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71 Cards in this Set
- Front
- Back
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What classes of bronchodilators are available for COPD?
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B2 agonist, anticholinergics, methylxanthines
no benefit of one class over another, inhaled preferred |
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How do bronchodilators work?
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reducing tone of airway smooth muscle (relaxation), thus minimizing airflow limitation
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What benefits from bronchodilators in COPD?
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increased exercise capacity, decreased air trapping in the lungs, relief of symptoms (dyspnea)
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Do bronchodilators cause significant improvements in pulmonary function measurements (FEV1)?
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may not
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Are AE more common with bronchodilators in COPD or asthma?
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COPD, older pts, more likely to have comorbid conditions
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What classes of short acting bronchodilators are available?
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SABA and anticholinergic
equally effective |
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How do SABA cause bronchodilaton?
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stimulating the enzyme adenyl cyclase to increase the formation of cyclic adenosine monophosphate
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What is responsible for mediating relaxation of bronchial smooth muscle leading to bronchodilation?
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cyclic adenosine monophosphate
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Do SABA improve mucociliary clearance?
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yes
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What are the less selective B agonists?
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metaproterenol, isoetharine, isoproterenol, epinephrine
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Should less selective B agonists be used?
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no: short duration and increased cardiostimulatory effects
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What are the SABA?
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preferred tx: albuterol, levalbuterol, pirbuterol
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What dosage forms are sympathomimetics (B2 agonist) available in?
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inhaled, PO, and parenteral
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Why is the use of PO and parenteral SABA discouraged in COPD?
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no more effective than MDI or DPI, and systemic AE are greater
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What is the most frequently used B2 agonist?
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albuterol
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What is albuteral a racemic mixture of?
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R-albuterol and S-albuterol
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What is action of R-albuterol?
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bronchodilator effect
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What is action of S-albuterol?
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no therapeutic effect
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What is levalbuterol (Xopenex)?
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single isomer formulation of R-albuterol
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How are quick onset B2 agonists used in COPD?
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prn for relief of symptoms or scheduled to prevent or reduce symptoms
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What is the duration of action of SABA?
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4-6hrs
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What are the short acting anticholinergics?
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ipratropium (Atrovent) (primary one) and atropine
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What is MOA of anticholinergics?
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produce bronchodilaiton by competitively inhibiting cholinergic receptors in bronchial smooth muscle
blocks acetylcholine, with net effect being a reduction in cyclic guanosine monophosphate |
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What action does cyclic guanosine monophosphate have?
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constrict bronchial smooth muscle
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What does activation of muscarinic receptors result in?
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M1,M3: bronchoconstriction
M2: inhibits further acetylcholine release |
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What kind of structure does ipratropium have?
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quaternary: absorbed poorly
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Why does ipratropium have few anticholinergic SE?
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lack of systemic absorption
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Why is ipratropium (Atrovent) preferred over atropine?
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fewer systemic effects
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What dosage forms are ipratropium bromide available in?
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MDI and solution for inhalation
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How much ipratropium/puff of HFA?
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17mcg
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Duoneb
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ipratropium/albuterol nebulizer solution
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Combivent
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ipratropium/albuterol MDI
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What is peak effect of ipratropium (Atrovent)?
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1.5-2hrs
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What is duration of ipratropium (Atrovent)?
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4-6hrs
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Does ipratropium or standard B2 agonist have a slower onset of action and more prolonged bronchodilator effect?
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ipratropium
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What is onset of effect of ipratropium?
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15-20 minutes
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Is ipratropium (Atrovent) or albuterol more suitable for PRN used?
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albuterol because of shorter onset of effect
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What is recommended dose of ipratropium?
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2 puffs QID, can be titrated to 24 puffs/day
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What dose of ipratropium (Atrovent) is needed to improve exercise performance in stable COPD?
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8-12 puffs prior to exercise, not with 4 puffs or fewer
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Does ipratropium (Atrovent) have an effect during sleep?
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improves arterial oxygen saturation and sleep quality
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What are the most common AE of ipratropium?
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dry mouth, nausea, occasional metalic taste
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What is recommended ts for pts with moderate to severe COPD who experience symptoms on a regular and consistent basis, or in whom short acting therapies don't provide relief?
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long acting bronchodilator
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What benefit from long acting compared to short acting bronchodilators?
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provide similar benefits to short acting agents and also reduce exacerbation frequency and improves QOL
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What long acting B2 agonists are available?
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salmeterol and formoterol and arformoterol
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How often are LABA dosed?
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Q12h
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What is onset of formoterol?
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similar to albuterol: 5 minutes
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What is onset of salmeterol?
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slower: 15-20 minutes
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Are LABA recommended for acute relief of symptoms?
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no
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When are LABA considered?
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frequent and persistent symptoms, reduce nocturnal symptoms, improve QOL
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How does improvement of lung function, exacerbation frequency, and QOL compare for LABA, SABA, or theophylline?
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LABA improve more
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What are benefits from LABA related to?
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improvement in inspiratory capacity
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Do LABA or ipratropium improve FEV1 more?
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LABA
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What is unique about formoterol and arformoterol?
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1st LABA available as nebulized solution
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What long acting anticholinergics are available?
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tiotropium bromide (Spiriva)
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What is action of tiotropium (Spiriva)?
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blocks effects of acetycholine by binding to muscarinic receptors in airway smooth muscle and mucus gland, blocking the cholinergic effects of bronchoconstriction and mucus secretion
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Is tiotropium (Spiriva) or ipratropium (Atrovent) more selective at blocking important muscarinic receptors?
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tiotropium (Spiriva): dissociates slowly from M1 and M3 receptors allowing prolonged bronchodilation, dissociation from M2 receptors is much faster, allowing ihibition of acetycholine release
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How long does tiotropium (Spiriva) protect against cholinergic bronchoconstriction?
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greater than 24hrs
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How does potency of tiotropium (Spiriva) and ipratropium (Atrovent) compare?
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Spiriva 10x more potent than Atrovent
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How long for bronchodilation from tiotropium (Spiriva)?
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30 minutes
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When is peak effect for tiotropium (Spiriva)?
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3hrs
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How often is Spiriva dosed?
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daily
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How is tiotropium (Spiriva) delivered?
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HandiHaler, a single-load, dry-powder, breath actuated device
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What SE for tiotropium (Spiriva)?
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well tolerated, acts locally: dry mouth most common
others: constipation, urinary retention, tachycardia, blurred vision, precipitation of narrow angle glaucoma symptoms |
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What benefits from tiotropium (Spiriva)?
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improves lung function and dyspnea, exacerbation frequency, and health related QOL
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Can tolerance develop to long acting anticholinergics?
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no, sustained long term therapy
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Can tolerance develop to LABA?
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yes
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How much does tiotropium (Spiriva) improve FEV1?
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12-22%
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How does tiotropium combined with pulmonary rehab compare to pulmonary rehab alone?
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improved exercise endurance and health status, reduced dyspnea compared to pulmonary rehab
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How does tiotropium (Spiriva) compare to salmeterol?
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tiotropium: greater improvement in trough FEV1, dyspnea, WOL
no difference in exacerbations |
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What benefit from combining anticholinergic and B agonist?
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allows lowest possible effective dose to be used and reduces potential AE from individual agents
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Combivent
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albuterol/ipratropium MDI, 2 classes of bronchodilators
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