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Y2S1-Pharmacology > Drugs used for asthma > Flashcards

Drugs used for asthma Flashcards

1
Q

What is meant by status asthmaticus?

A

It is a severe emergency condition of asthma that requires immediate and urgent treatment, hence the use of inhalers with a very rapid onset like salbutamol or IV drugs

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2
Q

Describe the pathobiology of asthma

A

Immediate Phase:
This phase triggers bronchial hyperreactivity and spasms. The primary goal here is to relieve the bronchospasm.

Delayed Phase:
When chemotaxins activate inflammatory cells, it leads to a delayed phase characterized by increased hyperreactivity, bronchospasm, and airway inflammation. There is also mucus production and inflammatory cells infiltrate the bronchial walls.

Therefore, in treating obstructive lung diseases, the therapeutic approach focuses on targeting bronchospasm, inflammation, or both.

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3
Q

What triggers bronchodilation?

A
  • The sympathetic system

1) cAMP

  • Triggered by the release of nor/and epinephrine
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4
Q

What triggers bronchoconstriction?

A
  • The parasympathetic system

1) Acetylcholine

2) Adenosine

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5
Q

What inhibits bronchoconstriction?

A

1) Theophylline

2) Muscarinic antagonists

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6
Q

What type of sympathetic receptors are found in the bronchi?

A

B-2 receptors

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7
Q

What type of parasympathetic receptors are found in the bronchi?

A

Muscarinic-1 receptor

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8
Q

What are some examples of (SYMPATHOMIMETIC AGENTS)
Beta2-Selective Drugs?

A

Short-acting:

1) Salbutamol (short-acting)

2) Pirbuterol

3) Terbutaline

4) Metaproterenol

Long-acting: (not used for acute attacks)

5) Salmeterol

6) FORMOTEROL

Ultra-Long-Acting:

7) Indacaterol

8) Vilanterol

  • They reverse bronchospasm
  • They are effective in the immediate phase (acute phase) not the delayed phase
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8
Q

What are the different families of medications to treat asthma?

A

1) SYMPATHOMIMETIC AGENTS
Beta2-Selective Drugs

2) METHYLXANTHINE DRUGS

3) LEUKOTRIENE PATHWAY INHIBITORS

4) ANTIMUSCARINIC AGENTS

5) Inhaled CORTICOSTEROIDS (ICS)

6) TARGETED (MONOCLONAL ANTIBODY) THERAPY

7) CROMOLYN & NEDOCROMIL

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9
Q

What is the mechanism of action of (SYMPATHOMIMETIC AGENTS)
Beta2-Selective Drugs?

A

1) Action: Bronchodilation

2) MOA: it decreases the calcium-mediated contraction in the bronchioles, by increasing cAMP which activates protein kinase-A, PKA will inhibit MLCK “myosin light chain kinase” (a mediator of contraction)

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10
Q

How are the (SYMPATHOMIMETIC AGENTS) Beta2-Selective Drugs absorbed and eliminated by the body?

A

1) Absorbed by inhalation

2) Excreted unchanged

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11
Q

What are the clinical uses of (SYMPATHOMIMETIC AGENTS)
Beta2-Selective Drugs?

A

1) Acute asthma attack

2) Preventing exercise-induced asthma attacks

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12
Q

What is the first-line drug for acute asthma attacks?

A

SYMPATHOMIMETIC AGENTS Beta2-Selective Drugs

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13
Q

When do we use the LABA

A

In patients needing prolonged broncho-dilating therapy

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14
Q

Why should we administer Inhaled corticosteroid with ULTRA-LABA

A

Because they can mask the symptoms of bronchial inflammation

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15
Q

What are some examples of METHYLXANTHINE DRUGS?

A

1) Theophylline (aminophylline i.v. form)

2) Theobromine

3) Caffeine

4) Roflumilast

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16
Q

What is the mechanism of action of the methylxanthine drugs?

A

The increase in the amount of cAMP by inhibiting phosphodiesterase PDE4, inducing bronchodilation

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17
Q

Which drug is a selective PDEE inhibitor?

A

Roflumilast

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18
Q

When is roflumilast indicated?

A

It is indicated when we need to decrease the exacerbation of severe COPD

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19
Q

Which class of drug is the second-line treatment for chronic asthma, that is not controlled by B2-agonist?

A

Methylxanthine drugs

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20
Q

Can we add theophylline to the inhaled B2 agonist?

A

No, Because it does not increase the bronchodilator response and may increase their side effects

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21
Q

What are the adverse effects of methylxanthine drugs?

A

1) Tachycardia

2) Dysrhythmia

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22
Q

What are some examples of leukotriene pathway inhibitors?

A
  • Leukotriene receptor antagonist

1) Montelukast

2) Zafirlukast

  • Lipoxygenase enzyme inhibitor

3) Zileuton

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23
Q

Which leukotriene pathway inhibitor inhibits the lipoxygenase enzyme?

A

Zileuton

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24
Q

What is the mechanism of action of the leukotriene pathway inhibitors?

A

1) Inhibition of the lipoxygenase enzyme

2) Inhibition of the leukotriene receptor

  • Inhibiting the action of LTC4, LTD4 & Histamine
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25
Q

Which drug is used as a third-line treatment of asthma?

A

Leukotriene pathway inhibitors

26
Q

Which drug is used in aspirin-induced-asthma?

A

Leukotriene pathway inhibitors

27
Q

What is the first-line treatment of asthma in children?

