RESUMEN
Triprolidine, a first-generation antihistamine for allergic rhinitis, has a shorter half-life and fewer persistent effects relative to other antihistamines and may be useful in the treatment of temporary sleep disturbance. Patients aged ≥18 years old were randomized 1:1:1 to receive either triprolidine 2.5 mg (n = 65), triprolidine 5 mg (n = 66), or placebo (n = 67) on 3 consecutive nights. Sleep disturbance index was monitored via wrist actimeter. Subjective measures were assessed via diary card. Triprolidine 2.5 mg had a significantly lower sleep disturbance index versus placebo on night 1 (P = .02); however, when adjusted for outliers, sleep disturbance index did not significantly differ between either dose of triprolidine versus placebo on night 1. Adjusted sleep disturbance index was significantly lower with triprolidine 2.5 and 5 mg versus placebo on night 3 (P = .0017 and P = .011, respectively) and for the mean of all 3 nights (P = .01 and P = .015, respectively). Sleep latency was significantly improved for triprolidine 2.5 mg versus placebo on nights 2 and 3 and for the mean of all 3 nights and for triprolidine 5 mg versus placebo for the mean of all 3 nights. Subjective measures showed those on both doses of triprolidine felt more refreshed on awakening versus placebo for the mean of all 3 nights, with no increase in daytime sleepiness. The frequency of adverse events was similar across groups. The optimum dose of triprolidine for treatment of temporary sleep disturbance was 2.5 mg. There were improvements in both objective and subjective measures of sleep quality versus placebo, with no safety concerns raised.
Asunto(s)
Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Trastornos del Sueño-Vigilia/tratamiento farmacológico , Triprolidina/uso terapéutico , Adulto , Relación Dosis-Respuesta a Droga , Método Doble Ciego , Femenino , Antagonistas de los Receptores Histamínicos H1/administración & dosificación , Antagonistas de los Receptores Histamínicos H1/efectos adversos , Humanos , Masculino , Persona de Mediana Edad , Latencia del Sueño/efectos de los fármacos , Calidad del Sueño , Triprolidina/administración & dosificación , Triprolidina/efectos adversosRESUMEN
The increase in survival rate of ß-thalassemia (ß-thal) patients allowed for the appearance and manifestation of several complications in almost every organ system. Priapism in ß-thal patients is rarely reported in the literature. We herein report and investigate the occurrence of two cases of priapism in two young patients with ß-thal intermedia (ß-TI). The potential mechanisms are due to either a cellular mechanism involving a thrombus obstructing the efferent venules of the corpora cavernosa leading to priapism, or a recently elucidated functional mechanism that causes alteration of nitric oxide (NO) response of the penis, ultimately causing priapism. This should incite clinicians for a close follow-up and monitoring of high risk patients who are susceptible to developing priapism.
Asunto(s)
Priapismo/etiología , Talasemia beta/fisiopatología , Antagonistas Adrenérgicos beta/uso terapéutico , Adulto , Terapia Combinada , Combinación de Medicamentos , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Humanos , Masculino , Priapismo/prevención & control , Propranolol/uso terapéutico , Seudoefedrina/uso terapéutico , Índice de Severidad de la Enfermedad , Resultado del Tratamiento , Triprolidina/uso terapéutico , Talasemia beta/tratamiento farmacológico , Talasemia beta/terapiaRESUMEN
The central histaminergic neuronal system is a powerful modulator of brain activity, and its functional disturbance is related to e.g. epilepsy. We have recently shown in the slice culture system that histaminergic neurons attenuate kainic acid (KA)-induced epileptiform activity and neuronal damage in the hippocampus through histamine 1 (H1) receptors. We now further examined the role of H1 receptors in the regulation of KA-induced seizures and neuronal damage in immature 9-day-old H1 receptor knock out (KO) mice. In the H1 receptor KO mice, behavioral seizures were significantly more severe and duration of seizures was significantly longer when compared to the wild type (WT) mice at the KA dose of 2mg/kg. Moreover, neuronal damage correlated with seizure severity, and it was significantly increased in the thalamus and retrosplenial granular cortex (RGC) of the KO mice. The H1 receptor antagonist triprolidine treatment supported these findings by showing significantly increased seizures severity and neuronal damage in the septum, thalamus, CA3 region of the hippocampus, and RGC in the KA-treated WT mice. Our present novel findings suggest that H1 receptors play a pivotal role in the regulation of seizure intensity and duration as well as seizure-induced neuronal damage in the immature P9 mice.
