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45 Cards in this Set
- Front
- Back
what's the main product of the lipoxygenase pathway?
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leukotrienes
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what is LTB4?
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a neutrophil chemotactic agent
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what do LTC4, D4, and E4 do? (4)
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-bronchoconstriction
-vasoconstriction -contraction of smooth muscle -↑ vascular permeability |
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what does PGI2 do? and what does it stand for?
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inhibits platelet aggregation and promotoes vasodilation
Platelet-Gathering Inhibitor |
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what converts membrane lipid to arachidonic acid and what drugs inhibit this step?
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phospholipase A2
corticosteroids inhibit this |
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what 2 pathways can arachidonic acid go down (i.e. what 2 enzymes convert it and to what)?
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lipoxygenase: converts AA to hydroperoxides (HPETEs) --> Leukotrienes (LTB, LTC, LTD)
Cyclooxygenase (COX-1, COX-2): AA to endoperoxides (PGG, PGH) -> Prostacyclin (PGI), Prostaglandins (PGE, PGF), and Thromboxane (TXA) |
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what drug inhibits lipoxygenase?
what does this do? |
Zileuton
this lowers the amount of Leukotrienes produced (so no increased Bronchial tone) |
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what drugs block the action of leukotrienes? (2)
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Zafirlukast
Montelukast |
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what 2 things do corticosteroids block?
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-phospholipase A2
-protein synthesis (of the cyclooxygenases) |
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what 3 types of drugs block the cyclooxygenases?
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NSAIDs
Acetaminophen COX-2 inhibitors |
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what do leukotrienes do?
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increase bronchial tone
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what does prostacyckin do (PGI)? (4)
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decreases the following:
-Platelet aggregation -Vascular tone -Bronchial tone -Uterine tone |
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what do prostaglandins do (PGE, PGF)? (3)
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-increase Uterine tone
-decrease Vascular tone -decrease Bronchial tone |
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what does thromboxane do (TXA)? (3)
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increases:
-platelet aggregation -vascular tone -bronchial tone |
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MOA of H-1 blockers?
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Reversible inhibitors of H1 histamine receptors.
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what drugs are 1st generation H-1 blockers?
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Diphenhydramine
Dimenhydrinate Chlorpheniramine |
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clinical uses of 1st generation H1 blockers? (3)
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Allergy
Motion sickness Sleep aid |
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toxicity of 1st generation H1 blockers? (3)
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-Sedation
-Antimuscarinic -Anti-α-adrenergic |
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what drugs are 2nd generation H-1 blockers? (3)
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Loratadine
Fexofenadine Desloratadine. |
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clinical use of 2nd generation H-1 blockers?
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allergy
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toxicity of 2nd generation H1 blockers?
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Far less sedating than 1st generation
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what drug is a nonspecific β-agonist?
What is its MOA? Adverse effect? |
Isoproterenol: relaxes bronchial smooth muscle (β2)
Adverse effect is tachycardia (β1). |
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what 2 drugs are β2 agonists?
what are their MOAs? adverse effects? clinical uses? |
Albuterol––relaxes bronchial smooth muscle (β2). Use during acute exacerbation.
Salmeterol––Long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia. |
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What drugs is a Methylxanthine?
MOA? Why is its usage limited? |
Theophylline––likely causes bronchodilation by inhibiting phosphodiesterase, thereby ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity).
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clinical use of 2nd generation H-1 blockers?
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allergy
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toxicity of 2nd generation H1 blockers?
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Far less sedating than 1st generation
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what drug is a nonspecific β-agonist?
What is its MOA? Adverse effect? |
Isoproterenol: relaxes bronchial smooth muscle (β2)
Adverse effect is tachycardia (β1). |
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what 2 drugs are β2 agonists?
what are their MOAs? adverse effects? clinical uses? |
Albuterol––relaxes bronchial smooth muscle (β2). Use during acute exacerbation.
Salmeterol––Long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia. |
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What drugs is a Methylxanthine?
MOA? Why is its usage limited? |
Theophylline––likely causes bronchodilation by inhibiting phosphodiesterase, thereby ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity).
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What drugs is a muscarinic antagonist used for asthma?
MOA? |
Ipratropium––competitive block of muscarinic receptors, preventing bronchoconstriction.
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MOA of Cromolyn?
For what in asthma tx is it good for? When is it not useful? Toxicity? |
Prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute asthmatic attack. Toxicity is rare.
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What 2 corticosteroids can be used for asthma?
MOA? 1st line for what? |
Beclomethasone, prednisone––inhibit the synthesis of virtually all cytokines. Inactivate NF-κB, the transcription factor that induces the production of TNF-α, among other inflammatory agents. 1st-line therapy for chronic asthma.
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What 3 asthma drugs are antileukotrienes?
MOAs? |
Zileuton––A 5-lipoxygenase pathway inhibitor.
Blocks conversion of arachidonic acid to leukotrienes. Zafirlukast and Montelukast––block leukotriene receptors. |
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what asthma agent(s) prevent antigen and IgE on mast cells from forming mediators of an asthmatic rxn (i.e. leukotrienes, mast cells, etc)?
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-Cromolyn
-Steroids |
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what asthma agent blocks the late response (inflammtion) phase of asthma?
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steroids
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what drugs block the early response (bronchoconstriction) phase of asthma? (3)
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-β-agonist
-Theophylline -Muscarinic antagonists |
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the early response of asthma is what?
which leads to what? |
bronchoconstriction
leads to symptoms |
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the late response of inflammation is what?
it leads to what? |
inflammation
leads to bronchial hyperreactivity |
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what endogenous chemical promotes bronchodilation?
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cAMP
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what 2 endogenous chemical promote bronchoconstriction?
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Adenosine and ACh
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what 2 agents for asthma block bronchoconstriction?
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-muscarinic antagonists
-theophylline |
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what drug class promotes Adenylate cyclase, which causes an increase in cAMP, which causes bronchdilation?
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β-agonists
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What 2 drugs are expectorants?
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Guaifenesin (Robitussin)
N-acetylcystine |
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MOA of Guaifenesin?
--does it suppress the cough reflex? What else is it called? |
Guaifenesin removes excess sputum but large doses are necessary
--does not suppress the cough reflex called Robitussin |
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MOA of N-acetylcystine?
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Mucolytic --> can loosen mucus plugs in CF patients
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