Proceedings of the Western Pharmacology Society最新文献_第10页

Platelet aggregation inhibition in patients receiving statins either fully or partially metabolized by CYP3A4. 接受他汀类药物完全或部分CYP3A4代谢的患者的血小板聚集抑制

Proceedings of the Western Pharmacology Society Pub Date : 2008-01-01

Sotir Polena, Manish P Gupta, Hafiza Shaikh, Kathleen Zazzali, Neil Coplan, Jonas Gintautas, Subir Singh Labana, Daniel Soffer

{"title":"Platelet aggregation inhibition in patients receiving statins either fully or partially metabolized by CYP3A4.","authors":"Sotir Polena, Manish P Gupta, Hafiza Shaikh, Kathleen Zazzali, Neil Coplan, Jonas Gintautas, Subir Singh Labana, Daniel Soffer","doi":"","DOIUrl":"","url":null,"abstract":"Clopidogrel therapy is the standard for prevention of cardiovascular thrombotic events. Clopidogrel is converted to an active thiol by the cytochrome P450 CYP 3A4 and 2C19 enzymes. Recent studies suggest that statins metabolized by CYP3A4 attenuate the anti-aggregatory effect of clopidogrel. We evaluated the effect of CYP3A4-metabolized statins (atorvastatin, group 1) and partially-CYP3A4-metabolized statins (simvastatin, group 2) on platelet aggregation inhibition (PAI) when given concomitantly with clopidogrel as compared to patients who were statin naive (group 3). PAI was measured by PlateletWorks (Helena Laboratories ICHOR) using the platelet P2Y12 receptor agonist ADP (20 micromol). All patients were on clopidogrel therapy (75 mg/day). Non-responsiveness was defined as a PAI of < 35%. There was no statistical difference in mean PAI among groups; a higher prevalence of clopidogrel non-responders was noted in group 1 compared to group 3 (p=0.002). Multivariate analysis, adjusting for unequal presence of metabolic syndrome and hypertension, we found no statistical difference between groups. Our data suggests that statins, either fully or partially metabolized by CYP3A4, do not influence PAI when clopidogrel is used at 75 mg/day, even after adjusting for risk factors. We concluded that concomitant statins with clopidogrel therapy does not influence the effect of clopidogrel in PAI.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28257651","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effects of inhibitory amino acids on adenosine release in the mouse hippocampus. 抑制性氨基酸对小鼠海马腺苷释放的影响。

Proceedings of the Western Pharmacology Society Pub Date : 2008-01-01

Pirjo Saransaari, Simo S Oja

引用次数: 0

A pilot study of the effect of diclofenac with B vitamins for the treatment of acute pain following lower-limb fracture and surgery. 双氯芬酸联合B族维生素治疗下肢骨折和手术后急性疼痛的初步研究。

Proceedings of the Western Pharmacology Society Pub Date : 2008-01-01

Alexis F Garza, Raúl Monroy-Maya, Marisela Soto-Ríos, Gerardo Reyes-García, Lourdes Carrillo-Alarcón, Héctor Ponce-Monter, Eduardo Rangel-Flores, Mario I Ortiz

{"title":"A pilot study of the effect of diclofenac with B vitamins for the treatment of acute pain following lower-limb fracture and surgery.","authors":"Alexis F Garza, Raúl Monroy-Maya, Marisela Soto-Ríos, Gerardo Reyes-García, Lourdes Carrillo-Alarcón, Héctor Ponce-Monter, Eduardo Rangel-Flores, Mario I Ortiz","doi":"","DOIUrl":"","url":null,"abstract":"The aim of this pilot study was to compare the efficacy and tolerability of the non-steroidal anti-inflammatory drug (NSAID), diclofenac (2-(2,6-dichloranilino) phenylacetic acid), for treatment of acute pain originated by lower-limb fracture and surgery, with that of diclofenac plus B vitamins. This clinical trial was single-center, prospective randomized and double-blinded. After giving informed consent, patients with lower-limb closed fractures rated their pain on a 10-cm visual analog scale (VAS). Patients were then randomized to receive 75 mg diclofenac or 75 mg diclofenac plus B vitamins (thiamine, pyridoxine and cyanocobalamin) twice daily (all intramuscularly). Patient evaluations of pain intensity were recorded throughout two periods: twenty-four hours pre-surgically and twenty-four hours postsurgical. Twenty-four hours after the first drug administration, patients underwent elective lower-limb surgery. Standardized general anesthetic techniques were used for all patients. Fourteen patients completed the study. The subjects' assessments of limb pain on the visual analog scale showed a significant reduction from baseline values regardless of the treatment group when surveyed at 12, 24, 36 and 48 hr post operation. All treatments showed a similar profile in pain reduction. There were reports of pain in the administration site, but in general, all the regimens were well tolerated.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28257654","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Wegener's granulomatosis presenting as fever of unknown origin in an African-American male. 非裔美国男性韦格纳肉芽肿病表现为不明原因的发热。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Md Aticul Islam, Farshad Bagheri, David Bencomo, Seyedqumars Mirfendereski, Kelly L Cervellione, Solangel Garcia, Katerina Teller, Bryan Falk, Jonas Gintautas, Ayaz Alwani

