ABSTRACT
Abstract Dexchlorpheniramine is a first-generation classical antihistamine, clinically used to treat allergies. The main objective of our study was to evaluate the effects of the dexchlorpheniramine reference standard (DCPA Ref. St) and a pharmaceutical formula on DNA in human peripheral blood mononuclear cells (PBMCs). We exposed PBMCs to five different concentrations (0.5, 2.5, 5, 10, and 50 ng/mL) of DCPA Ref. St DCPA Ref. St and pharmaceutical formula in order to evaluate their cytotoxic, genotoxic, and mutagenic potential. The results showed that both dexchlorpheniramine formulations did not affect PBMC viability and CD3+, CD4+, or CD8+ lymphocyte subpopulations. The DCPA Ref. St and pharmaceutical formula neither induced genotoxic or mutagenic effects nor numerical or structural chromosomal alterations in PBMCs after 24 hours of exposure.
Subject(s)
Humans , Leukocytes, Mononuclear/metabolism , Cytotoxicity, Immunologic , Drug Compounding , Genotoxicity , Mutagenicity Tests , DNA/analysis , Histamine Antagonists/adverse effects , Hypersensitivity/complicationsABSTRACT
Abstract Introduction: A combination of antihistamines and oral corticosteroids is often used to treat acute symptoms of allergic rhinitis. Objective: To evaluate safety and efficacy of desloratadine plus prednisolone in the treatment of acute symptoms of children (2-12 years) with allergic rhinitis, and to compare it to dexchlorpheniramine plus betamethasone. Methods: Children with moderate/severe persistent allergic rhinitis and symptomatic (nasal symptoms score [0-12] ≥ 6) were allocated in a double-blind, randomized fashion to receive dexchlorpheniramine plus betamethasone (n = 105; three daily doses) or desloratadine plus prednisolone (n = 105; single dose followed by two of placebo) for 7 days. At the beginning and end of the evaluation, the following were obtained: nasal symptoms score, extra nasal symptoms score, peak nasal inspiratory flow, blood biochemistry, and electrocardiogram. Ninety-six children of the dexchlorpheniramine plus betamethasone group and 98 of the desloratadine plus prednisolone group completed the protocol. Results: The two groups were similar regarding initial and final nasal symptoms scores, extra nasal symptoms scores and peak nasal inspiratory flow. A drop of 76.4% and 79.1% for nasal symptoms score, 86.0% and 79.2% for extra nasal symptoms score, as well as an increase of 25.2% and 24.3% for peak nasal inspiratory flow occurred for those treated with desloratadine plus prednisolone and dexchlorpheniramine plus betamethasone, respectively. There were no significant changes in blood chemistry. Sinus tachycardia was the most frequent electrocardiogram change, but with no clinical significance. Drowsiness was reported significantly more often among those of dexchlorpheniramine plus betamethasone group (17.14% × 8.57%, respectively). Conclusion: The desloratadine plus prednisolone combination was able to effectively control acute symptoms of rhinitis in children, improving symptoms and nasal function. Compared to the dexchlorpheniramine plus betamethasone combination, it showed similar clinical action, but with a lower incidence of adverse events and higher dosing convenience.
Resumo Introdução: A associação entre anti-histamínicos e corticosteroides orais é frequentemente empregada no tratamento de sintomas agudos de rinite alérgica. Objetivo: Avaliar a segurança e eficácia da associação desloratadina + prednisolona no tratamento de sintomas agudos de crianças (2-12 anos) com rinite alérgica e compará-las com as da associação dexclorfeniramina + betametasona. Método: Crianças com rinite alérgica persistente moderada/grave e sintomáticas (escore de sintomas nasais [0-12] ≥ 6) foram alocadas de modo duplo-cego e randômico para receber dexclorfeniramina + betametasona (n = 105; três doses diárias) ou desloratadina + prednisolona (n = 105; dose única seguida por duas de placebo) por 7 dias. No início e no fim da avaliação foram obtidos: escore de sintomas nasais, escore de sintomas extranasais, pico de fluxo inspiratório nasal, bioquímica sanguínea e eletrocardiograma. Do total, 96 crianças do grupo dexclorfeniramina + betametasona e 98 do grupo desloratadina + prednisolona concluíram o protocolo. Resultados: Os dois grupos foram iguais com relação ao escore de sintomas nasais, escore de sintomas nasais extranasais e pico de fluxo inspiratório nasal iniciais e finais. Observou-se queda de 76,4% e 79,1% nos escores para escore de sintomas nasais, de 86,0% e 79,2% para escore de sintomas extranasais, assim como incremento de 25,2% e de 24,3% para o pico de fluxo inspiratório nasal para os grupos desloratadina + prednisolona e dexclorfeniramina + betametasona, respectivamente. Não houve alterações significativas da bioquímica sanguínea. Taquicardia sinusal foi a alteração do eletrocardiograma mais encontrada, mas sem significância clínica. Sonolência foi significantemente mais referida entre os tratados com dexclorfeniramina + betametasona do que entre os desloratadina + prednisolona (8,57% × 17,14%, respectivamente). Conclusão: A associação desloratadina + prednisolona foi capaz de controlar efetivamente os sintomas agudos de rinite em crianças, melhorou sintomas e a função nasal. Na comparação com a associação dexclorfeniramina + betametasona, demonstrou ação clínica semelhante, mas com menor incidência de eventos adversos e maior comodidade posológica.
