ジフェノキシラート 化学特性,用途語,生産方法
効能
止瀉薬, 蠕動抑制薬, オピオイド受容体作動薬
使用
Antiperistaltic.
定義
ChEBI: A piperidinecarboxylate ester that is the ethyl ester of difenoxin.
適応症
Diphenoxylate (marketed in combination with atropine
as Lomotil in the United States) is chemically related
to both analgesic and anticholinergic compounds.
It is as effective in the treatment of diarrhea as the
opium derivatives, and at the doses usually employed, it
has a low incidence of central opioid actions. Diphenoxylate
is rapidly metabolized by ester hydrolysis to the
biologically active metabolite difenoxylic acid.
世界保健機関（WHO）
Diphenoxylate, a derivative of pethidine without analgesic
activity, is used in the symptomatic treatment of acute and chronic diarrhoea to
reduce intestinal motility. There is no clear evidence that it has any beneficial effect
in diminishing fluid losses and it has been associated with central nervous system
toxicity, particularly in children, which results in anorexia, nausea and vomiting,
headache, drowsiness, confusion, insomnia, dizziness, restlessness, euphoria and
depression. The World Health Organization recommends that diphenoxylate should
not be used for the management of diarrhoea in children and many countries have
since withdrawn products containing this compound indicated for paediatric use.
(Reference: (WHORUD) The Rational Use of Drugs, , , 1990)
一般的な説明
Diphenoxylate is a weak opioid agonist and isavailable combined with atropine (Lomotil) for use as an antidiarrhealagent. At low doses, the opioid effect is minimal,and the atropine is added to dissuade abuse. One studyfound both codeine and loperamide to be superior to diphenoxylatefor treating chronic diarrhea.83 The manufacturerhas strict dosing guidelines for pediatric use because opioidintoxication and deaths from diphenoxylate have beenreported.
臨床応用
Lomotil is recommended as adjunctive therapy in the management
of diarrhea. It is contraindicated in children under
2 years old and in patients with obstructive jaundice.
副作用
Adverse reactions often caused by the atropine in the
preparation include anorexia, nausea, pruritus, dizziness,
and numbness of the extremities.
ジフェノキシラート 上流と下流の製品情報
原材料
準備製品