Drugs for Asthma and COPD

Question 1

What are the two main classes of drugs used in the treatment of asthma?

Answer 1

1. bronchodilators – used to relieve acute symptoms and for control therapy
2. Anti-inflammatory agents – used to control or prevent symptoms.

Question 2

What kind of drugs are albuterol, levalbuterol, metaproterenol, and pirbuterol?

Answer 2

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

Question 3

What kind of drugs are salmeterol and formoterol?

Answer 3

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

Question 4

salmeterol

Answer 4

Long acting beta2 selective agonists (LABAs) - used in treatment of asthma

Question 5

formoterol

Answer 5

Long acting beta2 selective agonists (LABAs) - used in treatment of asthma

Question 6

what is the function of methylxanthine drugs?

Answer 6

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

Question 7

what kind of drug is theophylline and aminophylline, and what are they used for?

Answer 7

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

Question 8

How can atropine be used in the treatment of asthma?

Answer 8

Atropine: short acting muscarinic receptor antagonist (SAMRA) - low doses cause bronchodilation without increasing heart rate

effects last ~5 hours

Question 9

What kind of drug is ipratropium bromide?

Answer 9

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)

Question 10

How are corticosteroids used in the treatment of asthma?

Answer 10

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

Question 11

Budesonide

Answer 11

budesonide: corticosteroid used to treat asthma – reduces bronchial reactivity and decreases inflammation/ immune cells

Inhaled corticosteroids (ICS) first-line for treatment of chronic asthma

Question 12

what is the pathway by which leukotrienes are made

Answer 12

arachidonic acid —> 5-lypoxygenase —> leukotrienes —> LTC4, LTD4, LTE3, etc

Question 13

how are leukotriene antagonists used to treat asthma?

Answer 13

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)

Question 14

what kind of drugs are Zafirlukast and Montelukast and what are they used for?

Answer 14

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

Question 15

Zafirlukast

Answer 15

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

Question 16

Montelukast

Answer 16

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

Question 17

Omalizumab

Answer 17

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

Question 18

what do mepolizumab, reslizumab, and benralizumab target? what are they used for?

Answer 18

mAb targeting circulating IL-5 - subcutaneous administration lowers levels of circulating eosinophils

indicated for use in patients with eosinophilic asthma

Question 19

mepolizumab

Answer 19

mAb targeting circulating IL-5 - subcutaneous administration lowers levels of circulating eosinophils

indicated for use in patients with eosinophilic asthma

Question 20

benralizumab

Answer 20

mAb targeting IL-5 receptor alpha - subcutaneous administration lowers levels of circulating eosinophils

indicated for use in patients with eosinophilic asthma

Question 21

what treatment is given to patients with only occasional asthma symptoms required only on as needed basis?

Answer 21

Inhaled SABA (ex, albuterol)

Question 22

what three conditions dictate when patients with asthma require more than as-needed inhaled SABA?

Answer 22

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)

Question 23

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

Answer 23

COPD: mainly affects older adults that are current or former smokers

symptoms worsen slowly over time with limited relief form rapid-acting bronchodilators

Question 24

What kind of drugs are tiotropium bromide and aclidinium bromide and what are they used for?

Answer 24

Long-acting muscarinic receptor antagonists (LAMRAs) - inhaled bronchodilators

used to treat COPD (not typically used to treat asthma)

Question 25

tiotropium bromide

Answer 25

Long-acting muscarinic receptor antagonist (LAMRA) - inhaled bronchodilator

used to treat COPD (not typically used to treat asthma)

Question 26

aclidinium bromide

Answer 26

Long-acting muscarinic receptor antagonist (LAMRA) - inhaled bronchodilator

used to treat COPD (not typically used to treat asthma)

Question 27

how are Fluticasone-Vilanterol (Breo®) or Budesonide-Formoterol
(Symbicort®) used in treatment of COPD?

Answer 27

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.

Question 28

how are acute vs chronic COPD symptoms managed?

Answer 28

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]