Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Respiratory II > Bronchodilators, Corticosteroids, and the Pharmacotherapy of Asthma and COPD > Flashcards

Bronchodilators, Corticosteroids, and the Pharmacotherapy of Asthma and COPD Flashcards

1
Q

Drug List 1

A
  • b agonist Bronchodilators
    • Short-acting b agonists (SABA)
      • Albuterol, others
    • Long-acting b agonists (LABA)
      • Salmeterol, formoterol
    • Emergency, non-selective b agonist
      • Epinephrine
  • Muscarinic Antagonists
    • Ipratropium, tiotropium
  • Methylxanthine
    • Theophylline
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Drug list 2

A
  • Inhaled Corticosteroids (ICS)
    • Beclomethasone
    • Budesonide
    • Ciclesonide
    • Flunisolide
    • Fluticasone
    • Mometasone
    • Triamcinolone
  • Oral Corticosteroids
    • Methylprednisolone
    • Prednisone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Drug List 3

A
  • Leukotriene Receptor Antagonist (LTRA)
  • Montelukast
  • Zafirlukast
  • Cromolyn compounds
  • Cromolyn sodium
  • Anti-IgE Antibody
  • Omalizumab
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Bronchospasm

A
  • In allergic asthmatics patients, immediate hypersensitivity-type reactions can be continuously present at a sub-threshold level, resulting in mild-to-moderate inflammation without overt bronchoconstriction.
  • Overt bronchospasm then occurs upon exposure to a specific allergen or to a variety of nonspecific stimuli, e.g., cold air, dust, air pollution, exercise, etc.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Antihistamine

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Inflammatory Mediators in Asthma

A
  • Enormous variety of mediators are released. Thus, blocker of a single mediator, e.g., antihistamine, is unlikely to be effective in alleviating the symptoms or the progression of asthma.
  • Corticosteroids, which are capable of blocking many key steps in the inflammatory process, come closest to this ideal therapy.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Mast Cell Mediators of Inflammatory Processes

Preformed

A

CLASS: Preformed (immediate)

MEDIATOR : Histamine,TNF-alpha Proteases, Heparin

EFFECTS: Bronchoconstriction, itch, cough, vasodilation, edema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Mast Cell Mediators of Inflammatory Processes

Lipids

A

CLASS: Lipids (minutes)

MEDIATOR : Leukotrienes, Prostaglandins

EFFECTS: Bronchoconstriction,chemotaxis, mucus secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Mast Cell Mediators of Inflammatory Processes

Cytokines

A

CLASS: Cytokines (hours)

MEDIATOR: Interleukins, GM-CSF

EFFECTS: Bronchoconstriction. chemotaxis, inflammatory cell proliferation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Mast Cell Mediators of Inflammatory Processes

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Normal Airway vs Airway in Asthma

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Aerosol Delivery of Drugs

Factors to Consider

A
  • Particle size of aerosol is important.
  • Rate of breathing and breath holding.
  • Even under ideal conditions, 90% of inhaled drug is swallowed.
  • Therefore, ideally the best drugs also have poor absoption from the GI tract and/or rapid first-pass metabolism in the liver.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Particle Size in Inhalers

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Aerosol Delivery of Drugs

Devices

A
  • Metered Dose Inhalers (MDI)
    • with spacer device
  • Nebulizers
  • Dry powder inhalers
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Nebulizers

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Classifying Astham Severity in youths 12 and Older

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Stepwise Approach for Managing Astham in youths 12 and Older

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Stepwise Treatment: Kids 5 - 11

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Beta-Adrenergic Agonists

A
  • Therapeutic Use in Asthma and COPD:
    • Drug of choice for rapid relief of bronchospasm
    • Highly effective and safe for intermittent, prophylactic treatment of asthma.
  • Current Emphasis:
    • Intermittent use on an as-needed basis for relief of acute, severe bronchospasm. Not general prophylaxis.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Beta-Adrenergic Agonists

Overuse

A

Overuse:

