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Background: CSU (chronic spontaneous urticaria) is the most diagnosed dermatological condition reported to clinicians. Second-generation antihistamines have proven to be effective in controlling the CSU. Following the guidelines, combined use of antihistamines is less recommended owing to the lack of synergistic effects. It is vital to explore effective management options owing to the challenges of CSU. Aims: The present study aimed to assess the efficacy and safety of the combination of 5mg levocetirizine and 20mg bilastine to 40mg bilastine up dosing for treating subjects with chronic spontaneous urticaria. METHODS: The present study assessed 124 subjects that were divided into two groups of 62 subjects each where Group I subjects were given a tablet of Bilastine in a dose of 20 mg bd and Group II subjects were given a combined tablet of bilastine in 20 mg dose and Tablet Levocetirizine in 5 mg dose. Urticarial activity score 7 was used at baseline and follow-up visits of 2 and 6 weeks. Results: The study results showed that in both groups, there were a higher number of males in the age range of 20-30 years. Angioedema was seen in 15.6% and 23.3% of subjects from Groups I and II respectively. After 6 weeks, significant improvement was seen in both the groups concerning UAS 7 scores with p<0.05. In Group I, a remarkable decrease was seen in UAS 7 scores from 19.4% to 0.03% with minimum side effects. Conclusion: The present study concludes that up-dosing of bilastine is a well-tolerated, secure, and efficient method in comparison to the combined dose of 20 mg Bilastine and 5mg Levocetirizine depicting the up-dosing of Bilastine can be a valuable and efficient addition to the current arsenal of medication with minimal to no side-effects. [ABSTRACT FROM AUTHOR]

Background: Eosinophil-derived neurotoxin (EDN) is an important biomarker of eosinophilic inflammation. Methods: This study evaluated Montelukast treatment response according to EDN concentration in children with perennial allergic rhinitis (PAR). Fifty-two children with PAR were recruited and took a combination of Montelukast (5mg) and Levocetirizine (5mg) "Mont/Levo Group" or only Montelukast (5mg) "Mont Group" for 4 weeks. All caregivers were instructed to record rhinitis symptoms for 4 weeks. EDN was measured before and after treatment. Results: Daytime nasal symptom scores (DNSS) significantly decreased in both the Mont/Levo (p = 0.0001; n = 20) and Mont Group (p < 0.0001; n = 20), but there were no significant differences between the two groups. EDN concentration also significantly decreased after treatment in both groups (p < 0.0001 and p < 0.001, respectively). For secondary analysis, children with a high initial EDN concentration (EDN ≥ 53 ng/mL) were placed in the "High EDN Group", while those with a lower initial EDN concentration (EDN < 53 ng/mL) were put in the "Low EDN Group". Both groups experienced significant reductions in DNSS after either treatment regimen (p < 0.0001 and p = 0.0027, respectively) but the High EDN Group had greater reductions. EDN concentrations in the High EDN Group decreased significantly from either treatment (p < 0.0001). Conclusion: We found that children with AR and a high serum EDN concentration may respond well to Montelukast treatment. A therapeutic strategy using EDN concentrations in patients with AR to evaluate therapeutic response may help improve quality of care. [ABSTRACT FROM AUTHOR]

Background: Chronic spontaneous urticaria (CSU) refers to urticaria that has no specific cause or trigger, present on most days of the week for 6 weeks or more. The incidence of chronic urticaria in the pediatric age group is between 0.1% and 3%. Levocetirizine and bilastine are nonsedative second-generation antihistamines used to treat urticaria in both adults and children. Objective: The primary objective was to compare the effectiveness of levocetirizine and bilastine in cases of pediatric CSU using Urticaria Activity Score (UAS) and Urticaria Severity Score (USS). The secondary objective was to evaluate and compare the safety and quality of life (QoL) using the Dermatology Life Quality Index (DLQI) score. Materials and Methods: This was a randomized, observer-blinded study where 65 patients (6–16 years) with a history of urticaria >6 weeks were divided into two groups with computer-generated randomization. Thirty-two patients were included in Group A, who received levocetirizine, and 33 patients were included in Group B, who received bilastine. UAS7, USS, and DLQI were recorded at every visit. The primary outcome was measured using UAS and USS and the secondary outcome in the form of patient’s QoL was assessed using the DLQI score. Laboratory parameters were assessed at the first visit and at the end of 3 months. Results: There was a significant difference (P = 0.002) in UAS7, USS, and DLQI between the baseline and last visit scores for each group. There was no significant difference (P = 0.28) in the scores between the two groups. Laboratory parameters like liver enzymes and complete blood count also did not show any significant differences between the two groups. Conclusion: Both levocetirizine and bilastine are equally effective and safe in the treatment of CSU at the end of 3 months. However, bilastine showed a better fall in the DLQI as compared to levocetirizine.

