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Respiratory Medicine Midterm > Pharm of Asthma & COPD - Fitzpatrick > Flashcards

Pharm of Asthma & COPD - Fitzpatrick Flashcards

1
Q

Albuterol, levalbuterol, metaproterenol, terbutaline, salmeterol, formoterol, and indacaterol are all _ agonists

A

Selective adrenergic receptor

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2
Q

Albuterol, levalbuterol, metaproterenol, terbutaline are all _ acting selective Beta 2 adrenergic receptor agonists

A

Shorter

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3
Q

What are the long acting beta agonists?

A
  • salmeterol
  • formoterol
  • indacaterol
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4
Q

Ipratoropium and tiatropium are _ antagonists

A

muscarinic receptor

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5
Q

what bronchodilators are considered methylxanthines?

A

theophylline and rollumilast (COPD)

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6
Q

List all the drugs that are used as bronchodilators for asthma or COPD

A

SABA: albuteorl, levalbuteorl, metaproterenol, terbutaline
LABA: salmeterol, formoterol, indacaterol (COPD)

Muscarinic antagonists: Ipra and Tiatropium

Methylxanthines: Theophylline and roflumilast (COPD)

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7
Q

What drugs are used as inflammatory control in asthma or COPD

A

Leukotriene modulators: LTC4/D4 receptor antagonists: montelukast and zafirlukast

5-lipxoxygenase inhibitor: zileuton

Anti-inflammatory corticosteroids: Budesonide, fluticasone, beclomethasone, flunisalide, mometasone, predinisone

Anti-inflammatory drugs, biological: omalizumab (Anti-IgE antibody)

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8
Q

What class of drugs are used as inhaled agents to relieve acutely/urgently, intermittently as soon as symptoms of asthma attack appear and should be avoided in regularly schedule or overuse.

A

Short-acting beta-2 agonists (SABA). Can be used alone or with a controller

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9
Q

What is the purpose of controller asthma drugs?

A

limit frequent, severe asthma attacks. DOES NOT REPLACE relievers. relievers still needs to be used for asthmatic attack

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10
Q

what classes of asthma drugs are controllers?

A
  1. anti-inflammatory (corticostroids, leukotrienes modifers, anti-IgE ab)
  2. Bronchodilatros (LABA or anti-cholingergic agents)
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11
Q

when should an asthmatic patient start using a controller? what drug type?

A

greater than 2 attacks per week. Start on low dose inhaled corticosteroid (ICS)

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12
Q

_ is both a controller and reliever that has been used in kids and isn’t used much anymore due to it’s very narrow therapeutic window and thus difficult to control.

A

Theophylline

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13
Q

If a pt gets daily asthmatic attacks what asthma drugs should the person be on?

A
  • low-med dose ICS with LABA to prevent attack. still needs to use SABA if they do get an attack
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14
Q

when should a pt start taking high dose ICS with LABA and other class of asthma drugs?

A

Severe persistent with continual attacks and their peak flow have decreased to less than 60%

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15
Q

If an asthmatic attack can be predicted, what class of drugs and when should the pt take it?

A

SABA about 10 mins prior to engaging in the stimulating activity such as running in the cold.

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16
Q

what is the onset and how long does inhaled SABA last?

A

onset 5-15mins and duration is 4-6hrs

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17
Q

_ is an inhaled SABA similar to albuterol, but with racemic mixture of the drug.

A

Levalbuterol

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18
Q

what SABA also comes in oral version?

A

Metaproteronol and terbutaline

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19
Q

A pt with history of asthma attacks has been using more than 1 canister of SABA per month. What should the doctor recommend for this pt?

A

Switch to a controller and use SABA only for attacks

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20
Q

What are the 5 ICS controller drugs?

A
  • beclomethasone
  • triamcinolonoe
  • Flunisolide
  • budesonide
  • fluticasone
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21
Q

Which SABA is most selective?

A
  • Albuterol

- Levabuterol

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22
Q

Which beta drugs are contraindicated in asthma patients?

A

Beta2 antagonist such as Propranolol, nadolol, timolol, pindolol

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23
Q

Pt presents with mild persistent asthma should be prescribed what drug?

A

low dose daily inhaled corticosteroid particularly, budesonide and fluticasone, both of which are of high potency.

