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Pharm Exam 3 > Asthma / COPD > Flashcards

Asthma / COPD Flashcards

1
Q

Preferred Treatment Delivery Systems treating Asthma / COPD

Pros
Cons

A

Aerosolized delivery system preferred treated

++ Small particle size, delivered directly to lung in high concentration leading to reduced systemic exposure

– Required proper technique for effective therapy, expensive

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2
Q

Metered dose inhaler

Advantages / Disadvantages

A

Advantage - small, compact, portable, easy to use, can by used with space, no drug preparation

Disadvantage - proper technique / coordination w/ breath (requires a breath hold); contains propellants, expensive

*** proper technique to use it

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3
Q

Dry Powder Inhaler

Advantages / Disadvantages

A

Advan - Small, compact, portable, easy to use, cheaper vs MDI, no coordination needed

Disadvan - pt must prepare the dose, requires fast, deep inhalation (requires a breath hold), moisture sensitive

**Not ideal for COPD pt trouble taking deep breath

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4
Q

Soft mist inhaler

Advantages / Disadvantages

A

Advan - compact, portable, multi dose device, high lung deposition, does not contain propellants

Disadvan - complicated process for first dose, slow moving mist, cannot use spacer, expensive

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5
Q

Nebulizer

Advantages / Disadvantages

A

Advan - minimal technique required, pt is not required to hold breath

disadvantages - expensive, requires dose prep, bulky (not portable), administration time 5-15 min, needs a power source, cleaning needed

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6
Q

Bronchodilators no effect on ?

A

No effect on inflammation / immune response in someone with persistent asthma in this case you would need to put the patient on a steroid inhaler

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7
Q

Bronchodilation increased by

A

increase cAMP increased branchodilation

cAMP increased by ATP (enhanced by beta agonists)
cAMP decrease by PDE (inhibited by theophylline)

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8
Q

Bronchoconstriction increased by

A

Acetylcholine (inhabited by muscarinic antagonists)

adenosine (inhibited by theophylline)

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9
Q

Short acting B2 Agonist (SABA)

MOA
DOC for
Given

A

Albuterol, Proventil, Levalbuterol

MOA : stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Selective for B2 receptor

DOC for acute asthma attacks & exercise induced asthma

Onset - 5 min Duration 3-4 hours

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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10
Q

Albuterol

A

Albuterol, Proventil, Levalbuterol

MOA : stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Selective for B2 receptor

DOC for acute asthma attacks & exercise induced asthma

Onset - 5 min Duration 3-4 hours

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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11
Q

Lealbuterol

A

Albuterol, Proventil, Levalbuterol

MOA : stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Selective for B2 receptor

DOC for acute asthma attacks & exercise induced asthma

Onset - 5 min Duration 3-4 hours

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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12
Q

Proventil

A

Albuterol, Proventil, Levalbuterol

MOA : stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Selective for B2 receptor

DOC for acute asthma attacks & exercise induced asthma

Onset - 5 min Duration 3-4 hours

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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13
Q

Long Acting B2 Agonist (LABA)

MOA
Use
ADR

Long vs Ultra long

A

MOA - stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Slower onset of action - about 30 min
Longer duration - 12-24 hours
Not for rescue therapy

CANNOT be used as MONOtherapy in asthma
- ok in COPD

Long acting = Salmeterol ; Formoterol

Ultra long acting = indacaterol, Olodaterol, Vilanterol

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14
Q

Salmeterol

A

Long Acting B2 Agonist - LABA

MOA - stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Slower onset of action - about 30 min
Longer duration - 12-24 hours
Not for rescue therapy

CANNOT be used as MONOtherapy in asthma
- ok in COPD

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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15
Q

Formoterol

A

Long Acting B2 Agonist - LABA

MOA - stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Slower onset of action - about 30 min
Longer duration - 12-24 hours
Not for rescue therapy

CANNOT be used as MONOtherapy in asthma
- ok in COPD

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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16
Q

Indacaterol

A

Ultra - Long Acting B2 Agonist - LABA

MOA - stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Slower onset of action - about 30 min
Longer duration - 12-24 hours
Not for rescue therapy

CANNOT be used as MONOtherapy in asthma
- ok in COPD

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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17
Q

Olodaterol

A

Ultra - Long Acting B2 Agonist - LABA

MOA - stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Slower onset of action - about 30 min
Longer duration - 12-24 hours
Not for rescue therapy

CANNOT be used as MONOtherapy in asthma
- ok in COPD

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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18
Q

Vilanterol

A

Ultra - Long Acting B2 Agonist - LABA

MOA - stimulated adenylyl cyclase at B2 receptor - increases cAMP in bronchial smooth muscle causing bronchdilation

Slower onset of action - about 30 min
Longer duration - 12-24 hours
Not for rescue therapy

