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Inhaled Corticosteroids -
1) Medications
2) MOA
3) Indication
1) Medications:
-mometasone (Asmanex)
-fluticasone (Flovent)
-budesonide (Pulmicort)
-beclomethasone (Qvar)
-Block late-phase activation to allergen, inhibit inflammatory cell migration and activation
-Controller drug, prevention of inflammation
Comment:
-Need consistent use to be helpful
-Cornerstone medication of most asthma levels
Mast Cell Stabilizer -
-cromolyn sodium (Intal)
-nedocromil (Tilade)
2) MOA:
-Halts degradation of mast cells and release of histamine and other inflammatory mediators
3) Indication:
-Less clinical effect compared with ICS
Leukotriene Receptor Antagonist (aka Leukotriene Modifier) -
-montelukast (Singulair)
-zafirlukast (Accolate)
-Leukotriene inhibitor - zileuton (Zyflo)
-Inhibit action of inflammatory mediator (leukotriene) by blocking select receptor sites
-Likely less effective than ICS
-Particularly effective add-on medication when disease control is inadequate w/ ICS, when asthma is complicated by allergic rhinitis
-In mild, persistent asthma, an alternative, although not preferred, therapeutic option for controller therapy
Systemic Corticosteroids (oral or parenteral) -
1) MOA
2) Indication
1) MOA:
Inhibit eosinophilic action and other inflammatory mediators
2) Indication:
-Treatment of acute inflammation such as in asthma flare or COPD exacerbation
Comments:
-Oral route preferred whenever possible
-Indicated in treatment of acute asthma flare to reduce inflammation
-In higher doses and with longer therapy (> 2 weeks), adrenal suppression may occur
-No taper needed if use is short-term (< 10 days) and at lower dose (prednisone, 40-60 mg/d or less)
-Potential for causing gastropathy, particularly gastric ulcer and gastritis
Short-Acting Beta2-Agonists (SABAs) -
- Albuterol (Ventolin, Proventil)
- Pirbuterol (Maxair)
-Levalbuterol (Xopenex)
-Beta2-agonists; bronchodilation via stimulation of beta2-receptor site
-Rescue drugs for treatment of acute bronchospasm
-Albuterol and Pirbuterol:
*Onset of action - 15 mins
*Duration of action - 4-6 hours
-Compared w/ albuterol and pirbuterol, levalbuterol, a single isomer of the racemate albuterol, is often better tolerated w/ potentially better bronchodilation than the other short-acting beta2-agonists, owing to its lower recommended dose.
Long-Acting Beta2-Agonists (LABAs) -
-salmeterol (Serevent)
-formoterol (Foradil)
-arformotorol (Brovana)
- LABAs; bronchodilation through stimulation of receptor site beta2
-Prevention of bronchospasm
- Salmeterol:
*Onset of action: 1 hr
*DOA: 12 hrs
- Formoterol:
*Onset of action: 15-30 mins
-LABAs are indicated for prevention rather than treatment of bronchospasm
-Patient should also have SABA as rescue drug
-Although LABA use decreases number of asthma episodes, the use of these meds may increase the chance of a severe asthma episode and, rarely, increase risk of asthma death -- FDA-mandated box warning about this risk
Anticholinergic Agents -
-ipratropium bromide (Atrovent)
-tiotropium bromide (Spiriva)
-Anticholinergic and muscarinic antagonist, yielding bronchodilation
-Treatment of bronchospam, mild anti-inflammatory
-Onset of Action ≥ 30 mins
-Best used to avoid rather than treat bronchospasm assoc. w/ COPD and asthma
-Well tolerated
Theophylline:
-Mild bronchodilator via non-phosphodiesterase inhibitor
-Possible mild anti-inflammatory effect
-Prevention of bronchospasm, mild anti-inflammatory
-Narrow therapeutic index drug w/ numerous potential drug interactions
-Monitor carefully for toxicity by checking drug levels and clinical presentation
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