盐酸克林霉素

盐酸克林霉素用途

Clindamycin hydrochloride 是一种半合成的林可胺类抗生素,通过作用于 50S ribosomal 来抑制蛋白质的合成。

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盐酸克林霉素作用

克林霉素是一种半合成的抗生素，具有抗菌谱广，抗菌活性强的特点，对革兰氏阳性菌有明显的抗菌活性，可以有效的杀灭葡萄球菌、厌氧菌、肺炎球菌和链球菌。对于肺囊虫、弓形虫、恶性疟原虫等致病性寄生虫都有活性作用，而且不良反应小。目前应用于临床的克林霉素制品有盐酸克林霉素、克林霉素磷酸酯以及克林霉素棕榈酸酯，其中克林霉素磷酸酯和克林霉素棕榈酸酯本身没有抗菌活性，在体内代谢为克林霉素后发挥抗菌、抗寄生虫的作用。
盐酸克林霉素是林可霉素的衍生物，盐酸克林霉素的抗菌谱比林可霉素广，抗菌活性比林可霉素高4-8倍。它对革兰氏阳性需氧菌、葡萄球菌、链球菌均有抗菌活性，对支原体、衣原体及多种厌氧菌也有抗菌活性。

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盐酸克林霉素名称

[ CAS 号 ]:
21462-39-5

[ 中文名 ]:
盐酸克林霉素

[ 英文名 ]:
Clindamycin Hydrochloride

[中文别名 ]:

[英文别名 ]:

EINECS 244-398-6
Cleocin HCL
MFCD07793327
7(S)-Chloro-7-deoxylincomycin hydrochloride
(7S)-7-Chloro-7-deoxylincomycin hydrochloride
7-Chloro-7-deoxylincomycin hydrochloride
Clindimycin hydrochloride
clindamycin hydrochloride
Clindamycin Impurity 14

盐酸克林霉素生物活性

[ 描述 ]:

Clindamycin hydrochloride 是一种半合成的林可胺类抗生素,通过作用于 50S ribosomal 来抑制蛋白质的合成。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[体外研究]

克林霉素是细菌蛋白质合成的经典抑制剂,通过与50S核糖体亚基的23S核糖体RNA结合[1]。

[体内研究]

克林霉素盐酸盐在狗口服给药后快速吸收,平均吸收时间(MAT)为0.87小时,生物利用度为72.55％。在口服给药(0.503对0.458L/h/kg)后,克林霉素盐酸盐导致克林霉素的总清除率(CL)。克林霉素盐酸盐在稳态(IV)下的体积分布为2.48L/kg,表明克林霉素在体液和组织中的分布广泛。静脉注射和口服给药后克林霉素血清浓度大约保持在0.5μg/ mL以上,持续10小时[1]。克林霉素盐酸盐显着降低狗的基线水平42天的口腔恶臭。克林霉素盐酸盐还可导致狗牙菌斑,牙结石和牙龈出血的显着减少[2]。超声波结垢,根面刨削和抛光(USRP)后,盐酸克林霉素(2.5 mg/Lb)对牙周病的牙菌斑和口袋深度测量有显着影响,但对犬的牙龈炎没有影响[3]。在14至28天内治疗后,盐酸克林霉素导致犬浅表性细菌性脓皮病犬的完全缓解率为71.4％(15/21)[4]。

[动物实验]

对于第一个实验期，在左侧头静脉导管插入后，向所有动物静脉内施用11mg / kg BW克林霉素盐酸盐（第0天）。在给药后不久取出导管（18G×51mm Abbocath-T）。在（t = 0h）和2,5,10,15,20,30,45分钟，1,1.5,2之前，通过从导管插入的侧头静脉抽吸将血样（3mL）收集到塑料管中。给药后2.5,2,4,5,6,8,10,12和24小时。每次取样后，用2mL 1％肝素化生理盐水冲洗静脉内导管。在第28天，所有狗都接受一个Antirobe胶囊（150mg克林霉素盐酸盐）。通过将接受的克林霉素的总量除以其体重，在每只动物中进行从mg /动物到mg / kg BW的剂量标准化。按照上述技术，在紧接之前（t = 0h）和15,30,45分钟，1,1.5,2,2.5,3,4,5,6,8,10,12进行血样采集。药物给药后24小时。将所有血液样品在暗处静置20分钟。在4℃下以1500g离心10分钟后，将上清液转移到5-mL塑料管中并储存在-30℃，等待分析。

[参考文献]

[1]. Batzias GC, et al. Clindamycin bioavailability and pharmacokinetics following oral administration of clindamycin hydrochloride capsules in dogs. Vet J. 2005 Nov;170(3):339-45.

