2nd Generation Antihistamines Research Articles

Efficacy and safety of modern second-generation antihistamines

Allergic diseases are a huge problem for the practitioner today. Since 2nd generation antihistamines are the drugs of choice in the treatment of chronic urticaria and allergic rhinoconjunctivitis, the practitioner needs to be aware of the pharmacological properties, mechanisms of action, adverse effects and interactions with other drugs. The purpose of the review. This article provides an update on the clinical pharmacology, mechanisms of action, and safety of second- generation antihistamines. We identified potentially relevant studies by searching the electronic databases MEDLINE, SCOPUS, PubMed, Google Scholar and the Cochrane Database of Systematic Reviews over the last 5 years up to November 2022 using the terms: antihistamines, allergy, allergic rhinitis, urticaria, therapy, safety, efficacy, adverse effects, sedative antihistamines, second generation antihistamines, clinical trials. Further, according to the inclusion and exclusion criteria, as well as independent selection, all the authors of this article selected sources that met the criteria and compiled this review. Results. Recent studies have shown the efficacy and good tolerability of second-generation antihistamines, confirming their use as first-line drugs for the treatment of allergic rhinoconjunctivitis and urticaria.

Omalizumab in Chronic Spontaneous Urticaria: Assessment of Response in Twenty-Five Patients

Background Omalizumab is a recombinant humanized monoclonal antibody against immunoglobulin E (IgE). It is approved for the treatment of chronic spontaneous urticaria (CSU) in patients ≥12-years of age. Objective We carried out a retrospective cross-sectional study in 25 patients with CSU to evaluate the characteristics of response of CSU to omalizumab treatment. Method A retrospective cross-sectional study of a convenient sample of all patients diagnosed as CSU who have been using omalizumab treatment during the study period from January 2018 to January 2020 in the Dermatology Department in King Abdulaziz Hospital, Makkah, Saudi Arabia. Results A total of 25 patients have participated in this study. The average age of patients was 40-years. Majority of the patients were female (52.0%, n=15). The average duration of illness was 1.32-years. Majority of the patients (72.0%, n=18) received two courses of omalizumab treatment. Minority of patients (28.0%, n=7) received one course of omalizumab treatment which was statistically significant (p value<0.01). Number of patients who have been using oral 2nd generation antihistamine during the first course and 2nd course was (72%, n=18 out of 25) and (50%, n=9 out of 18) respectively. Number of flare-ups during 2nd course (1.72 flares up per patient, n=31 flare-ups among 18 patients) was less than the number of flares-up during 1st course (2.96 flares-up per patient, n=74 flare-ups among 25 patients) which was statistically significant (p value<0.01). Number of patients who showed no flare-ups during the 1st and 2nd course of omalizumab treatment was (16%, n=4 out of 25 patients) and (27.77%, n=5 out of 18 patients) respectively. The average intensity of flares-up during 2nd course of omalizumab treatment was less than the average intensity of flares-up during first course of omalizumab treatment as the following; during 2nd course ( 33.33%, n=6 out of 18 patients), (27.77% n=5 out of 18 patients), (11.11%, n=2 out of 18 patients) mild, moderate and severe flares-up respectively and the severity during 1st course was (40.0%, n=10 out of 25 patients), (28.0%, n=7 out of 25 patients), (16.0%, n=4 out of 25 patients) mild, moderate and severe flares-up respectively. Conclusion According to expert’s guidelines, CSU of ≥3-years would be treated with omalizumab for a minimum of one-year. In our study, in spite of the short duration of CSU (average duration was 1.32-years), the majority of patients (72.0%, n=18) received omalizumab for 1-year (two courses of omalizumab treatment) suggesting that the majority of patients with CSU in general requires omalizumab ≥1-year. Our study also showed 5 patients who were free of any flare-up and they were not using 2nd generation antihistamines suggesting that omalizumab alone as monotherapy can be effective

Plasmapheresis: Is it a potential alternative treatment for chronic urticaria?

BackgroundChronic urticaria is a common disease. Plasmapheresis is an alternative treatment that can be appropriate for patients who are resistant to treatment with 2nd generation antihistamines or for whom treatment with omalizumab is unsuitable.ObjectiveTo investigate the effect of plasmapheresis treatment in chronic urticaria.MethodsA retrospective analysis was performed based on the data of 98 patients suffering from refractory chronic urticaria who received plasmapheresis as an alternative treatment in Vilnius University’s Hospital Santaros Clinics from 2000 to 2020. The efficiency of the treatment was evaluated by clinical judgment.Results58.2% of the patients exhibited a complete or significant response; of these, 37.8% had temporary relief of symptoms and 20.4% achieved disease remission; 41.8% showed no response to the plasmapheresis. Men (34.8%) had a tendency to achieve disease remission more often than women (16%) (p < 0.05). One patient did not finish the plasmapheresis treatment due to the symptoms’ exacerbation and treatment with omalizumab was initiated.ConclusionPlasmapheresis is a safe and effective alternative treatment when traditional treatment is unavailable or does not relieve symptoms completely. Our data showed that plasmapheresis was effective in more than half of our patients.

