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INTRODUCTION: 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 6â 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.
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We aimed to determine the efficacy of the various available oral, topical, and procedural treatment options for hair loss in individuals with androgenic alopecia. Using the Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines, a systematic review of the National Library of Medicine was performed. Overall, 141 unique studies met our inclusion criteria. We demonstrate that many over the counter (e.g. topical minoxidil, supplements, low-level light treatment), prescription (e.g. oral minoxidil, finasteride, dutasteride), and procedural (e.g. platelet-rich plasma, fractionated lasers, hair transplantation) treatments successfully promote hair growth, highlighting the superiority of a multifaceted and individualized approach to management.
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Objectives: Perennial allergic rhinitis (PAR) is common in Japan. Second-generation antihistamines (SGAs) are commonly used for its treatment; however, it remains unclear which SGA is the most cost-effective. Additionally, the pharmacoeconomics of Japanese Kampo shoseiryuto (which was traditionally prescribed to treat PAR in Japan) remains poorly understood. In this study, we aimed to investigate the effectiveness of various SGAs and shoseiryuto for the treatment of PAR in Japanese outpatients, from the healthcare payer's perspective. Methods: The most cost- and clinically effective SGAs were determined from a list of 6 SGAs (bepotastine, 10 mg; cetirizine, 10 mg; ebastine, 10 mg; epinastine, 20 mg; loratadine, 10 mg; and olopatadine, 5 mg) together with shoseiryuto, using the overall improvement rate through a model-based analysis. The time horizon was 28 days. Costs were determined based on the Medical Fee Index in 2020. Deterministic and probabilistic sensitivity analyses were conducted to address the uncertainty of the base-case results. Results: Overall, bepotastine (10 mg) and ebastine (10 mg) were cost-effective. Shoseiryuto was less cost-effective than ebastine (10 mg) (dominated). Ebastine (10 mg) was the most cost-effective option based on deterministic and probabilistic sensitivity analyses. Conclusions: Ebastine (10 mg) was the most cost-effective treatment strategy for PAR among the agents evaluated in this study. This insight could aid in establishing an appropriate formulary for treating PAR in hospitals and communities.
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Due to the side effects of cetirizine overdose and the need to monitor its concentration in the human body, in this work, an electrochemical sensor has been prepared by utilizing a carbon paste electrode modified with Li2CoMn3O8/CC3N4 nanocomposite and ethyl-3-methyl-imidazolium chloride ionic liquid ([EMIM][Cl]) to determine cetirizine in the human blood serum sample and urine as well as drug samples. Li2CoMn3O8/CC3N4 nanocomposite was characterized by Fourier transform infrared (FT-IR), field emission scanning electron microscope (FESEM), and X-ray diffraction (XRD) analysis. The investigation of the influence of each modifier component showed that the existence of all components in modification has a synergistic effect. Li2CoMn3O8/CC3N4/IL nanocomposite has a larger surface area relative to the components alone, thus providing a more fine-grained media to facilitate electron transfer during the reaction between analyte and electrode. Determination of cetirizine was performed in phosphate buffer solution with pH 7.0 and detection limits obtained in the concentration ranges of 0.03-0.9 and 3-300 µM was 11.8 × 10-9 M. The diffusion coefficient (D = 9.2 × 10-6 cm2s-1) of cetirizine at the surface of the modified electrode was determined by chronoamperometry. Finally, simultaneous detection of cetirizine, phenylephrine and acetaminophen was performed using the suggested sensor without any interference.