CANNOT be used as MONOtherapy in asthma
- ok in COPD

ADRs
- Well tolerated with PRN use (mouth irritation, cough, etc)
- At HIGH doses :
Skeletal muscle tremor
Tachycardia / palpitations
Arrhythmia
Tolerance w/ excessive use (decrease responsiveness and decrease in number of B receptors)

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19
Q

Antimuscarinic Agents

A

MOA: competitively blocks muscarinic receptors and the effects of ACh in the airway = prevent vasoconstriction mediated by bagel discharge

No effects on chronic inflammation

Bronchodilationg effects last longer than B agonists

COPD almost exclusively

ADRs

  • minimally absorbed, generally well tolerated
  • potential for:
    • Dry mouth, eyes
    • bitter, metallic taste
    • constipation
    • Urinary retention
  • No tremors or arrhythmias
Ipratropium = short acting 
Tiotropium = long acting (approved for asthma) 
Aclidinium
Umeclidinum
Glycoprolate
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20
Q

Ipratropium

A

Short Acting Antimuscarinic agent

MOA: competitively blocks muscarinic receptors and the effects of ACh in the airway = prevent vasoconstriction mediated by bagel discharge

No effects on chronic inflammation

Bronchodilationg effects last longer than B agonists

COPD almost exclusively

ADRs

  • minimally absorbed, generally well tolerated
  • potential for:
    • Dry mouth, eyes
    • bitter, metallic taste
    • constipation
    • Urinary retention
  • No tremors or arrhythmias
21
Q

Tiotropium

A

Long Acting Antimuscarinic agent - approved for asthma

MOA: competitively blocks muscarinic receptors and the effects of ACh in the airway = prevent vasoconstriction mediated by bagel discharge

No effects on chronic inflammation

Bronchodilationg effects last longer than B agonists

COPD almost exclusively

ADRs

  • minimally absorbed, generally well tolerated
  • potential for:
    • Dry mouth, eyes
    • bitter, metallic taste
    • constipation
    • Urinary retention
  • No tremors or arrhythmias
22
Q

Aclidinium

A

Antimuscarinic agent

MOA: competitively blocks muscarinic receptors and the effects of ACh in the airway = prevent vasoconstriction mediated by bagel discharge

No effects on chronic inflammation

Bronchodilationg effects last longer than B agonists

COPD almost exclusively

ADRs

  • minimally absorbed, generally well tolerated
  • potential for:
    • Dry mouth, eyes
    • bitter, metallic taste
    • constipation
    • Urinary retention
  • No tremors or arrhythmias
23
Q

Umeclidinium

A

Short Acting Antimuscarinic agent

MOA: competitively blocks muscarinic receptors and the effects of ACh in the airway = prevent vasoconstriction mediated by bagel discharge

No effects on chronic inflammation

Bronchodilationg effects last longer than B agonists

COPD almost exclusively

ADRs

  • minimally absorbed, generally well tolerated
  • potential for:
    • Dry mouth, eyes
    • bitter, metallic taste
    • constipation
    • Urinary retention
  • No tremors or arrhythmias
24
Q

Glycoprolate

A

Short Acting Antimuscarinic agent

MOA: competitively blocks muscarinic receptors and the effects of ACh in the airway = prevent vasoconstriction mediated by bagel discharge

