RESUMO
General anxiety disorders are among the most prevalent mental health problems worldwide. The emergence and development of anxiety disorders can be due to genetic (30-50%) or non-genetic (50-70%) factors. Despite medical progress, available pharmacotherapies are sometimes ineffective or can cause undesirable side effects. Thus, it becomes necessary to discover new safe and effective drugs against anxiety. This study evaluated the anxiolytic effect in adult zebrafish (Danio rerio) of a natural pyrroloformamide (PFD), N-(4,5-dihydro-5-oxo-1,2-dithiolo-[4,3,b]-pyrrole-6-yl)-N-methylformamide, isolated from a Streptomyces sp. bacterium strain recovered from the ascidian Eudistoma vannamei. The complete structure of PFD was determined by a detailed NMR analysis, including 1H-13C and 1H-15N-HBMC data. In addition, conformational and DFT computational studies also were performed. A group of fishes (n = 6) was treated orally with PFD (0.1, 0.5 and 1.0 mg/mL; 20 µL) and subjected to locomotor activity and light/dark tests, as well as, acute toxicity 96 h. The involvement of the GABAergic and serotonergic (5-HT) systems was investigated using flumazenil (a silent modulator of GABA receptor) and 5-HT1, 5-HT2A/2C and 5-HTR3A/3B receptors antagonists, known as pizotifen, granisetron and cyproheptadine, respectively. PFD was nontoxic, reduced locomotor activity and promoted the anxiolytic effect in zebrafish. Flumazenil did not inhibit the anxiolytic effect of the PFD via the GABAergic system. This effect was reduced by a pretreatment with pizotifen and granisetron, and was not reversed after treatment with cyproheptadine. Molecular docking and dynamics studies confirmed the interaction of PFD with the 5-HT receptor.Communicated by Ramaswamy H. Sarma.
Pyrroloformamide (PFD), isolated from the marine Streptomyces sp. associated ascidian Eudistoma vannamei, showed no toxicity in adult zebrafish but reduced its locomotor activity.The structural elucidation of PFD was determined by the analysis of 1D and 2D NMR and HRESIMS data.The density functional theory (DFT) study confirmed the existence of two conformers as determined by NMR spectra.The serotonergic system modulated the anxiolytic effect of PFD via the 5-HT receptor in adult zebrafish.Molecular docking and dynamics studies confirmed the interaction of PFD with the 5-HT receptor.
Assuntos
Ansiolíticos , Animais , Ansiolíticos/farmacologia , Ansiolíticos/uso terapêutico , Peixe-Zebra , Serotonina , Flumazenil/farmacologia , Pizotilina , Simulação de Acoplamento Molecular , Granisetron , CiproeptadinaRESUMO
Introduction. Medical device colonization by pathogenic microorganisms is a risk factor for increasing infections associated with health care and, consequently, the morbidity and mortality of intubated patients. In Colombia, fungal colonization of endotracheal tubes has not been described, and this information could lead to new therapeutic options for the benefit of patients. Objective. To describe the colonizing fungi of the endotracheal tubes from patients in the intensive care unit, along with its antifungal sensitivity profile. Materials and methods. We conducted a descriptive, observational study in two health centers for 12 months. Endotracheal tubes were collected from patients in intensive care units. Samples were processed for culture, fungi identification, and antifungal sensitivity profile assessment. Results. A total of 121 endotracheal tubes, obtained from 113 patients, were analyzed: 41.32 % of the tubes were colonized by Candida albicans (64.62%), C. nonalbicans (30.77%), Cryptococcus spp. (3.08%) or molds (1.54%). All fungi evaluated showed a high sensitivity to antifungals, with a mean of 91%. Conclusion. Fungal colonization was found in the endotracheal tubes of patients under invasive mechanical ventilation. The antifungal sensitivity profile in these patients was favorable. A clinical study is required to find possible correlations between the colonizing microorganisms and infectivity.
Introducción. La colonización por microorganismos patógenos de los dispositivos médicos usados en las unidades de cuidados intensivos es un factor de riesgo para el aumento de infecciones asociadas con la atención en salud y, por lo tanto, al de la morbilidad y la mortalidad de los pacientes intubados. En Colombia, no se ha descrito la colonización por hongos de los tubos endotraqueales, con lo cual se podrían considerar nuevas opciones terapéuticas para el beneficio de los pacientes. Objetivo. Describir los hongos que colonizan los tubos endotraqueales de los pacientes en unidades de cuidados intensivos, junto con su perfil de sensibilidad a los antifúngicos. Materiales y métodos. Se realizó un estudio observacional, descriptivo, en dos centros hospitalarios durante 12 meses. Se recolectaron tubos endotraqueales de pacientes de las unidades de cuidados intensivos. Estos fueron procesados para cultivar e identificar hongos, y para establecer su perfil de sensibilidad a los antifúngicos. Resultados. Se analizaron 121 tubos endotraqueales obtenidos de 113 pacientes. De estos, el 41,32 % se encontró colonizado por los hongos Candida albicans (64,61 %), C. no-albicans (30,77 %), Cryptococcus spp. (3,08 %) o mohos (1,54 %). Todos los hongos evaluados presentaron una gran sensibilidad a los antifúngicos, con un promedio del 91 %. Conclusión. Se encontró colonización fúngica en los tubos endotraqueales de pacientes con asistencia respiratoria mecánica. El perfil de sensibilidad en estos pacientes fue favorable. Se requiere un estudio clínico para correlacionar los microorganismos colonizadores y su capacidad de generar infección.
Assuntos
Candida albicans , Granisetron , Colômbia , TolnaftatoRESUMO
ABSTRACT Introduction: This study was performed to evaluate the degree of 3-day chemotherapy-induced nausea and vomiting (CINV) in children with cancer who received highly emetogenic chemotherapy (HEC) to ascertain the efficacy of aprepitant single-dose on dayL 1 plus granisetron and dexamethasone (DEX). Methods: This clinical trial study was conducted on 120 patients in the age range of 5 to 18 years old who received chemotherapy. Patients were divided into two groups; Group A received aprepitant at 125 mg/kg on day 1 orally, followed by 80 mg/kg daily on days 2 and 3 and Group B received a single dose of aprepitant 125 mg/kg on day 1 orally and placebo on days 2 and 3. All groups received granisetron 3 mg/m2 on day 1 and DEX on days 1 to 3. The primary and secondary endpoints were to evaluate the proportion of patients with acute, delayed and overall CINV within each group. Results: There were no significant differences between the two groups for vomiting, nausea or the use of rescue therapy. The number of patients without vomiting on day 1 was similar in both groups (96.5% vs. 98.3%, respectively; p = 0.848). Conclusion: According to the results of this study, a single dose of aprepitant 125 mg/kg was as effective as administering three doses of aprepitant on 3 days. Therefore, the use of a single dose of aprepitant in combination with other standard treatment regimens to prevent CINV in children who received HEC was safe and efficacious and can be beneficial.
