pharmacotherpy of asthma M pharm 2nd sem. Bronchial asthma is a chronic respiratory disease characterized by inflammation and narrowing of airways in the lungs, which cause difficulty in breathing. Symptoms can include coughing, wheezing, shortness of breath and chest tightness. These symptoms can be mild or severe and can come and go over time. Although asthma can be a serious condition, it can be managed with the right treatment. Asthma affected an estimated 262 million people in 2019 (1) and caused 455 000 deaths.

1. Prepared by,
Abhishek Kumar Gupta
M.Pharm, 2ndSem.
Department of Pharmacology
ISF College of Pharmacy, Punjab
guptaabhishek8199@gmail.com
Pharmacotherapy for Asthma
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2. CONTENT
Sl.No. Title
1. Introduction to Asthma
2. Clinical feature
3. Risk factor
4. Classification and types of asthma
5. Inflammation and asthma symptoms
6. pathophysiology
7. Diagnosis of asthma
8. Drugs for treatment of asthma
9. Bronchodilators
10. Corticosteroids
14. References
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3. 3
OBSTRUCTIVE VS RESTRICTIVE PULMONARY DISEASE
Obstructive Restrictive
Characterized by an increase in resistance to air
flow due to partial or complete obstruction
Characterized by reduced expression of lung
parenchyma accompanied by decreased total lung
capacity
Total lung capacity normal Total lung capacity normal decreased
Asthma, chronic bronchitis, emphysema, and
small- airway disease
pulmonary fibrosis
Can not out air Can not in air

4. Symptoms can include coughing, wheezing, shortness of
breath and chest tightness. These symptoms can be mild
or severe and can come and go over time.
Although asthma can be a serious condition, it can be
managed with the right treatment.
Asthma affected an estimated 262 million people in 2019
(1) and caused 455 000 deaths.
Bronchial asthma is a chronic respiratory disease characterized by inflammation and
narrowing of airways in the lungs, which cause difficulty in breathing.
INTRODUCTION
4

5. CLINICAL FEATURES
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Recurrent episodes characterized by :-
 Breathlessness
 Wheezing
 Coughing – especially at night or early morning
 Tightness chest
 Hyperinflation
 Increased mucus production
TRIGGERS
 Allergens
 Respiratory tract infection
 Exercise
 Cold air
 Stress
 Drug aspirin

6. Endogenous
• Atopy
• Genetic predisposition
• Obesity
• Early infection
Environmental
• Indoor allergens
• Outdoor allergens
• Occupation sensitizers
• Passive smoking
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RISK FACTORS

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Atopic
(extrinsic)
• Predisposition towards
hyper reaction to normal
allergen
• Atopic are those patients
who have familiar
inherited disposition
towards reacting to
normal allergen
• External allergen may be
dust, cat, dog, etc
Non atopic
(intrinsic)
• Not allergic
• Aspirin
• Exercise
• Stress
• Cold
• Occupational toxin
inhalation eg- toluene
Types of asthma according to causes
clinical classification of asthma
Intermittent Chronic
 Twice a week
 Go away within few
minute
 More then twice a
week
 Duration more then
a day
More then twice a
week
 Duration more then
a day

8. 8
Allergens
Sensitizers
Viruses
Air pollution
Airway
inflammation
INFLAMATION AND ASTHMA SYMPTOMS
Symptoms
 Cough
 wheezing
 Chest tightness
 Dyspnea
Airway
hyperresponsiveness
Effects
Bronchospasm
Plasma exudation
Mucus secretion
Structural change
Triggers
 Allergens
 Exercise
 Cold air
 So2
 particulates
Sensory nerve
activation

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PATHOPHYSIOLOGY
 Fig- A & B, Comparison of a normal bronchus
with that in a person with asthma.
 Note the accumulation of mucus in the
bronchial lumen resulting from an increase in
the number of mucus secreting goblet cells in
the mucosa and hypertrophy of submucosal
gland.
 In addition, there is intense chronic
inflammation due to recruitment of eosinophils,
macrophages and other inflammatory cells.