Levocetirizine dihydrochloride is an effective antiallergenic drug applied mostly orally; however, developing a topical formulation for localized treatment could be beneficial. To achieve this, a modified formulation technique is necessary to enhance bioavailability efficiency and minimize possible side effects. Therefore, levocetirizine particles were prepared by immobilization on mesoporous silica material. Both the dihydrochloride form and its free base of levocetirizine were fixed on a silica-type Syloid support. Immobilization of the active ingredient levocetirizine in a free base form on a Syloid support by mixing in a dichloromethane solution provides better surface coverage (65.5%) than immobilization in the dihydrochloride form in water or methanol (24.5% for both). The successful binding of levocetirizine was confirmed by X-ray photoelectron spectroscopy and infrared measurements. The active ingredient in the form of hydrochloride is more likely to be in the pores, while the free base is bound to the surface in larger quantities. The time-dependent levocetirizine release showed that the liberation of the active ingredient from the Syloid is slower than the dissolution of the starting active ingredient itself, so it may be suitable for exerting a more reliable and prolonged local effect. A gel containing a Syloid-fixed levocetirizine free base was tested in vivo in a croton oil-induced ear edema mouse model. When compared to a reference gel, the half-dose formulation containing levocetirizine free base demonstrated a similar efficacy to Fenistil gel, indicating that the new formulation may offer superior effectiveness at lower doses. [ABSTRACT FROM AUTHOR]

AbstractObjectiveData sourcesStudy selectionsResultsConclusionThis meta-analysis aims to evaluate the efficacy and safety of montelukast combined with levocetirizine in the treatment of allergic rhinitis with asthma, and to provide objective and effective evidence-based medical evidence for clinical use.PubMed, Web of Science, Cochrane Library, WANFANG DATA, CNKI, and Chinese BioMedical Literature Database were retrieved to identify records related to montelukast combined with levocetirizine in the treatment of allergic rhinitis with asthma.First, the eligibility criteria were employed to screen search results. Then, two investigators independently assessed titles, abstracts, and the full text of all retrieved references to identify potentially eligible studies.As of 2024-02-03, a total of six articles were included in this meta-analysis, covering 2,950 patients with allergic rhinitis with asthma. The meta-analysis results exhibited a pooled NSS of −1.28 (95%CI: −1.64 to −0.92), suggesting that the combination of montelukast and levocetirizine was effective in the treatment of nasal symptoms of allergic rhinitis complicated with asthma. The meta-analysis of controlled trials showed that the SMD of NSS in the group of montelukast combined with levocetirizine was −2.56 (95%CI: −2.77 to −2.35). The result indicated that compared with the control group, the combination of montelukast with levocetirizine significantly improved the symptoms of allergic rhinitis.In summary, this meta-analysis demonstrated the efficacy of montelukast combined with levocetirizine in the treatment of nasal symptoms in AR with asthma, indicating that the combination of montelukast with levocetirizine is more effective in improving symptoms of allergic rhinitis than monotherapy and has good safety. [ABSTRACT FROM AUTHOR]

