Cotrimoxazole
(Synonyms: TMP-SMX, Trimethoprim-Sulfamethoxazole) 目录号 : GC47121A mixture of the antibiotics sulfamethoxazole and trimethoprom
Cas No.:8064-90-2
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
Cotrimoxazole is a mixture of the antibiotics sulfamethoxazole and trimethoprim .1,2 It is bactericidal against 12 patient-derived community-acquired methicillin-resistant S. aureus (MRSA) strains when used at a concentration of 0.05 mg/L.2 Cotrimoxazole (240 mg/kg) prevents lung and spleen bacterial colonization in a mouse model of inhaled B. mallei infection, but does not eradicate infection when administered post B. mallei exposure in the same model.3 It also resolves cutaneous tail lesions in a mouse model of S. xylosus infection.4 Formulations containing cotrimoxazole have been used in the treatment of MRSA infections and the prevention of glanders disease in human and veterinary medicine, respectively.
1.Lewis, E.L., Anderson, J.D., and Lacey, R.W.A reappraisal of the antibacterial action of cotrimoxazole in vitroJ. Clin. Pathol.27(2)87-91(1974) 2.Kaka, A.S., Rueda, A.M., Shelburne, S.A., III, et al.Bactericidal activity of orally available agents against methicillin-resistant Staphylococcus aureusJ. Antimicrob. Chemother.58(3)680-683(2006) 3.Barnes, K.B., Steward, J., Thwaite, J.E., et al.Trimethoprim/sulfamethoxazole (co-trimoxazole) prophylaxis is effective against acute murine inhalational melioidosis and glandersInt. J. Antimicrob. Agents41(6)552-557(2013) 4.Thornton, V.B., Davis, J.A., St. Clair, M.B., et al.Inoculation of Staphylococcus xylosus in SJL/J mice to determine pathogenicityContemp. Top. Lab. Anim. Sci.42(4)49-52(2003)
| Cas No. | 8064-90-2 | SDF | |
| 别名 | TMP-SMX, Trimethoprim-Sulfamethoxazole | ||
| Canonical SMILES | COC1=C(OC)C(OC)=CC(CC2=CN=C(N)N=C2N)=C1.NC3=CC=C(S(NC4=NOC(C)=C4)(=O)=O)C=C3 | ||
| 分子式 | C14H18N4O3.C10H11N3O3S | 分子量 | 543.6 |
| 溶解度 | DMF: 10mg/mL,DMSO: 10mg/mL,DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL,Ethanol: 0.3mg/mL | 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 | 1.8396 mL | 9.1979 mL | 18.3959 mL |
| 5 mM | 0.3679 mL | 1.8396 mL | 3.6792 mL |
| 10 mM | 0.184 mL | 0.9198 mL | 1.8396 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。
Cotrimoxazole and neonatal kernicterus: a review
Drug Chem Toxicol 2014 Apr;37(2):121-9.PMID:24099411DOI:10.3109/01480545.2013.834349.
Sulfamethoxazole (SMX) and trimethoprim (TMP) individually and a combination known as Cotrimoxazole (SMX-TMP) are widely used for the treatment of protozoan and bacterial infections. SMX-TMP is also one of the widely used antibiotics administered orally in neonates, along with gentamicin injection, for treating pneumonia and sepsis by home-based healthcare providers in Asian countries. Although the use of this drug has successfully reduced neonate mortality, there is a concern for it causing neurotoxicity. Previous clinical studies with sulfisoxazole have demonstrated occurrence of kernicterus in neonates. This sulfonamide is thought to displace bilirubin from its albumin-binding sites in plasma leading to an elevation of plasma bilirubin, which crosses the blood-brain barrier, reaches central neurons to cause kernicterus. We performed an extensive review of clinical and animal studies with Cotrimoxazole, which showed no reported incidences of kernicterus with SMX-TMP use in neonates. EndNote, BasicBiosis, Embase, PubMed and Toxline database searches were conducted using specific keywords yielding 74 full-length articles relevant to the review. This review has taken into account various factors, including the disease itself, direct effects of the drug and its metabolism through conjugation and acetylation through a thorough review of the literature to examine the potentials of SMX-TMP to cause kernicterus in neonates. SMX-TMP in oral doses administered to neonates for 7-10 days is unlikely to cause kernicterus. Also, this review recommends warranting the need of future studies using animal models and clinical studies in humans to address SMX-TMP toxicity.
Cotrimoxazole, clinical uses and malaria chemotherapy
Afr J Med Med Sci 2010 Mar;39(1):63-8.PMID:20632674doi
Microbial infections still account for considerable morbidity and mortality in sub-Saharan Africa. The importance of chemotherapeutic agents cannot be over-emphasized. Some antimicrobial agents provide broad spectrum of activity spanning different classes of bacterial and protozoan diseases. Cotrimoxazole, an antifolate antimicrobial was originally meant for treatment of bacterial diseases but has been shown to be an effective drug in the treatment of malaria amongst other conditions. This review attempted to explore the pharmacology of Cotrimoxazole, its many clinical uses and adverse effects. Specific experiences of the author in the application of Cotrimoxazole in the treatment of acute uncomplicated falciparum malaria were highlighted and suggestions on how to optimize the use of this drug were made.
Cotrimoxazole. Rationale for re-examining its indications for use
Drug Saf 1996 Apr;14(4):213-8.PMID:8713689DOI:10.2165/00002018-199614040-00001.
