Hakeem khan presented on asthma. Key points include:
1. Asthma is a chronic inflammatory disorder of the airways characterized by wheezing, coughing, and shortness of breath.
2. It is caused by factors like allergies, environment, emotions, and drugs.
3. Clinical features include coughing, wheezing, tightness in the chest, and labored breathing.
4. Treatment involves short-acting bronchodilators for relief of symptoms and long-acting controllers like inhaled corticosteroids to reduce inflammation.
1. Hakeem khan
Presented by,
Department of pharmacology
Luqman college of pharmacy
Gulbarga
2. ASTHMA
The asthma is derived from the Greek word meaning" difficulty in breathing”.
Asthma is physiologically characterized by increased responsiveness of trachea
and bronchi to various stimuli and by widespread narrowing of the airways.
Chronic inflammatory disorder of the airway.
Usually reversible, but not yet curable.
Contraction of bronchial smooth muscles.
Edema of mucosa.
4. CLINICAL FEATURES OF BRONCHIAL
ASTHMA
1. Coughing
2. Wheezing & dyspnoea.
3. Tightness in pain
4. Labored expiration .
5. Tachypnoea & tachycardia.
6. signs of infection.
7. Expiration time greater then inspiration time.
5. ASTHMA FACTS
About 17 million or 4 % Americans have asthma.
Rate of asthma increased 75% between 1980 and 2008.
Most common chronic childhood disease, affecting about 5
million children.
14 people die each day from asthma.
Nearly 2 million emergency room visits each year.
Male: Female ratio is 2:1.
10. Major Cells Implicated in
Inflammatory Response
Mast cells
Lymphocytes
Eosinophils
Neutrophils
11. General Goals of Asthma Therapy
Prevent chronic symptoms and asthma
exacerbations during the day and night
Maintain normal activity levels
Have normal or near-normal lung function
Have no or minimal side effects while receiving
optimal medications
12. General Pharmacologic Approach to
the Treatment of Asthma
1. “Relievers”
I. Short-acting bronchodilators
A. β 2-adrenergic agents
B. Anti-cholinergic (Parasympatholytic) agents
2. “Controllers”
1. Corticosteroids
2. Long-Acting bronchodilators
I. β 2-adrenergic agents
II. Methylxanthines
3. Mast cell stabilizers.
4. Leukotriene inhibitors
5. Anti-IgE monoclonal antibodies
15. Beta-2 Adrenergic Agonists – Short
acting agents
Mode of administration:
Inhaled/ Parenteral
Modes of action:
Here it leads to increase c AMP Formation in
bronchial muscle cell leading to relaxation &decrease
mediator release.
Relax airway smooth muscle
Decrease vascular permeability
May modulate mediator release from mast cells
and basophiles.
16. Role in therapy:
Medication of choice for treatment of acute exacerbations of
asthma and useful in the pretreatment of exercise-induced
bronchospasm (EIB)
Used to control episodic bronchoconstriction
Increased used – or even daily use of these agents is
a warning of deterioration of asthma and indicates
the need to intensify regular anti-inflammatory
therapy.
Dose:2-4 mg oral,0.25-0.5 i.m/s.c.
17. Side Effects Seen with Beta Agonist
Tremor
Palpitations and tachycardia
Headache
Insomnia
Nervousness
Dizziness
Nausea
19. Anticholinergic (Parasympatholytic)
Bronchodilators
Role in therapy:
Additive effect when nebulized together with a
rapid-acting beta-2 agonist for exacerbations of
asthma
Ipratropium can be used an alternative,who
experience adverse effects such as tachycardia,
arrhythmias, and tremors from beta-2 agonists.
Side effects:
Dryness of the mouth and bitter taste.
20. Dose: 40-80 ug. as in aerosol form by inhalation
SPASMOLYSIN 0.32 MG TAB.
Ipratopiam bromide: onset & (late peak 60-90 min).
Duration of action 4-6 hr.
