Antihistamines Research Articles

Dystocia due to a dicephalus monster fetus in a buffalo and It's successful per vaginal removal

Fetal anomalies and monstrosities are common causesof dystocia in bovines and are disturbances of development that involve the sexual organs and cause great distortion of the individual. The incidence of abnormal calvings in buffaloes is from 4.6% to 12.6%. Eight years aged native buffalo, with its third lactation with ahistory of natural service 306 days back was presented to the Veterinary Hospital, Hombal Village, Gadag taluk of Gadag district, Karnataka State. The animal was presented with the complaintof inspite of continuous straining for the last 06 h after the expulsion of the first water bag, there was no progression to the parturition stage. Pervagina lexamination reveale dafully dilatedcervix and abnormal fetus with two heads joined at the neck in anterior presentation with dorsolateral position witha deviation ofhead, one head was removed gently followed by anotherthat was 90-degree angle corrected and removed a female dead fetus under low caudal epidural anaesthesia. Adicephalusmonsterfetus was relieved pervaginally without surgicalintervention and reported. Post operative care consisted of intravenousantibiotics, fluids intra muscular anti-inflammatory and anti-histamine drugs for seven days.The buffalo hadan uneventful recovery.

General Synthesis of 3‐Azabicyclo[3.1.1]heptanes and Evaluation of Their Properties as Saturated Isosteres**

AbstractA general approach to 3‐azabicyclo[3.1.1]heptanes by reduction of spirocyclic oxetanyl nitriles was developed. The mechanism, scope, and scalability of this transformation were studied. The core was incorporated into the structure of the antihistamine drug Rupatidine instead of the pyridine ring, which led to a dramatic improvement in physicochemical properties.

General Synthesis of 3-Azabicyclo[3.1.1]heptanes and Evaluation of Their Properties as Saturated Isosteres.

A general approach to 3-azabicyclo[3.1.1]heptanes by reduction of spirocyclic oxetanyl nitriles was developed. The mechanism, scope, and scalability of this transformation were studied. The core was incorporated into the structure of the antihistamine drug Rupatidine instead of the pyridine ring, which led to a dramatic improvement in physicochemical properties.

#6189 PRECLINICAL VALIDATION OF REPURPOSABLE CANDIDATE DRUG COMPOUNDS FOR CYSTIC NEPHROPATHIES

Abstract Background and Aims Early-onset cystic kidney disease is a clinically and genetically heterogeneous and overlapping group of rare and often severe disorders with limited, mostly symptomatic treatment options. We developed and utilized inherited polycystic cystic kidney disease (PKD) models to search for pharmacological agents that can rescue or mitigate the disease phenotype. Method A high-content screening platform for identification of chemical modifiers of cyst formation and progression in a zebrafish genetic cystic nephropathy model (IFT172 Morpholino-based knockdown in Tg(wt1b:eGFP)), using robotic microscopy with automated image classification and phenotype quantification was used to screen 1280 compounds from the Prestwick library for their cyst-inhibiting activity. Compounds with cyst-inhibitory efficacy and low toxicity in the Zebrafish and oral and trans-placental availability were selected for further study in two rodent PKD models, i.e. PCK and PKD/Mhm (cy/+) rats. Groups of 3-week-old homozygous PCK and heterozygous PKD/Mhm rats were administered orally for 10 weeks three candidate compounds, which included an antihistamine, an anthelmintic and an antifungal agent, or regular ROD16 chow (sick controls). In experimental week 5, blood was taken, and the kidneys were imaged sonographically under anaesthesia. In the last experimental week, glomerular filtration rate was determined by transcutaneous FITC-sinistrin injection. Masson trichrome staining was used to evaluate cyst formation in kidneys. Results 60 compounds with cyst preventive or cyst size reducing activity were identified in the zebrafish screening model. While one third of these compounds caused severe general toxicity, 12 of them showed medium and 4 strong cyst-inhibitory activity with no or mild off-target effects. These substances were from anthelminthic, antihistamine, antifungal and proton pump inhibitor drug classes. Preliminary results in the rodent models suggest that anthelminthic treatment reduced the number of cysts in female (3.3±1.3 vs. untreated control, 5.4±0.9) but not male PCK rats (3.7±0.6 vs. 3.9±0.7) after 10 weeks of treatment. These changes were accompanied by improved glomerular filtration rate (GFR) in treated females (t½: 0.22±0.04 min vs. 0.3±0 min). An improvement in GFR was also observed in female PKD/Mhm rats after 10 weeks of treatment with the anthelmintic compound compared to untreated control animals (t½: 0.24±0.06 vs. 0.51±0.16 min, p = 0.02). Conclusion Candidate cyst-inhibitory drugs identified in a zebrafish model were applied in rat models of PKD. The administration of an anthelmintic agent had a positive impact on the progression of polycystic kidney disease. The beneficial effect appears to be sex specific. If further corroborated, our findings may allow repurposing of a drug approved for another indication to slow disease progression in patients with cystic kidney diseases.

