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89 Cards in this Set
- Front
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b agonist used for asthma
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albuterol
bitolterol epinephrine formoterol levalbuterol pirbuterol salmeterol terbutaline |
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short acting b agonist
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reserve for trmt of acute exacerbation and prophylazis of EIB
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long acting b agonist + inhaled corticosteroids
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maintenance trmt of moderate and severe persistent asthma
prophylaxis of EIB COPD |
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B agonist therapeutic eff
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relieve bronchoconstriction during acute asthma exacerbation
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moa b agonist
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stimulate b2 rec
activating cyclase ->inc intracellular production of cAMP |
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inc intracellular cAMP
activation cAMP |
dependent protein kinases -> bronchodilation, improve mucociliary clearance and reduced inflam cell mediator release
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tremor
gluconeogenesis insulin secretion activation of Na,K ATpase |
stimulation of b2 rec in skeletal muscle
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b1 rec affinity
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cardiac eff
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inhalation
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minimize systemic exposure and adverse rxns
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b agonist adv eff
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tremor
palpitation tachy nervousness ha |
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b agonist interaxn
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isoproterenol
induce myocardial ischemia, necrosis and arrhy |
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tachyphylaxis
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occur w/ regular use of inhaled or oral b agonist
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downregulation
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dec in the # of active B rec due to movement of rec fr the cell surface into the cell
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paradoxical bronchoconstriction
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result in cold freon effect
and use of adjuvants |
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S isomer of albuterol
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potential cause of inc airway hyperresponsiveness
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levalbuterol HCL
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comprise of the active R enantiomer
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b agonist + mao,tca or methyldopa
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lead to severe htn
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propranolol
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bronchospasm
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corticosteroids eff
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suppress the inflam response and dec airway hyperresponsiveness
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corticosteroids moa
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bind to glucocorticoid rec on the cytoplasm of cells
activated rec regulates transcription of target genes |
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corticosteroids reduce inflam via
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- inhibition of transcription and release of inflam genes
- inc transcription of anti inflam genes that produce proteins that participate in or suppress the inflam process |
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corticosteroid clinical eff
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-reduced production of inflam mediators
- enhanced b adrenergic rec expression - dec mucus prodxn - prevention of endothelial and vascular leakage |
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systemic corticosteroids
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used for rapid response during an exacerbation
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characteristics of systemic corticosteroids
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- good glucocorticoid activity
- minimal mineralocorticoid activity - short to intermediate duration of axn |
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iv corticosteroid
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emergency trmt
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most frequently used oral corticosteroids
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prednisolone
prednisone |
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inhaled corticosteroids
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chronic trmt
ist line therapy for mild to severe persistenet asthma for adults and children |
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list of inhaled corticosteroids
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beclomethasone cfc
beclomethasone hfa budesonide dpi flunisolide fluticasone triamcinolone |
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adult trmt of severe exacerbation
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prenisone
iv trmt - methylprednisoloone |
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inpatient trmt of asthma exacerbation in children
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prednisone, methylprenisolone
prednisolone |
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Corticosteroid + hepatic microsomal enzyme inducers (rifampin, barbiturates, hydantoins)
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caused enhanced corticosteroid metabolism
reducing efficacy |
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corticosteroid + estrogens, oral contra, ketoconazole, macrolide abx- ery,clari
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decrease corticosteroid clearance
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cyclosporine
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inc plasma conc of corticosteroids
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K depleting diuretics- thiazides, furosemide or K depleting drugs - amphotericin
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causes enhanced hypokalemia
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dec serum conc of isoniazid and salicylates
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corticosteroids
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leukotriene modifiers
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antiinflamm prop for use for asthma
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cellular effects of leukotrienes
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- enhanced migration of eosinophils and neutrophils
- inc adhesion of leukocytes - inc monocyte and neutrophil aggregation |
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inc capillary permeability and cause smooth muscle contraction
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leukotriene
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leukotriene rec antagonist
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montelukast
zafirlukast |
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eff of leu rec antagonist
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antiinflam
bronchodilator allow reduction in corticosteroid doses |
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moa of leu rec antagonist
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selective cysteinyl leokotriene 1 (CysLT1)rec antagonist -> prevent leukotrienes from interacting with their rec
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zafirlukast admin
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children over 12 yrs
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Churg-Strauss syndrome