No effects on chronic inflammation

Bronchodilationg effects last longer than B agonists

COPD almost exclusively

ADRs

  • minimally absorbed, generally well tolerated
  • potential for:
    • Dry mouth, eyes
    • bitter, metallic taste
    • constipation
    • Urinary retention
  • No tremors or arrhythmias
25
Theophylline
Oral Methylxanthine derivative MOA : - Non selectively inhibits phosphodiesterase - increases cAMP - bronchodilator - Block adenosine receptors in CNS - (increase cAMP/cGMP = reduced inflammation and smooth muscle relaxation) Available PO in IR and SR formulation Duration of Action ~ 12 hours Requires high concentration to be effective Considered "narrow therapeutic index" drug Metabolized by CYP450 = many DDI Clearance mediated by age, smoking status and other drugs - Younger clear drug faster - SMOKERS clear the drug faster than non smokers Requires therapeutic monitoring - range 10-20 (levels correlate with efficacy) ADRs - GI distress (the one to watch for - can cause Gerd and make it worse) - Tremor - Insomnia - In overdose - severe nausea & vomitting, hypotension, agitation, arrhythmias, cardiac arrest & seizures
26
Roflumilast
PDE-4 inhibitor MOA: not fully elucidated; selectively inhibits PDE-4 --- increases cAMP --- bronchodilator Used for severe or very severe COPD Should be given in combo with at least 1 other long acting bronchodilator for COPD Partially metabolized by CYP450 3A4 ADRs - Diarrhea, nausea, vomiting, abdominal pain, HA, dyspepsia - Psychiatric events** - Weight loss
27
Corticosteriods MOA DOC
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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly Oral / IV : Prednisone, Prednisolone, Methylprednisone, hydrocortisone Inhaled : Beclomethasone, Budesonide, Fluticasone propionate , Fluticasone furcate, Mometasone, FLunisolide, Ciclesonide
28
Corticosteroids Inhaled ADR
Thrush (Oral candidiasis) - counsel patients to rinse mouth after each use Dysphonia, sore throats cough
29
Corticosteroids Oral ADR
``` Adrenal suppression cushing syndrome growth retardation osteoporosis glucose intolerance infection risk mood changes weight gain edema ```
30
Beclomethasone
Inhaled Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
31
Budesonide
Inhaled Corticosteriod *Safest in pregnancy 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
32
Fluticasone propionate
Inhaled Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
33
Fluticasone furoate
Inhaled Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
34
Mometasone
Inhaled Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
35
Flunisolide
Inhaled Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
36
Ciclesonide
Inhaled Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
37
Prednisone
Oral/IV Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
38
Prednisolone
Oral/IV Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
39
Methylprednisolone
Oral/IV Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
40
Hydrocortisone
Oral/IV Corticosteriod 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: - Persistent asthma - prophylaxis May take 4 - 6 weeks for effects Do not abruptly D/C - taper dose slowly
41
Zileuton
Lipozygenase inhibitor (not very effective clinically) MOA: inhibits actions of 5-lipooxygenase to inhibit the synthesis of leukotrienes ADRs: - headache, insomnia, somnolence, GI upset - Hepatotoxicity - DO not administer if LFTs >3x ULN - Females > 65 YOA and in those with pre-existing LFT elevation at highest risk === monitor
42
Montelukast
Leukotriene receptor antagonist MOA: competitively blocks actions of leukotrienes at the LTD4 receptor Can be used for asthma, allergic symptoms, exercise induced bronchospasm, urticaria DDI - Zafirlukast & warfin = may increase risk of bleed ``` ADR - Generally well tolerated - Headache - Neuropsychiatric events: BBW Abnormal dreams, hostility, aggression, suicidality, agitation, hallucinations ```
43
Zafirlukast
Leukotriene receptor antagonist MOA: competitively blocks actions of leukotrienes at the LTD4 receptor Can be used for asthma, allergic symptoms, exercise induced bronchospasm, urticaria DDI - Zafirlukast & warfin = may increase risk of bleed ``` ADR - Generally well tolerated - Headache - Hepatotoxcity - Neuropsychiatric events: BBW Abnormal dreams, hostility, aggression, suicidality, agitation, hallucinations ```
44
Cromolyn Sodium
Mast Cell stabilizer MOA: block influx of Ca - prevention of mast cell degranulation - stabilize mast cell -- prevent release of inflammatory mediator - not for bronchodilator or anti-inflammation ; just stabilize mast cells Do not exert any direct bronchodilaitng, antihistaminic or anti-inflammatory effets Indicated for mild asthma cases , not rescue symptoms Clinical improvement may take 2 - 6 weeks Well tolerated - mild throat irritation, cough, abnormal taste
45
Nedocromil sodium
Mast Cell stabilizer MOA: block influx of Ca - prevention of mast cell degranulation - stabilize mast cell -- prevent release of inflammatory mediator - not for bronchodilator or anti-inflammation ; just stabilize mast cells Do not exert any direct bronchodilaitng, antihistaminic or anti-inflammatory effets Indicated for mild asthma cases , not rescue symptoms Clinical improvement may take 2 - 6 weeks Well tolerated - mild throat irritation, cough, abnormal taste
46
Omalizumab
Anti IgE agent MOA: monoclonal IgE antibody - inhibits binding of IgE to surface of mast cells & basophils = inhibits release of inflammatory mediators Indicated for allergic asthma not relieved w/ corticosteroid therapy must have evidence of allergic sensitization SQ injection every 2 - 4 weeks Indicated for >12 YOA Takes up 12 weeks to work ADRs - Injection site reactions - Anaphylaxis = usually 1.5 - 2 hours post dose - Arthralgia , headache - Pharyngitis, sinusitis
47
Mepolizumab
Il-5 antagonist MOA: humanized interleukin - 5 monoclonal antibody antagonist to reduce the amount of circulating eosinophils Used for maintenance of severe asthma for patient who continue to have exacerbation's despite adequate therapy Administered SC or IV every 4 weeks Not recommended for mono therapy - must be >18 YOA w. an eosinophilic phenotype ADR - Injection site reactions - headache - hypersensitivity reasons (anaphylaxis can be life threatening) - muscle & face pain
48
Reslizumab
Il-5 antagonist MOA: humanized interleukin - 5 monoclonal antibody antagonist to reduce the amount of circulating eosinophils Used for maintenance of severe asthma for patient who continue to have exacerbation's despite adequate therapy Administered SC or IV every 4 weeks Not recommended for mono therapy - must be >18 YOA w. an eosinophilic phenotype ADR - Injection site reactions - headache - hypersensitivity reasons (anaphylaxis can be life threatening) - muscle & face pain

Pharm Exam 3 (6 decks)

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