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1.
Am J Otolaryngol ; 41(3): 102390, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31926598

RESUMO

OBJECTIVES: We investigated the frequency of tinnitus in fibromyalgia patients and the effect of drugs used for routine fibromyalgia on tinnitus. METHODS: We included 101 diagnosed fibromyalgia patients. After detailed ear nose throat examination, audiometric tests and tinnitus handicap index (THI) were performed. After the tests, routine treatment for fibromyalgia was started by the physical therapy and rehabilitation department. Two months after the beginning of the treatment, THI were repeated again and the results were statistically evaluated. RESULTS: All patients included in the study were women. 74.3% of the patients had tinnitus. Pregabalin and selective serotonin and norepinephrine reuptake inhibitor (SNRI) antidepressant-treated patients were evaluated; In both groups, there was a statistically significant difference between pre- and post-treatment tinnitus levels (p < .001). However, there was no statistically significant difference between pregabalin group and diloxetine group according to treatment results. CONCLUSIONS: The incidence of tinnitus is high in fibromyalgia patients. That pregabalin and duloxetine agents routinely used in fibromyalgia require further experimental and human studies in order to be able to use in tinnitus.


Assuntos
Antidepressivos/uso terapêutico , Cloridrato de Duloxetina/uso terapêutico , Fibromialgia/tratamento farmacológico , Fibromialgia/etiologia , Pregabalina/uso terapêutico , Inibidores Seletivos de Recaptação de Serotonina/uso terapêutico , Zumbido/tratamento farmacológico , Zumbido/etiologia , Adulto , Idoso , Feminino , Fibromialgia/terapia , Humanos , Pessoa de Meia-Idade , Modalidades de Fisioterapia , Zumbido/diagnóstico , Adulto Jovem
2.
Int J Impot Res ; 17(2): 201-3, 2005.
Artigo em Inglês | MEDLINE | ID: mdl-15284834

RESUMO

In this paper, we evaluated the new antipsychotic, quetiapine-induced sexual dysfunctions (SDs). The study group consisted of 36 patients with schizophrenia receiving quetiapine. The changes in general sexual functions were assessed by using Arizona Sexual Experience Scale (ASEX) and Udvalg for Kliniske Undersogelser (UKU) Side Effect Rating Scale at baseline and week 4. Also, prolactin (PRL) values were determined at baseline and week 4. There was statistically significant difference with respect to the mean ASEX score at week 4 compared with baseline. The most frequent SD was diminished libido in both male (31.8%) and female subjects (28.6%). No significant correlation was found between ASEX scores and PRL values. The results suggest that SDs are an important problem using even novel antipsychotic, quetiapine.


Assuntos
Antipsicóticos/efeitos adversos , Dibenzotiazepinas/efeitos adversos , Disfunções Sexuais Psicogênicas/induzido quimicamente , Adulto , Antipsicóticos/uso terapêutico , Dibenzotiazepinas/uso terapêutico , Relação Dose-Resposta a Droga , Disfunção Erétil/induzido quimicamente , Feminino , Humanos , Libido , Masculino , Pessoa de Meia-Idade , Prolactina/sangue , Fumarato de Quetiapina , Esquizofrenia/tratamento farmacológico
3.
Eur Arch Psychiatry Clin Neurosci ; 254(4): 231-5, 2004 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-15309392

