Subjective benign paroxysmal positional vertigo in patients with osteoporosis or migraine / Vertigem posicional paroxística benigna subjetiva em pacientes com osteoporose ou migrânea

Abstract Introduction Subjective benign paroxysmal positional vertigo is a form of benign paroxysmal positional vertigo in which during the diagnostic positional maneuvers patients only present vertigo symptoms with no nystagmus. Objective To study the characteristics of subjects with subjective benign paroxysmal positional vertigo. Methods Prospective multicenter case-control study. All patients presenting with vertigo in the Dix-Hallpike test that presented to the participating hospitals were included. The patients were separated into two groups depending on whether nystagmus was present or not. An Epley Maneuver of the affected side was performed. In the follow-up visit, patients were checked to see if nystagmus and vertigo were present. Both groups of patients were compared to assess the success rate of the Epley maneuver and also to compare the presence of 19 variables. Results 259 patients were recruited, of which 64 belonged to the subjective group. Nystagmus was eliminated in 67.2% of the patients with benign paroxysmal positional vertigo. 89.1% of the patients with subjective benign paroxysmal positional vertigo remained unaffected by nystagmus, thus showing a significant difference (p = 0.001). Osteoporosis and migraine were the variables which reached the closest to the significance level. In those patients who were taking vestibular suppressors, the percentage of subjective benign paroxysmal positional vertigo was not significantly higher. Conclusions Subjective benign paroxysmal positional vertigo should be treated using the Epley maneuver. More studies are needed to establish a relationship between osteoporosis, migraine and subjective benign paroxysmal positional vertigo. The use of vestibular suppressants does not affect the detection of nystagmus.

Resumo Introdução A vertigem posicional paroxística benigna subjetiva é um tipo de vertigem posicional paroxística benigna na qual, durante as manobras posicionais diagnósticas, os pacientes apresentam apenas sintomas vertiginosos sem nistagmo. Objetivo Estudar as características de indivíduos com vertigem posicional paroxística benigna subjetiva. Método Estudo prospectivo multicêntrico de caso-controle. Foram incluídos todos os pacientes com vertigem no teste de Dix-Hallpike, que se apresentaram nos hospitais participantes. Os pacientes foram separados em dois grupos, dependeu da presença ou não do nistagmo. Uma manobra de Epley foi realizada no lado afetado. Na consulta de seguimento, os pacientes foram avaliados para verificar a presença ou não do nistagmo e da vertigem. Ambos os grupos de pacientes foram comparados para avaliar a taxa de sucesso da manobra de Epley e também para comparar a presença de 19 variáveis. Resultados Foram recrutados 259 pacientes, dos quais 64 pertenciam ao grupo subjetivo. O nistagmo foi eliminado em 67,2% dos pacientes com vertigem posicional paroxística benigna. Em 89,1% dos casos, os pacientes com vertigem posicional paroxística benigna subjetiva mantiveram-se não afetados pelo nistagmo, mostraram uma diferença significativa (p = 0,001). Osteoporose e enxaqueca foram as variáveis que atingiram o nível mais próximo ao de significância. Nos pacientes que tomavam supressores vestibulares, a porcentagem de vertigem posicional paroxística benigna subjetiva não foi significativamente maior. Conclusões A vertigem posicional paroxística benigna subjetiva deve ser tratada com a manobra de Epley. Mais estudos são necessários para estabelecer uma relação entre osteoporose, enxaqueca e vertigem posicional paroxística benigna subjetiva. O uso de supressores vestibulares não afeta a detecção do nistagmo.

Effects of Amisulpride Adjunctive Therapy on Working Memory and Brain Metabolism in the Frontal Cortex of Patients with Schizophrenia: A Preliminary Positron Emission Tomography/Computerized Tomography Investigation

