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Fexofenadine is useful in various allergic disease treatment.However,the pharmacokinetic variability information and quantitative factor identification of fexofenadine are very lacking.This study aimed to verify the validity of previously proposed genetic factors through fexofenadine population pharmaco-kinetic modeling and to explore the quantitative correlations affecting the pharmacokinetic variability.Polymorphisms of the organic-anion-transporting-polypeptide(OATP)1B1 and 2B1 have been proposed to be closely related to fexofenadine pharmacokinetic diversity.Therefore,modeling was performed using fexofenadine oral exposure data according to the OATP1B1-and 2B1-polymorphisms.OATP1B1 and 2B1 were identified as effective covariates of clearance(CL/F)and distribution volume(V/F)-CL/F,respectively,in fexofenadine pharmacokinetic variability.CL/F and average steady-state plasma con-centration of fexofenadine differed by up to 2.17-and 2.20-folds,respectively,depending on the OATP1B1 polymorphism.Among the individuals with different OATP2B1 polymorphisms,the CL/F and V/F differed by up to 1.73-and 2.00-folds,respectively.Ratio of the areas under the curves following single-and multiple-administrations,and the cumulative ratio were significantly different between OATP1B1-and 2B1-polymorphism groups.Based on quantitative prediction comparison through a model-based approach,OATP1B1 was confirmed to be relatively more important than 2B1 regarding the degree of effect on fexofenadine pharmacokinetic variability.Based on the established pharmacokinetic-pharmacodynamic relationship,the difference in fexofenadine efficacy according to genetic poly-morphisms of OATP1B1 and 2B1 was 1.25-and 0.87-times,respectively,and genetic consideration of OATP1B1 was expected to be important in the pharmacodynamics area as well.This population phar-macometrics study will be a very useful starting point for fexofenadine precision medicine.
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Background: Allergic rhinitis (AR) impacts 10-30% of the world affecting the quality of life of many. Hence, the requirement of a treatment targeted at delivering maximum symptom control and has minimum to no side effects. Objectives: Comparison of efficacy of Bilastine and Fexofenadine in patients suffering from intermittent allergic rhinitis with the help of Total Nasal Symptom Scoring(TNSS) and assessment of side effects- sedation and cardiac toxicity. Methodology: 60 subjects diagnosed with intermittent allergic rhinitis (IAR) were recruited and divided into groups of 30 each. One group was started on Bilastine 20mg OD and the other on Fexofenadine 120mg OD. TNSS was calculated based on symptom severity at presentation, on 10th day and 30th of antihistamine therapy. AEC values and ECG changes were compared for both groups at day 0, day 30. Measurement of sedation was done at day 10, day 30. Intergroup comparison and intragroup assessment of TNSS and its variables, sedative effects and ECG changes at day 0 and day 30 were done using Un-paired and Paired T-test. Results: Patients showed reduction in symptoms of AR with both drugs. TNSS and Rhinorrhoea showed significant improvement in Fexofenadine group as compared to Bilastine. AEC values showed significant reduction in both groups. Statistically significant ECG changes were seen after 30 days of Fexofenadine therapy but were clinically insignificant. No sedative effects were noted with both drugs. Conclusion: Both Bilastine and Fexofenadine were found to be effective in reducing symptoms in patients with IAR. Fexofenadine was more effective than Bilastine in overall symptom control and specifically in controlling rhinorrhoea after one month of therapy. Both the drugs had no sedative effects or cardiac toxicity.
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The aim of this work was to perform solubility studies for fexofenadine hydrochloride and establish dissolution conditions for this drug in oral suspension dosage form. The solubility study was executed through the shake-flask method, below 37 ºC±1 ºC, at 100 rpm stirring for 12 h in three buffer solutions: hydrochloric acid pH 2.0, acetate pH 4.5 and phosphate pH 6.8. The dissolution test was developed in vessels containing 900 mL of the same buffer, employing the paddle apparatus in speed of 25 and 50 rpm, below 37 ºC±0.5 ºC. The drug was classified as low solubility according to the Biopharmaceutics Classification System, since the dose/solubility ratio was higher than 250 mL in all media tested (326.55 mL in buffer pH 2.0; 2,456.33 mL in buffer pH 4.5 and 1,021.16 mL in buffer pH 6.8). The dissolution test showed that a release of 85% in 30 min could be established. The rotation speed of 25 rpm, media volume of 900 mL and insertion of the samples through weighted syringes are adequate. The buffered media pH 2.0 could be chosen as dissolution media.
