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PubMedDate not supplied

Safety of second generation antihistamines.

The sedation related to first-generation antihistamine use has been shown to compromise performance at school and at work, impair driving, and decrease the ability to handle tasks that require a high degree of alertness or concentration. Second-generation antihistamines are less likely to produce sedation. Loratadine, cetirizine, and fexofenadine are the most commonly prescribed second-generation antihistamines. Many tests have been conducted to assess the central effects of these three drugs. Compared with placebo, at recommended doses loratadine is not associated with performance impairment. Cetirizine, at recommended doses, has been shown to impair performance and cognition in several studies, although to a much lesser degree than older antihistamines. Clinical trials show fexofenadine is nonsedating, even at very high doses; psychomotor and driving tests reinforce these findings. Loratadine, cetrizine, and fexofenadine all have excellent safety records. Their cardiovascular safety has been demonstrated in drug-interaction studies, elevated-dose studies, and clinical trials. These three antihistamines have also been shown safe in special populations, including pediatric and elderly patients.

Aged↗

PubMedDate not supplied

Treatment of allergic rhinitis: effects of allergic rhinitis and antihistamines on performance.

Antihistamines are the most commonly used drugs for allergic rhinitis, and many antihistamines may cause subclinical side effects which are not noticeable by the patient. These include impaired driving performance, impaired work performance, reduced coordination, reduced motor skills, sleepiness and impaired information processing (arithmetic, verbal, and office skills). The newer nonsedating antihistamines should be used for the treatment of allergic rhinitis because they do not produce these effects. Recent studies have shown that children's learning in school may also be negatively affected by traditional antihistamines, and therefore, school children should definitely be given the nonsedating antihistamines. Not only does the treatment cause some impaired performance, but allergic rhinitis itself may result in changes in the patient's mood affect, and other aspects of personality. Physicians who treat allergic rhinitis should be aware of the potential performance effects of medications that they prescribe and the potential effects of the disease itself on the patient's personality.

Affect↗

PubMed1998

Treatment of allergic rhinitis: an evidence-based evaluation of nasal corticosteroids versus nonsedating antihistamines.

Allergic rhinitis is a high-cost, high-prevalence disease. In the 12 months ending March 31, 1997 $3.1 billion was spent in the United States for medications to manage this illness. Allergic rhinitis affects quality of life and interferes with work productivity. Nonsedating antihistamines are the most common and most expensive therapy for this condition. This study reviewed 13 randomized studies in which blinded investigators compared management of allergic rhinitis by means of intranasal steroids to management by means of nonsedating antihistamine. Evidence tables demonstrated that in all studies in which total nasal symptoms and nasal obstruction were recorded, the nasal steroid was statistically superior to the nonsedating antihistamine. For nasal blockage the nonsedating antihistamines did not perform better than placebo. For all other nasal symptoms the intranasal steroid was statistically superior in most reports and equal or numerically better in the remaining papers. When these data are linked to those from cost analysis and quality-of-life studies, the evidence strongly suggests that nasal steroids should be first-line therapy for allergic rhinitis. In four reports on the combination of a nonsedating antihistamine compared to a nasal steroid alone, there was no significant difference between these two treatments. Like asthma, allergic rhinitis is an inflammatory disease and should be managed with anti-inflammatory medication. Making such a change in the management of allergic rhinitis should increase efficacy and decrease costs.

Administration, Intranasal↗

PubMed2000

Efficacy of a steroid nasal spray compared with an antihistamine nasal spray in the treatment of perennial allergic rhinitis.

Allergic rhinitis is a common disease with a lifetime prevalence of 20% among the United States population. The cost of medication alone to manage allergic rhinitis in the United States was estimated to be $3.1 billion. The two most commonly prescribed classes of medications are antihistamines and topical nasal steroids. The data on comparing the efficacy of a commonly used antihistamine (azelastine hydrochloride) with that of topical steroids, however, are conflicting. Therefore, the reported study was undertaken to determine the efficacy of azelastine with that of a topical nasal steroid (flunisolide) in treating patients for the symptoms of perennial allergic rhinitis. Forty-four subjects were enrolled in a double-blind, placebo-controlled study using Balaam's design. In one group, patients were treated with topical nasal corticosteroids or placebo. In the other group, patients were treated with the antihistamine nasal spray or placebo. Subjective data were collected by the use of questionnaires and a daily diary, which focused on nasal symptoms, sleep, and daytime sleepiness. The results demonstrated that the topical nasal corticosteroid performed superiorly to the antihistamine nasal spray in improving sleep, daytime sleepiness, sneezing, ocular and nasal pruritus, and nasal congestion. Thus, the topical nasal corticosteroid was found to be more effective than antihistamine nasal spray in reducing symptoms of allergic rhinitis. This study provides further support for the use of topical nasal corticosteroids as first-line treatment for perennial allergic rhinitis.