{"title":"Wegener's granulomatosis presenting as fever of unknown origin in an African-American male.","authors":"Md Aticul Islam, Farshad Bagheri, David Bencomo, Seyedqumars Mirfendereski, Kelly L Cervellione, Solangel Garcia, Katerina Teller, Bryan Falk, Jonas Gintautas, Ayaz Alwani","doi":"","DOIUrl":"","url":null,"abstract":"Wegener's Granulomatosis (WG) is a rare, Multisystem disease of the medium and small sized arteries and veins. It most commonly involves the upper respiratory tract, lungs, and kidneys and often presents as chronic fatigue, upper respiratory infection, sinusitis, and otitis media. Symptoms can include fever, weight loss and fatigue, though these are not usually the primary presenting complaints. development of the disease is highly skewed across ethnicities, with up to 98% of cases being reported in caucasians. We present the case of a 56-year-old African-American male who presented primarily with complaints of uncontrollable fever of unknown origin (FUO) for past two weeks with accompanying sore throat, nasal congestion, night sweats, malaise, and unexplained weight loss of 10 pounds over the past month. Treatment with antibiotics for one week prior to admission showed no relief of symptoms. Chest x-ray showed focal course markings in the right upper lobe. Urinalysis revealed microscopic hematuria and leukocyturia. Chest and abdominal CT scans revealed a right lower lobe pulmonary nodule and heterogeneous areas of enhancement in the spleen. Head CT revealed right mastoid opification. Labs revealed proteinase-3 antibody titer > 100, which is characteristic of WG. Steroids and cyclophosphamide were started with relief of presenting symptoms. Renal biopsy showed pauci-immune P-ANCA associated crescentic and focally necrotizing glomerulonephritis and vascilitis. This case is unique in that the patient presented with primary complaint of FUO. WG should be considered as a rule-out in cases of uncontrollable FUO, even if none of the classic triad of symptoms is present. Though rare, WG should be considered in cases involving non-Caucasian patients.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37432831","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Screening of antimicrobial activity of marine sponge extracts collected from Tunisian coast. 突尼斯海岸海绵提取物抑菌活性的筛选。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Touati Ines, Bakhrouf Amina, Said Khaled, Gaddour Kamel

{"title":"Screening of antimicrobial activity of marine sponge extracts collected from Tunisian coast.","authors":"Touati Ines, Bakhrouf Amina, Said Khaled, Gaddour Kamel","doi":"","DOIUrl":"","url":null,"abstract":"The antibacterial activity of the ethyl acetate extracts of seven marine sponges collected from the Tunisian Mediterranean coast (Monastir) were tested against eight human pathogenic bacteria and six human pathogenic fungi using the agar disk diffusion method. The results show that 90% of the sponge extracts present significant activity against at least one bacterial strain. Extracts of the sponges Agelas oroides and Axinella damicornis appeared to be quite promising due to their capacity to inhibit the growth of Pseudomonas aeruginosa and gentamycin resistant strains of Listeria monocytogenese and Enterococcus feacalis as well as broad spectrum activity against all the other bacteria. The antifungal activity of these sponge extracts is not so promising, in fact only three among 9 sponge extracts show moderate capacity of growth inhibition against fungi strains. Agelas oroides which shows interesting antibacterial activity, has moderate activity against fungi strains tested in this study. Our results with antibacterial and antifungal activity in vitro open the way for complementary investigation in order to purify and identify active molecules.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37432834","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The peripheral antinociceptive effect of nalbuphine is associated with activation of ATP-sensitive K+ channels. 纳布啡的外周抗感觉作用与atp敏感的K+通道的激活有关。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Mario I Ortiz, Eduardo Fernández-Martínez, Héctor Ponce-Monter, Nury Pérez-Hernández, Arturo Macías, Eduardo Rangel-Flores, Gilberto Castañeda-Hérnandez

