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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
Q

Theophylline

A

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
Q

Roflumilast

A

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
Q

Corticosteriods

MOA
DOC

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:

  • 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
Q

Corticosteroids Inhaled ADR

A

Thrush (Oral candidiasis)
- counsel patients to rinse mouth after each use

Dysphonia, sore throats cough

29
Q

Corticosteroids Oral ADR

A 
Adrenal suppression
cushing syndrome 
growth retardation
osteoporosis
glucose intolerance
infection risk
mood changes
weight gain
edema
30
Q

Beclomethasone

A

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
Q

Budesonide

A

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
Q

Fluticasone propionate

A

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
Q

Fluticasone furoate

A

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
Q

Mometasone

A

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
Q

Flunisolide

A

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
Q

Ciclesonide

A

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
Q

Prednisone

A

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
Q

Prednisolone

A

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
Q

Methylprednisolone

A

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
Q

Hydrocortisone

A

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
Q

Zileuton

A

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
Q

Montelukast

A

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
Q

Zafirlukast

A

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
Q

Cromolyn Sodium

A

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
Q

Nedocromil sodium

A

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
Q

Omalizumab

A

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
Q

Mepolizumab

A

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
Q

Reslizumab

A

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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