Urticaria chronica új terápiás lehetőségei

Chronic urticaria is a multifactorial disease with increasing prevalence, that significantly deteriorates the quality of life of patients. Authors describe the pathomechanism of the disease, and they present the currently available treatment options and the promising future therapies as well. The therapeutic basis of chronic urticaria is the modern, 2nd generation antihistamines in a dosage of even four times higher than the regular one. In therapy resistant cases omalizumab or cyclosporin is advised. There is a growing demand for new medications because the number of those patients , who are non-responders or do not respond adequately to these therapies, is definitely increasing.

Primary care management of allergic rhinitis: a cross-sectional study in four ASEAN countries.

BackgroundIn primary care, general practitioners (GPs) and pharmacists are tasked with the frontline responsibility of identifying and managing allergic rhinitis (AR) patients. There are currently no consolidated data on current treatment practices, patient compliance, and usage of guidelines within Southeast Asian Nations (ASEAN). Objective: To assess the attitudes and practices on AR of GPs and pharmacists in 4 ASEAN countries (Philippines, Indonesia, Thailand, and Malaysia).MethodsA cross-sectional survey of 329 GPs and 548 pharmacists was conducted from May to November 2019. Participants answered a questionnaire focused on their i) current practice in the management of AR, ii) views on patient compliance, iii) understanding and usage of guidelines.ResultsClinical history was the most preferred method to diagnose AR by 95.4% of GPs and 58.8% of pharmacists. Second-generation antihistamines were the most widely available treatment option in GP clinics and pharmacies (94.8% and 97.2%) and correspondingly the most preferred treatment for both mild (90.3%, 76.8%) to moderatesevere rhinitis (90.3%, 78.6%) by GPs and pharmacists, respectively. Loratadine was ranked as the most preferred 2nd generation antihistamines (GP vs pharmacists: 55.3% vs 58.9%). More than 90% of GPs and pharmacists ranked length and efficacy of treatment as important factors that increase patient compliance. Awareness of the ARIA guidelines was high among GPs (80%) and lower among pharmacists (48.4%). However, only 63.3% of GPs and 48.2% of pharmacists knew how to identify AR patients.ConclusionsThe survey in the 4 ASEAN countries has identified a need to strengthen the awareness and use of ARIA guidelines among the primary care practitioners. Adherence to ARIA guidelines, choosing the appropriate treatment option and prioritizing factors that increases patient compliance may contribute to better management outcomes of AR at the primary care practice

Efficiency of Adding Omalizumab to Standard Therapy for Children with Recurrent Spontaneous Urticaria: Comparative Observational Study

Background. Recurrent spontaneous urticaria (RSU) is rare in children, thus, it is debilitating condition that always requires treatment. There are several limitations on the drugs use in children with RSU. Omalizumab is the effective medication for achieving the control of RSU, used in adolescents over 12 years of age.The aim of the study is to compare the efficiency of various approaches for RSU management in children.Methods. The three-year comparative study of patients with RSU aged from 1 to 17 years managed only with 2nd generation antihistamines in standard or increased doses for at least 3 months and patients managed in addition to standard treatment with omalizumab (300 mg once in 4 weeks subcutaneously) was conducted. The essential treatment outcomes are achieving control of the disease (UAS7 = 0) in 6 months and remission maintaining after 36 months of observation. Additional outcomes are decrease in the number of aggravations that required the use of glucocorticosteroids (GCS) during 3 years of followup; analysis of treatment outcomes of patients with severe urticaria in subgroups (including UAS7 levels).Results. The frequency of disease control (UAS7 = 0) by 6 months of therapy was significantly higher in patients of the omalizumab group — 76%, in the second group — 0%. The UAS7 in the omalizumab group was 0 (0; 1) points, in the group of patients on standard therapy — 13 (10; 16) points (p &lt; 0.05). Remission was observed in 53% of patients (9 people) in the omalizumab group in 36 months, in the comparison group — in 32% (13 people), p = 0.129; UAS7 in the omalizumab group was 0 (0; 8.5) points, in the comparison group — 8 (0; 13) points, p = 0.076. The use of systemic GCS for acute treatment decreased during 3 years of follow-up: in the omalizumab group — from 41 to 5.9%, in the group on 2nd generation antihistamines — from 46 to 19% (p = 0.258). The result of subgroup analysis was similar.Conclusion. Adding omalizumab to standard RSU therapy makes it possible to achieve control of the disease reliably faster in most cases. There was gradual decrease in RSU activity in the group on standard therapy during the 3-year follow-up: spontaneous remission was mentioned in 32% of children within 3 years.