RESUMO

A growing body of evidence indicates that oxidative stress is involved in the etiopathogenesis of some psychiatric disorders. In our previous study, we have found that social phobia (SP) seems to be associated with elevated antioxidant enzymes and malondialdehyde (MDA) levels, a lipid peroxidation product. In the present investigation, we sought to determine whether the increased radical burden observed in patients with SP would be attenuated with alleviation of symptoms. Thirty-nine patients diagnosed with generalized SP and 39 healthy controls participated in this study. The measurements of MDA, superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT) were performed before and after a period of 8 weeks of citalopram treatment. In this period, the patients received citalopram but controls did not. The initial dose of citalopram was 20mg, with 20 mg increments occurring every 2 weeks, to a maximum dose of 60 mg, with the mean daily dose of 38.9 +/- 13.3 mg/day. All patients were evaluated by using Liebowitz Social Anxiety Scale (LSAS). The mean MDA, SOD, GSH-Px and CAT levels of the patient group at baseline were significantly higher than those of controls. Antioxidant enzymes and MDA levels decrease significantly through citalopram treatment. Significant and positive correlation was observed between decrease in the total LSAS scores, and SOD or CAT levels. In conclusion, our results suggest that, in patients with SP, subchronic treatment with citalopram may decrease antioxidant enzymes and MDA values and that they are state markers of SP because they return to normal values with treatment.


Assuntos
Antidepressivos de Segunda Geração/farmacologia , Citalopram/farmacologia , Malondialdeído/sangue , Oxirredutases/sangue , Transtornos Fóbicos/sangue , Antidepressivos de Segunda Geração/uso terapêutico , Catalase/sangue , Citalopram/uso terapêutico , Glutationa Peroxidase/sangue , Humanos , Transtornos Fóbicos/tratamento farmacológico , Superóxido Dismutase/sangue
4.
Protein J ; 23(8): 495-500, 2004 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-15648971

RESUMO

Tosylphenylalanine chloromethyl ketone (TPCK) and tosyllysine chloromethyl ketone (TLCK) are irreversible modifiers of histidine which is located in the catalytic triad of chymotrypsin and trypsin, respectively. The effects of TPCK and TLCK on the histidine in the catalytic triad of the desensitized butyrylcholinesterase (BChE), prepared from human serum by heating at 45 degrees C for 24 h, were investigated in detail. It is found that these reagents do not modify, but reversibly inhibit the desensitized enzyme as a function of time. Just as it is for the native enzyme, TPCK is a hyperbolic mixed-type inhibitor of the desensitized BChE with Ki, alpha and beta values of 0.017 +/- 0.003 mM, 3.942 +/- 1.125 and 0.524 +/- 0.070, respectively. However, TLCK is the pure competitive inhibitor of the desensitized BChE with a Ki value of 0.008 +/- 0.000 mM, while it is hyperbolic mixed-type inhibitor of the native form. These findings show that the conformation of the active site cavity of desensitized BChE is different from that of the native enzyme.


Assuntos
Alquilantes/química , Butirilcolinesterase/química , Inibidores da Colinesterase/química , Histidina/química , Tosilina Clorometil Cetona/química , Tosilfenilalanil Clorometil Cetona/química , Sítios de Ligação , Butirilcolinesterase/sangue , Diálise , Humanos , Cinética
5.
Acta Psychiatr Scand ; 108(3): 208-14, 2003 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-12890276

RESUMO

OBJECTIVE: Previous studies demonstrate a relationship between lipid metabolism and suicide or impulsive-aggressive behaviours. Leptin seems to be related with lipid metabolism. Therefore, the aim was to measure total serum cholesterol and leptin levels in 16 medication-free schizophrenic patients with and without suicide attempts and in 16 healthy controls. METHOD: Subjects were assessed by using Impulsivity Rating (IRS) and Modified Overt Aggression Scale (MOAS). RESULTS: The patients had lower total cholesterol and leptin levels in serum compared with the controls. Significantly lower total cholesterol and leptin levels were observed in patients who had attempted suicide compared with those who had not. The levels were observed to be low in violent attempters when compared with non-violent attempters. MOAS and IRS scores were negatively correlated with both cholesterol or leptin levels in patients. CONCLUSION: The results indicated that medication-free schizophrenic patients have statistically significant lower serum cholesterol and leptin levels compared with controls and the difference is obvious in suicide attempters compared with non-suicide attempters and in violent attempters than non-violent attempters.