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Solubilidade , Suspensões/farmacologia , Dissolução/métodos , Biofarmácia , Preparações Farmacêuticas/análise , Cromatografia Líquida de Alta Pressão/métodos , Formas de DosagemRESUMO
Dipeptidyl peptidase IV (DPP IV) is relatively new anti-diabetic target. DPP IV inhibitors lower fasting andpostprandial glucose concentrations by preventing the degradation of the natural hypoglycemic incretin hormones:glucose-dependent insulinotropic peptide and glucagon-like peptide-1. In this work, the high throughput dockingsoftware FRED was used as a virtual screening tool against in house built drug database to discover new DPP IVinhibitors. One of the highest ranking hits, the antihistamine drug fexofenadine, was found to inhibit recombinanthuman DPP IV in vitro with IC50 = 4.6 (±1.0) µM. The anti-diabetic effect of fexofenadine was validated in vivo byoral glucose tolerance test. These results could be helpful in the development of novel DPP IV inhibitors based onfexofenadine scaffold for the treatment of type 2 diabetes.
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Objective To study clinical effects of the fexofenadine hydrochloride Tablets and BCG-PSN in the treatment of chronic urticaria. Methods 122 patients with chronic urticaria treated in Yiwu skin disease hospital from January 2016 to March 2017 were selected and randomly divided into the control group and the experimental group, 61 patients for each group. The control group was given Fexofenadine Hydrochloride Tablets treatment, the experimental group was given BCG-PSN on the basic treatment of the control group. The patients in the experimental group and the control group were treated for 3 months. The treatment effect and adverse reactions were compared between two groups. Results After the corresponding treatment, the number of invalid cases in the experimental group was 10. In the control group, 21 cases were ineffective. The effective rate of the experimental group was 63.93%, which was significantly higher than 32.97% of the control group with statistical significance (P<0.05). There were no obvious adverse reactions in the two groups, and there was no significant difference in the incidence of adverse reactions. After treatment, the integral score of the experimental group was (3.20±0.42), significantly lower than that of the control group (3.98±0.37), with statistical significance (P<0.05). Conclusion fexofenadine hydrochloride Tablets combined with BCG-PSN for the treatment of chronic urticaria could significantly improve clinical symptoms of patients with good efficacy, high safety and clinical application significance.
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Objective To analyze the clinical efficacy of desloratadine citrate disodium and fexofenadine in the treatment of refractory urticaria . Methods 100 patients with refractory urticaria were randomly divided into observation group and control group according to the digital table method, with 50 cases in each group.The control group were treated with desloratadine citrate disodium, and the observation group were treated with fexofenadine on the basis of control group.The efficacy, immunity function ( CD3 +, CD4 +, CD4 +/CD8 +) , the changes of inflammatory factors [ procalcitonin ( PCT) , C-reactive protein ( CRP) ] and the quality of life were compared between the two groups.The adverse reaction rate in two groups was recorded in two groups.Results The total efficacy in observation group (88.0%) was significantly higher than that in control group (72.0%)(P<0.05).The indicators of immunity function in observation group were significantly higher than those in control group(P<0.05).The inflammatory factors in observation group were significantly lower than those in control group ( P<0.05 ) .The sleep and exercise quality rate of the observation group were significantly higher than those in control group(86.0% vs.68.0%,84.0% vs.66.0%,P<0.05).Conclusion The combination of desloratadine citrate disodium and fexofenadine in the treatment of refractory urticaria has a good effect, can effectively improve the immune function, reduce the secretion of inflammatory factors, thus effectively relieve the clinical symptoms, improve their quality of life, and has high security.
