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Pharmacology II > Respiratory System Drugs > Flashcards

Respiratory System Drugs Flashcards

1
Q

Target area in respiratory system for drugs

A

conducting zone which includes the trachea, bronchi, and bronchioles

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2
Q

Conducting zone

A

area of the respiratory tree that contains sympathetic adrenergic neurons which activate beta-2 receptors, parasympathetic cholinergic neurons which activate muscarinic receptors, mucus-secreting (goblet) cells, and ciliated cells that remove inhaled particles

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3
Q

Albuterol MOA

A

short-acting beta-2 agonist (SABA) that leads to the activation of adenylate cyclase and an increase in intracellular concentration of cyclic AMP causing activation of protein kinase A which inhibits the phosphorylation of myosin and lowers intracellular concentration of calcium resulting in smooth muscle relaxation

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4
Q

beneficial effects of Albuterol

A

relieves bronchospasm, reduces airway resistance, facilitates mucous drainage, and increases vital capacity

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5
Q

Albuterol clinical indications

A

used in the management of acute bronchospasm in asthma and other chronic obstructive airway diseases

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6
Q

Albuterol adverse effects

A

sympathomimetic effects such as tachycardia, hyperglycemia, hypokalemia, tremor, and paradoxical bronchospasm

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7
Q

Metaproterenol MOA

A

moderately selective beta-2 agonist with slow onset of action

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8
Q

Metaproterenol clinical indications

A

available in an inhaled or oral form (oral form only in USA) as an alternative to Albuterol but is not recommended for routine use given its slow onset of action

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9
Q

Levalbuterol MOA

A

short-acting beta-2 agonist deemed inferior to albuterol for the management of acute asthma symptoms

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10
Q

Role of leukotrienes

A

chemoattractant for eosinophils and neutrophils that constrict bronchiolar smooth muscle, increase endothelial permeability, and promote mucous secretion

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11
Q

Zafirlukast MOA

A

first FDA-approved leukotriene receptor antagonist

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12
Q

Zafirlukast clinical indications

A

used orally in the prophylaxis and treatment of asthma, allergic rhinitis, and exercise-induced bronchospasm - generally thought of as less effective than inhaled glucocorticoids for the management of persistent asthma but often preferred for the treatment of asthma in kids because it is steroid-sparing

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13
Q

Zafirlukast contrindications

A

phenylketonuria and hepatic disease

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14
Q

Montelukast MOA

A

leukotriene receptor antagonist

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15
Q

Montelukast clinical indications

A

more commonly prescribed than Zafirlukast (possibly due to its availability as a generic drug) usually added on after initiation of ICS in adults for the prophylaxis and treatment of asthma, allergic rhinitis, and exercise-induced bronchospasm

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16
Q

Montelukast contraindications

A

phenylketonuria and hepatic disease

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17
Q

Zileuton MOA

A

inhibitor of 5-lipoxygenase which inhibits the synthesis of leukotrienes

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18
Q

Zileuton clinical indications

A

used in the management of chronic asthma only but infrequently used due to needing to be dosed 4 times daily

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19
Q

Zileuton adverse effects

A

elevation of liver enzymes and interferes with CYP metabolism

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20
Q

Theophylline MOA

A

a methylxanthine that is a competitive nonselective phosphodiesterase inhibitor that raises intracellular cAMP, activates PKA, inhibits TNF-alpha, and inhibits leukotriene synthesis leading to reduced inflammation and innate immunity and also works as a nonselective adenosine receptor antagonist leading to increased HR, inotropy, and BP

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21
Q

Theophylline clinical indications

A

used both orally and IV as an alternative treatment for asthma, bronchospasm, COPD, and infant apnea

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22
Q

Theophylline adverse effects

A

has a narrow therapeutic window and toxic side effects including heart arrhythmias, CNS excitation, insomnia, seizures, nausea, and diarrhea