Asunto(s)
Susceptibilidad a Enfermedades/fisiopatología , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Receptores Histamínicos H1/metabolismo , Convulsiones/tratamiento farmacológico , Triprolidina/uso terapéutico , Animales , Animales Recién Nacidos , Encéfalo/metabolismo , Encéfalo/patología , Recuento de Células/métodos , Distribución de Chi-Cuadrado , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Fluoresceínas , Ácido Kaínico , Ratones , Ratones Endogámicos C57BL , Ratones Noqueados , Compuestos Orgánicos , Receptores Histamínicos H1/deficiencia , Convulsiones/inducido químicamente , Convulsiones/genética , Convulsiones/patologíaRESUMEN
Clinical trials often identify two endpoints or response measures of interest. Depending on the drugs and the disease, the endpoints may be correlated or uncorrelated, reflect efficacy or safety, or one or both may be considered as primary. For visualization, plots of each endpoint from baseline to the end of the trial are presented for each treatment group. This paper illustrates the usefulness of developing bivariate, composite plots of both endpoints jointly. Two applications are presented: one of a fixed combination drug for treating allergic rhinitis, and the other of a dose comparison trial in duodenal ulcer.
Asunto(s)
Determinación de Punto Final , Resistencia de las Vías Respiratorias/efectos de los fármacos , Antialérgicos/uso terapéutico , Antiulcerosos/uso terapéutico , Cimetidina/uso terapéutico , Ensayos Clínicos como Asunto , Interpretación Estadística de Datos , Relación Dosis-Respuesta a Droga , Combinación de Medicamentos , Úlcera Duodenal/tratamiento farmacológico , Humanos , Descongestionantes Nasales/uso terapéutico , Seudoefedrina/uso terapéutico , Ensayos Clínicos Controlados Aleatorios como Asunto , Rinitis Alérgica Estacional/tratamiento farmacológico , Triprolidina/uso terapéuticoRESUMEN
BACKGROUND: Petasin (Ze 339) was recently introduced on the market as a potent herbal antiallergic drug for treatment of respiratory allergies such as hay fever. Few clinical studies have been performed so far addressing the clinical effectiveness of Ze 339. OBJECTIVE: To evaluate the antiallergic properties of Ze 339 using skin prick tests with different stimuli, such as codeine, histamine, methacholine, and a relevant inhalant allergen. METHODS: A randomized, double-blind, placebo-controlled study was performed in which Ze 339 was compared to acrivastine, a short-acting antihistamine, in 8 patients with respiratory allergy and in 10 nonatopic, healthy volunteers. Antiallergic activity of Ze 339 was determined by analyzing inhibitory potency in skin prick tests with codeine, histamine, methacholine, and an inhalant allergen. Wheal-and-flare reactions were assessed 90 minutes after a double dose of Ze 339, acrivastine, or placebo. An interval of at least 3 days was left between the skin tests. RESULTS: Acrivastine was identified as the only substance that significantly inhibited skin test reactivity to all solutions analyzed in all study subjects. In contrast, no significant inhibition could be demonstrated for Ze 339 with any test solution. Moreover, the results of Ze 339 did not differ significantly from placebo. CONCLUSIONS: In this study we found no antiallergic, particularly antihistaminic, effect of Ze 339 in skin tests using a variety of stimuli often used to evaluate immediate skin test reactivity. The mechanism by which Ze 339 is effective in the treatment of seasonal allergic rhinitis still needs to be elucidated.