Assuntos
Humanos , Pré-Escolar , Criança , Adolescente , Vômito , Dexametasona , Granisetron , Aprepitanto , NáuseaRESUMO
BACKGROUND: Chagas Disease (ChD) is a Neglected Tropical Disease (NTD) affecting 6 to 7 million people worldwide, mostly from Latin America. In Argentina, a national control program has been implemented since 1962, yet there are still an estimated 1.6 million infected individuals. Control programs were based almost exclusively on entomological surveillance and chemical control of households and were not continuous given a lack of coordination and resources. Argentina´s ChD program was originally vertical and centralized; later, it was partially and, in general, unsuccessfully transferred to the provinces. Herein, we describe the implementation of a control program for ChD with an ecohealth approach in rural settlements around the city of Añatuya, Santiago del Estero. METHODS: The program included yearly household visits for entomological surveillance and control, health promotion workshops, and structural house improvements. Improved structures included internal and external walls and roofs, as well as the construction of water wells and latrines, and the organization and improvement of peri-domestic structures. Activities were carried out by specifically trained personnel except for house improvements, which were performed by the community, under technical guidance and provision of materials. Data was collected using standardized questionnaires for household characterization, entomological infestation status and chemical control activities. RESULTS: This program was continuously implemented since 2005 with high community participation and adherence, incorporating 13 settlements and 502 households. During the surveillance phase, 4,193 domiciliary inspections were performed, and both the intra- and peri-domestic infestation rate were reduced from 17.9% to 0.2% (P < 0.01) and from 20.4% to 3%, respectively. Additionally, 399 households were structurally improved. CONCLUSION: The program is still ongoing and, after 14 years of implementation, has built social networks and collaboration between implementers and beneficiaries with a reduction of T. infestans infestation in the intra- and peri-domicile. This reduction, especially inside the household, has enabled access to diagnosis and treatment of the population, with minimal risk of re-infection.
Assuntos
Doença de Chagas , Humanos , Argentina/epidemiologia , Doença de Chagas/epidemiologia , Doença de Chagas/prevenção & controle , Participação da Comunidade , Granisetron , Promoção da Saúde , Doenças NegligenciadasRESUMO
The control of micturition depends on reflex mechanisms, however, it undergoes modulation from cortex, pons and medullary areas. This study investigated if the activation of 5-HT3 receptors in the medulla influences the urinary bladder (UB) regulation in rats. Isoflurane female Wistar rats were submitted to catheterization of the femoral artery and vein for mean arterial pressure (MAP) and heart rate (HR) recordings and injection of drugs, respectively. The UB was cannulated for intravesical pressure (IP) measurement. The Doppler flow probe was placed around the left renal artery for renal conductance (RC) recordings. Phenylbiguanide (PB) and granisetron (GN) were injected into the 4th brain ventricle in rats with guide cannulas implanted 5 days prior to the experiments; or PB and GN were randomly injected intravenously or applied topically (in situ) on the UB. PB injection into 4th V significantly increased IP (68.67 ± 11.70%) and decreased MAP (-29 ± 6 mmHg) compared to saline (0.34 ± 0.64% and -2 ± 2 mmHg), with no changes in the HR and RC. GN injection into the 4th V did not significantly change the IP and RC compared to saline, nevertheless, significantly increased MAP (25 ± 4 mmHg) and heart rate (36 ± 9 bpm) compared to saline. Intravenous PB and GN only produced cardiovascular effects, whilst PB but not GN in situ on the UB evoked increase in IP (111.60 ± 30.36%). Therefore, the activation of 5HT-3 receptors in medullary areas increases the intravesical pressure and these receptors are involved in the phasic control of UB. In contrast, 5-HT3 receptors in the medulla oblongata are involved in the pathways of the tonic control of the cardiovascular system. The activation of 5-HT3 receptors in the bladder cause increase in intravesical pressure and this regulation seem to be under phasic control as the blockade of such receptors elicits no changes in baseline intravesical pressure.
Assuntos
Isoflurano , Receptores 5-HT3 de Serotonina , Ratos , Feminino , Animais , Bexiga Urinária , Granisetron , Ratos Wistar , Isoflurano/farmacologia , Bulbo/fisiologia , Pressão SanguíneaRESUMO
INTRODUCTION: Intra- and postoperative nausea, vomiting and shivering are mentioned as the most common problem following spinal anesthesia. The aim of this study is to compare two different doses of granisetron to control the shivering, nausea, and vomiting caused by spinal anesthesia in women undergoing cesarean section (C/S). METHOD: This study is a randomized, triple-blind clinical trial. The participants received 1-mg or 3-mg granisetron. Women who underwent elective C/S were enrolled. Inclusion criteria were ASA (American Society of Anesthesiologists) physical status grade I or II and age range of 18-40 years. Primary outcome was changes in the score of shivering, and nausea and vomiting. Secondary outcomes were Apgar score, mean arterial pressure, systolic blood pressure, diastolic blood pressure, temperature and heart rate. RESULTS: According to binary logistic regression, the incidence of shivering (6.9% vs. 1.5%; p-value = 0.049), and nausea and vomiting (19.2% vs. 9.2%; p-value = 0.024) was significantly higher in patients received 1-mg granisetron in comparison with 3-mg granisetron. Multinomial logistic regression showed that the occurrence of shivering, and nausea and vomiting were not associated with the dose of granisetron. There was no significant difference between the age and Apgar score of 1 (p = 0.908) and 5 (p = 0.843) minute(s) between the two groups. CONCLUSION: This study showed that although 3-mg of granisetron reduces the incidence of intra- and postoperative shivering, nausea and vomiting after spinal anesthesia in comparison with 1-mg of granisetron, the difference was not statistically significant.