{"title":"The peripheral antinociceptive effect of nalbuphine is associated with activation of ATP-sensitive K+ channels.","authors":"Mario I Ortiz, Eduardo Fernández-Martínez, Héctor Ponce-Monter, Nury Pérez-Hernández, Arturo Macías, Eduardo Rangel-Flores, Gilberto Castañeda-Hérnandez","doi":"","DOIUrl":"","url":null,"abstract":"There is evidence that local peripheral administration of codeine and morphine produces antinociception through the activation of the ATP-sensitive K(+)-channel. Therefore we evaluated the participation of this channel in the antinociceptive action produced by nalbuphine in the formalin test. Female Wistar rats (160-200 g) were injected in the dorsal surface of the right hind paw with 50 microl of formalin (5%). Nociception was quantified as the number of flinches of the injected paw during 1 hr, whereas a reduction of the number of flinches was considered antinociception. Rats received a s.c. injection (50 microl) into the dorsal surface of the right hind paw of vehicle or increasing doses of nalbuphine (100-400 microg/paw) 20 min before formalin injection into the ipsilateral paw. To determine whether nalbuphine-induced peripheral antinociception was mediated by K(+)-channels, the effect of pretreatment (10 min before formalin injection) with the appropriate vehicle or the ATP-sensitive K(+)-channel inhibitor glibenclamide (25-100 microg/paw) on the antinociceptive effect induced by local peripheral nalbuphine (400 microg/paw) was assessed. Morphine was used as positive antinociceptive control. Local peripheral injection of nalbuphine produced a dose-dependent antinociception during both phases of the test. Local pretreatment with glibenclamide prevented nalbuphine-induced antinociception in a dose-dependent fashion in both phases of the test. Our data suggest that nalbuphine activates ATP-sensitive K(+)-channels in order to produce its peripheral antinociceptive effect.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433014","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

P2y receptor-mediated angiogenesis via vascular endothelial growth factor receptor 2 signaling. P2y受体通过血管内皮生长因子受体2信号介导的血管生成。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Sharif M Rumjahn, Karla A Baldwin, Iain L O Buxton

引用次数: 0

Comparison of antinociceptive efficacy and gastroprotection between celecoxib and diclofenac plus misoprostol in rats. 塞来昔布与双氯芬酸加米索前列醇对大鼠抗伤感受效果及胃保护作用的比较。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Gerardo Reyes-García, Myrna Déciga-Campos, Roberto Medina-Santillan, Vinicio Granados-Soto

{"title":"Comparison of antinociceptive efficacy and gastroprotection between celecoxib and diclofenac plus misoprostol in rats.","authors":"Gerardo Reyes-García, Myrna Déciga-Campos, Roberto Medina-Santillan, Vinicio Granados-Soto","doi":"","DOIUrl":"","url":null,"abstract":"The present study was designed to assess the antinociceptive efficacy and gastroprotective activity of the mixture of diclofenac and misoprostol and its comparison with celecoxib in rats. The effect of diclofenac/misoprostol and celecoxib was assessed in the 1% formalin test. Female Wistar rats were fasted 12 hr before experiments and diclofenac (10 and 50 mg/kg), misoprostol (100 microg/kg), celecoxib (30 and 100 mg/kg), saline and the combination of diclofenac (50 mg/kg) plus misoprostol (25, 50 and 100 microg/kg) were administered orally. Nociceptive behavior was assessed during the following hr. Diclofenac and celecoxib dose-dependently reduced formalin-induced nociception reaching similar maximal effects. Moreover, misoprostol did not produce antinociception, but increased diclofenac-induced antinociception. Animals were sacrificed 3 hr following drug administration and stomachs examined to assess gastric damage. Misoprostol did not produce any damage to the stomach. However, diclofenac, but not celecoxib, produced significant gastric damage (number of stomach ulcers) in a dose-dependent fashion. Misoprostol dose-dependently reduced diclofenac-induced ulcers. Data show that diclofenac and celecoxib lead to similar antinociception, with diclofenac being more active to produce gastric damage. However, diclofenac-induced gastric damage can be markedly reduced by misoprostol. In addition to its gastroprotective effect, misoprostol showed a synergic effect on diclofenac-induced anti-nociception. Considering the cardiovascular effects of COX-2 selective inhibitors, the combination of diclofenac and misoprostol could represent a safer and effective alternative for patients with pain.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Paraquat and maneb induced neurotoxicity. 百草枯和马草草诱导神经毒性。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Bessy Thrash, Subramaniam Uthayathas, Senthilkumar S Karuppagounder, Vishnu Suppiramaniam, Muralikrishnan Dhanasekaran

