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Pharmacology > Pharmacology of asthma > Flashcards

Pharmacology of asthma Flashcards

1
Q

What are the core drugs for the treatment of asthma?

A
  • Salbutamol
  • Fluticasone
  • Mometasone
  • Budesonide
  • Montelukast
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2
Q

What is the primary mechanism of action of Salbutamol?

A

Agonist at the β2 receptor on airway smooth muscle cells. Activation reduces Ca2+ entry and this prevents smooth muscle contraction.

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3
Q

What is the drug target for Salbutamol?

A

Beta 2 (β2) adrenergic receptor

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4
Q

What are the main side effects of salbutamol?

A

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

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5
Q

What type of agonist is salbutamol?

A

Salbutamol is a short acting beta agonist (SABA). It’s half life is 2.5-5hours.

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6
Q

Why are cardiac effects seen as side effects of salbutamol?

A

Beta 2 selectivity is not absolute – as a result, cardiac (beta 1) effects can be seen.
Hypokalaemia can be caused via an effect on sodium/ potassium ATPase. This effect can be exacerbated by coadministration with corticosteroids

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7
Q

What is the primary mechanism of action for Fluticasone?

A

Very powerful drugs. Multiple actions on many different cell types. Fluticasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce. (reduces the effect of IL-5 and IL-4 (proinflammatory) )

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8
Q

What is the drug target of Fluticasone?

A

Glucocorticoid receptor on inflammatory cells

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9
Q

What are the main side effects of Fluticasone?

A
  • Local side effects: Sore throat, hoarse voice, opportunistic oral infections
  • Systemic side effects: Growth retardation in children, Hyperglycaemia, Decreased bone mineral density, Immunosuppression, Effects on mood
    (Many others)
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10
Q

Which has a greater affinity to the glucocorticoid receptor, Fluticasone or cortisol?

A

Fluticasone

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11
Q

How is Fluticasone best delivered to the body?

A

Oral bioavailability <1%. Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature.

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12
Q

What is the primary mechanism of action of Mometasone?

A

Very powerful drugs. Multiple actions on many different cell types. Mometasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

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13
Q

What is the drug target of Mometasone?

A

Glucocorticoid receptor

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14
Q

What are the main side effects of Mometasone?

A
  • Local side effects: Sore throat, hoarse voice, opportunistic oral infections
  • Systemic side effects: Growth retardation in children, Hyperglycaemia, Decreased bone mineral density, Immunosuppression, Effects on mood
    (Many others)
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15
Q

Which has a greater affinity to the glucocorticoid receptor, Mometasone or cortisol?

A

Mometasone

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16
Q

How is the drug best delivered to the body?

A

Oral bioavailability (the proportion of drug that reaches the plasma VIA the GI tract) <1%. Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature.

17
Q

What is the primary mechanism of action of Budesonide?

A

Very powerful drugs. Multiple actions on many different cell types. Budesonide directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

18
Q

What is the drug target of Budesonide?

A

Glucocorticoid receptor

19
Q

What are the main side effects of Budesonide?

A
  • Local side effects: Hoarse voice, opportunistic oral infections
  • Systemic side effects: Growth retardation in children, Hyperglycaemia, Decreased bone mineral density, Immunosuppression, Effects on mood
    (Many others)
20
Q

Can Budesonide be inhaled? Why?

A

Yes: Oral bioavailability >10%. Therefore, inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract.

21
Q

Compare Budesonide with Fluticasone and Mometasone?

A

Budesonide is Less potent than fluticasone and mometasone

22
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, broncho-constriction and inflammation induced oedema

23
Q

What is the drug target of Montelukast?

A

CysLT1 leukotriene receptor

24
Q

What are the main side effects of Montelukast?

A
  • Mild side effects: Diarrhoea, Fever, Headaches, Nausea or vomiting
  • Serious side effects: Mood changes, Anaphylaxis
25
Q

How should Montelukast be administered for exercise- induced asthma?

A

For prophylaxis of exercise-induced bronchoconstriction, montelukast should be administered at least 2 hours before initiating exercise.

26
Q

What is “the seven step” process of prescribing drugs to patients ?

A
  1. Identify the patient’s problem
  2. Specify the therapeutic objective
  3. Select a drug on the basis of comparative efficacy, safety, cost and suitability
  4. Discuss choice of medication with patient (and carer) and make a shared decision about treatment
  5. Write a correct prescription
  6. Counsel the patient on appropriate use of the medicine
  7. Make appropriate arrangements for follow up (Monitor/stop the treatment)
27
Q

Describe the pattern of an asthma attack

A
  • There is both an “immediate” and “delayed” phase of asthma attacks
  • The early phase attack is “bronchospasm” that occurs between the first 0-1 hour after the trigger
  • The late phase is “inflammation” and that occurs roughly around 6 hours after the trigger
28
Q

What are the 2 types of therapeutic objectives with the treatment of asthma?

A

Short term = Relief
Relieve symptoms of breathlessness and expiratory wheeze during the acute asthma attack

Long term = Prevention
Dampen/prevent the late phase of the asthma attack
Reduce the risk of further asthma attacks.
Attempt to improve lung function

29
Q

why do you think the inhalation route is preferred over the oral route for Salbutamol?

A

Inhaled bronchodilators are preferred as they have quicker onset of action and fewer side effects than oral or IV administration

30
Q

Why do you think an oxygen driven nebulizer is the best method for delivering salbutamol in an emergency situation?

A

Advantages:
- many drug solutions
- Can deliver combinations
- Minimal patient cooperation required
- Can deliver to all patient ages
- Concentration and dose can be modified
- Normal breathing pattern

31
Q

Evidence suggests that only 20% of the inhaled dose of salbutamol (or any inhaled drug) penetrates deep enough into the lungs to be able to influence lung function (e.g. reduce breathlessness).

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

A
  1. Can be lost/ exhaled during inhalation process
  2. Must remain in the lung to produce an effect- but it can be absorbed from the lungs into the systemic circulation
  3. Can be removed from the lung via Mucociliary clearance (absorbed from the gut)
  4. Some will be absorbed across the mucous membrane in the oral cavity and pharynx
32
Q

What can be done to prevent the amount of inhaled salbutamol lose?

A

Use a spacer

33
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

“First-pass inactivation”= inactivation of a drug during the first liver passage

34
Q

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

A

Pharmacology (7 decks)

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