Asthma drugs – Flashcards
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What affects advance and retreat of glaciers?
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plate tectonics (moves continents to poles in increase glaciation in those areas) and cyclical climate changes
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early phase of asthma
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bronchospasm
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late phase of asthma
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inflammation
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B2 agonists (albuterol, salmeterol) MOA
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relaxation of bronchiole smooth muscle
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mast calls & T-lymphocytes release which mediators
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histamine, tryptase, PGD2, LTC4, PAF, IL-4, IL-5, GM-CSF, TNF, TGF
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eosinophils and neutrophils release which mediators
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ECP, MBP, Protease, PAF
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corticosteriods (beclomethasone, budesonide) MOA
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broad anti-inflammatory actions
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methylxanthines (theophylline) MOA
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relaxation of bronchiole smooth muscle, effects on T-cells & eosinophils, increased mucociliary clearance (all via increase in cAMP)
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cromolyn, nedocromil MOA
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inhibit release of inflammatory mediators
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leukotriene modifiers (zafirlukast, montelukast) MOA
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antagonize the actions of LTs in the airways
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muscarinic antagonists (ipratropium) MOA
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muscarinic blockade in airways (blocks parasympathetic bronchoconstriction)
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monoclonal antibodies (omalizumab) MOA
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block IgE binding to mast cells
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non-selective beta-agonists (3) used for asthma
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epinephrine, ephedrine, isoproterenol
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epinephrine - forms, onset & DA, adv rxns
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injectable, aerosolinhalation: onset in 15 minduration: 60-90 minadv rxn: tachycardia, arrythmias, MI, skeletal muscle tremor
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ephedrine for asthma (compared to epi)
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oral adm; longer acting; more CNS effects; less potent
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isoproterenol for asthma (compared to epi)
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more potent; short onset of 5 min; 60-90 min duration
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B2-selectives - onset, peak and DA if inhaled
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onset at 1-5 min; peak at 30 min; lasts for 2-6 hrs
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B2-selectives - oral DA
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~ 4-8 hrs
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B2-selective drugs
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albuterol (O/I), terbutaline (O/I), metaproterenol (O/I), bitolterol, pirbuterol, levalbuterol, salmeterol, formoterol
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long-acting B2-selective drugs (12 hours or longer - useful for nocturnal symptoms)
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salmeterol, formoterol --> both are dry powder inhalers
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% of dose from MDI that actually makes it into the lung
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2 - 10% (90% deposited in the mouth)
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tolerance to B2-selective agents tends to develop in response to which effect
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tolerance to anti-inflammatory effects (mast cells and lymphocyets) more than tolerance to brochodilation
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drug interaction with selective B2 agonists
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interaction b/w non-selective beta-blockers and selective B2 agonist (counteract one aother)
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Methylxanthine drugs (4)
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theophylline, aminophylline, enprofylline (3-propylxanthine), and Roflumilast (newest agent in clinical trials)
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two proposed methylxanthine MOA's (theophylline, aminophylline)
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Increased cAMP results in:1) inhibtion of PDE4 (requires high conc.), 2) blockade of adenosine receptors, A1 in bronchiole sm (seen at therapeutic concentrations)
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therapeutic index/range for methylxanthine drugs (theophylline, aminophylline)
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10-20 micrograms/ml (SEs appear around 20-25 micrograms/ml; higher than 40 can lead to seizures or arrhythmias)
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metabolism of methylxanthines (theophylline, aminophylline)
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CYP 450: 1A2 --> drug interactions
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what's special about roflumilast
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newest methylxanthine in clinical trials - high specificity for PDE4 in the lungs, less AE
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what's special about enprofylline
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potent bronchodilator that shows PDE4 inhibition, but no adenosine receptor antagonism
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muscarinic antagonists for asthma (2)
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Ipratropium & Tiotropium: Ipratropium bromide (quaternary ammonium compound)Tiotropium (Spiriva) – new agent with 24-hr duration of action
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muscarinic antagonists (Ipratropium & Tiotropium) - MOA
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blocking muscarinic receptors prevents parasympathetic bronchoconstriction - M3 receptor
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which disease state should muscarinic antagonists be used carefully in
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glaucoma
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muscarinic antagonists (Ipratropium & Tiotropium) - time to peak, DA
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Max effect in 30 min; duration of 3-5 hrs
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Combivent (MDI) - 2 products
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albuterol (b2 selective agonist) + ipratropium (muscarinic antagonist)
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MOA for Cromolyn (Intal) & Nedocromil (Tilade)
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inhibition of mast cell degranulation; inhibit mediator release from bronchial mast cells inhibition of parasympathetic & cough reflexes; not bronchodilators; no direct effects on smooth muscle
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uses for for Cromolyn (Intal) & Nedocromil (Tilade) (mast cell degranulation inhibitors)
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only prophylactic use – decrease immediate & late-phase asthmatic response to antigen-, exercise-, and irritant-induced asthma; effective when given before exercise or exposure to irritants
