Asthma

From Pharmpedia

In susceptible individuals, this inflammation causes recurrent episodes of wheezing, breathlessness, chest tightness, and coughing, particularly at night or in the early morning.

These episodes are usually associated with widespread but variable airflow obstruction that is often reversible either spontaneously or with treatment. The inflammation also causes an associated increase in the existing bronchial hyperresponsiveness to a variety of stimuli (NHLBI 1995).

1 Ahthma Symptoms occur or worsen in the presence of
2 Quick-relief medications
3 Long-term-control medications
4 References

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Ahthma Symptoms occur or worsen in the presence of

Inhalant allergens:

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Animal allergens

Occupational exposures

Irritants:

Other factors that can influence asthma severity:

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Quick-relief medications

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Short-acting beta2-agonists

Therapy of choice for relief of acute symptoms and prevention of EIB.

Albuterol

Bitolterol

Pirbuterol

Terbutaline

Mechanisms :

> Bronchodilation. Smooth muscle relaxation following adenylate cyclase activation and increase in cyclic AMP producing functional antagonism of bronchoconstriction.

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Anticholinergics

Ipratropium bromide may provide some additive benefit to inhaled beta2-agonists in severe exacerbations. May be an alternative bronchodilator for patients who do not tolerate inhaled beta2-agonists.

Mechanisms

> Bronchodilation.Competitive inhibition of muscarinic cholinergic receptors.

> Reduces intrinsic vagal tone to the airways. May block reflex bronchoconstriction secondary to irritants or to reflux esophagitis.

> May decrease mucus gland secretion.

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Systemic corticosteroids

Used for moderate-tosevere exacerbations to speed recovery and prevent recurrence of exacerbations.

Methylprednisolone

Prednisolone

Prednisone

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Long-term-control medications

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Corticosteroids:

Glucocorticoids are most potent and effective antiinflammatory medication currently available.

Inhaled form is used in the long-term control of asthma. Systemic corticosteroids are often used to gain prompt control of the disease when initiating long-term therapy.

Examples:

Inhaled:

Beclomethasone dipropionate

Budesonide

Flunisolide

Fluticasone propionate

Triamcinolone acetonide

Systemic:

Methylprednisolone

Prednisolone

Prednisone

Mechanisms

> Anti-inflammatory. Block late reaction to allergen and reduce airway hyperresponsiveness. Inhibit cytokine production, adhesion protein activation, and inflammatory cell migration and activation.

>Reverse beta2-receptor down-regulation. Inhibit microvascular leakage.

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Cromolyn sodium and nedocromil

Mild-tomoderate anti-inflammatory medications. May be used as initial choice for long-term-control therapy for children. Can also be used as preventive treatment prior to exercise or unavoidable exposure to known allergens.

Mechanisms

>Anti-inflammatory. Block early and late reaction to allergen. Interfere with chloride channel function. Stabilize mast cell membranes and inhibit activation and release of mediators from eosinophils and epithelial cells.

>Inhibit acute response to exercise, cold dry air, and SO2.

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Long-acting beta2-agonists

Long-acting bronchodilator used concomitantly with anti-inflammatory medications for long-term control of symptoms, especially nocturnal symptoms. Also prevents exercise-induced bronchospasm (EIB).

Examples :

Salmeterol (Inhaled)

sustained-release Albuterol (Oral)

Mechanisms

> Bronchodilation. Smooth muscle relaxation following adenylate cyclase activation and increase in cyclic AMP producing functional antagonism of bronchoconstriction.

> In vitro, inhibit mast cell mediator release, decrease vascular permeability, and increase mucociliary clearance.

>Compared to short-acting inhaled beta2-agonist, salmeterol(but not formoterol) has slower onset of action (15 to 30 minutes) but longer duration (>12 hours).

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Methylxanthines

Sustained-release theophylline is a mild-to-moderate bronchodilator used principally as adjuvant to inhaled corticosteroids for prevention of nocturnal asthma symptoms. May have mild antiinflammatory effect.

Theophylline, sustained-release tablets and capsules

Mechanisms

> Bronchodilation. Smooth muscle relaxation from phosphodiesterase inhibition and possibly adenosine antagonism

> May affect eosinophilic infiltration into bronchial mucosa as well as decrease T-lymphocyte numbers in epithelium.

>Increases diaphragm contractility and mucociliary clearance.

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Leukotriene modifiers

Zafirlukast, a leukotriene receptor antagonist, or zileuton, a 5-lipoxygenase inhibitor, may be considered an alternative therapy to low doses of inhaled corticosteroids or cromolyn or nedocromil for patients >_ 12 years of age with mild persistent asthma, although further clinical experience and study are needed to establish their roles in asthma therapy.

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References

http://www.nhlbi.nih.gov/guidelines/asthma/asthgdln.pdf

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Asthma

Contents

Ahthma Symptoms occur or worsen in the presence of

Quick-relief medications

Short-acting beta2-agonists

Anticholinergics

Systemic corticosteroids

Long-term-control medications

Corticosteroids:

Cromolyn sodium and nedocromil

Long-acting beta2-agonists

Methylxanthines

Leukotriene modifiers

References

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