BACKGROUND: Hypersensitivity reactions (HSR) are a known adverse effect of paclitaxel, occurring in approximately 10% of patients, typically during the first or second infusion of the medication. Corticosteroids, histamine-1 and histamine-2 receptor antagonists are given prior to paclitaxel infusions to reduce the incidence of HSR. There are limited data that suggest administration of cetirizine given prior to a platinum infusion as secondary prophylaxis may reduce HSR rates.
METHODS: The objective of this study was to assess the impact of a novel paclitaxel hypersensitivity prevention protocol including high-dose cetirizine administered 12 and 6 h prior to paclitaxel infusion on the rate of HSR compared to a historical control. The primary objective was the rate of HSR of any grade after the first cycle of paclitaxel. Secondary outcomes included grade of infusion reaction and incidence of severe HSR.
RESULTS: A total of 104 patients were included for analysis in the cetirizine group and 124 in the control group. Hypersensitivity reactions occurred in 37 (16.2%) patients in the overall population, and no statistical difference was observed between groups. (13.46% vs 18.55%; p = 0.23). Numerically more grade 3-4 HSRs occurred in the control group than the treatment group (30.77% vs 69.23; p = 0.51).
CONCLUSIONS: The addition of cetirizine to paclitaxel infusions resulted in numerically lower rates of HSR and a reduction in severity of grade 3-4 HSRs. Future studies with more robust compliance data and a larger patient population would be needed to appropriately assess the efficacy of our novel treatment regimen.

Post-burn pruritis is difficult to assess and treat. Antihistamines used in its treatment provide little relief. Identification of the itch neuronal pathway has inspired new alternatives including gabapentin in its management. The study compared the effectiveness of cetirizine, gabapentin, and a combination of gabapentin and cetirizine in treating post-burn pruritus. Burn patients were randomly assigned to treatment with Cetirizine (n=23), Gabapentin (n=23), or Cetirizine plus Gabapentin (n=23). Baseline assessment of the intensity or the severity of pruritus was evaluated after which treatment commenced with standard doses of the three study regimens. Quality of sleep was assessed at baseline (day 0) and repeated on day 3, day 7 and day 14. Approximately 97% of participants presented with moderate or severe itch; 69% with acute itch; and majority (94.2%) experienced pruritus between the first and fourth weeks. Gabapentin reduced itch by 92.9% in 14 days compared to cetirizine\'s 61.8%. The combined effect of cetirizine and gabapentin was comparable to using gabapentin alone. When itch became protracted over 6 weeks, the effectiveness of cetirizine in controlling itch worsened. It reduced itch intensity by only 37.7% whilst gabapentin did so at 89.4%. Itch intensity correlated positively with insomnia and controlling itch intensity improved sleep. Gabapentin was more effective for the treatment of post-burn pruritus than cetirizine. Controlling itch intensity improved sleep. In acute and moderate itch, a low-dose gabapentin could be added if cetirizine is the drug intended for its treatment.

暂无摘要。

Aims: Cetirizine is frequently administered at an increased dosage in clinical practice and recommended by several guidelines. Nonetheless, the pharmacokinetic (PK) profile and real-world safety data remain insufficient in the Chinese pediatric population. The objective of the current study is to develop a population pharmacokinetic (PPK) model for cetirizine in Chinese pediatric patients and to investigate the rationale behind its off-label usage. Methods: A prospective cohort study was conducted, enrolling children who had been diagnosed with allergic diseases and prescribed cetirizine. The outcomes were safety and pharmacokinetic (PK) parameters. Cetirizine concentrations were measured using a pre-established analytical method. Subsequently, a PK model was developed, followed by model evaluation and simulation. The developed PK model was employed to investigate the drug exposure differences across various age groups and to simulate scenarios of potential overdose. Results: Sixty-three children were enrolled, and 24 of them received a cetirizine dose exceeding the recommended dosage. A PPK model, based on published literature, served as the basis of our analysis, with adjustment made to estimate certain parameters. The final model evaluation and validation indicated accurate predictive performance and robust parameter estimation. Simulations conducted for the label-dose among age 1-12 indicated median maximum concentration at steady state (Cmax,ss) of 7 year old children could be the highest. The model was also used to predict the off-label dose scenarios and overdose patient to support the clinical decision. There were no adverse drug reactions in either group. Conclusion: This study provides evidence-based and model-based exploration for optimizing cetirizine usage in Chinese pediatric patients. The cetirizine PPK model showed accurate predictive performance and could be utilized to simulate individual patient exposure in real-world clinical scenarios.