A

Leukotriene pathway inhibitors as they are chewable and flavored

28
Q

What are the side effects of leukotriene pathway inhibitors?

A

Very few

29
Q

What are some examples of antimuscarinic agents used for asthma?

A

1) Short-Acting-Muscarinic antagonist:

  • Ipratropium bromide (inhaler)

2) Long-acting muscarinic antagonist (once daily)

  • Tiotropium bromide
  • Glycopyrronium bromide
    umeclidinium bromide
30
Q

When are the antimuscarinic agents mainly indicated?

A

In COPD

31
Q

What is the mechanism of action of the anti-muscarinic agents?

A

They induce bronchodilation by competitively antagonizing ACh action on the muscarinic receptors

32
Q

When should we use antimuscarinic agents to treat asthma?

A

We add it to the treatment regimen when the asthma is not controlled by the maximum dose of ICS and LABA

33
Q

What is the drug of choice for COPD patients needing a bronchodilator?

A

LAMA

34
Q

What are the adverse reactions of antimuscarinic agents?

A

1) Urinary retention

2) Dry mouth

3) Pharyngitis

35
Q

Which drug combination is useful for COPD and Asthma?

A

SABA (albuterol) + SAMA (IPRATROPIUM)

36
Q

What are the examples of ICS drugs?

A

1) Triamcinolone

2) Budesonide

3) Ciclesonide

4) Flunisolide

5) Mometasone

6) Fluticasone

37
Q

What is the mechanism of action of the inhaled corticosteroid?

A

They inhibit the transcription factor (Nuclear factor kappa-D), reducing the activation of the inflammatory cells and the release of cytokines

  • Reduces the hyperactivity, and decreases the delayed inflammation phase
38
Q

What are the clinical uses of ICS?

A

Added to bronchodilators to reduce inflammation and used as IV (hydrocortisone) in severe acute asthma

39
Q

What are the adverse effects of ICS?

A

1) Horseness of voice

2) Oral candidiasis

3) Adrenal suppression

40
Q

What are some examples of the targeted monoclonal antibody drugs?

A

1) Omalizumab (anti-IgE)

2) Dupilumab (IL-4 & 13 receptor antagonist)

3) Reslizumab & Mepolizumab (Blocks IL-5)

4) Benralizumab (IL-5 antagonist)

41
Q

Which monoclonal antibody inhibits IL-5?

A

1) Reslizumab

2) Mepolizumab

42
Q

Which monoclonal antibodies are anti-IgE?

A

Omalizumab

43
Q

Which monoclonal antibody is IL-4 & 13 antagonist?

A

Dupilumab

44
Q

Which monoclonal antibody is an IL-5 antagonist?

A

Benralizumab

45
Q

What is the mechanism of action of the monoclonal antibodies?

A

Their overall effect is to decrease the concentration of IgE in the plasma during both the early and late phases

46
Q

What are the clinical uses of monoclonal antibodies?

A

Used in persistent allergic asthma that is not controlled by inhaled corticosteroids

47
Q

What is the mode of administration of the monoclonal antibodies?

A

Given subcutaneously every 2-4 weeks

48
Q

What is the mechanism of cromolyn and nedocromil?

A

They inhibit the allergen by inhibiting the granulation of mast cells

49
Q

What is the mode of administration of cromolyn and nedocromil?

A

Inhalation

50
Q

What is the clinical use of cromolyn and nedocromil?

A

1) Prophylaxis for asthma

2) Reduces the symptoms of allergic rhinitis

51
Q

Which drugs can induce severe refractory eosinophilic asthma?

A

1) Mepolizumab

2) reslizumab

IL-5 inhibitor monoclonal antibodies

52
Q

What is the initial drug of choice in acute bronchospasm?

A

-SAMA

like albuterol

53
Q

What is the most useful drug in treating long-term COPD?

A
  • SAMA

Like ipratropium

  • It is ineffective in relieving acute bronchospasm by itself but can add some broncho-dilating effects to adrenergic agents
54
Q

When is theophylline indicated?

A

Used less often as a second-line drug, usually given orally with extended-release (ER for COPD)

55
Q

Which drugs are given prophylactically?

A

Cromolyn and nedocromil

  • Ineffective in acute bronchospasm
56
Q

Why do we use ICS early in asthma?

A

due to inflammation that is established with asthma, in acute asthma episodes of bronchoconstriction corticosteroids are given orally or IV for several days

57
Q

What should we give for moderate and severe asthma?

A

1) Moderate:

  • ICS + SABA (to prevent bronchoconstriction)

2) Severe:

  • ICS + SABA + LABA
  • Leukotriene pathway inhibitor might be added to control the symptoms and reduce the use of corticosteroids, especially in children
58
Q

What is the advantage of using multidrug regimens?

A

Smaller doses of each can be given

59
Q

What is an example of a combined drug ICS?

A

1) Combivent (albeuterol + ipratropium)

2) Advair (salmeterol + fluticasone)

60
Q

Which class of drugs can cause candidiasis, adrenal suppression, and hoarseness of voice?

A

Inhaled corticosteroid

61
Q

Which class of drug can cause tachycardia and dysrhythmias?

A

Methylxanthine drugs & B2 agonist

62
Q

Which drug can cause urinary retention, dry mouth, and pharyngitis?

A

Antimuscarinic agents

63
Q

Which drugs can cause tremors

A

B2-agonist in addition to the tachycardia and sometimes dysrhythmias

Y2S1-Pharmacology (14 decks)

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