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Antihistamines in asthma.

Reports in the literature have suggested that antihistamines are contraindicated in asthma because they dry the secretions in the upper and lower respiratory tracts. However, the consensus is that this is not the case. There may be a subset of asthmatics who report wheezing and a feeling of tightness in the chest after taking antihistamines but most of those who have severe perennial allergic rhinitis do not have adverse reactions and indeed benefit considerably from antihistamines.

Asthma↗

P's and blues: potentiation of propoxyphene withdrawal by a variety of antihistamines.

Three cases are presented of patients who experienced potentiation of propoxyphene's effects by different antihistamines. These included increased analgesia and mild euphoria as well as moderately severe symptoms of opiate withdrawal at therapeutic doses of propoxyphene. In one case, withdrawal symptoms were blocked with clonidine, an alpha-2 agonist. Since the specific antihistamine-opiate combination, pentazocine and tripelennamine, is associated with increased lethality, physicians are cautioned to avoid combining propoxyphene with antihistamines.

Adolescent↗

Appropriate use of second-generation antihistamines.

Antihistamines, one of the most frequently used groups of medications in the United States, are primarily used in treating allergic rhinitis and urticaria and also anaphylactic reactions, pruritus, and symptoms of anxiety. Second-generation antihistamines are safe and effective for treating allergic conditions. Control of nasal congestion may require additional medication. Further studies will determine if second-generation antihistamines can be used for other medical conditions.

Anti-Allergic Agents↗

Evaluation of the optimal oral antihistamine for patients with allergic rhinitis.

Because of its bothersome symptoms, allergic rhinitis (AR) is 1 of the top 10 reasons for patient visits to primary care physicians. This highly prevalent disease also results in loss of productivity, both at work and in school. Oral antihistamines are one of the most frequently prescribed medications for the management of AR and, with several agents available, it is important to discern the specific benefits and detriments of each. To assess the differences in efficacy and safety factors among antihistamines, the Individual therapeutic window of each agent can be used as a comparative reference tool because it defines the dose range over which an antihistamine is efficacious and free of adverse effects. As such, the therapeutic window includes both undesired effects, such as sedation, and desired properties, such as rapid onset of action, long duration of efficacy, broad age range of applicability, and potential to Improve quality of life. Therefore, agents with broad therapeutic windows, based on both efficacy and safety, are expected to be more favorable; this therapeutic window should be understood by the primary care physician when prescribing a medication.

Administration, Oral↗

Plasma serotonin and histamine levels in hemodialysis-related pruritus are not significantly influenced by 5-HT3 receptor blocker and antihistaminic therapy.

BACKGROUND: Elevated plasma histamine levels are considered to play a part in the pathophysiology of hemodialysis-related pruritus. However, antihistaminic therapy often fails to provide sufficient relief. Elevated serotonin levels in patients on dialysis therapy have also been described but the effects of 5-HT3 receptor antagonists on hemodialysis-related pruritus remain controversial. METHODS: we conducted a study to determine plasma histamine and serotonin levels before and after treatment with 5-HT3 receptor antagonists (tropisetron 5 mg and ondansetron 8 mg) and an antihistamine (cetirizine 10 mg). Eleven hemodialysis patients with a history of pruritus participated in this study,10 healthy volunteers served as control group. RESULTS: Histamine and serotonin values were normal in patients and controls. Treatment with cetirizine did not significantly reduce histamine levels in patients or in controls. Tropisetron and ondansetron likewise did not alter serotonin levels in patients. Tropisetron treatment did not significantly change serotonin levels in controls. CONCLUSION: Histamine and serotonin are no major mediators of pruritus in hemodialysis patients. Elevated histamine levels are occassionally seen and may be due to the increased mast cell number found in a subgroup of hemodialysis patients. Our findings explain the only marginal relief of antihistamines and the controversial antipruritic effect of serotonin receptor antagonists in hemodialysis-related pruritus.

Adult↗

The effect of education and drug samples on antihistamine prescribing costs in an HMO.