PPIs and gastric cancer: any causal relationship?

Hydrochloric acid is crucial in gastric physiology. In 1978 cimetidine, the first H2 antagonist of histamine receptors on the gastric parietal cell was introduced into therapy, inducing acid. Lasting the years, several studies focused on the potential relationship between inducing hypo-achlorhydria and risk of developing gastric cancer. In 1988 omeprazole, the first proton pump inhibitor, entered therapy. In 1996, Kuipers underlined the danger of progression of chronic atrophic gastritis in subjects taking PPIs. In 2018, one paper from Korea and an another on from Sweden suggested a possible relationship between long-term PPI therapy and the development of gastric cancer. Over the years, several articles, meta-analyzes and population based focused on relationship between long-term of PPI use and the onset of gastric cancer, with conflicting results. As reported, the presence of bias in the collection of cases, in particular concerning the evaluation of the H.p. status and presence of atrophic gastritis and intestinal metaplasia in subjects treated with PPI, can lead to noticeable errors in the results and conclusions, as demonstrated in the literature by exhaustive methodological studies of pharmacoepidemiology. A possible bias in the collection of case histories is due to the fact that PPIs are often administered to dyspeptic patients, among which there are patients already carriers of gastric neoplasia: the so-called inverse causality. Literature data, amended by methodological bias (sampling errors, lack of comparative assessment of Hp status and atrophic gastritis) NOT support a causal relationship between long-term PPIs therapy and the onset of gastric cancer.

Poly(tetrahydrofuran)-based fabric phase sorptive extraction combined with HPLC-UV for the determination of antihistamines in human urine

Herein, a poly(tetrahydrofuran)-based fabric phase sorptive extraction (FPSE) membrane was utilized for the isolation and determination of three antihistamine drugs (carbinoxamine, chlorpheniramine, and diphenhydramine) in human urine followed by HPLC-UV analysis. Among other membranes tested, the sol–gel poly(tetrahydrofuran) sorbent coated FPSE membrane was found to be more suitable for extracting the selected drugs. Based on their engineered affinity, the fabricated membranes are highly permeable that allows the extraction of biological samples with no previous pretreatment. The experimental parameters were systematically investigated and optimized using a central composite design of experiment and one-factor-at-a-time approaches. The proposed analytical scheme was validated in terms of linearity (0.10 – 5.0 μg mL−1), selectivity, limit of detection (0.03 μg mL−1), limit of quantitation (0.10 μg mL−1), precision (<12.7 % in all circumstances), and accuracy (% relative recovery: 88.1 – 113.7%). The membranes were reusable for at least 15 extractions with a set criterion of a 10% deviation of the initial performance. The final protocol was efficiently applied for the determination of selected antihistamines in authentic human urine after oral administration of chlorpheniramine and diphenhydramine-containing tablet and syrup, respectively.

Trends in Influenza and Related Health Resource Use During 2005-2021 Among Children in Japan.