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Objective To study clinical effects of the fexofenadine hydrochloride Tablets and BCG-PSN in the treatment of chronic urticaria. Methods 122 patients with chronic urticaria treated in Yiwu skin disease hospital from January 2016 to March 2017 were selected and randomly divided into the control group and the experimental group, 61 patients for each group. The control group was given Fexofenadine Hydrochloride Tablets treatment, the experimental group was given BCG-PSN on the basic treatment of the control group. The patients in the experimental group and the control group were treated for 3 months. The treatment effect and adverse reactions were compared between two groups. Results After the corresponding treatment, the number of invalid cases in the experimental group was 10. In the control group, 21 cases were ineffective. The effective rate of the experimental group was 63.93%, which was significantly higher than 32.97% of the control group with statistical significance (P<0.05). There were no obvious adverse reactions in the two groups, and there was no significant difference in the incidence of adverse reactions. After treatment, the integral score of the experimental group was (3.20±0.42), significantly lower than that of the control group (3.98±0.37), with statistical significance (P<0.05). Conclusion fexofenadine hydrochloride Tablets combined with BCG-PSN for the treatment of chronic urticaria could significantly improve clinical symptoms of patients with good efficacy, high safety and clinical application significance.
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Objective To investigate the effect of compound glycyrrhizin combined with fexofenadine hydrochloride in the treatment of chronic urticaria and its effect on plasma histamine.Methods 100 patients with chronic urticaria were selected as study objects,and they were divided into the control group(50 cases) and observation group(50 cases) according to the random number table method.The control group was treated with fexofenadine hydrochloride,while the observation group was treated with compound glycyrrhizin on the basis of the control group.The clinical effect and plasma histamine level were compared between the two groups.Results The effective rate of the observation group was 96.0%,which was significantly higher than 84.0% of the control group(χ2=7.951,P<0.05).After treatment,the plasma histamine content of the observation group was (2.38±0.26)ng/mL,which was lower than (3.10±0.29)ng/mL of the control group,and the difference between the two groups was statistically significant(t=6.084,P<0.05).Conclusion The compound glycyrrhizin combined with fexofenadine hydrochloride in the treatment of chronic urticaria can reduce the symptoms of the patients,reduce the number and size of the patients and effectively control the clinical symptoms of the patients.And it can effectively reduce the level of plasma histamine in patients with good clinical effect and application value,it is worth to be promoted in clinical.
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Objective To evaluate the efficacy of fexofenadine hydrochloride tablets at tapering doses for the treatment of chronic spontaneous urticaria. Methods After receiving evaluation of medical history and undergoing autologous serum skin test (ASST), 80 patients with chronic spontaneous urticaria were randomly divided into two groups:conventional dose group administrating fexofenadine hydrochloride tablets 120 mg/d for 12 consecutive weeks, tapering dose group administrating fexofenadine hydrochloride tablets 120 mg/d for the first 4 weeks followed by dose tapering of fexofenadine hydrochloride tablets by 30 mg at the 5th and 9th weeks. The urticaria activity score(UAS) and dermatology life quality index(DLQI)were evaluated before the treatment(baseline)as well as after 4?, 8?and 12?week treatment, and the total dose of fexofenadine hydrochloride was calculated. Results A total of 76 patients completed the 12?week treatment, including 37 patients in the conventional dose group and 39 patients in the tapering dose group. After 4?, 8?and 12?week treatment, a significant decrease was observed in the UAS in the conventional dose group(0.64 ± 0.82, 0.37 ± 0.68 and 0.27 ± 0.56 vs. 4.08 ± 0.79, all P0.05). After 8?and 12?week treatment, symptoms were controlled in 71.79%(28/39)and 82.05%(32/39)of patients in the tapering dose group, respectively, with the total dose of fexofenadine hydrochloride being significantly lower in the tapering dose group than in the conventional dose group (both P<0.001). Conclusion After 4- 8 weeks of treatment with fexofenadine hydrochloride, the tapering dose regimen and conventional dose regimen show similar clinical efficacy in patients with chronic spontaneous urticaria.
