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53 Cards in this Set
- Front
- Back
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List the 3 main goals of asthma pharmacologic therapy.
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(1) prevent/control asthma symtpoms
(2) reduce frequency and severity of asthma exacerbations (3) reverse airflow obstruction |
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Long-term control asthma meds are taken daily to maintain control of
(a) intermittent asthma (b) persistent asthma - whether mild, moderate or severe (c) persistent asthma of the severe type |
Long-term control asthma meds are taken daily to maintain control of
(b) persistent asthma - whether mild, moderate or severe |
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List the 7 categories of long-term control asthma medications.
Which category contains the drugs of choice in treating asthma long-term? |
(1) inhaled corticosteroids **drugs of choice**
(2) systemic corticosteroids (3) inhaled cromolyn sodium (4) inhaled long-acting beta2 agonists (5) theophylline (6) systemic leukotriene modifiers (7) omalizumab |
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Describe (in general) the mechanism of action of inhaled corticosteroids.
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They block the late reaction to allergens and reduce airway hyperresponsiveness.
They regulate gene transcription to decrease eosinopils, decrease T-cell and macrophage cytokines, and decrease mast cell numbers. Inhaled corticosteroids also decrease endothelial cell leakage, increase beta-2 receptors on smooth muscle and decrease mucus secretion. |
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Describe a good candidate for inhaled corticosteroid therapy.
When can a patient expect improvement in lung function? |
Candidates for inhaled corticosteroid therapy are those patients with persistent asthma who require an inhaled short acting beta2 agonist for symptom relief more than 2days/week or more than 2x/month for nighttime awakenings.
Maximal improvement in lung function does not occur for several weeks. |
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What are the clinical effects of inhaled corticosteroids?
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(1) reduced symptom severity
(2) improved peak expiratory flow (3) diminished airway hyperresponsiveness (4) exacerbation prevention (5) maybe even prevention of airway wall remodeling |
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What are the local adverse effects of inhaled corticosteroids?
Systemic adverse effects? |
Local adverse effects:
--oral candidiasis --dysphonia --reflex cough and bronchospasm Systemic adverse effects: --impaired linear growth in kids --bone metabolism/osteoporosis --disseminated Varicella --dermal thinning and inc ease of skin bruising --hypthalmic - pituitary - adrenal axis suppression |
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Although inhaled corticosteroids can produce systemic adverse effects, they have limited systemic bioavailability.. Why is this?
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Inhaled corticosteroids experience extensive 1st pass metabolism in the liver, which limits their systemic bioavailability.
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What patient demographic is at a higher risk of osteoporosis due to inhaled corticosteroid treatment?
How do you manage these patients? |
Elderly female patients are at more risk of developing osteoporosis when taking inhaled corticosteroids.
Appropriate management of these patients would be giving them calcium supplements and vitamin D. |
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To maintain control of asthma in a patient on inhaled corticosteroids, is it more appropriate to use a higher dose of the corticosteroid or is it better to add a long-acting inhaled beta2 agonist to a low/medium dose of inhaled corticosteroid?
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The latter option is more appropriate - adding a long-acting inhaled beta2 agonist to a low/medium dose of inhaled corticosteroid.
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Budesonide, fluticasone and mometasone are all examples of what kind of long-term control asthma medication?
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They are all inhaled corticosteroids.
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Describe a good candidate for systemic corticosteroid therapy.
Give an example of a systemic corticosteroid. |
Patients with severely uncontrolled asthma are good candidates for systemic corticosteroid therapy.
You might prescribe such a patient prednisone. |
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Describe (in general) the mechanism of action of inhaled cromolyn sodium and nedocromil.
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These 2 agents inhibit the activation and release of mediators from mast cells and eosinophils.
They inhibit both the early and late asthmatic response. |
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Inhaled cromolyn sodium and nedocromil are alternatives for the treatment of:
(a) mild persistent asthma (b) severe persistent asthma (c) intermittent asthma |
Inhaled cromolyn sodium and nedocromil are alternatives for the treatment of:
(a) mild persistent asthma. They can also prevent exercise-induced asthma or asthma that a patient knows will be brought on by unavoidable exposure to known allergens. |
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Which is better at inhibiting bronchospasm provoked by exercise or cold dry air: nedocromil or cromolyn?
