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Respiratory Medicine Midterm > Pharm of Asthma and COPD - Fitzy lecture > Flashcards

Pharm of Asthma and COPD - Fitzy lecture Flashcards

1
Q

Bronchodilators: Shorter acting selective beta-2 adrenergic receptor agonists

A

Albuterol
Levalbuterol
Metaproterenol
Terbutaline

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2
Q

Bronchodilators: Longer acting selective beta-2 adrenergic receptor agonists

A

Salmeterol
Formoterol
Indacaterol (COPD)

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3
Q

Bronchodilators: Muscarinic receptor antagonists

A

Ipratropium

Tiatropium

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4
Q

Bronchodilators: Methylxanthines

A

Theophylline

Roflumilast (COPD)

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5
Q

Leukotriene modulators - LTC4/D4 receptor antagonists

A

Montelukast

Zafirlukast

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6
Q

Leukotriene Modulators - 5-lipoxygenase inhibitor

A

Zileuton

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7
Q

Anti-inflammatory drugs: corticosteroids

A 
Budesonide
Fluticasone
Beclomethasone
Flunisolide
Mometasone
Prednisone (systemic)
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8
Q

Anti-inflammatory drugs: biologicals

A

Omalizumab (anti- IgE antibody)

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9
Q

Asthma controller use

A

Inhaled and oral agents: used chonically/daily during asymptomatic periods

Limit frequent, severe asthma attacks. Do not replace relievers which must till be used during asthmatic attack

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10
Q

Asthma Relievers

A

Bronchodilators - short acting beta-2 adrenergic receptor agonists, used alone or with controllers

Theophylline

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11
Q

Asthma Controllers

A

Anti-inflammatory - corticosteroids, leukotriene modifiers, anti-IgE antibody

+/- bronchodilators - long-acting beta-2 agonist, anti-cholinergic agent

theophylline

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12
Q

Mild intermittent asthma

A

Attacks: less than 2 per week
Peak Flow: near normal
Long-term control: n/a
Relief: SABA

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13
Q

Mild persistent asthma

A

Attacks: >2/wk
Peak Flow: near normal
Long-term control: Low dose ICS
Relief: SABA

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14
Q

Moderate persistent asthma

A

Attacks: daily
Peak Flow: 60-80% of predicted
Long-term control: Low med dose ICS with LABA
Relief: SABA

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15
Q

Severe persistent asthma

A

Attacks: continual
Peak Flow: less than 60% of predicted
Long-term control: high dose ICS with LABA + others
Relief: SABA

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16
Q

Inhaled SABA prn for mild intermittent asthma (Step 1)

A

Take prn for relief of symptoms.

Onset 5-15 min, lasting 4-6 hr

Use 10 minutes prior to predicted trigger (cold, exercise) to prevent onset of symptoms

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17
Q

SABA (inhaled)

A 
Relievers:
Albuterol
Levalbuterol
Metaproterenol
Terbutaline
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18
Q

LABA (inhaled)

A

Salmeterol
Formoterol

Controllers, not relievers

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19
Q

Location of action of inhaled B2 agonists

A

B2 selective adrenergic receptor agonists preferentially act on pulmonary smooth muscle, compared to cardiac smooth muscle

Relax smooth muscle and dilate airways

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20
Q

B2 receptor antagonists

A

harmful on airway, negate any beneficial effects on the heart in asthma patients with heart conditions

Propranolol
Nadolol
Timolol
Pindolol

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21
Q

Low dose daily inhaled corticosteroid in mild persistent asthma (Step 2)

A 
Budesonide - high potency
Fluticasone - high potency
Beclamethasone
Mometasone
Flunisolide
Prednisone (systemic, non inhaled)
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22
Q

Action of corticosteroids

A

CSR corticoid receptor when occupied –> dimerization, nuclear transport and gene transcription

Suppress inflammatory genes
Express anti-inflammatory genes
ICS not quick acting

Maximal effect on FEV1 may take 1 week or more

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23
Q

Benefits of daily inhaled corticosteroids

A

Fewer symptoms
fewer severe exacerbations
reduced use of SABA bronchodilators
Improved lung function (improve FEV1 >80% predicted)
Reduced airway inflammation (decline in leukocytes, LTs, cytokines, NO exhalation will decline

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24
Q

Complications of corticosteroids

A

Impair growth in children

oral candidiasis in adults due to localized mucosal immunosuppression

Post-menopausal systemic dosing can aggravate osteoporosis, overuse can confer risk of osteoporosis

25
Q

Systemic glucocorticoids used in asthma

A

Oral or IV

Prednisone
Prednisolone
Dexamethasone

Taper off after control of severe asthma attacks established

associated with impaired wound healing, psychosis, osteoporosis, HTN, glaucoma

26
Q

Medium dose ICS plus LABA plus SABA prn for moderate persistent asthma (Step 3)

A

daily attack with FEV1 60-80%

Corticosteroid and B2 receptor agonists

Budesonide/formoterol
Fluticasone/salmeterol

27
Q

Effects of beta adrenergic receptor agonists: SABA and LABA

A

Decreased blood potassium levels

increases blood sugar levels

28
Q

LABA agonists

A

Salmeterol, formoterol

not for immediate leave or substitution for anti-inflammatory drugs

beneficial with ICS

Don’t use alone as associated with increased risk of death in asthmatic patients

29
Q

Salmeterol black box warning

A

increased risk of asthma related death, reserve for patients who are not controlled on low-to-medium dose corticosteroid + rescue inhaler

30
Q

Leukotrienes

A

lipid mediates of inflammation

LTC4 and LTD4 promote inflammation, edema, mucus formation, bronchospasm

Phospholipase A2 converts phospholipids to arachidonic acid

5-lipoxygenase converts AA to LTA4.

