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Pharmacology Test 2 > Asthma & COPD > Flashcards

Asthma & COPD Flashcards

1
Q

What are the therapeutic targets?

A
  • smooth muscle dysfunction

- airway inflammation

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2
Q

2 broad categories for the treatment of asthma

A
  • bronchodilators

- anti-inflammatory agents

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3
Q

Bronchodilators

A

used to relieve acute symptoms and for control therapy; asthma attacks

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4
Q

Anti-inflammatory Agents

A

used to control or prevent symptoms

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5
Q

B2AR Agonists

2 kinds

A

SABAs: short-acting B2-selective agonists
LABAs: long-acting B2-selective agonists

Mainly treats SMOOTH MUSCLE DYSFUNCTION

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6
Q

Bronchodilators

3 types

A
  • epinephrine
  • ephedrine
  • isoproterenol
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7
Q

Epinephrine

A
  • bronchodilator

- non-selective adrenergic agonist

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8
Q

Ephedrine

A
  • bronchodilator
  • non-selective adrenergic agonist
  • releases NE
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9
Q

Isoproterenol

A
  • bronchodilator
  • non-selective beta agonist
  • not used as much anymore
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10
Q

SABAs

Short-Acting B2-Selective Agonists

A
  • little rationale for choice among SABAs
  • maximal bronchodilation is achieved in 15-30 minutes; persists 3-4 hours
  • used for relief of acute asthma symptoms and brochospasms

FAST

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11
Q

LABAs

Long-Acting B2-Selective Agonists

A
  • potent selective B2-agonists that are delivered by metered-dose or dry powder inhalers
  • duration of action is >_ 12 hours, due to high lipid solubility
  • NOT RECOMMEND AS MONOTHERAPY
  • – lack any anti-inflammatory actions
  • –WORK WELL WITH inhaled corticosteroids to improve asthma control

SLOW

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12
Q

Catch with LABAs

A

CAN NEVER BE GIVEN BY ITSELF

  • continued use causes airways to be refractory/non-responsive
  • NEED to pair with INHALED CORTICOSTEROIDS
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13
Q

Methylxanthines
(PDE inhibitors)
Mechanism

A
  • catalyze breakdown of PDE and blunt response

- relax smooth muscle b/c keep cAMP around by preventing breakdown

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14
Q

Methylxanthines

PDE inhibitors

A
  • relax bronchial smooth muscle
  • anti-inflammatory properties
  • reduce release of inflammatory mediators and cytokines
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15
Q

Theophylline

in treatment of asthma

A
  • Methylxanthines
  • effective for treatment of asthma
  • – must be CAREFULLY regulated
  • not widely used because of narrow TI; used when asthma is unresponsive to other drugs
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16
Q

Theophylline TI

A

Narrow TI

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17
Q

Which drug has a narrow TI

A

Theophylline

mathylxanthine

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18
Q

Muscarinic Receptor Antagonists
(SAMRA, LAMRA)
Mechanism

A
  • block M2R/M3R receptors
  • inhibits contraction from occurring
    (rather than inducing dilation)
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19
Q

Anti-muscarinics

A
  • not used much anymore
  • – B2-selective agonists preferred
  • has role in parasympathetic pathways
  • many times COMBINED with B2-agonist to enhance dilatory effects
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20
Q

Smooth Muscle Dysfunction

- leads to (4 things)

A

leads to:

  • bronchoconstriction
  • bronchial hyperreactivity
  • hyperplasia/hypertrophy
  • inflammatory mediator release
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21
Q

Airway Inflammation

A

leads to:

  • inflammatory cell infiltration/activation
  • mucosal edema
  • cellular proliferation
  • epithelial damage
  • basement membrane thickening
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22
Q

Anti-inflammatory agents

3 Types

A
  • leukotriene modifiers
  • corticosteroids
  • biologics
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23
Q

Leukotrienes in Asthma

A

potent bronchoconstrictors and are associated with

  • mucus hypersecretion
  • increased bronchial reactivity
  • mucosal edema
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24
Q

