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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
theophylline bronchodilator therapeutic range
5 - 15 mcg/mL
26
theophylline toxic concentration
> 20 mcg/mL
27
Aminophylline MOA
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)
28
ICS
Budesonide, Beclomethasone, Fluticasone (only inhaled form available), and Mometasone
29
ICS clinical indications
used to treat acute and/or persistent mild to severe asthma and COPD
30
ICS MOA
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
31
ICS adverse effects
cough, cataracts, thrush, hoarseness, HPA suppression, growth suppression, and reduction in bone density
32
OCS/systemic corticosteroids clinical indications
used primarily to abort an acute asthma attack not used long-term due to adverse effects
33
OCS
methylprednisolone, prednisolone, and prednisone
34
Salmeterol MOA
long-acting beta-2 agonist (LABA)
35
Formoterol MOA
long-acting beta-2 agonist (LABA) that is more potent and has a faster onset of action than salmeterol due to lower lipophilicity
36
difference between SABAs and LABAs
SABAs have a duration of action of approximately 4-6 hours whereas LABAs have a duration of action of approximately 12 hours
37
LABA clinical indications
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
38
Salmeterol pharmacokinetics
available in inhaler form in combination with ICS and as monotherapy in dry powder inhaler form
39
Formoterol pharmacokinetics
available in inhaler form in combination with ICS or as a nebulized solution
40
Combination LABA/ICS inhalers
Advair - salmeterol/fluticasone, Symbicort - formoterol/budesonide, and Dulera - formoterol/mometasone
41
Combivent
SABA/anticholinergic combination inhaler consisting of albuterol and ipratropium
42
Cromolyn MOA
mast cell stabilizer that blocks degranulation preventing the release of histamine and related mediators
43
Cromolyn clinical indications
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
44
Omalizumab MOA
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
45
Omalizumab clinical indications
used to control severe allergic forms of asthma that are steroid-resistant (expensive)
46
Omalizumab adverse effects
anaphylaxis and significantly increased risk of stroke and MI (by 60%)
47
treatment of mild to moderate asthma exacerbations
initiate SABA (4-10 puffs by pMDI + spacer every 20 minutes for 1 hour), prednisone, and oxygen therapy if below 93%
48
treatment of severe asthma exacerbations
transfer to an acute care facility and administer SABA, ipratropium, oxygen, and systemic corticosteroid in the meantime
49
asthma
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
50
COPD
a progressive chronic irreversible obstruction of the airway associated with a decrease in FEV1
51
GOLD stage 1 (mild) COPD
patients with FEV1 greater than or equal to 80% predicted value
52
GOLD stage 2 (moderate) COPD
patients with FEV1 less than 80% predicted value
53
GOLD stage 3 (severe) COPD
patients with FEV1 less than 50% predicted value
54
GOLD stage 4 (very severe) COPD
patients with FEV1 less than 30% predicted value
55
first-line treatment of COPD
LABA or LAMA monotherapy (or LABA + LAMA or LABA + LAMA + ICS if dyspnea not controlled with monotherapy)
56
treatment of COPD exacerbations
If already on LABA + LAMA + ICS then add azithromycin + OCS
57
Ipratropium MOA
short-acting muscarinic antagonist (SAMA) that causes relaxation of bronchial smooth muscle and blocks mucous production
58
Ipratropium clinical indications
used in the management of COPD and asthma specifically to block cholinergic (vagal) mediated bronchospasm and mucous production
59
Ipratropium adverse effects
overall well tolerated but can cause local and systemic anticholinergic effects, xerostomia, and urinary retention
60
Tiotropium MOA
long-acting muscarinic antagonist (LAMA) that causes relaxation of bronchial smooth muscle and blocks mucous production
61
Tiotropium clinical indications
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
location of cough receptors
