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Pharmacology > Drugs Used In Asthma > Flashcards

Drugs Used In Asthma Flashcards

1
Q

Classification of drugs used in asthma

A

Bronchodilators:
1. Selective beta-2 adrenoceptors agonist: salbutamol (SABA) & Salmeterol (LABA)

  1. Xanthine derivative : Theophylline & Aminophylline
  2. Anitimuscarinic drugs: Iptropium, Titropium, Oxitropium.

Anti-inflammatory drug:
1. Glucocorticoids : Beclomethazone, Fluticasone, Budenoside.

  1. Mast cells stabilizer: Cromolyn
  2. 5-lipoxygenase inhibitor: Zileuton
  3. Leukotriene receptor antagonist: Montelukast, Zafirlukast.
  4. Monoclonal anti-IgE antibodies: Omalizumab
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2
Q

MOA of Beta-2 Adrenoceptors agonists.

A
  1. Stimulate adenyl cyclase and increase cAMP in smooth muscles causing bronchodilation.
  2. Decreases intracellular calcium inactivation k+ channels.
  3. Inhibits myosin light chain kinase
  4. Relax airways
  5. Inhibit microvascular leakage
  6. Increase mucociliary transport.
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3
Q

Adverse effects of beta-2 adrenoceptors agonist.

A
  • Muscle tremor
  • Tachycardia
  • cardiac arrhythmia
  • Palpitation
  • worsen glucose intolerance in diabetes.
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4
Q

Clinical use of Beta-2 Adrenoceptors agonist drugs.

A
  1. Salbutamol, terbutaline, metaproterenol (Short-acting drugs)
    Useful in acute asthma, it has a fast onset of action.
  2. Salmeterol, Formeterol (Long- acting drugs)
    Useful for long term or chronic cases
    It resistant to desensitisation.
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5
Q

Beta 2 adrenoceptors agonist is combine with other drugs. What is it and why?

A

Beta-2 adrenoceptors agonist is combined with steroid.
Beta-2 adrenoceptors agonist drugs show tolerance due to down-regulation of receptors.
Steroid able to inhibit down-regulation.
Thus, combination of beta-2 adrenoceptors agonist drugs with steroids is recommended.

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6
Q

3 main MOA of xanthine derivative (Theophylline).

A
  1. Competitive inhibition of adenosine receptors.
    - blockade of adenosine receptors can inhibit early inflammatory process.
    - adenosine receptors stimulate: release of cytokines, respiratory depression and bronchoconstriction.
  2. Inhibition of phosphodiesterase enzyme
    - phosphodiesterase enzyme hydrolyze cyclic AMP (cAMP) to 5’ AMP.
    - inhibition of this enzyme cause an increase of cAMP, thus result in bronchodilation.
  3. Acetylation of core histone for inflammatory gene transcription.
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7
Q

Adverse effect of Theophylline

A
  • Gastrointestinal distress
  • tremor
  • CNS-alertness
  • hypotension
  • bradycardia
  • convulsion
  • arrhythmia
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8
Q

MOA of anitimuscarinic drugs

A

Exp: Iptropium (SAMA), Titropium (LAMA)

  • it is anticholinergic by blocking the muscarinic receptors
  • Produce bronchodilation by blocking contraction of airways. So, decrease secretion.
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9
Q

Titropium is long-acting drug. What is clinical use?

A
  • treat COPD

- Allergic rhinitis

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10
Q

Adverse effects of anitimuscarinic drugs

A
  1. Decrease salivary and lacrimal secretion
  2. Glaucoma
  3. Urinary retention
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11
Q

MOA of monoclonal anti-IgE antibodies : Omalizumab

A

It binds to IgE on sensitized mast cells and prevents release of mediators and asthma.

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12
Q

Clinical use of omalizumab

A

Useful for treatment of moderate to severe allergic asthma with non responding to conventional therapy

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13
Q

MOA of Glucocorticoids /Corticosteroids

A

Exp: Beclomethazone, Flucasone, Budenoside (potent anti-inflammatory drugs)

  • inhibits phospholipase A2 activity
  • result in reduce Bronchial oedema.
  • inhibit release of inflammatory mediators such as prostaglandin, Leukotriene from COX and LOX pathway.
  • inhibit antibody formation
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14
Q

Drug administration of Glucocorticoids?

A

MDI (metered dose inhibitors)

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15
Q

Adverse effects of Glucocorticoids

A
  1. Oropharyngeal candidiasis
  2. Dysphonia
  3. Growth retardation
  4. Hypothalamic-pituitary suppression
  5. Osteoporosis
  6. Weight gain
  7. Diabetes
  8. Myopathy
  9. Psychiatric disturbances
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16
Q

MOA of mast cells stabilizer (Cromolyn /cromoglycate)

A
  • it stabalise mast cells, decrease the release of mediators like leukotriene and histamine.
  • inhibit calcium influx into the mast cells.
  • alternate the function of chloride channels, thus inhibit cellular activation.
17
Q

Cromolyn is safe for?

A

Pregnancy

18
Q

Adverse effects of Cromolyn

A
  1. Cough and bronchospasm
  2. Hypersensitivity (rare)
  3. Urticaria
  4. Anaphylaxis
19
Q

Adverse effect of Zileuton

A

Hepatotoxicity

20
Q

Adverse effect of Montelukast (leukotriene receptor inhibitor)

A
  1. Headache
  2. Rashes
  3. Hepatotoxicity
  4. Neuropathy
  5. Churg strauss syndrome (esonophilia, vasculitis)

Pharmacology (16 decks)

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