OBJECTIVE: To examine the effect of an intervention designed to reduce antihistamine prescribing costs in an HMO. DESIGN: A quasi-experimental design with clinicians at one HMO site receiving an intervention. Their prescribing behavior before and after the intervention was compared to the prescribing behavior of clinicians at other HMO sites in a non-randomized control group. SETTING: A mixed model HMO in metropolitan Washington, DC. PARTICIPANTS: Group model clinicians at a single site received the intervention; network and group model clinicians at other sites composed the control group. INTERVENTION: An education memo addressed to clinicians discussing antihistamine prescribing costs and strategies for initial use of nonprescription or less expensive prescription agents, coupled with free antihistamine sample "trial packs" for patient use. OUTCOME MEASURE: The prescribing costs of the intervention group were compared to the prescribing costs of the non-randomized control group. The intervention group was surveyed regarding their attitudes toward the intervention. RESULTS: A 2% decline in costs was noted between the baseline and intervention year for both the intervention and control groups. Though clinicians indicated they were well disposed toward the intervention, they believe patient expectations were a major obstacle to the use of cheaper agents. CONCLUSION: We conclude that an effective intervention would require the targeting of major patient-related barriers to clinician behavior change.

Adult↗

[Second generation topical antihistaminics].

The article presents two topical antihistaminics: levocabastine and azelastine. Most attention is paid to discussing the pharmacokinetics and antihistamine, antiallergic and antiinflammatory activities of these drugs. Their clinical usefulness in allergic rhinitis and conjunctivitis is also presented. Finally the authors describe the adverse reaction observed after administrating of topical antihistaminics.

Administration, Topical↗

Non-H1-receptor effects of antihistamines.

Visit any international allergy meeting and you will soon learn that there are a plethora of very potent and effective histamine H1-receptor antagonists, or antihistamines as they are more often called. Thus, in order to make any particular antihistamine stand out therapeutically or commercially from the others, additional properties, e.g. anti-inflammatory properties, are often claimed. But are these claims valid and, if so, are the 'additional properties' clinically relevant? This document will review the evidence behind some of the 'additional properties' of antihistamines and lay the basis for discussion of their relevance.

Animals↗

Antihistamines and serum adhesion molecule levels.

BACKGROUND: Some antihistamines are capable of inducing decreased expression of adhesion molecules in nasal and conjunctival tissues of allergic rhinoconjunctivitis patients. This study aimed to determine if one month of therapy with loratadine 10 mg once daily would also induce any decrease in serum levels of soluble ICAM-1 (sICAM-1) or VCAM-1 (sVCAM-1). MATERIAL AND METHODS: 40 monosensitized House Dust Mite (HDM) mild-to-moderate allergic rhinitis patients were included in the study. During the study, twenty patients randomly received 10 mg loratadine daily, the other twenty did not take any antihistamine. All patients were treated with nasal budesonide daily and sodium cromoglycate nasal spray when needed. Serum soluble ICAM-1 and VCAM-1 levels were determined by immunoenzimatic assay before and in the end of the study period. RESULTS: After one month of loratadine sVCAM-1 levels had a significant decrease (from 724.8 to 625 ng/ml) while sICAM-1 levels had a slight but not significant increase. Control patients did not have significant variations in sVCAM-1 or sICAM-1 serum levels. During regular antihistamine therapy patients improved their clinical scores. CONCLUSIONS: Loratadine 10 mg daily during one month induced a decrease in sVCAM-1 but not in sICAM-1 levels in HDM allergic rhinitis patients.

Animals↗

Pharmacology and therapeutic use of antihistamines.

The classes of antihistaminic agents, their pharmacology and therapeutic uses, adverse effects, drug interactions, toxic overdoses and abuse are reviewed. It is concluded that antihistamines are valuable drugs for treating a number of conditions and diseases (e.g. allergic rhinitis, motion sickness and parkinsonism), but proof of efficacy has not been established for the treatment of cardiac arrhythmias, peptic ulcers, insomnia and headaches. Because responses to antihistamines may vary, titration of each patient's dose is recommended.

