Asthma and COPD Pharmacology (Fitz) Flashcards by Kelley Perry

Salmeterol, formoterol, and indacaterol (COPD) are what type of bronchodilator?

Longer acting, selective B2 agonist

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Ipratropium and tiatropium are what type of drugs?

Muscarinic receptor antagonists

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Theophylline and Roflumilast (COPD) are what type of drugs?

Methylxanthines

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Montelukast and Zafirlukast are what type of drugs?

LTC4/D4 receptor antagonists, Leukotrience modulators

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Zileuton is what type of drug/

5-lipoxygenase inhibitor, Leukotriene mediator

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Budesonide, fluticasone, beclomethasone, flunisolide, mometason, and prednisone are what type of drugs?

Corticosteroids, anti-inflamm drugs

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Omalizumab is what type of drug?

Biological (Anti-IgE Ab), anti-inflamm drug

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This type of asthma drug has a therapeutic purpose of relieving symptoms rapidly and rescue from an asthmatic attack

Reliever-Inhaled agents

Used: acutely/urgently/intermittently as soon as symptoms appear. Avoid regularly scheduled, or overuse of SABAs. Use prn

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This type of asthma drugs therapeutic purpose is to limit frequent, severe asthma attacks

Controllers-Inahled and oral agents

These do not replace relievers. The relievers must stil be used during an asthmatic attack

Used: chronically/daily during asymptomatic periods

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What is the MOA of a reliever?

Short acting B2 adrenergic receptor agonist (SABA)

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What is the general pharmacological agent used for mild intermittent asthma?

Inhaled SABA prn

Take as needed for relief of symptoms. Onset 5-15 mins, duration 4-6 hrs

If you can predict trigger of symptoms, use SABA ~10 mins prior to exposure

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List inhaled SABAs:

Albuterol (most widely used)
Levalbuterol
Metaproterenol
Terbutaline

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List inhaled LABA’s:

Salmeterol
Formoterol

These are CONTROLLERS and not relievers

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Inhaled B2 SABAs act preferentially on ___

Pulmonary smooth m.

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Propanolol, nadolol, timolol, pindolol are all contraindicated in asthma because they are this type of drug:

Beta blockers (b2 receptor antagonists)

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What is the recommended pharmacologic therapy for a pt with mild persistent asthma?

Step 1: inhaled SABA prn

Step 2: Add low dose daily inhaled corticosteroid (use SABA prn to relieve any attacks

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List some inhaled corticosteroids:

Budesonide (high potency)
Fluticasone (high potency)
Beclamethasone
Mometasone
Flunisolide
Prednisone (systemic)

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Daily inhaled corticosteroid benefits will demonstrate what effect on leukocytes, LT’s, cytokines, and NO exhalation on alveolar lavage?

Decline

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What are some concerns regarding side effects of inhaled corticosteroids and children? Adults? Post menopausal women?

May impair growth in children

In adults, may cause oral candidiasis (thrush)

In post-menopausal women, systemic dosing of corticosteroids for severe asthma can aggravate osteoporosis

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What are some oral, IV systemic glucocorticoids used in asthma?

Prednisone
Prednisolone
Dexamethasone

Systemic use associated with major adverse effects: impaired wound healing, psychosis, osteoporosis, HTN, glaucoma

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What is preferred pharmacological therapy for moderate persistent asthma?

Combo therapy using inhaled corticosteroids PLUS long-acting B2 adrenergic receptor agonist (LABA bronchodilator)

SABA prn to relieve attacks

What are some inhaled corticosteroid + LABA products for moderate persistent and severe persistent asthma?

Budesonide/formoterol (Symbicort)

Fluticasone/salmeterol (Advair)

List some LABA agonists:

Salmeterol

Formoterol

What is a generalized caution associated with LABA monotherapy?

Monotherapy with LABA alone is associated with increased risk of death in asthmatic pts

What is the black box warning on salmeterol (serevent and advair)?

May increase the risk of asthma related death (more pts who used salmeterol died from asthma problems)

This LT modifier inhibits 5-lipoxygenase; inhibits LT biosynthesis.

Zileuton

These LT modifiers antagonize cysteinyl LT receptors:

Zafirlukast | Montelukast

How many times per day and what age groups are associated with Zafirlukast and Montelukast?

