Estudio comparativo de la calidad biofarmacéutica de Alprazolam 0, 5 mg comercializadas en el mercado peruano / Comparative study of the biopharmaceutical quality of Alprazolam 0. 5 mg commercialized in the Peruvian market

El Alprazolam pertenece a las benzodiazepinas. Sus efectos se atribuyen a que actúa sobre receptores de membrana específicos, lo cual facilita la acción inhibitoria presináptica y postsináptica del ácido γ-aminobutírico (GABA), especialmente en la formación reticular ascendente. Se utiliza para el tratamiento de los estados de ansiedad, crisis de angustia, ataques de pánico y estrés intenso. Este estudio se realizó para analizar los parámetros comparativos de control de calidad in vitro mediante la evaluación de la variación de peso, friabilidad, dureza, tiempo de desintegración, perfil y eficiencia de disolución entre el medicamento innovador (Xanax®) y multifuentes que son comercializados en el mercado peruano. Para realizarlo, se seleccionaron tabletas de Alprazolam 0,5 mg multifuente de diferentes laboratorios comparándolos con el medicamento innovador y se evaluaron las características fisicoquímicas y biofarmacéuticas. Los ensayos farmacopeicos se evaluaron según lo establecido en la USP 42. Los resultados de las pruebas fisicoquímicas indicaron que las muestras analizadas no tenían diferencia significativa y estaban dentro de lo establecido en la farmacopea, así mismo el perfil y eficiencia de disolución permitieron establecer que el comportamiento biofarmacéutico de las mismas era muy similar para ambos tipos de molécula. Se estableció que las tabletas multifuentes de Alprazolam 0,5 mg de esta investigación son bioequivalentes con el innovador, por lo que permite proponer a la comunidad científica la determinación de la equivalencia biofarmacéutica como elemento de apoyo en la toma de decisiones de compra en el servicio farmacéutico

Alprazolam belongs to benzodiazepines. Its effects are attributed to the fact that it acts on specific membrane receptors, which facilitates the presynaptic and postsynaptic inhibitory action of γ-aminobutyric acid (GABA), especially in the ascending reticular formation. It is used to treat anxiety states, panic attacks, and intense stress. This study was carried out to analyze comparative parameters of in vitro quality control by evaluating the variation in weight, friability, hardness, disintegration time, profile and dissolution efficiency between the innovative drug (Xanax®) and multi-sources tablets that are marketed in the Peruvian market. To perform this, Alprazolam 0.5 mg multi-source tablets were selected from different laboratories comparing them with the innovative medicine and the physicochemical and biopharmaceutical characteristics were evaluated. Pharmacopoeial trials were evaluated as established in USP 42. The results of physicochemical tests indicated that analyzed samples did not have a significant difference and were within the established in the pharmacopoeia, as well as the profile and dissolution efficiency allowed to establish that their biopharmaceutical behavior was very similar for both types of molecules. It was established that Alprazolam 0.5 mg multi-source tablets from this research are bioequivalent with innovator, which makes it possible to propose to scientific community determination of biopharmaceutical equivalency as a support element in decision-making process for purchasing services pharmacist

Anti-stress activity of Ocimum sanctum and alprazolam in animal models

Background: Stress is the physiological, psychological and behavioral response by individuals when they perceive a lack of equilibrium between the demands placed upon them and their ability to meet those demands, which over a period of time leads to ill health. There are several ways of coping with stress. Some techniques of time management may help a person to control stress.Methods: Forced swim test- mice were randomized into two groups according to the body weights. Each group contains six animals. Each individual animal was allowed to swim inside the jar (25-12-25 cm) containing fresh water up to 15 cm height. Mice were allowed swim for 6 min. After initial struggle to escape the animal became immobile. Total immobility period was measured. Rotarod test- mice were randomized into two groups according to body weights. Each group contains six animals. Rats were placed on the lanes. Latency period was recorded at which each rat falls off the rod.Results: In first experiment, anti-stress activity of Ocimum sanctum in mice was demonstrated by measuring the immobility period during forced swim test and in the second experiment the measurement of the latency period of rats in rotarod apparatus was performed. Both the experimental procedures were compared with standard anti stress drug alprazolam.Conclusions: The present study suggests that Ocimum sanctum possess significant anti stress activity but less when compared to alprazolam.