  • Side effects intensify will overuse, but a greater danger is the tendency to continue to self-medicate during periods when symptoms are escalating.
  • To avoid a medical emergency, patients should be encouraged to seek medical attention as soon as possible after they detect a decline in the efficacy of their usual therapeutic regimen.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Beta-Adrenergic Agonists

Mechanism of Action:

A

Mechanism of Action:

  • Stimulate b2-adrenergic receptor on surface of bronchiolar smooth muscle cells.
  • b2-adrenergic receptor couples to Gs protein and activates adenylyl cyclase enzyme leading to increased cellular levels of cyclic AMP.
  • Cyclic AMP stimulates phosphorylation cascade that leads to decreased intracellular calcium and smooth muscle relaxation.
  • Also inhibit mediator release from mast cells.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Selectivity of
Beta-Adrenergic Agonists

A
  • Selectivity means these agonists have higher affinity, and thus, higher potency at b2-adrenergic receptors than at b1-adrenergic receptors.
  • Selectivity helps limit side effects mediated by activation of b1-receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Beta 2-Receptor Selectivity

A
24
Q

Rapid Acting-Short Duration
Beta 2-Adrenergic Agonists

A
  • Albuterol onset<15 min duration: 2-4 hr
  • Levalbuterol same
    • l-isomer of albuterol
  • Pirbuterol same
  • Terbutaline same
  • These agents are used as “rescue inhalers”. They are relatively fast at relieving bronchospasm, but have a relatively short duration of action.
25
Q

Long Acting
Beta 2-Selective Agonists (LABA)

A
  • Salmeterol:
    • slower onset
    • duration > 12 hours of useful bronchodilation
    • useful to control nighttime asthma attacks, also now used BID for prevention
    • not suitable for treatment of acute bronchospastic attacks because onset of action is too slow.
  • Formoterol
    • Similar to salmeterol
    • Not for acute attacks
26
Q

Less Selective or Nonselective
Beta -Adrenergic Agonists

A
  • Epinephrine
  • Isoproterenol
  • Metaproterenol
  • Isoetharine
    • Because of their very short duration of action and their lack of b2-selectivity, these agents are not frequently used.
    • Low-strength epinephrine inhalers sometimes prescribed for mild asthma
  • Racemic Epinephrine
    • aerosol used for pediatric patients
27
Q

Long-term Use of LABA

A
  • Continued use of a LABA may cause down-regulation of b2 receptors with loss of the protective effect from rescue therapy with a short-acting agent.
  • LABA should not be used for monotherapy in patients with persistent asthma, especially in children.
  • LABA should be used in asthma only in combination with an inhaled corticosteroid.
  • “Stop use of a LABA, if possible, once asthma control is achieved and maintain the use of an asthma-controller medication such as an inhaled corticosteroid”.
28
Q

Oral Therapy with
Beta -Adrenergic Agonists

A
  • Oral administration increases incidence of adverse side effects:
    • muscle tremor, cramps, cardiac tachyarrhythmias, metabolic disturbances, hypokalemia
  • Appropriate situations for oral therapy:
    • brief therapy in children with upper respiratory tract infections who cannot manipulate inhaler
    • in severe asthma exacerbations where inhaler cannot be used or when aerosol is irritating
    • oral albuterol and terbutaline are available
29
Q

Adverse Side Effects of
Beta -Adrenergic Agonists

A
  • Patients with cardiovascular disease or diabetes are at higher risk of adverse effects.
    • Skeletal muscle tremor (most frequent side effect)
    • CNS: restlessness, apprehension, anxiety, tremors
    • CVS: tachycardia, dysrhythmias, hyper- or hypotension
    • hypokalemia
    • worsen hyperglycemia in diabetics
    • drug interactions with thyroid, digitalis, methylxanthines
30
Q

Epinephrine: Emergency Use

A
  • Epinephrine is the drug of choice for treatment of anaphylactic reactions.
  • Give SQ (or IM or IV with dextrose)
  • Bronchodilation (mediated by beta 2 receptors)
  • Vasoconstriction (mediated by alpha 1 receptors)
  • maintains BP & decreases edema
  • Inhibition of mediator release (beta 2 receptors)
31
Q

