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N929 Pharmacology > Exam 1 Respiratory > Flashcards

Exam 1 Respiratory Flashcards

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1
Q

Airway smooth muscle extends to

A

distal terminal bronchioles

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2
Q

Airway smooth muscles are influence by

A

PSNS and SNS

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3
Q

Thoracic ganglia of the SNS innervate

A

smooth muscles of bronchi and pulmonary blood vessels

tracheobronchial blood vessels and glands

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4
Q

Sympathetic tone is

A

bronchodilation via beta 2 receptors

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5
Q

Vagus nerve of the PSNS system innervates

A

smooth muscles of bronchi

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6
Q

Beta adrenergic receptors located in the

A

smooth muscle of the blood vessels, skin muscle mesentary and bronchial smooth muscle

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7
Q

B2 adrenoreceptors cause

A

widening of airways (bronchodilation)

increase intracellular cyclic AMP

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8
Q

Nonadrenergic non-cholinergic nerves (NANC)

A

influences on inflammation and smooth muscle tone

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9
Q

M3

A

mediate bronchoconstriction via the activation of IP3 which increases the intracellular Ca2+ concentrations

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10
Q

Asthma causes recurrent episodes of

A 
wheezing
breathlessness
chest tightness
cough (night and early am)
tachypnea
prolonged expiration phase of respiration
fatigue
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11
Q

Asthma is

A

a chronic inflammatory disorder of the airways characterized by increase responsiveness of the tracheobronchial tree to a variety of stimuli

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12
Q

Asthma creates airways that are

A

inflammed, edematous
bronchial hypersensitivity/reactivity to irritant stimuli
difficult with air outflow

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13
Q

Degree of airway hyper-responsiveness and bronchoconstriction parallels

A

the extent of inflammation

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14
Q

Asthma is characterized by

A

inflammation
hyperreactivity
reversible airway obstruction

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15
Q

airway hyper-responsiveness and inflammation from allergen in bronchial mucosa leads to

A

activation of T2 lyphmocytes and cytokine release

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16
Q

Asthma medications are aimed

A

at flattening the response to the mediators

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17
Q

Asthma mediators

A 
eosinophils
mast cells
neutrophils
macrophages
basophils
T lymphocytes
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18
Q

Probably mediators of acute bronchoconstriction

A

cytokines, interleukins
arachiddonic acid metabolites, leukotrienes and prostraglandins
histamine, adenosine and platelet activating factor

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19
Q

Atopic Extrinisic asthama

A

produced by an allergen and IgE synthesis

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20
Q

COPD Factors

A 
genes
smoking
age/gender
lung growth/development
exposure to particles: cigarette smoke, occupational dust and fumes, indoor air pollution
socioeconomic status
asthma/bronchial hyperactivity
chronic bronchitis
infections
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21
Q

Neutrophils/marcophages

A

COPD

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22
Q

Esinophils/ mast cells

A

asthma

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23
Q

COPD/Emphysema/Bronchitis

A

cell death of destruction of the alveoli, thickening of membrane air gas exchange over inflated alveoli