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23
Q

Theophylline drug-drug interactions

A

fluoroquinolones, erythromycin, and some SSRIs

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24
Q

Theophylline monitoring parameters

A

LFTs, PFTs, and serum theophylline concentrations

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25
Q

theophylline bronchodilator therapeutic range

A

5 - 15 mcg/mL

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26
Q

theophylline toxic concentration

A

> 20 mcg/mL

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27
Q

Aminophylline MOA

A

a compound of theophylline with ethylenediamine with the same MOA as theophylline but less potent and shorter-acting than theophylline (only available outside of the USA)

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28
Q

ICS

A

Budesonide, Beclomethasone, Fluticasone (only inhaled form available), and Mometasone

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29
Q

ICS clinical indications

A

used to treat acute and/or persistent mild to severe asthma and COPD

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30
Q

ICS MOA

A

Inhibit phospholipase A and the synthesis of arachidonic acid suppressing the inflammatory and immune response and reducing edema and secretions by controlling the rate of protein synthesis, depressing the migration of PMNs and fibroblasts, and reversing capillary permeability and lysosomal stabilization at the cellular level

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31
Q

ICS adverse effects

A

cough, cataracts, thrush, hoarseness, HPA suppression, growth suppression, and reduction in bone density

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32
Q

OCS/systemic corticosteroids clinical indications

A

used primarily to abort an acute asthma attack not used long-term due to adverse effects

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33
Q

OCS

A

methylprednisolone, prednisolone, and prednisone

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34
Q

Salmeterol MOA

A

long-acting beta-2 agonist (LABA)

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35
Q

Formoterol MOA

A

long-acting beta-2 agonist (LABA) that is more potent and has a faster onset of action than salmeterol due to lower lipophilicity

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36
Q

difference between SABAs and LABAs

A

SABAs have a duration of action of approximately 4-6 hours whereas LABAs have a duration of action of approximately 12 hours

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37
Q

LABA clinical indications

A

used in the management of asthma and prevention of asthma attacks and exercise-induced bronchoconstriction and in COPD management - CAN NOT be used as monotherapy in the treatment of asthma but only in combination with ICS which is synergistic

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38
Q

Salmeterol pharmacokinetics

A

available in inhaler form in combination with ICS and as monotherapy in dry powder inhaler form

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39
Q

Formoterol pharmacokinetics

A

available in inhaler form in combination with ICS or as a nebulized solution

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40
Q

Combination LABA/ICS inhalers

A

Advair - salmeterol/fluticasone, Symbicort - formoterol/budesonide, and Dulera - formoterol/mometasone

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41
Q

Combivent

A

SABA/anticholinergic combination inhaler consisting of albuterol and ipratropium

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42
Q

Cromolyn MOA

A

mast cell stabilizer that blocks degranulation preventing the release of histamine and related mediators

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43
Q

Cromolyn clinical indications

A

formerly was the non-steroid inhaled medication of choice for asthma treatment prior to development of leukotriene receptor antagonists that is now used infrequently due to needing to be dosed four times daily

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44
Q

Omalizumab MOA

A

a recombinant DNA-derived humanized IgG1k monoclonal antibody that specifically binds to free human IgE in the blood and interstitial fluid as well as membrane-bound forms of IgE on the surface of B lymphocytes

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45
Q

Omalizumab clinical indications

A

used to control severe allergic forms of asthma that are steroid-resistant (expensive)

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46
Q

Omalizumab adverse effects

A

anaphylaxis and significantly increased risk of stroke and MI (by 60%)

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47
Q

treatment of mild to moderate asthma exacerbations

A

initiate SABA (4-10 puffs by pMDI + spacer every 20 minutes for 1 hour), prednisone, and oxygen therapy if below 93%

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48
Q

treatment of severe asthma exacerbations

A

transfer to an acute care facility and administer SABA, ipratropium, oxygen, and systemic corticosteroid in the meantime

