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Sample records for antihistaminics

  1. Antihistaminic

    African Journals Online (AJOL)

    antihistaminic and sedative-hypnotic activities. The animals were maintained in colony cages at. 25 ± 2 oC, relative humidity of 45 – 55 %, under a. 12 h light and dark cycle; they were fed standard animal feed. All the animals were acclimatized for a week before use [18]. The experimental protocol was duly approved by the ...

  2. Antihistamines.

    Science.gov (United States)

    Church, Martin K; Maurer, Marcus

    2014-01-01

    The discovery of histamine, its physiological role and reversal of its pharmacological effects by antihistamines takes us on a journey through the origins of modern physiology and the rising understanding of pharmacology at the end of the 19th and the early part of the 20th centuries. This journey, which has been traced in the excellent historical review by Michael Emanuel [Clin Exp Allergy 1999;29:1-11], is populated by some of the greatest scientists of the era, including six Nobel laureates - Bovet, Dale, Ehrlich, Richet, Windaus and Black. In addition, it laid the basis of medicinal chemistry not only for antihistamines, but also for the discovery of a plethora of drugs still in use today. © 2014 S. Karger AG, Basel.

  3. Antihistamine use in children.

    Science.gov (United States)

    Fitzsimons, Roisin; van der Poel, Lauri-Ann; Thornhill, William; du Toit, George; Shah, Neil; Brough, Helen A

    2015-06-01

    This review provides an overview of the use of antihistamines in children. We discuss types of histamine receptors and their mechanism of action, absorption, onset and duration of action of first-generation and second-generation H(1)-antihistamines, as well as elimination of H(1)-antihistamines which has important implications for dosing in children. The rationale for the use of H(1)-antihistamines is explored for the relief of histamine-mediated symptoms in a variety of allergic conditions including: non-anaphylactic allergic reactions, atopic eczema (AE), allergic rhinitis (AR) and conjunctivitis, chronic spontaneous urticaria (CSU) and whether they have a role in the management of intermittent and chronic cough, anaphylaxis, food protein-induced gastrointestinal allergy and asthma prevention. Second-generation H(1)-antihistamines are preferable to first-generation H(1)-antihistamines in the management of non-anaphylactic allergic reactions, AR, AE and CSU due to: their better safety profile, including minimal cognitive and antimuscarinic side effects and a longer duration of action. We offer some guidance as to the choices of H(1)-antihistamines available currently and their use in specific clinical settings. H(1)-antihistamine class, availability, licensing, age and dosing administration, recommended indications in allergic conditions and modalities of delivery for the 12 more commonly used H(1)-antihistamines in children are also tabulated. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://group.bmj.com/group/rights-licensing/permissions.

  4. Antihistamines for allergies

    Science.gov (United States)

    ... sharing features on this page, please enable JavaScript. Antihistamines are drugs that treat allergy symptoms . When taken by mouth, ... heat, direct light, and moisture. DO NOT freeze antihistamines. Keep all medicines where children cannot reach them. Side Effects of ...

  5. Pharmacology of antihistamines

    Directory of Open Access Journals (Sweden)

    Martin K Church

    2013-01-01

    Full Text Available H 1- antihistamines, the mainstay of treatment for urticaria, were developed from anticholinergic drugs more than 70 years ago. They act as inverse agonists rather than antagonists of histamine H 1 -receptors which are members of the G-protein family. The older first generation H 1- antihistamines penetrate readily into the brain to cause sedation, drowsiness, fatigue and impaired concentration and memory causing detrimental effects on learning and examination performance in children and on impairment of the ability of adults to work and drive. Their use should be discouraged. The newer second-generation H 1 -antihistamines are safer, cause less sedation and are more efficacious. Three drugs widely used for symptomatic relief in urticaria, desloratadine, levocetirizine and fexofenadine are highlighted in this review. Of these levocetirizine and fexofenadine are the most potent in humans in vivo. However, levocetirizine may cause somnolence in susceptible individuals, whereas fexofenadine has a relatively short duration of action and may be required to be given twice daily for all round daily protection. Although desloratadine is less potent, it has the advantages of rarely causing somnolence and having a long duration of action.

  6. Antihistamines, Decongestants, and Cold Remedies

    Science.gov (United States)

    ... suffers with an allergic attack or an infection. Antihistamine drugs block the action of histamine, therefore reducing these ... could take them together, increasing the dosage of antihistamine at night (while ... the same as another to drug side effects, you may wish to adjust the ...

  7. Antihistamines and itch.

    Science.gov (United States)

    Thurmond, Robin L; Kazerouni, Kayvan; Chaplan, Sandra R; Greenspan, Andrew J

    2015-01-01

    Histamine is one of the best-characterized pruritogens in humans. It is known to play a role in pruritus associated with urticaria as well as ocular and nasal allergic reactions. Histamine mediates its effect via four receptors. Antihistamines that block the activation of the histamine H₁receptor, H₁R, have been shown to be effective therapeutics for the treatment of pruritus associated with urticaria, allergic rhinitis, and allergic conjunctivitis. However, their efficacy in other pruritic diseases such as atopic dermatitis and psoriasis is limited. The other histamine receptors may also play a role in pruritus, with the exception of the histamine H₂receptor, H₂R. Preclinical evidence indicates that local antagonism of the histamine H₃receptor, H₃R, can induce scratching perhaps via blocking inhibitory neuronal signals. The histamine H₄receptor, H₄R, has received a significant amount of attention as to its role in mediating pruritic signals. Indeed, it has now been shown that a selective H₄R antagonist can inhibit histamine-induced itch in humans. This clinical result, in conjunction with efficacy in various preclinical pruritus models, points to the therapeutic potential of H₄R antagonists for the treatment of pruritus not controlled by antihistamines that target the H₁R.

  8. Allergy, Histamine and Antihistamines.

    Science.gov (United States)

    Church, Martin K

    2017-01-01

    This chapter concentrates on the role in allergic disease of histamine acting on H 1 -receptors. It is clear that allergy has its roots in the primary parasite rejection response in which mast cell-derived histamine creates an immediate hostile environment and eosinophils are recruited for killing. This pattern is seen in allergic rhinitis where the early events of mucus production and nasal itching are primarily histamine mediated whereas nasal blockage is secondary to eosinophil infiltration and activation. In asthma, the role of histamine is less clear. Urticaria is characterized by mast cell driven pruritic wheal and flare-type skin reactions that usually persist for less than 24 h. Although the events leading to mast cell degranulation have been unclear for many years, it is now becoming evident that urticaria has an autoimmune basis. Finally, the properties of first- and second-generation H 1 -antihistamines and their role in allergic is discussed.

  9. Antihistamines for the common cold.

    Science.gov (United States)

    De Sutter, An I M; Saraswat, Avadhesh; van Driel, Mieke L

    2015-11-29

    The common cold is an upper respiratory tract infection, most commonly caused by a rhinovirus. It affects people of all age groups and although in most cases it is self limiting, the common cold still causes significant morbidity. Antihistamines are commonly offered over the counter to relieve symptoms for patients affected by the common cold, however there is not much evidence of their efficacy. To assess the effects of antihistamines on the common cold. We searched CENTRAL (2015, Issue 6), MEDLINE (1948 to July week 4, 2015), EMBASE (2010 to August 2015), CINAHL (1981 to August 2015), LILACS (1982 to August 2015) and Biosis Previews (1985 to August 2015). We selected randomised controlled trials (RCTs) using antihistamines as monotherapy for the common cold. We excluded any studies with combination therapy or using antihistamines in patients with an allergic component in their illness. Two authors independently assessed trial quality and extracted data. We collected adverse effects information from the included trials. We included 18 RCTs, which were reported in 17 publications (one publication reports on two trials) with 4342 participants (of which 212 were children) suffering from the common cold, both naturally occurring and experimentally induced. The interventions consisted of an antihistamine as monotherapy compared with placebo. In adults there was a short-term beneficial effect of antihistamines on severity of overall symptoms: on day one or two of treatment 45% had a beneficial effect with antihistamines versus 38% with placebo (odds ratio (OR) 0.74, 95% confidence interval (CI) 0.60 to 0.92). However, there was no difference between antihistamines and placebo in the mid term (three to four days) to long term (six to 10 days). When evaluating individual symptoms such as nasal congestion, rhinorrhoea and sneezing, there was some beneficial effect of the sedating antihistamines compared to placebo (e.g. rhinorrhoea on day three: mean difference (MD) -0

  10. Complex Cognitive Performance and Antihistamine Use

    Science.gov (United States)

    1990-04-01

    urticaria, edema of mucous membranes, peripheral circulatory failure, bronchospasm , and increased gastric acid secretion (Di Palma, 1971). The...infants and children , especially, antihistamines in overdosage may cause hallucinations, convulsions, or death. As in adults, antihistamines may diminish...mental alertness in children . In the young child, they may produce excitation. Antihistamines are more likely to cause dizziness, sedation and

  11. The relation between antihistamine medication during early ...

    African Journals Online (AJOL)

    We will review classes of antihistamines (H1 antagonists) and the relationship between specific antihistamines and specific birth defects. Although many findings provide reassurance about the relative safety of many antihistamine drugs and that any malformation reported is most probably caused by chance, studies are still ...

  12. Contact allergens in oral antihistamines.

    Science.gov (United States)

    McEnery-Stonelake, Melissa; Silvestri, Dianne L

    2014-01-01

    Excipients in various formulations of active drugs occasionally include known contact allergens. Their ingestion may trigger dermatitis or cause it to become widespread or refractory to therapy. The aim of this study was to investigate the prevalence of common contact allergens among the excipients of oral antihistamines available in this country. We gathered the complete ingredient lists of 2119 different preparations of 12 oral antihistamines from the National Library of Medicine data bank and entered them into an electronic database for analysis. More than half the formulations (55.0%) contained at least 1 member of the 10 allergen families assessed. Most brompheniramine and doxepin preparations included potentially allergenic excipients, whereas fexofenadine was most often free of them. Sorbitan group members, azo dyes, and propylene glycol were the allergens found most frequently in the antihistamines, each present in over 25% of the products. Elixirs, liquids, solutions, suspensions, and syrups were more likely than nonchewable caplets, capsules, and tablets to contain the allergens tabulated (100% vs 39.3%, respectively). Chewable pills frequently contained azo dyes. Ingestion of antihistamines could precipitate a systemic contact dermatitis in a patient sensitized to an allergen present as an excipient in the medicine.

  13. The relation between antihistamine medication during early ...

    African Journals Online (AJOL)

    Rabah M. Shawky

    2015-05-11

    May 11, 2015 ... Abstract Antihistamines are a group of medications which can inhibit various histaminic actions at one of two histamine receptors (H1 or H2). H1 receptor antagonists are used for the relief of allergic dermatological and nondermatological conditions. We will review classes of antihistamines. (H1 antagonists) ...

  14. Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment

    Directory of Open Access Journals (Sweden)

    Anne-Marie Ellegaard

    2016-07-01

    Full Text Available Non-small cell lung cancer (NSCLC is one of the deadliest cancers worldwide. In search for new NSCLC treatment options, we screened a cationic amphiphilic drug (CAD library for cytotoxicity against NSCLC cells and identified several CAD antihistamines as inducers of lysosomal cell death. We then performed a cohort study on the effect of CAD antihistamine use on mortality of patients diagnosed with non-localized cancer in Denmark between 1995 and 2011. The use of the most commonly prescribed CAD antihistamine, loratadine, was associated with significantly reduced all-cause mortality among patients with non-localized NSCLC or any non-localized cancer when compared with use of non-CAD antihistamines and adjusted for potential confounders. Of the less frequently described CAD antihistamines, astemizole showed a similar significant association with reduced mortality as loratadine among patients with any non-localized cancer, and ebastine use showed a similar tendency. The association between CAD antihistamine use and reduced mortality was stronger among patients with records of concurrent chemotherapy than among those without such records. In line with this, sub-micromolar concentrations of loratadine, astemizole and ebastine sensitized NSCLC cells to chemotherapy and reverted multidrug resistance in NSCLC, breast and prostate cancer cells. Thus, CAD antihistamines may improve the efficacy of cancer chemotherapy.

  15. Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment.

    Science.gov (United States)

    Ellegaard, Anne-Marie; Dehlendorff, Christian; Vind, Anna C; Anand, Atul; Cederkvist, Luise; Petersen, Nikolaj H T; Nylandsted, Jesper; Stenvang, Jan; Mellemgaard, Anders; Østerlind, Kell; Friis, Søren; Jäättelä, Marja

    2016-07-01

    Non-small cell lung cancer (NSCLC) is one of the deadliest cancers worldwide. In search for new NSCLC treatment options, we screened a cationic amphiphilic drug (CAD) library for cytotoxicity against NSCLC cells and identified several CAD antihistamines as inducers of lysosomal cell death. We then performed a cohort study on the effect of CAD antihistamine use on mortality of patients diagnosed with non-localized cancer in Denmark between 1995 and 2011. The use of the most commonly prescribed CAD antihistamine, loratadine, was associated with significantly reduced all-cause mortality among patients with non-localized NSCLC or any non-localized cancer when compared with use of non-CAD antihistamines and adjusted for potential confounders. Of the less frequently described CAD antihistamines, astemizole showed a similar significant association with reduced mortality as loratadine among patients with any non-localized cancer, and ebastine use showed a similar tendency. The association between CAD antihistamine use and reduced mortality was stronger among patients with records of concurrent chemotherapy than among those without such records. In line with this, sub-micromolar concentrations of loratadine, astemizole and ebastine sensitized NSCLC cells to chemotherapy and reverted multidrug resistance in NSCLC, breast and prostate cancer cells. Thus, CAD antihistamines may improve the efficacy of cancer chemotherapy. Copyright © 2016 The Authors. Published by Elsevier B.V. All rights reserved.

  16. Multiple H1-antihistamine-induced urticaria.

    Science.gov (United States)

    Inomata, Naoko; Tatewaki, Satoko; Ikezawa, Zenro

    2009-04-01

    H(1)-antihistamines are widely used in the treatment of various allergic diseases. Particularly, a cornerstone of the management of chronic idiopathic urticaria is treatment with H(1)-antihistamines. However, a few cases of H(1)-antihistamine-induced urticaria have been reported. A 34-year-old woman presented with a 4-month history of recurrent urticaria, which was prominently exacerbated by the administration of H(1)-antihistamines. The patient consented to a provocation test of fexofenadine among drugs including cetirizine and hydroxyzine, which were suspected of inducing severe symptoms in episodes. One hour after challenge with 12 mg fexofenadine (one-fifth of the therapeutic dose), a urticarial reaction rapidly developed on nearly the entire body with remarkably increased levels of plasma histamine (190 nmol/L) and plasma leukotriene B4 (150 pg/mL). In challenge tests with other antihistamines, generalized urticaria occurred 5 and 1 h after intake of 10 mg loratadine and 10 mg bepotastine, respectively, whereas challenges with chlorpheniramine, mequitazine and azelastine were all negative. Skin prick tests with H(1)-antihistamines used in the challenges were all negative, indicating that the urticarial reactions after challenges with the causative drugs might not be immunoglobulin E-mediated. Among the causative drugs in our case, cetirizine and hydroxyzine are the piperazine derivatives, whereas fexofenadine, bepotastine, ebastine and loratadine are the piperidine derivatives. The chemical structures of both derivatives are very similar. Therefore, in this case, H(1)-antihistamine-induced urticaria may have been due to cross-reactivity between metabolites of these drugs, but not to drugs before metabolization. Hypersensitivity to H(1)-antihistamines should be considered when urticarial lesions worsen after H(1)-antihistamine treatment.

  17. Histamine, histamine receptors and antihistamines: new concepts.

    Science.gov (United States)

    Criado, Paulo Ricardo; Criado, Roberta Fachini Jardim; Maruta, Celina W; Machado Filho, Carlos d'Apparecida

    2010-01-01

    Drugs with antihistamine action are the most commonly prescribed medication in daily dermatologic practice, both to adults and children. This article addresses new concepts of the role of histamine receptors (H1 receptors) and discusses the anti-inflammatory effects of these drugs. Second generation antihistamines differs from first generation because of their high specificity and affinity for peripheral H1-receptors. Second generation antihistamines are also less likely to produce sedation because they have less effect on the central nervous system. Although the efficacy of the various H1-antihistamines in the treatment of allergic patients is similar, even when comparing first- and second-generation drugs, these drugs are still very different in terms of their chemical structure, pharmacology and toxic properties. Consequently, knowledge of their pharmacokinetic and pharmacodynamic characteristics is essential for a better medical care, especially that offered to pregnant women, children, the elderly, and patients with comorbidities.

  18. Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment

    DEFF Research Database (Denmark)

    Ellegaard, Anne-Marie; Dehlendorff, Christian; Vind, Anna C.

    2016-01-01

    non-localized cancer, and ebastine use showed a similar tendency. The association between CAD antihistamine use and reduced mortality was stronger among patients with records of concurrent chemotherapy than among those without such records. In line with this, sub-micromolar concentrations...... of loratadine, astemizole and ebastine sensitized NSCLC cells to chemotherapy and reverted multidrug resistance in NSCLC, breast and prostate cancer cells. Thus, CAD antihistamines may improve the efficacy of cancer chemotherapy...

  19. A Danish Survey of Antihistamine Use and Poisoning Patterns

    DEFF Research Database (Denmark)

    Jensen, Louise; Rømsing, Janne; Dalhoff, Kim

    2017-01-01

    -generation antihistamines. Accidental exposures constituted 33% of which 61% were due to play and 29% involved first-generation antihistamines. Single antihistamine exposures constituted 65% of DPIC exposures of which 98% involved only one brand of antihistamine. Multidrug exposures constituted 35% of DPIC exposures...... of the antihistamine use and poisoning pattern from 2007 to 2013 in Denmark based on two independent databases. There were 1049 antihistamine exposures in the national, advisory telephone service specialized in poisonings, the Danish Poison and Information Centre (DPIC), and 456 exposures in the three registers used...... within the State Serum Institute of Denmark (SSI), a department under the Danish Ministry of Health dealing with research-based health surveillance in Denmark. First-generation antihistamines constitute 61% and 73% of antihistamine registrations in DPIC and SSI, respectively. Antihistamine exposures...

  20. ANTIHISTAMINE MEDICATIONS: EFFICACY AND SAFETY OF USING IN PEDIATRIC PRACTICE

    OpenAIRE

    L.R. Giniyatova; O.I. Pikuza; L.Е. Ziganshina

    2010-01-01

    Therapy of allergic and many other diseases using antihistamine medications is the pressing topic in modern medicine. Since the first antihistamine medications were created, knowledge of effects from these drugs have expanded and changed. The article discusses approaches to classification, pharmacological properties, side effects of antihistamine medications, and provides literature review of information about justification for administering and safety of using antihistamine drugs in pediatri...

  1. Antihistamine provides sex-specific radiation protection

    Energy Technology Data Exchange (ETDEWEB)

    Mickley, G.A.

    1981-04-01

    Rats suffer an early transient performance decrement immediately after a sufficiently large dose of ionizing radiation. However, it has been shown that males experience a more severe incapacitation than females. This sex difference has been attributed to the low estrogen levels in the male. In support of this notion, supplemental estrogens in castrated male rats have produced less-severe performance decrements post-irradiation. Antihistamines have also previously been shown to alleviate radiation's effect on behavior. The present study revealed that antihistamines are only effective in altering the behavioral incapacitation of sexually intact male subjects. This contrasts with previous work which indicates that estrogens can only benefit gonadectomized rats. These findings suggest that different mechanisms may underly antihistamine and estrogen radiation protection.

  2. ANTIHISTAMINE MEDICATIONS: EFFICACY AND SAFETY OF USING IN PEDIATRIC PRACTICE

    Directory of Open Access Journals (Sweden)

    L.R. Giniyatova

    2010-01-01

    Full Text Available Therapy of allergic and many other diseases using antihistamine medications is the pressing topic in modern medicine. Since the first antihistamine medications were created, knowledge of effects from these drugs have expanded and changed. The article discusses approaches to classification, pharmacological properties, side effects of antihistamine medications, and provides literature review of information about justification for administering and safety of using antihistamine drugs in pediatric practice from the standpoint of evidence-based medicine. Key words: antihistamine medications, efficacy, safety, pharmacoepidemiology, children. (Pediatric Pharmacology. – 2010; 7(3:71-77

  3. Antihistamines for children with otitis media

    OpenAIRE

    Bonney, Asha G.; Goldman, Ran D.

    2014-01-01

    Question Otitis media is a very common condition in pediatrics and can be quite distressing for children and their parents. Is there a role for antihistamines and decongestants in the management of acute otitis media or otitis media with effusion in children?

  4. New insights into the second generation antihistamines

    NARCIS (Netherlands)

    Walsh, GM; Annunziato, L; Frossard, N; Knol, K; Levander, S; Nicolas, JM; Taglialatela, M; Tharp, MD; Tillement, JP; Timmerman, H

    2001-01-01

    Second generation antihistamines are recognised as being highly effective treatments for allergy-based disease and are among the most frequently prescribed and safest drugs in the world. However, consideration of the therapeutic index or the benefit/risk ratio of the H-1 receptor antagonists is of

  5. Optimal treatment of anaphylaxis: antihistamines versus epinephrine.

    Science.gov (United States)

    Fineman, Stanley M

    2014-07-01

    Anaphylaxis is a rapid, systemic, often unanticipated, and potentially life-threatening immune reaction occurring after exposure to certain foreign substances. The main immunologic triggers include food, insect venom, and medications. Multiple immunologic pathways underlie anaphylaxis, but most involve immune activation and release of immunomodulators. Anaphylaxis can be difficult to recognize clinically, making differential diagnosis key. The incidence of anaphylaxis has at least doubled during the past few decades, and in the United States alone, an estimated 1500 fatalities are attributed to anaphylaxis annually. The increasing incidence and potentially life-threatening nature of anaphylaxis coupled with diagnostic challenges make appropriate and timely treatment critical. Epinephrine is universally recommended as the first-line therapy for anaphylaxis, and early treatment is critical to prevent a potentially fatal outcome. Despite the evidence and guideline recommendations supporting its use for anaphylaxis, epinephrine remains underused. Data indicate that antihistamines are more commonly used to treat patients with anaphylaxis. Although histamine is involved in anaphylaxis, treatment with antihistamines does not relieve or prevent all of the pathophysiological symptoms of anaphylaxis, including the more serious complications such as airway obstruction, hypotension, and shock. Additionally, antihistamines do not act as rapidly as epinephrine; maximal plasma concentrations are reached between 1 and 3 hours for antihistamines compared with < 10 minutes for intramuscular epinephrine injection. This demonstrates the need for improved approaches to educate physicians and patients regarding the appropriate treatment of anaphylaxis.

  6. Effectiveness and safety of newgeneration antihistamines in ...

    African Journals Online (AJOL)

    Allergic diseases are on the increase, affecting 30-40% of the population. Histamine remains the most important mediator of clinical reactions in allergic diseases such as rhinitis, urticaria, and food and drug allergies. The need for more effective and safe antihistamines is critical and intensive drug development has become ...

  7. Histamine and antihistamines in atopic dermatitis.

    Science.gov (United States)

    Buddenkotte, Jörg; Maurer, Marcus; Steinhoff, Martin

    2010-01-01

    Itching (pruritus) is perhaps the most common symptom associated with inflammatory skin diseases and can be a lead symptom ofextracutaneous disease (e.g., malignancy, infection, metabolic disorders). In atopic dermatitis itching sensations constitute one of the most prominent and distressing features. The most characteristic response to itching is the scratch reflex: a more or less voluntary, often sub-conscious motor activity, to counteract the itch by slightly painful stimuli. The benefit of a short-termed relieve from itching through this scratch reflex though is counteracted by a simultaneous damage of the epidermal layer of the skin which leads to increased transepidermal water loss and drying, which in turn results in a cycle of more itching and more scratching. A wide range of peripheral itch-inducing stimuli generated within or administered to the skin are able to trigger pruritus, one of them being histamine. Based on early experiments, histamine has been suggested to may play a key role in the pathogenesis ofAD. This is reflected by a history for antihistamines in the therapeutic medication of AD patients. Antihistamines are believed to share a common antipruritic effect and therefore are prescribed to the vast majority of AD patient suffering from itch to act alleviating. The level of evidence in support of the benefits of antihistamine treatment, however, is low. To assess the benefit of antihistamines in the treatment of AD in a better way, their mechanisms and specific effects need to be understood more precisely. In particular their precise indication is crucial for successful use. This book chapter will therefore summarize and assess the role of histamine in AD and the efficacy of antihistamines in its treatment based on results of basic research and clinical studies.

  8. Histamine and H1-antihistamines: celebrating a century of progress.

    Science.gov (United States)

    Simons, F Estelle R; Simons, Keith J

    2011-12-01

    In this review we celebrate a century of progress since the initial description of the physiologic and pathologic roles of histamine and 70 years of progress since the introduction of H(1)-antihistamines for clinical use. We discuss histamine and clinically relevant information about the molecular mechanisms of action of H(1)-antihistamines as inverse agonists (not antagonists or blockers) with immunoregulatory effects. Unlike first (old)-generation H(1)-antihistamines introduced from 1942 to the mid-1980s, most of the second (new)-generation H(1)-antihistamines introduced subsequently have been investigated extensively with regard to clinical pharmacology, efficacy, and safety; moreover, they are relatively free from adverse effects and not causally linked with fatalities after overdose. Important advances include improved nasal and ophthalmic H(1)-antihistamines with rapid onset of action (in minutes) for allergic rhinitis and allergic conjunctivitis treatment, respectively, and effective and safe use of high (up to 4-fold) doses of oral second-generation H(1)-antihistamines for chronic urticaria treatment. New H(1)-antihistamines introduced for clinical use include oral formulations (bilastine and rupatadine), and ophthalmic formulations (alcaftadine and bepotastine). Clinical studies of H(3)-antihistamines with enhanced decongestant effects have been conducted in patients with allergic rhinitis. Additional novel compounds being studied include H(4)-antihistamines with anti-inflammatory effects in allergic rhinitis, atopic dermatitis, and other diseases. Antihistamines have a storied past and a promising future. Copyright © 2011 American Academy of Allergy, Asthma & Immunology. Published by Mosby, Inc. All rights reserved.

  9. Histamine, antihistamines, and the central nervous system.

    Science.gov (United States)

    Lieberman, Philip

    2009-01-01

    Histamine is a central nervous system (CNS) neurotransmitter. It acts in the brain via three receptors, H(1), H(2), and H(3). It is a mediator of "wakefulness" and its activity is necessary to maintain wakefulness, alertness, and reaction time. These activities can be impaired by H(1)-antagonists (reverse agonists) capable of penetrating the blood-brain barrier. By blocking the homeostatic effects of histamine in the CNS, drowsiness and functional impairment with or without drowsiness can occur. Several tests have been designed to assess the effects of antihistamines on the CNS. These include subjective measurements of drowsiness and more objective measurements of impairment. Second-generation antihistamines have been designed to minimize blood-brain barrier penetration by reducing lipophilicity and increasing the affinity for P-aminnoglycoprotein.

  10. Antihistamine from Tragia involucrata L. leaves.

    Science.gov (United States)

    Alagar Yadav, Sangilimuthu; Ramalingam, Sathishkumar; Jabamalai Raj, Anitha; Subban, Ravi

    2015-09-01

    Synthetic antihistamine drugs cause various adverse effects to overcome these problems with natural phytomedicine or phytoconstituents. Tragia involucrata leaves were extracted with soxhlet apparatus and fractionated with column chromatography the homogenized fractions were monitored with thin layer chromatography (TLC) and characterized by using UV-visible, FT-IR, 1H NMR, 13C NMR and MS spectral studies. Isolated compounds were screened their antihistamine activity on ileum preparation, bronchoconstriction and triple response on histamine-induced guinea pig. Antihistamine 5-hydroxy-1-methylpiperidin-2-one has been isolated and characterized from the leaves of Tragia involucrata L. A promising muscle relaxant, bronchorelaxant and anti-allergic effect of 5-hydroxy-1-methylpiperidin-2-one was observed in histamine-induced guinea pig and found to be 55.54±2.78% protection at the dose level of 12.5 mg/kg in bronchoconstriction effect and 49.05±2.45% protection in triple response. These findings were confirmed by in silico molecular docking also against histamine H1 receptor compared with chlorpheniramine maleate and mepyramine. This shows that the 5-hydroxy-1-methylpiperidine-2-one possess good inhibitory effect on histamine-induced guinea pig. The muscle relaxant, bronchodilating and anti-allergic potency of 5-hydroxy-1-methylpiperidin-2-one has been discussed in context with its probable profile as an anti-asthmatic agent from T. involucrata L. leaves. We can conclude that isolated 5-hydroxy-1-methylpiperidin-2-one from T. involucrata L. has potent antihistamine agent on histamine-induced guinea pig.

  11. Urticaria and the role of antihistamines in Pruritus | Thomas ...

    African Journals Online (AJOL)

    Nearly 50% of chronic idiopathic urticaria is associated with histamine-releasing autoantibodies. Episodes of urticaria lasting for more than 24 hours need to be evaluated for vasculitis and systemic disease. Antihistamines are the mainstay of treatment. Caution is to be taken while combining antihistamines with drugs like ...

  12. Antihistamines in pediatric allergy | El-Ghoneimy | Egyptian Journal ...

    African Journals Online (AJOL)

    Histamine is a key mediator in allergic diseases, where it exerts most of its effects through the H1 receptor and to a less extent the H2 receptor. H1-antihistamines provide rapid relief of many of the allergic symptoms and are considered the main stay of treatment of allergic rhinoconjunctivitis and urticaria. H1 antihistamines ...

  13. The clinical pharmacology of non-sedating antihistamines

    NARCIS (Netherlands)

    Yanai, Kazuhiko; Yoshikawa, Takeo; Yanai, Ai; Nakamura, Tadaho; Iida, Tomomitsu; Leurs, Rob; Tashiro, Manabu

    2017-01-01

    We previously reported on brain H1 receptor occupancy measurements of antihistamines in human brain using [11C]doxepin and positron emission tomography (PET). We proposed the use of brain H1 receptor occupancy to classify antihistamines objectively into three categories of sedating, less-sedating,

  14. Positron emission tomography evaluation of sedative properties of antihistamines.

    Science.gov (United States)

    Yanai, Kazuhiko; Zhang, Dongying; Tashiro, Manabu; Yoshikawa, Takeo; Naganuma, Fumito; Harada, Ryuichi; Nakamura, Tadaho; Shibuya, Katsuhiko; Okamura, Nobuyuki

    2011-07-01

    H(1) antihistamines are often used in the medication for allergic diseases, coughs and colds, and insomnia, with or without prescription, even though their sedative properties are a potentially dangerous unwanted side effect that is not properly recognized. These sedative properties have been evaluated using the incidence of subjective sleepiness, objective cognitive and psychomotor functions, and positron emission tomography (PET) measurement of H(1) receptor occupancy. This article reviews the current updated literature on the sedative properties of antihistamines examined by PET measurement of H(1) receptor occupancy. The use of PET to examine antihistamine penetration in the human brain in relation to psychometric and other functional measures of CNS effects is a major breakthrough and provides a new standard by which the functional CNS effects of antihistamines can be related directly to H(1) receptor occupancy. Therapy with antihistamines can be better guided by considering histamine H(1) receptor occupancy from the view of their sedative properties.

  15. Why are second-generation H1-antihistamines minimally sedating?

    Science.gov (United States)

    Hu, Yawen; Sieck, Deidra E; Hsu, Walter H

    2015-10-15

    H1-antihistamines are widely used in treating allergic disorders, e.g., conjunctivitis, urticaria, dermatitis and asthma. The first-generation H1-antihistamines have a much greater sedative effect than the second-generation H1-antihistamines. Researchers could not offer a satisfactory explanations until late 1990s when studies showed that second-generation H1-antihistamines were substrates of P-glycoprotein. P-glycoprotein, expressed in the blood-brain barrier, acts as an efflux pump to decrease the concentration of H1-antihistamines in the brain, which minimizes drug effects on the central nervous system and results in less sedation. P-glycoprotein is found in the apical side of the epithelium. It consists of transmembrane domains that bind substrates/drugs and nucleotide-binding domains that bind and hydrolyze ATP to generate energy for the drug efflux. This review mainly discusses interactions between P-glycoprotein and commonly used second-generation H1-antihistamines. In addition, it describes other possible determining factors of minimal sedating properties of second-generation H1-antihistamines. Copyright © 2015 Elsevier B.V. All rights reserved.

  16. Impairment of fear memory consolidation and expression by antihistamines.

    Science.gov (United States)

    Nonaka, Ayako; Masuda, Fumitaka; Nomura, Hiroshi; Matsuki, Norio

    2013-02-01

    Antihistamines are widely used to treat allergy symptoms. First-generation antihistamines have adverse effects on the central nervous system (CNS), such as hypnotic and amnesic effects, whereas second-generation antihistamines have poor brain penetration, and therefore, have fewer CNS-related adverse effects. Memory consists of several phases, including acquisition, consolidation, expression, and extinction. It remains unclear whether these phases are affected by antihistamines. We investigated the effects of diphenhydramine, a first-generation antihistamine, and levocetirizine and olopatadine, second-generation antihistamines, on memory phases. Mice were subjected to fear conditioning on day 1 and tested on day 2. Antihistamines were administered before conditioning, immediately after conditioning, or before the test session. Diphenhydramine (30mg/kg) decreased freezing time when administered immediately after conditioning or before the test session. These effects were not attributable to a change in locomotor activity. Levocetirizine (0.1, 1, 10mg/kg) and olopatadine (1, 10, 20mg/kg) had no effects on conditioned fear. We also examined the effect of diphenhydramine and levocetirizine on the expression of an activity-dependent gene associated with the test session. Diphenhydramine, but not levocetirizine, increased Arc transcription in the central nucleus of the amygdala. These data indicate that diphenhydramine, but not levocetirizine or olopatadine, impairs the consolidation and expression of conditioned fear. Copyright © 2012 Elsevier B.V. All rights reserved.

  17. Antihistamines as promising drugs in cancer therapy.

    Science.gov (United States)

    Faustino-Rocha, Ana I; Ferreira, Rita; Gama, Adelina; Oliveira, Paula A; Ginja, Mário

    2017-03-01

    Histamine is a biogenic amine, synthetized and released by mast cells, which acts as a vasodilator in several pathologic processes, namely in allergies and conjunctivitis. Its role on cancer is not fully understood. High levels of histamine have been associated with a bivalent behavior in regulation of several tumors (i.e. cervical, ovarian, vaginal, uterine, vulvar, colorectal cancer, and melanoma), promoting or inhibiting their growth. Histamine receptors (H1, H2, H3 and H4) are present in a vast group of cells, including tumor cells, making them sensitive to histamine variations. In this work, we review the role of mast cells and histamine on cancer development and the possibility of use antihistamines in the clinical management of this disease. Copyright © 2016 Elsevier Inc. All rights reserved.

  18. The relation between antihistamine medication during early pregnancy & birth defects

    Directory of Open Access Journals (Sweden)

    Rabah M. Shawky

    2015-10-01

    Full Text Available Antihistamines are a group of medications which can inhibit various histaminic actions at one of two histamine receptors (H1 or H2. H1 receptor antagonists are used for the relief of allergic dermatological and nondermatological conditions. We will review classes of antihistamines (H1 antagonists and the relationship between specific antihistamines and specific birth defects. Although many findings provide reassurance about the relative safety of many antihistamine drugs and that any malformation reported is most probably caused by chance, studies are still required to assure fetal safety. As pruritus is sometimes troublesome for pregnant women topical medications like emollients should be tried first in the first trimester of pregnancy. Also pregnant women should be advised to consult their health care provider before taking any medication.

  19. Effects of Antihistamine, Age, And Gender on Task Performance

    National Research Council Canada - National Science Library

    Gilliland, Kirby

    1999-01-01

    This investigation was designed to study the effects of the antihistamine, chlorpheniramine maleate, as well as the influence of age and gender, singly and in combination with chlorpheniramine maleate...

  20. H1-antihistamines induce vacuolation in astrocytes through macroautophagy

    International Nuclear Information System (INIS)

    Hu, Wei-Wei; Yang, Ying; Wang, Zhe; Shen, Zhe; Zhang, Xiang-Nan; Wang, Guang-Hui; Chen, Zhong

    2012-01-01

    H1-antihistamines induce vacuolation in vascular smooth muscle cells, which may contribute to their cardiovascular toxicity. The CNS toxicity of H1-antihistamines may also be related to their non-receptor-mediated activity. The aim of this study was to investigate whether H1-antihistamines induce vacuolation in astrocytes and the mechanism involved. The H1-antihistamines induced large numbers of giant vacuoles in astrocytes. Such vacuoles were marked with both the lysosome marker Lysotracker Red and the alkalescent fluorescence dye monodansylcadaverine, which indicated that these vacuoles were lysosome-like acidic vesicles. Quantitative analysis of monodansylcadaverine fluorescence showed that the effect of H1-antihistamines on vacuolation in astrocytes was dose-dependent, and was alleviated by extracellular acidification, but aggravated by extracellular alkalization. The order of potency to induce vacuolation at high concentrations of H1-antihistamines (diphenhydramine > pyrilamine > astemizole > triprolidine) corresponded to their pKa ranking. Co-treatment with histamine and the histamine receptor-1 agonist trifluoromethyl toluidide did not inhibit the vacuolation. Bafilomycin A1, a vacuolar (V)-ATPase inhibitor, which inhibits intracellular vacuole or vesicle acidification, clearly reversed the vacuolation and intracellular accumulation of diphenhydramine. The macroautophagy inhibitor 3-methyladenine largely reversed the percentage of LC3-positive astrocytes induced by diphenhydramine, while only partly reversing the number of monodansylcadaverine-labeled vesicles. In Atg5 −/− mouse embryonic fibroblasts, which cannot form autophagosomes, the number of vacuoles induced by diphenhydramine was less than that in wild-type cells. These results indicated that H1-antihistamines induce V-ATPase-dependent acidic vacuole formation in astrocytes, and this is partly mediated by macroautophagy. The pKa and alkalescent characteristic of H1-antihistamines may be the major

  1. H1-antihistamines induce vacuolation in astrocytes through macroautophagy

    Energy Technology Data Exchange (ETDEWEB)

    Hu, Wei-Wei; Yang, Ying; Wang, Zhe; Shen, Zhe; Zhang, Xiang-Nan [Department of Pharmacology, Key Laboratory of Medical Neurobiology of the Ministry of Health of China, Zhejiang Province Key Laboratory of Neurobiology, School of Basic Medical Sciences, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, 310058 (China); Wang, Guang-Hui [College of Pharmaceutical Sciences, Soochow University, Suzhou, 215123 (China); Chen, Zhong, E-mail: chenzhong@zju.edu.cn [Department of Pharmacology, Key Laboratory of Medical Neurobiology of the Ministry of Health of China, Zhejiang Province Key Laboratory of Neurobiology, School of Basic Medical Sciences, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, 310058 (China)

    2012-04-15

    H1-antihistamines induce vacuolation in vascular smooth muscle cells, which may contribute to their cardiovascular toxicity. The CNS toxicity of H1-antihistamines may also be related to their non-receptor-mediated activity. The aim of this study was to investigate whether H1-antihistamines induce vacuolation in astrocytes and the mechanism involved. The H1-antihistamines induced large numbers of giant vacuoles in astrocytes. Such vacuoles were marked with both the lysosome marker Lysotracker Red and the alkalescent fluorescence dye monodansylcadaverine, which indicated that these vacuoles were lysosome-like acidic vesicles. Quantitative analysis of monodansylcadaverine fluorescence showed that the effect of H1-antihistamines on vacuolation in astrocytes was dose-dependent, and was alleviated by extracellular acidification, but aggravated by extracellular alkalization. The order of potency to induce vacuolation at high concentrations of H1-antihistamines (diphenhydramine > pyrilamine > astemizole > triprolidine) corresponded to their pKa ranking. Co-treatment with histamine and the histamine receptor-1 agonist trifluoromethyl toluidide did not inhibit the vacuolation. Bafilomycin A1, a vacuolar (V)-ATPase inhibitor, which inhibits intracellular vacuole or vesicle acidification, clearly reversed the vacuolation and intracellular accumulation of diphenhydramine. The macroautophagy inhibitor 3-methyladenine largely reversed the percentage of LC3-positive astrocytes induced by diphenhydramine, while only partly reversing the number of monodansylcadaverine-labeled vesicles. In Atg5{sup −/−} mouse embryonic fibroblasts, which cannot form autophagosomes, the number of vacuoles induced by diphenhydramine was less than that in wild-type cells. These results indicated that H1-antihistamines induce V-ATPase-dependent acidic vacuole formation in astrocytes, and this is partly mediated by macroautophagy. The pKa and alkalescent characteristic of H1-antihistamines may be the

  2. Modulation of metabolic activity of phagocytes by antihistamines

    Science.gov (United States)

    Lojek, Antonin; Číž, Milan; Pekarová, Michaela; Ambrožová, Gabriela; Vašíček, Ondřej; Moravcová, Jana; Kubala, Lukáš; Drábiková, Katarína; Jančinová, Viera; Perečko, Tomáš; Pečivová, Jana; Mačičková, Tatiana; Nosál, Radomír

    2011-01-01

    The purpose of the study was to investigate the effects of H1-antihistamines of the 1st generation (antazoline, bromadryl, brompheniramine, dithiaden, cyclizine, chlorcyclizine, chlorpheniramine, clemastine) and the 2nd generation (acrivastine, ketotifen, and loratadine) on the respiratory burst of phagocytes. Reactive oxygen species generation in neutrophils isolated from rat blood was measured using luminol-enhanced chemiluminescence. Changes in nitrite formation and iNOS protein expression by RAW 264.7 macrophages were analysed using Griess reaction and Western blotting. The antioxidative properties of drugs in cell-free systems were detected spectrophotometrically, luminometrically, fluorimetrically, and amperometrically. The majority of the H1-antihistamines tested (bromadryl, brompheniramine, chlorcyclizine, chlorpheniramine, clemastine, dithiaden, and ketotifen) exhibited a significant inhibitory effect on the chemiluminescence activity of phagocytes. H1-antihistamines did not show significant scavenging properties against superoxide anion and hydroxyl radical, thus this could not contribute to the inhibition of chemiluminescence. H1-antihistamines had a different ability to modulate nitric oxide production by LPS-stimulated macrophages. Bromadryl, clemastine, and dithiaden were the most effective since they inhibited iNOS expression, which was followed by a significant reduction in nitrite levels. H1-antihistamines had no scavenging activity against nitric oxide. It can be concluded that the effects observed in the H1-antihistamines tested are not mediated exclusively via H1-receptor pathway or by direct antioxidative properties. Based on our results, antihistamines not interfering with the microbicidal mechanisms of leukocytes (antazoline, acrivastine and cyclizine) could be used preferentially in infections. Other antihistamines should be used, under pathological conditions accompanied by the overproduction of reactive oxygen species. PMID:21577279

  3. Effects of two antihistamine drugs on actual driving performance.

    OpenAIRE

    Betts, T; Markman, D; Debenham, S; Mortiboy, D; McKevitt, T

    1984-01-01

    A double blind placebo controlled experiment was conducted measuring the effects of the centrally active antihistamine triprolidine and the peripherally acting antihistamine terfenadine on actual driving performance in a group of experienced women drivers. Triprolidine greatly impaired driving behaviour, whereas terfenadine did not. Triprolidine also impaired subjective and objective measures of mood and arousal, and despite an awareness that their driving was impaired while they were taking ...

  4. H1-antihistamines induce vacuolation in astrocytes through macroautophagy.

    Science.gov (United States)

    Hu, Wei-Wei; Yang, Ying; Wang, Zhe; Shen, Zhe; Zhang, Xiang-Nan; Wang, Guang-Hui; Chen, Zhong

    2012-04-15

    H1-antihistamines induce vacuolation in vascular smooth muscle cells, which may contribute to their cardiovascular toxicity. The CNS toxicity of H1-antihistamines may also be related to their non-receptor-mediated activity. The aim of this study was to investigate whether H1-antihistamines induce vacuolation in astrocytes and the mechanism involved. The H1-antihistamines induced large numbers of giant vacuoles in astrocytes. Such vacuoles were marked with both the lysosome marker Lysotracker Red and the alkalescent fluorescence dye monodansylcadaverine, which indicated that these vacuoles were lysosome-like acidic vesicles. Quantitative analysis of monodansylcadaverine fluorescence showed that the effect of H1-antihistamines on vacuolation in astrocytes was dose-dependent, and was alleviated by extracellular acidification, but aggravated by extracellular alkalization. The order of potency to induce vacuolation at high concentrations of H1-antihistamines (diphenhydramine>pyrilamine>astemizole>triprolidine) corresponded to their pKa ranking. Co-treatment with histamine and the histamine receptor-1 agonist trifluoromethyl toluidide did not inhibit the vacuolation. Bafilomycin A1, a vacuolar (V)-ATPase inhibitor, which inhibits intracellular vacuole or vesicle acidification, clearly reversed the vacuolation and intracellular accumulation of diphenhydramine. The macroautophagy inhibitor 3-methyladenine largely reversed the percentage of LC3-positive astrocytes induced by diphenhydramine, while only partly reversing the number of monodansylcadaverine-labeled vesicles. In Atg5⁻/⁻ mouse embryonic fibroblasts, which cannot form autophagosomes, the number of vacuoles induced by diphenhydramine was less than that in wild-type cells. These results indicated that H1-antihistamines induce V-ATPase-dependent acidic vacuole formation in astrocytes, and this is partly mediated by macroautophagy. The pKa and alkalescent characteristic of H1-antihistamines may be the major

  5. Antihistamines and birth defects: a systematic review of the literature.

    Science.gov (United States)

    Gilboa, Suzanne M; Ailes, Elizabeth C; Rai, Ramona P; Anderson, Jaynia A; Honein, Margaret A

    2014-12-01

    Approximately 10 - 15% of women reportedly take an antihistamine during pregnancy for the relief of nausea and vomiting, allergy and asthma symptoms, or indigestion. Antihistamines include histamine H1-receptor and H2-receptor antagonists. This is a systematic evaluation of the peer-reviewed epidemiologic literature published through February 2014 on the association between prenatal exposure to antihistamines and birth defects. Papers addressing histamine H1- or H2-receptor antagonists are included. Papers addressing pyridoxine plus doxylamine (Bendectin in the United States, Debendox in the United Kingdom, Diclectin in Canada, Lenotan and Merbental in other countries) prior to the year 2001 were excluded post hoc because of several previously published meta-analyses and commentaries on this medication. The literature on the safety of antihistamine use during pregnancy with respect to birth defects is generally reassuring though the positive findings from a few large studies warrant corroboration in other populations. The findings in the literature are considered in light of three critical methodological issues: i) selection of appropriate study population; ii) ascertainment of antihistamine exposures; and iii) ascertainment of birth defect outcomes. Selected antihistamines have been very well studied (e.g., loratadine); others, especially H2-receptor antagonists, require additional study before an assessment of safety with respect to birth defect risk could be made.

  6. Ophthalmic antihistamines and H1-H4 receptors.

    Science.gov (United States)

    Wade, Laurie; Bielory, Leonard; Rudner, Shara

    2012-10-01

    Antihistamines exert pharmacologic effects by binding to four histamine receptors (H1-H4) at different affinities, producing variable effects depending on the receptor they predominantly bind to. This review's purpose is to determine the relative potency of antihistamines by comparing their binding affinities to these receptors. Studies on binding affinities of antihistamines to histamine receptors were reviewed and the dissociation constant for inhibitor binding (Ki) analyzed to determine the most and least potent antihistamine for each receptor. We retrieved the binding affinities for nineteen antihistamines. For H1 receptors, pyrilamine exhibited the highest affinity (Ki = 0.8 nM), and thioperamide the lowest (Ki = 280, 000 nM). For H2 receptors, ranitidine exhibited the highest affinity (Ki = 187 nM), and olopatadine the lowest (Ki = 100 ,000 nM). For the recently discovered H3 and H4 receptors, thioperamide exhibited the highest affinity (Ki = 1.1 nM), and olopatadine exhibited the lowest (Ki = 79 ,400 nM), to H3. Data on binding affinities to the H4 receptor exist for: ketotifen, pheniramine, ranitidine, cimetidine and thioperamide. Of these, thioperamide exhibited the highest affinity (Ki = 27 nM), whereas cimetidine and ranitidine exhibited the lowest affinity (Ki = >10, 000 nM) for H4 receptors. This review summarizes the relative potency of antihistamines based on their binding affinities to the four histamine receptors. Although data on binding affinities of antihistamines to the H4 receptor are sparse, it is apparent that further research on these histamine subtypes may open new venues for more direct treatment with a higher therapeutic efficacy on allergic disorders including those affecting the ocular surface.

  7. Use of second generation H1 antihistamines in special situations.

    Science.gov (United States)

    Dávila, I; del Cuvillo, A; Mullol, J; Jáuregui, I; Bartra, J; Ferrer, M; Montoro, J; Sastre, J; Valero, A

    2013-01-01

    Antihistamine drugs are one of the therapeutic classes most used at world level, at all ages and in multiple situations. Although in general they have a good safety profile, only the more recent drugs (second generation antihistamines) have been studied specifically with regard to the more important safety aspects. Given the variety of antihistamine drugs, they cannot all be considered equivalent in application to various special clinical situations, so that the documented clinical experience must be assessed in each case or, in the absence of such, the particular pharmacological characteristics of each molecule for the purpose of recommendation in these special situations. In general, there are few clinical studies published for groups of patients with kidney or liver failure, with concomitant multiple pathologies (such as cardiac pathology), in extremes of age (paediatrics or geriatrics) and in natural stages such as pregnancy or lactation, but these are normal situations and it is more and more frequent (among the elderly) for antihistamine drugs to be recommended. This review sets out the more relevant details compiled on the use of antihistamines in these special situations.

  8. Bioanalysis of antihistamines for clinical or forensic purposes.

    Science.gov (United States)

    Katselou, Maria; Papoutsis, Ioannis; Nikolaou, Panagiota; Spiliopoulou, Chara; Athanaselis, Sotiris

    2017-01-01

    Antihistamines are a class of drugs that inhibit the action of histamine and are used to alleviate symptoms associated with allergic reactions, but some of them can cause side effects, the most unpleasant and dangerous of which are the sedative effects that may hinder important psychological functions and impair skilled performance. These side effects could decrease safety in certain common and critical tasks, such as driving or operating machinery, leading to accidents. Antihistamines can also cause intoxications, sometimes lethal, especially when co-administered with alcohol or other sedative drugs. Thus, the development of analytical methods for their determination in biological fluids is considered to be useful for the investigation of clinical and forensic cases. These methodologies could also be used for pharmacokinetic studies. Several liquid and a few gas chromatographic methods have been developed for the determination of antihistamines in biological matrices after proper pretreatment procedures. This article reviews the published analytical methodologies that were gathered through the search in PubMed database and the recent developments on isolation or determination of antihistamines in biological materials. Current trends and future perspectives on bioanalysis of antihistamines are also discussed. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

  9. [Use of antihistamines in a physician's clinical practice].

    Science.gov (United States)

    Luss, L V

    2014-01-01

    Histamine that belongs to one of the most important mediators involved in the regulation of the body's vital functions plays a great role in the pathogenesis of different diseases. Histamine is released during inflammatory and allergic reactions, anaphylactic and anaphylactoid shock, pseudoallergic reactions, and others. Acting through histamine receptors, it leads to increased intracellular concentration of cyclic guanosine monophosphate, enhanced chemotaxis of eosinophils and neutrophils, production of prostaglandins and thromboxane B, suppressed synthesis of lymphokines, etc. and causes contraction of smooth muscles of particularly the bronchi and intestine, dilation of vessels and their increased permeability, mucus hypersecretion in the upper airways, lower blood pressure, angioedema and itch, etc. In this connection, antihistamines that block histamine-induced reactions in various ways: by inhibiting its biosynthesis, enhancing its neutralization, blocking the access to receptors, and suppressing the release from mast cells, occupy a prominent place in clinical practice. The review covers the classification, main mechanisms of pharmacological action, and indications for the use of antihistamines that not only have the well-known antihistamine properties, but have also a broad spectrum of anti-inflammatory activity. There are data on the benefits of a group of antihistamines, the quinuclidine derivatives (quifenadine, sequifenadine) that were designed by Academician M.D. Mashkovsky and are one of the first examples of designing new classes of multifunctional non-sedating antihistamines, which combines a high selective activity to block histamine type 1 receptors and an ability to block serotonin and to break down histamine directly in tissues.

  10. Gynecomastia induced by H1-antihistamine (ebastine) in a patient with idiopathic anaphylaxis

    OpenAIRE

    Jung, Hwa Sik; Park, Chan-Ho; Park, Young Tae; Bae, Mi Ae; Lee, Youn Im; Kang, Byung Ju; Jegal, Yangjin; Ahn, Jong Joon; Lee, Taehoon

    2015-01-01

    H1-antihistamine is generally a well-tolerated and safe drug. However, in resemblance with all other drugs, H1-antihistamines can also prompt adverse drug reactions (ADRs). We recently encountered the very unusual ADR of H1-antihistamine-induced gynecomastia. A 21-year-old man with idiopathic anaphylaxis was treated with ebastine (Ebastel), a second-generation H1-antihistamine, for the prevention of anaphylaxis. Three months later, the patient remained well without anaphylaxis, but had newly ...

  11. Antihistamine provides sex-specific radiation protection. [Ionizing radiation

    Energy Technology Data Exchange (ETDEWEB)

    Mickley, G.A.

    1981-04-01

    Rats suffer an early transient performance decrement immediately after a sufficiently large dose of ionizing radiation. However, it has been shown that males experience a more severe incapacitation than females. This sex difference has been attributed to the low estrogen levels in the male. In support of this notion, supplemental estrogens in castrated male rats have produced less-severe performance decrements post-irradiation. Antihistamines have also previously been shown to alleviate radiation's effect on behavior. The present study revealed that antihistamines are only effective in altering the behavioral incapacitation of sexually intact male subjects. This contrasts with previous work which indicates that estrogens can only benefit gonadectomized rats. These findings suggest that different mechanisms may underlie antihistamine and estrogen radiation protection.

  12. Patients Taking Antihistamines and Their Effects on Driving.

    Science.gov (United States)

    Kizu, Junko

    2017-01-01

    Sleepiness is known as one of the side effects of antihistamines, and impaired performance caused by these drugs has become problematic. Among the 13 second-generation antihistamines causing sleepiness to some extent, the package inserts of 8 drugs prohibit driving, 3 stress driving with care, and 2 give no driving-related warning. It was confirmed that the description did not necessarily reflect the results of the standard deviation of lateral position measurement study, which is considered the most effective study for evaluating the effects of drugs on automobile driving. Do these descriptions reflect actual patients' sleepiness? According to a questionnaire survey involving 2000 individuals taking second-generation antihistamines, 7.3% of respondents answered that they had always become sleepy after taking antihistamines (3.1-12.5% according to the type of antihistamine), 32.8% (27.8-45.8%) had become sleepy sometimes, 9.1% (3.1-15.8%) had previously become sleepy but not anymore, and 40.9% (27.1-49.1%) had never become sleepy. In addition, 10.3% (2.4-21.1%) reported intolerable sleepiness. Patients who had experience of receiving pharmaceutical education from pharmacists numbered 1296 (64.8%), and 80.2% of them had also received driving-related explanations, which included the prohibition of driving (32.8%), stressing the need to drive with care (54.7%), and the prohibition of medication before driving (12.0%). Concerning these explanations, the proportion who paid attention on a daily basis, paid slight attention, and paid no attention was 36.7, 31.2, and 32.1%, respectively. To provide effective and safe pharmacotherapy for the increasing number of patients taking antihistamines, pharmacists should ideally improve pharmaceutical education.

  13. 21 CFR 341.12 - Antihistamine active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Antihistamine active ingredients. 341.12 Section 341.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE COLD, COUGH, ALLERGY, BRONCHODILATOR, AND ANTIASTHMATIC DRUG PRODUCTS FOR OVER-THE...

  14. H1-antihistamines and oxidative burst of professional phagocytes

    Czech Academy of Sciences Publication Activity Database

    Nosál, R.; Drábiková, K.; Jančinová, V.; Moravcová, Jana; Lojek, Antonín; Číž, Milan; Mačičková, T.; Pečivová, J.

    2009-01-01

    Roč. 30, č. 1 (2009), s. 133-136 ISSN 0172-780X Institutional research plan: CEZ:AV0Z50040507; CEZ:AV0Z50040702 Keywords : chemiluminescence * H1- antihistamines * phagocytes Subject RIV: BO - Biophysics Impact factor: 1.047, year: 2009

  15. The efficacy of intranasal antihistamines in the treatment of allergic rhinitis.

    Science.gov (United States)

    Kaliner, Michael A; Berger, William E; Ratner, Paul H; Siegel, Charles J

    2011-02-01

    To discuss the new use of intranasal antihistamines as first-line therapies, compare and contrast this class of medication with the traditionally available medications, and discuss the potential for intranasal antihistamines to provide relief superior to second-generation oral antihistamines. Review articles and original research articles were retrieved from MEDLINE, OVID, PubMed (1950 to November 2009), personal files of articles, and bibliographies of located articles that addressed the topic of interest. Articles were selected for their relevance to intranasal antihistamines and their role in allergic rhinitis. Publications included reviews, treatment guidelines, and clinical studies (primarily randomized controlled trials) of both children and adults. This panel was charged with reviewing the place of intranasal antihistamines in the spectrum of treatment for allergic rhinitis. Intranasal antihistamines have been shown in numerous randomized, placebo-controlled trials to be more efficacious than the oral antihistamines. Although intranasal corticosteroids are considered by some to be superior to intranasal antihistamines, multiple studies have shown an equal effect of the 2 classes of medication. Both intranasal corticosteroids and intranasal antihistamines have been shown to reduce all symptoms of allergic rhinitis. In addition, some intranasal antihistamines have a more rapid onset of action than intranasal corticosteroids. The future of allergy treatment will likely involve a combination of both intranasal corticosteroids and intranasal antihistamines because of the benefits of local administration and their additive effect on efficacy. Copyright © 2011 American College of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  16. Antihistamines prescribed off-label among paediatric patients at a tertiary care hospital setting in Malaysia.

