장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킬 수 있음
특정 표적장기 독성 - 반복 노출
구분 2
경고
P260, P314, P501
예방조치문구:
P260
분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P272
작업장 밖으로 오염된 의복을 반출하지 마시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P302+P352
피부에 묻으면 다량의 물로 씻으시오.
P314
불편함을 느끼면 의학적인 조치·조언을 구하시오.
P333+P313
피부자극성 또는 홍반이 나타나면 의학적인 조치·조언를 구하시오.
Ziprasidone C화학적 특성, 용도, 생산
화학적 성질
Tan Solid
용도
Labelled Ziprasidone, which is used as an antipsychotic. Combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
정의
ChEBI: A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.
Biological Functions
"Ziprasidone is chemically similar to risperidone but with a substitution of piperzinyl and benzisothiazole for
piperidinyl and benzisoxazole and with minor aromatic modification. Like risperidone, ziprasidone is a high-affinity
antagonist at 5-HT2A/C and D2 receptors as well as at adrenergic α1/α2 and histamine H1 receptors. Moreover,
ziprasidone can activate 5-HT1A receptors that regulate dopaminergic neurotransmission in brain regions
involved in critical cognitive functions. Thus, in addition to D2 partial agonism, 5-HT1A agonism is now
thought to be an important pharmacological property for atypical antipsychotic drug efficacy.
일반 설명
Ziprasidone (Geodon, a benzisothiazolpiprazinylindolonederivative) also has the structuralfeatures of a hybrid molecule between a butyrophenone antipsychoticand a trazodone-like antidepressant. It is highlymetabolized to four major metabolites, only one of which, Smethyldihydroziprasidone,likely contributes to its clinical activity. In humans, less than 5% of the dose isexcreted unchanged. Reduction by aldehyde oxidase accountsfor about 66% of ziprasidone metabolism; two oxidative pathwaysinvolving hepatic CYP3A4 account for the remainder.
Mechanism of action
Ziprasidone
(half-life, 6 hours) has an oral bioavailability of approximately 60%, which can be enhanced in the presence of fatty
foods. It is extensively metabolized (<5% excreted unchanged) by aldehyde oxidase, which results in reductive
cleavage of the S–N bond, and then by S-methylation. Ziprasidone also can undergo CYP3A4-catalyzed
N-dealkylation and S-oxidation.