Asunto(s)
Antialérgicos/uso terapéutico , Petasites/química , Extractos Vegetales/uso terapéutico , Hipersensibilidad Respiratoria/tratamiento farmacológico , Sesquiterpenos/uso terapéutico , Administración por Inhalación , Adulto , Alérgenos/administración & dosificación , Alérgenos/inmunología , Antialérgicos/administración & dosificación , Estudios Cruzados , Método Doble Ciego , Esquema de Medicación , Femenino , Histamina/administración & dosificación , Histamina/inmunología , Humanos , Masculino , Cloruro de Metacolina/administración & dosificación , Cloruro de Metacolina/inmunología , Persona de Mediana Edad , Fitoterapia , Extractos Vegetales/administración & dosificación , Hipersensibilidad Respiratoria/etiología , Hipersensibilidad Respiratoria/inmunología , Sesquiterpenos/administración & dosificación , Piel/efectos de los fármacos , Piel/inmunología , Piel/patología , Pruebas Cutáneas/métodos , Resultado del Tratamiento , Triprolidina/administración & dosificación , Triprolidina/análogos & derivados , Triprolidina/uso terapéuticoRESUMEN
BACKGROUND: Common colds are usually treated by the patients themselves with over-the-counter (OTC) cold medications. Many cough and cold remedies are available and sold freely without prescription. The authors conducted a study to compare the efficacy, adverse effects, the quality of life (QOL) and the patient's opinion and appreciation on the drugs (POD) between Dayquil/Nyquil and Actifed DM plus paracetamol syrup. METHOD: In this prospective, investigator-blinded clinical trial, 120 patients, aged between 15 and 60 years old, with common colds within 72 hours, who accepted the trial and gave informed written consent, were randomized into two treatment groups. One patient was excluded due to evidence of bacterial infection. Fifty-nine patients were treated with Dayquil/Nyquil (D/N group), while the other 60 patients had Actifed DM plus paracetamol (ADM/P group) for three days. On day 1 the patient's demographic data (sex, age, body weight, blood pressure, co-existing diseases/conditions, drug use, and allergy to any drugs), the most prominent symptoms and its duration were recorded. All patients were screened for bacterial infection by physical examination, complete blood count and sinus radiographs. The symptoms (nasal obstruction, rhinorrhea, sneezing, cough, sore throat, fever and headache) and signs (injected nasal mucosa, nasal discharge and pharyngeal discharge) were scored, based on 4-point scale (0 to 3), on days 1 and 4. Changing of the symptoms and QOL were recorded on the diary card. The patient's opinion and appreciation on the drugs (POD) was assessed on day 4. The effectiveness (the ability to lessen the symptoms and signs), QOL and POD between two treatments were compared. RESULTS: The demographic data between the two groups were similar. The four most common prominent symptoms of common colds in our series were cough (47.9%), sore throat (26.17%), rhinorrhea (8.4%) and headache (8.4%). However, both treatments were equally effective in lessening the symptoms (P = 0.426) and signs (P = 0.716) of common cold from days 1 to 4. The adverse effects were significantly higher in ADM/P group than in D/N group (p = 0.006). In contrast, QOL in terms of alertness, freshness and sound sleep improved from day 1 to day 3 in both treatments, but the overall day-3 score was significantly higher in the D/N group than the ADM/P group (1.85 +/- 1.83; 1.25 +/- 1.94: p = 0.024). POD in terms of convenience, flavour of drug, effectiveness of the drug and a need to repeat the drug assessed on day 4, was also significantly higher in the D/N group than the ADM/P group (10.68 +/- 2.56; 8.92 +/- 2.27: p < 0.001). CONCLUSION: Dayquil/Nyquil are as effective as Actifed DM plus paracetamol in controlling the symptoms and signs of the common cold, but have fewer adverse effects. The quality of life assessed during the use of the drugs was significantly higher in the Dayquil/Nyquil group, and according to the patients, they prefered Dayquil/Nyquil more than Actifed DM plus paracetamol.
