asthma & COPD Flashcards

1
Q

Short Acting Beta2 Agonists (SABA) Agents

A

Albuterol

Levalbuterol

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2
Q

SABA

A
  • MOA: Stimulate adenylyl cyclase at beta2 receptor –> increase cAMP in bronchial smooth muscle –> bronchodilation
  • Selective for beta2 receptor
  • DOC for ACUTE ASTHMA ATTACKS and exercise induced asthma
  • Onset: 5 min
  • Duration: 3-4hr
  • Given (almost) exclusively via inhalation
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3
Q

SABA ADE

A
  • Well tolerated with PRN use: (as needed)
    Mouth irritation, cough
  • ADE at high doses: Skeletal muscle tremor, atachycardia/palpitation, arrhythmia, tolerance with exercise use (decreased responsiveness and decrease in number of beta receptors)
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4
Q

Long Acting Beta2 Agonist (LABA) Agents

A
Long acting
- Salmeterol
- Formoterol
Ultra-Long acting
- Indacterol
- Olodaterol
- Vilanterol (in combo with ICS)
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5
Q

LABA

A
  • MOA: Stimulate adenylyl cyclase at beta2 receptor –> increase cAMP in bronchial smooth muscle –> bronchodilation
  • Slower onset of action (~30 min)
  • Longer duration of action (12-24hrs)
  • NOT for rescue therapy
  • CANNOT be used as monotherapy in asthma
  • OK in COPD
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6
Q

LABA ADE

A
  • Well tolerated with PRN use: (as needed)
    Mouth irritation, cough
  • ADE at high doses: Skeletal muscle tremor, atachycardia/palpitation, arrhythmia, tolerance with exercise use (decreased responsiveness and decrease in number of beta receptors)
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7
Q

Antimuscarinic Agents

A
Short Acting
- Ipratropium
Long Acting
- Tiotropium
- Aclidinium
- Umeclidinium
- Glycoprolate
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8
Q

Antimuscarinic

A
  • MOA: competitively block muscarinic receptors (M1, M2, M3) and the effects of ACh in airway –> prevent vasoconstriction mediated by vagal discharge
  • No effects on chronic inflammation
  • bronchodilating effects last longer than Beta agonists
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9
Q

Antimuscarinic ADE

A
  • Minimally absorbed, generally well tolerated
  • Potential for: dry mouth, dry eyes, bitter/metallic taste, constipation, urinary retention
  • NO Tremors or Arrhythmia
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10
Q

Methylxanthine derivative agents

A

theophylline - oral

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11
Q

Methylxanthine derivative

A

MOA: (1) non-selectively inhibits phosphodiesterase (PDE) –> Increases cAMP –> bronchodilatuon (2) Block adenosine receptors in CNS (inhibits bronchoconstriction)

  • Available PO in IR and SR formulations
  • Duration of action ~ 12hrs
  • Requires high concentration to be effective
  • Considered narrow therapeutic index drug
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12
Q

Theophylline

A

Metabolized via CYP450 1A2 enzyme system
- MANY drug-drug interactions – febuxostat, bupropion, carbamazepine, macrolide antibiotics, etc.
Clearance mediated by age, smoking status and other drugs
- Younger patients clear drug faster vs. elders
- Smokers clear the drug faster vs. non-smokers
Requires therapeutic monitoring
- Therapeutic range 10-20 mcg/mL
- Levels correlate with efficacy

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13
Q

Theophylline ADE:

A
  • GI distress (enhanced gastric acid secretion)
  • Tremor
  • Insomnia
  • In overdose, severe nausea and vomiting, hypotension, agitation, arrhythmia, cardiac arrest, seizures
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14
Q

PDE-4 Inhibitor Agents

A

Roflumilast - Oral

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15
Q

PDE-4 Inhibitor

A

MOA: not fully elucidated; electively inhibits PDE-4 –> increases cAMP –> bronchodilation

  • Used for severe or very severe COPD (should be given in combo with at least one LAMA or LABA for COPD)
  • Given by mouth once daily (duration of action >10-20 hrs)
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16
Q

Roflumilast

A
  • Partially metabolized by CYP3A4 DDI with rifampin, phenobarbital, phenytoin, carbamazepine
  • ADE: diarrhea, nausea, vomiting, abdominal pain, headache, dyspepsia, psychiatric events, weight loss
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17
Q

Cotricosteroids

A

MOA: binds to glucocorticoid receptors to:

  • Inhibit inflammatory cell migration and activation
  • Inhibit cytokine and mediator release
  • Up regulate B2 receptors
  • Inhibit IgE synthesis

DOC for persistent Asthma (prophylaxis)
- May take 4-6 weeks for effects
multiple dosage forms
- Do not abruptly d/c–> taper dose slowly

