Drugs Used in COPD and Asthma Flashcards by Bridget Tesher

List 6 short-acting beta agonist bronchodilators

Albuterol
Levalbuterol
Metaproterenol
Pirbuterol
Epinephrine
Terbutaline

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Short-acting antimuscarinic bronchodilator

Ipratropium

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Combination short-acting bronchodilator

Albuterol/ipratropium

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List 4 Long-acting beta-adrenergic bronchodilators

Formoterol
Indacaterol
Olodaterol
Salmeterol

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2 long acting antimuscarinic bronchodilators

Aclidinium

Tiotropium

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What are 7 aerosol corticosteroids used in tx of asthma?

Beclomethasone
Mometasone
Fluticasone
Triamcinolone
Budesonide
Ciclesonide
Flunisolide

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3 examples of combination LABA+Corticosteroid inhalers used in asthma

Formoterol/budesonide
Formoterol/mometasone
Salmeterol/fluticasone

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Leukotriene inhibitors used in tx of asthma

Montelukast
Zafirlukast
Zileuton

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Methylxanthines used in tx of asthma

Dyphylline

Theophylline

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Monoclonal Ab used in tx of asthma

Omalizumab

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MOA, effects, and clinical applications of Albuterol

MOA: selective beta2 agonist

Effects: prompt, efficacious bronchodilation

Clinical applications: asthma, COPD

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Drug of choice in acute asthmatic bronchospasm

Albuterol

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Pharmacokinetics and toxicities of albuterol

Aerosol inhalation; duration several hours, also available via nebulizer and parenteral use

Toxicity: tremor, tachycardia; overdose causes arrhythmia

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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)

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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

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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

1. SABA prn 2. Add low dose corticosteroid inhaler (alternative: Cromolyn, LTRA, or theophylline) 3. Low dose corticosteroid inhaler+LABA or Medium dose corticosteroid inhaler (alt: add LTRA, thoephylline, or zileuton) 4. Medium dose corticosteroid inhaler + LABA (alt: medium dose corticosteroid + either LTRA, thoephylline, or zileuton) 5. High-dose corticosteroid + LABA and consider omalizumab for pts with allergies 6. High-dose corticosteroid + LABA + oral systemic corticosteroid, and conisder omalizumab for pts with allergies