Proceedings of the Western Pharmacology Society最新文献_第9页

Vasodilator mechanism of intermedin/adrenomedullin-2 in anesthetized rats. 麻醉大鼠中介素/肾上腺髓质素-2的血管扩张机制。

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

Aly Mohamed Abdelrahman, Catherine Cheuk Ying Pang

{"title":"Vasodilator mechanism of intermedin/adrenomedullin-2 in anesthetized rats.","authors":"Aly Mohamed Abdelrahman, Catherine Cheuk Ying Pang","doi":"","DOIUrl":"","url":null,"abstract":"We examined whether the vasodepressor effect of intermedin/adrenomedullin-2, a new member of the calcitonin gene-related peptide family, acted via activation of the nitric oxide/L-arginine pathway, the prostanoid pathway, or the opening of K+ channels. Intermedin/adrenomedullin-2 (0.3-30 nmol/kg) dose-dependently decreased mean arterial pressure (ED50 of 2.3 +/- 0.69 nmol/kg) and increased heart rate in anesthetized rats. The depressor effect of intermedin/adrenomedullin-2 (3 nmol/kg, ED70 dose) was unaffected by pretreatment with N(G)-nitro-L-arginine methyl ester (L-NAME, inhibitor of NO synthase, 50 mg/kg i.v.), indomethacin (cyclooxygenase inhibitor, 10 mg/kg i.v.), tetraethylammonium (TEA, nonspecific K(+)-channel blocker; 60 mg/kg i.v.) or the respective vehicle. Pretreatment with mecamylamine (ganglionic blocker, 10 mg/kg i.v.) augmented the depressor response and abolished the tachycardic effect of intermedin/adrenomedullin-2 (3 nmol/kg). Therefore, the depressor effect of intermedin/adrenomedullin-2 is not mediated via the nitric oxide/L-arginine pathway, production of prostanoids or opening of TEA-sensitive K+ channels, but is opposed by activity of the sympathetic nervous system. Its tachycardic effect is mediated via the baroreflex mechanism.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"43-6"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433096","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

Bioequivalence of two oral formulations of glyburide (glibenclamide). 格列本脲(格列本脲)两种口服制剂的生物等效性。

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

Francisco J Flores-Murrieta, Miriam del Carmen Carrasco-Portugal, Gerardo Reyes-García, Roberto Medina-Santillán, Jorge E Herrera

{"title":"Bioequivalence of two oral formulations of glyburide (glibenclamide).","authors":"Francisco J Flores-Murrieta, Miriam del Carmen Carrasco-Portugal, Gerardo Reyes-García, Roberto Medina-Santillán, Jorge E Herrera","doi":"","DOIUrl":"","url":null,"abstract":"Glyburide (glibenclamide) is a sulfonylurea derivative that is very widely used in the treatment of type II diabetes mellitus. Currently, there are several pharmaceutical formulations available in Mexico containing this drug, however, very limited information about their bioavailabilities is known. The purpose of this study was to compare the bioavailability of two formulations of glyburide used in Mexico, Daonil and Gen-Glybe. Twenty-four Mexican healthy volunteers participated in this study that was carried out following the recommendations of the Declaration of Helsinki. Subjects received a dose of 10 mg of glyburide (two tablets of 5 mg) under fasting conditions in two separate sessions using a randomized crossover design with a one week washout period. Plasma samples were obtained at selected times over 24 hours and stored frozen until analyzed. Pharmacokinetic parameters were obtained and values (mean +/- S.E.M.) were as follows: Cmax 273.32 +/- 25.84 versus 294.83 +/- 27.12 ng/ml; tmax 3.03 +/- 0.23 versus 2.87 +/- 0.24 h; and AUC24h 1396.66 +/- 130.18 versus 1557.99 +/- 140.24 ng x h/ml, for Daonil and Gen-Glybe tablets, respectively. Pharmacokinetic parameters were compared using analysis of variance for a cross-over design and ratios of AUC24h and Cmax and 90% confidence intervals were obtained. As confidence intervals did not exceed the limits of acceptance (80--125%) for Cmax and AUC24h, it is concluded that the formulations tested are bioequivalent.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"64-6"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433101","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 biological activity of derivatives of 2-[(o-; and p-substituted)aminophenyl]-3H-5-[(o-; and p-substituted)phenyl]-7-chloro-1,4-benzodiazepines and 1-alkyl-3H-5-[(o-; and p- substituted) phenyl]-7-chloro-1,4-benzodiazepin-2-one. 2-[(o-;]和p-substituted) aminophenyl] 3 h-5 - [(o -;和对取代)苯基]-7-氯-1,4-苯二氮卓类药物和1-烷基- 3h -5-[(o-;和对取代苯基]-7-氯-1,4-苯二氮杂平-2- 1。