UNASSIGNED: Bilastine is a novel second-generation antihistaminic. Very few studies in Indian population have compared the safety and efficacy of bilastine with other second-generation antihistaminic like cetirizine. Hence, the present study was planned.
UNASSIGNED: This was a randomized, open-label comparative parallel group study conducted on 70 patients of chronic spontaneous urticaria (CSU). Patients either received cetirizine 10 mg or bilastine 20 mg once daily for 6 weeks. The primary endpoint was to find out the difference in the mean total symptom score (MTSS) at baseline and 6 weeks. The secondary endpoint was to find out changes in the scale of the number of wheals, change in pruritus scale, scale for size of wheal, change for interference of wheals with sleep, change in visual analog scale (VAS) for sedation, change in scale for intensity of erythema, and change in Scale for Extent of Skin Area Involvement (SESI).
UNASSIGNED: Bilastine and cetirizine offer a significant reduction in MTSS, mean number of wheals, and mean pruritus scale at baseline to 1, 3, and 6 weeks. The mean difference in MTSS was significantly more in bilastine. Cetirizine showed a significant increase in VAS score for sedation as compared to bilastine. Both the drugs were well tolerated and safe. Adverse events like headache, gastric irritation, dryness of mouth, and sedation were more reported in cetirizine group.
UNASSIGNED: Bilastine was more efficacious than cetirizine in patients of CSU and the efficacy was seen earlier at 1 week, which was not seen in the cetirizine group.

To gain a comprehensive overview of the landscape of clinical trials for the H1-receptor antagonists (H1R antagonists) cetirizine, levocetirizine, loratadine, desloratadine, and fexofenadine and their potential use cases in drug repurposing (the use of well-known drugs outside the scope of the original medical indication), we analyzed trials from clincialtrials.gov using novel custom-coded software, which itself is also a key emphasis of this paper. To automate data acquisition from clincialtrials.gov via its API, data processing, and storage, we created custom software by leveraging a variety of open-source tools. Data were stored in a relational database and annotated facilitating a specially adapted web application. Through the data analysis, we identified use cases for repurposing and reviewed backgrounds and results in the scientific literature. Even though we found very few trials with published results for repurpose indications, extended literature research revealed some prominent use cases: Cetirizine seems promising in mitigating infusion-associated reactions and is also more effective than placebo in the treatment of androgenetic alopecia. Loratadine may be beneficial in the prophylaxis of G-CSF-related bone pain. In COVID-19, H1R antagonists may be helpful, but placebo-controlled scientific evidence is needed. For asthma, the effect of H1R antagonists only seems to be secondary by alleviating allergy symptoms. Our novel method to find potential use cases for repurposing of H1R antagonists allows for high automation, reduces human error, and was successful in revealing potential areas of interest. The software could be used for similar research questions and analyses in the future.

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.

暂无摘要。

UNASSIGNED: Female pattern hair loss (FPHL) is the most prevalent form of hair loss in women. It was aimed to evaluate the therapeutic effects of topical cetirizine 1%, versus topical minoxidil 2% in patients with FPHL.
UNASSIGNED: Through a triple-blind randomized clinical trial, 60 women with FPHL were randomly divided into two groups of treatment with topical cetirizine 1% or topical minoxidil 2%. The endpoint was changing in hair loss severity as well as terminal hair density and diameter, according to trichoscopic evaluation. Intention-to-treat analysis was also performed for those who accomplished 3 months of treatment.
UNASSIGNED: Both groups showed improvement in hair diameter and density after 6 months; however, the outcome was significant only in the minoxidil group. According to per-protocol analysis, minoxidil was significantly superior to cetirizine in hair density, but not in hair diameter. According to the hair loss severity scales, FPHL was significantly improved in both the cetirizine and minoxidil groups after 6 months of therapy. The dropout rate due to adverse effects was 10.0% and 6.6% in the cetirizine and minoxidil groups, respectively.
UNASSIGNED: Although inferior to topical minoxidil, topical cetirizine can provide favorable therapeutic effects for FPHL, specifically when patient incompatibility with Minoxidil is observed.
UNASSIGNED: The study is registered in the Iranian Registry of Clinical Trials (IRCT) with the registration code IRCT20200521047536N1.

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.