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1.
Summary

Studies are reviewed on diflunisal, a new analgesic agent with an improved therapeutic index, compared with acetylsalicylic acid, in animals and humans. Pharmacokinetic data indicate that a twice-daily dosage regimen of diflunisal is adequate for therapeutic purposes. Diflunisal inhibits prostaglandin E synthesis, but in humans at clinically effective doses it does not alter bleeding time or platelet aggregation. Diflunisal is uricosuric at clinically effective doses. No clinically important drug interactions with diflunisal have been found to date, although some slight alterations in blood and urine drug levels have been noted. The slight increase in prothrombin time seen when diflunisal and acenocoumarol were co-administered is not considered to be of major clinical importance.  相似文献   

2.
GC测定荆芥及荆芥油中的薄荷酮和胡薄荷酮   总被引:2,自引:0,他引:2  
目的 测定荆芥及荆芥油中的薄荷酮和胡薄荷酮.方法 采用GC法.用PEG-20M石英毛细管柱(30 m×0.53 mm×1 μm),FID检测器,氮气为载气,柱温140%,气化室和检测器温度均为250°C,不分流进样.以萘为内标.结果 薄荷酮的线性范围为0.2~2.5 mg·ml-1(r=0.9999),胡薄荷酮的线性范围为0.2~2.5 mg·ml-1(r=0.9992);薄荷酮和胡薄荷酮的平均回收率(n=9)分别为99.0%、99.6%.结论 所建方法简便、准确,可同时测定荆芥以及荆芥油中的薄荷酮和胡薄荷酮.  相似文献   

3.
Studies are reviewed on diflunisal, a new analgesic agent with an improved therapeutic index, compared with acetylsalicylic acid, in animals and humans. Pharmacokinetic data indicate that a twice-daily dosage regimen of diflunisal is adequate for therapeutic purposes. Diflunisal inhibits prostaglandin E synthesis, but in humans at clinically effective doses it does not alter bleeding time or platelet aggregation. Diflunisal is uricosuric at clinically effective doses. No clinically important drug interactions with diflunisal have been found to date, although some slight alterations in blood and urine drug levels have been noted. The slight increase in prothrombin time seen when diflunisal and acenocoumarol were co-administered is not considered to be of major clinical importance.  相似文献   

4.
Bivalirudin: pharmacology and clinical applications   总被引:3,自引:0,他引:3  
Bivalirudin (Hirulog, Angiomax) is a specific, reversible and direct thrombin inhibitor with a predictable anticoagulant effect. It is cleared by both proteolytic cleavage and renal mechanisms, predominantly glomerular filtration. Bivalirudin inhibits both circulating thrombin and fibrin bound thrombin directly by binding to thrombin catalytic site and anion-binding exosite I in a concentration-dependent manner. Bivalirudin prolongs activated partial thromboplastin time, prothrombin time, thrombin time and activated clotting time (ACT). ACT levels with bivalirudin do not correlate with its clinical efficacy. Bivalirudin with a provisional GpIIb/IIIa inhibitor is indicated in elective contemporary percutaneous coronary intervention (PCI). In respect to combined ischemic and hemorrhagic endpoints of death, myocardial infarction, unplanned urgent revascularization and major bleeding during PCI (including subgroups of patients with renal impairment and diabetes) bivalirudin is not inferior to unfractioned heparin and planned GpIIb/IIIa inhibitors. In addition, bivalirudin has been consistently shown to have significantly less in-hospital major bleeding than heparin alone or heparin in combination with a GpIIb/IIIa inhibitor. Bivalirudin appears to be also safe and effective during PCI in patients with heparin-induced thrombocytopenia. Finally, data from PCI studies support the safety and efficacy of bivalirudin, although its direct randomized comparison with unfractionated heparin is lacking.  相似文献   

5.
Invasive fungal infections are important causes of morbidity and mortality in hospitalised patients. Current therapy with amphotericin B and antifungal triazoles has overlapping targets and is limited by toxicity and resistance. Echinocandins are a new class of antifungal drugs, which inhibit the synthesis of 1,3-beta-D-glucan. This homopolysaccharide is an important component of the cell wall of many pathogenic fungi, providing osmotic stability and functioning in cell growth and cell division. Micafungin, which is a member of the echinocandin class, exhibits in vitro fungicidal or fungistatic activity against a variety of fungal pathogens which include Candida and Aspergillus species but not Cryptococcus, Fusarium or Zygomycetes. Micafungin demonstrates linear pharmacokinetics, which are not altered by drugs metabolised through the P450 enzyme system. The preclinical and clinical data strongly support the development of micafungin for treatment of proven or suspected mucosal and invasive Candida infections in immunocompetent and immunocompromised patients. This paper reviews the preclinical and clinical pharmacology of micafungin and its potential role for treatment of fungal invasive infections in patients.  相似文献   

