Leukotriene modifiers

a. Zafirlukast (Accolate), montelukast (Singulair) and zileuton (Zyflo) interfere with the actions of leukotriene inflammatory mediators, preventing bronchoconstriction. Zileuton is a 5-lipoxygenase inhibitor. Zafirlukast is a leukotriene receptor antagonist. Montelukast is similar to zafirlukast but is taken only once per day at night. Zafirlukast must be taken on an empty stomach.

b. Zafirlukast and zileuton may interfere with the metabolism ofwarfarin (Coumadin).

c. Zileuton has been associated with elevated levels of liver enzymes; thus, periodic monitoring of alanine transaminase is required. Zafirlukast (Accolate, 20 mg bid, on an empty stomach), montelukast (Singular, 10 mg PO qhs) and zileuton (Zyflo, 600 mg PO qid) are alternatives for patients with mild persistent asthma who are not candidates for inhaled anti-inflammatory medications.

4. Long-acting beta2 agonists. If inhaled anti-inflammatory medications do not prevent asthma symptoms, an inhaled long-acting beta2 agonist may be added. Long-acting beta2 agonists relax bronchial smooth muscle. Salmeterol (Serevent, 2 puffs bid), a long-acting beta2 agonist, has a slower onset of action (up to 30 minutes) but a longer duration (at least 12 hours) than short-acting beta2 agonists. Salmeterol improves nighttime and exercise-associated symptoms. Patients should not use salmeterol for acute asthma attacks.

5. Methylxanthines use has declined with the arrival of safer and more effective medications. However, they still have a role in asthma therapy when newer anti-inflammatory medications fail to provide relief. Theophylline produces smooth muscle relaxation resulting in bronchodilation but also improves diaphragmatic contractility and increases mucociliary clearance. It may also have some anti-inflammatory effects. Selected patients may benefit from a sustained-action theophylline preparation in the evening, with the drug titrated to a serum concentration ranging from 5 to 15 pg/mL. Theophylline sustained release (Theo-Dur, 100-400 mg PO bid).

Beta2 Agonists and Dosing

Drug

Trade name

Dosage

Long-Acting Agent

Salmeterol

Serevent

2 puffs bid

Short-Acting Agents

Albuterol

Ventolin Rotacaps

Proventil Ventolin

One inhaled capsule every four to eight hours prn

2-4 puffs q4-8h prn

Albuterol HTA

Proventil HFA

2-4 puffs q4-8h prn

Bitolterol

Tornalate

2-4 puffs q4-8h prn

Pirbuterol

Maxair

2-4 puffs q4-8h prn

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