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Thomas Jira - One of the best experts on this subject based on the ideXlab platform.
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Separation of (Z)- and (E)-isomers of thioxanthene and dibenz[b,e]oxepin derivatives with calixarenes and resorcinarenes as additives in nonaqueous capillary electrophoresis.
Electrophoresis, 2003Co-Authors: Torsten Sokoließ, Michael Gronau, Ulf Menyes, Ullrich Roth, Thomas JiraAbstract:Five acidic calix[4]arenes with carboxylic or sulfonic groups at either the upper or lower rim of the cavity and one resorc[4]arene were investigated to separate three thioxanthenes (flupentixol, clopenthixol, chlorprothixene) and a dibenz[b,e]oxepin derivative (Doxepin) with cis-/trans-isomerism by nonaqueous capillary electrophoresis (NACE). Partial filling of the capillary with the UV-absorbing selectors led to a low detection limit and an advantageous signal-to-noise ratio (S/N). A sufficient electrophoretic mobility of the calixarenes towards the anode was necessary to outweigh the oppositely directed electroosmotic flow (EOF). This depended from the functional groups, the dissociation and the hydrodynamic radius of the cyclophanes. In contrast, the resorcinarene was useable only by addition of sodium dodecyl sulfate (SDS) because only the complex of the two selectors had an anodic apparent electrophoretic mobility. p-Sulfonyl-calix[4]arene (ss-a1) was the most capable selector for all E/Z-isomers with maximal alpha-values ranging from 1.056 for Doxepin to 1.224 for chlorprothixene. This was due to the sufficient migration in reversed direction to the EOF even at low pH* values of 3.0. Otherwise, electrostatic as well as hydrophobic interactions with the positively charged isomers seem to contribute to a superior recognition. Increasing the concentration up to 15 mM ss-a1 and using acidic media (pH* 5.0) led to high separation efficiency. Changing the organic solvent provides a powerful tool to improve selectivity with N,N-dimethylformamide-methanol (DMF-MeOH)-mixtures for thioxanthenes. Further electrophoretic parameters were optimized, such as the concentration of the electrolytes, the addition of SDS, the kind of electrolytes and the voltage. Distinct differences in selectivities were found between the derivatives with thioxanthene and dibenzo[b,e]oxepin ring system, respectively. Further, the different basic side chain was responsible for the different selectivity at higher pH* values. In contrast, the substitution at position 2 of the thioxanthenes played a secondary role. Based on the studies of single parameters a method for a simultaneous separation of the four pairs of isomers within 13 min was developed.
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Separation of cis- and trans-isomers of thioxanthene and dibenz[b,e]oxepin derivatives on calixarene- and resorcinarene-bonded high-performance liquid chromatography stationary phases.
Journal of chromatography. A, 2002Co-Authors: Torsten Sokoließ, Ulf Menyes, Ulrich Roth, Thomas JiraAbstract:The chromatographic behavior of six calix[n]arene phases (n=4, 6, 8) and one calix[4]resorcinarene phase is described for the separation of cis- and trans-isomers of three thioxanthene (flupentixol, clopenthixol, chlorprothixene) and one benz[b,e]oxepin derivative (Doxepin). The influences of two different organic modifiers (MeOH, MeCN) for the separation of the isomers on every column are described. Different selectivities of the stationary phases exist as a function of the ring size of the calixarenes and their substitution at the "upper rim" with p-tert.-butyl groups. Furthermore, the influence of free phenol groups on the resorcinarene phase is discussed. Relations between structural elements of the analytes and the retention behavior on the stationary phases are found. The selectivity of the calixarene and resorcinarene stationary phases is compared with a RP-C18 phase containing the same base silica. Advantages of the resorcinarene as well as of the calixarene columns exist for the separation of cis- and trans-isomers of three compounds dependent from the substitution in position 2 of the thioxanthenes, respectively the kind of the basic side chain of all substances.
Parham Reisi - One of the best experts on this subject based on the ideXlab platform.