To determine the epidemiological trends in pediatric influenza and changes in healthcare resource use from 2005 to 2021 using nationally representative outpatient database in Japan. We conducted a retrospective cohort study consisting of 3.5 million children with 177 million person-months during 2005-2021 using Japan Medical Data Center claims database in Japan. We investigated trends in incidence rates of influenza and changes in healthcare resource use (eg, use of antivirals) over 17 years. Generalized estimation equations were used to investigate the impact of the 2009 influenza pandemic and the coronaviral disease 2019 (COVID-19) pandemic on incidence rates of influenza and related healthcare utilization. Annual incidence rates of influenza were estimated at 55 cases per 1000 person-years with a 93% relative increase [95% confidence interval (CI): 80%-107%] during the 2009 influenza pandemic and a 99.4% relative reduction (95% CI: 99.3%-99.4%) during the COVID-19 pandemic. Similar patterns were observed for health resource use, total healthcare costs, admission rates and antiviral agent use. Approximately 80% of children with influenza received prescriptions for antivirals. The most prescribed antivirals were oseltamivir, but we observed a temporal increase in zanamivir use during 2007-2009, an increasing trend in laminamivir use during 2010-2017, a temporal increase in baloxavir use in 2018. Symptomatic medications with serious side effects (codeine, salicylate, sedative antihistamine) showed decreasing trends over the study period. Influenza incidence and healthcare resource use were largely affected by the 2009 influenza pandemic and the COVID-19 pandemic. Our study indicates improvement of quality in healthcare delivered to children.

A clinicoepidemiological study on tinea incognita with assessment of its treatment strategies and drug prescribing practices in a tertiary care hospital.

The incidence of tinea incognita (TI) appears to have increased over recent years owing to the easy availability of topical corticosteroids as over-the-counter preparations. Describing the various clinicoepidemiological aspects of TI and assessing the treatment strategies and prescribing practices followed for its management. A prospective study was conducted with 170 patients in the department of Skin and STD of a tertiary care hospital at Salem from Jan 2022 to June 2022. The various sociodemographic information was obtained by interviewing the patients and a detailed dermatological examination was performed by the dermatologists to describe the morphology of lesions, and sites involved. The results were statistically analysed and expressed in the form of percentages. Most of the patients were in the age group of 41-50 years. The majority of patients were illiterate, unskilled workers, married, belonging to the lower middle class, from rural localities, and with positive family histories. Most of the patients were suffering from TI for more than 1 year. The commonly used treatment modality was combinational therapy which comprises oral and topical antifungals and antihistaminic drugs. The commonly prescribed antifungal was itraconazole. This study emphasises the need to spread awareness among the pharmacist and the community regarding the adverse consequences of practicing self-medication with topical corticosteroids.

Editorial introductions.

Editorial introductions.

Analysis of second-generation anti histamine fexofenadine soft gelatin capsules and its related compound by using RP-HPLC

Analysis of second-generation anti histamine fexofenadine soft gelatin capsules and its related compound by using RP-HPLC

Adsorption Characteristics of Cetirizine on Graphene Oxide

Water pollution caused by emerging contaminants such as pharmaceutical compounds is a growing problem worldwide. In this reported work, graphene oxide (GO) was directly used to remove an antihistamine drug, cetirizine. GO was prepared from graphite using a modified Hummer’s method and was characterized by UV–vis spectroscopy, Fourier-transformed infrared spectroscopy (FTIR), thermogravimetric analyzer (TGA), field scanning electron microscope (FE-SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), etc. GO was demonstrated to be a highly efficient adsorbent for removing cetirizine from an aqueous solution. The adsorption of cetirizine on GO at various pH levels showed that in acidic pH with the adsorption shows faster kinetics and complete removal of cetirizine within 10 min, followed by neutral pH, which showed relatively slower kinetics but complete removal of cetirizine. However, at basic pH, GO could not completely remove cetirizine after 24 h. At a neutral pH, GO showed maximum adsorption of 81.30 mg g−1 of cetirizine. The adsorption isotherm results showed good agreement with the Langmuir isotherm. The BET surface area analysis showed the presence of mesoporosity in GO. In addition, the BET analysis further revealed a type IV isotherm curve being followed. A plausible mechanism is also discussed in the paper. The recyclability experiment demonstrates an adsorption efficiency of 85% after four cycles. The thermodynamic study reveals that adsorption is thermodynamically less favorable at higher temperatures. Hence, the current study successfully demonstrates the use of GO as an efficient adsorbent in removing cetirizine. It also studies the various factors and interactions affecting adsorption. Thus, this study sheds light on the adsorption characteristics of cetirizine on graphene oxide.