OBJECTIVE: Dopamine plays a significant role in working memory by acting as a key neuromodulator between brain networks. Additionally, treatment of patients with schizophrenia using amisulpride, a pure dopamine class 2/3 receptor antagonist, improves their clinical symptoms with fewer side effects. We hypothesized that patients with schizophrenia treated with amisulpride and aripiprazole show increased working memory and glucose metabolism compared with those treated with cognitive behavioral therapy (CBT) and aripiprazole instead. METHODS: Sixteen patients with schizophrenia (eight in the amisulpride group [aripiprazole+amisulpride] and eight in the CBT group [aripiprazole+CBT]) and 15 age- and sex-matched healthy control subjects were recruited for a 12-week-long prospective trial. An [18F]-fluorodeoxyglucose-positron emission tomography/computerized tomography scanner was used to acquire the images. RESULTS: After 12 weeks of treatment, the amisulpride group showed greater improvement in the Letter-Number Span scores than the CBT group. Additionally, although brain metabolism in the left middle frontal gyrus, left occipital lingual gyrus, and right inferior parietal lobe was increased in all patients with schizophrenia, the amisulpride group exhibited a greater increase in metabolism in both the right superior frontal gyrus and right frontal precentral gyrus than the CBT group. CONCLUSION: This study suggests that a small dose of amisulpride improves the general psychopathology, working memory performance, and brain glucose metabolism of patients with schizophrenia treated with aripiprazole.

Aripiprazole for drug-induced sexual dysfunction in schizophrenic males / 中华男科学杂志

Objective@#To investigate the clinical effects of aripiprazole on sexual dysfunction induced by amisulpride or risperidone in male patients with schizophrenia.@*METHODS@#This study included 75 male patients with drug-induced secondary sexual dysfunction after treated with amisulpride or risperidone for first-episode schizophrenia between October 2014 and October 2016. We substituted aripiprazole for amisulpride or risperidone, gradually increased the dose from 10 to 30 mg/d within 2 weeks, and maintained 30 mg/d from the 3rd week. At 4 and 8 weeks after medication, we evaluated the sexual function of the patients, measured the levels of serum prolactin (PRL) and testosterone (T), obtained the scores of the Positive and Negative Symptoms Scale (PANSS), recorded adverse reactions, and compared the parameters with those before aripiprazole administration.@*RESULTS@#Compared with pre-aripiprazole administration, the patients showed significant increases after 4 weeks of medication in the sexual function score (24.3 ± 2.1 vs 32.6 ± 3.6, P 0.05). In comparison with pre-aripiprazole administration, the PANSS score was significantly decreased at 4 weeks after medication (62.1 ± 4.9 vs 57.2 ± 5.5, P <0.05) and even lower at 8 weeks (51.2 ± 5.2) (P <0.05). The incidence rates of medication-related excitation, dizziness, insomnia, and loss of appetite were 6.7%, 5.3%, 4.0% and 1.3% respectively, and no other serious adverse reactions were observed.@*CONCLUSIONS@#Aripiprazole is effective for the treatment of drug-induced sexual dysfunction in schizophrenic men by continuously alleviating their positive and negative symptoms and meanwhile improving their sexual function and restoring their sexual hormone levels.

A Study on Discontinuation Rate on Maintenance Treatment of Antipsychotic Agents in Schizophrenic Patients / 대한정신분열병학회지

OBJECTIVES: Relapse prevention is a major therapeutic goal in the treatment of schizophrenia. However, many patients experience multiple functional impairments and treatment resistance due to recurrence. This study was designed to investigate the follow-up of patients with using antipsychotic drugs and to compare the total treatment failure rate, withdrawal reasons, and duration period of antipsychotic drugs. METHODS: The subjects were 1963 patients who taking antipsychotic drugs under the diagnosis of schizophrenia. We selected 1836 patients using 10 antipsychotic drugs according to frequency of using. The rate of total treatment failure of them was divided into 6-month, 1-year, 2-year, 3-year, and 5-year according to the time of drug withdrawal. We compared the total treatment failure rate at 1 and 3-year between 10 antipsychotic drugs. RESULTS: The total treatment failure rate of clozapine was lowest compared with the other 9 antipsychotic drugs in all the surveyed periods. When evaluating actual number of subjects, olanzapine, sulpiride, risperidone, aripiprazole, amisulpride, and haloperidol were lower significantly compared with ziprasidone at 1-year in the total treatment failure rate, but there was no significant difference between them except clozapine at 3-year. The results of the analysis based on the number of prescriptions showed that the total treatment failure rate of the atypical antipsychotic drug was lower than that of the typical antipsychotic drug at 1-year, but the difference was decreased over time except quetiapine and ziprasidone. CONCLUSION: In conclusion, although there is some controversy about which drug to prescribe to the patient, the clinician needs a proper prescription considering various factors such as efficacy, side effects, price, and formulations of each drug.

