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  • 第一代和第二代H1 antihistamine和骨架(若為局部用標明在藥名後面)


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翻譯&機轉分類編輯

example編輯

HDCIs(Histidine decarboxylase inhibitors)編輯

histamine release inhibitors編輯

physiological antagonists編輯

H1 antihistamine編輯

  • 2nd generation H1 antihistamine有12個:
    • acrivastine
    • cetirizine
    • levocetirizine
    • loratadine
    • desloratadine
    • azacyclanol
    • terfenadine
    • fexofenadine
    • ebastine
    • carebastine
    • astemizole
    • mizolastine
  • topical H1 antihistamine有7個,且除了inhibitor of released histamine外尚有inhibitor of histamine release的功能(同khellin)
    • antazoline
    • ketotifen
    • olopatadine
    • epinastine(局部):nonsedating antihistamine
    • emedastine
    • azelastine
    • levocabastine
  • second generation的side effect由first generation的sedation變成cardiac arrythmia,譬如terfenadine and ebastine,此兩者的acid metaboltes:fexofenadinecarebastine則無。astemizole亦有、acravastine沒講、mizolastine和loratadine和desloratadine則無。cetirzinelevocetirizine亦無,but some drowsiness occurs( as first generation )

ethylenediamine編輯

Phenothiazines H1 antihistamine 編輯

H2 antihistamine編輯

功用編輯

延伸學習編輯

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H1 antihistamine骨架名 第一代 第二代 其他
ethylendiamine phenbenzamine(別和phenoxybenzamine搞混: 治療pheocromocytoma)
Pyrilamine
tripelennamine(pyribenzamine)
methapyrilene
thonzylamine
antazoline(局部、old drug,似α1 agonist(~zoline))
ethanolamine ether(aminoalky ether) Ex. benzhydryl ether(S is more pottent) Ex. diphenhydramine diphenhydramine(Benadryl)(Ex. dimenhydrinate(Dramamine)=diphenhydramine+8-chlorotheophylline)→phenyltoloxamine
bromodiphenhydramine
chlorodiphenhydramine
carbinoxamine
doxylamine
setastine
clemastine
orphenadrine antiparkinsonismspasmolytics(解痙藥)-drugs to skeletal muscle spasm-drugs for acute skeletal musle spasm: act on CNS from Foye e6th
alkylamine Ex.propylamines *飽和型 S(+)
pheniramine
chlorpheniramine→dexchlorpheniramine
brompheniramine→dexbrompheniramine
*不飽合型 E form
E-pyrrobutamine
E-triprolidine —(acidic congener in which a carboxylic acid-substituted chain has been attached)→ Acrivastine
dimethindene
piperazines: structure 和ethylenediamine和ethanolamine ether的benzhydryl ether相關 cyclizine
chlorcyclizine
meclizine
buclizine
oxatomide
hydroxyzine—(acidic metabolite(oxidation))→ cetirizine→levocetirizine
cinnarizine
tricyclic *phenothiazine
promethazine
ethopropazine
pyrathiazine
trimeprazine
methdilazine
*micellaneous
azatadine—(似)→ loratadine—(Metabolism)→desloratadine(decarboethoxyloratadine)
cyproheptadine Ex. (-)-3-methylcyproheptadine ketotifen, increase appetite for it's an antiserotonin
ketotifen(局部) 似cyproheptadine Ex. (-)-3-methylcyproheptadine
olopatadine(局部)
epinastine(局部):nonsedating antihistamine
ternenadine(2nd. generation (azacyclanol→)terfenadine(已下市)—(acid metabolite)→fexofenadine
Ebastine—(acid metabolite)→carebastine
astemizole(2nd. generation) 含benzimidazole emedastine(局部)有benzimidazole astemizole
mizolastine
azelastine(局部) 沒benzimidazole active metabolite
levocabastine(局部) levocabastine(局部)

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