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Background: Second generation antihistamines are first line therapy for chronic spontaneous urticaria (CSU). Sedation has been always a concern as a side effect of antihistamine for both patients and treating dermatologist. It is always better to prefer non-sedative antihistamine for CSU. Bepotastine is such promising non-sedative agent. Aim and Objectives: The objective of the study was to compare the efficacy and safety of bepotastine and levocetirizine in patients of CSU. Materials and Methods: This is a double arm, open label, randomized, and controlled study. Out of 99 patients, 50 patients belonged to Group A while 49 belonged to Group B. Subjects in Group A received bepotastine 10 mg twice daily while subjects in Group B received levocetirizine 5 mg once daily for 8 weeks. Patients were evaluated at baseline, day 14, day 28, and day 56 using Urticaria Activity Score (UAS) and Urticaria Control Test (UCT) for efficacy; and visual analog scale (VAS) for safety, that is, sedation. Results: The fall in mean UAS scores was statistically significant at day 14, day 28, and day 56 for both Groups A and B (P < 0.05) on intragroup comparison. While comparing the overall improvement between the two groups, there was no significant difference in UAS and UCT score at day 14, day 28, and day 56 between Group A and Group B, respectively (P > 0.05). At day 56, there was significant difference in mean VAS of Group A and B. Only one patient in Group B developed headache. Conclusion: Thus, both levocetirizine and bepotastine are equally effective for the treatment of CSU. Bepotastine has less sedative potential than levocetirizine.
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Background: Levocetirizine, the R-enantiomer of Cetirizine has pharmacokinetically and pharmacodynamically favourable characteristics, with rapid onset of action, high bioavailability, high affinity for and occupancy of the H1-receptor, limited distribution, minimal hepatic metabolism together with minimal side effects. Non-steroidal anti-inflammatory drugs (NSAIDs) have been used for many years for analgesic, anti-inflammatory, and more recently in the case of aspirin, antithrombotic purposes. Because of the significant side effect profiles of steroidal and NSAID medications, there is a greater interest in newer compounds such as antihistaminic drugs. This article will consider the potential or otherwise of the reported analgesic and anti-inflammatory effects of levocetirizine to enhance its effectiveness in the treatment of allergic disease with pain.Methods: Albino Wistar rats of either sex weighing 150-250 grams were used. For both Analgesic activity and Anti-inflammatory activity, 4 groups consisting of 6 animals per group were used. Group I: Control: 1% Gum acacia. 2ml/kg, Group II: Standard drug: Diclofenac sodium 4.5mg/kg; Group III: Test Drug 1: Levocetirizine 1mg/kg; Group IV: Test Drugs 2: Levocetirizine 1mg/kg+Diclofenac sodium 4.5mg/kg. Drugs were administered orally. For analgesic activity, Tail clip method and Hot plate method was used. For acute anti-inflammatory activity Carrageenan induced rat paw oedema method was used.Results: Levocetirizine, is found to have significant analgesic activity in rats (1 mg/kg dose) alone and in combination with Diclofenac Sodium in Haffner’s Tail Clip method and Eddy’s Hot Plate Method. Levocetirizine also has got prominent anti-inflammatory activity in acute models evidenced by percentage inhibition of acute rat paw oedema.Conclusions: Levocetirizine possess analgesic and acute anti-inflammatory activity alone and in combination with Diclofenac sodium.
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Background: Urticaria results from many different stimuli and numerous factors like immunologic, non-immunologic, genetic and modulating factors which are involved in its pathogenesis and ultimately converge on mast cells and basophils to release mediators and produce urticarial lesions. This study is aimed to compare the therapeutic effectiveness of Levocetirizine (newer generation H1 blocker), prednisolone (glucocorticoid) and their combination in the treatment of chronic urticaria.Methods: Group I (34 patients received tab Levocetirizine alone 5mg daily for 15 days). Group II (33 patients received tab Prednisolone alone 20mg /day for initial 3 days and later dose was gradually tapered by 5mg /day every 3 days to 5mg/day with total duration of 12 days). Group III (33 patients received the combination of Levocetirizine and Prednisolone).Results: The Group -I patients average eosinophil count before and after treatment was 4±1.4 and 2.4±0.8 respectively, with an average difference of 1.7±1.3. In Group - II patients average eosinophil count before and after treatment was 4.0±1.1 and 2.5±0.3 respectively, with an average difference of 1.5±1.1. In the Group - III patients the average eosinophil count before and after treatment was 4.3±1.0 and 2.1±1.0 with an average difference of 2.2±1.3. In G-I (n=34).Conclusions: Statistical analysis of the present study showed that the combination of Levocetirizine and prednisolone therapy was significantly (P<0.05) greater than prednisolone alone therapy and improvement with Levocetirizine alone (79%) was almost similar to combination therapy (85%).
