PHARMACOLOGY OF

ASTHMA
HE NDR A WAN A NUR AM I N

DEPARTMENT OF PHARMACOLOGY
MEDICAL FACULTY
LAMBUNG MANGKURAT UNIVERSITY
Respiratory Diseases
Any disease
process that
interferes with gas
exchange in the
lungs changes the
concentrations of
oxygen and
carbon dioxide in
the blood.
COPD
Chronic Obstructive Pulmonary Disease:
Caused by emphysema and chronic bronchitis
Causes irreversible changes to respiratory
system
Emphysema disease process with destruction
to alveoli caused by air pollution, tobacco
smoke, respiratory irritants
Chronic bronchitis symptoms include:
Productive cough, difficulty breathing,
increased respiratory infections, and restriction
of physical activity
Asthma
Respiratory Triggersfor asthma
condition include:
characterized by: Allergens
Bronchoconstrictio Air pollutants
n Cold air
Shortness of breath Infections
Wheezing Exercise
Chemical Mediators
During
the inflammatory process
chemical mediators are released:
Histamine:
Causes bronchoconstriction and mucosal
edema
Eosinophilic chemotatic factor of
anaphylaxis (ECF-A):
Attractseosinophils to site of irritation
Prolongs and worsens inflammation and the
asthmatic process
Chemical Mediators
Prostaglandins and leukotrienes:
Derived from arachadonic acid
Bronchoconstriction
Edema
Mucus production

Leukotrienes:
Potent bronchoconstrictors (LT-1)
Long durations of action
PHARMACOTHERAPY OF
ASTHMA
Role of Autonomic Nervous
System
Sympathetic stimulation increases cyclic
AMP, producing bronchodilation.
Parasympathetic stimulation produces
bronchoconstriction and increased
mucus secretion.
Sympathomimetic drugs produce
bronchodilation.
Bronchodilators
Beta-Adrenergic Drugs:
MOA: stimulate beta-2 receptors in lungs,
which causes bronchodilation
IND:
Prevention of bronchospasm
Treatment of bronchospasmrescue
treatment
Prevention of exercise-induced asthma
2
Bronchodilators
Beta-Adrenergic Drugs:
Side effects:
Nervousness
Skeletalmuscle tremors
Increased heart rate
Beta-Adrenergic Drugs
Epinephrine, Isoproterenol, ephedrine
Selective beta-2 drugs
Albuterol (salbutamol) -immediate action, 4-6
hour duration
Pirbuterol -immediate action, 4-6 hour
Formoterol -10-20 min onset, 12+ duration
Levalbuterol -immediate action, 4-6 hour
Metaproterenol -immediate action, 4-6 hour
Salmeterol - 10-20 min onset, 12+ duration
Terbutaline -immediate action, 4-6 hour
Bronchodilators
Methylxanthine Drugs:
MOA: inhibits phosphodiesterase, leading to
increased cyclic AMP
Physiologic effect: direct relaxation of
respiratory tract, leading to bronchodilation
IND: chronic bronchitis and COPD
Side effects: nausea and vomiting, flushing,
vasodilation, and hypotension, may cause
excessive cardiac stimulation
Methylxanthines
Caffeine
Theophyllinederivates theophylline,
aminophylline
Theobromine
Plant compound found naturally in tea,
cocoa and coffee (methylxanthine)
Bronchodilators
Anticholinergic Drugs:
MOA: block the action of acetylcholine,
leading to bronchodilation
IND: first-line therapy in the treatment of
COPD
Administered by oral inhalation, as little
drug is absorbed systemically
Bronchodilators
Ipratropium Bromide (Atrovent):
A quaternary derivative of atropine
IND: asthma and COPD
Side effects: excessive drying of mouth and
upper respiratory system
Tiotropium:
Similar to ipratropium but longer duration of
action
Antiinflammatory Drugs
Corticosteroids:
MOA: interfere with all stages of the
inflammatory and allergic response (inhibits
inflammatory mediators from mast cells)
Potent antiinflammatory actions
IND: control of chronic asthma and COPD
Main route of administration is oral inhalation,
but may be used systemically to treat initial
acute phase of inflammation
Adverse effects: oral infections, hoarseness, and
vocal cord disturbances
Corticosteroids
Adverse effects associated with systemic
steroid use include fluid retention, muscle
wasting, metabolic disturbances, and
increased susceptibility to infection.
Antiinflammatory Drugs
Antiinflammatory Drugs
Leukotriene Inhibitor Drugs:
zileuton (Zyflo)
MOA: prevent synthesis of leukotriene or
block the leukotriene receptor
IND: control of chronic asthma
Adverse effects:
Nausea, diarrhea, rash, headache, increased
liver enzymes, fever, dark urine, clay-colored
stools, or jaundice (signs of liver toxicity)
Antiallergic Agents
Cromolyn sodium:
MOA: interferes with antigen-antibody reaction
of mast cells
Prophylaxis, need more time (weeks), use of
bronchodilator
IND: prophylactic control of chronic asthma
Adverse effects:
Nasal stinging
Nasal irritation
Headache
Bad taste
Antiallergic Agents
Omalizumab (Xolair):
MOA: binds to and inactivates IgE
IND: reduction of the severity and
frequency of asthma attacks
Adverse effects:
Pain and inflammatory reaction at site of
injection
Mucolytics and Expectorants
Mucolytics:
Liquefy bronchial mucus dissolve mucoprotein and
mucopolysachharide bonds
Enable mucus to be removed by coughing or suction
apparatus
Acetylcysteine (added to bronchodilator to decrease
irritation, via nebulizer)
Bromhexin
Ambroxol
Expectorants: (Mucinex)
Facilitate removal of thickened mucus from the lungs, tx:
unproductive cough
Guaifenesin (GG)
Anti Histamine
Current evidence
does not support for
Asthma treatment.
2nd gen
antihistamines
reduce symptoms of
allergic asthma in
certain patients and
exacerbation in
adult patients with
Allergic Rhinitis.
Bronchodilators
References
Basic & Clinical Pharmacology by Bertram G.
Katzung(11th Edition). The McGraw-Hill Companies
Inc
Goodman & Gilmans Manual of Pharmacology
and Therapeutics (11th ed)
Farmakologi dan Terapi FK UI (edisi 5)
DiPiro JT, et al. Pharmacotherapy: A
Pathophysiologic Approach 6th Ed. San Fransisco:
McGraw Hill, 2005
Global Initiative for Asthma. Pocket Guide for
Asthma Management and Prevention (updated
2012)
 Contact: hendranuramin@gmail.com
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