青霉素V

青霉素V用途

青霉素V(苯氧甲基青霉素)是一种有效的口服抗生素。青霉素V对链球菌、艰难梭菌和金黄色葡萄球菌具有抗菌活性。青霉素V具有研究中耳炎、鼻窦炎、咽炎和扁桃体炎的潜力[1][2][3][4]。

青霉素V名称

[ CAS 号 ]:
87-08-1

[ 中文名 ]:
青霉素V

[ 英文名 ]:
Penicillin-V

[中文别名 ]:

[英文别名 ]:

penicillin-V
Oracillin
Pen-vee-oral
Fenospen
Penicillin phenoxymethyl
PenicillinV
Phenocillin
Beromycin
Phenopenicillin
Acipen-V

青霉素V生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[体外研究]

青霉素V(0.002-8.0mg/L)抑制链球菌的生长,最低抑制浓度(MIC)为0.004-0.008mg/L[2]。青霉素V(0.002-8.0 mg/L)对艰难梭菌具有抗菌活性,MIC50值为4.0 mg/L,MIC90值为8.0 g/L[3]。青霉素V(0.004-0.063 mg/L；18 h)抑制金黄色葡萄球菌的生长,MIC值为0.016 mg/L[4]。

[体内研究]

青霉素V(0.063-0.25mg/kg；s.c.)抑制小鼠大腿肌肉中金黄色葡萄球菌的生长[4]。青霉素V(2 mg/kg；s.c.)的血浆半衰期(61 min)和平均AUC(0.47 mg/L·h)[4]。青霉素V(100mg/kg；每天一次,持续5天)可避免大鼠急性化脓性中耳炎(AOM)的暴发性感染[5]。动物模型：无特异性病原体(SPF)雄性瑞士小鼠(20-25 g)接种金黄色葡萄球菌[4]剂量：0.063、0.13、0.25 mg/kg给药：S.c.结果：与对照组(3.5×107计数/mL)相比,0.25 g/kg剂量下的CFU数量(1.34×107计数/mL)减少。

[参考文献]

[1]. Sabath LD. Et, al. Phenoxymethylpenicillin (penicillin V) and phenethicillin. Med Clin North Am. 1970 Sep;54(5):1101-11.

[2]. Kamme C, et, al. In vitro effect on group A streptococci of loracarbef versus cefadroxil, cefaclor and penicillin V. Scand J Infect Dis. 1993;25(1):37-42.

[3]. Norén T, et, al. In vitro susceptibility to 17 antimicrobials of clinical Clostridium difficile isolates collected in 1993-2007 in Sweden. Clin Microbiol Infect. 2010 Aug;16(8):1104-10.

[4]. Overbosch D, et, al. Comparative pharmacodynamics and clinical pharmacokinetics of phenoxymethylpenicillin and pheneticillin. Br J Clin Pharmacol. 1985 May;19(5):657-68.

[5]. Hermansson A, et, al. Prevention of experimental acute otitis media with penicillin V. Acta Otolaryngol. Jan-Feb 1990;109(1-2):119-23.

[6]. Timm A, et al. Photolysis of four β‑lactam antibiotics under simulated environmental conditions: Degradation, transformation products and antibacterial activity. Sci Total Environ. 2019 Feb 15;651(Pt 1):1605-1612.

青霉素V物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
681.4±55.0 °C at 760 mmHg

[ 熔点 ]:
120 - 128ºC

[ 分子式 ]:
C₁₆H₁₈N₂O₅S

[ 分子量 ]:
350.389

[ 闪点 ]:
365.9±31.5 °C

[ 精确质量 ]:
350.093628

[ PSA ]:
121.24000

[ LogP ]:
1.88

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.651

[ 储存条件 ]:
−20°C

[ 稳定性 ]:
Stable. Combustible. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
Very slightly soluble in water, soluble in ethanol (96 per cent).

青霉素V毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RY4025000

CHEMICAL NAME :: Penicillanic acid, 6-phenoxyacetamido-

CAS REGISTRY NUMBER :: 87-08-1

BEILSTEIN REFERENCE NO. :: 0096259

LAST UPDATED :: 199612

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C16-H18-N2-O5-S

MOLECULAR WEIGHT :: 350.42

WISWESSER LINE NOTATION :: T45 ANV ESTJ CMV1OR& F1 F1 GVQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 10 mg/kg/2D

TOXIC EFFECTS :: Liver - liver function tests impaired Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - body temperature increase

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2220 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1775 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1600 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6578 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1351 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 gm/kg

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

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1775 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 822 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1096 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Rodent - mouse Ascites tumor

DOSE/DURATION :: 200 ug/L

REFERENCE :: NEOLA4 Neoplasma. (Karger-Libri, P.O. Box, CH-4009 Basel, Switzerland) V.4- 1957- Volume(issue)/page/year: 22,105,1975 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83957 No. of Facilities: 61 (estimated) No. of Industries: 2 No. of Occupations: 6 No. of Employees: 2874 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83957 No. of Facilities: 114 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 1964 (estimated) No. of Female Employees: 959 (estimated)

青霉素V安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R42/43

[ 安全声明 (欧洲) ]:
22-36

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

[ RTECS号 ]:
RY4025000

[ 海关编码 ]:
3003101300

青霉素V合成路线

详细合成路线

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青霉素V海关

[ 海关编码 ]: 3003101300

青霉素V文献

Fast targeted analysis of 132 acidic and neutral drugs and poisons in whole blood using LC-MS/MS.

Forensic Sci. Int. 243 , 35-43, (2014)

The aim of this study was to develop an LC-MS/MS based screening technique that covers a broad range of acidic and neutral drugs and poisons by combining a small sample volume and efficient extraction...

Molecularly imprinted polymer nanocarriers for sustained release of erythromycin.

Pharm. Res. 32(2) , 375-88, (2015)

To develop and evaluate molecularly imprinted nanocarriers for sustained release of erythromycin in physiological buffer media.Erythromycin-imprinted poly(methacrylic acid-co-trimethylolpropane trimet...

Follow-up study of implants with turned or oxidized surfaces placed after sinus augmentation.

Int. J. Oral Maxillofac. Implants 29(6) , 1380-7, (2014)

To compare long-term survival and clinical outcomes of endosseous implants with different surface characteristics in patients with sinus elevation procedures, autologous bone grafting, and delayed imp...

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