Successful Treatment of Chronic Spontaneous Urticaria Associated with Autoimmune Thyroiditis: Clinical Case

научный биометрический журнал, который знакомит читателя с клиническими рекомендациями и особенностями применения лекарственных и вакцинных средств у детей, предоставляет исчерпывающую информацию о воздействии лекарственных средств на плод, о проводимых в

The potential impact of 1st and 2nd generation antihistamines on male fertility

Histamine antagonists are medications used to block the action of histamine at histamine receptors. H1 antagonists are mainly taken to reverse the effects of histamine during allergic reactions. Cetirizine hydrochloride and pheniramine maleate are the most clinically used H1 antihistamines; they have common tolerable side effects such as sedation, dizziness, fatigue, dry mouth, and nausea. The effect of H1 antagonists on male hormones and its outcomes on male fertility are still unclear. The aim of the present study was to evaluate the possible effects of both cetirizine and pheniramine maleate on male fertility. Measurement of prolactin, FSH, and LH serum levels and sperm count during chronic use. Cetirizine hydrochloride significantly increased prolactin levels compared with pheniramine maleate and control groups. Hyperprolactinemia significantly decreased FSH and LH levels and sperm count in the cetirizine hydrochloride treated group. In conclusion, this study reports that the second-generation antihistamine cetirizine hydrochloride has potent and significant effects on male fertility compared with the first-generation H1 antihistamine pheniramine maleate through its changes in prolactin, LH, and FSH levels. These hormonal changes decreased spermatogenesis and sperm count.

New possibilities for symptomatic treatment of allergic rhinitis

Allergic rhinitis is one of the most common human diseases and causes a deterioration of the quality of life. The prevalence of allergic rhinitis in the Russian Federation and in the world has increased significantly. The main pharmacological group in the treatment of allergic rhinitis is the 2nd generation antihistamines with high affinity for H1-receptors. The article presents an overview of the new representative of the abovementioned group of drugs - the drug bilastine (Nixar®). 

A Cross-Sectional study of Drug Prescription Pattern in Urticaria patients attending Dermatology &amp; Venereology Department in a Rural Tertiary Care Teaching Hospital

Background: Urticaria is a very common skin condition characterized by recurrent, pruritic (itchy), pink-to-red edematous (swollen) lesions that often have pale centers (wheals). Histamine is the main mediator of urticaria and H1 antihistamines represent the initial and mainstay treatment of urticaria. The newer second generation H1 antihistamines are preferred over the older first generation H1 antihistamines as the initial choice of therapy due to its less sedating and less cholinergic side effects. Although numerous treatments are available for urticaria, there is little information about the prescription pattern for the treatment of urticaria. Hence this study was conducted. Methods: This was a cross-sectional study conducted on 100 newly diagnosed and untreated patients of urticaria who attended Dermatology and Venereology outpatient department of a rural tertiary care teaching hospital. The prescriptions were collected for the duration of 18 months and details of prescription (particulars of the patient, diagnosis, name of the drugs, dose, route of administration, total duration etc.) were collected in case record forms. Results: Majority of the patients (34) belonged to the age group of 21-35years. The mean age of the patients was 34.35±15.26 years. Most of the patients were treated with oral antihistamines. Among oral antihistamines, most of the patients received 2nd generation antihistamines either as monotherapy or in combination with 1st generation antihistamines and H2 blockers. Among 2nd generation antihistamines, fexofenadine was prescribed highest either as monotherapy or in combination with levocetirizine and cetirizine. Patients with more severe form of disease were treated with combination of oral and parenteral therapy. Further long term study is required for proper assessment of prescription pattern in urticaria patients. Conclusion: Most of the patients with urticaria can be effectively treated with Oral antihistaminic medication, and additional parenteral therapy may be required only for severe cases of acute on chronic urticaria. Keywords: Urticaria, Oral medication, Parenteral therapy, Antihistamines

CLINICAL AND PHARMACOLOGICAL PECULIARITIES OF CETIRIZINE USE FOR THE THERAPY OF ALLERGIC DISEASES IN CHILDREN

научный биометрический журнал, который знакомит читателя с клиническими рекомендациями и особенностями применения лекарственных и вакцинных средств у детей, предоставляет исчерпывающую информацию о воздействии лекарственных средств на плод, о проводимых в

