| 中文名称 | 甲砜霉素 |
| 英文名称 | Thiamphenicol |
| CAS号 | 15318-45-3 |
| 分子式 | C12H15Cl2NO5S |
| 分子量 | 356.22 |
| EINECS号 | 239-355-3 |
| 熔点 | 163-166 °C |
| 比旋光度 | D25 +12.9° (ethanol) |
| 沸点 | 695.9±55.0 °C(Predicted) |
| 密度 | 1.3281 (rough estimate) |
| 折射率 | 1.6000 (estimate) |
| 溶解度 | 乙醇:50 mg/mL,澄清,无色 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 11.05±0.46(Predicted) |
| 颜色 | 白色至类白色 |
| 水溶解性 | Soluble in acetonitrile or DMF. Slightly soluble in water |
| 默克索引编号 | 14,9301 |
| BRN | 2819542 |
| 安全说明 | 22-24/25 |
| WGK Germany | 2 |
| RTECS号 | AB6680000 |
| 海关编码 | 29414000 |
| 毒性 | human,TDLo,unreported,214mg/kg/10D (214mg/kg),BEHAVIORAL: SLEEPGASTROINTESTINAL: NAUSEA OR VOMITINGSKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE",Arzneimittel-Forschung. Drug Research. Vol. 24, Pg. 944, 1974. |
甲砜霉素为广谱抑菌剂。对大多数革兰氏阳性菌和革兰氏阴性菌均有抑制作用。特别是对革兰氏阴性杆菌作用强大,如对大肠杆菌、沙门氏菌、伤寒杆菌、产气杆菌、克雷伯氏杆菌、巴氏杆菌、布氏杆菌、痢疾杆菌等作用较强,革兰氏阳性菌中如炭疽杆菌、葡萄球菌、棒状杆菌、肺炎球菌、链球菌、肠球菌和放线菌对其亦较敏感。但对革兰氏阳性菌的作用不及青霉素和四环素。对钩端螺旋体、某些霉形体、部分衣原体和立克次氏体亦有作用。细菌对本品与氯霉素间有完全的交叉耐药性,与四环素类之间有部分文交叉耐药性。
Thiamphenicol (Thiophenicol) 是一种抗菌的抗生素,是Chloramphenicol的甲磺酰基类似物。Thiamphenicol shows a significant post-antibiotic effect (PAE) (0.33 to 2.9h) on all pathogens studied ( S. pneumoniae , S. aureus and Escherichia coli ) and a powerful bactericidal effect against β-lactamase-positive and -negative H. influenzae . Thiamphenicol MICs for the microorganisms analyzed are: 32 mg/L ( S. aureus and E. coli ), 2 mg/L ( S. pneumoniae ) and 0.25 mg/L ( H. influenzae ). Thiamphenicol shows a good in vitro activity against difficult-to-treat multiply resistant pathogens.
The pharmacokinetics of Thiamphenicol (30 mg/kg) after single intravenous (IV) and oral (PO) administration is investigated in Mulard ducks. After IV administration, for Thiamphenicol, the mean residence time is 2.83 hours, the general half-life is 1.96 hours, the clearance is 0.04 L/hr/kg. Pharmacokinetics after PO administration is very similar for IV administration. Thiamphenicol shows rapid absorption and bioavailability of more than 70%.