Erythromycin lactobionate
(Synonyms: 红霉素乳糖酸盐) 目录号 : GC43627A macrolide antibiotic and water-soluble form of erythromycin
Cas No.:3847-29-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Erythromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains.[1] It is effective against a host of bacterial genera, including Streptococcus, Staphylococcus, and Haemophilus (MIC90s range from 0.015-2.0 mg/l).[2] Erythromycin is known to potently inhibit the cytochrome P450 isoform CYP3A4, which can affect the metabolism of numerous clinically relevant medications.[3],[4] Erythromycin lactobionate is a soluble salt of erythromycin that is typically used for intraperitoneal or intravenous injections.[5],[6]
Reference:
[1]. Wilson, D.N. The A-Z of bacterial translation inhibitors. Crit. Rev. Biochem. Mol. Biol. 44(6), 393-433 (2009).
[2]. Kanatani, M.S., and Guglielmo, B.J. The new macrolides. Azithromycin and clarithromycin. Western J. Med. 160(1), 31-37 (1994).
[3]. Westphal, J.F. Macrolide - induced clinically relevant drug interactions with cytochrome P-450A (CYP) 3A4: An update focused on clarithromycin, azithromycin and dirithromycin. Br. J. Clin. Pharmacol. 50(4), 285-295 (2000).
[4]. Bibi, Z. Role of cytochrome P450 in drug interactions. Nutr. Metab. (Lond) 5(27), 1-10 (2008).
[5]. Hirakata, Y., Kaku, M., Tomono, K., et al. Efficacy of erythromycin lactobionate for treating Pseudomonas aeruginosa bacteremia in mice. Antimicrobial Agents and Chemotherapy 36(6), 1198-1203 (1992).
[6]. Austin, K.L., Mather, L.E., Philpot, C.R., et al. Intersubject and dose-related variability after intravenous administration of erythromycin. British Journal of Clinical Pharmacology 10(3), 273-279 (1980).
| Cas No. | 3847-29-8 | SDF | |
| 别名 | 红霉素乳糖酸盐 | ||
| 化学名 | 4-O-β-D-galactopyranosyl-D-gluconate erythromycin | ||
| 分子式 | C37H67NO13•C12H22O12 | 分子量 | 1092.2 |
| 溶解度 | 1mg/mL in water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9156 mL | 4.5779 mL | 9.1558 mL |
| 5 mM | 0.1831 mL | 0.9156 mL | 1.8312 mL |
| 10 mM | 0.0916 mL | 0.4578 mL | 0.9156 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
QTc-interval prolongation associated with slow intravenous Erythromycin lactobionate infusions in critically ill patients: a prospective evaluation and review of the literature
Pharmacotherapy 1996 Jul-Aug;16(4):663-74.PMID:8840374doi
Intravenous erythromycin has recently been associated with significant QTc interval prolongation, torsades de pointes, and sudden cardiac death. The prolonged the QTc interval attributed to erythromycin typically is associated with rapid infusion rates in excess of 10 mg/minute. We prospectively assessed the relationship between QTc interval prolongation and erythromycin administration by slow intravenous infusion (mean rate 8.9 +/- 3.5 mg/minute, range 3.9-16.7 mg/minute). Electrocardiographic (ECG) rhythm strips were prospectively obtained in 44 critically ill patients receiving intravenous antibiotics (22 received erythromycin and 22 ceftazidime, cefuroxime, cefotaxime, ceftriaxone, or ampicillin-sulbactam as controls). The ECG recordings were obtained immediately before and within 15 minutes after drug infusions. Only the first available set of ECG strips were evaluated. Two controls had evidence of hepatic dysfunction; no patients receiving erythromycin did. The QTc interval was calculated using Bazett's formula by two blinded investigators. For controls, mean +/- 1 SD (range) QTc intervals were 423 +/- 96 (300-550) msec at baseline and 419 +/- 96 (280-610) msec after infusion (p = 0.712). In contrast, in the erythromycin group, the interval was significantly prolonged from 524 +/- 105 (360-810) msec at baseline to 555 +/- 134 (400-980) msec after infusion (p = 0.034). No patients experienced a dysrhythmia as a consequence of erythromycin infusion. Despite slow rates of infusion, QTc interval prolongation was significant. The clinical importance of this finding remains to be determined.