Assuntos
Colesterol/sangue , Leptina/sangue , Esquizofrenia/sangue , Tentativa de Suicídio/psicologia , Tentativa de Suicídio/estatística & dados numéricos , Adulto , Agressão/psicologia , Análise de Variância , Estudos Transversais , Feminino , Humanos , Comportamento Impulsivo/psicologia , Masculino , Pessoa de Meia-Idade , Valor Preditivo dos Testes , Escalas de Graduação Psiquiátrica , Valores de Referência , Psicologia do Esquizofrênico , Violência/psicologia
6.
Biol Trace Elem Res ; 93(1-3): 55-62, 2003.
Artigo em Inglês | MEDLINE | ID: mdl-12835490

RESUMO

Human serum butyrylcholinesterase (BChE) has been converted into a stable but less active desensitized form when heated at 45 degrees C for 24 h. The desensitized BChE follows Michaelis-Menten kinetics, whereas native enzyme exhibits slightly negative cooperativity with respect to butyrylthiocholine binding. In this study, we investigated the effects of Ni2+, Co2+, and Mn2+ on the desensitized BChE. It is found that all three ions were noncompetitive inhibitors of the desensitized BChE, and Ki values have been determined as 7.816 +/- 1.060 mM, 48.722 +/- 4.635 mM, and 84.795 +/- 5.249 mM for Ni2+, Co2+, and Mn2+, respectively. In our previous study, these ions were linear mixed-type inhibitors of the native BChE. This finding confirms that desensitized BChE changes to a different conformation than native BChE. From the comparison of Ki values of the trace elements, it can be said that Ni2+ is a more effective inhibitor of the desensitized BChE than Co2+ and Mn2+.


Assuntos
Butirilcolinesterase/sangue , Butirilcolinesterase/metabolismo , Cobalto/farmacologia , Manganês/farmacologia , Níquel/farmacologia , Inibidores da Colinesterase/farmacologia , Estabilidade Enzimática , Temperatura Alta , Humanos , Cinética , Conformação Proteica/efeitos dos fármacos , Desnaturação Proteica
7.
Biol Trace Elem Res ; 91(2): 151-6, 2003 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-12719610

RESUMO

This study is aimed at investigating the inhibitory effect of cadmium ion on glutathione reductase activity of rabbit brain and liver and the relationship of this effect with dietary selenium. For this purpose, one group of New Zealand rabbits were fed a selenium-deficient diet, another group was fed a selenium-rich diet, and the control group was fed a normal diet. The brain and liver tissues of these groups were investigated for the in vitro inhibitory effects of Cd2+ on glutathione reductase activity. For liver, the percentage inhibition of glutathione reductase by 40 nmol/mg protein of Cd2+ was similar for selenium-deficient and control groups, but significantly lower in the selenium-rich group. For brain tissues, there was no difference with respect to cadmium inhibition of glutathione reductase in all three groups.


Assuntos
Antioxidantes/uso terapêutico , Cádmio/antagonistas & inibidores , Cádmio/toxicidade , Inibidores Enzimáticos/farmacologia , Glutationa Redutase/antagonistas & inibidores , Selênio/uso terapêutico , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/enzimologia , Dieta , Feminino , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Proteínas/metabolismo , Coelhos , Selênio/deficiência
8.
Urol Int ; 70(3): 211-5, 2003.
Artigo em Inglês | MEDLINE | ID: mdl-12660459

RESUMO

INTRODUCTION: Inguinal hernia and hydrocele are suggested to result from the persistence of smooth muscle (SM) which should undergo programmed cell death (PCD) after presenting transiently to propel the testis. Since Ca(2+) is involved in PCD, the Ca(2+) contents of the peritoneum and sacs associated with undescended testis, inguinal hernia and hydrocele were determined and compared. MATERIALS AND METHODS: Sacs were obtained from boys with undescended testis (n = 11), inguinal hernia (n = 22) and hydrocele (n = 10), and girls with inguinal hernia (n = 7). The calcium content of the sacs and peritoneal samples (n = 6) was determined through atomic absorption spectrophotometry. Calcium contents were compared according to their sources using the Mann-Whitney U test and p values of <0.05 were considered significant. RESULTS: While revealing similar Ca(2+) contents as the peritoneum, sacs associated with undescended testis and hydrocele contained more Ca(2+) contents than the sacs of boys and girls with inguinal hernia (p < 0.05). CONCLUSIONS: Sacs associated with inguinal hernia, which are known to contain SM all around the mesothelial layer, contain the least Ca(2+). Despite the decrease in SM, sacs associated with hydrocele contain more Ca(2+). Since PCD is associated with Ca(2+) overload and inhibition of Ca(2+) load inhibits PCD, differences in Ca(2+) content may reflect the inhibition of PCD at different stages and for different reasons in inguinal hernia or hydrocele of childhood.