Introduction: Chronic spontaneous urticaria (CSU) is characterized by urticaria persisting for more than 6 weeks. Antihistamines, notably sgAH (second generation antihistamines) are the first line of treatment for CSU. Areas covered: This consensus aimed to review the existing research on receptor occupancy of antihistamines, including levocetirizine, and translate its implications in the treatment of CSU. The consensus deliberations were under the banner of the Antihistamine Receptor Occupancy Group (AROG) from India, an expert panel of 12 dermatologists with a mix of institutional and practitioner backgrounds. This group analyzed the existing translational research on the receptor occupancy of levocetirizine to establish the clinical efficacy and safety of levocetirizine in the treatment of CSU using the grading of recommendations assessment, development, and evaluation (GRADE) method vis-a-vis the varied SGAH. Expert opinion: SGAH constitute the first step in the therapeutic ladder for managing CSU. Levocetirizine has high bioavailability, high affinity and occupancy of the H1 receptor, rapid onset of action, limited distribution and minimal hepatic metabolism. It exhibits significant anti-inflammatory effects at clinically relevant concentrations. The marked receptor occupancy translates to enhanced efficacy as compared to similarly dosed SGAH with the lower cost making it an appropriate drug for chronic use. Receptor occupancy should be the basis of intra-class head-to-head trials in CSU. [ABSTRACT FROM AUTHOR]

Background: Chronic spontaneous urticaria (CSU) refers to urticaria that has no specific cause or trigger, present on most days of the week for 6 weeks or more. The incidence of chronic urticaria in the pediatric age group is between 0.1% and 3%. Levocetirizine and bilastine are nonsedative second-generation antihistamines used to treat urticaria in both adults and children. Objective: The primary objective was to compare the effectiveness of levocetirizine and bilastine in cases of pediatric CSU using Urticaria Activity Score (UAS) and Urticaria Severity Score (USS). The secondary objective was to evaluate and compare the safety and quality of life (QoL) using the Dermatology Life Quality Index (DLQI) score. Materials and Methods: This was a randomized, observer-blinded study where 65 patients (6–16 years) with a history of urticaria >6 weeks were divided into two groups with computer-generated randomization. Thirty-two patients were included in Group A, who received levocetirizine, and 33 patients were included in Group B, who received bilastine. UAS7, USS, and DLQI were recorded at every visit. The primary outcome was measured using UAS and USS and the secondary outcome in the form of patient's QoL was assessed using the DLQI score. Laboratory parameters were assessed at the first visit and at the end of 3 months. Results: There was a significant difference (P = 0.002) in UAS7, USS, and DLQI between the baseline and last visit scores for each group. There was no significant difference (P = 0.28) in the scores between the two groups. Laboratory parameters like liver enzymes and complete blood count also did not show any significant differences between the two groups. Conclusion: Both levocetirizine and bilastine are equally effective and safe in the treatment of CSU at the end of 3 months. However, bilastine showed a better fall in the DLQI as compared to levocetirizine. [ABSTRACT FROM AUTHOR]

Author(s): Boggarapu Sneha [1]; Murali Narasimhan [1]; Priya Cinna T. Durai (corresponding author) [1]; Ramachandran Ramakrishnan [1] Introduction Urticaria refers to recurrent, short-lived, itchy wheals of the skin associated with [...], Introduction: Chronic spontaneous urticaria (CSU) is the most commonly diagnosed skin condition in dermatology outpatient departments. Second-generation antihistamines are shown to be effective in the control of CSU. As per the guidelines, a combination of antihistamines is less recommended due to the lack of synergistic effect, though used widely. Exploring effective treatment options are crucial, given the challenges posed by CSU. Aims and Objectives: To assess the safety and efficacy of Bilastine up-dosing versus combination of 20 mg Bilastine with 5 mg Levocetirizine in the treatment of CSU. Materials and Methods: This prospective randomized non-blinded comparative trial involved 62 patients, with 32 in group A and 30 in group B. Group A received Tablet Bilastine 20 mg bd, while Group B received a combination of Tablet Bilastine 20 mg and Tablet Levocetirizine 5 mg. Urticarial Activity Score 7 was performed at baseline and follow-up visits (every 2 weeks for 6 weeks). Results: Both groups had a higher number of male patients in the 20-30 years age group. Angioedema was present in 15.6 of group A and 23.3 in group B. After 6 weeks, both the groups showed a significant improvement in UAS 7 scores (P value Conclusion: Bilastine up-dosing proved to be efficient, secure, and well tolerated when compared to the combined dose of Levocetirizine 5 mg and Bilastine 20 mg, suggesting that up-dosing of Bilastine could be a valuable addition to the current medication arsenal with the minimal side effects. Keywords: Bilastine, chronic spontaneous urticaria, levocetirizine, updosing, UAS7 score