larynx and supralaryngeal area, trachea and bronchi, ear canals and eardrums, pleura, pericardium, and diaphragm, esophagus, and stomach
63
location of cough center
medulla and nucleus tractus solitarius
64
cough center stimulation of the spinal motor nerve leads to activation of
expiratory muscles and pelvic sphincters
65
cough center stimulation of the phrenic nerve leads to activation of
the diaphragm
66
cough center stimulation of the vagus nerve leads to activation of
the larynx, trachea, and bronchi
67
pathophysiology of cough
a defense mechanism of the respiratory system in response to irritants
68
Dextromethorphan MOA
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
Dextromethorphan clinical indications
used to relieve short-term cough
70
Dextromethorphan drug interactions
can cause serotonin syndrome if combined with MAOIs and SSRIs/SNRIs
71
Dextromethorphan adverse effects
mild and infrequent dizziness and drowsiness, hallucinogenic state at very high doses (when used recreationally), and serotonergic effects
72
Dextromethorphan contraindications
chronic cough, hepatic disease (hepatically metabolized), when operating machinery
73
Codeine MOA
thought to be centrally acting antitussive that suppresses cough reflex (without evidence to support this) and dries out bronchial secretions
74
Codeine clinical indications
used to relieve short-term cough
75
Codeine drug interactions
other opioids as it can lead to sedation and respiratory depression
76
Codeine pharmacokinetics
converted to morphine in the liver via cytochrome P450
77
Codeine adverse effects
tolerance, respiratory depression, sedation, nausea/vomiting, potential for abuse, pruritis
78
Codeine contraindications
ileus, respiratory depression, head injury, seizures, and hepatic failure
79
Benzonatate MOA
peripherally acting antitussive that anesthetizes stretch receptors of vagal afferent fibers in the lungs reducing the urge to cough after deep inhalation
80
Benzonatate clinical indications
primarily used to treat chronic cough but sometimes can be used for acute cough with variable success
81
Benzonatate drug interactions
can have an additive effect with other local anesthetics
82
Benzonatate adverse effects
pretty well tolerated but can cause GI upset and local anesthesia from chewing, overdose can cause cardiac arrhythmia, seizure, and bronchospasm
83
Benzonatate contraindications
patients with allergy to ester anesthetics
84
Guaifenesin MOA
an expectorant that loosens secretions to allow a more productive cough that increases volume and reduces viscosity of phlegm in trachea and bronchi
85
Guaifenesin clinical indications
a very common ingredient in cough syrups and is used to treat acute cough (available in syrups and pill form)
86
Guaifenesin contraindications
patients with chronic cough and in pediatrics due to increased risk of seizures
87
Guaifenesin adverse effects
excessive use can result in nephrolithiasis or kidney stones
88
Histamine is produced by
mast cells and basophils
89
cause of histamine release
immunologic trigger or a mechanical or chemical stimulus
90
general effects of histamine release
local vasodilation, transudation of fluid through endothelial cells, stimulation of nerve endings producing pain and itching
91
organ-specific effects of histamine release
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
First generation antihistamines
Diphenhydramine - Benadryl and Hydroxyzine - Vistaril or Atarax
93
Second generation antihistamine
Cetirizine - Zyrtec, Loratadine - Claritin, and Fexofenadine
94
First generation antihistamine pharmacokinetics
quick acting with the duration of action being ~ 6 hours
95
First generation antihistamine adverse effects
avoid in elderly, can cause delirium, dizziness, urinary retention
96
Cetirizine pharmacokinetics
crosses blood-brain-barrier a little
97
Cetirizine clinical indications
DOC used to treat itching and hives, available in 24-hour non-drowsy formulation
98
Cetirizine adverse effects
some drowsiness
99
Hydroxyzine clinical indications
used to treat allergic rhinitis as well as anxiety