Subject(s)
Humans , Male , Female , Child, Preschool , Child , Prednisolone/administration & dosage , Loratadine/analogs & derivatives , Rhinitis, Allergic/drug therapy , Glucocorticoids/administration & dosage , Time Factors , Severity of Illness Index , Betamethasone/administration & dosage , Betamethasone/adverse effects , Prednisolone/adverse effects , Peak Expiratory Flow Rate , Double-Blind Method , Reproducibility of Results , Treatment Outcome , Loratadine/administration & dosage , Loratadine/adverse effects , Statistics, Nonparametric , Histamine H1 Antagonists, Non-Sedating/administration & dosage , Histamine H1 Antagonists, Non-Sedating/adverse effects , Drug Combinations , Glucocorticoids/adverse effectsABSTRACT
Infection of the human central nervous system (CNS) by the larvae of Taenia solium, termed neurocysticercosis (NCC), is endemic in most developing countries, where it is a major cause of acquired seizures and other neurological morbidity, including neuropsychiatric symptoms. However, despite its frequent manifestation, some findings, such as cognitive impairment and dementia, remain poorly understood. Less commonly, NCC may affect the ventricular system and subarachnoid spaces and this form is known as extraparenchymal neurocysticercosis. A particular presentation of the subarachnoid form is called racemose cysticercosis, which has a progressive pattern, frequently leads to hydrocephalus and can be life-threatening. Here we review a case of the racemose variety of cysticercosis, complicated by hydrocephalus and reversible dementia, with remission of symptoms after derivation and that remained stable with use of dexchlorpheniramine. We discuss the challenges in diagnosis, imaging findings, treatment and follow-up of this disease.
A infecção do sistema nervoso central (SNC) pela larva da Taenia solium, intitulada neurocisticercose (NCC) é endêmica na maior parte dos países "em desenvolvimento", onde é a principal causa de convulsão adquirida, além de outras morbidades neurológicas, entre elas, sintomas neuropsiquiátricos. No entanto, apesar de manifestações neuropsiquiátricas serem frequentes, alguns achados, tais como comprometimento cognitivo e demência, continuam a ser mal compreendidos. Menos frequentemente, NCC pode afetar o sistema ventricular e espaços subaracnóideos e esta forma é conhecida como NCC extraparenquimatosa. Uma apresentação particular subaracnóidea, chamada cisticercose racemosa, é encontrada mais raramente, evolui de forma progressiva, associada a hidrocefalia e pode levar a morte. Neste artigo revisamos um caso da variedade racemosa de NCC, complicada com hidrocefalia e demência reversível que evoluiu com remissão dos sintomas após derivação ventricular e permaneceu estável com uso de dexclorfeniramina. Discutimos os desafios no diagnóstico, achados de imagem, tratamento e acompanhamento desta forma de doença.
Subject(s)
Humans , Neurocysticercosis , Taenia solium , Dementia , Histamine AntagonistsABSTRACT
This paper have a purpose to determine the condition of analysis of betamethasone and dexchlorpheniramine maleat on tablet using ultraviolet spectrophotometry and high perfomance liquid chromatography (HPLC) methods. The spectrophotometry method used phosphate buffer pH 7,2 as the solvent, whereas the HPLC method used HPLC, LC-10AT VP, Shimadzu;μ BondapakTM C18 10μm 125Å, 4,6 x 150 mm coloumn Waters (Irlandia); methanol buffer (45:55) pH 7,2 as mobile phase; ultraviolet detection 240 nm; flow rate 1 mL/menit. Result showed that the correlation coefficient of spectrophotometry were 0,9998 and 0,9997 for dexchlorpheniramine maleat dan betamethasone at wavelength 239 and 262. The LOD for spectrophotometry were 2,261 ppm for dexchlorpheniramine maleat at λ 239 ; 0,707 ppm for dexchlorpheniramine maleat at λ 262 ; 0,088 ppm for betamethasone at λ 239 ; dan 0,127 for betamethasone at λ 262, the LOQ were 7,536 ppm for dexchlorpheniramine maleat at λ 239 ; 2,357 ppm for dexchlorpheniramine maleat at λ 262 ; 0,295 for betamethasone at λ 239 ; dan 0,425 for betamethasone at λ 262. The recovery percentation of the spectrophotometry methods for dexchlorpheniramine maleat and betamethasone were 101,32% and 100,77%. The recovery percentation of the HPLC methods for dexchlorpheniramine maleat and betamethasone were 107,6% and 100,8%. Coefficient of variance of the spectrophotometry methods methods for dexchlorpheniramine maleat and betamethasone were 1,413 % and 0,466 %, coeffisien of variance of the robustness test of the spectrophotometry methods for dexchlorpheniramine maleat and betamethasone were 0,834 % and 1,140 %. Based on this research has been found that the the analysis method of spectrophotometry was eligible for the validation parameter value. These data may be applied in Pharmaceutical industries.
ABSTRACT
Sustained release film coated tablets containing dexchlorpheniramine maleate were prepared in such a structure as two-third of drug were dispersed in Eudragit RS 100 to form insoluble matrix that gradually releases drug by diffusional mechanism, the rest was dispersed in the immediate release part. The core tablets were compressed by a wet granulation process and the film coated tablets by a routine film coating process with Eudragit E suspension. The formed coated tablets have suitable technical characteristics. The third formulation with Eudragit RS- drug ratio 2:1 has got the dissolution extent and the release rate in vitro similar to those of Polaramine 6mg repetabs. They also meet the requirements invitro release rate versus time for sustained release capsules containing Chlorpheniramine maleate by USP XXIII. Therefore, these film coated tablets with dexchlorpheniramine maleate may be candidates for a sustained release dosage form