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49
Q

asthma

A

chronic inflammation of airways causing contraction of bronchial smooth muscle, acute bronchospasm, and increased secretion of mucous characterized by inability to get enough CO2 out

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50
Q

COPD

A

a progressive chronic irreversible obstruction of the airway associated with a decrease in FEV1

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51
Q

GOLD stage 1 (mild) COPD

A

patients with FEV1 greater than or equal to 80% predicted value

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52
Q

GOLD stage 2 (moderate) COPD

A

patients with FEV1 less than 80% predicted value

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53
Q

GOLD stage 3 (severe) COPD

A

patients with FEV1 less than 50% predicted value

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54
Q

GOLD stage 4 (very severe) COPD

A

patients with FEV1 less than 30% predicted value

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55
Q

first-line treatment of COPD

A

LABA or LAMA monotherapy (or LABA + LAMA or LABA + LAMA + ICS if dyspnea not controlled with monotherapy)

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56
Q

treatment of COPD exacerbations

A

If already on LABA + LAMA + ICS then add azithromycin + OCS

57
Q

Ipratropium MOA

A

short-acting muscarinic antagonist (SAMA) that causes relaxation of bronchial smooth muscle and blocks mucous production

58
Q

Ipratropium clinical indications

A

used in the management of COPD and asthma specifically to block cholinergic (vagal) mediated bronchospasm and mucous production

59
Q

Ipratropium adverse effects

A

overall well tolerated but can cause local and systemic anticholinergic effects, xerostomia, and urinary retention

60
Q

Tiotropium MOA

A

long-acting muscarinic antagonist (LAMA) that causes relaxation of bronchial smooth muscle and blocks mucous production

61
Q

Tiotropium clinical indications

A

used in the management of COPD specifically to block cholinergic (vagal) mediated bronchospasm and mucous production that is longer acting compared to ipratropium (only needs to be dosed once daily)

62
Q

location of cough receptors

A

larynx and supralaryngeal area, trachea and bronchi, ear canals and eardrums, pleura, pericardium, and diaphragm, esophagus, and stomach

63
Q

location of cough center

A

medulla and nucleus tractus solitarius

64
Q

cough center stimulation of the spinal motor nerve leads to activation of

A

expiratory muscles and pelvic sphincters

65
Q

cough center stimulation of the phrenic nerve leads to activation of

A

the diaphragm

66
Q

cough center stimulation of the vagus nerve leads to activation of

A

the larynx, trachea, and bronchi

67
Q

pathophysiology of cough

A

a defense mechanism of the respiratory system in response to irritants

68
Q

Dextromethorphan MOA

A

a centrally acting antitussive that crosses the blood-brain-barrier and activates sigma opioid receptors on the cough center in the medulla thereby suppressing the cough reflex, it does not affect ciliary activity in the bronchial tree

69
Q

Dextromethorphan clinical indications

A

used to relieve short-term cough

70
Q

Dextromethorphan drug interactions

A

can cause serotonin syndrome if combined with MAOIs and SSRIs/SNRIs

71
Q

Dextromethorphan adverse effects

A

mild and infrequent dizziness and drowsiness, hallucinogenic state at very high doses (when used recreationally), and serotonergic effects

72
Q

Dextromethorphan contraindications

A

chronic cough, hepatic disease (hepatically metabolized), when operating machinery

73
Q

Codeine MOA

A

thought to be centrally acting antitussive that suppresses cough reflex (without evidence to support this) and dries out bronchial secretions

74
Q

Codeine clinical indications

A

used to relieve short-term cough

75
Q

Codeine drug interactions

A

other opioids as it can lead to sedation and respiratory depression

76
Q

Codeine pharmacokinetics

A

converted to morphine in the liver via cytochrome P450

77
Q

Codeine adverse effects

A

tolerance, respiratory depression, sedation, nausea/vomiting, potential for abuse, pruritis