Asunto(s)
Acetaminofén/efectos adversos , Acetaminofén/uso terapéutico , Resfriado Común/tratamiento farmacológico , Dextrometorfano/efectos adversos , Dextrometorfano/uso terapéutico , Doxilamina/efectos adversos , Doxilamina/uso terapéutico , Efedrina/efectos adversos , Efedrina/uso terapéutico , Expectorantes/efectos adversos , Expectorantes/uso terapéutico , Medicamentos sin Prescripción/efectos adversos , Medicamentos sin Prescripción/uso terapéutico , Prometazina/efectos adversos , Prometazina/uso terapéutico , Triprolidina/efectos adversos , Triprolidina/uso terapéutico , Adolescente , Adulto , Combinación de Medicamentos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Satisfacción del Paciente , Estudios Prospectivos , Seudoefedrina , Calidad de VidaRESUMEN
BACKGROUND: Medications containing a combination antihistamine-decongestant are commonly used for allergic rhinitis yet onset-of-action comparisons for symptom relief after a single dose have not been performed. OBJECTIVE: To determine the onset of symptom relief and efficacy of antihistamine-decongestant medications (acrivastine-pseudoephedrine and loratadine-pseudoephedrine) compared with placebo in an outdoor park. METHODS: This study was conducted during the spring of 1997 using a double-blind, placebo-controlled design. Patients completed baseline rhinitis symptom diaries from 7:30 to 9:30 AM. Subjects with qualifying symptom scores received one dose of either acrivastine-pseudoephedrine, loratadine-pseudoephedrine, or placebo at 10:00 AM. Symptom diaries were recorded for the next 4 hours. RESULTS: Of 593 patients randomized to treatment, 592 were included in efficacy analysis. Acrivastine-pseudoephedrine and loratadine-pseudoephedrine demonstrated a mean onset-of-action by 45 and 30 minutes respectively for total symptom and rhinitis symptom scores for the five sites. Onset-of-action for nasal congestion scores was 45 minutes for both medications. Sites having higher pollen exposure (>100 pollen grains over 6 hours) demonstrated a difference between the antihistamine combinations: acrivastine-pseudoephedrine had an onset of action at 45 minutes for total symptom and rhinitis symptom scores, and 15 minutes for nasal congestion scores whereas loratadine-pseudoephedrine had onset-of-action for nasal congestion score of 105 minutes but failed to reach significance at any timepoint for total symptom and rhinitis symptom scores. CONCLUSIONS: Both antihistamine-decongestant combinations demonstrate an onset-of-action within 60 minutes of administration but under conditions of higher pollen exposure, the acrivastine combination was more effective for total symptoms, rhinitis symptoms, and nasal congestion with an onset-of-action within 45 minutes for rhinitis symptoms and 15 minutes for congestion.
Asunto(s)
Efedrina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Loratadina/uso terapéutico , Descongestionantes Nasales/uso terapéutico , Rinitis Alérgica Estacional/tratamiento farmacológico , Triprolidina/análogos & derivados , Adulto , Contaminantes Atmosféricos/inmunología , Alérgenos/inmunología , Antialérgicos/uso terapéutico , Método Doble Ciego , Combinación de Medicamentos , Femenino , Humanos , Masculino , Polen/inmunología , Rinitis Alérgica Estacional/etiología , Factores de Tiempo , Triprolidina/uso terapéuticoRESUMEN
It is accepted that studies evaluating histamine-induced wheal and flare reactions in the skin represent a simple and reliable method for demonstrating pharmacodynamic activity and pharmacokinetics of the H1-receptor antagonists. In this study, the effects of single oral doses of acrivastine (8 mg), loratadine (10 mg) and cetirizine (10 mg) on the histamine-induced wheal and flare reactions were compared in 60 healthy volunteers. The wheal and flare responses were produced by prick test using 1% histamine solution. Measurements were performed before the ingestion of antihistamines (baseline values) and afterwards at 15, 30, 90, 240, 360 min and 24 h. The values obtained for each antihistamine were compared with each other and with baseline values. Cetirizine was found to be superior to acrivastine and loratadine for the suppression of wheal and flare responses at 240, 360 min and 24 h (P < 0.05) and acrivastine was superior to the other two antihistamines for the suppression of flare response at 30 min (P < 0.05). Our results indicate that a single dose of cetirizine provides a more effective and long acting suppression on wheal and flare reactions in urticaria when compared to acrivastine and loratadine.