Effects Of Oral Lorazepam Versus Oral Alprazolam On The Postoperative Cognitive Function

Objectives: To compare the effect of oral Lorazepam 1 mg or oral alprazolam 0.5 mg given at night before surgery on cognitive function in patients undergoing elective general surgery receiving general anaesthesia. Methodology: In a prospective double-blind manner 128 patients aged 30 to 50 years belonging to ASA I and II scheduled for elective surgery under general anaesthesia were randomly divided into two equal groups. Group A (n=64) received oral lorazepam 1 mg and Group B (n=64) received oral alprazolam 0.5 mg). Cognitive function were assessed by 1. Rey’s Auditory Verbal Learning test, (RAVLT) test to assess the ability to form new verbal memory, 2. Trail Making Test (TMT) part A to assess psychomotor ability and 3. Digit Span Test to assess short term verbal memory. These were assessed thrice: 1) during preoperative assessment, 2) 30 minutes before induction and 3) 30 minutes after reversal of general anaesthesia, Results: Oral alprazolam affected cognitive processing speed more than oral lorazepam and the association was statistically significant (P-value <0.05) in one of the three tests performed. Other two tests showed statistically insignificant results. Conclusion: Lorazepam might be a better anxiolytic premedicant than alprazolam.

Comparative Evaluation of Melatonin, Pregabalin and Alprazolam as Premedicants for Perioperative Anxiety and Post Operative Pain for Laparoscopic Surgeries

The present study was undertaken to compare the effects of Melatonin 3 mg, Pregabalin 75 mg andAlprozolam 0.5 mg as premedicant drugs for reduction in perioperative anxiety and post operative pain,assessment of level of sedation. 150 patients of ASA grade I and II, between 20 - 50 years, of eithersex, undergoing laparoscopic surgery were divided into 3 groups of 50 patients each. Baseline anxietylevel and level after 1hr of drug was assessed. Also postoperative anxiety at different intervals wasassessed. Similarly postoperative pain and level of sedation at different intervals was assessed. Patients in group M were highly sedated as compared to group P and group A at all intervals and thedifference was statistically significant. All the three groups were comparable regarding postoperativepain, perioperative anxiety and side effects at all intervals and the difference was statistically insignificant at all intervals.

Alprazolam una alternativa terapéutica en Urgencia Hipertensiva / Alprazolam A Therapeutic Alternative in Hypertensive Urgency

Objetivo: Comparar la terapia combinada de captopril mas alprazolam versus captopril mas placebo en el manejo de urgencia hipertensiva (UH). Método: Es un ensayo clínico, uncéntrico, doble ciego, semialeatorizado, en edades comprendidas entre 45 y 80 años con UH que cumplían los criterios del JNC VII, atendidos en el servicio de emergencia entre Agosto 2017 ­ Febrero del 2018, distribuidos en grupo A (Control, n=41) y grupo B (experimental, n= 55) los cuales recibieron captopril mas placebo y alprazolam y captopril respectivamente. Resultados: Hubo predominio del género femenino en ambos grupos, y también el grado de ansiedad leve fue la más frecuente. En el grupo experimental hubo un descenso significativo a los 30, 60 y 90 minutos de la PAM de - 19%, -24 y -27% con una P 0.0000, en PAS a los 30 minutos era de -17%, 60 minutos de -22% y 90 minutos -26%, y en la PAD en los intervalos de tiempo antes citado fue -21%, -26% y -28%. Con una reducción igual o mayor a 25% de la presión arterial media en el grupo B, luego de 90 min de tratamiento. Según el RR aquellos que recibieron el tratamiento experimental tuvieron cerca de 7,5 veces más probabilidades de disminuir la presión arterial de forma efectiva a los 90 min, el NNT indica que es necesario tratar únicamente a 2 pacientes para que uno se beneficie. Conclusión: Acorde con estos resultados podemos discernir que el uso del alprazolam puede ser una alternativa terapéutica en la urgencia hipertensiva.

