614 - Asthma drugs Flashcards
What two pathways are targeted in asthma therapy?
Those involved in bronchoconstriction: 1. inflammatory processes 2. parasympathetic tone
What are three β2-agonists used to treat asthma?
albuterol, salmeterol, formoterol
Which of the β2-agonists are used as long-acting agents for asthma prophylaxis? What are the adverse effects?
Salmeterol, formoterol; tremor and arrhythmia
How do β2 agonists help in the treatment of asthma?
relax bronchial smooth muscle
Which of the β2 agonists are useful for acute exacerbations of asthma?
Albuterol
What is an example of a methylxanthine used for the treatment of asthma?
Theophylline
How does theophylline work?
likely causes bronchodilation by inhibiting phosphodiesterase → ↑ cAMP levels due to ↓ cAMP hydrolysis
Why is the usage of theophylline for the treatment of asthma limited?
Narrow therapeutic index (cardio- and neurotoxicity)
What metabolizes theophylline?
cytochrome P-450
How does theophylline relate to adenosine?
theophylline blocks the actions of adenosine
What is a muscarinic antagonist used in the treatment of asthma?
Ipratropium
How does ipratropium work as an asthma treatment?
competitive blockade of muscarinic receptors, preventing bronchoconstriction
What is another form of ipratropium that is used as a long-acting muscarinic antagonist in the treatment of COPD?
tiotropium
What are two corticosteroids used in asthma treatment?
beclomethasone, fluticasone
How do beclomethasone and fluticasone work?
- inhibit the synthesis of virtually all cytokines 2. inactivate NK-kB (transcription factor that induces the production of TNF-α and other inflammatory agents)
Are corticosteroids used as a first line therapy for asthma?
yes, for chronic asthma treatment
List 3 antileukotrienes used in asthma treatment:
- Montelukast 2. Zafirlukast 3. Zileuton
Which antileukotrienes block leukotriene receptors?
montelukast, zafirlukast
What treatment especially good for asprin-induced asthma?
leukotriene receptor blockers montelukast and zafirlukast
How does the antileukotriene zileuton work?
inhibits the 5-lipooxygenase pathway, blocking conversion of arachidonic acid to leukotrienes
What is omalizumab?
a monoclonal anti-IgE antibody which binds mostly unbound serum IgE and blocks binding to FcϵRI.
When would omalizumab be used in asthma treatment?
used in allergic asthma resistant to inhaled steroids and long-acting β2-agnoists
What is methacholine?
a muscarinic receptor agonist used in bornchial provocation challenge to help diagnose asthma
What is the treatment for pulmonary arterial hypertension? How does it work?
bosentan; competitively antagonizes endothelin-1 receptors, ↓ pulmonary vascular resistance
Fill in the blank:
Beta agonists
Muscarinic antagonists