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Acetaminofén , Nanocompuestos , Humanos , Técnicas Electroquímicas , Cetirizina , Fenilefrina , Espectroscopía Infrarroja por Transformada de Fourier , Nanocompuestos/química , Litio , Iones , Preparaciones FarmacéuticasRESUMEN
Enantioseparation and determination of chiral drugs are of vital importance in biochemical and pharmaceutical research due to the different biological activity, mechanism, and toxicity of individual enantiomers. As a second-generation H(1)-antagonist, cetirizine's pharmaceutical activity is mainly derived from the levocetirizine while the dextro-enantiomer is ineffective and even associated with side effects. Herein, the enantiomers of cetirizine were separated by capillary electrophoresis and identified by electronic circular dichroism. Satisfactory linear relationship was found between the circular dichroism signal at λmax and the electrophoretic peak area difference in the nonracemic mixture of enantiomers. It made possible identification and quantification of cetirizine enantiomers independent of single enantiomer standards. The method's feasibility was demonstrated on the enantiomeric excess experiments of oral drugs measured in human blank urine. Additionally, the separation and determination of cetirizine in human urine after administration were also realized by capillary electrophoresis, indicating the method was sensitive enough for pharmacokinetic study.
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Cetirizina , Electroforesis Capilar , Humanos , Cetirizina/análisis , Cetirizina/farmacocinética , Dicroismo Circular , Estándares de Referencia , Electroforesis Capilar/métodos , EstereoisomerismoRESUMEN
BACKGROUND: Literature on the effects of second-generation H1-antihistamines on angiogenesis is limited. OBJECTIVES: To investigate the effects of cetirizine, desloratadine, and rupatadine (second-generation H1-antihistamines commonly used in dermatology clinics) on angiogenesis in an in vivo chick chorioallantoic membrane (CAM) model. METHODS: The study was approved by the local ethics committee on animal experimentation. Forty fertilized specific pathogen free eggs were incubated and kept under appropriate temperature and humidity control. Drug solutions were prepared in identical concentrations by dissolving powders in phosphate-buffered saline (PBS). On the third day of the incubation, a small window was opened on the CAM and 0.1 mL desloratadine (1.5 µg/0.1 mL) in the first group, 0.1 mL cetirizine (1.5 µg/0.1 mL) in the second group, 0.1 mL rupatadine in the third group (1.5 µg/0.1 mL), and PBS (0.1 mL) in the fourth group were administered by injection. On the eighth day of incubation, the vascular structures of the CAMs were macroscopically examined and standard digital photographs were taken. The digital images were analyzed and data including mean vessel density, thickness, and number were compared between groups. p < 0.05 was considered statistically significant. RESULTS: Vessel densities were similar in the desloratadine, cetirizine, and control groups, whereas they were significantly less in the rupatadine group (p = 0.01). Furthermore, the rupatadine group had significantly lower vessel thickness and number compared with the other groups (p < 0.05 for both). CONCLUSIONS: Rupatadine showed anti-angiogenic effects in the chick CAM model, compared with desloratadine and cetirizine. The anti-angiogenic effect of rupatadine could be due to its platelet-activating factor (PAF) receptor inhibition. Thus, rupatadine could be a treatment agent in pathological processes in which angiogenesis is responsible. Further studies with larger series are needed to clarify this potential.
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Cetirizina , Antagonistas de los Receptores Histamínicos H1 no Sedantes , Animales , Cetirizina/farmacología , Cetirizina/uso terapéutico , Membrana Corioalantoides , PollosRESUMEN
Cetirizine hydrochloride (CTZ), a second-generation anti-histaminic drug, has been recently explored for its effectiveness in the treatment of alopecia. Niosomes are surfactant-based nanovesicular systems that have promising applications in both topical and transdermal drug delivery. The aim of this study was to design topical CTZ niosomes for management of alopecia. Thin film hydration technique was implemented for the fabrication of CTZ niosomes. The niosomes were examined for vesicle size, surface charge, and entrapment efficiency. The optimized niosomal formulation was incorporated into a hydrogel base (HPMC) and explored for physical characteristics, ex vivo permeation, and in vivo dermato-kinetic study. The optimized CTZ-loaded niosomal formulation showed an average size of 403.4 ± 15.6 nm, zeta potential of - 12.9 ± 1.7 mV, and entrapment efficiency percentage of 52.8 ± 1.9%. Compared to plain drug solution, entrapment of CTZ within niosomes significantly prolonged in vitro drug release up to 12 h. Most importantly, ex-vivo skin deposition studies and in vivo dermato-kinetic studies verified superior skin deposition/retention of CTZ from CTZ-loaded niosomal gels, compared to plain CTZ gel. CTZ-loaded niosomal gel permitted higher drug deposition percentage (19.2 ± 1.9%) and skin retention (AUC0-10h 1124.5 ± 87.9 µg/mL.h) of CTZ, compared to 7.52 ± 0.7% and 646.2 ± 44.6 µg/mL.h for plain CTZ gel, respectively. Collectively, niosomes might represent a promising carrier for the cutaneous delivery of cetirizine for the topical management of alopecia.