Rupatadine oral solution improves rhino‐conjunctive symptoms control in children with 6‐11 years weighing ≥25 kg with persistent allergic rhinitis

Background Clinical trials with the newer 2nd generation antihistamines in children under the age of 12 years have been performed previously but further studies are needed in order to show efficacy and safety in the most unfavourable clinical conditions such as persistent allergic rhinitis (PER). Rupatadine oral solution was developed for children with allergic rhinitis in view of its rapid onset of action and its lack of relevant side effects. These advantages were confirmed previously in a phase III study in children 6-11 years. Objective To assess the efficacy and safety of rupatadine (RUP) oral solution in a subgroup of children between 6 and 11 years weighing ≥25 kg with PER. Methods A subanalysis was performed from a previous placebocontrolled study carried out in patients between 6-11 years diagnosed as PER according to ARIA criteria. This analysis included patients with a positive prick test, weight ≥25 kg and basal nasal symptoms score (including rhinorrhea, nasal blockage, sneezing and nasal itching assessment) ≥24 obtained in 4 days throughout the 2-week screening period. Patients were allocated to treatment with either RUP oral solution (1 mg/ml) or placebo during 6 weeks. The dose was 5 ml of oral solution. The main efficacy endpoint was the change from baseline of the nasal (4TSS) and global symptoms (5TSS) score at 4 and 6 weeks of treatment. Furthermore the assessment of children’ sq uality of life at 4, 6w eeks by means of PRQLQ was also evaluated.

Clinical aspects of chronic urticaria in children

Purpose : Chronic urticaria is a disorder characterized by the appearance of wheals for more than 6 weeks; in most cases, the etiology is unknown. This study was aimed to discover the clinical aspects, the etiologic factors, and the course of chronic urticaria. Methods : 51 children who were diagnosed with chronic urticaria in the past 4 years, and who had had follow-ups more than 6 months after diagnosis in the pediatric department of Soonchunhyang University Hospital in Bucheon, were enrolled in the study. The laboratory findings, clinical aspects, and courses were retrospectively investigated by medical record review and telephone interview. Results : The median age of children with chronic urticaria was 4 years (8 months to 16 years) and the ratio of male to female was 1.4:1. Of the total, 39.2% of patients had a history of atopy. Angioedema occurred concurrently with urticaria in 11.8% of patients, and dermographism was seen in 41.2%. Results of thyroid function tests were normal and thyroid autoantibodies were absent in all cases. Regarding etiology, most cases (74.5%) were forms of idiopathic urticaria. Urticaria was induced by physical factors in 19.6% of patients. Open challenge tests revealed that 3 patients were allergic to food additives (glutamate 2, glutamate, and sulfite 1). In this study, most of the patients reported good response after medication of 1st- or 2nd-generation antihistamines alone. Follow-up at 6 months revealed that 70.6% of patients had experienced remission, and 84.8% of children who had follow-up at 1 year presented remission. Conclusion : Chronic urticaria in most patients was idiopathic. Remission occurred within 1 year of diagnosis, in most cases so chronic urticaria in children seems to have good prognosis.

A Survey of Patients' Understanding of Drowsiness as Side Effect of 2nd Generation Antihistamines

〔目的〕アレルギー性鼻炎治療で用いる抗ヒスタミン薬には，眠気の副作用を生じるものが多いが，患者自身がこの副作用を承知で内服しているか重要である。今回，眠気に対する患者認識度調査を行なった。〔方法〕平成19年2月～3月末に，アレルギー性鼻炎で当院外来受診し，抗ヒスタミン薬が処方された患者全員257名を対象に，本人同意取得後に薬局窓口にて，抗ヒスタミン薬によって生じる眠気に対するアンケート調査を行なった。〔結果〕232名 (平均年齢53.5±17.5歳，男85名，女147名) より有効回答を得た (有効回答率90.3%)。この内45名 (19.9%) が，抗ヒスタミン薬一般に眠気の副作用があることを知らなかった。さらに，この45名中24名は実際に眠気を有する抗ヒスタミン薬が処方され，21名は主治医から副作用の説明を受けていなく，眠気の副作用を知っていれば内服しなかったと答えた。また，この21名中10名はすでに内服後に，眠気を感じながら自動車運転を行なっていた。〔結論〕抗ヒスタミン薬による眠気の副作用が軽視されている現状が明らかとなった。患者への適切な服薬指導と副作用のチェック機能を果たす薬局機能の重要性が再認識された。