- 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[]
- Histamine antagonist(組織胺拮抗劑有四種機轉:
- synthesis inhibitor:HDCIs(Histidine decarboxylase inhibitors)
- histamine release inhibitors
- physiological antagonists:epinephrine
- histamine receptor antagonists, 通常稱作Antihistamines(抗組織胺，依照此抗組織胺為和哪一種histamine receptor結合而有不同的功能，是一種inverse agonist而非一種antagonist
- H1: treating pruritus
- H2: 抗胃潰瘍
example[]
HDCIs(Histidine decarboxylase inhibitors)[]
- trifluoromethylhistidine:不可逆抑制劑
- α-fluoromethylhistidine(FMH)
- some flavanoids
histamine release inhibitors[]
physiological antagonists[]
H1 antihistamine[]
- 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:fexofenadine和carebastine則無。astemizole亦有、acravastine沒講、mizolastine和loratadine和desloratadine則無。cetirizine和levocetirizine亦無，but some drowsiness occurs( as first generation )
ethylenediamine[]
Phenothiazines H1 antihistamine[]
- promethazine
- trimeprazine
- methdilazine
H2 antihistamine[]
功用[]
延伸學習[]
| H1 antihistamine骨架名 | 第一代抗組織胺 | 第二代抗組織胺 | 其他(註) |
|---|---|---|---|
| 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 | antiparkinsonism、spasmolytics(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 | 似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) |
懷孕與哺乳的抗組織胺[]
懷孕[]
Diphenhydramine(B)[1][2][3]、loratadine[4][3]、meclizine[1]、doxylamine[1]、cetirizine[4]
哺乳[]
建議優先使用第二代抗組織胺，除了分泌至乳汁的比例極少也較不會引起小朋友嗜睡。loratadine[5]