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In recent years, inflammatory diseases of the nose and paranasal sinuses have been on the rise. In addition to infectious diseases, in the modern world a large percentage of the population suffers from allergic diseases. The approach to therapy and the choice of a drug should take into account the pathogenesis of the inflammatory reaction in the nasal cavity and paranasal sinuses. By exerting its effect, the drug should reduce hyperemia and swelling of the nasal mucosa, reduce the level of mucus secretion, improve the drainage of the paranasal sinuses, i.e. possess vasoconstrictive and anti-allergic properties. As such a drug, you can use the combined intranasal spray Frinozol, which basically contains cetirizine and phenylephrine. The use of Frinozol in the complex treatment of inflammation of the mucous membrane of the nasal cavity and paranasal sinuses contributes to the rapid and pronounced weakening of the symptoms of the disease, and is also the key to successful therapy.
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Senos Paranasales , Rinitis , Humanos , Rinitis/tratamiento farmacológico , Senos Paranasales/cirugía , Cavidad Nasal , Mucosa Nasal/patología , Administración Intranasal , Inflamación/tratamiento farmacológicoRESUMEN
BACKGROUND: The clinical observation showed a potential additive effect of anti-PD-1 agents and cetirizine in patients with advanced melanoma. METHODS: Clinical outcomes of concomitant cetirizine/anti-PD-1 treatment of patients with stage IIIb-IV melanoma were retrospectively collected, and a transcriptomic analysis was performed on blood samples obtained at baseline and after 3 months of treatment. RESULTS: Patients treated with cetirizine concomitantly with an anti-PD-1 agent had significantly longer progression-free survival (PFS; mean PFS: 28 vs 15 months, HR 0.46, 95% CI: 0.28-0.76; p = 0.0023) and OS (mean OS was 36 vs 23 months, HR 0.48, 95% CI: 0.29-0.78; p = 0.0032) in comparison with those not receiving cetirizine. The concomitant treatment was significantly associated with ORR and DCR (p < 0.05). The expression of FCGR1A/CD64, a specific marker of macrophages, was increased after the treatment in comparison with baseline in blood samples from patients receiving cetirizine, but not in those receiving only the anti-PD1, and positively correlated with the expression of genes linked to the interferon pathway such as CCL8 (rho = 0.32; p = 0.0111), IFIT1 (rho = 0.29; p = 0.0229), IFIT3 (rho = 0.57; p < 0.0001), IFI27 (rho = 0.42; p = 0.008), MX1 (rho = 0.26; p = 0.0383) and RSAD2 (rho = 0.43; p = 0.0005). CONCLUSIONS: This retrospective study suggests that M1 macrophage polarization may be induced by cetirizine through the interferon-gamma pathway. This effect may synergize with the immunotherapy of advanced melanoma with anti-PD-1 agents.
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Melanoma , Receptor de Muerte Celular Programada 1 , Cetirizina/farmacología , Cetirizina/uso terapéutico , Humanos , Interferón gamma/uso terapéutico , Macrófagos/metabolismo , Melanoma/genética , Estudios RetrospectivosRESUMEN
A green, simple, quick and economical method is implemented for the first time for the simultaneous estimation of cetirizine (CTZ) and azelastine (AZE) as co-administered eye drops. The method relies on synchronous spectrofluorimetry with ∆λ = 60 nm. Cetirizine can be estimated at 231 nm and AZE can be measured at 294 nm, each at the other's zero crossing point. All factors affecting the method were studied and properly optimized. Good correlation was obtained in the range of 0.1-2 µg mL-1 for both drugs. The limits of detection were 0.014 and 0.010 µg mL-1 and limits of quantitation were 0.043 and 0.029 µg mL-1 for CTZ and AZE, respectively. Moreover, ICH guidelines were carried out to validate the adopted method. The method was suitable for the analysis of CTZ and AZE in synthetic mixtures, eye drops and aqueous humor. The mean percentage of recoveries of CTZ and AZE in spiked aqueous humor were 99.83 and 99.37, respectively. Furthermore, Green Analytical Procedure Index (GAPI) and analytical Eco-scale approaches were used to evaluate the greenness of the suggested method.