10. 10
PATHOPHYSIOLOGY
Inhaled allergen binds with dendritic cell and stimulate TH2 cells.
TH2 cell secrete cytokines that promote allergic inflammation and stimulate B cells to produce
IgE and other antibodies.
TH2
cells
IL-4 IL-5 IL-13
Stimulate the
production of IgE
by B cell
Stimulate mucus
secretion and
promotes IgE
production by B
cell
Activate required
eosinophil
cytokines

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12. 12
Diagnosis
Clinical and occupational history
Diagnostic test
Non- specific Specific
1.Lung function assessment
• Monitoring peak expiratory flow
• Serial spirometry's with reversibility
test if air flow obstruction
• Methacholine/histamine challenge test
if normal lung function
2. FeNO measurement
3.Sputum eosinophil count
1. Skin prick tests
2. Serum-specific IgE
3. Specific inhalation
challenge
4. Basophil activation test
DIAGNOSIS OF ASTHMA

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14. 14

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BRONCHODILATORS
 Bronchodilator are drug that relax constricted airway smooth muscle and cause
immediate reversal of airway obstruction in asthma.
 There are mainly three classes of bronchodilators are in current clinical use:
• β2 Adrenergic agonists (sympathomimetics)
• Theophylline (a methylxanthine)
• Anticholinergic agents (muscarinic receptor antagonist)
β2 Adrenergic agonists (sympathomimetics) :- Inhaled β2 agonists are the
bronchodilator treatment of choice in asthma because they are most effective
bronchodilator and have minimal side effect.

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CLASSIFICATION OF β2 AGONISTS
β2 Agonist
SABA(short acting) LABA(Long acting) Ultra LABA
• Salbutamol
• Terbutaline
• Levalbuterol
• Fenoterol
• metaproterenol
• Indacaterol (as
not approved
for asthma)
• Salmeterol
• Formoterol

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 Activation of β2 receptors (β2AR) results in
activation of AC via Gs' leading to an
increase in intracellular cAMP and activation
of PKA.
 PKA phosphorylates a variety of target
substrates, resulting in opening of Ca2+-
activated K+ channels (KCa), thereby
facilitating hyperpolarization, decreased PI
hydrolysis, increased Na+/Ca2+ exchange,
increased Na+, Ca2+-ATPase activity, and
decreased myosin light chain kinase (MLCK)
activity and increased myosin light chain
(MLC) phosphatase.
 β2 Receptors may also couple to KCa via Gs.
 PDE, cyclic nucleotide phosphodiesterase.
MECHANISM OFACTION OF β2 AGONISTS

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Therapeutic uses:
Side effects:
•Dilation of airway in asthma, chronic bronchitis, & emphysema
•Mild to moderate cases of asthma
•Adjunct therapy for the relief of pulmonary edema.
•Nausea, vomiting, anorexia
•Gastroesophageal reflux during sleep
•Sinus tachycardia, extra systolic palpitations, ventricular dysrhythmias
•Transient increased urination.

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LEUKOTRIENE ANTAGONISTS
An Leukotriene antagonists is a drug which functions as a leukotriene- related enzyme inhibitor
(arachidonate 5-lipoxygenase) or leukotriene receptor antagonist and consequently opposes the function of
these inflammatory mediators; leukotrienes are produced by the immune system. Leukotriene receptor
antagonists, such as montelukast, zafirlukast can be used to treat these diseases. They are less effective than
corticosteroids for treating asthma, but more effective for treating certain mast cell disorders.
Μ.Ο.Α:
Montelukast ,zafirlukast are competitively prevent the bronchoconstrictor effects of leukotrienes
By blocking their receptor
Prevent leukotrienes from attaching to receptor on cells in the lungs and in circulation
Blocking the inflammation in the lungs.

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Side effects:
• Headache
•Stomach pain, heartburn, upset stomach, nausea, diarrhea, Tooth pain
•Tired feeling
• Fever, stuffy nose, sore throat, cough, hoarseness
•Mild rash.
Uses:
Prophylaxis and chronic treatment of asthma.

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CORTICOSTEROIDS
•Are not bronchodilators
•Given as prophylactic medications, used alone or combined with beta-agonists
Mechanism of action
Inhibition of phospholipase A2 ↓prostaglandin and leukotrienes-
Mast cell stabilization →↓ histamine release-
Upregulation of ẞ2 receptors

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23. Route of administration.
• Inhalation
Budesonide, Fluticasone, Beclomethasone
Less side effects
• Oral
Prednisolone
• Parenteral
Hydrocortisone, Methylprednisolone
Status asthmaticus (IV infusion)
Side effects of systemic corticosteroids
Adrenal suppression
 Growth retardation in children
 Osteoporosis
Fluid retention, weight gain, hypertension
Hyperglycemia
Susceptibility to infections
Glaucoma
 Cataract
Fat distribution, wasting of the muscles
Psychosis
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24. 1. Goodman and Gilman’s ,The Pharmacological Basis of Therapeutics (12th edition)
2. Rang and Dale’s Pharmacology,6thedition published in 2012.
3.A complete Textbook of Medical Pharmacology by S.K Srivastava.
4. https://youtu.be/oNnuGtxZzgc?si=DKVkm_gCBEl77pnO.
5. https://image.slidesharecdn.com/bronchialasthma-drugsandstatusasthmaticus
REFERENCE
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