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Pharmacology Drugs > Asthma > Flashcards

Asthma Flashcards

1
Q

What are example of long acting beta agonists?

A
  • Formoterol: rapid onset and long duration

- Salmeterol: slow onset and long duration

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2
Q

What are examples of short acting beta agonists?

A
  • Salbutamol

- Terbutaline

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3
Q

What is the mechanism of action of Beta 2 agonists?

A
  • Binds to Beta 2 adrenoreceptor
  • Increases in Adenycylase activity
  • Increase in cAMP t inhibit the MLCK so relaxation
  • Increase in pKA to cause relaxation
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4
Q

What are the uses of Beta 2 receptor agonists?

A
  • Used for symptom relief through reversal of bronchoconstriction (mild intermittent asthma)
  • Prevention of bronchoconstriction i.e. on exercise
  • Used as required basis
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5
Q

What are some side effects of beta 2 receptor agonists?

A

-If used regularly, they reduce asthma control
Mast cell degranulation in response to allergen increases if beta 2 agonist used regularly

-Adrenergic so can cause tachycardia, palpitations, tremor

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6
Q

What are examples of inhaled corticosteroids?

A
  • Beclomethasone
  • Budesonide
  • Prednisolone
  • Dipropionate
  • Fluticasone
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7
Q

Describe the pharmacokinetics of Beclomethasone?

A

-Absorbed through gut and lungs

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8
Q

Describe the pharmacokinetics of Budesonide?

A

-Undergoes extensive first-pass metabolism

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9
Q

Describe the pharmacokinetics of Fluticasone?

A

-Undergoes extensive first-pass metabolism

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10
Q

What is the mechanism of action of inhaled corticosteroids?

A

Works by binding to Glucocorticoid recetor which affects gene in the nucleus afterwards to cause:

Transactivation

  • Stimulation of anti-inflammatory molecules such as Annexin-1
  • Increase in b2 receptors

Transpression
-Inhibition of pro-inflammatory mediators such as cytokines, chemokines, iNOS

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11
Q

What are the properties of adding lipophilic substituents to inhaled corticosteroids?

A
  • A very high affinity for the GCS receptor
  • Increased uptake and dwell time in tissue on local application
  • Rapid inactivation by hepatic biotransformation following systemic absorption
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12
Q

What are the uses of Inhaled corticosteroids?

A
  • Improve symptoms
  • Improve lung function
  • Reduce exacerbations
  • Prevent death

Better treatment response from eosinophilic patients

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13
Q

What are examples of Leukotriene Receptor antagonists?

A
  • Montelukast

- Zafirlukast

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14
Q

What is the mechanism of action of Leukotriene receptor antagonists?

A

-Block the effect of cysteinyl leukotirences which are released by mast cells and eosinophils and cause bronchoconstriction, mucus secretion and mucosal oedema and promote inflammatory cell recruitment

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15
Q

What are the use of leukotriene receptor antagonists?

A

Some anti-asthma activity but only useful in about 15% patients as add-on therapy

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16
Q

What some side effects of leukotriene receptor antagonists?

A
  • Angioedema
  • Dry mouth
  • Anaphylaxis
  • Arthralgia
  • Fever
  • Gastric Disturbance
  • Nightmares
17
Q

What are examples of Methylxanthines?

A
  • Theophylline

- Aminophylline

18
Q

What is the mechanism of action of Methylxanthines?

A
  • Anatagonise adenosine receptors

- Inhibit phosphodiesterase so increased cAMP. Unlke to be relevant in vivo

19
Q

What are the pharmacokinetics of Methylxanthines?

A
  • Poorly efficacious

- Narrow therapeutic window

20
Q

What are the uses of Methylxanthines?

A

-Asthma

21
Q

What are the side effects of Methylxanthines?

A
  • Nausea
  • Headache
  • Reflux
  • Arrythmias
  • Fits
  • Levels increase with CP450 inhibitorsr
22
Q

What are examples of LAMAs?

A
  • Tiotropium bromide

- Ipratropium Bromide

23
Q

What is the mechanism of action of LAMAs?

A
  • Anticholinergic used once daily

- Relative selectivity for M3 muscurinic receptor

24
Q

When are LAMAs used?

A
  • COPD
  • Severe asthma
  • Reduction of exacerbation in both and small improvement in lung function and symptoms
25
Q

How is iprtropium bromide used in practice?

A
  • Quaternary anticholinergic agent
  • Bronchodilation develops more slowly and less intense than adrenergic agonist. Response may last up to 6 hours
  • Useful add-on in acute severe/life-threatening asthma or moderate exacerbation with poor response to initial therapy
26
Q

What are the side effects of LAMAs?

A
  • Dry mouth
  • Urinary retention
  • Glaucoma (risk with nebulisation)
27
Q

What is severe asthma?

A

Severe Asthma: Any One of the following

  • Unable to complete sentences
  • Pulse ≥ 110 beats/min
  • Respiration ≥ 25/min
  • Peak Flow 33%-50% of best or predicted
28
Q

How is acute severe asthma treated?

A
  • Oxygen, high flow (aim to keep O2 94-98% sat)
  • Nebulised salbutamol - continuous if necessary, oxygen driven
  • Oral prednisolone ~40 mg daily for 10-14 days - can be stopped without tailing down
  • If moderate exacerbation not responding, or acute severe/life threatening, add nebulised ipratropium bromide
  • Consider IV aminophylline if no improvement and life threatening features not responding to above treatment (BEWARE if taking oral theophylline).
29
Q

What are the features of life threatening asthma?

A 
Life threatening features. All the severe symptoms plus any one of:
"	PEF <33%
"	sPO2 <92
"	PaO2 <8 kPa
"	PaCO2 >4.5 kPa
"	Silent chest
"	Cyanosis
"	Feeble respiratory effort
"	Hypotension, bradycardia, arrhythmia
"	Exhaustion, confusion, coma

Pharmacology Drugs (22 decks)

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