Amines↗

Antihistamines in rhinoconjunctivitis.

In allergic rhinoconjunctivitis, histamine is known to contribute predominantly to nasal itch, sneeze, rhinorrhea, conjunctival itch, and lacrimation and these symptoms benefit most from H1-antihistamine therapy. The discovery in the early 1980s of nonsedating H1-receptor antagonists contributed dramatically to the more widespread acceptance of this mode of therapy. This also led to the undertaking of well-designed clinical trials that have added significantly to our understanding of allergic rhinitis. Oral treatment modifies both nasal and ocular symptoms and provides effective control throughout a 24-h period with once- or twice-daily medication. The advent of topical H1-receptor antagonists offers a wider choice of treatments and provides equal or greater efficacy with lower systemic bioavailability. While having a major impact on rhinoconjunctivitis symptoms, H1-antihistamines do not fully modify disease since histamine is not the only contributor to symptom generation in allergic rhinoconjunctivitis. While the search for oral H1-antihistamines with more widespread "antiallergic" activity continues, the currently available medications modify predominantly histamine-regulated events despite in vitro evidence of greater potential. The development of these new medications may be the next significant advance in this mode of treatment.

Animals↗

[The place of new antihistamines in allergy management. Apropos of desloratadine].

Desloratadine, the active metabolite of loratadine, is a new antihistamine. Because of its anti allergy properties, desloratidine has an affinity for histamine receptors 25 to 100 times greater to those of the usual antihistamines, coupled with a capacity to inhibit the production of pro-inflammatory mediators. When evaluated in healthy volunteers, the half life of desloratadine has been estimated at 27 hours, which is comparable with a night time length of action. Many clinical studies made with patients suffering with allergic rhinitis or chronic idiopathic urticaria have shown a rapid symptom reduction, lasting 24 hours after first taking. This action was correlated with an improvement in socio-professional activity, sleep and quality of life in general. In patients suffering from allergic rhinitis, rhinomanometry showed a significant improvement in nasal congestion by desloratadine. The clinical advantages of desloratadine on antihistamines taken previously were measured in a study made on almost 48,000 patients, of whom 91% found its efficacity satisfactory. By its powerful action, coupled with an excellent tolerance profile, desloratadine represents a real therapeutic advance for allergic patients.

Anti-Allergic Agents↗

Histamine and the classic antihistamines.

The first steps leading to the recognition of histamine's biological activity were taken in 1907. The existence of histamine in the body was finally recognized by 1910, and many researchers were keen to establish its physiological role, especially with regard to clinical shock and hypersensitivity reactions. The Pasteur Institute succeeded in finding a drug that would act as a biochemical tool to block the actions of histamine in the body and thereby reveal more about its physiological role, but none of its compounds was potent or safe enough to use in humans. Developments over the following years were made in producing compounds safe enough for clinical application in the treatment of allergies, and variations in these early antihistamines led to other uses. The first of the ethanolamine-based antihistamines marketed in the 1940s were used as antiallergy drugs, motion sickness remedies and antiemetics. The problem of drowsiness induced by antihistamines was overcome by the 1980s with drugs such as terfenadine and acrivastine.

Journal Article↗

[Treatment of chronic idiopathic urticaria unresponsive to type 1 antihistamines in monotherapy].

