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Z. PHIRI
Department of Pharmacology
Midlands State University
overview
• Asthma is a chronic inflammatory disease of
the airways
• Has episodes of acute bronchoconstriction
causing
shortness of breath
cough
chest tightness
Wheezing
rapid respiration
Pathogenisis of Asthma
Asthma Pharmacotherapy
• Drugs are used for Quick relief and Long-term
control
• Quick relief medications are used to relieve
acute exacerbations and to prevent exercise-
induced bronchoconstriction (EIB) symptoms.
– short-acting beta agonists (SABAs),
– anticholinergics ( severe exacerbations),
– systemic corticosteroids
Asthma Pharmacotherapy
• Long-term control medications include
-inhaled corticosteroids (ICSs)
-long-acting beta agonists (LABAs)
-long-acting anticholinergics
-combination ICS and LABAs
• Inhaled corticosteroids are the drug of choice
• but is characterized by wide variability in
response among patients glucocorticoid-induced
transcript 1 gene (GLCCI1)
Inhaled Corticosteroids
• Steroids most potent anti-inflammatory agents.
• ICS are topically active, poorly absorbed, and least
to cause AE.
• e.g. Ciclesonide; Beclomethasone; Fluticasone; Budesonide; Mometasone
• Corticosteroids inhibit the release of arachidonic acid
through phospholipase A2 inhibition,
• Targets underlying airway inflammation by
decreasing the inflammatory cascade,
reversing mucosal edema,
decreasing the permeability of capillaries, and
inhibiting the release of leukotrienes;
decreases airway hyperresponsiveness
Adverse effects
• Airway inflammation
• nonsedating antihistamines.
• They compete with histamine for histamine receptor type 1 (H1)
receptor sites in the blood vessels, GI tract, and respiratory tract,
which, in turn, inhibits physiologic effects that histamine normally
induces at the H1 receptor sites.
• Other adverse effects (eg, anticholinergic symptoms) are generally
not observed.
• Topical azelastine and olopatadine are nasal sprays antihistamines.
• azelastine is effective at managing both allergic and nonallergic
rhinitis.
• Cetirizine , Levocetirizine, Fexofenadine , Loratadine
• Desloratadine – Long-acting tricyclic histamine antagonist selective
for H1-receptor. Major metabolite of Loratadine,
Leukotriene receptor antagonists