Use Of First-generation Antihistamines Research Articles

Navigating allergies safely: tailored solutions in special circumstances – a comprehensive review of antihistamines

Personalised medicine is critical in managing allergic diseases, with the variety of second-generation antihistamines necessitating tailored approaches to individual patient needs. This encompasses considerations of age, pregnancy, breastfeeding, hepatic and renal failure, drug interactions, and aging. This paper synthesises current research and guidelines on the use of antihistamines across diverse clinical scenarios, paying special attention to paediatric allergy treatment, including safety profiles of first- and second-generation antihistamines, their use during pregnancy, breastfeeding, and interactions with other drugs, as well as considerations for elderly patients. Second-generation antihistamines are preferred for allergy treatment due to their safety, minimal adverse effects, and efficacy, with a strong recommendation against the use of first-generation antihistamines due to their potential to induce severe adverse reactions. Cetirizine, levocetirizine, and desloratadine are favoured in infants; whereas loratadine, rupatadine, and bilastine are recommended for preschoolers and older children. The safety of selected second-generation antihistamines during pregnancy (notably cetirizine, levocetirizine, desloratadine) and breastfeeding (notably loratadine, desloratadine, fexofenadine), in patients with renal failure and elderly patients (bilastine, desloratadine, fexofenadine), and patients with hepatic failure (bilastine, fexofenadine) is highlighted. The choice of second-generation antihistamines should be based on the patients’ individual needs and conditions to achieve optimal therapeutic outcomes and ensure safety, emphasising the importance of drug selection in varying clinical contexts.

The impact of decreasing potentially inappropriate medications on activities of daily living in a convalescent rehabilitation setting

Background Polypharmacy or potentially inappropriate medications negatively affect the functional recovery of rehabilitation. However, limited research exists regarding the effect of decreasing in potentially inappropriate medications use on functional improvement of rehabilitation in geriatric Japanese patients. Objective To elucidate whether decreasing PIM during hospitalization could be a predictor of rehabilitation outcomes among geriatric patients in a convalescent rehabilitation setting. Setting This study was conducted at the convalescent rehabilitation ward in the Hitachinaka General Hospital in Japan. Methods This retrospective observational cohort study included consecutive geriatric patients admitted at the convalescent rehabilitation ward between 2010 and 2018. Participants were divided based on presence or absence of decreasing in potentially inappropriate medications use during hospitalization. A multiple linear regression analysis was performed to analyze whether decreasing potentially inappropriate medications use during hospitalization could be a predictor of Functional Independence Measure-Motor at discharge. Main outcome measures The primary outcome was the Functional Independence Measure-Motor at discharge. Results In total, 569 participants (interquartile range 73-85years; 33.6% men) were included in the present study. A multiple linear regression analysis of Functional Independence Measure-Motor at discharge, adjusting for confounding factors, revealed that decreasing in potentially inappropriate medications use was independently correlated with Functional Independence Measure-Motor at discharge. In particular, the use of first-generation antihistamines, antipsychotics, benzodiazepines, and non-steroidal anti-inflammatory drugs among potentially inappropriate medications decreased significantly during hospitalization. Conclusion Decreased potentially inappropriate medications use during hospitalization may be a predictor of improvement of rehabilitation outcomes in geriatric patients.

Parental perception of efficacy of antihistamines for pruritus in pediatric atopic dermatitis

Clinicians have previously prescribed antihistamines for relief of atopic dermatitis (AD) associated pruritus. The use of antihistamines in AD has recently received less emphasis from newly published practice parameters that currently only recommend short-term, intermittent use of first-generation antihistamines to induce sleep in patients with AD. Our study aimed to determine parents' perception of the usefulness of antihistamines in reducing their child's itch due to AD. A 12-question survey was mailed to parents of patients who were attending a pediatric allergy clinic. Patients with physician-diagnosed AD who had a clinic visit in the past 3 years were included. Questions included the following: time since AD diagnosis, itching frequency, impact on sleep, frequency and relief provided from using antihistamines, and comparison of antihistamines to other antipruritus treatments. Sixty-three percent of parents surveyed responded that antihistamines were helpful in the management of their child's AD, and only 5% did not find any itch relief. The majority of the responders were parents of younger patients (ages, 2-10 years) with immunoglobulin E sensitization and AD for more than a year. Eighty-five parents (68.5%) reported no interruption of sleep due to itching, and, among them, an almost equal number were currently solely using either a first- or second-generation antihistamine. The more antihistamines were perceived as relieving itching, the more they were used (ρ = 0.209, p = 0.025) and provided more relief than other products (ρ = -0.336, p < 0.001). When compared, parents ranked antihistamines to be as helpful as topical corticosteroids. Parents of pediatric patients with AD found that antihistamines were an important part of AD management.

