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what type of receptors are Histamine receptors? how manya re there? |
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metabotropic - G-protein 4 known |
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sedatives allergic rhinitis - stuffy nose |
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Gastric ulcers all end in "-tidine" |
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1st generation H1 Blockers, describe, 4 types |
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Nonselective - also bind alpha adrenergic and muscarinic receptors CNS penetration -> sedation Short t1/2 Alkylamines, ethanolamines, phenothiazines, piperazines |
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2nd generation H1 blockers |
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Definition
Selective H1 blockers limited/no CNS penetration - no sedation CYP metabolized - interferes w/ other drugs Intermediate t1/2 |
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3rd generation H1 blockers |
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Selective H1 blocker No CNS penetration Not CYP metabolized logn t1/2 H-receptor independent anti-inflammatory action |
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1st generation H1 blocker alkylamine |
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1st generation H1 blocker ethanolamine |
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1st genration H1 blocker ethanolamine |
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1st generation H1 blocker used in "coast guard cocktail" phenothiazine |
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1st generation H1 blocker piperazine |
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1st generation H1 blocker piperazine |
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2nd generation H1 blocker |
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2nd generation H1 blocker prodrug - CYP 3A4 -> fexofenadine |
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2nd generation H1 blocker |
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2nd generation H1 blocker prodrug -CYP 3A4 -> Carebastin |
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2nd generation H1 blocker |
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3rd generation H1 blocker |
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3rd generation H1 blocker |
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3rd generation H1 blocker longest t1/2 |
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3rd generation H1 blocker |
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H2 blocker first available, interacted w/ CYP enzymes and made action of other drugs unpredictable |
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