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24
Q

Explain how corticosteroid work to control asthma

A

Binds to CSRs–> receptors dimerise –> become TF –> express anti-inflammatory genes and suppress inflammatory genes

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25
Q

What is the onset of action for ICS?

A

Effect takes several hours— maximal effect on FEV1 may take 1 week or more

26
Q

what are the benefits of daily inhaled corticosteroids?

A
  • fewer symptoms
  • fewer severe exacerbations
  • reduced use of SABA bronchodilators
  • improved lung function ( FEV1 >80%)
  • reduced airway inflammation (alveolar lavage shows decline in leukocytes, LTs and cytokines)
27
Q

what are the side effects associated with ICS?

A
  • impair growth in growing kids
  • oral candidiasis (thrush). Standard solution is to rinse mouth with saline water after use)
  • In post menopausal women —> aggravate osteoporosis (mechanism: corticostroids interfere with vit d uptake in GI)
28
Q

what systemic glucocorticoids are use in asthma and for what kind of asthma is it used for? What AE’s are associated with it’s use?

A
  • Oral or IV: predinisone, predisolone, dexamethasone
  • used for severe asthma attack.
  • AE: impaired wound healing, psychosis, osteoporosis, htn, glucoma, growth suppression in kids
29
Q

how is moderate persistent asthma (daily attacks) treated?

A

ICS + LAVA

30
Q

What combo therapy is available for moderate persistent asthma?

A

corticosteroid/ beta2receptor agonist combo includes:

  1. Budesonide/formoterol (symbicort)
  2. Fluticasone/salmeterol (advair)
31
Q

Can LABA be used alone to treat moderate persistent asthma?

A

NO! monotherapy with LABA is associated with increased risk of death in asthmatic pts. Salmeterol or formoterol are not replacement therapy for ICS. they’re beneficial if used with ICS.

32
Q

what serum abnormalities are associated with SABA and LABA?

A

hypokalemia and hyperglycemia. The mechanism for hypokalemia is due to increased Na/Ca ATPase activity at the cellular level

33
Q

which leukotrienes are implicated in asthma to promote inflammation, edema, mucus formation and bronchospasm

A

cysteinyl leukotrienes such as LTC4 and LTD4

34
Q

what LT modifier drugs are available for asthma?

A

Zileuton

Zafirlukast and montelukast

35
Q

what is the MOA of zileuton?

A

inhibits 5-lipoxygenase; inhibits LT biosynthesis.

36
Q

What is the MOA of zakirlukast and montelukast?

A

Antagonists of cysteinyl LT receptors

37
Q

What makes LT modifier great is that they’re use to be used in infants and kids. What is age limit for zileuton, zafirlukast and montelukast?

A

Zileuton: BID approved for kids > 12y

Zakirlukast: BID approved for kids >5yr

Montelukast: QD approved for >1 yr

38
Q

what is the indication for LT receptor antagonists (zakirlukast, montelukast) and LT inhibitor (zileuton)

A
  1. Treats mild persistent asthma and is an ALTERNATIVE to ICS. ICS is first line, and if pts are intolerant to or will not take ICS then use LT receptor antagonists.
  2. Treats moderate persistent asthma as ALTERNATIVE or ADDITIVE to ICS + LABA
39
Q

what AE are associated with Zileuton?

A

Liver tox –> elevated ALT

- Flu like syndrome (chills, fever, fatigue, myalgia)

40
Q

what AE are associated with Zafirlukast and montelukast?

A

Liver tox: discontinue therapy (zafirlukast only)

  • Hypersensitivity (angiedema, rash)
  • Eosinophilia
41
Q

What kind of asthma is leukotriene modifier specially useful for?

A
  1. aspirin-sensitive asthma. These are associated with excessive leukotriene production. Pt tend to benefit when leukotriene modifier are added to inhaled and/or oral glucocorticoids
  2. Exercise-induced asthma: zileuton, montelukast and zafirlukast all prevent exercise-induced bronchospasm to a similar degree
42
Q

What class of drugs are useful for astham driggered by occupational/environmental antigen exposure

A

Anti-IgE monoclonal antibody: omalizumab which is a recombinant humanized monoclonal antibody targeted against IgE.

43
Q

What is the MOA of omalizumab?

A

It is an anti-IgE monoclonal antibody thats attractive to IgE. when IgE is bound to omalizumab, IgE cannot bind to IgE receptor on mast cells and basophils and thus no degranulation.