Assuntos
Apoptose , Cálcio/metabolismo , Criptorquidismo/metabolismo , Hérnia Inguinal/metabolismo , Hidrocele Testicular/metabolismo , Cálcio/fisiologia , Pré-Escolar , Feminino , Humanos , Lactente , Masculino , Músculo Liso/metabolismo , Peritônio/metabolismo
9.
Soc Psychiatry Psychiatr Epidemiol ; 38(2): 88-93, 2003 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-12563551

RESUMO

BACKGROUND: Conversion disorder (CD) is a common disease and its importance still continues in Turkey and particularly in Eastern Turkey. The aim of this study is to examine sociodemographic and clinical characteristics of CD. METHOD: Among 198 consecutive patients having CD diagnosed by structured DSM-III-R clinical interview, the psychosocial characteristics of the patients were clinically investigated. RESULTS: The most common subtype of CD was non-epileptic seizure (NES) (41.4 %). The psychosocial stress factors were found in the initiation or at the last episode of the disorder (88.9 %). The most prominent problem related with primary support group was traumatic event (37.9 %) followed by problems associated with migration and related economical problems which are the most important problems of the study area. The incidence of depressive disorders was high in patients with CD, and the histrionic personality disorder was the most prominent personality pathology among the patients. Direct referral to psychiatry clinics appeared to be low (12.1 %). CONCLUSION: Our findings have shown that traumatic events may have an important role in the occurrence, severity and duration of CD, and most of the patients seek help from religious healers. The study has also revealed that lower education level and socioeconomic and sociocultural problems may play a role in the occurrence of the disorder as well as regarding its course.


Assuntos
Transtorno Conversivo/epidemiologia , Transtorno Conversivo/patologia , Demografia , Adulto , Transtorno Conversivo/psicologia , Coleta de Dados , Feminino , Humanos , Incidência , Masculino , Pessoa de Meia-Idade , Personalidade , Fatores Socioeconômicos , Turquia/epidemiologia
10.
BJU Int ; 91(3): 252-4, 2003 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-12581014

RESUMO

OBJECTIVE: To evaluate serum leptin levels (an adipocyte hormone involved in the suppression of appetite) in patients with premature ejaculation before and after treatment with citalopram, a selective serotonin reuptake inhibitor, with the hypothesis that leptin levels might become normal during this treatment. PATIENTS AND METHODS: The inhibitory effect of serotonin on libido, ejaculation and orgasm is well documented. Although there is no direct evidence of an association involving brain pathways which are related to sexual behaviour, there is an interaction between leptinergic and serotonergic systems. In a previous study serum leptin levels were high in patients with premature ejaculation. The present study comprised 30 patients with premature ejaculation according to the Diagnostic and Statistical Manual of Mental Disorders Third Revised Version. Fifteen patients (group I) were randomly assigned to 8 weeks of citalopram treatment and the remainder (15, group II) received no therapy. The patients were asked to determine the average intravaginal ejaculation latency time, and their fasting serum leptin levels were measured at baseline and after 8 weeks. RESULTS: There was no significant difference in the mean intravaginal ejaculation latency time between the groups at baseline; it increased after 8 weeks of treatment with citalopram in group I, to a mean (sd) of 209 (72.1) s, but not in group II. No difference was detected in leptin levels between the groups at baseline, but at 8 weeks they were lower in group I. CONCLUSION: As hypothesized, leptin levels decreased in patients with premature ejaculation after treatment with citalopram, and this decrease seemed to be linked to the therapeutic effect. Further experimental studies are needed.