Assuntos
Antieméticos , Granisetron , Adolescente , Adulto , Antieméticos/farmacologia , Antieméticos/uso terapêutico , Cesárea , Método Duplo-Cego , Feminino , Granisetron/farmacologia , Granisetron/uso terapêutico , Humanos , Náusea e Vômito Pós-Operatórios/epidemiologia , Náusea e Vômito Pós-Operatórios/prevenção & controle , Gravidez , Estremecimento , Adulto JovemRESUMO
CONTEXT: Several antiemetics have been used in children with acute gastroenteritis. However, there is still controversy over their use. OBJECTIVE: To determine the effectiveness and safety of antiemetics for controlling vomiting in children with acute gastroenteritis. DATA SOURCES: Medline, Embase, Cochrane Central Register of Controlled Trials, Cumulative Index to Nursing and Allied Health Literature, Latin America and the Caribbean Literature on Health Sciences, and gray literature, until December 2018. STUDY SELECTION: We selected randomized clinical trials comparing metoclopramide, ondansetron, domperidone, dexamethasone, dimenhydrinate, and granisetron. DATA EXTRACTION: Two reviewers independently screened abstracts and full texts, extracted the data, and assessed the risk of bias. We performed pairwise and network meta-analysis using the random-effects model. RESULTS: Twenty-four studies were included (3482 children). Ondansetron revealed the largest effect in comparison to placebo for cessation of vomiting (odds ratio = 0.28 [95% credible interval = 0.16 to 0.46]; quality of evidence: high) and for hospitalization (odds ratio = 2.93 [95% credible interval = 1.69 to 6.18]; quality of evidence: moderate). Ondansetron was the only intervention that reduced the need for intravenous rehydration and the number of vomiting episodes. When considering side effects, dimenhydrinate was the only intervention that was worse than placebo. LIMITATIONS: Most treatment comparisons had low- or very low-quality evidence, because of risk of biases and imprecise estimates. CONCLUSIONS: Ondansetron is the only intervention that revealed an effect on the cessation of vomiting, on preventing hospitalizations, and in reducing the need for intravenous rehydration. Ondansetron was also considered a safe intervention.
Assuntos
Antieméticos/uso terapêutico , Gastroenterite/complicações , Vômito/tratamento farmacológico , Doença Aguda , Antieméticos/efeitos adversos , Criança , Pré-Escolar , Dexametasona/uso terapêutico , Diarreia/induzido quimicamente , Dimenidrinato/uso terapêutico , Domperidona/uso terapêutico , Hidratação/estatística & dados numéricos , Granisetron/uso terapêutico , Hospitalização , Humanos , Lactente , Metoclopramida/uso terapêutico , Metanálise em Rede , Ondansetron/uso terapêutico , Ensaios Clínicos Controlados Aleatórios como Assunto , Análise de Regressão , Vômito/complicaçõesRESUMO
Abstract Background and objectives Reducing pain on injection of anesthetic drugs is of importance to every anesthesiologist. In this study we pursued to define if pretreatment by granisetron reduces the pain on injection of etomidate similar to lidocaine. Methods Thirty patients aged between 18 and 50 years of American Society of Anesthesiologists physical status class I or II, whom were candidates for elective laparoscopic cholecystectomy surgery were enrolled in this study. Two 20 gauge cannulas were inserted into the veins on the dorsum of both hands and 100 mL of normal saline was administered during a 10 min period from each cannula. Using an elastic band as a tourniquet, venous drainage of both hands was occluded. 2 mL of granisetron was administered into one hand and 2 mL of lidocaine 2% at the same time into the other hand. One minute later the elastic band was opened and 2 mL of etomidate was administered to each hand with equal rates. The patients were asked to give a score from 0 to 10 (0 = no pain, 10 = severe pain) to each the pain sensed in each hand. Results Two patients were deeply sedated after injection of etomidate and unable to answer any questions. The mean numerical rating score for injection pain of intravenously administered etomidate after intravenous granisetron was 2.3 ± 1.7, which was lower when compared with pain sensed due to intravenously administered etomidate after administration of lidocaine 2% (4.6 ± 1.8), p < 0.05. Conclusion The result of this study demonstrated that, granisetron reduces pain on injection of etomidate more efficiently than lidocaine.
Resumo Justificativa e objetivos A redução da dor causada pela injeção de anestésicos é importante para todos os anestesiologistas. Neste estudo buscamos definir se o pré-tratamento com granisetrona reduz a dor causada pela injeção de etomidato de forma semelhante à lidocaína. Métodos Trinta pacientes entre 18 e 50 anos, estado físico ASA I ou II (de acordo com a classificação da Sociedade Americana de Anestesiologistas) e candidatos à colecistectomia laparoscópica eletiva foram incluídos neste estudo. Duas cânulas de calibre 20 foram inseridas nas veias do dorso de ambas as mãos e 100 mL de soro fisiológico foram administrados durante 10 minutos através de cada cânula. Com um torniquete elástico, a drenagem venosa de ambas as mãos foi ocluída. Granisetrona (2 mL) foi administrado em uma das mãos e lidocaína a 2% (2 mL) na outra mão ao mesmo tempo. Após um minuto, o torniquete foi afrouxado e 2 mL de etomidato foram administrados em velocidade igual a cada uma das mãos. Solicitamos dos pacientes uma classificação de 0 a 10 para a dor sentida em cada uma das mãos (0 = sem dor, 10 = dor intensa). Resultados Dois pacientes estavam profundamente sedados após a injeção de etomidato e, portanto, incapazes de responder a qualquer pergunta. O escore médio de classificação da dor à injeção de etomidato administrado por via endovenosa após granisetrona intravenoso foi de 2,3 ± 1,7, o que foi menor em comparação com a dor sentida à administração intravenosa de etomidato após a administração de lidocaína a 2% (4,6 ± 1,8), p < 0,05. Conclusão O resultado deste estudo demonstrou que granisetrona reduz a dor causada pela injeção de etomidato com mais eficácia do que lidocaína.
Assuntos
Humanos , Masculino , Feminino , Adulto , Dor/induzido quimicamente , Dor/tratamento farmacológico , Granisetron/uso terapêutico , Anestésicos Intravenosos/efeitos adversos , Etomidato/efeitos adversos , Manejo da Dor/métodos , Lidocaína/uso terapêutico , Método Duplo-Cego , Injeções Intravenosas , Pessoa de Meia-IdadeRESUMO
BACKGROUND AND OBJECTIVES: Reducing pain on injection of anesthetic drugs is of importance to every anesthesiologist. In this study we pursued to define if pretreatment by granisetron reduces the pain on injection of etomidate similar to lidocaine. METHODS: Thirty patients aged between 18 and 50 years of American Society of Anesthesiologists physical status class I or II, whom were candidates for elective laparoscopic cholecystectomy surgery were enrolled in this study. Two 20 gauge cannulas were inserted into the veins on the dorsum of both hands and 100mL of normal saline was administered during a 10min period from each cannula. Using an elastic band as a tourniquet, venous drainage of both hands was occluded. 2mL of granisetron was administered into one hand and 2mL of lidocaine 2% at the same time into the other hand. One minute later the elastic band was opened and 2mL of etomidate was administered to each hand with equal rates. The patients were asked to give a score from 0 to 10 (0=no pain, 10=severe pain) to each the pain sensed in each hand. RESULTS: Two patients were deeply sedated after injection of etomidate and unable to answer any questions. The mean numerical rating score for injection pain of intravenously administered etomidate after intravenous granisetron was 2.3±1.7, which was lower when compared with pain sensed due to intravenously administered etomidate after administration of lidocaine 2% (4.6±1.8), p<0.05. CONCLUSION: The result of this study demonstrated that, granisetron reduces pain on injection of etomidate more efficiently than lidocaine.
