Respiratory Medications Study Guide
1.
Bronchodilators
A.
Beta-2 Agonists
• MOA:
o Bind to beta-2 receptors on airway smooth muscle → activate cyclic AMP
pathway → muscle relaxation → bronchodilation
o Inhibit release of hypersensitivity mediators (mast cells) o Some beta-1 receptor
activity → possible cardiac side effects Pharmacokinetics:
o Absorbed in bronchi → metabolized in liver → excreted in urine Adverse
Effects: o Tachycardia, tremors Precautions:
o Monitor in arrhythmias, cardiovascular disease (CVD), hyperthyroidism
• Indications:
o SABA (Short-acting Beta Agonists): Acute asthma attacks, rescue inhalers
SABA on beta blockers: Add a SAMA to help with
bronchodilation o LABA (Long-acting Beta Agonists): Maintenance therapy,
must be combined with ICS (black box warning) avoid monotherapy
Don’t treat acute asthma with LABA. Initial episodes of
asthma exacerbation are treated by increasing frequency of SABAs
Special Notes: o If patient on beta-blocker + SABA → add SAMA for
better bronchodilation
• Examples:
o SABA: Albuterol (Proair, Ventolin, Proventil), Levalbuterol (Xopenex) o LABA:
Salmeterol (Serevent), Formoterol (Foradil), Arformoterol (Brovana)
,B.
Inhaled Anticholinergics (Muscarinic Antagonists)
• MOA:
o LAMAs: Block M3 receptors → prevent acetylcholine (ACh) from stimulating
airway goblet cells → reduce mucus production
o Cause bronchodilation by decreasing cyclic GMP → decrease smooth muscle
contractility Side Effects:
o “Can’t see, can’t pee, can’t spit, can’t poop” (anticholinergic side effects), more
common in elderly Precautions:
o Avoid in patients with urinary retention, BPH, or closed-angle glaucoma o Not
for acute bronchospasm unless combined with albuterol
• Examples:
o LAMA (Long-acting): Tiotropium bromide (Spiriva)
2.
Inhaled Corticosteroids (ICS)
• MOA:
o Inhibit airway inflammation and block inflammatory mediators o Inhibit IgE and
mast cell migration (reduce late-phase allergic reaction) Pharmacokinetics:
o Rapid absorption from lungs and GI tract o Swallowed portion undergoes first-
pass metabolism o Excreted in urine and feces Adverse Effects:
o Xerostomia (dry mouth), hoarseness, mouth irritation, dysgeusia (taste change),
oral candidiasis Precautions:
o Contraindicated in status asthmaticus
o High doses in children may suppress hypothalamic-pituitary-adrenal
(HPA) axis → adrenal fatigue
Administration:
o Must be taken routinely
o Rinse mouth and spit after use to prevent oral candidiasis o Use spacer devices
to reduce side effects
• Examples:
o Fluticasone, Mometasone, Beclomethasone, Budesonide, Ciclesonide
3.
, Leukotriene Modifiers
• Pathophysiology:
o Leukotrienes (from eosinophils/mast cells) cause bronchospasm, airway
hyperresponsiveness, vascular leakage
• Types:
o Leukotriene Receptor Antagonists (LTRA): Montelukast (Singulair) MOA:
Blocks cysteinyl leukotriene receptor (blocks LTD4 action) Pharmacokinetics:
o Rapidly absorbed from GI, protein bound, metabolized in liver, excreted in urine
• Adverse Effects: o Montelukast: headache, sore throat, mood changes, dyspepsia
• Precautions:
o Neuropsychiatric events reported: irritability, agitation, tremors, insomnia,
depression, suicidality
o Avoid in severe liver disease (especially Zileuton)
4.
Monoclonal Antibodies
• Example: Omalizumab (Xolair)
• MOA: Binds IgE → prevents IgE from attaching to mast cells and basophils
Indication: Severe persistent asthma
5.
Decongestants
• Examples:
o Oral: Pseudoephedrine (Sudafed) o Intranasal: Oxymetazoline (Afrin)
• MOA: Alpha-adrenergic receptor agonists → vasoconstrict nasal mucosal arterioles →
reduce nasal congestion Pharmacokinetics:
o Oral pseudoephedrine well absorbed, crosses BBB, metabolized in liver, excreted
in urine Adverse Effects:
o Oral: anxiety, restlessness, tremors o Topical: burning, stinging, dryness,
sneezing
• Precautions:
o Avoid oral decongestants in severe hypertension, CVD, or patients on