Assuntos
Citalopram/uso terapêutico , Ejaculação/efeitos dos fármacos , Leptina/sangue , Inibidores Seletivos de Recaptação de Serotonina/uso terapêutico , Disfunções Sexuais Fisiológicas/tratamento farmacológico , Adulto , Biomarcadores/sangue , Índice de Massa Corporal , Método Duplo-Cego , Humanos , Masculino , Disfunções Sexuais Fisiológicas/sangue
11.
J Protein Chem ; 22(6): 585-9, 2003 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-14703992

RESUMO

The effects of Ni2+, Co2+, and Mn2+ on human serum butyrylcholinesterase (BChE, acylcholine acylhydrolase E.C. 3.1.1.8) were investigated in this study. Inhibition kinetics of BChE were studied using butyrylthiocholine (BTCh) as substrate. The "1/v" versus "1/[BTCh]" plots in the absence (control plot) and in the presence of the metal ions intersected above 1/[BTCh]-axis for all trace elements. In addition, when the concentrations of the cations were increased at 4 mM BTCh, velocities decreased and drove to zero at high concentrations of the trace elements. These results demonstrate that Ni2+, Co2+, and Mn2+ are linear mixed-type inhibitors of BChE. alphaK(i) values have been determined as 53.20 mM,152.25 mM, and 190.24 mM for Ni2+, Mn2+, and Co2+, respectively, by using nonlinear regression analysis. From the comparison of alphaK(i) values of the trace elements, it can be said that BChE has more affinty to binding Ni2+ than Co2+ and Mn2+.


Assuntos
Butirilcolinesterase/sangue , Inibidores da Colinesterase/farmacologia , Cobalto/farmacologia , Manganês/farmacologia , Níquel/farmacologia , Humanos , Cinética
12.
Int J Impot Res ; 14(6): 502-5, 2002 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-12494286

RESUMO

BACKGROUND: Despite the limited number of available study comparing of their efficacy, selective serotonin re-uptake inhibitors (SSRI) have been thought to have beneficial effects for the patients with premature ejaculation. In the present study, we decided to examine the efficacy of citalopram, an SSRI, in the treatment of premature ejaculation. METHOD: The study was consisted of 26 married patients diagnosed with premature ejaculation according to Diagnostic and Statistical Manual of Mental Disorders Third Revised Version (DSM-III-R). The patients were randomly assigned to two groups, citalopram (group I) and placebo (group II), each consisting of 13 patients. The effects of drug on the ejaculatory function were assessed by the intravaginal ejaculation latency time. Additionally, all patients were screened by using Clinical Global Impression-Improvement Scale (CGI-I) and Yonsei Sexual Function Inventory-II (YSFI-II). RESULTS: The increase in the intravaginal ejaculation latency time in the citalopram group was statistically significant than that of placebo group. In addition, with respect to the subscales of the YSFI-II scale, similar overall significant improvements were seen in the patients given citalopram compared to those given placebo. Of group I patients, five (38.5%) were considered as 'very much improved' and four (30.8%) 'much improved' by CGI-I and only one of group II patients (7.7%) showed 'much improved'. CONCLUSION: The patients treated with citalopram showed significantly greater improvement compared to the patients receiving placebo.


