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*Beta-2 agonist
-b2-adrenergic receptors are the principal subtype expressed in bronchial tissue
-Activation of these receptors produces relaxation of airway smooth muscle
-Oral, injected, and inhaled (preferred) preparations are available
-The drug dose can also be delivered by nebulizers
-b2-adrenergic agonists are preferred for acute asthma and for maintenance
*b-adrenergic agonists (b2): adverse reactions
1)Vasodilatation and Tachycardia
2)Sometimes might cause arrhythmias by stimulation of the sinusal node
3)Anxiety, Tremor and Restlessness
4)Hypokalemia
5)Non b-selective agents (epinephrine, isoproterenol, and ephedrine) should not be used in patients receiving monoamine oxidizers
6)Hyperglycemia (i.e., systemic preparation) |
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*Beta-2 agonist
-b2-adrenergic receptors are the principal subtype expressed in bronchial tissue
-Activation of these receptors produces relaxation of airway smooth muscle
-Oral, injected, and inhaled (preferred) preparations are available
-The drug dose can also be delivered by nebulizers
-b2-adrenergic agonists are preferred for acute asthma and for maintenance
*b-adrenergic agonists (b2): adverse reactions
1)Vasodilatation and Tachycardia
2)Sometimes might cause arrhythmias by stimulation of the sinusal node
3)Anxiety, Tremor and Restlessness
4)Hypokalemia
5)Non b-selective agents (epinephrine, isoproterenol, and ephedrine) should not be used in patients receiving monoamine oxidizers
6)Hyperglycemia (i.e., systemic preparation) |
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*Long-Acting Beta- Agonists
*acts rapidly and can be used for acute asthma
-Safer than short acting beta agonists
-Should not be used as monotherapy
*b-adrenergic agonists (b2): adverse reactions
1)Vasodilatation and Tachycardia
2)Sometimes might cause arrhythmias by stimulation of the sinusal node
3)Anxiety, Tremor and Restlessness
4)Hypokalemia
5)Non b-selective agents (epinephrine, isoproterenol, and ephedrine) should not be used in patients receiving monoamine oxidizers
6)Hyperglycemia (i.e., systemic preparation) |
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*Long-Acting Beta- Agonists
*slow onset; not useful for acute asthma
-Safer than short acting beta agonists
-Should not be used as monotherapy
*b-adrenergic agonists (b2): adverse reactions
1)Vasodilatation and Tachycardia
2)Sometimes might cause arrhythmias by stimulation of the sinusal node
3)Anxiety, Tremor and Restlessness
4)Hypokalemia
5)Non b-selective agents (epinephrine, isoproterenol, and ephedrine) should not be used in patients receiving monoamine oxidizers
6)Hyperglycemia (i.e., systemic preparation) |
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*Muscarinic Antagonists
Anticholinergic Drugs: Muscarinic (M3) antagonists
-Muscarinic (M3) receptor antagonist: Ipratropium & Tiotropium
-Weak association between asthma and the cholinergic system
-Compared to b2 agonist, M3 antagonists have limited value in asthma
-Ipratropium is used in combination with Albuterol (b2 agonist)
-Rationale of using M3 antagonists:
1. to block the excitatory effect of M3 receptor on bronchial muscle contraction
2. to reduce mucus secretion at the level of the bronchial epithelium
-Inhaled preparations are available
-Ipratropium has a fast onset (5-15 min) and short lasting (4-6 hours) effect
-Tiotropium bromide (Spiriva™) is the long acting version: half life of 5-6 days
*Low incidence of side effects. They are limited to the gastrointestinal system. |
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*Muscarinic Antagonists
Anticholinergic Drugs: Muscarinic (M3) antagonists
-Muscarinic (M3) receptor antagonist: Ipratropium & Tiotropium
-Weak association between asthma and the cholinergic system
-Compared to b2 agonist, M3 antagonists have limited value in asthma
-Ipratropium is used in combination with Albuterol (b2 agonist)
-Rationale of using M3 antagonists:
1. to block the excitatory effect of M3 receptor on bronchial muscle contraction
2. to reduce mucus secretion at the level of the bronchial epithelium
-Inhaled preparations are available
-Ipratropium has a fast onset (5-15 min) and short lasting (4-6 hours) effect
-Tiotropium bromide (Spiriva™) is the long acting version: half life of 5-6 days