Assuntos
Anestésicos Intravenosos/efeitos adversos , Etomidato/efeitos adversos , Granisetron/uso terapêutico , Lidocaína/uso terapêutico , Manejo da Dor/métodos , Dor/induzido quimicamente , Dor/tratamento farmacológico , Adulto , Método Duplo-Cego , Feminino , Humanos , Injeções Intravenosas , Masculino , Pessoa de Meia-IdadeRESUMO
INTRODUCCIÓN: El análisis de costo-efectividad de ondansetrón, alizaprida, domperidona, granisetrón, aprepitant, propofol, dexametasona, dimenhidrinato, metoclopramida y haloperidol para la profilaxis y/o tratamiento de pacientes con náusea y vómito en Colombia, se desarrolla en el marco del mecanismo técnico-científico para la ampliación progresiva del plan de beneficios y la definición de la lista de exclusiones, establecido en el artículo 15 de la Ley 1751 de 2015. Estas tecnologías fueron seleccionadas por la Dirección de Beneficios, Costos y Tarifas del Aseguramiento en Salud del Ministerio de Salud y Protección Social (MSPS), y remitidas al Instituto de Evaluación Tecnológica en Salud (IETS) para su evaluación. La náusea es una sensación desagradable, de asco intenso a los alimentos, o de vómito inminente, y está asociada a la disminución de la actividad motora gástrica, el incremento del tono de la pared duodenal y reflujo de su contenido al estómago, lo que causa su distensión. Ésta, se acompaña de manifestaciones del sistema nervioso autónomo como hiper-salivación, palidez, sudación, taquicardia y taquipnea El vómito, por su parte, es la expulsión fo
Assuntos
Humanos , Vômito/tratamento farmacológico , Dexametasona/uso terapêutico , Propofol/uso terapêutico , Ondansetron/uso terapêutico , Granisetron/uso terapêutico , Dimenidrinato/uso terapêutico , Domperidona/uso terapêutico , Aprepitanto/uso terapêutico , Haloperidol/uso terapêutico , Metoclopramida/uso terapêutico , Náusea/tratamento farmacológico , Avaliação em Saúde/economia , Eficácia , ColômbiaRESUMO
Orally disintegrating systems have carved a niche amongst the oral drug delivery systems due to the highest compliance of the patients, especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to withstand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. The purpose of this research was to mask the bitter taste of granisetron hydrochloride. To mask the taste Kollicoat(r) Smartseal 30D was used as coating polymer for pellet coating. The coated pellets of the drug was directly compressed with different superdisintegrant as AC-Di-Sol, Explotab and Kollidon CL in different concentration 5.0-7.5% w/w into an ODT. The prepared tablets were evaluated for hardness, friability, weight variation, wetting time, wet absorption ratio, in-vitro disintegration time and in vitro dissolution studies. Tablets exhibited quick disintegration characteristics with Kollidon CL in concentration 7.5% w/w i.e., within 20 seconds, which is characteristic of orally disintegrating dosage forms. More than 98% of drug was released from the formulations within 15 minutes. Formulations subjected to stability testing as per the ICH guidelines for 3 months, indicated stability with no change in taste, hardness, drug content, disintegration time and dissolution profiles. Thus, the results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated dosage forms in the oral cavity.
Sistemas de desintegração oral têm um nicho entre os sistemas de administração de medicamentos por via oral devido à maior aceitação dos pacientes, especialmente os de geriatria e pediatria. Além disso, pacientes que sofrem de disfagia, enjoo de movimento, emese repetida e distúrbios mentais preferem estes medicamentos porque não podem engolir grande quantidade de água. Além disso, os fármacos que exibem absorção satisfatória a partir da mucosa oral ou que se destinam a ação farmacológica imediata podem ser vantajosamente formulados nestas formas de dosagem. No entanto, a formulação destas formas farmacêuticas exige-lhes resistência mecânica suficiente para suportar os rigores do manuseio e capacidade de desintegrar dentro de alguns segundos em contato com a saliva. O objetivo desta pesquisa foi o de mascarar o gosto amargo de cloridrato de granisetrona. Para mascarar o sabor, utilizou-se Kollicoat smartseal 30D como polímero para io revestimento dos péletes. Os péletes revestidos do fármaco foram diretamente comprimidos com superdesintegrante diferente como Ac-Di-Sol, Explotab e Kollidon CL, em diferentes concentrações 5.0-7.5% m/m em comprimidos de dispersão oral (ODT). Os comprimidos preparados foram avaliados quanto à dureza, friabilidade, variação de peso, ao tempo de umedecimento, à razão de absorção de umidade, ao tempo de desintegração in vitro e em estudos de dissolução in vitro. Os comprimidos apresentaram características de desintegração rápida com Kollidon CL, em concentração de 7,5% m/m, ou seja, dentro de 20 segundos, o que é característico para formas farmacêuticas de desintegração oral. Mais do que 98% do fármaco foi liberado a partir das formulações no prazo de 15 minutos. Formulações submetidas a testes de estabilidade de acordo com as diretrizes da ICH por 3 meses indicaram estabilidade sem alteração no sabor, dureza, teor de fármaco, tempo de desintegração e perfis de dissolução. Assim, os resultados demonstraram que o mascaramento de gosto foi bem-sucedido e atingiu-se rápida desintegração das formas de dosagem na cavidade oral.
