Pulmonary Agents
DRUGS FOR ASTHMA
What are the classifications of asthma severity?
Mild intermittent; mild persistent; moderate persistent; severe persistent
What are the main classifications of drugs for asthma?
Bronchodilators; anti-inflammatory agents
Name the drug class for each of the following medications:
Albuterol
Short-acting β2-adrenergic agonist
Epinephrine
Short-acting β2-adrenergic agonist
Terbutaline
Short-acting β2-adrenergic agonist
Salmeterol
Long-acting β2-adrenergic agonist
Formoterol
Long-acting β2-adrenergic agonist
Isoproterenol
Short-acting β-adrenergic agonist
Metaproterenol
Short-acting β-adrenergic agonist
Fluticasone
Inhaled corticosteroid
Flunisolide
Inhaled corticosteroid
Beclomethasone
Inhaled corticosteroid
Triamcinolone
Inhaled corticosteroid
Budesonide
Inhaled corticosteroid
Methylprednisolone
Systemic corticosteroid
Prednisone
Systemic corticosteroid
Cromolyn
Mast cell stabilizer
Nedocromil
Mast cell stabilizer
Ipratropium
Inhaled anticholinergic
Tiotropium
Inhaled anticholinergic
Theophylline
Phosphodiesterase inhibitor; adenosine antagonist; methylxanthine
Zileuton
5-Lipoxygenase inhibitor
Zafirlukast
Leukotriene receptor antagonist
Montelukast
Leukotriene receptor antagonist
How do β2-agonists help treat asthma?
Bronchodilation via β2-adrenoceptor-mediated smooth muscle relaxation
How do corticosteroids help treat asthma?
Decrease production and release of proinflammatory cytokines; decrease inflammatory cell activation, recruitment, and infiltration; decrease vascular permeability; decrease mucous production; increase number and sensitivity of β2-adrenergic receptors
How do mast cell stabilizers help treat asthma?
Prevent mast cell degranulation, thereby decreasing release of histamine, platelet activating factor, leukotrienes, and other mediators that cause bronchoconstriction. Therefore only useful before exposure to allergen.
How do inhaled anticholinergics help treat asthma?
Competitively inhibit muscarinic receptors, thereby inhibiting vagal-mediated bronchoconstriction; reduce mucous production
How do phosphodiesterase inhibitors help treat asthma?
Increase cAMP which causes bronchodilation
How do 5-lipoxygenase inhibitors help treat asthma?
Inhibits production of leukotrienes (LTC4, LTD4, LTE4) from arachidonic acid, thereby preventing bronchoconstriction
What β2-adrenergic agonist is commonly used as a tocolytic agent (stops premature labor by relaxing uterine smooth muscle)?
Terbutaline
What cation can be used as a tocolytic agent?
Mg2+ (Magnesium ion)
Is cromolyn used for treatment or prevention of an asthma attack?
Prevention
Is nedocromil effective during an acute asthma attack?
No
What are the side effects of mast cell stabilizers?
Bitter taste; throat irritation
What are the side effects of β2-adrenergic agonists?
Tachycardia; muscle tremors; anxiety; arrhythmias; hyperglycemia; hypokalemia; hypomagnesemia (systemic side effects are minimized when drug is delivered via inhalation)
What are the side effects of 5-lipoxygenase inhibitors and leukotriene antagonists?
Increased liver function tests (LFTs); headache; Churg-Strauss syndrome
What is the main nonsystemic side effect of inhaled corticosteroids?
Thrush
What is thrush?
Oropharyngeal candidiasis
How can you prevent thrush when using inhaled corticosteroids?
Use of a spacer device; rinse mouth with water after medication use
What is a possible systemic side effect of inhaled corticosteroids in children?
Decreased growth of long bones
If using an inhaled corticosteroid and β2-adrenergic agonist together, which do you use first?
β2-adrenergic agonist (bronchodilates the airways, thereby increasing amount of corticosteroid that is delivered to its site of action)
What are the side effects of theophylline?
Tachycardia; arrhythmias; nausea; diarrhea; central nervous system (CNS) excitation (narrow therapeutic index)
Give an example of a methylxanthine other than theophylline:
Caffeine; theobromine; aminophylline
Why do inhaled anticholinergics have a minimal side effect profile?
Quaternary ammonium derivatives of atropine, therefore, do not leave the pulmonary system and cannot cross the blood-brain barrier
What are examples of systemic anticholinergic side effects?
Dry mouth; dry eyes; constipation; urinary retention; blurred vision; mydriasis; drowsiness; tachycardia
How do you treat β-blocker-induced bronchospasm?
With anticholinergics such as ipratropium and tiotropium
Name two drugs used to treat an acute asthma attack:
- Epinephrine
- Albuterol
What is the IV form of theophylline called?
Aminophylline (2:1 complex of theophylline and ethylenediamine)
What is the term used to describe a severe asthma attack that does not respond to usual asthma therapy?
Status asthmaticus
How is status asthmaticus treated?
Oxygen; inhaled albuterol; intravenous or oral corticosteroids; inhaled anticholinergics
What is the drug of choice for mild asthma?
Short-acting α2-adrenergic agonist
What is the maintenance drug of choice for chronic asthma?
Inhaled glucocorticoid
How is theophylline primarily metabolized?
Hepatic cytochrome P-450 enzymes (CYP 1A2 and CYP 3A4)
Give examples of medications that can lead to increased theophylline levels when used concomitantly:
Cimetidine; erythromycin; fluoroquinolones
What drug can cause asthma, nasal polyps, and rhinitis?
Aspirin (“aspirin triad”); seen in the rare case of aspirin sensitivity where inhibition of cyclooxygenase (COX) leads to a buildup of leukotrienes
CHRONIC OBSTRUCTIVE PULMONARY DISEASE AGENTS
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