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A simple, rapid and precise reverse phase liquid chromatographic (RP-HPLC) method was developed and subsequently validated for simultaneous estimation of Ambroxol hydrochloride and Fexofenadine hydrochloride in bulk drug and in a synthetic mixture. The method is based on High Performance Liquid Chromatography (HPLC) on a reversed – phase column, Hypersil ODS C18 (Hypersil ODS 250 x 4.6 mm, 5, Make: Thermo Scientific) prepacked column. The separation was carried out using a mobile phase containing a buffer and acetonitrile (56:44 v/v), was pumped at a flow rate of 0.8 mL/min, column temperature at 35º C using UVdetection at 225 nm. Both the drugs were well resolved on the stationary phase and the retention times were around 2.424 minute for Ambroxol hydrochloride and 3.753 minute for Fexofenadine hydrochloride. The method was validated and shown to be linear for both the drugs. The correlation coefficients for Ambroxol hydrochloride and Fexofenadine hydrochloride are 0.9994 and 0.9992 respectively.
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Objective To study the effect of tripterygium glycosides(TG)in treating urticaria chronica(UC).Methods 91 cases of UC in our hospital from February 2012 to March 2013 were randomly divided into the observation group(45 cases)and the con-trol group(46 cases)according to the digital method.The control group was treated with fexofenadine,while on this basis the obser-vation group was added with TG.The UAS,VAS and LFS scores before and after treatment,curative effects,serum IL-4,IFN-γand IgE levels change and adverse reactions were compared between the two groups.Results The VAS,LFS and UAS scores after treatment in the observation group were significantly lower than those before treatment and the control group after treatment;the curative effect after 4-week treatment in the observation group was significantly higher than that in the control group;the IL-4 and IgE levels after treatment in the observation group were significantly lower than those before treatment and the control group after treatment;the IFN-γlevel was significantly higher than that before treatment and the control group after treatment,all the differ-ences above were statistically significant(P0.05).Conclusion TG combined with fexofenadine in the treatment of UC has better effect.
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Background: Allergic rhinitis (AR) has impact on the physical, psychological and social aspects of the patients’ life and work. Therefore, it is imperative to identify the treatment options for AR. Objective: This randomized, open label, prospective, two arm, comparative, multicentric study evaluated the efficacy and safety of montelukast 10 mg + fexofenadine 120 mg (MF) fixed dose combination (FDC) versus montelukast 10 mg + levocetirizine 5 mg (ML) FDC in subjects with AR. Materials and methods: The adult subjects were randomized to either treatment: ML (n = 62), MF (n = 56), administered once-daily for 14 days. The primary endpoint was the change in total symptom score (TSS) (the sum of total nasal symptom score [TNSS]) and total ocular symptom score (TOSS]) at the end of study as compared to baseline. The secondary endpoints were TNSS and TOSS: At the end of study as compared to baseline, physician’s and patient’s global assessment for efficacy and tolerability and adverse events. Results: Both groups were comparable with respect to demographic characters and vital parameters. In MF group, the reduction in TSS at the end of study was 93.86% as compared to 87.71% in ML. The changes in TNSS and TOSS at the end of study were 92.52% and 95.34% in MF group as compared to 85.58% and 92.23% in ML group. Global impression by investigator showed 53.23% subjects rated excellent to very good with MF as compared to 36.36% subjects with ML. Global impression by subjects showed excellent to very good rating for 50% subjects with MF and for 34.54% subjects with ML. Conclusions: Montelukast + fexofenadine showed better improvement in symptoms of AR and a better global impression by both investigators and subjects compared to montelukast + levocetirizine.
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Background:Allergic rhinitis is one of the most common conditions in clinical practice. Motelukast and second generation antihistamine fexofenadine are routinely used in the management of allergic rhinitis. Individually both drugs have been found to be effective in allergic rhinitis. Fixed dose combination of montelukast 10 mg plus fexofenadine 120 mg is available in India is also used in the treatment of allergic rhinitis. Objective: To evaluate the efficacy and safety of montelukast and fexofenadine fixed dose combination in the management of patients with allergic rhinitis. Material and methods: Post marketing observational study was conducted in 809 patients from all over India. All the patients were treated with montelukast 10 mg plus fexofenadine 120 mg fixed dose combination once daily for 14 days. The primary outcome criteria was the change in total symptom score (Sum of total nasal symptom score and total ocular symptom score) at the end of study compared to baseline. The secondary outcome criteria included change in total nasal symptom score (nasal congestion, rhinorrhea, nasal itching, and sneezing) and total ocular symptom score (Itching/burning eyes, tearing/ watering eyes and eye redness) at the end of study compared to baseline and physician’s and patient’s global assessment for efficacy and tolerability. The patients were evaluated at baseline, day 7 and day 14 for efficacy evaluation while the safety parameters were assessed at screening and day 14. Results: The fixed dose combination of fexofenadine plus montelukast was significantly effective in reducing total symptom score, total nasal symptom score and total ocular symptom score (p<0.0001 for all parameters). The global assessment of efficacy evaluation by both patient and investigators demonstrated “excellent to good” efficacy in >95% of patients. Most of the study population reported “good” tolerability with the fixed drug combination. No adverse events were reported in the study. Conclusion: The fixed dose combination of fexofenadine plus montelukast was found to be efficacious and well tolerated in allergic rhinitis in Indian adult patients.
