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:

1. Epinephrine
   
2. 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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