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40 Cards in this Set
- Front
- Back
What are the respiratory effects of Epinephrine?
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1. Bronchodilation via direct stimulation of beta-2-adrenoceptors
2. Vasoconstriction of small blood vessels decreases local congestion & edema 3. Acts in the CNS to increase respiratory rate & tidal volume and thus dec. CO2 in the alveoli 4. Rapid onset of action (30 sec) when given s.c. |
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What are the respiratory effects of Isoproterenol?
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1. Bronchodilation via direct stimulation of beta-2-adrenoceptors
2. Rebound bronchoconstriction may occur after prolonged use 3. Arterial pO2 may decline in some pts/ b/c perfusion is increased (CO) more than ventilation (give O2 to prevent problem) 4. Limited use in asthma due to adverse cardio effects and dev. of tolerance due to B2 receptor down reg. (down reg. reversed by inhaled corticosteroids) |
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What drug are for outpatient use that cause bronchodilation via beta-2-adrenoceptor stimulation?
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1. Salmeterol
2. Albuterol 3. Terbutaline |
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What are the effects of Salmeterol, Albuterol, Terbutaline?
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1. Preferentially dilate the smaller & more peripheral airways
2. Inhibit the release of inflammatory compounds from mast cells 3. Inhibit the accumulation of eosinophils 4. Improve mucociliary transport in proximal and distal airways 5. Tolerance develops due to beta-2 receptor downregulation |
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Is Salmeterol a LABA or a SABA? Do you still need to give a SABA? Is it a substitiute for corticosteroids?
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1. LABA --> slow onset, long lasting
(bronchodilation ~ 24 hrs) 2. Still give a SABA 3. NOT a substitute for corticosteroids * Do NOT use in patients w/ deteriorating asthma |
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What are the S/E's of the beta-2-adrenoceptor agonists?
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May cause a paradoxical bronchospasm after excessive inhalation
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What is the MOA of Corticosteroids?
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Inhibit the recruitment of leukocytes & monocytes & prevents the release of PGs, LTs, PAF, TNF, and IL-1
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What is the preferred route of administration of Corticosteroids for the treatment of asthma?
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Inhaled (Aerosol) Corticosteroids
* If the response to inhaled CS is inadequate, the dose may be inc. up to 4-fold before resorting to p.o. therapy |
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When would systemic administration of corticosteroids for the treatment of asthma be appropriate?
(Descending dose pack) |
Treatment of acute exacerbations for 5-10 days exerts little toxicity, and adrenal suppression dissipates within 1-2 weeks
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What are the adverse effects of inhaled corticosteroids?
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1. Bone resorption may occur--dose dependent
2. Adrenal suppression w/ higher doses 3. Pupura may occur--dose related |
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What are the major adverse effects of Inhaled corticosteroids?
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1. Dysphonia
2. oropharyngeal Candidiasis *mitigate BOTH by rinsing the mouth & throat w/ water after use & employing spacer or reservoir devices |
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What are two corticosteroids are good for children because they have a high "first-pass" metabolism?
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1. Budesonide
2. Fluticasone *50% first-pass metabolism if swallowed |
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What are the general properties of Muscarinic receptor antagonists in the airways?
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1. Poorly lipid-soluble quaternary compounds which do not enter CNS or cross placenta
2. Dilated large and small sized airways |
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What is the MOA of Muscarinic receptor antagonists?
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Muscarinic receptor blockade prevents bronchoconstriction and bronchial secretion
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What are the two Muscarinic receptor antagonists? (on the drug list)
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1. Ipratropium
2. Tiotropium |
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Which has a longer bronchodilatory effect? Ipratropium or Tiotroprium.
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Tiotroprium --persists for 24 hrs
Ipratroprium --persists for 4-8 hrs |
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What are the clinical uses of Muscarinic receptors antagonists?
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1. TERTIARY therapeutic agent in asthma
2. Prophylaxis to prevent attacks in patients w/ a poor response or intolerance to the beta-2 agonists |
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What M receptor antagonist is the DOC for patients with COPD?