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Aim: To compare the therapeutic efficacy and safety of Rupatadine and mometasone with Levocetirizine which is most commonly used drug.To study the effects of levocetirizine, Rupatadine and mometasone on absolute eosino-phil count and IgE levels. Methodology:The participants were randomlydivided into 3 groups of 25 patients each and treated as follows: Group I: were treated with Levocetirizine 5mg OD for 14 days, Group II: were treated with Rupatadine 10mg OD for 14 days, Group III: were treated with Mometasone two sprays (50mcg of mometasone in each spray) in each nostril once daily (total daily dose of 200mcg) for 14 days. The patients were asked to report at the hospital after 14 day and they were followed up with regard to clinical improvement of symptoms and signs and any adverse effects as reported by the patient. Rhinoscopy finding, X-ray of para nasal sinus, improvement in symp-toms (sneezing, Itching, nasal discharge, nasal blockage and anosmia) Absolute eosinophils count, Serum IgE levels and adverse reports were studied and investigation were compared before and after treatment. Result: Rhinoscope finding showed treatment with mometasone became normal but X-Ray of para nasal sinus results showed levocetir-zine showed higher rate of improvement. In improvement of symptoms sneezing, itching and nasal discharge was high mometasone. In all groups post treatment there was no changes in Ig E and Absolute Eosinophil’s count. ADR reported with mometaxone. Conclusion: The three drugs, levocetirizine, rupatadine and mometasone were found to have similar levels of efficacy in controlling the symptoms of the allergic rhinitis. The physical signs improved better with mometasone than the other 2 drugs. The 3 drugs levocetirizine, rupatadine and mometasone had no significant effect on the absolute eosinophil count and the serum IgE levels. Adverse effects were found to be more with levoce-tirizine than the other two drugs. Considering this factor and also the fact that long term use of corticosteroids like mometasone is undesirable, rupatadine appears to be a better choice in the treatment of allergic rhinitis.
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Objective To observe the effect of Bupiyichang pills combined with levocetirizine in the treatment of 56 patients with chronic urticaria,so as to provide clinical guidance and basis.Methods 118 patients with chronic urticaria were selected for our study,and after informed consent they were randomly divided into observation group and control group.The observation group were was treated by Bupiyichang pills combined with levocetirizine,and the control group were was treated by levocetirizine.When they were curingAfter treatment for 10,20,and 30 days,the effective rates in the two groups were calculated and compared with each other.And at the day before treating and the day after treating for 20 days,the serum IgE levels in each group was detected and compared.The falling ranges between the two groups were calculated and compared.Results When they were curing treated for 10,20,and 30 days,the effective rates in the observation group were 76.79％,94.64 ％,85.71％,respectively,which in those of the control group were 59.68％,74.19％,64.52％,respectively,the differences between the two groups were statistically significance significant (x2 =3.94,9.11,6.97,all P ＜ 0.05).At the day before treating and the day after treating for 20 days,the serum IgE levels in the observation group were (384.71 ± 65.62) U/mL and (214.59 ±40.71) U/mL respectively,the difference was statistically significance significant (t =10.93,P ＜ 0.05);and the serum IgE levels in the control group were (380.25 ± 67.81)U/mL and (256.99 ± 53.21)U/mL respectively,the difference was statistically significancesignificant (t =9.37,P ＜ 0.05).The falling ranges in the observation group and the control group were (170.12 ± 35.59) U/mL and (123.26 ± 53.31) U/mL respectively,the difference was statistically significance significant between the two groups (t =7.82,P ＜ 0.05).Conclusion Bupiyichang pills combined with levocetirizine is more effective than single medication of levocetirizine.
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Objective To discuss the clinical therapeutic effect of Kangmin xiaoyan lotion combined with levocetirizine hydrochloride in the treatment of facial recurrent dermatitis. Methods Eighty cases of facial recurrent dermatitis were randomly divided into treatment group and control group,40 cases in each group.The treatment group was given Kangmin xiaoyan lotion with wet compression for 20 min in the morning and evening,and levocetirizine hydrochloride 10 mL orally once daily;the control group was only given levocetirizine hydrochloride orally once daily.One month later,the symptoms and signs of skin lesions and adverse reactions in each group were observed. Results One month after the treatment,the scores of symptoms and signs were significantly decreased in the two groups (P<0.05).After the treatment,the scores were significantly different between the two groups (P<0.05).Clinical efficacy of the treatment group and control group was 92.5% and 65.0%,with significant difference(P<0.05). Conclusion Kangmin xiaoyan lotion can be effective in the treatment of facial recurrent dermatitis,and it is worthy of clinical application.
