Fluindione
(Synonyms: 氟茚二酮) 目录号 : GC49518
A vitamin K antagonist
Cas No.:957-56-2
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
Fluindione is a vitamin K antagonist.1 It inhibits vitamin K epoxide reductase (VKOR; IC50 = 6.6 nM), including VKOR containing certain substitution mutations. Fluindione inhibits platelet and fibrin deposition, as well as prevents β-thromboglobulin release and thrombin-antithrombin complex formation, in an ex vivo model of tissue factor-induced thrombus formation using isolated human whole blood.2 Fluindione has previously been used in the treatment of emboligenic heart disease, deep vein thrombosis, pulmonary embolism, and in the prevention of thromboembolic complications in patients with heart disease.
1.Chen, X., Jin, D.-Y., Stafford, D.W., et al.Evaluation of oral anticoagulants with vitamin K epoxide reductase in its native milieuBlood132(18)1974-1984(2018) 2.Bossavy, J.P., Sakariassen, K.S., Thalamas, C., et al.Antithrombotic efficacy of the vitamin K antagonist fluindione in a human ex vivo model of arterial thrombosis: Effect of anticoagulation level and combination therapy with aspirinArterioscler. Thromb. Vasc. Biol.19(9)2269-2275(1999)
| Cas No. | 957-56-2 | SDF | Download SDF |
| 别名 | 氟茚二酮 | ||
| Canonical SMILES | O=C1C2=C(C(C1C3=CC=C(C=C3)F)=O)C=CC=C2 | ||
| 分子式 | C15H9FO2 | 分子量 | 240.2 |
| 溶解度 | DMF: insol,DMSO: 1 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): insol | 储存条件 | -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 | 4.1632 mL | 20.816 mL | 41.632 mL |
| 5 mM | 0.8326 mL | 4.1632 mL | 8.3264 mL |
| 10 mM | 0.4163 mL | 2.0816 mL | 4.1632 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。
Immunoallergic adverse effects of Fluindione
Prescrire Int 2010 Nov;19(110):255-6.PMID:21284358doi
Bleeding is the main adverse effect of all vitamin K antagonists. Fluindione, an indanedione derivative, can also have serious immunoallergic adverse effects. Several hypersensitivity reactions affecting various organ systems have been reported in detail in patients taking Fluindione, mainly cutaneous, hepatic or renal disorders, often associated with fever. Cases of isolated kidney and liver damage have also been reported. Fluindione has been linked to cases of acute generalised exanthematic pustulosis. An immunoallergic mechanism is suspected, based on several factors, including the involvement of several organs, the types of damage, the chronological sequence of events, outcome after Fluindione withdrawal, and cases of positive rechallenge. About a hundred reports of non-haemorrhagic adverse effects attributed to Fluindione were recorded in the French pharmacovigilance database during the course of a single year (July 2008 to June 2009). In practice, when anticoagulant therapy with a vitamin K antagonist is needed, it is better to use warfarin, the best-assessed oral anticoagulant. If Fluindione is nonetheless prescribed, the patient must not only be taught how to manage vitamin K antagonist therapy but also how to recognise signs of hypersensitivity.
Reversible Fluindione-Induced Chronic Interstitial Nephritis
Case Rep Nephrol 2016;2016:9818195.PMID:27127666DOI:10.1155/2016/9818195.
Fluindione is well known to induce acute drug-induced interstitial nephritis (IN). Most cases occurred soon after the onset of treatment. We report a unique case of severe subacute fluindione-induced IN diagnosed 2 years after the treatment was begun. Renal function dramatically improved after Fluindione withdrawal and steroid therapy.
Fluindione and drug reaction with eosinophilia and systemic symptoms: an unrecognised adverse effect?
Eur J Clin Pharmacol 2012 Jan;68(1):101-5.PMID:21792562DOI:10.1007/s00228-011-1101-9.