{"title":"Paraquat and maneb induced neurotoxicity.","authors":"Bessy Thrash, Subramaniam Uthayathas, Senthilkumar S Karuppagounder, Vishnu Suppiramaniam, Muralikrishnan Dhanasekaran","doi":"","DOIUrl":"","url":null,"abstract":"Parkinson's disease is a progressive neurological disorder associated with selective degeneration of nigrostriatal dopaminergic neurons. It is the most common of the neurodegenerative movement disorders, affecting approximately 1% of the population over age 65. Though the exact cause of the neurodegeneration is unknown, it has been shown that environmental factors can contribute to the onset of Parkinson's disease. Parkinsonian symptoms are seen following exposure to the herbicide paraquat, and the fungicide maneb. Furthermore, evidence clearly shows that neurodegeneration develops in environments where workers are co-exposed to paraquat and maneb. These neurotoxins cause a pesticide-induced loss of dopaminergic neurons, inducing a Parkinsonian phenotype. The specific mechanisms by which these environmental neurotoxins affect the nigral dopaminergic neurons are unknown. This gap in mechanistic understanding raises a need for further examination of their cytotoxic effects. Despite advances in pharmacotherapy that have improved quality of life, the mortality rate among Parkinson's disease sufferers remains largely unchanged. There is need for a proactive treatment strategy that could provide neuroprotection or neurorestoration. Since evidence has shown that environmental neurotoxins play an important role in nigral degeneration, there is obviously a need to take a closer look at such toxins since a greater understanding could aid in development of novel pharmacological agents with anti-parkinson and neuroprotective effects. In this review, we intend to examine the role of environmental toxins, namely paraquat and maneb, in the neurotoxicity that leads to dopamine depletion.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433193","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The phospholipidosis-lnducing potential of the chemopotentiating drug, N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE, tesmilifene) correlates with its stimulation of phosphatidylserine synthesis and exposure on the plasma membrane in MCF-7 breast cancer cells. 化学增强药物N,N-二乙基-2-[4-(苯基甲基)苯氧基]乙胺(DPPE，替斯米利芬)的磷脂诱导潜能与其刺激MCF-7乳腺癌细胞的磷脂酰丝氨酸合成和暴露在质膜上相关。

Proceedings of the Western Pharmacology Society Pub Date : 2007-01-01

Fred Y Xu, Gary Queen, Lorne Brandes, Grant M Hatch

{"title":"The phospholipidosis-lnducing potential of the chemopotentiating drug, N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE, tesmilifene) correlates with its stimulation of phosphatidylserine synthesis and exposure on the plasma membrane in MCF-7 breast cancer cells.","authors":"Fred Y Xu, Gary Queen, Lorne Brandes, Grant M Hatch","doi":"","DOIUrl":"","url":null,"abstract":"N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE, tesmilifene), a potent chemopotentiating drug currently in Phase III clinical trials of metastatic breast cancer, increases cytotoxicity of anthracyclines and taxanes in a variety of multi-drug resistance expressing (MDR+) tumor cell lines in vitro; inhibits binding of histamine to CYP3A4, a lipid/prostanoid-regulatory P450; and modulates serum levels of HDL/LDL cholesterol and phospholipids in vivo. Since increased exposure of phosphatidylserine (PS) on the outer cell membrane leaflet is associated with apoptosis, increased clearance of dead cells by phagocytes and inhibition of the P-glycoprotein pump, the effect of DPPE on PS synthesis was assessed in vitro in a human breast cancer cell line. MCF-7 cells were incubated with 5 microM DPPE for 24 hr or 5 days, followed by addition of [1-(14)C]arachidonic acid for 4 hr; or [3H]serine for 8 hr. Compared to untreated cells, a 27-42% (p < 0.05) increase in [1-(14)C]arachidonic acid incorporated into all phospholipids, including a 1.9-fold increase (p < 0.05) in PS was observed in DPPE-treated cells. [3H]Serine incorporation into PS was elevated 37%, while the pool size of PS was elevated 23% (p < 0.05) in DPPE-treated cells, indicating elevated de novo PS biosynthesis. Annexin-5 binding studies indicated an elevation in exposure of PS on the surface of the plasma membrane in DPPE-treated cells. DPPE-treatment also resulted in N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)-1,2-dihexadecanoyl-sn-glycero-3-phosphoethanolamine accumulation indicative of phospholipidosis-inducing potential. Thus, the chemopotentiating effect of DPPE may be due to its phospholipidosis-inducing potential and stimulation of PS synthesis leading to an increased exposure of PS on the cell surface which could potentially enhance cancer cell clearance by phagocytes.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433100","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0