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35 Cards in this Set
- Front
- Back
Question: One effect that theophylline, nitroglycerin, isoproterenol, and histamine have in common is?
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Tachycardia
Note: nitroglycerin evokes a compensatory sympathetic reflex. |
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Question: A 23 year old woman is using an albuterol inhaler for frequent acute episodes of asthma and complains of symptoms that she ascribes to the albuterol. What are possible side effects?
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At high dosage, induces beta1 cardiac effects as well as beta2-mediated smooth and skeletal muscle effects.
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Question: What drug is most likely to have adverse effects when used daily over long periods for severe asthma.
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Prednisone by mouth.
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Question: A 12 year old girl in asthma clinic has suboptimal response to her current therapy, and nedocromil is being considered for addition to the regimen. Nedocromil's major action is?
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Block of mediator release from mast cells.
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Question: What drug does NOT have a direct bronchodilator effect: Epinephrine, terbutaline, theophylline, ipratropium, nedocromil?
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Nedocromil
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Question: What are some established prophylactic strategy for asthma?
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Avoidance of antigen exposure; blockade of leukotriene receptors; inhibition of phospholipase A2; inhibition of mediators from mast cells and leukocytes.
Note: blockade of histamine receptors has not been est. |
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Question: An ex-smoker with COPD has frequent bronchospasm. What drug is a bronchodilator useful in COPD and least likely to cause cardiac arrhythmia?
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Ipratropium--a muscarnic antagonist.
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Question: What is a nonselective but very potent and efficacious bronchodilator that is not active by the oral route?
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Epinephrine is the most potent and efficacious agent for asthma; however, is nonselective and can cause hypertension and arrhythmias.
Beta2 agonist are preferred. |
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Question: What prophylactic agent stabilizes mast cells?
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Cromolyn and nedocromil.
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Question: PT is suffering seizures from overdosing . He took a drug orally and sometimes had insomnia after taking it. What drug is a direct bronchodilator used in asthma by the oral route and capable of causing insomnia?
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Theophylline.
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Question: What drug is used parenterally in life-saving situations for severe status asthmaticus and acts by inhibiting phospholipase As.
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Prednisone.
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Question: What has a slow onset but long duration of action and is always used in combination with a corticosteroid by inhalation?
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Salmeterol and formoterol.
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For acute asthma, what are the classes of "reliever drugs?"
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Beta2 agonists, muscarinic antagonists, and theophylline.
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Long-term preventive treatment for anti-inflammatory drugs used in treatment for chronic asthma are?
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Anti-inflammatory: corticosteroids
Mediators from mast cells and other inflammatory cells: cromolyn and nedocromil. Leukotriene antagonists: can have an effect on both bronchoconstriction and inflammation for prophylaxis. |
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Beta2 selective agonist:
Short-acting (for acute episodes) and long-acting (prophylaxis)? |
Short-acting: albuterol, terbutaline, metaproterenol (NOT a beta blocker!).
Long-acting: salmeterol and formoterol Note: epinephrine and isoproterenol are used occasionally. |
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How do beta2 agonist cause bronchodilation?
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Stimulation of Gs adenylyl cyclase that increases cAMP in smooth muscles.
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When long acting beta2 agonist are used alone, there is an increase risk of? How can you prevent this?
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Asthma mortality, which when used with corticosteroids, they improve control by improving the response to corticosteroids.
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Other than acute asthma episodes, short-acting beta2 agonist can also help with? However, at what cost?
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COPD PTs can benefit, although there is an increase risk of toxicity (arrhythmias since they often have concurrent cardiac disease).
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What are the SE of beta2 agonist?
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Skeletal muscle tremor.
At high dose, significant beta1 affects: tachycardia; arrhythmias. Excess use can lead to loss of responsiveness (tolerance, tachyphylaxis) COPD PTs: they often have concurrent cardiac disease and arrhythmias can occur at normal dosage. |
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Methylxanthines are? What are three examples? Which one is only used for the treatment of asthma?
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Purine derivatives.
Caffeine (coffee), theophylline (tea), and theobromine (cocoa). Theophylline can be used for asthma. |
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What is the MOA of methylxanthines?
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They inhibit phosphodiesterase (PDE), an enzyme that degrades cAMP to AMP; therefore, methylxanthines increase cAMP.
Also block adenosine receptors in CNS. |
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What are the clinical effects of theophylline?
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Bronchodilation, CNS stimulation, cardiac stimulation, vasodiltation, increase BP (via release of norepinephrine) and increase GI motility.
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What are the clinical usage of methylxanthines?
Aminophylline and pentoxifylline? |
Not as safe or effective as beta2 agonist (narrow therapeutic index: cardiotoxicity and neurotoxicity).
Slow release theophylline for control of nocturnal asthma. Aminophylline: salt of theophylline sometimes prescribed. Pentoxifylline: intermittent claudication (decreased viscosity of blood). |
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What are the SE of methylxanthines?
Antidote for theophylline? |
GI distress, tremor, insomnia, hypotension, cardiac arrhythmias, and seizures.
Beta-blockers for reversing cardiovascular toxicity |
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What are two antimuscarinic agent designed for aerosol use? MOA?
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Ipratropium and tiotropium (longer acting analog).
They prevent bronchoconstriction mediated by vagal discharge. |
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Compare Ipratropium and tiotropium against beta2 agonist? Which one is more effective with COPD and why?
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The antimuscarinic are useful in 1/3 - 2/3 of asthma PTs whereas beta2 agonist are useful for nearly all.
Antimuscarinic antagonist are more useful with COPD since they do not cause arrhythmias. |
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What two drugs prevent the release of leukotrienes and histamine from mast cells?
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Cromolyn and nedocromil.
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What clinical effect do cromolyn and nedocromil have? Clinical uses and SE?
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Do not have bronchodiltation actions; however, they prevent bronchoconstriction when faced with an allergic antigen.
Asthma, nasal and eye drops for hay fever, and to prevent food allergies. Cough and irritation of airways. |
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MOA of corticosteroids? Their effect?
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Reduce release of phospholipase A2, therefore, reducing arachidonic acid. Also, increases the responsiveness of beta2 receptors in the airways.
Prevent expression of inflammation and decrease leukotrienes that cause bronchoconstriction. |
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Clinical uses and SE of corticosteroids?
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Early usage may prevent severe, progressive inflammatory changes characteristic of long-standing asthma.
In status asthmaticus, parenteral steroids are lifesaving. Small degree of adrenal suppresion--rarely significant. Regular use of inhaled steroids DOES cause growth retardation; but children eventually reach their predicted adult stature. |
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If oral therapy of steroid is needed, then?
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Alternate day therapy: giving the drug a slightly higher dosage every other day than smaller doses every day.
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What are two leukotriene receptor blockers? What are they effective against?
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Zafirlukast and montelukast.
Preventing exercise-, antigen-, and aspirin-induced bronchospasm. |
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What drug selectively inhibits 5-lipoxygnease? Its use and SE.
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Zileuton.
Prevents exercise-, antigen-, and aspirin-induced bronchospasm. Elevated liver enzymes; therefore, less popular than leukotriene receptor blockers. |
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How does aspirin produce bronchospasm?
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Divert all eicosanoid production to leukotrienes with COX pathway is blocked.
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What drug is a monoclonal AB that binds to IgE on sensitized mast cells to prevent release of inflammatory mediators?
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Omalizumab
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