pulm Flashcards
(107 cards)
1
Q
why is the respiratory system a good system for drug delivery?
A
rapid and efficient
2
Q
how are drugs administered through the respiratory system?
A
aerosol
and drugs are smoked
3
Q
what is an aerosol?
A
suspension of liquid or fine particles in air
4
Q
what is the advantage of an aerosol?
A
drugs can be delivered to the site of action with limited systemic effects
5
Q
is it possible for an aerosol produce significant systemic effects?
A
yes…think about meth or crack that gets smoked, addicts use the tissues of the lungs to get the drug to their brains
6
Q
most drugs that have rapid onset also have what?
A
short half life….meth is an exception. rapid onset, long half life
7
Q
what do pulmonary drugs target?
A
lungs, but can still have systemic effects
8
Q
how are aerosols delivered? (methods)
A
nebulizers
dry powder inhaler (DPI)
metered dose inhaler (MDI)
9
Q
what does a nebulizer do?
A
turns a liquid into a fine mist
10
Q
what are the common problems with aerosol therapy?
A
- difficult to determine if the correct dose is given
- can alter breathing pattern
- drugs can end up in oral mucosa, not lungs
11
Q
what are the features of asthma?
A
airway inflammation
airway hyperresponsiveness
bronchoconstriction
hyper secretions of mucus
12
Q
what is atopy?
A
inherited predisposition to allergic diseases such as asthma, allergic rhinitis, or eczema
13
Q
atopy is the underlying factor in what?
A
almost all asthma in children
most asthma in adults
14
Q
based on the drawing on slide 8, what are some features of an inflamed airway?
A
- smooth muscle layer widened due to edema
- more mucus on the surface of the airway
- plasma leakage
15
Q
what are the goals of asthma therapy?
A
- end acute bronchial constriction
- reduce inflammation
- reduce hypersecretions of mucus
16
Q
what is the overarching def. of COPD?
A
chronic obstructive pulmonary disease
-lung condition with non-reversible airflow limitation
17
Q
what are 2 examples of COPD?
A
chronic bronchitis
emphysema
18
Q
what are the treatment goals of COPD?
A
reduce inflammation
relieve bronchoconstriction
reduce risk or treat infection (infection control)
control cough
19
Q
what type of drug is used for acute bronchoconstriction?
A
beta 2 adrenergic agonists
20
Q
how do beta 2 adrenergic agonists work to reduce bronchoconstriction?
A
stimulate beta 2 receptors found in the smooth muscle of the bronchi and bronchioles, causing the muscles to relax
21
Q
what type of drug delivery is aerosol?
A
parenteral
22
Q
what are some side affects of beta 2 agonists?
A
tachycardia
nervousness
shaking
severe effects, pulmonary edema, myocardial infarction, cardiac arrhythmia.
23
Q
what is a drug that stimulates beta 1 and beta 2 receptors?
A
don’t know…find out
24
Q
What is the advantage of selective β-2 agonists vs. non-selective agents?
A
don’t know…find out
25
what drug provides rapid therapeutic effect in the event of acute bronchoconstriction?
epinephrine (racemic)
26
epinephrine can also be used to treat what?
bronchiolitis
RSV
status asthmaticus
27
what is status asthmaticus?
severe, prolonged asthma that is unresponsive to standard drug treatment.
28
describe the series of events that beta 2 agonists precipitate
Stimulation of β-2 receptors increases activity of adenylcyclase enzyme
Increase in adenylcyclase activity increases production of intracellular cyclic AMP
The increase of cyclic AMP activates protein kinase A
Protein kinase A inhibits phosphorylation of myosin
Decrease of phosphorylation of myosin lowers intracellular ionic Ca++ concentrations=
relaxation of the bronchioles
29
stimulation of beta 2 receptors causes an increase in what type of activity?
activity of adenylcyclase enzyme
30
what does the induction of adenylcyclase cause?
increase in production of intracellular cyclic AMP
31
what does an increase of cyclic AMP cause?
activation of protein kinase A
32
what does protein kinase A do?
inhibits phosphorylation of myosin and lowers intracellular calcium concentrations that results in relaxation of bronchioles
33
how long does an ultra short acting beta 2 agonist work?