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Nedocromil is more effective at inhibiting bronchospasm provoked by exercise and cold dry air.
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How are nedocromil and cromolyn administered?
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They are are to be used prophylactically and should be administered 4 times per day.
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TRUE or FALSE
Nedocromil and cromolyn reduce the need for quick-relief beta2 agonists. |
TRUE
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Describe the adverse effects of nedocromil and cromolyn.
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They virtually have no systemic toxicity.
They can produce a transient cough. |
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Describe the mechanism of action of inhaled beta2 agonists.
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They relax the airway smooth muscle by stimulating beta2 receptors, wich increases cAMP and produces functional antagonism to bronchoconstriction.
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Under what circumstances would you prescribe an inhaled long-acting beta2 agonist for an asthmatic patient?
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Inhaled LABA's are preferred for concomitant use with inhaled corticosteroids for long-term control of moderate to severe asthma.
LABA's should NOT be used as monotherapy for persistent asthma. |
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Are inhaled LABA's to be used for acute exacerbations of asthma?
Can LABA's prevent exercise-induced bronchospasm? |
Inhaled LABA's are NOT to be used for acute exacerbations, but can be used to prevent exercise-induced bronchospasm.
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Which inhaled LABA has a quicker onset of action?
a) salmeterol b) albuterol |
a) albuterol
Albuterol has a quicker onset of action compared to salmeterol. |
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Which is more effective in controlling moderate persistent asthma?
a) raising the dose of corticosteroid b) adding an inhaled LABA to inhaled corticosteroids c) adding a systemic corticosteroid to inhalled corticosteroids |
b) adding an inhaled LABA to inhaled corticosteroids
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Which has the slowest onset of action?
a) albuterol b) formoterol c) salmeterol |
c) salmeterol
Salmeterol has a slower onset of action compared to albuterol and formoterol's onset is comparable to that of albuterol. |
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Describe theophylline's mechanism of action.
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Theophylline can cause smooth muscle relaxation either (a) by inhibition of phosphodiesterase leading to increased cAMP or (b) by antagonism of adenosine receptors.
Low dose theophylline may enhance HDAC activity and may synergize with corticosteroid induction of HDAC expression to decrease inflammatory gene expression. |
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Describe the clinical use of theophylline.
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It is used as an adjuvant to inhaled corticosteroids for prevention of nocturnal asthma symptoms in patients with mild-moderate persistent asthma.
It is not recommended for exacerbations. |
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Routine serum concentration monitoring is essential when a patient is taking theophylline.
What would you expect if a patient's plasma concentration is above 15ug/mL? Above 40ug/mL? |
Above 15ug/mL : anorexia, nausea/vomiting, insomnia, tremor, reflux aggravation, hyperactivity
Above 40ug/mL: seizures, cardiac arrhythmias |
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How is theophylline administered?
Why is this important when it comes to the close serum concentration monitoring that is required when a person takes theophylline? |
Theophylline is administered orally. Thus, its absorption and metabolism by the liver may be affected by many factors, which may cause significant changes in steady-sate serum concentrations.
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How do leukotrienes contribute to an asthma attack?
Name 2 examples of drugs that act to modify leukotrienes' role in asthma. |
Leukotrienes are released from mast cells, eosinophils, and basophils. They cause airway smooth muscle contraction, increase vascular permeability, increase mucus secretion, and attract/activate inflammatory cells in the airways of asthmatic patients.
Drugs such as montelukast and zileuton modify these leukotrienes and are used in the long-term control of persistent asthma. |
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Decribe the mechanism of action of montelukast.
Describe its clinical use. |
Montelukast is a leukotriene receptor antagonist.
It is used to control asthma in patients >2yo and can be used to treat allergic rhinitis (usually combined with an antihistamine or intranasal corticosteroid). |
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What adverse effect may occur with administration of montelukast?
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Neuropsychiatric events such as agitation, anxiousness, dream abnormalities, and depression may occur in patients taking leukotriene modifiers.
