Benzamides 化学特性,用途語,生産方法
適応症
Metoclopramide has been used extensively in the treatment of nausea and
vomiting secondary to GI disease and chemoradiotherapy. Surprisingly,
there is lile evidence for its efficacy in PONV. At standard doses, it blocks
D2 receptors in the gut and CTZ, but at higher doses, it also acts as a 5-HT3
receptor antagonist. Current preparations are available for intravenous, oral
and intramuscular administration. Adverse effects include extrapyramidal
symptoms, hypotension and sedation. Extrapyramidal symptoms are dose
related and occur most often in children and young adults. It is
recommended that intravenous administration take place over 1–2min to
reduce the risk of adverse effects.
一般的な説明
The benzamides evolved from observations that the gastroprokineticand antiemetic agent, metoclopramide, has antipsychoticactivity related to D
2 receptor block. It washoped that the group might yield compounds with diminishedEPS liability. This expectation appears to have beenmet. An H-bond between the amido H and the unsharedelectrons of the methoxyl group to generate a pseudo ring isconsidered important for antipsychotic activity in thesecompounds. Presumably, when the protonated amine is superimposedon that of protonated DA, this pseudo ringwould superimpose on DA’s aromatic ring.These featurescan be seen in sulpiride and remoxipride.
Benzamides 上流と下流の製品情報
原材料
準備製品