Pulm Pharmacotherapeutics Flashcards

1
Q

Short Acting Beta Agonists

A

● Albuterol (ProAir, Proventil, Ventolin)
● Levalbuterol (Xopenex)
● Terbutaline

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2
Q

Short Acting Beta Agonists MOA

A

○ Stimulate Beta-2 adrenergic receptors
in muscularis of bronchioles.
○ Results in relaxation with
bronchodilation of the airway.
○ Acts within 5 minutes and has a
duration of 3-4 hours.

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3
Q

Indications for SABAs:

A

○ Relief of bronchospasm from any cause
■ Asthma
■ Chronic Obstructive Pulmonary Disease
■ Anaphylaxis
■ Exercise-induced bronchospasm
○ Terbutaline has an off-label use of Tocolysis

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4
Q

Contraindications of SABAs:

A

No significant contraindications. Because severe bronchospasm can be life-threatening, the benefits usually outweigh risks

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5
Q

Black Box Warning for Terbutaline

A

■ PO Terbutaline is not approved for and should not be used for
acute or maintenance tocolysis. Injectable Terbutaline should not
be used for prolonged tocolysis. Serious reactions, including
cardiac arrhythmias, pulm edema, MI, and death have occurred.

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6
Q

Minor Side Effects of SABAs

A

○ All side effects are related to overstimulation
of Beta-2 and Beta-1 receptors (sympathetic).
■ Tremor is most common
■ Others: Tachycardia, palpitations,
hypokalemia, hyperglycemia

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7
Q

Major Adverse Reactions SABAs

A

On rare occasion, SABAs have been associated with…
■ Paradoxical bronchospasm
■ Significant hypertension
■ Arrhythmias
■ Cardiac arrest

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8
Q

If Pt is requiring SABA more than 2 x per week, ____

A

needs ICS

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9
Q

Long Acting Beta Agonists

A

● Formoterol (Foradil, Perforomist)
● Salmeterol (Serevent)
● Arformoterol (Brovana

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10
Q

Long Acting Beta Agonists MOA

A

○ Stimulate Beta-2 adrenergic receptor
in muscularis of bronchioles.
○ Results in relaxation with
bronchodilation of the airway.
○ Acts within 15-20 minutes and has a
duration of > 12 hours.

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11
Q

Long Acting Beta Agonists Indications

A

○ Salmeterol, Foroterol and Arfomoterol are indicated for: COPD
maintenance, as well as prevention of Exercised-Induced
Bronchospasm and Asthma

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12
Q

Black Box Warning (BBW) for LABAs

A

○ LABAs have been shown to increase risk of death in asthma patients when used as monotherapy or when used regularly in
asthma maintenance

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13
Q

Long Acting Beta Agonists contraindications

A

○ Asthma monotherapy or acute asthma exacerbation
○ Otherwise, same cautions as SABAs-
■ Caution in patients in whom tachycardia is undesirable

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14
Q

Minor Side Effects and Major Adverse Reactions of LABAs

A

○ Same as SABAs
○ Plus increased risk of asthma-death if used as
monotherapy or rescue medication as previously stated

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15
Q

LABAs are considered one of the mainstays of
_____

A

COPD maintenance from GOLD class 2 -4

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16
Q

Inhaled Corticosteroids

A

● Budesonide (Pulmicort)
● Fluticasone (Flovent)
● Flunisolide (Aerospan)
● Beclomethasone (QVAR)
● Mometasone (Asmanex)

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17
Q

Inhaled Corticosteroids MOA

A

○ Inhibits or decreases localized
inflammation by blocking
phospholipase A2, a precursor to
arachidonic acid (the precursor to
leukotrienes and prostaglandins)

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18
Q

Inhaled Corticosteroids Indications

A

○ Long-term Asthma maintenance
■ Reduces frequency and severity of exacerbations
○ Maintenance of COPD in GOLD class 3-4.
■ Always used in combo with LABA, not monotherapy

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19
Q

Inhaled Corticosteroids Contraindications

A

○ Not to be used as acute asthma rescue
medication
○ Caution in any significant pulmonary
infection (such as TB)

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20
Q

ICS minor side effects

A

○ Systemic side effects are uncommon because of low systemic
absorption (compared to oral corticosteroids)
■ Very little if any effect on blood glucose levels
○ Oral Candidiasis (Thrush)
○ Hoarseness of voice
○ Sore throat
○ Headaches are common

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21
Q

Major Adverse Reactions of ICS

A

○ Bronchospasm sometimes occurs
○ If used at high doses for several years, may see Osteoporosis
○ Some studies have connected ICSs with stunted growth in young
children using an ICS long-term. However, asthma itself can
cause stunted growth