The chronic idiopathic urticaria treatment is a difficult and often frustrating problem for physicians. Due to the lack of definitive medical therapeutic programs to relieve the symptoms and prevent from their recurrence, several pharmacologic approaches to the management of chronic idiopathic urticaria are proposed. The chronic urticaria pharmacologic therapy is therefore fit to abrogate effects of histamine and other mediators on cutaneous vasculature and inflammatory cells that participate in the pathogenesis of the urticaria. The most common approach is to avoid all aggravating factors and to block histamine. The mainstay therapy is the H1 antihistamines. A significant number of patients may remain unresponsive even after an increase in the dose or a change in the type of H1 antihistaminic drug. In these cases, several therapies can be associated: combinations of H1 antihistamines, nonsedating one tablet (morning) and one sedating (evening), this approach is very usual but no study has confirmed it rational; addition an H2 antagonist to the previous treatment for some patients may improve control of their symptoms; alternatively, the tricyclic antidepressant, Doxepin is usually prescribed. The results of other drugs reported in the literature is unpredictable, to include them in a strategy therapy. The results with Badrenergic agents, nifedipine, ketotifen, leukotriene antagonists and tranexamic acid are variable and don't appear better than those with H1 antagonists. The efficiency of danazol has to be confirmed by other controlled studies. Warfarin, sulfasalazine and ultraviolet radiation have been used apparently successfully, but no controlled study has been published. Only when the above treatments have failed then immunosuppresive therapies, intravenous immunoglobulin and plasmapheresis can be proposed for chronic idiopathic urticaria.

Adrenergic beta-Agonists↗

Central nervous system side-effects of antihistamines in schoolchildren.

There are no studies available in the literature on the effects of classical antihistamines on the central nervous system (CNS) in children. Clinical studies indicate that somnolence occurs more often with classical antihistamines than with placebo. There is no difference in inducing somnolence in children between placebo and astemizole or terfenadine, two new antihistamines that have thoroughly been shown to have no sedative effect greater than placebo in adults. A double-blind, cross-over trial investigating the CNS-effects of astemizole and chlorpheniramine in schoolchildren failed to show a negative effect of either of these drugs on performance.

Astemizole↗

A comparison of new nonsedating and classical antihistamines in the treatment of primary acquired cold urticaria (ACU).

The efficacy of the new nonsedating antihistamines loratadine and cetirizine was compared in a randomized, single-blind, crossover, controlled study with that of the classical antihistamines cyproheptadine and ketotifen in seven patients with primary acquired cold urticaria (ACU). The patients received each of the four drugs for 14 consecutive days with a 7-day interval between drugs. We evaluated clinical symptomatology, adverse effects, minimum time of cold contact stimulation required to induce an immediate coalescent wheal (CSTT), and inhibition of histamine-induced wheal response. Both loratadine and cetirizine showed suppression of symptoms with infrequent adverse effects. Important side-effects were observed in patients receiving cyproheptadine. Improvement in CSTT was statistically significant for all drugs compared with baseline values, without differences among them. The histamine-induced skin test was significantly inhibited by all antihistamines. Wheal reductions were 34.6% for loratadine and 50.9% for cetirizine. This study suggests that both loratadine and cetirizine may be effective in the treatment of primary ACU.

Adult↗

[Clinical aspects of anti-inflammatory action of antihistamines].

Antihistamines are accepted in the therapy of allergic seasonal and perennial rhinitis. In the paper some anti-inflammatory effects of antihistamines have been presented, and their action mechanisms and clinical applications have been discussed in relation to the new preparates of antihistamines.

Cetirizine↗

Studies of the "antihistaminic" effect of pyribenzamine administered by various routes.

Utilizing histamine electrophoresis, the degree and duration of "antihistaminic" effect of varying doses of Pyribenzamine(R) administered by different routes were studied. Delayed action Pyribenzamine in 50 mg. and 100 mg. dosage exerted a small but measurable anti-whealing effect five hours after ingestion. The larger dose exerted approximately twice the effect of the smaller. The anti-whealing activity lasted five to six hours. Pyribenzamine given intravenously affected the whealing response one hour after administration. A peak of activity was reached two to two and a half hours after injection, and "antihistaminic" effect continued for a total of five hours. The inunction of 250 mg. and 500 mg. of Pyribenzamine in an ointment base resulted in sufficient absorption of the drug to produce a measurable anti-whealing effect. The "antihistaminic" activity was noted three hours after application and lasted 10 to 12 hours from the time of inunction.

Histamine↗