Asthma Medications Flashcards
Epinephrine
- bronchodilator
- nonselective agonists of both beta-1 and beta-2 adrenoreceptors
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- use in asthma has been larely supplanted by the development of less cardiotoxic, beta-2 selective agents
- toxicities include tachycardia, arrhythmias, and worsening of angina pectoris
Ephedrine
- bronchodilator
- nonselective agonists of both beta-1 and beta-2 adrenoreceptors
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- use in asthma has been larely supplanted by the development of less cardiotoxic, beta-2 selective agents
- toxicities include tachycardia, arrhythmias, and worsening of angina pectoris
Isoproterenol
- bronchodilator
- nonselective agonists of both beta-1 and beta-2 adrenoreceptors
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- use in asthma has been larely supplanted by the development of less cardiotoxic, beta-2 selective agents
- toxicities include tachycardia, arrhythmias, and worsening of angina pectoris
Albuterol
- short-acting beta-2 Selective Adrenoreceptor Agonist (SABA)
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- maximal broncodilation achieved in 15-30 min and persists for 3-4 hrs
- used for relief of acute asthma symptoms and bronchospasm
- inhalation is the preferred route of delivery for maximal local effect on airway smooth muscle with minimal systemic toxicity
- appear to be safe and effective when taken on an “as needed” basis for relief of symptoms
Terbutaline
- short-acting beta-2 Selective Adrenoreceptor Agonist (SABA)
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- maximal broncodilation achieved in 15-30 min and persists for 3-4 hrs
- used for relief of acute asthma symptoms and bronchospasm
- inhalation is the preferred route of delivery for maximal local effect on airway smooth muscle with minimal systemic toxicity
- appear to be safe and effective when taken on an “as needed” basis for relief of symptoms
Metaproterenol
- short-acting beta-2 Selective Adrenoreceptor Agonist (SABA)
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- maximal broncodilation achieved in 15-30 min and persists for 3-4 hrs
- used for relief of acute asthma symptoms and bronchospasm
- inhalation is the preferred route of delivery for maximal local effect on airway smooth muscle with minimal systemic toxicity
- appear to be safe and effective when taken on an “as needed” basis for relief of symptoms
Pirbuterol
- short-acting beta-2 Selective Adrenoreceptor Agonist (SABA)
- relaxes bronchial smooth muscle
- inhibits the release of bronchoconstricting substances from mast cells
- maximal broncodilation achieved in 15-30 min and persists for 3-4 hrs
- used for relief of acute asthma symptoms and bronchospasm
- inhalation is the preferred route of delivery for maximal local effect on airway smooth muscle with minimal systemic toxicity
- appear to be safe and effective when taken on an “as needed” basis for relief of symptoms
Salmeterol
-long-acting beta-2 selective agonist (LABA)
-*** a partial agonist of beta-2 adrenoreceptors
-relaxes bronchial smooth muscle
inhibits the release of bronchoconstricting substances from mast cells
-duration of action is >12 hours, due to high lipid solubility
-useful in cases of refractory or severe asthma
-not recommended as monotherapy (no anti-inflammatory actions), but work well in combination with inhaled corticosteroids
-chronic use is associated with a small bust statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Formoterol
-long-acting beta-2 selective agonist (LABA)
-relaxes bronchial smooth muscle
inhibits the release of bronchoconstricting substances from mast cells
-duration of action is >12 hours, due to high lipid solubility
-useful in cases of refractory or severe asthma
-not recommended as monotherapy (no anti-inflammatory actions), but work well in combination with inhaled corticosteroids
-***Performist preparation of formoterol is only approved for the treatment of chronic COPD symptoms
-chronic use is associated with a small bust statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Arformoterol
-long-acting beta-2 selective agonist (LABA)
-relaxes bronchial smooth muscle
inhibits the release of bronchoconstricting substances from mast cells
-duration of action is >12 hours, due to high lipid solubility
only approved for the treatment of chronic COPD symptoms
-chronic use is associated with a small bust statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Vilanterol
-long-acting beta-2 selective agonist (LABA)
-relaxes bronchial smooth muscle
-***only available as a combination with a corticosteroid
inhibits the release of bronchoconstricting substances from mast cells