78
Q

Codeine contraindications

A

ileus, respiratory depression, head injury, seizures, and hepatic failure

79
Q

Benzonatate MOA

A

peripherally acting antitussive that anesthetizes stretch receptors of vagal afferent fibers in the lungs reducing the urge to cough after deep inhalation

80
Q

Benzonatate clinical indications

A

primarily used to treat chronic cough but sometimes can be used for acute cough with variable success

81
Q

Benzonatate drug interactions

A

can have an additive effect with other local anesthetics

82
Q

Benzonatate adverse effects

A

pretty well tolerated but can cause GI upset and local anesthesia from chewing, overdose can cause cardiac arrhythmia, seizure, and bronchospasm

83
Q

Benzonatate contraindications

A

patients with allergy to ester anesthetics

84
Q

Guaifenesin MOA

A

an expectorant that loosens secretions to allow a more productive cough that increases volume and reduces viscosity of phlegm in trachea and bronchi

85
Q

Guaifenesin clinical indications

A

a very common ingredient in cough syrups and is used to treat acute cough (available in syrups and pill form)

86
Q

Guaifenesin contraindications

A

patients with chronic cough and in pediatrics due to increased risk of seizures

87
Q

Guaifenesin adverse effects

A

excessive use can result in nephrolithiasis or kidney stones

88
Q

Histamine is produced by

A

mast cells and basophils

89
Q

cause of histamine release

A

immunologic trigger or a mechanical or chemical stimulus

90
Q

general effects of histamine release

A

local vasodilation, transudation of fluid through endothelial cells, stimulation of nerve endings producing pain and itching

91
Q

organ-specific effects of histamine release

A

bronchoconstriction in the lungs, contraction of smooth muscle in GI tract, and potent stimulation of gastric acid, pepsin, and intrinsic factor secretion in the GI tract, brain-neurotransmitter

92
Q

First generation antihistamines

A

Diphenhydramine - Benadryl and Hydroxyzine - Vistaril or Atarax

93
Q

Second generation antihistamine

A

Cetirizine - Zyrtec, Loratadine - Claritin, and Fexofenadine

94
Q

First generation antihistamine pharmacokinetics

A

quick acting with the duration of action being ~ 6 hours

95
Q

First generation antihistamine adverse effects

A

avoid in elderly, can cause delirium, dizziness, urinary retention

96
Q

Cetirizine pharmacokinetics

A

crosses blood-brain-barrier a little

97
Q

Cetirizine clinical indications

A

DOC used to treat itching and hives, available in 24-hour non-drowsy formulation

98
Q

Cetirizine adverse effects

A

some drowsiness

99
Q

Hydroxyzine clinical indications

A

used to treat allergic rhinitis as well as anxiety

100
Q

Azelastine MOA

A

intranasal antihistamine indicated for allergic rhinitis in adults and children > 12 years old

101
Q

Azelastine adverse effects

A

nosebleeds (epistaxis), headaches, somnolence, and poor taste

102
Q

Olopatadine MOA

A

intranasal antihistamine with same indications as azelastine

103
Q

Pseudoephedrine MOA

A

a sympathomimetic that is an alpha and beta-2 adrenergic receptor agonist that causes direct stimulation of alpha receptors of the respiratory mucosa resulting in vasoconstriction and stimulation of beta-2 receptors resulting in bronchodilation, this reduces tissue hyperemia, edema, and nasal congestion opening blocked eustachian tubes

104
Q

Pseudoephedrine clinical indications

A

available behind the counter and used to treat acute nasal congestion, sinusitis, and otitis media

105
Q

Pseudoephedrine adverse effects

A

increases heart rate and contractability

106
Q

Pseudoephedrine contraindications

A

in patients with heart disease, severe hypertension, or uncontrolled diabetes

107
Q

Phenylephrine MOA

A

a sympathomimetic that is an alpha-1 adrenergic receptor agonist that causes vasoconstriction

