Term
Where are H1 receptors located? |
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Definition
Smooth Muscle Endothelium Brain |
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Term
Where are H2 receptors located? |
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Definition
Gastric Mucosa, Cardiac Muscle, Mast Cells, Brain |
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Term
Where are H3 receptors located? |
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Definition
Presynaptic Brain, Myenteric Plexus |
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Term
Where are H4 receptors located? |
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Definition
Eosinophils, Neutrophils, CD4 Tcells |
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Term
What is the triple response that an Intradermal injection of histamine can cause? |
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Definition
Redness Inflammation Flare Response |
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Term
In which types of patients is histamine contraindicated in? |
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Definition
Pts with asthma, active ulcer disease or GI bleeding |
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Term
What are some adverse effects of histamine? |
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Definition
Flushing Hypotension Tachycardia HA Wheals Bronchoconstriction GI Upset |
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Term
Describe the relationship between a physiologic antagonist and histamine. Give an example of a physiologic antagonist. |
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Definition
Smooth m. actions opposite those of histamine, but work through different receptors Example = Epinephrine |
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Term
Describe the relationship between a release inhibitor and histamine. Give an example of a release inhibitor. |
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Definition
Reduce degradation of mast cells resulting from antigen-IgE interaction Examples = Cromolyn and Nedocromil |
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Term
Describe the relationship between a receptor antagonist and histamine. |
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Definition
Competitively antagonize the actions of histamine |
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Term
What are anti-histamines used for? What receptor do they work on? |
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Definition
Anti-histamines are used for allergies. They block the H1 receptors |
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Term
What are H2 Blockers used to treat? |
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Definition
Reduce the amount of stomach acid, so reduce GERD and Heart burn |
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Term
Which anti-histamine generation has more sedative effects? |
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Definition
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Term
Which anti-histamine generation is more likely to block autonomic receptors? |
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Definition
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Term
Which anti-histamine generation is rapidly absorbed? When is its peak onset? |
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Definition
Both 1st and 2nd; Peak onset in 1 to 2 h |
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Term
Which anti-histamine generation has a shorter duration of action? |
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Definition
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Term
Which anti-histamine generation is more lipid soluble? What does this allow the drug to do? |
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Definition
1st generation; Allows it to cross the BBB |
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Term
Which anti-histamine generation is metabolized by the CYP-450 system in the liver and therefore has a higher possibility of drug interactions? Which drugs is it likely to interact with? |
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Definition
2nd Generation Interacts with -azoles, macrolides (erythromycin), and sedating agents |
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Term
Which anti-histamine generation generally has a less sedating action? |
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Definition
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Term
Which anti-histamine generation is used in N/V associated with pregnancy? |
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Definition
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Term
Which anti-histamine generation has anti-parkinson's effects? |
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Definition
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Term
Which anti-histamine generation is used in motion sickness and vestibular disturbances? |
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Definition
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Term
Which generation of anti-histamines has serotonin blocking actions? |
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Definition
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Term
What effect do H2 Blockers have on H1 receptors? |
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Definition
Thought to have NO effect on H1 receptors |
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Term
Is there a low toxicity or high toxicity with H2 blockers? |
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Definition
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Term
Which two 2nd generation anti-histamines are no longer on the US market due to their potential to cause arrhythmias? |
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Definition
Terfenadine (Seldane) and Astemizole (Hismanal) |
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Term
What 3 drugs are 2nd generation H1 anti-histamines? |
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Definition
Cetirizine (Zyrtec) Fexofenadine (Allegra) Lortadine (Claritin) |
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Term
What do anti-histamine drugs end in? |
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Definition
-zine -dine -mine -nate [Dimenhydrinate (Dramamine) - only one ending in -nate] |
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Term
What 11 drugs are 1st generation H1 anti-histamines? |
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Definition
5 - mines Brompheniramine Diphenhydramine Chlorpheniramine Carbinoxamine Tripelennamine 4 - zines = Hydroxyzine Cyclizine Meclizine Promethazine 1 - dine Cyproheptadine 1 -nate Dimenhydrinate |
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Term
What 4 drugs are H2 anti-histamines? |
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Definition
Cimetidine Rantidine Famotidine Nizatidine |
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