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DEPARTMENT OF PHARMACOLOGY
ADVANCED PHARMACOLOGY - II
PRESENTATION ON: PHARMACOTHERAPY OF
ASTHMA
By: Kashikant Yadav
M Pharm(Pharmacology)
KARNATAKA COLLEGE OF PHARMACY
ASTHMA DEFINITION
Asthma is defined as a chronic inflammation disease of
airway that is characterised by increase responsiveness of
tracheobronchial tree to a multiplicity of stimuli.
Extrinsic: episodic , atopy
Intrinsic: perennial , status asthmaticus.
CAUSES
Asthma may be triggered because of :
1)Environmental Factors:
Air pollutants
Smoking
Dust
Pets
Chemicals
2)Genetic Factors:
Family history
Certain genes
SYMPTOMS
 Asthma ppt
TYPES
 Extrinsic Asthma ( Allergic )
 Intrinsic Asthma ( Non- Allergic)
 Mixed Asthma ( Extrinsic and Intrinsic)
 Occupational Asthma
 Drug Induced Asthma
- Aspirin Induced Asthma
- NSAID Induced Asthma
 Exercise Induced Asthma
 Cough Variant Asthma
- Very Common ( Especially in children )
 Asthma ppt
 Asthma ppt
BRONCHODIALATORS
A bronchodilator is a substance that dilates the bronchi and bronchioles,
decreasing resistance in the respiratory airway and increasing airflow to the lungs.
Bronchodilators may be endogenous (originating naturally within the body),
Bronchodilators are either short-acting or long-acting.
e.g : Salbutamol, Theophylline, Ipratropium bromide.
M.O.A :
 Increase levels of energy- producing cAMP.
 This is done competitively inhibiting phosphodiesterase ( PDE), the enzyme
that breaks down cAMP.
 Result: decreased cAMP levels, smooth muscle relaxation bronchodialation,
and increased airflow.
Contd…..
Therapeutic uses:
 Dilation of airway in asthma, chronic bronchitis, & emphysema
 Mild to moderate cases of asthma
 Adjunct therapy for the relief of pulmonary edema.
Side effects:
 Nausea , vomiting , anorexia
 Gastroesophagal reflux during sleep
 Sinus tachycardia , extrasystolic , palpitations , ventricular dysrhythmias
 Transient increased urination.
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.
M.O.A:
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.
Contd…..
Kinetics:
The half life of Leukotriene antagonists is less than 5 minutes.
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.
Mast cell stabilizers
Cromolyn - Nedocromil
 Act by stabilization of mast cell
membrane
 Have poor oral absorption
 Given by inhalation
 Not bronchodilators
 Not effective in acute attack of
asthma
 Prophylactic anti-inflammatory
drugs
 Children respond better than
adults
Uses
 Prophylactic therapy in asthma especially in children
 Allergic rhinitis
 Conjunctivitis
Side effects
 Bitter taste
 minor upper respiratory tract irritation (burning sensation)
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 β2 receptors
 Asthma ppt
Routes 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
Inhalation therapy has less side effects
 Oropharyngeal candidiasis (thrush)
 Dysphonia (voice hoarseness)
Withdrawal
Abrupt stop of corticosteroids should be avoide
and dose should be tapered (adrenal insufficiency
syndrome)
Anti-IgE antibody
Omalizumab
 A monoclonal antibody directed against human IgE
 It binds to the IgE on sensitized mast cells and prevents activation
by asthma triggers and subsequent release of inflammatory mediators
 Expensive-not first line therapy
 Asthma ppt
Differentiating Asthma From COPD
Asthma
 Reversible
 No parenchymal destruction
 Eosinophils , T- cells
 Responds well to steroids
COPD
 Irreversible
 Tissue destruction
 Primarily neutrophils
 Less responsive to steroids
 Smoking
Recent Advances in the Treatment of Asthma
 Novel class of bronchodilators
 Immunomodulatory therapies
 Newer anti- inflammatory therapies
 Mediator antagonists
 Miscellaneous approaches
 Cytokine modifiers
 Chemokine Receptor antagonist.