Zafirlukast-2x daily approved for children > 5 yrs Montelukast-1x daily approved for children > 1 yr

How many times per day and what age group is associated with Zileuton?

2x daily approved for children > 12 yrs

This drug type can be used as an alternative to ICS in mild persistent asthma:

LT receptor antagonists

This drug type can be used as an alternative or additive to ICS + LABA in moderate persistent asthma:

LT receptor antagonists

What are some adverse effects (<2% incidence) of Zileuton?

Liver toxicity --> elevation in ALT Flu-like syndrome

What are some adverse effects (<2% incidence) of Zafirlukast and Montelukast?

Liver toxicity --> discontinue therapy (zafirlukast only) Hypersensitivity --> angioedema, rash Eosinophilia

LT modifiers are a reasonable first line controller agent for these types of pts:

Pts who either will not take or cannot tolerate inhaled corticosteroids Studies show better adherence to 1x daily montelukast vs ICS in children and adults

What are some special uses for LT modifiers (asthma-related)?

Aspirin-sensitive asthma Exercise-induced asthma

___ is a recombinant humanize monoclonal Ab targeted against IgE. It is used to blunt allergic rxn only when environmental or occupational allergens provoke asthma

Omalizumab

What is the black box warning of Omalizumab?

Anaphylaxis presenting as bronchospasm, hypotension, syncope, urticaria, angioedema of throat or tongue, has been reported to occur after administration of Xolair

What are some conditions in which Theophylline can be used to tx asthma?

- if asthma is not adequately controlled with conventional doses of ICS + LABA - if pt adheres to oral drug, but not an inhaled regimen and Montelukast is ineffective - if inhalation is difficult (e.g. Toddlers) and Montelukast is ineffective - as additive acute therapy in the ICU for pts failing to respond to other measures

What is the cellular actions of theophylline?

Inhibits PDE-inhibits breakdown of cAMP, blockade of adenosine receptors Has a narrow therapeutic index

What are some adverse effects of theophylline?

Like caffeine. CNS: stimulation, nervousness, restlessness, insomnia, tremors, anorexia. Cardiovascular: palpitations, arrhythmias, convulsions

What are some anticholinergic bronchodilators of the M receptor antagonist variety used in COPD?

Ipratropium and tiotropium

Ipratropium and tiatropium have what effect on bronchial tone? What about methacholine?

Ipratropium and tiatropium cause bronchodilation Methacholine causes bronchoconstriction

This M antagonist for COPD is short acting (6 hrs), quick onset (15 mins), dosed 3-4x/day and is less selective (M1, M2, and M3 antagonist)

Ipratropium

This M antagonist for COPD is long-acting (24 hrs), onset of 30 mins, dosed at 1x/daily, and more selective (M1 and M3 receptors)q

Tiotropium

What is the main use of ipratropium and tiotropium in asthmatic pts?

Pts who do not tolerate or do not respond to SABAs or LABAs

What meds are used for Gold Stage I for intermittent COPD symptoms?

Short acting-Ipratropium, albuterol; or combo

What meds are used for Gold Stage II for persistent COPD symptoms?

Long acting & short acting--> Tiotropium + albuterol; Salmeterol or formeterol + Ipratropium, albuterol or combo

What meds are used for GOld Stage III for frequent COPD exacerbations?

Long acting, 2 mechanisms --> tiatropium + salmeterol or fomoterol

What meds are used for Gold Stage IV for respiratory failure in COPD?

Add inhaled corticosteroids to long acting --> tiatropium; budesonid/formoterol; fluticasone/salmeterol

___ is an oral, PDE-4 inhibitor that is approved to reduce the risk of COPD exacerbations in pts with a hx of frequent COPD exacerbations. It has generally been limited to COPD pts with continued exacerbations despite maximally tolerated inhaled therapies

Roflumilast

These drug type have no role in management of COPD (but do for asthma):

LT modifiers and mast cell stabilizers Chronic tx with systemic glucocorticoids should be avoided because of an unfavorable benefit-to-risk ratio

Albuterol, levalbuterol, metaproterenol, and terbutaline are what type of bronchodilator?

Shorter acting, selective B2 agonists