RESUMO
Ultrasound and microwave as green processes are investigated in this study, focusing on the extraction selectivity towards antioxidant extraction from rosemary leaves. Due to its richness in valuable compounds such as rosmarinic, carnosic and ursolic acids, rosemary is a reference matrix for extraction study. In this work, six alternative processes are compared: ultrasound (bath, reactor and probe), microwave (reflux under microwave, microwave under nitrogen pressure and microwave under vapor pressure). The main result of this study is that selective extraction can be achieved according to extraction techniques and therefore to the extraction process.
Assuntos
Fracionamento Químico/métodos , Micro-Ondas , Rosmarinus/química , Terpenos/isolamento & purificação , Ondas Ultrassônicas , Abietanos/análise , Abietanos/química , Abietanos/isolamento & purificação , Cinamatos/análise , Cinamatos/isolamento & purificação , Depsídeos/análise , Depsídeos/isolamento & purificação , Química Verde , Terpenos/análise , Triterpenos/análise , Triterpenos/isolamento & purificação , Ácido Rosmarínico , Ácido UrsólicoRESUMO
The sedative properties of astemizole-D and triprolidine-D were compared in a double-blind, placebo-controlled, repeated-measures design study comprising three experimental treatments, each with a duration of 2 days (n = 12). Sedation was assessed by continuous electroencephalographic measurement (C-EEG), intermittent performance testing and subjective measures. C-EEG monitoring revealed that triprolidine-D produced significantly more daytime sedation and drowsiness than either astemizole-D or placebo (p < 0.05). Intermittent performance testing did not reveal consistent psychomotor deficits. There were no differences from placebo; the only significant findings showed that astemizole-D improved tracking accuracy at T + 65 h (p < 0.05) compared to baseline. Also, when scores were summed across all time points, astemizole-D improved scores significantly in contrast to triprolidine-D for the total scores (p < 0.05). It is concluded that, in contrast to triprolidine-D, astemizole-D does not produce daytime drowsiness or sedation.
Assuntos
Astemizol/farmacologia , Antagonistas dos Receptores Histamínicos H1/farmacologia , Triprolidina/farmacologia , Adulto , Astemizol/efeitos adversos , Preparações de Ação Retardada , Método Duplo-Cego , Quimioterapia Combinada , Eletroencefalografia/efeitos dos fármacos , Efedrina/farmacologia , Feminino , Antagonistas dos Receptores Histamínicos H1/efeitos adversos , Humanos , Pessoa de Meia-Idade , Sono/efeitos dos fármacos , Simpatomiméticos/farmacologia , Triprolidina/efeitos adversosRESUMO
The possible central nervous system effects of topical administration of levocabastine, a new H1-antagonist, were investigated in a double-blind, placebo-controlled, crossover study using a battery of objective and subjective tests. These were carried out in 12 volunteers up to five hours postapplication. Neither the recommended (0.5 mg/mL) nor the four times higher (2.0 mg/mL) concentration level was found to be distinguishable from placebo, while the verum (triprolidine 10 mg) was significantly worse, on both objective and subjective measures.
Assuntos
Cognição/fisiologia , Antagonistas dos Receptores Histamínicos H1/farmacologia , Piperidinas/farmacologia , Desempenho Psicomotor/fisiologia , Administração Tópica , Adolescente , Adulto , Cognição/efeitos dos fármacos , Relação Dose-Resposta a Droga , Método Duplo-Cego , Feminino , Antagonistas dos Receptores Histamínicos H1/administração & dosagem , Humanos , Pessoa de Meia-Idade , Piperidinas/administração & dosagem , Desempenho Psicomotor/efeitos dos fármacosRESUMO
Twelve healthy volunteers were randomly allocated to receiving in a double-blind cross-over fashion levocabastine eye drops (0.5 mg/ml solution) and placebo. They were advised to instill 2 drops per eye, four times daily. Each treatment was administered for a period of 1 week. Before and after each treatment period psychomotor function was assessed using Critical Flicker Fusion Test and the Choice Reaction Time Test. At the same time intervals a subjective evaluation of sedation was given using a Visual Analogue of Sedation. Both objective and subjective measurements showed that no significant treatment effects could be detected. It is concluded that repeated instillations of levocabastine eye drops are devoid of any sedative side effects.
Assuntos
Sistema Nervoso Central/efeitos dos fármacos , Antagonistas dos Receptores Histamínicos H1/farmacologia , Piperidinas/farmacologia , Adulto , Método Duplo-Cego , Feminino , Antagonistas dos Receptores Histamínicos H1/sangue , Humanos , Masculino , Pessoa de Meia-Idade , Soluções Oftálmicas , Piperidinas/sangue , Desempenho Psicomotor/efeitos dos fármacosRESUMO
Forty-four patients, with symptoms of nasal obstruction, sneezing, itching and/or rhinorrhea, were entered into a placebo-controlled, double-blind study to evaluate the clinical efficacy of a topical antihistamine drug, levocabastine, applied 4 times a day for 14 days. At the end of the treatment the placebo patients were treated with levocabastine and the levocabastine patients were treated with beclomethasone dipropionate in a single-blind design for another 14 days. This study showed that levocabastine is significantly more active than placebo with reference to nasal discharge and sneezing. Placebo application improved the symptom score. Levocabastine could not be proved to be more effective against nasal obstruction than placebo in the double-blind trial. In the single-blind set-up, levocabastine resulted in an additional improvement in the score for obstruction, after the placebo period. Although the allergic group tended to respond better, no statistically significant difference could be detected between allergic and non-allergic patients. After treatment with levocabastine, beclomethasone dipropionate administration could not improve the results for nasal discharge and sneezing. For nasal congestion, beclomethasone dipropionate proved to be superior to levocabastine.
