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CPT > Pharmacology of Airway Control > Flashcards

Pharmacology of Airway Control Flashcards

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1
Q

What are the 3 main parts of asthma pathophysiology

A
  • mucosal oedema
  • mucus plugging
  • bronchoconstriction
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2
Q

What is inflammation in asthma driven by leading to the changes

A

Th-2 driven / eosinophillic inflammation

Lead to

  • mucosal oedema
  • bronchoconstriction
  • mucus plugging

Also leads to
- airway remodelling

All lead to
BRONCHIAL HYPERRESPONSIVENESS

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3
Q

Asthma control consists of 5 criteria

What are they ?

A
  • minimal symptoms during day and night
  • minimal need for reliever med
  • no exacerbations
  • no limitation of physical activity
  • normal lung function (FEV1 and / or PEF >80% predicted or best )
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4
Q

Before initiating a new drug therapy what should be checked

A
  • check compliance with existing therapies
  • check inhaler technique
  • eliminate trigger factors
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5
Q

Outline the stepwise treatment approach for asthma ?

5 steps

A

1 - short acting B2 agonists , consider low dose ICS

2 - regular low dose ICS

3
A - LABA + low dose ICS

B - If LABA no effect, increase dose of ICS
If control inadequate with LABA - LABA + medium dose ICS
If still inadequate- continue LABA and ICS and consider trial do other therapy (e.g. LTRA , LAMA)

4 - LABA + high dose ICS
Addition of another drug, e.g. LTRA, LAMA

5 - Daily steroid tablet (lowest dose providing adequate control)
+ high dose ICS
+ consider others to minimise steroid tablets

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6
Q

What is used to treat mild intermittent asthma in step 1 of asthma control ?
Give 2 examples

A

Short Acting β-2 agonists

  • salbutamol
  • terbutaline
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7
Q

How do the short acting B2 agonists provide symptom relief

A
  • main action is on airway smooth muscle
  • reversal of bronchoconstriction
  • prevention of bronchoconstriction i.e. on exercise (so useful touse before exercise )
  • possibly inhibit mast cell degranulation if used intermittently
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8
Q

How often should Short-acting b2 agonists be used ?

A

As-required basis

Do not use regularly - reduces asthma control

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9
Q

Why is regular use of B2 agonists bad

A

On regular use
Mast cell degranulation in response to allergen increases
Therefore better to use intermittently

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10
Q

B2 receptor function in airway smooth muscle ?
(Slide 12 image )
How the receptor works and effects

A
  • When B2 agonist binds to B2 adrenoceptor, αs dissociates from beta-gamma subunit
  • αs goes onto stimulate adenyl cyclase
  • increase intracellular cAMP
  • # which inhibits the myosin light chain kinase and activates PKA (protein kinase A)
  • relaxation
  • inhibition of agonist-induced contraction
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11
Q

Fast onset, short duration inhaled B2- agonists.

2 examples ?

A
  • salbutamol

- terbutaline

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12
Q

Fast onset, long duration inhaled B2-agonists.

3 examples and time of duration ?

A
  • formoterol (12h)
  • olodaterol (24h)
  • indacaterol (24h)
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13
Q

Slow onset, long duration inhaled B2-agonists.

2 examples ?

A

Salmeterol (12h)

Vilanterol (24h)

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14
Q

Side effects of B2-agonists ?

A

Side effects are adrenergic

  • tachycardia
  • palpitations
  • tremor
  • headache
  • nausea
  • cardiac arrhythmia
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15
Q

What is step2 of asthma control

A

Regular preventer therapy

Inhaled corticosteroids

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16
Q

According to BTS guidelines, what are the 4 conditions in which inhaled corticosteroid should be started ?

A
  • using B2 agonist 3 or more times/week
  • symptoms 3 or more times/week
  • waking up once or more / week
  • exacerbation requiring oral steroids in last 2yrs (Consider )
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17
Q

What do corticosteroids do ?

A
  • Reduce inflammation (esp target eosinophillic inflam)
  • Reduce bronchial hyper-responsiveness
    (Not really shows to affect airway remodelling)

Improves symptoms, improves lung function, prevent exacerbations, prevent death

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18
Q

2 main molecular mechanisms of action of steroids ?