Intravenous erythromycin lactobionate-induced severe nausea and vomiting
DICP 1989 Jan;23(1):40-4.PMID:2655295DOI:10.1177/106002808902300108.
Intravenous Erythromycin lactobionate has been used for several years to treat various infectious diseases. Several cases of severe nausea and vomiting associated with its use have been reported in Europe but only a few cases have been reported in the U.S. The official product information does not refer to severe nausea and vomiting associated with its intravenous use; however, we report six additional cases of severe nausea and vomiting associated with rapid administration of Erythromycin lactobionate, and review the current literature on the characteristics of this adverse effect.
Erythromycin lactobionate: pharmacokinetics and uterine tissue levels
Eur J Drug Metab Pharmacokinet 1987 Jul-Sep;12(3):153-60.PMID:3436337DOI:10.1007/BF03189891.
Erythromycin is well-known for its properties of tissular diffusion. An estimation of its concentration in uterine tissue seemed worthwhile, in order to justify the use of Erythromycin lactobionate in uterine infections by sensitive micro-organisms. The authors studied the uterine levels of this macrolid, after perfusion of 1g of Erythromycin lactobionate, over a period of one hour. The protocol involved a group of 15 women, who were to undergo a hysterectomy for benign non-inflammatory pathology. The uterine specimens and plasmatic pharmacokinetics of the antibiotic constitute the data. The concentrations of antibiotic were determined by microbiological methods. 2 sets of results emerge: during perfusion, the uterine erythromycin levels are equal or inferior to simultaneous serum levels. after perfusion, the uterine levels are superior to serum levels. A bicompartmental linear model was used, which simulated the tissular levels in standard treatment with Erythromycin lactobionate. If the erythromycin 4 micrograms/ml critical concentration is compared with uterine tissue concentration, the antibiotic may be expected to be active against a uterine affected by sensitive micro-organisms during a period of approximately 5 hours. This result must be confirmed by a clinical study.
Gastrointestinal side effects after intravenous Erythromycin lactobionate
Br J Clin Pharmacol 1986 Mar;21(3):295-9.PMID:3964530DOI:10.1111/j.1365-2125.1986.tb05193.x.
Ten healthy normal volunteers received an intravenous infusion of Erythromycin lactobionate over 60 min to a total dose of 800 mg (n = 9), and 524 mg (n = 1). Blood samples were collected at 10 min intervals for 100 min and gastric contents aspirated, via a nasogastric tube, from pre-dose to 105 min after start of infusion. Incidence and severity of three gastrointestinal symptoms (nausea, stomach discomfort and feelings of hunger), two CNS symptoms (dizziness and faintness) and a 'control' symptom (back pain) were measured using 100 mm visual analogue scales. Rate of infusion and plasma erythromycin concentration correlated with nausea (P less than 0.001) and stomach discomfort (P less than 0.001); plasma erythromycin concentration was also correlated with dizziness (P less than 0.05). Concentrations of active erythromycin in the aspirate were pH dependent. In one subject the concentration of erythromycin in the aspirate exceeded that in the plasma by 100 fold. Bile staining of samples containing the highest levels of microbiologically active erythromycin makes the origin of the erythromycin in these samples uncertain.
Effects of intravenous Erythromycin lactobionate in respiratory infections
J Int Med Res 1987 Jul-Aug;15(4):245-50.PMID:3653502DOI:10.1177/030006058701500409.
The antibiotic Erythromycin lactobionate given intravenously acts almost exclusively on Gram-positive bacteria. Even at high plasma and tissue concentrations there is an almost total absence of side-effects. It could be considered, therefore, as first choice in the treatment of patients with infectious respiratory diseases. Most of the 40 patients admitted to the present study were elderly and all had either acute or chronic and becoming acute respiratory disease. Their clinical symptoms and levels of phlogosis improved on treatment with Erythromycin lactobionate without any interruption of therapy due to side-effects and toxicity. The absence of unfavourable pharmacological interactions further enhances the usefulness of the drug. In view of the excellent response to monotherapy with Erythromycin lactobionate and the few groups of resistant bacteria found in those cases when it was possible to check, it was not considered necessary to investigate any synergistic association with other antibiotics. It can be concluded, therefore, that therapy with Erythromycin lactobionate in patients with infective respiratory disease is favourable and patients show excellent tolerability.