108
Q

Phenylephrine clinical indications

A

available in oral or intranasal preparations but less effective than pseudoephedrine for the treatment of nasal congestion and rhinitis symptoms (efficacy is questionable)

109
Q

Phenylephrine adverse effects

A

increases systolic and diastolic blood pressure and induces reflex bradycardia

110
Q

Phenylephrine contraindications

A

combination with ACE inhibitors or CCBs can increase clearance making it less effective

111
Q

Phenylephrine drug interactions

A

MAOIs and TCAs can increase its concentration

112
Q

Oxymetazoline (Afrin) MOA

A

long-acting topical or intranasal decongestant with duration of action ~ 12 hours

113
Q

Oxymetazoline (Afrin) clinical indications

A

used to treat acute rhinitis caused by the common cold for maximum of 3 days

114
Q

Oxymetazoline (Afrin) adverse effects

A

use longer than duration of 3 days can cause rebound congestion

115
Q

Intranasal fluticasone (Flonase) MOA

A

glucocorticoid receptor agonist that causes vasoconstriction and inhibits the effects of cells and mediators of inflammation

116
Q

Flonase clinical indications

A

used for the treatment and prevention of allergic rhinitis and the treatment of nasal polyps, not indicated for treating acute upper respiratory infections

117
Q

Flonase adverse effects

A

epistaxis and pharyngitis, systemic absorption of the steroid is possible

118
Q

Intermittent asthma symptoms

A

2 days per week or less

119
Q

Mild persistent asthma symptoms

A

more than 2 days per week but less than daily

120
Q

Moderate persistent asthma symptoms

A

symptoms daily

121
Q

Severe persistent asthma symptoms

A

symptoms several times daily

122
Q

Intermittent asthma nighttime awakenings

A

2 times per month or less (treat with step 1)

123
Q

Moderate persistent asthma nighttime awakenings

A

3-4 times per month

124
Q

Moderate persistent asthma nighttime awakenings

A

4 or more times per month but less than nightly (treat with step 3)

125
Q

Severe persistent asthma nighttime awakenings

A

often nightly (treat with step 4 or 5)

126
Q

Step 1 asthma treatment

A

SABA (Albuterol) prn

127
Q

Step 2 asthma treatment

A

SABA prn plus low-dose ICS

128
Q

Step 3 asthma treatment

A

SABA prn plus low-dose ICS and LABA/medium-dose ICS

129
Q

Step 4 asthma treatment

A

SABA prn plus medium-dose ICS and LABA

130
Q

Step 5 asthma treatment

A

SABA prn plus high-dose ICS and LABA (also consider adding on Omalizumab for patients with allergies or tiotropium)

131
Q

Step 6 asthma treatment

A

SABA prn plus high-dose ICS plus LABA plus OCS (also consider adding on Omalizumab or tiotropium)

132
Q

Mild or Category A COPD

A

few symptoms, low risk with FEV1/FVC ratio < 0.7 and FEV1 _> 80% predicted

133
Q

Moderate or Category B COPD

A

increased symptoms, low risk with FEV1/FVC ration < 0.7 and FEV1 50%-79% predicted

134
Q

Severe or Category C COPD

A

few symptoms, high risk with FEV1/FVC ration < 0.7 and FEV1 30%-49%

135
Q

Very Severe or Category D COPD

A

increased symptoms, high risk with FEV1/FVC ratio < 0.7 and FEV1 < 30%

136
Q

Mild COPD treatment

A

SABA for symptom control and consider LAMA or LABA

137
Q

Moderate COPD treatment

A

SABA for symptom control plus LAMA or LABA

138
Q

Severe COPD treatment

A

SABA for symptom control plus LAMA

139
Q

Very severe COPD treatment

A

SABA for symptom control plus LAMA or LAMA/LABA or LABA/ICS, if exacerbation add on OCS and possibly azithromycin if smoker

Pharmacology II (5 decks)

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