A Study on Discontinuation Rate on Maintenance Treatment of Antipsychotic Agents in Schizophrenic Patients / 대한정신분열병학회지

OBJECTIVES: Relapse prevention is a major therapeutic goal in the treatment of schizophrenia. However, many patients experience multiple functional impairments and treatment resistance due to recurrence. This study was designed to investigate the follow-up of patients with using antipsychotic drugs and to compare the total treatment failure rate, withdrawal reasons, and duration period of antipsychotic drugs. METHODS: The subjects were 1963 patients who taking antipsychotic drugs under the diagnosis of schizophrenia. We selected 1836 patients using 10 antipsychotic drugs according to frequency of using. The rate of total treatment failure of them was divided into 6-month, 1-year, 2-year, 3-year, and 5-year according to the time of drug withdrawal. We compared the total treatment failure rate at 1 and 3-year between 10 antipsychotic drugs. RESULTS: The total treatment failure rate of clozapine was lowest compared with the other 9 antipsychotic drugs in all the surveyed periods. When evaluating actual number of subjects, olanzapine, sulpiride, risperidone, aripiprazole, amisulpride, and haloperidol were lower significantly compared with ziprasidone at 1-year in the total treatment failure rate, but there was no significant difference between them except clozapine at 3-year. The results of the analysis based on the number of prescriptions showed that the total treatment failure rate of the atypical antipsychotic drug was lower than that of the typical antipsychotic drug at 1-year, but the difference was decreased over time except quetiapine and ziprasidone. CONCLUSION: In conclusion, although there is some controversy about which drug to prescribe to the patient, the clinician needs a proper prescription considering various factors such as efficacy, side effects, price, and formulations of each drug.

Galactocele medicamentosa pós-mamoplastia de aumento: relato de caso e revisão da literatura / Galactocele due to drugs prescribed after augmentation mammoplasty: a case report and literature review

A mamoplastia de aumento é um procedimento cirúrgico muito comum e seguro na cirurgia plástica, mas o mesmo não está isento de complicações. A galactocele após mamoplastia de aumento é raramente descrita na literatura. Este relato de caso refere-se a uma paciente de 34 anos de idade, que fazia uso de sulpirida há 2 anos e 4 meses e desenvolveu galactocele cerca de 100 dias após mamoplastia de aumento. O diagnóstico deve ser suspeitado quando se observar uma mama aumentada de volume, associada a calor local, dor ou desconforto mamário no pós-operatório. Acredita-se que a melhor conduta seja a drenagem cirúrgica, a fim de confirmar o diagnóstico de galactocele e excluir a presença de abscesso mamário.

Augmentation mammaplasty is a common and safe plastic surgery procedure, but it is not free from complications. Galactocele after augmentation mammaplasty is rarely described in the literature. We discuss the case of a 34-year-old woman who had been taking sulpiride for 2 years and 4 months and developed galactocele approximately 100 days after augmentation mammaplasty. However, diagnosis should be suspected if breast size increases and it is associated with postoperative local heat, pain or breast discomfort. We believe that the surgeon must surgically drain galactocele to confirm diagnosis, especially to exclude the presence of breast abscess.

Pharmacological Treatments for Tinnitus / 한양의대학술지

Pharmacotherapy has been constantly chosen by the clinician among the available treatment options for tinnitus. Medications that have been prescribed off-label to treat tinnitus can be grouped into several categories: benzodiazepines, antidepressants, anticonvulsants, N-methyl-D-aspartate (NMDA) receptor antagonists, dopamine receptor modulators, muscle relaxants, and others. In this article, a wide variety of compounds once used in the treatment of tinnitus and evidenced by clinical trials are reviewed with respect to the mechanisms of action and the drug efficacy. Only a few of the various pharmacological interventions investigated have some beneficial effects against tinnitus: clonazepam, acamprosate, neramexan, and sulpiride. Sertraline and pramipexole were effective in subgroups of patients with psychiatric symptoms or presbycusis. However, no agents have been identified to provide a reproducible long-term reduction of tinnitus in excess of placebo effects. In rodent tinnitus models, L-baclofen, memantine, and KCNQ2/3 channel activators have been demonstrated to reduce tinnitus development. Limitation of the use of an effective high dosage during a longer treatment duration due to dose-dependent side effects of the centrally acting drugs may influence the results in clinical studies. More effective and safer innovative agents should be developed based on the further understanding of tinnitus neural mechanisms and valid animal models, and should be supported by improved clinical trial methodology. The management of tinnitus patients through a tailored treatment approach depending on the detailed classification of tinnitus subtypes will also lead to better treatment outcomes.

