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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
Systemic glucocorticoids used in asthma
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
Medium dose ICS plus LABA plus SABA prn for moderate persistent asthma (Step 3)
daily attack with FEV1 60-80% Corticosteroid and B2 receptor agonists Budesonide/formoterol Fluticasone/salmeterol
27
Effects of beta adrenergic receptor agonists: SABA and LABA
Decreased blood potassium levels increases blood sugar levels
28
LABA agonists
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
Salmeterol black box warning
increased risk of asthma related death, reserve for patients who are not controlled on low-to-medium dose corticosteroid + rescue inhaler
30
Leukotrienes
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
Zileuton
LT modifier inhibits 5-lipoxygenase inhibits LT biosynthesis 2x daily approved for children older than 12
32
Zafirlukast
LT modifier Antagonist of cysteinyl LT receptors 2x daily, approved for children older than 5
33
Montelukast
LT modifier antagonist of cysteinyl LT receptors 1 x daily, approved for children older than 1
34
LT receptor antagonists in mild persistent asthma (step 2)
alternative to ICS
35
LT receptor antagonists/inhibitor in moderate persistent asthma (step3)
alternative or additive to ICS + LABA
36
Adverse effects of Zileuton
Liver toxicity - elevated ALT Flu like symptoms - chills, fever, fatigue, myalgias
37
Adverse effects of zafirlukast and montelukast
Liver toxicity - discontinue therapy (Zafirlukast only) Hypersensitivity - angioedema, rash, eosinophilia
38
Clinical indication for Leukotriene modifiers
first line for patient who will not take or cannot tolerate inhaled corticosteroids
39
Aspirin sensitive asthma
excessive leukotriene production tend to benefit from leukotrienes modifiers are added to inhaled and/or oral glucocorticoids
40
Exercise induced asthma
zileuton, montelukast, zafirlukast all prevent exercise-induced bronchospasm
41
Omalizumab
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
Omalizumab boxed warning
anaphylaxis as early as 1st dose also beyond 1 year after beginning treatment
43
Theophylline in asthma
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
Cellular actions of theophylline
inhibition of PDE4 thus inhibiting breakdown of cAMP Blockade of adenosine receptors
45
Adverse effects of theophylline
CNS stimulation, nervousness, restlessness, insomnia, tremors, anorexia Cardiovascular: palpitations, arrhythmias, convulsions
46
COPD vs asthma
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
Ipatropium and tiatropium MOA
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
Vagus nerve
innervates airways, releases ACh causing pulmonary sm. m. constriction and increase mucus discharge
49
Ipratropium
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
Tiotropium
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
Gold stages for COPD
I - intermittent symptoms II - persistent symptoms III - frequent exacerbations IV - respiratory failure
52
Stage I bronchodilators for COPD
Short acting | Ipratropium, albuterol or combination
53
Stage II bronchodilators for COPD
Long acting and short acting Tiotropium and albuterol Salmeterol or formoterol + ipratropium, albuterol, or combination
54
Stage III bronchodilators for COPD
Long acting - 2 mechanisms Tiatropium + salmeterol or fomoterol
55
Stage IV bronchodilators for COPD
Add inhaled corticosteroid to long acting Tiatropium Budesonid/formoterol Fluticasone/salmeterol
56
Roflumilast
PDE4 inhibitor reduce risk of COPD exacerbation in patients with frequent exacerations
57
Leukotriene modifiers in COPD
No role of leukotriene modifiers and mast cell stabilizers in management of COPD
58
Glucocorticosteroids in COPD
chronic treatment with systemic glucocorticosteroids avoided because of unfavorable benefit to risk ratio

Respiratory Medicine Midterm (11 decks)

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