Purpose: Fluindione is an oral vitamin K antagonist (indanedione derivative) exclusively marketed in France and Luxembourg, known to have immuno-allergic adverse effects such as hepatitis, fever or interstitial nephritis. A few cases of drug reaction with eosinophilia and systemic symptoms (DRESS) have been reported with Fluindione. The aim of the present study was to investigate fluindione-induced DRESS cases reported in France and to describe their characteristics. Methods: We searched for potential cases of DRESS with Fluindione reported in the French pharmacovigilance database since 2000. Results: Thirty-six cases of DRESS were included and concerned 17 women and 19 men. The mean age was 65 years (median: 68 years, range: 28-95 years). Kidneys and liver were the most frequent organs involved. Thirty-five cases were serious. In 5 cases, the effect was life-threatening. Most of the patients recovered. Fluindione was the only medicine suspected in 26 cases. Skin patch tests, performed in 10 cases, were positive with Fluindione in 9 cases. Conclusions: Fluindione is not known to be a frequent cause of DRESS. However, the number of reports found is probably underestimated. The seriousness of DRESS, as all immuno-allergic adverse effects, contraindicates Fluindione reintroduction. Coumarinic derivatives are the alternatives in patients who need oral anticoagulant treatment.
[Fluindione-induced acute exanthematous pustulosis with renal involvement]
Ann Dermatol Venereol 2003 Dec;130(12 Pt 1):1146-9.PMID:14724519doi
Introduction: Fluindione (Previscan) is an oral anti-vitamin K anticoagulant, widely prescribed in France. Contrary to phenindione, which is also an indanedione derivative, very few cases of immunoallergic reactions have been described. Case report: A 68 year-old man, treated with Fluindione for cardiac arrhythmia, presented with a pustular eruption and erythema twenty days after initiation of treatment. The eruption was associated with hyperthermia, arthralgia, neutrophilia (11,000/mm2), hepatic cytolysis and renal involvement including acute renal failure, hematuria and proteinuria. In view of the absence of any earlier case in the literature, we did not impute Fluindione and the drug was reintroduced and led to the rapid recurrence of all the same manifestations. Discussion: These manifestations were consistent with an immunoallergic reaction to Fluindione (probable intrinsic imputability I3) and acute interstitial nephritis (probable intrinsic imputability I3). We believe this is the first case of acute generalized exanthematous pustulosis induced by Fluindione (intrinsic imputability Bo). A few rare cases of fluindione-induced hypersensitivity reactions and acute interstitial nephritis, however, have been described.
Acute and chronic nephropathy induced by Fluindione must be addressed
Nephrol Dial Transplant 2012 Apr;27(4):1554-8.PMID:21931126DOI:10.1093/ndt/gfr500.
Background: Among the vitamin K antagonists (VKA), indanedione-derived VKA is suspected to induce an immunoallergic risk. One indanedione-derived VKA, Fluindione, is still being used in France. The aim of this study was to evaluate the contribution of VKA to acute and chronic nephritis. Methods: Twenty-four cases of biopsy proven acute interstitial nephritis (AIN) were retrospectively selected, based on a first intake of VKA within the previous 12 months as well as an increase of at least 50% of the basal level of serum creatinine. The 24 cases were all treated with Fluindione VKA and not with coumarinic VKA. Results: The subjects studied included 20 men and 4 women, with a mean age of 73.0±9.3 years (range: 44-84). The delay between Fluindione introduction and the appearance of an AIN, proven by biopsy when available, was 11.9±6.9 weeks (range: 3-28). Creatinine increased from 123.0±56.4 μmol/L (range: 56-335) at Fluindione introduction to 460.7±265.3 μmol/L (range: 109-1200) at the time of AIN discovery. The treatment then consisted of stopping the Fluindione and introducing steroids for 21 patients. If a VKA was necessary, Fluindione was replaced by a coumarinic VKA. After 6 months, 1 patient died and 15 patients presented severe chronic kidney disease (CKD Stages 4-5). Two patients still required chronic dialysis after 6 months and five patients after 3 years. Patients with pre-existing kidney disease were more prone to develop severe CKD with Fluindione. Conclusion: In this large study, arguments are presented to incriminate Fluindione in the induction of acute and chronic nephritis.