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This study describes the development of a rapid, selective, precise and sensitive reverse phase high-performance liquid chromatography method for the quantitative determination of Levocetirizine Dihydrochloride (LCD) in human plasma and pharmaceutical dosage form. Extraction of drug from plasma was done by employing optimized liquid-liquid extraction procedure. The sample was analyzed using Acetonitrile: Methanol: 20mM Ammonium Acetate Buffer pH-5 (25:55:20 % v/v/v) as mobile phase. Chromatographic separation was achieved on Prontosil C-18 column (4.6 x 250mm, 5μ particle size) as stationary phase using isocratic elution (at a flow rate of 1 mL/min). The peak was detected using UV-PDA detector set at 232 nm and retention time was found to be 8 min for LCD. The calibration curve obtained was linear (r2= 0.9998) over the concentration range of 2-10 μg/mL. Method was validated for precision, robustness and recovery. The limit of detection (LOD) and limit of quantitation (LOQ) was 0.0057 and 0.174 µg/mL respectively. There was no significant difference between the amount of drug spiked in plasma and the amount recovered and plasma did not interfere in estimation. Thus, the proposed method is suitable for the analysis of LCD in tablet dosage forms and human plasma.
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OBJECTIVE:To establish a method for the determination of related substances in Levo-cetirizine hydrochloride chewable tablet. METHODS:RP-HPLC was performed on the column of Venusil XBP-CN with mobile phase of acetonitrile-0.05 mol/L Sodium dihydrogen phosphate solution(pH value adjusted to 3.0 by phosphoric acid)(60∶40,V/V)at a flow rate of 1.0 ml/min, the detection wavelength was 230 nm,column temperature was 25 ℃,and volume injection was 20 μl. RESULTS:Levo-cetirizine hydrochloride chewable tablet showed good separation with related substances;the linear range of levo-cetirizine hydrochloride was 1.2-2.8 μg/ml(r=0.999 9);the quantification limit and detection limit was 1.4 ng/ml and 0.3 ng/ml,respectively;RSDs of preci-sion,stability and reproducibility tests were lower than 1%;recovery was 96.3%-105.0%(RSD=1.7%,n=9);the contents of re-lated substances were no more than 0.17%. CONCLUSIONS:The method is simple,sensitive,reproducible,accurate and reli-able,and can be used for the determination of related substances in Levo-cetirizine hydrochloride chewable tablet.
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Levocetirizine is a second-generation nonsedative antihistaminic agent that has been demonstrated to be safe and effective for treating allergic disease. There was only one case report of levocetirizine-induced liver toxicity, but a liver biopsy was not performed. In this article, we present the first case of levocetirizine-induced liver injury with histologic findings. A 48-year-old man was hospitalized with jaundice and generalized pruritus that had developed after 2 months of therapy with levocetirizine for prurigo nodularis. Laboratory findings revealed acute hepatitis with cholestasis. A liver biopsy demonstrated portal inflammation and hepatitis with apoptotic hepatocytes. The patient fully recovered 3 weeks after withdrawing levocetirizine. Although levocetirizine is safe and effective, physicians should be aware of its potential hepatotoxicity.
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Humans , Male , Middle Aged , Cetirizine/adverse effects , Chemical and Drug Induced Liver Injury/diagnosis , Histamine H1 Antagonists, Non-Sedating/adverse effects , Hypersensitivity/drug therapy , Jaundice/etiology , Liver/pathology , Pruritus/etiologyABSTRACT
Objective To evaluate the efficacy and safety of olopatadine hydrochloride for the treatment of chronic idiopathic urticaria (CIU). Methods A multicentre, double-blind, randomized, parallel-group, controlled clinical trial was conducted. A total of 144 patients with CIU from 3 research centers were enrolled into this study, and randomly and equally divided into a test group and a control group. The test group administrated olopatadine hydrochloride 5 mg twice a day for 28 consecutive days, while the control group administrated levocetirizine hydrochloride 5 mg in the forenoon and a placebo tablet of olopatadine hydrochloride 5 mg in the afternoon for 28 consecutive days. The symptom score reducing index(SSRI)served as the primary outcome, and global assessment score for efficacy and total response rates as the secondary outcome. Results Totally, 137 patients completed the trial, including 70 in the test group and 67 in the control group. As intention-to-treat analysis showed, there were no significant differences in the total response rate between the test group and control group on day 7 (64.29% (45/70)vs. 56.72%(38/67), P > 0.05), 14(82.86%(58/70)vs. 74.63%(50/67), P > 0.05), or 28(87.14%(61/70)vs. 77.61%(52/67), P >0.05)after start of treatment. The SSRI was significantly higher in the test group than in the control group after 4 weeks of treatment(82.67% ± 22.70% vs. 70.51% ± 32.07%, P 0.05), and adverse reactions mainly included lethargy, dry mouth, fatigue, etc. Conclusion Olopatadine hydrochloride is effective and safe for the treatment of CIU.
