IDing histamine structures Metcalf

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14 Terms

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Ethylenediamines

1st gen H1 antihistamines

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Ethanolamine ethers

1st gen H1 antihistamines

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Alkylamines

1st gen H1 antihistamines

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Piperazines

1st gen H1 antihistamines, multiple effects

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Tricyclics

1st gen H1 antihistamines, multiple effects

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Piperadine

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Carbomate

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Fexofenadine

2nd Generation, H1, Non-sedating antihistamine

Blockade of hERG K+ channels

LOOK FOR THE BLUE CIRCLED STRUCTURE FOR DRUGS ENDING IN “ine”

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Terfenadine, Astemizole

Life threatening hERG K+ ion channel

Not marketed

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Loratadine, Desloratadine

2nd Generation, H1, Non-sedating antihistamine

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Cetirizine

hydroxyzine oxidized to make this

2nd gen

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Acrivastine

Second gen non-sedating antihistamine: notice constrained amine

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H2 antagonists (ex: Cimetidine)

Imidazole ring like histamine (causes increases side effects)

4 atom side chain includes sulfur

EWG Substituted guanidine

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PPIs (ex: Omeprazole)

Metabolized by CYP 2C19

Isomers metabolized unequally in patient populations — Use of S isomer (Esomeprazole) provides greater bioavailability in extensive metabolizers