The Role of Spinal Dopaminergic Transmission in the Analgesic Effect of Nefopam on Rat Inflammatory Pain

BACKGROUND: Nefopam has been known as an inhibitor of the reuptake of monoamines, and the noradrenergic and/or serotonergic system has been focused on as a mechanism of its analgesic action. Here we investigated the role of the spinal dopaminergic neurotransmission in the antinociceptive effect of nefopam administered intravenously or intrathecally. METHODS: The effects of intravenously and intrathecally administered nefopam were examined using the rat formalin test. Then we performed a microdialysis study to confirm the change of extracellular dopamine concentration in the spinal dorsal horn by nefopam. To determine whether the changes of dopamine level are associated with the nefopam analgesia, its mechanism was investigated pharmacologically via pretreatment with sulpiride, a dopaminergic D2 receptor antagonist. RESULTS: When nefopam was administered intravenously the flinching responses in phase I of the formalin test were decreased, but not those in phase II of the formalin test were decreased. Intrathecally injected nefopam reduced the flinching responses in both phases of the formalin test in a dose dependent manner. Microdialysis study revealed a significant increase of the level of dopamine in the spinal cord by intrathecally administered nefopam (about 3.8 fold the baseline value) but not by that administered intravenously. The analgesic effects of intrathecally injected nefopam were not affected by pretreatment with sulpiride, and neither were those of the intravenous nefopam. CONCLUSIONS: Both the intravenously and intrathecally administered nefopam effectively relieved inflammatory pain in rats. Nefopam may act as an inhibitor of dopamine reuptake when delivered into the spinal cord. However, the analgesic mechanism of nefopam may not involve the dopaminergic transmission at the spinal level.

Evaluation of the pressure ulcers risk scales with critically ill patients: a prospective cohort study / Avaliação das escalas de risco para úlcera por pressão em pacientes críticos: uma coorte prospectiva / Evaluación de las escalas de riesgo para úlcera por presión en pacientes críticos: una cohorte prospectiva

AIMS: to evaluate the accuracy of the Braden and Waterlow risk assessment scales in critically ill inpatients. METHOD: this prospective cohort study, with 55 patients in intensive care units, was performed through evaluation of sociodemographic and clinical variables, through the application of the scales (Braden and Waterlow) upon admission and every 48 hours; and through the evaluation and classification of the ulcers into categories. RESULTS: the pressure ulcer incidence was 30.9%, with the Braden and Waterlow scales presenting high sensitivity (41% and 71%) and low specificity (21% and 47%) respectively in the three evaluations. The cut off scores found in the first, second and third evaluations were 12, 12 and 11 in the Braden scale, and 16, 15 and 14 in the Waterlow scale. CONCLUSION: the Braden scale was shown to be a good screening instrument, and the Waterlow scale proved to have better predictive power. .

OBJETIVOS: avaliar a acurácia das escalas de avaliação de risco de Braden e de Waterlow, em pacientes críticos internados. MÉTODO: trata-se de uma coorte prospectiva, com 55 pacientes nas unidades intensivas, por meio de avaliação de variáveis sociodemográficas e clínicas, de aplicação das escalas (Waterlow e Braden), na admissão e a cada 48 horas, da avaliação e classificação das úlceras em categorias. RESULTADOS: a incidência de úlcera por pressão foi de 30,9%, as escalas de Braden e de Waterlow apresentaram, nas três avaliações, alta sensibilidade (41% e 71 %) e baixa especificidade (21% e 47%), respectivamente. Os escores de coorte encontrados na primeira, segunda e terceira avaliações foram de 12, 12 e 11, na escala de Braden, e de 16, 15 e 14 na escala de Waterlow. CONCLUSÃO: a escala de Braden apresentou-se como bom instrumento de triagem, e a de Waterlow com melhor poder preditivo. .

OBJETIVOS: evaluar la precisión de las escalas de evaluación de riesgo de Braden y de Waterlow en pacientes críticos internados. MÉTODO: se trata de una cohorte prospectiva, con 55 pacientes en las unidades intensivas, por medio de evaluación de variables sociodemográficas y clínicas, de aplicación de las escalas (Waterlow y Braden) en la admisión y a cada 48 horas; de la evaluación y clasificación de las úlceras en categorías. RESULTADOS: la incidencia de úlcera por presión fue de 30,9%, las escalas, de Braden y de Waterlow, presentaron, en las tres evaluaciones, alta sensibilidad (41% y 71 %) y baja especificidad (21% y 47%), respectivamente. Los puntajes de corte encontrados en la primera, en la segunda y en la tercera evaluación fueron de 12, 12 y 11, en la escala de Braden, y de 16, 15 y 14, escala de Waterlow. CONCLUSIÓN: la escala de Braden se presentó como un buen instrumento de detección, y la de Waterlow con mejor poder de predicción. .