Assuntos
Comprimidos/farmacocinética , Química Farmacêutica , Granisetron/análise , Administração Bucal , Vias de Administração de MedicamentosRESUMO
Evaluar y caracterizar el abordaje farmacoterapéutico antiemético en el periodo postoperatorio en pacientes adultos sometidos a cirugía en el Hospital Clínica Bíblica, hospital privado en Costa Rica. Métodos: Se seleccionaron pacientes, con edades entre 18 y 75 años, sometidos a cirugía, en quienes se había utilizado algún antiemético profiláctico al proceso quirúrgico, excluyéndose los pacientes que permanecieran hospitalizados menos de 24 horas tras la cirugía. Resultados: Dentro de la terapia profiláctica antiemética utilizada en este Hospital, se incluyó: granisetrón, metoclopramida, dexametasona, dimenhidrinato, entre otros; el granisetrón fue el antiemético más utilizado en un 81 por ciento de los casos, solo o en combinación. El uso de la dexametasona junto con el granisetrón fue la combinación más utilizada en un 57 por ciento. Sin hacer asociación al procedimiento quirúrgico, las náuseas y vómitos postoperatorios se presentaron en un 12 por ciento con el granisetrón, en un 25 por ciento con la metoclopramida, en un 9 por ciento con el dimenhidrinato, en un 13 por ciento con la dexametasona y en un 14 por ciento con otros antieméticos. Las cirugías que presentaron más incidencia de NVPO fueron las cirugías ortopédicas en un 30 por ciento, y las cirugías laparoscópicas en un 28 por ciento. En los casos en los que se utilizó fentanyl como anestésico, se presentaron vómitos en un 18 por ciento de los pacientes, mientras que en los casos en que no se utilizó fentanyl, el porcentaje de NVPO fue del 9 por ciento. Conclusión: A pesar del amplio uso de antieméticos profilácticamente, las náuseas y vómitos postoperatorios siguen presentándose en los pacientes de este Hospital. No se ha encontrado un algoritmo que permita prevenir totalmente las náuseas y vómitos postoperatorios, a pesar de la gran cantidad de conocimientos adquiridos en este campo. Se debe tomar en cuenta el riesgo individual de cada paciente y la satisfacción de este...
To evaluate and characterize the pharmaco-therapeutic approach with antiemetics during the postoperative, in adult patients undergoing surgery at a private hospital in Costa Rica(Hospital Clinica Biblica) Methods: This is an observational, prospective and cohort study. Those patients who had surgery and received antiemetic prophylaxis before the procedure were selected (ages between 18 and 75 years) excluding those who had hospitalization shorter than 24 hours.Results: Prophylactic antiemetic therapy in this private hospital utilizes granisetron, metoclopramide, dexamethasone, and dimenhydrinate, Granisetron, either alone or incombination, was the most used antiemetic in 81%. The combination most commonly used was dexamethasone and granisetron (57%). Without considering the surgical procedure, the incidence of postoperative nausea and vomiting (PONV) was 12% in patients taking granisetron, 25% with metoclopramide, 9% with dimenhydrinate, 13% with dexamethasone and 14% with otherantiemetics. On the other hand, looking at the procedure, the incidence of PONV in patients undergoing orthopedic surgery was by 30%, and 28% in those after laparoscopic surgery Finally,in cases in which fentanyl was used as an anesthetic 18% of the patients presented PONV, whereas in patients cases were fentanyl was not used, the rate of was 9%. Conclusion: Despite the widespread use of prophylactic antiemetics, PONV is still seen in thepatients at this private hospital. In spite of the wealth of knowledge in this field, physicians have not yet found an algorithm capable of the total prevention of PONV. Individual risks and patient`s satisfaction should be taken into account. Further research on this matter must continue in orderto unify and improve criteria of PONV treatment.
Assuntos
Humanos , Masculino , Feminino , Adulto , Pessoa de Meia-Idade , Antieméticos/análise , Antieméticos/uso terapêutico , Dexametasona , Cirurgia Geral , Granisetron , Metoclopramida , Náusea e Vômito Pós-Operatórios/tratamento farmacológico , Complicações Pós-Operatórias , Costa RicaRESUMO
INTRODUCCIËN: Las náuseas y vómitos por quimioterapia (NVIQ) constituyen una complicación importante. La introducción de los antiserotoninérgicos 5HT3 (AR 5HT3 ) unida a los esteroides, ha posibilitado un mayor control de estos síntomas. OBJETIVO: evaluar económicamente dos alternativas para el tratamiento antiemético en cáncer. MÉTODOS: se utilizaron varias técnicas de evaluación económica para dos alternativas de tratamiento antiemético. Para la primera línea, la técnica de minimización de costos (MC), que incluyó los esquemas de granisetron más dexametasona y ondansetron más dexametasona. El análisis de costoefectividad (ACE) evaluó el tratamiento alternativo después del fallo del esquema que contiene ondansetron, se realizaron los análisis de relación costo-efectividad medio (ACEM) y costo-efectividad incremental (ACEI). También análisis de sensibilidad. RESULTADOS: para los esquemas de tratamientos utilizados en la primera línea por cada paciente tratado, se logró un ahorro de $0,76 en la quimioterapia moderadamente emetógena (QME) y la quimioterapia altamente emetógena (QAE). En el ACEM, la opción que utilizó ondansetron como tratamiento de segunda línea para la QME es de $22,77 y de $4,034 para el esquema que utilizó el granisetron, para cada caso controlado. La terapia para QAE que utilizó ondansetron necesita $ 65,41 y la opción que utilizó granisetron $ 13,45, para cada paciente controlado respectivamente. En el ACEI se obtuvo un resultado no satisfactorio para el esquema que contiene ondansetron de $1,490/ caso adicional controlado en la QME y de $3,140/ caso adicional controlado para la QAE. CONCLUSIONES: el tratamiento antiemético que produjo mayor ahorro económico como terapia antiemética de primera línea es el que utilizó ondansetron, y en segunda línea el esquema que utilizó granisetron