Assuntos
Piperidinas/uso terapêutico , Rinite Alérgica Perene/tratamento farmacológico , Rinite Alérgica Sazonal/tratamento farmacológico , Administração Intranasal , Beclometasona/uso terapêutico , Ensaios Clínicos como Assunto , Método Duplo-Cego , Feminino , Humanos , Masculino , Piperidinas/administração & dosagemRESUMO
The effect of levocabastine, a new specific H1 antagonist, has been investigated against a placebo in nasal provocation tests on 42 allergic patients divided into two parallel groups. The results obtained show that it significantly inhibited the nasal reaction to the allergen and seems to have a long-lasting effect in allergic patients.
Assuntos
Antagonistas dos Receptores Histamínicos H1/uso terapêutico , Testes de Provocação Nasal , Piperidinas/uso terapêutico , Rinite/diagnóstico , Administração Intranasal , Adolescente , Adulto , Feminino , Antagonistas dos Receptores Histamínicos H1/administração & dosagem , Humanos , Masculino , Pessoa de Meia-Idade , Piperidinas/administração & dosagemRESUMO
From clinical-pharmacologic and clinical data involving over 2,800 patients, astemizole appears to be a very effective and well-tolerated antihistamine. It is superior to placebo and commonly used antihistamines for the relief of rhinitis, particularly rhinorrhea and sneezing. It has a pronounced effect on ocular itching and lacrimation in conjunctivitis and on pruritus and wheals in urticaria. This superiority is due to a very specific, almost complete and sustained histamine H1-blockade. The clinical data confirm the experimental data in relation to its lack of sedative effects.
Assuntos
Benzimidazóis/uso terapêutico , Conjuntivite Alérgica/tratamento farmacológico , Antagonistas dos Receptores Histamínicos H1/uso terapêutico , Rinite Alérgica Perene/tratamento farmacológico , Rinite Alérgica Sazonal/tratamento farmacológico , Urticária/tratamento farmacológico , Astemizol , Ensaios Clínicos como Assunto , Método Duplo-Cego , Feminino , Humanos , MasculinoRESUMO
Astemizole is a potent H1-antagonist devoid of sedative effects, which was found at single oral daily doses to be very effective in the treatment of allergic rhinitis, allergic conjunctivitis, and urticaria. Its interaction potential on other drugs was studied in various ways. Studies on salivary antipyrine clearance, the 6-beta-hydrocortisol excretion, the elimination rate of ethanol and the indocyanine-green clearance are presented. No changes were observed. Astemizole also was given in combination with diazepam or alcohol. Psychomotor performance failed to show any effects. In none of these studies was there any evidence of interaction of astemizole on other drugs. This review summarizes the data available thus far.
Assuntos
Benzimidazóis/farmacologia , Antagonistas dos Receptores Histamínicos H1/farmacologia , Animais , Anticoagulantes/farmacologia , Astemizol , Benzimidazóis/administração & dosagem , Benzimidazóis/metabolismo , Método Duplo-Cego , Avaliação de Medicamentos , Interações Medicamentosas , Etanol/farmacologia , Antagonistas dos Receptores Histamínicos H1/administração & dosagem , Antagonistas dos Receptores Histamínicos H1/metabolismo , Humanos , Inativação Metabólica/efeitos dos fármacos , Cinética , Masculino , Camundongos , Distribuição Aleatória , RatosRESUMO
From the start of the Astemizole clinical investigations, until now the results of 39 trials including more than 2300 patients are available. These results show that Astemizole is an effective and safe Histamine-H1-antagonist for the therapy of hayfever, chronic allergic rhinitis, allergic conjunctivitis, chronic urticaria and allergic bronchitis in adults and children. Astemizole was superior to placebo and the classical antihistamines like Clemastine, Terfenadine, Ketotifen, Mequitazine, pheniramine and Chlorphenamine.
Assuntos
Benzimidazóis/uso terapêutico , Antagonistas dos Receptores Histamínicos H1/uso terapêutico , Hipersensibilidade/tratamento farmacológico , Astemizol , Beclometasona/uso terapêutico , Benzimidazóis/efeitos adversos , Bronquite/tratamento farmacológico , Ensaios Clínicos como Assunto , Conjuntivite/tratamento farmacológico , Método Duplo-Cego , Quimioterapia Combinada , Antagonistas dos Receptores Histamínicos H1/efeitos adversos , Humanos , Rinite Alérgica Perene/tratamento farmacológico , Rinite Alérgica Sazonal/tratamento farmacológico , Urticária/tratamento farmacológicoRESUMO
A longterm investigation containing three distinct studies has been carried out in order to clarify efficacy and inocuity of clopimozide in the maintenance treatment of chronic psychotics. Twelve patients took part in the pilot study (Study I) during which the optimal weekly dose was established to be 24 mg. These patients were then subdivided into two groups for a controlled study with placebo (Study II). This double-blind evaluation has clearly established the superiority of cloprimozide over placebo. Patients were evaluated at the start and completion of the study with three scales. During the surveillance period (Study III), clopimozide was administered daily with a mean dose of 2.5 mg. Results were equally satisfying as those obtained during weekly treatment. The appearance of side-effects, mostly akatsia and dyskinesia, was only noted during the weekly administration. They could be efficiently controlled with dexetimide.