Administration, Intranasal↗

PubMedDate not supplied

Impact of sedating antihistamines on safety and productivity.

The use of sedating antihistamines by allergy sufferers remains common, and physicians continue to prescribe these older antihistamines with great frequency. Precautionary statements warning of possible drowsiness and the need for caution when driving or operating machinery, which are required for sedating antihistamines, don't appear to be having much impact. Sedating antihistamines are frequently found to be a causal factor in fatal traffic accidents and are the leading medication found on autopsy of pilots who have crashed their aircraft. Patients taking sedating antihistamines frequently don't feel sleepy, yet they have difficulty staying awake and their brain functioning is impaired. The impact on safety is found in the increased risk of traumatic work-related injuries, driving accidents, and aviation fatalities. The cognitive and psychomotor deficits translate into losses in worker productivity and student learning.

Efficiency↗

PubMed2002

Histamine and antihistamines in anaphylaxis.

Anaphylaxis and anaphylactoid reactions are potentially fatal. These disorders are sometimes iatrogenic, and increase with increased exposure to drugs, synthetic substances, and medical procedures. Non-IgE-mediated anaphylactoid reactions are common in medical settings and are clinically indistinguishable from anaphylaxis. These reactions may be unrecognized if a rigid classic definition of anaphylaxis is used. Histamine is a primary mediator of anaphylaxis and signs and symptoms of anaphylaxis can be reproduced by histamine infusion. Histamine triggers a cascade of inflammatory mediators and modulates its own release. H1-antihistamines are adjunctive treatment therapy for acute anaphylaxis and anaphylactoid reactions, in which many mediators of inflammation are involved. Compared with epinephrine, the first-response medication of choice, antihistamines have a slow onset of action, and they cannot block events that occur subsequent to histamine binding to its receptors. Antihistamines are an important component of regimens for the prevention of anaphylaxis and anaphylactoid reactions in patients at risk, and may eventually have more widespread application in the perioperative setting. In some instances, such as with exercise-induced anaphylaxis and reactions to latex in sensitized individuals, prophylaxis regimens are not always effective. H2-antagonists are not detrimental in the therapy of anaphylaxis and many studies show a favorable outcome when combining H1- and H2-antagonist therapy for prophylaxis. They should be added to therapy at the discretion of the treating physician. Because of decreased antimuscarinic and central nervous system side effects, the newer antihistamines can be given in high doses, allowing more complete blockade of histamine receptors. These agents should lead to a reevaluation of the usefulness of antihistamines in both the treatment of acute anaphylaxis and in prophylactic regimens. The unavailability of parenterally administered second-generation H1-antagonists limits their usefulness in acute anaphylaxis and perioperative prophylaxis.

Anaphylaxis↗

PubMed1992

Nonsedating antihistamines: pharmacology, clinical efficacy and adverse effects.

Antihistamines are effective therapy for histamine-mediated conditions, including seasonal and perennial allergic rhinitis and chronic urticaria. Until recently, all antihistamines produced some degree of drowsiness, as well as anticholinergic side effects. Several nonsedating antihistamines have been developed. Two of these antihistamines--terfenadine and astemizole--are commercially available. The lack of central nervous system effects is attributed to the inability of these drugs to penetrate the blood-brain barrier. They also have no appreciable binding to cholinergic receptors. Clinical trials have demonstrated that the newer agents are as effective as classic antihistamines and that they have no greater incidence of central nervous system or anticholinergic side effects than placebo.

Astemizole↗

PubMed2005

A two-year course of specific immunotherapy or of continuous antihistamine treatment reverse eosinophilic inflammation in severe persistent allergic rhinitis.