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OBJECTIVE:To prepare Levocetirizine hydrochloride chewable tablets,and to investigate the stability. METH-ODS:Levocetirizine hydrochloride chewable tablets were prepared with wet granulation. Using accumulative dissolution rate within 45 min as index,the formulation of Levocetirizine hydrochloride chewable tablets was optimized by orthogonal design with the in-ternal and external ratio of MCC and carboxymethyl starch sodium,the amount of magnesium stearate as factors. The dissolution rate and content uniformity of optimized tablet were verified. The appearance,dissolution rate,related substance and content change of the tablet were investigated within 10 d under the condition of high temperature(60 ℃),high light(4 500 lx)and high moisture (92.5%). RESULTS:The optimized formulation of the tablet was as levocetirizine hydrochloride 5 mg,lactose 30 mg, microcrystalline cellulose 90 mg(internal-external ratio 4∶5),mannitol 60 mg,aspartame 10 mg,carboxymethyl starch sodium 12 mg(internal-external ratio 1∶1)and magnesium stearate 1.0%. The accumulative dissolution rates of 3 batches of optimized tablet were(97.23±1.21)%,(98.49±1.28)% and(98.15±1.94)%. The content uniformity were 2.30,2.34 and 2.60. Those indicators had no significant change except related substance increased slightly under high temperature on 10th day and high moisture on 5th day. CONCLUSIONS:Levocetirizine hydrochloride chewable tablets is prepared successfully with good stability.
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PURPOSE: To evaluate the efficacy and safety of once-daily ciclesonide in comparison to both levocetirizine alone, and a ciclesonide/levocetirizine combination in patients with seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR). METHODS: Subjects exhibiting moderate to severe allergic rhinitis for longer than 1 year were randomized in an open-label, 3-arm, parallel group, multicenter study. Subjects received 200 microg ciclesonide, 5 mg levocetirizine, or a combination of both. Changes from baseline until the end-of-study visit (2 weeks following) were evaluated by reflective total nasal symptom scores (rTNSSs), reflective total ocular symptom scores (rTOSSs), physician-assessed overall nasal signs and symptoms severity (PANS), and rhinoconjunctivitis quality-of-life questionnaires (RQLQ). RESULTS: Significant improvements in rTNSS, PANS, and RQLQ in the ciclesonide monotherapy group were observed in comparison to the levocetirizine alone group. Three individual symptoms of rTNSS, including runny nose, nasal itching, and congestion, were improved in the ciclesonide-treated group. rTOSS scores for ciclesonide monotherapy improved from baseline, but no superiority over levocetirizine was shown. The absolute score and changes in rTNSS and PANS were positively correlated. Ciclesonide spray was more effective than levocetirizine in reducing nasal symptoms in both SAR and PAR patients. Ciclesonide and levocetrizine were well tolerated alone and in combination. CONCLUSIONS: Our results provide support for an AR and its Impact on Asthma (ARIA) recommendation stipulating that ciclesonide is superior to levocetirizine for the treatment of AR, with tolerable safety. Addition of levocetirizine to ciclesonide did not give further clinical benefit over monotherapy.
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Humans , Asthma , Estrogens, Conjugated (USP) , Nose , Pruritus , Rhinitis , Rhinitis, Allergic, Seasonal , Surveys and QuestionnairesABSTRACT
Objective To explore the clinical efficacy and value of azo steen,montelukast sodium combined with levocetirizine in the treatment of chronic urticaria. Methods 150 cases with chronic urticaria admitted in department of dermatology of Hubei Zhongshan Hospital were divided into A,B and C group,each group had 50 cases. Patients in group A were received montelukast sodium and levocetirizine treatment,which in group B were received montelukast sodium and azo steen treatment,group C were received above three kinds of drug treatment. Total effective rate,adverse reaction and safety in three groups were observed and compared. Results Total effective rate of group C was significantly higher than A and B group(P<0.05), and the safety of group C were better than A and B group(P<0.05 ),too. The occurrence of adverse reaction in group C was significantly less than that in group A and B (P <0.05 ).Conclusion Azo steen,montelukast sodium combined with levocetirizine has good efficacy in treatment of chronic urticaria. It can relieve itching wheals and other symptoms in a short time,with less adverse reaction.
