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31 Cards in this Set
- Front
- Back
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Short Acting Beta-2 Agonists:
Use Mechanism Time of onset, peak, duration |
Use: relief of acute syx; preventative tx prior to exercise for exercise-induced bronchospasm
Mech: Bronchodilation SM via stimulation of beta2 adrenergic receptors-->activates adenylyl cyclase-->cAMP-->inhibition of phosphorylation of myosin-->relaxation Takes 3-5 minutes to kick in; peaks at 30-60 minutes; lasts 4-6 hours |
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Albuterol:
Class Suffix AEs |
-buterol:
Lavelabuterol Pirbuterol SABA AE: Tach, palpitations, skeletal muscle, tremor HYPOKALEMIA, inc'd lactic acid, HA, hyperglycemia |
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Which SABA will not be phased out by 2013?
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The ones that end in HFA (phasing out CFC use in inhalers)
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Chronic use of SABA can lead to _____.
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Downregulation and decreased binding affinity (tolerance!).
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Which types of SABA are preferred? Why?
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Albuterol or levalbuterol--greater beta-2 selectivity
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Long-Acting Beta-2 Agonists:
Use Mechanism Time of onset, duration How do they differ structurally from SABA? |
Long-term prevention of syx, esp nocturnal; must be ADDED to anti-inflamm (steroidal) tx
Not for tx of acute syx! Mech: Similar to SABA, but long lipophilic side chain causes it to remain in lung tissue longer, continually engaging/disengaging from receptor |
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Salmeterol:
Class Onset, duration |
Salmeterol : LABA
Onset 15-30 mins, duration >12hrs |
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Formoterol:
Class Onset, duration |
LABA
Onset 5 min, duration 12 hrs |
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Sustained release albuterol:
Class Onset, duration |
LABA TABLETS
Onset 30 min, duration 4-6 hrs |
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The drug class is beneficial ONLY when added to inhaled corticosteroid therapy.
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LABA
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Ipratropium Bromide:
Use Mechanism AE's |
Relief of acute bronchospasm (not FDA approved for asthma) when added to SABA
Alternative for those w/beta-agonist intolerance Doe not block exercise induced asthma! Mech:bronchodilation via psymp innervation of vagus--nonselective competitive inhibitor of muscarinic receptors (M3 in lung!)-->dec'd cGMP-->dec contractility of SM AE's: Drying of mouth and resp secretions, inc'd wheezing, blurred vision if sprayed in eyes CAREFUL WITH PEANUT ALLERGIES |
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Should ipratropium bromide be used alone in treating acute asthma attacks? Why or why not?
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No, time to reach maximal bronchodilation is much slower than with beta-agonists: 2 hrs vs 30 minutes.
However, may provide addl benefits if ADDED to SABA. |
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Systemic Corticosteroids:
Use Mechanism Effects on beta-2 receptors |
Short-term burst tx to gain prompt control of acute asthma
Long-term prevention of syx in severe persistent asthma Mech: Anti-inflamm; GC-receptor in cytoplasm; inc production anti-inflamm mediators, suppression of proinflamm mediators Inc'd number beta-2 receptors, improving responsiveness Also: reduces mucous secretions, airway remodeling |
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Hydrocortisone:
Suffix Class |
-sone: prednisone, methylprednisolone, dexamethasone
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Long-Term Effects of Systemic Corticosteroids
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HPA suppression (don't stop suddenly!)
HTN Immunosuppression Hypokalemia Hyperglycemia |
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Inhaled Corticosteorids:
Use Mechanism AEs |
Long-term prevention of syx
Suppression, control, reversal of inflammn Reduces need for oral corticosteroid Mech same as oral; local activtn receptors AE: Thrush Dysphonia Reflex cough, bronchospasm Disseminated varicella |
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Cromolyn:
Use Mechanism |
First-line medication for children (ICS more effective in controlling asthma though)
Long-term prevention of syx Preventive for exercise-induced asthma or w/known allergen Mech: Mast cell stabilizer; prevents degranulation and inhibits allergic mediated bronchocontriction by preventing type 1 allergic reactions (no release of histamine, SRS-A: slow-reacting substance of anaphylaxis ) |
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This drug is only available as a nebulizer.
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Cromolyn
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Theophylline:
Use Mechanism AEs |
Long-term control and prevention of syx (esp nocturnal)
Not for acute relief Mech: bronchodilation via nonselective PDE inhibition (thus inc'd cAMP); competitive antagonist of adenosine-->inc'd catecholamine release (just like coffee) MANY DRUG INTERACTIONS and dose-related toxicities: -Insomnia, GI upset, aggravation of ulcer/reflux -Dose related: tachy, N/V |
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Leukotriene Modifiers:
Use |
Long-term control, prevention of syx
Can be used as monotx in mild asthma and adjunct tx in chronic asthma |
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Zafirlukast:
Class Suffix Use Mechanism |
-kast: zafirlukast, montelukast
Luekotriene modifier Long-term control/prevention CysLT1 receptor antag; blocks LTC4/D4/E4 effects |
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Zileuton:
Class Use Mechanism |
Leukotriene modifier
5-LO inhibition; prevent synthesis of LK's from arachidonic acid 5-LO inhibition |
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Which leukotriene modifiers can be used in those over 12 months old?
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Montelukast (Singulair)--most used
Zileuton (4 tablets a day) |
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Which leukotriene modifiers can be used in those over 7 years old?
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Zafirlukast
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Omalizumab:
Class Use |
Anti-IgE: binds to IgE at Fc site, interfering with binding of IgE to mast cells and bphils
INJECTION ONLY Mod-severe persistent asthma w/poz skin tests or invitro activity to aeroallergen AND syx adequately contr'd by corticosteroids Improves QOL, reduces asthma syx |
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What is the goal of pharmacologic management of stable COPD?
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Prevention and control of symptoms; improve health status, exercise tolerance
No medication has been shown to modify long-term decline in lung function or prolong survival |
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What drug class is central to symptom management of COPD?
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Bronchodilators: choice depends on individual response
Albuterol is first-line |
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Effect of bronchodilators on FEV1 in asthma vs COPD.
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In asthma, there will be an increase FEV1 (asthma is reversible)
In COPD, there will be little change in FEV1 (COPD is an irreversible process) |
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Tiotropium Bromide:
Class Use Mechanism AEs |
Tiotropium bromide = long-acting anticholinergics (~to ipratropium but dissociates more slowly); faster dissocn from M2 than M3, thus longer duration in lungs
Use: COPD only AEs: Dry mouth, constipation, urinary retention, tachy, blurred vision |
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Guideliens for inhaled corticosteroids in patients with COPD.
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Trial of 6 weeks to 3 mos; if no response, discontinue.
Only for those with symptomatic COPD. |
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Treatment Approach in Stable COPD by GOLD Classification
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Mild: SABA PRN
Mod: scheduled tx w/at least 1 LA-bronchodilator, rehab Severe: Add ICS if repeated exacerbations V Severe: Long-term O2 if chronic resp failure, surgery |