A
  • Transactivation : activation of anti-inflammatory genes

- Transrepression : inhibits production of pro-inflammatory proteins

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19
Q

How is potency or inhaled GCS increased ?

What 3 properties are added

A

Addition of lipophillic side chain on D- ring

  • v high affinity for the GCS receptor
  • increases uptake and dwell time (in tissue on local application )
  • rapid inactivation (by hepatic biotransformation following systemic absorption )
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20
Q

Systemic concentration of inhaled drugs =

A

Active drug from the gut + absorption from lungs

Active drug from the gut - after gut absorption and first pass metabolism in liver

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21
Q

Give 3 examples of Inhaled Corticosteroids

A
  • Beclomethasone
  • Budesonide
  • Fluticasone
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22
Q

How is beclomethasone absorbed

A

Through gut and lungs

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23
Q

Which 2 undergo extensive first pass metabolism

A

Budesonide and fluticasone

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24
Q

Which patients have better treatment response to inhaled steroids

A

Patients with eosinophillic asthma

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25
What is step 3 of asthma control
Add-on therapy | First choice - Long acting B2-agonists (formoterol, salmeterol )
26
When should the add-in LABA be used
When patient not controlled on 400mcg/day ICS | Flat ICS dose - response curve
27
Before initiating a new drug therapy, what should be done
Re-check pt med compliance Check inhaler technique (is it the right inhaler, as they still using it correctly ) Eliminate trigger factors
28
Pharmacological properties of Formoterol and Salmeterol What is the usual dosage of each ?
F - 12mcg bd | S - 50mcg bd
29
Onset of action of each
F : 1-3min | S : 10-20min
30
Duration of action of both
F & S - 12hrs
31
Molecular properties of each
F - moderately lipophillic S - highly lipophillic
32
Order the potency of Salmeterol, Terbutaline, Formoterol
Formoterol > Salmeterol > Terbutaline
33
Efficacy of Formoterol, Salmeterol and terbutaline
Formoterol and Terbutaline have higher efficacy (achieve higher max relaxation of muscle ) Salmeterol has lower efficacy - lower max relaxation
34
What must LABA always be prescribed with and why ?
Must be prescribed in conjunction with inhaled steroid as they are not anti-inflammatory on their own
35
5 examples of combined inhalers containing both ICS & LABA
``` • Budesonide/formoterol • Beclomethasone/formoterol • Fluticasone/formoterol • Fluticasone/salmeterol All these twice daily ``` •Fluticasone furoate / vilanterol - once daily
36
Rationale for combining both
- easier to use - more likely to be compliant - 1 prescription to worry Blount - potentially cheaper than 2 individual inhalers - safety
37
What are 4 alternatives to step 3/ step 4 add-ons
- High dose ICS - Leukotriene receptor antagonists - Theophylline - Tiotropium
38
Give 2 examples of Leukotriene Receptor Agonists
- Montelukast | - Zafirlukast
39
What is LTC4 released by and what does it do
``` Mast cells and eosinophils Induce - bronchoconstriction - mucus secretion - mucosal oedema a - promote inflammatory cell recruitment ```
40
What do LRAs do - mechanism ?
Block the effect of cytseinyl leukotrienes in the airway at the CysLT1 receptor Some anti asthma activity but only useful in about 15% of patients
41
Side effects of Leukotriene Receptor Antagonists?
- Angioedema - Arthralgia - Anaphylaxis - Dry mouth - Fever - Gastric disturbances - Nightmares Rarely a problem in clinical practice No important DDIs
42
2 examples of methylxanthines
- Theophylline | - Aminophylline
43
MOA of methylxanthines
Antagonise adenosine receptors | Inhibit phosphodiesterase - increase cAMP
44
Therapeutic window of methylxanthines
Narrow | 10-20 mmol/L
45
Frequent side effects of methylxanthines
- Nausea - Headache - Reflux
46
Potentially life threatening toxic complications of methylxanthines
- Arrhythmias | - Fits
47
DDIs of methylxanthines
Levels of methylxanthines are increased by cytochrome P450 inhibitors E.g. erythromycin, ciprofloxacin
48
Give an example of LAMA (long acting muscuranic receptor antagonists )