Objective: To compare the combination therapy of captopril plus alprazolam versus captopril plus placebo in the management of hypertensive emergency (UH). Method:It is a clinical trial, uncentric, double blind, semi-randomized, in ages between 45 and 80 years withUH that met the criteria of JNC VII, attended in the emergency service between August 2017 -February 2018, distributed in group A (Control, n = 41) and group B (experimental, n = 55) who received captopril plus placebo and alprazolam and captopril respectively. Results: There was a predominance of the female gender in both groups, and also the degree of mild anxiety was the most frequent. In the experimental group there was a significant decrease at 30, 60 and 90 minutes of the MAP of -19%, -24 and -27% with a P 0.0000, in PAS at 30 minutes it was -17%, 60 minutes of -22% and 90 minutes -26%, and in the PAD in the aforementioned time intervals it was -21%, -26% and -28%. With a reduction equal to or greater than 25% of the average blood pressure in group B, after 90 min of treatment. According to the RR those who received the experimental treatment were about 7.5 times more likely to lower blood pressure effectively at 90 min, the NNT indicates that it is necessary to treat only 2 patients for one to benefit. Conclusion:According to these results we can discern that the use of alprazolam can be a therapeutic alternative in the hypertensive emergency

Evaluation of learning and memory effect of atorvastatin and simvastatin in alprazolam induced amnesia in mice

Background: The study was undertaken to evaluate the learning and memory effect of lipid lowering drugs atorvastatin and simvastatin in alprazolam induced amnesic mice.Methods: The study was carried out on albino mice, divided into 4 groups of 6 animals each (either sex, 3-4 months of age, weight 25-30g). Amnesia was induced by administering Alprazolam (2mg/kg for 14 days) in all 4 groups from 1st to 14th day. In addition, group 2, 3 and 4 received Piracetam (400mg/kg), Atorvastatin (5mg/kg) and Simvastatin (5mg/kg) from 8th to 14th day respectively. The learning and memory of the animals was assessed by employing Elevated plus maze (EPM) and Step-down type passive avoidance (SDA) model.Results: Results were compared among the different groups using one way-ANOVA followed by post hoc Tukey’s test. The measured parameters were compared with standard drug Piracetam. In EPM model Atorvastatin (p<0.049) and Simvastatin (p<0.007) were comparable with standard drug Piracetam, whereas in SDA model only simvastatin group (p<0.001) showed significant result.Conclusions: In EPM model, both the statins showed significant improvement in learning and memory in alprazolam induced amnesic mice. However further studies are required to support these observations.

A comparative analysis of anxiolytic activity of Arnica montana and alprazolam in rats using open field test

Background: Anxiety affects around 7.3% of the total population worldwide. Benzodiazepines are preferred anxiolytic agents and are still frequently used in spite of the side effect profile including muscle relaxation, memory disturbances, sedation, physical dependence. Arnica montana, a traditional herb is known to possess significant anxiolytic effect at the dose of 100mg/kg. In this study, Arnica montana has been compared for the first time with alprazolam, a most commonly used anxiolytic drug.Methods: Forced swim test was used to induce anxiety. Anxiolytic action of study drugs which were given orally, was evaluated using Open field test (OFT) in healthy wistar rats of either sex. Behavior of rats, locomotion and number of squares crossed was recorded. Rats were divided into four groups with eight rats in each group. Study groups were Group I Control; Group II Alprazolam 0.08mg/kg; Group III Arnica montana extract (AME) 100mg/kg; Group IV AME + Alprazolam group 100mg/kg+0.08mg/kg. Statistical analysis was done using ANOVA followed by Tukey抯 test (p<0.05).Results: Increase in frequency of rearing was significant (p<0.05) in AME group and highly significant (p<0.001) in Alprazolam and combination group in comparison to control. Decrease in frequency of grooming was highly significant (p<0.001) in Alprazolam and combination group. AME also showed significant (p<0.05) decrease in grooming activity.Conclusions: Arnica montana extract showed anxiolytic activity and can be used as an add on drug after further studies and validation in the treatment of anxiety disorders.