Author(s): Abhishek De (corresponding author) [1]; Sushil Singh [1]; Disha Chakraborty [1]; Aarti Sarda [2]; Kiran Godse [3] Introduction Chronic spontaneous urticaria (CSU) is defined by the appearance of wheals [...], Introduction: The treatment options for chronic spontaneous urticaria (CSU) primarily include second generation non-sedative antihistamine (SGAHs). Bilastine is a newer, nonsedating SGAH approved for urticaria in February 2019 by the Drugs Controller General of India. Its major advantages are in terms of superior efficacy, lack of drug interactions and adverse effects, including sedation, compared to conventional SGAHs. The role of cytokines in the pathogenesis of CSU is well known. However, there is a shortage of data regarding the change in serum levels of proinflammatory cytokines following H1 antihistamines. We conducted this trial to evaluate the role of bilastine in cytokine modulation and autoimmunity, thereby explaining its role in modifying the disease process in CSU. Materials and Methods: This prospective study was conducted in a tertiary institute in Kolkata on patients aged 12 years and above with a CSU >6 months. These patients had an unsatisfactory response, as per the Urticaria Activity Score 7 (UAS7), to previous antihistamine therapies in standard doses. Treatment effectiveness was determined by comparing the UAS7 at baseline with that at weeks 4, 8 and 12. Also, baseline serum interleukin-6 (IL-6) and IL-17 were compared with those at the end of the study, that is, 12 weeks. Results: Thirty patients who matched the inclusion criteria and signed informed consent were included in the study. At the end of 12 weeks, 10 of patients (n = 3) achieved a complete treatment response (UAS = 0), whereas 43.33 of patients (n = 13) were labelled as having well-controlled urticaria (UAS Conclusion: We conclude that bilastine at a once-daily continuous dose of 40 mg for 3 months is safe and effective in CSU patients who are refractory to treatment at the standard doses of SGAHs. Improved symptomatic control with bilastine was also associated with better control over the inflammatory process, as suggested by the lowering of mean cytokine levels in our study. Keywords: Antihistamines, autoimmunity, bilastine, chronic spontaneous urticaria, cytokines

The purpose of this study was to enhance the stability of montelukast and levocetirizine for the development of a fixed-dose combination (FDC) monolayer tablet. To evaluate the compatibility of montelukast and levocetirizine, a mixture of the two drugs was prepared, and changes in the appearance characteristics and impurity content were observed in a dry oven at 60 °C. Excipients that contributed minimally to impurity increases were selected to minimize drug interactions. Mannitol, microcrystalline cellulose, croscarmellose sodium, hypromellose, and sodium citrate were chosen as excipients, and montelukast–levocetirizine FDC monolayer tablets were prepared by wet granulating the two drugs separately. A separate granulation of montelukast and levocetirizine, along with the addition of sodium citrate as a pH stabilizer, minimized the changes in tablet appearance and impurity levels. The prepared tablets demonstrated release profiles equivalent to those of commercial products in comparative dissolution tests. Subsequent stability testing at 40 ± 2 °C and 75 ± 5% RH for 6 months confirmed that the drug content, dissolution rate, and impurity content met the specified acceptance criteria. In conclusion, the montelukast–levocetirizine FDC monolayer tablet developed in this study offers a potential alternative to commercial products. [ABSTRACT FROM AUTHOR]

Levocetirizine, an antihistamine, has been analyzed in relation to temperature by volumetric, acoustic, and spectroscopic methods to investigate its interaction with glucose, the predominant carbohydrate. Density and ultrasonic velocity for LC (0–0.10 mol dm−3) at different temperature (298.15, 308.15 and 318.15 K) in water and in aqueous solution of glucose (0.05, 0.10 and 0.15 mol kg−1) have been recorded using Anton Paar DSA 5000 M. The apparent molar volume (Vϕ), limiting apparent molar volume (Vϕ0), apparent molar compressibility (Kϕ,S), limiting apparent molar compressibility (Kϕ,S0) were computed utilizing the experimental data. In addition, the transfer parameters of LC from water to aqueous glucose solutions were identified and elucidated using the co-sphere model. The transfer volumes have been utilized to estimate the interaction coefficients. Limiting apparent molar expansibility (ϕE0) and Hepler’s constant was obtained to throw light upon the structure-making or structure-breaking effect of solute. Multiple acoustical parameters like isentropic compressibility (KS), relaxation strength (r), intermolecular free length (Lf), specific acoustic impedance (Z), Wada’s constant (W), relative association (RA), Rao’s constant (Rm), molar volume (Vm), Van der Waals constant (b), and free volume (Vf) were determined to validate the thermodynamic results.

