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Sympathomimetic Agents
Along with corticosteroids, are the most widely
used drugs for asthma.
They relax smooth muscle and inhibit release of
bronchoconstricting substances from mast cells.
They also inhibit microvascular leakage, increase
ciliary activity and increase cAMP.
They cause tachycardia and tremor as side
effects.
Adrenoceptor agonists are best delivered by
inhalation for greatest effect and least systemic
toxicity.
Even in best conditions, 80-90% of the aerosol is
deposited in the mouth or pharynx.
Effectiveness can be increased by holding the
breath in inspiration.
Side effects include tremor and nervousness.
Short acting 2 selective drugs:
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Albuterol (salbutamol)
Terbutaline
Metaproterenol
Pirbuterol
Bronchodilation is maximal within 15-30 min. and
persists for 3-4 hr.
All can be diluted in saline for administration
from a nebulizer.
Long-acting 2 selective agonists:
Salmeterol
Formoterol
Their duration of action is 12 hr.
They are usually used with other drugs (eg:
inhaled corticosteroids)
Methylxanthines
Methylxanthines:
Theophylline (tea)
Theobromine (cocoa)
Caffeine (coffee)
Theophylline is most selective in its smooth
muscle effects.
Caffeine has the most marked CNS effects.
Theophylline is not an ideal drug, but has a low
cost.
Aminophylline is an injectable derivative of
theophylline.
They Inhibit phosphodiesterase (PDE) and
increase cAMP.
Adenosine causes airway contraction and
histamine release.
Theophylline derivatives also nay inhibit
adenosine receptors.
Theophylline also improves contractility and
reverses fatigue of the diaphragm in patients
with COPD.
So theophylline can diminish dyspnea even in
patients with irreversible airflow obstruction.
Rate of metabolism: Children > adults > neonates
and young infants
Cigarette smoking induces metabolizing enzymes.
Theophylline has a narrow therapeutic window.
Improvement in lung function is seen at 5-20
mg/L.
Vomiting, abdominal discomfort, headache, and
anxiety occur at 15 mg/L in some, and at >20
mg/L in all patients.
Higher levels (> 40 mg/L) causes seizures or
arrhythmias.
These may NOT be preceded by GI or neurologic
warning symptoms.
Methylxanthines stimulate secretion of both
gastric acid and digestive enzymes.
Caffeine (mg)
Coffee
Brewed, regular
Instant
Espresso
142227
142227
57
40180
30120
120
Tea
Brewed, leaf or bag
Instant
Iced
227
227
340
80
50
70
Soft Drinks
Pepsi, Diet Pepsi
340
38
9/24/2014
empperezmd2014
Antimuscarinic Agents
Involvement of parasympathetic system in
respiratory diseases varies among individuals.
Antimuscarinic agents are used:
Instead of inhaled -agonists in
asthmatics
In addition to inhaled -agonists in
asthmatics
In COPD patients
Ipratropium is a polar drug used for asthma.
Tiotropium is used for COPD.
Corticosteroids
Their most important action is inhibition of
airway mucosal inflammation.
Inhalational therapy minimizes their adverse
effects.
Inhalational drugs include:
Beclomethasone
Budesonide
Fluticasone
Triamcinolone
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Zafirlukast, montelukast
They are weaker than inhaled corticosteroids, but
reduce the frequency of exacerbations
One advantage is that they are taken orally;
children comply poorly with inhaled therapies.
Montelukast is approved for children as young as
6 years of age.
5-10% of asthmatics are exquisitely sensitive to
aspirin and other NSAIDs.
It is thought to result from inhibition of
cyclooxygenase.
LT antagonists are useful for preventing this
problem.
Anti-IgE Antibodies
Omalizumab inhibits the binding of IgE to mast
cells but does not activate IgE already bound.
It also inhibits IgE synthesis by B lymphocytes.
The murine antibody has been humanized and it
does not cause sensitization.
Omalizumab's effect is reduction of both the
severity of asthma and corticosteroid dosage.
Patients most likely to respond are those with the
greatest need:
Patients with a history of repeated
exacerbations
A high requirement for corticosteroid
treatment
Poor pulmonary function
Omalizumab treatment reduced exacerbations
requiring hospitalization by 88%.
These benefits justify the high cost of this
treatment in severe disease.
Treatment strategy
All asthmatics should be instructed for severe,
attacks:
To take up to four puffs of albuterol
every 20 minutes over 1 hour.
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Acute Asthma
In mild attacks subcutaneous epinephrine or
inhalation of a receptor agonist are equally
effective.
Both of them are superior to IV aminophylline.
For severe attacks:
Oxygen
Frequent administration of aerosolized
albuterol
Systemic treatment with corticosteroids.
Patients should be closely watched.
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