Trimethoprim was specifically developed in the late 1960s as a sulphonamide potentiator and was launched in combination with sulfamethoxazole as Cotrimoxazole. Laboratory data showed synergy of antimicrobial action for the combination and suggested that the use of both agents would delay the emergence of resistance. However, the tissue distribution of trimethoprim and sulfamethoxazole does not favour synergy, and resistance among common pathogens to sulfamethoxazole is high. Clinical studies comparing trimethoprim alone with Cotrimoxazole for the treatment of respiratory tract and urinary tract infections have failed to show any benefit from the combination. The development of delayed resistance by use of the combination has not been substantiated. The common adverse effects seen with Cotrimoxazole are gastrointestinal disturbances and skin rashes which are well described adverse effects of sulphonamides. Comparative studies suggest that these are less common with trimethoprim alone. Serious adverse effects such as liver disorders and Stevens-Johnson syndrome appear more common with Cotrimoxazole. Where there is little evidence for benefit from the use of the combination, the exposure of patients to the additional risk from the adverse effects and drug interactions of 2 drugs cannot be justified. Therefore use of Cotrimoxazole should be restricted to those situations such as Pneumocystis carnii pneumonia where the combination has been shown to be beneficial.
Cotrimoxazole prophylaxis for opportunistic infections in children with HIV infection
Cochrane Database Syst Rev 2006 Jan 25;2006(1):CD003508.PMID:16437457DOI:10.1002/14651858.CD003508.pub2.
Background: The majority of children with HIV infection live in low-income countries without access to antiretroviral drugs. The prevention and early treatment of opportunistic infections are the mainstay of their medical management. Cotrimoxazole is cheap and effective against a wide range of organisms, including Pneumocystis jiroveci pneumonia (PCP), which is an important cause of death and illness in the first year of life. It is safe with relatively few side effects. Diagnosis of HIV in children is complicated by the presence of maternal antibodies in early life. Providing prophylaxis based initially on maternal status is one possible solution. However, routine prophylactic treatment is difficult to deliver in low-resource settings, and could also lead to increased resistance to the drug. Objectives: To assess the effects of routinely administered Cotrimoxazole on death and illness episodes in children with HIV infection, and in infants of HIV-infected mothers. Search strategy: We searched the Cochrane HIV/AIDS registry, MEDLINE, the Cochrane Controlled Trials Register, LILACS, AIDSLINE, AIDSTRIALS and AIDSDRUGS databases, and proceedings and abstracts from AIDS and TB conferences (search date Feb 2005). We checked reference lists of pertinent articles, and contacted pharmaceutical companies and experts in the field. Selection criteria: Randomised or quasi-randomised trials comparing routinely administered Cotrimoxazole versus placebo or no treatment in children (age less than 15 years) with HIV infection, or children less than 18 months with HIV infected mothers. Data collection and analysis: Two reviewers independently assessed trial eligibility and quality. Where data were incomplete or unclear trial authors were contacted for further details. Main results: One study was identified that fulfilled the inclusion criteria. It studied 534 children with HIV infection in Lusaka, Zambia. The study was conducted in an area of high bacterial resistance to Cotrimoxazole (60-80%). A reduction in mortality of 33% was seen in the Cotrimoxazole group as compared to placebo, relative risk 0.67 (95% CI 0.53 - 0.85). There was also a beneficial effect on hospitalisation, relative risk 0.77 (95% CI 0.62 - 0.96). There was no difference in adverse events between groups, and the beneficial effect was seen across all ages and CD4%. Authors' conclusions: A single trial has shown a beneficial effect from the use of Cotrimoxazole prophylaxis in HIV infected children in Zambia. It must be decided whether this can be extrapolated to other resource-poor settings.
Safety of Cotrimoxazole in pregnancy: a systematic review and meta-analysis
J Acquir Immune Defic Syndr 2014 Aug 15;66(5):512-21.PMID:24853309DOI:10.1097/QAI.0000000000000211.
Introduction: Cotrimoxazole is widely prescribed to treat a range of infections, and for HIV-infected individuals it is administered as prophylaxis to protect against opportunistic infections. Some reports suggest that fetuses exposed to Cotrimoxazole during early pregnancy may have an increased risk of congenital anomalies. We carried out this systematic review to update the evidence of Cotrimoxazole safety in pregnancy. Methods: Three databases and 1 conference abstract site were searched in duplicate up to October 31, 2013, for studies reporting adverse maternal and infant outcomes among women receiving Cotrimoxazole during pregnancy. This search was updated in MEDLINE via PubMed to April 28, 2014. Studies were included irrespective of HIV infection status or the presence of other coinfections. Our primary outcome was birth defects of any kind. Secondary outcomes included spontaneous abortions, terminations of pregnancy, stillbirths, preterm deliveries, and drug-associated toxicity. Results: Twenty-four studies were included for review. There were 232 infants with congenital anomalies among 4196 women receiving Cotrimoxazole during pregnancy, giving an overall pooled prevalence of 3.5% (95% confidence interval: 1.8% to 5.1%; τ² = 0.03). Three studies reported 31 infants with neural tube defects associated with first trimester exposure to Cotrimoxazole, giving a crude prevalence of 0.7% (95% confidence interval: 0.5% to 1.0%) with most data (29 neural tube defects) coming from a single study. The majority of adverse drug reactions were mild. The quality of the evidence was very low. Conclusions: The findings of this review support continued recommendations for Cotrimoxazole as a priority intervention for HIV-infected pregnant women. It is critical to improve data collection on maternal and infant outcomes.