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34 Cards in this Set
- Front
- Back
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What is the molecular target of albuterol?
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beta2 adranergic receptors
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What is the molecular target of long-acting beta2 agonists (salmeterol, formoterol)?
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beta2 adranergic receptors (they are partial agonists and so last longer and don't have the downregulation of betaAR like you see w/ full agonists)
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What is the molecular target of theophyiline?
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It inhibits cAMP PDE --> increase cAMP --> decrease bronchospasm and inflammation
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What is the molecular target of inhaled corticosteroids?
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They target lung inflammation w/o systemic effects. They also block migration of inflammatory cells (e.g. PMNs)
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What is the molecular target of leukotriene receptor antagonists (zafirlukast, montelukast, zileuton)?
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Zileuton targets 5-lipoxygenase.
zafrilukast and montelukast target the leukotriene receptors |
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What is the molecular target of omalizumab?
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Humanized monoclonal Ab against IgE
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What is the molecular target of muscarinic receptor antagonists (ipratroprium, tiatroprium)?
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Tiotropium - Selective for M1 and M3 muscarinic receptor on bronchial sm
Ipratroprium - Not selective for any particular muscarinic receptor NOTE: They are both competitive antagonists |
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What is asthma?
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chronic inflammatory dz accompanied by episodic bronchoconstriction
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What is used for rescue/symptomatic relief/acute therapy in asthma?
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beta2-agonists (epi, albuterol)
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What does epinephrine do to bronchial smooth muscle?
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relaxes it!
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What does acetylcholine do to bronchial smooth muscle?
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Acts on M3-muscarinic receptors to cause contraction.
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What can happen if albuterol alone is used for tx of asthma (w/o steroids)?
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This may increase the level of inflammation
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Name 2 long-acting b2-receptor agonists.
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Salmeterol and formoterol
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True or False: Long-acting b2-agonists are useful alone.
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FALSE!!! They are combined w/ inhaled corticosteroids in maintenance therapy
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Give 6 anti-inflammatory drugs (or classes)
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1. corticosteroids
2. theophylline 3. cromolyn 4. nedocromil 5. leukotriene antagonists 6. omalizumab |
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Name 5 inhaled corticosteroids
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1. beclomethasone
2. triamcinolone 3. flunisolide 4. fluticasone 5. budesonide |
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What are the most common side effects of ICS?
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1. oropharyngeal candidiasis
2. dysphonia 3. modest decreases in bone density |
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True or False: There is generally good compliance with ICS?
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FALSE
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What are some of the pharmacological important facts about cAMP in the lungs?
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1. high cAMP results in relaxed bronchial sm
2. high cAMP levels in mast cells prevents degranulation in allergic rxns 3. high cAMP inhibits the function of immune and inflammatory cells |
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What do inhibitors of cyclic nucleotide phosphodiesterases do to the levels cAMP?
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increase them!
epi --> ++B2AR --> ++Gs --> ++adenlyate cyclase --> ++cAMP --> ++PKA --> ++protein phosphorylation |
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What are some examples of cAMP PDE inhibitors?
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caffeine and theophylline
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What is the mechanism of action of theophylline?
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inhibits all 15 cyclic nucleotide PDE causing bronchodilation and inhibition of pro-inflammatory mediators
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What is the problem w/ theophylline?
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it has a very narrow therapeutic window
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What is the major PDE isozyme in inflammatory cells?
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PDE4
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What is the mechanism of Cromolyn Sodium and Nedocromil?
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unclear. Seem to act as mast cell "stabalizers"
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What is the use of cromolyn sodium and nedocromil?
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they are anti-inflammatory drugs, but not steroids. Some advantage in kids. Useful in mild to moderate asthma.
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Name 3 leukotriene blockers.
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zafirlukast, montelukast, zileuton
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What are the major advantages of leukotriene blockers?
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mild to moderate asthma. oral admin, few side-effects, high levels of compliance. useful in asthmatics w/ high sensitivity to aspirin
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What limits the usefulness of zileuton?
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hepatotoxicity
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What are the major disadvantages of leukotriene receptors
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not as generally effective as ICS for mainenance of moderate to severe asthma
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What is the major advantage of omalizumab?
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only given by subq injections q2-4 wks. reduces free IgE by > 95%
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What is the major disadvantage of omalizumab?
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cost. $12000/yr
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Name 2 muscarinic antagonists
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ipratroprium and tiotropium
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Are muscarinic receptor antagonists more useful in asthma or COPD?
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COPD
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