Effect of noise and crowding related stress on serum level of cortisol ACTH, epinephrine and insulin in female albino rats

Noise and crowding are the most stressful factors for human beings.Study aimed to clarify their effect on cortisol, ACTH, epinephrine, insulin and the amelioration effectof Sulpiride. Thirty six female rats were divided into six groups [6/each]:1- Rats served as control, 2- Rats treated with Sulpiride drug, 3- Rats exposed to noise [90db, 3hr. perday] for 45 days. 4- Rats exposed to noise and treated with sulpiride drug, 5- Rats exposed tocrowding. 6- Rats exposed to noise and treated with Sulpiride drug. Noise and crowding stresses caused a significant increase of cortisol, ACTH and epinephrinewhile there was a significant decrease in insulin hormone. Sulpiride drug ameliorated theseparameters. it is useful to use Sulpiride drug with people who are exposing to noise and crowdingstress

Effect of crowding stress on lung and heart of the adult albino rats and the possible protective role of sulpiride

Exposure to crowding stress is associated with increased respiratory system morbidity, However, the underlying mechanisms are unclear. Thus, there is a need for more study of this harmful effect. Sulpiride had been shown to have a protective role against crowding stress on other systems but this role was not studied well on the respiratory and cardiovascular systems. Investigating the possible harmful effects of crowding on adult albino rats' lung and heart and the possible protective role of combined sulpiride treatment. The present study was carried out on 24 adult albino rats of local strain weighing 120 +/- 3 g which were randomly divided equally into Group 1[C, untreated negative control], Group 2 [Cr, crowding exposed or positive control] where rats were exposed to crowding in a cage [20x20x20 cm- 6 rats /cage] for 1 month, Group 3[D, sulpiride-treated] where the rats were exposed to sulpiride "0.028 mg/B.W./day" and Group 4 [Cr+D, crowding + sulpiride-treated]. Paraffin sections were prepared for histological, histochemical and morphometric studies. The data were statistically analysed. The rats exposed to crowding only or sulpiride only showed highly significant damaging changes on lung such as thickening in the interalveolar septa and obliteration of the alveoli, inflammatory cells infiltration within the pulmonary interstitium, peribronchiolar infiltration and fibrosis, thickening of the pulmonary blood vessels walls, interstitial collagen fibres deposition and apoptotic cellular changes. On the level of heart, significant decrease in the diameters of the myocardial muscle fibres with focal areas of necrosis, apoptotic changes and increased collagen fibres deposition was marked in sulpiride group. When crowding and sulpiride treatments were combined, the damaging effects were maximized on the lung and heart. These results provided evidence that crowding stress causes obvious lung and heart tissue damages. No protective role for sulpiride was proofed. This is because using sulpiride alone or in combination with crowding showed marked damaging effects on the lung and heart tissues

Effect of noise and crowding stresses on hypothalamic-pituitary-gonadal axis and protective effect of sulpiride drug in adult female albino rats

Noise and crowding are the most stressful factors which cause depressant effects on human beings, especially females.Therfore this study was aimed at clarifying their effects on hypothalamus pituitary gonadal axis hormones [luteinizing hormone [LH] and follicle-stimulating hormone [FSH], estrogen [E2]and progesterone as well as prolactin [PRL]and the possible protective effect of antidepressant drug;sulpiride. Sixty adult female rats were divided into six groups [10/each]: 1- Rats served as control, 2- Rats treated with sulpiride drug only, 3- Rats exposed to noise [90db, 3hr. per day] for 45 days, 4- Rats exposed to noise and treated with sulpiride drug, 5- Rats exposed to crowding and 6- Rats exposed to crowding and treated with sulpiride drug. Results: Noise and crowding stresses caused a significant decrease of estrogen [E2], progesterone [P], LH and FSH levels and high significant increase in PRL level. Sulpiride drug ameliorated these parameters changes except PRL level which showed a high significant level compared to control group. It is useful to use antidepressant drug [e.g. sulpiride] with people who are exposing to noise and crowding stress