    Science.gov (United States)

    Tan, Rou Wei; Mohamed Shah, Noraida

    2016-10-01

    Background Antihistamines are widely prescribed to children but should be used with caution in young children. Objective To determine the paediatric prescribing pattern of antihistamines with a focus on the off-label prescribing and factors that influence such prescribing. Setting Paediatric wards of a tertiary care hospital setting in Malaysia. Methods The pharmacy-based computer system and medical records were used to collect the required data. Labelling status of each antihistamine was determined based on the information provided in the product leaflets. Main outcome measure Antihistamines prescribed off-label and factors associated with such prescribing. Results Of the 176 hospitalised children aged antihistamine in the year 2012, 60.8 % received it in an off-label manner. Of 292 antihistamine prescription items, 55.5 % were prescribed off-label. Loratadine (35.3 %) was the most frequently prescribed antihistamine and chlorpheniramine maleate (34.0 %) was the most common antihistamine prescribed off-label. The main reason for the off-label prescribing of antihistamines was prescribing at higher than the recommended dose (30.2 %). Binary logistic regression showed that children aged antihistamines. Conclusion Prescribing antihistamines for children in an off-label manner was prevalent at the studied locations and warrants further investigation on the consequences of such prescribing.

  17. Comparison of intranasal corticosteroids and antihistamines in allergic rhinitis: a review of randomized, controlled trials.

    Science.gov (United States)

    Nielsen, Lars P; Dahl, Ronald

    2003-01-01

    For several years there has been discussion of whether first-line pharmacological treatment of allergic rhinitis should be antihistamines or intranasal corticosteroids. No well documented, clinically relevant differences seem to exist for individual nonsedating antihistamines in the treatment of allergic rhinitis. Likewise, the current body of literature does not seem to favor any specific intranasal corticosteroid. When comparing efficacy of antihistamines and intranasal corticosteroids in allergic rhinitis, present data favor intranasal corticosteroids. Interestingly, data do not support antihistamines as superior in treating conjunctivitis associated with allergic rhinitis. Safety data from comparative studies in allergic rhinitis do not indicate differences between antihistamines and intranasal corticosteroids. Combining antihistamines and intranasal corticosteroids in the treatment of allergic rhinitis does not provide additional beneficial effects to intranasal corticosteroids alone. Considering present data, intranasal corticosteroids seem to offer superior relief in allergic rhinitis, when compared with antihistamines.

  18. The role of antihistamines in chronic actinic dermatitis treatment

    Directory of Open Access Journals (Sweden)

    E. V. Orlov

    2016-01-01

    Full Text Available Inveterate actinic dermatitis is an immunologically mediated photodermatosis characterized by itchy eczematous dermhelminthiasis exposed to sunlight. The disease proceeds in the same way as the atopic eczema or atopic dermatitis. The treatment of patients with inveterate actinic dermatitis is similar to the treatment of patients with atopic dermatitis and eczema. Administration of the modern antihistaminic preparation desloratadine (Aerius in the treatment has a positive effect on the skin process relief and on some cellular and humoral immunity factors.

  19. Analysis for commonly prescribed non-sedating antihistamines

    Directory of Open Access Journals (Sweden)

    Michael E. El-Kommos

    2015-03-01

    Full Text Available A comprehensive review with 185 references for the analysis of commonly prescribed members of an important class of drugs, non-sedating antihistamines (NSAs, is presented. The review covers most of the methods described for the analysis of cetirizine (CTZ, ebastine (EBS, fexofenadine (FXD, ketotifen (KET and loratadine (LOR in pure forms, in different pharmaceutical dosage forms and in biological fluids. The review covers the period from 1991 till now.

  20. Gynecomastia induced by H1-antihistamine (ebastine) in a patient with idiopathic anaphylaxis.

    Science.gov (United States)

    Jung, Hwa Sik; Park, Chan-Ho; Park, Young Tae; Bae, Mi Ae; Lee, Youn Im; Kang, Byung Ju; Jegal, Yangjin; Ahn, Jong Joon; Lee, Taehoon

    2015-07-01

    H1-antihistamine is generally a well-tolerated and safe drug. However, in resemblance with all other drugs, H1-antihistamines can also prompt adverse drug reactions (ADRs). We recently encountered the very unusual ADR of H1-antihistamine-induced gynecomastia. A 21-year-old man with idiopathic anaphylaxis was treated with ebastine (Ebastel), a second-generation H1-antihistamine, for the prevention of anaphylaxis. Three months later, the patient remained well without anaphylaxis, but had newly developed gynecomastia. Because anaphylaxis recurred after the cessation of H1-antihistamine, the preventive medication was changed to omalizumab. A few months later, his gynecomastia had entirely disappeared. Physicians should be aware of this exceptional ADR of H1-antihistamine.

  1. Are antihistamines effective in children? A review of the evidence.

    Science.gov (United States)

    De Bruyne, Pauline; Christiaens, Thierry; Boussery, Koen; Mehuys, Els; Van Winckel, Myriam

    2017-01-01

    During the last decades, much attention has been paid to off-label and unlicensed prescriptions in paediatrics. However, on-label prescribing can also cause health issues. In this paper, the case of first-generation H 1 -antihistamines is investigated, notably the range of indications for which products are licensed in different European countries and the evidence base (or lack thereof) for each indication, as well as reported adverse drug reactions. Review of the Summary of Product Characteristics of first-generation H 1 -antihistamines with a focus on paediatric use. This is plotted against the evidence available in the literature. This investigation shows a large variability in labelled indications and licensing ages when compared in five different European countries. Moreover, most of the indications are not based on clinical trials evaluating efficacy and safety of these drugs in children. Many of the licensed indications of first-generation antihistamines do not appear to be evidence based. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://www.bmj.com/company/products-services/rights-and-licensing/.

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

    Science.gov (United States)

    Chawla, Vonita; Hogan, Mary Beth; Moonie, Sheniz; Fenwick, Ginger L; Hooft, Anneka; Wilson, Nevin W

    2016-01-01

    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 antihistamines to be as helpful as topical corticosteroids. Parents of pediatric patients with AD found that antihistamines were an important part of AD management.

  3. Selecting the optimal oral antihistamine for patients with allergic rhinitis.

    Science.gov (United States)

    Lehman, Jeffrey M; Blaiss, Michael S

    2006-01-01

    Allergic rhinitis (AR) is now recognised as a global health problem that affects 10-30% of adults and up to 40% of children. Each year, millions of patients seek treatment from their healthcare provider. However, the prevalence of AR maybe significantly underestimated because of misdiagnosis, under diagnosis and failure of patients to seek medical attention. In addition to the classical symptoms such as sneezing, nasal pruritus, congestion and rhinorrhoea, it is now recognised that AR has a significant impact on quality of life (QOL). This condition can lead to sleep disturbance as a result of nasal congestion, which leads to significant impairment in daily activities such as work and school. Traditionally, AR has been subdivided into seasonal AR (SAR) or perennial AR (PAR). SAR symptoms usually appear during a specific season in which aeroallergens are present in the outdoor air such as tree and grass pollen in the spring and summer and weed pollens in the autumn (fall); and PAR symptoms are present year-round and are triggered by dust mite, animal dander, indoor molds and cockroaches. Oral histamine H(1)-receptor antagonists (H(1) antihistamines) are one of the most commonly prescribed medications for the treatment of AR. There are several oral H(1) antihistamines available and it is important to know the pharmacology, such as administration interval, onset of action, metabolism and conditions that require administration adjustments. When prescribing oral H(1) antihistamines, the healthcare provider must take into account the clinical efficacy and weigh this against the risk of adverse effects from the agent. In addition to the clinical efficacy, potential for improvement in QOL with a particular treatment should also be considered.

  4. H1-Antihistamine Premedication in NSAID-Associated Urticaria.

    Science.gov (United States)

    Trautmann, Axel; Anders, Diana; Stoevesandt, Johanna

    Therapeutic options for pain management are restricted in patients with nonsteroidal anti-inflammatory drug (NSAID)-induced or NSAID-exacerbated urticaria because strong cyclooxygenase (COX)-I inhibiting NSAID cannot be used. Alternative NSAID such as weak COX-I inhibitors or selective COX-II inhibitors are sometimes not sufficiently effective or have potentially troublesome adverse effects. To date, prophylactic premedication with H 1 -antihistamines is rarely practiced in patients concurrently suffering from recurrent pain and NSAID-associated urticaria. Our data analysis aims to clarify whether prophylactic premedication before the intake of NSAID is effective, safe, and practicable. Data of 21 patients with NSAID-induced or NSAID-exacerbated urticaria who underwent single dose NSAID provocation 30 minutes after premedication with 5 mg desloratadine were retrospectively evaluated. After H 1 -antihistamine premedication, 17 patients tolerated 16 single dose provocation tests with strong COX-I inhibitors and 2 tests with weak COX-I inhibitors. Despite H 1 -antihistamine premedication, 2 patients developed acute urticaria after intake of 400 mg ibuprofen. Another 2 patients with acute urticaria after intake of 800 mg ibuprofen tolerated 400 mg ibuprofen and 1000 mg paracetamol, respectively. In the majority of patients with NSAID-induced or NSAID-exacerbated urticaria concurrently suffering from intermittent pain, a premedication regimen with 5 mg desloratadine 30 minutes before intake of a strong COX-I inhibitor seems to be effective, safe, and practicable. Copyright © 2016 American Academy of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  5. Antihistamines and driving ability: Evidence from 30 years Dutch on-road driving research

    NARCIS (Netherlands)

    Verster, J.C.; Van De Loo, A.J.A.E.; Garssen, J.

    2015-01-01

    Background: Since all antihistamines are capable of crossing the blood-brain barrier, they may also cause sedation which may impair daily activities such as driving a car. The purpose of this review was to examine the effects of antihistamines on driving ability. Method: A literature search revealed

  6. Systemic antihistamines--a common outside the guidelines therapeutic strategy in hand eczema management.

    Science.gov (United States)

    Jankowska-Konsur, A; Reich, A; Szepietowski, J C

    2016-01-01

    Hand eczema (HE) is the most common skin disease affecting hands. Although the current treatment guidelines do not recommend use of systemic antihistamines as routine therapy, they seem to be widely used by physicians handling with this problem. The aim of the study was to investigate the attitude to prescribe systemic antihistamines in HE. A 10-item questionnaire was distributed among physicians participating in regional dermatological conferences. 127 valid questionnaires were analysed. A total of 127 physicians participated in the survey. 124 (97.6%) responders prescribe antihistamines in HE and 16 (12.6%) subjects declared routine use of oral antihistamines in the HE management. Significantly more dermatologists than other specialists used antihistamines in the treatment of HE accompanying atopic dermatitis (77.8% vs. 54.5%, P antihistamines in HE due to their anti-inflammatory properties (40.3% vs. 20.0%, P = 0.02). Regarding the type of eczema, antihistamines were prescribed most frequently in acute allergic HE (n = 92, 72.4%) and in HE accompanying atopic dermatitis (n = 86, 67.7%). Despite the lack of the large, randomized, controlled studies on the effectiveness of the systemic antihistamines in the treatment of HE, this type of therapy seems to be prevalently used among the physicians. © 2015 European Academy of Dermatology and Venereology.

  7. EFFICACY OF H1 ANTIHISTAMINES IN CHILDREN WITH FOOD ALLERGY

    Directory of Open Access Journals (Sweden)

    I.I. Balabolkin

    2007-01-01

    Full Text Available The authors assesed a clinical efficacy of Zirtek (cetirizin in 27 children with atopic dermatitis and 40 children with bronchial asthma, associated with food sensitization. Positive therapeutic effect was achieved in 92,5% patients with atopic dermatitis and 87,5% children with bronchial asthma. The improvement of lung functions, decreasing bronchial hyperrecactivity in children with bronchial asthma and of itch and skin`s inflammation in patients with atopic dermatitis are achieved.Key words: food allergy, h1 antihistamines, cetirizine.

  8. An overview of the novel H1-antihistamine bilastine in allergic rhinitis and urticaria.

    Science.gov (United States)

    Jáuregui, Ignacio; García-Lirio, Eduardo; Soriano, Ana María; Gamboa, Pedro M; Antépara, Ignacio

    2012-01-01

    Currently available second-generation H1-antihistamines include a wide group of drugs with a better therapeutic index (or risk-benefit ratio) than the classic antihistamines, although their properties and safety profiles may differ. Bilastine is a newly registered H1-antihistamine for the oral treatment of allergic rhinitis and urticaria, with established antihistaminic and antiallergic properties. Clinical studies in allergic rhinitis and chronic urticaria show that once-daily treatment with bilastine 20 mg is effective in managing symptoms and improving patient's quality of life, with at least comparable efficacy to other nonsedative H1-antihistamines. As far as studies in healthy volunteers, clinical assays and clinical experience can establish, bilastine's safety profile is satisfactory, since it lacks anticholinergic effects, does not impair psychomotor performance or actual driving, and appears to be entirely free from cardiovascular effects.

  9. Antihistamines for treating rhinosinusitis: systematic review and meta-analysis of randomised controlled studies.

    Science.gov (United States)

    Seresirikachorn, K; Khattiyawittayakun, L; Chitsuthipakorn, W; Snidvongs, K

    2018-02-01

    Without the release of histamines, patients with rhinosinusitis may not benefit from antihistamines. Additionally, anticholinergic effects may do more harm than good. This study aimed to investigate the effectiveness of antihistamines in treating rhinosinusitis. An electronic search was performed. Randomised controlled trials comparing antihistamines with either placebo or other treatments for patients with rhinosinusitis were selected. Two studies (184 patients) met the inclusion criteria. Loratadine decreased nasal obstruction in allergic rhinitis patients with acute rhinosinusitis (mean difference = -0.58; confidence interval = -0.85 to -0.31, p antihistamines in treating rhinosinusitis. The number of included studies in this systematic review is limited. Antihistamines may relieve nasal obstruction in allergic rhinitis patients with acute rhinosinusitis.

  10. Effect of radiosterilization of some antihistamines on their toxicity

    International Nuclear Information System (INIS)

    El-Sayed, M.E.; Roushdy, H.M.; Naiema, M.; Seham, H.M.H.

    1985-01-01

    The effect of gamma irradiation of pgeniramine maleate and menhydrinate solutions at the radiation levels of 15,25 and 50KGY on their toxicity has been investigated. Irradiation of pheniramine maleate and dimenhydrinate solutions at dose levels of 15,25 and 50KGY resulted in no significant change in neither the gross toxicity of the two drugs nor in their LD 50's on rats. Pheniramine maleate and dimenhydrinate whether irradiated or not, resulted in no significant increase in serum GPT or alkaline phosphatase activities when given at a dose of 15mg/Kg suggesting no significant alteration to liver function in rats. Higher doses of the two antihistaminics, namely, the minimal lethal doses and the LD 50's induced hydropic degeneration of liver cells, lymphocytic infiltration of the portal tract and focal areas of necrosis of hepatic cells mostly in the central lobule. Fatty infiltration was observed with dimenhydrinate. Radiation treatment of those antihistamines up to 50KGY resulting in no alteration in their toxicity projects the high radiation stability of pheniramine maleate and dimenhydrinate and confirms gamma irradiation is a successful method for their sterilization

  11. [Antihistamines in the treatment of allergic rhinitis--update 2008/2009].

    Science.gov (United States)

    Kruszewski, Jerzy

    2009-09-01

    The following paper reviews the latest news on antihistamines used in the treatment of allergic rhinitis. It describes the new results of investigations on clinical application of H3 and H4 receptors in therapy of allergic diseases as well as the effect of emedastine on histamine-induced tissue remodeling. Contemporary clinical research of these drugs fulfills the requirements of placebo-controlled trials, including the comparison with a reference drug, usually cetirizine. The paper discusses efficacy and safety of a new drug--bilastine, and the possibility to improve clinical outcome by combining antihistamine drugs with inhaled glucocorticosteroids and antileukotrienes. It also presents the studies on high efficacy of nasal antihistamines, which most probably results from their high concentration in inflamed tissue, as well as describes the latest news on safe use of antihistamines, including studies of fexofenadine enantiomers in drug interactions with P-glycoprotein, safety of a new antihistamine medication--rupatadine, and psychostimulating effect of some other antihistamines. The review shows that antihistamines, the most frequently used class of anti-allergy medications, have been constantly improved, which is of significant importance for progress of allergic diseases treatment.

  12. Assessment of the effects of antihistamine drugs on mood, sleep quality, sleepiness, and dream anxiety.

    Science.gov (United States)

    Ozdemir, Pinar Guzel; Karadag, Ayşe Serap; Selvi, Yavuz; Boysan, Murat; Bilgili, Serap Gunes; Aydin, Adem; Onder, Sevda

    2014-08-01

    There are limited comparative studies on classic and new-generation antihistamines that affect sleep quality and mood. The purpose of this study was to determine and compare the effects of classic and new-generation antihistamines on sleep quality, daytime sleepiness, dream anxiety, and mood. Ninety-two patients with chronic pruritus completed study in the dermatology outpatient clinic. Treatments with regular recommended therapeutic doses were administered. The effects of antihistaminic drugs on mood, daytime sleepiness, dream anxiety, and sleep quality were assessed on the first day and 1 month after. Outpatients who received cetirizine and hydroxyzine treatments reported higher scores on the depression, anxiety, and fatigue sub-scales than those who received desloratadine, levocetirizine, and rupatadine. Pheniramine and rupatadine were found to be associated with daytime sleepiness and better sleep quality. UKU side effects scale scores were significantly elevated among outpatients receiving pheniramine. Classic antihistamines increased daytime sleepiness and decreased the sleep quality scores. New-generation antihistamines reduced sleep latency and dream anxiety, and increased daytime sleepiness and sleep quality. Both antihistamines, significantly increased daytime sleepiness and nocturnal sleep quality. Daytime sleepiness was significantly predicted by rupadatine and pheniramine treatment. Cetirizine and hydroxyzine, seem to have negative influences on mood states. Given the extensive use of antihistamines in clinical settings, these results should be more elaborately examined in further studies.

  13. Risk of first-generation H(1)-antihistamines: a GA(2)LEN position paper

    DEFF Research Database (Denmark)

    Church, M K; Maurer, M; Simons, F E R

    2010-01-01

    : To increase consumer protection by bringing to the attention of regulatory authorities, physicians and the general public the potential dangers of the indiscriminate use first-generation H(1)-antihistamines purchased over-the counter in the absence of appropriate medical supervision. METHODS: A GA(2)LEN...... consumer protection by recommending that older first-generation H(1)-antihistamines should no longer be available over-the-counter as prescription- free drugs for self-medication of allergic and other diseases now that newer second- generation nonsedating H(1)-antihistamines with superior risk...

  14. Study on the biological activity of certain antihistamines subjected to radiation sterilization

    International Nuclear Information System (INIS)

    El-Sayed, M.E.; Roushdy, H.M.; Seham, H.H.M.

    1986-01-01

    The effect of gamma irradiation of pheniramine maleate and dimenhydrinate solution the dose levels 15, 25 and 50 KGY on their antihistaminic activity has been investigated using the histamine aerosol and guinea pig ileum methods. From the results obtained it could be concluded that, the antihistaminic activity of both pheniramine maleate and dimenhydrinate was not significantly changed by radiation exposure at the dose levels 15, 25 and 50 KGY. Accordingly, both of the two drugs can be safely sterilized by gamma-irradiation without encountering deleterious effect on their antihistaminic activity

  15. Histamine H4 receptor antagonists: the new antihistamines?

    Science.gov (United States)

    Fung-Leung, Wai-Ping; Thurmond, Robin L; Ling, Ping; Karlsson, Lars

    2004-11-01

    Antihistamines (histamine H1 receptor antagonists) are a mainstay treatment for atopic allergy, yet they are only partially effective in relieving the symptoms of the disease. They also have very limited value for the treatment of asthma, despite the well-characterized bronchoconstrictory effects of histamine. The recent discovery of a fourth histamine receptor (H4), and the realization that it is exclusively expressed on hematopoietic cell types that are most implicated in the development and symptomatology of allergy and asthma, suggests that pharmacological targeting of the H4 receptor, either alone or in combination with H1 receptor antagonists, may prove useful for treating both allergy and asthma. Here we review the known biology associated with the H4 receptor, as well the effects of a highly selective H1 receptor antagonist.

  16. CHOICE AND STUDY OF BASE FOR PRODUCTION OF SUPPOSITORIES WITH ANTIHISTAMINIC ACTION

    Directory of Open Access Journals (Sweden)

    N. V. Prokuschenko

    2014-01-01

    Full Text Available Russian pharmaceutical industry development is made possible by new medicinal forms production. To widen the assortment of antihistaminic drugs we have offered a model mixture of suppositories

  17. Non-sedating antihistamine drugs and cardiac arrhythmias -- biased risk estimates from spontaneous reporting systems?

    DEFF Research Database (Denmark)

    De Bruin, M L; van Puijenbroek, E P; Egberts, A C G

    2002-01-01

    AIMS: This study used spontaneous reports of adverse events to estimate the risk for developing cardiac arrhythmias due to the systemic use of non-sedating antihistamine drugs and compared the risk estimate before and after the regulatory action to recall the over-the-counter status of some...... of these drugs. METHODS: All suspected adverse drug reactions (ADRs) reported until July 1999 to the Netherlands Pharmacovigilance Foundation Lareb were used to calculate the ADR reporting odds ratio, defined as the ratio of exposure odds among reported arrhythmia cases, to the exposure odds of other ADRs (non......-sedating antihistamines. In general non-sedating antihistamines are associated with cardiac arrhythmia to a higher extent in comparison with other drugs (ADR reporting odds ratio 2.05 [95% CI: 1.45, 2.89]). The association between arrhythmias and non-sedating antihistamine drugs calculated before 1998...

  18. Antihistamines and driving-related behavior : a review of the evidence for impairment

    Science.gov (United States)

    2004-05-01

    A review of the scientific literature concerning the effects of antihistamines on driving-related skills was conducted. After reviewing all pertinent publications from 1998 and earlier, a total of 130 publications were found to meet criteria for incl...

  19. Synergistic effect of broad-spectrum Sunscreens and antihistamines in the control of idiopathic solar urticaria

    DEFF Research Database (Denmark)

    Faurschou, A.; Wulf, Hans Chr.

    2008-01-01

    Background: It can be difficult to provide patients with idiopathic solar urticaria adequate protection from sunlight. In a nonrandomized controlled trial, we used a standardized phototest procedure to determine the effects of using sunscreen and antihistamine to control idiopathic solar urticaria....... The patients were then treated with a high-protection, broad-spectrum sunscreen and a nonsedative antihistamine alone and in combination and underwent similar phototesting. The use of sunscreen allowed the patients to tolerate much higher doses of UV radiation (32-38 times the MUD on untreated skin......). Antihistamine use did not increase the patients' MUD but did suppress wheal formation and itch, and only immediate erythema sharply located in the irradiated areas occurred. The combination of sunscreen and antihistamine acted synergistically and increased the tolerance to UV radiation markedly (80-267 times...

  20. TREATMENT OF ALLERGIC RHINITIS IN CHILDREN: SELECTION OF ANTIHISTAMINE DRUG AND NECESSITY OF FURTHER INVESTIGATIONS

    OpenAIRE

    A. V. Karaulov

    2013-01-01

    This literature review contains analysis of research results on treatment of allergic rhinitis in children according to the evidence-based medicine. Oral and intranasal antihistamine drugs along with intranasal steroids are the first-line drugs for treatment of allergic rhinitis, although the latter are more efficient in suppression of nasal stuffiness. First- and second-generation antihistamine agents used nowadays in medical practice are discussed in the article. The advantages of non-sedat...

  1. Comparative Effects of Antihistamines on Aircrew Performance of Simple and Complex Tasks Under Sustained Operations

    Science.gov (United States)

    1991-12-01

    PA. Spector, S.L. (1987). The pharmacology of antihistamines . Proceedings of Current Pharmacotherapy for Allergic Rhinitis and Urticaria. The Journal...Questionnaire. An ANOVA was conducted with the antihistamine questionnaire data. The results of comparisons for each symptom by drug, day, and session...281-282. Boggs, P.B. (1987). Clinical Experience with Terfenadine Worldwide Trials. Proceedings of Current Pharmacotherapy for Allergic Rhinitis and

  2. Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines

    Directory of Open Access Journals (Sweden)

    S Rico

    2009-08-01

    Full Text Available S Rico1,2, RM Antonijoan1,3, MJ Barbanoj1,2,31Centre d’lnvestigació de Medicaments, Institut de Recerca; Servei de Farmacologia Clínica, Hospital de la Santa Creu i Sant Pau, Barcelona, Spain; 2Departament de Farmacologia i Terapèutica, Universitat Autònoma de Barcelona, Barcelona, Spain; 3Centro de investigación Biomédica en Red de Salud Mental CIBERSAM, SpainAbstract: In 2003 a consensus group on new-generation antihistamines (CONGA defined the characteristics required for a third-generation H1 antihistamine as there had been much controversy about this issue since the early 1990s. One of the antihistamines that had been claimed to belong to such a group is the second-generation antihistamine, ebastine. The objective of this review is to analyze the pharmacology of ebastine, in light of the CONGA recommendations for the development of new-generation antihistamines: (1 anti-inflammatory properties, (2 potency, efficacy and effectiveness, (3 lack of cardiotoxicity, (4 lack of drug interactions, (5 lack of CNS effects, and (6 pharmacological approach. Ebastine seems to have anti-inflammatory properties that help to ameliorate nasal congestion, though this has not yet been conclusively demonstrated. Its pharmacological–therapeutic profile does not differ greatly from that of other second-generation antihistamines. Its cardiac safety has been widely assessed and no cardiac toxicity has been found at therapeutic doses despite initial concerns. The risk of potentially relevant drug interactions has been investigated and ruled out. Ebastine does not produce sedation at therapeutic doses and drug interaction studies with classical CNS depressants have not demonstrated a synergistic effect. Pharmacologically, ebastine is an H1 inverse agonist. Perhaps the answer to the quest for new-generation antihistamines lies not only in H1 but in a combined approach with other histamine receptors.Keywords: ebastine, antihistamines, third-generation, CONGA

  3. Usefulness of HeLa cells to evaluate inverse agonistic activity of antihistamines.

    Science.gov (United States)

    Mizuguchi, Hiroyuki; Ono, Shohei; Hattori, Masashi; Sasaki, Yohei; Fukui, Hiroyuki

    2013-03-01

    Antihistamines are thought to antagonize histamine and prevent it from binding to the histamine H1 receptor (H1R). However, recent studies indicate that antihistamines are classified into two groups, i.e., inverse agonists and neutral antagonists on the basis of their ability to down-regulate the constitutive activity of H1R. As H1R is an allergy-sensitive gene whose expression influences the severity of allergic symptoms, inverse agonists should more potently alleviate allergic symptoms than neutral antagonists by inhibiting H1R constitutive activity. Therefore, it is important to assess inverse agonistic activity of antihistamines. Here we report a novel assay method using HeLa cells expressing H1R endogenously for evaluation of inverse agonistic activity of antihistamines. Pretreatment with inverse agonists down-regulated H1R gene expression below to its basal level. On the other hand, basal H1R mRNA expression was unchanged by neutral antagonist pretreatment. Both inverse agonists and neutral antagonists suppressed histamine-induced H1R mRNA elevation. Classification of antihistamines on the basis of their suppressive activity of basal H1R gene expression was consistent with that of inositol phosphate accumulation in H1R-overexpressed cells. Our data suggest that the assay method using HeLa cells is more convenient and useful than the existing methods and may contribute to develop new antihistamines with inverse agonistic activity. Copyright © 2013 Elsevier B.V. All rights reserved.

  4. Molecular pharmacology of antihistamines in inhibition of oxidative burst of professional phagocytes.

    Science.gov (United States)

    Nosáľ, Radomír; Jančinová, Viera; Drábiková, Katarína; Perečko, Tomáš

    2015-04-01

    Antihistamines of the H₁and H₃/H₄groups interfere with oxidative burst of human professional phagocytes in vitro. In the concentration of 10 μM, H₁antihistamines of the 1st and 2nd generation inhibited oxidative burst of human neutrophils in the rank order of potency: dithiaden > loratadine > brompheniramine > chlorpheniramine > pheniramine. Of the H₁antihistamines, the most effective was dithiaden in suppressing oxidative burst of whole human blood and dose-dependently the chemiluminescence of isolated neutrophils at extra- and intracellular level. Inhibition of free oxygen radical generation in isolated neutrophils by dithiaden resulted from the inhibition of protein kinase C activation. The potentiation of recombinant caspase-3 by dithiaden is supportive of the antiinflammatory effect of dithiaden and suggestive of increasing the apoptosis of professional phagocytes. Of the H₃/H₄antihistamines, the most effective was JNJ7777120 in decreasing chemiluminescence in whole blood and also at extra- and intracellular sites of isolated neutrophils. JNJ 10191584 and thioperamide were less effective and the latter significantly potentiated free oxygen radical generation intracellularly. The results demonstrated that, compared with the H₃/H₄antihistamines investigated, H₁antihistamines were much more potent in inhibiting free oxygen radical generation in human professional phagocytes. This finding should be taken into account therapeutically.

  5. Histamine receptors and antihistamines: from discovery to clinical applications.

    Science.gov (United States)

    Cataldi, Mauro; Borriello, Francesco; Granata, Francescopaolo; Annunziato, Lucio; Marone, Gianni

    2014-01-01

    The synthesis and the identification of histamine marked a milestone in both pharmacological and immunological research. Since Sir Henry Dale and Patrick Laidlaw described some of its physiological effects in vivo in 1910, histamine has been shown to play a key role in the control of gastric acid secretion and in allergic disorders. Using selective agonists and antagonists, as well as molecular biology tools, four histamine receptors (H1R, H2R, H3R and H4R) have been identified. The Nobel Prize in Physiology and Medicine was awarded to Daniel Bovet in 1957 for the discovery of antihistamines (anti-H1R) and to Sir James Black in 1988 for the identification of anti-H2R antagonists. Anti-H1R and anti-H2R histamine receptor antagonists have revolutionized the treatment of certain allergic disorders and gastric acid-related conditions, respectively. More recently, anti-H3R antagonists have entered early-phase clinical trials for possible application in obesity and a variety of neurologic disorders. The preferential expression of H4R by several immune cells and its involvement in the development of allergic inflammation provide the rationale for the use of anti-H4R antagonists in allergic and in other immune-related disorders. © 2014 S. Karger AG, Basel.

  6. Balanced discussion of second-generation antihistamines' data

    Directory of Open Access Journals (Sweden)

    Boev R

    2016-11-01

    Full Text Available Rossen Boev,1 Jürgen WG Bentz2 1UCB Pharma, Bulle, Switzerland; 2UCB Pharma, Brussels, Belgium It is with interest that we read the paper “Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine” by Wang et al1, in which the authors provide insights into the burden of allergic diseases in the Asia-Pacific region. Unfortunately, we found that the review provides some unsubstantiated information, incorrect statements, and/or data inconsistencies as listed below.The abstract states that bilastine “has very low potential for drug–drug interactions”; however, the drug label lists interactions with ketoconazole, erythromycin, diltiazem, and other intestinal efflux transporters, leading to 2–3-fold increases in drug maximum serum concentration and area under the curve2. Also, food interactions decrease bilastine’s bioavailability by 30%, and the label recommendation is that it is taken 1 hour before or 2 hours after intake of food or fruit juice2. View the original article by Wang et al.

  7. Second-generation H1-antihistamines in chronic urticaria: an evidence-based review.

    Science.gov (United States)

    Kavosh, Eric R; Khan, David A

    2011-12-01

    The effects of urticaria are predominantly mediated by histamine release; therefore, H1-antihistamines are the mainstay of treatment. Second-generation H1-antihistamines, compared with their first-generation counterparts, have demonstrated improved peripheral H1-receptor selectivity and decreased lipophilicity (which minimizes CNS adverse effects), and antiallergic properties in addition to being histamine inverse agonists. Evidence of clinical efficacy and tolerability of second-generation H1-antihistamines available in the US for the treatment of chronic urticaria (CU) was analyzed using the GRADE system to develop the strength of recommendations for particular therapies. The evidence for the safety and efficacy of the majority of second-generation H1-antihistamines available in the US is of high quality and leads to a strong recommendation for their use in CU. There is a limited amount of data of variable quality comparing the efficacy between various second-generation H1-antihistamines in CU leading to weak recommendations for using cetirizine over fexofenadine and levocetirizine over desloratadine. Limited data of variable quality exist for the efficacy of higher doses of second-generation H1-antihistamines in CU patients not responsive to standard doses. These limited data lead to a strong recommendation that higher than recommended doses of fexofenadine do not offer greater efficacy in control of CU and a weak recommendation that higher doses of levocetirizine and desloratadine are more effective in CU unresponsive to standard doses. More studies of higher quality are required to make any firm recommendations regarding second-generation H1-antihistamines in the treatment of physical urticarias. All second-generation H1-antihistamines appear to be very well tolerated in CU patients, with rare reports of adverse effects. Due to the relatively large gaps in the quantity and quality of evidence, particularly for choice of H1-antihistamines, use of higher doses

  8. Comparison of antileukotrienes and antihistamines in the treatment of allergic rhinitis.

    Science.gov (United States)

    Ho, Ching-Yin; Tan, Ching-Ting

    2007-01-01

    The aim of this study was to compare the effect of antileukotriene (anti-LT), antihistamine, and a combination of anti-LT and antihistamine on the symptoms and nasal resistance in allergic rhinitis patients. We performed a placebo-controlled study, with 120 persistent, moderate to severe allergic rhinitis patients randomly selected to receive the different treatments for 4 weeks: no treatment, 10 mg of cetirizine once per day, 20 mg of zafirlukast once per day, 20 mg of cafirlukast twice per day, a combination of 20 mg of zafirlukast and 10 mg of cetirizine once per day, or a combination of 20 mg of zafirlukast twice per day and 10 mg cetirizine once per day. The nasal secretion nitric oxide (NO) concentration, nasal symptom score, and nasal resistance were measured before and after treatment. Total symptom scores improved in each treated group compared with the control group (p antihistamine significantly improved allergy symptoms compared with no treatment, low-dose anti-LT, or antihistamine alone (p antihistamine can effectively treat allergic rhinitis.

  9. High-dose anti-histamine use and risk factors in children with urticaria

    Science.gov (United States)

    Uysal, Pınar; Avcil, Sibelnur; Erge, Duygu

    2016-01-01

    Aim The drugs of choice in the treatment of urticaria in children are H1-antihistamines. The aim of the study was to evaluate children with urticaria and define risk factors for requirement of high-dose H1-antihistamines in children with urticaria. Material and Methods The medical data of children who were diagnosed as having urticaria admitted to our outpatient clinic between January 2014 and January 2016 were searched. The medical histories, concomitant atopic diseases, parental atopy histories, medications, treatment responses, blood eosinophil and basophil counts, and serum total IgE levels were recorded. In addition, the urticaria activity score for seven days, autoimmune antibody tests, and skin prick test results were evaluated in children with chronic urticaria. Results The numbers of the children with acute and chronic urticaria were 138 and 92, respectively. The age of the children with chronic urticaria was higher than that of those with acute urticaria (p0.05). There was a negative correlation between blood eosinophil count and the UAS7 score in children with chronic urticaria (r=−0.276, p=0.011). Chronic urticaria and requirement of high dose H1-antihistamines were significant in children aged ≥10 years (purticaria. Conclusion The requirement of high-dose H1-antihistamines was higher with children’s increasing age. Disease severity and basopenia were risk factors for the requirement of high-dose H1-antihistamines. PMID:28123332

  10. Histamine H1Receptor Gene Expression and Drug Action of Antihistamines.

    Science.gov (United States)

    Fukui, Hiroyuki; Mizuguchi, Hiroyuki; Nemoto, Hisao; Kitamura, Yoshiaki; Kashiwada, Yoshiki; Takeda, Noriaki

    2017-01-01

    The upregulation mechanism of histamine H 1 receptor through the activation of protein kinase C-δ (PKCδ) and the receptor gene expression was discovered. Levels of histamine H 1 receptor mRNA and IL-4 mRNA in nasal mucosa were elevated by the provocation of nasal hypersensitivity model rats. Pretreatment with antihistamines suppressed the elevation of mRNA levels. Scores of nasal symptoms were correlatively alleviated to the suppression level of mRNAs above. A correlation between scores of nasal symptoms and levels of histamine H 1 receptor mRNA in the nasal mucosa was observed in patients with pollinosis. Both scores of nasal symptoms and the level of histamine H 1 receptor mRNA were improved by prophylactic treatment of antihistamines. Similar to the antihistamines, pretreatment with antiallergic natural medicines showed alleviation of nasal symptoms with correlative suppression of gene expression in nasal hypersensitivity model rats through the suppression of PKCδ. Similar effects of antihistamines and antiallergic natural medicines support that histamine H 1 receptor-mediated activation of histamine H 1 receptor gene expression is an important signaling pathway for the symptoms of allergic diseases. Antihistamines with inverse agonist activity showed the suppression of constitutive histamine H 1 receptor gene expression, suggesting the advantage of therapeutic effect.

  11. Prediction of the Efficacy of Antihistamines in Chronic Spontaneous Urticaria Based on Initial Suppression of the Histamine- Induced Wheal.

    Science.gov (United States)

    Sánchez, J; Zakzuk, J; Cardona, R

    2016-01-01

    Antihistamines are the first line of treatment for chronic spontaneous urticaria. However, there is no effective method to predict whether an antihistamine will have a beneficial clinical effect or not. To assess whether the change in histamine-induced wheal and flare measurements 24 hours after administration of antihistamine can predict the efficacy of treatment. We performed a multicenter, triple-blind, randomized study. Patients received a daily oral dose of cetirizine, fexofenadine, bilastine, desloratadine, or ebastine over 8 weeks. After 4 weeks, a higher dose of antihistamine was administered to patients who did not experience a clinical response. A histamine skin prick test was carried out at baseline and 24 hours after the first dose of antihistamine. Disease severity (Urticaria Activity Score [UAS]), response to the histamine skin prick test, and impact on the patient's quality of life (Dermatology Life Quality Index [DLQI]) were determined every 2 weeks. The study population comprised 150 patients (30 per group) and 30 controls. Twenty-four hours after administration of antihistamine, inhibition of the histamine wheal by >75% was significantly associated with better UAS and DLQI scores. The safety and efficacy of the 5 antihistamines were similar. After updosing, rates of disease control (DLQI score antihistamines but has limited utility for identifying nonresponders. The clinical significance of these data could be relevant in the search for new urticaria treatment regimens.

  12. TREATMENT OF ALLERGIC RHINITIS IN CHILDREN: SELECTION OF ANTIHISTAMINE DRUG AND NECESSITY OF FURTHER INVESTIGATIONS

    Directory of Open Access Journals (Sweden)

    A. V. Karaulov

    2013-01-01

    Full Text Available This literature review contains analysis of research results on treatment of allergic rhinitis in children according to the evidence-based medicine. Oral and intranasal antihistamine drugs along with intranasal steroids are the first-line drugs for treatment of allergic rhinitis, although the latter are more efficient in suppression of nasal stuffiness. First- and second-generation antihistamine agents used nowadays in medical practice are discussed in the article. The advantages of non-sedative 2d-genereation antihistamine drugs, especially so called active metabolites (fexofenadine, cetirizine, levocetirizine, desloratadine are emphasized. The data on loratadine and desloratadine as ones of the most effective drugs in childhood allergic rhinitis are shown in detail. The possible directions for the further investigations in order to provide effective control over allergic inflammation in children resistant to medicinal agents are discussed.

  13. Seizures induced by desloratadine, a second-generation antihistamine: clinical observations.

    Science.gov (United States)

    Cerminara, Caterina; El-Malhany, Nadia; Roberto, Denis; Lo Castro, Adriana; Curatolo, Paolo

    2013-08-01

    Some clinical experiences indicate that H1-antihistamines, especially first-generation H1-antagonists, occasionally provoke convulsions in healthy children as well as epileptic patients. Desloratadine is a frequently used second-generation antihistamine considered to be effective and safe for the treatment of allergic diseases. We describe four children who experienced epilepsy associated with the nonsedating H(1)-antagonist desloratadine and discuss the neurophysiologic role of the central histaminergic system in seizure susceptibility. In conclusion, we recommend caution in treating epileptic patients with the histamine H(1)-antagonists, including second- and third-generation drugs that are frequently referred because they are considered to be nonsedating antihistamines. Georg Thieme Verlag KG Stuttgart · New York.

  14. Synergistic effect of broad-spectrum Sunscreens and antihistamines in the control of idiopathic solar urticaria

    DEFF Research Database (Denmark)

    Faurschou, A.; Wulf, Hans Chr.

    2008-01-01

    . Observations: Three patients with idiopathic solar urticaria underwent phototesting with UV-B and UV-A radiation. The minimal urticarial dose (MUD) was determined 15 minutes after irradiation. The patients were subsequently tested with 5 times the MUD, and the reaction was graded every minute for 15 minutes....... The patients were then treated with a high-protection, broad-spectrum sunscreen and a nonsedative antihistamine alone and in combination and underwent similar phototesting. The use of sunscreen allowed the patients to tolerate much higher doses of UV radiation (32-38 times the MUD on untreated skin......). Antihistamine use did not increase the patients' MUD but did suppress wheal formation and itch, and only immediate erythema sharply located in the irradiated areas occurred. The combination of sunscreen and antihistamine acted synergistically and increased the tolerance to UV radiation markedly (80-267 times...

  15. Role of leukotriene antagonists and antihistamines in the treatment of allergic rhinitis.

    Science.gov (United States)

    Cobanoğlu, Bengü; Toskala, Elina; Ural, Ahmet; Cingi, Cemal

    2013-04-01

    Allergic rhinitis is the most common atopic disorder seen in ENT clinics. It is diagnosed by history, physical exam and objective testing. Patient education, environmental control measures, pharmacotherapy, and allergen-specific immunotherapy are the cornerstones of allergic rhinitis treatment and can significantly reduce the burden of disease. Current treatment guidelines include antihistamines, intranasal corticosteroids, oral and intranasal decongestants, intranasal anticholinergics, intranasal cromolyn, and leukotriene receptor antagonists. In the mechanism of allergic rhinitis, histamine is responsible for major allergic rhinitis symptoms such as rhinorrhea, nasal itching and sneezing. Its effect on nasal congestion is less evident. In contrast, leukotrienes result in increase in nasal airway resistance and vascular permeability. Antihistamines and leukotriene receptor antagonists are commonly used in the treatment of allergic rhinitis. The published literature about combined antihistamines and leukotriene antagonists in mono- or combination therapy is reviewed and presented.

  16. Adverse drug reactions of systemic antihistamines in children in the Netherlands.

    Science.gov (United States)

    de Vries, Tjalling W; van Hunsel, Florence

    2016-10-01

    Antihistamines are used for the treatment of allergic rhinitis, allergic conjunctivitis, chronic spontaneous urticaria and atopic eczema. To study the reports of adverse drug reactions (ADRs) in children using antihistamines to provide prescribers with an overview of the possible toxicity. We studied ADRs in children reported to the Netherlands Pharmacovigilance Centre Lareb in the years 1991-2014, assessed the Naranjo score and, when possible, computed the reporting OR. Serious ADRs included one death (malignant neuroleptic syndrome), cardiac arrhythmia (one case) and convulsions (three cases). Skin eruptions, headache and somnolence were the most frequently reported ADRs. Aggression and agitation were also reported. Toxicity can occur with second-generation antihistamines. The main toxicity relates to skin eruptions and central nervous system problems. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://www.bmj.com/company/products-services/rights-and-licensing/

  17. Relative Efficacy of Seven Common H1 Receptor Antagonist Antihistamines in Chronic Idiopathic Urticaria

    Directory of Open Access Journals (Sweden)

    Mohan Singh

    1987-01-01

    Full Text Available The order of clinical potency of seven Hi receptor antagonist antihistamines in usual therapeutic doses was evaluated in 30 patients of chronic idiopathic urticaria by a double blind, placebo controlled trial utilizing a self-assessment method. The analysis of mean whealing and, itching scores established a potency sequence in the -decreasing order of cyproheptidine, hydroxyzine, chlorpheniramine, embramine, promethazine, dimeth′mdene and dexchlorpheniramme. The differences between the first five antihistamines were not statistically significant, though these were superior to ddxchlorpheniralmine and placebo. Dexchlorpheniramine was statistically better than placebo.

  18. The future antihistamines: histamine H3 and H4 receptor ligands.

    Science.gov (United States)

    Yu, Fuqu; Bonaventure, Pascal; Thurmond, Robin L

    2010-01-01

    The field of histamine research has progressed far from a century ago when the first biological functions of histamine were identified. It is now known that histamine function is mediated by four histamine receptors, which belong to the G-protein-coupled receptor family. While antihistamines that target the first two receptors have enjoyed clinical and commercial success, efforts to find new antihistamines against the histamine H3 and H4 receptors are still in the early stages. Here we will review the therapeutic potential of targeting these new histamine receptors.

  19. Comparison of first- and second-generation antihistamine prescribing in elderly outpatients: A health insurance database study in 2013.

    Science.gov (United States)

    Lee, Young-Mi; Song, Inmyung; Lee, Eui-Kyung; Shin, Ju-Young

    2017-10-01

    This descriptive study analyzed the scale of first- and second-generation antihistamine prescription in elderly outpatients in Korea and the characteristics associated with this prescription. We conducted a drug utilization study using the Korea Health Insurance Review and Assessment Service-Aged Patient Sample (HIRA-APS) database from January 1 to December 31, 2013. The study subjects were elderly outpatients aged 65 years and older who were prescribed antihistamines. The study drugs included 6 first-generation and 16 second-generation antihistamines. The prescription pattern of first-generation antihistamines was based on region, diagnosis, and clinical specialty. Multivariate logistic regression analysis was used to determine the factors associated with first-generation antihistamine prescription. Odds ratios (ORs) with 95% confidence interval (CI) were calculated. A total of 1,152,556 elderly outpatients were identified as having visited various medical facilities in 2013, of which 23.4% received at least one prescription for first-generation antihistamine monotherapy. First-generation antihistamines were more likely to be prescribed in secondary care hospitals (OR = 1.74; 95% CI 1.69 - 1.78) than in tertiary care hospitals, and in urban areas (OR = 1.21; 95% CI 1.20 - 1.21) than in the Seoul metropolitan area. First-generation antihistamines were also more likely to be prescribed for treating the common cold (OR = 1.06; 95% CI 1.05 - 1.06) than any other disease. A large proportion (23.4%) of elderly outpatients in Korea received prescriptions for first-generation antihistamines. Efforts to reduce prescriptions of first-generation antihistamines are recommended, especially prescriptions associated with common cold diagnosis in secondary care hospitals and in urban areas.
.

  20. Comparative Evaluation of the Efficacy in Treating Children with Seasonal Allergic Rhinitis Using Antihistamine Combined with Ectoine Nasal Spray and Antihistamine Monotherapy: Results of an Open Randomized Study

    Directory of Open Access Journals (Sweden)

    N. V. Minaeva

    2015-01-01

    Full Text Available Objective: Our aim was to evaluate the efficacy of an ectoine nasal spray in treating children with seasonal allergic rhinitis.Methods: An open randomized study of children aged 3–17 with the aggravation of early spring hay fever. All participants received oral antihistamine, and the children of the treatment group — oral antihistamine plus ectoine nasal spray. The symptoms of the disease and the amount of additional drug therapy were analyzed on the 1st, 10th and 21st day of treatment. Results: The group with patients who received an ectoine nasal spray (n = 24 showed a significant, if compared to the control group (n = 18, decrease in the severity of all symptoms of rhinitis — nasal congestion from the 14th day of treatment (p = 0.010, nasal discharge — from the 15th day of treatment (p = 0.036, nasal irritation and sneezing — from the 17th day of treatment (p = 0.020, as well as the symptoms of allergic conjunctivitis such as itchy eyes — from the 18th day of treatment (p = 0.020 and conjunctival hyperemia — from the 19th day of treatment (p = 0.040. The use of an ectoine nasal spray was accompanied by a decrease in the frequency of the assignment of drugs for the additional rhinitis treatment.Conclusion: An ectoine nasal spray in combination with antihistamines induces a more rapid relief of major symptoms of seasonal allergic rhinitis and allergic conjunctivitis in children, as well as reduces the need for additional medical treatment of the disease, if compared to the antihistamine monotherapy.

  1. Chemical constituents and antihistamine activity of Bixa orellana leaf extract

    Directory of Open Access Journals (Sweden)

    Yong Yoke Keong

    2013-02-01

    Full Text Available Abstract Background Bixa orellana L. has been traditionally used in Central and South America to treat a number of ailments, including internal inflammation, and in other tropical countries like Malaysia as treatment for gastric ulcers and stomach discomfort. The current study aimed to determine the major chemical constituents of the aqueous extract of B. orellana (AEBO and to evaluate the antihistamine activity of AEBO during acute inflammation induced in rats. Methods Acute inflammation was produced by subplantar injection of 0.1 mL of 0.1% histamine into the right hind paw of each rat in the control and treatment groups. The degree of edema was measured before injection and at the time points of 30, 60, 120, 180, 240 and 300 min after injection. Changes of peritoneal vascular permeability were studied using Evans blue dye as a detector. Vascular permeability was evaluated by the amount of dye leakage into the peritoneal cavity in rats. To evaluate the inhibitory effect of AEBO on biochemical mediators of vascular permeability, the levels of nitric oxide (NO and vascular endothelial growth factor (VEGF were determined in histamine-treated paw tissues. The major constituents of AEBO were determined by gas chromatography–mass spectrometry (GC-MS analysis. Results AEBO produced a significant inhibition of histamine-induced paw edema starting at 60 min time point, with maximal percentage of inhibition (60.25% achieved with a dose of 150 mg/kg of AEBO at 60 min time point. Up to 99% of increased peritoneal vascular permeability produced by histamine was successfully suppressed by AEBO. The expression of biochemical mediators of vascular permeability, NO and VEGF, was also found to be downregulated in the AEBO treated group. Gas chromatography–mass spectrometry (GC-MS analysis revealed that the major constituent in AEBO was acetic acid. Conclusions The experimental findings demonstrated that the anti-inflammatory activity of AEBO was

  2. Effect of H1-antihistamines on the oxidative burst of rat phagocytes

    Czech Academy of Sciences Publication Activity Database

    Králová, Jana; Číž, Milan; Nosál, R.; Drábiková, K.; Lojek, Antonín

    2006-01-01

    Roč. 55, č. 1 (2006), S15-S16 ISSN 1023-3830 R&D Projects: GA ČR(CZ) GA305/04/0896 Institutional research plan: CEZ:AV0Z50040507 Keywords : H1-antihistamines * reactive oxygen species * phagocytes Subject RIV: BO - Biophysics Impact factor: 1.485, year: 2006

  3. Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines.

    Science.gov (United States)

    Stahl, Stephen M

    2008-12-01

    Numerous "antihistamines" as well as various psychotropic medications with antihistamine properties are widely utilized to treat insomnia. Over-the-counter sleep aids usually contain an antihistamine and various antidepressants and antipsychotics with antihistamine properties have sedative-hypnotic actions. Although widely used for the treatment of insomnia, many agents that block the histamine H1 receptor are also widely considered to have therapeutic limitations, including the development of next-day carryover sedation, as well as problems with chronic use, such as the development of tolerance to sedative-hypnotic actions and weight gain. Although these clinical actions are classically attributed to blockade of the H1 receptor, recent findings with H1 selective agents and H1 selective dosing of older agents are challenging these notions and suggest that some of the clinical limitations of current H1-blocking agents at their currently utilized doses could be attributable to other properties of these drugs, especially to their simultaneous actions on muscarinic, cholinergic, and adrenergic receptors. Selective H1 antagonism is emerging as a novel approach to the treatment of insomnia, without tolerance, weight gain, or the need for the restrictive prescription scheduling required of other hypnotics.

  4. Non-sedating antihistamine drugs and cardiac arrhythmias : biased risk estimates from spontaneous reporting systems?

    NARCIS (Netherlands)

    De Bruin, M L; van Puijenbroek, E P; Egberts, A C G; Hoes, A W; Leufkens, H G M

    AIMS: This study used spontaneous reports of adverse events to estimate the risk for developing cardiac arrhythmias due to the systemic use of non-sedating antihistamine drugs and compared the risk estimate before and after the regulatory action to recall the over-the-counter status of some of these

  5. Anti-inflammatory and Antihistaminic Study of a Unani Eye Drop Formulation

    Directory of Open Access Journals (Sweden)

    Latif Abdul

    2010-03-01

    Full Text Available The Unani eye drop is an ophthalmic formulation prepared for its beneficial effects in the inflammatory and allergic conditions of the eyes. In the present study, the Unani eye drop formulation was prepared and investigated for its anti-inflammatory and antihistaminic activity, using in vivo and in vitro experimental models respectively. The Unani eye drop formulation exhibited significant anti-inflammatory activity in turpentine liniment-induced ocular inflammation in rabbits. The preparation also showed antihistaminic activity in isolated guinea-pig ileum. The anti-inflammatory and antihistaminic activity of eye drop may be due to presence of active ingredients in the formulation. Although there are many drugs in Unani repository which are mentioned in classical books or used in Unani clinical practice effectively in treatment of eye diseases by various Unani physicians. Inspite of the availability of vast literature, there is a dearth of commercial Unani ocular preparations. So, keeping this in mind, the eye drop formulation was prepared and its anti-inflammatory and antihistaminic activity was carried out in animal models. Thus, in view of the importance of alternative anti-inflammatory and anti- allergic drugs, it becomes imperative to bring these indigenous drugs to the front foot and evaluate their activities.

  6. Assessment of type of allergy and antihistamine use in the development of glioma

    Science.gov (United States)

    McCarthy, Bridget J.; Rankin, Kristin; Il'yasova, Dora; Erdal, Serap; Vick, Nicholas; Ali-Osman, Francis; Bigner, Darell D.; Davis, Faith

    2010-01-01

    Background Allergies have been associated with decreased risk of glioma, but associations between duration and timing of allergies, and antihistamine use and glioma risk have been less consistent. The objective was to investigate this association by analyzing types, number, years since diagnosis, and age at diagnosis of allergies, and information on antihistamine usage, including type, duration, and frequency of exposure. Methods Self-report data on medically-diagnosed allergies and antihistamine use were obtained for 419 glioma cases and 612 hospital-based controls from Duke University and NorthShore University HealthSystem. Results High- and low-grade glioma cases were statistically significantly less likely to report any allergy than controls (OR= 0.66, 95% CI: 0.49–0.87 and 0.44, 95% CI: 0.25–0.76, respectively). The number of types of allergies (seasonal, medication, pet, food, and other) was inversely associated with glioma risk in a dose-response manner (p-value for trend Impact A comprehensive study of allergies and antihistamine use using standardized questions and biological markers will be essential to further delineate the biological mechanism that may be involved in brain tumor development. PMID:21300619

  7. Effectiveness and safety of antihistamines up to fourfold or higher in treatment of chronic spontaneous urticaria

    NARCIS (Netherlands)

    van den Elzen, Mignon T; van Os-Medendorp, Harmieke; van den Brink, Imke; van den Hurk, Karin; Kouznetsova, Ouliana I; Lokin, Alexander S H J; Laheij-de Boer, Anna-Marijke; Röckmann, Heike; Bruijnzeel-Koomen, Carla A F M; Knulst, André C

    2017-01-01

    Background: Treatment with second-generation antihistamines is recommended in patients with chronic spontaneous urticaria (CSU). Some patients remain unresponsive even after up-dosing up to fourfold. Many third line treatment options have limited availability and/or give rise to significant side

  8. A survey of the factors associated with concerns about oral antihistamine use in Japanese pruritic skin disease patients.

    Science.gov (United States)

    Moriue, Junko; Yoneda, Kozo; Nakai, Kozo; Hosokawa, Yoichiro; Moriue, Tetsuya; Kubota, Yasuo

    2013-12-01

    To improve health outcomes during the treatment for pruritic skin diseases, it is important to understand which factors most influence patients' concerns about oral antihistamine drugs. To survey the nature of patients' concerns about oral antihistamine drugs and to examine the factors associated with them. Patients with pruritic skin diseases expressed their concerns regarding the use of oral antihistamine drugs. The independent effects of the patients' background characteristics on their concerns were examined by multiple logistic regression analysis. A total of 291 outpatients were completed the study. Overall, 32% of patients were worried about using oral antihistamine drugs. The most common concern was about their adverse drug events (except drowsiness) and the effects of long-term use. Overall, being concerned about antihistamine use was found to be significantly and independently associated with a younger age, severe itching, being a homemaker, and having previous personal experience of embarrassment due to drowsiness caused by taking over-the-counter drugs. Several factors are associated with altered self-reported concerns about antihistamines. Our results suggest the importance of understanding the nature of patients' fears about oral antihistamine use so that sound advice can be offered to them in a timely manner.

  9. Antihistamines modulate the integrin signaling pathway in h9c2 rat cardiomyocytes: Possible association with cardiotoxicity.

