DRUGS USED IN ASTHMA

DR.FOUZIA
ASTHMA
Asthma is a chronic disorder
of airways characterized by
airway obstruction
hyper responsiveness
inflammation.
Symptoms
Shortness of breath
chest tightness
associated with coughing
and excess sputum production.
CLASSIFICATION OF DRUGS FOR ASTHMA
Bronchodilators (Relievers)
1-β-Agonists (β2-selective)
Short-acting
Albuterol, Terbutaline
Phosphodiestrase (PDE) inhibitors
Aminophylline
Antimuscarinic agents
Ipratropium bromide, Tiotropium
CLASSIFICATION OF DRUGS FOR ASTHMA
Anti-inflammatory (Controllers)
1-Corticosteroids
Inhalational
Beclomethasone, Budesonide, Fluticasone,
Systemic
Hydrocortisone, Prednisolone, Prednisone
2-Long-acting bronchodilators
Salmeterol
Formeterol
CLASSIFICATION OF DRUGS FOR ASTHMA
Prophylactic drugs:
1-Mast cell stabilizers
Cromolyn, Nedocromil
2-Leukotriene pathway inhibitors
1-5-Lipoxygenase inhibitor
Zileuton
2-LTD4-receptor antagonists
Zafirlukast
Montelukast
ROUTES OF ADMINISTRATION IN ASTHMA
1-Inhalational
Delivery devices
Metered- dose inhalers
Space chambers
Dry powder inhalers
Nebulizers
2-Oral route
3-Parenteral route
β2-AGONISTS
Produce bronchodilation
Mechanism of action:
Binding β2  ↑ cAMP  Bronchodilation
Inhibit release of mediators from mast cells
Route:
Inhalation, Oral (Albuterol,Terbutaline), S/C (Terbutaline)
Use in asthma
1-Occasional symptoms as needed
2-Nocturnal symptoms more than twice a week
3-Acute severe asthma combine with ICS
METHYLXANTHINE (PDEI)
Caffeine (Coffee)
Theophylline (tea)
Theobromine (Cocoa)
Mechanism of action
of Theophylline
1-Inhibition of PDE
Relaxation of smooth
muscles of bronchi
METHYLXANTHINE (PDEI)
Pharmacological effects:
1-Respiration
Bronchodilation
2-CNS
↑ alertness , ↓ fatigue, nervousness, insomnia
3-CVS
↑ heart rate and force of contraction
4-Skeletal Muscle
Improve contractility of skeletal muscle, reverse fatigue of diaphragm
in patients with COPD
METHYLXANTHINE (PDEI)
A/R
Headache
Nausea
Vomiting
Abdominal discomfort
Restlessness
Behavioral disturbances, difficulty in learning(school children)
Cardiac arrthymias
Seizures
ANTIMUSCARINIC
Bronchodilation
Mechanism of action
Block M3 receptors
A/R
Rebound ↑ airway resistance
Bitter taste of ipratropium
Precipitation of glaucoma
CORTICOSTEROIDS
Anti-inflammatory effect
↓Bronchial hyper reactivity, & frequency of asthma exacerbations
Anti-inflammatory Effects in Asthma
1-Inhibit infiltration by lymphocytes, eosinophils, mast cells.
3-Inhibit inflammatory cytokines from TH2 cells
4-↓ Airway edema
5-Potentiate effects of β agonists on bronchial smooth muscles
MAST CELL STABILIZERS
Mechanism of action
Inhibit histamine
release from mast cells
and eosinophilic recruitment
Advantages
1-Prophylactic use
2-↓ need for ICS
3- Excellent safety profiles
LEUKOTRIENE PATHWAY INHIBITORS
LTC4 and LTD4
Bronchoconstriction
Mucosal edema
Zileuton:
Inhibition of 5-lipoxygenase
Monteleukast:
Antagonist of LTD4-R
USES
1-Prophylaxis of asthma
↓frequency of asthma exacerbations
MANAGEMENT OF ASTHMA
1-Educate patient to avoid allergens
2-Prophylaxis of asthma
Mast cell stabilizers
Cromolyn Nedocromil
3-Acute asthma:
1-High flow O2 to maintain O2 saturation above 90%
2-High dose of Short acting beta blockers (SABA) by nebulizer
3- Salbutamol +Ipratropium bromide by O2 driven nebulizer
4-Aminophyllin infusion
5-Intubate the patient for assisted ventilation