Anaphylaxis Treatments

A
  • Albuterol via nebulizer
  • IV fluids
  • Oxygen
  • Secondary therapy
    • H1 antagonist - diphenhydramine
    • H2 antagonist - ranitidine
    • Corticosteroid - hydrocortisone, methylprednisolone
    • Aminophylline
    • NE, glucagon - for hypotension
32
Q

Atropine and Ipratropium Bromide

A
33
Q

Bronchodilators:
Ipratropium bromide

A
  • A quaternary muscarinic receptor antagonist
  • If given parenterally, effects are like atropine
  • But, only given as inhaled aerosol
    • few side effects, even when swallowed because is poorly absorbed from GI and does not cross into brain
    • quaternary amine- poor diffusion across membranes
  • Parasympathetic - mediated bronchospasm is a significant component of airway resistance in some asthmatics and COPD patients, especially psychogenic exacerbations
34
Q

CNS Airway Control

A
35
Q

Ipratropium bromide
and Tiotropium

Therapeutic Use

A
  • Therapeutic Use:
    • Bronchodilation develops more slowly and is usually less intense than that produced by b-agonists.
    • Useful bronchodilation lasts up to 6 hours.
    • Principal use of ipratropium is in COPD.
    • Combined with albuterol = COMBIVENT
    • Also used intranasally to reduce secretions in the upper and lower respiratory tract in allergic rhinitis and chronic postnasal drip syndrome.
    • Tiotropium: newer long-acting agent (QD dosing) used for maintenance therapy in chronic bronchitis and emphysema; dry powder inhaler device
36
Q

Methylxanthine Bronchodilators:
Theophylline

A
  • Methylxanthines
    • theophylline, caffeine, theobromine
    • found in coffee, tea, chocolate, cocoa, colas
  • Diverse cellular actions
    • adenosine receptor antagonists
    • block cyclic AMP degradation – PDE inhibitor
    • lower intracellular calcium
    • hyperpolarize cell membranes
37
Q

Theophylline

A
  • Bronchodilation is a clinically relevant effect of theophylline
  • Other effects include CNS stimulation, modest peripheral vasodilation, improved skeletal muscle contractility, and a thiazide-like diuresis
38
Q

Theophylline

Therapeutic Use:

A
  • Therapeutic Use:
    • Formerly a first-line agent for treatment of asthma
    • Now has a far less prominent role because:
    • benefits are modest
    • narrow therapeutic window
    • considerable variation in absorption and elimination between different patients
    • monitoring of plasma concentrations is often required
  • Nocturnal asthma can be improved with slow-release theophylline, but inhaled corticosteroids and salmeterol are probably more effective.
  • IV formulation = aminophylline
39
Q

Anti-Inflammatory Agents
Corticosteroids

A
  • In asthma (and some COPD) an inflammatory response is responsible for the underlying disease process.
  • So many inflammatory mediators are involved that a blocker of any given autocoid or cytokine, e.g., antihistamine, is ineffective in alleviating the symptoms of asthma.
  • Corticosteroids block many of the steps involvedin the inflammatory cascade
40
Q

Anti-Inflammatory Agents
Corticosteroids

A
  • Mechanism of Action
    • corticosteroids are steroid receptor agonists that bind to intracellular receptors that translocate to the cell nucleus and positively or negatively regulate gene transcription. This takes time.
    • corticosteroids inhibit the production and release of cytokines, vasoactive and chemoattractive factors, lipolytic and proteolytic enzymes, decrease mobilization of leukocytes to areas of injury, and decrease fibrosis.
    • General anti-inflammatory response.
41
Q

Corticosteroid Mechanism

A
42
Q

Inhaled Corticosteroids

A
  • Beclomethasone dipropionate (Beclovent)
  • Budesonide dipropionate (Pulmicort)
  • Ciclesonide (Alvesco)
  • Flunisolide (AeroBid)
  • Fluticasone (Flovent)
  • Mometasone (Asmanex Twisthaler)
  • Triamcinolone acetonide (Azmacort)
43
Q

Systemic Corticosteroids

A
  • IV or oral
    • Prednisone
    • Methylprednisolone
    • Hydrocortisone
44
Q