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

Eduardo Cortés-Cortés, Raúl Salazar Franco, Isidro Ebromares Martínez, Olivia García-Mellado De Cortés, Elia Brosla Naranjo-Rodríguez, Carolina López-Rubalcava

引用次数: 0

Effect of taurine on the concentrations of glutamate, GABA, glutamine and alanine in the rat striatum and hippocampus. 牛磺酸对大鼠纹状体和海马中谷氨酸、GABA、谷氨酰胺和丙氨酸浓度的影响。

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

Svetlana M Molchanova, Simos S Oja, Pirjo Saransaari

引用次数: 0

Kainic acid does not modify the oral pharmacokinetics of carbamazepine in rats. Kainic酸不改变卡马西平在大鼠体内的口服药代动力学。

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

Beatriz Pérez-Guillé, Miriam del Carmen Carrasco-Portugal, Alfonso Alfaro-Rodríguez, Norma Labra-Ruiz, Rosa Soriano-Rosales, Francisco J Flores-Murrieta, Fructuoso Ayala-Guerrero

{"title":"Kainic acid does not modify the oral pharmacokinetics of carbamazepine in rats.","authors":"Beatriz Pérez-Guillé, Miriam del Carmen Carrasco-Portugal, Alfonso Alfaro-Rodríguez, Norma Labra-Ruiz, Rosa Soriano-Rosales, Francisco J Flores-Murrieta, Fructuoso Ayala-Guerrero","doi":"","DOIUrl":"","url":null,"abstract":"Carbamazepine (CBZ) is a widely used antiepileptic agent that frequently interacts with other drugs. Recently, it has been reported that CBZ is able to modify the disturbed sleep patterns induced by kainic acid in epileptics. As a pharmacokinetic-pharmacodynamic characterization in the same animal is not possible due to the stress induced by blood sampling, it is important to establish if kainic acid is able to modify the pharmacokinetics of CBZ. Two groups of seven rats were used in this study. Animals received an oral dose of 50 mg/kg of CBZ alone or with 10 mg/kg of kainic acid. Blood samples (0.1 mL) were obtained at selected times for 12 hr and stored frozen until analyzed by HPLC. Pharmacokinetic parameters were: Cmax 6.51 +/- 1.32 and 6.63 +/- 0.95 microg/mL, tmax 3.55 +/- 0.98 and 1.82 +/- 0.59 hr, AUC 66.61 +/- 28.16 and 73.54 +/- 15.35 microg x h/mL and t1/2 7.16 +/- 2.55 and 5.80 +/- 1.37 hr. No statistically significant difference was observed in any parameter indicating that kainic acid is not able to modify oral pharmacokinetics of CBZ and pharmacokinetic-pharmacodynamic studies may be carried out using two groups of animals, one for the pharmacodynamics and another for the pharmacokinetic evaluation.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"67-8"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433102","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

An atypical course of myasthenia gravis. 重症肌无力的不典型病程。

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

Subir Singh Labana, Salah Qureshi, Thambirajah Nandakumar, Kelly L Cervellione, Guha K Venkatraman, Hasit Thakore, Jonas Gintautas