18
Q

Inhaled Corticosteroids

A
Beclomethasone
Budesonide - Safe in pregnancy
Fluticasone propionate
Fluticasone furoate
Mometasone
Flunisolide
Ciclesonide
19
Q

Oral/IV Corticosteroids

A

Prednisone
Prednisolone
Methylprednisolone
Hydrocortisone

20
Q

ADE ICS

A
  • Thrush (oral candidiasis) counsel patients to rinse mouth after each use
  • Dysphonia
  • Sore throat
  • Cough
21
Q

Oral Corticosteroids ADEs

A
  • Adrenal suppression
  • Cushing syndrome
  • Growth retardation
  • Osteoporosis
  • Glucose intolerance
  • Infection risk
  • Mood changes
  • Weight gain
  • Edema
22
Q

Coritcosteroids for Kids

A
  • Potential growth stunting in children
  • Still preferred DOC in children for asthma
  • Lowest dose possible & monitor changes in growth
23
Q

Bronchodilators

A
  • SABA
  • LABA
  • Muscarinic Antagonsit
  • Methylxanthine derivatives
  • PDE-4 Inhibitors
24
Q

Leukotriene Antagonists

A
  • Lipoxygenase inhibitors

- Leukotriene receptor antagonists

25
Q

Lipoxygenase inhibitors Agents

A

Zileuton - oral

26
Q

Lipoxygenase inhibitors MOA

A

inhibits actions of 5-lipoxygenase to inhibit the synthesis of leukotrienes

27
Q

Lipoxygenase Inhibitors ADE

A
  • Headache
  • Insomnia
  • Somnolence
  • GI upset
  • Hepatotoxicity
    DO NOT administer if LFTs>3XULN
    Females > 65 years of age and those with pre-existing LFT elevations are at highest risk –> monitor
28
Q

Leukotriene Receptor Antagonist Agents

A

Montelukast - oral

Zafirlukast - oral

29
Q

Leukotriene Receptor Antagonist

A

MOA: Competitively block action of leukotrienes at the LTD4 receptor
Can be used for Asthma allergic symptoms, exercise-induced bronchospams, uricaria

30
Q

Leukotriene Receptor Antagonists DDI

A

Zafirlukast - Warfarin –> may increase risk of bleed

31
Q

Leukotriene Receptor Antagonists ADE

A
  • Generally well tolerated
  • Headache
  • Hepatoxicity (Zafirlukast)
  • Neuropsychiatric events (anmormal dreams, hostility, aggression, suicidality, agitation, hallucinations)
32
Q

Mast Cell Stabilizers Agents

A

Cromolyn sodium

Nedocromil sodium

33
Q

Mast Cell Stabilizers MOA

A

Block influc of Ca –> prevention of mast cell degranulation –> stabilize mast cell –> prevent release of inflammatory mediators
- Do not exert any direct bronchodilating, antihistaminic, or anti-inflammatory effects

34
Q

Mast Cell Stabilizers

A
  • Indicated for mild asthma cases (not used much)
  • Not for rescue symptoms
  • Requires multiple daily doses
  • Clinical improvement may take 2-6 weeks for effect
  • Well tolerated (mild throat irritation, couch, abnormal taste in mouth)
  • NO DDI
35
Q

Immunotherapy

A

Anti IgE agents

IL-5 Antagonists

36
Q

Anti IgE Agents

A

Omalizumab

37
Q

Anti IgE

A
  • MOA: Monocolonal IgE antibody –> inhibits binding of IgE to surface of mast cells & basophils –> inhibits release of inflammatory mediators
  • Indicated for allergic asthma not relieved with corticosteroid therapy (MUST have evidence of allergic sensitization)
  • Dose based on IgE levels and body weight (SQ every 2-4 wk)
38
Q

Omalizumab

A
  • Indicated for >12 years of age
  • Clinical improvement delayed (12 weeks to work)
  • ADE: injection site reaction, Anaphylaxsis –> usually 1.5-2hr after dose, arthralgia, headache, pharyngitis, sinusitis, malignancies (immunosuppression)
  • NO DDI
39
Q

IL-5 Antagonist Agents

A

Mepolizumab

Reslizumab

40
Q

IL-5 Antagonist

A
  • MOA: Humanized interleukin -5 (IL-5) monoclonal antibody antagonist to reduce the amount of circulating eosinophils
  • used for the maintenance of severe asthma for patients who continue to have exacerbation despite adequate therapy
  • Administered SC (Mepolizumab) or IV (Reslizumab) every 4 weeks by HCP
  • NOT recommended for monotherapy (must be >18yr of age with an eosinophilic phenotype
41
Q

IL-5 Antagonist ADE:

A
  • injection site reactions
  • Headache
  • Hypersensitivity reactions (anaphylaxis can be life threatening)
  • Malignancy
  • Muscle and face pain