Corticosteroids

A
  • Corticosteroids have potentially important adverse side effects.
  • Aerosol delivery of the steroid has significantly improved the safety of treatment for moderate to severe asthma.
  • Asthmatics who require inhaled b-adrenergic agonist therapy 3 - 4 or more times weekly are candidates for inhaled steroid therapy.
45
Q

Corticosteroids

Preparations

A
  • Available preparations have equivalent efficacy and potential side effects, but differ in the amount of drug aerosolized per inhaler activation, i.e., high-dose and low-dose.
  • Therefore, the dose of inhaled steroid must be empirically determined for each patient.
46
Q

Corticosteroids

for Asthmatics

A
  • Asthmatic patients maintained on inhaled corticosteroids show improvement of symptoms and lower requirements for “rescue” with a bronchodilator.
47
Q

Corticosteroids

Systemic Therapy

A
  • Systemic Therapy
    • Systemic (i.v. or oral) steroid therapy is used in severe asthmatic attacks requiring hospitalization.
    • For severe asthma, prednisone or methylprednisolone is given i.v., followed by oral doses and gradual tapering of the dose.
    • For acute, sever exacerbations, oral prednisone is administered for 1 -2 weeks.
    • Longer treatments require tapering of the dose to account for hypothalamic-pituitary-adrenal suppression.
48
Q

Corticosteroids:
Potential Side Effects

A
  • HPA suppression - low risks until high doses
  • Bone resorption - modest risks
  • Carbohydrate and lipid - minor risks
  • Cataracts and skin thinning - dose-related
  • Purpura - dose-related
  • Dysphonia - usually resolves
  • Candidiasis - use spacer device and rinse mouth
  • Growth retardation - of concern in children
49
Q

Combination Products

A
  • Fluticasone propionate + Salmeterol (Advair Diskus, Advair HFA)
  • Budesonide + Formoterol
  • (Symbicort HFA)
  • Mometasone + Formoterol (Dulera)
  • Not useful for acute bronchospastic attack
  • Cost Range: ~$145-$175/month
50
Q

Chronic Obstructive Pulmonary Disease (COPD)

A
  • Emphysema and chronic bronchitis
  • Smoking cessation
  • Alveolar destruction is the main pathophysiological component (irreversible component)
  • Some patients have inflammation and bronchospasm (reversible components)
    • Drug therapy is applicable to the reversible component of COPD
51
Q
A
52
Q

Chronic Obstructive Pulmonary Disease (COPD)

Inhaled ipratropium bromide or tiotropium

A
  • Inhaled ipratropium bromide or tiotropium
    • especially useful in patients with a vagally-mediated psychogenic component.
  • Inhaled beta 2-adrenergic agonists
    • As with asthma, continuous (overuse) of bronchodilators may be associated with worsening of symptoms.
  • A subgroup of COPD patients may benefit from corticosteroid therapy, but generally mixed results of steroids in COPD.
53
Q

Cromolyn Compounds

A
  • Cromolyn sodium (Intal)
  • Cromolyn sodium is an anti-inflammatory agent that indirectly inhibits antigen-induced bronchospasm and directly inhibits the release of histamine and other autocoids from sensitized mast cells.
  • May suppress the activating effects of chemoattractant peptides on eosinophils, neutrophils, and monocytes.
54
Q

Cromolyn Compounds:
Therapeutic Use

A
  • Cromolyn compounds do not directly relax smooth muscle, therefore they are not useful for control of acute bronchospasm.
  • Cromolyn compounds are primarily prophylactic. When inhaled several times daily, they inhibit both the immediate and late asthmatic responses to antigenic challenge or exercise.
55
Q

Corticosteroids vs. Bradykinin/Angiotensin

A
56
Q

Leukotriene inhibitors

A
  • Zafirlukast
    • LTD4 receptor antagonist
  • Montelukast
    • LTD4 receptor antagonist
  • Alternative or adjunctive therapy to low-dose corticosteroids for mild persistent asthma.
  • Useful as oral prophylaxis in exercise-induced asthma

Respiratory II (14 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions