Drugs for Asthma and COPD Flashcards
What are the two main classes of drugs used in the treatment of asthma?
- bronchodilators – used to relieve acute symptoms and for control therapy
- Anti-inflammatory agents – used to control or prevent symptoms.
What kind of drugs are albuterol, levalbuterol, metaproterenol, and pirbuterol?
short acting beta2 selective agonists (SABAs) – relax bronchial smooth muscle, and inhibit the release of bronchoconstricting substances from mast cells, some have anti-inflammatory effects
Used in treatment of asthma
What kind of drugs are salmeterol and formoterol?
Long acting beta2 selective agonists (LABAs) – duration of action 12+ hours due to high lipid solubility
used in treatment of asthma, not recommended as monotherapy because they lack anti-inflammatory action - work well with inhaled corticosteroids
Via metered-dose or dry powder inhalers
salmeterol
Long acting beta2 selective agonists (LABAs) - used in treatment of asthma
formoterol
Long acting beta2 selective agonists (LABAs) - used in treatment of asthma
what is the function of methylxanthine drugs?
PDE inhibitors – increase intracellular cAMP levels to cause bronchodilation, used to treat asthma
improve contractility of skeletal muscle - can reverse fatigue of the diaphragm in patients with COPD
ex: theophylline, aminophylline
narrow therapeutic window
what kind of drug is theophylline and aminophylline, and what are they used for?
Methylxanthine drugs (PDE inhibitors) – increase intracellular cAMP levels to cause bronchodilation
used to treat asthma, but have a narrow therapeutic window - toxicity can cause N/V, G.I., discomfort, seizures, and arrhythmia
How can atropine be used in the treatment of asthma?
Atropine: short acting muscarinic receptor antagonist (SAMRA) - low doses cause bronchodilation without increasing heart rate
effects last ~5 hours
What kind of drug is ipratropium bromide?
Ipratropium bromide: short acting muscarinic receptor antagonist (SAMRA) - induces bronchodilation
can be used to treat asthma when symptoms inadequately controlled by SABA alone
derivative of atropine (also SAMRA)
How are corticosteroids used in the treatment of asthma?
Don’t relax airway smooth muscle directly, but reduce bronchial reactivity —> reduce frequency of asthma, exacerbations
Inhibit mucosal inflammation and recruitment of immune cells
Aerosol treatment is most effective way to decrease systemic adverse effects – inhaled corticosteroids (ICS) are now first line agents to treat chronic asthma
ex: Fluticasone, Beclomethasone, Budesonide
Budesonide
budesonide: corticosteroid used to treat asthma – reduces bronchial reactivity and decreases inflammation/ immune cells
Inhaled corticosteroids (ICS) first-line for treatment of chronic asthma
what is the pathway by which leukotrienes are made
arachidonic acid —> 5-lypoxygenase —> leukotrienes —> LTC4, LTD4, LTE3, etc
how are leukotriene antagonists used to treat asthma?
leukotrienes are potent bronchoconstrictors - associated with mucus hypersecretion, increased bronchial reactivity, and mucosal edema
Therefore, antagonists help reduce these effects - effective in blocking airway responses to exercise and antigen challenge
Can be taken orally
ex: Zafirlukast and Montelukast (both LTD4 receptor antagonists), zileuton (5-lipoxygenase inhibitor)
what kind of drugs are Zafirlukast and Montelukast and what are they used for?
Zafirlukast and Montelukast: LTD4 (leukotriene) receptor antagonists (LTRAs), used in treatment of asthma
recall leukotrienes are potent bronchoconstrictors - associated with mucus hypersecretion, increased bronchial reactivity, and mucosal edema
Zafirlukast
LTD4 (leukotriene) receptor antagonist (LTRA) used in treatment of asthma
recall leukotrienes are potent bronchoconstrictors - associated with mucus hypersecretion, increased bronchial reactivity, and mucosal edema
Montelukast
LTD4 (leukotriene) receptor antagonist (LTRA) used in treatment of asthma
recall leukotrienes are potent bronchoconstrictors - associated with mucus hypersecretion, increased bronchial reactivity, and mucosal edema
Omalizumab
murine mAb that binds IgE to inhibit its binding to mast cells and basophils
used in treatment of asthma - lessens frequency of asthma attacks and reduces corticosteroid requirements
what do mepolizumab, reslizumab, and benralizumab target? what are they used for?
mAb targeting circulating IL-5 - subcutaneous administration lowers levels of circulating eosinophils
indicated for use in patients with eosinophilic asthma
mepolizumab
mAb targeting circulating IL-5 - subcutaneous administration lowers levels of circulating eosinophils
indicated for use in patients with eosinophilic asthma
benralizumab
mAb targeting IL-5 receptor alpha - subcutaneous administration lowers levels of circulating eosinophils
indicated for use in patients with eosinophilic asthma
what treatment is given to patients with only occasional asthma symptoms required only on as needed basis?
Inhaled SABA (ex, albuterol)
what three conditions dictate when patients with asthma require more than as-needed inhaled SABA?
a. rescued therapy required 2+ times per week
b. nocturnal symptoms occur 2+ times per month
c. FEV1 <80% predicted
first choice of addition would be low dose ICS (budesonide), can also use oral anti-leukotriene (montelukast)
theophylline reserved for patients who respond poorly to other treatments (narrow TI)
preventable and treatable disease,
characterized by persistent airflow limitation that is usually
progressive and associated with enhanced chronic inflammatory
response in the airways and lungs to noxious particles or gases
COPD: mainly affects older adults that are current or former smokers
symptoms worsen slowly over time with limited relief form rapid-acting bronchodilators
What kind of drugs are tiotropium bromide and aclidinium bromide and what are they used for?
Long-acting muscarinic receptor antagonists (LAMRAs) - inhaled bronchodilators
used to treat COPD (not typically used to treat asthma)
tiotropium bromide
Long-acting muscarinic receptor antagonist (LAMRA) - inhaled bronchodilator
used to treat COPD (not typically used to treat asthma)
aclidinium bromide
Long-acting muscarinic receptor antagonist (LAMRA) - inhaled bronchodilator
used to treat COPD (not typically used to treat asthma)
how are Fluticasone-Vilanterol (Breo®) or Budesonide-Formoterol
(Symbicort®) used in treatment of COPD?
Corticosteroid-LABA combinations mainly utilized for those with frequent exacerbations.
Not used as control therapy in those
without exacerbations because of potential for secondary bacterial
infections of the lungs.
how are acute vs chronic COPD symptoms managed?
acute: inhalation of SABA (albuterol), SAMRA (ipratropium), or SABA-SAMRA combination
[think S for Short]
chronic: LAMRA (tiotropium or aclidinium bromide), corticosteroid-LABA combination (fluticasone-vilanterol, aka Breo), or LAMRA-LABA-corticosteroid combination
[think L for Long]