    Science.gov (United States)

    Yun, J S; Kim, S Y

    2015-08-01

    The identification of biomarkers for toxicity prediction is crucial for drug development and safety evaluation. The selective and specific biomarkers for antihistamines-induced cardiotoxicity is not well identified yet. In order to evaluate the mechanism of the life-threatening effects caused by antihistamines, we used DNA microarrays to analyze genomic profiles in H9C2 rat cardiomyocytes that were treated with antihistamines. The gene expression profiles from drug-treated cells revealed changes in the integrin signaling pathway, suggesting that cardiac arrhythmias induced by antihistamine treatment may be mediated by changes in integrin-mediated signaling. It has been reported that integrin plays a role in QT prolongation that may induce cardiac arrhythmia. These results indicate that the integrin-mediated signaling pathway induced by antihistamines is involved in various biological mechanisms that lead to cardiac QT prolongation. Therefore, we suggest that genomic profiling of antihistamine-treated cardiomyocytes has the potential to reveal the mechanism of adverse drug reactions, and this signal pathway is applicable to prediction of in vitro cardiotoxicity induced by antihistamines as a biomarker candidate. © The Author(s) 2014.

  10. Blood-brain barrier in vitro models as tools in drug discovery: assessment of the transport ranking of antihistaminic drugs.

    Science.gov (United States)

    Neuhaus, W; Mandikova, J; Pawlowitsch, R; Linz, B; Bennani-Baiti, B; Lauer, R; Lachmann, B; Noe, C R

    2012-05-01

    In the course of our validation program testing blood-brain barrier (BBB) in vitro models for their usability as tools in drug discovery it was evaluated whether an established Transwell model based on porcine cell line PBMEC/C1-2 was able to differentiate between the transport properties of first and second generation antihistaminic drugs. First generation antihistamines can permeate the BBB and act in the central nervous system (CNS), whereas entry to the CNS of second generation antihistamines is restricted by efflux pumps such as P-glycoprotein (P-gP) located in brain endothelial cells. P-gP functionality of PBMEC/C1-2 cells grown on Transwell filter inserts was proven by transport studies with P-gP substrate rhodamine 123 and P-gP blocker verapamil. Subsequent drug transport studies with the first generation antihistamines promethazine, diphenhydramine and pheniramine and the second generation antihistamines astemizole, ceterizine, fexofenadine and loratadine were accomplished in single substance as well as in group studies. Results were normalised to diazepam, an internal standard for the transcellular transport route. Moreover, effects after addition of P-gP inhibitor verapamil were investigated. First generation antihistamine pheniramine permeated as fastest followed by diphenhydramine, diazepam, promethazine and second generation antihistaminic drugs ceterizine, fexofenadine, astemizole and loratadine reflecting the BBB in vivo permeability ranking well. Verapamil increased the transport rates of all second generation antihistamines, which suggested involvement of P-gP during their permeation across the BBB model. The ranking after addition of verapamil was significantly changed, only fexofenadine and ceterizine penetrated slower than internal standard diazepam in the presence of verapamil. In summary, permeability data showed that the BBB model based on porcine cell line PBMEC/C1-2 was able to reflect the BBB in vivo situation for the transport of

  11. High-dose anti-histamine use and risk factors in children with urticaria.

    Science.gov (United States)

    Uysal, Pınar; Avcil, Sibelnur; Erge, Duygu

    2016-12-01

    The drugs of choice in the treatment of urticaria in children are H1-antihistamines. The aim of the study was to evaluate children with urticaria and define risk factors for requirement of high-dose H1-antihistamines in children with urticaria. The medical data of children who were diagnosed as having urticaria admitted to our outpatient clinic between January 2014 and January 2016 were searched. The medical histories, concomitant atopic diseases, parental atopy histories, medications, treatment responses, blood eosinophil and basophil counts, and serum total IgE levels were recorded. In addition, the urticaria activity score for seven days, autoimmune antibody tests, and skin prick test results were evaluated in children with chronic urticaria. The numbers of the children with acute and chronic urticaria were 138 and 92, respectively. The age of the children with chronic urticaria was higher than that of those with acute urticaria (p0.05). There was a negative correlation between blood eosinophil count and the UAS7 score in children with chronic urticaria (r=-0.276, p=0.011). Chronic urticaria and requirement of high dose H1-antihistamines were significant in children aged ≥10 years (p<0.001, p=0.015). High UAS7 score (OR: 1.09; CI 95%: [1.03-1.15]) and basopenia (OR: 6.77; CI 95%: [2.01-22.75]) were associated with the requirement of high-dose H1-AH in children with chronic urticaria. The requirement of high-dose H1-antihistamines was higher with children's increasing age. Disease severity and basopenia were risk factors for the requirement of high-dose H1-antihistamines.

  12. A comparison of the clinical efficacy and safety of intranasal fluticasone propionate and antihistamines in the treatment of rhinitis.

    Science.gov (United States)

    Foresi, A

    2000-01-01

    Adequate management of allergic rhinitis is needed to avoid its considerable adverse social, clinical, and economic impact. Both topical intranasal steroids and oral or topical antihistamines are recognised as effective treatments for this condition. In comparative studies, however, intranasal steroids and, in particular, fluticasone propionate aqueous nasal spray (FPANS), have afforded consistently better symptomatic relief, and have a greater beneficial effect on quality of life. Furthermore, the addition of an antihistamine to FPANS therapy has generally produced little further benefit. Intranasal administration is associated with a low systemic absorption of fluticasone propionate and, following regular use of FPANS, placebo, or an oral antihistamine, no significant differences were seen between treatment groups in plasma or urinary cortisol. Overall, therefore, the data indicate that FPANS is superior to second-generation antihistamines in the management of allergic rhinitis.

  13. Pro-arrhythmic potential of oral antihistamines (H1): combining adverse event reports with drug utilization data across Europe.

    Science.gov (United States)

    Poluzzi, Elisabetta; Raschi, Emanuel; Godman, Brian; Koci, Ariola; Moretti, Ugo; Kalaba, Marija; Wettermark, Bjorn; Sturkenboom, Miriam; De Ponti, Fabrizio

    2015-01-01

    There is appreciable utilisation of antihistamines (H1) in European countries, either prescribed by physician and purchased by patients for self-medication. Terfenadine and astemizole underwent regulatory restrictions in '90 because of their cardiac toxicity, but only scarce clinical data are available on other antihistamines. To investigate the pro-arrhythmic potential of antihistamines by combining safety reports of the FDA Adverse Event Reporting System (FAERS) with drug utilization data from 13 European Countries. We identified signals of antihistamine arrhythmogenic potential by analyzing FAERS database for all cases of Torsades de Pointes (TdP), QT abnormalities (QTabn), ventricular arrhythmia (VA) and sudden cardiac death/cardiac arrest (SCD/CA). Number of cases ≥3 and disproportionality were used to define alert signals: TdP and QTabn identified stronger signals, whereas SCD/CA identified weaker signals. Drug utilization data from 2005 to 2010 were collected from administrative databases through health authorities and insurance. Antihistamines were reported in 109 cases of TdP/QT prolongation, 278 VA and 610 SCD/CA. Five agents resulted in stronger signals (cetirizine, desloratadine, diphenhydramine, fexofenadine, loratadine) and 6 in weaker signals (alimemazine, carbinoxamine, cyclizine, cyproeptadine, dexchlorpheniramine and doxylamine). Exposure to antihistamines with stronger signal was markedly different across European countries and was at least 40% in each Country. Cetirizine was >29 Defined Daily Doses per 1000 inhabitants per day (DID) in Norway, desloratadine >11 DID in France and loratadine >9 DID in Sweden and Croatia. Drugs with weaker signals accounted for no more than 10% (in Sweden) and in most European countries their use was negligible. Some second-generation antihistamines are associated with signal of torsadogenicity and largely used in most European countries. Although confirmation by analytical studies is required, regulators and

  14. Early pregnancy exposure to antihistamines and risk of congenital heart defects: results of two case-control studies.

    Science.gov (United States)

    Smedts, Huberdina P M; de Jonge, Linda; Bandola, Sarah J G; Baardman, Marlies E; Bakker, Marian K; Stricker, Bruno H C; Steegers-Theunissen, Régine P M

    2014-09-01

    We aimed to study the association between use of antihistamines in early pregnancy and congenital heart defects (CHD) in the offspring. Two case-control studies. HAVEN study, Erasmus MC, University Medical Centre, Rotterdam, and Eurocat Northern Netherlands (NNL), University Medical Center Groningen, Groningen, the Netherlands. We studied 361 children with CHD and 410 controls without congenital malformations from the HAVEN study and replicated the analyses in 445 children with CHD and 530 controls from the Eurocat NNL registry. Information about antihistamine use in early pregnancy and potential confounders was obtained from questionnaires postpartum. We calculated the association between antihistamines and CHD risk by multivariable logistic regression analysis. Odds ratios (OR) with 95% confidence intervals (CI). In the HAVEN study, 25 of 771 mothers used antihistamines that were associated with an increased CHD risk (OR 3.0, 95% CI 1.2-7.3), particularly atrioventricular septal defects (AVSD) (OR 5.1, 95 % CI 1.3-20.5) and perimembranous ventricular septal defects (pVSD) (OR 5.1, 95% CI 1.8-14.4). Mothers with severe nausea who did not use antihistamines had a reduced risk (OR 0.7, 95% CI 0.5-0.98), whereas nauseous mothers using antihistamines showed an almost fivefold increased risk of pVSD (OR 4.8, 95% CI 1.1-21.8). The association between antihistamines and AVSD was confirmed in the Eurocat cohort (OR 3.5, 95% CI 1.4-8.7), but we could not replicate the association with overall CHD risk. We found a positive association between antihistamine use in early pregnancy and CHD risk, particularly AVSD, which seemed to be independent of nausea/vomiting.

  15. Analysis of pharmaceutical preparations containing antihistamine drugs by micellar liquid chromatography.

    Science.gov (United States)

    Martínez-Algaba, C; Bermúdez-Saldaña, J M; Villanueva-Camañas, R M; Sagrado, S; Medina-Hernández, M J

    2006-02-13

    Rapid chromatographic procedures for analytical quality control of pharmaceutical preparations containing antihistamine drugs, alone or together with other kind of compounds are proposed. The method uses C18 stationary phases and micellar mobile phases of cetyltrimethylammonium bromide (CTAB) with either 1-propanol or 1-butanol as organic modifier. The proposed procedures allow the determination of the antihistamines: brompheniramine, chlorcyclizine, chlorpheniramine, diphenhydramine, doxylamine, flunarizine, hydroxyzine, promethazine, terfenadine, tripelennamine and triprolidine, in addition to caffeine, dextromethorphan, guaifenesin, paracetamol and pyridoxine in different pharmaceutical presentations (tablets, capsules, suppositories, syrups and ointments). The methods require minimum handling sample and are rapid (between 3 and 12 min at 1 mLmin(-1) flow rate) and reproducible (R.S.D. values<5%). Limits of detection are lower than 1 microgmL(-1) and the recoveries of the analytes in the pharmaceutical preparations are in the range 100+/-10%.

  16. A comparison of the anti-inflammatory properties of intranasal corticosteroids and antihistamines in allergic rhinitis.

    Science.gov (United States)

    Howarth, P H

    2000-01-01

    Allergic rhinitis manifests itself clinically due to the local release of mediators from activated cells within the nasal mucosa. Treatment strategies aim either to reduce the effects of these mediators on the sensory neural and vascular end organs, or to reduce the tissue accumulation of the activated cells that generate them. Corticosteroids intervene at a number of steps in the inflammatory pathway, and, by reducing the release of cytokines and chemokines, inhibit cell recruitment and activation. These effects are evident both in vivo and in vitro. While antihistamines also have some anti-inflammatory effects in vitro, these require higher concentrations than with corticosteroids and are not consistently reproduced in vivo. In addition, although antihistamines and corticosteroids might appear to have complementary mechanisms of action, clinical trials suggest that their co-administration does not confer any additional long-term benefits compared with that achieved with corticosteroids alone. Topical corticosteroids are therefore the preferred anti-inflammatory therapy for persistent allergic rhinitis.

  17. Identification of a coumarin based antihistamine as an anti filoviral entry inhibitor

    Science.gov (United States)

    2017-06-20

    similar glycosaminoglycans(O’Hearn et al., 2015; Salvador et al., 2013), or C-type lectin family members like LSECtin (liver and lymph node ... node -specific ICAM-3 grabbing nonintegrin), mannose-binding lectin, and hMGL (human macrophage galactose- and N- TR-17-126 Distribution Statement A...antihistamines exhibit potent inhibitory activity against both pseudotyped EBOV and MARV in adenocarcinomic human alveolar basal epithelial cells (A549). More

  18. Double-blind placebo-controlled trial of dapsone in antihistamine refractory chronic idiopathic urticaria.

    Science.gov (United States)

    Morgan, Matt; Cooke, Andrew; Rogers, Laura; Adams-Huet, Beverley; Khan, David A

    2014-01-01

    Management of antihistamine refractory chronic idiopathic urticaria (CIU) has poorly defined therapeutic options. To evaluate the efficacy of dapsone (4,4'-diaminodiphenylsulfone) in antihistamine refractory CIU compared with placebo. Twenty-two patients with antihistamine refractory CIU were randomly assigned to 100 mg of dapsone daily or placebo for 6 weeks in a 14-week double-blind, placebo-controlled crossover trial. End points were measured from a daily diary that reflected the weekly hive score, the weekly itch score, and a visual analog scale (VAS) score. Secondary to a carryover effect, the first period results were analyzed as a parallel design that compared placebo with dapsone directly by using repeated-measures analysis. After 6 weeks, the patients in the dapsone arm showed mean improvement over baseline in VAS (2.3 [95% CI, 0.6-4.1], P = .01), urticaria score (-3.5 [95% CI, -6.2 to -0.9], P = .01), and itch score (-4.8 [95% CI, -7.6 to -2.1], P = .001), whereas the placebo arm showed no improvement over baseline for VAS, urticaria, or itch scores. Dapsone showed greater improvement compared with placebo for itch (P = .047) and VAS (P = .04). Of the 22 patients, 3 showed complete resolution of hives and itch with dapsone, whereas 31% and 41% had ≥ 50% resolution of hives and itch, respectively. No serious adverse effects were observed with dapsone. To our knowledge, this is the first double-blind, placebo controlled study of dapsone in CIU and indicates that dapsone has efficacy in patients with antihistamine refractory CIU. Copyright © 2014 American Academy of Allergy, Asthma & Immunology. Published by Elsevier Inc. All rights reserved.

  19. Double-Blind Placebo Controlled Trial of Dapsone in Antihistamine Refractory Chronic Idiopathic Urticaria

    Science.gov (United States)

    Morgan, Matt; Cooke, Andrew; Rogers, Laura; Adams-Huet, Beverley; Khan, David A.

    2014-01-01

    Background Management of antihistamine refractory CIU has poorly defined therapeutic options. Objective To evaluate the efficacy of dapsone in antihistamine refractory CIU compared to placebo. Methods Twenty-two patients with antihistamine refractory CIU were randomly assigned to 100 mg of dapsone daily or placebo for 6 weeks in a 14 week double-blind, placebo-controlled crossover trial. Endpoints were measured from a daily diary reflecting weekly hive score (WHS) and weekly itch score (WIS) and a visual analog score. Secondary to a carryover effect, the first period results were analyzed as a parallel design comparing placebo to dapsone directly using repeated measures analysis. Results After 6 weeks patients in the dapsone arm showed mean improvement over baseline in VAS (+2.3 [0.6,4.1], p=0.01), urticaria score (-3.5 [-6.2, -0.9], p=0.01), and itch score (-4.8 [-7.6, -2.1], p=0.001), whereas the placebo arm showed no improvement over baseline for VAS, urticaria or itch scores. Dapsone showed greater improvement compared to placebo for itch (p=0.047) and VAS (p=0.04). Of the 22 patients, 3 showed complete resolution of hives and itch with dapsone, while 31% and 41% had ≥ 50% resolution of hives and itch respectively. No serious adverse effects were observed from dapsone. Conclusion To our knowledge, this is the first DBPC study of dapsone in CIU and suggests dapsone has efficacy in antihistamine refractory CIU patients. PMID:25213055

  20. H1 antihistamines in allergic rhinitis: The molecular pathways of interleukin and toll - like receptor systems

    Directory of Open Access Journals (Sweden)

    Jonny Karunia Fajar

    2016-03-01

    Full Text Available The complex interaction between inflammatory mediators in allergic rhinitis (AR is determined by the role of genetic polymorphisms, including interleukin (IL and toll-like receptor (TLR genes. This study aimed to discuss the effects of H1-antihistamines on IL and TLR systems. Several ILs involved in AR pathogenesis are: IL-4 (rs2243250, rs1800925, rs1801275, rs2227284, rs2070874, IL-6 (rs1800795, rs1800797, IL-10 (rs1800871, rs1800872, IL-12R (rs438421, IL-13 (rs1800925, rs20541, IL-17 (rs3819024, IL-18 (rs360721, rs360718, rs360717, rs187238, IL-23R (rs7517847, and IL-27 (rs153109, rs17855750. In the IL system, histamines stimulate the IL production in Type 2 helper T (Th2 cells through protein kinase A (PKA, janus kinase-signal transducer and activator of transcription (JAK-STAT pathway, and the activation of H1-histamine receptor and histidine decarboxylase (HDC genes. On contrary, antihistamines down-regulate the H1-histamine receptor gene expression through the transcription suppression of HDC and IL genes and suppress histamine basal signaling through the inverse agonistic activity. TLRs involved in AR pathogenesis are TLR2 (rs4696480, rs3804099, rs5743708, TLR4 (rs4986790, TLR6 (rs2381289, TLR7 (rs179008, rs5935438, TRL8 (rs2407992, rs5741883, rs17256081, rs4830805, rs3788935, rs178998, and TLR10 (rs11466651. In the TLR system, histamines trigger the TLR expression by stimulating interferon-γ (IFN-γ to up-regulate mast cells and by stimulating receptor-interacting protein (RIP to activate IκB kinase-β. Contrastingly, antihistamines suppress TIR-domain-containing adaptor protein inducing IFN-β (TRIF and RIP protein and thus inhibit the expression of TLR. In addition, several studies indicated that H1-antihistamines inhibit the IL and TLR systems indirectly.

  1. Antihistamines and other prognostic factors for adverse outcome in hyperemesis gravidarum.

    Science.gov (United States)

    Fejzo, Marlena S; Magtira, Aromalyn; Schoenberg, Frederic Paik; MacGibbon, Kimber; Mullin, Patrick; Romero, Roberto; Tabsh, Khalil

    2013-09-01

    The purpose of this study is to determine the frequency of adverse perinatal outcome in women with hyperemesis gravidarum and identify prognostic factors. This is a case-control study in which outcomes of first pregnancies were compared between 254 women with hyperemesis gravidarum treated with intravenous fluids and 308 controls. Prognostic factors were identified by comparing the clinical profile of patients with hyperemesis gravidarum with a normal and an adverse pregnancy outcome. Binary responses were analyzed using either a Chi-square or Fisher exact test and continuous responses were analyzed using a t-test. Women with hyperemesis gravidarum have over a 4-fold increased risk of poor outcome including preterm birth and lower birth weight (p<0.0001). Among maternal characteristics, only gestational hypertension had an influence on outcome (p<0.0001). Treatment as an outpatient and/or by alternative medicine (acupuncture/acupressure/Bowen massage) was associated with a positive outcome (p<0.0089). Poor outcomes were associated with early start of symptoms (p<0.019), and treatment with methylprednisolone (p<0.0217), promethazine (p<0.0386), and other antihistamines [diphenhydramine (Benadryl), dimenhydrinate (Gravol), doxylamine (Unisom), hydroxyzine (Vistaril/Atarax), doxylamine and pyridoxine (Diclectin/Bendectin)] (p<0.0151) independent of effectiveness. Among these medications, only the other antihistamines were prescribed independent of severity: they were effective in less than 20% of cases and were taken by almost 50% of patients with an adverse outcome. Poor outcomes are significantly greater in women with HG and are associated with gestational hypertension, early symptoms, and antihistamine use. Given these results, there is an urgent need to address the safety and effectiveness of medications containing antihistamines in women with severe nausea of pregnancy. Copyright © 2013 Elsevier Ireland Ltd. All rights reserved.

  2. Effect of Antihistamine Eye Drops on the Conjunctival Provocation Test with Japanese Cedar Pollen Allergen

    Directory of Open Access Journals (Sweden)

    Yoshihiro Dake

    2006-01-01

    Conclusions: Preadministration of antihistamine eye drops suppressed the symptoms induced by the allergen, which suggests that this is an effective early therapy for Japanese cedar pollinosis, if it is started before the pollen season. However, self-protection by patients using a mask may not be effective enough to suppress nasal symptoms during the pollen season, requiring them to additionally wear glasses to avoid exposure to the allergen.

  3. Effects of antihistamines on innate immune responses to severe bacterial infection in mice.

    Science.gov (United States)

    Metz, Martin; Doyle, Elizabeth; Bindslev-Jensen, Carsten; Watanabe, Takeshi; Zuberbier, Torsten; Maurer, Marcus

    2011-01-01

    Sedating and non-sedating histamine H(1) receptor (H1R) antagonists and H2R blockers are widely used drugs which are generally considered to be safe medications. However, recently, these drugs have been shown to possibly impair the outcome of perforating appendicitis in children. It was the aim of this study to characterize the effects of histamine receptor blockade in severe bacterial infections in more detail. To obtain information on the safety of histamine receptor blockade in more detail, we used pharmacological and genetic approaches targeting histamine receptors and performed cecal ligation and puncture (CLP), a mouse model of septic peritonitis. After induction of septic peritonitis, morbidity and mortality were monitored closely. Here, we show that oral treatment with first-generation H1R antihistamine diphenhydramine, H2R blocker cimetidine and H3/4R blocker thioperamide impairs optimal innate immune responses in severe murine bacterial sepsis. However, these adverse effects are not mediated by H1R, as mice deficient for H1R show similar rates of morbidity and mortality after CLP as their wild-type controls. Similarly, the second-generation antihistamine desloratadine neither affects morbidity nor mortality after CLP. Our findings indicate that sedating first-generation H1R antihistamines and H2R blockers might impair innate immune responses to bacteria and that these drugs should be used with caution in patients with severe bacterial infections. Copyright © 2011 S. Karger AG, Basel.

  4. Quantitative electrophysiological monitoring of anti-histamine drug effects on live cells via reusable sensor platforms.

    Science.gov (United States)

    Pham Ba, Viet Anh; Cho, Dong-Guk; Kim, Daesan; Yoo, Haneul; Ta, Van-Thao; Hong, Seunghun

    2017-08-15

    We demonstrated the quantitative electrophysiological monitoring of histamine and anti-histamine drug effects on live cells via reusable sensor platforms based on carbon nanotube transistors. This method enabled us to monitor the real-time electrophysiological responses of a single HeLa cell to histamine with different concentrations. The measured electrophysiological responses were attributed to the activity of histamine type 1 receptors on a HeLa cell membrane by histamine. Furthermore, the effects of anti-histamine drugs such as cetirizine or chlorphenamine on the electrophysiological activities of HeLa cells were also evaluated quantitatively. Significantly, we utilized only a single device to monitor the responses of multiple HeLa cells to each drug, which allowed us to quantitatively analyze the antihistamine drug effects on live cells without errors from the device-to-device variation in device characteristics. Such quantitative evaluation capability of our method would promise versatile applications such as drug screening and nanoscale bio sensor researches. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. Antihistamine-resistant angioedema in women with negative family history: estrogens and F12 gene mutations.

    Science.gov (United States)

    Bork, Konrad; Wulff, Karin; Witzke, Günther; Stanger, Christian; Lohse, Peter; Hardt, Jochen

    2013-12-01

    In women with sporadic recurrent angioedema with an unknown cause who are unresponsive to antihistamines and have normal C1 inhibitor activity and a negative family history of angioedema, it is unclear whether they have idiopathic angioedema or hereditary angioedema with normal C1 inhibitor, and what impact exogenous estrogens have on their angioedema. A cohort of 147 women was analyzed for F12 exon 9 mutations and for the influence of oral contraceptives, hormonal replacement therapy, and pregnancy on their angioedema. A total of 142 women had idiopathic angioedema unresponsive to antihistamines. Five women had an F12 mutation and thereby hereditary angioedema with F12 mutations. Among the women with idiopathic angioedema, 63 had never taken estrogens. There was no estrogen impact in 42 women, a moderate impact in 15 women, and a severe impact in 22 women. The type and dose of estrogens did not differ in women with and without an estrogen impact. In 5 women, idiopathic angioedema disappeared after desogestrel use. Among the 5 women with hereditary angioedema with F12 mutations, angioedema symptoms occurred during 4 pregnancies, whereas no symptoms occurred during any of the 58 pregnancies in women with idiopathic angioedema. Women with recurrent angioedema unresponsive to antihistamines may have idiopathic angioedema or, more rarely, hereditary angioedema with F12 mutations. Both conditions may be provoked or aggravated by exogenous estrogens. In idiopathic angioedema, treatment with progestins may be helpful. Copyright © 2013. Published by Elsevier Inc.

  6. A review of the effects of antihistamines on mental processes related to automobile driving.

    Science.gov (United States)

    Gengo, F M; Manning, C

    1990-12-01

    The newer, second-generation H1-receptor antagonists have been shown to have potent antiallergic effects without inducing sleepiness. However, because traditional antihistamines may cause functional or cognitive impairment, the clinician still must consider warning patients about activities that could be hazardous. Because the effects of drugs on driving an automobile are difficult to measure directly, studies must use surrogate activities in a laboratory setting. Effects of antihistamines on the central nervous system are assessed with psychomotor tests, which are selected on the basis of their relativity to real-world activities, to develop a profile of mental processes that may be affected. This article reviews the psychomotor tests and study design used to characterize the intensity and duration of drug effects after single and multiple doses and in combination with other impairing agents such as ethanol. Several studies have been published that assess the effects of cetirizine, an H1-receptor blocker, on mental performance. In the study discussed here, diphenhydramine hydrochloride and hydroxyzine were used as positive controls to demonstrate that the period during which some traditional antihistamines impair performance is different than the period of reported drowsiness they induce. The results of this series of studies show that cetirizine induced minimal changes in mental performance tests and only following the highest (20 mg) dose studied.

  7. Effects of antihistamines on the function of human α7-nicotinic acetylcholine receptors.

    Science.gov (United States)

    Sadek, Bassem; Khanian, Seyedeh Soha; Ashoor, Abrar; Prytkova, Tatiana; Ghattas, Mohammad A; Atatreh, Noor; Nurulain, Syed M; Yang, Keun-Hang Susan; Howarth, Frank Christopher; Oz, Murat

    2015-01-05

    Effects of the histamine H₁ receptor (H1R) antagonists (antihistamines), promethazine (PMZ), orphenadrine (ORP), chlorpheniramine (CLP), pyrilamine (PYR), diphenhydramine (DPH), citerizine (CTZ), and triprolidine (TRP) on the functional properties of the cloned α7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes were investigated. Antihistamines inhibited the α7-nicotinic acetylcholine receptor in the order PYR>CLP>TRP>PMZ>ORP≥DPH≥CTZ. Among the antihistamines, PYR showed the highest reversible inhibition of acetylcholine (100 µM)-induced responses with IC₅₀ of 6.2 µM. PYR-induced inhibition was independent of the membrane potential and could not be reversed by increasing the concentration of acetylcholine. Specific binding of [¹²⁵I] α-bungarotoxin, a selective antagonist for α7-nicotinic acetylcholine receptor, was not changed in the presence of PYR suggesting a non-competitive inhibition of nicotinic receptors. In line with functional experiments, docking studies indicated that PYR can potentially bind allosterically with the α7 transmembrane domain. Our results indicate that the H₂-H₄ receptor antagonists tested in this study (10 µM) showed negligible inhibition of α7-nicotinic acetylcholine receptors. On the other hand, H₁ receptor antagonists inhibited the function of human α7-nicotinic acetylcholine receptor, with varying potencies. These results emphasize the importance of α7-nicotinic acetylcholine receptor for future pharmacological/toxicological profiling. Copyright © 2014 Elsevier B.V. All rights reserved.

  8. Topical antihistamines and mast cell stabilisers for treating seasonal and perennial allergic conjunctivitis.

    Science.gov (United States)

    Castillo, Mayret; Scott, Neil W; Mustafa, Mohammad Z; Mustafa, Mohammed S; Azuara-Blanco, Augusto

    2015-06-01

    Seasonal/perennial allergic conjunctivitis is the most common allergic conjunctivitis, usually with acute manifestations when a person is exposed to allergens and with typical signs and symptoms including itching, redness, and tearing. The clinical signs and symptoms of allergic conjunctivitis are mediated by the release of histamine by mast cells. Histamine antagonists (also called antihistamines) inhibit the action of histamine by blocking histamine H1 receptors, antagonising the vasoconstrictor, and to a lesser extent, the vasodilator effects of histamine. Mast cell stabilisers inhibit degranulation and consequently the release of histamine by interrupting the normal chain of intracellular signals. Topical treatments include eye drops with antihistamines, mast cell stabilisers, non-steroidal anti-inflammatory drugs, combinations of the previous treatments, and corticosteroids. Standard treatment is based on topical antihistamines alone or topical mast cell stabilisers alone or a combination of treatments. There is clinical uncertainty about the relative efficacy and safety of topical treatment. The objective of this review was to assess the effects of topical antihistamines and mast cell stabilisers, alone or in combination, for use in treating seasonal and perennial allergic conjunctivitis. We searched CENTRAL (which contains the Cochrane Eyes and Vision Trials Register) (2014, Issue 7), Ovid MEDLINE, Ovid MEDLINE In-Process and Other Non-Indexed Citations, Ovid MEDLINE Daily, Ovid OLDMEDLINE (January 1946 to July 2014), EMBASE (January 1980 to July 2014), the metaRegister of Controlled Trials (mRCT) (www.controlled-trials.com), ClinicalTrials.gov (www.clinicaltrials.gov) and the World Health Organization (WHO) International Clinical Trials Registry Platform (ICTRP) (www.who.int/ictrp/search/en). We did not use any date or language restrictions in the electronic searches for trials. We last searched the electronic databases on 17 July 2014. We also searched the

  9. Bilastine: A New Nonsedating Oral H1 Antihistamine for Treatment of Allergic Rhinoconjunctivitis and Urticaria

    Directory of Open Access Journals (Sweden)

    Ole D. Wolthers

    2013-01-01

    Full Text Available Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine. In the fasting state bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice. Therefore, it is recommended that bilastine is taken at least one hour before and no sooner than two hours after a meal. Clinical studies sponsored by the manufacturer have shown that bilastine 20 mg once daily is as efficacious as other nonsedating antihistamines in allergic rhinoconjunctivitis and chronic urticaria in individuals from 12 and 18 years of age, respectively. Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms. The observations indicate that non-sedating antihistamines, as opposed to what has been thought previously, may be helpful in patients with allergic rhinitis in whom nasal obstruction is a major concern. Current international guidelines need to be revised in the light of the recent evidence. Research into aspects of pharmacokinetics and efficacy and adverse effect profiles of bilastine in children under 12 years of age is needed as are dose-response assessments and studies planned rigorously with the aim of assessing quality of life effects.

  10. State-dependent interaction in the antihistamine-induced disruption of a radiation-induced conditioned taste aversion

    Energy Technology Data Exchange (ETDEWEB)

    Rabin, B.M. (Armed Forces Radiobiology Research Inst., Bethesda, MD); Hunt, W.A.; Lee, J.

    1982-06-01

    Two experiments were run to evaluate the possibility that injection of antihistamine can produce a state-dependent acquisition of a radiation-induced conditioned taste aversion. In the first experiment, pretreating rats with the antihistamine chlorpheniramine maleate prior to their initial exposure to sucrose and to low-level irradiation on the conditioning day did not prevent the acquisition of a taste aversion to sucrose when the antihistamine was also administered prior to a subsequent preference test. In the second experiment, rats were both conditioned and tested for a radiation-induced aversion in a drug-free state. Under these condtions, the rats continued to show an aversion to sucrose despite pretreating them with chlorpheniramine prior to irradiation. Since rats conditioned under the antihistamine do not show the radiation-induced conditioned taste aversion when tested for sucrose preference in a nondrug state, it would seem that pretreating rats with an antihistamine prior to conditioning affects only the retrieval of the previously learned response and not its acquisition.

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

    Science.gov (United States)

    Mateus, C

    2003-05-01

    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.

  12. H1-antihistamines for chronic spontaneous urticaria: an abridged Cochrane Systematic Review.

    Science.gov (United States)

    Sharma, Maulina; Bennett, Cathy; Carter, Ben; Cohen, Stuart N

    2015-10-01

    Chronic spontaneous urticaria is characterized by recurrent itchy wheals. First-line management is with H1-antihistamines. We sought to conduct a Cochrane Review of H1-antihistamines in the treatment of chronic spontaneous urticaria. A systematic search of major databases for randomized controlled trials was conducted. We included 73 studies with 9759 participants; 34 studies provided outcome data for 23 comparisons. Compared with placebo, cetirizine 10 mg daily in the short and intermediate term (RR 2.72; 95% confidence interval [CI] 1.51-4.91) led to complete suppression of urticaria. Levocetirizine 20 mg daily was effective for short-term use (RR 20.87; 95% CI 1.37-317.60) as was 5 mg for intermediate-term use (RR 52.88; 95% CI 3.31-843.81). Desloratadine 20 mg was effective for the short term (RR 15.97; 95% CI 1.04-245.04) as was 5 mg in the intermediate term (RR 37.00; 95% CI 2.31-593.70). There was no evidence to suggest difference in adverse event rates between treatments. Some methodological limitations were observed. Few studies for each comparison reported outcome data that could be incorporated in meta-analyses. At standard doses, several antihistamines are effective and safe in complete suppression of chronic spontaneous urticaria. Research on long-term treatment using standardized outcome measures and quality of life scores is needed. Copyright © 2015 American Academy of Dermatology, Inc. Published by Elsevier Inc. All rights reserved.

  13. Evaluation of Efficacy and Sedative Profiles of H1 Antihistamines by Large-Scale Surveillance Using the Visual Analogue Scale (VAS

    Directory of Open Access Journals (Sweden)

    Norimasa Izumi

    2008-01-01

    Conclusions: The sedative properties of the H1 antihistamines obtained from VAS analysis were very similar to those of H1R occupancy from positron emission tomography (PET studies and PIR from meta-analysis. Our results indicate that large-scale surveillance using VAS might be useful to evaluate the profiles of H1 antihistamines.

  14. Use of antihistamines and risk of ventricular tachyarrhythmia : a nested case-control study in five European countries from the ARITMO project

    NARCIS (Netherlands)

    Poluzzi, Elisabetta; Diemberger, I.; de Ridder, M.; Koci, A.; Clo, M.; Oteri, A.; Pecchioli, S.; Bezemer, I.D.; Schink, T.; Pilgaard Ulrichsen, S.; Boriani, G.; Sturkenboom, M. C.J.; De Ponti, F.; Trifirò, G.

    2017-01-01

    Purpose: After regulatory restrictions for terfenadine and astemizole in ‘90s, only scarce evidence on proarrhythmic potential of antihistamines has been published. We evaluate the risk of ventricular tachyarrhythmia (VA) related to the use of individual antihistamines. Methods: A matched

  15. Anti-histamine effect of Rubia tibetica, used to treat anaphylaxis caused by tick bites in the Pamir Mountains, Afghanistan

    DEFF Research Database (Denmark)

    Jeppesen, Anne S.; Kristiansen, Uffe; Soelberg, Jens

    2012-01-01

    Ethnopharmacological relevance: The roots of Rubia tibetica are chewed as an antidote to anaphylaxis caused by bites of the tick Ornithodoros lahorensis by the Wakhi people in Afghanistan. Aims of the study: To test whether Rubia tibetica possess anti-histamine effect. Materials and methods: Water...... and ethanol extracts of roots of Rubia tibetica were tested for anti-histamine effect on the H 1-receptor in the guinea pig ileum assay. Fixed concentrations of plant extract with increasing concentrations of histamine were examined. Mepyramine was used as control. Results and conclusion: The ethanol extract...... of Rubia tibetica showed dose-dependent anti-histamine effect, whereas the water extract had little activity. The chewing of Rubia tibetica roots may alleviate the fatal swelling of the tongue during anaphylaxis....

  16. Anti-histamine effect of Rubia tibetica, used to treat anaphylaxis caused by tick bites in the Pamir Mountains, Afghanistan.

    Science.gov (United States)

    Jeppesen, Anne S; Kristiansen, Uffe; Soelberg, Jens; Jäger, Anna K

    2012-06-14

    The roots of Rubia tibetica are chewed as an antidote to anaphylaxis caused by bites of the tick Ornithodoros lahorensis by the Wakhi people in Afghanistan. To test whether Rubia tibetica possess anti-histamine effect. Water and ethanol extracts of roots of Rubia tibetica were tested for anti-histamine effect on the H1-receptor in the guinea pig ileum assay. Fixed concentrations of plant extract with increasing concentrations of histamine were examined. Mepyramine was used as control. The ethanol extract of Rubia tibetica showed dose-dependent anti-histamine effect, whereas the water extract had little activity. The chewing of Rubia tibetica roots may alleviate the fatal swelling of the tongue during anaphylaxis.

  17. The effect of some commercially available antihistamine and decongestant intra-nasal formulations on ciliary beat frequency.

    Science.gov (United States)

    Su, X Y; Li Wan Po, A

    1993-06-01

    The effects of azelastine (0.1%) nasal spray (Rhinolast) on ciliary beat frequency are investigated and compared with those of oxymetazoline hydrochloride (Vicks Sinex), xylometazoline (Otrivine) and ephedrine hydrochloride (0.5%). It is shown that all four formulations exert a ciliotoxic effect. The antihistamine (azelastine) and the two long-acting alpha sympathomimetic decongestants (xylometazoline and oxymetazoline) had comparable effects which were milder than those observed with ephedrine, the less specific alpha and beta sympathomimetic agent. The results suggest that the intranasal application of all four products should be restricted to short-term therapy. Oral antihistamine therapy and not topical therapy should still be the first-line therapy for antihistamine-responsive rhinitis until non-ciliotoxic formulations can be developed.

  18. The anti-anaphylactic and histamine-releasing properties of the antihistamines. Their effect on the mast cells

    Science.gov (United States)

    Mota, I.; Da Silva, W. Dias

    1960-01-01

    It has been shown that, depending upon their concentration, antihistamines act in three different ways: (a) by competitive inhibition of histamine as already known; (b) by destroying mast cells and releasing histamine; and (c) by preventing mast cell damage and histamine release in anaphylaxis. Furthermore, antihistamines potentiated mast cell damage and histamine release by compound 48/80, when acting on guinea-pig tissues, and inhibited these same phenomena when acting on rat tissues. It is concluded that the effect of antihistamines in anaphylaxis is possibly due both to their competitive inhibition of histamine on smooth muscle receptors and to their inhibition of mast cell damage and histamine release by antigen. PMID:13773171

  19. Synthesis of Some Phenylpyrazolo Benzimidazolo Quinoxaline Derivatives as Potent Antihistaminic Agents

    Directory of Open Access Journals (Sweden)

    C. H. Sridevi

    2010-01-01

    Full Text Available 2,3-Diphenyl quinoxaline (NI was fused with benzimidazole (NII by a methylene bridge, which was then allowed for acetylation. The acetylated product (NIV was made to react with different aromatic aldehydes to give chalcones (NV1-NV5. Chalcones refluxed with substituted acid hydrazides to afford different phenyl pyrazolo benzimidazole quinoxaline derivatives (NVI 1-NVI 15. The structure of chalcones and phenyl pyrazolo benzimidazole quinoxaline derivatives were confirmed by m.p, TLC and spectral data. All the synthesized compounds were screened for their antihistaminic activity. Compounds NVI-3, NVI-12, NVI-13, NVI-14 and NVI-15 were shown good % protection of antihistamic activity.

  20. A Differentiated Approach to the Prescription of Antihistamines in Allergic Diseases in Childhood

    Directory of Open Access Journals (Sweden)

    O.Ye. Abaturov

    2016-08-01

    Full Text Available The comparative analysis of current data on pharmacodynamics, pharmacokinetics, clinical efficacy and side effects of the first generation drug antihistamine demetinden and the third-generation levocetirizinum is presented. Levocetirizinum shows the highest selectivity to H1-receptor having anta­gonist properties does not penetrate the central nervous system and has no sedative effects. The drug has anti-inflammatory effects due to suppression of release of inflammation mediators and cellular response. Levocetirizinum has favorable pharmacokinetics and half-life, no drug interactions. The clinical stu­dies demonstrated its high efficiency in ruducing the symptoms of allergic diseases.

  1. Enantioseparation of Six Antihistamines with Immobilized Cellulose Chiral Stationary Phase by HPLC.

    Science.gov (United States)

    Zhou, Jie; Luo, Pei; Chen, Shanshan; Meng, Lingchang; Sun, Chong; Du, Qiuzheng; Sun, Fang

    2016-04-01

    A stereoselective high performance liquid chromatography method has been developed for the chiral separation of the enantiomers of six antihistamines, doxylamine, carbinoxamine, dioxopromethazine, oxomemazine, cetirizine and hydroxyzine. The effects of mobile phase additive, column temperature and flow rate on the retention time and resolution were studied. Enantiomeric separation of cetirizine, doxylamine and hydroxyzine were achieved on cellulose tris-(3,5-dichlorophenylcarbamate) immobilized on silica gel chiral stationary phase known as Chiralpak IC (RS = 3.74, RS = 1.85 and RS = 1.74, respectively). © The Author 2015. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

  2. [Analysis of the Cochrane Review: Antihistamines for the Common Cold. Cochrane Database Syst Rev. 2015;11:CD009345].

    Science.gov (United States)

    Sterrantino, Carmel; Duarte, Gonçalo; Costa, João; Vaz-Carneiro, António

    2016-03-01

    The common cold is an acute, self-limiting inflammation of the mucosa of the upper airways, which may involve one or all the sinuses, nasopharynx, oropharynx and larynx. It is common to have at least one episode per year. Common cold symptoms, which may include sore throat, sneezing, nasal congestion, runny nose, headache, malaise and mild fever usually disappear within a few days without treatment. The causative agent of most colds is rhinovirus. Although not associated with mortality, common cold is associated with significant morbidity. There is no vaccine or cure for common cold and, therefore, their treatment is centered on relieving the symptoms. This Cochrane review aimed to synthesize the existing evidence about the clinical benefit of antihistamines, used as monotherapy, compared with placebo or no treatment in children and adult patients with common cold. A total of 18 randomized clinical trials with 4342 participants were included. Main results were: 1) Antihistamines have a small (days one and two) beneficial effect in the short term on the severity of overall symptoms in adult patients, although this effect is not present in the medium to long term; 2) antihistamines were not associated with a clinically significant beneficial effect on the individual symptoms (nasal congestion, rhinorrhea, and sneezing); 3) Antihistamines are not associated with an increased risk of adverse effects; 4) No conclusion can be made about the effectiveness of antihistamines in pediatric populations. Our interpretation of the results is that the available evidence is insufficient to support the prescription or buying OTC antihistamines to relieve the symptoms of common cold without allergic component.

  3. Pro-arrhythmic potential of oral antihistamines (H1: combining adverse event reports with drug utilization data across Europe.

    Directory of Open Access Journals (Sweden)

    Elisabetta Poluzzi

    Full Text Available There is appreciable utilisation of antihistamines (H1 in European countries, either prescribed by physician and purchased by patients for self-medication. Terfenadine and astemizole underwent regulatory restrictions in '90 because of their cardiac toxicity, but only scarce clinical data are available on other antihistamines.To investigate the pro-arrhythmic potential of antihistamines by combining safety reports of the FDA Adverse Event Reporting System (FAERS with drug utilization data from 13 European Countries.We identified signals of antihistamine arrhythmogenic potential by analyzing FAERS database for all cases of Torsades de Pointes (TdP, QT abnormalities (QTabn, ventricular arrhythmia (VA and sudden cardiac death/cardiac arrest (SCD/CA. Number of cases ≥3 and disproportionality were used to define alert signals: TdP and QTabn identified stronger signals, whereas SCD/CA identified weaker signals. Drug utilization data from 2005 to 2010 were collected from administrative databases through health authorities and insurance.Antihistamines were reported in 109 cases of TdP/QT prolongation, 278 VA and 610 SCD/CA. Five agents resulted in stronger signals (cetirizine, desloratadine, diphenhydramine, fexofenadine, loratadine and 6 in weaker signals (alimemazine, carbinoxamine, cyclizine, cyproeptadine, dexchlorpheniramine and doxylamine. Exposure to antihistamines with stronger signal was markedly different across European countries and was at least 40% in each Country. Cetirizine was >29 Defined Daily Doses per 1000 inhabitants per day (DID in Norway, desloratadine >11 DID in France and loratadine >9 DID in Sweden and Croatia. Drugs with weaker signals accounted for no more than 10% (in Sweden and in most European countries their use was negligible.Some second-generation antihistamines are associated with signal of torsadogenicity and largely used in most European countries. Although confirmation by analytical studies is required, regulators

  4. Is there a role for nonsedating antihistamines in motion sickness? Fallout from space research may soon benefit your patients

    Science.gov (United States)

    Kohl, R. L.

    1991-01-01

    The rotating chair test, a novel research technique for simulating motion sickness, is used to study the effect of nonsedating oral antihistamines in preventing or forestalling motion sickness. After receiving terfenadine, astemizole, doxepin, or placebo, four groups of male volunteers were rotated at accelerating speed, and they made head movements out of the axis of rotation until they perceived that vomiting would occur if additional head movements were made. Those pretreated with doxepin or terfenadine experienced a statistically significant prophylactic effect, as measured by increased tolerance to Coriolis stimulation. This suggests that selective peripheral H1 antihistamine action may protect against motion sickness.

  5. Advances in the molecular modeling and quantitative structure-activity relationship-based design for antihistamines.

    Science.gov (United States)

    Galvez, Jorge; Galvez-Llompart, Maria; Zanni, Riccardo; Garcia-Domenech, Ramon

    2013-03-01

    Nowadays the use of antihistamines (AH) is increasing steadily. These drugs are able to act on a variety of pathological conditions of the organism. A number of computer-aided (in silico) approaches have been developed to discover and develop novel AH drugs. Among these methods stand the ones based on drug-receptor docking, thermodynamics, as well as the quantitative structure-activity relationships (QSAR). This review collates the most recent advances in the use of computer approaches for the search and characterization of novel AH drugs. Within the QSAR methods, particular attention will be paid to those based on molecular topology (MT) because of their demonstrated efficacy in discovering new drugs. Collateral topics will also be dealt with including: docking studies, thermodynamic aspects, molecular modeling and so on. These issues will be treated to the extent that they have interest as complementary to QSAR-MT. Given the importance of the use of AHs, the search for new drugs in this field has become imperative today. In this regard, the use of QSAR methods based on MT, namely QSAR-MT, has proven to be a powerful tool when the goal is discovering new hit or lead structures. It has been shown that antihistaminic activity is complex and different for the four known types of receptors (H1 to H4) and that electronic, steric and physicochemical issues determine drug activity. These factors, along with the purely structural ones, can be deduced from topological and topochemical information.

  6. Omalizumab is efficacious for management of recalcitrant, antihistamine-resistant chronic urticaria.

    Science.gov (United States)

    Lang, D M

    2015-06-01

    Chronic urticaria continues to be a challenging condition for both patients and physicians. Despite improved understanding of chronic urticaria, many patients continue to experience ongoing symptoms and impaired quality of life. Omalizumab is a recombinant humanized monoclonal antibody that binds to the domain at which IgE binds to the high-affinity IgE receptor on mast cells and basophils. The efficacy of omalizumab for antihistamine-resistant chronic urticaria has been demonstrated in several randomized controlled trials as well as observational studies. Omalizumab is generally well tolerated, and is associated with less potential for harm compared with other therapeutic alternatives (e.g., calcineurin inhibitors) for recalcitrant chronic urticaria. Omalizumab has become the best-studied agent for treatment of antihistamine-resistant chronic urticaria, and the agent for which the data in support of its efficacy is most methodologically sound. Omalizumab is an effective therapeutic option for patients with recalcitrant chronic urticaria. Copyright 2015 Prous Science, S.A.U. or its licensors. All rights reserved.

  7. Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells.

    Science.gov (United States)

    Kim, Jiwon; Song, Jin-Ho

    2017-03-05

    Microglial NADPH oxidase is a major source of toxic reactive oxygen species produced during chronic neuroinflammation. Voltage-gated proton channel (H V 1) functions to maintain the intense activity of NADPH oxidase, and channel inhibition alleviates the pathology of neurodegenerative diseases such as ischemic stroke and multiple sclerosis associated with oxidative neuroinflammation. Antagonists of histamine H 1 receptors have beneficial effects against microglia-mediated oxidative stress and neurotoxicity. We examined the effects of the H 1 antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells recorded using the whole-cell patch clamp technique. Diphenhydramine and chlorpheniramine reduced the proton currents with almost the same potency, yielding IC 50 values of 42 and 43μM, respectively. Histamine did not affect proton currents, excluding the involvement of histamine receptors in their action. Neither drug shifted the voltage-dependence of activation or the reversal potential of the proton currents, even though diphenhydramine slowed the activation and deactivation kinetics. The inhibitory effects of the two antihistamines on proton currents could be utilized to develop therapeutic agents for neurodegenerative diseases and other diseases associated with H V 1 proton channel abnormalities. Copyright © 2017 Elsevier B.V. All rights reserved.

  8. Pro-arrhythmic potential of oral antihistamines (H1) : Combining adverse event reports with drug utilization data across Europe

    NARCIS (Netherlands)

    E. Poluzzi (Elisabetta); E. Raschi (Emanuel); B. Godman (Brian); A. Koci (Ariola); U. Moretti (Ugo); M. Kalaba (Marija); B. Wettermark (Bjorn); M.C.J.M. Sturkenboom (Miriam); F. de Ponti (Fabrizio)

    2015-01-01

    textabstractBackground: There is appreciable utilisation of antihistamines (H1) in European countries, either prescribed by physician and purchased by patients for self-medication. Terfenadine and astemizole underwent regulatory restrictions in '90 because of their cardiac toxicity, but only scarce

  9. Oral antihistamines for the symptom of nasal obstruction in persistent allergic rhinitis--a systematic review of randomized controlled trials

    NARCIS (Netherlands)

    Hore, I.; Georgalas, C.; Scadding, G.

    2005-01-01

    BACKGROUND: Oral antihistamines are recommended by a World Health Organisation working group as a first-line pharmacological treatment in mild persistent allergic rhinitis. There is, however, uncertainty with respect to their effectiveness for a common symptom, that of nasal obstruction. OBJECTIVE:

  10. Efficacy and safety of omalizumab in patients with chronic idiopathic/spontaneous urticaria who remain symptomatic on H1 antihistamines

    DEFF Research Database (Denmark)

    Saini, Sarbjit S; Bindslev-Jensen, Carsten; Maurer, Marcus

    2015-01-01

    ASTERIA I was a 40-week, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of subcutaneous omalizumab as add-on therapy for 24 weeks in patients with chronic idiopathic urticaria/spontaneous urticaria (CIU/CSU) who remained symptomatic despite H1 antihistamine...

  11. Comparative investigations of the influence of H1-antihistamines on the generation of reactive oxygen species by phagocytes

    Czech Academy of Sciences Publication Activity Database

    Králová, Jana; Nosál, R.; Drábiková, K.; Jančinová, V.; Denev, P.; Moravcová, Aneta; Kubala, Lukáš; Číž, Milan; Lojek, Antonín

    2008-01-01

    Roč. 57, č. 1 (2008), S01-S02 ISSN 1023-3830 R&D Projects: GA AV ČR(CZ) 1QS500040507 Institutional research plan: CEZ:AV0Z50040507; CEZ:AV0Z50040702 Keywords : H1- antihistamines * phagocytes * ROS Subject RIV: BO - Biophysics Impact factor: 1.457, year: 2008

  12. Early pregnancy exposure to antihistamines and risk of congenital heart defects : results of two case-control studies

    NARCIS (Netherlands)

    Smedts, Huberdina P. M.; de Jonge, Linda; Bandola, Sarah J. G.; Baardman, Marlies E.; Bakker, Marian K.; Stricker, Bruno H. C.; Steegers-Theunissen, Regine P. M.

    UNLABELLED: We aimed to study the association between use of antihistamines in early pregnancy and congenital heart defects (CHD) in the offspring. DESIGN: Two case-control studies. SETTING: HAVEN study, Erasmus MC, University Medical Centre, Rotterdam, and Eurocat Northern Netherlands (NNL),

  13. Differential thermodynamic driving force of first- and second-generation antihistamines to determine their binding affinity for human H1 receptors.

    Science.gov (United States)

    Hishinuma, Shigeru; Sugawara, Kenta; Uesawa, Yoshihiro; Fukui, Hiroyuki; Shoji, Masaru

    2014-09-15

    Differential binding sites for first- and second-generation antihistamines were indicated on the basis of the crystal structure of human histamine H1 receptors. In this study, we evaluated differences between the thermodynamic driving forces of first- and second-generation antihistamines for human H1 receptors and their structural determinants. The binding enthalpy and entropy of 20 antihistamines were estimated with the van't Hoff equation using their dissociation constants obtained from their displacement curves against the binding of [(3)H]mepyramine to membrane preparations of Chinese hamster ovary cells expressing human H1 receptors at various temperatures from 4°C to 37°C. Structural determinants of antihistamines for their thermodynamic binding properties were assessed by quantitative structure-activity relationship (QSAR) analyses. We found that entropy-dependent binding was more evident in second- than first-generation antihistamines, resulting in enthalpy-entropy compensation between the binding forces of first- and second-generation antihistamines. QSAR analyses indicated that enthalpy-entropy compensation was determined by the sum of degrees, maximal electrostatic potentials, water-accessible surface area and hydrogen binding acceptor count of antihistamines to regulate their affinity for receptors. In conclusion, it was revealed that entropy-dependent hydrophobic interaction was more important in the binding of second-generation antihistamines, even though the hydrophilicity of second-generation antihistamines is generally increased. Furthermore, their structural determinants responsible for enthalpy-entropy compensation were explored by QSAR analyses. These findings may contribute to understanding the fundamental mechanisms of how the affinity of ligands for their receptors is regulated. Copyright © 2014 Elsevier Inc. All rights reserved.

  14. The concept of receptor occupancy to predict clinical efficacy: a comparison of second generation H1 antihistamines.

    Science.gov (United States)

    Gillman, Sherwin; Gillard, Michel; Strolin Benedetti, Margherita

    2009-01-01

    Second generation H1 antihistamines are considered first-line therapy for allergic rhinitis and chronic idiopathic urticaria, largely because of their nonsedating effects. Evaluating pharmacokinetic and pharmacodynamic parameters and clinical efficacy of a drug is important, but models to predict clinical efficacy are lacking. Receptor occupancy (RO), a predictor for human pharmacodynamics and antihistamine potency that takes into account the affinity of the drug for the receptor and its free plasma concentration, may be a more accurate way to predict a drug's clinical efficacy. This study was designed to assess the concept of RO as a surrogate for clinical efficacy, using examples of second generation oral antihistamines. A literature review was conducted using MEDLINE. Search terms included allergy, allergic rhinitis, drug efficacy, over-the-counter drugs, perennial allergic rhinitis, seasonal allergic rhinitis, second generation antihistamines, chronic idiopathic urticaria, and treatment outcomes. Abstracts and posters from recent allergy-related society meetings were also used. RO of several second generation H1 antihistamines was derived from noncomparative and head-to-head studies. Fexofenadine and levocetirizine showed similar RO at 4 hours, both higher than that of desloratadine. Levocetirizine established higher RO than fexofenadine or desloratadine at 12 and 24 hours. RO for these agents appeared to correlate with pharmacodynamic activity in skin wheal and flare studies and with efficacy in allergen challenge chamber studies. Parameters affecting RO included time from dosing, pH, and dosing regimen. RO did not appear to be linearly related to drug concentration. Results indicate that RO is an accurate predictor of in vivo pharmacodynamic activity and clinical efficacy.

  15. The effectiveness of modern antihistamines for treatment of allergic rhinitis - an IPD meta-analysis of 140,853 patients.

    Science.gov (United States)

    Mösges, Ralph; König, Volker; Köberlein, Juliane

    2013-06-01

    Allergic rhinitis represents a worldwide health problem. The prevalence is increasing. The aim of this study was to analyse the correlation between the severity of allergic rhinitis and an adequate treatment dose of modern oral antihistamines. From a comprehensive databank containing data from ten different open-label prospective observational studies including raw data of 140,853 patients with allergic rhinitis, symptomatology variables were analysed and scored to study the effects of treatment with four antihistamines (Desloratadine, Ebastine, Fexofenadine, Levocetirizine) alone or in combination with intranasal corticosteroids. The patient data were collected in 23,606 study centres from Germany, mostly medical specialist and some primary care physicians in private practice. The analyses were performed via individual patient data meta-analysis techniques. Finally 92,900 patient data from nine of ten studies could be analysed. One study with data of 47,953 patients was excluded due to incomplete treatment documentation. Both monotherapy analysis subgroups (Total Symptom Score and Total Nasal Symptom Score) were significantly better than those of their combinations with intranasal steroids. Monotherapy with levocetirizine was determined to be significantly more effective in lowering the Total Symptom Score (p antihistamines. In the next stage, a greater positive effect of levocetirizine was demonstrated in relation to the severity of the clinical symptoms of allergic rhinitis (Total Nasal Symptom Score in cases with severe symptomatology [effect size = -0.09]). Levocetirizine asserted itself as the only antihistamine compared with the others as significant in this analysis. The study authors recommend monotherapy with the new-generation antihistamine levocetirizine, especially in severe cases of allergic rhinitis.