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22
Q

____ is drug of choice for Asthma in pregnancy

A

Budesonide

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23
Q

Inhaled Anticholinergics

A

● Ipratropium (Atrovent)
● Tiotropium (Spiriva)

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24
Q

Inhaled Anticholinergics MOA

A

○ Normal parasympathetic stimulation
of M3 and M1 muscarinic receptors results in bronchoconstriction and increased bronchial secretions
○ Anticholinergics block these receptors, thereby decreasing or preventing bronchoconstriction and reducing mucus secretions

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25
Q

Inhaled Anticholinergics Indications

A

○ COPD maintenance (another option)
○ Can also be used during acute asthma and acute COPD
exacerbations, especially in combination with Albuterol

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26
Q

Inhaled Anticholinergics Contraindications

A

should be used with caution
in patients with…
■ Glaucoma
■ Urinary retention
■ Prostatic hypertrophy

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27
Q

Combination Therapies: Fluticasone/Salmeterol

A

○ For both Asthma and COPD Maintenance

28
Q

Combination Therapies: Mometasone/Formoterol (Dulera)

A

For Asthma Maintenance

29
Q

Combination Therapies: Budesonide/Formoterol (Symbicort)

A

For both Asthma and COPD Maintenance

30
Q

Methylxanthines

A

● Theophylline
● Aminophylline
● An old class of medications that can
be very toxic but are kept around because
they are an alternative option for Asthma and
COPD, although slow workers

30
Q

Combination Therapies: Ipratropium/Albuterol (Combivent, DuoNeb)

A

For both Asthma and COPD Exacerbations

31
Q

Methylxanthines MOA

A

○ MOA is not well understood. Theories:
■ Inhibition of Phosphodiesterase (the
enzyme that degrades cAMP).
Increased cAMP can cause
bronchodilation
■ Inhibition of intracellular calcium,
thereby decreasing smooth muscle
contraction
■ Competitive antagonist of adenosine
on the adenosine receptor

32
Q

Methylxanthines Indications

A

○ Adjunct or back up therapy for…
■ COPD exacerbation or maintenance
■ Asthma exacerbation or maintenance
○ Theophylline is more effective and available IV and PO
○ Aminophylline is not as useful and only available IV

33
Q

Methylxanthines Contraindications

A

○ Active or symptomatic coronary artery disease
■ These increase the force and speed of cardiac contraction
■ This in turn impairs the coronary oxygen-supply and demand
○ Caution in any significant medical comorbidities

34
Q

Methylxanthines Minor side effects/Major adverse reactions

A

○ Adverse reactions are common because of the unpredictability of serum levels and a very narrow therapeutic index
■ GI: Nausea, vomiting, diarrhea
■ CNS: Headaches, seizures
■ Stimulatory effects: Insomnia, tremor, restlessness
■ Cardiovascular: Arrhythmias, ischemia, hypotension, shock
■ Kidneys: Excessive diuresis with dehydration

35
Q

Other Anti-Inflammatories include:

A

○ Mast Cell Stabilizer: Cromolyn (Intal)
○ Leukotriene Receptor Antagonists:
■ Montelukast (Singulair)
■ Zafirlukast (Accolate)
○ Leukotriene Synthesis Inhibitor: Zileuton (Zyflo)
○ Monoclonal Antibody: Omalizumab (Xolair)

36
Q

Mast Cell Stabilizer

A

Cromolyn Inhaled (Intal)- nebulizer

37
Q

Mast Cell Stabilizer MOA

A

○ Degranulation of mast cells in response to an allergen releases proinflammatory cytokines such as Histamine, Leukotrienes, etc.
○ Cromolyn stabilizes mast cells, preventing
release of this cytokines

38
Q

Mast Cell Stabilizer indications

A

○ Maintenance of Allergy-related Asthma
■ An alternative daily med (although not as effective as ICS)

39
Q

Mast Cell Stabilizer Contraindications

A

○ Acute asthma exacerbation (this is not a rescue medication)

40
Q

Leukotriene Receptor Antagonists

A

● Montelukast (Singulair)
● Zafirlukast (Accolate)

41
Q

Leukotriene Receptor Antagonists MOA

A

○ Leukotriene (LT) receptors exert
several effects commonly associated
with asthma (bronchoconstriction,
mucosal edema, mucus secretion)
○ LT receptor antagonists selectively
block the receptors from being
bound by LT, thereby preventing
bronchoconstriction and secretions