Levocetirizine dihydrochloride is an effective antiallergenic drug applied mostly orally; however, developing a topical formulation for localized treatment could be beneficial. To achieve this, a modified formulation technique is necessary to enhance bioavailability efficiency and minimize possible side effects. Therefore, levocetirizine particles were prepared by immobilization on mesoporous silica material. Both the dihydrochloride form and its free base of levocetirizine were fixed on a silica-type Syloid support. Immobilization of the active ingredient levocetirizine in a free base form on a Syloid support by mixing in a dichloromethane solution provides better surface coverage (65.5%) than immobilization in the dihydrochloride form in water or methanol (24.5% for both). The successful binding of levocetirizine was confirmed by X-ray photoelectron spectroscopy and infrared measurements. The active ingredient in the form of hydrochloride is more likely to be in the pores, while the free base is bound to the surface in larger quantities. The time-dependent levocetirizine release showed that the liberation of the active ingredient from the Syloid is slower than the dissolution of the starting active ingredient itself, so it may be suitable for exerting a more reliable and prolonged local effect. A gel containing a Syloid-fixed levocetirizine free base was tested in vivo in a croton oil-induced ear edema mouse model. When compared to a reference gel, the half-dose formulation containing levocetirizine free base demonstrated a similar efficacy to Fenistil gel, indicating that the new formulation may offer superior effectiveness at lower doses.

Levocetirizine, a levorotatory enantiomer of anti-histamine cetirizine, available as hydrochloride and useful in the management of intermittent or persistent allergic rhinitis and hay fever. Levocetirizine may interact different drugs including NSAIDswhich may cause severe adverse effects as a result of drug interactions. UV spectroscopy is a precise and applicable method with less time consumption for the calibration curve study, quantification of drugs and also to estimate drug availability alone or in the presence of another drug. In the present study, levocetirizine, diclofenac sodium, flurbiprofen, mefenamic acid and meloxicam (reference standards) were submitted for calibration curve studies, lonequantification and finally percentavailability after drug interaction of levocetirizine with diclofenac sodium, flurbiprofen, mefenamic acid and meloxicam at pH 4, 7.4 and 9 whichmight resulted in increased, decreased or even loss of availability of the drugs. Diclofenac sodium decreased availability of levocetirizine up to 0.0% at pH 4 and 9 but increased at pH 7.4. On the other hand, levocetirizine decreased percent availability of diclofenac sodium by 4.9% pH4 but increased 170% and 206.57 % at pH 7.4 and 9.Flurbiprofen interactions with levocetrizine in different buffers and showed significant rise in availability of levocetirizine in all pH but showed significant decreased availability of flurbiprofin in three buffers. Mefenamic acid caused decreased in pH 7.4 but increased in pH 9. However, availability of mefenamic acid was decreased in both pH. Although, availability of levocetirizine doesn't seem to be effected a lot in the presence of meloxicam but meloxicam was significantly decreased in pH 4 and 7.4. Further, in vivo studies should be conducted to ensure and avoid the adverse effects as result of these interactions. Precaution should be taken and co-administration of levocetirizine with NDSAIDs should be avoided and time duration between these drugs taken should be adjusted. [ABSTRACT FROM AUTHOR]