Aim of the study was to evaluate the effect of a 2-year course of subcutaneous specific immunotherapy or continuous oral antihistamine treatment on the eosinophilic inflammation in nasal secretions of patients with severe persistent allergic rhinitis caused by house dust-mites. After informed consent, 31 rhinitis patients, sensitive to dust-mite antigens, were enrolled: 12 were randomly assigned to specific immunotherapy (group A), 11 to continuous oral antihistamine (cetirizine) treatment (group B), and 8 to an oral antihistamine (cetirizine) on demand (group C). Nasal scrapings were performed with a cotton-tipped swab and cells counted before and after 24 months of therapy. Intercellular adhesion molecule-1 and eosinophil cationic protein expression in cytological smears were assessed by immuno-histochemistry. All patients completed the study. The percentage of inflammatory cell types was comparable in the 3 groups at the beginning of the study. Eosinophils, identified as cells expressing eosinophil cationic protein, significantly decreased dropping to zero after 2 years of treatment in groups A and B, while no change was observed in group C. Expression of intercellular adhesion molecule-1 also decreased significantly in groups A and B, but not in group C. This decrease was associated with a significant reduction in epithelial shedding. In the 2-year period studied, specific subcutaneous immunotherapy and continuous oral antihistamine treatment were found to be effective in reducing eosinophilic infiltration and adhesion molecule expression in the nasal mucosa of patients with persistent allergic rhinitis. Furthermore, immunotherapy was more effective in controlling epithelial disruption while antihistamines appeared to be more active in controlling nasal inflammation. Both treatments induced a significant decrease in intercellular adhesion molecule-1 expression in epithelial cells and also a dramatic reduction of eosinophil cationic protein positive staining. These parameters can be considered useful means for controlling the state of persistent inflammation which is typical of persistent respiratory allergy. Nasal scraping was demonstrated to be a simple and safe procedure for monitoring some nasal inflammation parameters.

Administration, Oral↗

PubMed2006

[Comparison of clinical efficacy and cost-quality of antihistamines in early treatment for Japanese cedar pollinosis].

BACKGROUND: Japanese cedar pollinosis (JCP) affects more than 16% of the Japanese population. The estimated direct and indirect costs for this disease totaled 286 billion yen in 1998. In JCP therapy, antihistamines are first line agents. It is well known that starting treatment for JCP with antihistamines before initial day of the pollen scattering can relieve nasal symptom severity during pollen season. The aim of this study is to assess the clinical efficacy and cost-quality of 7 major second-generation antihistamines in early treatment for Japanese cedar pollinosis (JCP). METHODS: Patients were randomly selected from 16 ENT clinical sites in Osaka and Wakayama between February 24 and March 8, 2003 (peak pollen season). Effectiveness was assessed using patient'ratings of nasal and ocular symptoms and overall assessment in their condition compared to previous season ones. Costs include direct costs of the drugs used for treatment to JCP from January to March. RESULTS: One hundred seventy-five patients who were treated with antihistamine monotherapy (azelastine: n=15, cetirizine: n=15, ebastine: n=36, epinastine: n=16, fexofenadine: n=16, loratadine: n=60, oxatomide: n=17) and 510 non-treatment patients were evaluated. Among 8 groups, there were significant differences in sneezing, rhinorrhea, ocular itching and overall health condition. However, among 7 monotherapy groups, there were no differences in each symptom or the overall assessment. In cost-quality analysis, there were significant differences in a cost for each effective patient (defined as those with improvement in their overall condition) among 7 drugs. The top three cost-efficacious drugs resulted in azelastine, loratadine and fexofenadine. CONCLUSION: These results show that there were no significant differences in clinical efficacy in early treatment for JCP among 7 antihistamines. But Japanese National Health Insurance drug price scheme led to significant differences in cost-quality.

Adolescent↗

PubMed1991

Antihistamine update.

Antihistamines are a diverse group of drugs, each possessing the ability to inhibit various actions of histamine. Because they act principally through competitive inhibition of the histamine receptor, they are helpful as a means of preventing rather than reversing these actions. As a result of a resurgence of interest in antihistamine therapy during the past decade, a new class of H1 blockers, clinically devoid of sedative and anticholinergic effects, has evolved. Thus, the choice of antihistamine can now be based on the side effects profile as well as the clinical profile. As we continue to develop a better understanding of these newer agents, we will be able to select more rationally the antihistaminic agent most appropriate to the specific disorder. Used judiciously, the antihistamines available today have a broad application of therapeutic uses, with few significant side effects.

Drug Interactions↗

PubMed1978

Discriminable effects of antihistamine drugs.