100
Azelastine MOA
intranasal antihistamine indicated for allergic rhinitis in adults and children > 12 years old
101
Azelastine adverse effects
nosebleeds (epistaxis), headaches, somnolence, and poor taste
102
Olopatadine MOA
intranasal antihistamine with same indications as azelastine
103
Pseudoephedrine MOA
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
Pseudoephedrine clinical indications
available behind the counter and used to treat acute nasal congestion, sinusitis, and otitis media
105
Pseudoephedrine adverse effects
increases heart rate and contractability
106
Pseudoephedrine contraindications
in patients with heart disease, severe hypertension, or uncontrolled diabetes
107
Phenylephrine MOA
a sympathomimetic that is an alpha-1 adrenergic receptor agonist that causes vasoconstriction
108
Phenylephrine clinical indications
available in oral or intranasal preparations but less effective than pseudoephedrine for the treatment of nasal congestion and rhinitis symptoms (efficacy is questionable)
109
Phenylephrine adverse effects
increases systolic and diastolic blood pressure and induces reflex bradycardia
110
Phenylephrine contraindications
combination with ACE inhibitors or CCBs can increase clearance making it less effective
111
Phenylephrine drug interactions
MAOIs and TCAs can increase its concentration
112
Oxymetazoline (Afrin) MOA
long-acting topical or intranasal decongestant with duration of action ~ 12 hours
113
Oxymetazoline (Afrin) clinical indications
used to treat acute rhinitis caused by the common cold for maximum of 3 days
114
Oxymetazoline (Afrin) adverse effects
use longer than duration of 3 days can cause rebound congestion
115
Intranasal fluticasone (Flonase) MOA
glucocorticoid receptor agonist that causes vasoconstriction and inhibits the effects of cells and mediators of inflammation
116
Flonase clinical indications
used for the treatment and prevention of allergic rhinitis and the treatment of nasal polyps, not indicated for treating acute upper respiratory infections
117
Flonase adverse effects
epistaxis and pharyngitis, systemic absorption of the steroid is possible
118
Intermittent asthma symptoms
2 days per week or less
119
Mild persistent asthma symptoms
more than 2 days per week but less than daily
120
Moderate persistent asthma symptoms
symptoms daily
121
Severe persistent asthma symptoms
symptoms several times daily
122
Intermittent asthma nighttime awakenings
2 times per month or less (treat with step 1)
123
Moderate persistent asthma nighttime awakenings
3-4 times per month
124
Moderate persistent asthma nighttime awakenings
4 or more times per month but less than nightly (treat with step 3)
125
Severe persistent asthma nighttime awakenings
often nightly (treat with step 4 or 5)
126
Step 1 asthma treatment
SABA (Albuterol) prn
127
Step 2 asthma treatment
SABA prn plus low-dose ICS
128
Step 3 asthma treatment
SABA prn plus low-dose ICS and LABA/medium-dose ICS
129
Step 4 asthma treatment
SABA prn plus medium-dose ICS and LABA
130
Step 5 asthma treatment
SABA prn plus high-dose ICS and LABA (also consider adding on Omalizumab for patients with allergies or tiotropium)
131
Step 6 asthma treatment
SABA prn plus high-dose ICS plus LABA plus OCS (also consider adding on Omalizumab or tiotropium)
132
Mild or Category A COPD
few symptoms, low risk with FEV1/FVC ratio < 0.7 and FEV1 _> 80% predicted
133
Moderate or Category B COPD
increased symptoms, low risk with FEV1/FVC ration < 0.7 and FEV1 50%-79% predicted
134
Severe or Category C COPD
few symptoms, high risk with FEV1/FVC ration < 0.7 and FEV1 30%-49%
135
Very Severe or Category D COPD
increased symptoms, high risk with FEV1/FVC ratio < 0.7 and FEV1 < 30%
136
Mild COPD treatment
SABA for symptom control and consider LAMA or LABA
137
Moderate COPD treatment
SABA for symptom control plus LAMA or LABA
138
Severe COPD treatment
SABA for symptom control plus LAMA
139
Very severe COPD treatment
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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