Recent Trends of Antipsychotics Polypharmacy in Schizophrenia / 대한정신약물학회지

Antipsychotics polypharmacy is a common practice in clinical settings despite the opposition of most guidelines for treatment of schizophrenia. This article reviews the evidence of antipsychotics polypharmacy and summarizes advantages and disadvantages shown in clinical trials. Clinicians choose antipsychotics polypharmacy to control the positive and negative symptoms more effectively especially in treatment resistant patients or to reduce adverse effects. There are some theoretical possibilities that antipsychotics polypharmacy affects a broader range of receptors, enhances D2-receptor blockade and optimizes pharmacokinetic effects. Clinical evidence suggests that clozapine co-administered with risperidone, sulpiride, or amisulpride reduces psychotic symptoms in treatment-resistant patients and that aripiprazole with other antipsychotics reduces metabolic side effects. On the other hand, antipsychotics polypharmacy is associated with problems such as dose-dependent side effects, metabolic problems, increased mortality and treatment cost. Considering pros and cons, antipsychotics polypharmacy must be started after close scrutiny of the patient's medication history not just by clinical judgment. Also, changing the regimen from polypharmacy to monotherapy should be considered as a reasonable option to schizophrenic patients in stationary status.

Trends in Scientific Literature on Atypical Antipsychotics in South Korea: A Bibliometric Study

OBJECTIVE: We have carried out a bibliometric study on the scientific publications in relation to atypical or second-generation antipsychotic drugs (SGAs) in South Korea. METHODS: With the EMBASE and MEDLINE databases, we selected those publications made in South Korea whose title included the descriptors atypic* (atypical*) antipsychotic*, second-generation antipsychotic*, clozapine, risperidone, olanzapine, ziprasidone, quetiapine, sertindole, aripiprazole, paliperidone, amisulpride, zotepine, asenapine, iloperidone, lurasidone, perospirone and blonanserin. We applied some bibliometric indicators of paper production and dispersion with Price's law and Bradford's law, respectively. We also calculated the participation index (PI) of the different countries, and correlated the bibliometric data with some social and health data from Korea (such as total per capita expenditure on health and gross domestic expenditure on research and development). RESULTS: We collected 326 original papers published between 1993 and 2011. Our results state fulfilment of fulfilled Price's law, with scientific production on SGAs showing exponential growth (correlation coefficient r=0.8978, as against an r=0.8149 after linear adjustment). The most widely studied drugs were risperidone (91 papers), aripiprazole (77), olanzapine (53), and clozapine (43). Division into Bradford zones yielded a nucleus occupied by the Progress in Neuro-Psychopharmacology and Biological Psychiatry (36 articles). A total of 86 different journals were published, with 4 of the first 10 used journals having an impact factor being greater than 4. CONCLUSION: The publications on SGAs in South Korea have undergone exponential growth over the studied period, without evidence of reaching a saturation point.

Effect of storax on concentration of sulpiride in brain and blood by MD-HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the effect of traditional Chinese medicine storax on the concentration of combined western medicine sulpiride in brain and blood, discuss the effect of storax in inducing resuscitation and increasing the permeability of the gastrointestinal barrier (GB) and the blood-brain-barrier (BBB), and explore the interaction between storax and sulpiride.</p><p><b>METHOD</b>Rats were orally administered with the drugs for one week, probes were implanted in their brains and necks by surgery. After balance for 60 min, brain microdialysis and blood microdialysis were adopted for collect dislysates from blood in right atrum and cerebral hippocampus at time periods of 30, 60, 90, 120, 150, 180 min. The concentration of sulpirde in the samples was detected by RP-HPLC. Statistical approaches were adopted to compare the contents of sulpirde in brain and blood of the two groups.</p><p><b>RESULT</b>The sulpiride combined with storax group showed a significant higher concentration of sulpiride than the pure sulpiride group. The pure sulpiride group showed a concentration ratio between sulpiride in brain and blood of 1:0.2; while the sulpiride combined with storax group increased the concentration ratio between sulpiride in brain and blood to 1:0.3. Compared with the pure sulpiride group, the sulpiride combined with storax group showed an increase of concentration by 39% in brain and 69% in blood.</p><p><b>CONCLUSION</b>Storax can notably increase the concentration of sulpiride in rat brain and blood, indicating that it can increase the permeation of sulpiride through gastrointestinal barrier and BBB. This study reveals the mechanism of storax in inducing resuscitation by promoting the permeation through gastrointestinal barrier and BBB.</p>