INTRODUCTION: the occurrence of nauseas and vomiting from chemotherapy are a significant complication. With appearance of antiserotoninergics 5HT3 (AR 5HT3) combined with steroids, have allowed a great control of these symptoms. OBJECTIVE: The aim of present paper is to asses in a economic way two alternatives for antiemetic tratment in cancer. METHODS: Some techniques of economical assessment to two alternatives of antiemetic treatment were used. For the first line, the cost minimization (CM) technique including the Granisetron hydrochloride schemes plus Dexamethasone and Ondansetron hydrochloride plus Dexamethasone. The cost-effectiveness analysis (CEA) assessed the alternative treatment after the scheme failure containing Ondansetron; we performed mean cost-effectiveness (MCE) and incremental cost-effectiveness (ICE) analyses, as well as the sensitivity analysis. RESULTS: For the treatment schemes used in the first line by patient with treatment, it is possible to achieve a saving of $0.76 in the moderately emethogenic chemotherapy (MECM) and the highly emethogenic chemotherapy (HECT). In MCE, the option using Ondansetron as a second line treatment for MECM is of $22.77 and of $4.034 for scheme uses Granisetron for each controlled case. Therapy for HECT using Ondansetron needs percent65,41 and option using Granisetron needs $13.45 for each controlled patient, respectively. In the case of ICE a non-satisfactory result of $1.490 for scheme containing Ondansetron/controlled additional case in MECM, and of $3.140/controlled additional case for HECT. CONCLUSIONS: Antiemetic treatments with a higher economical save as first-line antiemetic therapy is that using Ondansetron, and in second line the scheme using Granisetron
Assuntos
Humanos , Antineoplásicos/efeitos adversos , Antieméticos/uso terapêutico , Granisetron/economia , Ondansetron/economia , Custos de Medicamentos/estatística & dados numéricosRESUMO
JUSTIFICATIVA E OBJETIVOS: A incidência de náuseas e vômitos pós-operatórios (NVPO) gira em torno de 30 por cento. A profilaxia de NVPO foi objeto de múltiplos estudos, tanto para tentar diminuir esse problema como para comparar o índice custo-benefício do tratamento utilizado. Esse estudo comparou a eficácia de cinco fármacos antieméticos em apendicectomia. MÉTODO: Estudo clínico prospectivo controlado, duplamente encoberto de 150 pacientes ASA I e II com IMC < 30, submetidos a apendicectomia. Os pacientes foram divididos em seis grupos: Grupo 1 (n = 25): 5 mL solução fisiológica a 0,9 por cento; Grupo 2 (n = 25): droperidol 0,625 mg; Grupo 3 (n = 25): metoclopramida 20 mg; Grupo 4 (n = 25): tropisetron 5 mg; Grupo 5 (n = 25): granisetron 1 mg; Grupo 6 (n = 25): dexametasona 4 mg. A monitoração foi realizada com ECG, PANI, SpO2, P ET CO2, analisador de gases anestésicos e estimulador de nervo periférico. Foi avaliada a presença de NVPO, complicações e o grau de satisfação nas primeiras 48 horas. RESULTADOS: O droperidol apresentou incidência 4 por cento de NVPO, os grupos de granisetron, tropisetron e metoclopramida apresentaram 12 por cento de NVPO (p < 0,05). O grupo de dexametasona apresentou 24 por cento e o controle 28 por cento de NVPO. CONCLUSÕES: Na profilaxia de NVPO em apendicectomia de urgência o uso de baixas doses de droperidol foi mais efetivo que o dos outros fármacos.
BACKGROUND AND OBJECTIVES: It is calculated that the incidence of postoperative nausea and vomiting (PONV) is approximately 30 percent. The prophylaxis of PONV has been the subject of several studies, both to decrease this problem and to compare the cost-benefit ration of the treatment used. The objective of this study was to compare the efficacy of 5 antiemetic drugs with a control group in emergency appendectomy. METHODS: A controlled, double-blind, prospective study with 150 patients, ASA I and II, BMI < 30, undergoing appendectomy, was undertaken. Patients were divided in six groups: Group 1 (n = 25): 5 mL of normal saline; Group 2 (n = 25): 0.625 mg of droperidol; Group 3 (n = 25): 20 mg of metoclopramide; Group 4 (n = 25): 5 mg of tropisetron; Group 5 (n = 25): 1 mg of granisetron; Group 6 (n = 25): 4 mg of dexamethasone. Monitoring included ECG, non-invasive blood pressure, O2 saturation, P ET CO2, anesthetic gas analyzer and peripheral nerve stimulator. The presence of PONV, complications and the degree of satisfaction in the first 48 hours were evaluated. RESULTS: The incidence of PONV in the droperidol group was 4 percent while in the granisetron, tropisetron and metoclopramide groups it was 12 percent (p < 0.05). The dexamethasone group had a 24 percent incidence and the control group 28 percent. CONCLUSIONS: Low doses of droperidol were more effective in the prophylaxis of PONV in emergency appendectomy than the other drugs.
JUSTIFICATIVA Y OBJETIVOS: La incidencia de náuseas y vómitos peri operatorios (NVPO) se estima en un 30 por ciento. La profilaxis de NVPO ha sido objetivo de múltiples estudios, tanto para intentar disminuir este problema como a su vez comparar índice costo-beneficio de la terapia utilizada. Este estudio evalúa la utilización de 5 fármacos antieméticos en relación a grupo control para apendicectomía de urgencia. MÉTODO: Estudio clínico prospectivo controlado, doble ciego de 150 pacientes ASA I y II con IMC < 30, beneficiarios de apendicectomía. Los pacientes fueron divididos en seis grupos: Grupo 1 (n = 25): 5 ml solución salina; Grupo 2 (n = 25): droperidol 0,625 mg; Grupo 3 (n = 25): metoclopramida 20 mg; Grupo 4 (n = 25): tropisetrón 5 mg; Grupo 5 (n = 25): granisetrón 1 mg; Grupo 6 (n = 25): dexametasona 4 mg. El monitoreo se realizó con ECG, NIBP, SATO2, P ET CO2, analizador de gases anestésicos y ENP. Se evaluó la presencia de NVPO, complicaciones y grado de satisfacción en las primeras 48 horas. RESULTADOS: Droperidol presentó un 4,0 por ciento de NVPO en comparación con los grupos de granisetrón, tropisetrón y metoclopramida que presentaron un 12,0 por ciento de NVPO (p < 0,05). El grupo de dexametasona presento 24,0 por ciento y el control un 28,0 por ciento de NVPO. CONCLUSIONES: En la profilaxis para NVPO en la apendicectomía de urgencia se muestra más efectivo el uso de dosis bajas de droperidol en comparación con otros fármacos.