42
Q

Leukotriene Receptor Antagonists Indications

A

○ Both Montelukast and Zafirlukast:
Asthma maintenance
○ Montelukast only:
■ Prevention of exercise-induced
bronchospasm
■ Allergic Rhinitis

43
Q

Leukotriene Receptor Antagonists contraindications

A

○ Acute asthma attack- these are
not rescue medications

44
Q

Leukotriene Receptor Antagonists adverse reactions

A

○ Although rare, LT receptor antagonists are a possible cause of
Churg-Strauss Syndrome
■ An allergic granulomatosis, form of vasculitis
○ Zafirlukast can cause hepatitis or hepatic failure

45
Q

Leukotriene Receptor Antagonists follow up

A

○ Caution is advised during pregnancy for both medications
■ Montelukast has a mild risk of congenital limb defects
■ Zafirlukast has no known risk for teratogenicity
○ If taking Zafirlukast, consider monitoring LFTs regularly

46
Q

Leukotriene Synthesis Inhibitor MOA

A

● Mechanism of Action:
○ Inhibits the enzyme 5-Lipoxygenase,
which is the enzyme that catalyzes
formation of Leukotrienes
○ Prevents binding of LT receptors by
preventing creation of LT

47
Q

Leukotriene Synthesis Inhibitor

A

● Zileuton (Zyflo)
○ A relatively new PO medication. Costs up to $3,800/month

48
Q

Leukotriene Synthesis Inhibitor Indications

A

○ An alternative for Asthma
Maintenance (Step 3 and 4 protocol)

49
Q

Leukotriene Synthesis Inhibitor contraindications

A

○ Active liver disease
○ Caution if acute asthmathis is not a rescue
medication

50
Q

Leukotriene Synthesis Inhibitor adverse reactions

A

○ Hepatotoxicity, liver failure
■ Elevated LFTs are common, but full hepatotoxicity is rare
○ Behavior problems (i.e. - aggression) are possible

51
Q

Monoclonal Antibody

A

Omalizumab (Xolair) - A subcutaneous injection
administered every 2-4 weeks (about $2580 each)

52
Q

Monoclonal Antibody MOA

A

○ A recombinant humanized
mouse monoclonal antibody
○ Binds to free IgE, which prevents it from binding to mast cells and other WBCs,
thereby decreasing allergic
inflammation

53
Q

Monoclonal Antibody indications

A

○ Alternative to maintenance of moderate to severe persistent
Allergic-type Asthma
■ An appropriate alternative in Step 5 and 6 protocol

54
Q

Monoclonal Antibody BBW

A

Anaphylaxis has occurred after first dose,
and even after 1 year on treatment. Caution
is advised. Educate patients as well

55
Q

Monoclonal Antibody side effects

A

○ Localized injection-site reactions
○ Some get nausea, myalgias, headaches, URI-like symptoms

56
Q

Monoclonal Antibody adverse reactions

A

○ Anaphylaxis
○ Possible Churg-Strauss
Syndrome
○ Cerebrovascular event
○ Cardiovascular event
○ Increased risk of malignancy

57
Q

Other Rescue Medications

A

● Epinephrine is an adjunct therapy that is sometimes administered
to a patient in severe respiratory distress secondary to asthma
(“silent chest”)
○ Can cause bronchodilation
● PO (and occasionally IV) Corticosteroids are also used

58
Q

Antitussives

A

● Benzonatate (Tessalon)
● Dextromethorphan

59
Q

Antitussives MOA

A

○ Dextromethorphan acts centrally by
inhibiting the cough center of the
brain, elevating the threshold for
initiation of a cough
○ Benzonatate acts peripherally, works
by anesthetizing the local nerve
endings of the cough receptors.
Decreasing cough reflex

60
Q

Antitussives Contraindications

A

○ None of significance for Benzonatate
○ Dextromethorphan should not be taken
within 14 days of a MAO inhibitor

61
Q

Antitussives Adverse reactions

A

○ Dextromethorphan can be abused, so prescribe with caution
○ If taken with MAO inhibitors, can develop Serotonin Syndrome

62
Q

Expectorant

A

● Guaifenesin- OTC medication often in combo “cold” pills.

63
Q

Expectorant MOA

A

○ Increase the amount of fluid in the airway tract, which
increases the flow and clearance of local irritants, as well as
reducing the viscosity of mucus that has built up in airways.

64
Q

Expectorant Indications

A

○ Loosening of mucus in chest congestion (and URIs)

65
Q

Expectorant Adverse reactions

A

○ Possible cause of kidney stones with chronic use