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PMY2107 Applied Clinical Pharmacology and Therapeutics > Bronchodilators > Flashcards

Bronchodilators Flashcards

1
Q

How can respiratory disease close airways (3 points)

A

Narrowing of airways due to inflammation and swelling.
Constriction of muscles around airways.
Increased production of sticky mucus.

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2
Q

What are two relievers as bronchodilators?

Acts on autonomic nervous system.

A

Short-acting Beta-2 agonists.
Muscarinic antagonists.
(Fast onset)

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3
Q

What are three controllers as bronchodilators?

Acts on autonomic nervous system.

A

Long-acting Beta-2 agonists.
Methylxanthines.
Leukotriene receptor antagonists.
(Slow onset)

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4
Q

Sympathetic nerves innervate bronchioles and Beta-2 receptors are present here. What does sympathetic stimulation cause?

A

Relaxes the muscles - bronchioles/airways open up.

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5
Q

Parasympathetic nerves innervate the bronchus and bronchioles and muscarinic (M3) receptors are present here. What does parasympathetic stimulation cause?

A

Constricts the muscles - bronchioles/airways close.

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6
Q

What class of receptor is B2 receptors?

A

G-Protein Coupled Receptors.

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7
Q

What class of receptor is M3 receptors?

A

G-Protein Coupled Receptors.

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8
Q

Name 4 types of bronchodilators in general.

A

Beta-2 agonists.
Muscarinic antagonists.
Methylxanthines.
Leukotriene receptor antagonists.

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9
Q

What are short acting inhalers called?

A

Relievers

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10
Q

What are long acting inhalers called?

A

Controllers/Preventers

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11
Q

What do B2-adrenergic agonists do?

A

Stimulate B2 receptors preferentially.

Cause relaxation of smooth muscles in bronchioles.

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12
Q

What are short acting inhalers used for?

A

These are reliever inhalers, used for occasional relief of symptoms - asthma attacks.

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13
Q

What are long acting inhalers used for?

A

These are controller inhalers, used for controlling chronic symptoms - COPD.

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14
Q

How are B2 adrenergic agonists delivered and why?

A

Via aerosolising inhalers.

Minimise adverse effects. Administered via mouth - reaches lungs - immediate access to site of action.

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15
Q

Give two examples of SABAs and the duration.

A

Salbutamol
Terbutaline
Fast onset. Duration: 4 hours

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16
Q

Give two examples of LABAs and the duration.

A

Formoterol
Salmeterol
Slow onset. Duration: 8-12 hours

17
Q

Why can’t salmeterol be given to treat asthma attack?

A

It is slow acting. Attack needs a SABA.

18
Q

Sometimes LABAs are given with steroids. Why might this be?

A

Steroids deal with inflammatory effects.

Salmeterol deals with constriction of airways.

19
Q

How does muscarinic antagonist work as bronchodilators?

A

Block action of Ach on M3 muscarinic receptors and cause relaxation of smooth muscle.

20
Q

What kind of substrate is the bronchodilator which blocks M3 receptors?

A

Competitive anatgonist.

21
Q

Muscarinic antagonists are used as bronchodilators. Name 3 examples of inhalers used?

A 
All are short acting:
Ipratropium bromide (Atrovent)
Oxitropium (Oxivent)
Tiotropium bromide (Tiova)
22
Q

Methylxanthines have two mechanisms of action. What are they?

A

Acts as bronchodilator.

Acts as anti-inflammatory.

23
Q

How does methylxanthines act as bronchodilators?

A

Acts as a competitive inhibitor of phosphodiesterase - results in raised intracellular cAMP and PKA activation.

24
Q

How do methylxanthines act as anti-inflammatory agents?

A

Inhibits TNF-alpha and blocks leukotriene synthesis - dampens and relieves the inflammation.

25
Q

What is the main methyxanthine used in the treatment of asthma and COPD?

A

Theophylline.

26
Q

How is theophyline administered?

A

Administered orally as tablets - not effective through inhalation.
Available in immediate and sustained release formulations.

27
Q

Why is theophylline not used as first line medication?

A

Due to narrow therapeutic window.
Can have serious side effects.
Used as last resort in hospital so patient can be monitored.

28
Q

How are leukotrienes produced?

A

Produced by the oxidation of arachidonic acid by the lipoxygenase pathway. Arachidonate 5-lipoxygenase catalyzes this reaction.

29
Q

What is the effect of leukotriene release in asthma?

A

Causes bronchoconstriction and contributes to inflammation.

30
Q

What are leukotriene receptor antagonists used as?

A

As preventer drugs.

31
Q

Describe leukotriene receptor antagonist MOA.

A

Block action of leukotrienes on receptors.
Causes bronchodilation, relaxes airways.
Dampen inflammation.
Relieve symptoms.

32
Q

Give an example of a leukotriene receptor antagonist drug.

A

Montelukast.
Zafirlukast.
Pranlukast.

PMY2107 Applied Clinical Pharmacology and Therapeutics (21 decks)

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