Rats were trained to discriminate drug vs. no-drug in a shock-escape T-maze task; a right turn was required when rats were drugged and a left turn when undrugged. The three antihistamine drugs pyrilamine, dimenhydrinate (Dramamine) and diphenhydramine (Benadryl) were discriminated after an average of 20 training sessions indicating that their effects were only moderately discriminable. After criterion performance was achieved under the training conditions, substitution tests were conducted during which rats received a novel drug and were then run in the maze with both goals accessible. Rats trained with antihistamine drugs made drug choices during tests with other antihistamines. Rats trained with other types of drugs made no-drug choices during tests with antihistamines. The results suggest that the antihistamines share a discriminable effect which is relatively unique to that class of drugs.

Animals↗

PubMed1981

Combined H1 and H2 antihistamine therapy in chronic urticaria.

Chronic urticaria is a frustrating problem for the patient and the physician. The cause is usually undetermined, and the therapy is directed toward controlling symptoms. Recent evidence that human skin blood vessels possess H2 receptors, as well as the commonly recognized H1 receptors, suggests a possible reason for the frequent failure of H1 antihistamines in controlling this disorder. Eighteen patients with refractory chronic idiopathic urticaria participated in a double-blind, cross-over study to evaluate the efficacy of combined H1 (hydroxyzine hydrochloride) and H2 (cimetidine) antihistamines vs H1 antihistamines alone. This study indicates that combined H1 and H2 antihistamine therapy is statistically more effective than H1 antihistamines alone in controlling the symptoms of chronic urticaria.

Adult↗

PubMed1981

Effects of antihistaminic drugs in tests for antidepressant action.

Antihistaminics of various chemical structures: chlorcyclizine, chloropyramine, chlorpheniramine, clemastine, diphenhydramine, mepyramine, promethazine, and thenalidine were investigated for the action in tests for antidepressant drugs. The antihistaminics did not affect significantly the spontaneous locomotor activity of rats. Most of them (chloropyramine, chlorpheniramine, diphenhydramine, promethazine and thenalidine) increased amphetamine hypermotility but chlorcyclizine significantly inhibited, and clemastine and mepyramine did not affect it. In mice, chlorcyclizine, mepyramine and promethazine inhibited amphetamine hypermotility, while others antihistaminics were without effect. L-DOPA-induced hypermotility in mice was inhibited by all compounds tested. With the exception of chlorpheniramine and mepyramine, all tested antihistaminics produced hypothermia in mice, although fife of them (chlorpheniramine, diphenhydramine, chlorcyclizine, chloropyramine and thenalidine) antagonized the reserpine-induced hypothermia. With the exception of mepyramine and clemastine, the compounds tested shortened the period of immobility of rats in the behavioral despair test. The results indicate that only few antihistaminics have pharmacological profile resembling tricyclic or atypical antidepressant drugs.

Amphetamine↗

PubMed1993

Nonsedating H1 antihistamines in chronic urticaria.

Histamine type 1 (H1) receptor antagonists are the principal therapy for chronic urticaria. Their usefulness, however, is sometimes compromised by undesirable central nervous system (CNS) side effects such as daytime sedation and anticholinergic side effects such as dry mouth. Second-generation, nonsedating antihistamines (terfenadine, astemizole, loratadine, and cetirizine hydrochloride) are just as effective as the potent first-generation antihistamines such as hydroxyzine. Yet they do not cause the CNS and anticholinergic side effects seen with the older agents. Cardiovascular side effects, which have been recently reported with terfenadine and astemizole, are dose related and rare, generally occurring in patients who overdose or who take concomitant medications that increase serum antihistamine levels. The second-generation antihistamines also offer twice daily and once daily dosage schedules, which are more convenient than the two- to four-times daily schedules of the older agents. They should therefore be considered first-line agents for the treatment of chronic urticaria. This article is a review of the role of the nonsedating antihistamines in the treatment of chronic urticaria.

Central Nervous System↗

PubMed1994

[Second generation non-sedative antihistaminics].

In the 1980's a new group of antihistamines was developed, which has got, besides its increased efficiency, fewer by effects. Considering their pharmacokinetic characteristics and effects, the requirements the modern second generation antihistamine should meet, can be summarized as follows: the modern antihistamine should be selective, peripheral H1 receptor antagonist, should have a low affinity to the H1 receptors of the brain, be void of antikolinerg and antiserotonin effect, should stabilize the membrane of the mastocytes and/or have an impeding effect on eosinophil accommodation. The introduction of modern, second generation antihistamines was started by terfenadin in 1985, and was followed by astemizole, loratadine and cetirizine in 1988. The author gives a thorough survey of the pharmacokinetic characteristics of the second generation antihistamines and their clinical importance.