Asunto(s)
Cetirizina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Loratadina/uso terapéutico , Triprolidina/análogos & derivados , Urticaria/tratamiento farmacológico , Adulto , Estudios Cruzados , Femenino , Histamina , Humanos , Masculino , Persona de Mediana Edad , Método Simple Ciego , Triprolidina/uso terapéutico , Urticaria/etiologíaRESUMEN
Certirizine, a potent H1-blocking agent, is often recommended as an emergency drug in anaphylactic reactions because of its well documented fast onset of action. In this randomized, cross-over study we compared the onset of action after a single dose of two recently introduced antihistamines, acrivastine and fexofenadine, with that of cetirizine. The inhibition of the wheal-and-flare reaction produced by skin prick test with histamine in 20 healthy volunteers and with a relevant pollen allergen in 20 atopic patients, respectively, were measured before and at regular intervals up to 60 min after the ingestion of acrivastine (8 mg and 16 mg), fexofenadine (120 mg) and cetirizine (10 mg and 20 mg). Wheal-and-flare reaction were significantly inhibited 20 min after the intake of 16 mg acrivastine in atopic patients and 30 min after intake of 8 mg acrivastine in healthy volunteers, whereas cetirizine produced a significant inhibition of the wheal-and-flare reaction within 40-60 min. No significant inhibition could be observed within 60 min after fexofenadine intake. Therefore, in clinical settings when a fast onset of the H1-blocking action is mandatory (e.g., after insect stings or for short-term prophylaxis) we recommend acrivastine.
Asunto(s)
Alérgenos/inmunología , Antialérgicos/uso terapéutico , Cetirizina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Histamina/inmunología , Terfenadina/análogos & derivados , Triprolidina/análogos & derivados , Adolescente , Adulto , Antialérgicos/efectos adversos , Cetirizina/efectos adversos , Estudios Cruzados , Femenino , Antagonistas de los Receptores Histamínicos H1/efectos adversos , Humanos , Hipersensibilidad Inmediata/tratamiento farmacológico , Hipersensibilidad Inmediata/inmunología , Masculino , Persona de Mediana Edad , Estudios Prospectivos , Rinitis Alérgica Estacional/tratamiento farmacológico , Rinitis Alérgica Estacional/inmunología , Pruebas Cutáneas , Terfenadina/efectos adversos , Terfenadina/uso terapéutico , Triprolidina/efectos adversos , Triprolidina/uso terapéuticoRESUMEN
Pilots with allergic diseases, who need antihistaminic drug therapy, have to be grounded temporarily because this therapy is considered to interfere with flight safety due to its sedative effects. There is evidence that loratadine is practically void of these sedative effects, and therefore might be prescribed to pilots. A study was conducted to determine the effects of loratadine on performance and alertness. In a randomized, double-blind, within subjects design, 18 male subjects were studied, employing loratadine 10 mg, triprolidine hydrochloride 5 mg, and placebo. Objective (vigilance, complex tasks) and subjective tests, tailored to the specific tasks of aircrew, were applied under hypobaric conditions that prevail in an intact cockpit. With respect to alertness and performance, the results of this study showed no significant differences between loratadine and placebo during a period of 1 to 6 hours after drug ingestion. Triprolidine, used as a positive control, showed significant detrimental effects on both subjective and objective measures. It is anticipated that a single dose of loratadine 10 mg will not affect flying performance. This finding might also have implications for the treatment of allergic disorders of personnel involved in other highly skilled jobs.