  16. Electrooxidation of antihistamine drug methdilazine and its analysis in human urine and blood samples

    Directory of Open Access Journals (Sweden)

    Nagaraj P. Shetti

    2016-12-01

    Full Text Available The electrochemical oxidation of an antihistamine drug, methdilazine, was studied in 9.2 pH with 0.2 M phosphate buffer as supporting electrolyte at 25 ± 0.2°C. Glassy carbon electrode was used to perform the experiment at cyclic voltammetry, linear sweep voltammetry and differential pulse voltammetric techniques. The dependence of the current on pH, concentration and scan rate were investigated. Differential pulse voltammetric technique was adopted to know the linear relation between peak current and methdilazine concentration. The linear response was obtained in the range of 3.0 μM–1.0 mM with a detection limit of 0.1 μM. The proposed method was also applied for the quantitative determination of methdilazine in pharmaceuticals and biological samples.

  17. Second generation antihistamines in the treatment of seasonal allergic rhinitis due to Parietaria and cypress pollen.

    Science.gov (United States)

    Macchia, L; Caiaffa, M F; Di Paola, R; De Michele, G; Bariletto, G; Iudice, A; Tursi, A

    2001-12-01

    Second generation antihistamines have been employed in the treatment of seasonal allergic rhinitis for many years. However, their effects on two distinctive Mediterranean allergic conditions, viz. Parietaria pollinosis and cypress pollinosis, have been scarcely investigated, so far. A comparative efficacy and side effect trial of astemizole and terfenadine in the treatment of seasonal allergic rhinitis due to either Parietaria or cypress pollen was carried out in 27 adult patients, according to a double-blind, double-dummy parallel-group design. Airborne pollen monitoring allowed comparison of symptom scores with pollen counts. Seven patients (26%) withdrew, due to poor symptom control. In contrast, in a subset of 15 patients who completed the trial, treatment led to a substantial and statistically significant decline in symptom severity in both the astemizole and the terfenadine study group. However, no statistically significant inter-group differences could be detected. Copyright 2001 Academic Press.

  18. Novel Functional Aspect of Antihistamines: The Impact of Bepotastine Besilate on Substance P-Induced Events

    Directory of Open Access Journals (Sweden)

    Shun Kitaba

    2009-01-01

    Full Text Available Besides histamine, substance P (SP has been demonstrated to play a crucial role in pruritic skin diseases. Although antihistamines are frequently used for pruritic skin diseases, little is known concerning the effect on an SP-induced event such as mast cell degranulation and the upregulation of adhesion molecules or the nitric oxide (NO synthesis in endothelial cells. Our aim was to study the effect of bepotastine besilate on SP-induced degranulation of rat basophillic leukemia (RBL-2H3 cells and expression of adhesion molecules and NO synthesis in human dermal microvascular endothelial cells (HMVECs. Bepotastine besilate significantly inhibited SP-induced degranulation of RBL-2H3 cells and NO synthesis in HMVECs. Bepotastine besilate significantly inhibited expression of adhesion molecules in HMVESs, while it failed to suppress SP-induced upregulation of the adhesion molecules in HMVECs. Therefore, bepotastine besilate is assumed to act favorably on SP-induced basophil degranulation and NO synthesis in HMVECs.

  19. Should antihistamines be re-considered as antiasthmatic drugs as adjuvants to anti-leukotrienes?

    Science.gov (United States)

    Bartho, Lorand; Benko, Rita

    2013-02-15

    In spite of histamine mimicking the symptoms of allergic bronchoconstriction and severe anaphylaxis, histamine antagonists most probably represent no effective treatment for these conditions. Anti-leukotrienes proved effective for preventing attacks of allergic asthma. In vitro evidence supports a supra-additive effect of histamine H1 receptor antagonists and anti-leukotrienes in vitro, in asthma models utilizing human bronchi. The same seems to hold true for human allergen provocation tests in vivo. We conclude that combinations of second-generation antihistamines and anti-leukotrienes deserve a large-scale clinical trial for preventing and/or treating attacks of allergic asthma. If useful, these drugs could provide a cost-effective alternative to some recent antiasthmatics. Given that redundant mechanisms may be included in asthma pathophysiology, other combinations (including thromboxane or platelet activating factor antagonists) could also be considered. Copyright © 2013 Elsevier B.V. All rights reserved.

  20. Cost and utilization impacts of oral antihistamines in the California Medi-Cal program.

    Science.gov (United States)

    Hay, Joel W; Leahy, Michael

    2005-01-01

    Newer oral allergic rhinitis (AR) medications, the second-generation antihistamines (SGAs) have gained widespread acceptance because of their efficacy and reduced side effects relative to first-generation antihistamines (FGAs). There are no empirical studies comparing the costs of treatment of SGAs relative to FGAs. We analyzed data from a 20% beneficiary sample (approximately 120,000 continuously enrolled beneficiaries per year) for the Medi-Cal Fee-for-Service program during 1999 to 2000. AR medications available under Medi-Cal included three SGA medications (loratadine, fexofenadine, and cetirizine) and over 200 FGA products containing either diphenhydramine or chlorpheniramine or both. Because multiple medications were evaluated, a sample selection model was estimated using a two-stage multinomial logistic--variance components regression framework. SGA medications have significantly lower total direct health-care treatment costs per patient than FGA medications with costs ranging from US 347 dollars to US 448 dollars less (P < 0.001), despite higher AR medication costs. Total drug expenditures were also not significantly different for patients using SGA or FGA medications despite SGA prescriptions averaging US 47 dollars higher than FGAs. Emergency department visits, inpatient admissions and physician office visits were also significantly lower for patients using SGA medications. Significant cost and utilization reductions were associated with all of the SGA medications relative to FGA drugs, despite their higher acquisition costs. If facing higher copayments for prescription AR drugs, many patients, particularly lower income patients, may choose cheaper over-the-counter (OTC) FGAs rather than SGAs. Our analysis finds this might lead to increased overall health-care treatment costs, unless Medicaid and health insurance plans subsidize OTC AR medications.

  1. Global scanning of antihistamines in the environment: Analysis of occurrence and hazards in aquatic systems.

    Science.gov (United States)

    Kristofco, Lauren A; Brooks, Bryan W

    2017-08-15

    Concentration of the global population is increasingly occurring in megacities and other developing regions, where access to medicines is increasing more rapidly than waste management systems are implemented. Because freshwater and coastal systems are influenced by wastewater effluent discharges of differential quality, exposures in aquatic systems must be considered. Here, we performed a global scanning assessment of antihistamines (AHs), a common class of medicines, in surface waters and effluents. Antihistamines were identified, literature occurrence and ecotoxicology data on AHs collated, therapeutic hazard values (THVs) calculated, and environmental exposure distributions (EEDs) of AHs compared to ecotoxicity thresholds and drug specific THVs to estimate hazards in surface waters and effluents. Literature searches of 62 different AHs in environmental matrices identified 111 unique occurrence publications of 24 specific AHs, largely from Asia-Pacific, Europe, and North America. However, the majority of surface water (63%) and effluent (85%) observations were from Europe and North America, which highlights relatively limited information from many regions, including developing countries and rapidly urbanizing areas in Africa, Latin America and Asia. Less than 10% of all observations were for estuarine or marine systems, though the majority of human populations reside close to coastal habitats. EED 5 th and 95 th centiles for all AHs were 2 and 212ng/L in surface water, 5 and 1308ng/L in effluent and 6 and 4287ng/L in influent, respectively. Unfortunately, global hazards and risks of AHs to non-target species remain poorly understood. However, loratadine observations in surface waters exceeded a THV without an uncertainty factor 40% of the time, indicating future research is needed to understand aquatic toxicology, hazards and risks associated with this AH. This unique global scanning study further illustrates the utility of global assessments of pharmaceuticals

  2. Novos anti-histamínicos: uma visão crítica New antihistamines: a critical view

    Directory of Open Access Journals (Sweden)

    Inês Cristina Camelo-Nunes

    2006-11-01

    Full Text Available OBJETIVO: Avaliar criticamente os mais novos anti-histamínicos anti-H1 e os diferentes termos utilizados para denominá-los, com base na revisão de evidências sobre o papel dos anti-H1 no tratamento das doenças alérgicas. FONTES DOS DADOS: Artigos originais, revisões e consensos indexados nos bancos de dados MEDLINE e PUBMED de 1998 a 2006. Palavra chave: anti-histamínicos. SÍNTESE DOS DADOS: Os anti-histamínicos de segunda geração diferenciam-se dos de primeira geração por sua elevada especificidade e afinidade pelos receptores H1 periféricos e pela menor penetração no sistema nervoso central (SNC, com conseqüente redução dos efeitos sedativos. Embora os anti-histamínicos de segunda geração sejam, geralmente, melhor tolerados do que seus predecessores, alguns efeitos adversos, principalmente cardiotoxicidade, surgiram com alguns deles. Nos últimos 20 anos, novos compostos, com diferentes farmacocinéticas, foram sintetizados. A maioria deles manifesta propriedades antiinflamatórias que independem de sua atividade no receptor H1. Aprimoramentos mais recentes, geralmente na forma de metabólitos ativos, levaram ao uso do termo anti-histamínico de terceira geração. Esse termo surgiu espontaneamente, sem uma descrição clara de seu significado e implicações clínicas, criando grande confusão entre os profissionais da saúde. CONCLUSÕES: Com base nas evidências sobre anti-histamínicos anti-H1, nenhum deles pode ser considerado como "anti-histamínico de terceira geração". Para tanto, seria preciso comprovar que a nova classe de anti-histamínicos possui vantagens clínicas distintas sobre os compostos existentes e preenche pelo menos três pré-requisitos: ausência de cardiotoxicidade, de interações medicamentosas e de efeitos sobre o SNC.OBJECTIVE: To perform a critical evaluation of the more recent H1 antihistamines and the various terms used to describe them, based on a review of evidence on their role in

  3. H1-antihistamine up-dosing in chronic spontaneous urticaria: patients' perspective of effectiveness and side effects--a retrospective survey study.

    Science.gov (United States)

    Weller, Karsten; Ziege, Claudia; Staubach, Petra; Brockow, Knut; Siebenhaar, Frank; Krause, Karoline; Altrichter, Sabine; Church, Martin K; Maurer, Marcus

    2011-01-01

    The guidelines recommend that first line treatment of chronic spontaneous urticaria should be second generation non-sedating H(1)-antihistamines with a positive recommendation against the use of old sedating first generation antihistamines. If standard dosing is not effective, increasing the dosage up to four-fold is recommended. The objective of this study was to obtain the chronic spontaneous urticaria-patient perspective on the effectiveness and unwanted effects of H(1)-antihistamines in standard and higher doses. This was a questionnaire based survey, initially completed by 368 individuals. 319 (248 female, 71 male, median age 42 years) had a physician-confirmed diagnosis of chronic spontaneous urticaria and were included in the results. Participants believed standard doses (manufacturers recommended dose) of second generation antihistamines to be significantly (Pdrugs. Furthermore, they believed that second generation drugs caused significantly (Pantihistamines. Three-quarters of the patients stated that they had up-dosed with antihistamines with 40%, 42% and 54% reporting significant added benefit from taking 2, 3 or 4 tablets daily respectively. The number of reports of unwanted effects and sedation following up-dosing were not significantly different from those reported for standard doses. This survey supports the urticaria guidelines recommendations that the first line treatment for chronic spontaneous urticaria should be second generation rather than first generation H(1)-antihistamines and that, if standard dosing is not effective, the dosage should be increased up to four-fold.

  4. Collision-induced dissociation pathways of H1-antihistamines by electrospray ionization quadrupole time-of-flight mass spectrometry.

    Science.gov (United States)

    Do, Jung-Ah; Noh, Eunyoung; Yoon, Soon-Byung; Lee, Ji Hyun; Park, Sung-Kwan; Mandava, Suresh; Baek, Sun Young; Lee, Jongkook

    2017-06-01

    Over the past decades, mass spectrometry technologies have been developed to obtain mass accuracies of one ppm or less. Of the newly developed technologies, quadrupole time-of-flight mass spectrometry (Q-TOF-MS) has emerged as being well suited to routine and high-throughput analyses of pharmaceuticals. Dietary supplements and functional foods have frequently been found to be contaminated with pharmaceuticals. In our continuous efforts to develop methodologies to protect public health against adulterated dietary supplements, we have constructed a mass spectral database for 21 H 1 -antihistamines encountered as adulterants by using liquid chromatography-electrospray ionization (LC-ESI)/Q-TOF-MS, and have proposed their possible collision-induced dissociation pathways. This database will be very useful for the rapid and accurate detection of H 1 -antihistamines (known) and their analogues (unknown) illegally added to dietary supplements as well as in other sample matrices.

  5. The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

    Directory of Open Access Journals (Sweden)

    Reggie Bosma

    2017-09-01

    Full Text Available The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (Kd or Ki value or target modulation (IC50. However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and modulation is lost. Drug-target residence time is a measure for the lifetime of the drug-target complex, which has recently been receiving considerable interest, as target residence time is shown to have prognostic value for the in vivo efficacy of several drugs. In this study, we have investigated the relation between the increased residence time of antihistamines at the histamine H1 receptor (H1R and the duration of effective target-inhibition by these antagonists. Hela cells, endogenously expressing low levels of the H1R, were incubated with a series of antihistamines and dissociation was initiated by washing away the unbound antihistamines. Using a calcium-sensitive fluorescent dye and a label free, dynamic mass redistribution based assay, functional recovery of the H1R responsiveness was measured by stimulating the cells with histamine over time, and the recovery was quantified as the receptor recovery time. Using these assays, we determined that the receptor recovery time for a set of antihistamines differed more than 40-fold and was highly correlated to their H1R residence times, as determined with competitive radioligand binding experiments to the H1R in a cell homogenate. Thus, the receptor recovery time is proposed as a cell-based and physiologically relevant metric for the lead optimization of G protein-coupled receptor antagonists, like the H1R antagonists. Both, label-free or real-time, classical signaling assays allow an efficient and physiologically relevant determination of kinetic properties of drug molecules.

  6. The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

    Science.gov (United States)

    Bosma, Reggie; Witt, Gesa; Vaas, Lea A. I.; Josimovic, Ivana; Gribbon, Philip; Vischer, Henry F.; Gul, Sheraz; Leurs, Rob

    2017-01-01

    The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (Kd or Ki value) or target modulation (IC50). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and modulation is lost. Drug-target residence time is a measure for the lifetime of the drug-target complex, which has recently been receiving considerable interest, as target residence time is shown to have prognostic value for the in vivo efficacy of several drugs. In this study, we have investigated the relation between the increased residence time of antihistamines at the histamine H1 receptor (H1R) and the duration of effective target-inhibition by these antagonists. Hela cells, endogenously expressing low levels of the H1R, were incubated with a series of antihistamines and dissociation was initiated by washing away the unbound antihistamines. Using a calcium-sensitive fluorescent dye and a label free, dynamic mass redistribution based assay, functional recovery of the H1R responsiveness was measured by stimulating the cells with histamine over time, and the recovery was quantified as the receptor recovery time. Using these assays, we determined that the receptor recovery time for a set of antihistamines differed more than 40-fold and was highly correlated to their H1R residence times, as determined with competitive radioligand binding experiments to the H1R in a cell homogenate. Thus, the receptor recovery time is proposed as a cell-based and physiologically relevant metric for the lead optimization of G protein-coupled receptor antagonists, like the H1R antagonists. Both, label-free or real-time, classical signaling assays allow an efficient and physiologically relevant determination of kinetic properties of drug molecules. PMID:29033838

  7. The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor.

    Science.gov (United States)

    Bosma, Reggie; Witt, Gesa; Vaas, Lea A I; Josimovic, Ivana; Gribbon, Philip; Vischer, Henry F; Gul, Sheraz; Leurs, Rob

    2017-01-01

    The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (K d or K i value) or target modulation (IC 50 ). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and modulation is lost. Drug-target residence time is a measure for the lifetime of the drug-target complex, which has recently been receiving considerable interest, as target residence time is shown to have prognostic value for the in vivo efficacy of several drugs. In this study, we have investigated the relation between the increased residence time of antihistamines at the histamine H 1 receptor (H 1 R) and the duration of effective target-inhibition by these antagonists. Hela cells, endogenously expressing low levels of the H 1 R, were incubated with a series of antihistamines and dissociation was initiated by washing away the unbound antihistamines. Using a calcium-sensitive fluorescent dye and a label free, dynamic mass redistribution based assay, functional recovery of the H 1 R responsiveness was measured by stimulating the cells with histamine over time, and the recovery was quantified as the receptor recovery time . Using these assays, we determined that the receptor recovery time for a set of antihistamines differed more than 40-fold and was highly correlated to their H 1 R residence times, as determined with competitive radioligand binding experiments to the H 1 R in a cell homogenate. Thus, the receptor recovery time is proposed as a cell-based and physiologically relevant metric for the lead optimization of G protein-coupled receptor antagonists, like the H 1 R antagonists. Both, label-free or real-time, classical signaling assays allow an efficient and physiologically relevant determination of kinetic properties of drug molecules.

  8. Super-additive interaction of the reinforcing effects of cocaine and H1-antihistamines in rhesus monkeys

    Science.gov (United States)

    Wang, Zhixia; Woolverton, William L.

    2009-01-01

    Histamine H1 receptor antagonists can be sedating and have behavioral effects, including reinforcing and discriminative stimulus effects in non-humans, that predict abuse liability. Previous research has suggested that antihistamines can enhance the effects of some drugs of abuse. We have reported a synergistic interaction between cocaine and diphenhydramine (DPH) in a self-administration assay with monkeys. The present study was designed to extend those findings to other combinations of cocaine and DPH, and to the mixture of cocaine and another H1-antihistamine, pyrilamine. Rhesus monkeys were prepared with chronic i.v. catheters and allowed to self-administer cocaine, DPH or pyrilamine alone or as mixtures under a progressive-ratio schedule of reinforcement. Cocaine, DPH and pyrilamine alone maintained self-administration and cocaine was the stronger reinforcer. When cocaine was combined with DPH or pyrilamine in a 1:1, 1:2 or 2:1 ratio of the ED50s, the combinations were super-additive as reinforcers. Reinforcing strength of the combinations was greater than that of the antihistamines alone but not greater than cocaine. The data support the prediction that the combination of cocaine and histamine H1 receptor antagonists could have enhanced potential for abuse relative to either drug alone. The interaction may involve dopamine systems in the CNS. PMID:18930758

  9. [New generation antihistamines as monotherapy or in combination. What is the relevance for daily clinical routine for allergic rhinoconjunctivitis].

    Science.gov (United States)

    Mösges, R; Köberlein, J

    2007-06-01

    The guidelines of German and European associations of allergology recommend the treatment of severe allergic rhinitis with a combination of oral antihistamines and nasal steroids. Many patients face this option rather skeptically, so that ENT specialists mostly use antihistamine monotherapy with a higher dosage. This increased dose may cause drowsiness, as has been demonstrated for cetirizine and loratadine. However, ebastine is a non-sedating antihistamine. Furthermore, it has been shown that improved clinical efficacy can be attained with an increased dosage of 20 mg daily in comparison to the usual dosage of 10 mg/day without increasing the rate of side effects. In this prospective post-marketing survey, the treatment of 4,307 patients with allergic rhinitis was documented during the pollen season 2005. The severity of rhinitis symptoms and satisfaction with the treatment were recorded. Treatment with 20 mg ebastine daily as monotherapy led to a significantly greater reduction in symptoms (P=0.002) than the combination therapy. This outcome could be attributed to an assumed better compliance in patients with monotherapy.

  10. Interference of antihistamines and anti-allergic drugs with antigen-induced paw edema in boosted and unboosted mice.

    Science.gov (United States)

    Amorim, C Z; Cordeiro, R S; Vargaftig, B B

    1992-06-17

    The protective effects of two antihistamines and two anti-allergic drugs against anaphylactic paw edema were studied in immunized animals that had or had not received a booster injection of antigen. The injection of 1 or 10 micrograms/paw ovalbumin induced acute paw edema of similar intensity in both groups. The antihistamine meclizine and the mixed anti histamine/anti-5-HT antagonist cyproheptadine reduced the anaphylactic reaction by 55 and 84% respectively, in non-boosted animals and were less effective against edema induced by 1 microgram antigen in boosted animals. The effectiveness of these drugs was also reduced when boosted mice were challenged with 10 micrograms antigen, where meclizine and cyproheptadine inhibited edema by 31 and 59%, respectively. The anti-allergic compounds ketotifen and azelastine, although effective against allergic inflammation in non-boosted mice, had a reduced or no effect in boosted mice. Our results suggest that allergic edema is less sensitive to antihistamine and anti-allergic drugs in boosted mice, which may be accounted for by an increased role of other mediators.

  11. Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.

    Science.gov (United States)

    Chen, Chen

    2008-01-01

    Cetirizine, marketed as a racemic mixture containing both levocetirizine and dextrocetirizine, is a member of the second generation H(1) antihistamines clinically used for the treatment of symptoms associated with seasonal allergic rhinitis. Recently, its single R-enantiomer levocetirizine has been approved by the FDA as the newest antihistamine. Cetirizine is a piperazine derivative related to the first generation H(1) antagonist hydroxyzine, and is the major metabolite in the blood circulation after hydroxyzine administration in humans. The acid functionality of cetirizine in combination with one of the basic nitrogens of piperazine ring makes this compound a very unique zwitterion. The molecular structure of cetirizine allows its carboxylic group to interact with the basic nitrogen via folded conformers, therefore, it possesses relatively high lipophilicity at physiological pH (LogD=1.5). While both cetirizine and hydroxyzine possess high affinity at the H(1) receptor, the R-configured levocetirizine has much slower dissociation rate from the H(1) receptor than R-hydroxyzine, making it an insurmountable antagonist. In addition, the pharmacokinetics of cetirizine significantly differs from those of the basic and lipophilic hydroxyzine. For example, cetirizine has much lower CNS penetration than hydroxyzine, which may be explained by the zwitterionic structure of cetirizine and its P-glycoprotein activity. Cetirizine exhibits high intestinal absorption in humans and its oral bioavailability is estimated to be greater than 70%. Very importantly, cetirizine, especially levocetirizine, has a negligible interaction with the liver enzymes, and is mainly excreted in the urine as the parent despite its high plasma protein binding (88 approximately 96%). The recommended dose of levocetirizine is 5 mg once daily, while its pharmacokinetic half-life is about 7 h in humans. This review will focus on the physicochemical, pharmacological and pharmacokinetic properties of

  12. Ethosomes-based topical delivery system of antihistaminic drug for treatment of skin allergies.

    Science.gov (United States)

    Goindi, Shishu; Dhatt, Bhavnita; Kaur, Amanpreet

    2014-01-01

    Cetirizine is indicated for the treatment of allergic conditions such as insect bites and stings, atopic and contact dermatitis, eczema, urticaria. This investigation deals with development of a novel ethosome-based topical formulation of cetirizine dihydrochloride for effective delivery. The optimised formulation consisting of drug, phospholipon 90 G™ and ethanol was characterised for drug content, entrapment efficiency, pH, vesicular size, spreadability and rheological behaviour. The ex vivo permeation studies through mice skin showed highest permeation flux (16.300 ± 0.300 µg/h/cm(2)) and skin retention (20.686 ± 0.517 µg/cm(2)) for cetirizine-loaded ethosomal vesicles as compared to conventional formulations. The in vivo pharmacodynamic evaluation of optimised formulation was assessed against oxazolone-induced atopic dermatitis (AD) in mice. The parameters evaluated were reduction in scratching score, erythema score, skin hyperplasia and dermal eosinophil count. Our results suggest that ethosomes are effective carriers for dermal delivery of antihistaminic drug, cetirizine, for the treatment of AD.

  13. H1-antihistamine up-dosing in chronic spontaneous urticaria: patients' perspective of effectiveness and side effects--a retrospective survey study.

    Directory of Open Access Journals (Sweden)

    Karsten Weller

    Full Text Available BACKGROUND: The guidelines recommend that first line treatment of chronic spontaneous urticaria should be second generation non-sedating H(1-antihistamines with a positive recommendation against the use of old sedating first generation antihistamines. If standard dosing is not effective, increasing the dosage up to four-fold is recommended. The objective of this study was to obtain the chronic spontaneous urticaria-patient perspective on the effectiveness and unwanted effects of H(1-antihistamines in standard and higher doses. METHODOLOGY/PRINCIPAL FINDINGS: This was a questionnaire based survey, initially completed by 368 individuals. 319 (248 female, 71 male, median age 42 years had a physician-confirmed diagnosis of chronic spontaneous urticaria and were included in the results. Participants believed standard doses (manufacturers recommended dose of second generation antihistamines to be significantly (P<0.005 more effective than first generation drugs. Furthermore, they believed that second generation drugs caused significantly (P<0.001 fewer unwanted effects and caused significantly (P<0.001 less sedation than first generation antihistamines. Three-quarters of the patients stated that they had up-dosed with antihistamines with 40%, 42% and 54% reporting significant added benefit from taking 2, 3 or 4 tablets daily respectively. The number of reports of unwanted effects and sedation following up-dosing were not significantly different from those reported for standard doses. CONCLUSIONS: This survey supports the urticaria guidelines recommendations that the first line treatment for chronic spontaneous urticaria should be second generation rather than first generation H(1-antihistamines and that, if standard dosing is not effective, the dosage should be increased up to four-fold.

  14. Comparison of five new antihistamines (H1-receptor antagonists) in patients with allergic rhinitis using nasal provocation studies and skin tests.

    Science.gov (United States)

    van Steekelenburg, J; Clement, P A R; Beel, M H L

    2002-04-01

    It was the aim of the authors to compare all of the latest second-generation antihistamines and to see if there were significant differences in their efficacy. It is important for ENT specialists to know if these differences exist, as it is for general practitioners trying to choose between these drugs. In 12 confirmed grass pollen allergic patients the authors performed nasal smears to asses eosinophilia, histamine/grass pollen skin tests, and grass pollen nasal provocation tests. All tests were performed before and after administration of one of five different antihistamines (cetirizine, loratadine, ebastine, fexofenadine, mizolastine) or placebo. The order of administration of antihistamines and placebo was randomised, and patients were not aware of which drug they were given. A decrease in nasal eosinophilia (nasal smear), or nasal or skin reactivity (provocation tests) was looked for. A significant decrease in nasal eosinophilia was observed for all antihistamines but not for placebo. For the grass pollen nasal provocation tests, the decrease was significant for nasal blockage and sneezing; for rhinorrhea there was an insignificant decrease that was true for all antihistamines. A significant reduction in histamine/grass pollen skin test reactivity was also observed for all antihistamines, during an 8 h observation period. A significant difference in efficacy between the different antihistamines could not be found with any of the tests performed. For the newer nonsedating H1-antagonists there appears to be no clinically relevant differences in activities--at least not in our study. Preference of the patient may be the most important factor in making a choice between these drugs.

  15. Preseasonal prophylactic treatment with antihistamines suppresses nasal symptoms and expression of histamine H₁ receptor mRNA in the nasal mucosa of patients with pollinosis.

    Science.gov (United States)

    Mizuguchi, H; Kitamura, Y; Kondo, Y; Kuroda, W; Yoshida, H; Miyamoto, Y; Hattori, M; Fukui, H; Takeda, N

    2010-12-01

    Administration of antihistamines 2-4 weeks before the pollen season showed a greater inhibitory effect on nasal allergy symptoms in patients with seasonal allergic rhinitis. However, the mechanism of slow-onset effects of preseasonal treatment with antihistamines remains unclear. Here, we investigated the effect of preseasonal prophylactic treatment with antihistamines on nasal symptoms and the expression of histamine H₁ receptor (H1R) mRNA of the nasal mucosa in patients with cedar pollen pollinosis. During the peak pollen period, the expression of H1R mRNA in the nasal mucosa and the scores of sneezing and watery rhinorrhea in patients receiving preseasonal prophylactic treatment with antihistamines were significantly suppressed in comparison with those in the patients without treatment. Moreover, there was a significant correlation between the nasal symptoms and the expression of H1R mRNA in both patients with or without preseasonal prophylactic treatment. These findings suggest that preseasonal prophylactic treatment with antihistamines is more effective than on-seasonal administration to patients with pollinosis in reducing nasal symptoms during the peak pollen period by suppressing H1R gene expression in the nasal mucosa. Copyright 2010 Prous Science, S.A.U. or its licensors. All rights reserved.

  16. Efficacy of H, antihistamine, corticosteroids and cyclophosphamide in the treatment of chronic dermographic urticaria

    Directory of Open Access Journals (Sweden)

    Kumar Rajesh

    2002-01-01

    Full Text Available H, antihistamines relieve urticaria by blocking the action of histamine on the target tissue, while demonstration of autoantibodies in the sera of a proportion of the patients having chronic idiopathic urticaria, use of immunosuppressive drugs for the treatment of these patients has acquired the greater rationality. We evaluated the role of corticosteroids and cyclophosphamide in the treatment of chronic dermographic urticaria. Twenty-five patients, 13 males and 12 females, between 18-53 years in age, having chronic dermographic urticaria were taken up for this study. The patients were divided into three groups. Group I patients (n=9 were treated with cetirizine hydrochloride 10 mg per day orally, group II patients (n=7 were treated with betamethasone 2 mg along with cyclophosphamide 50 mg along with cetirizine 10 mg per day for a total period of 4 weeks. The patients were evaluated every week to record the therapeutic response and side effects, and then followed up without treatment for a period of 6 months to look for recurrence of the urticaria, if any. Six patients in group I and all the patients in group II and group III had complete remission while the remaining patients in group I had partial relief. The side effects included drowsiness in 4 patients. All the patients in group II had weight gain, 4 patients had acne and 2 patients developed cushingoid features. Majority of the patients relapsed within 3 days after stopping the treatment. Supplementation of the treatment with oral corticosteroids or cyclophosphamide was more effective in controlling the symptoms as compared to cetirizine alone. But a four weeks supplementation was not adequate for preventing the relapses when the drugs were withdrawn.

  17. Computational Analysis of Structure-Based Interactions for Novel H1-Antihistamines

    Science.gov (United States)

    Yang, Yinfeng; Li, Yan; Pan, Yanqiu; Wang, Jinghui; Lin, Feng; Wang, Chao; Zhang, Shuwei; Yang, Ling

    2016-01-01

    As a chronic disorder, insomnia affects approximately 10% of the population at some time during their lives, and its treatment is often challenging. Since the antagonists of the H1 receptor, a protein prevalent in human central nervous system, have been proven as effective therapeutic agents for treating insomnia, the H1 receptor is quite possibly a promising target for developing potent anti-insomnia drugs. For the purpose of understanding the structural actors affecting the antagonism potency, presently a theoretical research of molecular interactions between 129 molecules and the H1 receptor is performed through three-dimensional quantitative structure-activity relationship (3D-QSAR) techniques. The ligand-based comparative molecular similarity indices analysis (CoMSIA) model (Q2 = 0.525, R2ncv = 0.891, R2pred = 0.807) has good quality for predicting the bioactivities of new chemicals. The cross-validated result suggests that the developed models have excellent internal and external predictability and consistency. The obtained contour maps were appraised for affinity trends for the investigated compounds, which provides significantly useful information in the rational drug design of novel anti-insomnia agents. Molecular docking was also performed to investigate the mode of interaction between the ligand and the active site of the receptor. Furthermore, as a supplementary tool to study the docking conformation of the antagonists in the H1 receptor binding pocket, molecular dynamics simulation was also applied, providing insights into the changes in the structure. All of the models and the derived information would, we hope, be of help for developing novel potent histamine H1 receptor antagonists, as well as exploring the H1-antihistamines interaction mechanism. PMID:26797608

  18. Comparative efficacy of steroid nasal spray versus antihistamine nasal spray in allergic rhinitis.

    Science.gov (United States)

    Ghimire, Anand; Das, Balabhadra Prasad; Mishra, Subhash Chandra

    2007-03-01

    This prospective randomized case controlled study was conducted to determine the efficacy of antihistamine (azelastine) nasal spray and compare it to steroid (beclomethasone) nasal spray on the symptoms of allergic rhinitis. Seventy five symptomatic patients of allergic rhinitis were included in this study. Diagnosis was made on the basis of history and physical examination. The patients were divided into three groups randomly. Group A was treated with Azelastine nasal spray, Group B was treated with Beclomethasone nasal spray and Group C was control group and only treated with steam inhalation. Efficacy of the treatment was assessed in the terms of Total Rhinitis Symptom Complex (TSC) scores and individual symptom score which was calculated on the basis of Okuda's grading system. Base line total symptom complex (TSC) scores were reduced in group A and group B by 84.0% after 4 week treatment whereas in group C it was reduced by only 38.0%. Decrease in mean score for sneezing was 95.0% in group A and group B whereas it was only 28.3% in group C. Similarly decrease in mean score for rhinorrhoea in azelastine group was 94.4% and in beclomethasone group was 95.3% in comparison to steam inhalation group where it was 25.0%. Only the beclomethasone reduced nasal stuffiness score significantly by 95.0%. No significant adverse effects of the drugs were observed. The present study establishes the relative efficacy and tolerability ofazelastine nasal spray as compared to beclomethasone nasal spray in symptomatic patients of allergic rhinitis.

  19. Autologous serum therapy in chronic urticaria: A promising complement to antihistamines

    Directory of Open Access Journals (Sweden)

    Panchami Debbarman

    2014-01-01

    Full Text Available Background: Chronic urticaria (CU is a vexing problem and patients of CU suffer from the morbidity that arise from irritable itch and weals and are also subjected to a huge antihistamine pill burden. The symptoms are more in autoreactive urticaria (AU where auto-antibodies in blood flares-up the condition. Search for newer effective modalities which can reduce pill burden is a felt need. Aims: This study evaluates the effectiveness of autologous serum therapy (AST in CU and also determines its usefulness in AU. Materials and Methods: Double blind, parallel group, randomized, controlled study. Fifty four patients were given AST and 57 patients were given injection normal saline (placebo, along with cetirizine in an on-demand basis in both groups. AST/Placebo was given weekly for nine weeks and followed-up for a total period of 24 weeks. AU was diagnosed by autologous serum skin test. Urticaria total severity score (TSS, Urticaria activity score (UAS, Dermatologic life quality index (DLQI was used as primary effectiveness variables. Safety parameters assessed were the spontaneously reported adverse events and laboratory parameters. Results: TSS showed significant improvement from baseline, 7 th week and 8 th week onwards in AST group and placebo group respectively. Group comparison showed significant improvement 4 th week onwards. UAS showed similar results. DLQI showed significant improvement in AST group compared to placebo at the end of study. Both AU and non-AU patients showed comparable improvement of TSS. Conclusion: AST shows promise in treatment of urticaria regardless of the autoreactive nature.

  20. Topical antihistamines display potent anti-inflammatory activity linked in part to enhanced permeability barrier function.

    Science.gov (United States)

    Lin, Tzu-Kai; Man, Mao-Qiang; Santiago, Juan-Luis; Park, Kyungho; Roelandt, Truus; Oda, Yuko; Hupe, Melanie; Crumrine, Debra; Lee, Hae-Jin; Gschwandtner, Maria; Thyssen, Jacob P; Trullas, Carles; Tschachler, Erwin; Feingold, Kenneth R; Elias, Peter M

    2013-02-01

    Systemic antagonists of the histamine type 1 and 2 receptors (H1/2r) are widely used as anti-pruritics and central sedatives, but demonstrate only modest anti-inflammatory activity. Because many inflammatory dermatoses result from defects in cutaneous barrier function, and because keratinocytes express both Hr1 and Hr2, we hypothesized that H1/2r antagonists might be more effective if they were used topically to treat inflammatory dermatoses. Topical H1/2r antagonists additively enhanced permeability barrier homeostasis in normal mouse skin by the following mechanisms: (i) stimulation of epidermal differentiation, leading to thickened cornified envelopes; and (ii) enhanced epidermal lipid synthesis and secretion. As barrier homeostasis was enhanced to a comparable extent in mast cell-deficient mice, with no further improvement following application of topical H1/2r antagonists, H1/2r antagonists likely oppose mast cell-derived histamines. In four immunologically diverse, murine disease models, characterized by either inflammation alone (acute irritant contact dermatitis, acute allergic contact dermatitis) or by prominent barrier abnormalities (subacute allergic contact dermatitis, atopic dermatitis), topical H1/2r agonists aggravated, whereas H1/2r antagonists improved, inflammation and/or barrier function. The apparent ability of topical H1r/2r antagonists to target epidermal H1/2r could translate into increased efficacy in the treatment of inflammatory dermatoses, likely due to decreased inflammation and enhanced barrier function. These results could shift current paradigms of antihistamine utilization from a predominantly systemic to a topical approach.

  1. Comparison of a nasal glucocorticoid, antileukotriene, and a combination of antileukotriene and antihistamine in the treatment of seasonal allergic rhinitis.

    Science.gov (United States)

    Pullerits, Teet; Praks, Lea; Ristioja, Vahur; Lötvall, Jan

    2002-06-01

    Allergic rhinitis requires active intervention for symptom relief. A combination of antileukotriene and antihistamine drugs has been suggested to provide additive treatment benefits for patients with allergic rhinitis. We evaluated how such a combination treatment would affect symptoms and local mucosal eosinophilia in comparison with a nasal glucocorticoid. In a double-blind, randomized study 62 patients with grass pollen-induced allergic rhinitis received a nasal glucocorticoid (fluticasone propionate aqueous nasal spray [FPANS], 200 microg/d), an antileukotriene (montelukast, 10 mg/d), a combination of montelukast with an antihistamine (loratadine, 10 mg/d), or placebo throughout the season. Cromoglycate eyedrops and a limited amount of loratadine were allowed as rescue medication for severe symptoms. Patients recorded their symptoms for nasal blockage, itching, rhinorrhea, and sneezing. Before and during the season, nasal biopsy specimens were obtained from patients for evaluation of local eosinophilic inflammation. During the peak season, both FPANS and combined montelukast-loratadine were significantly more effective than placebo and montelukast alone for daytime symptom prevention. For nighttime symptoms, FPANS was significantly more effective compared with all other treatments, whereas combined montelukast-loratadine and montelukast alone did not provide significant symptom prevention compared with placebo. The pollen-induced increase in the numbers of epithelial eosinophils was significantly lower for FPANS-treated patients compared with that seen in all other treatment groups. In patients with seasonal allergic rhinitis, intranasal glucocorticoids are more effective than an antileukotriene drug or combined antileukotriene-antihistamine for the reduction of pollen-induced nasal eosinophilic inflammation and for control of nasal symptoms.

  2. Rationale for selecting antihistamine drugs for the therapy of chronic urticaria in terms of efficacy and safety

    Directory of Open Access Journals (Sweden)

    O. V. Skorokhodkina

    2014-01-01

    Full Text Available Goal of the study. To compare the efficacy of antihistamine drugs for the therapy of chronic urticaria taking into consideration their effect on the patients’ cognitive functions. Materials and methods. The study involved 178 patients with chronic urticaria who were divided into six groups taking second generation antihistamine drugs: Cetirizine (n = 38, Levocetirizine (n = 27, Fexofenadine (n=26, Ebastine (n = 33, Loratadine (n = 26 and Desloratadine (n = 28. The patients recorded dynamic changes in clinical symptoms of the disease (number of urticarial components, skin itching intensity, availability or absence of urticarial derniographism, angioedema signs and signs of the shortness of breath and reduced blood pressure in their individual diaries. Baseline signs of the patients’ cognitive condition and those recorded during the treatment were studied using the Kraepelin’s arithmetic test (modified by Schulte, I.M. Lushchikhina’s verbal and visual thinking assessment method and method for memorizing ten words. The control group comprised 31 subjects without chronic urticaria. Results of the study. Ebastine and Fexofenadine are the most efficient antihistamine drugs for the treatment of chronic urticaria. At the same time, they do not have any negative effect on the patients’ cognitive functions so they can be recommended for long-term treatment of chronic urticaria. In spite of its evident positive therapeutic effect, Cetirizine reduces mental alertness and deteriorates thinking in patients with chronic urticaria. Because of this, the drug must be prescribed with care for long-term administration to those patients whose professional activities demand increased attention concentration. Loratadine has a positive effect on the patients’ attention and thinking. However, taking into consideration its low efficacy, the drug can be prescribed as the basis therapy for the treatment of light forms of chronic urticaria.

  3. Histamina, receptores de histamina e anti-histamínicos: novos conceitos Histamine, histamine receptors and antihistamines: new concepts

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    Paulo Ricardo Criado

    2010-04-01

    Full Text Available As drogas com ação anti-histamínica estão entre as medicações mais comumente prescritas na prática dermatológica diária, tanto em adultos como em crianças. Este artigo aborda os novos conceitos da função dos receptores de histamina (receptores H1 e discute os efeitos anti-inflamatórios dessas drogas. A segunda geração de anti-histamínicos difere da primeira geração devido a sua elevada especificidade e afinidade pelos receptores H1 periféricos e devido a seu menor efeito no sistema nervoso central, tendo como resultado menores efeitos sedativos. Embora a eficácia dos diferentes anti-histamínicos H1 (anti-H1 no tratamento de doentes alérgicos seja similar, mesmo quando se comparam anti-H1 de primeira e de segunda geração, eles são muito diferentes em termos de estrutura química, farmacologia e propriedades tóxicas. Consequentemente o conhecimento de suas características farmacocinéticas e farmacodinâmicas é importante para a melhor prática médica, especialmente em gestantes, crianças, idosos e doentes com comorbidades.Drugs with antihistamine action are the most commonly prescribed medication in daily dermatologic practice, both to adults and children. This article addresses new concepts of the role of histamine receptors (H1 receptors and discusses the anti-inflammatory effects of these drugs. Second generation antihistamines differs from first generation because of their high specificity and affinity for peripheral H1-receptors. Second generation antihistamines are also less likely to produce sedation because they have less effect on the central nervous system. Although the efficacy of the various H1-antihistamines in the treatment of allergic patients is similar, even when comparing first- and second-generation drugs, these drugs are still very different in terms of their chemical structure, pharmacology and toxic properties. Consequently, knowledge of their pharmacokinetic and pharmacodynamic characteristics

  4. Suppression of histamine- and allergen-induced skin reactions: comparison of first- and second-generation antihistamines.

    Science.gov (United States)

    dos Santos, Rosaly Vieira; Magerl, Markus; Mlynek, Agnieszka; Lima, Hermenio C

    2009-06-01

    Nonsedating antihistamines (nsAHs) are recommended as first-line therapeutics for the treatment of mast cell-driven disorders, including allergic rhinitis and urticaria. However, their superiority over first-generation AHs (fgAHs) has recently been called into question, mainly because of the lack of supporting head-to-head therapeutic studies. To compare the effects of 3 modem nsAHs with those of the fgAH hydroxyzine on histamine- and allergen-induced skin reactions in a controlled, double-blind, clinical trial. Skin prick tests with histamine and Dermatophagoides pteronyssinus extract were performed before and 4 hours after treatment with hydroxyzine, 25 mg; desloratadine, 5 mg; epinastine, 20 mg; fexofenadine, 120 mg; or placebo. Wheal and erythema development was evaluated by digital photography and planimetric analyses. The nsAHs prevented the development of positive reactions to histamine in only 10% to 20% of all individuals tested (n = 75). In contrast, more than 50% of all hydroxyzine-treated individuals showed negative test reactions to histamine (ie, wheals allergic skin reactions. Our results suggest that higher doses of nsAHs than those currently recommended are required for the treatment of skin responses to obtain antihistaminic and antiallergic effects that are equivalent to those of fgAHs.

  5. Bitterness prediction of H1-antihistamines and prediction of masking effects of artificial sweeteners using an electronic tongue.

    Science.gov (United States)

    Ito, Masanori; Ikehama, Kiyoharu; Yoshida, Koichi; Haraguchi, Tamami; Yoshida, Miyako; Wada, Koichi; Uchida, Takahiro

    2013-01-30

    The study objective was to quantitatively predict a drug's bitterness and estimate bitterness masking efficiency using an electronic tongue (e-Tongue). To verify the predicted bitterness by e-Tongue, actual bitterness scores were determined by human sensory testing. In the first study, bitterness intensities of eight H(1)-antihistamines were assessed by comparing the Euclidean distances between the drug and water. The distances seemed not to represent the drug's bitterness, but to be greatly affected by acidic taste. Two sensors were ultimately selected as best suited to bitterness evaluation, and the data obtained from the two sensors depicted the actual taste map of the eight drugs. A bitterness prediction model was established with actual bitterness scores from human sensory testing. Concerning basic bitter substances, such as H(1)-antihistamines, the predictability of bitterness intensity using e-Tongue was considered to be sufficiently promising. In another study, the bitterness masking efficiency when adding an artificial sweetener was estimated using e-Tongue. Epinastine hydrochloride aqueous solutions containing different levels of acesulfame potassium and aspartame were well discriminated by e-Tongue. The bitterness masking efficiency of epinastine hydrochloride with acesulfame potassium was successfully predicted using e-Tongue by several prediction models employed in the study. Copyright © 2012 Elsevier B.V. All rights reserved.

  6. P21 (Cdc42/Rac)-activated kinase 1 (pak1) is associated with cardiotoxicity induced by antihistamines.

    Science.gov (United States)

    Yun, Jaesuk; Kim, So Young; Yoon, Kyung Sik; Shin, Heejung; Jeong, Ho-Sang; Chung, Hyejoo; Kim, Young-Hoon; Shin, Jisoon; Cha, Hye Jin; Han, Kyoung Moon; Hyeon, Seungha; Lee, Tac-Hyung; Park, Hye-Kyung; Kim, Hyung Soo

    2016-12-01

    Astemizole, a non-sedating histamine H 1 receptor blocker, is widely known to cause cardiac arrhythmia, which prolongs the QT interval. However, the precise molecular mechanism involved in antihistamine-induced cardiovascular adverse effects other than hERG channel inhibition is still unclear. In this study, we used DNA microarray analysis to detect the mechanisms involved in life-threatening adverse effects caused by astemizole. Rat primary cardiomyocytes were treated with various concentrations of astemizole for 24 h and the corresponding cell lysates were analyzed using a DNA microarray. Astemizole altered the expression profiles of genes involved in calcium transport/signaling. Using qRT-PCR analysis, we demonstrated that, among those genes, p21 (Cdc42/Rac)-activated kinase 1 (pak1) mRNA was downregulated by treatment with terfenadine and astemizole. Astemizole also reduced pak1 protein levels in rat cardiomyocytes. In addition, astemizole decreased pak1 mRNA and protein levels in H9c2 cells and induced an increase in cell surface area (hypertrophy) and cytotoxicity. Fingolimod hydrochloride (FTY720), a pak1 activator, inhibited astemizole-induced hypertrophy and cytotoxicity in H9c2 cells. These results suggest that antihistamine-induced cardiac adverse effects are associated with pak1 expression and function.

  7. Intranasal corticosteroids compared with oral antihistamines in allergic rhinitis: A systematic review and meta-analysis.

    Science.gov (United States)

    Juel-Berg, Nanna; Darling, Peter; Bolvig, Julie; Foss-Skiftesvik, Majken H; Halken, Susanne; Winther, Lone; Hansen, Kirsten Skamstrup; Askjaer, Nikolaj; Heegaard, Steffen; Madsen, Anders R; Opstrup, Morten S

    2017-01-09

    Intranasal corticosteroids (INS) (corticosteroid nasal sprays) and oral antihistamines (OA) are two of the most common treatments for patients with allergic rhinitis (AR). To our knowledge, there are no systematic reviews on this topic including trials published after 2007. To compare INS with nonsedating OAs as treatments for AR. The systematic review and meta-analysis were based on the Grades of Recommendation, Assessment, Development, and Evaluation principles and the Patient, Intervention, Comparison, and Outcome approach. Primary literature was searched up to January 22, 2015. Criteria for eligibility were randomized controlled trials that compared the efficacy and/or adverse effects of INS and OA in patients with AR. Continuous outcome data were analyzed by using standardized mean differences (SMD) for multiple outcome measures, and mean differences in the case of a single study or outcome. Pooled estimates of effects, 95% confidence interval (CI), were calculated by using random-effects models. The meta-analysis included five randomized controlled trials with a total of 990 patients. INS were superior to OAs in improving total nasal symptoms score (SMD -0.70 [95% CI, -0.93 to -0.47]) and in relieving the following: nasal obstruction (SMD -0.56 [95% CI, -0.82 to -0.29]), rhinorrhea (SMD -0.47 [95% CI, -1.00 to 0.05]), nasal itching (SMD -0.42 [95% CI, -0.65 to -0.18]), sneezing (SMD -0.52 [95% CI, -0.73 to -0.32]), and quality of life mean difference -0.90 [95% CI, -1.18 to -0.62]). There was no difference in relief of ocular symptoms (SMD -0.08 [95% CI, -0.23 to 0.08]). In addition, four randomized controlled trials were included in a narrative analysis. The results in the narrative analysis were comparable with those found in the meta-analysis. INS were superior to OAs in improving nasal symptoms and quality of life in patients with AR.

  8. Anticonvulsant efficacy of antihistamine cyproheptadine in rats exposed to the chemical warfare nerve agent soman.

    Science.gov (United States)

    Winkler, Jennifer L; Skovira, Jacob W; Kan, Robert K

    2017-01-01

    Organophosphate compounds, such as soman and sarin, are highly toxic chemical warfare nerve agents that cause a build-up of acetylcholine in synapses and neuromuscular junctions. Current therapies aim to prevent seizures and protect against brain injury following exposure. The present study was designed to evaluate the effectiveness of the antihistamine cyproheptadine in improving survival and controlling seizures in rats exposed to soman. Rats were pretreated with the oxime reactivator HI-6 (125mg/kg, ip) 30min prior to soman exposure (225μg/kg, sc) and then treated with atropine methylnitrate (AMN, 2.0mg/kg, im) 1min after soman. Cyproheptadine (10, 13, 16 or 20mg/kg, ip) was given at one of three time points: 1min after soman intoxication, at the onset of soman-induced seizures or 5min after seizure onset. Control animals were exposed to soman and given an equivalent volume of sterile water instead of cyproheptadine. The incidence of seizures, mortality, neuron counts, neuropathology and apoptosis in specific regions of the brain were evaluated. In animals given HI-6 and AMN the incidence of soman-induced seizure and mortality rate within the first 24h were 100%. When cyproheptadine was given at a dose of 13 or 20mg/kg 1min after soman exposure, the incidence of seizures was reduced from 100% to 13% and 30%, respectively. In addition, cyproheptadine given at 1min after soman exposure increased the survival rate to 100% regardless of dose. When cyproheptadine was administered at seizure onset, seizures were terminated in 100% of the animals at doses above 10mg/kg. The survival rate with cyproheptadine treatment at the onset of seizure was ≥83%. Seizures terminated in ≥75% of the animals that received cyproheptadine 5min after soman-induced seizure onset. When given at 5min after seizure onset the survival rate was 100% at all tested doses of cyproheptadine. The neuropathology scores and the number of TUNEL positive cells in the brain regions examined

  9. Antihistamine medication may alleviate negative effects of prenatal exposure to polycyclic aromatic hydrocarbons (PAH) on lung function in children. Birth cohort prospective study.

    Science.gov (United States)

    Jedrychowski, Wieslaw A; Perera, Frederica P; Maugeri, Umberto; Majewska, Renata; Spengler, Jack; Mroz, Elzbieta; Flak, Elzbieta; Klimaszewska-Rembiasz, Maria; Camman, David

    2015-05-01

    The main purpose of the present study was to test the hypothesis that the depressed lung growth attributable to prenatal exposure to polycyclic aromatic hydrocarbons (PAH) may be modified by the intake of antihistamine medications. Individual prenatal PAH exposure was assessed by personal air monitoring in 176 children who were followed over nine years, in the course of which outdoor residential air monitoring, allergic skin tests for indoor allergens, lung function tests (FVC, FEV(1), FEV(05), and FEF(25-75)) were performed. The analysis with the General Estimated Equation (GEE) showed no association between prenatal PAH exposure and lung function in the group of children who were reported to be antihistamine users. However, in the group of antihistamine non-users all lung function tests except for FEF(25-75) were significantly and inversely associated with prenatal airborne PAH exposure. The results of the study suggest that the intake of antihistamine medications in early childhood may inhibit the negative effect of fetal PAH exposure on lung growth and provides additional indirect evidence for the hypothesis that lung alterations in young children resulting from PAH exposure may be caused by the allergic inflammation within lung. © 2014 Wiley Periodicals, Inc.

  10. Antihistamines suppress upregulation of histidine decarboxylase gene expression with potencies different from their binding affinities for histamine H1 receptor in toluene 2,4-diisocyanate-sensitized rats

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    Hiroyuki Mizuguchi

    2016-04-01

    Full Text Available Antihistamines inhibit histamine signaling by blocking histamine H1 receptor (H1R or suppressing H1R signaling as inverse agonists. The H1R gene is upregulated in patients with pollinosis, and its expression level is correlated with the severity of nasal symptoms. Here, we show that antihistamine suppressed upregulation of histidine decarboxylase (HDC mRNA expression in patients with pollinosis, and its expression level was correlated with that of H1R mRNA. Certain antihistamines, including mepyramine and diphenhydramine, suppress toluene-2,4-diisocyanate (TDI-induced upregulation of HDC gene expression and increase HDC activity in TDI-sensitized rats. However, d-chlorpheniramine did not demonstrate any effect. The potencies of antihistamine suppressive effects on HDC mRNA elevation were different from their H1R receptor binding affinities. In TDI-sensitized rats, the potencies of antihistamine inhibitory effects on sneezing in the early phase were related to H1R binding. In contrast, the potencies of their inhibitory effects on sneezing in the late phase were correlated with those of suppressive effects on HDC mRNA elevation. Data suggest that in addition to the antihistaminic and inverse agonistic activities, certain antihistamines possess additional properties unrelated to receptor binding and alleviate nasal symptoms in the late phase by inhibiting synthesis and release of histamine by suppressing HDC gene transcription.

  11. Repeated pre-treatment with antihistamines suppresses [corrected] transcriptional up-regulations of histamine H(1) receptor and interleukin-4 genes in toluene-2,4-diisocyanate-sensitized rats.

    Science.gov (United States)

    Mizuguchi, Hiroyuki; Hatano, Masaya; Matsushita, Chiyo; Umehara, Hayato; Kuroda, Wakana; Kitamura, Yoshiyuki; Takeda, Noriaki; Fukui, Hiroyuki

    2008-12-01

    Antihistamines are effective for treatment of seasonal nasal allergy. Recently, prophylactic treatment with antihistamines in patients with pollinosis was reported to be more effective when started before the pollen season. The administration with antihistamines from 2 to 6 weeks before onset of the pollen season is recommended for management of allergic rhinitis in Japan. To determine the reason for the effectiveness of prophylactic treatment with antihistamines, the effects of repeated pre-treatment with antihistamines before provocation with toluene 2,4-diisocyanate (TDI) on their nasal allergy-like behavior and up-regulations of histamine H(1) receptors (H1R) and interleukin (IL)-4 mRNAs in their nasal mucosa were examined. Provocation with TDI induced sneezing and up-regulations of H1R and IL-4 mRNAs in the nasal mucosa of TDI-sensitized rats. Repeated pre-treatments with antihistamines including epinastine, olopatadine, or d-chlorpheniramine for 1 to 5 weeks before provocation with TDI suppressed TDI-induced sneezing and the up-regulations of H1R and IL-4 mRNAs in the nasal mucosa more than their administrations once or for 3 days before TDI provocation. Our data indicate that repeated pre-treatment with antihistamines before provocation with TDI is more effective than their single treatment in reducing nasal allergy-like behavior by causing additional suppression of up-regulations of H1R and IL-4 mRNAs in the nasal mucosa.

  12. Antihistamines suppress upregulation of histidine decarboxylase gene expression with potencies different from their binding affinities for histamine H1 receptor in toluene 2,4-diisocyanate-sensitized rats.

    Science.gov (United States)

    Mizuguchi, Hiroyuki; Das, Asish K; Maeyama, Kazutaka; Dev, Shrabanti; Shahriar, Masum; Kitamura, Yoshiaki; Takeda, Noriaki; Fukui, Hiroyuki

    2016-04-01

    Antihistamines inhibit histamine signaling by blocking histamine H1 receptor (H1R) or suppressing H1R signaling as inverse agonists. The H1R gene is upregulated in patients with pollinosis, and its expression level is correlated with the severity of nasal symptoms. Here, we show that antihistamine suppressed upregulation of histidine decarboxylase (HDC) mRNA expression in patients with pollinosis, and its expression level was correlated with that of H1R mRNA. Certain antihistamines, including mepyramine and diphenhydramine, suppress toluene-2,4-diisocyanate (TDI)-induced upregulation of HDC gene expression and increase HDC activity in TDI-sensitized rats. However, d-chlorpheniramine did not demonstrate any effect. The potencies of antihistamine suppressive effects on HDC mRNA elevation were different from their H1R receptor binding affinities. In TDI-sensitized rats, the potencies of antihistamine inhibitory effects on sneezing in the early phase were related to H1R binding. In contrast, the potencies of their inhibitory effects on sneezing in the late phase were correlated with those of suppressive effects on HDC mRNA elevation. Data suggest that in addition to the antihistaminic and inverse agonistic activities, certain antihistamines possess additional properties unrelated to receptor binding and alleviate nasal symptoms in the late phase by inhibiting synthesis and release of histamine by suppressing HDC gene transcription. Copyright © 2016 The Authors. Production and hosting by Elsevier B.V. All rights reserved.

