Drugs Used in COPD and Asthma Flashcards
List 6 short-acting beta agonist bronchodilators
Albuterol Levalbuterol Metaproterenol Pirbuterol Epinephrine Terbutaline
Short-acting antimuscarinic bronchodilator
Ipratropium
Combination short-acting bronchodilator
Albuterol/ipratropium
List 4 Long-acting beta-adrenergic bronchodilators
Formoterol
Indacaterol
Olodaterol
Salmeterol
2 long acting antimuscarinic bronchodilators
Aclidinium
Tiotropium
What are 7 aerosol corticosteroids used in tx of asthma?
Beclomethasone Mometasone Fluticasone Triamcinolone Budesonide Ciclesonide Flunisolide
3 examples of combination LABA+Corticosteroid inhalers used in asthma
Formoterol/budesonide
Formoterol/mometasone
Salmeterol/fluticasone
Leukotriene inhibitors used in tx of asthma
Montelukast
Zafirlukast
Zileuton
Methylxanthines used in tx of asthma
Dyphylline
Theophylline
Monoclonal Ab used in tx of asthma
Omalizumab
MOA, effects, and clinical applications of Albuterol
MOA: selective beta2 agonist
Effects: prompt, efficacious bronchodilation
Clinical applications: asthma, COPD
Drug of choice in acute asthmatic bronchospasm
Albuterol
Pharmacokinetics and toxicities of albuterol
Aerosol inhalation; duration several hours, also available via nebulizer and parenteral use
Toxicity: tremor, tachycardia; overdose causes arrhythmia
Albuterol has similar MOA, effects, clinical applications, pharmacokinetics, and toxicities to what other beta agonists?
Metaproterenol
Terbutaline (although terbutaline is available as an oral drug)
MOA, effects, and clinical applications of salmeterol
MOA: Selective beta2 agonist
Effects: slow onset, primarily preventative action; potentiates corticosteroid effects
Clinical applications: bronchodilation, prevention of asthma exacerbation
Pharmacokinetics and toxicities associated with salmeterol
Aerosol inhalation; duration 12-24 hrs (high lipid solubility allows longer MOA)
Toxicity: tremor, tachycardia; overdose leads to arrhythmias
Salmeterol has similar MOA, effects, clinical applications, pharmacokinetics, and toxicities to what other beta agonist?
Formoterol
Nonselective alpha and beta agonist that causes bronchodilation + all other sympathomimetic effects on CV and other organ systems; used in anaphylaxis and sometimes for asthma (although rarely)
Epinephrine
MOA, effects, and clinical applications of isoproterenol
MOA: B1 and B2 agonist (available as aerosol, nebulizer, or parenteral)
Effects: bronchodilation + powerful CV effects
Clinical use: asthma (but beta 2 selective agents are preferred)
MOA, effects, and clinical applications of fluticasone
MOA: alters gene expression (corticosteroid)
Effects: reduces mediators of inflammation; powerful prophylaxis of exacerbations
Clinical use: asthma; adjunct in COPD, hay fever (nasal)
Pharmacokinetics and toxicities associated with fluticasone
Aerosol; duration several hours
Toxicity: oropharyngeal candidiasis, vocal cord changes (limited by aerosol application)
Fluticasone has similar MOA, effects, clinical applications, pharmacokinetics, and toxicities to what other agents?
Beclomethasone
Budesonide
Flunisolide
Others…
It’s not in the DSA or lecture, but just in case: MOA, effects, clinical use, pharmacokinetics, and toxicities associated with cromolyn
MOA: alter function of delayed Cl- channels; inhibit inflammatory cell activation
Effect: prevention of bronchospastic response to allergen inhalation
Clinical use: asthma (other routes used for ocular, nasal, and GI allergy) [largely replaced now with inhaled bronchodilators and leukotriene inhibitors]
Pharmacokinetics: aerosol; duration 6-8 hrs
Toxicity: cough
MOA, effects, and clinical use of theophylline
MOA: unknown; PDE inhibition, adenosine receptor antagonist
Effects: bronchodilation, cardiac stim, increased skeletal muscle strength (diaphragm)
Clinical uses: mild to severe persistent asthma, chronic asthma, COPD,
Pharmacokinetics and toxicities associated with theophylline
Oral administration; duration 8-12 hrs but ER preparations often used; metabolized by CYP450 enzymes
Toxicity: nausea, vomiting, tremor, arrhythmias [very high doses can lead to medullary stimulation, convulsions, and death]
Drug similar to theophylline but with better therapeutic ratio
Roflumilast (FYI — not mentioned in DSA)
MOA, effects, and clinical use of montelukast and zafirlukast
MOA: block leukotriene D4 receptors (via CysLT1 receptors)
Effects: block airway response to exercise and antigen challenge
Clinical uses: prophylaxis of asthma, especially in children and ASA-induced asthma
T/F: montelukast and zafirlukast are orally administered, last several hours, and have minimal toxicities associated with them
True
MOA and main toxicity of zileuton
Inhibits lipoxygenase —> reduces synthesis of leukotrienes
Risk of hepatotoxicity
MOA, effects, and clinical use of Omalizumab
MOA: humanized IgE antibody reduces circulating IgE
Effects: reduces frequency of asthma exacerbations
Clinical uses: severe asthma that is inadequately controlled by other agents
Pharmacokinetics and toxicities associated with omalizumab
Parenteral; duration 2-4 weeks
Toxicity: injection site reactions (anaphylaxis extremely rare)
T/F: LABAs like salmeterol and formoterol are given as daily control inhalers, and are ALWAYS combined with an inhaled corticosteroid
True
General “step-up” protocol in asthma tx
- SABA prn
- Add low dose corticosteroid inhaler (alternative: Cromolyn, LTRA, or theophylline)
- Low dose corticosteroid inhaler+LABA or Medium dose corticosteroid inhaler (alt: add LTRA, thoephylline, or zileuton)
- Medium dose corticosteroid inhaler + LABA (alt: medium dose corticosteroid + either LTRA, thoephylline, or zileuton)
- High-dose corticosteroid + LABA and consider omalizumab for pts with allergies
- High-dose corticosteroid + LABA + oral systemic corticosteroid, and conisder omalizumab for pts with allergies