A Case of Amisulpride Induced Tardive Blepharospasm in Schizophrenia / 대한정신약물학회지

Tardive blepharospam is characterized by repetitive, forceful, and sustained involuntary contractions of the orbicularis oculi. We report here one case of neuroleptic-induced tardive blepharospasm that developed during high-dose amisulpride treatment and was treated with clozapine. The patient was a 29-year-old man with a 6-year history of schizophrenia. After 33 months of amisulpride treatment (1200 mg/day), involuntary eye-blinking had developed. Following exclusion of all other possible etiopathological causes of the blepharospasm, we decided to switch the drug treatment from amisulpride to clozapine. On the fourteenth day of clozapine (250 mg/day) treatment, we observed significant improvements in eye-blinking and psychotic symptoms. Four months later, the eye-blinking had remitted completely. We suggest that amisulpride may cause blepharospasm and lead to an impaired ability to perform daily activities. Therefore, we recommend that clinicians regularly monitor involuntary movements in patients receiving antipsychotic treatment, especially when high doses of amisulpride are involved.

Antipsychotic-Induced Sexual Dysfunction and Its Management

Sexual dysfunction is a common condition in patients taking antipsychotics, and is the most bothersome symptom and adverse drug effect, resulting in a negative effect on treatment compliance. It is known that hyperprolactinemia is a major cause of sexual dysfunction. Based on the blockade of dopamine D2 receptors, haloperidol, risperidone, and amisulpride are classed as prolactin-elevating antipsychotics, while olanzapine, clozapine, quetiapine, ziprasidone, and aripiprazole are classed as prolactin-sparing drugs. Risperidone and the other typical antipsychotics are associated with a high rate of sexual dysfunction as compared to olanzapine, clozapine, quetiapine, and aripiprazole. With regard to treatment in patients suffering from sexual dysfunction, sildenafil was associated with significantly more erections sufficient for penetration as compared to a placebo. Subsequent studies are needed in order to provide physicians with a better understanding of this problem, thereby leading toward efficacious and safe solutions.

Gap Junction Contributions to the Goldfish Electroretinogram at the Photopic Illumination Level

Understanding how the b-wave of the electroretinogram (ERG) is generated by full-field light stimulation is still a challenge in visual neuroscience. To understand more about the origin of the b-wave, we studied the contributions of gap junctions to the ERG b-wave. Many types of retinal neurons are connected to similar and different neighboring neurons through gap junctions. The photopic (cone-dominated) ERG, stimulated by a small light beam, was recorded from goldfish (Carassius auratus) using a corneal electrode. Data were obtained before and after intravitreal injection of agents into the eye under a photopic illumination level. Several agents were used to affect gap junctions, such as dopamine D1 and D2 receptor agonists and antagonists, a nitric oxide (NO) donor, a nitric oxide synthase (NOS) inhibitor, the gap junction blocker meclofenamic acid (MFA), and mixtures of these agents. The ERG b-waves, which were enhanced by MFA, sodium nitroprusside (SNP), SKF 38393, and sulpiride, remained following application of a further injection of a mixture with MFA. The ERG b-waves decreased following NG-nitro-L-arginine methyl ester (L-NAME), SCH 23390, and quinpirole administration but were enhanced by further injection of a mixture with MFA. These results indicate that gap junction activity influences b-waves of the ERG related to NO and dopamine actions.

[Evaluation of sperm quality, maturation and DNA integrity in adult mice treated with sulpiride]

Use of certain antipsychotic drugs has severe effects on fertility in males. Hypothalamus and hypophysial impressions and changes in plasma hormones concentration like prolactin, LH and FSH can affect sperm production. In this study, we investigated the effects of sulpiride on sperm quality, maturation and DNA damage. Twenty for adult male mice [age: 6-8 weeks] were divided into three groups. The treatment group received 40 mg/kg sulpiride solution and the control sham group was given carrier of the drug intraperitoneally [IP] daily for 45 days but the control group received nothing. Finally, all the mice were sacrificed by cervical dislocation and their cauda epididymis were removed surgically. The excised specimens were placed in 1 ml HTF medium and incubated for 30 min in CO2 incubator to allow the spermatozoa to swim out. Later, sperm count, motility and viability were analyzed. Additionally, sperm chromatin quality and DNA integrity were assessed by aniline blue and acridine orange staining. Significant decrease in sperm motility and count were observed in the treatment group while the number of abnormal sperm increased as compared with the other two groups. Sperm viability and DNA maturation showed significant reduction and the rate of DNA damage increased in comparison with the control sham and the control groups [P<0.05]. The study showed that sulpiride has negative effects on sperm parameters in treated animals and in some cases it could cause secondary infertility