  13. Association of skeletal muscle relaxers and antihistamines on mortality, hospitalizations, and emergency department visits in elderly patients: a nationwide retrospective cohort study.

    Science.gov (United States)

    Alvarez, Carlos A; Mortensen, Eric M; Makris, Una E; Berlowitz, Dan R; Copeland, Laurel A; Good, Chester B; Amuan, Megan E; Pugh, Mary Jo V

    2015-01-27

    High-risk medication exposure in the elderly is common and associated with increased mortality, hospitalizations, and emergency department (ED) visits. Skeletal muscle relaxants and antihistamines are high-risk medications commonly prescribed in elderly patients. The objective of this study was to determine the association between skeletal muscle relaxants or antihistamines and mortality, hospitalizations, and emergency department visits. This study used a new-user, retrospective cohort design using national Veteran Affairs (VA) data from 128 hospitals. Veterans ≥65 years of age on October 1, 2005 who received VA inpatient/outpatient care at least once in each of fiscal year (FY) 2005 and FY 2006 were included. Exposure to skeletal muscle relaxants and antihistamines was defined by the National Committee for Quality Assurance Healthcare Effectiveness Data and Information Set measures for high-risk medications in the elderly. Primary outcomes identified within one year of exposure were death, ED visit, or hospitalization; ED visits or hospitalizations due to falls and fracture were also assessed. Propensity score matching (1 to 1 match) was used to balance covariates between exposed patients and non-exposed patients. In this cohort of 1,807,404 patients 55,566 patients were included in the propensity-matched cohort for skeletal muscle relaxants and 60,058 patients were included in the propensity-matched cohort for anti-histamines. Mortality was lower in skeletal muscle relaxants-exposed patients (adjusted odds ratio [AOR] 0.87, 95% CI 0.81-0.94), but risk of emergency care (AOR 2.25, 95% CI 2.16-2.33) and hospitalization (AOR 1.56, 95% CI 1.48-1.65) was higher for patients prescribed skeletal muscle relaxants. Similar findings were observed for emergency and hospital care for falls or fractures. Mortality (AOR 1.93, 95% CI 1.82-2.04), ED visits (AOR 2.35, 95% CI 2.27-2.43), and hospitalizations (AOR 2.21, 95% CI 2.11-2.32) were higher in the antihistamine

  14. Proposal of employ of extract of Desmodium adscendens as anti-histaminic natural drug: trials of efficacy by Reflectance Spectrophotometry

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    Lorenzo Martini

    2014-01-01

    Full Text Available Introduction: Aim of our study is to propose the ancient plant Desmodium adscendens, that is hitherto known for combating, when orally administered, a plethora of other ailments and diseases and considered even an anti-histaminic, for external use. An inhibition of histamine depot by inhibiting the enzymatic activity of histidine decarboxylase can be suspected, since biological principles contained in D.A. belong to the same pharmacological class of natural derivatives that elicit the same effects (nicotinic acid, cyanides and quercetine and of synthetic alkylammines (e.g contained in bubble baths. Desmodium adscendens is a perennial plant, growing wild in Africa, especially in Camerun and Ivory Coast as well as in South and Central America and the continent of Asia. Aborigines were accustomed to employ the entire plant for rites of initiation and other shamanistic ceremonies. Notwithstanding, it has been used for thousands of years by peoples native to those areas where it grows for a variety of health issues. This plant has been studied in France, Italy, India and Canada and appreciable are the results with regard to bronchial dilation, relaxation of smooth muscles, antihistamine effects, when orally administered, albeit there is a neat evidence of an extreme paucity of references about its ability to act as a completely natural anti-histaminic herb for external use. Material and Methods: To conduct our study we have recruited 24 volunteers out from 4 cathegories of employees generally suffering from Type I Contact Dermatities. They were prayed to spread the hydroglyceric extract of Desmodium adscendens every morning at 10.00 a.m. and every afternoon at 03.00 p.m onto the skin of forearms and cheeks, where an artificial rash was evoked by the use of a mix made up with allergenic herbs. As far as the evaluation of the degree of severity of skin inflammation is concerned we have used the Reflectance Spectrophotoscopy, to measure the erythematous

  15. Impact of acupuncture on antihistamine use in patients suffering seasonal allergic rhinitis: secondary analysis of results from a randomised controlled trial.

    Science.gov (United States)

    Adam, Daniela; Grabenhenrich, Linus; Ortiz, Miriam; Binting, Sylvia; Reinhold, Thomas; Brinkhaus, Benno

    2018-02-10

    Seasonal allergic rhinitis (SAR) is a common disease that has detrimental effects on the quality of life (QoL) of affected individuals. Approximately 18% of patients try to alleviate their symptoms through acupuncture. The ACUSAR (ACUpuncture in Seasonal Allergic Rhinitis) study (ClinicalTrials.gov registration no. NCT00610584) assessed the impact of acupuncture on SAR, showing significant improvements in rhinitis-specific QoL (RQoL) and in rescue medication (RM) use. A secondary analysis of SAR patients' use of antihistamine. Patients were randomised into three study groups: acupuncture plus RM, sham acupuncture plus RM, and RM alone. The patients documented their medication use before and during the intervention period (8 weeks). The main outcome was the number of days with antihistamine use. Statistical analyses were conducted using parametric and non-parametric tests. The robustness of the results was tested by sensitivity analyses using non-parametric bootstrapping. The data from 414 patients were analysed. The acupuncture group used antihistamines significantly less often compared with the other groups (acupuncture vs sham acupuncture: mean difference -4.49 days, p=0.01; acupuncture vs RM: mean difference -9.15 days, pantihistamine in contrast to only 16% in the RM group. The pre-post comparison suggested that the acupuncture patients did not need to increase the days of antihistamine use to alleviate their symptoms, unlike the other groups. Acupuncture appeared to significantly reduce the number of days of antihistamine use while improving RQoL and SAR symptoms; it can therefore be considered a valuable, additional treatment option for patients with SAR. NCT00610584; Post-results. © Article author(s) (or their employer(s) unless otherwise stated in the text of the article) 2018. All rights reserved. No commercial use is permitted unless otherwise expressly granted.

  16. A randomized placebo-controlled double-blind pilot study of methotrexate in the treatment of H1 antihistamine-resistant chronic spontaneous urticaria

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    Vinod K Sharma

    2014-01-01

    Full Text Available Background: Chronic urticaria not responsive to antihistamines is a difficult disease to manage. Methotrexate has been used in difficult chronic urticarias with some benefit. Objective: To evaluate the efficacy of methotrexate in the treatment of chronic spontaneous urticaria poorly responsive to H1 antihistaminics. Methods: In a randomized double-blind trial at the Department of Dermatology and Venereology of a tertiary care centre, 29 patients with chronic spontaneous urticaria not responding well to H1 antihistaminics were recruited. Patients were randomly allocated to receive either a weekly dose of oral methotrexate 15 mg or placebo (calcium carbonate for a total duration of 12 weeks, after which treatment was stopped and patients were followed up for relapse of urticaria. Each group also received levocetrizine 5 mg once daily for symptom control. Primary outcome measured was a reduction by >2/3 rd of baseline urticaria scores after 12 week therapy. Secondary outcome was a reduction in antihistamine requirement after stopping therapy. Results: Fourteen patients were randomized to the methotrexate group and fifteen patients to the placebo group. Out of 17 patients who completed therapy, the primary outcome was achieved by 3.5 ± 1.9 (out of 10 patients in the methotrexate group and by 3.67 ± 1.03 (out of 7 patients in the placebo group (P > 0.05. Ten patients followed up, after stopping therapy, for a mean period of 3.5 ± 2.4 months; 3 remained in remission and 7 had relapsed. One patient had uncontrollable nausea and vomiting after taking methotrexate and was withdrawn from the study. The placebo group did not experience any side effects. Conclusions: Methotrexate 15 mg weekly for 3 months did not provide any additional benefit over H1 antihistamines in this study but an adequately powered study with longer follow up is required to assess its utility.

  17. Synthesis and anti-inflammatory effects of new piperazine and ethanolamine derivatives of H(1)-antihistaminic drugs.

    Science.gov (United States)

    Ahmadi, Abbas; Khalili, Mohsen; Nafarie, Ali; Yazdani, Arash; Nahri-Niknafs, Babak

    2012-10-01

    In addition to their antihistamine effects, H1-receptor antagonists possess pharmacological properties that are not uniformly distributed among this class of drugs, such as anti-inflammatory, anti-allergic and antiplatelet activities. In this paper, Cyclizine (1-benzhydryl-4-methyl-piperazine, I), bromodiphenhydramine (2-[(4-bromophenyl)-phenylmethoxy]-N, N-dimethylethanamine, II) and some of their new piperazine and ethanolamine derivatives (III-VIII) inducing changes in substitution of phenyl and amine moieties were synthesized and their acute and chronic antiinflammatory effects were evaluated by standard pharmacological tests. The results showed that substitution of phenyl by tolyl, anisol and cumene groups in piperazine family could remarkably decrease acute inflammation in these new drugs. Also, substitution of dimethylamine by morpholine group could not decrease this inflammation in new synthesized ethanolamine family. But the results from the cotton pellet-induced granuloma formation in rats showed that none of drugs (I-VIII) were effective to reduce the chronic inflammation.

  18. Radiation-released histamine in the rhesus monkey as modified by mast cell depletion and antihistamine. Scientific report

    Energy Technology Data Exchange (ETDEWEB)

    Doyle, T.F.; Strike, T.A.

    1975-06-01

    Changes in blood histamine concentrations of rhesus monkeys were measured after a 4000-rad dose of mixed gamma-neutron radiation. All animals were pretreated with amino-guanidine to retard histamine catabolism. Histamine concentrations increased from 26 + or - 13.5 to 235 + or - 16 ng/ml after irradiation. When the animals were pretreated with an antihistamine, chlorpheniramine (3 mg/kg), histamine concentrations changed from 25.7 + or - 13.5 to 462 + or - 226 ng/ml after irradiation. When the monkeys were pretreated with a specific mast cell histamine depleter, compound 48/80 (1mg/kg per day) for four consecutive days and then irradiated (4000 rads), histamine concentrations did not change significantly. When 48/80 was given 20 min after irradiation, histamine concentrations changed from 18 + or - 2 ng/ml to a maximum of 35 + or - 9 ng/ml after 48/80 injection. (Author) (GRA)

  19. Leukotriene receptor antagonists in monotherapy or in combination with antihistamines in the treatment of chronic urticaria: a systematic review

    Directory of Open Access Journals (Sweden)

    Gabriele Di Lorenzo

    2008-12-01

    Full Text Available Gabriele Di Lorenzo1, Alberto D’Alcamo1, Manfredi Rizzo1, Maria Stefania Leto-Barone1, Claudia Lo Bianco1, Vito Ditta1, Donatella Politi1, Francesco Castello1, Ilenia Pepe1, Gaetana Di Fede2, GiovamBattista Rini11Dipartimento di Medicina clinica e delle Patologie Emergenti; 2Dipartimento di Discipline Chirurgiche ed Oncologiche, Università degli Studi di Palermo, ItalyAbstract: In vitro and in vivo clinical and experimental data have suggested that leukotrienes play a key role in inflammatory reactions of the skin. Antileukotriene drugs, ie, leukotriene receptor antagonists and synthesis inhibitors, are a class of anti-inflammatory drugs that have shown clinical efficacy in the management of asthma and in rhinitis with asthma. We searched MEDLINE database and carried out a manual search on journals specializing in allergy and dermatology for the use of antileukotriene drugs in urticaria. Montelukast might be effective in chronic urticaria associated with aspirin (ASA or food additive hypersensitivity or with autoreactivity to intradermal serum injection (ASST when taken with an antihistamine but not in mild or moderate chronic idiopathic urticaria [urticaria without any possible secondary causes (ie, food additive or ASA and other NSAID hypersensitivity, or ASST]. Evidence for the effectiveness of zafirlukast and the 5-lipoxygenase inhibitor, zileuton, in chronic urticaria is mainly anecdotal. In addition, there is anecdotal evidence of effectiveness of antileukotrienes in primary cold urticaria, delayed pressure urticaria and dermographism. No evidence exists for other physical urticarias, including cholinergic, solar and aquagenic urticarias, vibratory angioedema, and exercise-induced anaphylaxis.Keywords: chronic idiopathic urticaria, leukotriene receptor antagonists, montelukast, zafirlukast, antihistamine

  20. Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in psychomotor and driving performance in healthy subjects.

    Science.gov (United States)

    Patat, A; Stubbs, D; Dunmore, C; Ulliac, N; Sexton, B; Zieleniuk, I; Irving, A; Jones, W

    1995-01-01

    The pharmacodynamic interaction between mizolastine, a new H1 antihistamine, and ethanol was assessed in a randomized, double-blind, three-way crossover, placebo-controlled study. Eighteen healthy young male volunteers received mizolastine 10 mg, or cetirizine 10 mg or placebo once daily for 7 days with a 1-week wash-out interval. An oral dose of ethanol or ethanol placebo, given 2 h after dosing on days 5 or 7 of each treatment period, was administered to achieve a peak blood alcohol concentration (BAC) of 0.7 g/l then maintained for 1 h by two further doses of ethanol. Driving ability and psychomotor performance were evaluated using actual and simulated driving tests, critical flicker fusion threshold (CFF), adaptive tracking and divided attention (DAT) tasks. Ethanol produced a significant decrement in all tasks up to 5.5 h after administration: an increase in steering movements of 4.6, in lateral deviation of 0.45 m, in braking reaction time of 80 ms, in driving test and DAT performance of + 3.2; and a decrease in CFF and in tracking speed of 2.6 m.s-1. Neither mizolastine nor cetirizine significantly impaired driving ability or arousal (CFF) compared with the placebo. However, both drugs significantly impaired DAT performance 6:00 h post-dose (increase of + 2.1 for mizolastine and + 2.4 for cetirizine). The tracking speed was significantly decreased 7:50 h after mizolastine administration (-1.3 m.s-1) and more consistently from 1:30 to 7:50 h after cetirizine administration (-1.4 m.s-1). No significant adverse interaction, i.e. potentiation, occurred between ethanol and either antihistamine.(ABSTRACT TRUNCATED AT 250 WORDS)

  1. H1-antihistamine-refractory chronic spontaneous urticaria: it's worse than we thought - first results of the multicenter real-life AWARE study.

    Science.gov (United States)

    Maurer, M; Staubach, P; Raap, U; Richter-Huhn, G; Bauer, A; Ruëff, F; Jakob, T; Yazdi, A S; Mahler, V; Wagner, N; Lippert, U; Hillen, U; Schwinn, A; Pawlak, M; Behnke, N; Chaouche, K; Chapman-Rothe, N

    2017-05-01

    Most data on chronic spontaneous urticaria (CSU) originate from highly selected patient populations treated at specialized centres. Little is known about CSU patient characteristics and the burden of CSU in routine clinical practice. AWARE (A World-wide Antihistamine-Refractory chronic urticaria patient Evaluation) is an ongoing global study designed to assess chronic urticaria in the real-life setting. To describe the baseline characteristics of the first 1539 German AWARE patients with H1-antihistamine-refractory CSU. This prospective non-interventional study included patients (18-75 years) with a diagnosis of H1-antihistamine-refractory CSU for > 2 months. Baseline demographic and disease characteristics, comorbidities, and pharmacological treatments were recorded. Quality of life (QoL) was assessed using the dermatology life quality index (DLQI), chronic urticaria QoL questionnaire (CU-Q 2 oL), and angioedema QoL questionnaire (AE-QoL, in cases of angioedema). Previous healthcare resource utilization and sick leave data were collected retrospectively. Between March and December 2014, 1539 patients were assessed in 256 sites across Germany. The percentage of females, mean age, and mean body mass index were 70%, 46.3 years, and 27 kg/m 2 , respectively. The mean urticaria control test score was 7.9, one in two patients had angioedema, and the most frequent comorbidities were chronic inducible urticaria (CIndU; 24%), allergic rhinitis (18.2%), hypertension (18.1%), asthma (12%), and depression (9.5%). Overall, 57.6% of patients were receiving at least one pharmacological treatment including second-generation H1-antihistamines (46.3%), first-generation H1-antihistamines (9.1%), and corticosteroids (15.8%). The mean DLQI, total CU-Q 2 oL, and total AE-QoL scores were 8.3, 36.2, and 46.8, respectively. CSU patients reported frequent use of healthcare resources, including emergency services (29.7%), general practitioners (71.9%), and additional allergists or

  2. Can Twitter Be a Source of Information on Allergy? Correlation of Pollen Counts with Tweets Reporting Symptoms of Allergic Rhinoconjunctivitis and Names of Antihistamine Drugs.

    Directory of Open Access Journals (Sweden)

    Francesco Gesualdo

    Full Text Available Pollen forecasts are in use everywhere to inform therapeutic decisions for patients with allergic rhinoconjunctivitis (ARC. We exploited data derived from Twitter in order to identify tweets reporting a combination of symptoms consistent with a case definition of ARC and those reporting the name of an antihistamine drug. In order to increase the sensitivity of the system, we applied an algorithm aimed at automatically identifying jargon expressions related to medical terms. We compared weekly Twitter trends with National Allergy Bureau weekly pollen counts derived from US stations, and found a high correlation of the sum of the total pollen counts from each stations with tweets reporting ARC symptoms (Pearson's correlation coefficient: 0.95 and with tweets reporting antihistamine drug names (Pearson's correlation coefficient: 0.93. Longitude and latitude of the pollen stations affected the strength of the correlation. Twitter and other social networks may play a role in allergic disease surveillance and in signaling drug consumptions trends.

  3. Simultaneous determination of ten antihistamine drugs in human plasma using pipette tip solid-phase extraction and gas chromatography/mass spectrometry.

    Science.gov (United States)

    Hasegawa, Chika; Kumazawa, Takeshi; Lee, Xiao-Pen; Fujishiro, Masaya; Kuriki, Ayako; Marumo, Akemi; Seno, Hiroshi; Sato, Keizo

    2006-01-01

    Ten antihistamine drugs, diphenhydramine, orphenadrine, chlorpheniramine, diphenylpyraline, triprolidine, promethazine, homochlorcyclizine, cyproheptadine, cloperastine and clemastine, have been found to be extractable from human plasma samples using MonoTip C18 tips, inside which C18- bonded monolithic silica gel was fixed. Human plasma (0.1 mL) containing the ten antihistamines was mixed with 0.4 mL of distilled water and 25 microL of a 1 M potassium phosphate buffer (pH 8.0). After centrifugation of the mixture, the supernatant fraction was extracted to the C18 phase of the tip by 25 repeated aspirating/dispensing cycles using a manual micropipettor. The analytes retained on the C18 phase were then eluted with methanol by five repeated aspirating/dispensing cycles. The eluate was injected into a gas chromatography (GC) injector without evaporation and reconstitution steps, and was detected by a mass spectrometer with selected ion monitoring in the positive-ion electron impact mode. The separation of the ten drugs from each other and from impurities was generally satisfactory using a DB-1MS column (30 m x 0.32 mm i.d., film thickness 0.25 microm). The recoveries of the ten antihistamines spiked into plasma were 73.8-105%. The regression equations for the ten antihistamines showed excellent linearity with detection limits of 0.02-5.0 ng/0.1 mL. The within-day and day-to-day coefficients of variation for plasma were not greater than 9.9%. The data obtained from determination of diphenhydramine and chlorpheniramine in human plasma after oral administration of the drugs are also presented. Copyright 2006 John Wiley & Sons, Ltd.

  4. The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicity

    Czech Academy of Sciences Publication Activity Database

    Králová, Jana; Račková, L.; Pekarová, Michaela; Kubala, Lukáš; Nosál, R.; Jančinová, V.; Číž, Milan; Lojek, Antonín

    2009-01-01

    Roč. 9, 7-8 (2009), s. 990-995 ISSN 1567-5769 R&D Projects: GA AV ČR(CZ) 1QS500040507; GA ČR(CZ) GA525/06/1196 Institutional research plan: CEZ:AV0Z50040507; CEZ:AV0Z50040702 Keywords : H1-antihistamines * nitric oxide * inducible nitric oxide synthase Subject RIV: BO - Biophysics Impact factor: 2.214, year: 2009

  5. Effect of treatment with intranasal corticosteroid and oral antihistamine on cytokine profiles of peripheral blood mononuclear cells of patients with allergic rhinitis sensitive to chenopodium album.

    Science.gov (United States)

    Farrokhi, Shokrollah; Mousavi, Tahereh; Arshi, Saba; Javahertarash, Naser; Varasteh, Abdolreza; Falak, Reza; Rezaei, Nima; Salekmoghadam, Alireza

    2010-12-01

    Patients with allergic rhinitis (AR) show increased production of the Th2-related cytokines. Almost always, intranasal corticosteroid (INC) and antihistamine are used as routine therapy of AR. This study was performed to determine the in vitro secretion of cytokines profiles of PBMCs in patients with AR sensitive to Chenopodium album (Ch.a) pollens before and after treatment with INC (Fluticasone propionate) and oral antihistamine (Loratadine). PBMCs of 20 patients with AR, were tested in vitro for cytokine production. These cells were stimulated with natural or recombinant Ch.a. The levels of IL-4, IL-13 and IFN-, were measured in supernatants of cultured cell 96h after stimulation using ELISA. The PBMCs of 20 normal individuals were also similarly treared for comparison of results. The production of IL-4 by the patients' cells stimulated with either Ch.a or rCh.a was significantly higher than normal levels before therapy (p=0.04 and p=0.02, respectively). After therapy, a significant decrease in production of IL-4 and a significant increase in production of IL-10 were found in PBMCs stimulated with natural Ch.a, in comparison to the results before stimulation (p=0.03 for IL-4; p=0.04 for IL-10). Similarly, these results were seen in the production of IL-4 and IL-10 stimulated with rCh.a allergen after therapy in comparison to the results before stimulation (p=0.01 for IL-4; p=0.03 for IL-10). This study suggests INC (Fluticasone propionate) and oral antihistamine (Loratadine) have the capacity to inhibit the production of IL-4 and shift Th2/Th1 responses, probably due to increase the level of immunoregulatory IL-10. Therefore, it could be concluded that therapy with INC and antihistamine has pharmacologic and immunologic therapeutic effects on AR patients.

  6. Road traffic crash risk associated with prescription of hydroxyzine and other sedating H1-antihistamines: A responsibility and case-crossover study.

    Science.gov (United States)

    Orriols, Ludivine; Luxcey, Audrey; Contrand, Benjamin; Bénard-Laribière, Anne; Pariente, Antoine; Gadegbeku, Blandine; Lagarde, Emmanuel

    2017-09-01

    H1 antihistamines differ from each other by their ability to cross the blood-brain barrier. The resulting sedating effect can be sought in therapy but may be a driving hazard. The aim of this study was to estimate the impact of sedating H1-antihistamines on the risk of road traffic crash, with a particular focus on hydroxyzine which is also indicated as an anxiolytic in France. The study consisted in extracting and matching data from three French nationwide databases: the national healthcare insurance database, police reports and the police national database of injurious crashes. All sedating H1-antihistamines, including hydroxyzine, were considered in the study. A case-control analysis, in which responsible drivers were cases and non-responsible were controls was performed. A case-crossover analysis, comparing for the same subject exposure during a period immediately before the crash with exposure during an earlier period, was also conducted. The extraction and matching procedures over the July 2005-December 2011 period led to the inclusion of 142,771 drivers involved in an injurious road traffic crash. The responsibility study found an increased risk of being responsible for an injurious road traffic crash in hydroxyzine users who were registered with a long-term chronic disease (mostly psychiatric disorders) on the day of the crash (OR=1.67 [1.22-2.30]). Among them, the risk was even higher in drivers with highest exposure levels (OR=2.60 [1.23-5.50]). There was no impact of sedating H1 antihistamine treatment initiation on the risk of crash. Even if it is difficult to disentangle the part of the increased risk that would be causally related to hydroxyzine and the part related to behaviours of patients with a heavy psychiatric disorder, our study raises the alarm on the crash risk linked to hydroxyzine utilization in countries in which the anxiolytic indication is widespread. Copyright © 2017 Elsevier Ltd. All rights reserved.

  7. Next-day residual sedative effect after nighttime administration of an over-the-counter antihistamine sleep aid, diphenhydramine, measured by positron emission tomography.

    Science.gov (United States)

    Zhang, Dongying; Tashiro, Manabu; Shibuya, Katsuhiko; Okamura, Nobuyuki; Funaki, Yoshihito; Yoshikawa, Takeo; Kato, Masato; Yanai, Kazuhiko

    2010-12-01

    Antihistamines often are self-administered at night as over-the-counter (OTC) sleep aids, but their next-day residual sedative effect has never been evaluated using a reliable quantitative method such as positron emission tomography (PET). We performed a double-blind, placebo-controlled, crossover study in which we evaluated the residual effect the next day after nighttime administration of diphenhydramine, a commonly used OTC sleep aid, in terms of brain H₁ receptor occupancy (H₁RO) measured using ¹¹C-doxepin-PET. We also compared the results of diphenhydramine with those of bepotastine, a second-generation antihistamine. Eight healthy adult male subjects underwent PET measurement the morning (11:00) after random oral administration of diphenhydramine (50 mg), bepotastine (10 mg), or placebo the night before (23:00). Binding potential ratios and H₁ROs were calculated in different brain regions of interest such as the cingulate gyrus, frontotemporal cortex, and cerebellum. Subjective sleepiness and plasma drug concentration also were measured. Calculation of binding potential ratios revealed significantly lower values for diphenhydramine than for bepotastine or placebo in all regions of interest (P drug or the placebo. In conclusion, the next-day residual sedative effect after nighttime administration of the OTC sleep aid diphenhydramine was verified for the first time by direct PET measurement of H₁RO. Taking into account the possible hangover effect of OTC antihistamine sleep aids, care needs to be taken during their administration.

  8. Cerebral histamine H1 receptor binding potential measured with PET under a test dose of olopatadine, an antihistamine, is reduced after repeated administration of olopatadine.

    Science.gov (United States)

    Senda, Michio; Kubo, Nobuo; Adachi, Kazuhiko; Ikari, Yasuhiko; Matsumoto, Keiichi; Shimizu, Keiji; Tominaga, Hideyuki

    2009-06-01

    Some antihistamine drugs that are used for rhinitis and pollinosis have a sedative effect as they enter the brain and block the H(1) receptor, potentially causing serious accidents. Receptor occupancy has been measured with PET under single-dose administration in humans to classify antihistamines as more sedating or as less sedating (or nonsedating). In this study, the effect of repeated administration of olopatadine, an antihistamine, on the cerebral H(1) receptor was measured with PET. A total of 17 young men with rhinitis underwent dynamic brain PET with (11)C-doxepin at baseline, under an initial single dose of 5 mg of olopatadine (acute scan), and under another 5-mg dose after repeated administration of olopatadine at 10 mg/d for 4 wk (chronic scan). The H(1) receptor binding potential was estimated using Logan graphical analysis with cerebellum as reference region input. The acute scan showed a slight decrease in H(1) receptor binding potential across the cerebral cortex (by 15% in the frontal cortex), but the chronic scan showed a marked decrease (by 45% from the acute scan in the frontal cortex). Behavioral data before and after the PET scans did not reveal any sedative effect. The results may be interpreted as either intracerebral accumulation of olopatadine or H(1) receptor downregulation due to repeated administration. The study shows feasibility and potential value for PET in evaluating the pharmacologic effect of a drug not only after a single dose but also after repeated administration.

  9. Night-time sedating H1-antihistamine increases daytime somnolence but not treatment efficacy in chronic spontaneous urticaria: a randomized controlled trial

    Science.gov (United States)

    Staevska, M; Gugutkova, M; Lazarova, C; Kralimarkova, T; Dimitrov, V; Zuberbier, T; Church, MK; Popov, TA

    2014-01-01

    Background Many physicians believe that the most effective way to treat chronic urticaria is to take a nonsedating second-generation H1-antihistamine in the morning and a sedating first-generation H1-antihistamine, usually hydroxyzine, at night to enhance sleep. But is this belief well founded? Objectives To test this belief by comparing the effectiveness and prevalence of unwanted sedative effects when treating patients with chronic spontaneous urticaria (CSU) with levocetirizine 15 mg daily plus hydroxyzine 50 mg at night (levocetirizine plus hydroxyzine) vs. levocetirizine 20 mg daily (levocetirizine monotherapy). Methods In this randomized, double-blind, cross-over study, 24 patients with difficult-to-treat CSU took levocetirizine plus hydroxyzine or levocetirizine monotherapy for periods of 5 days each. At the end of each treatment period, assessments were made of quality of life (Chronic Urticaria Quality of Life Questionnaire, CU-Q2oL), severity of urticaria symptoms (Urticaria Activity Score, UAS), sleep disturbance during the night and daytime somnolence. Results Both treatments significantly decreased UAS, night-time sleep disturbances and CU-Q2oL scores (P urticaria guidelines, which state that first-line treatment for urticaria should be new-generation, nonsedating H1-antihistamines only. PMID:24472058

  10. Ginecomastia induzida por anti-histamínicos no tratamento da urticária crônica Antihistaminic-induced gynecomastia in chronic urticaria treatment

    Directory of Open Access Journals (Sweden)

    Ana Paula Fusel de Ue

    2007-06-01

    Full Text Available Os anti-histamínicos são drogas muito usadas na prática do dermatologista, sendo a primeira escolha no tratamento da urticária crônica. Os efeitos colaterais mais comuns são os relacionados ao sistema nervoso central. A ginecomastia é decorrente de várias causas, entre elas a indução por drogas. Apresenta-se caso de ginecomastia induzida por anti-histamínico H1,em paciente em tratamento de urticária crônica. A investigação laboratorial e radiológica descartou outras causas para a ginecomastia, que involuiu com a retirada da medicação. Objetiva-se discutir os efeitos colaterais dos anti-histamínicos e apresentar caso de ginecomastia induzida por drogas.Antihistaminic drugs are very commonly used in dermatological practice, and are the first-line therapy to chronic urticaria. The commonest side effects are related to the central nervous system. Gynecomastia, in turn, may be due to a myriad of disorders, including the use of medication. The case of H1 antihistaminic-induced gynecomastia in a patient undergoing chronic urticaria treatment is reported. Radiological and laboratorial investigations discarded other possible causes for the gynecomastia, which disappeared after removal of the medication. Antihistaminic-related side effects, including gynecomastia, are discussed.

  11. Effects of antihistamine on up-regulation of histamine H1 receptor mRNA in the nasal mucosa of patients with pollinosis induced by controlled cedar pollen challenge in an environmental exposure unit

    Directory of Open Access Journals (Sweden)

    Yoshiaki Kitamura

    2015-11-01

    Full Text Available In the present study, we examined the effects of antihistamine on the up-regulation of H1R mRNA in the nasal mucosa of patients with pollinosis induced by controlled exposure to pollen using an environmental exposure unit. Out of 20 patients, we designated 14 responders, whose levels of H1R mRNA in the nasal mucosa were increased after the first pollen exposure and excluded 6 non-responders. Accordingly, the first exposure to pollen without treatment significantly induced both nasal symptoms and the up-regulation of H1R mRNA in the nasal mucosa of the responders. Subsequently, prophylactic administration of antihistamine prior to the second pollen exposure significantly inhibited both of the above effects in the responders. Moreover, the nasal expression of H1R mRNA before the second pollen exposure in the responders pretreated with antihistamine was significantly decreased, as compared with that before the first pollen exposure without treatment. These findings suggest that antihistamines suppressed histamine-induced transcriptional activation of H1R gene in the nasal mucosa, in addition to their blocking effect against histamine on H1R, resulting in a decrease of nasal symptoms. These findings further suggest that by their inverse agonistic activity, antihistamines suppress the basal transcription of nasal H1R in the absence of histamine in responders.

  12. Effects of antihistamine on up-regulation of histamine H1 receptor mRNA in the nasal mucosa of patients with pollinosis induced by controlled cedar pollen challenge in an environmental exposure unit.

    Science.gov (United States)

    Kitamura, Yoshiaki; Nakagawa, Hideyuki; Fujii, Tatsuya; Sakoda, Takema; Enomoto, Tadao; Mizuguchi, Hiroyuki; Fukui, Hiroyuki; Takeda, Noriaki

    2015-11-01

    In the present study, we examined the effects of antihistamine on the up-regulation of H1R mRNA in the nasal mucosa of patients with pollinosis induced by controlled exposure to pollen using an environmental exposure unit. Out of 20 patients, we designated 14 responders, whose levels of H1R mRNA in the nasal mucosa were increased after the first pollen exposure and excluded 6 non-responders. Accordingly, the first exposure to pollen without treatment significantly induced both nasal symptoms and the up-regulation of H1R mRNA in the nasal mucosa of the responders. Subsequently, prophylactic administration of antihistamine prior to the second pollen exposure significantly inhibited both of the above effects in the responders. Moreover, the nasal expression of H1R mRNA before the second pollen exposure in the responders pretreated with antihistamine was significantly decreased, as compared with that before the first pollen exposure without treatment. These findings suggest that antihistamines suppressed histamine-induced transcriptional activation of H1R gene in the nasal mucosa, in addition to their blocking effect against histamine on H1R, resulting in a decrease of nasal symptoms. These findings further suggest that by their inverse agonistic activity, antihistamines suppress the basal transcription of nasal H1R in the absence of histamine in responders. Copyright © 2015 Japanese Pharmacological Society. Production and hosting by Elsevier B.V. All rights reserved.

  13. Antihistamines do not inhibit the wheal induced by the intradermal injection of autologous serum in resistant chronic idiopathic urticaria.

    Science.gov (United States)

    Magen, Eli; Mishal, Joseph; Zeldin, Yuri; Schlesinger, Menachem

    2012-01-01

    Some patients with chronic idiopathic urticaria (CIU) are resistant to conventional doses of antihistamines (AHs). This study was designed to check whether the skin wheal and flare reaction produced by the intradermal injection of autologous serum (AS) and by histamine differs in AH-resistant and AH responder CIU patients. CIU patients with treatment failure under fexofenadine at 180 mg q.d. increased their daily dose of AH to 4 tablets daily. Those with significant improvement of urticaria activity score under fexofenadine at 180 mg were included in the CIU group. Subjects with treatment failure despite a full 8-week fourfold fexofenadine treatment were included in the resistant CIU (R-CIU group). The control group consisted of sex- and age-matched patents with allergic rhinitis. The AS skin test and intradermal histamine-induced wheal and flare reaction were performed at baseline (without AH), after 8 and 16 weeks (under AH treatment). Forty-six subjects were included in the CIU group, 21 were in the R-CIU group, and 44 were in the control group. Under AH therapy, the skin reaction to intradermal histamine injection was significantly diminished in all study groups. In the R-CIU group, fexofenadine at 180 mg did not suppress AS-induced wheal reaction (5.96 ± 2.25 mm; p = 0.85), and with a fourfold AH dose some reduction of AS-induced wheal (3.79 ± 1.74 mm; p = 0.008) was observed but remained larger than in the CIU (2.31 ± 1.12; p = 0.006) and control groups (2.52 ± 1.36; p = 0.037). AHs do not inhibit the wheal induced by the intradermal injection of AS in R-CIU.

  14. Effect of disodium cromoglycate (DSCG) and antihistamines on postirradiation cerebral blood flow and plasma levels of histamine and neurotensin

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Pautler, E.L.; Carraway, R.E.; Cochrane, D.E.; Hampton, J.D.

    1988-02-01

    In an attempt to elucidate mechanisms underlying the irradiation-induced decrease in regional cerebral blood flow (rCBF) in primates, hippocampal and visual cortical blood flows of rhesus monkeys were measured by hydrogen clearance, before and after exposure to 100 Gy, whole-body, gamma irradiation. Systemic blood pressures were monitored simultaneously. Systemic arterial plasma histamine and neurotensin levels were determined preirradiation and postirradiation. Compared to control animals, the irradiated monkeys exhibited an abrupt decline in systemic blood pressure to 23% of the preirradiation level within 10 min postirradiation, falling to 12% by 60 min. A decrease in hippocampal blood flow to 32% of the preirradiation level was noted at 10 min postirradiation, followed by a slight recovery to 43% at 30 min and a decline to 23% by 60 min. The cortical blood flow for the same animals showed a steady decrease to 29% of the preirradiation levels by 60 min postirradiation. Animals given the mast cell stabilizer disodium cromoglycate and the antihistamines mepyramine and cimetidine before irradiation did not exhibit an abrupt decline in blood pressure but displayed a gradual decrease to a level 33% below preirradiation levels by 60 min postirradiation. Also, the treated, irradiated monkeys displayed rCBF values that were not significantly different from the nonirradiated controls. The plasma neurotensin levels in the irradiated animals, treated and untreated, indicated a nonsignificant postirradiation increase above control levels. However, the postirradiation plasma histamine levels in both irradiated groups showed an increase of approximately 1600% above the preirradiation levels and the postirradiation control levels.

  15. [Treatment of nausea and vomiting with 5HT3 receptor antagonists, steroids, antihistamines, anticholinergics, somatostatinantagonists, benzodiazepines and cannabinoids in palliative care patients : a systematic review].

    Science.gov (United States)

    Benze, G; Geyer, A; Alt-Epping, B; Nauck, F

    2012-09-01

    Various recommendations exist for the treatment of nausea and vomiting in palliative care but only few studies and even less systematic reviews look into antiemetic therapy for patients receiving palliative care. This systematic review aims to analyze the current evidence for antiemetic treatment with 5HT3 receptor antagonists, steroids, antihistamines, anticholinergics, somatostatin analogs, benzodiazepines and cannabinoids in palliative care patients with far advanced cancer not receiving chemotherapy or radiotherapy, acquired immune deficiency syndrome (AIDS), chronic obstructive pulmonary disease (COPD), progressive heart failure, amyotrophic lateral sclerosis (ALS) or multiple sclerosis (MS). Results regarding evidence of treatment with prokinetic and neuroleptic agents will be published separately. The electronic databases PubMed and EmBase were systematically searched for studies (published 1966-2011) dealing with antiemetic therapy in palliative care and electronic retrieval was completed by manual searching. Studies with patients undergoing chemotherapy or radiotherapy, pediatric studies and studies published in languages other than English or German were excluded. Studies addressing therapy with 5HT3 receptor antagonists, steroids, antihistamines, anticholinergics, somatostatin analogs, benzodiazepines or cannabinoids were identified and selected for this systematic review. In the general search 75 relevant studies were found. Of those 36 addressed 5HT3 receptor antagonists, steroids, antihistamines, anticholinergics, somatostatin analogs, benzodiazepines and cannabinoids, 13 considered 5HT3 receptor antagonists, 10 somatostatin antagonists, 9 steroids, 5 cannabinoids, 4 anticholinergics, 1 antihistamines and none benzodiazepines. Furthermore six systematic reviews exist. Evidence for any drug used as an antiemetic is low. Concerning 5HT3 receptor antagonists data are insufficient for recommendations on the treatment of patients with AIDS and MS due to

  16. Assessment of efficacy and impact on work productivity and attendance after a mandatory switch to generic second-generation antihistamines: results of a patient survey in Norway

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    Ødegård Tone

    2011-02-01

    Full Text Available Abstract Background In 2006, the Norwegian Medicines Agency mandated a switch from desloratadine, ebastine, or fexofenadine to cetirizine or loratadine in patients with allergic rhinitis (AR or chronic urticaria (CU. In an online survey, patients whose medication was switched assessed the impact on efficacy, fatigue, and work productivity/attendance. Methods Allergy patients in Norway completed a 25-item online survey. Patients aged ≥ 18 years with AR or CU who were switched to cetirizine or loratadine from desloratadine, ebastine, or fexofenadine were included. Participants rated post-switch efficacy, fatigue, and effect on work productivity/attendance compared with their pre-switch medication. Patients also reported post-switch change in number of doctor visits required, total treatment cost, and whether they had switched or wanted to switch back to their previous medications. Results Of 1920 patients invited, 493 responded and 409 of these were eligible. Previous antihistamines were desloratadine (78.4% of respondents, ebastine (16.0%, and fexofenadine (5.6%. Post-switch, 64.7% received cetirizine and 35.3% loratadine. Compared with previous therapy, cetirizine and loratadine were rated less effective by 46.3% of respondents; 28.7% reported increased fatigue; and 31.6% reported decreased work productivity with the generic agents. At the time of the survey, 26% of respondents had switched back to their previous medication. Conclusions This is the first survey to assess the impact on patient-reported outcomes of a mandated switch from prescription to generic antihistamines in Norway. The findings suggest that patient response to different antihistamines will vary and that treatment decisions should be individualized for optimal results.

  17. The importance of taking a history of over-the-counter medication use: a brief review and case illustration of "PRN" antihistamine dependence in a hospitalized adolescent.

    Science.gov (United States)

    Gracious, Barbara; Abe, Naomi; Sundberg, Jane

    2010-12-01

    Over-the-counter (OTC) and prescription medication abuse has been rapidly increasing, yet publications on OTC abuse in adolescents are limited. We present a brief literature review and a novel report of antihistamine dependence emerging after admission in an adolescent, subsequently treated with naltrexone. This case highlights the need to take a thorough history of OTC, herbal, and prescription drug use from parents and patients separately and repeatedly, at initial presentation, and again if withdrawal symptoms emerge. General strategies for combating OTC and prescription abuse are given.

  18. FT-IR and FT-Raman spectra, molecular structure and first-order molecular hyperpolarizabilities of a potential antihistaminic drug, cyproheptadine HCl

    Science.gov (United States)

    Sagdinc, Seda G.; Erdas, Dilek; Gunduz, Ilknur; Sahinturk, Ayse Erbay

    2015-01-01

    Cyproheptadine hydrochloride (CYP HCl) {4-(5H-dibenzo[a,d]-cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride} is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local-anesthetic properties. The geometry optimization, Mulliken atomic charges and wavenumber and intensity of the vibrational bands of all of the possible modes of CYP HCl have been calculated using ab initio Hartree-Fock (HF) and density functional theory (DFT) employing the B3LYP functional with the 6-311G(d,p) basis set. We have compared the calculated IR and Raman wavenumbers with experimental data. Quantum-chemical calculations of the geometrical structure, energies, and molecular electrostatic potential and NBO analysis of CYP HCl have been performed using the B3LYP/6-311G(d,p) method. The electric dipole moment (μ), static polarizability (α) and the first hyperpolarizability (β) values of the title compound have been computed using HF and DFT methods. The study reveals that the antihistaminic pharmacological property of CYP HCl has a large β value and, hence, may in general have potential applications in the development of non-linear optical materials. The experimental and calculated results for CYP HCl have also been compared with those for mianserin HCl.

  19. Efficacy of single dose antihistamine vs. single dose valerian-hops in subjective sleep measures among war refugees: a comparison trial

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    Omar Salem Gammoh

    Full Text Available Abstract Background Many sedatives and anxiolytics are used in single dose or chronically to aid sleep. Clinically important sedatives include valerian-hops and antihistamines as they are used over the counter and are highly accessible and safe agents. Objectives To evaluate and compare a single dose of chlorpheniramine versus valerian-hops combination in modulating subjective sleep measures in insomniac war refugees. Methods Insomnia among refugees was screened using the Insomnia Severity Index (ISI. Insomniac subjects were randomized to received a single dose valerian-hops (320/80 mg (n = 65, or chlorpheneramine (4 mg (n = 50 or placebo (n = 76 two hours prior sleeping. Participants were instructed to complete Leeds Sleep Evaluation Questionnaire (LSEQ, visual analogue scales of anxiety and sedation. Also sleep latency, total hours slept and self-rated improvement were obtained. Results Almost 75% of screened refugees had insomnia. Chlorpheneramine reduced sleep latency and anxiety significantly, however it resulted in poor sleep quality. Valerian-hops group showed marked anxiolysis one hour after dosing, a sleep quality similar to placebo and better than chlorpheneramine, and better alertness compared to placebo. Participants satisfaction was higher with chlorpheneramine and there was no difference in the total hours slept. Discussion Valerian-hops combination may provide better sleep quality than antihistamines.

  20. New model for prediction binary mixture of antihistamine decongestant using artificial neural networks and least squares support vector machine by spectrophotometry method

    Science.gov (United States)

    Mofavvaz, Shirin; Sohrabi, Mahmoud Reza; Nezamzadeh-Ejhieh, Alireza

    2017-07-01

    In the present study, artificial neural networks (ANNs) and least squares support vector machines (LS-SVM) as intelligent methods based on absorption spectra in the range of 230-300 nm have been used for determination of antihistamine decongestant contents. In the first step, one type of network (feed-forward back-propagation) from the artificial neural network with two different training algorithms, Levenberg-Marquardt (LM) and gradient descent with momentum and adaptive learning rate back-propagation (GDX) algorithm, were employed and their performance was evaluated. The performance of the LM algorithm was better than the GDX algorithm. In the second one, the radial basis network was utilized and results compared with the previous network. In the last one, the other intelligent method named least squares support vector machine was proposed to construct the antihistamine decongestant prediction model and the results were compared with two of the aforementioned networks. The values of the statistical parameters mean square error (MSE), Regression coefficient (R2), correlation coefficient (r) and also mean recovery (%), relative standard deviation (RSD) used for selecting the best model between these methods. Moreover, the proposed methods were compared to the high- performance liquid chromatography (HPLC) as a reference method. One way analysis of variance (ANOVA) test at the 95% confidence level applied to the comparison results of suggested and reference methods that there were no significant differences between them.

  1. Position statement of the Brazilian Academy of Rhinology on the use of antihistamines, antileukotrienes, and oral corticosteroids in the treatment of inflammatory sinonasal diseases.

    Science.gov (United States)

    Mion, Olavo de Godoy; Mello, João Ferreira de; Dutra, Daniel Lorena; Andrade, Nilvano Alves de; Almeida, Washington Luiz de Cerqueira; Anselmo-Lima, Wilma Teresinha; Filho, Leonardo Lopes Balsalobre; Carvalho E Castro, Jair de; Guimarães, Roberto Eustáquio Dos Santos; Lessa, Marcus Miranda; Maniglia, Sérgio Fabrício; Meireles, Roberto Campos; Nakanishi, Márcio; Pignatari, Shirley Shizue Nagata; Roithmann, Renato; Romano, Fabrizio Ricci; Santos, Rodrigo de Paula; Santos, Marco César Jorge Dos; Tamashiro, Edwin

    Inflammatory conditions of the nose and paranasal sinuses are very prevalent in the general population, resulting in marked loss of quality of life in affected patients, as well as significant work, leisure, and social activity losses. These patients require specific and specialized treatment. A wide range of oral medications are available. The present document is aimed to clarify, for professionals treating patients with inflammatory sinonasal diseases, both specialists and general practitioners, specific oral therapies in noninfectious nasal inflammatory conditions. The methodology used to create this article included the search for the key words: oral corticosteroids, antihistamines, antileukotrienes, rhinitis, rhinosinusitis in the MEDLINE and EMBASE databases in the last 5 years. Since no relevant article was found for the text on the subject of interest in the last 5 years, the search was extended for another 5 years, and so on, according to the authors' needs. Relevant literature was found regarding the use of antihistamines, antileukotrienes and oral corticosteroids in these conditions. The Brazilian Academy of Rhinology emphasizes, after extensive discussion by the collegiate, key points in the treatment with these drugs. There is support in the literature for the use of these drugs; however, final considerations about the role of each of them have been made. Copyright © 2017. Published by Elsevier Editora Ltda.

  2. Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract of Zanthoxylum alatum seeds on isolated tissue preparations: An ex vivo study.

    Science.gov (United States)

    Saikia, Beenita; Barua, Chandana Choudhury; Haloi, Prakash; Patowary, Pompy

    2017-01-01

    The aim of this study was to evaluate anticholinergic, antihistaminic, and antiserotonergic activity of the n-hexane extract of the seeds of Zanthoxylum alatum (ZAHE) on isolated ileum of rat and guinea pig and fundus of rat. ZAHE was prepared using soxhlet extraction and cumulative concentration response curves were constructed using various doses on the tissues for acetylcholine (ACh), 5-hydroxytryptamine (5-HT), and histamine with or without n-hexane extract. Atropine, ketanserin, and pheniramine maleate were used as antagonists for ACh, serotonin, and histamine, respectively. ZAHE-induced concentration-dependent inhibition of isolated ileum and fundus in rat and ileum of guinea pig. The half maximal effective concentration (EC 50 ) of ACh in the presence of atropine (10 -6 M; P pheniramine maleate (10 -6 M; P < 0.01) and ZAHE (300 μg/ml; P < 0.01 and 1000 μg/ml; P < 0.05) was also significantly higher than EC 50 of histamine alone. From the study, it was observed that ZAHE shows significant anticholinergic, antiserotonergic, and antihistaminic activity. The study provides sufficient evidence that the seeds can be used in gastric disorders, cough, chest infection, etc., as per folklore claims.

  3. Preseasonal prophylactic treatment with antihistamines suppresses IL-5 but not IL-33 mRNA expression in the nasal mucosa of patients with seasonal allergic rhinitis caused by Japanese cedar pollen.

    Science.gov (United States)

    Kitamura, Yoshiaki; Mizuguchi, Hiroyuki; Ogishi, Hirotaka; Kuroda, Wakana; Hattori, Masashi; Fukui, Hiroyuki; Takeda, Noriaki

    2012-04-01

    These findings suggest that the down-regulation of interleukin (IL)-5 gene expression in collaboration with the suppression of histamine H(1) receptor (H1R) gene expression in the nasal mucosa provides the basis for better therapeutic effects of preseasonal prophylactic treatment with antihistamines in patients with seasonal allergic rhinitis caused by Japanese cedar pollen. The effects of prophylactic administration of antihistamines on the expression of IL-5 and IL-33 mRNA in the nasal mucosa of the patients with pollinosis were investigated. Eight patients had already visited the hospital before the peak pollen period and started preseasonal prophylactic treatment with antihistamines. Seventeen patients who first visited the hospital during the peak pollen period were designated as the no treatment group. After local anesthesia, nasal mucosa was obtained by scraping the inferior concha with a small spatula during the peak pollen period. During the peak pollen period, the expression of IL-5 mRNA, but not that of IL-33 mRNA, in the nasal mucosa of patients receiving preseasonal prophylactic treatment with antihistamines was significantly lower in comparison with that of patients without treatment. Moreover, there was a significant correlation between the expression of IL-5 mRNA and the nasal symptoms or the expression of H1R mRNA.

  4. IC Treatment: Antihistamines

    Science.gov (United States)

    ... IC Epidemiology (RICE) Study Boston Area Community Health (BACH) Survey ICA Pilot Research Program Funding Opportunities Clinical ... IC Epidemiology (RICE) Study Boston Area Community Health (BACH) Survey ICA Pilot Research Program Funding Opportunities Clinical ...

  5. Efficacy and Safety of Omalizumab in Patients with Chronic Idiopathic/Spontaneous Urticaria Who Remain Symptomatic on H1 Antihistamines: A Randomized, Placebo-Controlled Study

    Science.gov (United States)

    Saini, Sarbjit S; Bindslev-Jensen, Carsten; Maurer, Marcus; Grob, Jean-Jacques; Bülbül Baskan, Emel; Bradley, Mary S; Canvin, Janice; Rahmaoui, Abdelkader; Georgiou, Panayiotis; Alpan, Oral; Spector, Sheldon; Rosén, Karin

    2015-01-01

    ASTERIA I was a 40-week, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of subcutaneous omalizumab as add-on therapy for 24 weeks in patients with chronic idiopathic urticaria/spontaneous urticaria (CIU/CSU) who remained symptomatic despite H1 antihistamine treatment at licensed doses. Patients aged 12–75 years with CIU/CSU who remained symptomatic despite treatment with approved doses of H1 antihistamines were randomized (1:1:1:1) in a double-blind manner to subcutaneous omalizumab 75 mg, 150 mg, or 300 mg or placebo every 4 weeks for 24 weeks followed by 16 weeks of follow-up. The primary end point was change from baseline in weekly itch severity score (ISS) at week 12. Among randomized patients (N=319: placebo n=80, omalizumab 75 mg n=78, 150 mg n=80, 300 mg n=81), 262 (82.1%) completed the study. Compared with placebo (n=80), mean weekly ISS was reduced from baseline to week 12 by an additional 2.96 points (95% confidence interval (CI): −4.71 to −1.21; P=0.0010), 2.95 points (95% CI: −4.72 to −1.18; P=0.0012), and 5.80 points (95% CI: −7.49 to −4.10; Pomalizumab 75-mg (n=77), 150-mg (n=80), and 300-mg groups (n=81), respectively. The omalizumab 300-mg group met all nine secondary end points, including a significant decrease in the duration of time to reach minimally important difference response (⩾5-point decrease) in weekly ISS (Pomalizumab 75-mg, 150-mg, 300-mg, and placebo groups, respectively, experienced a serious adverse event. Omalizumab 300 mg administered subcutaneously every 4 weeks reduced weekly ISS and other symptom scores versus placebo in CIU/CSU patients who remained symptomatic despite treatment with approved doses of H1 antihistamines. PMID:25046337

  6. Evaluation of cytotoxic action of antihistamines – desloratadine and loratadine – using bulls spermatozoa as a test object

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    O. Kuzminov

    2014-02-01

    Full Text Available Antihistamines with active ingredients of loratadine and desloratadine are produced by Ukrainian pharmaceutical industry. According to the law, ther are assessed for their potential danger to human health and the environment, including alternative test objects. Evaluation has been carried out with regard to cytotoxic effect of pharmacological substances (loratadine and desloratadine using the bull sperm suspension as test objects, standardized and highly sensitive to toxic substances. Sperm was divided into the control sample (dissolved by phosphate-buffered saline and the investigated sample. Loratadine was added to phosphate-buffered saline in doses of 1/500 LD50 (12.3 mg, 1/100 LD50 (61.5 mg and LD50 (6150 mg. Desloratadine doses were 1/500 LD50 (1.25 mg, 1/100 LD50 (6.25 mg and LD50 (625 mg. Survival of spermatozoa was defined until termination of rectilinear forward movement in sperm intacted at +2…+5 °C. Respiratory activity (ex tempore was defined in 1.0 ml thermostated cell (temperature of 38.5 °C by polarography with the automatic registration of process flow by potentiometer; restorative activity was defined potentiometrically, using the open microelectrodes that were inserted in thermostated polarographic cell. Survival of spermatozoa in the sperm under the impact of loratadine in doses of 1/500 LD50 and 1/100 LD50 is respectively 136.0 ± 26.2 hours and 144.0 ± 19.6 hours. Adding LD50 dose of loratadine reduced survival to 112.0 ± 26.2 hours, which is lower than the control (160.0 ± 26.1 hours, respectively, by 10.0–15.0 and 30.0%. Loratadine reduces the respiratory activity of sperm: in the dose of 1/500 LD50 by 20.5%, in the dose of 1/100 LD50 – by 43.6%, and that of 100 LD50 – by 61.5% compared to the control. Restorative sperm activity under the impact of the loratadine reduced by 84.0% (dose of 1/500 LD50, 98.0% (dose of 1/100 LD50, 80.0% (dose LD50 compared to controls. The survival of spermatozoa in the sperm

  7. Misuse and dependence on non-prescription codeine analgesics or sedative H1 antihistamines by adults: a cross-sectional investigation in France.

    Science.gov (United States)

    Roussin, Anne; Bouyssi, Annabelle; Pouché, Lucie; Pourcel, Laure; Lapeyre-Mestre, Maryse

    2013-01-01

    Given the growing worldwide market of non-prescription drugs, monitoring their misuse in the context of self-medication represents a particular challenge in Public Health. The aim of this study was to investigate the prevalence of misuse, abuse, and dependence on non-prescription psychoactive drugs. During one month, in randomly solicited community pharmacies, an anonymous questionnaire was offered to adults requesting paracetamol (control group), codeine combined with paracetamol in analgesics, or sedative H1 antihistamines. Responses about misuse (drug use not in agreement with the Patient Information Leaflet) abuse (excessive drug use having detrimental consequences), and dependence (established according to questions adapted from the Diagnostic and Statistical Manual of Mental Disorders, 4th Edition criteria) on psychoactive drugs were compared to those of the paracetamol control group. 295 patients (mean age 48.5 years, 68.5% of women) having used one of the studied drugs during the previous month were included. Misuse and dependence to codeine analgesics concerned 6.8% and 17.8% of the patients exposed to these drugs, respectively, (n = 118), which was significantly higher than for paracetamol. 19.5% had used codeine analgesics daily for more than six months. Headache was the most frequent reason for persistent daily use. A high prevalence of persistent daily users of sedative H1 antihistamines was also observed. Whereas these drugs are recommended only for short treatment courses of occasional insomnia, 72.2% of the participants having taken doxylamine (n = 36) were daily users, predominantly for more than six months. Results on misuse and dependence on non-prescription codeine analgesics suggest that chronic pain, in particular chronic cephalalgia, requires better medical care. In addition, as for hypnotics on prescription, persistent use of doxylamine for self-medication is not justified until an acceptable benefit-risk ratio for chronic sleep

  8. Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract of Zanthoxylum alatum seeds on isolated tissue preparations: An ex vivo study

    Science.gov (United States)

    Saikia, Beenita; Barua, Chandana Choudhury; Haloi, Prakash; Patowary, Pompy

    2017-01-01

    Objectives: The aim of this study was to evaluate anticholinergic, antihistaminic, and antiserotonergic activity of the n-hexane extract of the seeds of Zanthoxylum alatum (ZAHE) on isolated ileum of rat and guinea pig and fundus of rat. Materials and Methods: ZAHE was prepared using soxhlet extraction and cumulative concentration response curves were constructed using various doses on the tissues for acetylcholine (ACh), 5-hydroxytryptamine (5-HT), and histamine with or without n-hexane extract. Atropine, ketanserin, and pheniramine maleate were used as antagonists for ACh, serotonin, and histamine, respectively. Results: ZAHE-induced concentration-dependent inhibition of isolated ileum and fundus in rat and ileum of guinea pig. The half maximal effective concentration (EC50) of ACh in the presence of atropine (10−6 M; P < 0.05) and ZAHE (1000 μg/ml; P < 0.01) was significantly higher than EC50of ACh alone. The EC50of 5-HT in the presence of ketanserin (10−5 M; P < 0.01) and ZAHE (1000 μg/ml; P < 0.05) was higher than EC50of 5-HT alone. Similarly, the EC50of histamine in the presence of pheniramine maleate (10−6 M; P < 0.01) and ZAHE (300 μg/ml; P < 0.01 and 1000 μg/ml; P < 0.05) was also significantly higher than EC50of histamine alone. Conclusion: From the study, it was observed that ZAHE shows significant anticholinergic, antiserotonergic, and antihistaminic activity. The study provides sufficient evidence that the seeds can be used in gastric disorders, cough, chest infection, etc., as per folklore claims. PMID:28458421

  9. Misuse and dependence on non-prescription codeine analgesics or sedative H1 antihistamines by adults: a cross-sectional investigation in France.

