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8/6/2019 Drug Asthma
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Drugs Used in AsthmaDrugs Used in Asthma
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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
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Clinical hallmarks of asthma Recurrent, episodic bouts of
Coughing
Shortness of breath
Chest tightness
Wheezing
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Triggers of asthma
On exposure to
Allergens
Certain pollutants
On exercise
After a viral upper respiratory infection
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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
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The two phases of asthma
FEV1; forced expiratory volume in 1 second
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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
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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
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Asthma therapies - 1 Contraction of airway smooth muscle
Bronchodilators
Beta-adrenoceptor stimulants
Methylxanthine drug
Antimuscarinic agents
Short-term relievers
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Bronchodilation is promoted by
cAMP
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Asthma therapies - 2 Mucosal thickening from edema and cellular
infiltration
Inspissation in the airway lumen ofabnormally thick, viscid plugs of mucus
Anti-inflammatory agent Corticosteroid
Cromolyn or nedocromil Leukotriene antagonist
Long-term controllers
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Immunopathogenesis of asthma
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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
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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
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Sympathomimetic agents
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Bronchodilation is promoted by
cAMP
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Sympathomimetic agents F2 selective agents
Relax airway smooth muscle
Inhibit release of some bronchoconstricting
substances from mast cells
Toxic effects
mediated mainly byF1 receptors Tachycardia
Skeletal muscle tremor
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Sympathomimetic agents;
Kinetics
measured by forced expiratory flow ratemeasured by forced expiratory flow rate
short acting;short acting;
albuterol, terbutalinealbuterol, terbutaline
halfhalf--life; 2life; 2--3 hours3 hours
long acting agonists;long acting agonists;
salmeterol, formoterolsalmeterol, formoterol
up to 12 hoursup to 12 hours
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Methylxanthine drugsSourceSource tea (theophylline), coffeetea (theophylline), coffee
(caffeine), cocoa (theobromine)(caffeine), cocoa (theobromine)
CNS Smooth m.
Mainly used
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Bronchodilation is promoted by
cAMP
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Pharmacodynamics of
methylxanthines CNS effects; nervousness, insomnia,CNS effects; nervousness, insomnia,
convulsion, deathconvulsion, death
Cardiovascular effects; positive chronotropicCardiovascular effects; positive chronotropicand inotropic effects on the heartand inotropic effects on the heart
Effects on the GI tract; stimulate secretion ofEffects on the GI tract; stimulate secretion ofboth gastric acid and digestive enzymesboth gastric acid and digestive enzymes
Effects on kidney; weak diureticsEffects on kidney; weak diuretics
Effects on smooth muscle; bronchodilationEffects on smooth muscle; bronchodilation Effects on skeletal muscle; improveEffects on skeletal muscle; improve
contractilitycontractility
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Methylxanthine drugs;
clinical uses Narrow therapeutic window; 5Narrow therapeutic window; 5--20 mg/L20 mg/L
Should only be used where methods to measureShould only be used where methods to measure
theophylline blood levels are availabletheophylline blood levels are available Metabolized by liverMetabolized by liver
Decreased clearance in liver diseaseDecreased clearance in liver disease
Smoking induces hepatic enzymesSmoking induces hepatic enzymes
Increased clearance in cigarette smokingIncreased clearance in cigarette smoking
Children clear theophylline faster than adultsChildren clear theophylline faster than adults
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Antimuscarinic agents
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Bronchodilation is promoted by
cAMP
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Antimuscarinic agents AtropineAtropine
Effective bronchodilatorEffective bronchodilator
too many side effects; not used today intoo many side effects; not used today intreatment of asthmatreatment of asthma
Ipratropium bromideIpratropium bromide poorly absorbedpoorly absorbed
does not readily cross blooddoes not readily cross blood--brain barrierbrain barrier
less systemic adverse effectsless systemic adverse effects
Also effective in patients with chronic obstructiveAlso effective in patients with chronic obstructivepulmonary disease (COPD)pulmonary disease (COPD)
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Response of patient with
COPD
to ipratropium or metaproterenol
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Response of patient
with asthma
to ipratropium or salbutamol
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Corticosteroids Inhaled corticosteroids:Inhaled corticosteroids:
lipidlipid--solublesoluble
beclomethasonebeclomethasone,, budesonidebudesonide,, flunisolideflunisolide,,
fluticasonefluticasone,, triamcinolonetriamcinolone
Oral corticosteroids for severe asthma:Oral corticosteroids for severe asthma:
prednisone,prednisone, prednisoloneprednisolone
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Corticosteroids;
Mechanism of actionMechanism of action AntiAnti--inflammatoryinflammatory
Inhibition of the lymphocytic,Inhibition of the lymphocytic,
eosinophiliceosinophilic airway mucosalairway mucosalinflammation of asthmatic airwaysinflammation of asthmatic airways
Inhibition of production of inflammatoryInhibition of production of inflammatorycytokinescytokines
PotentiationPotentiation of the effects ofof the effects ofFF--receptor agonistsreceptor agonists
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Immunopathogenesis of asthma
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Corticosteroids;
Side effectsSide effects Systemic effectsSystemic effects
Adrenal suppression, osteoporosis,Adrenal suppression, osteoporosis,
cataractscataracts with oral corticosteroids therapywith oral corticosteroids therapy
Gradual tapering is neededGradual tapering is needed
OropharyngealOropharyngeal candidiasiscandidiasis,,hoarsenesshoarseness
with inhaled topical corticosteroidswith inhaled topical corticosteroids
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Bronchial asthma Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Cromolyn & Nedocromil
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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 ofallergens
On airway nerves; Inhibition of cough
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Cromolyn & Nedocromil;
Clinical uses Prophylactic uses in acute asthma
Before exercise
Before unavoidable exposure to an allergen
Reduce symptomatic severity and the needfor bronchodilator medications in perennialasthma
Reduce symptoms of allergic
rhinoconjunctivitis Poorly absorbed
rare adverse effects
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Bronchial asthma
Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Bronchial asthma
Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Immunopathogenesis of asthma
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Bronchial asthma
Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Bronchial asthma
Pathogenesis of asthma
Pharmacology of agents used in thetreatment of asthma Sympathomimetic agents
Methylxanthine drugs
Antimuscarinic agents
Corticosteroids
Cromolyn & Nedocromil Leukotriene pathway inhibitors
Other drugs in the treatment of asthma
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Other drugs in the treatment of
asthma Anti-IgE monoclonal antibodies
Calcium channel blockers
Nitric oxide donors
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Mast cell mediator release
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Newly generated lipid mast cell mediators