Tissue specific isomerases convert to LTB4 and LTC4, LTD4, LTE4

31
Q

Zileuton

A

LT modifier

inhibits 5-lipoxygenase
inhibits LT biosynthesis

2x daily
approved for children older than 12

32
Q

Zafirlukast

A

LT modifier

Antagonist of cysteinyl LT receptors

2x daily, approved for children older than 5

33
Q

Montelukast

A

LT modifier

antagonist of cysteinyl LT receptors

1 x daily, approved for children older than 1

34
Q

LT receptor antagonists in mild persistent asthma (step 2)

A

alternative to ICS

35
Q

LT receptor antagonists/inhibitor in moderate persistent asthma (step3)

A

alternative or additive to ICS + LABA

36
Q

Adverse effects of Zileuton

A

Liver toxicity - elevated ALT

Flu like symptoms - chills, fever, fatigue, myalgias

37
Q

Adverse effects of zafirlukast and montelukast

A

Liver toxicity - discontinue therapy (Zafirlukast only)

Hypersensitivity - angioedema, rash, eosinophilia

38
Q

Clinical indication for Leukotriene modifiers

A

first line for patient who will not take or cannot tolerate inhaled corticosteroids

39
Q

Aspirin sensitive asthma

A

excessive leukotriene production

tend to benefit from leukotrienes modifiers are added to inhaled and/or oral glucocorticoids

40
Q

Exercise induced asthma

A

zileuton, montelukast, zafirlukast all prevent exercise-induced bronchospasm

41
Q

Omalizumab

A

recombinant humanized monoclonal antibody targeted against IgE

IgE bound to omalizumab cannot bind to IgE receptor on mast cells and basophils

Used to blunt allergic reaction only when environmental or occupational allergens provoke asthma

42
Q

Omalizumab boxed warning

A

anaphylaxis as early as 1st dose also beyond 1 year after beginning treatment

43
Q

Theophylline in asthma

A

oral

If asthma not adequately controlled with conventional doses of ICS + LABA

If pt adheres to oral drug, but not inhaled and montelukast is ineffective

Inhalation difficult (toddlers) and montelukast ineffective

Additive in ICU patients failing to respond to IV corticoids, etc

44
Q

Cellular actions of theophylline

A

inhibition of PDE4 thus inhibiting breakdown of cAMP

Blockade of adenosine receptors

45
Q

Adverse effects of theophylline

A

CNS stimulation, nervousness, restlessness, insomnia, tremors, anorexia

Cardiovascular: palpitations, arrhythmias, convulsions

46
Q

COPD vs asthma

A

alveolar disruption and much worse fibrosis in COPD

Smokers - COPD
younger than 35 - asthma
chronic productive cough - COPD
Breathlessness - persistent and progressive = COPD, variable = asthma

Nocturnal breathlessness - asthma

Diurnal or day-to-day variation of symptoms - asthma

47
Q

Ipatropium and tiatropium MOA

A

inhibit muscarinic M1-M3 receptors

relieve parasympathetic tone, relieving bronchoconstriction, decrease mucus discharge

foundation for treatment of COPD

Can be used in asthma, but less effective than B2 adrenergic receptor agonists (SABA or LABA)

48
Q

Vagus nerve

A

innervates airways, releases ACh causing pulmonary sm. m. constriction and increase mucus discharge

49
Q

Ipratropium

A

inhaled
short acting - 6 hrs, dose 3-4 x/day
quick onset - 15 min

Less selective M1-M3 antagonist

Quaternary amine +
peripheral effects
NOT CNS due to charge

50
Q

Tiotropium

A

Inhaled
Long acting, once per day dose
Onset 30 min

More selective, M1 and M3

Quaternary amine +
Peripheral effects
NOT CNS due to charge

51
Q

Gold stages for COPD

A

I - intermittent symptoms
II - persistent symptoms
III - frequent exacerbations
IV - respiratory failure

52
Q

Stage I bronchodilators for COPD

A

Short acting

Ipratropium, albuterol or combination

53
Q

Stage II bronchodilators for COPD

A

Long acting and short acting

Tiotropium and albuterol

Salmeterol or formoterol + ipratropium, albuterol, or combination

54
Q

Stage III bronchodilators for COPD

A

Long acting - 2 mechanisms

Tiatropium + salmeterol or fomoterol

55
Q

Stage IV bronchodilators for COPD

A

Add inhaled corticosteroid to long acting

Tiatropium
Budesonid/formoterol
Fluticasone/salmeterol

56
Q

Roflumilast

A

PDE4 inhibitor

reduce risk of COPD exacerbation in patients with frequent exacerations

57
Q

Leukotriene modifiers in COPD

A

No role of leukotriene modifiers and mast cell stabilizers in management of COPD

58
Q

Glucocorticosteroids in COPD

A

chronic treatment with systemic glucocorticosteroids avoided because of unfavorable benefit to risk ratio

Respiratory Medicine Midterm (11 decks)

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