    Directory of Open Access Journals (Sweden)

    Anne Roussin

    Full Text Available BACKGROUND: Given the growing worldwide market of non-prescription drugs, monitoring their misuse in the context of self-medication represents a particular challenge in Public Health. The aim of this study was to investigate the prevalence of misuse, abuse, and dependence on non-prescription psychoactive drugs. METHOD: During one month, in randomly solicited community pharmacies, an anonymous questionnaire was offered to adults requesting paracetamol (control group, codeine combined with paracetamol in analgesics, or sedative H1 antihistamines. Responses about misuse (drug use not in agreement with the Patient Information Leaflet abuse (excessive drug use having detrimental consequences, and dependence (established according to questions adapted from the Diagnostic and Statistical Manual of Mental Disorders, 4th Edition criteria on psychoactive drugs were compared to those of the paracetamol control group. RESULTS: 295 patients (mean age 48.5 years, 68.5% of women having used one of the studied drugs during the previous month were included. Misuse and dependence to codeine analgesics concerned 6.8% and 17.8% of the patients exposed to these drugs, respectively, (n = 118, which was significantly higher than for paracetamol. 19.5% had used codeine analgesics daily for more than six months. Headache was the most frequent reason for persistent daily use. A high prevalence of persistent daily users of sedative H1 antihistamines was also observed. Whereas these drugs are recommended only for short treatment courses of occasional insomnia, 72.2% of the participants having taken doxylamine (n = 36 were daily users, predominantly for more than six months. CONCLUSIONS: Results on misuse and dependence on non-prescription codeine analgesics suggest that chronic pain, in particular chronic cephalalgia, requires better medical care. In addition, as for hypnotics on prescription, persistent use of doxylamine for self-medication is not justified until

  10. Evidence for the hERG Liability of Antihistamines, Antipsychotics, and Anti-Infective Agents: A Systematic Literature Review From the ARITMO Project.

    Science.gov (United States)

    Hazell, Lorna; Raschi, Emanuel; De Ponti, Fabrizio; Thomas, Simon H L; Salvo, Francesco; Ahlberg Helgee, Ernst; Boyer, Scott; Sturkenboom, Miriam; Shakir, Saad

    2017-05-01

    A systematic review was performed to categorize the hERG (human ether-a-go-go-related gene) liability of antihistamines, antipsychotics, and anti-infectives and to compare it with current clinical risk of torsade de pointes (TdP). Eligible studies were hERG assays reporting half-minimal inhibitory concentrations (IC50). A "hERG safety margin" was calculated from the IC50 divided by the peak human plasma concentration (free C max ). A margin below 30 defined hERG liability. Each drug was assigned an "uncertainty score" based on volume, consistency, precision, and internal and external validity of evidence. The hERG liability was compared to existing knowledge on TdP risk (www.credibledrugs.org). Of 1828 studies, 82 were eligible, allowing calculation of safety margins for 61 drugs. Thirty-one drugs (51%) had evidence of hERG liability including 6 with no previous mention of TdP risk (eg, desloratadine, lopinavir). Conversely, 16 drugs (26%) had no evidence of hERG liability including 6 with known, or at least conditional or possible, TdP risk (eg, chlorpromazine, sulpiride). The main sources of uncertainty were the validity of the experimental conditions used (antihistamines and antipsychotics) and nonuse of reference compounds (anti-infectives). In summary, hERG liability was categorized for 3 widely used drug classes, incorporating a qualitative assessment of the strength of available evidence. Some concordance with TdP risk was observed, although several drugs had hERG liability without evidence of clinical risk and vice versa. This may be due to gaps in clinical evidence, limitations of hERG/C max data, or other patient/drug-specific factors that contribute to real-life TdP risk. © 2016, The American College of Clinical Pharmacology.

  11. Two-step targeting and dosimetry for small cell lung cancer xenograft with anti-NCAM/antihistamine bispecific antibody and radioiodinated bivalent hapten.

    Science.gov (United States)

    Hosono, M; Hosono, M N; Kraeber-Bodéré, F; Devys, A; Thédrez, P; Faivre-Chauvet, A; Gautherot, E; Barbet, J; Chatal, J F

    1999-07-01

    The "affinity enhancement system," a two-step targeting technique using bispecific antibody and radiolabeled bivalent hapten, has been reported to be useful for carcinoembryonic antigen-expressing tumors. The purpose of this study was to evaluate the efficacy of this method for targeting human small cell lung cancer using an antineural cell adhesion molecule antibody. Antineural cell adhesion molecule/antihistamine bispecific antibody NK1NBL1-679 was prepared by coupling an equimolecular quantity of a Fab' fragment of NK1NBL1 to a Fab fragment of antihistamine 679. Athymic mice inoculated with NCI-H69 small cell lung cancer cells expressing neural cell adhesion molecule were administered bispecific antibody and then 48 h later 125I-labeled bivalent histamine hapten. 125I-labeled intact NK1NBL1 was injected into other groups of mice. Biodistributions were examined as a function of time. In mice of the two-step targeting, tumor uptake was 2.5 +/- 0.2, 3.2 +/- 0.4, 6.4 +/- 2.0, 7.2 +/- 2.7, 6.1 +/- 2.1 and 2.2 +/- 0.4 %ID/g at 5, 30 min, 5, 24, 48 and 96 h, and tumor-to-blood, tumor-to-liver and tumor-to-kidney ratios were 1.4 +/- 1.1, 10.8 +/- 13.2 and 4.6 +/- 4.7, respectively, at 5 h, whereas 125I-labeled NK1NBL1 showed a tumor uptake of 5.7 +/- 0.4 %ID/g and tumor-to-blood, tumor-to-liver and tumor-to-kidney ratios of 0.3 +/- 0.1, 1.1 +/- 0.2 and 0.9 +/- 0.1, respectively, at 5 h. These results were confirmed by autoradiographic studies, which demonstrated clear tumor-to-normal tissue contrast. Dosimetry showed that the affinity enhancement system could enhance the therapeutic potential of the antineural cell adhesion molecule antibody NK1NBL1. This two-step targeting method seems promising for the diagnosis and therapy of small cell lung cancer.

  12. A comparison of intranasal corticosteroid, leukotriene receptor antagonist, and topical antihistamine in reducing symptoms of perennial allergic rhinitis as assessed through the Rhinitis Severity Score.

    Science.gov (United States)

    Sardana, Niti; Santos, Carah; Lehman, Erik; Craig, Timothy

    2010-01-01

    Rhinitis symptom complex consists of rhinorrhea, congestion, itchy mucosa, itchy eyes, and sneezing. Available medications vary in their benefit for each of these symptoms. It was the purpose of this article to compare symptom reduction with three different classes of medications. Montelukast, azelastine, and budesonide were compared to determine the effect on individual, as well as total, symptom scores using the Rhinitis Severity Score (RSS). All three medications were compared with placebo and showed efficacy in prior studies using Balaam's crossover design. The inclusion and exclusion criteria and all procedures were identical for all three studies. In analyzing the data from the RSS questionnaire, we used the procedure PROC MIXED in SAS specific for Balaam's crossover design (SAS Institute, Inc., Cary, NC). Although all three medications were effective compared with placebo, montelukast had the greatest effect of the three medications on reduction of ocular itching and throat and palate itching. Azelastine's effect was greater than budesonide and montelukast for reduction of rhinorrhea. Systemic medication, montelukast, as expected, provided better relief for symptoms distant from the nasal cavity, and the antihistamine, azelastine, reduced rhinorrhea, more than either montelukast or budesonide.

  13. Effect of disodium cromoglycate (DSCG) and antihistamines on post-irradiation cerebral blood flow and plasma levels of histamine and neurotensin

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Pautler, E.L.; Carraway, R.E.; Cochrane, D.E.; Hampton, J.D.

    1988-01-01

    In an attempt to elucidate mechanisms underlying the irradiation-induced decrease in regional cerebral blood flow (rCBF) in primates, hippocampal and visual cortical blood flows of rhesus monkeys were measured by hydrogen clearance, before and after exposure to 100-Gy, whole-body, gamma irradiation. Systemic blood pressures were monitored simultaneously. Systemic arterial plasma histamine and neurotensin levels were determined preirradiation and postirradiation. Compared to control animals, the irradiated monkeys exhibited an abrupt decline in systemic blood pressure to 23% of the preirradiation level within 10-min postirradiation, falling to 12% by 60 min. A decrease in hippocampal blood flow to 32% of the preirradiation level was noted at 10-min postirradiation, followed by a slight recovery to 43% at 30 min and a decline to 23% by 60 min. The cortical blood flow for the same animals showed a steady decrease to 29% of the preirradiation levels by 60-min postirradiation. Animals given the mast-cell stabilizer disodium cromoglycate and the antihistamines mepyramine and cimetidine before irradiation did not exhibit an abrupt decline in blood pressure but displayed a gradual decrease to a level 33% below preirradiation levels by 60 min postirradiation. Also, the treated, irradiated monkeys displayed rCBF values that were not significantly different from the nonirradiated controls. The plasma neurotensin levels in the irradiated animals, treated and untreated, indicated a nonsignificant postirradiation increase above control levels.

  14. Fiber optic LDF to monitor vascular dynamics of urticarial dermographism in pressure-tested patients before and after treatment with antihistamines

    Science.gov (United States)

    Eikje, Natalja Skrebova; Arase, Seiji

    2008-02-01

    The local microcirculatory dynamics underlying phenomenon of urticarial dermographism (UD) are not yet sufficiently elucidated in dermatological patients. A fiber optic laser Doppler flowmeter (LDF) was used to monitor skin blood flow (SBF) changes on the back of the patients with UD before and after application of the series of pressure stimuli (9.8×10 4, 14.7×10 4, 19.6×10 4 and 24.5×10 4 Pa). All patients acted as self-controls to assess their disease activity by means of SBF values based on response to pressure stimuli before and after treatment with antihistamines, when compared to baseline SBF. Throughout 30 minutes evaluation inter-subject SBF values at pressure-tested sites were noticeably distinguished as high, moderate and low. By LDF we could differentiate the highest development of vascular dynamics after 5 minutes, coming back to normal within about 30 minutes in one group of patients, and the vascular dynamics reaching its maximum in 15 minutes, but with no fade after 30 minutes, in another group of patients. All treatment regimens in both groups of patients by LDF produced a measurable reduction already during 1-2 days of therapy, accompanied by a reduction in SBF baseline values in patients with severe and moderate symptoms of UD.

  15. A fast ultra high pressure liquid chromatographic method for qualification and quantification of pharmaceutical combination preparations containing paracetamol, acetyl salicylic acid and/or antihistaminics.

    Science.gov (United States)

    Deconinck, E; Sacré, P Y; Baudewyns, S; Courselle, P; De Beer, J

    2011-09-10

    A fully validated UHPLC method for the identification and quantification of pharmaceutical preparations, containing paracetamol and/or acetyl salicylic acid, combined with anti-histaminics (phenylephrine, pheniramine maleate, diphenhydramine, promethazine) and/or other additives as quinine sulphate, caffeine or codeine phosphate, was developed. The proposed method uses a Waters Acquity BEH C18 column (2 mm × 100 mm, 1.7 μm) with a gradient using an ammonium acetate buffer pH 4.0 as aqueous phase and methanol as organic modifier. The obtained method was fully validated based on its measurement uncertainty (accuracy profile) and robustness tests. Calibration lines for all components were linear within the studied ranges. The relative bias and the relative standard deviations for all components were respectively smaller than 1.5% and 2%, the β-expectation tolerance limits did not exceed the acceptance limits of 10% and the relative expanded uncertainties were smaller than 5% for all of the considered components. A UHPLC method was obtained for the identification and quantification of these kind of pharmaceutical preparations, which will significantly reduce analysis times and workload for the laboratories charged with the quality control of these preparations. Copyright © 2011 Elsevier B.V. All rights reserved.

  16. Effect of omalizumab on angioedema in H1 -antihistamine-resistant chronic spontaneous urticaria patients: results from X-ACT, a randomized controlled trial.

    Science.gov (United States)

    Staubach, P; Metz, M; Chapman-Rothe, N; Sieder, C; Bräutigam, M; Canvin, J; Maurer, M

    2016-08-01

    Chronic spontaneous urticaria (CSU) severely impacts quality of life (QoL), especially in patients with wheals and angioedema. Omalizumab is approved as add-on therapy for CSU patients; however, its effect on patients who are double-positive for wheals and angioedema has not been systematically studied. The primary objective was to evaluate the efficacy of omalizumab vs placebo at week 28 using the Chronic Urticaria Quality of Life (CU-Q2oL) questionnaire. Number of angioedema-burdened days, time interval between successive angioedema episodes, disease activity, angioedema-specific and overall QoL impairment were secondary objectives. X-ACT was a phase III, randomized, double-blind study conducted in 24 centres (Germany), which selectively included CSU patients with angioedema and wheals. Patients were randomized (1 : 1) to omalizumab 300 mg or placebo (every 4 weeks up to week 24) (ClinicalTrials.gov number: NCT01723072). Of the 91 patients randomized to omalizumab (n = 44) or placebo (n = 47) at baseline, 68 completed the 28-week treatment phase (omalizumab, 35; placebo, 33). Omalizumab was superior to placebo in improving CU-Q2oL scores at week 28 (P omalizumab (0.3) vs placebo (1.1). The median time to first recurrence of angioedema was 57-63 days with omalizumab and Omalizumab significantly improved angioedema-specific QoL (P omalizumab. Omalizumab was an effective treatment option for patients with moderate-to-severe CSU symptoms and angioedema unresponsive to high doses of antihistamine treatment. © 2016 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  17. D-Optimal mixture design optimization of an HPLC method for simultaneous determination of commonly used antihistaminic parent molecules and their active metabolites in human serum and urine.

    Science.gov (United States)

    Kanthiah, Selvakumar; Kannappan, Valliappan

    2017-08-01

    This study describes a specific, precise, sensitive and accurate method for simultaneous determination of hydroxyzine, loratadine, terfenadine, rupatadine and their main active metabolites cetirizine, desloratadine and fexofenadine, in serum and urine using meclizine as an internal standard. Solid-phase extraction method for sample clean-up and preconcentration of analytes was carried out using Phenomenex Strata-X-C and Strata X polymeric cartridges. Chromatographic analysis was performed on a Phenomenex cyano (150 × 4.6 mm i.d., 5 μm) analytical column. A D-optimal mixture design methodology was used to evaluate the effect of changes in mobile phase compositions on dependent variables and optimization of the response of interest. The mixture design experiments were performed and results were analyzed. The region of ideal mobile phase composition consisting of acetonitrile-methanol-ammonium acetate buffer (40 mm; pH 3.8 adjusted with acetic acid): 18:36:46% v/v/v was identified by a graphical optimization technique using an overlay plot. While using this optimized condition all analytes were baseline resolved in rate and analytes peaks were detected at 222 nm. The proposed bioanalytical method was validated according to US Food and Drug Administration guidelines. The proposed method was sensitive with detection limits of 0.06-0.15 μg/mL in serum and urine samples. Relative standard deviation for inter- and intra-day precision data was found to be <7%. The proposed method may find application in the determination of selected antihistaminic drugs in biological fluids. Copyright © 2017 John Wiley & Sons, Ltd.

  18. Validated spectroscopic methods for determination of anti-histaminic drug azelastine in pure form: Analytical application for quality control of its pharmaceutical preparations

    Science.gov (United States)

    El-Masry, Amal A.; Hammouda, Mohammed E. A.; El-Wasseef, Dalia R.; El-Ashry, Saadia M.

    2018-02-01

    Two simple, sensitive, rapid, validated and cost effective spectroscopic methods were established for quantification of antihistaminic drug azelastine (AZL) in bulk powder as well as in pharmaceutical dosage forms. In the first method (A) the absorbance difference between acidic and basic solutions was measured at 228 nm, whereas in the second investigated method (B) the binary complex formed between AZL and Eosin Y in acetate buffer solution (pH 3) was measured at 550 nm. Different criteria that have critical influence on the intensity of absorption were deeply studied and optimized so as to achieve the highest absorption. The proposed methods obeyed Beer's low in the concentration range of (2.0-20.0 μg·mL- 1) and (0.5-15.0 μg·mL- 1) with % recovery ± S.D. of (99.84 ± 0.87), (100.02 ± 0.78) for methods (A) and (B), respectively. Furthermore, the proposed methods were easily applied for quality control of pharmaceutical preparations without any conflict with its co-formulated additives, and the analytical results were compatible with those obtained by the comparison one with no significant difference as insured by student's t-test and the variance ratio F-test. Validation of the proposed methods was performed according the ICH guidelines in terms of linearity, limit of quantification, limit of detection, accuracy, precision and specificity, where the analytical results were persuasive. The absorption spectrum of AZL (16 μg·mL- 1) in 0.1 M HCl. The absorption spectrum of AZL (16 μg·mL- 1) in 0.1 M NaOH. The difference absorption spectrum of AZL (16 μg·mL- 1) in 0.1 M NaOH vs 0.1 M HCl. The absorption spectrum of eosin binary complex with AZL (10 μg·mL- 1).

  19. Central nervous system effects of the second-generation antihistamines marketed in Japan--review of inter-drug differences using the proportional impairment ratio (PIR-.

    Directory of Open Access Journals (Sweden)

    Tatsuya Isomura

    Full Text Available BACKGROUND: Second-generation antihistamines (AHs have, in general, fewer sedative effects than the first-generation. However, important inter-drug differences remain in the degree of cognitive and/or psychomotor impairment. The extent to which a particular compound causes disruption can be conveniently compared, to all other AHs, using the Proportional Impairment Ratio (PIR. Although the PIR can differentiate the relative impairment caused by individual drugs, there is no indication of the reliability of the ratios obtained. OBJECTIVE: To calculate the PIRs -together with 95% confidence intervals (CIs, as an index of reliability- and compare AHs currently, or soon to be, available in Japan, with respect to their intrinsic capacity to cause impairment. METHODS: Results from studies of cetirizine, desloratadine, ebastine, fexofenadine, levocetirizine, loratadine, mequitazine, and olopatadine were included in the PIR calculations. All data utilised came from crossover studies in healthy volunteers which were randomised and placebo and positive-internal controlled. Existing databases from studies reporting the sedative effects of AHs on objective (speed, accuracy, memory and subjective (feeling psychometrics were augmented, via results from suitable studies published after the previous reviews. The null value for a PIR was one. RESULTS: A total of 45 studies were finally included for this review. Of the AHs assessed, fexofenadine, ebastine, and levocetirizine showed a PIR for objective tests of 0. However, only fexofenadine (PIR = 0.49 had an upper limit of the 95% CI of less than 1. Fexofenadine, levocetirizine, desloratadine, olopatadine, loratadine, and mequitazine all had a PIR for subjective ratings of 0, but the upper limits of the 95% CIs were all in excess of 1, although fexofenadine (PIR = 2.57 was the lowest. CONCLUSIONS: The results show that there are differences between second-generation AHs in the extent of sedation produced

  20. Validated spectroscopic methods for determination of anti-histaminic drug azelastine in pure form: Analytical application for quality control of its pharmaceutical preparations.

    Science.gov (United States)

    El-Masry, Amal A; Hammouda, Mohammed E A; El-Wasseef, Dalia R; El-Ashry, Saadia M

    2018-02-15

    Two simple, sensitive, rapid, validated and cost effective spectroscopic methods were established for quantification of antihistaminic drug azelastine (AZL) in bulk powder as well as in pharmaceutical dosage forms. In the first method (A) the absorbance difference between acidic and basic solutions was measured at 228nm, whereas in the second investigated method (B) the binary complex formed between AZL and Eosin Y in acetate buffer solution (pH3) was measured at 550nm. Different criteria that have critical influence on the intensity of absorption were deeply studied and optimized so as to achieve the highest absorption. The proposed methods obeyed Beer ' s low in the concentration range of (2.0-20.0μg·mL -1 ) and (0.5-15.0μg·mL -1 ) with % recovery±S.D. of (99.84±0.87), (100.02±0.78) for methods (A) and (B), respectively. Furthermore, the proposed methods were easily applied for quality control of pharmaceutical preparations without any conflict with its co-formulated additives, and the analytical results were compatible with those obtained by the comparison one with no significant difference as insured by student's t-test and the variance ratio F-test. Validation of the proposed methods was performed according the ICH guidelines in terms of linearity, limit of quantification, limit of detection, accuracy, precision and specificity, where the analytical results were persuasive. Copyright © 2017 Elsevier B.V. All rights reserved.

  1. Trace analysis of three antihistamines in human urine by on-line single drop liquid-liquid-liquid microextraction coupled to sweeping micellar electrokinetic chromatography and its application to pharmacokinetic study.

    Science.gov (United States)

    Gao, Wenhua; Chen, Yunsheng; Chen, Gaopan; Xi, Jing; Chen, Yaowen; Yang, Jianying; Xu, Ning

    2012-09-01

    A rapid and efficient dual preconcentration method of on-line single drop liquid-liquid-liquid microextraction (SD-LLLME) coupled to sweeping micellar electrokinetic chromatography (MEKC) was developed for trace analysis of three antihistamines (mizolastine, chlorpheniramine and pheniramine) in human urine. Three analytes were firstly extracted from donor phase (4 mL urine sample) adjusted to alkaline condition (0.5 M NaOH). The unionized analytes were subsequently extracted into a drop of n-octanol layered over the urine sample, and then into a microdrop of acceptor phase (100 mM H(3)PO(4)) suspended from a capillary inlet. The enriched acceptor phase was on-line injected into capillary with a height difference and then analyzed directly by sweeping MEKC. Good linear relationships were obtained for all analytes in a range of 6.25 × 10(-6) to 2.5 × 10(-4)g/L with correlation coefficients (r) higher than 0.987. The proposed method achieved limits of detections (LOD) varied from 1.2 × 10(-7) to 9.5 × 10(-7)g/L based on a signal-to-noise of 3 (S/N=3) with 751- to 1372-fold increases in detection sensitivity for analytes, and it was successfully applied to the pharmacokinetic study of three antihistamines in human urine after an oral administration. The results demonstrated that this method was a promising combination for the rapid trace analysis of antihistamines in human urine with the advantages of operation simplicity, high enrichment factor and little solvent consumption. Copyright © 2012 Elsevier B.V. All rights reserved.

  2. Dapsona como alternativa no tratamento de urticária crônica não responsiva a anti-histamínicos Dapsone as an alternative to the treatment of chronic urticaria non-responsive to antihistamines

    Directory of Open Access Journals (Sweden)

    Juliana Soares Pires

    2008-10-01

    Full Text Available FUNDAMENTOS: A urticária crônica é dermatose que interfere negativamente na qualidade de vida de seus portadores. O tratamento clássico com anti-histamínicos muitas vezes é ineficaz. OBJETIVO: Avaliar a eficácia e a segurança do uso da dapsona no tratamento da urticária crônica não responsiva a anti-histamínicos. METÓDOS: Realizou-se estudo retrospectivo mediante a revisão de prontuários de pacientes atendidos em ambulatório especializado em urticária entre novembro de 1996 e março de 2007. RESULTADOS: Foram avaliados 20 pacientes com urticária crônica de difícil controle, que receberam tratamento com dapsona na dose de 100mg/dia. Associados à dapsona, foram mantidos anti-histamínicos em altas doses, que, isoladamente, não controlavam os sintomas. Quatorze pacientes (70% responderam com melhora do quadro, observada tanto na diminuição ou desaparecimento das lesões quanto na redução do prurido; três (15% não obtiveram nenhum sucesso com a medicação; e três (15% tiveram o tratamento suspenso em decorrência de efeitos colaterais. CONCLUSÃO: Neste estudo, conclui-se que a dapsona é opção segura e eficaz para pacientes com urticária crônica grave não responsiva a anti-histamínicos.BACKGROUND: Chronic urticaria is a dermatosis that negatively interferes in quality of life of affected individuals. The classic treatment with antihistamines is many times ineffective. OBJECTIVE: To evaluate the efficacy and safety of using dapsone in the treatment of chronic urticaria non-responsive to antihistamines. METHODS: A retrospective study was carried out by reviewing the medical charts of patients seen at an outpatient’s clinic specialized in urticaria, between November 1996 and March 2007. RESULTS: Twenty patients with difficult to control chronic urticaria and who were treated with 100 mg/day of dapsone were evaluated. High doses of antihistamines were maintained and associated with dapsone. Antihistamines alone did

  3. Antihistamines: Understanding Your OTC Options

    Science.gov (United States)

    ... CorrectlyPain Relievers: Understanding Your OTC OptionsAntacids and Acid Reducers: OTC Relief for Heartburn and Acid RefluxOTC Cough ... Loss and Diet Plans Nutrients and Nutritional Info Sugar and Sugar Substitutes Exercise and Fitness Exercise Basics ...

  4. Effect of antihistamines, disodium cromoglycate (DSCG) or methysergide on post-irradiation cerebral blood flow and mean systemic arterial blood pressure in primates after 25 Gy, whole-body, gamma irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Forcino, C.D. [Armed Forces Radiobiology Research Inst., Bethesda, MD (United States)

    1995-06-01

    Exposure to ionizing radiation causes hypotension, cerebral ischemia and release of histamine (HA) and serotonin (5-HT). To investigate the relationship among these responses, rhesus monkeys (Macaca mulatta) received physiological saline (i.v.), disodium cromoglycate (DSCG), antihistamines (AH, mepyramine and cimetidine), or methysergide (METH), then were given 25 Gy whole-body irradiation. Monkeys receiving DSCG, AH or METH had higher post-irradiation mean arterial blood pressure (MBP) than saline-treated controls. Compared to levels in controls, post-irradiation hippocampal blood flow (rCBF) levels were higher in monkeys receiving DSCG, AH or METH. Treatment with the 5-HT{sub 2} receptor antagonist methysergide was the most effective in maintaining both rCBF and MBP after irradiation. Results support the hypothesis that the irradiation-induced cerebral ischemia and, to some extent, the hypotension is mediated by serotonin through 5-HT{sub 2} receptor sites. (author) 72 refs.

  5. A direct comparison of the efficacy of antihistamines in SAR and PAR: randomised, placebo-controlled studies with levocetirizine and loratadine using an environmental exposure unit - the Vienna Challenge Chamber (VCC).

    Science.gov (United States)

    Stübner, P; Zieglmayer, R; Horak, F

    2004-06-01

    The Vienna Challenge Chamber (VCC) is an established method for the controlled exposure of patients to specific allergens, used to make valid comparisons between antihistamines. The aim of the significantly more than loratadine at all time two placebo-controlled, randomised studies reported here was to compare the efficacy and safety of levocetirizine 5 mg od and loratadine 10 mg od in subjects suffering from seasonal allergic rhinitis (SAR) or perennial allergic rhinitis (PAR). During each study period, SAR and PAR subjects were exposed to grass pollen or house-dust mite allergens, respectively for 6 h on 2 consecutive days in the VCC. Each day, medications were administered 2 h after the start of the challenge; with a washout of at least 5 days between each period. The main criterion for evaluation of efficacy was the major symptom complex (MSC) for SAR and the complex symptom score (CSS) for PAR. The pattern of patients' response was similar in SAR and PAR. Both levocetirizine and loratadine were superior to placebo in alleviating SAR and PAR symptoms at all time intervals evaluated during the two study days. Levocetirizine decreased the mean MSC score intervals in SAR subjects, with the most marked difference observed on day 2 (p = 0.002). In PAR patients, although with borderline significance (p = 0.08), levocetirizine decreased the mean CSS more than loratadine. Levocetirizine appeared to have a faster onset of action than loratadine in SAR (45 min versus 1 h 15 min) and PAR (1 h versus 1 h 30 min). However, these apparent differences were not tested for statistical significance. Both medications were well tolerated and no treatment-related adverse events were reported. This level of antihistamine efficacy was maintained regardless of whether the subjects' rhinitis was seasonal or perennial. This study demonstrated that levocetirizine is superior to loratadine in improving symptoms in SAR and that there is a similar trend in PAR.

  6. Co-administration of chenopodium album allergens and CpG oligodeoxynucleotides effects on peripheral blood mononuclear cells of patients with Allergic Rhinitis treated with intranasal corticosteroids and antihistamines.

    Science.gov (United States)

    Farrokhi, Shokrollah; Mousavi, Tahereh; Arshi, Saba; Varasteh, Abdolreza; Rezaei, Nima; Salekmoghadam, Alireza

    2011-06-01

    Allergic Rhinitis (AR) is one of the most common chronic diseases in the developed countries. This study was performed to investigate the effect of CpG-ODN in alteration of T-helper (Th)1/Th2 balance of patients with AR treated with intranasal corticosteroids (INCs) and antihistamines. Peripheral blood mononuclear cells (PBMCs) of 20 patients with AR were isolated before and after 45 days therapy. Cytokine production (IL-4, IL-10, IL-13, IFN-γ) and specific Ch.a IgE in response to CpG co-administration of natural chenopodium album (CpG/Ch.a) or recombinant Ch.a (CpG/rCh.a) allergen were investigated in supernatants.of cultured PBMCs using ELISA Intracellular IL-10 was also assessed in CD4+ cells using flow cytometry. Significant increase in production of IFN-γ and IL-10 and decrease in production of IL-4 were found in supernatants of cultured PBMCs activated with CPG/ch.a and CPG/rch.a. of both CpG/Ch.a and CpG/rCh.a compared to allergens alone, before and after therapy. After therapy, IFN-γ production with CpG/Ch.a was significantly increased in comparison with before (237 vs. 44 pg/ml, p=0.001). IFN-γ and IL-10 production with CpG/rCh.a was significantly increased after therapy compared to before (407.6 vs. 109 pg/ml, p=0.01 for IFN-γ; 171.7 vs. 52.6 pg/ml, p=0.008 for IL-10), whilst IL-4 was significantly decreased (2.1 vs. 5.8 pg/ml, p=0.02). Intracellular IL-10 expression was also significantly increased in response to either CpG/Ch.a or CpG/rCh.a that showed intracellular assay could be more sensitive than ELISA. Also, treatment with intranasal corticosteroids and antihistamines could enhance this CpG effect, in vitro.

  7. Evaluation of the antihistamine effects of olopatadine and levocetirizine during a 24-h period: a double-blind, randomized, cross-over, placebo-controlled comparison in skin responses induced by histamine iontophoresis.

    Science.gov (United States)

    Takeo, Tomohiro; Kasugai, Chikatoshi; Tanaka, Rui; Ando, Takashi; Ogawa, Akina; Akita, Yoichi; Watanabe, Daisuke

    2013-12-01

    The antihistamine effects of olopatadine and levocetirizine, in standard-dose application described in their information (5 mg twice a day for olopatadine; 5 mg once daily for levocetirizine), were examined from 11.5 to 24 h after application. The test was designed in a double-blind, randomized, cross-over, placebo-controlled study of 12 healthy volunteers on histamine-induced flare and wheal response using an iontophoresis technique. The suppressive effect of olopatadine on the wheals induced by a 0.1-mA histamine iontophoresis lasted for 24 h after dosing. Both drugs inhibited flare induced by histamine iontophoresis almost completely until 24 h after the first administration. Suppression of the 0.2-mA-induced wheal response by levocetirizine, taken once daily, decreased with time, although 0.1-mA-induced flare was almost completely suppressed by the drug. Olopatadine completely suppressed even the wheal response induced by a 0.2-mA histamine iontophoresis. Compared with the placebo, the two drugs significantly suppressed the subjective itching assessed by visual analog scale at all intervals. There were no significant differences in subjective drowsiness and objective cognitive function between drug- and placebo-treated subjects. These results demonstrate that olopatadine seems to be more potent than levocetirizine when administrated in a standard dose. In conclusion, mild to moderate urticaria could be controlled by standard application as described in their information. On the other hand, severe urticaria could be managed by a standard application of olopatadine, but levocetirizine may need an additional dose to control severe urticaria. © 2013 Japanese Dermatological Association.

  8. Workshift and Antihistamine Effects on Task Performance

    National Research Council Canada - National Science Library

    Gilliland, Kirby

    1997-01-01

    Sixteen male subjects, well trained on a battery of cognitive performance assessment tasks, participated in a study to Investigate the effects on human operator performance of work shift (Day Shift vs. Mid shift...

  9. Histamine and Antihistamines / Histamin i antihistamini

    Directory of Open Access Journals (Sweden)

    Stojković Nikola

    2015-03-01

    Full Text Available Poslednjih godina beleži se kontinuirani rast prevalencije alergijskih oboljenja. Alergijski imunski odgovor predstavlja jednu kompleksnu mrežu ćelijskih događaja u kojoj učestvuju mnogobrojne imunske ćelije i medijatori. On predstavlja interakciju urođenog i stečenog imunskog odgovora. Ključnu ulogu u imunološkoj kaskadi zauzima histamin, prirodni sastojak tela, koga u alergijskom inflamatornom odgovoru oslobađaju mastociti i bazofili. Cilj ovog rada bio je naglasiti ulogu histamina u alergijskim imunološkim događajima, njegov efekat na Th1 i Th2 subpopulaciju limfocita i produkciju odgovarajućih citokina, kao i ulogu blokatora histamina u tretmanu ovih stanja. Histamin ostvaruje svoj efekat vezivanjem za četiri tipa svojih receptora koji su široko distribuirani u organizmu. Blokatori histamina blokiraju mnogobrojne efekte histamina vezivanjem za ove receptore. Cetirizin, visoko selektivni antihistaminik druge generacije, ne ostvaruje svoje efekte samo vezivanjem za H1 receptore već dovodi do atenuisanja mnogobrojnih zbivanja tokom inflamacijskog procesa. Dobro poznavanje efekata histaminskih blokatora, među njima i cetirizina, može dovesti do pravog odabira terapije u tretmanu alergijskih oboljenja.

  10. A Comparison of Health Care Resource Utilization and Costs for Patients with Allergic Rhinitis on Single-Product or Free-Combination Therapy of Intranasal Steroids and Intranasal Antihistamines.

    Science.gov (United States)

    Harrow, Brooke; Sedaghat, Ahmad R; Caldwell-Tarr, Amanda; Dufour, Robert

    2016-12-01

    Allergic rhinitis (AR) is a common condition that can be treated with a number of different therapies. Treatments such as intranasal antihistamines (INAs) and intranasal steroids (INSs) are widely used by AR patients. For some allergy sufferers, a combination of therapies, specifically an INA and an INS, is required to address their symptoms. A new treatment, the formulation of azelastine hydrochloride and fluticasone pro-pionate used as a single spray (MP-AzeFlu), has become available for AR patients who need both types of treatment. In this regard, the comparison with the alternative concomitant use of INAs and INSs is of interest. The current study examines the health care resource utilization and costs for each cohort. To examine the resource utilization and costs associated with AR for patients treated with MP-AzeFlu or concurrent therapy with single-ingredient INA and INS sprays (free-combination therapy). A retrospective administrative claims study for commercially insured patients from a large U.S. health plan was performed. Patients with an AR diagnosis and a prescription claim for MP-AzeFlu or free-combination therapy between September 1, 2012, and September 30, 2013, were identified. Patients were aged at least 12 years at index date (first prescription fill for intranasal therapy) and were required to have 12 months pre-index and 6 months post-index of continuous enrollment. Health care resource utilization and costs were assessed for the post-index period. The cohorts were adjusted on baseline demographic and clinical characteristics using inverse propensity treatment weights. Other covariates, prescriber specialty, product switching during the post-index period, and pre-index total costs were included in the regression models measuring outcomes. One clinical characteristic of interest was the presence of asthma as comorbidity. A subset analysis of AR patients with asthma was also performed. All-cause-related pharmacy fills as well as pharmacy, medical

  11. Medications and Older Adults

    Science.gov (United States)

    ... older adults and often require the use of antihistamines. Antihistamines are divided into two classes: first generation antihistamines and second generation antihistamines. First generation antihistamines, while ...

  12. In Vitro Anticholinergic and Antihistaminic Activities of Acorus ...

    African Journals Online (AJOL)

    The present investigation was aimed at determining the effects of hexane, acetone, methanol and aqueous extracts of Acorus calamus leaves (ACHE, ACAE, ACME and ACAQE) on cholinergic and histaminic system using isolated frog rectus abdominis muscle and guinea pig ileum. A dose dependent potentiation of Ach ...

  13. Intranasal corticosteroids compared with oral antihistamines in allergic rhinitis

    DEFF Research Database (Denmark)

    Juel-Berg, Nanna; Darling, Peter; Bolvig, Julie

    2017-01-01

    in the case of a single study or outcome. Pooled estimates of effects, 95% confidence interval (CI), were calculated by using random-effects models. Results: The meta-analysis included five randomized controlled trials with a total of 990 patients. INS were superior to OAs in improving total nasal symptoms...

  14. Therapy of antihistamine-resistant chronic spontaneous urticaria.

    Science.gov (United States)

    Greiwe, Justin; Bernstein, Jonathan A

    2017-04-01

    Chronic urticaria affects up to 1-3% of the general population and contributes to significant direct and indirect medical costs as well as decreased quality of life, which has a significant economic impact on our health care system. Areas covered: Given the prevalence of this condition on a large sector of the population, finding lasting relief for refractory cases is essential and is the focus of this review. Expert commentary: The choice of appropriate therapy in chronic refractory urticaria is not a 'one-size fits all' approach. Treatment should take multiple factors into consideration including the chronicity of hives, presence of physical urticaria, type of cellular infiltrate on skin histopathology, patient age, concomitant comorbid conditions, as well as patient preference and cost.

  15. 21 CFR 341.72 - Labeling of antihistamine drug products.

    Science.gov (United States)

    2010-04-01

    ..., dexbrompheniramine maleate, dexchlorpheniramine maleate, phenindamine tartrate, pheniramine maleate, pyrilamine..., pheniramine maleate, pyrilamine maleate, thonzylamine hydrochloride, or triprolidine hydrochloride identified... under 6 years of age: consult a doctor. (10) For products containing pheniramine maleate identified in...

  16. Hazards of antihistamine dependence in psychiatric patients: a case report.

    Science.gov (United States)

    Rao, Mukund G; Varambally, Shivarama; Venkatasubramanian, Ganesan; Gangadhar, Bangalore N

    2015-01-01

    Excessive use of over-the-counter (OTC) medications has been a growing public health problem. We present the case of a patient with avoidant personality disorder, social phobia, and dull normal intelligence, with dependence to pheniramine maleate. His anxiety symptoms, initially unresponsive to conventional treatment, reduced only after stopping pheniramine during inpatient care. This case emphasizes the need for awareness and regular monitoring of the use of OTC medications in vulnerable patient populations.

  17. Complex Cognitive Performance and Antihistamine Use (Executive Summary)

    Science.gov (United States)

    1990-04-01

    Table for Confusion, Sleepiness, and Performance Scales ..... 30 ii INTRODUCTION Individuals suffering from allergic rhinitis , perennial or seasonal...nonsedative HI-receptor antagonist astemizole in perennial allergic and nonallergic rhinitis . Journal of Allergy and Clinical Immunology, 75, 720-727...Wurtman, J. J. (1986). Managing your mind and mood through food . NY: Harper and Row. 34

  18. Anti-histaminic potentials of Cnidoscolus aconitifolius in the ...

    African Journals Online (AJOL)

    Similarly, the observable significant reduction in the paw size was comparable to the Ibuprofen (100 mg/kg). Different concentrations of EECA (0.025, 0.05, 0.1 and 0.2 mg/kg) were assessed on the histamine release from the mast cells. The rats administered with 0.2mg/kg had the most profound effects on the histamine ...

  19. Sinus Pain: Can Over-the-Counter Medications Help?

    Science.gov (United States)

    ... attributes of the individual drug including side effects. Antihistamine Medications Antihistamines combat allergic problems leading to nasal ... after use. Newer non-sedating antihistamines are available. Antihistamine-Decongestant Combination Products Antihistamines and decongestant products are ...

  20. Neurotransmitter mechanisms of the action of the antihistamine dimebon on the brain

    Energy Technology Data Exchange (ETDEWEB)

    Shadurskaya, S.K.; Khomenko, A.I.; Pereverzev, V.A.; Balakeevskii, A.I.

    1986-11-01

    To discover the possible mechanism of the stimulating effect of dimebon on the CNS, the action of the drug was studied on catecholamine concentrations and turnover and activity of forms of monoamine oxidase (MAO), differing in the substrate metabolized, in brain structures involved in the regulation of the emotional state and in the regulation of motor activity in rats. /sup 3/H-serotonin creatinine-sulfate, /sup 3/H-dopamine hydrochloride, and /sup 14/C- benzylamine hydrochloride were used as substrates. The results show that dimebon can inhibit MAO activity in the basal ganglia and other brain structures both in vitro and in vivo, and can cause changes in DA and NA metabolism and in functional activity of catecholaminergic neuronal structures of the brain.

  1. Effects of antihistamines on innate immune responses to severe bacterial infection in mice

    DEFF Research Database (Denmark)

    Metz, Martin; Doyle, Elizabeth; Bindslev-Jensen, Carsten

    2011-01-01

    Sedating and non-sedating histamine H(1) receptor (H1R) antagonists and H2R blockers are widely used drugs which are generally considered to be safe medications. However, recently, these drugs have been shown to possibly impair the outcome of perforating appendicitis in children....

  2. Antihistamine response: a dynamically refined function at the host-tick interface

    Czech Academy of Sciences Publication Activity Database

    Valdés, James J.

    2014-01-01

    Roč. 7, OCT 31 2014 (2014), s. 491 ISSN 1756-3305 R&D Projects: GA MŠk(CZ) EE2.3.30.0032 Institutional support: RVO:60077344 Keywords : dynamics * histamine * lipocalin * competitive binding * tick saliva * ticks Subject RIV: EC - Immunology Impact factor: 3.430, year: 2014

  3. Antihistaminic and cardiorespiratory effects of diphenhydramine hydrochloride in anesthetized dogs undergoing excision of mast cell tumors.

    Science.gov (United States)

    Sanchez, Andrea; Valverde, Alexander; Sinclair, Melissa; Mosley, Cornelia; Singh, Ameet; Mutsaers, Anthony J; Hanna, Brad; Johnson, Ron; Gu, Yu; Beaudoin-Kimble, Michelle

    2017-10-01

    OBJECTIVE To evaluate the effects of IV diphenhydramine hydrochloride administration on cardiorespiratory variables in anesthetized dogs undergoing mast cell tumor (MCT) excision. DESIGN Randomized, blinded clinical trial. ANIMALS 16 client-owned dogs with MCTs. PROCEDURES In a standardized isoflurane anesthesia session that included mechanical ventilation, dogs received diphenhydramine hydrochloride (1 mg/kg [0.45 mg/lb], IV; n = 8) or an equivalent volume of saline (0.9% NaCl) solution (IV; control treatment; 8) 10 minutes after induction. Cardiorespiratory variables were recorded throughout anesthesia and MCT excision, and blood samples for determination of plasma diphenhydramine and histamine concentrations were collected prior to premedication (baseline), throughout anesthesia, and 2 hours after extubation. RESULTS Cardiorespiratory values in both treatment groups were acceptable for anesthetized dogs. Mean ± SD diastolic arterial blood pressure was significantly lower in the diphenhydramine versus control group during tumor dissection (52 ± 10 mm Hg vs 62 ± 9 mm Hg) and surgical closure (51 ± 10 mm Hg vs 65 ± 9 mm Hg). Mean arterial blood pressure was significantly lower in the diphenhydramine versus control group during surgical closure (65 ± 12 mm Hg vs 78 ± 11 mm Hg), despite a higher cardiac index value. Plasma histamine concentrations were nonsignificantly higher than baseline during maximal manipulation of the tumor and surgical preparation in the diphenhydramine group and during surgical dissection in the control group. CONCLUSIONS AND CLINICAL RELEVANCE IV administration of diphenhydramine prior to MCT excision had no clear clinical cardiorespiratory benefits over placebo in isoflurane-anesthetized dogs.

  4. Effect of antihistamines on anaphylactoid oedema in rats using a modified plethysmometer for measuring foot volume.

    Science.gov (United States)

    Elegbe, R A; Oyebola, D D

    1979-01-01

    This study reports the quantitative effect of the H1--and H2--receptor antagonists on dextran-induced anaphylactoid oedema in rats. The findings indicate that mepyramine, promethazine and chlorpromazine which are H1--receptor antagonists significantly inhibited this anaphylactoid oedema. While on the other hand burimamide an H2--receptor antagonist at doses below 500 micrograms/kg inhibit dextran-induced oedema but at higher doses enhances oedema formation in the test rats. E.D50 values obtained for mepyramine, chlorpromazine and promethazine are 5.01 mg/kg, 0.36 mg/kg, 1.78 mg/kg respectively. The dual effects of burimamide on dextran-induced oedema merits further investigation and confirmation with the aid of other H1--and/or H2--receptor systems. A modification of the plethysmometric method of Buttle et. al. (1957) is also described.

  5. Topical antihistamines display potent anti-inflammatory activity linked in part to enhanced permeability barrier function

    DEFF Research Database (Denmark)

    Lin, Tzu-Kai; Man, Mao-Qiang; Santiago, Juan-Luis

    2013-01-01

    antagonists likely oppose mast cell-derived histamines. In four immunologically diverse, murine disease models, characterized by either inflammation alone (acute irritant contact dermatitis, acute allergic contact dermatitis) or by prominent barrier abnormalities (subacute allergic contact dermatitis, atopic...... of epidermal differentiation, leading to thickened cornified envelopes; and (ii) enhanced epidermal lipid synthesis and secretion. As barrier homeostasis was enhanced to a comparable extent in mast cell-deficient mice, with no further improvement following application of topical H1/2r antagonists, H1/2r...... dermatitis), topical H1/2r agonists aggravated, whereas H1/2r antagonists improved, inflammation and/or barrier function. The apparent ability of topical H1r/2r antagonists to target epidermal H1/2r could translate into increased efficacy in the treatment of inflammatory dermatoses, likely due to decreased...

  6. Effects of anti-histaminic and anti-cholinergic substances on human thermoregulation during cold provocation.

    Science.gov (United States)

    Tribukait, A; Nobel, G; Mekjavic, I B; Eiken, O

    2010-01-15

    The roles of histaminergic and cholinergic neuron systems in the regulation of body temperature have been studied almost exclusively in animals. Recently, we have found that motion sickness, i.e. a condition where hippocampal cholinergic mismatch signals induce a release of histamine in the vomiting centre, accelerates the decline in body temperature in men during exposure to cold. In the present study we measured the thermoregulatory effects of two substances commonly used against motion sickness, i.e. the histamine (H1) receptor blocker dimenhydrinate (DMH) and the muscarine receptor blocker scopolamine (SCOP). In three trials, control (CN), DMH and SCOP, 10 male subjects were immersed in 15 degrees C water for a maximum of 90 min. The trials were separated by a minimum of three days and their order was alternated between subjects. In all trials the subject received, in a double blind fashion, a transdermal patch (SCOP or placebo) 12-14 h before immersion and a tablet (DMH or placebo) 1h before immersion. Mean skin temperature, rectal temperature (T(rec)), the difference in temperature between the non-immersed right forearm and 3rd finger of the right hand (T(ff)), and oxygen uptake (VO(2)) were recorded. The fall in T(rec) was smaller in the DMH than in the CN and SCOP conditions. The recordings of T(ff) and VO(2) suggest that SCOP attenuates peripheral vasoconstriction while DMH increases shivering thermogenesis. Notably, thermal discomfort was reduced in the SCOP condition. Findings are thoroughly discussed in the context of animal studies on the neuropharmacology and neurophysiology of thermoregulation and motion sickness.

  7. Reversible dementia due to Neurocysticercosis: improvement of the racemose type with antihistamines

    Directory of Open Access Journals (Sweden)

    Gislaine Cristina Lopes Machado-Porto

    Full Text Available Infection of the human central nervous system (CNS by the larvae of Taenia solium, termed neurocysticercosis (NCC, is endemic in most developing countries, where it is a major cause of acquired seizures and other neurological morbidity, including neuropsychiatric symptoms. However, despite its frequent manifestation, some findings, such as cognitive impairment and dementia, remain poorly understood. Less commonly, NCC may affect the ventricular system and subarachnoid spaces and this form is known as extraparenchymal neurocysticercosis. A particular presentation of the subarachnoid form is called racemose cysticercosis, which has a progressive pattern, frequently leads to hydrocephalus and can be life-threatening. Here we review a case of the racemose variety of cysticercosis, complicated by hydrocephalus and reversible dementia, with remission of symptoms after derivation and that remained stable with use of dexchlorpheniramine. We discuss the challenges in diagnosis, imaging findings, treatment and follow-up of this disease.

  8. Tannate complexes of antihistaminic drug: sustained release and taste masking approaches.

    Science.gov (United States)

    Rahman, Ziyaur; Zidan, Ahmed S; Berendt, Robert T; Khan, Mansoor A

    2012-01-17

    The aim of this investigation was to evaluate the complexation potential of brompheniramine maleate (BPM) and tannic acid (TA) for sustained release and taste masking effects. The complexes (1:1-1:7 TA to BPM ratio) were prepared by the solvent evaporation method using methanol, phosphate buffer pH 6.8 or 0.1N HCl as common solvents. The complexes were characterized microscopically by scanning electron microscopy (SEM), chemically by Fourier transform infrared (FTIR) and solid-state NMR (SSNMR), thermally by differential scanning calorimetry (DSC), for crystallinity by powder X-ray powder diffraction (PXRD), for organoleptic evaluation by electronic tongue (e-tongue), and for solubility in 0.1N HCl and phosphate buffer pH 6.8. The dissolution studies were carried out using the USP II method at 50 rpm in 500 ml of dissolution media (0.1N HCl or phosphate buffer pH 6.8). SEM images revealed that the morphology of complexes were completely different from the individual components, and all complexes had the same morphological characteristics, irrespective of the solvent used for their preparation, pH or ratio of BPM and TA. The FTIR spectra showed the presence of chemical interactions between the TA and BPM. DSC, PXRD and SSNMR indicated that the drug lost its crystalline nature by formation of the complex. Complexation has significantly reduced the solubility of BPM and sustained the drug release up to 24h in phosphate buffer pH 6.8 media. The bitter taste of the BPM was completely masked which was indicated by Euclidean distance values which was far from the drug but near to its placebo in the complexes in all ratios studied. The taste masked complexes can be potentially developed as suitable dosage forms for pediatric use. In summary, complexation of BPM and TA effectively sustained the dissolution and masked the bitter taste of drug for the development of suitable dosage forms for pediatric use. Published by Elsevier B.V.

  9. Delayed phase of hematoporphyrin-induced phototoxicity: modulation by complement, leukocytes, and antihistamines

    Energy Technology Data Exchange (ETDEWEB)

    Lim, H.W.; Young, L.; Hagan, M.; Gigli, I.

    1985-02-01

    The role of complement, leukocytes, and histamine was investigated in the delayed phase of hematoporphyrin-induced phototoxicity in guinea pigs. The phototoxic response was quantified by the accumulation of intravenously injected (/sup 125/I)bovine serum albumin in the skin. There was a greater than 6-fold increase in the vascular response at the completion of irradiation, which subsided partially to reach a plateau of twice the preirradiation level between 0.5 h and 12 h. At 18 h, the vascular responsiveness returned to the baseline value. The 7 h timepoint was selected in this study to evaluate the modulation of the delayed phase. In complement-depleted guinea pigs, as well as in leukopenic animals, the enhancement in the vascular response was significantly suppressed (p vs control, less than 0.0001 and 0.0022, respectively). Cimetidine, when administered prior to irradiation, significantly suppressed the phototoxic response (p vs control, 0.0365). The combination of diphenhydramine and cimetidine, administered 6 h after the induction of phototoxicity, also suppressed the vascular response (p vs control, less than 0.0001). These data indicate that the expression of the delayed phase of hematoporphyrin-induced phototoxicity, similar to the early phase, requires the presence of an intact complement system, leukocytes, and histamine.

  10. Effects of histamine and antihistamines on the kinetics of carbon dioxide in the rat

    Energy Technology Data Exchange (ETDEWEB)

    Russell, J.C.; Chambers, M.M.

    1981-01-01

    We have investigated the effects of chlorpheniramine (an H1 histamine inhibitor) and metiamide (an H2 inhibitor) on response to 14C pulse-labeling of carbon dioxide in the rat in the presence and absence of histamine. Neither chlorpheniramine nor metiamide alone had any effect upon the gastric venous/arterial ratio (VG/A) or the peripheral venous/arterial ratio (Vp/A). As in the case with no drug present, Vp/A rose with time following pulse-labeling to a value of 1.15-1.20. The presence of a preexisting steady-state infusion of histamine caused no changes in the ratios in the presence or absence of the inhibitors. The inhibitors did completely abolish the oscillations of both VG/A and Vp/A caused by initiation of histamine infusion coincident with the pulse-labeling. The results suggest that the histamine effects are largely mediated through H1 receptors.

  11. Inverse agonistic activity of antihistamines and suppression of histamine H1 receptor gene expression.

    Science.gov (United States)

    Mizuguchi, Hiroyuki; Ono, Shohei; Hattori, Masashi; Fukui, Hiroyuki

    2012-01-01

    Histamine H(1) receptor (H1R) expression influences the severity of allergy symptoms. We examined the effect of inverse agonists on H1R gene expression. Two inverse agonists (carebastine and mepyramine), but not the neutral antagonist oxatomide, decreased inositol phosphate accumulation. The inverse agonists also decreased H1R gene expression and down-regulated H1R mRNA below basal expression, while basal H1R mRNA expression was maintained after oxatomide treatment. These results suggest that inverse agonists more potently alleviate allergy symptoms by not only inhibiting stimulus-induced up-regulation of H1R gene expression but also by suppressing basal histamine signaling through their inverse agonistic activity.

  12. Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus.

    Science.gov (United States)

    Dunford, Paul J; Williams, Kacy N; Desai, Pragnya J; Karlsson, Lars; McQueen, Daniel; Thurmond, Robin L

    2007-01-01

    Histamine is a potent mediator of itch in humans, yet histamine H(1) receptor antagonists have been shown to be of limited use in the treatment of certain chronic pruritic diseases. The histamine H(4) receptor is a recently described histamine receptor, expressed on hematopoietic cells, linked to the pathology of allergy and asthma. The contribution of the novel histamine H(4) receptor to histaminergic and allergic pruritus was investigated. Histamine and a selective histamine H(4) receptor agonist caused scratching responses in mice, which were almost completely attenuated in histamine H(4) receptor knockout mice or by pretreatment with the selective histamine H(4) receptor antagonist, JNJ 7777120. Pruritus induced by allergic mechanisms was also potently inhibited with histamine H(4) receptor antagonist treatment or in histamine H(4) receptor knockout mice. In all cases, the inhibitory effect of histamine H(4) receptor antagonist was greater than those observed with histamine H(1) receptor antagonists. The histamine H(4) receptor-mediated pruritus was shown to be independent of mast cells or other hematopoietic cells and may result from actions on peripheral neurons. These results demonstrate that the histamine H(4) receptor is involved in pruritic responses in mice to a greater extent than the histamine H(1) receptor. Histamine H(4) receptor antagonists may have therapeutic utility for treating chronic pruritic diseases in humans where histamine H(1) receptor antagonists are not effective.

  13. Antihistamines block radiation-induced increased intestinal blood flow in canines

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Doyle, T.F.; Donlon, M.A.; Gossett-Hagerman, C.J.

    1985-06-01

    Radiation-induced systemic hypotension is accompanied by increased intestinal blood flow (IBF) and an increased hematocrit (HCT) in dogs. Histamine infusion leads to increased IBF and intestinal edema with consequent secretion of fluid into the intestinal lumen. This study was performed to determine whether these effects could be diminished by prior administration of H1 and H2 histamine blockers. Dogs were given an iv infusion of mepyramine (0.5 mg/min) and cimetidine (0.25 mg/min) for 1 hr before and for 1 hr after radiation (H1 and H2 blockers, respectively). Mean systemic arterial blood pressure (MBP), IBF, and HCT were monitored for 2 hr. Systemic plasma histamine levels were determined simultaneously. Data obtained indicated that the H1 and H2 blockers, given simultaneously, were successful in blocking the increased IBF and the increased HCT seen after 100 Gy, whole-body, gamma radiation. However, the postradiation hypotension was only somewhat affected, with the MBP falling to a level 28% below the preradiation level. Plasma histamine levels reached a sharp peak, as much as 20% above baseline, at 4 min postradiation. These findings implicate histamine in the radiation-induced increase in IBF and HCT but not for the gradual decrease in postradiation blood pressure.