Assuntos
Adolescente , Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Adulto Jovem , Abdome/cirurgia , Antieméticos/uso terapêutico , Náusea e Vômito Pós-Operatórios/prevenção & controle , Método Duplo-Cego , Dexametasona/uso terapêutico , Droperidol/uso terapêutico , Granisetron/uso terapêutico , Indóis/uso terapêutico , Metoclopramida/uso terapêutico , Estudos Prospectivos , Adulto JovemRESUMO
BACKGROUND AND OBJECTIVES: It is calculated that the incidence of postoperative nausea and vomiting (PONV) is approximately 30%. The prophylaxis of PONV has been the subject of several studies, both to decrease this problem and to compare the cost-benefit ration of the treatment used. The objective of this study was to compare the efficacy of 5 antiemetic drugs with a control group in emergency appendectomy. METHODS: A controlled, double-blind, prospective study with 150 patients, ASA I and II, BMI < 30, undergoing appendectomy, was undertaken. Patients were divided in six groups: Group 1 (n = 25): 5 mL of normal saline; Group 2 (n = 25): 0.625 mg of droperidol; Group 3 (n = 25): 20 mg of metoclopramide; Group 4 (n = 25): 5 mg of tropisetron; Group 5 (n = 25): 1 mg of granisetron; Group 6 (n = 25): 4 mg of dexamethasone. Monitoring included ECG non-invasive blood pressure, O2 saturation, P(ET)CO2, anesthetic gas analyzer and peripheral nerve stimulator. The presence of PONV complications and the degree of satisfaction in the first 48 hours were evaluated. RESULTS: The incidence of PONV in the droperidol group was 4% while in the granisetron, tropisetron and metoclopramide groups it was 12% (p < 0.05). The dexamethasone group had a 24% incidence and the control group 28%. CONCLUSIONS: Low doses of droperidol were more effective in the prophylaxis of PONV in emergency appendectomy than the other drugs.
Assuntos
Abdome/cirurgia , Antieméticos/uso terapêutico , Náusea e Vômito Pós-Operatórios/prevenção & controle , Adolescente , Adulto , Idoso , Dexametasona/uso terapêutico , Método Duplo-Cego , Droperidol/uso terapêutico , Feminino , Granisetron/uso terapêutico , Humanos , Indóis/uso terapêutico , Masculino , Metoclopramida/uso terapêutico , Pessoa de Meia-Idade , Estudos Prospectivos , Tropizetrona , Adulto JovemRESUMO
Introducción y objetivos: La incidencia de náuseas y vómitos posoperatorios (NVPO) se estima en un 30 por ciento. La profilaxis de NVPO ha sido objetivo de múltiples estudios, tanto para intentar disminuir este problema como para comparar el índice costo-beneficio de la terapia utilizada. En este estudio se compara, evaluando los índices costo/beneficio, la eficacia de cinco fármacos antieméticos utilizados para apendicectomía de urgencia con la de un grupo control. Pacientes y método: Estudio clínico prospectivo controlado, doble ciego, de 150 pacientes ASA I-II con IMC<30, sometidos a apendicectomía. Los pacientes fueron divididos en seis grupos; Grupo 1 (n= 25): 5 ml de solución salina; Grupo 2 (n= 25): droperidol, 0,625 mg; Grupo 3 (n= 25): metoclopramida, 20 mg; Grupo 4 (n= 25): tropisetrón, 5 mg; Grupo 5 (n= 25): granisetrón,1 mg; Grupo 6 (n= 25): dexametasona, 4 mg. El monitoreo se realizó con ECG, NIBP, SATO2, EtCO2, analizador de gases anestésicos y ENP. Se evaluaron: la presencia de NVPO, las complicaciones y el grado de satisfacción en las primeras 48 horas. Resultados: La incidencia de NVPO en el grupo del droperidol fue de un 4,0 por ciento, mientras que en los grupos de granisetrón, tropisetrón y metoclopramida fue de 12,0 por ciento (p < 0.05). En el grupo de la dexametasona y en el de control se observó una incidencia de NVPO de 24,0 y 28,0 por ciento respectivamente. Conclusiones: En la profilaxis para NVPO en apendicectomía de urgencia, el uso de dosis bajas de doperidol es más efectivo que el empleo de otros fármacos, siendo excelente su índice costo-beneficio.
Assuntos
Humanos , Adulto , Pessoa de Meia-Idade , Apendicectomia , Antieméticos/uso terapêutico , Náusea e Vômito Pós-Operatórios/epidemiologia , Náusea e Vômito Pós-Operatórios/prevenção & controle , Anestesia Geral/efeitos adversos , Anestesia Geral/métodos , Análise Custo-Benefício , Dexametasona/uso terapêutico , Droperidol/uso terapêutico , Emergências , Granisetron , Indóis/uso terapêutico , Complicações Pós-OperatóriasRESUMO
Introducción y objetivos: La incidencia de náuseas y vómitos posoperatorios (NVPO) se estima en un 30 por ciento. La profilaxis de NVPO ha sido objetivo de múltiples estudios, tanto para intentar disminuir este problema como para comparar el índice costo-beneficio de la terapia utilizada. En este estudio se compara, evaluando los índices costo/beneficio, la eficacia de cinco fármacos antieméticos utilizados para apendicectomía de urgencia con la de un grupo control. Pacientes y método: Estudio clínico prospectivo controlado, doble ciego, de 150 pacientes ASA I-II con IMC<30, sometidos a apendicectomía. Los pacientes fueron divididos en seis grupos; Grupo 1 (n= 25): 5 ml de solución salina; Grupo 2 (n= 25): droperidol, 0,625 mg; Grupo 3 (n= 25): metoclopramida, 20 mg; Grupo 4 (n= 25): tropisetrón, 5 mg; Grupo 5 (n= 25): granisetrón,1 mg; Grupo 6 (n= 25): dexametasona, 4 mg. El monitoreo se realizó con ECG, NIBP, SATO2, EtCO2, analizador de gases anestésicos y ENP. Se evaluaron: la presencia de NVPO, las complicaciones y el grado de satisfacción en las primeras 48 horas. Resultados: La incidencia de NVPO en el grupo del droperidol fue de un 4,0 por ciento, mientras que en los grupos de granisetrón, tropisetrón y metoclopramida fue de 12,0 por ciento (p < 0.05). En el grupo de la dexametasona y en el de control se observó una incidencia de NVPO de 24,0 y 28,0 por ciento respectivamente. Conclusiones: En la profilaxis para NVPO en apendicectomía de urgencia, el uso de dosis bajas de doperidol es más efectivo que el empleo de otros fármacos, siendo excelente su índice costo-beneficio. (AU)
Assuntos
Humanos , Adulto , Pessoa de Meia-Idade , Apendicectomia , Náusea e Vômito Pós-Operatórios/epidemiologia , Náusea e Vômito Pós-Operatórios/prevenção & controle , Antieméticos/uso terapêutico , Anestesia Geral/efeitos adversos , Anestesia Geral/métodos , Complicações Pós-Operatórias , Droperidol/uso terapêutico , Dexametasona/uso terapêutico , Indóis/uso terapêutico , Granisetron , Análise Custo-Benefício , EmergênciasRESUMO
Several studies demonstrated the involvement of 5-hydroxytryptamine (5-HT) and its different receptor subtypes in the modulation of neurotransmission of cardiovascular reflexes in the nucleus tractus solitarii (NTS). Moreover, anatomic evidence suggests that nucleus raphe obscurus (ROb) is a source of 5-HT-containing terminals within the NTS. In the present study we investigated the possible changes in the cardiovascular responses to peripheral chemoreceptor activation by potassium cyanide (KCN, i.v.) following ROb stimulation with L-glutamate (10 nmol/50 nL) and also whether 5-HT3 receptors in the caudal commissural NTS are involved in this neuromodulation. The results showed that stimulation of the ROb with L-glutamate in awake rats (n=15) produced a significant reduction in the bradycardic response 30 s after the microinjection (-182+/-19 vs -236+/-10 bpm; Wilcoxon test) but no changes in the pressor response to peripheral chemoreceptor activation (43+/-4 vs 51+/-3 mmHg; two-way ANOVA) in relation to the control. Microinjection of 5--HT3 receptors antagonist granisetron (500 pmol/50 nL), but not the vehicle, into the caudal commissural NTS bilaterally prevented the reduction of chemoreflex bradycardia in response to microinjection of L-glutamate into ROb. These data indicate that 5-HT-containing projections from ROb to the NTS play an inhibitory neuromodulatory role in the chemoreflex evoked bradycardia by releasing 5-HT and activating 5-HT3 receptors in the caudal NTS.