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Acetatos/administração & dosagem , Acetatos/análogos & derivados , Acetatos/farmacologia , Adulto , Combinação de Medicamentos , Feminino , Humanos , Índia , Masculino , Pessoa de Meia-Idade , Quinolinas/administração & dosagem , Quinolinas/análogos & derivados , Quinolinas/farmacologia , Vigilância de Produtos Comercializados , Rinite Alérgica/tratamento farmacológico , Rinite Alérgica/epidemiologia , Terfenadina/administração & dosagem , Terfenadina/análogos & derivados , Terfenadina/farmacologia , Resultado do TratamentoRESUMO
Fexofenadine (Allegra(R) 180) is a second-generation antihistamine. It is widely used as anti-allergic drug, which suppresses various allergic reactions mediated by histamines. A few cases of H1-antihistamine-induced urticaria have been reported. Herein, we report a rare case of fexofenadine-induced urticaria which was confirmed by a prick test, oral provocation test, and flow cytometry assisted-basophil activation test.
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Teste de Degranulação de Basófilos , Citometria de Fluxo , Hipersensibilidade , Terfenadina , UrticáriaRESUMO
The purpose of the present study was to comparatively evaluate the effect of newer antihistamines on psychomotor functions in Indian population. Seventy five patient volunteers were included in the study. Volunteers were put into 5 groups based on the type of antihistamine prescribed. Group-1 volunteers included those who were prescribed no antihistamine, group-2 were prescribed first generation antihistamines, group 3, 4 & 5 were prescribed second generation antihistamines cetrizine, fexofenadine and loratadine respectively. A battery of four psychomotor function tests: critical flicker fusion threshold (CFFT), digit symbol substitution test (DSST), finger tapping (FT) and visual analogue scale (VAS) for day time sedation was used in the study. First generation antihistamines impaired psychomotor functions establishing the validity of psychomotor function tests chosen for the study. Second generation antihistamines did not significantly affect CFFT frequency, but DSST score was significantly reduced. Fexofenadine significantly reduced FT score. All antihistamines produced sedation except loratadine on VAS. Second generation antihistamines impaired psychomotor performance in Indian patients, however there were individual differences evident in respect to the effect of drugs.
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BACKGROUND: Fexofenadine (Allegra(R)) is a H1-receptor selective antihistamine which exhibits consistent efficacy and safety in the treatment of allergic diseases. We thought that fexofenadine may be useful in treatment of the pruritus associated with eczema. OBJECTIVE: The purpose of this study was to evaluate the efficacy and safety of fexofenadine in the treatment of pruritus associated with eczema. METHODS: In this study, patients with atopic and allergic contact dermatitis were divided into a group given fexofenadine 180 mg once daily with topical prednicarbate treatment group or a topical prednicarbate treatment only group, for 1 week. The primary efficacy parameter was the mean change from baseline in pruritus score, and the secondary parameters were the mean change in the incidence of scratching, the mean change in visual analogue scale (0~100 mm) of pruritus, and a comparison of patient satisfaction. RESULTS: 435 patients were included and the mean age was 32.9 years old. The mean pruritus score at baseline was 3.55 point in fexofenadine group and 3.51 point in the control group. Regarding the mean change in pruritus score, fexofenadine significantly decreased the severity of pruritus compared with the control group (p<0.05). There were no significant differences in the decrease in the incidence of scratching between the two groups. A decrease in pruritus levels utilizing visual analogue scale was significant in the fexofenadine group (p<0.05) and patient satisfaction was significantly higher in the fexofenadine group (p=0.0192). There was no significant difference in the incidence of adverse events between two groups (p=0.6237). CONCLUSION: Fexofenadine administered 180 mg once daily in combination with topical prednicarbate treatment was effective and well tolerated in this study.