2-3 hours
34
how long does a short acting beta 2 agonist last?
3-6 hours
35
how long does an intermediate beta 2 agonist last?
8 hours
36
how long does a long acting beta 2 agonist last?
12 hours
37
Why is tachycardia observed if these agents are selective for β-2 receptors?
don't know...vagus nerve suppression maybe???
38
what it is a mirror image of a molecular compound called?
what is a R-Enantiomer?
39
what is the R-Enantiomer of albuterol?
levabuterol
40
why use the R-Enantiomer of albuterol (levabuterol)?
beta 2 selective drugs are usually a mixture of R and S isomers (enantiomers). only the R isomer activates the beta 2 receptors
41
what type of isomer activates the beta 2 receptors?
only R isomers
42
what type of beta 2 agonist is highly selective and has a long duration of action?
formoterol
43
explain how formoterol works
- highly lipophilic
- enters plasma membrane in form of depot
- gradually released into aqueous phase to activate B2 receptors=long duration
44
what type of activity is not demonstrated by salmeterol?
aqueous phase activity
45
what can happen in short acting beta 2 agonists are overused?
tolerance because b2 receptors may become unresponsive to stimulation
46
how can tolerance to short acting beta 2 agonists be reversed?
use of inhaled corticosteroids
47
do long acting beta 2 agonists carry a risk of tolerance?
no
48
beta 2 agonists cause bronchodilation, while anticholinergics ______________.
anticholinergics inhibit bronchoconstriction and decrease mucus secretions
49
how does an inhaled anticholinergic work?
decreased cGMP formation
decreased cGMP=decreased smth ms contractility
=inhibition of bronchoconstriction and mucus secretion
50
what does an inhaled anticholinergic do at the receptor level?
blocks muscarinic cholinergic receptors
| non-specific anticholinergic
51
inhaled anticholinergic are used for the symptomatic relief of what condition?
COPD
52
what are the side effects of inhaled anticholinergics?
```
dry mouth
nervousness
GI upset
headache
worsening narrow-angle glaucoma
prostatic hypertrophy
```
53
what type of drugs blocks M receptors in the lungs?
atropine derivatives
54
2 things about tiotropium (Spiriva)
longer-acting
| structural analog of ipratropium bromide
55
why does tiotropium (Spiriva) have a long-acting effect?
slow dissociation rate from M receptors
56
what drug has been FDA approved for maintenance of COPD?
tiotropium (Spiriva)
57
what are the primary actions of inhaled corticosteroids in the lungs? 4
suppresses airway inflammation
decreases mucous cell secretions
reduces edema
assists with repair of damaged epithelium
58
how do inhaled corticosteroids work?
increases number and sensitivity of beta 2 receptors leading to increased effectivenesss of beta 2 agonist agents
59
In most acute severe asthma attacks, IV administration of corticosteroids offers__________over PO dosing (and what is PO dosing?)
little advantage
| PO=per os or oral
60
how long will full action of systemic corticosteroids will take?
48-72 hrs
61
how long should oral corticosteroids should be taken for?
7-10 days with doses titrated down; should not discontinue rapidly.
62
what is the advantage to inhaled corticosteroids compared to systemic corticosteroids?
even at high doses, inhaled corticosteroids do not appear to cause significant adverse effects while long-term systemic corticosteroid treatment is associated with serious adverse effects
63
long-term systemic corticosteroid treatment is associated with what serious adverse effects?
```
adrenal gland atrophy
peptic ulcers
hyperglycemia
osteopenia and osteoporosis
aseptic necrosis of the hip
immune suppression
```
64
long-term systemic corticosteroid treatment is associated with what unpleasant side effects?
moon face and weight redistribution
| thin skin/acne/fatigue/GI disturbance
65
what is an advantage of fluticasone propionate (Flovent)?
the bioavailability of fluticasone is minimal outside of the airway
66
why is the bioavailability of fluticasone minimal outside of the airway?
it is subject to rapid liver inactivation (CYP450 3A4 pathway) and the metabolite that is produced is largely inactive and has limited affinity for the glucocorticoid receptor
67
what are some inhaled medications that contain both corticosteroid and a bronchodilator
advair diskus contains fluticasone and salmeterol
| symbicort contains budesonide and formoterol
68
what is the name of the bronchodilators that are related to caffeine?