Experimental solubility of fexofenadine hydrochloride (antihistamine) drug in SC-CO2: Evaluation of cubic equations of state

Fexofenadine hydrochloride is an antihistamine drug which is used in the treatment of allergy symptoms, like urticaria and hay fever. In this research, the solubility of fexofenadine hydrochloride was measured in supercritical carbon dioxide (SC-CO2) at different pressures (120–270 bar) and temperatures (308.2–338.2 K), for the first time. The solubility data were in the range of 0.073 < y × 104 < 0.854. The experimental data on the solubility of fexofenadine hydrochloride were correlated by two approaches: (1) three cubic equations of state (CEoSs) with two mixing rules, and (2) nine density-based correlations with 3–6 adjustable parameters. Among CEoS, Peng-Robinson EoS with Kwak-Mansoori mixing rule, showed more accuracy, especially at higher pressures with an average absolute relative deviation percent (AARD%) of 5.48. Moreover, Garlapati and Madras (model I) with AARD% of 5.65 showed more accurate correlation compared to density-based models. Finally, total, vaporization, and solvation enthalpies of the fexofenadine hydrochloride-CO2 system were calculated to be 39.5759, 52.4635, and − 12.8876 kJ.mol−1, respectively.

The Second Qatar Allergy and Immunology Conference: An Editorial.

The 2nd Qatar Allergy and Immunology Conference was organized by the Adult Allergy and Immunology Division of Hamad Medical Corporation (HMC) over two days as a hybrid conference on the 10th and 11th of February 2023 at ITQAN Clinical Simulation and Innovation Centre. The conference was preceded by two pre-conference workshops directed toward physicians and nurses on the 9th of February, 2023. The workshops aimed to promote awareness about allergic and immunologic diseases among physicians and nurses. The 2nd Qatar Allergy and Immunology Conference represented a great learning platform for healthcare professionals and opportunities to update knowledge, present research, and meet professionals since allergy and immunology practice is a rapidly evolving science focusing on allergic and immunologic conditions and their advanced treatment options. The conference’s scientific program focused on the following topics: airway allergy and asthma, skin allergies, diagnosis and management of primary immunodeficiency diseases, and novel therapeutics for allergic diseases. One of the significant achievements of this year’s conference is conducting a focused research symposium that provides a flagship platform for medical students and faculty scholars to present their research experiences and up-to-date health topics and to share their experiments and research findings with a broader community. It aimed to gather scientists and physicians from across Qatar and internationally with recent updates regarding the role of precision medicine in allergy and immunology science and practice. HMC supported the event in partnership with the Qatar Allergy and Immunology Society (QAIS) (a chapter of the Qatar Medical Association). It was accredited for 21.25 CPD Category 1 as defined by the Ministry of Public Health’s Department of Healthcare Professions. The conference hosted many expert speakers from Qatar, the Gulf region, and internationally. The total number of participants was 1082, comprised of physicians, nurses, and scientists. We received 34 abstracts, 32 were accepted for poster presentations, and the best six were selected for the oral presentation session. Another achievement of our conference is advocating the Arabic language. One lecture and one oral abstract were presented in Arabic to demonstrate the importance and simplicity of using the Arabic language in medical education and science.

Migraine, Allergy, and Histamine: Is There a Link?

The relationship between migraines and allergies is controversial. Though they are epidemiologically linked, the underlying pathophysiological connection between them remains unclear. Migraines and allergic disorders have various underlying genetic and biological causes. As per the literature, these conditions are epidemiologically linked, and some common pathophysiological pathways have been hypothesized. The histaminergic system may be the clue to understanding the correlation among these diseases. As a neurotransmitter in the central nervous system with a vasodilatory effect, histamine has a well-documented influence on the allergic response and could be involved in the pathophysiology of migraines. Histamine may influence hypothalamic activity, which may play a major role in migraines or may simply influence their severity. In both cases, antihistamine drugs could prove useful. This review examines whether the histaminergic system, particularly H3 and H4 receptors, may provide a mechanistic link between the pathophysiology of migraines and allergic disorders, two common and debilitating conditions. Identifying their connection could help identify novel therapeutic strategies.