Anti-histamínicos no resfriado comum: Uma prescrição igualmente comum

ANTIHISTAMINES IN THE COMMON COLD: A COMMON PRESCRIPTON FOR A COMMON CONDITION Goals: Antihistamines are popular among doctors for treatment of symptoms of the common cold. The aim of this paper is to review the evidence for the effectiveness and safety of antihistamines as the sole treatment for symptoms of the common cold in children and adults. Data sources:Medline, evidence-based medicine internet sites, Index of Portuguese Medical Journals and references of selected articles. Review methods: Clinical guidelines, systematic reviews, and randomized controlled trials (RCT), published between January 1980 and October 2010 were collected using the MeSH terms: antihistamine and common cold. The Strength Of Recommendation Taxonomy (SORT) scale of the American Academy of Family Physicians was used for assigning levels of evidence and the strength of recommendation. Results: Seventy articles were found and seven were selected for this review. These include two guidelines on the management of the common cold that do not recommend antihistamines as a sole treatment option and one Cochrane meta-analysis that found no clinical benefit from the use of antihistamines alone. The results of some studies included suggested an increased risk of sedative effects with the use of first generation antihistamines. The authors of this meta-analysis recommend discontinuing the practice of prescribing these drugs in the common cold (level of evidence 1). Four RCT found that different antihistamines were no more effective than placebo in reducing acute cough. Three studies showed no significant differences in side effects (level of evidence 1). Conclusions: The evidence shows that the use of antihistamines as monotherapy in symptomatic treatment of the common cold is ineffective in children and adults (SOR A). Many trials suggest an increased risk of sedative effects with this therapy (SOR B). Sedation may be confused with prostration that would suggest a worsening of the clinical situation. This may add an unnecessary cost to a common prescription.

Atopic dermatitis.

Atopic dermatitis (AD) is a common, chronic skin disorder that can significantly impact the quality of life of affected individuals as well as their families. Although the pathogenesis of the disorder is not completely understood, it appears to result from the complex interplay between defects in skin barrier function, environmental and infectious agents, and immune abnormalities. There are no specific diagnostic tests for AD; therefore, the diagnosis is based on specific clinical criteria that take into account the patient’s history and clinical manifestations. Successful management of the disorder requires a multifaceted approach that involves education, optimal skin care practices, anti-inflammatory treatment with topical corticosteroids and/or topical calcineurin inhibitors (TCIs), the use of first-generation antihistamines to help manage sleep disturbances, and the treatment of skin infections. Systemic corticosteroids may also be used, but are generally reserved for the acute treatment of severe flare-ups. Topical corticosteroids are the first-line pharmacologic treatments for AD, and evidence suggests that these agents may also be beneficial for the prophylaxis of disease flare-ups. Although the prognosis for patients with AD is generally favourable, those patients with severe, widespread disease and concomitant atopic conditions, such as asthma and allergic rhinitis, are likely to experience poorer outcomes.

Potentially inappropriate prescribing (IP) for elderly medical inpatients in Taiwan: A hospital-based study

Older people tend to have multiple comorbid conditions and subsequent polypharmacy, which place them at higher risk of adverse drug events, drug–drug and drug–disease interactions and IP. IP includes several patterns, such as inappropriate dose or duration, prescribing drugs having significant drug–disease or drug–drug interactions, and the omission of potentially beneficial medications. The main purpose was to evaluate the prevalence of IP among medical inpatients in a medical center, so to evaluate the associative factors of IP in Taiwan. From January to December of 2009, all patients aged 65 years and older who were discharged from the medical wards of Taipei Veterans General Hospital were randomly sampled for study (the sampling rate around 1.0%). The IP was evaluated by the STOPP and START criteria. Each medical record was carefully reviewed by physicians who had been trained. Overall, 520 records of elderly medical ward inpatients (mean age=79.2±6.7 years, 73.8% males) were included for study. In total, 3455 items of medication were prescribed for these 520 patients (mean=6.6±3.2 items). According to STOPP criteria, 36.2% of the study subjects had at least one potentially inappropriate medication (PIM). The most common PIMs were: (1) medications that may adversely affect those who are prone to falls, e.g., benzodiazepines, neuroleptics and first generation antihistamines (14.2%). (2) Ca-channel blockers with chronic constipation (12.3%). (3) Use of neuroleptic agents (5.6%). (4) Long-term, long-acting benzodiazepines (2.5%). (5) Prolonged use of first generation antihistamines (2.1%). Besides, 218 patients (41.9%) had at least one potentially prescribing omission (PPO). Common PPOs included: (1) statin therapy in diabetes mellitus if coexisting major cardiovascular risk factors present (19.0%). (2) Antiplatelet therapy in diabetes mellitus with co-existing major cardiovascular risk factors (12.5%). (3) Metformin with type 2 diabetes with or without metabolic syndrome (in the absence of renal impairment) (8.7%). (4) Angiotensin converting enzyme inhibitor or angiotensin II receptor blockers with chronic heart failure (7.3%). (5) Aspirin or clopidogrel with a documented history of atherosclerotic coronary, cerebral or peripheral vascular disease in patients with sinus rhythm (7.1%). Logistic regression showed that older age and number of medications were significant risk factors for PIMs. In conclusion, the prevalence of PIMs among elderly medical inpatients in a medical center in Taiwan was 36.2% and PPOs was 41.9%. Further study is needed to clarify the underlying causes of potentially IP to promote better quality of prescribing for older patients.

