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43 Cards in this Set
- Front
- Back
common feature of autacoids?
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the ability to be formed by certain tissues, and then act on those SAME tissues
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Histamine is found in all tissues, especially high [ ] in?
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1) lung
2) skin 3) intestinal mucosa |
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histamine is synthesized from ?
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histadine
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histamine is stored intracellularly in vesicles with?
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heparin
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storage sites of histamine?
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1) mast cells & basophills
2) GI mucosa 3) nerve endings in certain areas of the brain 4) cells of rapidly growing or regenerating tissue |
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release of histamine is caused by?
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1) allergic reactions
2) cellular injury 3) drugs (opioids, sux, contrast, vanc, anti-protozoal) |
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activation of H1 receptor causes?
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constriction of bronchi and gut
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H2 receptor ?
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gastric acid secretion
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H1 and H2 receptors?
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vascular dilation
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H3 receptor?
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inhibition of histamine release and synthesis (like autoreceptor)
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circulatory effects of histamine?
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1) increased capillary permeability
2) vasodilation 3) triple response of Lewis |
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triple response of Lewis?
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1) red spot
2) wheal 3) flare or red flush |
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hyposecretion of histamine?
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1) pernicious anemia
2) gastric carcinoma 3) atropic gastritis |
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hypersecretion of histamine?
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1) diodenal ulcer
2) Zollinger-Ellison syndrome |
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clinical use of histamine for diagnosis?
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Histalog (histamine analog Betazole) = less H1 receptor activity (H2:H1 = 10:1)
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Impromidine?
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investigational drug
greater H2 selectivity (H2:H1 = 10,000:1) |
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1st generation antihistamines
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1) Alkylamines
2) Ethanolamines 3) Ethylenediamines 4) Phenothiazines 5) Piperazines 6) Piperidines 7) Phthalazinone |
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1) Alkylamines
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1) Brompheniramine (in Dimetane)
2) Chlorpheniramine (Chlor-Trimeton) 3) Dexchlorpheniramine (Polaramine) 4) Triprolidine (Actifed) |
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Alkylamines have marked potential for producing?
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sedation
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2) Ethanolamines
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1) Carbinoxamine (Rondec)
2) Clemastine (Tavist) 3) Dimenhydrinate (Dramamine) 4) Diphenhydramine (Benadryl) 5) Doxylamine (Unisom) |
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Clemastine (Tavist) also blocks?
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at muscarinic receptors
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Dimenhydrinate (Dramamine) is used to treat?
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motion sickness
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Dephenhydramine (Benadryl) is active metabolite of?
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dimenhydrinate
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Benaryl
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1) sedation
2) motion sickness 3) anticholinergic |
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Doxylamine (Unisom) is used as ?
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OTC sleep aid
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3) Ethylenediamines
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1) Tripelennamine (PBZ)
2) Pyrilamine (in cold medecine) |
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4) Phenothiazines
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1) Promethazine (Phenergan)
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Phenergan also blocks at?
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alpha adrenergic receptors
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5) Piperazines
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1) Hydroxyzine (Vistaril, Atarax)
2) Meclizine (Bonine OTC, Antivert) |
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Meclizine is used to treat?
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1) motion sickness
2) vertigo 3) Meniere's syndrome |
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6) Piperidines
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antihistaminic / antiserotogenic
1) Cyproheptadine (Periactin) |
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SE of Cyprohepatidine?
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increase appetite and wt gain
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7) Phthalazinone
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1) Azelastine (Astelin)
- 1st antihistamine nasal spray - for seasonal allergic rhinitis |
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2nd generation antihistamines
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1) Loratadine (Claritine)
2) Desloratadine (Clarinex) 3) Cetirizine (Zyrtec) 4) Fexofenadine (Allegra) |
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benefit of 2nd generation antihistamines?
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non-sedation
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primary active metabolite of Claritin?
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desloratadine (Clarinex)
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Are H1 antagonists effective in severe hypersensitivity reactions?
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No. b/c hypotension is cauused by histamine acting at both H1 and H2 receptors
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antihistamine and MAOI?
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MAOI can prolong and intensify their anticholinergic effects
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episodes of syncope in pts with H1 antagonists?
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Discontinue H1 antagonists.
SE = severe arrhythmia |
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H2 receptor antagonists
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1) Cimetidine (Tagamet)
2) Ranitidine (Zantac) 3) Famotidine (Pepcid) 4) Nizatidine (Axid) |
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H2 receptor antagonists inhibit?
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action of histamine at parietal cell H2 receptors = decrease in acid secretion
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SE of Cimetidine?
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1) gynecomastia
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Cimetidine decreases metabolism of?
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1) Warfarin
2) Phenytoin 3) Theophyllin |