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Applied Pharmacology bs > Asthma Treatments > Flashcards

Asthma Treatments Flashcards

1
Q

What are the two main (firs line ) drugs used to treat asthma?

A
  • glucocorticoids (steroids)

- B2 adrenergic agonists

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2
Q

What are the two types of asthma?

A 
CHRONIC
- recurrent attacks of reversible airway obstruction 
- controlled with drugs 
ACUTE SEVERE
- not easily reversible 
- can be fatal
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3
Q

What is asthma?

A
  • inflammation in the airways
  • hyper-reactivity of bronchioles eg. to irritant chemicals, cold air, stimulant drugs
  • results in bronchoconstriction and mucus secretion
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4
Q

Asthma has two stages in an attack, bronchospasm and late phase with is the inflammation. What drugs are needed in these two phases?

A
  • bronchodilator for bronchospasm stage

- anti- inflammatory for late stage

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5
Q

There are short and long acting b2 adrenergic receptor agonists. What are examples of these?

A 
SALBUTAMOL 
- short acting 
- max effect within 30 min (lasts 4-6 hours)
- used as needed to control symptoms 
SALMETEROL 
- long acting 
- duration of action = 12 hours 
- twice daily dose in patients not controlled with glucocorticoids
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6
Q

What are the actions of B2 adrengic receptor agonist such as salbutamol and salmeterol?

A
  • direct action on B2 adrenoceptors on bronchiole smooth muscle to relax muscle
  • inhibit mediator release from mast cells & monocytes
  • may act on cilia to increase mucus clearance
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7
Q

B2 agonist are administered through inhalation to target action in lung & minimise systemic effects. What are the unwanted effects of these drugs?

A
  • results from absorption into systemic circulation
  • most common is tremor
  • some tolerance to B2 agonist may develop - prevented by glucocorticoids
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8
Q

Theophylline are used with steroid when asthma response to B2 agonist is inadequate. What are the mechanisms of action in these drugs?

A
  • mechanism is still unclear

- phosphodiesterase (PDE) inhibitor

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9
Q

Theophtlline is a second line drug (sustained- release tablet. it can also be given IV in acute severe asthma. What are the unwanted side effects of Theophylline?

A
  • CNS: stimulant (tremor, sleep disturbance)
  • Cardiovascular: stimulate heart, vasodilation
  • GI tract: anorexia, nausea, vomiting
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10
Q

What is the main muscarinic receptor antagonist used?

A

ipratropium

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11
Q

What are the mechanism of action in muscarinic receptor antagonist such as ipratropium?

A
  • block action of endogenous acetylcholine at muscarinic receptors
  • this relaxes bronchial smooth muscles
  • inhibits elevated mucus secretion in asthma
  • may increase clearance of bronchial secretions
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12
Q

muscarinic receptor antagonists are used when B2 agonists and steroids are insufficient. What are the unwanted side effects ?

A
  • few unwanted side effects and are mostly safe and well tolerated
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13
Q

What are examples of leukotriene receptor antagonists?

A
  • montelucast (1 X daily)

- Zafirlukast (2 X daily )

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14
Q

leukotriene receptor antagonist such as montelucast and Zafirlukast are used for what?

A
  • to prevent exercise induced and asprin sensitive asthma
  • main use as add on for uncontrolled, mild- moderate asthma.
  • action addictive with B2 agonist
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15
Q

What are the actions of leukotriene antagonist such as montelucast and Zafirlukast?

A
  • act at cysteinyl-leukotriene receptors - on bronchiole smooth muscle cells
  • prevent actions of LTC4, LTDD, which are:
  • bronchial spasmogens
  • stimulate mucus secretion
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16
Q

What are the unwanted side effects of leukotriene antagonist?

A
  • very few
  • headache
  • GI disturbance
17
Q

Glucocorticoids are anti-inflammatory drugs that are usually given by inhalation. Give examples of these drugs.

A
  • Beclometasone
  • Budesonide
  • Fluticasone propionate
  • Ocassionally prednisolone or hydrocortisone
18
Q

What are the actions of glucocorticoids such as beclometasone, budesonide, fluticasone propionate?

A
  • reduce production of cytokines, spasmogens (LTC4, LTD4) and leucocyte chemotaxins (LTB4, PAF)
  • therefore reduction in bronchospasm
  • reduction in recruitment and activation of inflammatory cells
19
Q

How long do glucocorticoids take to work?

A

full effect takes several days to develop

20
Q

What are the detailed mechanisms of how glucocorticoids do their actions?

A
  • enter cells
  • bind to intracellular receptors in cytoplasm (GRa, GRB)
  • receptor complex moves to nucleus
  • binds to DNA in nucleus
    alters gene transcription
    eg. introduction of lipocortin, repression of IL-3
21
Q

What are the clinical uses of glucocorticoids?

A
  • patients requiring regular bronchodilators to control attacks
  • IV hydrocorticoids and oral prednisolone for acute exacerbations
  • short course prednisolone if deterioration or prolonged use needed for some patients
  • give inhaled steroid, with additional agent for severe asthma eg. budesonide + B2 agonist or theophylline
22
Q

What are the unwanted side effects of glucocorticoids such as beclometasone, budesonide, fluticasone propionate?

A
  • oropharyngeal thrush and dysphonia, this is reduced by using spacer device as it:
  • reduces oropharyngeal drug deposition
  • increases airways drug deposition
  • Other side effects of the glucocorticoids are:
  • adrenal suppression
  • patients should carry steroid card
23
Q

Cromoglicate/ nedocromil cab reduce both early and late phase responses. it reduce bronchial hyper-reactivity. What is it effective against?

A 
effective in asthma caused by 
- antigen 
- exercise
- irritants 
Not all asthmatics respond 
- its unpredictable 
- children respond better than adults
24
Q

Cromoglicate mechanisms are not fully understood. what do we know about their actions?

A
  • mast cell stabiliser
  • may reduce neuronal reflexes (desensitise to irritants)
  • inhibit release of T-cell cytokines
  • affect inflammatory cells and mediators
25
Q

What are the unwanted side effects of cromoglicate mechanisms

A
  • few
  • irritation of upper respiratory tract
  • hypersensitivity reactions reported, but rare
26
Q

Cromoglicate is given by inhalation. What are the clinical uses?

A
  • to prevent both phases of attack
  • most effective in children
  • effects may take weeks to develop
27
Q

A new development of biologic agent is omalizumab (Xolair) what are its actions?

A
  • binds to human IgE
  • inhibits binding of IgE to IgE receptor on the surface of mast cells and basophils
  • inhibits IgE-mediated cascade of asthma
28
Q

Omalizumab is give by sub-cutaneous injection every 2-3 weeks, why?

A
  • absorbed slowly

- peak plasma concentration in 7-8days

29
Q

What are the unwanted side effects of omalizumab?

A
  • few but can be severe
  • anaphylaxis - allergic reaction to protein
  • malignancies (slightly higher rate than normal )
30
Q

How is mild asthma with rare attacks treated?

A
  • inhaled B2 agonist when required
31
Q

How is mild asthma with more frequent attacks treated?

A
  • glucocorticoids for prophylaxis

- B2 agonist when needed for acute attack

32
Q

How do you treat moderate to severe asthma?

A
  • drug combination preferred usually
  • B2 agonist with glucocorticoids
  • in combined inhaler
    other drugs added when approach fails to control attacks

Applied Pharmacology bs (10 decks)

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