Asunto(s)
Medicina Aeroespacial , Antialérgicos/uso terapéutico , Aviación , Ambiente Controlado , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Loratadina/uso terapéutico , Adulto , Antialérgicos/administración & dosificación , Nivel de Alerta/efectos de los fármacos , Concienciación/efectos de los fármacos , Método Doble Ciego , Fatiga/inducido químicamente , Hemoglobinas/análisis , Antagonistas de los Receptores Histamínicos H1/administración & dosificación , Humanos , Loratadina/administración & dosificación , Masculino , Destreza Motora/efectos de los fármacos , Oxígeno/sangre , Placebos , Presión , Desempeño Psicomotor/efectos de los fármacos , Fases del Sueño/efectos de los fármacos , Triprolidina/administración & dosificación , Triprolidina/uso terapéuticoRESUMEN
BACKGROUND: Acrivastine is a second-generation H1-antagonist chemically related to triprolidine, but more polar and with less central nervous system penetration than triprolidine. OBJECTIVE: The efficacy of the antihistamine-decongestant combination product (Semprex-D capsules) containing acrivastine 8 mg plus pseudoephedrine HCl 60 mg was evaluated for the treatment of seasonal allergic rhinitis symptoms. METHODS: A total of 676 patients sensitive to mountain cedar pollen was enrolled into a 6-center, randomized, double-blind, placebo-controlled, parallel, 4-group study designed to compare acrivastine + pseudoephedrine, acrivastine, pseudoephedrine, and placebo. Patients with demonstrable diary symptom scores at baseline took study medication (4 doses/day) and recorded symptom scores twice daily for 2 weeks. The effectiveness of the acrivastine + pseudoephedrine combination was examined relative to the individual components and placebo in terms of changes in diary symptom scores. RESULTS: Over the 2-week period, the combination of acrivastine plus pseudoephedrine was significantly more effective than (1) acrivastine, pseudoephedrine, and placebo (P < .001) for relief of all symptoms; (2) pseudoephedrine (P < .001) for relieving allergy symptoms, ie, running nose, sneezing, itchy nose/throat and tearing; and (3) acrivastine (P < .001) for reducing nasal congestion. Relative to placebo, small increases in adverse experience rates were observed with acrivastine + pseudoephedrine for dry mouth, insomnia, somnolence, and headache. CONCLUSION: These findings in a large clinical trial demonstrate (1) the efficacy of acrivastine and (2) that each component of the combination of acrivastine 8 mg plus pseudoephedrine HCl 60 mg contributes to the overall efficacy, thereby supporting the conclusion that the combination is rational, safe, and effective for the treatment of allergic rhinitis.
Asunto(s)
Efedrina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Rinitis Alérgica Estacional/tratamiento farmacológico , Triprolidina/análogos & derivados , Adolescente , Adulto , Anciano , Método Doble Ciego , Quimioterapia Combinada , Femenino , Antagonistas de los Receptores Histamínicos H1/efectos adversos , Humanos , Masculino , Persona de Mediana Edad , Polen/inmunología , Rinitis Alérgica Estacional/etiología , Árboles/inmunología , Triprolidina/efectos adversos , Triprolidina/uso terapéuticoRESUMEN
BACKGROUND: Semprex-D capsules contain acrivastine 8 mg (a second generation H1-antagonist) plus pseudoephedrine HCl 60 mg and were developed to satisfy the needs of allergy suffers who prefer combination products designed to provide broader symptom relief. Approval of combination products by the US Food and Drug Administration requires demonstration that each component contributes to the overall effectiveness. OBJECTIVE: The objective of the study was to demonstrate that both acrivastine and pseudoephedrine share in the efficacy of the combination in relieving allergy symptoms in patients sensitive to ragweed pollen. METHODS: This was a double-blind, randomized, placebo-controlled, parallel groups, balanced design, multicenter (13 sites) study. Patients 12 years of age or older with skin test reactivity to ragweed were recruited. Patients who qualified for the study were dispensed either (1) acrivastine + pseudoephedrine, (2) acrivastine, (3) pseudoephedrine, or (4) placebo with instructions to take one capsule 4 times daily and to record allergy symptom scores in a symptom diary 3 times daily for 14 days. Assessments of health, global allergy symptoms, protocol compliance, adverse events, and vital signs were also documented. RESULTS: A total of 702 patients were enrolled in this study. Over the 2-week period, the combination of acrivastine + pseudophedrine was significantly more effective than acrivastine, pseudoephedrine, and placebo for relief of all symptoms (P range .01 to .001); pseudoephedrine for treating symptoms responsive to antihistamines (P = .003); and acrivastine for treating symptoms responsive to nasal decongestants (P < .001). Relatively small increases in adverse experience rates were observed for the combination relative to the placebo. CONCLUSIONS: These findings in a large clinical trial demonstrate that each component of the combination of acrivastine 8 mg plus pseudoephedrine HCl 60 mg contributes to the overall efficacy, thereby supporting the conclusion that the combination is rational, safe, and effective for the treatment of allergic rhinitis.