Acupuncture at back- points of five , Geshu (BL 17) and Shenmen (HT 7) for the treatment of menopausal insomnia / 中国针灸

<p><b>OBJECTIVE</b>To compare the clinical efficacy differences between acupuncture at back- points of five , Geshu (BL 17), Shenmen (HT 7) and regular medication for the treatment of menopausal insomnia.</p><p><b>METHODS</b>A total of 128 female patients of menopausal insomnia were randomly divided into an observation group and a control group, 64 cases in each one. Four patients in the observation group and 2 patients in the control group dropped out during the treatment. The patients in the observation group were treated with acupuncture at Feishu (BL 13), Xinshu (BL 15), Pishu (BL 20), Ganshu (BL 18), Shenshu (BL 23), Geshu (BL 17) and Shenmen (HT 7), once a day, and there was an interval of 2 days between every 5 days of treatment. The patients in the control group were treated with oral administration of alprazolam (0.4 mg or 0.8 mg) before sleep. Three-week treatment was taken as one course, and totally three courses were given in the two groups. Pittsburgh sleep quality index (PSQI), levels of estradiol (E), follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were observed before treatment and 30 days after treatment; the efficacy was evaluated 30 days after treatment.</p><p><b>RESULTS</b>Each item score and total score of PSQI 30 days after treatment were lower than those before treatment in the two groups (all <0.05), the scores in the observation group were lower than those in the control group (all <0.05). The levels of E 30 days after treatment were higher than those before treatment in the two groups (both <0.05), but the level of FSH and LH 30 days after treatment were lower than those before treatment in the two groups; the level in the observation group was superior to that in the control group (all <0.05). The total effective rate was 98.3% (59/60) in the observation group, which was better than 95.2% (59/62) in the control group (<0.05).</p><p><b>CONCLUSION</b>Acupuncture at Feishu (BL 13), Xinshu (BL 15), Ganshu (BL 18), Pishu (BL 20), Shenshu (BL 23), Geshu (BL 17), and Shenmen (HT 7) has better efficacy for menopausal insomnia than alprazolam.</p>

The Meta-analysis on efficacy and safety of Eszopiclon and Alprazolam in the treatment of insomnia / 西安交通大学学报(医学版)

Objective To make a systematic evaluation of the efficacy and safety of Eszopiclon and Alprazolam in the treatment of insomnia.Methods By searching the PubMed,Cochrance Library,CNKI, WANFANG,and VIP database,we studied the literature published between 2005 to 2016 on the efficacy and safety of Eszopiclon and Alprazolam in the treatment of insomnia.We collected the randomized controlled trials (RCTs), evaluated the quality of methods and then analyzed the data using RevMan5.3 software.Results A total of 18 RCTs were included,involving 2088 patients.According to Meta-analysis,Eszopiclon group had a significantly higher total efficacy rate [RR=1.07,95% CI (1.02,1.11),P=0.003],lower severity of adverse reactions [MD=-0.43,95% CI(-0.75,-0.12),P=0.008]and incidence of adverse reactions [RR=0.46,95% CI(0.32, 0.66),P<0.0001]than Alprazolam group.However,the two groups did not significantly differ in sleep quality scores after 4-week teatment [MD=-0.05,95% CI(-0.22,0.12),P=0.54].Conclusion Eszopiclon is more effective on insomnia than Alprazolam,with better safety,and it deserves wide clinical use.

Efecto de la pre-medicación con alprazolam por vía oral sobre la presión arterial en pacientes hipertensos en cirugías electivas: un ensayo clínico / Effect of premedication with alprazolam orallyadministered on blood pressure in hypertensive patientsin elective surgeries: a clinical trial