Currently, there is insufficient information on the variability in levocetirizine pharmacometrics among individuals, a crucial aspect for establishing its clinical use. The gender differences in pharmacokinetics and the extent of variation in pharmacodynamics have not been definitively identified. The primary goal of this study was to investigate gender differences in levocetirizine pharmacokinetics and quantitatively predict and compare how these gender-related pharmacokinetic differences impact pharmacodynamics, using population pharmacokinetic–pharmacodynamic modeling. Bioequivalence results for levocetirizine (only from the control formulation) were obtained from both healthy Korean men and women. Physiological and biochemical parameters for each individual were utilized as pharmacokinetic comparison and modeling data between genders. Pharmacodynamic modeling was performed using reported data on antihistamine responses following levocetirizine exposure. Gender, weight, body surface area, peripheral distribution volume, albumin, central–peripheral inter-compartmental clearance, and the fifth sequential absorption rate constant were explored as effective covariates. A comparison of the model simulation results showed a higher maximum concentration and faster plasma loss in females than in males, resulting in a faster recovery to baseline of the antihistamine effect; however, the absolute differences between genders in the mean values were not large within 10 ng/mL (for plasma concentrations) or % (wheal and flare size changes). Regarding the pharmacokinetics and pharmacodynamics of levocetirizine, the gender effect may not be significant when applying the usual dosage (5 mg/day). This study will be useful for bridging the knowledge gap in scientific precision medicine by introducing previously unconfirmed information regarding gender differences in levocetirizine pharmacometrics. [ABSTRACT FROM AUTHOR]

Data on drug transfer into human breast milk are sparse. This study aimed to quantify concentrations of cetirizine and levocetirizine in breast milk and to estimate drug exposure to infants. Breastfeeding women at least 8 weeks postpartum and using cetirizine or its pure (R)‐enantiomer levocetirizine were eligible to participate. Breast milk samples were collected at six predefined times during a dose interval (0, 2, 4, 8, 12 and 24 h after drug intake) at steady state. Infant drug exposure was estimated by calculating the absolute infant dose (AID) and the weight‐adjusted relative infant dose (RID). In total, 32 women were eligible for final inclusion, 31 women using cetirizine and one woman using levocetirizine. Means of the individual maximum and average cetirizine milk concentrations were 41.0 and 16.8 μg/L, respectively. Maximum concentrations occurred on average 2.4 h after intake, and the mean half‐life in milk was 7.0 h. Estimated AID and RID for cetirizine in a day were 2.5 μg/kg and 1.9%, respectively. The corresponding values for levocetirizine were 1.1 μg/kg and 1.9%. No severe adverse events were reported. Our findings demonstrate that the transfer of cetirizine and levocetirizine into breast milk is low and compatible with breastfeeding. [ABSTRACT FROM AUTHOR]

Author(s): Tejasvi Dwivedi [1]; Sri Sai Kaumudi Chirumamilla [1]; Jivtesh Singh [1]; Satyaki Ganguly [1] Dear Editor, A 37-year-old male, an office worker by profession, not trained in the handling [...]

Background: Urticaria is a common skin disease which often causes impairment in the quality of life. The ideal drug for chronic urticaria would have antihistaminic and anti-inflammatory actions. Bepotastine besilate is a recently approved novel anti-allergic agent with multiple mechanisms of action; levocetirizine is a potent and selective second-generation H1 receptor antagonist used in the treatment of urticaria. Aim: To compare the efficacy and safety of bepotastine besilate versus levocetirizine in patients with chronic spontaneous urticaria. Methods: The study design is a randomised, open-label, parallel-group, prospective interventional study. The study subjects were randomly assigned to either of the two groups a and b, each group had 50 patients with chronic urticaria. Statistical analyses were performed using (SPSS, version 18) for all the variables. Chi-square test was used for comparison between categorical variables. An unpaired student's t-test was done for quantitative variables. Results: There was a significant decrease in mean urticaria activity score (P < 0.001), chronic urticaria quality of life (P < 0.001) and clinical global improvement (P < 0.001) in both the treatment groups but this improvement was higher in the bepotastine than in the levocetirizine group. There was no significant difference in the mean of absolute eosinophil count, C-reactive protein, aspartate transaminase, alanine transaminase from baseline to 4th week between the two study groups. Visual analogue scale showed statistically significant improvement from baseline to 4th week (P < 0.001) of follow-up but this increase was higher in levocetirizine group (0.64-4.24) than in bepotastine group (0.56-2.56). Limitations: Blinding was not done. To assess the efficacy and safety of bepotastine, a larger study can be planned. Conclusion: This study found that bepotastine is superior to levocetirizine and showed a statistically significant reduction in mean urticaria activity score 7, improved quality of life and clinical global improvement in patients with urticaria. [ABSTRACT FROM AUTHOR]