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24
Q

Obstruction is either

A

not reversible or incompletely reversible by bronchodilators

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25
Cell death is caused by
desctruction of alveoli due to lung parenchyma, degraded matrix and toxic actions of inflammatory cells
26
COPD
results in enlargement of air spaces, fibrosis, and increase mucous production
27
Steroids have
limited effect on inflammation process
28
Inhaled corticosteroids help
reduce frequency of excerbations
29
Bronchodilators in COPD
best for patients with chronic breathlessness "worsened by exertion"
30
Steps of Airway Outflow Disorders
``` step 1: short acting bronchodilators step 2: regular inhaled corticosteroids step 3: long acting bronchodilators step 4: PDE inhibitors, methyxanthines, leukotriene inhbitor Step 5: oral corticosteroid other- cromolyns ```
31
Bronchdilators
B2 agonist anticholinergics methylxanthines
32
Receptor selectivity to B2 is ____ more times more strongly than B1
200-400
33
Short acting Beta agonist
terbutaline, albuterol, levalbuterol, salbutamol
34
Long acting beta agonist
salmeterol
35
MOA of Beta Agonist
Coupled to stimluatory G proteins activate adenlyl cyclase which increases the production of cAMP which leads to bronchodilation, reduced Ca release and alters membrane conductance inhibits mediator release from mast cells increases mucous clearance by action of the cilia
36
Pharmacokinetics of B adrenergic agonist
``` rapid onset of action (within minutes) short DOA (4-6 hours) good for use as a rescue inhaler given: inhalation/aerosol powder or nebulized orally or injected (SC) short or long acting ```
37
Side effects of Beta Adrenegic agonist
``` minimized by inhalation delivery tremor increased HR vasodilation metabolic changes (hypok, hyperg, hypomagnesmia) ```
38
Albuterol
preferred selective beta 2 agonist
39
Albuterol Dose
100mcg/puff 2 puff 4-6hrs nebulizer 2.5-5mg in 5ml of saline
40
DOA of albuterol
4 hours with some relief evident up to 8 hours
41
R albuterol has more affinity
to beta 2
42
S albuterol more affinity
to beta 1
43
Albuterol has _____ effects with volatile anesthetics on bronchomotor tone
addictive
44
Side effects of Albuterol
tachycardia, hypokalemia
45
Anesthetic use of Albuterol
4 puffs blunt airway response to tracheal intubation in asthmatic patients
46
Metaproterenol-alupent
beta 2 agonist for treatment of asthma administered via metered dose not to exceed 16 puff/day
47
Pirbuterol-Maxair
beta two agonist 2 puffs (400mcg) via metered dose not to exceed 12 inhalations/day
48
Terbutaline
administered SC,oral, inhalation treats asthma SC administration resembles epi response
49
Terbutaline SC dose for children
0.01mg/kg
50
Terbutaline SC dose for adult
0.25mg q15 min
51
Terbutaline Metered dose inhaler is and each dose is
16-20puff/day | 200mcgs
52
Long acting B agonist examples
salmeterol combination with fluticasone formoterol
53
Long acting B agonist
have liphophic side chains that resist degradtion duration 12-24 hours good for prevention not flare up
54
MOA of bronchodilators/anticholinergics
competitive antagonist at muscarinic acetylcholine receptors
55
Uses of bronchodilators/anticholinergics
treatment of COPD | secondary line of treatment for asthma in patients resistant to beta agonist or significant cardiac disease
56
Examples of Bronchodilators/Anticholinergics
atropine ipratropium bromide tiotropium
57
Atropine
naturally occuring alkaloid highly absorbed across respiratory epithelium causes systemic anticholinergic effects (tachycardia, dry mouth, nausea, Gi upset)
58
How is atropine dosed
1-2 mg diluted in 3-5 ml sof saline via nebulizer
59
Ipratropium bromide
quaternary ammonium salt derivative of atropine | antagonizes endongenous ach at m3
60
Dose of Ipratropium bromide
40-80mcg via metered dose in 2-4 puffs via nebulizer
61
DOA and onset of Ipratropium bromide
slow onset 30 minutes | DOA 4-6 hours
62
Compared to atropine, Ipratropium bromide is ____
not siginicantly absorbed
63
S/E of Ipratropium bromide
inadvertent oral absorption | dry mouth and GI upset
64
Tiotropium
quaternary ammonium salt long acting anticholinergic not significantly absorbed across resp epithelium= few side effects approved by FDA for COPD
65
COPD medications