Los ansiolíticos como el alprazolam podrían colaborar en mantener la presión arterial en pacientes hipertensos que deberán someterse a cirugía. El objetivo fue evaluar eficacia de la pre-medicación con alprazolam vía oral para mantener estables cifras de presión arterial en hipertensos programados para cirugías. Ensayo clínico aleatorizado, controlado y a doble ciego. Los pacientes fueron asignados al grupo que recibió alprazolam como premedicación (Grupo A) o al grupo control (Grupo P) que no lo recibió. Se registraron la variación de la presión arterial media (PAM), frecuencia cardíaca (FC) y frecuencia respiratoria (FR) entre el día previo y el día de la cirugía. En el Grupo A se encontró un aumento promedio de la PAM de 0,27 mmHg y en el grupo P de 7,52 mmHg (p= 0,0035). La variación promedio de la FC fue de 2,13 latidos por minuto en el Grupo A y de 5,38 latidos por minuto en el Grupo P (p= 0,0008); y de la frecuencia respiratoria fue de -2,29 respiraciones por minuto en el Grupo A y de -1,18 respiraciones por minuto en el Grupo P (p=0,206).Se halló un aumento significativo de la PAM y la FC en el Grupo P con respecto al Grupo A, no así de la FR. La administración del alprazolam como pre-medicación operatoria evita aumentos significativos de la presión arterial y de la frecuencia cardíaca en los pacientes hipertensos.

Anxiolytics such as alprazolam may help to maintain blood pressure in hypertensive patients who undergo surgery. The aim was to evaluate efficacy of pre-medication with alprazolam orally administered to maintain stable blood pressure in hypertensives programmed for surgeries. Randomized, controlled, double-blind clinical trial. Patients were assigned to the group that received alprazolam as premedication (Group A) or to the control group (Group P) which did not receive it. The variation of the mean arterial pressure(MAP), heart rate (HR) and respiratory rate (RR) were recorded between the day before andthe day of the surgery. In Group A, we found an average increase in MAP of 0.27 mmHgand in the Group P 7.52 mmHg (p = 0.0035). The mean HR variation was 2.13 beats perminute in Group A and 5.38 beats per minute in Group P (p = 0.0008). The mean RR variantion was -2.29 breaths per minute in Group A and -1.18 breaths per minute in Group P (p = 0.206). There was a significant increase in the MAP and HR in Group P compared toGroup A, but not in the RR. The administration of alprazolam as an operative premedication avoids significant increases in blood pressure and heart rate in hypertensive patients.

The Efficacy and Safety of Clonazepam in Patients with Anxiety Disorder Taking Newer Antidepressants: A Multicenter Naturalistic Study

OBJECTIVE: This study compared the efficacy and tolerability of clonazepam with other benzodiazepines in patients with anxiety disorders. METHODS: Inclusion criteria were as follows: age >20 years, diagnosis of anxiety disorder according to the Diagnostic and Statistical Manual of Mental Disorders 4th edition, text revision (DSM-IV-TR) criteria, taking only one type of antidepressant, and prescribed one of three oral benzodiazepines (alprazolam, clonazepam, or lorazepam). At baseline and week 6, clinical benefit was evaluated using the Clinical Global Impression-Severity Scale (CGI-S), Clinical Global Impression-Anxiety Scale (CGI-anxiety), and Clinical Global Impression-Sleep Scale (CGI-sleep). RESULTS: Among 180 patients, no differences in demographic characteristics among the three benzodiazepine groups were noted. After six weeks of treatment, all benzodiazepine groups showed significant improvements in CGI-S, CGI-anxiety, and CGI-sleep scores (p<0.001). There were no differences in mean changes in CGI-S, CGI-anxiety and CGI-sleep among the three benzodiazepine groups. The incidence of side effects was significantly lower in the clonazepam group than with the other benzodiazepines. The incidences of adverse events for the clonazepam, alprazolam, and lorazepam groups were 26.7% (n=20), 48.4% (n=31), and 43.9% (n=18), respectively. CONCLUSION: The present study suggests that clonazepam is as efficacious as other benzodiazepines for the treatment of various anxiety disorders. Furthermore, the safety profile of clonazepam was superior to the other benzodiazepines in this study.

Simultaneous determination of clomipramine and four benzodiazepines in human plasma by HPLC-DAD after solid phase extraction / 中国药理学通报