Assuntos
Citalopram/uso terapêutico , Ejaculação/efeitos dos fármacos , Inibidores Seletivos de Recaptação de Serotonina/uso terapêutico , Disfunções Sexuais Fisiológicas/tratamento farmacológico , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Placebos , Tempo de Reação/efeitos dos fármacos , Fatores de Tempo , Resultado do Tratamento , Vagina
13.
Int J Impot Res ; 14(6): 547-9, 2002 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-12494295

RESUMO

In the present study, we aimed to examine the efficacy of sildenafil in patients with an antipsychotic (olanzapine)-induced erectile dysfunction (ED). The study group comprised 10 patients who experienced ED associated with the use of olanzapine. The patients initially received 50 mg sildenafil at baseline. If clinically indicated, titration up to 100 mg was permitted. All patients were assessed by Clinical Global Impression-Improvement (CGI-I) and International Index of Erectile Dysfunction (IIEF) scales at baseline and weeks 2 and 4. At final assessment, three patients were considered 'very much improved' and four 'much improved' according to CGI-I. Our results suggest that sildenafil use is effective and well-tolerated in patients with olanzapine-induced ED.


Assuntos
Antipsicóticos/efeitos adversos , Disfunção Erétil/induzido quimicamente , Disfunção Erétil/tratamento farmacológico , Inibidores de Fosfodiesterase/uso terapêutico , Piperazinas/uso terapêutico , Pirenzepina/análogos & derivados , Pirenzepina/efeitos adversos , Benzodiazepinas , Humanos , Masculino , Olanzapina , Ereção Peniana/efeitos dos fármacos , Inibidores de Fosfodiesterase/efeitos adversos , Piperazinas/efeitos adversos , Purinas , Citrato de Sildenafila , Sulfonas , Resultado do Tratamento
14.
Arch Androl ; 48(5): 345-50, 2002.
Artigo em Inglês | MEDLINE | ID: mdl-12230820

RESUMO

Leptin is a fat cell-derived hormone signaling the hypothalamus about food intake, the regulation of weight, and sexual behavior. The inhibitory effect of serotonin on libido, ejaculation, and orgasm is well documented. There is an interaction between leptinergic and serotonergic systems in the central nervous system. This study was conducted to evaluate serum leptin levels of the patients with premature ejaculation. The study group consisted of 15 patients with premature ejaculation according to Diagnostic and Statistical Manual of Mental Disorders, Third Revised Version (DSM-III-R) and 15 healthy controls. The fasting serum leptin levels were measured. Significantly high serum leptin levels in the patients were found after body mass index or age adjustment. The intravaginal ejaculation latency time negatively correlated with leptin levels in both patient and control groups. In addition, there was a positive correlation between leptin levels and the duration of illness. It would appear that leptin may be associated with premature ejaculation.


Assuntos
Ejaculação , Leptina/sangue , Disfunções Sexuais Fisiológicas/sangue , Humanos , Masculino
15.
Urol Int ; 69(2): 111-5, 2002.
Artigo em Inglês | MEDLINE | ID: mdl-12187040

RESUMO

In addition to an increase in contractility, contracted fibers and small and electron-dense mitochondria have suggested an increase of cytosolic Ca(2+) within the cremaster muscles (CM) associated with undescended testis. Therefore, the Ca(2+) content of CM associated with an undescended testis was determined and compared with the Ca(2+) content associated with inguinal hernia and hydrocele and in internal oblique muscles. CM samples from boys with undescended testis (n = 9), inguinal hernia (n = 15), and hydrocele (n = 7) and from girls with inguinal hernia (n = 8) were obtained. The calcium contents of these samples and of samples from internal oblique muscle (n = 6) were determined by atomic absorption spectrophotometry. While the Ca(2+) contents of CM from boys with undescended testis and from girls with inguinal hernia were similar (p > 0.05), the internal oblique muscle and the CM from boys with inguinal hernia and hydrocele contained more Ca(2+) than CM from boys with undescended testis (p < 0.05). Despite evidence of an increase in cytosolic calcium, the decrease in total calcium content suggests a decrease in the adenylyl cyclase activity, thus inhibition of influx of Ca(2+), but an increase in phospholipase C activity, and generation of more inositol 1,4,5-trisphosphate and mobilization of calcium from internal stores. Since the sympathetic system acts through adenylyl cyclase in striated muscles and is sexually dimorphic, similar Ca(2+) contents as encountered in girls suggest an alteration in the balance of autonomic innervation against the sympathetic system in boys with undescended testis.