Estudo da interação de antipsicóticos atípicos e albumina sérica com base em modelos matemáticos e espectrofluorimétricos / Study of the interaction of atypical antipsychotics and serum albumin based on mathematical and spectrofluorimetric models

Os antipsicóticos são drogas utilizadas no tratamento de muitos transtornos psiquiátricos, sendo classificados em dois grupos: típicos e atípicos. Os típicos formam o grupo de drogas que bloqueiam especialmente os receptores de dopamina e, por isto, causam efeitos colaterais característicos, que se manifestam através de sintomas extrapiramidais e podem terminar em discinesia tardia. Os atípicos apresentam eficácia antipsicótica similar à dos antipsicóticos típicos, mas produzem menos efeitos colaterais extrapiramidais e não causam discinesia tardia. Os antipsicóticos se ligam às proteínas plasmáticas, principalmente a albumina, a qual representa cerca de 60% do total das proteínas no soro humano. Neste trabalho estudamos os processos de interação de duas drogas antipsicóticas atípicas, risperidona e sulpirida, com as albuminas séricas humana (HSA) e bovina (BSA), através da técnica de supressão da fluorescência intrínseca do triptofano. A partir dos espectros de fluorescência, a análise dos dados foi feita obtendo-se os gráficos e as constantes de Stern-Volmer. A análise da supressão da fluorescência foi feita a partir da média aritmética dos dados oriundos dos experimentos realizados em cada condição adotada. Como a molécula da sulpirida é fluorescente desenvolvemos uma modelagem matemática do processo de interação, que nos permitiu então obter os dados referentes à supressão da fluorescência da proteína. Os resultados mostraram que a risperidona e a sulpirida suprimem a fluorescência de ambas albuminas por um processo de quenching estático, formando complexos droga-albumina. A risperidona tem uma afinidade com a HSA cerca de 6,5 vezes maior do que a sulpirida, a 37 oC. As constantes de associação calculadas para a interação risperidona-HSA, através da Teoria de Stern-Volmer, foram 1,43 (± 0,05) x 105 M-1, a 37 °C, e 2,56 (± 0,09) x 105 M-1, a 25 ºC1; e para a sulpirida, 2,20 (± 0,08) x 104 M-1, a 37 ºC, e 5,46 (± 0,20) x 104 M-1, a 25 ºC...

Antipsychotics are drugs used to treat many psychiatric disorders. They are classified into two groups: typical and atypical. The typical group act blocking dopamine receptors in particular and it causes characteristic side effects with extrapyramidal symptoms, and can lead to tardive dyskinesia. The atypical group presents similar efficacy to typical group, but they produce less extrapyramidal side effects and does not cause tardive dyskinesia. Antipsychotics bind to plasmatic proteins, mainly to albumin, which represents about 60% of total human serum proteins. In this study we studied the interactions of two atypical antipsychotic drugs, risperidone and sulpiride, with human serum albumin (HSA) and bovine (BSA) through the technique of intrinsic tryptophan fluorescence quenching. From the fluorescence spectra, a data analysis was made to obtain Stern-Volmer plots and constants. Quenching analysis was performed used from using arithmetic means of data from experiments for each adopted condition. As sulpiride molecule is fluorescent, a mathematical modeling for interaction process was made. It allows us then to obtain the data referents to fluorescence quenching of protein. Results showed that risperidone and sulpiride quench the fluorescence for both albumins by static quenching process, forming complexes drug-albumin. The risperidone affinity to HSA is about 6.5 higher than supiride, at 37 oC. Stern-Volmer constants for interaction risperidone-HSA were 1.43 (± 0.05) x 105 M-1, at 37oC, and 2.56 (± 0.09) x 105 M-1, at 25 oC; and for sulpiride were 2.20 (± 0.08) x 104 M-1, at 37 oC, and 5.46 (± 0.20) x 104 M-1, at 25 oC. As the quenching ratio for BSA was higher than HAS, we suggested that the primary site for risperidone on albumin is closer of the domain of trypthophan 134 of BSA than the domain of trypthophan 212 of HAS. The same is suggested for the primary site of supiride at 37oC.