Histamine H1 Antagonists↗

PubMed1997

Distribution of antihistamines into the CSF following intranasal delivery.

The preferential absorption of certain drug compounds from the nasal cavity into the cerebrospinal fluid (CSF) raises questions regarding the transport processes controlling drug disposition following intranasal delivery. The disposition characteristics of several structurally similar antihistamine compounds, hydroxyzine, chlorpheniramine, triprolidine, and chlorcyclizine, into the CSF following nasal administration were studied using the rat as an animal model. The antihistamines were administered either intranasally or intra-arterially, and serial CSF and plasma samples were collected from the cisterna magna and the femoral artery, respectively. The drug levels in CSF and plasma were assayed by HPLC. Hydroxyzine concentrations in plasma and CSF were found to be significantly greater than most of the other compounds tested. In addition, hydroxyzine also showed the most rapid systemic absorption following nasal administration. Interestingly, the hydroxyzine levels in CSF following intranasal administration were significantly higher than those following intra-arterial administration. The AUC ratios between CSF and plasma for hydroxyzine after intranasal and intra-arterial administration were 4.0 and 0.4, respectively. The AUC ratios for triprolidine, the other antihistamine with measurable CSF concentrations, were 0.5 and 0.7, respectively. The distribution of antihistamines from the nasal membrane into the CSF appears to be controlled by a combination of their molecular properties. It also appears that the intranasal delivery of drugs with optimal physicochemical characteristics can result in an improved CNS bioavailability compared to those achieved from an equivalent parenteral dose.

Administration, Intranasal↗

PubMed2000

Sedation and antihistamines: a review of inter-drug differences using proportional impairment ratios.

The use of antihistamines (AHs) has until recently been associated with a number of undesirable side effects, the most troublesome of which is sedation. There are two aspects to sedation. The first, an objectively determined measure based on the results of psychometric tests from controlled trials, and the second, the subject's response to the administration of a drug. Since AHs are largely used in ambulant patients, a complete evaluation of sedation should be performed through standardised objective and subjective tests, shown to be sensitive to the central effects of AHs.An extensive review of the literature identified 76 studies of H(1) receptor antagonists in healthy volunteers, in which assessment of sedation was the primary objective. Results from studies published in peer-reviewed journals which employed a placebo condition as well as a positive internal control using a crossover design were analysed to determine the extent to which a particular antihistamine produced impairments on a battery of psychometric tests. The impairment index for each antihistamine was calculated and subsequently compared with the impairment index obtained for all other AHs.The calculation of this proportional impairment ratio enabled the sedative potential of an individual antihistamine to be identified relative to all other AHs and thus allowed the ranking of AHs with respect to their ability to cause impairments of cognitive and psychomotor function.Findings from this review clearly demonstrate that there are distinct classes of AHs with respect to their ability to impair cognitive function and psychomotor performance. Copyright 2000 John Wiley & Sons, Ltd.

Journal Article↗

PubMedDate not supplied

Quantitative relationships between the structure of beta-adrenolytic and antihistamine drugs and their retention on an alpha 1-acid glycoprotein HPLC column.

Chromatographic retention parameters of a series of 7 beta-adrenolytics and of 12 antihistamine drugs were determined employing an alpha 1-acid glycoprotein (AGP) high-performance liquid chromatographic (HPLC) column. For the group of antihistamines capillary electrophoretic (CE) retention was additionally measured in the presence of either AGP or human serum albumin (HSA). Two series of solutes hydrophobicity parameters were obtained by reversed-phase HPLC on an immobilized artificial membrane (IAM) column. The solutes studied were subjected to molecular modelling and the structural descriptors obtained were applied in studies of quantitative structure-retention (protein binding) relationships (QSRR). It was found that retention on AGP correlates well with the literature on physiological protein binding data. This retention was demonstrated to depend on hydrophobicity: to a lesser extent in the case of beta-adrenolytics and strongly in the case of antihistamines. Hydrophobicity, along with molecular width and electron excess charge on aliphatic nitrogen was demonstrated to describe retention of antihistamines on AGP. The AGP column is recommended as a convenient reactor for studies of drug-protein interactions. Preliminary CE data do not correlate with the HPLC data.

Adrenergic beta-Antagonists↗