Assuntos
Cálcio/análise , Criptorquidismo/etiologia , Músculo Esquelético/química , Sistema Nervoso Simpático/fisiopatologia , Adenilil Ciclases/metabolismo , Pré-Escolar , Citosol/química , Feminino , Hérnia Inguinal/metabolismo , Humanos , Inositol 1,4,5-Trifosfato/metabolismo , Masculino , Espectrofotometria Atômica , Hidrocele Testicular/metabolismo , Fosfolipases Tipo C/metabolismo
16.
J Protein Chem ; 21(3): 145-9, 2002 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-12018615

RESUMO

Butyrylcholinesterase purified from human serum as 6600-fold was heated at 37 degrees, 40 degrees, 45 degrees, and 50 degrees C for 24 hr. It was observed that the enzyme heated at 45 degrees C for 24 hr converted to a stabilized form and followed Michaelis-Menten kinetics, whereas the enzyme samples, heated at the other temperatures for 24 hr, shown negative cooperativity with respect to its substrate, butyrylthiocholine. Even the sample heated at 45 degrees C for 12 hr shown negative cooperativity. On the contrary to the heated enzyme at 40 degrees C for 24 hr, the heated enzyme at 45 degrees C for 24 hr could not be reactivated when it was kept at 4 degrees C for 24 hr. In the kinetic studies, it was found that substrate analogs choline and benzoylcholine inhibited both the native enzyme and the enzyme heated at 45 degrees C for 24 hr competitively, whereas succinylcholine was the partial competitive inhibitor of native enzyme but the pure competitive inhibitor of the heated enzyme.


Assuntos
Butirilcolinesterase/sangue , Butirilcolinesterase/química , Ligação Competitiva , Butirilcolinesterase/metabolismo , Colina/análogos & derivados , Colina/metabolismo , Inibidores da Colinesterase/química , Ativação Enzimática , Temperatura Alta , Humanos , Cinética , Desnaturação Proteica , Termodinâmica
17.
Int Clin Psychopharmacol ; 17(3): 115-9, 2002 May.
Artigo em Inglês | MEDLINE | ID: mdl-11981352

RESUMO

Recently, atypical antipsychotics have been used for the management of the patients with refractory obsessive-compulsive disorder (OCD). The aim of the present study was to evaluate the results of quetiapine augmentation to a serotonin reuptake inhibitor (SRI) in the patients with refractory OCD. Fifty-two patients with OCD according to DSM-IV entered 3 months of an open-label phase treatment with a SRI with or without concomitant adjunctive treatment regimen. Of them, 27 patients were refractory OCD. These patients were randomly divided into two groups, SRI plus quetiapine and SRI plus placebo, for an 8-week single-blind phase. The course of OCD was evaluated by Yale-Brown Obsession-Compulsion (Y-BOCS) and Clinical Global Impression-Severity of Illness and Improvement (CGI-SI and I) Scales every other week for 8 weeks. Of the 14 patients in group I, nine (64.4%) showed significant improvement with 60% or greater improvement on the Y-BOCS and one (7.1%) partial improvement with 30% or greater improvement on the Y-BOCS, whereas no improvement was observed in group II. The addition of quetiapine to ongoing SRI therapy has been found to be effective and well-tolerated approach in patients with refractory OCD.


Assuntos
Antipsicóticos/farmacologia , Dibenzotiazepinas/farmacologia , Transtorno Obsessivo-Compulsivo/tratamento farmacológico , Inibidores Seletivos de Recaptação de Serotonina/uso terapêutico , Administração Oral , Adolescente , Adulto , Antipsicóticos/administração & dosagem , Dibenzotiazepinas/administração & dosagem , Resistência a Medicamentos , Quimioterapia Combinada , Feminino , Humanos , Masculino , Placebos , Fumarato de Quetiapina , Método Simples-Cego , Resultado do Tratamento
18.
Phytother Res ; 16(1): 88-90, 2002 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-11807975

RESUMO

In this study, it was shown that abietic acid, an abietane diterpenoid, inhibited soybean 5-lipoxygenase (linoleate: oxygen oxidoreductase, EC 1.13.11.12) and an IC(50) of 29.5 +/- 1.29 microM was determined. Since the lipoxygenase pathway leads to the biosynthesis of leukotrienes this result supports the view that abietic acid may be used in the treatment of allergic reactions.