Marketed preparations: 20 ug /puff metered dose
inhaler. 2 puff 3-4 times daily.
IPRANASE 0.084 % nasal spray 1-2 sprays in each
nostrils 2-3 times daily.
23. Inhaled Glucocorticoids
Mechanisms of action:
They inhibit the formation and release of cytokines and
chemical mediators & reduces bronchial hyper reactivity.
Inhibition of the release of prostaglandins and
leukotrienes thus preventing the smooth muscle
contraction and mucous secretions also suppresses
inflammatory responses due to AG:AB reaction.
Role in therapy:
Most effective anti-inflammatory medication for the
treatment of asthma.
26. Systemic Glucocorticoids
Mode of administration:
Oral
Parenteral
Mechanisms of action:
They inhibit the formation and release of cytokines
and chemical mediators & reduces bronchial hyper
reactivity.
Inhibition of the release of prostaglandins and
leukotrienes thus preventing the smooth muscle
contraction and mucous secretions also suppresses
inflammatory responses due to AG:AB reaction.
Role in therapy:
Long-term oral Glucocorticoids therapy may be
required to control severe persistent asthma.
E.g. Hydrocortisone and methylprednisolone.
28. Adrenergic Bronchodilators – Long-
Acting Agents
Modes of administration:
Inhaled
Oral
Mechanisms of action:
Here it leads to increase c AMP Formation in
bronchial muscle cell leading to relaxation &decrease
mediator release.
Effects persists for at least 12 hours
29. Adrenergic Bronchodilators – Long-
Acting Agents
Role in therapy:
Long-acting inhaled beta-2 agonists should be
considered when standard introductory doses of
inhaled Glucocorticoids fail to achieve control of
asthma .
Because long-term treatment with these agents does not
appear to influence the persistent inflammatory changes
in asthma, this therapy should be combined with inhaled
Glucocorticoids
Fluticosone propionate – salmeterol and bedesonide-
formoterol inhalers (Advair®)
30. Adrenergic Bronchodilators – Long-
Acting Agents
Its action starts within 5 min & lasts for 2-3
hours.
systemic adverse effect :
For e.g., cardiovascular stimulation, skeletal
muscle tremors, and hypokalemia, palpitation.
Dose: 5 mg oral,0.25 mg sc,250 ug by inhalation.
BRICAREX 2.5 mg tab,3 mg/5 ml syrup.
31. Methylxanthines
Mode of administration
Oral or Parenteral
Mechanisms of action
Inhibition of phosphodiasterase III and IV. These are
responsible of metabolism of cAMP.(Bronchodilation,cardiac
stimulation & vasodilation occur.)
Blocking of adenosine receptor on airway muscles (A1) and
those present on mast cells (A3).it contract bronchial
muscles,depresses cardiac pace maker& inhibit gastric
secretion .
Role in therapy
Sustained release theophylline is effective in controlling
asthma symptoms and improving lung function.
32. Methylxanthines
Pharmacokinetic: Theophyllene-half life 7-12 hrs.
Preparations & doses: 100-300 mgTDS.oral
THELONG 100,200 Mg SR tab.
AMINOPHYLLINE 250-500 Mg
Side effects :
Gastrointestinal symptoms – nausea, vomiting
CNS – Seizures
Cardiovascular – tachycardia, arrhythmias
Pulmonary – stimulation of the respiratory
center
33. Leukotriene modifiers
A relatively new class of anti-asthma drugs that
include cysteinyl leukotriene 1 (CysL T1)
receptor antagonists.
e.g. montelukast, zafirlukast
5-lipoxeygenase inhibitor :
e.g. zileuton
34. Leukotriene modifiers
Mode of administration
Oral
Mechanism of action
Receptor antagonists block the CysLT1 receptors
on airway smooth muscle and thus inhibit the
effects of cysteinyl leukotrienes that are release
from mast cells and eosinophils
35. Leukotriene modifiers
Role in therapy
These agents have a small and variable
bronchodilator effect, reduce symptoms, improve
lung function, and reduce asthma exacerbations.