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Tiotropium
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What are the toxicities and S/E of Muscarinic receptor antagonists?
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1. Dry mouth and bitter taste
2. Use w/ caution in pts. with angle-closure glaucoma, GI or GU obstruction of prostatic hypertrophy |
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What are the pulmonary toxicities of leukotrienes?
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1. Bronchoconstriction
2. Increased mucus production 3. Increased vascular permeability 4. Chemotaxis for eos/neutrophils 5. Increased leukocyte adhesion |
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What drugs are Leukotriene receptor antagonists and what specific receptors are they antagonistic against?
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1. Zafirlukast
2. Montelukast *LTC4 & LTD4 |
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What are the effects of the LT receptor antagonists?
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Decrease the late bronchoconstriction cause by challenge w/ allergens
Maximal therapeutic effect occurs after 1 wk of therapy; decreased need for rescue w/ a SABA Used as an ALTERNATIVE to inhaled corticosteroids, but not as effective Major adverse side effect is HEADACHE |
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Zafirlukast can increase the plasma concentration of other drugs by inhibiting ____________
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CYP2C9
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What is a really good drug for exercise induced Asthma?
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Cromolyn sodium
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What is the bioavailability of Cromolyn sodium?
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low, only 10% absorbed from the LUNGS and GI tract
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What forms does Cromolyn sodium come in?
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1. Powder in capsules for inhalation
2. Powder in aerosol 3. Nasal spray & opthalamic drops |
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What is the MOA of Cromolyn sodium?
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1. PROPHYLACTIC thearpy prevents immediate and delayed antigen-induced degranulation of mast cells
2. Prevents the release of chemical mediators from mast cells by preventing the increase in intracellular calcium concentration induced by the formation of IgE-antigen bridges on the cell surface *Use 10-15 minutes prior to exposure to antigen |
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What are the pharmacologic effects of Cromolyn sodium?
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1. Reduces the frequency & severity of the bronchospasm
(beneficial effects may take 3-4 wks to develop) 2. Long-term therapy can reduce the overall reactivity to histamine and leukotrienes by preventing the bronchial damage caused by mast cell products |
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What are the toxicities and S/Es of Cromolyn sodium?
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No contraindications
Use aerosol w/ care in patients w/ CAD or cardiac arrhythmias: hydrocarbon propellants can elicit adverse cardiac effects Few adverse effects during long-term therapy --> throat irritation, cough, dry mouth and wheezing |
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What is the MOA of Theophylline?
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Inhibition of phosphodiesterase which degrades cAMP
A specfic adenosine receptor antagonist |
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What are the general properties of Theophylline/Aminophylline?
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Hepatic merabolism; t1/2 decreased in smokers
Crosses the placenta Secreted in milk: usually no effect in nursing children Aminophylline is more water soluble than Theophyline Found in OTC asthma remedies |
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What are the pharmacolgical effects of Theophylline/Aminophylline?
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*See pages 336-337*
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What are the toxicities and S/E's of Theophylline/Aminophylline?
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*See pg. 337
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In patients with what disease is Theophyline contraindicated?
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Active gastic ulcer disease
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The toxic effects of Theophylline appear at __________ and are prominent at ___________.
(plasma concentrations) |
15 mg/L
20+ mg/L |
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What is periodic deep and shallow breathing occuring in cycles of 45 seconds to 3 minutes called?
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Cheyne-Stokes breathing
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When does Cheyne-Stokes breathing usually occur?
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Heart failure--delay of blood flow from lungs to CNS
CNS injury--increased gain in respiratory center response to CO2 |
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What is the treatment for Cheyne-Stokes breathing?
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Aminophylline--normalized respiration
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What is neonatal apnea?
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Apnea of greater than 15 seconds in duration that causes recurrent cerebral hypoxia which may produce serious neurological damage
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What drugs increase respiratory rate and improve blood gases in preterm infants w/ intermittent apnea?
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Aminophylline or Caffeine (iv)
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