Assuntos
Abies , Abietanos , Diterpenos/farmacologia , Inibidores Enzimáticos/farmacologia , Lipoxigenase/metabolismo , Fenantrenos/farmacologia , Extratos Vegetais/farmacologia , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Ácido Linoleico/farmacologia , Estrutura Molecular , Fenantrenos/química , Fenantrenos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
19.
Biol Trace Elem Res ; 81(2): 141-52, 2001 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-11554395

RESUMO

Since selenium and vitamin E have been increasingly recognized as an essential element in biology and medicine, current research activities in the field of human medicine and nutrition are devoted to the possibilities of using these antioxidants for the prevention or treatment of many diseases. The present study was aimed at investigating and comparing the effects of dietary antioxidants on glutathione reductase and glutathione peroxidase activities as well as free and protein-bound sulfhydryl contents of rat liver and brain tissues. For 12-14 wk, both sex of weanling rats were fed a standardized selenium-deficient and vitamin E-deficient diet, a selenium-excess diet, or a control diet. It is observed that glutathione reductase and glutathione peroxidase activities of both tissues of the rats fed with a selenium-deficient or excess diet were significantly lower than the values of the control group. It is also shown that free and bound sulfhydryl concentrations of these tissues of both experimental groups were significantly lower than the control group. The percentage of glutathione reductase and glutathione peroxidase activities of the deficient group with respect to the control were 50% and 47% in liver and 66% and 61% in the brain, respectively; while these values in excess group were 51% and 69% in liver and 55% and 80% in brain, respectively. Free sulfhydryl contents of the tissues in both experimental groups showed a parallel decrease. Furthermore, the decrease in protein-bound sulfhydryl values of brain tissues were more pronounced than the values found for liver. It seems that not only liver but also the brain is an important target organ to the alteration in antioxidant system through either a deficiency of both selenium and vitamin E or an excess of selenium alone in the diet.


Assuntos
Fenômenos Fisiológicos da Nutrição Animal , Antioxidantes/farmacologia , Encéfalo/metabolismo , Fígado/metabolismo , Selênio/farmacologia , Vitamina E/farmacologia , Animais , Encéfalo/efeitos dos fármacos , Feminino , Glutationa Peroxidase/metabolismo , Glutationa Redutase/metabolismo , Fígado/efeitos dos fármacos , Masculino , Ratos , Ratos Wistar
20.
Arch Biochem Biophys ; 386(1): 25-9, 2001 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-11360997

RESUMO

Benactyzine and drofenine are widely used anticholinergic drugs. Benactyzine is used to treat organophosphate poisoning and drofenine acts on smooth muscle to stop muscle spasms. Both of these drugs are esters. After they enter the bloodstream, they will interact with butyrylcholinesterase (BChE; acylcholine acyl hydrolase: EC 3.1.1.8), which has an ability to hydrolyze a wide variety of esters. Therefore, the kinetic analysis of their inhibitory effects on human serum BChE was examined using butyrylthiocholine as substrate. Both drugs were competitive inhibitors of BChE and the Ki values of benactyzine and drofenine were calculated to be 0.010 +/- 0.001 and 0.003 +/- 0.000 mM, respectively, using the Systat (version 5.03, 1991) nonlinear regression analysis software package. According to these parameters, drofenine is a more potent competitive inhibitor of BChE than benactyzine.


Assuntos
Benactizina/farmacologia , Butirilcolinesterase/sangue , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Fenilacetatos/farmacologia , Ligação Competitiva , Humanos , Cinética , Modelos Lineares , Modelos Químicos , Ligação Proteica , Conformação Proteica
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