Pivmecillinam (FL-1039)
(Synonyms: 匹美西林; FL-1039) 目录号 : GC32260
Pivmecillinam (FL-1039) (FL-1039) 是一种广谱青霉素抗生素美西林的口服活性前药。
Cas No.:32886-97-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pivmecillinam (FL-1039) is an orally active prodrug of mecillinam, an extended-spectrum penicillin antibiotic.
[1]. Nicolle LE. Pivmecillinam in the treatment of urinary tract infections. J Antimicrob Chemother. 2000 Aug;46 Suppl A:35-39. [2]. Graninger W. Pivmecillinam--therapy of choice for lower urinary tract infection. Int J Antimicrob Agents. 2003 Oct;22 Suppl 2:73-8. [3]. Holme E, et al. Carnitine deficiency induced by pivampicillin and pivmecillinam therapy. Lancet. 1989 Aug 26;2(8661):469-73.
| Cas No. | 32886-97-8 | SDF | |
| 别名 | 匹美西林; FL-1039 | ||
| Canonical SMILES | O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2/N=C/N3CCCCCC3)N1C2=O)OCOC(C(C)(C)C)=O | ||
| 分子式 | C21H33N3O5S | 分子量 | 439.57 |
| 溶解度 | Soluble in DMSO | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.275 mL | 11.3748 mL | 22.7495 mL |
| 5 mM | 0.455 mL | 2.275 mL | 4.5499 mL |
| 10 mM | 0.2275 mL | 1.1375 mL | 2.275 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。
Pivmecillinam in the treatment of urinary tract infections
J Antimicrob Chemother 2000 Sep;46 Suppl 1:35-9; discussion 63-5.PMID:11051622doi
The efficacy of Pivmecillinam for empirical treatment of acute uncomplicated urinary tract infection (UTI) was initially reported in clinical trials published in the 1970s and 1980s. Bacteriological cure rates observed in these trials were consistently >85%, and studies of different dosing regimens suggested that a 3 day course was appropriate. Comparative studies reported that Pivmecillinam was equivalent to other antimicrobial agents in terms of clinical and bacteriological outcomes. These studies also documented that Pivmecillinam was effective for treatment of Staphylococcus saprophyticus infections, was acceptable for use in pregnancy and was well tolerated. Subsequent widespread use of Pivmecillinam in Scandinavian countries has led to a body of clinical experience which confirms the efficacy and safety of this antimicrobial agent in the treatment of acute cystitis. Recently, two large, prospective, randomized, double-blind, multi-centre clinical trials have been completed to assist in defining the role of this antimicrobial agent in the treatment of acute cystitis. A comparison of 3 day courses of Pivmecillinam or norfloxacin, both at 400 mg bd, showed higher bacteriological cure rates with norfloxacin but generally similar clinical outcomes. A second, dose-ranging study found that Pivmecillinam, given bd for 7 days, led to superior bacteriological and clinical outcomes at short-term follow-up than the 3 day regimen. Pooling bacteriological outcomes from the two studies showed similar outcomes with 7 days of Pivmecillinam 200 mg bd or 3 days of norfloxacin 400 mg bd. The shorter, 3 day, course achieved similar short-term clinical outcomes to 7 days of Pivmecillinam and 3 days of norfloxacin in women aged < or =50 years. These recent studies confirm earlier reports and clinical experience that Pivmecillinam is effective and well tolerated for the treatment of acute cystitis in women.
Clinical evaluation of a novel beta-lactam antibiotic: Pivmecillinam (FL 1039)
Infection 1975;3(3):154-60.PMID:177372DOI:10.1007/BF01641339.
Pivmecillinam, a new penicillin-like antibiotic, is a member of the amidinopenicillanic acid group. Its mode of action differs from that of the classical penicillins and it exhibits no cross-resistance with them. Fifty-two gerontopsychiatric patients, median age 81 years, with E. coli, Klebsiella, and Proteus bacteriurias were divided into three comparable groups. In a ten week open clinical trial the patients were treated with Pivmecillinam, pivampicillin or the two drugs given alternately in doses reduced in stages. The bacteriuria in all groups cleared almost completely in three days. Pivmecillinam compared favourably with pivampicillin especially at the end of the reduced medication. The alternating treatment seemed to be superior to treatment with either drug administered separately. No development of resistance was observed. No toxic effect on the liver, kidney, or bone marrow was seen in any of the three groups. In the group receiving Pivmecillinam alone, no ampicillin-like skin rashes occurred.