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What adverse effects are associated with zafirlukast?
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--Churg-Strauss Syndrome
--increases half-life of warfarin |
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Describe the mechanism of action of zileuton.
Describe its clinical use. |
Zileuton inhibits synthesis of all leukotrienes by inhibiting 5-lipoxygenase enzyme, which catalyzes the conversion of arachidonic acid to leukotrienes.
Zileutron is used to control asthma, used to treat allergic rhinitis, and can attenuate bronchoconstriction from exercise and aspirin. |
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What adverse effects are associated with zileuton?
What are its drug interactions? |
Zileuton may cause liver toxicity.
It is to be avoided in pregnancy. It is metabolized by several CYP's and may inhibit the metabolism of warfarin and theophylline. |
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Describe the mechanism of action of omalizumab.
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It is a recombinant DNA-derived IgG monoclonal antibody that inhibits the binding of IgE to IgE receptors on mast cells and basophils.
Omalizumab also reduces the number of the IgE receptors on basophils in atopic patients. |
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Describe the clearance and elimination of omalizumab.
What is omalizumab's elimination half-life? |
Clearance involves IgG clearance processes as well as clearance via complex formation with its target ligand, IgE.
Liver elimination of IgG includes degradation in the liver reticuloendothelial system and endothelial cells. Intact IgG is also excreted in bile. The serum elimination half-life is 26 days. |
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Describe a good candidate for omalizumab therapy.
What is omalizumab's clinical effects in these patients? How long after starting therapy can a patient expect improvement? |
Adult and adolescent patients with severe persistent asthma who have a positive skin test to an aeroallergic and whose symptoms are not well controlled with inhaled corticosteroids, LABA's or leukotriene modifiers are good candidates for omalizumab therapy.
These patients will have an approximate 96% decrease in serum free IgE. It takes several weeks for treatment response. Patients should be treated for at least 12 weeks before efficacy is assessed. |
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What are the adverse reactions associated with omalizumab?
How soon after omalizumab administration can these adverse reactions take place? |
The most serious adverse reactions that can occur with omalizumab are malignancies and anaphylaxis.
Anaphylactic reactions are rare and can occur within 2h after injection but some can occur up to 4days after injection. |
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Identify the specific long-term-control asthma medication (or category) described by the following...
(1) this category is used concomitantly with inhaled corticosteroids for the control of moderate-severe asthma (2) this drug is a leukotriene receptor antagonist and may cause neuropsychiatric events (3) this drug is given orally and requires routine serum concentration monitoring (4) this drug is given prophylactically and is more effective than cromolyn at inhibiting bronchospasm provoked by cold dry air (5) this category is indicated for those with severely uncontrolled persistent asthma (6) this drug inhibits leukotriene synthesis and may inhibit metabolism of warfarin and theophylline (7) this category is the most consistently effective anti-inflammatory medication for those with persistent asthma (8) this drug can reduce the number of IgE receptors on basophils and may cause anaphylaxis (9) these 2 drugs inhibit both the early and late asthmatic response and must be given prophylactically (10) this category is indicated for patients who require an inhaled short acting beta2 agonist for symptom relief more than 2 days/week |
(1) inhaled LABA's
(2) montelukast (3) theophylline (4) nedocromil (5) systemic corticosteroids (6) zileuton (7) inhaled corticosteroids (8) omalizumab (9) inhaled cromolyn and nedocromil (10) inhaled corticosteroids |
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Describe the mechanism of action of inhaled short-acting beta2 agonists.
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They relax the airway smooth muscle by stimulating beta2 receptors, which increases cAMP and produces functional antagonism to bronchoconstriction.
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Which of the following is the therapy of choice for relief of acute asthma symptoms and prevention of exercise induced bronchoconstriction?
a) tiotropium bromide b) prednisone c) albuterol d) omalizumab |
c) albuterol
Inhaled short-acting beta2 agonists are therapy of choice for the relief of acute asthma symptoms and prevention of exercise induced bronchoconstriction. |
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How long does it take for inhaled short-acting beta agonists to begin working?