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Effects of Doxepin on gene expressions of Bcl-2 family, TNF-α, MAP kinase 14, and Akt1 in the hippocampus of rats exposed to stress
Research in Pharmaceutical Sciences, 2017Co-Authors: Parham Reisi, Nastaran Eidelkhani, Laleh Rafiee, Maryam Radahmadi, Mohammad Kazemi, Hojjatallah AlaeiAbstract:Stress is one of the effective factors in the development of depressive disorders that performs some parts of its effects by affecting hippocampus. Since Doxepin has been shown to have neuroprotective effects, in this study, we focused on the effects of Doxepin on the expression of involved genes in neuronal survival and plasticity in the rat hippocampus following chronic stress. Male Wistar rats were divided into four groups, the control, the stress, the stress-Doxepin 1 mg/kg and the stress-Doxepin 5 mg/kg, respectively. To induce stress, the rats were placed within adjustable restraint chambers for 6 h/day, for 21 days. Before daily induction of the stress, rats received an i.p. injection of Doxepin. At the end of experiments, expression of Bax, Bad, Bcl-2, tumor necrosis factor alpha (TNF-α), mitogen‑activated protein kinase 14 (MAPK14) and serine-threonine protein kinase AKT1 genes were detected by reverse transcription polymerase chain reaction (RT-PCR) in the hippocampus. Results showed significant enhancements in expression of Bax, Bad and Bcl-2 genes in the stressed rats, whereas expression of TNF-α, MAPK14, and AKT1 genes didn’t show significant differences. Doxepin could decrease the expression of Bax and Bad genes in the stress group, but had no significant effects on the expression of other genes. The present findings indicated that Doxepin can probably change the pattern of gene expression in the hippocampus to maintain neurons against destructive effects of stress.
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the effects of Doxepin on stress induced learning memory impairments and tnf α level in the rat hippocampus
Research in Pharmaceutical Sciences, 2015Co-Authors: Ali Ahmad Azadbakht, Maryam Radahmadi, Shaghayegh Haghjooye Javanmard, Parham ReisiAbstract:Stress has a profound impact on the nervous system and causes cognitive problems that are partly related to the inflammatory effects. Besides influencing the content of neurotransmitters, antidepressants such as Doxepin are likely to have anti-inflammatory, anti-oxidative, and anti-apoptotic effects. Therefore, the present study investigated the effects of Doxepin on passive avoidance learning and the levels of tumor necrosis factor-alpha (TNF-α) in the rat hippocampus following repeated restraint stress. Male Wistar rats were divided into five groups. Chronic stress was induced by keeping animals within an adjustable restraint chamber for 6 h every day for 21 successive days. In stress-Doxepin group, stressed rats were given 1, 5 and 10 mg/kg of Doxepin intraperitoneally (i.p) for 21 days and before placing them in restraint chamber. Healthy animals who served as control group and stressed rats received normal saline i.p. For evaluation of learning and memory, initial latency and step-through latency were determined using passive avoidance learning test. TNF-α levels were measured in hippocampus by enzyme-linked immunosorbant assay (ELISA) at the end of experiment. Induced stress considerably decreased the step through latencies in the rats (P<0.05) but Doxepin administration prevented these changes. Stress-Doxepin groups did not reveal any differences compared to control group at any given doses. TNF-α level was increased significantly (P<0.05) in stress group. Only the low dose of Doxepin (1 mg/kg) decreased TNF-α level. The present findings indicated that learning and memory are impaired in stressful conditions and Doxepin prevented memory deficit. It seems that inflammation may involve in induced stress memory deficits, and that Doxepin is helpful in alleviating the neural complications due to stress.
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Effects of different doses of Doxepin on passive avoidance learning in rats.
Advanced biomedical research, 2013Co-Authors: Mahsa Gharzi, Parham Reisi, Hamid Reza Dehghani Dolatabadi, Shaghayegh Haghjooy JavanmardAbstract:Background: Studies have shown that Doxepin has anti-inflammatory effects and reduces oxidative stress. Due to the fact that other tricyclic antidepressants have been shown to have neuroprotective effects, this study aimed to investigate the effects of different doses of Doxepin on passive avoidance learning in rats. Materials and Methods: Old male Wistar rats were used in this study. Doxepin was administered intraperitoneally (1, 5 and 10 mg/kg) for 21 days. Passive avoidance learning test was used for evaluation of learning and memory. Rats received foot electrical shock on fifteen day, and step through latencies were evaluated one week after the electrical shock in retention phase. Results: Administration of Doxepin considerably increased the step through latencies in the rats that received the doses of 1 and 5 mg/kg ( P Conclusion: These results indicate that Doxepin has desirable effects on cognitive functions in low doses. Therefore, Doxepin can be considered as memory enhancers that understanding the underling mechanisms need further investigation.
M K Nieuwenhuis - One of the best experts on this subject based on the ideXlab platform.
