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氯噻酮

氯噻酮用途

Chlorthalidone 是一种噻嗪类利尿剂,可用于治疗高血压。

氯噻酮名称

[ CAS 号 ]:
77-36-1

[ 中文名 ]:
氯噻酮

[ 英文名 ]:
Chlorthalidone

[中文别名 ]:

氯塞酮

[英文别名 ]:

Higroton
(±)-Chlorthalidone
Chlorthalidone
MFCD00036257
chlortalidone
(±)-Hygroton
EINECS 201-022-5

氯噻酮生物活性

[ 描述 ]:

Chlorthalidone 是一种噻嗪类利尿剂,可用于治疗高血压。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 心血管疾病

[体内研究]

氯噻酮是一种类似噻嗪类的利尿剂。口服摄入后,在2-6小时内达到峰值血清浓度。氯噻酮的半衰期约为42小时(范围29-55)小时,在长期给药后达到45-60小时。然而,氯噻酮的半衰期的个体差异很大。氯噻酮通过肾脏不变地排泄。氯噻酮的利钠作用在18小时时最大,持续超过48小时。比较不同剂量的氯噻酮,已观察到每日25毫克几乎与较高剂量一样有效,但低钾血症风险较低[1]。氯噻酮可减少草酸钙的结石复发,但氢氧化镁则不会。在预防复发的草酸钙肾结石中检查了氯噻酮或氢氧化镁的有效性。在双盲随机分配设计中,每日剂量为25或50毫克。氯噻酮,650或1,300毫克。给予氢氧化镁或相同的安慰剂。与预处理率相比,所有组显示显着减少的结石事件。在试验期间,安慰剂组发生的结石比预测的结石少56.1％(p <0.01),而接受低剂量和高剂量氢氧化镁的组分别显示73.9％和62.3％的结石(p小于0.001且小于分别为0.01)。氯噻酮治疗导致预测率下降90.1％,两种剂量均产生类似结果。当比较治疗时,氯噻酮明显优于安慰剂或氢氧化镁(p小于0.01)。当给予安慰剂或无效治疗时,观察到的结石事件的大量减少强调了当使用历史对照时发生的积极治疗偏差并且他们证明需要适当的实验设计[2]。

[参考文献]

[1]. Barrios V, et al. Which thiazide to choose as add-on therapy for hypertension? Integr Blood Press Control. 2014 Jul 30;7:35-47.

[2]. Ettinger B, et al. Chlorthalidone reduces calcium oxalate calculous recurrence but magnesium hydroxide does not. J Urol. 1988 Apr;139(4):679-84.

[相关活性小分子]

氯噻酮物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 熔点 ]:
265-267ºC (dec.)

[ 分子式 ]:
C₁₄H₁₁ClN₂O₄S

[ 分子量 ]:
338.766

[ 精确质量 ]:
338.012817

[ PSA ]:
117.87000

[ LogP ]:
-0.74

[ 外观性状 ]:
白色至淡黄色-白色结晶粉末无气味的

[ 折射率 ]:
1.694

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: soluble5mg/mL, clear (warmed)

氯噻酮MSDS

详细MSDS(安全技术说明书)

氯噻酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DB1556000

CHEMICAL NAME :: Benzenesulfonamide, 2-chloro-5-(1-hydroxy-3-oxo-1-isoindolinyl)-

CAS REGISTRY NUMBER :: 77-36-1

BEILSTEIN REFERENCE NO. :: 0312295

LAST UPDATED :: 199612

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C14-H11-Cl-N2-O4-S

MOLECULAR WEIGHT :: 338.78

WISWESSER LINE NOTATION :: T56 BVM DHJ DQ DR DG CSZW

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 2587 ug/kg/8D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - headache Gastrointestinal - nausea or vomiting

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 258,484,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5714 ug/kg/4D-I

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section Endocrine - hyperglycemia Blood - other changes

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 220,1592,1972

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 12 mg/kg/6D-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - changes in sodium Nutritional and Gross Metabolic - changes in chlorine

REFERENCE :: SMJOAV Southern Medical Journal. (Southern Medical Assoc., POB 2446, Birmingham, AL 35205) V.1- 1908- Volume(issue)/page/year: 79,629,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,249,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,249,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,249,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,249,1982 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30 mg/kg

SEX/DURATION :: male 3 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - impotence

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 281,714,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2200 mg/kg

SEX/DURATION :: female 2-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: MPHEAE Medicina et Pharmacologia Experimentalis. (Basel, Switzerland) V.12-17, 1965-67. For publisher information, see PHMGBN. Volume(issue)/page/year: 12,245,1965 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5337 No. of Facilities: 76 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1116 (estimated) No. of Female Employees: 652 (estimated)

氯噻酮安全信息

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
DB1556000

[ 海关编码 ]:
2935009090

氯噻酮合成路线

详细合成路线

氯噻酮制备

由苯酐与氯苯加成、经硝化、还原得邻（3-氨基-4-氯苯甲酰）苯甲酸，然后经重氮化、置换、氯磺化，最后经环合、胺化制得。

氯噻酮海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

氯噻酮文献

Which diuretic is the preferred agent for treating essential hypertension: hydrochlorothiazide or chlorthalidone?

Curr. Cardiol. Rep. 14(6) , 673-7, (2012)

Since their introduction over 50 years ago thiazide and thiazide-like diuretics have been a mainstay in the treatment of hypertension. Yet despite outcome evidence with chlorthalidone, the preponderan...

Comparing clinical effectiveness and drug toxicity with hydrochlorothiazide and chlorthalidone using two potency ratios in a managed care population.

J. Clin. Hypertens. (Greenwich.) 17(2) , 134-40, (2015)

This study compared the clinical effectiveness and drug toxicity of chlorthalidone and hydrochlorothiazide. Electronic health records and claims data were used to identify patients initially prescribe...

Chlorthalidone versus hydrochlorothiazide for the treatment of hypertension in older adults: a population-based cohort study.

Ann. Intern. Med. 158(6) , 447-55, (2013)

Some evidence suggests that chlorthalidone may be superior to hydrochlorothiazide for the treatment of hypertension.To compare the effectiveness and safety of chlorthalidone and hydrochlorothiazide in...

更多文献

氯噻酮