The Economic Impact of Payer Policies after the Rx-to-OTC Switch of Second-Generation Antihistamines

Objective As a result of the over-the-counter (OTC) introduction of loratadine, health plans have been struggling to determine the best policy to incorporate this change within their existing drug benefit structure for second-generation antihistamines (SGA). The objective of this study was to examine the economic impact of payer policies in response to the Rx-to-OTC switch of loratadine. Study Design Decision analysis was used to model the budgetary impact and cost-effectiveness of four policies for SGA benefits for the managed care organization (MCO), employer, and Medicaid perspectives separately. Patients and Methods Outcomes included direct medical costs and lost productivity (employers only), discounted, quality-adjusted life-years (QALYs) saved because of amelioration of allergic rhinitis symptoms and avoidance of unintentional injuries associated with the use of first-generation antihistamines (FGA). Bayesian probabilistic sensitivity analysis was conducted using second-order Monte Carlo simulation. Results Providing limited OTC and second-tier prescription benefits would cost approximately $0.13 and $0.30 compared to third-tier prescription benefits for employers and MCOs, respectively, and would save Medicaid $.02 per member per month (PMPM). Providing limited coverage for OTC loratadine while retaining second-tier prescription benefits for SGA was the optimal policy for a willingness to pay below $26,200 per QALY for all payers. Conclusions Offering second-tier prescription and limited OTC benefits provides greater effectiveness and is not significantly more expensive PMPM than discontinuation. Some of the drug savings from limiting coverage of prescription SGA may be attenuated by the cost of lost productivity and direct medical expenditures due to unintentional injuries associated with increased FGA use in addition to the increased cost of therapeutic substitutes.

Transitioning the second-generation antihistamines to over-the-counter status: a cost-effectiveness analysis.

A U.S. Food and Drug Administration advisory committee deemed the second-generation antihistamines (SGA) safe for over-the-counter use against the preliminary opposition of the manufacturers. As a result, loratadine is now available over-the-counter. First-generation antihistamines (FGA) are associated with an increased risk of unintentional injuries, fatalities, and reduced productivity. Access to SGA over-the-counter could result in decreased use of FGA, thereby reducing deleterious outcomes. The societal impact of transitioning this class of medications from prescription to over-the-counter status has important policy implications. To examine the cost-effectiveness of transitioning SGA to over-the-counter status from a societal perspective. A simulation model of the decision to transition SGA to over-the-counter status was compared with retaining prescription-only status for a hypothetical cohort of individuals with allergic rhinitis in the United States. Estimates of costs and effectiveness were obtained from the medical literature and national surveys. Sensitivity analysis was performed using a second-order Monte Carlo simulation. Discounted, quality-adjusted life-years saved as a result of amelioration of allergic rhinitis symptoms and avoidance of motor vehicle, occupational, public and home injuries and fatalities; discounted direct and indirect costs. Availability of SGA over-the-counter was associated with annual savings of 4 billion dollars (2.4-5.3 billion dollars) or 100 dollars (64-137 dollars) per allergic rhinitis sufferer and 135,061 time-discounted quality-adjusted life years (84,913-191,802). The sensitivity analysis provides evidence in support of these results. Making SGA available over-the-counter is both cost-saving and more effective for society, largely as a result of reduced adverse outcomes associated with FGA-induced sedation. Further study is needed to determine the differential impact on specific vulnerable populations.