{"title":"An atypical course of myasthenia gravis.","authors":"Subir Singh Labana, Salah Qureshi, Thambirajah Nandakumar, Kelly L Cervellione, Guha K Venkatraman, Hasit Thakore, Jonas Gintautas","doi":"","DOIUrl":"","url":null,"abstract":"Myasthenia gravis (MG) is a chronic neuromuscular disease which leads to varying degrees of weakness in the skeletal muscles. Some of the symptoms of the disorder include weakness of the eye muscles, difficulty in swallowing and slurred speech. When only the muscles of the eyes are affected, the illness is termed ocular myasthenia, which is often characterized by abrupt onset of diplopia and ptosis of the eyelid. In most patients with ocular-onset MG, there is a progression to involvement of other muscle groups within the first two years (generalized myasthenia). In the case reported here, a 39-year-old male of Ecuadorian descent complained of difficulty seeing, double vision, dizziness, unsteady gait, difficulty maintaining balance and fatigue for the previous two days. Neurological examination was remarkable for total external ophthalmoplegia. There was no external bulbar muscle paralysis, motor weakness, muscle wasting, sensory deficits or sphincter dysfunction. His laboratory workup was significant for elevated acetylcholine receptor antibody. He was diagnosed with ocular MG after differential diagnoses were ruled out based on the onset and presentation of symptoms, the patient's age and a normal magnetic resonance imaging exam. No signs of generalized myasthenia were detected. His symptoms improved dramatically after treatment with Acetyl cholinesterase (AchE) inhibitors and steroids, regaining much of his ocular mobility and ability to walk without gait imbalance. At follow-up visits, the patient remained healthy with no evidence development of other myasthenic signs. This case is atypical since ocular MG does not normally occur in the absence of other myasthenic forms.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"140-2"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37432832","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

Non-invasive assessment of arterial stiffness indices by applanation tonometry and pulse wave analysis in patients with rheumatoid arthritis treated with TNF-alpha blocker remicade (infliximab). 使用tnf - α受体阻滞剂remicade(英夫利昔单抗)治疗的类风湿关节炎患者，通过压压血压计和脉搏波分析对动脉僵硬指数进行无创评估。

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

Alma Cypiene, Aleksandras Laucevicius, Algirdas Venalis, Ligita Ryliskyte, Jolanta Dadoniene, Zaneta Petrulioniene, Milda Kovaite, Violetta Laskova, Jonas Gintautas

{"title":"Non-invasive assessment of arterial stiffness indices by applanation tonometry and pulse wave analysis in patients with rheumatoid arthritis treated with TNF-alpha blocker remicade (infliximab).","authors":"Alma Cypiene, Aleksandras Laucevicius, Algirdas Venalis, Ligita Ryliskyte, Jolanta Dadoniene, Zaneta Petrulioniene, Milda Kovaite, Violetta Laskova, Jonas Gintautas","doi":"","DOIUrl":"","url":null,"abstract":"Rheumatoid arthritis (RA) is accompanied by long lasting inflammation, which may lead to arterial dysfunction and premature aging of the arteries. The purpose of this clinical work was to determine the modification of carotid-radial pulse wave velocity (PWV) and aortic augmentation index (AIx) in young-aged RA patients and the influence of treatment with anti-TNF-alpha (infliximab) on these measures. We examined 68 RA patients (mean age 40.68 yrs) with moderate or high disease activity (DAS28 5.37 +/- 0.94) and 87 controls (mean age 38.10 yrs). PWV and AIx were assessed non-invasively by applanation tonometry. A blood test included serum lipid profile, and high-sensitivity CRP measurements. We found that in RA patients, AIx (p < 0.001) was significantly higher while PWV (p = 0.315) did not differ as compared to control. Multiple regression analysis revealed the presence of RA is an independent predictor for AIx (R2 = 0.718, adjusted R2 = 0.707; p < 0.001). Analysis (Mann-Whitney test) in 15 RA patients revealed lowering of PWV (p = 0.004) under infliximab therapy with no change in AIx (p = 0.573), suggesting the improvement of arterial wall function by anti-TNF-alpha therapy. We conclude that increased AIx is more prominent in RA patients as compared to the controls. PWV appears to be a less sensitive marker for the detection of enhanced development of arterial stiffness in relatively young-aged RA patients. However, PWV may serve as a good marker to discern effects of infliximab on artery elasticity.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"119-22"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37432956","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

