トリクロルメチアジド

トリクロルメチアジド
IUPAC命名法による物質名
臨床データ
販売名 フルイトラン
Drugs.com Micromedex Detailed Consumer Information
胎児危険度分類
  • B (D if used to treat pregnancy-induced hypertension)
法的規制
  • JP: 処方箋医薬品
  • (Prescription only)
薬物動態データ
排泄ほぼ未変化体のまま尿中排泄
データベースID
CAS番号
133-67-5 チェック
ATCコード C03AA03 (WHO)
PubChem CID: 5560
IUPHAR/BPS英語版 7314
DrugBank DB01021Template:drugbankcite
ChemSpider 5359 ×
UNII Q58C92TUN0 ×
KEGG D00658 en:Template:keggcite
ChEMBL CHEMBL1054Template:ebicite
化学的データ
化学式C8H8Cl3N3O4S2
分子量380.6558 g/mol
テンプレートを表示

トリクロルメチアジド(Trichlormethiazide)はヒドロクロロチアジドと同じくチアジド系降圧利尿薬の一つである[1]腎臓遠位尿細管でのNa+/Cl再吸収を阻害する。またK+排泄を増加させる。通常、心不全肝硬変副腎皮質ホルモン治療、その他に伴う浮腫の治療や高血圧の治療に使用される[1]獣医学の分野では、ウマの四肢遠位の軽度腫脹や打撲の治療にデキサメタゾンと併用される[2]。商品名フルイトラン塩野義製薬製造販売。

効能・効果

日本で承認されている効能・効果は、以下の通りである[3]

  • 高血圧症(本態性、腎性等)
  • 悪性高血圧
  • 心性浮腫(鬱血性心不全)
  • 腎性浮腫
  • 肝性浮腫
  • 月経前緊張症

禁忌

下記の患者には禁忌とされている。

副作用

重大な副作用として添付文書に記載されているものは、再生不良性貧血低ナトリウム血症低カリウム血症である。

5%以上に現れる(または頻度不明の)副作用として、発疹、顔面潮紅、光線過敏症、電解質失調(低クロール性アルカローシス、血中カルシウム上昇等)、血清脂質増加、高尿酸血症、高血糖症が記載されている。

作用機序

トリクロルメチアジドは遠位尿細管でのクロル(塩素)イオン再吸収と、ナトリウムイオンの再吸収を阻害する。ナトリウム、クロルとともに水分が排泄され、その結果、利尿効果がもたらされる[1]

合成経路

トリクロルメチアジドの化学名は、1,1-dioxide 3,4-dihydro-3-(dichlormethyl)-6-chloro-2H-1,2,4-benzothiadiazin-7-sulfonamideである。

トリクロルメチアジド合成法[4][5][6][7][8][9]

出典

  1. ^ a b c DrugBank: DB01021 (Trichlormethiazide)”. DrugBank. 2008年1月23日閲覧。
  2. ^ Trichlormethiazide and Dexamethasone for veterinary use”. Wedgewood Pharmacy. 2008年1月24日閲覧。
  3. ^ フルイトラン錠1mg/フルイトラン錠2mg 添付文書” (2013年9月). 2015年7月4日閲覧。
  4. ^ Scherico Ltd., Br. GB 949373  (1960).
  5. ^ G. de Stevens, L.H. Werner, Ger. DE 1147233  (1960).
  6. ^ De Stevens, G; Werner, L. H.; Barrett, W. E.; Chart, J. J.; Renzi, A. H. (1960). “The chemistry and pharmacology of hydrotrichlorothiazide”. Experientia 16: 113-4. PMID 13815073. 
  7. ^ M.H. Sherlock, N. Sperber, J. Topliss, Experientia, 16, 184 (1960).
  8. ^ Scherico Ltd., GB 954023  (1960).
  9. ^ W.J. Close, アメリカ合衆国特許第 3,264,292号 (1960).

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