Acute and subchronic effects of levocetirizine and diphenhydramine on memory functioning, psychomotor performance, and mood

Background: Central nervous system adverse effects, such as sedation, often accompany the use of first-generation antihistamines. These effects might interfere with memory functioning and psychomotor performance. Levocetirizine was recently introduced as a new antihistamine said to be free from sedative effects. Objective: We sought to investigate the effects of levocetirizine (5 mg), diphenhydramine (50 mg), and placebo on memory and psychomotor performance after acute (day 1) and subchronic (day 4) daily administration in 48 healthy volunteers (24 men and 24 women). Methods: This study was a double-blind, placebo-controlled, randomized clinical trial. Treatments were administrated on days 1, 2, 3, and 4, 3 hours before the start of the laboratory test battery (performed on days 1 and 4), comprising a word-learning test, the Sternberg Memory Scanning Test, a tracking test (easy and hard version), and a divided attention test (tracking and memory scanning simultaneously). Statistical analyses were performed separately for days 1 and 4 by using analysis of variance. Results: On day 1, diphenhydramine significantly impaired tracking performance (easy: F1,90 = 25.9, P < .0001; hard: F1,90 = 20.5, P < .0001) and divided attention (tracking: F1,90 = 23.8, P < .0001; memory scanning: F1,90 = 22.0, P < .0001). Results on word-learning tests and Sternberg Memory Scanning Tests were not significantly impaired. On day 4, the effects of diphenhydramine did not reach significance. In contrast, on both days 1 and 4, levocetirizine did not significantly impair laboratory test performance. Conclusion: The results show that memory, attention, and tracking performance are unaffected after acute and subchronic administration of levocetirizine (5 mg), whereas diphenhydramine (50 mg) significantly affected divided attention and tracking after acute administration. (J Allergy Clin Immunol 2003;111:623-7.)

Use and safety of antihistamines in children

ABSTRACT: Although first-generation antihistamines remain popular for the treatment of seasonal allergic rhinitis, atopic dermatitis, and urticaria in children, second- and third-generation antihistamines hold clear advantages over the first-generation agents, especially for the pediatric patient. The less frequent dosing schedule of the second- and third-generation agents makes administration easier for the parent. With less sedation and lower risk of adverse effects, the safety profile of second- and third-generation agents appears superior to that of first-generation agents. After briefly discussing the use of first-generation antihistamines, the pharmacokinetics, safety, and use of the newer antihistamines loratadine, cetirizine, and fexofenadine in the pediatric patient are reviewed.

Do sedating H 1-antihistamines still have a role to play in the management of chronic idiopathic urticaria?

Summary At present, the mainstay therapy for chronic idiopathic urticaria remains second generation (“non sedating”) antihistamines. Efficacy, however, is not always sufficient to allow monotherapy, and therefore first generation (sedating) antihistamines are often used either alone or in combination with second generation antihistamines. The rationale for such therapy is, however, poorly investigated in clinically controlled trials. The only parameter favoring use of first generation antihistamines is their relatively low price, whereas their actions on other receptors (e.g. the muscarinic receptors) together with their sedative potential are major disadvantages in comparison with second generation antihistamines, where specific H1-blockade can be achieved and sedation can be avoided. In selected cases, the dose of second generation antihistamines may be increased in order to increase efficacy and in some cases the accompaning sedation is also used for therapy.

Reduction of the central nervous system adverse effects associated with antihistamines in the management of allergic disorders: Strategies and progress

To reduce the risks associated with the treatment of allergic disorders, physicians should understand the benefits and risks of drugs in the antihistamine class. The risk of central nervous system adverse effects associated with antihistamine use is significant with the use of first-generation antihistamines, which show pharmacologic activity in serotonergic, α-adrenergic, dopaminergic, and muscarinic-cholinergic pathways. Adverse effects reported with the use of first-generation antihistamines most often include drowsiness, fatigue, and an inability to concentrate; these effects may result in decreased compliance with therapy. The second-generation antihistamines have the property of low lipid solubility, which slows access across the blood–brain barrier. The low sedative profile of these new drugs may also be linked to a more pronounced binding to peripheral rather than brain histamine H1-receptors. The use of antihistamines with lower lipid solubility and greater specificity can provide an effective alternative for the relief of allergic symptoms, can improve compliance, and can reduce neurologic side effects. Because of the differences now recognized in the side effects of drugs of this class, an individualized approach to selection of antihistamine therapy is required. (J Allergy Clin Immunol 1996;98:S319-25.)