 Asthma ppt

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Asthma ppt

  • 1. DEPARTMENT OF PHARMACOLOGY ADVANCED PHARMACOLOGY - II PRESENTATION ON: PHARMACOTHERAPY OF ASTHMA By: Kashikant Yadav M Pharm(Pharmacology) KARNATAKA COLLEGE OF PHARMACY
  • 2. ASTHMA DEFINITION Asthma is defined as a chronic inflammation disease of airway that is characterised by increase responsiveness of tracheobronchial tree to a multiplicity of stimuli. Extrinsic: episodic , atopy Intrinsic: perennial , status asthmaticus.
  • 3. CAUSES Asthma may be triggered because of : 1)Environmental Factors: Air pollutants Smoking Dust Pets Chemicals 2)Genetic Factors: Family history Certain genes
  • 6. TYPES  Extrinsic Asthma ( Allergic )  Intrinsic Asthma ( Non- Allergic)  Mixed Asthma ( Extrinsic and Intrinsic)  Occupational Asthma  Drug Induced Asthma - Aspirin Induced Asthma - NSAID Induced Asthma  Exercise Induced Asthma  Cough Variant Asthma - Very Common ( Especially in children )
  • 9. BRONCHODIALATORS A bronchodilator is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs. Bronchodilators may be endogenous (originating naturally within the body), Bronchodilators are either short-acting or long-acting. e.g : Salbutamol, Theophylline, Ipratropium bromide. M.O.A :  Increase levels of energy- producing cAMP.  This is done competitively inhibiting phosphodiesterase ( PDE), the enzyme that breaks down cAMP.  Result: decreased cAMP levels, smooth muscle relaxation bronchodialation, and increased airflow.
  • 10. Contd….. Therapeutic uses:  Dilation of airway in asthma, chronic bronchitis, & emphysema  Mild to moderate cases of asthma  Adjunct therapy for the relief of pulmonary edema. Side effects:  Nausea , vomiting , anorexia  Gastroesophagal reflux during sleep  Sinus tachycardia , extrasystolic , palpitations , ventricular dysrhythmias  Transient increased urination.
  • 11. 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. M.O.A: 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.
  • 12. Contd….. Kinetics: The half life of Leukotriene antagonists is less than 5 minutes. 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.
  • 13. Mast cell stabilizers Cromolyn - Nedocromil  Act by stabilization of mast cell membrane  Have poor oral absorption  Given by inhalation  Not bronchodilators  Not effective in acute attack of asthma  Prophylactic anti-inflammatory drugs  Children respond better than adults
  • 14. Uses  Prophylactic therapy in asthma especially in children  Allergic rhinitis  Conjunctivitis Side effects  Bitter taste  minor upper respiratory tract irritation (burning sensation)
  • 15. 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 β2 receptors
  • 17. Routes of administration  Inhalation  Budesonide, Fluticasone, Beclomethasone  Less side effects  Oral  Prednisolone  Parenteral  Hydrocortisone, Methylprednisolone  Status asthmaticus (IV infusion)
  • 18. 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
  • 19. Inhalation therapy has less side effects  Oropharyngeal candidiasis (thrush)  Dysphonia (voice hoarseness) Withdrawal Abrupt stop of corticosteroids should be avoide and dose should be tapered (adrenal insufficiency syndrome)
  • 20. Anti-IgE antibody Omalizumab  A monoclonal antibody directed against human IgE  It binds to the IgE on sensitized mast cells and prevents activation by asthma triggers and subsequent release of inflammatory mediators  Expensive-not first line therapy
  • 22. Differentiating Asthma From COPD Asthma  Reversible  No parenchymal destruction  Eosinophils , T- cells  Responds well to steroids COPD  Irreversible  Tissue destruction  Primarily neutrophils  Less responsive to steroids  Smoking
  • 23. Recent Advances in the Treatment of Asthma  Novel class of bronchodilators  Immunomodulatory therapies  Newer anti- inflammatory therapies  Mediator antagonists  Miscellaneous approaches  Cytokine modifiers  Chemokine Receptor antagonist.