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44 Cards in this Set
- Front
- Back
What is the effect of cholestyramine on the serum triglyceride level?
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Slight increase (cholestyramine is a bile acid resin)
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What is the effect of colestipol on HDL?
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No effect! (colestipol is a bile acid resin)
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What is the effect of lovastatin on HDL?
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Increase (lovastatin is an HMG-CoA reductase inhibitor)
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Name 2 side effects of pravastatin.
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Increase LFTs and cause myositis (prevastatin is an HMG-CoA reductase inhibitor)
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What is the effect of Niacin on HDL?
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Increase
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What are the side effects of clofibrate?
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Incease LFTs and cause myositis (Clofibrate is a "Fibrate")
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Which increases HDL most: simvastatin, niacin, or gemfibrozil?
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Niacin
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Which decreases triglyceride level most: colestipol, Atorvastatin, niacin, or bezafibrate?
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Bezafibrate
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What is the main effect of ezetimibe?
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decrease serum LDL (a cholesterol absorption inhibitor)
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Gemfibrozil increases the activity of which enzyme?
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Lipoprotein lipase (which converts VLDL to IDL)
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What enzyme breaks down membrane lipid into arachidonic acid?
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Phospholipase A2
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What two enzymes are responsible for the production of Hydroperoxides (HPETEs) and Endoperoxidases, respectively from arachidonate?
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Lipoxygenase= HPETE, Cyclooxygenases=endoperoxidases
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What major class of products do HPETEs give rise to?
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Leukotrienes
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What are the 3 major products of Endoperoxides?
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Prostacyclin (PGI), Prostaglandins (PGE, PGF), Thromboxane (TXA)
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In general what effect do leukotrienes have on bronchial tone?
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Leukotrienes in general increase bronchial tone
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In the arachodonic acid pathway, what two enzymes do corticosteroids block?
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Phospholipase A2, COX-2
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NSAIDs, Acetaminophen and "-coxibs" inhibitors block which arachadonic acid pathway enzymes
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NSAIDs-non-selectively block COX-1 and COX-2, acetaminophen blocks CNS COX, COX-2 inhibitors block COX-2
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What are the 4 major effects of Prostacyclin
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decrease platelet aggregation, decrease vascular tone, decrease bronchial tone, decrease uterine tone
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What are the 3 major effects of Prostaglandins
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increased uterine tone, decrease vascular tone, decrease bronchial tone
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What are the 3 major effects of Thromboxane
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increase platelet aggregation, increase vascular tone, increase bronchial tone
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Zileuton is a ________ pathway inhibitor?
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Lipoxygenase
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Zariflukast blocks synthesis of what compounds?
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Lekukotrienes
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Bronchodilation is mediated by what molecule (intracellular)
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cAMP
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Bronchoconstriction is mediated by _________ and ___________ (neurotransmitters)
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Ach and adenosine
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How many asthma drug categories are there?
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7- (1) nonspecific B-agonists, (2) B2 agonists, (3) Methylxanthines, (4) muscarinic antagonist, (5) cromolyn, (6) corticosteroids, (7) Antileukotrienes
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What is the only nonspecific B-agonist drug and what are its effects?
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Isoprotenerol-relaxes bronchial smooth muscle (B2) and tachycardia (B1) (adverse effect).
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What are the two B2 selective agonist asthma drugs?
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Albuterol- relaxes bronchial smooth muscle (B2), Salmetrol
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What are the indications for Albuterol and Salmetrol, respectively?
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Albuterol- use during acute exarcebation, Salmetrol- long-acting agent for prophylaxis
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what are the notable adverse effects of B2 agonist?
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arythmias and tremor
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B2-agonists activate this enzyme in bronchial smooth muscle that leads to an increase in ________ = bronchodilation
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B2 agonists activate adenylate cyclase and increase conversion of ATP to cAMP
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What are the likely mechanism of action theophylline?
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bronchodialation by inhibition phosphodiesterase (PDE), decreasing cAMP hydrolysis and antagnonizing adenosine action
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Why is usage of theophylline limited?
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limited b/c narrow therapeutic index (cardiotoxicity, neurotxicity)
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What kind of drug is Ipratropium?
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muscarinic antagonist
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How does mechanism of action of Ipratropium?
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competitive block of muscarinic receptors= prevention of bronchoconstriction
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cromolyn works by inhibiting the release of _______ from ______ cell?
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prevents release of mediators from mast cells
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Cromolyn is mainly used for the ______ of athsma and it is not indicated for _______ treatment of athsma?
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Used only for prophylaxis, not effective during acute episode. Also, toxicity rare
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__________and ________ are two major corticosteroids used for treatment of what kind of asthma?
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Beclomethasone and prednisone are 1st line therapy for chronic asthma
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What is the mechanism of action of corticosteroids?
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inhibits the synthesis of virtually of cytokines-->inactivates NF-KB, the transcription factor that induces the production of TNF-a, amonth other inflammatory agents.
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Zileuton blocks the conversion of _______ to ________.
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zileuton is a 5-lipoxygenase pathway inhibitior. Blocks the conversion of arachidonic acti to leukotrienes
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Zafirlukast works by_______ ________ ________
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bloking leukotriene receptors
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What the most basic asthma treatment strategy?
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avoidance of exposure to antingen (dust, pollen, etc)
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After exposure to antigen crosslinks IgE on mast cells. This is prevented by the following drugs: _________ and ________
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cromolyn and steroids
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Following allergen exposure mediators are released (ex. _______ and _________). This triggers an ______ asthmatic response characterized by ________ and may be treated with the following 3 asthmatic drug categories to treat the symptoms.
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examples of mediators are leukotrienes and histamine. Following allergen exposure an early asthmatic response characterized by bronchoconstriction that can be treated with B-agonsists, methylxanthines, and muscarinic antagonists.
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Also, mediators elicit a ________ response is which leads to bronchial __________ and is treated with __________.
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mediators elicit a late response and this leads to bronchial hyperactivity. This is best treated with steroids.
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