Efficacy of Antihistamine Nasal Spray Compared with Oral Antihistamine in Treatment of Allergic Rhinitis

Introduction: Allergic rhinitis is described as nasal membrane inflammation and is characterized by a symptom complex of sneezing, nasal congestion, itching, and rhinorrhea. These structures are also involved to some extent due to the continuity of the mucosal wall of the nose with the paranasal sinus and its communication with the ears through the Eustachian tube and with the eyes with the nasolacrimal duct. Objective: To determine the efficacy of antihistamine nasal spray compared with oral antihistamine in treatment of allergic rhinitis. Method: This Randomized control trial was conducted at the ENT department, Services Hospital, Lahore for 18 months from 01-02-2020 to 31-08-2022. Sample 450 patients of Allergic rhinitis of both sexes between the ages of 15-50 years were selected using simple random sampling technique. Patients were divided into 2 groups. Group A received oral antihistamine ebastine 10mg OD whereas Group B received nasal antihistamine spray olopatadine 0.6% (600mcg/100microlitre). Patients were then followed up every 2 weeks for 01 month. Data was enetered and analyzed in SPSS. Results: Total 450 patients were enrolled. The mean age was 24.5+ 3.0 years. There were 270(60%) male and 180(40%) female. In group A, there were 72(32%) patients 10 to 30 years of age group and 153(68%) were 30 to 50 years of age group. In group B, 65(28.8%) patients between 10 to 30 years and 160(71.1%) above 30 years of age group. Table: 2 In our study, sneezing was the most common 441(98%) followed by rhinorrhea 427(94.8%), nasal obstruction 338(75.1%), etc…In Group A, 153(68%) patients got relief and 72(32.0%) patients felt decrease in symptoms of Allergic rhinitis. In Group B, 144(64.0%) patients got relieved of symptoms, 81(36.0%) patients were partially relieved. Conclusion: The conclusion of the study that oral antihistamine and intranasal antihistamine nasal spray proved that treatment results of both treatment options were comparable in terms of reduction in the symptoms of allergic rhinitis. AIM: Our aim of the research is to determine the efficacy of antihistamine nasal spray compared with oral anti histamines in the treatment of allergic rhinitis. The sedating effects of oral antihistamines can totally be avoided in case nasal sprays have the same efficacy. Keywords: Allergic rhinitis, Antihistamine, Seasonal allergic rhinitis,

P19-derived neuronal cells express H1, H2, and H3 histamine receptors: a biopharmaceutical approach to evaluate antihistamine agents

Histamine is a biogenic amine implicated in various biological and pathological processes. Convenient cellular models are needed to screen and develop new antihistamine agents. This report aimed to characterize the response of neurons differentiated from mouse P19 embryonal carcinoma cells to histamine treatment, and to investigate the modulation of this response by antihistamine drugs, vegetal diamine oxidase, and catalase. The exposure of P19 neurons to histamine reduced cell viability to 65% maximally. This effect involves specific histamine receptors, since it was prevented by treatment with desloratadine and cimetidine, respectively, H1 and H2 antagonists, but not by the H3 antagonist ciproxifan. RT-PCR analysis showed that P19 neurons express H1 and H2 receptors, and the H3 receptor, although it seemed not involved in the histamine effect on these cells. The H4 receptor was not expressed. H1 and H2 antagonists as well as vegetal diamine oxidase diminished the intracellular Ca2+ mobilization triggered by histamine. The treatment with vegetal diamine oxidase or catalase protected against mortality and a significant reduction of H2O2 level, generated from the cells under the histamine action, was found upon treatments with desloratadine, cimetidine, vegetal diamine oxidase, or catalase. Overall, the results indicate the expression of functional histamine receptors and open the possibility of using P19 neurons as model system to study the roles of histamine and related drugs in neuronal pathogenesis. This model is less expensive to operate and can be easily implemented by current laboratories of analysis and by Contract Research Organizations.