Pivmecillinam--therapy of choice for lower urinary tract infection
Int J Antimicrob Agents 2003 Oct;22 Suppl 2:73-8.PMID:14527775DOI:10.1016/s0924-8579(03)00235-8.
Pivmecillinam is the pro-drug of mecillinam, a beta-lactam antibiotic with a novel site of action and with specific and high activity against Gram-negative organisms such as Escherichia coli and other Enterobacteriaceae. Since its introduction, it has been widely used for the treatment of acute lower urinary tract infections (UTI), primarily in the Nordic countries. In contrast to the increasing resistance of urinary pathogens to other beta-lactams particularly ampicillin/amoxycillin and to other UTI antibiotics such as trimethoprim and trimethoprim/sulphamethoxazole (TMP/SMX), the level of resistance has remained on a low level. Less than 2% of E. coli community isolates are resistant to mecillinam. This paper reviews the clinical data on Pivmecillinam with a special focus on the safety aspects. A large number of studies from the 70s to 80s have proven the clinical efficacy and safety of Pivmecillinam for empirical treatment of acute cystitis. More recent studies confirm short-term treatment with Pivmecillinam results in clinical and bacteriological cure rates similar to those obtained with other UTI agents. Both clinical studies in pregnant women with UTI and large epidemiological studies have confirmed the safety of Pivmecillinam used in pregnancy. In the Nordic countries Pivmecillinam has been the most widely used agent for treatment of UTI in pregnancy for many years. Ecological aspects of antibiotic treatment are important both with regard to adverse effects and development of resistance due to disturbance of the normal micro flora. Studies have shown that Pivmecillinam has a very minor impact on the normal oropharyngeal, intestinal and skin microflora. The clinical implications of this are a low frequency of diarrhoea and Candida vaginitis as confirmed in the clinical studies. The high and increasing level of resistance among E. coli to currently recommended first-line agents for acute cystitis requires a re-evaluation of treatment guidelines. With the low resistance, its proven efficacy and favourable safety profile, Pivmecillinam is a suitable first-line agent for empirical treatment of acute cystitis.
Pharmacokinetics of Pivmecillinam
Br J Clin Pharmacol 1977 Jun;4(3):267-73.PMID:197981DOI:10.1111/j.1365-2125.1977.tb00711.x.
1 The plasma concentration/time curves of ampicillin and mecillinam in normal subjects were measured after oral administration of ampicillin (500 mg) and Pivmecillinam (400 and 600 mg). 2 Similar plasma concentration/time curves of ampicillin and mecillinam in the starved normal subjects followed oral administration of ampicillin (500 mg) and Pivmecillinam (600 mg). 3 The plasma concentration/time curve of mecillinam was measured in the same normal subjects after oral administration of Pivmecillinam (400 mg) with a reproducible standardized Lundh test meal. 4 There was no statistically significant difference in the plasma concentration/time curve of mecillinam after Pivmecillinam/400 mg) and the meal compared with the plasma concentration/time curve after oral Pivmecillinam (400 mg) was given to the same subjects when starved. After administration of Pivmecillinam (400 mg) with meal, Tasc was significantly delayed beyond the value obtained when the subjects were starved. 5 The pharmacokinetics of Pivmecillinam in coeliac disease are normal. This finding contrasts with previous studies on the pharmacokinetics of another pivaloyloxymethylpenicillin ester, pivampicillin, in this condition.
[Urinary antimicrobial prophylaxis]
Arch Pediatr 2002 May;9(5):511-8.PMID:12053547DOI:10.1016/s0929-693x(01)00835-1.
Antibiotics are usually used to prevent childhood recurrent urinary tract infections: cystitis or pyelonephritis. The mechanism of action of these antibiotics, although imperfectly known, seems to be double: the antibiotic acts by its bactericidal effect, but also probably for minimal concentrations by reducing adhesion capability of bacteria to the urothelium. The most commonly used molecules are cotrimoxazole, trimethoprime, Pivmecillinam, cefaclor and nalidixic acid. However all have not been studied rigorously as for their prophylactic capacity, and in particular very little is known for patients presenting with vesico-ureteral reflux.