  14. Antihistamines block radiation-induced increased intestinal blood flow in canines

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Doyle, T.F.; Donlon, M.A.; Gossett-Hagerman, C.J.

    1985-01-01

    Radiation-induced systemic hypotension is accompanied by increased intestinal blood flow (IBF) and an increased hematocrit (HCT) in dogs. Histamine infusion leads to increased IBF and intestinal edema with consequent secretion of fluid into the intestinal lumen. This study was performed to determine whether these effects could be diminished by prior administration of H/sub 1/ and H/sub 2/ histamine blockers. Dogs were given an iv infusion of mepyramine (0.5 mg/min) and cimetidine (0.25 mg/min) for 1 hr before and for 1 hr after radiation (H sub 1 and H sub 2 blockers, respectively). Mean systemic arterial blood pressure (MBP), IBF, and HCT were monitored for 2 hr. Systematic plasma histamine levels were determined simultaneously. Data obtained indicated that the H sub 1 and H sub 2 blockers, given simultaneously, were successful in blocking the increased IBF and the increased HCT seen after 100 Gy, whole-body, gamma radiation. However, the postradiation hypotension was only somewhat affected, with the MBP falling to a level 28% below the preradiation level. Plasma histamine levels reached a sharp peak, as much as 20% above baseline, at 4 min postradiation. These findings implicate histamine in the radiation-induced increase in IBF and HCT but not for the gradual decrease in postradiation blood pressure. (Author)

  15. Thermodynamics of the interaction between antihistamines with native and hydroxypropyl-cyclodextrin derivatives in aqueous solutions

    International Nuclear Information System (INIS)

    Alvarez-Lopez, Enrique; Perez-Casas, Silvia

    2013-01-01

    Highlights: • The complexes formation between cyclodextrins and pheniramines were studied by ITC. • In all the cases, the process is enthalpy driven. • The interactions between cyclodextrins and pheniramines are discussed. -- Abstract: The interactions of native and hydroxypropyl-cyclodextrin derivatives with pheniramine, (±)-brompheniramine, (+)-brompheniramine, (±)-chlorpheniramine, (+)-chlorpheniramine, carbinoxamine maleate salts and doxylamine succinate salt have been studied by isothermal titration calorimetry at T = 298.15 K in aqueous solution. The enthalpies and association constants for the complex formation were obtained, from which the Gibbs energy and entropy changes were derived. The thermodynamic parameters corresponding to the transfer process of the guest from the native to the modified CD are also calculated. The results show that the hydrophobic interactions are important in this process, but the size of the guest and the nature of the substituent are also of some importance

  16. [Roles of histamine in the pathogenesis of bronchial asthma and reevaluation of the clinical usefulness of antihistamines].

    Science.gov (United States)

    Yamauchi, Kohei; Shikanai, Toshiki; Nakamura, Yutaka; Kobayashi, Hitoshi; Ogasawara, Masahito; Maeyama, Kazutaka

    2011-02-01

    Histamine has been reported to play an important role in pathogenesis of bronchial asthma. However, H1-blockers are not recommended as the first drug for asthma therapy in the guidelines. Histamine may play various roles in allergic airway inflammation through the H1 receptor (H1R), H2R, and H4R in immune cells including T lymphocytes and dendritic cells. We therefore evaluated its role in allergic airway inflammation with the use of histamine-deficient mice. The results suggested that histamine plays a role in the prevention of goblet cell hyperplasia. Organic cation transporter-3 (OCT-3) is thought to be a transporter of histamine. Polymorphism of OCT-3 {R120R (T/C)} was associated with the severity of asthma. Recently, it has been proposed that both asthma and allergic rhinitis should be treated as a single airway disease. Comorbidity of asthma and allergic rhinitis is very high (70-80%) and they share similar allergic inflammation. H1-blockers are recommended as first-line drugs to treat allergic rhinitis in the guidelines. Therefore H1-blockers are strongly recommended for patients with both asthma and allergic rhinitis.

  17. The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

    NARCIS (Netherlands)

    Bosma, Reggie; Witt, Gesa; Vaas, Lea A I; Josimovic, Ivana; Gribbon, Philip; Vischer, Henry F; Gul, Sheraz; Leurs, Rob

    2017-01-01

    The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (Kd or Ki value) or target modulation (IC50). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and

  18. Treating intermittent allergic rhinitis: a prospective, randomized, placebo and antihistamine-controlled study of Butterbur extract Ze 339.

    Science.gov (United States)

    Schapowal, Andreas

    2005-06-01

    Intermittent allergic rhinitis (IAR) causes patients distress and impairs their work performance and quality of life. A variety of medicines are used by sufferers whose anguish frequently leads to trying new treatments, increasingly from herbal sources. Prospective, randomized, double-blind, parallel group comparison study of Butterbur extract (Ze 339; 8 mg total petasine; one tablet thrice-daily), fexofenadine (Telfast 180, one tablet once-daily) and placebo in 330 patients. Protocol and analysis were according to the latest guidelines on new treatments for allergic rhinitis. The primary efficacy variable was a change in symptoms from baseline to endpoint during daytime. The secondary efficacy variables were: (a) as per primary variable (evening/night); (b) Physician's global assessment; (c) Responder rates. Safety was closely monitored. Both active treatments were individually significantly superior to placebo (p<0.001) in improving symptoms of IAR, while there were no differences between the two active treatments (p=0.37). Superiority to placebo was similarly shown during the evening/night (p<0.001), by physicians' own assessment and by responder rates. Both treatments were well tolerated. Butterbur Ze 339 and Fexofenadine are comparably efficacious relative to placebo. Despite being a herbal drug, Butterbur Ze 339 has now been subject to a series of well controlled trials and should be considered as an alternative treatment for IAR. Copyright (c) 2005 John Wiley & Sons, Ltd.

  19. The ARIA/EAACI criteria for antihistamines: an assessment of the efficacy, safety and pharmacology of desloratadine

    NARCIS (Netherlands)

    Bousquet, J.; Bindslev-Jensen, C.; Canonica, G. W.; Fokkens, W.; Kim, H.; Kowalski, M.; Magnan, A.; Mullol, J.; van Cauwenberge, P.

    2004-01-01

    Background: The definition of allergic rhinitis and the classification of its severity and treatment have advanced in recent years following the publication of the Allergic Rhinitis and its Impact of Asthma (ARIA) document. The ARIA and the European Academy of Allergology and Clinical Immunology

  20. A mini review on biological activities of pyridazinone derivatives as antiulcer, antisecretory, antihistamine and particularly against histamine H3R.

    Science.gov (United States)

    Asif, Mohammad

    2015-01-01

    Pyridazinone derivatives and their related analoges were introduced for gastric antiulcer and antisecretory activities. Selected compounds were applied to ulcer models and showed their antiulcer and anti secretary activities. Some pyridazinone compounds are recently reported as H3R antagonists. Some amine analogs of pyridazinones, pyridazinone- phenethylamines and 4,5-fused pyridazinones showed histamine H3R antagonist activity with significant affinity for rat and human H3R. These pyridazinone analogs also showed excellent selectivity and metabolic stability, with adequate pharmacokinetics.

  1. Development of a voltammetric procedure for assay of the antihistamine drug hydroxyzine at a glassy carbon electrode: Quantification and pharmacokinetic studies.

    Science.gov (United States)

    Beltagi, A M; Abdallah, O M; Ghoneim, M M

    2008-01-15

    An electrochemical study of hydroxyzine at a glassy carbon electrode was carried out in the Britton-Robinson universal buffer of pH 2-11. Hydroxyzine was oxidized in a single two-electron irreversible process controlled mainly by adsorption. A simple, sensitive and time-saving square-wave adsorptive anodic stripping voltammetric procedure has been developed for determination of hydroxyzine in its commercial tablets and human serum without prior extraction. The optimized procedural conditions were: frequency=120Hz, scan increment=10mV, pulse-amplitude=25mV, accumulation potential=-0.3V, accumulation time=90-300s and a Britton-Robinson universal buffer of pH 4 as a supporting electrolyte. Mean recoveries of 100.5+/-0.71 and 98.6+/-1.12% (n=5) were achieved for assay of hydroxyzine in Atarax 10 and 25mg dosage forms, respectively. Limit of detection of 1.5x10(-8)molL(-1) (5.624ngmL(-1)) and limit of quantitation of 5.0x10(-8)molL(-1) (18.746ngmL(-1)) were achieved in human serum with a mean recovery of 98.4+/-1.22%, without prior extraction of the drug. Moreover, the described procedure was applied for evaluating the pharmacokinetic parameters of hydroxyzine in plasma of two healthy volunteers after administration of a single oral dose (Atarax)-25mg).

  2. Utility of 4-chloro-7-nitrobenzofurazan (NBD-CI) for the Spectrophotometric and spectrofluorometric determination of several antihistamine and antihypertensive drugs.

    Science.gov (United States)

    Abd, El-Hay Soad S; Colyer, Christa L; Hassan, Wafaa S; Shalaby, Abdalla

    2013-01-01

    New, sensitive, and selective spectrophotometric and spectrofluorometric methods have been developed for determination of clemastine hydrogen fumarate (Clem), loratadine (Lor), losartan potassium (Los), and ramipril (Ram) in both pure form and pharmaceutical formulations using 4-chloro-7-nitrobenzofurazan (NBD-CI), which is a highly sensitive chromogenic and fluorogenic reagent. The relation between absorbance at 470, 467, 471, and 469 nm and the concentration was linear over the ranges 5-35, 10-100, 10-90, and 10-120 microg/mL for Clem, Lor, Los, and Ram, respectively. The complexation products were also measured spectrofluorometrically at the emission wavelength 535 nm for Clem, Lor, and Ram and at 538 nm for Los with excitation at 477 and 452 nm for Clem and Lor, respectively, and 460 nm for both Los and Ram. The fluorescence intensity was directly proportional to the drug concentration over the ranges 0.05-0.5, 5-20, 1-6, and 2-15 microg/mL for Clem, Lor, Los, and Ram, respectively. The methods were successfully applied for the determination of the studied drugs in pharmaceutical dosage forms with excellent recovery.

  3. Glassy carbon electrode modified with multi-walled carbon nanotubes sensor for the quantification of antihistamine drug pheniramine in solubilized systems.

    Science.gov (United States)

    Jain, Rajeev; Sharma, Sanjay

    2012-02-01

    A sensitive electroanalytical method for quantification of pheniramine in pharmaceutical formulation has been investigated on the basis of the enhanced electrochemical response at glassy carbon electrode modified with multi-walled carbon nanotubes in the presence of sodium lauryl sulfate. The experimental results suggest that the pheniramine in anionic surfactant solution exhibits electrocatalytic effect resulting in a marked enhancement of the peak current response. Peak current response is linearly dependent on the concentration of pheniramine in the range 200-1500 μg/mL with correlation coefficient 0.9987. The limit of detection is 58.31 μg/mL. The modified electrode shows good sensitivity and repeatability.

  4. Glassy carbon electrode modified with multi-walled carbon nanotubes sensor for the quantification of antihistamine drug pheniramine in solubilized systems

    Directory of Open Access Journals (Sweden)

    Rajeev Jain

    2012-02-01

    Full Text Available A sensitive electroanalytical method for quantification of pheniramine in pharmaceutical formulation has been investigated on the basis of the enhanced electrochemical response at glassy carbon electrode modified with multi-walled carbon nanotubes in the presence of sodium lauryl sulfate. The experimental results suggest that the pheniramine in anionic surfactant solution exhibits electrocatalytic effect resulting in a marked enhancement of the peak current response. Peak current response is linearly dependent on the concentration of pheniramine in the range 200–1500 μg/mL with correlation coefficient 0.9987. The limit of detection is 58.31 μg/mL. The modified electrode shows good sensitivity and repeatability. Keywords: Pheniramine, Sodium lauryl sulfate (SLS, Glassy carbon electrode modified with multi-walled carbon nanotubes (GCE-MWCNTs, Solubilized systems, Voltammetric quantification

  5. USING OF FIRST GENERATION OF Hl ANTIHISTAMINES As ALTERNATIVE OF LOCAL ANESTHETIC IN ODONTOLOGIC USE IN ANESTHESIA INFILTRATIVE TECHNICS. EXPERIMENTAL STUDY IN ANIMALS

    OpenAIRE

    Rodríguez Alfaro, Miguel; Burga Sánchez, Jonny; Chumpitaz Cerrate, Victor; Varas Hilario, Roberto; López Bellido, Roger; Chuquihuaccha Granda, Vilma; Zegarra Cuya, Juan

    2014-01-01

    The presence of adverse drug reactions with local anesthetics takes us to the search of effective alternatives to this drugs. 60 albino rabbits divided into 6 groups were submifted to infiltrative anesthetic technique in the maxilla with lidocaine, mepivacaine, bupivacaine, chlorpheniramine and dimenhidrinate, in front of sodium chloride 0,9%. The pain threshold belzavior was evaluated with electrical stimulation from Ruhnkorff s bobbin behind the drllg application and comparison between grou...

  6. Iniencephaly

    Science.gov (United States)

    ... Pregnant women should avoid taking antiepileptic drugs, diuretics, antihistamines, and sulfa drugs, which have been shown to be associated with ... Pregnant women should avoid taking antiepileptic drugs, diuretics, antihistamines, and sulfa drugs, which have been shown to be associated with ...

  7. Experience of Using Levocetirizine in Pediatric Practice

    Directory of Open Access Journals (Sweden)

    Yu.V. Marushko

    2014-11-01

    Full Text Available The paper represents the latest views on antihistamine drugs use in pediatrics. For today, the most essential issue at acute and chronic allergic diseases in children is the use of new antihistamine drug — levocetirizine.

  8. Finding Relief from Allergy's Grip

    Science.gov (United States)

    ... version of this page please turn Javascript on. Antihistamines. These medications counter the effects of histamine, the ... allergic reactions. While helpful in alleviating symptoms, older antihistamines often can cause adverse side effects, such as ...

  9. Trimethobenzamide

    Science.gov (United States)

    ... Trimethobenzamide is in a class of medications called antihistamines. Trimethobenzamide may work by decreasing activity in the ... sure to mention any of the following: antidepressants; antihistamines; barbiturates such as phenobarbital (Luminal); belladonna alkaloids (Donnatal); ...

  10. Mastocytosis

    Science.gov (United States)

    ... mastocytosis, but treatment can help stop your symptoms. Antihistamines (which are often used to treat allergies) are ... symptoms, such as sneezing, runny nose, and hives.Antihistamines: Understanding Your OTC OptionsRead Article >>Over-the-counter ...

  11. Allergic Rhinitis Quiz

    Science.gov (United States)

    ... the best strategy for managing allergic rhinitis? Avoidance Antihistamines or nasal corticosteroid sprays Immunotherapy (allergy shots) It ... pollen or pet dander isn't always feasible. Antihistamines often help for short-term relief of symptoms. ...

  12. Cyproheptadine

    Science.gov (United States)

    ... Cyproheptadine is in a class of medications called antihistamines. It works by blocking the action of histamine, ... pharmacist if you are allergic to cyproheptadine, other antihistamines, or any other medications.tell your doctor and ...

  13. Hydroxyzine

    Science.gov (United States)

    ... Hydroxyzine is in a class of medications called antihistamines. It works by blocking the action of histamine ... Be sure to mention any of the following: antihistamines; azithromycin (Zithromax, ZMax), certain antidepressants such as citalopram ( ...

  14. Allergic conjunctivitis

    Science.gov (United States)

    ... avoid secondhand smoke. Take over-the-counter oral antihistamines. These medicines can offer more relief, but they ... for treatments such as eye drops that contain antihistamines or eye drops that reduce swelling. Mild eye ...

  15. Atopic dermatitis - children - homecare

    Science.gov (United States)

    ... if scratching at night is a problem. Give antihistamines or other medicines by mouth as prescribed by ... Antihistamines taken by mouth may help if allergies cause your child's itchy skin. These medicines are often ...

  16. Medical Surveillance Monthly Report (MSMR). Volume 22, Number 9, September 2015

    Science.gov (United States)

    2015-09-01

    classification and service among active component service members, 1 January 2014 through 31 December 2014 Antihistamine drugs "= ~ Anti-infective...service members, 1 January 2014 through 31 December 2014 Antihistamine drugs Anti-infective agents Autonomic drugs Blood formation, coagulation...therapeutic classification and age among active component service members, 1 January 2014 through 31 December 2014 Antihistamine drugs Anti

  17. Aspirin-Exacerbated Respiratory Disease: Evaluation and Management

    Science.gov (United States)

    2011-01-01

    maintained and stable on antihistamines , topical steroids, leu- kotriene modifiers and immunotherapy. Sometimes omali- zumab needs to be added to...that patients discontinue their antihistamines , decongestants and short-acting inhaled beta- agonists prior to aspirin challenge. These medications...10 mg daily – Oral corticosteroids if necessary – Stop antihistamines and decongestants 48hr prior to aspirin challenge – Stop short acting

  18. Brain Activation by H1 Antihistamines Challenges Conventional View of Their Mechanism of Action in Motion Sickness: A Behavioral, c-Fos and Physiological Study in Suncus murinus (House Musk Shrew

    Directory of Open Access Journals (Sweden)

    Longlong Tu

    2017-06-01

    Full Text Available Motion sickness occurs under a variety of circumstances and is common in the general population. It is usually associated with changes in gastric motility, and hypothermia, which are argued to be surrogate markers for nausea; there are also reports that respiratory function is affected. As laboratory rodents are incapable of vomiting, Suncus murinus was used to model motion sickness and to investigate changes in gastric myoelectric activity (GMA and temperature homeostasis using radiotelemetry, whilst also simultaneously investigating changes in respiratory function using whole body plethysmography. The anti-emetic potential of the highly selective histamine H1 receptor antagonists, mepyramine (brain penetrant, and cetirizine (non-brain penetrant, along with the muscarinic receptor antagonist, scopolamine, were investigated in the present study. On isolated ileal segments from Suncus murinus, both mepyramine and cetirizine non-competitively antagonized the contractile action of histamine with pKb values of 7.5 and 8.4, respectively; scopolamine competitively antagonized the contractile action of acetylcholine with pA2 of 9.5. In responding animals, motion (1 Hz, 4 cm horizontal displacement, 10 min increased the percentage of the power of bradygastria, and decreased the percentage power of normogastria whilst also causing hypothermia. Animals also exhibited an increase in respiratory rate and a reduction in tidal volume. Mepyramine (50 mg/kg, i.p. and scopolamine (10 mg/kg, i.p., but not cetirizine (10 mg/kg, i.p., significantly antagonized motion-induced emesis but did not reverse the motion-induced disruptions of GMA, or hypothermia, or effects on respiration. Burst analysis of plethysmographic-derived waveforms showed mepyramine also had increased the inter-retch+vomit frequency, and emetic episode duration. Immunohistochemistry demonstrated that motion alone did not induce c-fos expression in the brain. Paradoxically, mepyramine increased c-fos in brain areas regulating emesis control, and caused hypothermia; it also appeared to cause sedation and reduced the dominant frequency of slow waves. In conclusion, motion-induced emesis was associated with a disruption of GMA, respiration, and hypothermia. Mepyramine was a more efficacious anti-emetic than cetirizine, suggesting an important role of centrally-located H1 receptors. The ability of mepyramine to elevate c-fos provides a new perspective on how H1 receptors are involved in mechanisms of emesis control.

  19. Toxicological Findings in 889 Fatally Injured Obese Pilots Involved in Aviation Accidents

    Science.gov (United States)

    2010-05-01

    drugs —such as antihistaminics , decongestants, non-narcotic analgesics, and quinine (table IV) . Including ethanol, some of these substances can...reuptake inhibitors (1) and antihistamines (33) were present . a similar drug usage pattern was notable in epidemiological studies conducted for the period...levels (11) . the drugs found in these 11 obese pilots were a heart medication, a benzodiazepine, antihistamin - ics, and narcotic analgesics . a

  20. 75 FR 51984 - Federal Advisory Committee; Meeting of the Uniform Formulary Beneficiary Advisory Panel

    Science.gov (United States)

    2010-08-24

    ... (Nonsteroidal Anti-Inflammatory, Mast Cell Stabilizers, Steroids, and Antihistamines), Renin-Angiotensin Antihypertensives (RAAS), pertinent utilization management issues, drugs recommended for non-formulary placement due...

  1. 29 CFR Appendix A to Subpart T to... - Examples of Conditions Which May Restrict or Limit Exposure to Hyperbaric Conditions

    Science.gov (United States)

    2010-07-01

    ... or drug use. Conditions requiring continuous medication for control (e.g., antihistamines, steroids, barbiturates, moodaltering drugs, or insulin). Meniere's disease. Hemoglobinopathies. Obstructive or...

  2. Histamine H1 antagonists and clinical characteristics of febrile seizures

    Directory of Open Access Journals (Sweden)

    Zolaly MA

    2012-03-01

    Full Text Available Mohammed A ZolalyDepartment of Pediatrics, College of Medicine, Taibah University, Al-Madinah Al-Munawarah, Kingdom of Saudi ArabiaBackground: The purpose of this study was to determine whether seizure susceptibility due to antihistamines is provoked in patients with febrile seizures.Methods: The current descriptive study was carried out from April 2009 to February 2011 in 250 infants and children who visited the Madinah Maternity and Children's Hospital as a result of febrile convulsions. They were divided into two groups according to administration of antihistamines at the onset of fever.Results: Detailed clinical manifestations were compared between patients with and without administration of antihistamines. The time from fever detection to seizure onset was significantly shorter in the antihistamine group than that in the nonantihistamine group, and the duration of seizures was significantly longer in the antihistamine group than in the nonantihistamine group. No significant difference was found in time from fever detection to seizure onset or seizure duration between patients who received a first-generation antihistamine and those who received a second-generation antihistamine.Conclusion: Due to their central nervous system effects, H1 antagonists should not be administered to patients with febrile seizures and epilepsy. Caution should be exercised regarding the use of histamine H1 antagonists in young infants, because these drugs could potentially disturb the anticonvulsive central histaminergic system.Keywords: antihistamine, nonantihistamine, histamine H1 antagonist, febrile seizures

  3. Untitled

    African Journals Online (AJOL)

    both chloroquine and an antihistaminic agent and would possess the requisite drug release. profiles. This study aims at the development of an encapsulated dosage form containing chloro- quine and chlorpheniramine, a common antihis- tamine, which would allow the release ofa suffi- cient amount of the antihistamine to ...

  4. Lysophosphatidylserine-induced release of intra-cellular amines in mice.

    OpenAIRE

    Bigon, E.; Bruni, A.; Mietto, L.; Toffano, G.

    1980-01-01

    In the presence of mouse plasma, lysophosphatidylserine stimulates histamine secretion from isolated mast cells. The extensive modification of carbohydrate metabolism produced by lysophosphatidylserine in mice was largely prevented by the antihistaminic drug, pyrilamine. However, to prevent completely the change in carbohydrate metabolism induced by lysophosphatidylserine the administration of an antihistamine and an adrenoceptor antagonist was required. It is concluded that the effect of lys...

  5. Omalizumab use during pregnancy for CIU: a tertiary care experience.

    Science.gov (United States)

    Cuervo-Pardo, L; Barcena-Blanch, M; Radojicic, C

    2016-07-01

    The treatment of antihistamine and steroid resistant Chronic Idiopathic Urticaria (CIU) during pregnancy poses a challenge due to teratogenicity of immunosuppressants. Omalizumab is a recently FDA approved therapy for CIU and is classified as pregnancy category B. We present an initial series of subjects treated at a tertiary care center for antihistamine and steroid resistant CIU with omalizumab who became pregnant during therapy.

  6. Desloratadine shows no effect on performance during 6 h at 8,000 ft simulated cabin altitude

    NARCIS (Netherlands)

    Valk, P.J.L.; Roon, D.B. van; Simons, M.; Rikken, G.

    2004-01-01

    Sustained vigilance is required by pilots and crew during flight; therefore, the use of antihistamines with sedating properties is widely prohibited. The purpose of this study was to determine the effects of desloratadine, a long-acting, nonsedating antihistamine, on healthy volunteers placed under

  7. Cognitive performance effects of bilastine 20 mg during 6 hours at 8000 ft cabin altitude

    NARCIS (Netherlands)

    Valk, P.J.L.; Simons, M.; Jetten, A.M.; Valiente, R.; Labeaga, L.

    2016-01-01

    INTRODUCTION: Bilastine is a new oral, second generation antihistamine used in the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. It is considered a nonsedating antihistamine and might be recommended for use in pilots, pending research on the effects on flying-related

  8. Allergic Conjunctivitis

    African Journals Online (AJOL)

    combination of topical vasoconstrictor and antihistamine therapies, topical antihistamines with mast cell stabilising properties, topical mast cell .... exposure, and keep car and home windows closed during the peak pollen .... Tsubota K, Takamura E, Hasegawa T, Kobayashi T. Detection by brush cytology of mast cells and ...

  9. Vijayapandi et al., Afr J Tradit Complement Altern Med. (2013) 10(1 ...

    African Journals Online (AJOL)

    AJTCAM

    Acetylcholine is believed to affect the memory, sleep, and concentration abilities, and also to be involved in some severe diseases such as Alzheimer, Parkinson ... of abundant antihistamines in the market, the search continues for the development of novel antihistaminic agents with reduced sedation, anticholinergic and.

  10. Histamine H1 antagonists and clinical characteristics of febrile seizures.

    Science.gov (United States)

    Zolaly, Mohammed A

    2012-01-01

    The purpose of this study was to determine whether seizure susceptibility due to antihistamines is provoked in patients with febrile seizures. The current descriptive study was carried out from April 2009 to February 2011 in 250 infants and children who visited the Madinah Maternity and Children's Hospital as a result of febrile convulsions. They were divided into two groups according to administration of antihistamines at the onset of fever. Detailed clinical manifestations were compared between patients with and without administration of antihistamines. The time from fever detection to seizure onset was significantly shorter in the antihistamine group than that in the nonantihistamine group, and the duration of seizures was significantly longer in the antihistamine group than in the nonantihistamine group. No significant difference was found in time from fever detection to seizure onset or seizure duration between patients who received a first-generation antihistamine and those who received a second-generation antihistamine. Due to their central nervous system effects, H1 antagonists should not be administered to patients with febrile seizures and epilepsy. Caution should be exercised regarding the use of histamine H1 antagonists in young infants, because these drugs could potentially disturb the anticonvulsive central histaminergic system.

  11. Comparison of the efficacy of olopatadine and fexofenadine in chronic idiopathic urticaria patients: a crossover study.

    Science.gov (United States)

    Tanizaki, Hideaki; Yamamoto, Yosuke; Nakamizo, Satoshi; Otsuka, Atsushi; Miyachi, Yoshiki; Kabashima, Kenji

    2015-01-01

    Olopatadine is one of the second-generation H1 antihistamines that were used for treating allergic disorders initially in Asia, and now also in Western countries. Whereas several trials compared the efficacy on chronic urticaria among second-generation H1 antihistamines, no study has directly compared the clinical efficacy between olopatadine and other H1 antihistamines in patients with chronic idiopathic urticaria (CIU). In this study, we address this issue for the first time and conclude that olopatadine is a good candidate for the treatment of CIU. © 2015 S. Karger AG, Basel.

  12. CME 8876.indd

    African Journals Online (AJOL)

    Sedating antihistamines. Thereafter, maintenance as for chronic disease. Ultraviolet (UV) light. Non-steroidal systemic drugs: azathioprine, cyclosporin, methotrexate, mycophenolate. Refer to dermatologist/paediatrician/allergist as appropriate. Potent TCSs. Phototherapy (narrow-band UVB). Cyclosporin, methotrexate, oral ...

  13. Allergy Meds Could Affect Your Driving

    Science.gov (United States)

    ... itchy skin rashes known as hives. Medications containing antihistamines, drugs which counteract the effect of histamines, can help ... sedatives (sleep medications), or tranquilizers while taking some ... be found in the Drug Facts label, Filie says. Alcohol and sedatives can ...

  14. Drug and poison information - the Tygerberg experience

    African Journals Online (AJOL)

    100. TABLE VI. Pharmacotherapy consultations. Drug categories. Antimicrobial. Cardiovascular. Anti-epileptic. Neuroleptic and anti-histamine. Antidepressant. Benzodiazepines, barbiturates and other sedative hypnotics. Respiratory. Miscellaneous. Total. 1986 - 1988. 1990 - 1991. No. %. No. %. Average (%). 312. 29,1.

  15. Malaria Parasite Infection and Chloroquine-Induced Pruritus: The ...

    African Journals Online (AJOL)

    induced body scratching, whereas, the histaminergic system was implicated in CQ-induced itching. Keywords: Rats, parasitaemia, chloroquine, opioids, antihistamine, naltrexone. West African Journal of Pharmacology and Drug Research Vol.

  16. Dry Mouth Treatment: Tips for Controlling Dry Mouth

    Science.gov (United States)

    ... Dry Mouth Mouthwash, which also offer protection against tooth decay. Avoid using over-the-counter antihistamines and decongestants ... and drinks because they increase your risk of tooth decay. Brush with a fluoride toothpaste — ask your dentist ...

  17. ORIGINAL ARTICLE

    African Journals Online (AJOL)

    User

    1Department of Pharmacology, 2Department of Pharmacognosy, 3Department of Pharmaceutical Chemistry, Faculty of Pharmacy and. Pharmaceutical ... Keywords: Ulcer, traditional medicine, rodent, Musa x paradisiaca, acetic acid. Journal of Medical and ..... antihistaminic and gastric mucosal cell regenerative property.

  18. Drowsiness

    Science.gov (United States)

    ... known cause) may be a sign of a sleep disorder. Depression , anxiety , stress , and boredom can all contribute ... tranquilizers, sleeping pills, antihistamines) Not sleeping long enough Sleep disorders (such as sleep apnea and narcolepsy ) Too much ...

  19. Download this PDF file

    African Journals Online (AJOL)

    the' study. The exclusion criteria included any subject with other degenerative eye conditions, dry eye syndrome, keratoconjunctivitis sicca, blepharoconjunctivitis and trachoma. Subjects who had received topical eye medications or systemic medications such as antihistamines, phenothiazines, diazepam and artane and.

  20. Medication for Behavior Modification in Birds

    NARCIS (Netherlands)

    van Zeeland, Yvonne

    2018-01-01

    The use of behavior modifying drugs may be considered in birds with behavior problems, especially those refractory to behavior modification therapy and environmental management. To accomplish behavior change, a variety of drugs can be used, including psychoactive drugs, hormones, antihistamines,

  1. Hives (Urticaria)

    Science.gov (United States)

    ... Staying Safe Videos for Educators Search English Español Hives (Urticaria) KidsHealth / For Teens / Hives (Urticaria) What's in this ... prescribed an antihistamine to treat it. What Is Urticaria? The medical name for hives is urticaria . It's ...

  2. Scabies (For Parents)

    Science.gov (United States)

    ... allow bacteria to get into the injured skin. Impetigo , a bacterial skin infection, may affect skin that's ... also develops a bacterial skin infection (such as impetigo) and an antihistamine to help relieve the itching. ...

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

    Directory of Open Access Journals (Sweden)

    Yu. G. Levina

    2014-01-01

    Full Text Available The review is dedicated to treatment of allergic diseases in children, particularly to the use of the 2nd generation antihistamine. It demonstrates that mediator histamine has the crucial role in pathophysiology of the allergic reaction. Antihistamines block histamine action aimed at H1 receptors by way of competitive inhibition. The 2nd generation antihistamines are the drugs of choice for the treatment of allergic diseases due to the absence of sedative effect. The review presents clinical and pharmacological description of the selective 2nd generation antihistamine cetirizine, efficacy and safety of which have been appraised in numerous long-term clinical studies in children with allergic rhinitis, urticaria and atopic dermatitis. 

  4. Bug bites and stings: When to see a dermatologist

    Medline Plus

    Full Text Available ... borne diseases, it’s important to take steps to reduce your risk. To help prevent bug bites, dermatologists ... take an over-the-counter oral antihistamine. To reduce swelling , apply an ice pack to the bite. ...

  5. Medline Plus

    Full Text Available ... mast cells to release histamine. Histamine then produces allergy symptoms. A stuffy and runny nose, sneezing and ... antihistamines may be used to help alleviate severe allergy symptoms.

  6. 21 CFR 520.784 - Doxylamine succinate tablets.

    Science.gov (United States)

    2010-04-01

    ...) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.784 Doxylamine... use. (1) The drug is used in conditions in which antihistaminic therapy may be expected to alleviate...

  7. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Science.gov (United States)

    2010-04-01

    ... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS... antihistaminic therapy may be expected to lead to alleviation of some signs of disease. (3) Limitations. Do not...

  8. 21 CFR 522.2063 - Pyrilamine maleate injection.

    Science.gov (United States)

    2010-04-01

    ...) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522... treating horses in conditions in which antihistaminic therapy may be expected to lead to alleviation of...

  9. 21 CFR 522.784 - Doxylamine succinate injection.

    Science.gov (United States)

    2010-04-01

    ... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS...) Conditions of use. (1) The drug is used in conditions in which antihistaminic therapy may be expected to...

  10. Simplifying Effective Treatment of Chronic Hives in Children

    Science.gov (United States)

    ... with the antihistamine hydroxyzine, or cetirizine, the active product of ingested hydroxyzine. Those who did not respond to one of those medications with a complete suppression of their daily hives then received cyclosporine, in closely monitored doses to ...

  11. Bug bites and stings: When to see a dermatologist

    Medline Plus

    Full Text Available ... correct dose. For bites that itch , apply an ice pack or an over-the-counter anti-itch ... counter oral antihistamine. To reduce swelling , apply an ice pack to the bite. If you experience any ...

  12. Iatrogenic nocturnal eneuresis- an overlooked side effect of anti histamines?

    Directory of Open Access Journals (Sweden)

    D Italiano

    2015-01-01

    Full Text Available Nocturnal enuresis is a common disorder in childhood, but its pathophysiological mechanisms have not been fully elucidated. Iatrogenic nocturnal enuresis has been described following treatment with several psychotropic medications. Herein, we describe a 6-year-old child who experienced nocturnal enuresis during treatment with the antihistamine cetirizine. Drug rechallenge was positive. Several neurotransmitters are implicated in the pathogenesis of nocturnal enuresis, including noradrenaline, serotonin and dopamine. Antihistamine treatment may provoke functional imbalance of these pathways resulting in incontinence.

  13. Topische Antihistaminika bei saisonaler allergischer Rhinitis : eine Untersuchung mit Dimetindenmaleat als Nasenspray

    OpenAIRE

    Haaf- von Below, Stephanie

    2003-01-01

    Topical antihistamines in seasonal allergic rhinitis - A trial with dimethindenemaleate (DMM) as a nasal spray. This study investigates the efficacy and safety of dimethindenemaleate (0,1%) vs. placebo nasal spray in the therapy of seasonal allergic Rhinitis. 175 patients were randomised in a multicenter placebo-controlled double blind study (phase III) with parallel groups. This thesis investigates especially DMM nasal spray in comparison with other frequently used topical antihistamines: az...

  14. Designing Novel Smart Hydrogel Formulations for the Controlled Delivery of Ocular Therapies in Contact Lens Devices

    OpenAIRE

    Phelan, David

    2015-01-01

    The major challenge to ocular drug delivery is poor bio-availability of the delivered drug, due to the anatomy of the eye. This work presents an approach to address this problem, using novel contact lens drug delivery vehicles. Antihistamines were used as a model drug due to their physical properties and molecular weight. 15% of the world’s population suffer from allergic reactions confirming antihistamines as a relevant ocular pharmaceutical. A novel pilot scale wet cast moulding proce...

  15. Fexofenadine-Induced Urticaria

    OpenAIRE

    Lee, Sang Woo; Byun, Ji Yeon; Choi, You Won; Myung, Ki Bum; Choi, Hae Young

    2011-01-01

    Fexofenadine (Allegra? 180) is a second-generation antihistamine. It is widely used as anti-allergic drug, which suppresses various allergic reactions mediated by histamines. A few cases of H1-antihistamine-induced urticaria have been reported. Herein, we report a rare case of fexofenadine-induced urticaria which was confirmed by a prick test, oral provocation test, and flow cytometry assisted-basophil activation test.

  16. Chronic idiopathic angioedema: a single center experience.

    Science.gov (United States)

    Eli, Magen; Joseph, Mishal; Kuznik, Boris; Menachem, Schlesinger

    2014-10-01

    Chronic idiopathic angioedema (CIA) is defined as three or more episodes of angioedema in a period of > 6 months without a clear etiology. In the study, we tried to explore clinical and laboratory characteristics of patients with CIA unaccompanied by urticaria. We retrospectively reviewed clinical and laboratory characteristics of 1238 patients with chronic urticaria and/or angioedema referred to our allergy clinic. Eight hundred and forty-one (67.9%) subjects had chronic urticaria without angioedema (CU Group), 323 (26.1%) had both urticaria and angioedema (CU + CA group), and 74 (5.9%) had chronic angioedema without urticaria (CA). In 29 (39.2%) cases of CA, no etiologic factor of angioedema was discovered, thus the patients were defined as having chronic idiopathic angioedema (CIA Group). Twenty-two (75.8%) subjects had antihistamine-responsive CIA and seven (24.1%) had antihistamine-unresponsive CIA. There were no statistically significant differences in clinical (except of urticarial eruptions) and laboratory characteristics between CU, CA + CU, and CIA groups. Antihistamine responsive and antihistamine-unresponsive CIA groups had no distinguishable clinical or laboratory features. We suppose that CIA, at least its antihistamine-responsive form, represents a rare form of chronic spontaneous urticaria. The reasons why in CIA there are no other clinical signs of mast cell/basophil activation, such as pruritus, urticarial, and dermatographism, are largely unknown and have to be elucidated in future studies. © 2014 The International Society of Dermatology.

  17. Effects of levocetirizine and diphenhydramine on regional glucose metabolic changes and hemodynamic responses in the human prefrontal cortex during cognitive tasks.

    Science.gov (United States)

    Kikuchi, Asuka; Nasir, Fairuz Binti Mohammadi; Inami, Akie; Mohsen, Attayeb; Watanuki, Shoichi; Miyake, Masayasu; Takeda, Kazuko; Koike, Daigo; Ito, Takayasu; Sasakawa, Junpei; Matsuda, Rin; Hiraoka, Kotaro; Maurer, Marcus; Yanai, Kazuhiko; Watabe, Hiroshi; Tashiro, Manabu

    2018-03-13

    Antihistamines often have sedative side effects. This was the first study to measure regional cerebral glucose (energy) consumption and hemodynamic responses in young adults during cognitive tests after antihistamine administration. In this double-blind, placebo-controlled, three-way crossover study, 18 healthy young Japanese men received single doses of levocetirizine 5 mg and diphenhydramine 50 mg at intervals of at least six days. Subjective feeling, task performances, and brain activity were evaluated during three cognitive tests (word fluency, two-back, and Stroop). Regional cerebral glucose consumption changes were measured using positron emission tomography with [ 18 F]fluorodeoxyglucose. Regional hemodynamic responses were measured using near-infrared spectroscopy. Energy consumption in prefrontal regions was significantly increased after antihistamine administration, especially diphenhydramine, whereas prefrontal hemodynamic responses, evaluated with oxygenated hemoglobin levels, were significantly lower with diphenhydramine treatment. Stroop test accuracy was significantly impaired by diphenhydramine, but not by levocetirizine. There was no significant difference in subjective sleepiness. Physiological "coupling" between metabolism and perfusion in the healthy human brain may not be maintained under pharmacological influence due to antihistamines. This uncoupling may be caused by a combination of increased energy demands in the prefrontal regions and suppression of vascular permeability in brain capillaries after antihistamine treatment. Further research is needed to validate this hypothesis. Copyright © 2018 John Wiley & Sons, Ltd.

  18. Anafylaksi efter bi- eller hvepsestik i Region Syddanmark i perioden 2008-2011

    DEFF Research Database (Denmark)

    Oropeza, Athamaica Ruiz; Mikkelsen, Søren; Bindslev-Jensen, Carsten

    intramuskulær adrenalin (64 % ifølge Sampson’s skala og 76 % ifølge Muraro’s). Af de 38 patienter der blev set i Odense fik 66 % intravenøs (IV) binyrebarkhormon, 63 % IV antihistamin og 5 % IV adrenalin (blandt dem med moderat til svær anafylaksi fik op til 77 % IV binyrebarkhormon og op til 82 % IV...... antihistamin). Blandt de 55 patienter i resten af Region Syddanmark fik 80 % IV binyrebarkhormon, 78 % IV antihistamin og 7 % IV adrenalin (blandt dem med moderat til svær anafylaksi fik op til 94 % IV binyrebarkhormon og op til 90 %, IV antihistamin). Af dem der fik IV adrenalin havde 2 ud af 2 tidligere fået...... intramuskulær adrenalin i Odense-området og 1 ud af 4 i resten af Region Syddanmark. Konklusion: Over 50 % af de reporterede tilfælde af allergi efter bi- og hvepsestik kunne gradueres som moderat til svær anafylaksi. Lang de fleste fik behandling med IV binyrebarkhormon og antihistamin, men kun omkring 50 % af...

  19. Histamine and tryptase in nasal lavage fluid after allergen challenge

    DEFF Research Database (Denmark)

    Jacobi, H H; Skov, P S; Poulsen, L K

    1999-01-01

    BACKGROUND: Antihistamines (H1-receptor antagonists) act by competitive antagonism of histamine at H1-receptors. In addition, high concentrations of some antihistamines inhibit allergen-induced histamine release from mast cells in vitro. OBJECTIVE: The purpose of this study was to determine...... the effect of intranasal azelastine or systemic cetirizine (both potent antihistamines) on the allergen-induced release of mast-cell mediators from the human nasal mucosa in vivo. METHODS: Patients allergic to birch pollen (n = 11) and control subjects not allergic to birch pollen (n = 5) were included......, nasal allergen challenges were performed, and the number of sneezes were counted. In addition, nasal lavage fluid was collected, and the levels of mast-cell mediators (histamine and tryptase) were measured. RESULTS: The allergen challenge of patients allergic to pollen produced sneezing...

  20. Diagnosis and management of cold urticaria.

    Science.gov (United States)

    Singleton, Reid; Halverstam, Caroline P

    2016-01-01

    Cold urticaria is a physical urticaria characterized by a localized or systemic eruption of papules upon exposure of the skin to cold air, liquids, and/or objects. In some cases, angioedema and anaphylaxis also may occur. The symptoms of cold urticaria can have a negative impact on patients' quality of life. Second-generation H1 antihistamines are the first line of treatment in cold urticaria; however, patients who are unresponsive to initial treatment with H1 antihistamines may require further management options. Avoidance of cold exposure is the most effective prophylactic measure. In mild to moderate cases, the primary goal of therapy is to improve the patient's quality of life. In more severe cases, treatment measures to protect the patient's airway, breathing, and circulation may be necessary. We report the case of a 23-year-old man with cold urticaria who was refractory to initial therapy with H1 antihistamines. A review of the literature also is provided.

  1. Fexofenadine Suppresses Delayed-Type Hypersensitivity in the Murine Model of Palladium Allergy.

    Science.gov (United States)

    Matsubara, Ryota; Kumagai, Kenichi; Shigematsu, Hiroaki; Kitaura, Kazutaka; Nakasone, Yasunari; Suzuki, Satsuki; Hamada, Yoshiki; Suzuki, Ryuji

    2017-06-25

    Palladium is frequently used in dental materials, and sometimes causes metal allergy. It has been suggested that the immune response by palladium-specific T cells may be responsible for the pathogenesis of delayed-type hypersensitivity in study of palladium allergic model mice. In the clinical setting, glucocorticoids and antihistamine drugs are commonly used for treatment of contact dermatitis. However, the precise mechanism of immune suppression in palladium allergy remains unknown. We investigated inhibition of the immune response in palladium allergic mice by administration of prednisolone as a glucocorticoid and fexofenadine hydrochloride as an antihistamine. Compared with glucocorticoids, fexofenadine hydrochloride significantly suppressed the number of T cells by interfering with the development of antigen-presenting cells from the sensitization phase. Our results suggest that antihistamine has a beneficial effect on the treatment of palladium allergy compared to glucocorticoids.

  2. Fexofenadine Suppresses Delayed-Type Hypersensitivity in the Murine Model of Palladium Allergy

    Directory of Open Access Journals (Sweden)

    Ryota Matsubara

    2017-06-01

    Full Text Available Palladium is frequently used in dental materials, and sometimes causes metal allergy. It has been suggested that the immune response by palladium-specific T cells may be responsible for the pathogenesis of delayed-type hypersensitivity in study of palladium allergic model mice. In the clinical setting, glucocorticoids and antihistamine drugs are commonly used for treatment of contact dermatitis. However, the precise mechanism of immune suppression in palladium allergy remains unknown. We investigated inhibition of the immune response in palladium allergic mice by administration of prednisolone as a glucocorticoid and fexofenadine hydrochloride as an antihistamine. Compared with glucocorticoids, fexofenadine hydrochloride significantly suppressed the number of T cells by interfering with the development of antigen-presenting cells from the sensitization phase. Our results suggest that antihistamine has a beneficial effect on the treatment of palladium allergy compared to glucocorticoids.

  3. Critical appraisal of bepotastine in the treatment of ocular itching associated with allergic conjunctivitis

    Directory of Open Access Journals (Sweden)

    Jeremy B Wingard

    2011-02-01

    Full Text Available Jeremy B Wingard, Francis S MahUPMC Eye Center, Department of Ophthalmology, University of Pittsburgh School of Medicine, Pittsburgh, PA, USAAbstract: Bepotastine besilate 1.5% solution is an H1-antihistamine recently approved by the Food and Drug Administration for the topical treatment of ocular itching associated with allergic conjunctivitis. Several clinical studies have demonstrated its safety as well as its efficacy versus placebo. This review finds that bepotastine besilate 1.5% solution is a suitable alternative to other agents within the class of H1-antihistamines, but there are no clinical trial data to suggest that it holds any specific advantages over other agents.Keywords: allergic conjunctivitis, antihistamine, ocular itching

  4. Can human allergy drug fexofenadine, an antagonist of histamine (H1) receptor, be used to treat dog and cat? Homology modeling, docking and molecular dynamic Simulation of three H1 receptors in complex with fexofenadine.

    Science.gov (United States)

    Sader, Safaa; Cai, Jun; Muller, Anna C G; Wu, Chun

    2017-08-01

    Fexofenadine, a potent antagonist to human histamine 1 (H 1 ) receptor, is a non-sedative third generation antihistamine that is widely used to treat various human allergic conditions such as allergic rhinitis, conjunctivitis and atopic dermatitis. Encouragingly, it's been successfully used to treat canine atopic dermatitis, this supports the notion that it might have a great potential for treating other canine allergic conditions and other mammal pets such as dog. Regrettably, while there is a myriad of studies conducted on the interactions of antihistamines with human H 1 receptor, the similar studies on non-human pet H 1 are considerably scarce. The published studies using the first and second generation antihistamines drugs have shown that the antihistamine response is varied and unpredictable. Thus, to probe its efficacy on pet, the homology models of dog and cat H 1 receptors were built based on the crystal structure of human H 1 receptor bound to antagonist doxepin (PDB 3RZE) and fexofenadine was subsequently docked to human, dog and cat H 1 receptors. The docked complexes are then subjected to 1000ns molecular dynamics (MD) simulations with explicit membrane. Our calculated MM/GBSA binding energies indicated that fexofenadine binds comparably to the three receptors; and our MD data also showed the binding poses, structural and dynamic features among three receptors are very similar. Therefore, our data supported the application of fexofenadine to the H 1 related allergic conditions of dog and cat. Nonetheless, subtle systemic differences among human, dog and cat H 1 receptors were also identified. Clearly, there is still a space to develop a more selective, potent and safe antihistamine alternatives such as Fexofenadine for dog or cat based on these differences. Our computation approach might provide a fast and economic way to predict if human antihistamine drugs can also be safely and efficaciously administered to animals. Copyright © 2017 Elsevier Inc

  5. The benefit of H2 receptors antagonist Rupatadine in treatment for urticaria

    Directory of Open Access Journals (Sweden)

    A. A. Kubanov

    2014-01-01

    Full Text Available Second generation antihistamine drugs are mainly used for the therapy of patients suffering from urticaria; however, they are efficient in 45-60% of cases only. New drugs for treatment of urticaria need to be developed and implemented, and second generation antihistamine drug Rupatadine is one of them. At the same time, Rupatadine efficiently inhibits the inflammatory action of the platelet-activating factor. Due to its double action, Rupatadine used perorally in the dose of 10 mg once a day is an efficient drug for treatment of urticaria, and its safety was confirmed by clinical trials.

  6. TNF-Alpha Inhibitors for Chronic Urticaria

    DEFF Research Database (Denmark)

    Sand, Freja Lærke; Thomsen, Simon Francis

    2013-01-01

    be effective and relatively safe treatment options in a significant proportion of patients with chronic urticaria who do not respond sufficiently to high-dose antihistamines or in whom standard immunosuppressive drugs are ineffective or associated with unacceptable side effects.......Patients with severe chronic urticaria may not respond to antihistamines, and other systemic treatment options may either be ineffective or associated with unacceptable side effects. We present data on efficacy and safety of adalimumab and etanercept in 20 adult patients with chronic urticaria...

  7. Air Force Operational Medicine: Using the Estimating Supplies Program to Develop Materiel Solutions for the Operational Clinical Requirements of the Expeditionary Medical Support (EMEDS). Volume 2. EMEDS System [Basic

    Science.gov (United States)

    2009-09-01

    reaction  3  310.90  Alcohol dependence syndrome  2  303.90  Other and unspecified alcohol dependence  1  305.90  Other, mixed, or unspecified  drug ...generation, nonsedating  antihistamine   which enhances the range of  antihistamines  available in the AS. It also satisfies the  Clinical Requirement

  8. Self-reported hair loss in patients with chronic spontaneous urticaria treated with omalizumab: an under-reported, transient side effect?

    Science.gov (United States)

    Konstantinou, G N; Chioti, A G; Daniilidis, M

    2016-09-01

    Omalizumab has been recently approved for treating patients with refractory to H1- antihistamines chronic spontaneous urticaria (CSU). Although hair loss is listed among omalizumab side effects, there are no available data to estimate its frequency. We describe for the first time hair loss as a side effect associated with omalizumab administration in three women, 38, 62 and 70 years old, suffering from refractory to H1-antihistamines CSU. This information was retrieved from their Chronic Urticaria Quality of Life Questionnaires. Despite this side effect, all patients agreed to continue omalizumab regular administration. Hair loss appeared to be transient, lasting up to four months. All cases finally benefited from omalizumab continuation.

  9. Advertisements impact the physiological efficacy of a branded drug

    Science.gov (United States)

    Kamenica, Emir; Naclerio, Robert; Malani, Anup

    2013-01-01

    We conducted randomized clinical trials to examine the impact of direct-to-consumer advertisements on the efficacy of a branded drug. We compared the objectively measured, physiological effect of Claritin (Merck & Co.), a leading antihistamine medication, across subjects randomized to watch a movie spliced with advertisements for Claritin or advertisements for Zyrtec (McNeil), a competitor antihistamine. Among subjects who test negative for common allergies, exposure to Claritin advertisements rather than Zyrtec advertisements increases the efficacy of Claritin. We conclude that branded drugs can interact with exposure to television advertisements. PMID:23878212

  10. [Reactions to insect stings and bites].

    Science.gov (United States)

    Ljubojević, Suzana; Lipozencić, Jasna

    2011-01-01

    Reaction to insect sting and bite may be local, such as erythema, edema and pruritus, or systemic, such as anaphylactic reaction. Diagnosis can be made by patient history, clinical picture, skin testing, total and specific IgE level, and provocation test. Local reactions are treated with cold compresses, topical corticosteroids and oral antihistamines. Oral and intramuscular antihistamines and corticosteroids are used for the treatment of mild systemic reactions, and in severe reaction epinephrine injections are added. Hyposensitization is indicated in patients with severe systemic reaction, positive skin tests and high level of specific IgE antibodies.

  11. Eosinophilic cystitis

    DEFF Research Database (Denmark)

    Mosholt, Karina Sif Søndergaard; Dahl, Claus; Azawi, Nessn Htum

    2014-01-01

    frequency, dysuria, urgency, pain and haematuria. Common clinical findings were presence of bladder mass, peripheral eosinophilia and thickened bladder wall. A variety of medical treatments were used, most frequently steroids, antibiotics and antihistamines. Recurrence occurred in patients on tapering...... or discontinuing prednisone, among other reasons. There is no consensus about the treatment of EC, but In light of our findings in this review, the treatment of choice in our department will be tapered prednisone over 6-8 weeks in combination with antihistamine....

  12. Histamine release positive test associates with disease remission in chronic spontaneous urticaria

    DEFF Research Database (Denmark)

    Berti, A; Yacoub, M R; Skov, Per Stahl

    2017-01-01

    Summary: Background. Histamine release (HR) test has previously been shown to predict the presence of endogenous histamine-releasing factors in chronic spontaneous urticaria (CSU). Objectives and methods. Twenty CSU patients unresponsive to antihistamine treatment were enrolled in order to evaluate...... with a positive HR test had a significant reduction of disease activity (p = 0.003) whereas patients with a negative HR test did not (p > 0.05), leading to disease remission and antihistamine treatment withdrawal in 67% (6/9) of positive HR test patients versus 18% (2/11) of negative HR test patients (p = 0...

  13. Allergisk reaktion i forbindelse med anæstesi kræver grundig postoperativ udredning

    DEFF Research Database (Denmark)

    Blichfeldt, Louise; Garvey, Lene Heise; Krøigaard, Mogens

    2012-01-01

    allergy to fentanyl investigated at the Danish Anaesthesia Allergy Centre. Allergy to this drug could not be demonstrated by skin tests or challenge. The reaction was due to unspecific histamine release induced by several opioids given at the same time. Future pretreatment with antihistamine...

  14. Effects of bepotastine and fexofenadine on histamine-induced flare, wheal and itch.

    Science.gov (United States)

    Tanizaki, Hideaki; Ikoma, Akihiko; Fukuoka, Miyuki; Miyachi, Yoshiki; Kabashima, Kenji

    2012-01-01

    Urticaria is mainly caused by mast cell-derived histamine through the histamine H(1) receptor. Antihistamines are occasionally used on demand upon a recurrence of urticaria; therefore, rapidly acting agents should be explored. The onset of action is assumed to depend on time to maximum concentration (T(max)), but the speed of action needs to be evaluated not only through blood concentration analysis but also by measuring in vivo effectiveness. In this study, we chose two representative second-generation antihistamines (bepotastine and fexofenadine) with relatively short T(max) values and evaluated their effects on histamine-induced skin responses using both visual and laser Doppler imaging scales. Suppression of histamine-induced flare and itch was observed 3 and 6 h after administration of both antihistamines. Attenuation of itch was seen 30 min after the administration of each drug and thereafter until 6 h. In addition, bepotastine suppressed flare formation after only 30 min following application. These results suggest that antihistamines suppress histamine-induced itch and flare, followed by wheal formation, and that bepotastine suppresses skin symptoms sooner after administration than fexofenadine does, which is relatively consistent with the T(max) results. Copyright © 2012 S. Karger AG, Basel.

  15. Acute Renal Failure Due to Massive Envenomation Byafricanized ...

    African Journals Online (AJOL)

    We present a case of a 50 years old gardener who had multiple beestings. He had no significant feature of anaphylaxis and initially appeared to be improving with fluids, steroids and antihistamines until few days into hospital admission, when he developed features of uraemia. A diagnosis of acute renal failure secondary to ...

  16. 21 CFR 341.70 - Labeling of OTC drug products containing ingredients that are used for treating concurrent...

    Science.gov (United States)

    2010-04-01

    ... product contains the established name of the drug, if any, and identifies the product as an “antihistamine... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Labeling of OTC drug products containing ingredients that are used for treating concurrent symptoms (in either a single-ingredient or combination drug...

  17. 21 CFR 341.3 - Definitions.

    Science.gov (United States)

    2010-04-01

    ... or facilitate the removal of secretions from the respiratory airways. (e) Antihistamine drug. A drug... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Definitions. 341.3 Section 341.3 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE...

  18. 55 cases of allergic reactions to hair dye: a descriptive, consumer complaint-based study

    DEFF Research Database (Denmark)

    Søsted, H; Agner, T; Andersen, Klaus Ejner

    2002-01-01

    for angio-oedema. The 55 cases comprised a total of 75 visits to the health service and 5 admissions to hospital. 18 persons had sick leave, which supports the impression of very severe dermatitis reactions. 60% were treated with antihistamine, while 52% were treated with corticosteroids. 29% of the cases...

  19. The Acute Phase Response and Soman-Induced Status Epilepticus: Temporal, Regional and Cellular Changes in Rat Brain Cytokine Concentrations

    Science.gov (United States)

    2010-07-22

    Deleterious effects of IL-9-activated mast cells and neuroprotection by antihistamine drugs in the developing mouse brain. Pediatr Res 2001, 50:222-230. 20...evidence. Epilepsia 2005, 46:1724-1743. 14. Wallenstein MC: Attenuation of penicillin models of epilepsy by nonsteroidal anti-inflammatory drugs . Exp

  20. L-proline-catalysed synthesis of functionalized unsymmetrical ...

    Indian Academy of Sciences (India)

    drugs such as nifedipine, nicardipine and amlodipine which are effective cardiovascular agents in the treat- ment of hypertension.1 In particular, indenopyridines are one of the highly important medicinal scaffolds, which were developed initially as antihistamines,2 are useful inhibitors of spermatogenesis in animals3.