-duration of action is >12 hours, due to high lipid solubility
only approved for the treatment of chronic COPD symptoms
-chronic use is associated with a small bust statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Theophylline
- methylxanthine drug
- inhibit the phosphodiesterase that converts cyclic AMP to AMP
- antagonist of mast cell adenosine receptors
- bronchodilation and relaxation of airway smooth muscle
- relieves airflow obstruction in acute asthma and reduces severity of symptoms
- improves contractility of isolated skeletal muscle and reverses fatigue of the diaphragm in COPD patients
- because of toxicity issues, now reserved for patients who respond poorly to an inhaled corticosteroid combined with an “as needed” beta-2 agonist
- toxicities mandate occasional measurement of plasma levels of the drug
- plasma level >20 mg/L can lead to anorexia, nausea, vomiting, abd discomfort, headache, anxiety
- plasma level >40 mg/L can lead to seizures and arrhythmias
Aminophylline
- methylxanthine drug
- ethylenediamine salt of theophylline
- inhibit the phosphodiesterase that converts cyclic AMP to AMP
- antagonist of mast cell adenosine receptors
- bronchodilation and relaxation of airway smooth muscle
- relieves airflow obstruction in acute asthma and reduces severity of symptoms
- improves contractility of isolated skeletal muscle and reverses fatigue of the diaphragm in COPD patients
- because of toxicity issues, now reserved for patients who respond poorly to an inhaled corticosteroid combined with an “as needed” beta-2 agonist
- toxicities mandate occasional measurement of plasma levels of the drug
- plasma level >20 mg/L can lead to anorexia, nausea, vomiting, abd discomfort, headache, anxiety
- plasma level >40 mg/L can lead to seizures and arrhythmias
Atropine
- muscarinic receptor Antagonist (MA)
- antagonize the effect of acetylcholine at muscarinic receptors
- bronchodilation through inhibition of the parasympathetic pathways associated with bronchoconstriction
- potential toxicities have limited the use of atropine
- urinary retention, tachycardia, loss of visual accommodation, agitation
Ipratropium Bromide
- muscarinic receptor Antagonist (MA)
- antagonize the effect of acetylcholine at muscarinic receptors
- bronchodilation through inhibition of the parasympathetic pathways associated with bronchoconstriction
- ipratropium bromide alone or in combination with albuterol (e.g. Combivent and DuoNeb) are useful int he treatment of acute severe asthma and acute COPD symptoms (the combination is synergistic)
- reduced toxicity relative to atropine, due to selective airway delivery, with minimized potential for absorption into the circulation and entry into the CNS
Tiotropium Bromide
- muscarinic receptor Antagonist (MA)
- antagonize the effect of acetylcholine at muscarinic receptors
- bronchodilation through inhibition of the parasympathetic pathways associated with bronchoconstriction
- long-acting muscarinic antagonist (LAMA)
- only approved for the treatment chronic COPD symptoms
- reduced toxicity relative to atropine, due to selective airway delivery, with minimized potential for absorption into the circulation and entry into the CNS
Aclidinium Bromide
- muscarinic receptor Antagonist (MA)
- antagonize the effect of acetylcholine at muscarinic receptors
- bronchodilation through inhibition of the parasympathetic pathways associated with bronchoconstriction
- long-acting muscarinic antagonist (LAMA)
- only approved for the treatment chronic COPD symptoms
- reduced toxicity relative to atropine, due to selective airway delivery, with minimized potential for absorption into the circulation and entry into the CNS
Itratropium Bromide-Albuterol
-MA in combination with SABA
Beclomathesone
- corticosteroid
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- toxicity: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in growth rate of 1 cm in children during 1st year, but none thereafter
Budesonide
- corticosteroid
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- toxicity: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in growth rate of 1 cm in children during 1st year, but none thereafter
Flunisolide
- corticosteroid
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- toxicity: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in growth rate of 1 cm in children during 1st year, but none thereafter
Fluticasone
- corticosteroid
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- toxicity: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in growth rate of 1 cm in children during 1st year, but none thereafter
Mometasone
- corticosteroid
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- toxicity: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in growth rate of 1 cm in children during 1st year, but none thereafter
