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Respiratory Pharmacology > Bronchial Asthma > Flashcards

Bronchial Asthma Flashcards

1
Q

Mention non-pharmacological treatment of asthma

A

Smoking cessation
Physical activity
Avoid NSAIDs

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2
Q

Mention as-needed reliever in all steps of BA & its alternative

A

Low dose ICS may be given ICS/formoterol as formaterol has rapid onset with rapid relief
A: SABA

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3
Q

Mention initial treatment in all 5 steps of BA

A 
Step 1: Low dose ICS-formoterol
Step 2: Low dose ICS or as-needed low dose ICS - Formoterol
Step 3: Low dose ICS - LABA
Step 4: Medium dose ICS + LABA
Step 5: High dose ICS + LABA
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4
Q

Describe mechanism of selective beta2 agonist

A

Increase intracellular cAMP:

  1. Bronchodilatation
  2. Mast cell stabilization
  3. Increased bronchial mucocilirat clearnace
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5
Q

Mention examples of SABA & routes of administration

A

Salbutamol (albuterol) , terbutaline

Inhalation, oral, IV

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6
Q

Describe indications of action of SABA

A

-Rapid onset & short acting (4hrs) used as short-term reliever in Asthma & COPD, prophylactic in exercise induced asthma (10 min before).

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7
Q

Mention examples & routes of administration of LABA

A

Salmeterol - formeterol

Inhalation

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8
Q

Mention adverse effects of Selective beta2 agonists

A

Tremors, tachycardia, tolerance, hypokalemia, hypoxemia.

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9
Q

GR: Selective beta2 agonists cause tolerance & hypoxemia

A

T: down rehulation of beta receptor with regular use.
H: V/Q ratio worsens (b2 stimulation, vasodilation mora than BD, insufficient oxygenation)

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10
Q

Unlike other LABA, formeterol can be used as ….. + …..

A

Rescue medication (rapid onset) + ICS

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11
Q

GR: LABA should never be administered alone.

A

As their anti-inflammatory effect is insignificant & their bronchodilator effect masks the progression in asthma severity so inc risk of mortlaity.

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12
Q

GR: Epinephrine is rarely used in asthma

A

It is replaced by selective b2 agonists due to shorter action, non-selectivity leading to tachycardia, arrhythmia & inc BP.

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13
Q

Uses of epinephrine

A

Bronchospasm esp in anaphylaxis

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14
Q

GR: Ephedrine is rarely used

A

CNS side effects & availability of more effective agents

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15
Q

Route of administration of antimuscurinic drugs.

A

Inhalation alone or w/ b2 agonists

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16
Q

Mechanism of action of antimuscarinic drugs

A

M3 receptors in bronchial musculature, blockade of vagally-mediated bronchospasm and mucus secretion.

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17
Q

Indications of ipratropium

A
  1. Bronchodilator in BB-induced asthma, that due to psychogenic stimuli & patients intolerant to b2 agonists/ theophylline esp cardiac, elderly & thyrotoxic patients.
  2. Adujant to b2 agonists
  3. COPD
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18
Q

Disadvantages of ipratropium

A
  1. Tolerance: due to acting on M2 as well as M3

2. Delayed onset of action & less effective than b2 agonists in asthma

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19
Q

Use & advantage of tiotropium

A

Maintenance therapy in COPD

It is not associated with tolerance

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20
Q

Caffeine is more selective on ………, while theophylline is more selective on …….. .

A

CNS & cerebral vessels

Smooth muscles

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21
Q

Mechansim of action of methylxathines

A
  1. Inhibit phosphodiesterase, inc cAMP:
    a. Direct BD
    b. Anti-inflammatory, dec mast cell mediators & cytokines.
  2. Block adenosine receptors, BD
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22
Q

Methylxanthines are metabolized in …. By ….

A

Liver, CYP450

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23
Q

Factors increasing theophylline serum level

A

Neonates & elderly, hepatoc disease, heart failure, viral infections, enzyme inhibitors (erythromycin, OC, cipro, zileuron, zafirlukast)

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24
Q

Factors decreasing theophylline serum level

A

Children, heavy smokers & drinkers, enzyme inducers (rifampicin, phenobarbital, phenytoin, carbamazepine)

25
Q

Describe the anti-asthma & skeletal muscle effects of theophylline

A
  1. Bronchodilation (for acute) , anti-inflammatory (for chronic)
  2. Inc contractility & reverse fatigue of diaphragm in COPD
26
Q

Mention CNS pharmacological & adverse effects of theophylline

A

P: alertness, respiratory stimulant
A: insomnia, anxiety, headache, convulsions, tremors.

27
Q

Describe CVS pharmacological & adverse effects

A

P: VC of cerebral blood vessels
A: +ve inotropic & chronotropic, sinus tachycardia & arrythmia, VD & hypotension, cardiac arrest.