[2]. Warrick JM, et al. Effect of clindamycin hydrochloride on oral malodor, plaque, calculus, and gingivitis in dogs with periodontitis. Vet Ther. 2000 Winter;1(1):5-16.

[3]. Nielsen D, et al. Effects of treatment with clindamycin hydrochloride on progression of canine periodontal disease after ultrasonic scaling. Vet Ther. 2000 Summer;1(3):150-8.

[4]. Bloom PB, et al. Efficacy of once-daily clindamycin hydrochloride in the treatment of superficial bacterial pyoderma in dogs. J Am Anim Hosp Assoc. 2001 Nov-Dec;37(6):537-42.

[相关活性小分子]

盐酸克林霉素物理化学性质

[ 沸点 ]:
628.1ºC at 760 mmHg

[ 熔点 ]:
141°C

[ 分子式 ]:
C₁₈H₃₄Cl₂N₂O₅S

[ 分子量 ]:
461.444

[ 闪点 ]:
333.6ºC

[ 精确质量 ]:
460.156555

[ PSA ]:
127.56000

[ LogP ]:
1.52030

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
1.79E-19mmHg at 25°C

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: 50 mg/mL, clear, colorless

盐酸克林霉素MSDS

详细MSDS(安全技术说明书)

盐酸克林霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GF2275000

CHEMICAL NAME :: Clindamycin, hydrochloride

CAS REGISTRY NUMBER :: 21462-39-5

LAST UPDATED :: 199706

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C18-H33-Cl-N2-O5-S.Cl-H

MOLECULAR WEIGHT :: 461.50

WISWESSER LINE NOTATION :: T6OTJ BS1 CQ DQ EQ FYYG1&MV- BT5NTJ A1 D3 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2193 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 18,354,1971

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 745 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 18,354,1971

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2618 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 21,516,1972

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 273 mg/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: -,331,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2539 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 18,354,1971

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 361 mg/kg

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

REFERENCE :: UPJOH* "Compounds Available for Fundamental Research, Volume II-6, Antibiotics, A Program of Upjohn Company Research Laboratory." (Kalamazoo, MI 49001) Volume(issue)/page/year: 2(6),-,1971

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1036 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 18,354,1971

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 245 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 21,516,1972

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1100 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: TOIZAG Toho Igakkai Zasshi. Journal of Medical Society of Toho University. (Toho Daigaku Igakkai, 21-16, Omori-nishi, 5-chome, Ota-ku, Tokyo 143, Japan) V.1- 1954- Volume(issue)/page/year: 18,354,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4823 No. of Facilities: 69 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 3168 (estimated) No. of Female Employees: 1697 (estimated)

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盐酸克林霉素安全信息

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36-37/39

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

[ WGK德国 ]:
2

[ RTECS号 ]:
GF2275000

[ 海关编码 ]:
2941904000

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盐酸克林霉素上游产品

盐酸克林霉素下游产品

盐酸克林霉素制备

氯林可霉素是洁霉素的衍生物，是洁霉素7位上的羟基被氯原子取代后所得的半合成抗生素

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盐酸克林霉素海关

[ 海关编码 ]: 2941904000

盐酸克林霉素文献

Performance characterization of a quantitative liquid chromatography-tandem mass spectrometric method for 12 macrolide and lincosamide antibiotics in salmon, shrimp and tilapia.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 967 , 203-10, (2014)

This paper describes an extension and performance characterization of a quantitative confirmatory multi-residue liquid chromatography-tandem mass spectrometric method for residues of macrolide and lin...

Development of a method to quantify clindamycin in vitreous humor of rabbits' eyes by UPLC-MS/MS: application to a comparative pharmacokinetic study and in vivo ocular biocompatibility evaluation.

J. Pharm. Biomed. Anal. 102 , 346-52, (2015)

Ocular toxoplasmosis may result in uveitis in the posterior segment of the eye, leading to severe visual complications. Clindamycin-loaded poly(lactide-co-glycolide) (PLGA) implants could be applied t...

A biodegradable antibiotic-impregnated scaffold to prevent osteomyelitis in a contaminated in vivo bone defect model.

Eur. Cell. Mater. 27 , 332-49, (2014)

Open fractures are at risk of serious infection and, if infected, require several surgical interventions and courses of systemic antibiotics. We investigated a new injectable formulation that simultan...

更多文献

盐酸克林霉素

盐酸克林霉素用途

盐酸克林霉素作用

盐酸克林霉素名称

盐酸克林霉素生物活性

盐酸克林霉素物理化学性质

盐酸克林霉素MSDS

详细MSDS(安全技术说明书)

盐酸克林霉素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

盐酸克林霉素安全信息

盐酸克林霉素上下游产品

盐酸克林霉素上游产品

盐酸克林霉素下游产品

盐酸克林霉素制备

盐酸克林霉素海关

盐酸克林霉素文献

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