

What is the drug target for Mometasone?

A

Glucocorticoid receptor

20
Q

What are the main local side effects of Mometasone?

A

Sore throat
Hoarse voice
Opportunistic oral infections

21
Q

What are the main systemic side effects of Mometasone?

A 
Growth retardation in children
Hyperglycaemia 
Decreased bone mineral density
Immunosuppression
Effects on mood

(Many others)

22
Q

How do Mometasone and Cortisol differ in affinity for the glucocorticoid receptor?

A

Mometasone has greater affinity for the glucocorticoid receptor compared to cortisol

23
Q

What is the oral bioavailability of Mometasone?

A

Oral bioavailability <1%

24
Q

Any systemic delivery of Mometasone via the inhaled route is predominantly through the pulmonary vasculature.

Why is this?

A

Oral bioavailability <1%

25
Q

What is the primary mechanism of action of Budesonide?

A

Very powerful drug that has multiple actions on many different cell types

Mometasone directly decreases inflammatory cells, e.g. eosinophils, monocytes, mast cells, macrophages, and dendritic cells

It reduces the (n) of these cells and also the (n) of cytokines they produce

26
Q

What is the drug target for Budesonide?

A

Glucocorticoid receptor

27
Q

What are the main local side effects of Budesonide?

A

Hoarse voice

Opportunistic oral infections

28
Q

What are the main systemic side effects of Budesonide?

A 
Growth retardation in children
Hyperglycaemia 
Decreased bone mineral density
Immunosuppression
Effects on mood

(Many others)

29
Q

How does budesonide compare in potency to fluticasone and mometasone?

A

Less potent than fluticasone and mometasone

30
Q

What is the primary mechanism of action of Montelukast?

A

Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells

Decreases eosinophil migration, bronchoconstriction and inflammation induced oedema

31
Q

What is the drug target of Montelukast?

A

CysLT1 leukotriene receptor

32
Q

What is the primary mechanism of action of Montelukast?

A

Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells

Decreases eosinophil migration, decrease bronchoconstriction and reduce inflammation-induced oedema

33
Q

What are the main serious side effects associated with using montelukast?

A

Mood changes

Anaphylaxis

34
Q

Why would someone with asthma administer montelukast at least 2 hrs before initiating exercise?

A

For prophylaxis of exercise induced bronchoconstriction

35
Q

What process is characteristic of the immediate phase of an asthma attack?

A

Mainly bronchospasm

36
Q

What process is characteristic of the delayed phase of an asthma attack?

A

Inflammatory reaction

37
Q

What does the management of asthma in children under 5yo require?

A

Careful and relatively frequent monitoring

38
Q

What does the management of asthma in children under 5yo require?

A

Careful and relatively frequent monitoring

  • Can help minimise asthma symptoms by following a written asthma action plan you develop with the child’s doctor to monitor symptoms and adjust treatment as necessary
39
Q

A three year old child, newly diagnosed with asthma, has been prescribed salbutamol as a reliever therapy for future symptom relief.

She has also been provided with a spacer to help with delivery to the lungs.

Why do you think inhalation route is preferred over the oral route?

A

Local (inhalation) vs systemic (oral) administration: inhalation - directly to lungs where drug can interact with target

Much smaller doses given with inhaled administration of salbutamol vs oral administration because inhalation = local administration

Fewer side effects - some of drug will leak out into systemic circulation via local route (to lungs) BUT much less so than via oral route

40
Q

A three year old child, newly diagnosed with asthma, has been prescribed salbutamol as a reliever therapy for future symptom relief.

She has also been provided with a spacer to help with delivery to the lungs.

What is the benefits of using a nebuliser with treatment?

A

Patient is 3yo —-> easier for her to receive full dose with nebuliser (she has to do less work)

If patient is having difficulty breathing, can add extra drugs to the mix + oxygen to help (all administered with help of nebuliser)

41
Q

Katie (3yo) is brought to A&E by her parents as she’s having great difficulty breathing.

She is wheezing upon exhalation and is coughing occasionally. She also has a slight temperature.

Katie is administered inhaled salbutamol (2.5mg; SABA) via an oxygen-driven nebuliser every 20mins and she recovers within an hour.

Why do you think the nebuliser was the best method for delivering the salbutamol in this urgent situation?

A

Patient is 3yo —-> easier for her to receive full dose with nebuliser (she has to do less work)

If patient is having difficulty breathing, can add extra drugs to the mix + oxygen to help (all administered with help of nebuliser)

Advantages

  • Many drug solutions
  • Can deliver combinations
  • Minimal patient co-operation needed
  • Can deliver to all patient ages
  • Concentration and dose can be modified
  • Normal breathing pattern
42
Q

Evidence suggests that only 20% an inhaled drug penetrates deep enough into the lungs to be able to produce an effect and influence lung function (e.g. reduce breathlessness).

What do you think happens to the other 80% of the inhaled drug?

A
  1. Breathed out (exhaled)
  2. Down oesophagus + into stomach - a huge amount gets swallowed (>80%)

(Oesophagus —along GI tract —> absorbed from gut —> liver etc.)

  1. Mucociliary clearance
  2. Some escapes into systemic circulation (because lungs = heavily vascularised so some will be absorbed from lungs - will diffuse out of lungs + go elsewhere)
  3. Some absorbed across mucus membranes of oral cavity + pharynx
43
Q

What are the advantages of using a spacer when administering inhaled drugs?

Are there any disadvantages?

A
  • Less drug exhaled
  • Less drug passes down into stomach
  • More gets into lungs

However
- Can contribute to loss as some drug can get trapped in spacer

44
Q

What is the approximate proportion of inhaled drug that ends up in:

a) Inhaler device
b) mouth/throat
c) lungs

With vs Without a spacer?

What conclusions can you draw from this?

A

Without spacer:

a) ID - 10%
b) M/T - 81%
c) L - 9%

With spacer:

a) ID - 57%
b) M/T - 22%
c) L - 21%

With a spacer, more of the inhaled drug reaches the lungs where it can hopefully produce an effect

45
Q

Like salbutamol, a significant proportion of inhaled fluticasone is actually swallowed. Despite this, the oral bioavailability (i.e. the proportion of drug that reaches the plasma VIA the gastrointestinal tract) is less than 1%.

Why is this the case?

A

Because of first pass metabolism/inactivation

The swallowed portion of the drug will pass from the gut to the liver where it’s bioavailability will be significantly reduced due to the metabolism it undergoes in this organ.

46
Q

Why might monteklaust be particularly useful for NSAID (Non-steroidal anti-inflammatory drug)-induced asthma?

A

NSAIDs inhibit COX enzyme (cyclooxygenase), thromboxane production + production of some anti-inflammatory prostaglandins

In asthma - results in overproduction of leukotrienes = pro-inflammatory —-> some asthmatic patients react to this —-> can exacerbate asthma

Montelukast acts within same pathway but inhibits leukotriene production –> reducing inflammatory effect

BRS2 Pharmacology and Therapeutics (6 decks)

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