Leukotriene modifiers are less effective than
long-acting inhaled beta-2 agonists therapy.
36. Leukotriene modifiers
Side effects
These drugs are usually well tolerated, and few if
any effects have been recognized.
○ Zileuton has been associated with liver toxicity.
○ GIT Disturbances.
Half life- montelukast-3-6hr 10 mg OD & zafirlukast
- 8-12 hr 20 mg BD.
EMLUCAST 4 mg tab.
38. Anti-IgE Antibodies
Agents directed at diminishing the production of IgE
through effects on interleukin 4 or on IgE itself have
been evaluated
Recombinant human monoclonal antibody that
forms complexes with free IgE blocks the
interaction of IgE with mast cells and basophiles.
E.g. Omalizumab.
39. TREATMENT:
STEP UP APPROACH:-
STEP – I:Short acting β-agonist are given.
STEP –II: Short acting β-agonist +Beclomethasone BID or
fluticasone .
Dose:50-200 ug/BID.
STEP –III: Short acting β-agonist +Beclomethasone BID
or fluticasone.
Here salmiterol may be added. 50ug BID.
40. STEP –IV: High dose inhaled steroids
added+Ipratropium.
STEP –V: Regular steroids+Beclomethasone (dose :
800-2000ug).
Prednisolone may be given.
41.
42. What is COPD??
A set of lung diseases that limit air flow and is
not fully reversible.
COPD patients report they are “hungry” for air.
Usually progressive and is associated with
inflammation of the lungs as they respond to
noxious particles or gases.
Potentially preventable with proper precautions
and avoidance of precipitating factors.
Symptomatic treatment is available.
44. Major Clinical features of COPD
1. Chronic Bronchitis is characterized by
Chronic inflammation and excess mucus
production.
Presence of chronic productive cough.
2. Emphysema is characterized by
Damage to the small, sac-like units of the lung
that deliver oxygen into the lung and remove the
carbon dioxide.
Chronic cough.
45. Primary Symptoms
Chronic Bronchitis
Chronic cough
Shortness of breath
Increased mucus
Frequent clearing of throat
Emphysema
Chronic cough
Shortness of breath
Limited activity level
48. What can cause COPD?
Smoking is the primary risk factor
Long-term smoking is responsible for 80-90 %
of cases
○ Smoker, compared to non-smoker, is 10 times
more likely to die of COPD.
Prolonged exposures to harmful particles and
gases from:
Second-hand smoke,
Industrial smoke,
Chemical gases, vapors & fumes.
Dusts from grains, minerals & other materials.
49. 1. Stop smoking, if you smoke, to prevent further damage to
your body Smoking cessation is critical for all severities of
COPD
2. Avoid or protect yourself from exposures to Second-hand
smoke and Other substances such as chemical vapors, fumes,
mists, dusts, and diesel exhaust fumes that irritate your lungs.
50. How is COPD Treated?
COPD can be managed, but not cured.
Treatment is different for each individual and is based
on severity of the symptoms
Early diagnosis and treatment can
Slow progress of the disease
Relieve symptoms
Improve an individual’s ability to stay active
Prevent and treat complications
Improve quality of life
51. What medications are used to
treat symptoms?
Bronchodilators –
○ Relaxes muscles around airways.
Steroids
○ Reduces inflammation.
Oxygen therapy
○ Helps with shortness of breath.
52. REFERENCES
1. Sharma HL and Sharma KK “Principle of pharmacology” First
edition 2007, Page no.658-667.
2. RANG and DALE’S Pharmacology sixth edition 2007 page
no.356-366.
3. Tripathi KD “Essentials of medical pharmacology” sixth edition
2008, page no. 213-230.
4. F. S. K. “Essentials of pharmacotherapeutics” forth edition
2007, Page no.544-552.
5. www.google.com
6. TEXT BOOK OF PATHOLOGY ,Fifth Edn ,H.Mohan,page
no.485-494