Asunto(s)
Alérgenos/inmunología , Efedrina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Proteínas de Plantas/inmunología , Polen/inmunología , Rinitis Alérgica Estacional/tratamiento farmacológico , Triprolidina/análogos & derivados , Adolescente , Adulto , Anciano , Niño , Preescolar , Método Doble Ciego , Quimioterapia Combinada , Efedrina/efectos adversos , Femenino , Antagonistas de los Receptores Histamínicos H1/efectos adversos , Humanos , Masculino , Persona de Mediana Edad , Triprolidina/efectos adversos , Triprolidina/uso terapéuticoRESUMEN
In order to assess the efficacy of Rinasek in symptomatic treatment of seasonal and nonseasonal rhinitis, 40 ambulatory otorhinolaryngologic patients were multicentrically examined in a placebo controlled double-blind study. Clinical and other findings show that the drug worked excellent in 46.6%, well in 13.3%, weak in 13.3% and in 10% of patients it had no effects. Consequently, Rinasek worked positively in 73.2%, and that is the best reason to recommend its application.
Asunto(s)
Efedrina/uso terapéutico , Rinitis Alérgica Perenne/tratamiento farmacológico , Rinitis Alérgica Estacional/tratamiento farmacológico , Rinitis Vasomotora/tratamiento farmacológico , Triprolidina/uso terapéutico , Adulto , Anciano , Método Doble Ciego , Combinación de Medicamentos , Evaluación de Medicamentos , Efedrina/efectos adversos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Seudoefedrina , Triprolidina/efectos adversosRESUMEN
In a placebo-controlled, randomized, and double-blind 1-day field study, the efficacy and onset of action of capsule acrivastine 8 mg were evaluated in 42 patients suffering from allergic rhinoconjunctivitis elicited by natural grass pollen exposure. Before and for 2 h after treatment, the patients scored the severity of five rhinoconjunctivitis symptoms every 10 min on a 0-5 scale (0 = no symptoms; 5 = very severe symptoms). The number of sneezes was recorded, and every 30 min, measurements of nasal peak flow were made. Before treatment, there was no difference in median total symptom score (mTSS) between the acrivastine group (A) and the placebo group (P) (12 and 12, respectively). Time of onset was estimated by an exponential decay model to be 19 min (95% confidence interval 0-39 min). A statistically significant difference in percent reduction of mTSS between A and P was observed for the first time 46 min after treatment start (A = 22%, P = 0%, P < 0.05). A 50% reduction in total symptom score (TSS) was achieved within 60 min by 38% in A and 17% in P (NS), and within 80 min in 52% and 17%, respectively (P < 0.05). The median time for 50% reduction in TSS (MT50) was 80 min for A and > 120 min for P (P < 0.01). The symptom score of sneezing and number of sneezes were evaluated for periods of 30 min. The difference between A and P became statistically significant from 31-60 and 61-90 min, respectively (P < 0.05 and P < 0.01). Objective and subjective determinants in the different time intervals were well correlated. Improvement of nasal congestion was observed in A at 91-120 min, as measured by nasal peak flow.
Asunto(s)
Conjuntivitis Alérgica/tratamiento farmacológico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Rinitis Alérgica Estacional/tratamiento farmacológico , Triprolidina/análogos & derivados , Administración Oral , Adulto , Conjuntivitis Alérgica/fisiopatología , Método Doble Ciego , Femenino , Humanos , Masculino , Persona de Mediana Edad , Polen , Rinitis Alérgica Estacional/fisiopatología , Triprolidina/uso terapéuticoAsunto(s)
Efedrina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Rinitis Alérgica Estacional/tratamiento farmacológico , Triprolidina/análogos & derivados , Combinación de Medicamentos , Efedrina/efectos adversos , Efedrina/farmacocinética , Antagonistas de los Receptores Histamínicos H1/efectos adversos , Antagonistas de los Receptores Histamínicos H1/farmacocinética , Humanos , Triprolidina/efectos adversos , Triprolidina/farmacocinética , Triprolidina/uso terapéuticoRESUMEN
Renal cell carcinoma exhibits chemoresistance attributable in part to the P-glycoprotein drug efflux mechanism. Acrivastine is a hydrophylic antihistamine that has been shown in vitro to reverse this form of resistance. After five patients were treated on a dose-finding study, seventeen patients with metastatic or unresectable renal cell carcinoma were entered into a phase II study of vinblastine in combination with acrivastine. Patients received oral acrivastine at doses of 400 mg every 4 hours for 6 days and a 96-hour continuous infusion of vinblastine at a dose of 1.6 mg/m2/24 h. Of 15 evaluable patients, no tumor responses were seen. The regimen was well-tolerated with the majority of toxicities being gastrointestinal and hematologic. Serum levels of acrivastine, its principal metabolite (270C81) and vinblastine were measured during the study. Based on in vitro data, the plasma levels of acrivastine were within a range adequate to block P-glycoprotein activity. High doses of acrivastine were well-tolerated clinically, however, the combination of acrivastine and vinblastine was not active against renal cell carcinoma.