44
Q

what black box warning are associated with omaliizumab?

A
  • Anaphylaxis. can occur as early as after 1st dose, but also beyond 1 yr after starting tx. These pts need to be observed closely and docs should prepare to treat anaphylaxis
45
Q

when is theophylline, aminophylline used?

A
  1. If asthma is not adequately controlled with conventional doses of ICS + LABA,
  2. if pt adheres to oral drugs, but not an inhaled regimen and montelukast is ineffective
  3. if inhalation is difficult and montelukast is ineffective
  4. As additive acute therapy in ICU for pts failing to respond to other measures (IV corticoids)
46
Q

what is the MOA, and AE of theophylline?

A

MOA: PDE inhibitor (particularly PDE-4)(blockage of adenosine receptor) thus increase cAMP —> sustained bronchodilation
AE: like caffeine. CNS: stimulation, nervousness, restlessness, insomnia, tremors, anorexia/cardiovascular: palpitations, arrhythmias, convulsions

47
Q

What two major differences distinguish COPD from asthma

A
  1. COPD is irreversible

2. COPD is associated with alveolar disruption

48
Q

The immune cells are implicated in COPD vs asthma?

A
  1. COPD: CD8+, neutrophils, macrophages

2. Asthma: CD4+, eosinophils

49
Q

What symptoms are intrinsic to COPD and not seen in asthma?

A
  • Chronic, productive cough

- persistent, progressive breathlessness

50
Q

What symptoms are intrinsic to asthma and not seen in COPD

A
  • Nocturnal breathlessness

- day to day variation in symptoms

51
Q

In COPD, the main way to dilate bronchioles is via _

A

muscarinic antagonism, whereas in asthma its SABA or LABA

52
Q

What are the main drugs used for COPD?

A

muscarinic (M1,2,3) receptor antagonists: Ipratoropium and Tiotropium

53
Q

What is the rationale to use a cholinomimetic such as methacholine in a pt suspected of COPD?

A

It is used as a challenge test to identify a hyper-reactive airway as seen in pts with chronic respiratory disorders

54
Q

what nerve innervates the smooth muscle of airways, and is thus the target for COPD therapy?

A

Vagus nerve

55
Q

what two things are specifically targeted with anti-COPD treatment?

A
  • Pulmonary smooth muscle –> Bronchodilate
  • mucus glands –> decrease mucus discharge
  • Cholinergic valgal tone is exaggerated in COPD so that airway resistance improves to a greater extent than in normal with an anticholinergic drug. anti COPD drugs inhibit cholinergic reflex bronchoconstriction and reduce vagal cholinergic tone– the main reversible component in COPD. these drugs DO NOT halt disease progression, just treats symptoms and prevent exacerbation
56
Q

What are the main differences between Ipra and Triotropium?

A

Ipra: short acting (6hrs) quick onset (15mins), dose 3-4x/day, less selective (works on M1,M2 and M3)

Tio: long acting 24hrs, QD, selective to M1 and M3 only

Both are inhaled, quaternary amine with ONLY peripheral effects.

57
Q

what are the four stages of COPD?

A

I. Intermittent symptoms
II. Persistent symptoms
III. Frequent exacerbations
IV. Resp failure

58
Q

indicate what drugs would be used in each stage of COPD

A

I: Shorting acting Ipratropium, albuterol; or combo
II: long and short acting: Tio + albuterol; Salmeterol or formoterol + ipra, albuterol or combo
III: long acting with 2 mchanism: Tia + salmeterol or fomoterol
IV: Add ICS to long acting - Tia, advair or symbicort

59
Q

Can ipratopium and tiotropium be used in asthma?

A

Yes but not as effective as SABA or LABA. It can be used ONLY for who who are intolerant or do not respond to SABA or LABA.

60
Q

What is the MOA and indication for Roflumilast?

A

Roflimulast is a PDE4 inhibitor that is approved to reduce the risk of COPD exacerbations in pts with hx of frequent COPD exacerbations (at least two/yr or one requiring hospitalization. In practice, roflumilast use is limited to COPD pts with continued exacerbation despite maximally tolerated inhaled therapies

61
Q

what drugs should be avoided in COPD pts?

A
  • -Leukotriene modifiers and mast cell stabilizer.

- - Shronic treatment with systemic glucocorticosteroids –> risk of infection

Respiratory Medicine Midterm (7 decks)

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