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Pharmacology 1 > asthma and drugs used in treatment > Flashcards

asthma and drugs used in treatment Flashcards

1
Q

what is asthma?

A

an condition associated with:

  • airway hyperresponsiveness
  • reversible airflow limitation
  • bronchial inflammation
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2
Q

what are the symptoms of asthma?

A
  • wheezing
  • shortness of breath
  • cough
  • worse at night
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3
Q

what are the triggers for asthma?

A
  • emotion
  • diet
  • cold air/ exercise
  • pollutants (cigerette smoke, dust, fumes)
  • exposure to allergens
  • drugs (asiprin, beta blockers)
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4
Q

what are the long term aims of asthma treatment?

A
  • abolish symptoms
  • maintain optimal lung function
  • prevent permenant lung damage
  • prevent death from acute attack
  • avoid unnecessary side effects
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5
Q

what are the differences between reliever and preventer medication for asthma?

A

reliever - bronchodilator → relax smooth muscle / widens airway (works rapidly and directly to reverse bronchoconstriction)

preventer - anti-inflammatory → stops response to allergen

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6
Q

give four examples of reliever medication used in asthma

A
  1. salbutamol (ventalin) - ß2 adrenoceptor agonist
  2. salmeterol
  3. ipratropium
  4. theophylline
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7
Q

give three examples of preventer medication used in asthma

A
  1. beclometasone
  2. sodium cromoglicate
  3. montelukast
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8
Q

which target is most appropriate to treating asthma?

A

ß2 receptors as these are found in:

  • lungs
  • blood vessels
  • muscle spindles
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9
Q

what does salbutamol have a similar structure to?

A

adrenaline

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10
Q

how can ß2 agonists be given?

A

inhaled or orally

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11
Q

name two short acting ß2 agonists and explain when they would be given

A

salbutamol

terbutaline

*inhaled beefore exertion to reduce exercise induced asthma - duration of action 3-5hrs

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12
Q

name two long-acting ß2 agonists and explain when they would be given

A

salmeterol

formoterol

* only used in patients taking inhaled steriods - can be taken 1-2 times daily - duration of actio 12hrs

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13
Q

what are the side effects of ß2 agonists? explain why these occur

A
  • tremor - ß2 receptors in muscles activated
  • increased HR - stimulation of cells in SA node
  • reduced K+ (hypokalaemia) - stimulation of sodium/potassium pump
  • nervous tension/ headache - activation of ß2 receptors in CNS
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14
Q

how can the systemic effects of ß2 agonists be reduced?

A

by inhaling drug

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15
Q

what are the doses give for oral and inhaled salbutamol?

A

oral - 4mg

inhaled - 100-200microgram

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16
Q

name three devices used to deliver asthma drugs

A
  1. metered dose inhaler (MDI) - coordination needed
  2. spacer - more efficient at getting drug into lungs and lower airway
  3. breath activated inhaler - breath enough to activate
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17
Q

describe the distribution of drug using an MDI device

A
  • 50% initially impacts in mouth
  • 10% reaches lungs (target)
  • 90% eventually swallowed (explains systemic side effects)
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18
Q

what are the benefits of using an accuhaler?

A
  1. less coordination needed to deliver drug
  2. counter indicates drug doses remaining
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19
Q

describe what a turbohaler is

A
  • dry powder inhaler
  • powder stored with a desiccant to keep powder dry
  • contains no lactose so no taste
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20
Q

what is a nebuliser and what is it commonly used for?

A
  • air/oxygen blows through drug solution creating a fine mist which is inhaled
  • mask used
  • commonly used in severe asthma attacks and with children
21
Q

when would a glucocorticosteroid be used in asthma?

A

as a preventer

22
Q

name five glucovorticosteroids that are used via an inhaler to prevent asthma attacks

A

bedometasone - oral inhalant or nasal spray

fluticasone

mometasone

budesonide - relief begins within 10hrs

ciclesonide

* relief from symptoms can take 3-7 days

23
Q

why are the systemic effects of inhaled glucocorticosteroids reduced?

A

poor bioavailablity

24
Q

what can glucocorticosteroids often be administered in combination with?

A

ß2 agonists

25
Q

give two examples of combination inhalers which have a glucocorticosteroid and an ß2 agonist together

A

symbicort - budesonide / formoterol

fluticasone / salmeterol

26
Q

what does SMART stand for?