28
Q

Mention adverse effects of theophylline on GIT

A

Anorexia, nausea, vomitting (CI: peptic ulcer)

Proctitis

29
Q

Effect of theophylline on kidney

A

Weak diuretic action

30
Q

GR: Increased risk of toxicity with theophylline (disadvatages of theophylline

A

Narrow safety margin
Saturation kinetics requiring drug monitoring
High Risk of drug interactions

31
Q

Indications of theophylline

A
  1. 2nd or 3rd line of treatment in BA, for relief of acute bronchospasm, long-term control esp nocturnal asthma (SR), acute severse asthma.
  2. COPD
  3. Neonatal apnea
32
Q

Aminophylline is

A

Theophylline & ethylenediamine to increase solubility

33
Q

Indication of SR theophylline

A

Control medication & in nocturnal dyspnea, as it is long acting

34
Q

Advantages of low dose theophylline

A

Full anti-inflammatory effect

No need to monitor level

35
Q

What is the goal of asthma treatment?

A

To achieve and maintain clinical control (by suppressing inflammation using long term controller medication)

36
Q

What is the mechanism of action of glucocorticoids in asthma?

A

Immunosuppresive & anti-inflammatory: inhibit phosphodiesterase, dec influx of inflammmatory cell/mediators, dec bronchial inflammation & hyper-responsiveness.
-Potentiate beta2 agonists: downregulate b2 receptors

37
Q

Indications of corticosteroids in asthma

A
  1. Control medication
  2. Rescue medication in acute exacerbations not responding to b2 agonists
  3. Acute severe asthma
38
Q

GR: Oral corticosteroids should be given in the early morning.

A

To coincide with circadian rhythm of CS to dec adrenal suppression.

39
Q

Ciclesonide is a prodrug activated by ……

A

Bronchial esterases

40
Q

Advantages of Ciclesonide over other ICS

A

High 1st pass metabolism & tight plasma protein binding, less systemic side effects
Less frequent candidiasis

41
Q

Adverse effects of glucocorticoids

A
  1. Oropharyngeal candidiasis
  2. Hoarseness of voice
  3. Cataract - glaucoma
  4. Osteoporosis
  5. Retardation of growth
  6. Hypertension
  7. Diabetes
  8. Cushing syndrome
  9. Adrenal suppression
42
Q

Side effects of glucocorticoids are minimized by

A
  • Gargling & spitting following inflammation

- Use of spacer device

43
Q

Mention limitations of zileuton

A

Liver toxicity & frequent dosing

44
Q

Describe the mechanism of Zafirlukast-Montelukast.

A

LTs receptor anatgonists, bronchodilation & anti-inflammatory

45
Q

Mention indications of Montelukast

A
  1. Control medications in persistent asthma:
    - Alternatives to inhaled steroids in mild persistent asthma (for patients intolerant to steroids or cannot use inhalers)
    - Added in moderate to severe cases
  2. Aspirin induced asthma
  3. Exercise-induced asthma (prophylactic)
46
Q

Advantages of Motelukast

A
  1. Oral therapy (easier than inhalation)
  2. Long duration of action
  3. Well-tolerated (minimal side effects)
47
Q

Adverse effects of Leukotriene pathway inhibitors

A
  1. Headache & dyspepsia
  2. Elevated livers enzymes (zileutin, zafirlukast)
  3. Enzyme inhibition (zafirlukast)
48
Q

Mechanism of action of cromolyn & nedocromil

A
  1. Inhibit mast cells degranulation, inhibit release of mediators, inhibit early response.
  2. Inhibit eosinophil activation, inhibit late inflammatory response to antigen.
49
Q

Route of administration of cromolyn & nedocromil

A

Aerosol & microfine powder

50
Q

Uses of cromolyn & nedocromil

A

Prophylaxis of antigen & exercise-induced asthma .
Chronic use for mild persistent asthma , dec bronchial hyper-responsiveness.
Allergic rhinoconjunctivitis

51
Q

Adverse effects of cromolyn & nedocromil Na

A
  1. Throat irritation, cough, bronchospasm.

2. Stinging in the eye (with eye drops).

52
Q

Mechanism of action of Ketotifen

A

Mast cell stabilization & antihistamine

53
Q

Mechanism, usage, adverse effects of omalizumab

A

Anti-IgE monoclonal antibody
Add-on therapy in severe uncontrolled allergic asthma
Inc risk of anaphylaxis & reaction at the site of injection

54
Q

Anti IL5 uses & adverse effects

A

Add-on therapy in severe uncontrolled allergic asthma

Headache & reaction at site

55
Q

Anti IL4 uses & adverse effects

A

-Add-on therapy in severe uncontrolled allergic asthma on high dise ICS/LABA
-Atopic dermatitis
+injection site reaction, blood eosinophilia

56
Q

Management of mild to moderate acute exacerbations

A

Give inhaled SABA
Prednisolone
Controlled oxygen

57
Q

GR: Severe acute asthma is refractory to the usual lines of treatment.

A

Due to down regulation of beta receptors, mucus plug & acidosis.

58
Q

Management of severe acute asthma

A
  1. Endotracheal intubation & suction of bronchial secretion
  2. Humidified oxygen inhalation
  3. IV fluids, correction of acid-base balance, electrolytes, dehydration.
  4. Drug therapy
59
Q

Drug therapy of severe acute asthma

A 
A. SABA +/- ipratropium
B. Systemic glucocorticoids
C. Aminophylline
D. Artificial respiration
E. Antibiotics/avoid sedatives

Respiratory Pharmacology (3 decks)

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