*Low incidence of side effects. They are limited to the gastrointestinal system. |
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*Inhaled Glucocorticoids
Corticosteroids and asthma
-Up-regulation of b2 receptors
-Inhibit the response to inflammation and decrease bronchial reactivity
-Decrease cytokines production (late-phase reaction)
-Inhaled (ICS) and oral preparations are available
-Commonly used in combination therapy with long-acting b2 agonists (Salmeterol/Fluticasone & Budesonide/Formoterol)
*ICS have no role in acute asthma
-Long-term systemic therapy (more than three weeks) should be restricted to patients who do not respond to ICS, beta agonists or a combination of these drugs
*Adverse Reactions: ICS are much safer agents than systemic steroids
- hoarseness
- oropharyngeal candidiasis
- coughing or wheezing
- detectable changes in serum cortisol appears with ICS >800 mg/day (adult)
- HPA axis suppression usually occurs with ICS >1600 mg/day (adult) |
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*Inhaled Glucocorticoids
Corticosteroids and asthma
-Up-regulation of b2 receptors
-Inhibit the response to inflammation and decrease bronchial reactivity
-Decrease cytokines production (late-phase reaction)
-Inhaled (ICS) and oral preparations are available
-Commonly used in combination therapy with long-acting b2 agonists (Salmeterol/Fluticasone & Budesonide/Formoterol)
*ICS have no role in acute asthma
-Long-term systemic therapy (more than three weeks) should be restricted to patients who do not respond to ICS, beta agonists or a combination of these drugs
*Adverse Reactions: ICS are much safer agents than systemic steroids
- hoarseness
- oropharyngeal candidiasis
- coughing or wheezing
- detectable changes in serum cortisol appears with ICS >800 mg/day (adult)
- HPA axis suppression usually occurs with ICS >1600 mg/day (adult) |
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*Leukotriene Antagonists
Cysteinyl leukotriene (Cys-LT1) antagonists: Montelukast & Zafirlukast
-Weak anti-inflammatory and bronchodilator actions
-It does not appear to be useful by itself in patients with moderate to severe asthma
-Rationale of using Montelukast: selective inhibition of leukotriene receptor Cys-LT1
1. to block leukotriene-induced bronchial muscle contraction
2. to block leukotriene-induced pro-inflammatory agents
• Adding anti-Cys-LT1 to ICS therapy in patients with moderate asthma is beneficial
• Its lower the doses of corticosteroids in patients on daily steroid therapy
-Leukotrienes (LTs) are released from eosinophils mast cells and macrophages
-Increase cytokine production
-Anti-LTs also have been used successfully by some authors to control rhinitis, atopic dermatitis, and urticaria |
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*Leukotriene Antagonists
Cysteinyl leukotriene (Cys-LT1) antagonists: Montelukast & Zafirlukast
-Weak anti-inflammatory and bronchodilator actions
-It does not appear to be useful by itself in patients with moderate to severe asthma
-Rationale of using Montelukast: selective inhibition of leukotriene receptor Cys-LT1
1. to block leukotriene-induced bronchial muscle contraction
2. to block leukotriene-induced pro-inflammatory agents
• Adding anti-Cys-LT1 to ICS therapy in patients with moderate asthma is beneficial
• Its lower the doses of corticosteroids in patients on daily steroid therapy |
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*Antibodies
**Omalizumab is a recombinant DNA-derived humanized IgG1k monoclonal antibody that selectively binds to human immunoglobulin E (IgE). IgE is commonly involved with allergies when present in high amounts in the body.
-is a humanized antibody drug approved for patients with moderate-to-severe or severe allergic asthma, which is caused by hypersensitivity reactions to certain harmless environmental substances. Omalizumab's cost is high ($10,000 to $30,000 per year), as compared to other drugs used for asthma, and hence omalizumab is mainly prescribed for patients with severe, persistent asthma, which cannot be controlled even with high doses of corticosteroids. Like other protein and antibody drugs, omalizumab causes anaphylaxis (a life-threatening systemic allergic reaction) in 1 to 2 patients per 1,000.[1] |
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