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45 Cards in this Set

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what's the main product of the lipoxygenase pathway?
leukotrienes
what is LTB4?
a neutrophil chemotactic agent
what do LTC4, D4, and E4 do? (4)
-bronchoconstriction
-vasoconstriction
-contraction of smooth muscle
-↑ vascular permeability
what does PGI2 do? and what does it stand for?
inhibits platelet aggregation and promotoes vasodilation

Platelet-Gathering Inhibitor
what converts membrane lipid to arachidonic acid and what drugs inhibit this step?
phospholipase A2

corticosteroids inhibit this
what 2 pathways can arachidonic acid go down (i.e. what 2 enzymes convert it and to what)?
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)
what drug inhibits lipoxygenase?

what does this do?
Zileuton

this lowers the amount of Leukotrienes produced (so no increased Bronchial tone)
what drugs block the action of leukotrienes? (2)
Zafirlukast
Montelukast
what 2 things do corticosteroids block?
-phospholipase A2
-protein synthesis (of the cyclooxygenases)
what 3 types of drugs block the cyclooxygenases?
NSAIDs
Acetaminophen
COX-2 inhibitors
what do leukotrienes do?
increase bronchial tone
what does prostacyckin do (PGI)? (4)
decreases the following:
-Platelet aggregation
-Vascular tone
-Bronchial tone
-Uterine tone
what do prostaglandins do (PGE, PGF)? (3)
-increase Uterine tone
-decrease Vascular tone
-decrease Bronchial tone
what does thromboxane do (TXA)? (3)
increases:
-platelet aggregation
-vascular tone
-bronchial tone
MOA of H-1 blockers?
Reversible inhibitors of H1 histamine receptors.
what drugs are 1st generation H-1 blockers?
Diphenhydramine
Dimenhydrinate
Chlorpheniramine
clinical uses of 1st generation H1 blockers? (3)
Allergy
Motion sickness
Sleep aid
toxicity of 1st generation H1 blockers? (3)
-Sedation
-Antimuscarinic
-Anti-α-adrenergic
what drugs are 2nd generation H-1 blockers? (3)
Loratadine
Fexofenadine
Desloratadine.
clinical use of 2nd generation H-1 blockers?
allergy
toxicity of 2nd generation H1 blockers?
Far less sedating than 1st generation
what drug is a nonspecific β-agonist?

What is its MOA?

Adverse effect?
Isoproterenol: relaxes bronchial smooth muscle (β2)

Adverse effect is tachycardia (β1).
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.
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).
clinical use of 2nd generation H-1 blockers?
allergy
toxicity of 2nd generation H1 blockers?
Far less sedating than 1st generation
what drug is a nonspecific β-agonist?

What is its MOA?

Adverse effect?
Isoproterenol: relaxes bronchial smooth muscle (β2)

Adverse effect is tachycardia (β1).
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.
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).
What drugs is a muscarinic antagonist used for asthma?

MOA?
Ipratropium––competitive block of muscarinic receptors, preventing bronchoconstriction.
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.
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.
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.
what asthma agent(s) prevent antigen and IgE on mast cells from forming mediators of an asthmatic rxn (i.e. leukotrienes, mast cells, etc)?
-Cromolyn
-Steroids
what asthma agent blocks the late response (inflammtion) phase of asthma?
steroids
what drugs block the early response (bronchoconstriction) phase of asthma? (3)
-β-agonist
-Theophylline
-Muscarinic antagonists
the early response of asthma is what?

which leads to what?
bronchoconstriction

leads to symptoms
the late response of inflammation is what?

it leads to what?
inflammation

leads to bronchial hyperreactivity
what endogenous chemical promotes bronchodilation?
cAMP
what 2 endogenous chemical promote bronchoconstriction?
Adenosine and ACh
what 2 agents for asthma block bronchoconstriction?
-muscarinic antagonists
-theophylline
what drug class promotes Adenylate cyclase, which causes an increase in cAMP, which causes bronchdilation?
β-agonists
What 2 drugs are expectorants?
Guaifenesin (Robitussin)

N-acetylcystine
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
MOA of N-acetylcystine?
Mucolytic --> can loosen mucus plugs in CF patients