Triamcinolone Acetonide
- corticosteroid
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- toxicity: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in growth rate of 1 cm in children during 1st year, but none thereafter
Budesonide-Formoterol
- corticosteroid
- combination with LABA
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- useful in the chronic treatment of refractory and severe asthma that is poorly controlled by standard doses of inhaled corticosteroid alone
- toxicty: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in grwoth rate of 1 cm in children during 1st year, but none thereafter
- chronic use of combinations with LABAs is associated with a small but statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Fluticasone-Salmeterol
- corticosteroid
- combination with LABA
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- useful in the chronic treatment of refractory and severe asthma that is poorly controlled by standard doses of inhaled corticosteroid alone
- toxicty: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in grwoth rate of 1 cm in children during 1st year, but none thereafter
- chronic use of combinations with LABAs is associated with a small but statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Fluticasone-Vilanterol
- corticosteroid
- combination with LABA
- inhibit the production of inflammatory cytokines
- alleviate airway obstruction by inhibiting mucosal inflammation in asthmatic airways
- reduce bronchial reactivity
- reduce the frequency of asthma exacerbation if administered chronically
- potentiate the effects of beta-2 agonists
- inhalation treatment most effective way to minimize systemic absorption and potential for adverse effects
- first-line agents for the treatment of moderate chronic asthma together with an “as needed” beta-2 agonist
- *** only approved for the treatment of chronic COPD sxs
- toxicty: oropharyngeal candidiasis; low risk of osteoporosis and cataracts in adults; reduction in grwoth rate of 1 cm in children during 1st year, but none thereafter
- chronic use of combinations with LABAs is associated with a small but statistically significant increase in the low risk of a fatal asthma attack, particularly for African Americans
Zileuton
- antileukotrienes
- inhibits 5-lipoxygenase, thereby inhibiting leukotriene synthesis
- inhibit the mucosal hypersecretion, bronchial reactivity, and mucosal edema produced by leukotrienes
- anti-inflammatory effects are less pronounced than those of corticosteroids, but are equally efective at reducing the frequency of exacerbations
- effective in blocking airway responses to exercise and antigen challenge
- second-line agents for the treatment of chronic moderate asthma together with an “as needed” beta-2 agonist
- can be taken orally, and is therefore useful for patients that comply poorly with inhaled therapies
- appear to have little toxicity
- has been associated with a few reports of liver toxicity
Zafirlukast
- antileukotrienes
- antagonize the binding of leukotriene D4 (LTD4) to its receptor
- inhibit the mucosal hypersecretion, bronchial reactivity, and mucosal edema produced by leukotrienes
- anti-inflammatory effects are less pronounced than those of corticosteroids, but are equally efective at reducing the frequency of exacerbations
- effective in blocking airway responses to exercise and antigen challenge
- second-line agents for the treatment of chronic moderate asthma together with an “as needed” beta-2 agonist
- can be taken orally, and is therefore useful for patients that comply poorly with inhaled therapies
Montelukast
- antileukotrienes
- antagonize the binding of leukotriene D4 (LTD4) to its receptor
- inhibit the mucosal hypersecretion, bronchial reactivity, and mucosal edema produced by leukotrienes
- anti-inflammatory effects are less pronounced than those of corticosteroids, but are equally efective at reducing the frequency of exacerbations
- effective in blocking airway responses to exercise and antigen challenge
- second-line agents for the treatment of chronic moderate asthma together with an “as needed” beta-2 agonist
- can be taken orally, and is therefore useful for patients
Omalizumab
- anti-IgE agent
- monoclonal antibody that targets IgE and inhibits IgE binding to mast cells and basophils
- subcutaneous administration lowers plasma IgE to undetectable levels
- lessens the frequency and severity of asthma attacks
- reduces corticosteroid requirements
- useful in patients with chronic severe asthma inadequately controlled by corticosteroid-LABA combination therapy
- anaphylaxis and malingnant neoplasms occur infrequently