tiotropium Ipratropium bromide atropine
66
Examples of Methylxanthines- Phosphodiesterase Inhibitors
Theophylline, Aminophylline
67
MOA of Methylxanthines
nonspecific inhibition of phosphodieterase isoenzymes (types 3 and 4) which prevent cAMP degradtion in airway smooth muscle as well as in inflammatory cells
68
PDIs have multiple MOAs and are nonselective they have
various side effects and have a narrow TI
69
theophylline
therapeutic plasma level of 10-20mcg/ml toxic at >20mcg/ml Susceptile to drug to drug interactions due to metabolism by CYP 450 (cimetidine and antifungals ie CYP 450 inhibitors)... increase level of drug metabolized in liver excreted in kidney
70
What drug do you have to caution with halothene?
theophylline
71
Side Effects of PDI
``` headache N/V irritability/restlessness insomnia cardiac arrthymias seizures SJS ```
72
Anti-Inflammatory agents
inhaled corticosteroids cromolyns leukotriene inhibitors anti- IgE antibodies
73
Examples of Inhaled corticosteroids
beclomethasone triamcinolone fluticasone budensonide
74
Pre-op Considerations with inhalated corticosteroids
may consider use of corticosteroid administration 1-2 hours preop they prolong the response of beta agonist may consider 5 day course of combined corticosteroid and albuterol to minimize the risk of intubation evoked bronchospasm
75
Inhaled corticosteroids
reduce the number of inflammatory cells in the airways and the damage to airway epithelium vascular permeability is reduced which decreases airway edema overall reduction in airway hyper-sensitivity
76
inhaled corticosteroids are considered the most
important drug in management of asthma | major preventative treatment for patients with asthma
77
MOA of Inhaled Corticosteroids
alters gene transcription increases transcription of genes for beta 2 receptor and anti-inflammatory proteins decreases transcription of genes for pro-inflammatory proteins induce apoptosis in inflammatory cells (esinophils, TH2, lymphocytes) indirect inhibition of mast cells over time reverses many ft of asthma used as suppressive therapy not a cure
78
Side Effects of Corticosteroids
``` oropharyngeal candidiasis osteopenia/osteoporosis delayed growth in children hoarseness hyperglycemia ```
79
Cromolyn
stabilizes mast cells
80
MOA of Cromolyn
inhibits antigen-induced release of histamine including release of inflammatory mediators from eosinophils, neutrophils, monocytes, macrophages, lymphocytes, and leukotrienes form pulm mast cells inhibits allergic response to antigen but not the allergic response once it has been activated
81
Administration of Cromolyn
inhalation 8-10% enters the systemic circulation | take 4x daily
82
How much inhaled dose reaches oropharynx is swallow of inhaled corticosteroids
80-90%
83
How much inhaled corticosteroid reaches airway
25%
84
Principle use of cromolyn
prophlaytic therapy of bronchial asthma
85
Cromolyn does not
relieve allergic response after initiation | not a rescue inhaler
86
S/e of cromolyn are
laryngeal edema angioedema uticaria anaphylaxis
87
Leukotriene Inhibitors
synthesized from arachidonic acid when inflammatory cells are activatd not effective in the treatment of acute asthma attacks few extrapulmonary effects
88
Leukotriene Inhibitor examples
zileuton | montelukast
89
Zileuton
lipoxygenase inhibitor which blocks the biosynthesis of leukotrienes from arachiondic acid produces bronchodilation, improves asthma symptoms and has shown long term improvements in PFTs low bioavailability, low potency and significant adverse effects hepatotoxic no widely used
90
Montelukast-singulair
leukotriene receptor antagonist block the mechanism of bronchoconstriction and smooth muscle effects blocks the ability of leukotrienes to bind to cysteinyl-leukotriene 1 receptor improve bronchial tone, pulm function, and asthma symptoms
91
Montelukast-singulair with warfin
can result in prolonged PT
92
Omalizumab
monoclonal antibody derived from DNA given in the early and late phase of asthmatic response given SC 2-4 parenterally infused high cost and incovenience binds to igE (decrease IgE circulating quantity and prevent IgE from binding to mast cell) down regulation of receptors adverse effet: triggering of immune response

N929 Pharmacology (16 decks)

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