methylxanthines
69
what are the effects of methylxanthines?
bronchodilation
inhibit pulmonary edema
increase cilia activity
70
how do methylxanthines inhibit pulmonary edema?
by decreasing vascular permeability
71
what are the side effects of methylxanthines?
increases cardiac output
peripheral vasodilation
diuretic effect
CNS stimulation
72
how are methylxanthines administered?
orally (PO) and IV
73
why has use of methylxanthines decreased?
narrow margin of safety and drug toxicity/adverse side effects
74
why must serum levels be monitored when administering methylxanthines?
don't know
75
how are mast cell stabilizers used?
prophylaxis to prevent acute asthma attacks
76
what drug is an immunosuppressant monoclonal antibody?
omalizumab
77
how do mast cell stabilizers work?
inhibit release of histamine from mast cells
78
what is the half life of a mast cell stabilizer?
2.5 hours so must be used long term to be of significant benefit
79
what are leukotrienes?
strong chemical mediators of bronchoconstriction and mucous secretion
80
how are leukotrienes formed?
formed by the lipoxygenase pathway of arachidonic acid metabolism in response to cellular injury
81
2 examples of opioid antitussive
codeine
| hydrocodone bitartrate
82
what are leukotriene modifiers?
drugs that counteract the effects of leukotrienes
83
what are leukotriene modifiers used for?
long-term treatment of asthma and allergies
84
how does zileuton work?
reduces formation of leukotrienes
85
how do monelukast and zariflukast work?
block leukotriene receptors
86
how does omalizumab work
binds to immunoglobulin E, preventing IgE attachment to mast cells and basophils
this in turn prevents the release of pro-inflammatory and pro-allergic substances
87
who gets prescribed omalizumab?
patients with severe, persistent asthma, which cannot be controlled even with high doses of corticosteroids
88
how are mucolytics and expectorants are used ?
to reduce the viscosity of bronchial mucous and aid in its removal
89
example of OTC mucolytic/expectorant?
guaifenesin
90
what is an antitussive?
reduces cough reflex
91
how are most antitussives used?
in combination with other agents such as a mucolytic/expectorant
92
what happens in RDS?
condition where the lungs are not producing surfactant
93
who is most at risk for RDS?
premature infants
94
how does surfactant work in the lungs?
forms a thin layer on the inner surface of the alveoli allowing the lung to remain open during respiration
95
what cells produce surfactant?
type II alveolar cells
96
what is RSV?
Respiratory Syncytial Virus
| a virus that normally affects infants and young children
97
how is RSV treated?
```
non-selective β-adrenergic drugs
selective β-adrenergic drugs
oxygen
ribavirin
supportive care
```
98
how can RSV be prevented?
monthly injection consisting of RSV antibodies can be given during peak RSV season to reduce the risk of infection
99
what is anaphylaxis?
A severe, sometimes life-threatening allergic reaction to a variety of agents
100
what agents can cause anaphylaxis?
1- Foods: nuts, shellfish, milk, and eggs
2- Stinging insects: honeybees, wasps
3- Medications e.g. Penicillins
101
what are the symptoms of anaphylaxis?
Flushing, urticaria, pruritis, bronchospasm, cramping, hypotension
102
anaphylaxis treatment
epinephrine
103
how does epinephrine work?
- alpha agonist activity: Increased peripheral vascular resistance, reverse vascular permeability
- beta agonist activity: Bronchodilatation, positive ionotropic effect
104
look at slide 40 extra credit
look at slide 40 extra credit
105
what type of drug stimulates bronchodilation
beta 2 agonists
106
what type of drug inhibits bronchoconstriction?
anticholenergic
107
```
what is the effect of each?
Beta 2 agonist
anticholinergics
corticosteroids
leukotriene modifiers
```
Beta 2 agonist=asthma, causes bronchodilation by stimulation of B2 receptors
Anticholinergics=COPD, inhibits bronchoconstriction by blocking/inhibition of M receptors
Corticosteroids=increases number and sensitivity of beta 2 receptors leading to increased effectiveness of beta 2 agonist agents
leukotriene modifiers=asthma and allergies, counter affect leukotrienes
