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클로자핀

클로자핀
클로자핀 구조식 이미지
카스 번호:
5786-21-0
한글명:
클로자핀
동의어(한글):
클로자핀
상품명:
Clozapine
동의어(영문):
Iprox;W-801;Fazaclo;ozapine;Lepotex;LEPONEX;LIPONEX;HF-1854;Klozapol;clorazil
CBNumber:
CB7776111
분자식:
C18H19ClN4
포뮬러 무게:
326.82
MOL 파일:
5786-21-0.mol

클로자핀 속성

녹는점
182-185°C
끓는 점
482.71°C (rough estimate)
밀도
1.1327 (rough estimate)
굴절률
1.6110 (estimate)
인화점
9℃
저장 조건
Store at RT
용해도
ethanol: 1 mg/mL
산도 계수 (pKa)
3.70, 7.60(at 25℃)
물리적 상태
powder
색상
pale yellow
Merck
14,2423
CAS 데이터베이스
5786-21-0(CAS DataBase Reference)
NIST
Clozapine(5786-21-0)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xn,Xi,T,F
위험 카페고리 넘버 22-36/37/38-68-63-39/23/24/25-23/24/25-11
안전지침서 26-36/37-45-16-7
유엔번호(UN No.) UN 2811 6.1/PG 3
WGK 독일 3
RTECS 번호 HP1750000
위험 등급 6.1(b)
포장분류 III
HS 번호 29339900
유해 물질 데이터 5786-21-0(Hazardous Substances Data)
독성 LD50 in mice, rats (mg/kg): 61, 58 i.v.; 199, 260 orally (Lindt)
그림문자(GHS):
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H225 고인화성 액체 및 증기 인화성 액체 구분 2 위험 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H301 삼키면 유독함 급성 독성 물질 - 경구 구분 3 위험 P264, P270, P301+P310, P321, P330,P405, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 P264, P280, P305+P351+P338,P337+P313P
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고
H341 유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재) 생식세포 변이원성 물질 구분 2 경고 P201,P202, P281, P308+P313, P405,P501
H361 태아 또는 생식능력에 손상을 일으킬 것으로 의심됨 생식독성 물질 구분 2 경고 P201, P202, P281, P308+P313, P405,P501
H370 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴(노출되어도 특정 표적장기 독성을 일으키지 않는다는 결정적인 노출경로가 있다면 노출경로를 기재) 특정 표적장기 독성 - 1회 노출 구분 1 위험 P260, P264, P270, P307+P311, P321,P405, P501
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P210 열·스파크·화염·고열로부터 멀리하시오 - 금연 하시오.
P260 분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P281 요구되는 개인 보호구를 착용하시오
P311 의료기관(의사)의 진찰을 받으시오.
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P405 밀봉하여 저장하시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

클로자핀 MSDS


8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine

클로자핀 C화학적 특성, 용도, 생산

화학적 성질

Yellow Crystalline Solid

용도

An antipsychotic

용도

depigmentor

정의

ChEBI: A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatr c disorders like schizophrenia.

상표명

Clozaril (Novartis); Fazaclo (Avanir);Leponox.

World Health Organization (WHO)

Clozapine, a tricyclic neuroleptic, was introduced in 1972 for the treatment of psychosis. In 1975 its use was associated with cases of agranulocytosis, particularly in Finland. These cases, which included several fatalities, resulted in the withdrawal of the drug in some countries. However, clozapine remains available in at least 30 countries, in some cases only on special request, for the treatment of severe psychotic disorders unresponsive to other neuroleptics provided that close monitoring of the blood count is feasible. In 1989, it was introduced in the United States for the treatment of severe schizophrenia. Lately, the use of clozapine in the United Kingdom has been associated with convulsions. (Reference: (WHODIB) WHO Drug Information Bulletin, 2: 10, , 1977)

일반 설명

Clozapine, 8-chloro-11-(4-methyl-1-piperazinyl)5H-dibenzo[b,e] [1,4] diazepine (Clozaril), is a yellowcrystalline powder that is only slightly soluble in water. Withthe introduction of clozapine, a different pharmacological antipsychotics.106 Unlike typical antipsychotics, clozapine is largelydevoid of EPS. The lack of EPS with this compound waspostulated to be caused by its preferential binding tomesolimbic rather than striatal DA receptors.Furthermore,clozapine was shown to exhibit potent affinity for 5-HT2Areceptors.
DMCZ shows partial agonism at D2 and D3 receptors andexhibits a distinctly different pharmacological profile comparedwith clozapine and other atypical antipsychotics.Unlike clozapine, which is a potent M1 muscarinic antagonist,DMCZ is a potent M1 agonist. Agonism at muscarinicreceptors has been proposed to be useful for impaired cognitionin schizophrenia. Burnstein et al.found thatDMCZ acted as a partial agonist at DA D2 and D3 receptors.These investigators suggested that the low incidence of EPSassociated with clozapine may be caused by the partial agonismof DMCZ at D2 and D3 receptors. Thus, DMCZ maybe of interest as an atypical antipsychotic with an improvedside effect profile compared with clozapine.

일반 설명

The dibenzodiazepine derivative is clozapine(Clozaril). It is not a potent antipsychotic on a milligrambasis (note the orientation of the N-methyl piperazino grouprelative to the chlorine atom). In addition to their moderatepotencies at DA receptors (mainly D4), clozapine interactwith varying affinities at several other classes of receptors(α1 and α2 adrenergic, 5-HT1A, 5-HT2A, 5-HT2C, muscariniccholinergic, histamine H1, and others). It is effective againstboth positive and negative symptoms of schizophrenia andhas a low tendency to produce EPS. Clozapine has proved effectiveeven in chronically ill patients who respond poorly tostandard neuroleptics. However, there are legal restrictionson its use because of a relatively high frequency of agranulocytosis.As a rule, two other antipsychotics are tried beforerecourse to therapy with clozapine. Clozapine is metabolized preferentially by CYP3A4 into demethylated, hydroxylated,and N-oxide derivatives that are excreted in urine and feces.Elimination half-life averages about 12 hours. Other clozapine-like atypical antipsychotics may lack a 2-Cl substituenton the aromatic ring (e.g., olanzapine and quetiapine).

생물학적 활성

Atypical antipsychotic drug, with a much lower tendency to cause extrapyramidal side effects than conventional neuroleptics. Displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT 2A/2C and dopamine receptor blockade (K i values are 21, 170, 170, 230 and 330 nM for D 4 , D 3 , D 1 , D 2 and D 5 receptors respectively).

Clinical Use

Although clozapine demonstrates a favorable pharmacologicalprofile compared with typical antipsychotics, its useis restricted by a relatively high incidence of agranulocytosis.The exact mechanism for the cause of agranulocytosishas not been confirmed, but a highly reactive nitrenium ionthat is formed by the action of hepatic enzymes appears tobe involved.The mean elimination half-life of clozapine following a single 75-mg dose is 8 hours. Because of severaladverse effects, clozapine is only used in refractory casesof schizophrenia. Individuals with a history of seizures orpredisposed to seizures should be cautioned when takingclozapine. Similar to other atypical antipsychotic agents,clozapine causes an increased risk of mortality in elderly individualswith dementia-related psychoses.

클로자핀 준비 용품 및 원자재

원자재

준비 용품


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