Methemoglobinemia and transesophageal echo. 高铁血红蛋白血症和经食管回声。

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

Marcelo A Jiminez, Sotir Polena, Neil L Coplan, Kashyapkumar Patel, Jonas Gintautas

{"title":"Methemoglobinemia and transesophageal echo.","authors":"Marcelo A Jiminez, Sotir Polena, Neil L Coplan, Kashyapkumar Patel, Jonas Gintautas","doi":"","DOIUrl":"","url":null,"abstract":"Methemoglobin (MHb) is the oxidized form of Hemoglobin (Hb) containing iron in its ferric (Fe3+) rather than ferrous (Fe2+) state. Under physiologic conditions, diaphorase II accounts for only a small percentage of the red blood cell reducing capacity but can be pharmacologically activated by exogenous cofactors. Methemoglobinemia is an abnormal elevation of MHb levels resulting in impaired oxygen delivery to tissues as well as a left shift of the oxygen-Hb dissociation curve. We present the case of a 56-year-old female patient who underwent transesophageal echocardiography (TEE) prior to elective cardioversion. Prep for TEE included use of Hurricane spray. Twenty min after receipt, the patient's O2 saturation by pulse oximetry dropped from 100% to 86%; heart rate and blood pressure were unchanged. Physical exam revealed pallor, perioralcyanosis and acrocyanosis without tachypnea, respiratory distress, or jugular venous distension. A 100% non-rebreather mask provided no improvement. MHb was suspected and arterial blood gasses were drawn which was dark chocolate in appearance. Methylene Blue at 1 mg/kg over 5 minutes was administered empirically. ABG results were: pH 7.44/ CO2 40/ O2 315/ HCO2 26/ O2 sat 69%; MHb levels were 30.1% confirming the diagnosis of methemoglobinemia. This condition resolved within minutes. Though uncommon, MHb is the most Sported adverse event associated with topical benzocaine use. Untreated, it can lead to significant cardiopulmonary compromise, neurologic sequelae, and even death. Prompt recognition of this potentially life-threatening side-effect is essential in order to provide opportune treatment.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"134-5"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37432959","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

Palmitic acid analogues exhibiting antinociceptive activity in mice. 棕榈酸类似物在小鼠中表现出抗伤害性活性。

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

Myrna Déciga-Campos, Rosa Mariana Montiel-Ruiz, Gabriel Navarrete-Vázquez, Francisco Javier López-Muñoz

{"title":"Palmitic acid analogues exhibiting antinociceptive activity in mice.","authors":"Myrna Déciga-Campos, Rosa Mariana Montiel-Ruiz, Gabriel Navarrete-Vázquez, Francisco Javier López-Muñoz","doi":"","DOIUrl":"","url":null,"abstract":"Three palmitic acid derivatives were synthesized and evaluated as a potential platform for antinociceptive drug development. Female Swiss Webster mice were given N-(4-Methoxy-2-nitrophenyl)hexadecanamide (1), 2-amino-3-(palmitoylamino)benzoic acid (2) or 4-amino-3-(palmi-toylamino)benzoic acid (3) orally in doses of 10-100 mg/kg. The animals were tested for nociception using the hot plate and abdominal constriction response (writhing) tests. Compound 1 generated a dose-dependent antinociceptive effect, reflected by longer latencies (paw-lick and escape responses) and a decrease in writhing. Morphine (1.5-6 mg/kg, p.o.) and diclofenac (10-100 mg/kg, p.o.) were used as positive controls, respectively. Compounds 2 and 3 were less active in both nociceptive tests. The antinociception provoked by compound 1 was partially blocked by naloxone (1 mg/kg, i.p.) suggesting that this pharmacological effect could be due to the activation of micro-opioid receptors. N-(4-Methoxy-2-nitrophenyl)hexadecanamide showed antinociceptive effects in both nociceptive tests suggesting the possibility that this compound may define a new type of antinociceptive.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":"50 ","pages":"75-7"},"PeriodicalIF":0.0,"publicationDate":"2007-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37433015","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

New approaches in analyzing the pharmacological properties of herbal extracts. 草药提取物药理性质分析的新方法。

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

Matthias Hamburger

引用次数: 0