When will their effect peak? How long do these drugs act? |
70% of maximum effect in 5 minutes or less
Peak effect in 30-60 minutes. The drugs last 4-6hours. |
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Your patient uses a short-acting beta2 inhaler to control her asthma symptoms when needed.
When asking her about the use of her inhaler and how controlled her symptoms have been, at what point would you need to consider prescribing long-term control medications? |
You need to consider putting your patient on long-term asthma meds if she is using her quick-acting inhaler more than 2 days per week or more than twice per month for nighttime awakenings caused by asthma symptoms.
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What dose-dependent adverse effects can occur in patients using a quick-acting beta2 agonist inhaler?
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Dose-dependent sympathomimetic effects:
--tremor --anxiety --heart pounding --tachycardia --small decreases in serum K+ and magnesium |
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Describe the mechanism of action of inhaled anti-cholinergics.
Name 2 examples of drugs in this category. |
They are competitive inhibitors of muscarinic cholinergic receptors. They bind to muscarinic receptors in airway smooth muscle cells and mucus glands adn inhibit the bronchoconstrictive and secretory effects of ACh.
Tiotropium and ipratropium are 2 examples. |
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What is the clinical use of ipratropium?
For what condition is it the treatment of choice? The nasal spray-form of ipratropium is used to treat what condition? |
Ipratropium is used to relieve bronchospasm in chronic bronchitis and COPD.
Ipratropium is the treatment of choice for bronchospasm due to beta-blocker therapy. Nasal spray ipratropim is approved for use in allergic rhinorrhea. |
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What is tiotropium's advantage over ipratropium?
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Tiotropium requires once daily administration whereas ipratropium must be used 4 times daily.
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Which of the following drugs does not block exercise-induced asthma?
a) inhaled cromolyn b) salmeterol c) ipratropium |
c) ipratropium
Ipratropium does not block exercise-induced asthma. |
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What are the adverse effects associated with tiotropium and ipratropium?
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--drying of mouth
--bitter taste --constipation --tachycardia --blurred vision |
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The primary clincial use of ipratropium and tiotropium is for:
a) COPD b) persistent asthma c) exercise-induced asthma |
The primary clincial use of ipratropium and tiotropium is for:
a) COPD |
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Describe the clinical use of sytemic corticosteroids in asthmatic patients.
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They are used for severe exacerbations unresponsive to bronchodilators to speed recovery and prevent recurrence of exacerbations.
They are also used as short term "burst" therapy in patients who have initiated long-term therapy with inhaled corticosteroids. |
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For the following patient descriptions, identify which drug would be most beneficial:
(1) patient has elevated serum IgE and severe persistent asthma with symptoms that are not well controlled with inhaled corticosteroids or LABA's or montelukast (2) patient has bronchospasms and recent diagnosis of COPD; it is noted in the chart that he has compliance issues (3) patient with moderate-severe persistent asthma and using a fluticasone inhaler is having nocturnal symptoms (4) very active pediatric patient who has exercise-induced asthma and sometimes does not have her short acting inhaler handy when she needs it (5) patient with mild persistent asthma who absolutely hates using her inhaler |
(1) omalizumab
(2) tiotropium (3) inhaled LABA (to be used concomitantly with fluticasone) (4) montelukast or zileuton (5) theophylline (it is an alternative for long-term therapy when issues with adherence to using inhalers arise) |
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For the following patient descriptions, identify which drug would be the best treatment:
(1) patient uses a quick-acting inhaler but has been woken up 4 times in the past month by her asthma symptoms (2) patient has mild-moderate astha and is allergic to pollen; he is going on an all day outdoor fieldtrip with his son and wants to know if there is anything he can take to prevent asthma symptoms (3) patient has asthma symptoms 1 day per week but is not currently taking any medications to control/relieve them (4) patient uses a quick acting inhaler but is having severe exacerbations that do not respond to his inhaler - you are going to prescribe him an inhaled corticosteroid that will take several weeks to take maximal effect so you need to control the exacerbations in the meantime |
(1) inhaled corticosteroid (fluticasone, budesonide, mometasone)
(2) inhaled cromolyn or nedocromil (3) short acting beta2 agonist (albuterol) (4) prednisone |