Leukotriene Modifiers

Strategy for Therapeutic Use

A
  • inhibit 5-lipoxygenase (first step)
  • – Zileuton
  • block binding of LTD4 to CysLT receptor (inhibits further down the pathway
  • – Zafirlukast
  • – Montelukast
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25
Leukotriene Modifiers | Considerations for Use
ALL ORAL | - all have different mechanisms
26
Zileuton - dosage - inhibits
Leukotriene Modifiers - dosed 2 or 4x/day - inhibits multiple CYPs
27
Zafirlukast
Leukotriene Modifiers - dosed 2x/day - inhibits multiple CYPs
28
Montelukast
Leukotriene Modifiers - dosed 1x/day - no hepatic toxicity and does NOT inhibit CYPS - most widely used
29
``` Corticosteroids Therapeutic use in Asthma - target - effects - how administered ```
target: glucocorticoid receptors - inhibit eosinophilic influx - inhibit airway mucosal inflammation - reduce frequency of exacerbations if administered chronically - potentiate effects of B2 agonists (make effective for longer) - oral steroids for urgent, short-term treatment (can be given high dose oral if emergent)
30
Corticosteroid Considerations
* ** Aerosol Rx most effective at minimizing systemic adverse effects *** - lots of side effects when used long term - use as little as possible to get desired results
31
Inhaled Corticosteroids - bioavailability - name 2
- extremely low bioavailability due to extensive first-pass hepatic metabolism - -- budesonide - -- fluticasone
32
Dual Controller Therapy in Asthma
ICS + LABA vs. increased-dose ICS - much safer than LABA alone (DO NOT DO) - helps mitigate patient being refractory to LABA or SABA - escalating doses of ICS detrimental ICS + LABA vs ICS + LTRA *** patient dependent Asthma control in patients using ICS + LABA - dependent on severity - used for exacerbation treatment
33
As disease gets more severe
add on additional therapies | - monoclonal antibodies only for those with severe asthma who is not responding to anything else
34
Biologics | Used For
used for: - eosinophilic asthma - allergic eosinophilic inflammation - nonallergic eosinophilic inflammation
35
Omalizumab: Anti-IgE therapy
- mast cells BIG for allergic asthma: inhibit IgE & cut asthma off at the source (stops mast cell production) - -- lowers plasma IgE to undetectable levels - injection - lowers amount of corticosteroids needed *** indicated for use in patients with a positive skin test or in vitro reactivity to perennial aeroallergen***
36
Omalizumab Indication
Anti-IgE therapy | *** indicated for use in patients with a positive skin test or in vitro reactivity to perennial aeroallergen***
37
Anti-IL5 or IL-5 Receptor therapy
- eosinophilic asthma - affects maturation and differentiation of eosinophils; can also effect basophils - injection * ** Indicated for use in patients with eosinophilic asthma
38
Mepolizumab
Anti-IL5 or IL-5 Receptor therapy
39
Reslizumab
Anti-IL5 or IL-5 Receptor therapy
40
Benralizumab
Anti-IL5 or IL-5 Receptor therapy
41
Anti-IL5 or IL-5 Receptor therapy Indication
*** Indicated for use in patients with eosinophilic asthma
42
Anti-IL5 or IL-5 Receptor therapy Benralizumab Reslizumab Mepolizumab
Mepolizumab & Reslizumab target CIRCULATING IL5 Benralizumab targets receptor level IL5
43
Clinical Pharmacology of Mild to Moderate Asthma
- bronchodilators are rapidly effective, safe, and inexpensive - inhaled SABA on "as needed" basis Additional treatment is necessary if: - "rescue" therapy is required >2x/week - nocturnal symptoms occur >2x/month - FEV is <80% predicted
44
Clinical Pharmacology of Refractory and Severe Asthma
- ICS + LABA - -- marketed 2 in one inhalers - if asthma is inadequately controlled-- candidates for biologics
45
COPD
Irreversible - common preventable and treatable disease - progressive with enhanced chronic inflammatory response in the airways and lungs to noxious particles or gases - mainly effects older people - symptoms worsen over time, with limited relief because so much destruction of lung
46
Drugs used in COPD
Bronchodilators - anti-cholinergics - B2 agonists
47
Clinical Pharmacology of COPD
inhaled bronchodilator and brochodilator-steroid combinations
48
Tiotropium Bromide (Spiriva)
COPD | - long-acting muscarinic receptor antagonists (LAMRAs)
49
Aclidinium Bromide (Tudorza)
COPD | - long-acting muscarinic receptor antagonists (LAMRAs)
50
Fluticasone-Vilanterol (Breo)
COPD | - corticosteroid-LABA combination
51
Budesonide-Formoterol (Symbicort)
COPD - corticosteroid-LABA combination Also used for asthma treatment
52
Revefenacin (Yupelri)
COPD | - LAMRA that specifically TARGETS M3 MUSCARINIC RECEPTORS OVER M2
53
Clinical Pharmacology of Acute COPD Symptoms
- inhalation of SABA, a SAMRA, or SABA-SAMRA combination
54
Clinical Pharmacology of Chronic COPD Symptoms
- LAMRA or a Corticosteroid-LABA combination is indicated
55
B2 Agonists | - naming
- Albuterol, Salmeterol, Formoterol OL
56
Anti-muscarinics | - naming
- Tiotropium Bromide, Aclidinium Bromide IUM Bromide
57
Leukotriene Receptor Antagonists
- Zafirlukast, Montelukast KAST
58
Corticosteroids
- Fluticasone, Beclomethasone, Budesonide SONE
59
Biologics
- Omalizumab, Mepolizumab, Benralizumab MAB
60
budesonide
Inhaled corticosteroids
61
fluticasone
Inhaled corticosteroids

Pharmacology Test 2 (8 decks)

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