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37 Cards in this Set
- Front
- Back
Statistics for the Prevalence of asthma
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1-3% of all office visits
500,000 hospital admissions yearly More pediatric hospital admissions than any other single illness 5000 deaths annually (can be avoided) 60 million people suffer from asthma and alelrgies 5% of US adults and 8% of children |
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True or False: Asthma is characterized by the irreversible narrowing of bronchial airways.
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False - the narrowing is REVERSIBLE
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Pathological characteristics of asthma
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1. reversible narrowing of bronchial airways
2. marked increase in bronchial responsiveness 3. lymphocyte inflammation of bronchial mucosa "Remodeling" of bronchial mucosa |
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What is the functional unit of the lungs?
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alveoli - gas exchange occurs here
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More severe forms of asthma lead to a chronic inflammatory response. What are the characteristics?
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1. epithelial shedding (evolves into epithelial fibrosis)
2. mucous hypersecretion (mucus plug) 3. airway wall remodeling |
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Of the causes of airway restriction in asthma, ?? is most easily revered by current therapy?
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contraction of smooth muscle
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Why is a sustained therapy with anti-inflammatory agents required to treat asthma?
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asthma is incurable
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What cells increase with asthma and the inflammation of airway wall?
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eosinophils, mast cells, basophils, and macrophages
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Lymphocytes in asthma are biased towards which cell: Th1 or Th2? It also involves which interleukins?
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Th2
IL-4, 5, & 13 IL-4 = IgE IL-5 = Eosinophil survival |
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List possible irritants responsible for asthma
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smoke
cold air inhaled gases (perfumes, cleaning agents) pollution particles from combustion of fuels exercise |
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MOA of allergens and 2nd exposure in asthma - "early asthmatic response"
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*Allergens provoke IgE production
*IgE attaches to mast cell *2nd exposure triggers degranulation of mast cell and production of acute inflammatory mediators - histamine, LTs, and PGs diffuse through airway mucosa |
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Effects of histamines, LTs, and PGs
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*msucle contraction and vascular leakage
* edema formation due to chemical mediators *acute bronchoconstriction |
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"late asthmatic response"
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*influx of inflammatory cells into bronchial mucosa
*increase in bronchial reactivity *may last several weeks *Late phase mediators are generally Th2 derived cytokines (IL-4, 5, and 13) |
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What does IL-4 do?
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activate B cells to produce IgE Abs which lead to mast cell degranulation and release of histamine, LTs, and chemotactants
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Genetic abnormalities leading to asthma
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*predisposition to develop IgE to common allergens
- Genetic abnormality in the IL-4 gene |
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Definition of asthma
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Asthma is an inflammatory disorder characterized by bronchial hyperreactivity causing bronchoconstriction
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Sympathomimetic agents: classification; MOA; Adverse effects
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Classification: alpha and beta adrenergic agonists
MOA: relax airway smooth muscle via beta2 stimulation Adverse effects: tachycardia and skeletal muscle tremor |
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Nonselective and selective sympathomimetic agents
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NONSELECTIVE:
epinephrine ephedrine isoproterenol SELECTIVE: beta2-agonists (albuterol) |
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Epinephrine: selectivity and adverse effects
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Nonselective: stimulates alpha, beta1, and beta2
Adverse effects: tachycardia, arrythmias, worsening of angina *Primary use is for bronchospasm relief in anaphylaxis |
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Isoproterenol: selectivity and side effects
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Non selective: beta1 and beta2 agonists
Side effects: tachycardia and arrythmias *Potent bronchodilator: max effect in 5 min (epi 15 min) |
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Ephedrine: selectivity and other info
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Nonselective
Similar to epinephrine but much weaker Used infrequently for asthma Used OTC as weight loss/appetit suppressant Primatene mist/bronkaid |
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Beta2-Selective agonists MOA and types
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MOA: relaxation of airway smooth muscle via Beta2
Short-acting and long-acting *Beta 2 receptors on inflammatory cells decrease release of inflammatory mediators and cytokines |
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Short-acting Beta2-Selective agonists: MOA; indication; dose
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MOA: relaxation of airway smooth muscle via beta2
Indication: asthma induced dyspnea "rescue inhaler" Dose: 1-2 puffs Q4-6h PRN Onset of action: 1-5min Duration: 2-6hours |
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What is better for short acting beta2 agonists: inhalers or PO?