Aim To establish a novel,highly sensitive,rapid and cost-effective HPLC method to simultaneously determine tri-cyclic antidepressant clomipramine and four benzodiazepines of diazepam,alprazolam,clonazepam,oxazepam in human plasma pretreated by solid phase extraction.Methods The assay was achieved by using C8 column (4.6 mm ×1 50 mm,5 μm)kept at 45 ℃,mobile phase 73.2:26.8 V/V (50 mmol·L -1 ,pH 3.0 phosphate buffer:acetonitrile)with flow rate of 1 .2 ml· min -1 ,and UV detection was set at λ220 nm.Solid phase ex-traction was performed on C1 cartridges.Results The calibra-tion curve was demonstrated to be linear (r >0.9994)in the ranges of 5 ~200 μg·L -1 for alprazolam and clonazepam,1 0 ~500 μg·L -1 for diazepam,20 ~500 μg· L -1 for clomipra-mine,and 7.5 ~2000 μg·L -1 for oxazepam;the limit of detec-tion (LOD)was 1 .5,1 .4,3.0,5.5 and 2.2 μg·L -1 for al-prazolam,clonazepam,diazepam,clomipramine and oxazepam respectively.Intra-day and inter-day precision revealed a coeffi-cient of variation of 2.2% ~1 2.6% and 2.1 % ~1 3.2%,re-spectively.Extraction yield ranged from 81 .1 % ~1 00.1 % for all analytes.Conclusion The developed method is accurate, reproducible,convenient,and suitable for routine therapeutic drug monitoring of clomipramine and the four benzodiazepines.

Comparative Study of Only Paroxetine and Paroxetine Combined with Alprazolam in the Treatment of Diabe-tes Complicated with Anxiety and Depression / 中国药房

OBJECTIVE:To compare the efficacy and safety of only paroxetine vs. paroxetine combined with alprazolam in the treatment of diabetes complicated with anxiety and depression. METHODS:Totally 86 patients with diabetes complicated with anxi-ety and depression were randomly divided into observation group and control group. The patients in observation group were given paroxetine 20 mg,qd,and alprazolam 0.4 mg,tid;patients in control group were given paroxetine alone. The treatment course lasted for 8 weeks in 2 groups. The clinical data was compared,including fasting plasma glucose(FPG),2 h postprandial glucose (2 h PG),glycated hemoglobin (HbA1c),cortisol,adrenocorticotropic hormone (ACTH) levels and scores of Hamilton anxiety scale (HAMA) and Hamilton depression scale (HAMD). The adverse reactions were observed. RESULTS:After treatment,FP-BG,2 h PG,HbA1c,cortisol,ACTH levels and scores of HAMA and HAMD in observation group were significantly lower than control group,with significant difference(P0.05). CONCLUSIONS:Compared with paroxetine alone,paroxetine combined with alprazolam can improve more in blood glucose,endocrine levels and adverse mood symptoms in the treatment of diabetes complicated with anxiety and de-pression,with similar safety.

Observation on the Efficacy and Safety of Alprazolam by Progressive Dose Increasing in the Treatment of Chronic Tinnitus / 中国药房

OBJECTIVE:To observe the efficacy and safety of alprazolam by progressive dose increasing in the treatment of chronic tinnitus. METHODS:Totally 50 patients with chronic tinnitus were included. They were orally treated with Alprazolam tab-let 0.4 mg in the first 1 and 2 week(s),once every night at bedtime;0.4 mg in 3 and 4 weeks,once in the morning and once in the evening;0.4 mg in 5 and 6 weeks,three times a day. If the treatment of tinnitus was invalid,then the gradual withdrawl was conducted by twice a day for continuous 3 d,0.4 mg each time;then once a day,0.4 mg each time,for continuous 3 d. The re-sponders were maintained 12 weeks,and gradual withdrawal was conducted,and followed by follow-up for 3 months. The clinic data was observed,including the clinical efficacy,tinnitus disability scale(THI)score,visual analogue scale(VAS)score,tinnitus loudness(TI)and incidence of adverse reactions before and after treatment. RESULTS:The effective rate was 66.67%;after treat-ment,the scores of THI and VAS,and TI were significantly lower than before,with significant differences(P<0.05). There were no obvious adverse reactions during treatment. CONCLUSIONS:The alprazolam by progressive dose increasing has obvious effica-cy in the treatment of chronic tinnitus,with good safety.

