Glossary of gi, blood lipids, asthma pharm 4-23-06

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

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