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form of eosinophilic vasculitis
assoc with zafirlukast, montelukast and pranlukast |
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aspirin
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inc zafirlukast levels
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erythromycin, theo and terfenadine
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dec zafirlukast con
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inc anticoagulant effect of warfarin and levels of dofetilide
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zafirlukast
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hepatic enzyme inducers
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rifampin
phenobarbital |
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chewable montelukast
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contain aspartame and shld be avoided in pt's with phenylketonuria
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zileuton
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only lipoxygenase inhibitor
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eff of zileuton
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antiinflam
bronchodilator |
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moa of zileuton
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prevent the formation of leukotriene
blks 5-lipoxygenase |
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5 lipoxygenase
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enzyme resp for leukotriene formation
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zileuton adv eff
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HA
abd pain asthenia nausea dyspepsia myalgia |
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zileuton + propranolol, terfendadine ,theo
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inc conc of zileuton
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zileuton + warfarin
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anticoagulant eff of warfarin inc
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ALT- hepatic enz
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elevalted in zileuton therapy
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symptoms of liver dysfuntion
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right upper quadrant abd pain
flu like sx fatigue nausea lethargy itching jaundice |
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nonsteroidal drugs with anti inflam prop
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cromolyn
nedocromil |
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cromolyn
nedocromil eff |
suppress nonspecific airway reactivity
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c/n moa
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act locally by stabilizing mast cells and thereby inhibiting mast cell degranulation
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inflammatory cells
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macrophages
eosinophils neutrophils monocytes platelets |
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not effective during an acute asthma exacerbation
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c/n
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theophylline
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methylxanthine
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theo indication
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alternative to long acting b agonist in trmt of asthma
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theo eff
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produce bronchodilation to a lesser extent than b agonist
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nonbronchodilator eff
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- reduced mucus secretion
- enhanced mucociliary transport - improved diaphradmatic contractility - reduced fatigability |
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theo-induced phosphodiesterase inhibition
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results in increased levels of cAMP
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theo moa
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- alteration of intracellular calcium
- increased binding og cAMP to its binding protein - adenosine antagonism - inc circulating catecholamine - inhibition of production of contractile prostaglandins (PGE2 AND PGF2alpha) |
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theo max recom dose in children under age of 1
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0.2 x (age in weeks) +5= mg/kg/day given in divided doses
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theo max recom dose in children 1 and older
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16mg/kg/day in divided doses
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methylxanthine compds
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oxtriphylline
dyphylline |
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maintenance infusion rate of theo
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0.4mg/kg/hr
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factors that inc theo clearance (dec levels)
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age 1-9 yrs
cbz pheno phenytoin rifampin fever food high protein diet smoking (mj /tobacco |
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factors that dec theo clearance
(inc levels) |
elderly
premature neonate term infants < 6 mos cor pulmonale chf decompensated fever/ viral illness fatty foods high carbohydrate diet liver dysfxn |
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drugs that inc theo levels
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allopurinol
nonselective B blkers ccb cimetidine clindamycin fluroquinolones influenza virus vac macrolides oral contra ticlid zafirlukast |
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fluroquinolones
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cipro
grepafloxacin norfloxacin prulifloxacin |
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macrolide
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clarithromycin
erythromycin |
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fatty foods
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increase rate of absorption of some prodts
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liver dysfxn
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cirrhosis
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anticholinergics
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blk postganglionic muscarinic rec in the airway -> bronchodilation
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COPD
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response to anticholinergics is most pronounced
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Ipratropium br
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quarternary amm compd
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ipr br indication
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combine with b agonist for trmt of severe, acute asthma exacerbation
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glycopyrrolate
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quarternary amm compd used with b agonist for trmt of sever, acute asthma exacerbations
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antihistamines
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for coexisting allergic rhinitis
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mgso4
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iv admin
modest ability to cause bronchodilation |
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immunotherapy
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improve asthma control
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mucus
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contribute to airway obstruction in asthma
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mucolytics
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precipitate bronchospasm and shld not be used for trmt of asthma
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