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Humor Acuoso , Cetirizina , Soluciones Oftálmicas , Ftalazinas , Espectrometría de Fluorescencia/métodosRESUMEN
In this study, two solvents (deep eutectic and water/deep eutectic solvents) were used for N-doped carbon dots (N-CDs) preparation by microwave irradiation. The solvent can influence surface chemical composition, quantum yield, morphology, and fluorescence of CDs. N-CDs synthesized in water/deep eutectic solvent (DES) had better quantum yield (24.5%) with respect to N-CDs synthesized in deep eutectic solvent (17.4%). These carbon dots were used as a rapid and high sensitive "off-on" fluorescent probe for the determination of Fe3+ ion and cetirizine. Morphology and structure of the N-CDs were characterized by FT-IR, UV-Vis, XRD and TEM. Linear range and detection limit for N-CDs synthesis in deep eutectic solvent for cetirizine were 0.08-48 µM and 15 nM, respectively and for N-CDs synthesis in water/deep eutectic solvent were 0.03-50 µM and 10 nM, respectively. Applicability of this nanoprobe was tested in cetirizine determination in serum sample. Antibacterial activities of the two synthesized N-CDs were also investigated using agar disk diffusion method.
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Carbono/química , Cetirizina/análisis , Disolventes Eutécticos Profundos , Compuestos Férricos/análisis , Puntos Cuánticos/química , Espectrometría de Fluorescencia/métodos , Antibacterianos/farmacología , Carbono/farmacología , Cetirizina/farmacología , Compuestos Férricos/farmacología , Concentración de Iones de Hidrógeno , Límite de Detección , Microscopía Electrónica de Transmisión , Microondas , Factores de TiempoRESUMEN
PURPOSE: Cetirizine is a less sedative alternative to diphenhydramine for the prevention of infusion-related reactions (IRR) to paclitaxel. However, its use remains controversial. In this study, we assessed feasibility for a future definitive non-inferiority trial comparing cetirizine to diphenhydramine as premedication to prevent paclitaxel-related IRR. METHODS: This was a single-center randomized prospective feasibility study. Participants were paclitaxel-naive cancer patients scheduled to start paclitaxel chemotherapy. They were randomly assigned to receive either intravenous diphenhydramine 50 mg + oral placebo (control) or intravenous placebo + oral cetirizine 10 mg (intervention) for their first two paclitaxel treatments. The percentage of eligible patients completing a first paclitaxel treatment and the recruitment rate were assessed (feasibility outcomes). Drowsiness was measured at baseline and at selected time points using the Stanford Sleepiness Scale (SSS) (safety outcome). IRR events were also documented (efficacy outcome). RESULTS: Among 37 eligible patients, 27 were recruited and randomized (control 13; intervention 14) and 25 completed the study. The recruitment rate was 4.8 participants/month, meeting the primary feasibility target. Drowsiness was the main adverse effect associated with the premedication. The increase in drowsiness compared to baseline (ΔSSS) was greater in the diphenhydramine group compared to the cetirizine group (median ΔSSS 2 (IQR 3.25) vs median ΔSSS 0 (IQR 1), p < 0.01) when measured one hour after the premedication administration. One participant had an IRR and no unexpected serious adverse event occurred. CONCLUSION: The trial methods were feasible in terms of recruitment, retention, and safety. Cetirizine was significantly less sedating than diphenhydramine. IRR were infrequent and a larger trial is warranted to confirm non-inferiority for IRR prevention. TRIAL REGISTRATION: ClinicalTrials.gov, NCT04237090 (22.01.2020).
