ロペラミド塩酸塩 化学特性,用途語,生産方法
外観
白色～わずかにうすい黄色, 結晶性粉末～粉末
溶解性
エタノール(95)にやや溶けやすく、水に難溶である。
用途
腸管のオピオイド受容体に作 用し、腸管蠕動運動抑制作用を示します。ま た、アセチルコリン遊離抑制作用も示します。
用途
腸管のオピオイド受容体に作
用し、腸管蠕動運動抑制作用を示します。ま
た、アセチルコリン遊離抑制作用も示します。
効能
止瀉薬, 蠕動抑制薬, オピオイド受容体作動薬
商品名
ロスポリア (日医工); ロペミン (ヤンセンファーマ); ロペミン (ヤンセンファーマ); ロペラミド塩酸塩 (ダイト)
化学的特性
White Solid
使用
Loperamide hydrochloride is a Ca2+ channel protein inhibitor and MOR activator.
適応症
Loperamide hydrochloride (Imodium) structurally
resembles both haloperidol and meperidine. In equal
doses, loperamide protects against diarrhea longer than
does diphenoxylate. It reduces the daily fecal volume
and decreases intestinal fluid and electrolyte loss.
Loperamide produces rapid and sustained inhibition of
the peristaltic reflex through depression of longitudinal
and circular muscle activity.The drug also possesses antisecretory
activity, presumably through an effect on intestinal
opioid receptors.
定義
ChEBI: A hydrochloride obtained by combining loperamide with one equivalent of hydrochloric acid. Used for treatment of diarrhoea resulting from gastroenteritis or inflammatory bowel disease.
一般的な説明
Loperamide is an antidiarrheal agent used in controlling acute nonspecific diarrhea and chronic diarrhea associated with inflammatory bowel diseases.
生物活性
High affinity μ -opioid receptor agonist with peripheral selectivity (K i values are 2, 48 and 1156 nM for μ -, δ - and κ -opioid receptors respectively). Antidiarrhoeal and antihyperalgesic agent. Also a Ca 2+ channel blocker; at low micromolar concentrations it blocks broad spectrum neuronal HVA Ca 2+ channels and at higher concentrations it reduces Ca 2+ flux through NMDA receptor operated channels.
作用機序
Loperamide also is a potent inhibitor of intestinal CYP3A4, increasing the intestinal absorption of
other CYP3A4 substrates. The clinically significant drug interactions of loperamide with
coadministered CYP3A4 and CYP2C8 substrates or inhibitors would be limited, however, because
of its two metabolic pathways.
薬物動態学
Loperamide is
marketed as capsules (2 mg) and liquid (1 mg/5 mL) preparations. The recommended dose is 4 mg
initially and an additional 2 mg following each diarrheal stool. The dose should not exceed 16
mg/day. It is too lipophilic to dissolve in water for an intravenous dosage form, a property that limits
its abuse potential. The compound is highly lipophilic and undergoes slow dissolution, thus limiting
the bioavailability of the agent to approximately 40% of the dose. Its low oral bioavailability also
can be attributed to first-pass metabolism by both CYP2C8 and CYP3A4 to its primary N-demethyl
metabolite. Peak plasma levels are reached in approximately 5 hours, with an elimination half-life
of approximately 11 hours. Approximately 1% of the dose is excreted into the urine unchanged.
臨床応用
Loperamide is effective
against a wide range of secretory stimuli and can be
used in the control and symptomatic relief of acute diarrhea
that is not secondary to bacterial infection.
副作用
Adverse effects associated with its use include abdominal
pain and distention, constipation, dry mouth, hypersensitivity,
and nausea and vomiting.
ロペラミド塩酸塩 上流と下流の製品情報
原材料
準備製品