Asthma and COPD Pharmacology (Fitz) Flashcards

1
Q

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

A

Longer acting, selective B2 agonist

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2
Q

Ipratropium and tiatropium are what type of drugs?

A

Muscarinic receptor antagonists

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3
Q

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

A

Methylxanthines

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4
Q

Montelukast and Zafirlukast are what type of drugs?

A

LTC4/D4 receptor antagonists, Leukotrience modulators

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5
Q

Zileuton is what type of drug/

A

5-lipoxygenase inhibitor, Leukotriene mediator

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6
Q

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

A

Corticosteroids, anti-inflamm drugs

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7
Q

Omalizumab is what type of drug?

A

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

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8
Q

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

A

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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9
Q

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

A

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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10
Q

What is the MOA of a reliever?

A

Short acting B2 adrenergic receptor agonist (SABA)

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11
Q

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

A

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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12
Q

List inhaled SABAs:

A

Albuterol (most widely used)
Levalbuterol
Metaproterenol
Terbutaline

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13
Q

List inhaled LABA’s:

A

Salmeterol
Formoterol

These are CONTROLLERS and not relievers

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14
Q

Inhaled B2 SABAs act preferentially on ___

A

Pulmonary smooth m.

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15
Q

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

A

Beta blockers (b2 receptor antagonists)

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16
Q

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

A

Step 1: inhaled SABA prn

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

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17
Q

List some inhaled corticosteroids:

A
Budesonide (high potency)
Fluticasone (high potency)
Beclamethasone
Mometasone
Flunisolide
Prednisone (systemic)
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18
Q

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

A

Decline

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19
Q

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

A

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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20
Q

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

A

Prednisone
Prednisolone
Dexamethasone

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

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21
Q

What is preferred pharmacological therapy for moderate persistent asthma?

A

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

SABA prn to relieve attacks

22
Q

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

A

Budesonide/formoterol (Symbicort)

Fluticasone/salmeterol (Advair)

23
Q

List some LABA agonists:

A

Salmeterol

Formoterol

24
Q

What is a generalized caution associated with LABA monotherapy?

A

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

25
Q

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

A

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

26
Q

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

A

Zileuton

27
Q

These LT modifiers antagonize cysteinyl LT receptors:

A

Zafirlukast

Montelukast

28
Q

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

A

Zafirlukast-2x daily approved for children > 5 yrs

Montelukast-1x daily approved for children > 1 yr

29
Q

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

A

2x daily approved for children > 12 yrs

30
Q

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

A

LT receptor antagonists

31
Q

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

A

LT receptor antagonists

32
Q

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

A

Liver toxicity –> elevation in ALT

Flu-like syndrome

33
Q

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

A

Liver toxicity –> discontinue therapy (zafirlukast only)

Hypersensitivity –> angioedema, rash

Eosinophilia

34
Q

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

A

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

35
Q

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

A

Aspirin-sensitive asthma

Exercise-induced asthma

36
Q

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

A

Omalizumab

37
Q

What is the black box warning of Omalizumab?

A

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

38
Q

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

A
  • 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
39
Q

What is the cellular actions of theophylline?

A

Inhibits PDE-inhibits breakdown of cAMP, blockade of adenosine receptors

Has a narrow therapeutic index

40
Q

What are some adverse effects of theophylline?

A

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

41
Q

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

A

Ipratropium and tiotropium

42
Q

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

A

Ipratropium and tiatropium cause bronchodilation

Methacholine causes bronchoconstriction

43
Q

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)

A

Ipratropium

44
Q

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

A

Tiotropium

45
Q

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

A

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

46
Q

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

A

Short acting-Ipratropium, albuterol; or combo

47
Q

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

A

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

48
Q

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

A

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

49
Q

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

A

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

50
Q

___ 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

A

Roflumilast

51
Q

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

A

LT modifiers and mast cell stabilizers

Chronic tx with systemic glucocorticoids should be avoided because of an unfavorable benefit-to-risk ratio

52
Q

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

A

Shorter acting, selective B2 agonists