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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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Fixed drug eruption is an uncommon adverse drug reaction caused by delayed cell-mediated hypersensitivity. Levocetirizine is an active (R)-enatiomer of cetirizine and there have been a few reports of fixed drug eruption related to these antihistamines. We experienced a case of levocetirizine-induced fixed drug eruption and cross-reaction with other piperazine derivatives confirmed by patch test. A 73-year-old female patient presented with recurrent generalized itching, cutaneous bullae formation, rash and multiple pigmentation at fixed sites after taking drugs for common cold. She took bepotastine besilate (Talion®) and levocetirizine (Xyzal®) as antihistamine. She took acetaminophen, pseudoephedrine 60 mg / triprolidine 2.5 mg (Actifed®), dihydrocodeinebitartrate 5 mg / di-methylephedrine hydrochloride 17.5 mg / chlorpheniramine maleate 1.5 mg / guaifenesin 50 mg (Codening®) and aluminium hydroxide 200 mg / magnesium carbonate 120 mg (Antad®) at the same time. Patch test was done with suspected drugs and the result was positive with levocetirizine. We additionally performed patch test for other antihistamines such as cetirizine, hydroxyzine, fexofenadine and loratadine. Piperazine derivatives (cetirizine and hydroxyzine) were positive, but piperidine derivatives (fexofenadine and loratadine) were negative to patch test. There was no adverse drug reaction when she was challenged with fexofenadine. We report a case of levocetirizine-induced fixed drug eruption confirmed by patch test. Cross-reactions were only observed in the piperazine derivatives and piperidine antihistamine was tolerant to the patient.
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Aged , Female , Humans , Acetaminophen , Carbon , Cetirizine , Chlorpheniramine , Common Cold , Drug Eruptions , Drug-Related Side Effects and Adverse Reactions , Exanthema , Guaifenesin , Histamine Antagonists , Hydroxyzine , Hypersensitivity , Loratadine , Magnesium , Patch Tests , Pigmentation , Pruritus , Pseudoephedrine , TriprolidineABSTRACT
Our study aims to design a controlled drug delivery system for Levocetirizine dihydrochloride by using chitosan beads. The beads were prepared by ionotropic gelation process, with Sodium tri poly phosphate (TPP) as an ionic agent. The formed beads were then further crosslinked using glutaraldehyde and the excess glutaraldehyde were then washed. The physical properties of the prepared beads such as beads sizes, shapes, encapsulation efficiencies, invitro release and degree of swelling were determined. The produced beads from all batches showed a very good spherical geometry with the bead size found to be less than 2mm. The drug loading efficiency was around 77.5% for all batches. The degree of swelling was found to be 1.4. FTIR, DSC and XRD studies shows the absence of the interaction between chitosan and the drug. This methodology of preparation of chitosan beads seems to be highly simple, commercially viable and a promising technique for controlling the release of drugs.
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Objective To study the effects of Xiaofengzhiyang Particles and Levocetirizine on elderly urticaria and effects on the serum levels of IL-2 and IgE.Methods 96 elderly patients were randomly divided into two groups.The patients in study group were prescribed with Xiaofengzhiyang Particles and Levocetirizine.The patients in control group were prescribed with Levocetirizine,two weeks for a course.The curative effect and serum levels of IL-2 and IgE were observed after treatment.Results The complete cure rate of the study group was 69.6％,the control group was 52.5％.There was significant difference between the two groups(P＜0.05).The serum levels of IL-2 and IgE were significantly decreased in study group(all P＜0.01).Conclusion Xiaofengzhiyang Particles combined with Levocetirizine is effective in treating elderly urticaria,and the two drugs together could reduce the serum levels of IL-2 and IgE.
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A simple and rapid high-performance liquid chromatographic (HPLC) method for the determination levocetirizine has been developed. The chromatographic system consisted of a Water 2695 binary gradient pump, Water 2487 dual wavelength absorbance detector, and Empower 2 software. Separation was achieved on the XTerra symmetry C18 column at room temperature. The sample was introduced through an injector valve with a 20 μL sample loop. The results obtained showed a good agreement with the declared content. Recovery values of levocetirizine in tablets were from 99.57-100.48 %. The proposed method is rapid, accurate and selective; it may be used for the quantitative analysis of levocetirizine from raw materials, in bulk drugs and other dosage formulations.