GUANFACINE HCL

GUANFACINE HCL 구조식 이미지
카스 번호:
29110-48-3
상품명:
GUANFACINE HCL
동의어(영문):
GUANFACINE HYDROCHLORIDE;Tenex;Intuniv;lon798;estulic;bs100-141;Guarfacine;Guanfascine;GUANFACINE HCL;Guanfacine HCL powder
CBNumber:
CB0767424
분자식:
C9H10Cl3N3O
포뮬러 무게:
282.55
MOL 파일:
29110-48-3.mol
MSDS 파일:
SDS

GUANFACINE HCL 속성

녹는점
215-217℃
RTECS 번호
CY1481000
저장 조건
Inert atmosphere,Room Temperature
용해도
H2O: 12 mg/mL @60 °C, 가용성
물리적 상태
고체
물리적 상태
단단한 모양
색상
하얀색
Merck
14,4561
안정성
흡습성
InChIKey
DGFYECXYGUIODH-UHFFFAOYSA-N
CAS 데이터베이스
29110-48-3(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
유엔번호(UN No.) 3249
WGK 독일 3
위험 등급 6.1(b)
포장분류 III
HS 번호 2925294500
독성 LD50 in mice: 165 mg/kg orally (Coward)
그림문자(GHS): GHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H301 삼키면 유독함 급성 독성 물질 - 경구 구분 3 위험 GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
예방조치문구:
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P321 (…) 처치를 하시오.
P405 밀봉하여 저장하시오.
NFPA 704
0
2 0

GUANFACINE HCL C화학적 특성, 용도, 생산

용도

Centrally acting a-adrenoceptor agonist. Antihypertensive

일반 설명

Guanfacine hydrochloride,N-(aminoiminomethyl)-2,6-dichlorobenzeneacetamide(Tenex), is structurally related to clonidine hydrochloride andguanabenz acetate and shares many of their pharmacologicalproperties. The drug has a longer duration of action than eitherclonidine hydrochloride or guanabenz acetate. It lasts upto 24 hours. It also requires much longer (8–12 hours) for apeak effect to occur after the drug is administered.

생물학적 활성

Selective α 2A -adrenoceptor agonist (K d = 31 nM). Displays 60-fold selectivity over α 2B -adrenoceptors. Also available as part of the α 2 -Adrenoceptor Tocriset™ .

Pharmacokinetics

The pharmacokinetic properties for guanfacine differ from those of clonidine, guanabenz, and α-methyldopa. At pH 7.4, guanfacine is predominately (67%) in the nonionized, lipid-soluble base form, which accounts for its high oral bioavailability (>80%). Following an oral dose, peak plasma concentrations occur in 1 to 4 hours, with a relatively long elimination half-life of 14 to 23 hours. The maximum blood pressure response occurs in 8 to 12 hours after oral administration and is maintained up to 36 hours following its discontinuation. Following IV dosing, guanfacine achieves the highest concentrations in liver and kidney, with low concentrations in the brain. Guanfacine is 64% bound to plasma proteins. In patients with hepatic or renal impairment, its elimination half-life may be prolonged.
Guanfacine is metabolized principally by hepatic hydroxylation to its inactive metabolite, 3-hydroxyguanfacine (20%), which is eliminated in the urine as its glucuronide (30%), sulfate (8%), or mercapturic acid conjugate (10%), and 24 to 37% is excreted as unchanged guanfacine. Its nearly complete bioavailability suggests no evidence of any first-pass effect. Guanfacine and its inactive metabolites are excreted principally in urine, with approximately 80% of its oral dose excreted in urine within 48 hours.

Clinical Use

Overall, the therapeutic applications for guanfacine are similar to those of the other centrally acting α2-adrenergic agonists and methyldopa. It has been effective as monotherapy in the treatment of patients with mild to moderate hypertension. One advantage for guanfacine is its once-a-day dosing schedule. The use of diuretics to prevent accumulation of fluid may allow a reduction in the dosage for guanfacine.

부작용

Overall, although the frequency of troublesome adverse effects produced by guanfacine is similar to that produced by clonidine and the other centrally acting sympatholytics, their incidence and severity are lower with guanfacine. Unlike clonidine, abrupt discontinuation of guanfacine rarely results in rebound hypertension. When a withdrawal syndrome has occurred, its onset was slower and its symptoms less severe than the syndrome observed with clonidine.

GUANFACINE HCL 준비 용품 및 원자재

원자재

준비 용품


GUANFACINE HCL 공급 업체

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Hebei Yanxi Chemical Co., Ltd.
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ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32480 60
career henan chemical co
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Chongqing Chemdad Co., Ltd
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CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 47465 58
Zhengzhou Alfa Chemical Co.,Ltd
+8618530059196
sale04@alfachem.cn China 12321 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 19892 58
Hubei Ipure Biology Co., Ltd
+8613367258412
ada@ipurechemical.com China 10326 58

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