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Cetirizina , Paclitaxel , Cetirizina/efectos adversos , Difenhidramina/efectos adversos , Método Doble Ciego , Estudios de Factibilidad , Humanos , Premedicación , Estudios ProspectivosRESUMEN
The incidence of anticholinergic syndrome due to second generation antihistamines is infrequently reported. Largely due to their decreased affinity for central nervous system (CNS) receptors, second generation antihistamines are rarely associated with anticholinergic symptoms, though toxicity is still possible particularly when taken in excess. We report a case of a six year old boy who presented with agitation, hallucinations, fixed and dilated pupils, tachycardia, and hyperthermia consistent with anticholinergic toxicity several hours after accidental overdose of a second generation antihistamine, cetirizine. Early identification of this rare phenomenon is important not only for appropriate emergency management but also for avoidance of potentially invasive and unnecessary tests which may further increase patient morbidity.
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Antialérgicos/envenenamiento , Síndrome Anticolinérgico/etiología , Cetirizina/envenenamiento , Antialérgicos/administración & dosificación , Cetirizina/administración & dosificación , Niño , Sobredosis de Droga/complicaciones , Humanos , MasculinoRESUMEN
Hydroxyzine and cetirizine are first- and second-generation oral antihistamine drugs, respectively, used to treat allergic reactions in horses. Cetirizine is also a metabolite of hydroxyzine, which may lead to complexities in regulating their use in equine sporting events. The aim of the research was to be able to provide detection times (DT) from pharmacokinetic studies in thoroughbred horses to better inform trainers, and their veterinary surgeons, prescribing these substances for treatment of Thoroughbred racehorses. Six and two horses were given 9 repeated administrations of hydroxyzine HCl (500 mg BID) or cetirizine HCl (190 mg BID), respectively. Plasma and urine hydroxyzine and cetirizine concentrations were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). A holistic non-linear mixed effects PK model was developed that described both plasma and urine concentrations of hydroxyzine and cetirizine, either from administration of each individually or cetirizine as a metabolite of hydroxyzine. Using the parameters obtained from this PK model in conjunction with methodology developed by Toutain afforded possible screening limits (SL) that can regulate for a DT of 4 days in either plasma or urine. Hydroxyzine and cetirizine concentration prediction intervals for the 80th , 95th and 99th percentiles of a virtual horse population were performed in order to assess the statistical protection of the DT. However, it is down to the individual racing authorities to apply their own risk management.
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Hidroxizina , Preparaciones Farmacéuticas , Administración Oral , Animales , Cetirizina , Cromatografía Liquida/veterinaria , Antagonistas de los Receptores Histamínicos H1 , Caballos , Espectrometría de Masas en Tándem/veterinariaRESUMEN
Patients with allergic rhinitis (AR) have a predisposition to frequent acute respiratory viral infections (ARVI). Inflammation of the mucous membrane of the nasal cavity and paranasal sinuses in such patients is more pronounced against the background of a combination of allergic and infectious inflammation. OBJECTIVE: To evaluate the effect of therapy using modern antihistamines on the condition and severity of symptoms in adult patients with exacerbation of AR caused by plant pollen (seasonal) (SAR) and the development of ARVI. MATERIAL AND METHODS: An observational study was conducted at the Department of Otorhinolaryngology of the Evdokimov Moscow State University of Medicine and Dentistry of the Ministry of Health of the Russian Federation from April to August 2021. Included are patients of both sexes aged 18 to 65 years with a previously (at least 1 year ago) verified diagnosis of mild and moderate acute SAR in the acute stage, who sought medical help for ARVI. All patients were prescribed therapy with the inclusion of a drug belonging to the pharmacological group of antihistamines of the 2nd generation (a course of 14 days). In addition, patients received symptomatic ARVI therapy according to indications, including nasal decongestants (as needed), antipyretic and antitussive drugs. RESULTS: Based on the data obtained, it was possible to prove that the use of modern antihistamines in patients comorbid with AR and ARVI has a pronounced therapeutic effect. Theoritin provides a therapeutic effect at an early stage in relation to nasal and non-nasal symptoms of SAR/ARVI, and also quickly improves the quality of life of patients, which makes its use promising for the treatment of ARVI against the background of AR. The drug has an antihistamine activity comparable to cetirizine and surpasses it in its ability to suppress an allergic inflammatory reaction, for example on the skin, as well as in the duration of preservation of the antihistamine effect. CONCLUSION: The presented results indicate the effectiveness of theoritin and cetirizine in the treatment of patients with seasonal exacerbation of allergic rhinitis, comorbid for acute respiratory viral infections.