6.
目的应用网络药理学方法研究荆芥挥发油抗炎的主要成分和分子机制。方法通过中药系统药理数据库和分析平台(TCMSP)和Swiss Target Prediction平台获得主要成分对应靶点,筛选活性成分,构建分子-靶点网络。进行蛋白质相互作用分析,靶点基因本体(GO)富集分析,京都基因与基因组百科全书(KEGG)通路分析。应用Systems Dock分子对接,结合文献验证。结果荆芥挥发油13个主要成分对应45个靶点,IL-6、TNF、IL-1β、IL-10、PTGS2、PTGS1、CHRM1、CHRNA7为炎症靶点,作用于NF-κB、IL-17信号通路,通过药物反应、γ-氨基丁酸通路等生物过程,胞外配体门控离子通道活性、GABA-A受体结合等分子功能发挥作用,与酒精滥用、2型糖尿病、精神疾病、肠病、肺病等相关。分子对接得到8,9-去氢百里香酚、苯甲醛、石竹烯、葎草烯、D-吉玛烯、胡薄荷酮是重要成分,对CHRNA7、PTGS2和PTGS1作用明显。结论该方法初步揭示荆芥挥发油抗炎的有效成分及潜在靶点。  相似文献   

7.
Thalidomide is attracting new interest. Since the discovery of its remarkable efficacy in erythema nodosum leprosum, the drug has been used successfully in a variety of dermatologic and other diseases whose apparent common thread is immune dysregulation. Meanwhile, immunomodulatory and anti-inflammatory activities of thalidomide, particularly its inhibition of tumour necrosis factor alpha (TNF-a), have been identified and elucidated. The drug has also been found to inhibit angiogenesis. Recent clinical trials have shown thalidomide effective in graft-versus-host disease, Behçet's syndrome and aphthous ulcers and wasting associated with HIV infection. Provocative findings in other diseases, including primary HIV infection, HIV-associated diarrhoea, inflammatory bowel disease, cancer and sepsis, have suggested additional clinical applications. Use of thalidomide in women capable of childbearing is controversial. However, guidelines have emerged for prevention of teratogenicity and peripheral neuropathy, the drug's other major adverse effect. With appropriate safeguards, thalidomide may hold benefit for patients with a broad variety of disorders in which existing treatments are inadequate. Its current use may represent only a small part of its therapeutic potential.  相似文献   

8.
Thalidomide is attracting new interest. Since the discovery of its remarkable efficacy in erythema nodosum leprosum, the drug has been used successfully in a variety of dermatologic and other diseases whose apparent common thread is immune dysregulation. Meanwhile, immunomodulatory and anti-inflammatory activities of thalidomide, particularly its inhibition of tumour necrosis factor alpha (TNF-alpha), have been identified and elucidated. The drug has also been found to inhibit angiogenesis. Recent clinical trials have shown thalidomide effective in graft-versus-host disease, Beh?et's syndrome and aphthous ulcers and wasting associated with HIV infection. Provocative findings in other diseases, including primary HIV infection, HIV-associated diarrhoea, inflammatory bowel disease, cancer and sepsis, have suggested additional clinical applications. Use of thalidomide in women capable of childbearing is controversial. However, guidelines have emerged for prevention of teratogenicity and peripheral neuropathy, the drug's other major adverse effect. With appropriate safeguards, thalidomide may hold benefit for patients with a broad variety of disorders in which existing treatments are inadequate. Its current use may represent only a small part of its therapeutic potential.  相似文献   

9.
Limonene is one of the most simple cyclic monoterpenes, and two enantiomers, d- and l-limonene occur due to the chiral carbon at 4-position. Cyclization of GPP into limonene is catalyzed by the limonene synthase, and some l-limonene synthase cDNAs have already been cloned from several species of plants, mainly from Labiatae family. However, the d-limonene synthase gene has not yet been obtained, therefore, no information is available on the molecular mechanism of stereochemical regulation in limonene formation. To resolve this, we cloned the d-limonene synthase gene (dLMS) from Schizonepeta tenuifolia (Labiatae) by a reverse genetic approach, and we found that both d- and l-limonene synthase share similar features such as a transit peptide, an arginine rich domain, and a metal cation binding site in their structures. Here, we report on the cloning of dLMS, and the putative stereochemical regulation mechanism is discussed based on the comparison of the deduced amino acid sequence of dLMS with those of known l-limonene synthases.  相似文献   

10.
Oshima Y  Takata S  Hikino H 《Planta medica》1989,55(2):179-180
Four new monoterpenoids, shizonodiol, shizonol, and shizonepetosides D and E, have been isolated from SCHIZONEPETA TENUIFOLIA spikes along with the known flavonoids, diosmetin, hesperetin, and luteolin.  相似文献   

11.
This study investigated the antioxidative and anti-inflammatory activities of aqueous extracts of Schizonepeta tenuifolia Briq. (STE). The results showed that STE displayed radical scavenging and reducing activity, as well as liposome protection activity. In addition, the implementation of an HPLC with a photodiode array detector helped to identify polyphenolic components including hesperidin, luteolin, and diosmetin. STE administration in the range of 125-500 mg/kg showed concentration dependent inhibition on carrageenan induced inflammatory response in mice. The anti-inflammatory effects of STE could be related to tissue NO and tumor necrosis factor a (TNF-α) suppression, and associated with the reduction of lipid peroxidation and an increase in antioxidant enzyme activities including catalase, superoxide dismutase, and glutathione peroxidase in vivo. Overall, the results showed that STE might serve as a natural inhibitor of oxidation and inflammation.  相似文献   