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Doxepin cream is not effective in reducing itch in burn scar patients a multicenter triple blind randomized clinical crossover trial
Burns, 2020Co-Authors: Kelly A A Kwa, C M Legemate, Anouk Pijpe, Meijde A Vries, Esther Middelkoop, M E Van Baar, Roelf S Breederveld, M K NieuwenhuisAbstract:Objective: To evaluate the effect of Doxepin hydrochloride 5% cream on reducing pruritus in burn scar patients compared to a placebo cream. Method: We conducted a multicenter triple-blind randomized clinical placebo-controlled crossover trial in which burn patients ≥18 years with an itch intensity ≥3 on a Visual Analogue Scale (VAS) were randomized between a Doxepin-placebo or placebo-Doxepin treatment protocol. Patients used each cream during two weeks with a wash-out period of one week in between. Primary outcome was change in itch intensity in two weeks’ time using the VAS. Secondary outcome included the impact of itch (Burn Itch Questionnaire). Other parameters were the use of hydrating cream, silicon treatment, pressure garments, and other antipruritic medication. Results: Twenty-seven patients were included. The change in itch intensity (VAS) was not different during the Doxepin and placebo period (p = 0.994); neither the Doxepin cream nor placebo cream reduced itch intensity. However, based on the Burn Itch Questionnaire, we observed a statistically significant decrease in itch intensity and improvement in impact scores in both treatment groups, but no difference in the degree of reduction between the groups. Conclusion: Doxepin cream was not effective in reducing pruritus in our burn patient study population.
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comparing Doxepin cream to oral antihistamines for the treatment of itch in burn patients a multi center triple blind randomized controlled trial
Burns Open, 2019Co-Authors: Kelly A A Kwa, Anouk Pijpe, Meijde A Vries, Esther Middelkoop, M E Van Baar, Roelf S Breederveld, M K Nieuwenhuis, Anuschka S Niemeijer, H C Kuipers, Z M RashaanAbstract:Abstract Background Doxepin cream, an antihistaminic agent, has shown promising results in the treatment of pruritus in burn patients. However, its effectiveness has not been studied comprehensively. Objective To evaluate whether Doxepin cream is more effective than oral antihistamines in reducing pruritus. Methods We performed a multicenter triple-blind randomized controlled trial of twelve weeks randomizing burn patients ≥18 years with an itch intensity ≥3 on a Visual Analogue Scale (VAS) between Doxepin hydrochloride 5% cream with placebo tablet or oral antihistamine (clemastine) with placebo cream. Primary endpoint was change in itch intensity. Secondary endpoints included impact of itch (Burn Itch Questionnaire), quality of life (SF-36), somnolence, and erythema (DermaSpectrometer). Results Thirty-one (of the intended 108) subjects could be included: 13 were randomized to the Doxepin and 18 to the clemastine group. The skewed distribution is attributable to the low inclusion rate. Both groups showed a significant reduction in itch intensity over a period of twelve weeks (Doxepin p = 0.043, clemastine p = 0.019) with no difference between both groups in: mean itch intensity difference (p = 0.199), any of the domains (p = 0.940, p = 0.698, p = 0.859) of the Burn Itch Questionnaire, quality of life, somnolence (p = 0.143) and erythema (p = 0.796). Conclusion The effectiveness of Doxepin cream was similar to oral antihistamines in reducing itch. However, considering the study ’s limitations, a superior effect of Doxepin cream cannot be completely ruled out. We recommend that future studies use a cross-over design so fewer inclusions are needed to obtain adequate power.
Torsten Sokoließ - One of the best experts on this subject based on the ideXlab platform.
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Separation of (Z)- and (E)-isomers of thioxanthene and dibenz[b,e]oxepin derivatives with calixarenes and resorcinarenes as additives in nonaqueous capillary electrophoresis.
