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262B Pharmacology > L12 - Respiratory Pharmacology > Flashcards

L12 - Respiratory Pharmacology Flashcards

1
Q

How is the airway smooth muscle in the lungs regulated?

A

by the autonomic nervous system:

  • sympathetic = bronchodilaton
  • parasympathetic = bronchoconstriction
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2
Q

What happens to the airways in asthma?

A
  • asthma is chronic inflammatory disease of the airways
  • contracted smooth muscle
  • inflammation and swelling = decreased lumen diameter
  • excess mucous
    it is hard to breathe out
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3
Q

What are the types of intervention used for asthma treatment/management?

A
  • preventers: anti-inflammatory compounds

- relievers: bronchodilators

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4
Q

What are the types of preventers for asthma?

A
  • corticosteroids
  • cromolyns
  • leukotriene antagonists
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5
Q

What are the effects of corticosteroids in asthma?

A
  • reduce number of airways inflammatory cells
  • reduce damage to airways epithelium
  • reduce vascular permeability
    must be used regularly for beneficial effects: cannot help with long-term uncontrolled asthma
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6
Q

What are the administration routes for corticosteroids in asthma?

A
  • inhalation

- oral

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7
Q

What is an example of an inhaled corticosteroid?

A

fluticasone

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8
Q

What is an example of an oral corticosteroid?

A

prednisolone - liquid or tablet

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9
Q

What are the benefits of an inhaled corticosteroid?

A
  • need lower concentration of drug = very little into systemic circulation
  • minimises potential for adverse reactions
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10
Q

What are some of the problems associated with inhaled corticosteroids?

A
  • a lot of the drug is swallowed so difficult to get to the lungs
  • problem with disposition around the mouth and upper airways - risk of fungal infection because immuno-suppressant
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11
Q

When is prednisolone given?

A

orally only for certain circumstances: early during acute asthma exacerbations or for chronic severe asthma

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12
Q

How is prednisolone given?

A
  • given with oxygen (40-60%) and bronchodilators (salbutamol) because the steroid doesn’t take effect immediately while the bronchodilator does
  • high dose (40-60 mg daily) for a short course (4-10 days) then stop
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13
Q

What are the adverse effects of oral corticosteroid?

A
  • suppressing pituitary/adrenal function
  • euphoria
  • buffalo hump
  • hypertension
  • thinning of skin
  • thin arms and legs: muscle wasting
  • benign intercranial hypertension
  • cataracts
  • moon face with red cheeks
  • increased abdominal fat
  • avascular necrosis of femoral head
  • easy bruising
  • poor wound healing
  • osteoporosis
    hyperglycaemia
  • negative nitrogen balance
  • increased appetite
  • increased susceptibility to infection
  • obesity
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14
Q

Why are leukotriene antagonists effective in asthma treatment?

A

leukotrienes cause bronchoconstriction so blocking their effect is beneficial:

  • anti-inflammatory
  • bronchodilation
  • reduce vasoconstriction
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15
Q

What is an advantage of leukotriene antagonists over corticosteroids in asthma management?

A
  • leukotrienes less potent because only target leukotriene pathway - less ADR
  • steroid receptors are located throughout the body = more systemic side effects
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16
Q

What are the types of leukotriene antagonists?

A
  • leukotriene receptor antagonists

- lipoxygenase antagonsts: inhibit the enzyme involved in the production of all leukotrienes

17
Q

What drugs are examples of leukotriene receptor antagonists?

A
  • montelukast

- zafirlukast

18
Q

What drug is an example of lipoxygenase antagonists?

A

zileuton - inhibits 5-lipoxygenase

19
Q

What are relievers in asthma treatment? What effect do they have?

A
  • relievers are drugs that are used to manage the symptoms

- they modulate the ANS (B2) to cause bronchodilation

20
Q

What effect do B agonists have in asthma?

A
  • target B2 receptors

B2 receptors are found in the lungs and their activation causes bronchodilation with minimal effect on the heart

21
Q

What are the types of B agonists in asthma treatment? Give examples

A

(reliever) SABA - Short Acting Beta Agonist:
- salbutamol, terbutaline
(controller) LABA - Long Acting Beta Agonist:
- salmeterol, formoterol

22
Q

What is salbutamol used for?

A
  • acute inhalation treatment of bronchospasm

- prevent exercise-induced asthma `

23
Q

What is the onset and duration of salbutamol? When is it used?

A

onset: 10-15 minutes
duration: 2-5 hours
used on an “as required” basis - regular use shows no benefits
- not used for nocturnal asthma because the effects wear off

24
Q

What are the adverse effects of SABAs?

A

at high doses:

  • sympathetic NS activation = skeletal muscle tremor
  • still has effect on heart = increased HR and force of contraction
25
Q

What are LABAs used for?

A

they are symptom controllers so used in adjunctive role with inhaled corticosteroids as prophylactic
- used in nocturnal asthma because effect lasts through the night

26
Q

What is an example of a fixed dose combination inhaler? What are the advantages of combination inhaler over separate drug administration?

A
  • symbicort: LABA + glucocorticoid

- better outcomes than when taken separately and allows steroid dose to be reduced = reduce ADR

27
Q

What is the first line treatment for asthma?

A

beta agonists

28
Q

What are the autonomic NS receptor types that are targeted in asthma treatment and why?

A

beta receptors:
- B2 receptors are found in the lungs and their activation causes bronchodilation
muscarinic receptors:
- nearly all types are found in the lungs and their activation causes bronchoconstriction so can inhibit (lesser effect than B2 receptor targeting)

29
Q

What is the muscarinic receptor subtype that when activated causes bronchoconstriction?

A

M3

30
Q

What is the mechanism of action of muscarinic receptor blockers?

A

block effects of parasympathetic stimulation via muscarinic receptor antagonism

31
Q

What is the onset, and duration of muscarinic receptor blockers?

A

onset: 30+ minutes
duration: 3-5 hours

32
Q

What is an example of a muscarinic receptor blocker?

A

ipratopium

33
Q

What are the adverse effects associated with muscarinic receptor blockers?

A
  • dry mouth because salivary glands have muscarinic receptors
  • GI motility disorders (constipation, diarrhea, vomiting)
  • cardiac effects
  • urinary retention
  • blurred vision
    headache
34
Q

Apart from beta agonists and muscarinic receptor blockers, what is another reliever (?) that can cause bronchodilation?

A

methylxanthines

35
Q

What is an example of a methylxanthine?

A

theophylline

36
Q

What are the effects of theophylline?

A

phosphodiesterase inhibitor
- prevents the break down of cAMP = increased cAMP which causes bronchodilation
adenosine receptor antagonism
- may produce toxic effects e.g. tachycardia, psychomotor agitation, GI tract disturbances

262B Pharmacology (18 decks)

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