Intranasal drugs possibilities in the treatment of patients with rhinitis medicamentosa

Introduction. The article presents the physiology of nasal breathing, as well as the problem of nasal obstruction and the mechanisms of its development. Topical issues of rhinitis medicamentosa are discussed, based on the pathogenic links of this condition. It has been established that there is no single treatment regimen for rhinitis medicamentosa at the moment.Objectives. To evaluate the effectiveness and safety of the use of intranasal drugs in patients with medical rhinitis.Materials and methods. A comparative study of the clinical use of the complex preparation Frinozol®, the active substances of which are the decongestant phenylephrine and the antihistamine drug cetirizine, intranasal glucocorticosteroid Nosefrin®, as well as their combinations, was carried out in patients with rhinitis medicamentosa.Results. The results showed that the use of Frinozol®, Nozefrin®, as well as a combination of these drugs leads to a decrease in the frequency of use of nasal decongestants, and in a larger percentage of cases or to the complete cessation of their use by patients with drug-induced rhinitis. The combination of Frinozol – Nozefrin is somewhat more effective. However, a number of patients resume the use of nasal decongestants after some time, which leads to the need for additional courses of conservative therapy. In the course of the observational study, we noted excellent and good tolerability of the drugs, and patient satisfaction with the treatment in all groups.Conclusions. The problem of drug-induced rhinitis remains unresolved, which is why the search for optimal and effective schemes for the conservative treatment of this disease continues. The use of intranasal glucocorticosteroids and topical antihistamines can significantly reduce the frequency of use of nasal decongestants, or completely abandon their use.

Development and evaluation of pH sensitive semi-interpenetrating networks: assessing the impact of itaconic acid and aloe vera on network swelling and cetirizine release.

Hydrogels are crosslinked three-dimensional networks, and their properties can be easily tuned to target the various segments of the gastrointestinal tract (GIT). Cetirizine HCl (CTZ HCl) is an antihistaminic drug, which when given orally can upset the stomach. Moreover, this molecule has shown maximum absorption in the intestine. To address these issues, we developed a pH-responsive semi-interpenetrating polymer network (semi-IPN) for the delivery of CTZ HCl to the lower part of the GIT. Initially, 10 different formulations of itaconic acid-grafted-poly (acrylamide)/aloe vera [IA-g-poly (AAm)/aloe vera] semi-IPN were developed by varying the concentration of IA and aloe vera using the free radical polymerization technique. Based on swelling and sol-gel analysis, formulation F5 containing 0.3%w/w aloe vera and 6%w/w IA was chosen as the optimum formulation. The solid-state characterization of the optimized formulation (F5) revealed a successful incorporation of CTZ HCl in semi-IPN without any drug-destabilizing interaction. The in vitro drug release from F5 showed limited release in acidic media followed by a controlled release in the intestinal environment for over 72h. Furthermore, during the in vivo evaluation, formulation F5 did not affect the hematological parameters, kidney, and liver functions. Clinical observations did not reveal any signs of illness in rabbits treated with hydrogels. Histopathological images of vital organs of treated animals showed normal cellular architecture. Thus, the results suggest a non-toxic nature and overall potential of the developed formulation as a targeted drug carrier.

Green quality by design HPLC approach for the simultaneous determination of Bilastine and Montelukast

For the simultaneous estimation of two co-formulated antihistaminic drugs (Bilastine and Montelukast), a novel and eco-friendly reversed-phase HPLC approach with both diode array and fluorescence detection modes was designed. Rather than using the routine methodology, the Quality by Design (QbD) approach was adopted to speed up the method development and to test robustness of the method. To evaluate the effect of variable factors on chromatographic response, a full factorial design was used. The chromatographic separation was performed using isocratic elution on the C18 column. The mobile phase consists of 92% methanol, 6% acetonitrile, and 2% phosphate buffer with 0.1 (v/v) triethylamine adjusted to pH 3, it was pumped at a flow rate of 0.8 mL/min with an injection volume of 20 μL. The developed stability indicating HPLC approach was used to assess the stability of montelukast (MNT). It was subjected to a variety of stress conditions, including hydrolytic (acid–base), oxidative, thermal, and photolytic stress conditions. All of these conditions were found to have relevant degradation pathways. Under the described experimental conditions, MNT degradation followed pseudo-first-order kinetics. The kinetic parameters of its degradation (rate constant and t1/2) were calculated and a proposal for the degradation pathway was postulated.

Probing Diverse Interactions of Model Amino Acids Prevalent in Aqueous Solutions of Anti-Histaminic Drug by Physicochemical Contrivance

Probing Diverse Interactions of Model Amino Acids Prevalent in Aqueous Solutions of Anti-Histaminic Drug by Physicochemical Contrivance