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35 Cards in this Set
- Front
- Back
______ catalyzes decarboxylation of histidine to histamine
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Histidine decarboxylase
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In what cells is histamine made
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Enterochromaffin-like cells
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Histamine causes bronchial smooth muscle constriction/dilation?
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Constriction
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Most prominent effect of histamine on the vasculature is __
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Dilation of the postcapillary venule bed
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Histamine induces/suppresses gastric acid secretion
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Induces - causes Ca2+ influx into parietal cells
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Activation of the H1 receptor leads to increase in levels of what
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IP3, DAG
THIS IS THE ALLERGIC TYPE OF HISTAMINE RECEPTOR IP3 triggers release of Ca2+ DAG activates protein kinase C |
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H1 receptors found in (3)
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Brain, Vascular Endothelium, Smooth Muscle
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Major functinon of H2 receptors is to
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Mediate Gastric acid secretion
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H3 receptor function to provide
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Feedback inhibition
Decrease Calcium influx |
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H4 receptors are localized to ___ cells and lead to decreased cAMP
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Hematopoietic cells
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Can mast cell degranulation occur as a response to a local tissue damage?
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Fuckin right
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3 strategies of histamine pharm. Name the example drugs
1. Administer inverse agonists, or competetive antagonists of histamine receptor - For Allergies |
Diphenhydramine
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2. Prevent Mast cell degranulation - Asthma
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Cromolyn, Nedocromil
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3. Administer physiologic antagonists to counter the pathologic effects of histamine - Anaphylaxis
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Epinephrine
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First/Second generation H1 antihistamines are neutral at physiologic pH and readily cross the BBB
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First
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First/Second generation H1 antihistamines are ionized at physiologic pH and don't cross the BBB
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Second
(Loratadine, Ceterizine, Fexofanadine) |
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Two dx's that H1 antihistamines aren't effective for
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Urticarial vasculitis, hereditary angiodema
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H1 antihistamines should not be used as the sole therapy for
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Asthma
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H1 antihistamines reach peak plasma concentration in _ to _ hours and are metabolized by the...
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2-3,, liver
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____ a second gen. H1 antihist is metabolized by P450 into an active metabolite so inhibitors of P450 can affect the metabolism of it
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Loratadine
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Along with the fact that second gen H1 antihist's are ionized at phys. pH, what is another reason they don't readily cross the BBB?
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The exhibit high binding to albumin and are thus less free to diffuse into the CNS
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Two of the most commonly used H2 receptor antagonists
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Cimetidine and Ranitidine
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Common adverse effect of Cimetidine the H2 receptor antagonist
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Inhibits Cytochrome P450 mediated drug metabolism
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H3 receptor antagonists induce what
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Wakefulness
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Diphenhydramine
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First gen. H1 antihistamine
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Pyrilamine
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First gen. H1 antihistamine
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Doxepin
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First gen. H1 antihistamine (tricyclic antidepressant for sad people)
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Chlorpheniramine
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First gen. H1 antihistamine
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Promethazine
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First gen. H1 antihistamine
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Hydroxyzine
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First gen. H1 antihistamine
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Citerizine
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2nd Gen. H1 Antihistamine
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Acrivastine
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2nd Gen. H1 Antihistamine2nd Gen. H1 Antihistamine
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Azelastine
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2nd Gen. H1 Antihistamine
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Anything that ends in -dine
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2nd Gen. H1 Antihistamine
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Cimetidine, Famotidine, Nizatidine, Ranitidine
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H2 receptor antagonist
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