L24 drugs used in COPD Flashcards

1
Q

COPD

A

chronic obstructive pulmonary disease

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2
Q

COPD affects more than ____ of the US adult population

A

10%

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3
Q

COPD is the _____ leading cause of death in US in 2018

A

4th

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4
Q

_____- of COPD pateints are smokers

A

85%

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5
Q

COPD irreversible airflow obstruction due to

A

emphysema
chronic bronchitis

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6
Q

COPD symptoms

A

-chronic cough
-sputum
-dyspnea
-barrel chest

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7
Q

emphysema

A

-permanent enlargement of bronchioles and alveoli due to destruction of their walls
-dyspnea due to insufficient gas exchange
-cigarette smoking is the major cause
-frequently asymptomatic until the later stage of life

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8
Q

patholphysiology of emphysema

A

tissue damage by proteases
oxidative injury by reactive oxygen species (ROS)

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9
Q

tissue damage by proteases

A

-irritants in cigarette smoke cause inflammation in alveoli.
-Neutrophils and macrophages accumulate.
-Activated neutrophils and macrophages release proteases (ex. neutrophil
elastase), resulting tissue damage.

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10
Q

oxidative injury by reactive oxygen species (ROS)

A

-ROS in cigarette smoke deplete antioxidants in the lungs (ex. superoxide
dismutase, glutathione).
-ROS inactivate ⍺1-antitrypsin, which normally suppresses the protease activities.
-Activated neutrophils also release ROS

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11
Q

alpha 1-antitrypsin

A

-Protease inhibitor produced in the liver (53 kDa)
-Inhibits neutrophil elastase.
-Limits lung tissue damage

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12
Q

alpha 1-antitrypsin deficiency

A

-Rare genetic disorder leading to insufficient ⍺1-Antitrypsin activity
-increased neutrophil migration
-Increased lung damage via inflammation and protease activity

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13
Q

chronic bronchitis

A

-chronic inflammation in bronchial tubes
(mucus hypersecretion and fibrosis and narrowing of airways)
-frequently coexists with emphysema
-cigarette smoking is the major cause

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13
Q

symptoms of chronic bronchitits

A

-producing cough
-wheezing
-shortness of breathe/ chest pain

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14
Q

pathophysiology of chronic bronchitis

A

-Initiated by the exposure to irritants (cigarette smoke or other air pollutants)
 Hypersecretion of the bronchial mucous glands.
 Hypertrophy of mucous glands
 Metaplastic formation of mucin-secreting goblet cells
 Inflammation with infiltration of CD8+ T cells, macrophages, and neutrophils (no involvement of eosinophils)
-Microbial infection may paly a secondary role in maintaining inflammation and
exacerbating symptoms.

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15
Q

tissue remodeling in COPD

A

-Fibrosis of small airways
-Hyperinflation of lungs:
 Alveolar enlargement
 Alveolar wall destruction
-Mucus hypersecretion

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16
Q

asthma vs COPD in site

A

asthma; proximal airways
COPD; peripheral airways

17
Q

asthma vs COPD in onset

A

asthma; childhood
COPD; late adulthood

18
Q

asthma vs COPD in symptoms

A

asthma; episodic attack
COPD; progressive deterioration of pulmonary function

19
Q

cells affects in asthma vs COPD

A

asthma: mast cells, eosinophils, CD4+ T cells
COPD; neutrophils, macrophages, CD8+ T cells

20
Q

key mediators in asthma vs COPD

A

asthma: IL-4, IL-5, IL-13
COPD; IL-8, TNF-alpha, IL-1b, IL-6

21
Q

nonpharmacological therapy treatment of COPD

A

-Smoking cessation
-Exercise
-Immunization
-Long-term oxygen therapy

22
Q

pharmacological therapy in treatment of COPD

A

-Bronchodilators
 β2 selective agonists (short-acting, long-acting, and ultra-long-acting)
-Antimuscarinic agents (short-acting and long-acting)
-Methylxanthines
-Corticosteroids for patients with exacerbations
-alpha 1-antitrypsin replacement therapy (rare)

23
Q

beta 2 selective agonist: short-acting (SABA)

A

-Albuterol, levalbuterol
-Repid onset, but the response is less than seen in asthma.

24
Q

beta 2 selective agonist long acting (LABA)

A

-Salmetrol, formoterol
-Every 12 hours
-Not for acute relief of symptoms

25
Q

beta 2 selective agonist: ultra long acting (Ultra LABA)

A

-Indacaterol, olodaterol, vilanterol, bambuterol
-Once a day
-Can be used as monotherapy for COPD (not for asthma).
-Combination
 Fluticasone furoate/vilanterol

26
Q

antimuscarinic agents: short acting (SAMA)

A

-ipratropium
-As effective as albuterol in patients with COPD

27
Q

antimuscarinic agents: long acting (LAMA)

A

-Tiotropium, aclidinium, umeclidinium
-Once a day
-Approved for maintenance therapy of COPD.
-Quaternary amine salt like ipratropium
-Combination
 Fluticasone furoate/umeclidinium
bromide/vilanterol

28
Q

mathylxantines

A

-Once considered first-line therapy for COPD.
-Mostly replaced by LABA and antimuscarinics.
-Theophylline

29
Q

methylxantines: theoohylline

A

 Used in patients who are intolerant to or cannot use inhaled bronchodilators.
 Bronchodilation and anti-inflammatory action
 Systemic administration may be beneficial on peripheral airways

30
Q

roflumilast

A

 Phosphodiesterase-4 (PDE4) inhibitor
 Increases the intracellular cAMP concentration as methylxanthines.
 Suppresses the release of cytokines and chemokines
 Approved for COPD, but not for asthma

31
Q

corticosteroids uses in COPD

A

-Short-term systemic use for acute exacerbations
-inhalation therapy for chronic stable COPD

32
Q

mechanisms of cortiosteroids

A

 Decrease mucus release by reducing capillary permeability
 Suppress protease release from immune cells
 Suppress prostaglandin production

33
Q

alpha 1-antitrypsin replacement therapy: products

A

-Derived from donated blood
-Prolastin® , Aralast®, Zemaira®

34
Q

alpha 1- antitrypsin replacement therapy

A

-Reduces lung tissue loss and destruction in patients with severe ⍺1-Antitrypsin deficiency.
-Expensive (>$50k a year)

35
Q

short acting beta 2 selective agonist (SABA)

A

-Albuterol
-Levalbuterol (Xopenex®)

36
Q

long acting beta 2 selective agonist (LABA)

A

-Salmetrol (Serevent ®)
-Formoterol

36
Q

ultra long acting beta 2 selective agonists

A

-Indacaterol (Arcapta® )
-Olodaterol (Strieverdi®)
-Vilanterol (
-Bambuterol (Bambec ®, Oxeol ®)

36
Q

methylxanthine

A

theophylline

36
Q

antimuscarinic

A

-Ipratropium (Atrovent ®)
-Tiotropium (Spiriva ®)
-Aclidinium (Tudorza ®, Pressair®)
-Umeclidinium (Incruse Ellipta ®)

36
Q

PDE4 inhibitor

A

Roflumilast (Daliresp ®)

36
Q

combinations

A

-Fluticasone furoate/vilanterol (Breo
Ellipta ®)
-Fluticasone furoate/umeclidinium
bromide/vilanterol (Trelegy Ellipta ®)