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?
- Increase
- What are the side effects of clofibrate?
- Incease LFTs and cause myositis (Clofibrate is a "Fibrate")
- Which increases HDL most: simvastatin, niacin, or gemfibrozil?
- Niacin
- Which decreases triglyceride level most: colestipol, Atorvastatin, niacin, or bezafibrate?
- 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?
- Leukotrienes
- 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?
- Lipoxygenase
- Zariflukast blocks synthesis of what compounds?
- Lekukotrienes
- Bronchodilation is mediated by what molecule (intracellular)
- cAMP
- 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.