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Infecciones del Sistema Respiratorio , Rinitis Alérgica Estacional , Rinitis Alérgica , Adulto , Cetirizina , Femenino , Antagonistas de los Receptores Histamínicos/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Humanos , Inflamación/tratamiento farmacológico , Masculino , Calidad de Vida , Infecciones del Sistema Respiratorio/diagnóstico , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Rinitis Alérgica/complicaciones , Rinitis Alérgica/diagnóstico , Rinitis Alérgica/tratamiento farmacológico , Rinitis Alérgica Estacional/complicaciones , Rinitis Alérgica Estacional/diagnóstico , Rinitis Alérgica Estacional/tratamiento farmacológicoRESUMEN
INTRODUCTION: Recently CDK4/6 inhibitors have been introduced for the treatment of hormone positive breast cancer resistant to endocrine therapy. Among their side effects, alopecia is often reported being associated to patients' distress and depressive symptoms. CASE REPORT: We report the case of a 70-year-old woman affected by breast cancer in treatment with Palbociclib, who developed alopecia.Management and Outcome: We prescribed a topical solution with cetirizine. Global photography, trichoscopy and trichogram were assessed. All evaluations demonstrated alopecia improvement. DISCUSSION: Currently, no treatment options for CDK 4/6 inhibitors induced alopecia have been proposed. Herein, we report the use of topical cetirizine.
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Alopecia/inducido químicamente , Alopecia/tratamiento farmacológico , Antineoplásicos/efectos adversos , Cetirizina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Piperazinas/efectos adversos , Inhibidores de Proteínas Quinasas/efectos adversos , Piridinas/efectos adversos , Administración Tópica , Anciano , Neoplasias de la Mama/complicaciones , Neoplasias de la Mama/tratamiento farmacológico , Cetirizina/administración & dosificación , Quinasas Ciclina-Dependientes/antagonistas & inhibidores , Femenino , Antagonistas de los Receptores Histamínicos H1/administración & dosificación , Humanos , Metástasis de la Neoplasia/tratamiento farmacológico , Piperazinas/uso terapéutico , Inhibidores de Proteínas Quinasas/uso terapéutico , Piridinas/uso terapéutico , Cuero Cabelludo/patología , Resultado del TratamientoRESUMEN
A simple and sensitive flow injection-chemiluminescence (FI-CL) method was developed for determination of cetirizine dihydrochloride (CTZH) in pharmaceuticals. The method is primarily based on the enhancement effect of CTZH on the tris(2,2'-bipyridyl)ruthenium (II)-diperiodatoargentate (III) ([Ru(bpy)3 ]2+ -Ag(III) complex) CL system in an acidic medium. The optimum investigated variables of the CL reaction were: [Ru(bpy)3 ]2+ , 50 × 10-6 mol/L; sulfuric acid, 1.0 × 10-3 mol/L; Ag(III) complex, 100 × 10-6 mol/L; potassium hydroxide, 1.0 × 10-3 mol/L; flow rate, 3.0 ml/min and sample loop volume, 300 µl. The detection and quantification limits were 2.0 × 10-4 and 5.0 × 10-4 mg/L (S/N of 3 and 10) respectively with a linear calibration range of 5.0 × 10-4 to 7.5 mg/L (R2 = 0.9999, n = 11), injection throughput of 110/h and the relative standard deviations of 1.5-3.5% over the range studied. The methodology was successfully applied to determine CTZH in different pharmaceutical samples and validated with a high-performance liquid chromatography method, and resulted in the recovery of 94.6-108.6%. The probable CL reaction mechanism is described in brief.