Background: Management of chronic spontaneous urticaria (CSU) is challenging because of its unpredictable course and negative influence on the quality of life. Second-generation antihistaminics are the first-line treatment. Levocetirizine, a time-tested antihistaminic, has proven efficacy in CSU. Bepotastine, which was previously used for allergic rhinitis and conjunctivitis, has recently been tried in urticaria. It may be a better alternative to levocetirizine because of its long-term safety. Objectives: The aim of this study was to compare the efficacy and safety of levocetirizine and bepotastine in CSU. Materials and Methods: A randomized, active-controlled, open-label, prospective, interventional study was conducted on 70 patients of CSU. After initial clinical assessment and baseline investigations, bepotastine and levocetirizine were prescribed to separate groups of 35 patients for a period of 12 weeks. Urticaria Activity Score (UAS) and Dermatology Life Quality Index (DLQI) were used for assessing the severity of disease. Follow-up visits were planned for evaluating clinical improvement and adverse effects. Results were compared using Mann–Whitney U test and Fisher's exact test. P < 0.05 was considered statistically significant. Results: The reduction in UAS and DLQI score in levocetirizine group was better than bepotastine group, and the results were statistically significant at 12 weeks (P = 0.0001). Incidence of adverse effects such as sedation and weight gain was higher in levocetirizine group at 12th week (P = 0.0003). Conclusion: The result of the study reveals the superiority of levocetirizine in terms of efficacy, i.e., reduction of UAS and DLQI scores. Bepotastine although slightly lower in efficacy shows better safety profile.

Drug-induced neuropsychiatric effects are important for disease management. We aim to evaluate the neuropsychiatric effects of montelukast–levocetirizine combination therapy in children. This descriptive study was conducted with children aged 2–5 years, diagnosed with asthma and allergic rhinitis, who began to receive montelukast and levocetirizine combination therapy. The respiratory and asthma control test for children (TRACK), Rhino Conjunctivitis Scoring System (RCSS), and common neuropsychiatric effects (irritable behavior, hallucinations, headaches, nightmares, sleep disorders, behavioral and mood disorder, restlessness, depression) were ascertained by the questionnaire applied before and 4 weeks after the treatment. Parents answered on behalf of their children. The most common finding before and after treatment was irritable behavior. While irritable behavior was observed in 82.4% (n = 56) of children before the treatment, this percentage was 63.2% (n = 43) after the treatment (p = 0.004). The percentage of children who developed at least one neuropsychiatric symptom after treatment was 22.1% (n = 15). There was no significant effect of age, gender, RCSS, TRACK, or allergy test positivity on the development of neuropsychiatric symptoms (p > 0.05). According to the results, at least one neuropsychiatric finding developed in approximately one in five children. Identifying risk factors will enable more careful treatment or consideration of alternative treatments for children at higher risk in the clinical follow-up period. [ABSTRACT FROM AUTHOR]

In this work, we extracted, purified, and characterized two active pharmaceutical ingredients, levocetirizine and levosalbutamol (from commercial tablet formulations), and used them as chiral selectors for enantioresolution of gatifloxacin through thin-layer chromatographic (TLC) method. The silica gel was impregnated with a chiral selector for the enantioresolution of gatifloxacin. The mobile phase used was a combination of acetonitrile, methanol, and triethylamine (4:4:2, V/V, pH 9) and (2:6:2, pH 9), respectively, with levocetirizine and levosalbutamol (as chiral selector in stationary phase at pH 5). The detection limit for enantiomers of gatifloxacin was observed to be 4.2 and 4.9 μg spot‒1, respectively, with levocetirizine and levosalbutamol as chiral selectors. This is the first report on levocetirizine and levosalbutamol as chiral selectors for TLC resolution of gatifloxacin enantiomers. [ABSTRACT FROM AUTHOR]