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**inhalers are better than PO because it is direct impact/contact with problem area
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Aerosol delivery - info. and Ideal drug
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*Provides topical application of drugs to lungs
Theoretically: high concentration in lungs with low systemic delivery - minimizes side effects *No aerosol device can produce uniform particles Ideal drug: poorly absorbed from GI tract or extensively metabolized via first pass |
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MDI vs Nebulizer
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*MDI's are less expensive and portable
*Nebulizer don't require hand breathing coordination **SLOW, deep breath and held for 5-10sec |
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Drug list of short acting beta2 selective agonists
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Proventil/Ventolin/Proair (albuterol)
Combivent/Duoneb (albuterol/ipratropium) Maxair (pirbuterol) Xopenex (levalbuterol) Brethine (terbutaline) Alupent (metaproterenol) |
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Which isomer activates the beta receptor: the R or S isomer?
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The R isomer. Most preparations are mixture of R and S isomers. The S isomer may promote inflammation.
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Proventil/Proair/Ventolin HFA (Albuterol): MOA; Use; Contraindications; Side effects; Drug interactions; Dosage forms
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MOA: Relaxes bronchial smooth muscle by stimulation of beta2 receptor
USE: bronchodilator in reversibly airway obstruction due to asthma & COPD; prevention of exercise-indued bronchospasm CONTRAINDICATIONS: hypersenesitivity to albuterol or adrenergic amines SIDE EFFECTS: increased heart rate, decreased K+, increase risk of arrhythmias and blood glucose DRUG INTERACTIONS: alpha and beta blockers may decrease effect; MAO-I, TCAs, and sympathomimetic agents increase effect DOSAGE FORMS: PO, Nebulizer, and aerosol |
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Long-acting beta2-selective agonists: MOA; duration
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MOA: relax airway smooth muscle via beta2 stimulation
DURATION: 12 hours or longer *highly lipophilic molecules *Not anti-inflammatory effects *Not recommended as monotherapy |
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Drug list of long-acting beta2 agonists
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Serevent (salmeterol)
Advair (salmeterol/fluticasone) Foradil (formoterol) Brovana (arformoterol) Perforomist (formoterol) |
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Foradil (formoterol): MOA; Use; Contraindications; warnings/precautions; drug interactions; dose
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MOA: relaxes bronchial smooth muscle via beta2 stimulation
USE: maintenance treatment in asthma and prevention of bronchospasm in patients 5 and older CONTRAINDICATIONS: hypersensitivity to formoterol WARNINGS/PRECAUTIONS: do not use as a component of chronic therapy without an anti-inflammatory agent. Do not use to treat acute asthmatic episodes DRUG INTERACTIONS: May decrease the effect of beta-blockers. Nonselective alpha/beta blockers may decrease the effect of beta2 agonists. MAO-Is, TCAs, and sympathomimetics increase effects DOSE: 12mcg capsule inhaled Q12h |
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Corticosteroids are the best treatment for asthma ??.
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Prevention
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Corticosteroids have ant-inflammatory effects through these actions.
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*Alter cytokine production
*Inhibit eiconsanoid synthesis *inhibt accumulation of basophils, eosinophils, and leukocytes in lung tissue *decrease vascular permability |
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Main difference between corticosteroids and sympathomimetics
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Corticosteroids do NOT relax airway smooth muscle but sympathomimetics due
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short term side effects (5-10days) of corticosteroids
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mood disturbances
increased appetite impaired glucose control |
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long term systemic side effects of corticosteroids
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disruption of HPA axis resulting in lack of cortisol production
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