Assuntos
Bradicardia/metabolismo , Células Quimiorreceptoras/metabolismo , Coração/inervação , Receptores 5-HT3 de Serotonina/metabolismo , Reflexo/fisiologia , Núcleo Solitário/metabolismo , Animais , Pressão Sanguínea/efeitos dos fármacos , Células Quimiorreceptoras/efeitos dos fármacos , Estado de Consciência , Ácido Glutâmico/administração & dosagem , Granisetron/administração & dosagem , Frequência Cardíaca/efeitos dos fármacos , Injeções Intraventriculares , Masculino , Microinjeções , Vias Neurais/metabolismo , Ratos , Ratos Wistar , Receptores 5-HT3 de Serotonina/efeitos dos fármacos , Reflexo/efeitos dos fármacos , Antagonistas da Serotonina/administração & dosagem , Núcleo Solitário/efeitos dos fármacosRESUMO
BACKGROUND: 5HT-3 antagonists and corticosteroids control less than 50% of delayed chemotherapy induced nausea and vomiting (CINV) episodes. MATERIALS AND METHODS: Two pilot phase II studies were conducted at our institution in which all patients received ondansetron 16 mg and dexamethasone 20 mg before highly and moderately emetogenic chemotherapy on day 1. Patients on study 1 received metoclopramide 10 mg PO q8 h, granisetron 0.5 mg PO QD and dexamethasone 8 mg QD on days 2 and 3, whereas only metoclopramide was continued on the same schedule on day 4. On study 2, patients received the same medications, but no drugs were given on day 2, and the same treatment schedule was given to them but from days 3 to 5 instead. Patients were interviewed on days 1 and 6. RESULTS: Twenty-one patients participated on each study. There were no significant clinical differences between these two studied populations. Complete CINV control occurred from days 2 to 5 in 23.1% (95% CI: 8 to 47%) on study 1 vs 61.9% (95% CI: 38 to 81%) of the patients on study 2. By logistic regression, complete CINV control was correlated significantly with antiemetic treatment group (p=0.011) even when we considered only patients who achieved complete CINV control during the first 24 h (p=0.031). CONCLUSIONS: Skipping day 2 antiemetic medications does not seem to worsen delayed CINV control and may even improve it, perhaps by avoiding tachyphylaxis to these medications. A randomized controlled study is in progress to confirm these results.
Assuntos
Antieméticos/administração & dosagem , Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos , Hipersensibilidade Tardia/induzido quimicamente , Náusea/induzido quimicamente , Náusea/prevenção & controle , Vômito/induzido quimicamente , Vômito/prevenção & controle , Adolescente , Adulto , Idoso , Análise de Variância , Brasil , Dexametasona/administração & dosagem , Hipersensibilidade a Drogas/etiologia , Hipersensibilidade a Drogas/prevenção & controle , Feminino , Granisetron/administração & dosagem , Humanos , Hipersensibilidade Tardia/prevenção & controle , Modelos Logísticos , Masculino , Metoclopramida/administração & dosagem , Pessoa de Meia-Idade , Ondansetron/administração & dosagem , Projetos Piloto , Qualidade de Vida , Projetos de Pesquisa , Antagonistas da Serotonina/administração & dosagem , Resultado do TratamentoRESUMO
CONTEXT AND OBJECTIVE: Chemotherapy-induced emesis is a limiting factor in treating children with malignancies. Intensive chemotherapy regimens along with emetogenic drug administration have increased the frequency and severity of emesis and nausea. Our study was designed to consider the importance of this problem and the need for improvement in emesis treatment for patients receiving chemotherapy. Our objective was to compare the efficacy and safety of the antiemetic drug granisetron and a regimen of metoclopramide plus dimenhydrinate. DESIGN AND SETTING: Open, prospective and randomized study at Instituto de Oncologia Pediátrica, Department of Pediatrics, Universidade Federal de São Paulo. METHODS: From February to August 1994, 26 patients (mean age: 14 years) with osteosarcoma received 80 chemotherapy cycles of iphosphamide (2,500 mg/m2) plus epirubicin (75 mg/m2) or carboplatin (600 mg/m2), or epirubicin (75 mg/m2) plus carboplatin (600 mg/m2). Eighty chemotherapy treatments were analyzed regarding nausea and vomiting control. Patients were randomized to receive either a single dose of granisetron (50 microg/kg) or metoclopramide (2 mg/kg) plus dimenhydrinate (5 mg/kg infused over eight hours). Emesis and nausea were monitored for 24 hours by means of the modified Morrow Assessment of Nausea and Emesis. Statistical analysis utilized the chi-squared, Student t and Mann-Whitney tests, plus data exploration techniques. RESULTS: 62.5% of the patients undergoing chemotherapy responded completely to granisetron, whereas 10% responded to metoclopramide plus dimenhydrinate (p < 0.0001). No severe adverse reactions were found in either of the treatments given. CONCLUSION: In children and adolescents with osteosarcoma, granisetron was safe and more efficient than metoclopramide plus dimenhydrinate for controlling chemotherapy-induced emesis and nausea.