Electrophoresis, 2003Co-Authors: Torsten Sokoließ, Michael Gronau, Ulf Menyes, Ullrich Roth, Thomas JiraAbstract:Five acidic calix[4]arenes with carboxylic or sulfonic groups at either the upper or lower rim of the cavity and one resorc[4]arene were investigated to separate three thioxanthenes (flupentixol, clopenthixol, chlorprothixene) and a dibenz[b,e]oxepin derivative (Doxepin) with cis-/trans-isomerism by nonaqueous capillary electrophoresis (NACE). Partial filling of the capillary with the UV-absorbing selectors led to a low detection limit and an advantageous signal-to-noise ratio (S/N). A sufficient electrophoretic mobility of the calixarenes towards the anode was necessary to outweigh the oppositely directed electroosmotic flow (EOF). This depended from the functional groups, the dissociation and the hydrodynamic radius of the cyclophanes. In contrast, the resorcinarene was useable only by addition of sodium dodecyl sulfate (SDS) because only the complex of the two selectors had an anodic apparent electrophoretic mobility. p-Sulfonyl-calix[4]arene (ss-a1) was the most capable selector for all E/Z-isomers with maximal alpha-values ranging from 1.056 for Doxepin to 1.224 for chlorprothixene. This was due to the sufficient migration in reversed direction to the EOF even at low pH* values of 3.0. Otherwise, electrostatic as well as hydrophobic interactions with the positively charged isomers seem to contribute to a superior recognition. Increasing the concentration up to 15 mM ss-a1 and using acidic media (pH* 5.0) led to high separation efficiency. Changing the organic solvent provides a powerful tool to improve selectivity with N,N-dimethylformamide-methanol (DMF-MeOH)-mixtures for thioxanthenes. Further electrophoretic parameters were optimized, such as the concentration of the electrolytes, the addition of SDS, the kind of electrolytes and the voltage. Distinct differences in selectivities were found between the derivatives with thioxanthene and dibenzo[b,e]oxepin ring system, respectively. Further, the different basic side chain was responsible for the different selectivity at higher pH* values. In contrast, the substitution at position 2 of the thioxanthenes played a secondary role. Based on the studies of single parameters a method for a simultaneous separation of the four pairs of isomers within 13 min was developed.
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Separation of cis- and trans-isomers of thioxanthene and dibenz[b,e]oxepin derivatives on calixarene- and resorcinarene-bonded high-performance liquid chromatography stationary phases.
Journal of chromatography. A, 2002Co-Authors: Torsten Sokoließ, Ulf Menyes, Ulrich Roth, Thomas JiraAbstract:The chromatographic behavior of six calix[n]arene phases (n=4, 6, 8) and one calix[4]resorcinarene phase is described for the separation of cis- and trans-isomers of three thioxanthene (flupentixol, clopenthixol, chlorprothixene) and one benz[b,e]oxepin derivative (Doxepin). The influences of two different organic modifiers (MeOH, MeCN) for the separation of the isomers on every column are described. Different selectivities of the stationary phases exist as a function of the ring size of the calixarenes and their substitution at the "upper rim" with p-tert.-butyl groups. Furthermore, the influence of free phenol groups on the resorcinarene phase is discussed. Relations between structural elements of the analytes and the retention behavior on the stationary phases are found. The selectivity of the calixarene and resorcinarene stationary phases is compared with a RP-C18 phase containing the same base silica. Advantages of the resorcinarene as well as of the calixarene columns exist for the separation of cis- and trans-isomers of three compounds dependent from the substitution in position 2 of the thioxanthenes, respectively the kind of the basic side chain of all substances.
Golnaz Vaseghi - One of the best experts on this subject based on the ideXlab platform.
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protective effects of Doxepin cream on radiation dermatitis in breast cancer a single arm double blind randomized clinical trial
British Journal of Clinical Pharmacology, 2020Co-Authors: Laleh Shariati, Alireza Amouheidari, Hajar Naji Esfahani, Alireza Abed, Shaghayegh Haghjooy Javanmard, Ismail Laher, Ahmad Ghasemi, Golnaz VaseghiAbstract:AIMS Breast cancer is the most frequently occurring cancer in women. Lumpectomy followed by radiotherapy is suggested to be as effective as a total mastectomy. Radiation-induced dermatitis often occurs as a result of breast radiotherapy. Recent studies suggest that Doxepin has promising anti-inflammatory properties. This study was undertaken to evaluate the effects of Doxepin therapy on radiation dermatitis. METHODS A double-blind randomized clinical trial was launched from 2016 to 2017, with a total of 48 patients who had undergone breast-conserving surgery and received postoperative radiation therapy. Radiotherapy was applied 5 days per week for 5 weeks. Adverse dermatological effects were evaluated by a physician at the beginning of the fifth week of radiotherapy and the patients were then randomly assigned (1:1 ratio) to receive either Doxepin (5%) or placebo cream for 7 days. RESULTS There were no significant differences in the dermatitis grade between Doxepin and placebo groups at baseline (P > .5). The occurrence of acute dermatitis (grade 2 or higher) was significantly lower with the use of Doxepin than with placebo (P ≤ .0001, Zα = 1.96 at 95% confidence interval). CONCLUSION Doxepin cream prevents dermatitis grade 2 or higher during post-operative breast irradiation. Doxepin cream is easy to use, affordable and prevents pain and irritation.