Electrospun fibers containing levocetirizine, a BCS III drug, were prepared from three water-soluble polymers, hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA). Fiber-spinning technology was optimized for each polymer separately. The polymers contained 10 wt% of the active component. An amorphous drug was homogeneously distributed within the fibers. The solubility of the drug in the polymers used was limited, with a maximum of 2.0 wt%, but it was very large in most of the solvents used for fiber spinning and in the dissolution media. The thickness of the fibers was uniform and the presence of the drug basically did not influence it at all. The fiber diameters were in the same range, although somewhat thinner fibers could be prepared from PVA than from the other two polymers. The results showed that the drug was amorphous in the fibers. Most of the drug was located within the fibers, probably as a separate phase; the encapsulation efficiency proved to be 80–90%. The kinetics of the drug release were evaluated quantitatively by the Noyes–Whitney model. The released drug was approximately the same for all the polymers under all conditions (pH), and it changed somewhere between 80 and 100%. The release rate depended both on the type of polymer and pH and varied between 0.1 and 0.9 min−1. Consequently, the selection of the carrier polymer allowed for the adjustment of the release rate according to the requirements, thus justifying the use of electrospun fibers as carrier materials for levocetirizine. [ABSTRACT FROM AUTHOR]

A practical, transition metal‐free method allows the enantioselective synthesis of α,α‐diarylmethylamines by asymmetric α‐arylation of benzylamines. Enantioselective lithiation of N′‐aryl‐N‐benzyl‐N‐isopropyl ureas using a chiral lithium amide base generates a benzyllithium that undergoes an unactivated stereospecific intramolecular nucleophilic aromatic substitution to generate an α,α‐diarylmethylamine in the form of its urea derivative, in up to >99 % ee. Treatment with acid induces an "azatropic shift" with retention of configuration, the product of which may be hydrolysed to the target amine. [ABSTRACT FROM AUTHOR]

Allergic rhinitis occupies a special place among diseases of the upper respiratory tract. Every year the urgency of the problem increases due to the annual increase in the incidence among all age groups of the population. Allergic diseases are often associated with other respiratory diseases or cause them, which requires early diagnosis and selection of competent therapy. Allergic reactions can range from seasonal allergens, such as tree or weed pollen, to year-round irritants, such as dust and pet dander. Currently, the pathogenesis of allergic rhinitis is being actively studied. There is still debate about the most accurate classification of allergic rhinitis, reflecting all its aspects, such as the time of onset and duration of symptoms, their impact on patients’ lives. This is necessary to find the best methods of treatment with maximum efficiency. The main clinical manifestations of allergic rhinitis are nasal itching, sneezing, swelling of the nasal mucosa and rhinorrhea. Often, to relieve symptoms, patients are forced to take many drugs for a long time, which has a significant impact on their quality of life. All over the world, new ways are being developed to optimize the treatment of this group of patients, among which combinations of several drugs used to treat allergic rhinitis, which meet all safety and efficacy requirements. The most commonly used and most effective combinations of drugs are combinations of intranasal glucocorticosteroids with topical histamine H1 receptor antagonists, as well as leukotriene receptor blockers with oral antihistamines.

Antihistamines such as levocetirizine dihydrochloride (LC) are commercially used in oral tablets and oral drops to reduce allergic symptoms. In this study, LC was nano-spray-dried using three mucoadhesive polymers and four cyclodextrin species to form composite powders for nasal administration. The product was composed of hydroxypropyl methylcellulose polymer, including LC as a zwitterion, after neutralization by NaOH, and XRD investigations verified its amorphous state. This and a sulfobutylated-beta-cyclodextrin sodium salt-containing sample showed crystal peaks due to NaCl content as products of the neutralization reaction in the solutions before drying. The average particle size of the spherical microparticles was between 2.42 and 3.44 µm, except for those containing a polyvinyl alcohol excipient, which were characterized by a medium diameter of 29.80 µm. The drug was completely and immediately liberated from all the samples at pH 5.6 and 32 °C; i.e., the carriers did not change the good dissolution behavior of LC. A permeability test was carried out by dipping the synthetic cellulose ester membrane in isopropyl myristate using modified horizontal diffusion cells. The spray-dried powder with β-cyclodextrin showed the highest permeability (188.37 µg/cm2/h), as this additive was the least hydrophilic. Products prepared with other cyclodextrins (randomly methylated-beta-cyclodextrin, sulfobutylated-beta-cyclodextrin sodium salt and (hydroxypropyl)-beta-cyclodextrin) showed similar or slightly higher penetration abilities than LC. Other polymer excipients resulted in lower penetration of the active agent than the pure LC. [ABSTRACT FROM AUTHOR]