Asunto(s)
Carcinoma de Células Renales/tratamiento farmacológico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Neoplasias Renales/tratamiento farmacológico , Triprolidina/análogos & derivados , Vinblastina/uso terapéutico , Adulto , Anciano , Resistencia a Múltiples Medicamentos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Estadificación de Neoplasias , Triprolidina/uso terapéuticoRESUMEN
The purpose of this study was to assess the time of onset of action of acrivastine in suppressing the wheal response to histamine (10 mg/ml) and allergen (10,000 and 100,000 BU/ml) in the skin prick test. Ten subjects with a well-documented allergy to pollen received single doses of 8 mg of acrivastine and placebo according to a randomized, double-blind, placebo-controlled, crossover treatment design. Duplicate skin prick tests were performed 0, 15, 20, 25, 30, and 60 min after medication. The results demonstrated a statistically significant suppression of the wheal reactions 15-20 min after medication, depending on the reaction producers used. The sum of all three producers showed a statistically significant effect on the wheal reaction 15 min after medication. The upper 95% confidence limit for time lag from dosing of acrivastine until reduction from placebo level commences was 6.5 min. The study substantiates that orally administered acrivastine has a rapid onset of action in the skin of allergic subjects. The results indicate that allergen SPT is a more sensitive tool for studying antihistaminergic activity than histamine SPT.
Asunto(s)
Alérgenos , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Polen , Triprolidina/análogos & derivados , Urticaria/tratamiento farmacológico , Administración Oral , Adulto , Intervalos de Confianza , Método Doble Ciego , Femenino , Histamina/inmunología , Humanos , Masculino , Persona de Mediana Edad , Pruebas Cutáneas , Factores de Tiempo , Triprolidina/uso terapéutico , Urticaria/diagnóstico , Urticaria/inmunologíaRESUMEN
The new H1 antihistamines are a major therapeutic advancement in the treatment of allergic disorders such as urticaria and allergic rhinitis. Their efficacy combined with greatly reduced sedating and anticholinergic side effects makes the new class of H1 antihistamines the first-line treatment in the management of urticaria and mild angioedema. The choice of a particular low-sedating H1 antihistamine depends on pharmacokinetic considerations, the severity of the problem (systemic steroids and epinephrine are the first-line treatment for severe angioedema), and the requirement for limiting the frequency of administration. The efficacy of the new H1 antihistamines in the treatment of itch due to atopic eczema and systemic disease remains uncertain, and further controlled clinical trials are needed to elucidate their possible role in these conditions.
Asunto(s)
Dermatitis Atópica/tratamiento farmacológico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Urticaria/tratamiento farmacológico , Astemizol/farmacología , Astemizol/uso terapéutico , Cetirizina/farmacología , Cetirizina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/farmacología , Humanos , Loratadina/farmacología , Loratadina/uso terapéutico , Terfenadina/farmacología , Terfenadina/uso terapéutico , Triprolidina/análogos & derivados , Triprolidina/farmacología , Triprolidina/uso terapéuticoRESUMEN
Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis. Acrivastine was more effective than placebo and similar in efficacy to clemastine or terfenadine in the treatment of seasonal allergic rhinitis. In the treatment of dermatoses in which histamine has a pathogenetic role, the efficacy of acrivastine was superior to that of placebo and similar to that of usual dosages of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine or terfenadine. Acrivastine caused less drowsiness than clemastine, the incidence of adverse effects being indistinguishable from that with placebo or terfenadine. Thus, acrivastine is an effective addition to drugs currently available for the treatment of patients with allergic diseases in whom a histamine H1-receptor antagonist is indicated. Because of its rapid onset of action acrivastine will be particularly useful for 'on demand' therapy in patients with intermittent symptoms.