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Preparaciones Farmacéuticas , Rutenio , 2,2'-Dipiridil , Cetirizina , Análisis de Inyección de Flujo , Luminiscencia , Mediciones Luminiscentes , PlataRESUMEN
IgE-mediated inflammatory responses upon allergen contact in allergic rhinitis (AR) are associated with rapid alterations of circulating blood cell numbers detectable in a complete blood count (CBC). Aim of this study was to evaluate whether intake of antihistamines may modulate allergen-induced CBC dynamics in male and female patients. A total of N = 112 specific allergen challenges were performed in otherwise healthy AR subjects. Seventy-two (n = 72) subjects received placebo and forty (n = 40) received cetirizine (H1-receptor antagonist) per os prior to allergen exposure in a randomized, double-blind trial at the Vienna Challenge Chamber (VCC); a subgroup of twenty-five (n = 25) subjects received cetirizine and placebo on different study days (parallel group). Blood samples and symptom scores were taken at baseline and immediately after 6 h of airway challenge simulating ambient allergen contact. Female sex was associated with a pronounced circulating monocyte increase (p < .01) and male sex with an eosinophil decrease (p < .05) in the placebo group, but not in cetirizine treated subjects. The significant increase in segmented neutrophils (p < .001) and decrease in circulating erythrocytes (p < .01) upon allergen challenge was less prominent after cetirizine intake in both sexes. A more prominent thrombocyte increase in female subjects (p < .05) was noted upon allergen exposure, regardless of prior cetirizine intake. Cetirizine inhibited the mobilization of neutrophils, lymphocytes and decline in erythrocyte numbers, but did not affect thrombocyte increase upon allergen challenge. It further diminished gender-specific blood cell dynamics. Overall, as reflected in a simple CBC, cetirizine critically diminished immediate and late innate immune responses subsequent to allergen exposure.
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Alérgenos/inmunología , Cetirizina/uso terapéutico , Antagonistas de los Receptores Histamínicos H1/uso terapéutico , Rinitis Alérgica Estacional/tratamiento farmacológico , Rinitis Alérgica/tratamiento farmacológico , Adulto , Método Doble Ciego , Eosinófilos/efectos de los fármacos , Eosinófilos/inmunología , Femenino , Humanos , Inmunidad Innata/efectos de los fármacos , Inmunidad Innata/inmunología , Masculino , Rinitis Alérgica/inmunología , Rinitis Alérgica Estacional/inmunologíaRESUMEN
Cetirizine is a second-generation antihistamine, derived from the metabolism of hydroxyzine, highly specific for the H1 receptors, and with marked antiallergic properties. Although its history began more than 30 years ago, it remains one of the most used drugs in children with a leading role in the medical care of children with allergic diseases. Cetirizine use is licensed for paediatric patients for the treatment of allergic rhinitis, and chronic spontaneous urticaria, in Europe in children older than 2 years old and in the USA in children older than 6 months old. This review provides a practical update on the use of cetirizine in children and adolescents.
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Aim: This work aimed to develop topical nanoemulsion gels of cetirizine, a second-generation antihistamine, to avoid its oral intake drawbacks and enhance skin permeation.Methods: Cetirizine nanoemulsions were formulated and characterised for their particle size, polydispersity index, zeta potential, drug release and drug permeation through rat skin. The optimised formulation, obtained using 23 full factorial design, was incorporated in carbopol and chitosan gels and evaluated clinically for urticaria treatment.Results: The optimised formulation had particle size of 32.015 ± 1.87 nm, polydispersity index of 0.29 ± 0.04, zeta potential of -19.31 ± 0.43 mV, cetirizine percent released of 98.50 ± 1.23% and permeability coefficient of 7.65 cm.h-1. Cetirizine nanoemulsion gels were more effective than their control gels in urticaria treatment with significant decrease in the degree of wheals and itching and higher recovery percent.Conclusion: Cetirizine nanoemulsion topical gels are expected to be a rational and effective tool for avoiding cetirizine oral side effects and targeting the affected skin.