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Pharmaco Ca2 > Asthma > Flashcards

Asthma Flashcards

1
Q

Asthma is due to

A

Chronic airway inflammation and hyperresponsiveness of airway to minute amt of irritant

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2
Q

What is an asthma controller

A

Anti inflammatory to prevent recurrent attack

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3
Q

What is fluticasone

A

Fluticasone is an inhaled corticosteroid that is used as a controller. Anti inflammatory effect

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4
Q

Why is fluticasone inhaled instead of given orally

A

Extensive first pass, clearedby liver asap if given orally

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5
Q

How does fluticasone exert anti inflammatory effect

A

Decrease inflammatory cells in airway dramatically

Decrease shedding of epithelial cells which makes airway sensitive to irritants

Increase macrophage efferocytosis

Down regulate cox2, 5-lox, pla2 at lungs, upregulate pla2 inhibitor annexin 1

Increase b2 receptor expression on airway smooth muscle for bronchodilation

As a result decrease airway hyperresponsiveness due to inflammation, prevent airway wall remodelling, decrease need for beta 2 agonist

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6
Q

What is 1st line prophylactic asthma therapy

A

Fluticasone

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7
Q

Side effects of fluticasone

A

Inhaled corticosteroid.

Immunosuppression leading to opportunistic infections eg oropharyngeal candidiasis

Dysphonia (hoarse throat), cough

Easy bruising due to skin thinning hence small bump can easily break vessel

Adrenal suppression

Post subcapsular cataracts

Osteoporosis

Growth retardation in pediatric patients

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8
Q

Are leukotriene receptor antagonists controllers or relievers?

A

Controller

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9
Q

Mechanism of montelukast

A

Montelukast inhibits leukotriene receptor as it is a competitive antagonist against cysteinyl leukotriene receptor, decreasing pathogenesis of asthma

Leukotrienes cause bronchoconstriction, airway hyper responsiveness, c fibre release of substance p, mucus hypersecretion, airway smooth muscle hyperplasia

Hence montelukast is bronchodilator and anti inflammatory

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10
Q

How is montelukast administered

A

Orally

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11
Q

When do use montelukast

A

Aspirin induced asthma (inhibit cox, increase leukotrienes)

Exercise induced asthma

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12
Q

Compare montelukast and fluticasone

A

Montelukast less effective than ICS

But steroid sparing

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13
Q

Side effects of montelukast

A

Rare psychological reaction, resulting in agitation, hallucination, depression

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14
Q

What does sodium cromoglycate do

A

Asthma controller

Mast cell stabiliser, inhibits mast cell degranulation induced by IgE cross linking with fcE receptor

Promote annexin 1 secretion, inhibit pla2 and block histamine and eicasanoid release from mast cells

Blocks antigen/exercise induced bronchospasm

No bronchodilator effect

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15
Q

How is sodium cromoglycate administered

A

Inhaled solution only for prophylactic control of asthma

Nasal spray/ophthalmic prep for allergic reaction/conjunctivitis

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16
Q

What are the side effects of sodium cromoglycate

A

Throat irritation, mouth dryness, coughing (preventable by inhaling b2 agonist first)

Bitter unpleasant taste

17
Q

What does anti IgE monoclonal antibody do

A

Asthma controller. Depletes igE, prevent mast cell degranulation and decrease mediator release

Anti IgE mab bind IgE to block IgE from binding to receptor

Downregulate fce1 receptor expression

18
Q

Sodium cromoglycate and monoclonal antibodies used for what type of asthma

A

Antigen induced asthma eg allergic asthma, allergic rhinitis

19
Q

What does anti il5/5r and anti il4r mab do

A

Anti il5/5r blocks il5 and reduces eosinophil function

Anti il4r blocks il4 and il13 function

20
Q

What are some disadvantages of using monoclonal antibodies

A

Expensive, only for allergic asthma, delivered subcutaneously (no inhalation/oral)

21
Q

What is an asthma reliever what are the three types of relievers

A

Bronchodilator for rescue therapy

B2 agonist, theophylline, muscarinic antagonist

22
Q

What does salbutamol do

A

B2 agonist, binds to b2 GPCR. Activate adenylnyl cyclase, increase cyclic amp. Decreases intracellular Ca2+ and MLCKinase, increases K+ efflux causing hyperpolarisation. This results in airway smooth muscle relaxation

Mast cell stabilisation

Reduce edema by decreasing microvascular leakiness

Increase mucociliary clearance

23
Q

Compare salbutamol, formoterol, indacaterol, salmeterol

A

Salbutamol is short acting, formoterol and salmeterol long acting (12h) indacaterol long acting (24h)

Indacaterol is used to treat COPD only

Salbutamol is hydrophilic, f and salm amphiphilic, indacaterol is lipophilic

Indacaterol slow onset the rest are rapid onset

24
Q

Describe ICS-LABA combination therapy

A

Used for long term maintenance of nocturnal asthma. Ics-formoterol is reliever of choice. Use Saba salbutamol as reliever/rescue therapy when patient is on ICS-LABA maintenance

25
Q

Side effects of b2 agonists

A

Fine tremor or skeletal muscle when high dose given (tremor is first sign of overdose)

Leg cramps

Peripheral vasodilatation

Cross react with b1 receptor at the heart to cause aspirations, tachycardia

Hyperglycemia and hypokalemia at the liver

26
Q

What happens if LABA b agonist is given alone

A

Asthma related death. B2 downregulated hence rescue therapy not effective

Need to give with ics that increases b2 expression on airway smooth muscle

27
Q

How is theophylline administered

A

Given systemically via tablet or iv

28
Q

3 mechanisms of theophylline

A
  • Inhibit phosphodiesterase to prevent breakdown of cAMP —> decrease intracellular K+, decrease MLCK, increase hyperpolarisation via K+ efflux —> airway smooth muscle relaxation
  • inhibit GPCR adenosine receptor as adenosine can cause asm contraction
  • increase epinephrine release from adrenal medulla to bind to b2
29
Q

Describe use of theophylline

A

Less effective bronchodilator than b2 agonist

Add on therapy to ics-formoterol combination

Increases contractility of fatigue diaphragm to improve lung function in COPD

30
Q

Side effects of theophylline

A

Narrow ti, potential drug drug interaction (ciprofloxacin inhibits metabolism of theophylline)

Anorexia, abdominal discomfort, arrhythmia

31
Q

Name examples of muscarinic antagonists

A

Ipratropium bromide (short acting)

Tiotropium bromide (long acting)

32
Q

Mechanism of action of muscarinic antagonists

A

Bronchodilator/reliever

Decrease mucus secretion

Anti inflammatory because Ach binds to musc receptor of inflammatory cel to trigger inflammation

Inhibit m3 receptor mediated bronchoconstriction

33
Q

When are muscarinic antagonists used

A

Add on therapy to ICS+B2 or when patient intolerant to b2 agonists

More effective for COPD `

34
Q

Side effects of muscarinic antagonists

A

Urinary retention, dry mouth

Paradoxical bronchospasm

Unpleasant taste (like sodium cromoglycate)

Pharmaco Ca2 (11 decks)

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