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Humanos , Dermatite Alérgica de Contato , Dermatite Atópica , Eczema , Incidência , Satisfação do Paciente , Prednisolona , Prurido , TerfenadinaRESUMO
The present study was designed to evaluate the efficacy of fexofenadine in the Indian population suffering from allergic rhinitis and chronic urticaria. A total number of two hundred patients of either sex with similar demographic profile were included in the study according to inclusion and exclusion criteria. These patients were treated with fexofenadine 120mg once daily for allergic rhinitis and fexofenadine 180mg for chronic urticaria for 7 days. The efficacy was evaluated on the basis of symptoms evaluation scale score and medication effectiveness scale score at baseline, on the 3rd day and on the 7th day of completion of treatment. Results indicate that fexofenadine is highly effective in the Indian population (p<0.001) suffering from allergic rhinitis and chronic urticaria.
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The present study was conducted to assess and compare the cognitive and psychomotor effects of fexofenadine, a newer second generation antihistamine with cetirizine, diphenhydramine and placebo in 10 healthy adult volunteers in a double blind, randomized cross over study. Following single dose of each drug, the volunteers were subjected to perform a series of tests of cognitive and psychomotor performance at 1, 3 and 6 hours post dose. The test battery consisted of both subjective and objective tests which were further grouped into instrumental and non-instrumental. Instrumental tests included – Simple reaction time (SRT), Multiple Choice ReactionTime Task (MCRT) and Critical Flicker Fusion frequency threshold (CFFT). The tests used in the non instrumental group were- Stanford Sleepiness Scale (SSS), Digit Cancellation Task (DCT), Digit Symbol Substitution Task (DSST) and mental arithmetic tests. Fexofenadine at doses of 120 mg was not significantly different from placebo in any of the tests used. However, as expected for a verum, all the measures were significantly disrupted by diphenhydramine 25 mg upto 6 hours post dose. Cetirizine 10 mg has produced significant subjective somnolence at 3 & 6 hours post dose but without any impairment of objective tests. These results allow the conclusion that fexofenadine at its recommended therapeutic dose of 120 mg is free from impairment effects on aspects of psychomotor function and hence can be used safely. Cetirizine is mildly sedating though it did not impair any of the objective psychometric tests.
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Fexofenadine, the derivative of terfenadine, has been shown to produce no side-effect on the heart, not distributed to the central nervous system (CNS), and having high selectivity for peripheral histamine H1-receptors. Fexofenadine is an effective antihistamine for the treatment of many allergic diseases. The authors have studied the CNS depressant effects of a higher dose of Fexofenadine, a 180 mg tablet, in 20 normal Thai volunteers, 10 males and 10 females with ages ranging from 25 to 52 years, using a double blind cross-over placebo controlled design by comparing it with chlorpheniramine 4 mg tablet. The test methods were both subjective and objective, i.e., visual analogue scale, alertness rating scale, card sorting test, glassbead picking test, and recording of the reaction time to light stimulation. Neither the fexofenadine 180 mg tablet nor the placebo caused any CNS side-effects. However, the chlorpheniramine 4 mg tablet caused significant CNS side-effects.
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Fexofenadine, derivative of Terfenadine has been proved to be not distributed to the CNS, having high selectivity for peripheral histamine H1-receptors. Fexofenadine is an effective antihistamine for the treatment of many allergic diseases. The authors have studied the CNS depressant effects of Fexofenadine in 20 nomal Thai volunteers; 10 males, 10 females, age ranged 25 to 52 years, using the double blind cross-over placebo controlled design comparing with chlorpheniramine. The test methods were both subjective and objective i.e. visual analogue scale, alertness rating scale, card sorting test, glassbead picking test, recording of the reaction time test for light stimulation. There is no CNS side effect caused by Fexofenadine as well as placebo. Chlorpheniramine caused significant CNS side effects.