Asthma Drugs Beta-2 agonists Metaproterenol, terbutaline, albuterol, salbutamol, isoetharine, salmeterol MOA: bronchodilation, also inc mucus clearance, dec microvasc perm, dec inflam cell mediator release Metered dose inhaler preferred over nebulizer due to lower side effects Short acting (albuterol) for acute Rx, long acting (salmeterol bid) for prophylaxis/maintenance PK: usually first pass effect Tox: tolerance due to receptor downregulation*, CV, CNS, hypoK, hyperGlc Salmeterol Long acting beta-2 agonist for prophylaxis/maintenance PK: bid Formoterol Long acting beta-2 agonist for prophylaxis/maintenance PK: bid Ipratropium bromide MOA: Cholinergic & reflex bronchoconstr blocker Acute Rx (2nd line behind or in combination w/ beta-2 agonist) 1st line COPD Rx PK: slightly slower onset than beta-2 agonists Theophylline (methylxanthines) MOA: relaxes SMC -> bronchodilation Also inc resp mm contractility Acute Rx with caution PK: highly variable (indiv therapy, start at low dose), zero order elim at high dose, many drug interactions Tox: worse w/ higher serum conc*, CNS, (-) GI, (+) CV, (+) metabolic, diuresis Systemic steroids Acute Rx with caution Inhaled steroids Beclomethasone, triamcinolone, flunisolide, fluticasone, budesonide MOA: block phospholipase A2 -> dec inflam cell mediator release 1st line prophylaxis/maintenance Rx, perhaps in combination with long acting beta agonist PK: use minimum dose req'd Tox: laryngeal myopathy*, Candida thrush*, ?cataracts, ?dec growth, osteoporosis Advair(TM) Fluticasone + salmeterol Prophylaxis/maintenance Rx only PK: bid max Cromolyn MOA: anti-inflammatory, details unclear Prophylaxis Rx against exercise & allergen challenge Rx allergic rhinitis Tox: HA, nausea Nedocromil MOA: anti-inflammatory, broader than cromolyn Prophylaxis Rx against exercise & cold challenge Zafirlukast MOA: leukotriene-R blocker Prophylaxis/maintenance Rx PK: oral bid, CYP-450 drug interactions Tox: HA, gastritis, parhyngitis, rhinitis, eosinophilic vasculitis (rare but serious) Montelukast MOA: leukotriene-R blocker Prophylaxis/maintenance Rx Preferred over zafirlukast (no effect on CYP-450, no vasculitis) Steroid sparing therapy PK: qd Zileuton MOA: 5-lipoxygenase inhibitor -> dec leukotriene synthesis Prophylaxis/maintenance Rx, but not used often PK: qid Omalizumab MOA: human anti-IgE mAb Rx severe recurrent asthma, expensive PK: every 4 wks Tox: anaphylaxis