12.
Two new sesquiterpenes named petafolias A–B were isolated from the aerial parts of Schizonepeta tenuifolia. Their structures were elucidated by various spectroscopic techniques (UV, IR, MS, CD, 1D, and 2D NMR).  相似文献   

13.
Danshen, the dried root of Salvia miltiorrhiza, has been widely used in China and, to a lesser extent, in Japan, the United States, and other European countries for the treatment of cardiovascular and cerebrovascular diseases. In China, the specific clinical use is angina pectoris, hyperlipidemia, and acute ischemic stroke. The current review covers its traditional uses, chemical constituents, pharmacological activities, pharmacokinetics, clinical applications, and potential herb-drug interactions based on information obtained in both the English and Chinese literature. Although numerous clinical trials have demonstrated that certain Danshen products in China are effective and safe for the treatment of cardiovascular diseases, most of these lack sufficient quality. Therefore, large randomized clinical trials and further scientific research to determine its mechanism of actions will be necessary to ensure the safety, effectiveness, and better understanding of its action.  相似文献   

14.
15.
《Pharmaceutical biology》2013,51(8):1053-1061
Context: Sinomenium acutum (Thumb.) Rehd. et Wils. (Menispermaceae, SA) has been used as a traditional Chinese medicine in the treatment of various diseases for hundreds of years; it possesses favorable effects against autoimmune diseases, especially rheumatoid arthritis (RA). A great number of investigations have been done on SA in the last decade, but they are usually scattered across various publications.

Objective: The purpose of this article is to summarize and review the published scientific information about the chemical constituents, pharmacological effects, pharmacokinetics, and clinic applications of this plant since 2000.

Results: The information for 89 cases included in this review was compiled. The SA contains alkaloids, sterols, phospholipids, and some other components. A great deal of pharmacological and clinic research has been done on sinomenine, a main compound from SA, which mainly focuses on the immune system, cardiovascular system, and nervous system.

Conclusion: Previous studies strongly support its potential as an effective adaptogenic herbal remedy. There is no doubt that SA is being widely used now and will have extraordinary potential for the future.  相似文献   

16.
Podophyllotoxin derivatives like etoposide 7a, etophos 7b, and teniposide 7c are used clinically as potent chemotherapeutic agents for a variety of tumors including small cell lung carcinoma, testicular cancer, and malignant lymphoma. These compounds derived from a series of modifications which converted podophyllotoxin 1a from an entity that interacted with tubulin and blocks mitosis to one that induced a block in late S or early G2 by interacting with topoisomerase II. Synthetic studies on podophyllotoxin derivatives can be divided in four general approaches (the oxo-ester route, the digydroxy acid route, the tandem conjugate addition route and the Diels-Alder route). Albeit a number of synthetic sequences afforded products with excellent enantiopurities, the low overall yields still disqualify synthesis as an alternative for naturally produced materials. An alternative route based on the enzyme-catalyzed cyclization of synthetic intermediates to analogues of the podophyllotoxin family is being explored. Synthetic dibenzylbutanolides, which were revealed by biosynthetic studies to be the precursors of aryltetralin lignans, have been treated with enzymes derived from cell cultures of Podophyllum peltatum, Catharanthus roseus, Nicotiana sylvestris and Cassia didymobotrya. The ciclyzation process afforded however compounds with a different stereochemistry in the C ring. The obtainment of a novel compound with a bynzylidenebenzylbutirolactone structure still leaves considerable scope for exploring biotransformations in order to obtain podophyllotoxin analogues via a combination of synthetic chemistry and biotechnological methods.  相似文献   

17.
18.
《中国药房》2015,(4):532-534
目的:优选荆芥药材中橙皮苷的提取工艺。方法:以橙皮苷含量为考察指标,采用高效液相色谱法,通过单因素试验考察不同超声提取时间、料液比、提取次数、乙醇体积分数对橙皮苷含量的影响;通过正交试验L(934)确定荆芥橙皮苷提取的最优提取工艺,并进行验证试验。结果:优选的提取工艺为50%乙醇溶液超声提取1次,提取时间为30 min,料液比为1∶30(g∶ml)。3次验证试验结果显示橙皮苷的含量分别为0.27%、0.28%、0.28%。结论:该提取工艺稳定、可行,适合荆芥橙皮苷的提取。  相似文献   

19.
20.
吡非尼酮是近年来上市用于治疗特发性肺纤维化的药物。研究证实该药具有抑制胶原合成、抗炎和抗氧化的作用。吡非尼酮作为一种广谱的抗纤维化药物,在特发性肺纤维化、肝纤维化、肾纤维化、心脏组织纤维化、多发性硬化症、神经纤维瘤、子宫肌瘤、恶性胶质瘤的治疗和器官移植纤维化的预防方面均具有广阔的应用前景。  相似文献   

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