A

Symbicort Maintance And Reliever Therapy

27
Q

explain the mechanism of action of glucocorticosteroids (GCs)

A
  • GCs are synthesised from cholesterol allowing them to cross cell membrane
  • when inside the cell GCs bind to steroid receptors
  • teh dry-receptor complex forms a dimer which can cross into nucleus
  • in nucleus the dimer binds to specific DNA sequence inducing or supressing genes
  • protein production influenced
  • GCs inhibit transcription of COX-2 gene - reducing protein production and inflammation
28
Q

what are the side effects of glucocorticosteroids?

A
  • local immunosuppression - oral thrush
  • local effects on vocal cords - dysphonia (hoarseness)
29
Q

what is prednisolone used forn and how does it work?

A
  • treats acute asthma attack
  • short course - 7 days (high dose)
  • continue with high dose inhaled steroid in chronic/severe asthma
  • works by: suppressing immune system activity and release of inflammatory mediators
30
Q

explain the danger of stopping glucocorticosteroids abruptly

A

results in acute adrenal insuffiency as patients ability to synthesise GCs has been suppressed → leads to patient being unable to maintain a stress response leading to addisonian crisis

31
Q

what are antimuscarinic bronchodilators and what are they used for?

A
  • short acting (reliever)
  • used alonside high-dose inhaled glucocorticosteroids for severe asthma
32
Q

what is the mechanism of action for antimuscarinic bronchodilators?

A
  • block muscarinic receptors → inhibits bronchconstriction activated by parasympathetic nervous system
33
Q

given an example of an antimuscarinic bronchodilator and explain its side effects

A

ipratropium - causes dry mouth and precipitates glaucoma

34
Q

what are cromones and how do they work?

A

cromones

  • inhibit release of chemicals from inflammatory cells (mast cells) → prevents bronchospasm
  • reduces allergen induced responses and bronchospasm during/after exercise
35
Q

name 2 cromones

A
  1. nedocromil sodium
  2. sodium cromoglicate

* stops mass cells releasing histamine and other chemicals - mainly used in children

36
Q

what do leukotrienes cause?

A
  • bronchoconstriction
  • release of inflammatory cells
  • increase in secretions in airways
37
Q

what do leukotriene receptors antagonists do?

A

relax airways and prevent inflammation

38
Q

give two examples of leukotriene receptor antagonists and explain side effects

A

montelukast

zafirlukast

*causes GI disturbance

39
Q

when is theophylline (aminophylline) used?

A

orally or IV in patients with persistant symptoms / severe acute asthma

40
Q

can theophylline be used with other drugs?

A

yes - ß agonists and/or steroids

41
Q

what are the drawbacks and side effects of theophylline?

A

drawbacks: narrow therapetic window

side effects: increased HR, palpitations, convulsions, headache

42
Q

explain the mechanism of action of theophylline

A
  • blocks phosphodiesterase enzyme (PDE) which breaksdown into 5’AMP - therefore more cAMP is available to stimulate smooth muscle relaxation
43
Q

what is omalizumab (xolair) used for and how it given?

A
  • an antibody (given subcutaneously) every 2-4 weeks
  • reduces effect of allergen induced reactions
  • used in adults with severe allergic asthma not controlled by ß agonists and glucocorticosteroids
44
Q

what are the side effects of omalizumab?

A
  • bruising
  • pain on injection
  • small risk of anaphylaxis
45
Q

what is the mechanism of action of omalizumab?

A
  • antibody inhibits binding of IgE to receptor surface of mast cell and basophils
  • prevents release of pro-inflammatory mediators and reduces allergen induced airway reactions
46
Q

describe the treatment strategy for asthma from mild to severe

A
  1. inhaled short acting ß2 agonists (as needed)
  2. inhaled steroids
  3. add inhaled long acting ß2 agonists and increase dose of inhaled steroids
  4. short and long acting ß2 agonists and inhaled steroids and another drug (eg. LTR antagonist)
  5. continuous or frequent use of oral steriods (and immunosuppressants
47
Q

what can be substituted for inhaled ß2 agonists in stage 1 of the asthma treatment strategy?

A

ipratropium

oral ß agonists

theophyllines

48
Q

describe what therapy would be given in acute asthma attack

A
  1. bronchodilators given via nebuliser
  2. glucocorticosteroids given (oral prednislone, IV hydrocortisone) - route depends on severity
  3. oxygen therapy needed if O2 saturation reduced (<93%)
  4. in poor response aminophylline injection (severe, acute attacks)

Pharmacology 1 (11 decks)

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