Tiotropium bromide (SPIRIVA)
49
Tiotropium bromide How many times a day is it taken ? What 2 things is it licensed for ? Which receptor is it selective for ?
- It is a long acting anti-cholinergic - once daily Used for : - severe asthma - COPD - relative selectivity for M3 muscarinic receptor - reduces exacerbations in both asthma and COPD, small improvements in lung function and symptoms
50
Tiotropium bromide | 3 Side effects?
- dry mouth - urinary retention - glaucoma (more of a risk with nebulisation of ipratropium )
51
3 examples of LAMAs licensed for COPD only ?
- Aclidinium (2x daily) - Umeclidinium - Glycopyrronium
52
4 LABA/LAMA combinations licensed for COPD only:
* Tiotropium/Olodaterol * Aclidinium/formoterol (twice daily) * Umeclidinium/vilanterol * Glycopyrronium/indacaterol
53
What is step 5 of asthma control ?
- oral steroids (usually 10mg o.d. or more for maintenance therapy ) - biological therapies
54
Give 2 examples of biological therapy types used in step 5
Anti-IgE Anti-IL-5
55
Give an example of Anti-IgE drug
Omalizumab
56
What is the criteria to use Omalizumab
Strict criteria - atopy (usually indicated for prophylaxis of severe persistent allergic asthma ) - IgE must be within strict range
57
How does Anti-IgE therapy work
Works by preventing IgE binding to high affinity IgE receptor (Fc
58
Give 2 examples of Anti-IL-5 drugs
- Mepolizumab | - Reslizumab
59
How do Anti-IL-5 work
- Reduce peripheral blood & airway eosinophil numbers - Most effective at reducing rate of severe asthma exacerbations - More effective if >3 exacerbations/year with blood eos >0.3x109/L in last year - Also allow steroid tapering (on average 10 mg → 5 mg)
60
Asthma is a variable disease | List 4 things that can cause exacerbations
- allergens - viral infection - cold weather - exercise
61
Self- management plans | Asthma action plans
Every asthmatic should have a self-management plan with written instructions on when and how to step-up and step down treatment
62
Stepping down
• Once asthma is controlled stepping down is recommended • If stepping down does not take place these patients may receive a higher dose than is necessary • Patients should be maintained at the lowest possible dose of inhaled steroid
63
Drug delivery via inhaler devices 10 micron particles - deposited in ? 1-5 micron particles - deposited in ? 0.5 microns - too small so ?
10 micron particles - mouth and oropharynx 1-5 micron particles - small airways - most effective 0.5 microns - Inhaled to alveoli and exhaled without being deposited in lungs
64
Inhaler devices
- If pt is unable to use a device satisfactorily an alternative should be found - Pt should have ability to use inhaler device assessed by a competent healthcare professional - medication needs to be titrated against clinical response to ensure optimum efficacy - Re-assess inhaler technique as part of a structured clinical review
65
What are the 4 conditions defining acute severe asthma in adults ?
Any one of : - unable to complete sentences - pulse =/> 110bpm - respirations =/> 25/min - peak flow 33-50% of best or predicted
66
What are life threatening features of asthma? | any of severe asthma plus any of following
* PEF <33% * sPO2 <92 * PaO2 <8 kPa * PaCO2 >4.5 kPa * Silent chest * Cyanosis * Feeble respiratory effort * Hypotension, bradycardia, arrhythmia * Exhaustion, confusion, coma
67
What is considered near fatal asthma ?
PaCo2 >6kPa or require mechanical ventilation
68
Treatment of acute severe asthma | 5 steps ?
1. High flow OXYEGN - aim sats 94-98% 2. Nebulised SALBUTAMOL - continuous if necessary, oxygen driven 3. Oral PREDNISOLONE ~40mg daily for 10-14 days (Can be stopped without tailing down) 4. If moderate exacerbation not responding or acute severe / life threatening, add nebulised IPRATROPIUM BROMIDE 5. If no improvement and life threatening features not responding to above treatment - consider IV AMINOPHYLLINE ( BEWARE - if taking oral theophylline )
69
What is Iprotrapium bromide (ATROVENT) ?
- A quaternary anticholinergic agent | - Bronchodilation develops more slowly and less intense than adrenergic agonists. Response may last up to 6 hours.
70
What is Iprotrapium bromide useful for ?
Useful ADD-ON in acute severe / life-threatening asthma | Or moderate exacerbation with poor response to initial therapy

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