Drug Asthma

Drugs Used in Asthma
Bronchial asthma
Pathogenesis of asthma Pharmacology of agents used in the treatment of asthma
Sympathomimetic agents Methylxanthine drugs Antimuscarinic agents Corticosteroids Cromolyn & Nedocromil Leukotriene pathway inhibitors Other drugs in the treatment of asthma
Bronchial asthma
Clinical hallmarks of asthma

Recurrent, episodic bouts of
Coughing Shortness of breath Chest tightness Wheezing
Triggers of asthma
On exposure to
Allergens Certain pollutants
On exercise After a viral upper respiratory infection
Pathologic features of asthma

Contraction of airway smooth muscle Mucosal thickening from edema and cellular infiltration Inspissation in the airway lumen of abnormally thick, viscid plugs of mucus
The two phases of asthma
FEV1; forced expiratory volume in 1 second
Immunopathogenesis of asthma
Bronchial asthma
Bronchial asthma
Asthma therapies - 1
Contraction of airway smooth muscle Bronchodilators
Beta-adrenoceptor stimulants Methylxanthine drug Antimuscarinic agents
Short-term relievers
Bronchodilation is promoted by cAMP
Asthma therapies - 2
Mucosal thickening from edema and cellular infiltration Inspissation in the airway lumen of abnormally thick, viscid plugs of mucus Anti-inflammatory agent
Corticosteroid Cromolyn or nedocromil Leukotriene antagonist
Long-term controllers
Bronchial asthma
Bronchial asthma
Sympathomimetic agents
Sympathomimetic agents
F2 selective agents Relax airway smooth muscle Inhibit release of some bronchoconstricting substances from mast cells Toxic effects
mediated mainly by F1 receptors Tachycardia Skeletal muscle tremor
Sympathomimetic agents; Kinetics

measured by forced expiratory flow rate short acting;
albuterol, terbutaline half-life; 2-3 hours half2-
long acting agonists;

salmeterol, formoterol up to 12 hours
Bronchial asthma
Bronchial asthma
Methylxanthine drugs
Source tea (theophylline), coffee (caffeine), cocoa (theobromine)
CNS
Smooth m. Mainly used
Pharmacodynamics of methylxanthines
CNS effects; nervousness, insomnia, convulsion, death Cardiovascular effects; positive chronotropic and inotropic effects on the heart Effects on the GI tract; stimulate secretion of both gastric acid and digestive enzymes Effects on kidney; weak diuretics Effects on smooth muscle; bronchodilation Effects on skeletal muscle; improve contractility
Methylxanthine drugs; clinical uses

Narrow therapeutic window; 5-20 mg/L 5 Should only be used where methods to measure theophylline blood levels are available
Metabolized by liver
Decreased clearance in liver disease
Smoking induces hepatic enzymes

Increased clearance in cigarette smoking
Children clear theophylline faster than adults
Bronchial asthma
Bronchial asthma
Antimuscarinic agents
Antimuscarinic agents
Atropine
Effective bronchodilator too many side effects; not used today in treatment of asthma poorly absorbed does not readily cross blood-brain barrier bloodless systemic adverse effects Also effective in patients with chronic obstructive pulmonary disease (COPD)
Ipratropium bromide

Response of patient with COPD to ipratropium or metaproterenol
Response of patient with asthma to ipratropium or salbutamol
Bronchial asthma
Bronchial asthma
Corticosteroids
Inhaled corticosteroids:
lipid-soluble lipid beclomethasone, budesonide, flunisolide, beclomethasone, budesonide, flunisolide, fluticasone, fluticasone, triamcinolone
Oral corticosteroids for severe asthma:

prednisone, prednisolone
Corticosteroids; Mechanism of action

Anti-inflammatory AntiInhibition of the lymphocytic, eosinophilic airway mucosal inflammation of asthmatic airways Inhibition of production of inflammatory cytokines Potentiation of the effects of Freceptor agonists
Corticosteroids; Side effects

Systemic effects
Adrenal suppression, osteoporosis, cataracts with oral corticosteroids therapy Gradual tapering is needed
Oropharyngeal candidiasis, candidiasis, hoarseness

with inhaled topical corticosteroids
Bronchial asthma
Bronchial asthma
Cromolyn & Nedocromil
Cromolyn & Nedocromil; Mechanism of action

Inhibit cellular activation
Alteration in the function of delayed chloride channels in the cell membrane On mast cells; inhibition of the early response to antigen challenge On eosinophils; inhibition of the inflammatory response to inhalation of allergens On airway nerves; Inhibition of cough
Cromolyn & Nedocromil; Clinical uses

Prophylactic uses in acute asthma
Before exercise Before unavoidable exposure to an allergen
Reduce symptomatic severity and the need for bronchodilator medications in perennial asthma Reduce symptoms of allergic rhinoconjunctivitis Poorly absorbed
rare adverse effects
Bronchial asthma
Bronchial asthma
Leukotriene pathway inhibitors

Block the synthesis of leukotriene
5-lipoxygenase inhibitor Zileuton
Inhibit the action of leukotriene D4 (LTD4)

Inhibition of the binding of LTD4 to its receptor on target tissue Zafirlukast and montelukast
Bronchial asthma
Bronchial asthma
Other drugs in the treatment of asthma

Anti-IgE monoclonal antibodies Calcium channel blockers Nitric oxide donors
. (xanthine) . . . .
Mast cell mediator release
Newly generated lipid mast cell mediators

Drug Asthma

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Drug Asthma

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Drugs Used in Asthma

Clinical hallmarks of asthma

On exercise After a viral upper respiratory infection

Pathologic features of asthma

The two phases of asthma

FEV1; forced expiratory volume in 1 second

Bronchodilation is promoted by cAMP

Bronchodilation is promoted by cAMP

Sympathomimetic agents; Kinetics

long acting agonists;

Smooth m. Mainly used

Bronchodilation is promoted by cAMP

Methylxanthine drugs; clinical uses

Smoking induces hepatic enzymes

Children clear theophylline faster than adults

Bronchodilation is promoted by cAMP

Response of patient with COPD to ipratropium or metaproterenol

Response of patient with asthma to ipratropium or salbutamol

Oral corticosteroids for severe asthma:

Corticosteroids; Mechanism of action

Corticosteroids; Side effects

Oropharyngeal candidiasis, candidiasis, hoarseness

Cromolyn & Nedocromil

Cromolyn & Nedocromil; Mechanism of action

Cromolyn & Nedocromil; Clinical uses

Leukotriene pathway inhibitors

Inhibit the action of leukotriene D4 (LTD4)

Other drugs in the treatment of asthma

Mast cell mediator release

Newly generated lipid mast cell mediators

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