Use of triazolam and alprazolam as premedication for general anesthesia / 대한마취과학회지

BACKGROUND: Triazolam has similar pharmacological properties as other benzodiazepines and is generally used as a sedative to treat insomnia. Alprazolam represents a possible alternative to midazolam for the premedication of surgical patients. The purpose of this study was to evaluate the anxiolytic, sedative, and amnestic properties of triazolam and alprazolam as pre-anesthetic medications. METHODS: Sixty adult patients were randomly allocated to receive oral triazolam 0.25 mg or alprazolam 0.5 mg one hour prior to surgery. A structured assessment interview was performed in the operating room (OR), the recovery room, and the ward. The levels of anxiety and sedation were assessed on a 7-point scale (0 = relaxation to 6 = very severe anxiety) and a 5-point scale (0 = alert to 4 = lack of responsiveness), respectively. The psychomotor performance was estimated using a digit symbol substitution test. As a memory test, we asked the patients the day after the surgery if they remembered being moved from the ward to the OR, and what object we had shown them in the OR. RESULTS: There were no significant differences between the groups with respect to anxiety and sedation. The postoperative interviews showed that 22.2% of the triazolam-treated patients experienced a loss of memory in the OR, against a 0% memory loss in the alprazolam-treated patients. In comparison with alprazolam 0.5 mg, triazolam 0.25 mg produced a higher incidence of amnesia without causing respiratory depression. CONCLUSIONS: Oral triazolam 0.25 mg can be an effective preanesthetic medication for psychomotor performance.

Biochemical and ultra-structural studies of the effect of alprazolam as an anxiolytic drug on the cerebellum of adult male mice.

In the recent decade, there has been increasing concern on the hazard effect of drugs on different species. Stressful life events contribute to the development of many neurodegenerative and neuropsychiatric disorders including depression and anxiety. Alprazolam (ALP) is commonly used and approved for the medical treatment of panic and anxiety disorders, such as generalized anxiety or social anxiety disorders. Thus, it was of a particular interest to investigate the effect of ALP on the neurons of cerebellar cortex of mice, where mice have genomic similarities to human. So, biochemical, histological and ultrastructural investigations are reported on the cerebellum of adult male mice subjected to three different doses of ALP, for two months. These doses were equivalent to the human therapeutic doses as 0.5, 1 and 1.5 mg. In a dose dependant manner, significant decreases in the levels of both acetylcholine enzyme activities and total glutathione are recorded, indicating that the activity of acetylcholine esterase was inhibited by free radical formation. Little histopathological changes were observed in the cerebellar cortex of mice administered with 0.5 mg ALP. Marked alterations were observed in the Purkinje neurons of cerebellar cortex of mice administered with 1 and 1.5 mg ALP, where unstained haloes are seen around most of these cells. Their nuclei were eccentrically placed, and pyknotic. The intracellular structure of Purkinje cells showed dilatation of both rER and Golgi apparatus. Many small vesicles near the Golgi bodies were accumulated to form clusters, probably indicate disturbance in the vesicular transport between rER and Golgi apparatus. These results reflect the injured effect of high dose ALP on brain activity, performing in the possible ultrastructural abnormalities as well as its oxidative stress.

Comparação de cromatografia líquida de alta eficiência e titulação em meio não aquoso para quantificação de alprazolam em cápsulas manipuladas / Comparison of high performance liquid chromatography and non-aqueous titration for the quantitation of alprazolam in compounded capsules

O objetivo pretendido com o presente trabalho foi avaliar a adequabilidade e viabilidade de dois métodos analíticos para quantificação de alprazolam em cápsulas manipuladas: cromatografia líquida de alta eficiência (CLAE) e titulação em meio não aquoso. A quantificação de alprazolam por CLAE fase normal foi realizada em coluna de sílica (30 x 4,6 mm) e fase móvel composta por acetonitrila, clorofórmio, butanol, água e ácido acético glacial (85:8:5:2:0,05). No método titulométrico, as amostras foram dissolvidas em mistura de ácido acético glacial e anidrido acético (3:2) e tituladas com ácido perclórico 0,1 M até o segundo ponto de inflexão. O teor médio de alprazolam obtido por CLAE foi 94,61%, demonstrando a adequabilidade do método proposto. Já as análises por titulação apresentaram teores equivalentes a 128,87% e 91,49% do valor rotulado, devido a interferências detectadas pela presença de excipientes da formulação. A adaptação e o desenvolvimento de métodos analíticos simples e viáveis são de extrema importância para avaliar e garantir a qualidade de medicamentos manipulados, de acordo com as exigências da legislação vigente.

The aim of this study was to assess the suitability and viability of two analytical methods for the quantitation of alprazolam in compounded capsules: high performance liquid chromatography (HPLC) and non-aqueous titration. Quantitation by normal phase HPLC was performed with a silica column (30 x 4.6 mm) and a mobile phase composed of acetonitrile, chloroform, butyl alcohol, water and glacial acetic acid (85:8:5:2:0.05). In the titration method, samples were dissolved in a mixture of glacial acetic acid and acetic anhydride (3:2) and titrated potentiometrically with 0.1 M perchloric acid until the second inflection point. The mean content of alprazolam obtained by HPLC was 94.61% of the label value, showing the suitability of the proposed method. On the other hand, the titration analysis returned contents equivalent to 128.87% and 91.49% of the label value, owing to interference caused by the presence of formulation excipients. The adaptation and development of simple and viable analytical methods are extremely important, in order to assay and ensure the quality of compounded formulations, according to the requirements of the current legislation.

A comparative study of the effect of ondansetron, granisetron and alprazolam on anxiety in wistar rats.

Objective: The study was undertaken to compare the effect of ondansetron, granisetron and alprazolam on anxiety in rats. Materials and Methods: Elevated plus maze and Open field test were used to compare the effect of drugs on anxiety in rats. Six groups of rats were treated with 2% gum acacia orally, alprazolam 0.08mg/kg body weight of the rat orally, ondansetron (0.01mg/kg, 1mg/kg intraperitoneally) and granisetron (0.01mg/kg and 1mg/kg intraperitoneally) respectively. The time spent, number of entries and rears in the arms of the elevated plus maze and central and peripheral areas in the open field test Results: Alprazolam and ondansetron significantly increased (P<0.05) the time spent in open arm of elevated plus maze and central squares in the open field and decreased (P<0.05) the time spent in the closed arm of elevated maze and peripheral squares in the open field as compared to control. There was no significant difference between the effects of alprazolam and ondansetron. Granisetron did not produce any significant effect in any of the models. Conclusion: Ondansetron, but not granisetron, produced anxiolytic activity in rats which was comparable to alprazolam.

Effects of alprazolam on capture stress-related serum cortisol responses in Korean raccoon dogs (Nyctereutes procyonoides koreensis)

The purpose of this study was to evaluate the effect of alprazolam on the stress that Korean raccoon dogs (Nyctereutes procyonoides koreensis) may experience while caught in a live trap by measuring their serum cortisol response. The animals were placed in a live trap with or without being pretreated with oral doses of alprazolam. In both groups, pre-trap blood samples were initially collected without anesthesia before the animals were positioned in the live trap; then post-trap blood samples were collected after the animals had remained in the live trap for 2 h. Changes in cortisol levels were observed using a chemiluminescent immunoassay. The level of cortisol increased in the control group and decreased in the alprazolam-pretreatment group (p < 0.05). In this study, we demonstrated that alprazolam pretreatment reduced stress during live trap capture.

Clinical analysis of dompeird one combined with flupentixol, melitracen (deanxit) and alprazolam in the treatment of functional dyspepsia / 中国医师杂志

Objective To evaluate the efficacy and safety of domperidone combined with flupentix-ol,melitracen ( deanxit ) and alprazolam in the treatment of functional dyspepsia .Methods One hundred and sixty patients with functional dyspepsia were randomly divided into the treatment group ( n =80 ) and the control group ( n =80 ) .The treatment group was given domperidone combined with flupentixol , meli- tracen (deanxit) and alprazolam, and the control group was only given domperidone for 4 weeks.The im-provement of clinical symptoms such as stomach burn ,early enough, abdominal distension, sour regurgita -tion and eructation were evaluated by clinical symptom score .Results Compared with patients in the con-trol group, the rate of marked improvement and rates of improvement for patients in the treatment group were all better ( P <0.01).Furthermore, the adverse reaction is light .Conclusion The application of domp-eridone combined with flupentixol, melitracen ( deanxit ) and alprazolam is quite effective in treating patients with FD.