  1. Download this PDF file

    African Journals Online (AJOL)

    Essential Drug List. Some were leaning towards the use of a placebo/demulcent such as Simple Linctus BPC, rather than the ubiquitous diphenhydramine- containing products widely ... settled. Ten years ago, a review in Drugs argued that the ... Antihistamines H1 receptor blockade, usually diphenhydramine combined with ...

  2. Response of the Human Circadian System to Millisecond Flashes of Light

    Science.gov (United States)

    2011-07-01

    sleep, including daily use of antihistamines or antidepressants. Subjects were of intermediate chronotype as determined by the Horne-Östberg...study of sleep and circadian rhythms. Sleep 26: 342–392. 12. Murphy PJ, Myers BL, Badia P (1996) Nonsteroidal anti-inflammatory drugs alter body

  3. Intenderet suicidium med cyclizin

    DEFF Research Database (Denmark)

    Hatting, Nikolaj Preus; Hansen, Peter Martin

    2017-01-01

    Cyclizine is an antihistamine with a sedative effect. In Denmark it is an over-the-counter drug, whereas it is a prescription drug in many other countries. It possesses anticholinergic and antiemetic properties, although the exact mechanism of action is unknown. At doses greater than 5 mg/kg potent...

  4. Intranasal Oxytocin for the Treatment of Pain Associated with Interstitial Cystitis

    Science.gov (United States)

    2014-09-01

    GRA score, which will be collected at 6 and 24 hours post drug or placebo administration. This is a seven-point symmetric scale previously validated...at relieving symptoms. These include bladder distention, bladder instillation with DMSO, oral drugs (Pentosan Polysulfate Sodium (Elmiron), aspirin...ibuprofen, tricyclic antidepressants, antihistamines , narcotic analgesics such as acetaminophen (Tylenol) with codeine or longer- acting narcotics

  5. 14 CFR Appendix A to Part 121 - First Aid Kits and Emergency Medical Kits

    Science.gov (United States)

    2010-01-01

    ... administer required drugs) 4 Needles (sizes necessary to administer required drugs) 6 50% Dextrose injection... dose ampule or equivalent 2 Nitroglycerin tablets 10 Basic instructions for use of the drugs in the kit... administer required medications) 4 Analgesic, non-narcotic, tablets, 325 mg 4 Antihistamine tablets, 25 mg 4...

  6. effect of zidovudine on the liver function of adult albino wistar rats

    African Journals Online (AJOL)

    2014-09-30

    Sep 30, 2014 ... Zidovudine is a type of antiretroviral drug used for the treatment of human immunodeficiency virus (HIV) infection. This study ... demonstrates that the use of antiretroviral drugs could have adverse effects on the liver that could lead to hepatic damage in .... Oxidation of the Antihistamine Drug Terfenadine in.

  7. Platelet Activation after Presyncope by Lower Body Negative Pressure in Humans

    Science.gov (United States)

    2014-12-29

    sleeping habits and to avoid exercise, alcohol, and the use of autonomic stimulants such as prescription (e.g., antihistamines and decongestants) or...nonprescription (e.g., caffeine) drugs for 24 h before the study. LBNP Procedure Each subject was instrumented with a 21-gauge needle in an antecubital

  8. Download this PDF file

    African Journals Online (AJOL)

    drugs and antipsychotics (Table 4). Respiratory system drugs included antihistamines, cough preparations, cortico- steroids, cromoglicate, bronchodilators and mucolytics (Table 5). Seven categories of cardiovascular system drugs were prescribed with B-blockers being the most prescribed and nitrates the least as shown in ...

  9. Motion Sickness Prevention by 8 Hz Stroboscopic Environment during Actual Air Transport

    Science.gov (United States)

    2011-09-01

    antihistamines ( Drug Facts and Comparisons, 1999; Physician’s Desk Reference, 2001). Alternative remedies such as acupuncture, acupressure...Therefore, most drugs that are used to prevent or ameliorate motion sickness symptoms target these neurotransmitters. While the precise action of these...medications in preventing motion sickness is not known, most of these drugs fall into three classes: antidopaminergics, anticholinergics, and

  10. American College of Sports Medicine Roundtable on Exertional Heat Stroke - Return to Duty/Return to Play: Conference Proceedings

    Science.gov (United States)

    2010-01-01

    dysfunctions likely include blood brain barrier breakdown, blood-cerebral spinal fluid barrier break- down, serum protein leakage, and exacerbated drug ...nonsteroidal antiinflammatory drugs (NSAID), to compromise hypothalamic and liver function, exac- erbate tissue injury, and/or impede tissue recovery must be...factors for EHS include age 940 yr, med- ications (anticholinergics, antihistamines , stimulants to include medication for attention deficit

  11. Synthesis of carbon-14 labeled doxylamine succinate

    Energy Technology Data Exchange (ETDEWEB)

    Rao, P.N.; Damodaran, K.M.

    1986-05-01

    Doxylamine succinate, N,N-dimethyl-2-(1-phenyl-1-(2-pyridinyl)-ethoxy)ethanamine succinate is an antihistamine used primarily as a sedative. Carbon-14 labeled doxylamine succinate, required for toxicological studies, was synthesized in two steps starting from 2-benzoyl pyridine.

  12. A Forehead-Mounted Measure of O2 Saturation: The Potential for in Cockpit Hypoxia Early Detection and Warning

    Science.gov (United States)

    2010-07-09

    purported to be capable of sensing, actuating, storing, and communicating an individual’s physiological state. If industry is successful in...past 24 hours. (circle all that apply) a. None b. Sedatives/Tranquilizers c. Aspirin /Tylenol/any analgesic d. Antihistamines

  13. An overview of anti-allergic drug therapy and the histamine-1 ...

    African Journals Online (AJOL)

    cytokines, tumour necrosis factor (TNF)-alpha (TNF-α) and interleukin (IL)-4. ... as a number of inflammatory biomarkers, such as N-alpha- .... first-generation H1 antihistamines, including promethazine, chlorpheniramine, dexchlorpheniramine and cyclizine, and the newer, non-sedating, selective H1-receptor blockers, or.

  14. Snoring and Sleep Apnea

    Science.gov (United States)

    ... Adopt a healthy and athletic lifestyle to develop good muscle tone and lose weight. • Avoid tranquilizers, sleeping pills, and antihistamines before bedtime. • Avoid alcohol for at least four hours and heavy meals or snacks for three hours before retiring. • Establish regular sleeping ...

  15. The Intriguing Role of Histamine in Exercise Responses.

    Science.gov (United States)

    Luttrell, Meredith J; Halliwill, John R

    2017-01-01

    In humans, histamine is a molecular transducer of physical activity responses, and antihistamines modify more than 25% of the genes responding to exercise. Although the upstream signal that results in release of histamine within exercising skeletal muscle remains to be identified, it is likely a fundamental exercise response and not an allergic reaction.

  16. Bug bites and stings: When to see a dermatologist

    Medline Plus

    Full Text Available ... in Medical Dermatology™ Excellence in Dermatopathology™ Excellence in Pediatric Dermatology™ Donate Search Menu Donate Member resources and ... for (var c = 0; c public SPOT Skin ... an over-the-counter oral antihistamine. To reduce swelling , apply an ice pack ...

  17. Hypersensitivity to laminaria: a case report and review of literature.

    Science.gov (United States)

    Sierra, Tania; Figueroa, Melissa M; Chen, Katherine T; Lunde, Britt; Jacobs, Adam

    2015-04-01

    We report a case of laminaria hypersensitivity treated with diphenhydramine and corticosteroids. A literature review identified 10 previously reported cases, with 8 recognized as anaphylaxis, and good outcomes with corticosteroids and antihistamines despite limited epinephrine utilization. Laminaria hypersensitivity is likely IgE mediated with an increased anaphylaxis risk with prior exposure. Copyright © 2015 Elsevier Inc. All rights reserved.

  18. Scorpion sting in the right ear of a young adult: a case report ...

    African Journals Online (AJOL)

    He had made attempts to remove the insect with the cotton bud but all proved abortive. Two drops of 2% plain xylocaine and 5 drops of cerumol were applied on the affected ear. He was managed with analgesics, anxiolytic, antihistamine and ear syringing. The family physician; a frontline doctor and first point of contact for ...

  19. Topical treatment options for allergic conjunctivitis

    African Journals Online (AJOL)

    of topical dual-acting agents which have mast cell stabilising properties and act as antihistamines. Although corticosteroids are among the most effective agents in the treatment of .... diclofenac, has been shown to reduce ocular inflammation in VKC, and to reduce topical steroid use in these patients.9. Although ketorolac ...

  20. Thermal degradation kinetics and solid state, temperature ...

    Indian Academy of Sciences (India)

    WINTEC

    These derivatives are substituted in positions. 2 and 10 and are commonly known as antipsychotic, anti- cholinergic and antihistaminic drugs. Due to their charac- teristic structure they exhibit valuable analytical properties. (Kojlo et al 2001). They have been intensely studied in a number of fields such as chemical, biological ...

  1. In-Vivo Evaluation of the Antiplasmodial Effect of Amodiaquine and ...

    African Journals Online (AJOL)

    Purpose: Antihistamine H1 receptor antagonists like promethazine (PR) are capable of reversing resistance of Plasmodium falciparum to some antimalarials drugs like amodiaquine (AQ). This work was carried out to evaluate the antiplasmodial activity of amodiaquine and amodiaquine-promethazine combination in ...

  2. South African Family Practice - Vol 47, No 7 (2005)

    African Journals Online (AJOL)

    http://dx.doi.org/10.1080/20786204.2005.10873255 · Urticaria and angioedema: a practical approach. BA Muller, J Roy, A Lucille. Effectiveness and safety of newgeneration antihistamines in allergenic rhinitis and urticaria · EMAIL FREE FULL TEXT EMAIL FREE FULL TEXT DOWNLOAD FULL TEXT DOWNLOAD FULL ...

  3. The collapsed football pla yer

    African Journals Online (AJOL)

    (antihistamines, strychnine, cocaine), may also cause SCD. In persons >35 years of age the primary cause of death is coronary artery disease.7. SCD occurs in previously apparently healthy and fit individuals and can also occur in recreational players, including coaches. Physical activity, particularly in short, intense bursts ...

  4. 78 FR 14217 - Control of Alcohol and Drug Use: Addition of Post-Accident Toxicological Testing for Non...

    Science.gov (United States)

    2013-03-05

    ... posted without change to http://www.regulations.gov ; this includes any personal information. Please see... average employee will finish his or her railroad career without ever being required to provide post... potential value of such benefits. The inclusion of tramadol and sedating antihistamines will generate safety...

  5. Allergic Rhinitis | Sommers | South African Family Practice

    African Journals Online (AJOL)

    ... but the antihistamines are less effective for nasal congestion and minimally address the problem of inflammation. Immune-based specifically targeted molecules, such as the cloned humanised monoclonal antibody-inhibiting human IgE omalizumab, are presently being studied in patients with seasonal allergic rhinitis.

  6. Omalizumab in patients with chronic spontaneous urticaria : A systematic review and GRADE assessment

    NARCIS (Netherlands)

    Urgert, M. C.; Van Den Elzen, M. T.; Knulst, A. C.; Fedorowicz, Z.; Van Zuuren, E. J.

    2015-01-01

    Summary Chronic spontaneous urticaria (CSU) is characterized by the occurrence of hives, angio-oedema or both for a period of at least 6 weeks. Many patients remain symptomatic despite treatment with H1 antihistamines, even at higher doses. This systematic review assessed the quality of

  7. Chronic urticaria in the real-life clinical practice setting in Sweden, Norway and Denmark

    DEFF Research Database (Denmark)

    Thomsen, S F; Pritzier, E C; Anderson, C D

    2017-01-01

    (19.6%), allergic rhinitis (16.5%) and food allergies (8.2%). Overall, 60.1% of patients reported using treatments for CU including non-sedative H1-antihistamines (40.5%), corticosteroids (19%), montelukast (14.6%) and omalizumab (8.2%). Pharmacological treatment rates increased to 96.2% during...

  8. A comparison of the effect of diphenhydramine and desloratadine on vigilance and cognitive function during treatment of ragweed-induced allergic rhinitis.

    Science.gov (United States)

    Wilken, Jeffrey A; Kane, Robert L; Ellis, Anne K; Rafeiro, Elizabeth; Briscoe, Maureen P; Sullivan, Cynthia L; Day, James H

    2003-10-01

    Decrements in cognitive performance are associated with the use of sedating antihistamines. Most, but not all, second-generation antihistamines have been found to be nonsedating. To examine the central nervous system (CNS) profile of a new second-generation antihistamine, desloratadine. Subjects with ragweed-induced allergic rhinitis (aged 18-60 years) who demonstrated a predetermined severity of symptoms after priming with ragweed pollen in the Environmental Exposure Unit were randomized to receive a single dose of desloratadine, 5 mg; diphenhydramine, 50 mg; or placebo. A comprehensive battery of repeatable, automated neuropsychological tests was administered to subjects before treatment (symptomatic baseline) and 90 minutes after taking study medication. Both desloratadine (P = .04) and diphenhydramine (P allergic rhinitis compared with placebo, but treatment with diphenhydramine was associated with clinically meaningful decrements on all vigilance parameters (P allergic rhinitis symptoms without adversely affecting performance. Diphenhydramine improved allergic rhinitis symptoms but caused significant decrements in vigilance and cognitive functioning. Thus, efficacy of antihistamine treatment must be balanced against the associated effects on CNS functioning.

  9. Desloratadine and levocetirizine improve nasal symptoms, airflow, and allergic inflammation in patients with perennial allergic rhinitis: a pilot study.

    Science.gov (United States)

    Ciprandi, Giorgio; Cirillo, Ignazio; Vizzaccaro, Andrea; Civardi, Elisa; Barberi, Salvatore; Allen, Michela; Marseglia, Gian Luigi

    2005-12-01

    Nasal obstruction is the main symptom in patients with perennial allergic rhinitis. Some new antihistamines have been demonstrated to be capable of improving this symptom. The aim of this pilot study was to evaluate nasal symptoms, nasal airflow, eosinophils, and IL-4 in patients with perennial allergic rhinitis, before and after treatment with two new antihistamines: desloratadine and levocetirizine. Thirty patients with perennial allergic rhinitis were evaluated, 26 males and 4 females (mean age 26+/-7.1 years). All of them received either desloratadine (5 mg/daily) or levocetirizine (5 mg/daily) or placebo for 4 weeks. The study was double-blind, parallel-group, placebo-controlled, and randomized. Total symptom score (including: rhinorrhea, nasal itching, sneezing, and nasal obstruction) was assessed before and after treatment. Rhinomanometry and decongestion test, nasal lavage, and nasal scraping were performed in all subjects before and after treatment. Eosinophils were counted by conventional staining; IL-4 was measured by immunoassay of fluids recovered from nasal lavage. Desloratadine and levocetirizine treatment induced significant symptom relief and significant reduction of IL-4. Both antihistamines significantly affected all parameters in comparison with placebo. This pilot study demonstrates the effectiveness of antihistaminic treatment in: i) relieving nasal symptoms, including obstruction, ii) improving nasal airflow, iii) exerting decongestant activity, iv) reducing eosinophil infiltration, and v) diminishing IL-4 levels.

  10. Efficacy and safety of azelastine nasal spray for the treatment of allergic rhinitis.

    Science.gov (United States)

    Golden, S J; Craig, T J

    1999-07-01

    Azelastine hydrochloride is a nasally administered antihistamine that is effective and safe for the treatment of perennial and seasonal allergic rhinitis. In addition to acting as a histamine H1-receptor antagonist, azelastine also inhibits the production or release of many chemical mediators of the allergic response such as leukotrienes, free radicals, and cytokines. After nasal administration, azelastine is systemically absorbed with a bioavailability of about 40%. The side effects of azelastine are drowsiness, headache, and bitter taste. Azelastine has a rapid onset of action with a benefit in about 2 hours and a prolonged duration of activity (12 to 24 hours). Studies have shown azelastine to be more effective than placebo in terms of reduction of the major and total symptom complexes of allergic rhinitis. Comparison studies have demonstrated that azelastine is as effective as ebastine, loratadine, cetirizine hydrochloride, and terfenadine at symptom reduction, with varying results when compared with the corticosteroids budesonide and beclomethasone. Although there are conflicting studies, some have demonstrated that azelastine reduces the nasal congestion of allergic rhinitis. This feature that distinguishes it from oral antihistamines is of great interest because corticosteroids are known to be quite effective for the relief of nasal congestion, whereas the antihistamines are effective for the sneezing, itchy eyes, itchy nose, and watery eyes, but not the congestion. Azelastine nasal spray seems to be an efficacious treatment for allergic rhinitis with a rapid onset and long duration of activity, but without the systemic adverse effects of traditional sedating antihistamines.

  11. Nonprescription medications for respiratory symptoms: Facts and marketing fictions.

    Science.gov (United States)

    Weinberger, Miles; Hendeles, Leslie

    2018-05-01

    There are many nonprescription (over-the-counter [OTC]) medications available on pharmacy shelves marketed for relief of respiratory symptoms. The number of such medications has been increasing. This review provides an evidence-based examination of OTC products used for respiratory symptoms. Antihistamines, decongestants, mucolytics, antitussives, and intranasal steroids were selected as the most common OTC medications taken by adults and children for various respiratory symptoms. Controlled clinical trials of efficacy were identified by searching a medical literature data base. Those trials and key publications related to the pharmacokinetics and pharmacodynamics of the products were reviewed. Comparisons of the various OTC antihistamines' ability to suppress the effects of histamine were related to their clinical benefit. Intranasal corticosteroids are the preferred agents for maintenance therapy of persistent nasal congestion and are highly effective for symptoms of inhalant allergy other than allergic conjunctivitis. The disconnect between marketing claims and evidence was demonstrated for antihistamines and oral alpha-1 adrenergic agonist decongestants. Data for OTC mucolytics and antitussives were insufficient to justify their use based on the evidence. There was little relationship between marketing claims and evidence regarding OTC medications used for respiratory symptoms. Analysis of data supported cetirizine, levocetirizine, and fexofenadine as the most effective of the OTC antihistamines. There were no data that supported the use of oral phenylephrine as a decongestant. Neither OTC mucolytics or antitussives provided sufficient evidence to justify their use.

  12. Pankreatisk pannikulitis er nekrose af fedtceller i subcutis ledsaget af intense smerter

    DEFF Research Database (Denmark)

    Jørgensen, Louise Møller; Halkjær, Liselotte Brydensholt; Lauritsen, Anne Øberg

    2012-01-01

    We report an unusual history of pain in a young patient in the intensive care unit. A 33 year-old alcoholic male with acute pancreatitis had generalized intense pain and developed erythema on the lower truncus and the lower extremities. Treatment with different antibiotics, antihistamines...

  13. Topical Promethazine Side Effects: Our Experience and Review of the Literature

    Directory of Open Access Journals (Sweden)

    C. Cantisani

    2013-01-01

    Full Text Available Promethazine hydrochloride is a first-generation H1 receptor antagonist, antihistamine, and antiemetic medication that can also have strong sedative effects. The apparent ability of topical H1r/2r antagonists to target epidermal H1/2r was translated into increased efficacy in the treatment of inflammatory dermatoses, likely due to decreased inflammation and enhanced barrier function.

  14. [Pharmacological prophylaxis of vestibulo-autonomous syndrome (motion sickness) in model investigations].

    Science.gov (United States)

    Shashkov, V S; Iasnetsov, V V; Shashkov, A V; Il'ina, S L; Galle, R R; Sabaev, V V; Potapov, M G

    2000-01-01

    The authors summarize results of multiyear investigations at the Institute of Biomedical Problems of induced motion sickness and development of prophylactic medicaments representing various classes of biologically active substances (choline blocking agents, sympathomimetics, antihistamines etc.) prescribed singularly or in an combination based on the knowledge of MS-provoking inter-receptor interactions and therapeutic effects of drugs.

  15. Psychiatric co-morbidity associated with pheniramine abuse and dependence

    Science.gov (United States)

    Pal, Hemraj; Kumar, Rajesh; Bhushan, Shashi; Berry, Neeraj

    2005-01-01

    The abuse of cough syrups containing antihistamines and codeine is being increasingly noted. The abuse of antihistamines alone has also been reported. The use of antihistamines alone or in combination with other substances of abuse may predispose individuals to develop psychiatric symptoms or syndromes as a part of intoxication, withdrawal or as co-morbid conditions. We present two case reports to highlight the occurrence of co-morbid psychopathology in association with antihistamine abuse and dependence. Case I used high doses of pheniramine for about 2 years and became suspicious of his wife; he even doubted the paternity of his yet-to-be-born child. The associated behavioural abnormalities suggested that he was acting out on the delusion. He also had seizures associated with the intake of a high dose of pheniramine. Case II had multiple substance use, and dependence on alcohol and pheniramine. He demonstrated abnormal behaviour suggestive of psychosis and organic brain syndrome that persisted for a few days and remitted on discontinuation of the substances. These two cases demonstrate the occurrence of psychotic syndromes associated with heavy pheniramine use. The psychopathology can vary from an independent psychotic syndrome to an organic brain syndrome-like disorder.

  16. Knowledge, Attitude and Practice of Commercial Drivers in Dar es ...

    African Journals Online (AJOL)

    Purpose: The objective of this study was, first, to assess the knowledge, attitude and practice of commercial drivers in Dar es Salaam with regard to medicines that impair driving, and second, to evaluate the adequacy of antihistamine label information. Methods: Drivers were interviewed using a questionnaire after obtaining ...

  17. Allergic Rhinitis

    African Journals Online (AJOL)

    Therefore, β2 agonists can resolve asthma attacks but they have no effect on rhinitis. On the contrary, H1 receptor antago- nists treat rhinitis symptoms, but they are quite ineffective on broncho.constriction. However, a synergistic effect has been demonstrated for antihistamines in association with antileukot- rienes.

  18. A facile microwave-assisted synthesis of 8,9-cycloalkathieno[3,2-e ...

    Indian Academy of Sciences (India)

    Asthma and chronic obstructive pulmonary disease. (COPD) are prevalent inflammatory disorders of the lung and are poorly managed.1 Available antiasthmatic agents such as anticholinergic agents, β2 selective adrenergic agonists, methyl xanthines, antihistamines, mast cell stabilizers and corticosteroids are inadequate-.

  19. The Use of Levocetirizine (L-Cet Syrup in Children with Allergic Diseases

    Directory of Open Access Journals (Sweden)

    Yu.V. Marushko

    2015-10-01

    Full Text Available The article deals with the application of antihistamines in allergic diseases in children. In particular, attention is paid to the L-enantiomer of cetirizine, a selective H1 receptor antagonist levocetirizine. A review of recent literature data on the efficacy and safety of this drug is presented.

  20. Acute and Chronic Urticaria: Evaluation and Treatment.

    Science.gov (United States)

    Schaefer, Paul

    2017-06-01

    Urticaria commonly presents with intensely pruritic wheals, sometimes with edema of the subcutaneous or interstitial tissue. It has a lifetime prevalence of about 20%. Although often self-limited and benign, it can cause significant discomfort, continue for months to years, and uncommonly represent a serious systemic disease or life-threatening allergic reaction. Urticaria is caused by immunoglobulin E- and non-immunoglobulin E-mediated release of histamine and other inflammatory mediators from mast cells and basophils. Diagnosis is made clinically; anaphylaxis must be ruled out. Chronic urticaria is idiopathic in 80% to 90% of cases. Only a limited nonspecific laboratory workup should be considered unless elements of the history or physical examination suggest specific underlying conditions. The mainstay of treatment is avoidance of triggers, if identified. The first-line pharmacotherapy is second-generation H1 antihistamines, which can be titrated to greater than standard doses. First-generation H1 antihistamines, H2 antihistamines, leukotriene receptor antagonists, high-potency antihistamines, and brief corticosteroid bursts may be used as adjunctive treatment. In refractory chronic urticaria, patients can be referred to subspecialists for additional treatments, such as omalizumab or cyclosporine. More than one-half of patients with chronic urticaria will have resolution or improvement of symptoms within a year.

  1. Management of chronic urticaria in Asia: 2010 AADV consensus guidelines

    Science.gov (United States)

    2012-01-01

    This guideline is a result of a consensus reached during the 19th Asian-Australasian Regional Conference of Dermatology by the Asian Academy of Dermatology and Venereology Study Group in collaboration with the League of Asian Dermatological Societies in 2010. Urticaria has a profound impact on the quality of life in Asia and the need for effective treatment is required. In line with the EAACI/GA2LEN/EDF/WAO guideline for the management of urticaria the recommended first-line treatment is new generation, non-sedating H1-antihistamines. If standard dosing is ineffective, increasing the dosage up to four-fold is recommended. For patients who do not respond to a four-fold increase in dosage of non-sedating H1-antihistamines, it is recommended that therapies such as H2-antihistamine, leukotriene antagonist, and cyclosporine A should be added to the antihistamine treatment. In the choice of second-line treatment, both their costs and risk/benefit profiles are the most important considerations. PMID:22701866

  2. Fulltext PDF

    Indian Academy of Sciences (India)

    Admin

    tibodies, e.g. CD3 is present on. T cells whereas CD19 is present on B cells. 13. Histamines: Derivatives of the amino acid Histidine that are released by mast cells upon ex- posure to allergens. Binding to their receptors leads to smooth muscle contraction, mucus se- cretion, etc. Anti-histamines are widely used to counter ...

  3. The pharmacotherapy of low back pain

    African Journals Online (AJOL)

    (AHR-85), the monocarbamate of 3-(o-methoxyphenoxy)-1,2-propanediol with chemically related interneuronal depressant drugs. J.Pharmacol.Exp.Ther. 1958. Feb;122(2):239-246. 13. Rumore M, Schlichting D. Analgesic effects of antihistaminics. Life Sci. 1985;36(5):403-416. 14. Syvälahti E, Kunelios R, Lauren L. Effects ...

  4. Diphenhydramine overdose

    Science.gov (United States)

    ... antihistamine. It is used in some allergy and sleep medicines. Overdose occurs when someone takes more than the normal or recommended amount of this medicine. This can be by accident or on purpose. This article is for information only. DO NOT ...

  5. The usage and efficacy of a combination analgesic preparation

    African Journals Online (AJOL)

    QuickSilver

    in everyday practice for pain relief. The secondary objective was to correlate efficacy of the treatment with the demographic characteristics of the ... feine, antihistamines, pemoline, amino acids, and vitamins. The World Health Organisation (WHO) recommends that analgesia be administered according to a three rung “Pain.

  6. Synthesis of 1-Substituted-4-(Pyridin-4-yl)

    African Journals Online (AJOL)

    Purpose: To synthesize a new series of 1-substituted-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a]quinazolin- 5(4H)-ones and evaluate them for H1-antihistaminic activity with negligible side effects in guinea pigs. Methods: The synthesized compounds were characterized by Infrared spectroscopy (IR), proton nuclear magnetic ...

  7. ACUTE AND SUBCHRONIC EFFECTS OF THE H-1-HISTAMINE RECEPTOR ANTAGONIST EBASTINE IN 10, 20 AND 30 MG DOSE, AND TRIPROLIDINE 10 MG ON CAR DRIVING PERFORMANCE

    NARCIS (Netherlands)

    BROOKHUIS, KA; DEVRIES, G; DEWAARD, D

    1 The effects of a new antihistamine, ebastine (10, 20 and 30 mg), on several parameters of driving performance in actual traffic were studied in 15 healthy male volunteers. Subjects were treated for 5 days, and their driving performance tested on day 1 and day 5. The study was double-blind, placebo

  8. Clinical utility and patient adherence with ebastine for allergic rhinitis

    Directory of Open Access Journals (Sweden)

    Giorgio Ciprandi

    2010-10-01

    Full Text Available Giorgio CiprandiDepartment of Internal Medicine, San Martino Hospital, Genoa, ItalyAbstract: Allergic rhinitis (AR is a high prevalence disease, affecting 10%–20% of the general population. AR is sustained by an IgE-mediated reaction, and by a complex inflammatory network of cells, mediators, and cytokines, becoming chronic when exposure to allergen persists. A Th2-biased immune response is the basis for the allergic inflammation. Histamine plays a relevant role in symptom occurrence. Therefore, antihistamine use represents a cornerstone in AR management. Ebastine, a novel antihistamine, is effective overall in controlling symptoms, and its safety profile is good. Recently, a new formulation has been developed, ie, a fast-dissolving tablet. Several studies have demonstrated its favorable characteristics. In conclusion, ebastine is an effective and well tolerated antihistamine that may be prescribed for the treatment of AR. The fast-dissolving tablet formulation provides a new option which may be particularly convenient for the patient.Keywords: allergic rhinitis, histamine, antihistamines, ebastine, tablets

  9. Complementary Fluorescence and Phosphorescence Study of the Interaction of Brompheniramine with Human Serum Albumin

    NARCIS (Netherlands)

    Tardioli, S.; mr. Lammers, I.; Hooijschuur, J.H.; Ariese, F.; van der Zwan, G.; Gooijer, C.

    2012-01-01

    Binding of the antihistamine drug brompheniramine (BPA) to human serum albumin (HSA) is studied by measuring quenching of the fluorescence and room temperature phosphorescence (RTP) of tryptophan. The modified Stern-Volmer equation was used to derive association constants and accessible fractions

  10. Diprosone Ointment In Psoriasis

    African Journals Online (AJOL)

    trial. No other local applications, no oral steroids and no oral antihistaminics were permitted during the trial, and none of the patients had been on them for at least a week before the trial. Study Design. The patients were assigned at random in double-blind. fashion to product A (Diprosone) or to product B. (Topilar).

  11. Recurrent facial urticaria following herpes simplex labialis

    Directory of Open Access Journals (Sweden)

    Vijay Zawar

    2012-01-01

    Full Text Available We describe recurrent acute right-sided facial urticaria associated with herpes labialis infection in a middle-aged female patient. Antiviral medications and antihistamines not only successfully cleared the herpes infection and urticaria but also prevented further recurrences.

  12. Solar urticaria

    Directory of Open Access Journals (Sweden)

    Srinivas C

    1995-01-01

    Full Text Available A 35-year-old female and a 41-year-old male presented with clinical features suggestive of solar urticaria. The diagnosis of solar urticaria and the effectiveness of a combination of H1 and H2 blocking antihistamines were confirmed by phototesting with a solar simulator

  13. Life-threatening ACE inhibitor-induced angio-oedema successfully treated with icatibant

    DEFF Research Database (Denmark)

    Ostenfeld, Sarah; Bygum, Anette; Rasmussen, Eva Rye

    2015-01-01

    We present a case of a 75-year-old woman treated with an ACE inhibitor, who presented with angio-oedema of the tongue and had difficulty speaking. No symptoms of anaphylaxis or urticaria were present. The patient was treated intravenously with antihistamine and glucocorticoid in combination...

  14. Life-threatening systemic toxicity and airway compromise from a common European adder bite to the tongue

    DEFF Research Database (Denmark)

    Hoegberg, L C G; Jessen, C L; Lambertsen, K

    2009-01-01

    A 24-year-old man was bit on the tongue by a European common adder. Within 15 min following envenomation, he experienced tongue swelling, hypotension and impaired consciousness. Antihistamine, corticosteroid and crystalloids were administered. Within 105 min of envenomation, increasing oral...

  15. How not to miss autoinflammatory diseases masquerading as urticaria

    DEFF Research Database (Denmark)

    Krause, K; Grattan, C E; Bindslev-Jensen, C

    2012-01-01

    symptoms including recurrent fever attacks, arthralgia or arthritis and fatigue. Autoinflammatory diseases are often associated with a diagnostic delay of many years and do not respond to antihistamines and other treatments of urticaria. Also, the chronic inflammation may lead to long-term complications...

  16. Účinek H1-antihistaminik na oxidativní vzplanutí fagocytů

    Czech Academy of Sciences Publication Activity Database

    Králová, Jana; Číž, Milan; Nosál, R.; Drábiková, K.; Lojek, Antonín

    2005-01-01

    Roč. 54, č. 4 (2005), s. 196 R&D Projects: GA ČR(CZ) GA305/04/0896 Institutional research plan: CEZ:AV0Z50040507 Keywords : antihistamines * oxidative burst * phagocytes Subject RIV: BO - Biophysics

  17. SUMMARY

    African Journals Online (AJOL)

    drug was identified in 66.6% of responders and these consisted of. Antihistamines in 54%, corticosteroids in 7.9%, and Vitamin B Complex in 6.3%. Itching with oral CQ occurred in 100% of the responders and in 49% with intramuscular injection ...

  18. Severe food allergy and anaphylaxis: Treatment, risk assessment ...

    African Journals Online (AJOL)

    Adjunctive measures include nebulised bronchodilators for lower-airway obstruction, nebulised adrenaline for stridor, antihistamines and corticosteroids. Patients with an anaphylactic reaction should be admitted to a medical facility so that possible biphasic reactions may be observed and risk-reduction strategies initiated ...

  19. ÿþM i c r o s o f t W o r d - a a m , 2 0 0 8 , v o l . 7 , N o . 2 , 9 1

    African Journals Online (AJOL)

    ÿþE m m a n u e l A m e h

    But, there was no associated epistaxis or sneezing bouts or otalgia. For this problem patient has received several topical medications without relief. Past medical history was not contributory. No known drug allergy, and currently on a topical antihistamine nasal drop. The patient is a second of six siblings in a monogamous ...

  20. Bug bites and stings: When to see a dermatologist

    Medline Plus

    Full Text Available ... correct dose. For bites that itch , apply an ice pack or an over-the-counter anti-itch cream, such as hydrocortisone. Another option is to take an over-the-counter oral antihistamine. To reduce swelling , apply an ice pack to the bite. If you experience any ...

  1. Nigella sativa provides protection against metabolic syndrome ...

    African Journals Online (AJOL)

    Improvement in all other parameters like blood pressure, circumference of waist and serum triglyceride was also observed. Thus, Nigella seeds were found to be effective as an adjuvant therapy in patients of dyslipidemia and hyperglycemia. Keywords: Nigella sativa, toxicity, hyperglycemia, adjuvant, antihistaminic, ...

  2. Management of Allergic Rhinitis: A Review for the Community Pharmacist.

    Science.gov (United States)

    May, J Russell; Dolen, William K

    2017-12-01

    Allergic rhinitis is a highly prevalent disease affecting the quality of life of millions of North Americans. The management of allergic rhinitis includes allergen avoidance, pharmacotherapy, and immunotherapy. Current pharmacologic options include oral and intranasal antihistamines, intranasal corticosteroids, oral and intranasal decongestants, oral and intranasal anticholinergics, and leukotriene receptor antagonists. Second-generation oral antihistamines and intranasal corticosteroids are the mainstays of treatment, with practice guidelines recommending intranasal corticosteroids as first-line treatment for moderate to severe allergic rhinitis. Clinical trials studying a widely used intranasal corticosteroid, fluticasone propionate, in comparison with second-generation oral antihistamines, cetirizine, loratadine, or montelukast, were selected to support the comparative review of the efficacy and tolerability of these 2 classes of medications. Studies evaluating the combination of fluticasone propionate with an oral antihistamine were also included to review the efficacy and tolerability of combination therapy to treat allergic rhinitis. Studies comparing fluticasone propionate with cetirizine had mixed findings; fluticasone propionate was found to have equal or greater efficacy in reducing nasal symptom scores. Combination therapy of fluticasone propionate and the oral antihistamine, loratadine, was found to have efficacy comparable with that of intranasal corticosteroid alone. Many of these medications are available over the counter in the pharmacy, and the community pharmacist plays an important role as part of the patient's health care team in managing this disease. Pharmacotherapy is patient-specific, based on type, duration, and severity of symptoms, comorbidities, prior treatment, and patient preference. This article aims to provide an overview of the pathophysiology, available treatment options, guideline recommendations, and role of the pharmacist for

  3. A double dose of levocetirizine leads to better control of histamine-induced flare, wheal and itch in healthy donors.

    Science.gov (United States)

    Tanizaki, Hideaki; Nakamizo, Satoshi; Nakahigashi, Kyoko; Miyachi, Yoshiki; Kabashima, Kenji

    2013-01-01

    Levocetirizine is classified as a nonsedating second-generation antihistamine. This drug is used to treat allergic disorders such as urticaria and pruritus. Thus far, studies have demonstrated an increase in efficacy for refractory urticaria by increasing doses of antihistamines; however, more lines of supportive evidence for these guidelines are required to justify this management strategy. In this study, we found that a double dose of levocetirizine suppressed histamine-induced flare formation more rapidly and sustainably, and wheal and itch more extensively, compared with the conventional dose using both visual and laser Doppler imaging scales in a noninvasive manner. These results suggest that double-dosed levocetirizine treatment suppresses histamine-induced skin symptoms more rapidly, profoundly and sustainably than conventionally dosed levocetirizine treatment. © 2013 S. Karger AG, Basel.

  4. Comparison of the efficacy of fexofenadine 120 and 240 mg/day on chronic idiopathic urticaria and histamine-induced skin responses in Japanese populations.

    Science.gov (United States)

    Tanizaki, Hideaki; Nakahigashi, Kyoko; Miyachi, Yoshiki; Kabashima, Kenji

    2013-12-01

    H1-antihistamines are the first-line treatment of chronic idiopathic urticaria (CIU), but CIU is occasionally refractory to the conventional treatment doses. Guidelines in Europe recommend increasing doses as second-line therapy; however, more supportive evidences for these guidelines are required to justify this management strategy. In this study, the authors evaluated the effect of conventional and double doses of fexofenadine HCl on CIU and on histamine-induced skin responses by iontophoresis using visual and laser Doppler imaging scales in healthy donors. Cutaneous manifestations in CIU and histamine-induced flare and itch in healthy donors were attenuated more extensively by a double dose of fexofenadine HCl compared with a conventional dose. The above findings support the management strategy that increasing the dose of non-sedative antihistamines is the second-line treatment choice for refractory CIU even in Japanese populations.

  5. PECULIARITIES OF CLINICAL COURSE AND TREATMENT OF ALLERGIC RHINITIS ASSOCIATED WITH CANDIDA IN SCHOOLCHILDREN

    Directory of Open Access Journals (Sweden)

    T. G. Malanicheva

    2011-01-01

    Full Text Available 60 children 7–15 years old with year-round allergic rhinitis (AR and colonization of mucous tunic with Candida and Staphylococcus aureus were observed. At the first stage main group (35 children was treated with antibiotic fusafungine — Bioparox which is active against Candida and Staphylococcus aureus in dosage 4 inhalations 4 times daily during 7–10 days combined with antihistamine drugs. At the second stage patients received anti-allergic treatment of year-round AR with cromones, topical corticosteroids and antihistamine drugs according to the severity of a disease. The second group (25 children was treated according to the traditional anti-allergicь scheme of therapy. Complex treatment with fusafungine resulted in beneficial therapeutic effect in 77 % patients. Exacerbation period decreased 1.8 times lower and remission was 2.7 times longer. Cultural mycological and bacteriological analyses were negative in most patients with AR.

  6. Acute Generalized Exanthematous Pustulosis (AGEP Induced by Cetirizine in a Child A Case Report

    Directory of Open Access Journals (Sweden)

    Gunseli Pancar

    2014-12-01

    Full Text Available Acute Generalized Exanthematous Pustulosis (AGEP, is a rare cutaneous rash characterized by widespread sterile non-follicular pustules. AGEP is a rare disease in childhood and it is often due to drugs. Antibiotics, sulphanamides and antipyretic-analgesics are the main reasons of this drug reaction . Cetirizine is a second generation antihistamine is often used in the treatment of angioedema, atopic dermatitis and urticaria in children. Cetirizine induced AGEP was not reported in the literature. In this case a twelve year old child was admitted with urticarial plaques located on her trunk. She developed maculopapular lesions and pustular eruption with Cetirizine (once a day treatment. Cetirizine was stopped and the nonfollicular pustules cleared with a desquamation. The result of the oral challenge test was positive. We present this rare case to show that the antihistamines (cetirizine may cause AGEP in childhood.

  7. Pregnancy: a therapeutic dilemma

    Directory of Open Access Journals (Sweden)

    Ligia Brzezińska-Wcisło

    2017-10-01

    Full Text Available Treatment during pregnancy is problematic. The Food and Drug Administration established drug categories to help in the treatment process. First-generation antihistamines are considered safe but they have sedative properties. Second-generation antihistamines cause less adverse reactions but besides cetirizine and loratadine they belong to category C. All retinoids should be avoided during pregnancy due to the risk of fetal malformations. Antimalarial drugs should be considered based on the clinical data. Sulfones can be considered as safe for use during pregnancy only with proper monitoring. Prednisone is administered in pregnancy. Other glucocorticosteroids have a different safety profile. Cyclosporine A treatment should be reserved as rescue therapy in severe stages of the disease. Treatment during pregnancy should be precise when it comes to pregnant woman and safe for the fetus.

  8. Acute Generalized Exanthematous Pustulosis (AGEP Induced by Cetirizine in a Child A Case Report

    Directory of Open Access Journals (Sweden)

    Gunseli Pancar

    2016-05-01

    Full Text Available Acute Generalized Exanthematous Pustulosis (AGEP, is a rare cutaneous rash characterized by widespread sterile non-follicular pustules. AGEP is a rare disease in childhood and it is often due to drugs. Antibiotics, sulphanamides and antipyretic-analgesics are the main reasons of this drug reaction . Cetirizine is a second generation antihistamine is often used in the treatment of angioedema, atopic dermatitis and urticaria in children. Cetirizine induced AGEP was not reported in the literature. In this case a twelve year old child was admitted with urticarial plaques located on her trunk. She developed maculopapular lesions and pustular eruption with Cetirizine (once a day treatment. Cetirizine was stopped and the nonfollicular pustules cleared with a desquamation. The result of the oral challenge test was positive. We present this rare case to show that the antihistamines (cetirizine may cause AGEP in childhood.

  9. Experimentally induced nasal hypersecretion does not reduce the efficacy of intranasal levocabastine

    DEFF Research Database (Denmark)

    Borum, Stefan; Nielsen, K; Bisgaard, H

    1998-01-01

    In allergic rhinitis, a nasal H1-antihistamine spray seems to be well suited for usage on an as-needed basis, because it has a quick onset of action, and many patients prefer to take medicine only when they have symptoms. It is a prerequisite, however, that nasal hypersecretion during a rhinitis...... episode does not significantly reduce the efficacy of intranasal treatment by washing away the drug before it reaches the H1-histamine receptors. In order to investigate this problem, we have induced nasal hypersecretion with a methacholine challenge in one experiment and in four experiments we have......% (p antihistamine spray. We conclude that experimentally induced nasal hypersecretion does not reduce the efficacy...

  10. Otitis Media with Effusion: Our National Practice.

    Science.gov (United States)

    Roditi, Rachel E; Rosenfeld, Richard M; Shin, Jennifer J

    2017-08-01

    Otitis media with effusion (OME) is the focus of an updated multidisciplinary clinical practice guideline published by the American Academy of Otolaryngology-Head and Neck Surgery Foundation (AAO-HNSF) and the American Academy of Pediatrics (AAP). Based on data from clinical trials, the guideline recommends against using antihistamines, antibiotics, oral steroids, and intranasal steroids for OME. To understand practice patterns related to these guidelines, we assessed nationally representative data. Despite controlling for age, sex, race/ethnicity, and other potential confounders individualized for each medication class, an increased risk of antihistamine (odds ratio [OR], 3.53), antibiotic (OR, 4.31), and intranasal steroid administration (OR, 3.58) was seen when OME was diagnosed. These analyses have demonstrated opportunities for quality improvement in the care of patients with OME, quantifying gaps in practice relevant to proposed quality measures. Education targeted according to practice setting may facilitate appropriate therapy and/or referral for definitive intervention in children with OME.

  11. Delayed pressure urticaria - dapsone heading for first-line therapy?

    Science.gov (United States)

    Grundmann, Sonja Alexandra; Kiefer, Sabine; Luger, Thomas Anton; Brehler, Randolf

    2011-11-01

    Pressure urticaria as a subform of physical urticaria is rare and treatment is often difficult. Established therapeutic regimes include antihistamines (generally exceeding approved dosages in order to achieve a therapeutic benefit) or antihistamines combined with montelukast. Complete relief of symptoms is difficult. We used dapsone as an early therapeutic alternative in the event of treatment failure and established a standardized therapeutic regime at our clinic. We surveyed 31 patients retrospectively who had received dapsone between 2003-2009. In 74 % of patients in whom symptoms persisted despite established therapies, the results of treatment with dapsone were good or very good. Longer-term pressure urticaria and the co-existence of a chronic spontaneous urticaria were associated with a smaller benefit (pdapsone in patients with pressure urticaria has such a good risk-benefit ratio that we support early treatment initiation. © The Authors • Journal compilation © Blackwell Verlag GmbH, Berlin.

  12. Treating rhinitis in the older population: special considerations

    Directory of Open Access Journals (Sweden)

    Slavin Raymond G

    2009-12-01

    Full Text Available Abstract Rhinitis in the elderly is a common but often neglected condition. Structural changes in the nose associated with aging, predisposes the elderly to rhinitis. There are a number of specific factors that affect medical treatment of the elderly including polypharmacy, cognitive dysfunction, changes in body composition, impairment of liver and renal function and the cost of medications in the face of limited resources. Rhinitis in the elderly can be placed in several categories and treatment should be appropriate for each condition. The most important aim is to moisten the nasal mucosa since the nose of the elderly is so dry. Great caution should be used in treatment with first generation antihistamines and decongestants. Medications generally well tolerated by the elderly are second generation antihistamines, intra-nasal anti-inflammatory agents, leukotriene modifiers and iprapropium nasal spray.

  13. Interaction of active compounds from Aegle marmelos CORREA with histamine-1 receptor

    Science.gov (United States)

    Nugroho, Agung Endro; Agistia, Dany Dwi; Tegar, Maulana; Purnomo, Hari

    2013-01-01

    The aim of this study is to determine the affinity of six active compounds of Aegle Marmelos Correa, they are (E, R)-Marmin, skimmianine, (S)-aegeline, aurapten, zeorin, and dustanin as antihistamines in histamine H1 receptor in comparison to cetirizin, diphenhydramine and chlorpheniramine as ligands comparison. Previously, in the in vitro study marmin obviously antagonized the histamine H1 receptor in a competitive manner. Methods: molecular docking to determine the interaction of ligand binding to its receptor. Lower docking score indicates more stable binding to that protein. Results: Marmin, skimmianine, aegeline, aurapten, zeorin, and dustanin were potential to develop as antihistamine agents, especially as histamine H1 receptor antagonists by interacting with amino acid residues, Asp107, Lys179, Lys191, Asn198, and Trp428 of histamine H1 receptor. Conclusions: Based on molecular docking, Amino acid residues involved in ligand protein interactions were Asp107, Lys179, Lys191, Asn198, and Trp428. PMID:23750086

  14. Paroxysmal Hypnogenic Dyskinesia Responsive to Doxylamine: A Case Report

    Directory of Open Access Journals (Sweden)

    Daniel M. Williams

    2012-01-01

    Full Text Available Paroxysmal hypnogenic dyskinesia is a rare clinical entity characterized by intermittent dystonia and choreoathetoid movements that begin exclusively during sleep, often with consciousness preserved once the patient is awakened during the episodes. They occur almost every night and are often misdiagnosed as sleeping disorders. Paroxysmal hypnogenic dyskinesia is currently known to be a form of frontal lobe epilepsy, but not in all cases. We present a 19-year-old male patient with paroxysmal hypnogenic dyskinesia who responded to antihistamines. This supports an alternative theory from 1977 (before the cases had been adequately described that the disorder lies in dysregulation in the basal ganglia. This description now appears similar to acute dystonic reactions such as extrapyramidal symptoms from antipsychotic medications, which also respond to antihistamines.

  15. Correlation between the histopathology of chronic urticaria and its clinical picture.

    Science.gov (United States)

    Marques, Raquel Zappa Silva; Criado, Roberta Fachini Jardim; Machado, Carlos D'Apparecida Santos; Tamanini, Juliana Milhomem; Mello, Cristina van Blarcum de Graaff; Speyer, Carolina

    2016-01-01

    Chronic urticaria is characterized by transient, pruritic lesions of varying sizes, with central pallor and well-defined edges, with disease duration longer than six weeks. Its cellular infiltrate consists of neutrophils, lymphocytes and eosinophils. There is a subgroup of patients with eosinophilic or neutrophilic urticaria, resistant to the treatment with antihistamines, but that respond to a combination of antihistamine with other drugs. To evaluate the present infiltration in chronic urticaria biopsies and correlate it with the clinical disease activity and response to treatment. Forty-one patients with chronic urticaria were classified according to the score of severity of the disease, response to treatment and type of perivascular infiltrate. Inflammatory infiltrates were divided in eosinophilic (46.30%), neutrophilic and mixed. An association was found between the eosinophilic infiltrate and clinical scores of greater severity (p = 0.002). This association shows that the eosinophilic inflammatory infiltrates denote high clinical activity, which means more severe and exuberant clinical pictures of the disease.

  16. [Study of the association of Malassezia furfur with chronic urticaria among the ship crews].

    Science.gov (United States)

    Tang, Xin-ping; Zeng, Kang; Chen, Guan-hua; Bi, Long-yan; Fan, Long-zhong; Shao, Chang-fa

    2003-08-01

    To investigate the association of Malassezia furfur with chronic urticaria in the crew members of ships. A comparative mycological study of 126 crew members of ships with chronic urticaria and 45 normal control subjects was carried out. The 82 urticaria patients identified as positive for Malassezia furfur were divided into groups A and B to receive treatment with antihistaminics (group A) and antihistaminics combined with 2% ketoconazole shampoo(group A). The carrier rates of Malassezia furfur were significantly higher in urticaria patients than in the normal control subjects (P0.05). But 6 to 8 weeks from the end of the treatment course, better therapeutic effect was noted in group B (PMalassezia furfur findings (PMalassezia furfur may play an important role in the prevalence of chronic urticaria among the crew members, and anti-fungal treatment may produce better long-term therapeutic effect.

  17. Lack of effects of astemizole on vestibular ocular reflex, motion sickness, and cognitive performance in man

    Science.gov (United States)

    Kohl, Randall L.; Homick, Jerry L.; Cintron, Nitza; Calkins, Dick S.

    1987-01-01

    Astemizole was orally administered to 20 subjects in a randomized, double-blind design to assess the efficacy of this peripherally active antihistamine as an antimotion sickness drug possessing no central side-effects. Measures of vestibular ocular reflex (VOR) were made to evaluate the agent as a selective vestibular depressant. Following one week of orally administered astemizole (30 mg daily), a Staircase Profile Test, a VOR test, and a variety of tests of cognitive performance were administered. These tests revealed no statistically significant effects of astemizole. This leads to the conclusion that, although the drug probably reaches the peripheral vestibular apparatus in man by crossing the blood-vestibular barrier, a selective peripheral antihistamine (H1) action is inadequate to control motion sickness induced through cross-coupled accelerative semicircular canal stimulation in a rotating chair.

  18. Allergic conjunctivitis: an update on diagnosis and management.

    Science.gov (United States)

    O'Brien, Terrence P

    2013-10-01

    The focus of this review is to provide a logical paradigm for the diagnosis and treatment of ocular allergies, with a focus on seasonal allergic conjunctivitis (SAC) and perennial allergic conjunctivitis (PAC). Several classes of topical medications are currently available for the management of ocular allergies, including: lubricating agents, vasoconstrictors, antihistamines, mast cell stabilizers, and topical corticosteroids. SAC and PAC make up the vast majority of ocular allergy cases. A proactive approach to these diseases, anticipating the regional spring and fall allergen spikes, is needed for optimally managing these disorders. A multifaceted treatment regimen comprising patient education, lifestyle modification, and topical medications (such as antihistamines and/or mast cell stabilizers and corticosteroids) may be required in order to manage ocular allergies effectively. The appropriate treatment paradigm is based on the severity of the patients' signs and symptoms. For moderate-to-severe cases, especially chronic vernal keratoconjunctivitis, atopic keratoconjunctivitis, and giant papillary conjunctivitis, comanagement with an ophthalmologist is recommended.

  19. Cutaneous larva migrans

    Directory of Open Access Journals (Sweden)

    Aleksandra Wieczorek

    2016-09-01

    Full Text Available Introduction . Cutaneous larva migrans (CLM is a tropical zoonosis, caused by parasites, usually Ancylostoma braziliense. Humans are an accidental host. Polish patients with CLM are usually tourists visiting tropical and subtropical countries. The first symptoms do not always appear as creeping eruptions, which complicates the diagnosis. Objective. To present the case of a man with CLM after returning from Thailand to Poland and associated diagnostic difficulties. Case report. We present a case of a 28-year-old man who returned to Poland from Thailand. The first symptoms appeared as disseminated pruritic papules. No improvement after treatment with corticosteroids and antihistamines was observed. The diagnosis was established after the appearance of serpentine erythemas and improvement after albendazole therapy. Conclusions. In the case of returnees from exotic countries suffering from raised, pruritic rashes, and no improvement after treatment with corticosteroids and antihistamines, parasitic etiology should be considered.

  20. DIAGNOSIS AND MANAGEMENT CHRONIC INSOMNIA

    Directory of Open Access Journals (Sweden)

    G.A Dian Puspitha Candra

    2013-03-01

    Full Text Available Insomnia is defined as difficulty to start sleeping, maintain it, or low quality sleeping, if the condition persist for more than one month, it is called chronic insomnia. Diagnosis is made through anamnesa and sleep wake diaries, aktigraphy, polisomnography. Pharmachologycally drugs that have been used to treat insomnia are benzodiazepin reseptor agonis, antihistamine, antidepressant. Non pharmacological ways include behavioural intervention for insomnia, give significant result in decreasing sleep latency, reducing awakness duration during the night and improving total sleeping time.

  1. Clinical Management of Heat-Related Illnesses

    Science.gov (United States)

    2012-01-01

    drugs that decrease thirst •  Haloperidol drugs that decrease Sweating •  Antihistamines •  Anticholinergics •  Phenothiazines •  Benztropine...hyperthermia, but it may also occur as a result of elec- trolyte abnormalities. The use of norepinephrine and other α-adrenergic drugs should be avoided because...they cause vaso- constriction, thereby reducing heat exchange through the skin. Anticholinergic drugs that inhibit sweating (e.g., atropine) should

  2. PCBs Alter Dopamine Mediated Function in Aging Workers

    Science.gov (United States)

    2011-01-01

    58.23 % Women 39 41.03 % 73 49.32 % a Number of observations varies across characteristics due to missing values. b Cardiovascular drugs (Class 24...inhibitors. c CNS active medications include: antihistamines , sympathomimetic agents, beta- adrenergic blocking agents, angiotensin-converting enzyme...comprehensive medical history, including use of over-the- counter and prescription drugs , as well as (if applicable) female reproductive histories

  3. Drugs and Alcohol in Civil Aviation Accident Pilot Fatalities from 2004-2008

    Science.gov (United States)

    2011-09-01

    over the past 20 years. Factors were examined that could influence drug trends noted over the years. Diphenhydramine, an H1 antihistamine with...Oklahoma City, OK 73125 September 2011 Final Report Drugs and Alcohol in Civil Aviation Accident Pilot Fatalities From 2004-2008 DOT/FAA/AM-11/13 Office...2. Government Accession No. 3. Recipient’s Catalog No. DOT/FAA/AM-11/13 4. Title and Subtitle 5. Report Date September 2011 Drugs

  4. Motion Sickness Prevention by Stroboscopic Environment during Simulated Military Transport

    Science.gov (United States)

    2009-07-20

    known, most of these drugs fall into three classes: antidopaminergics, anticholinergics, and antihistamines ( Drug Facts and Comparisons, 1999...vomiting 2 center also is directly stimulated by motion and by high levels of acetylcholine. Therefore, most drugs that are used to prevent or...Brendley, K. W., Marti, J., & DiZio, P. 2003. Motion Coupled Visual Environment (MOCOVE): Drug -Free Alleviations of Motion Sickness. U.S

  5. Effects of bilastine on T-wave morphology and the QTc interval

    DEFF Research Database (Denmark)

    Graff, Claus; Struijk, Johannes J.; Kanters, Jørgen K.

    2012-01-01

    The International Conference of Harmonisation (ICH) E14 guideline for thorough QT studies requires assessing the propensity of new non-antiarrhythmic drugs to affect cardiac repolarization. The present study investigates whether a composite ECG measure of T-wave morphology (Morphology Combination...... Score [MCS]) can be used together with the heart rate corrected QT interval (QTc) in a fully ICH E14-compliant thorough QT study to exclude clinically relevant repolarization effects of bilastine, a novel antihistamine....

  6. Development of Antidepressants as Novel Agents To Treat Small Cell Lung Cancer

    Science.gov (United States)

    2014-08-01

    results led us to further investigate the effects and mech- anisms of action of the two best candidate drugs , the TCA imi- pramine and the antihistamine ...used a systematic drug repositioning bioinformatics approach querying a large compendium of gene expression profiles to identify candidate U.S. Food...and Drug Administration (FDA)-approved drugs to treat SCLC. We found that tricyclic antidepressants and related molecules potently induce apoptosis

  7. CHOICE OF OPTIMAL COMPOSITION OF FEXOFENSDINE GEL WITH ANTI-ALLERGIC EFFECT

    Directory of Open Access Journals (Sweden)

    Z. D. Khadzhieva

    2015-01-01

    Full Text Available The prospects of topical formulation development with fexofenadine are conditioned by the possibility of its use in symptomatic, as well as in the combined therapy of allergic reactions on a skin, and the expansion of the pharmaceutical market of antihistamine drugs for external application. The article presents a study of a choice of optimal gel composition with fexofenadine with antiallergic action, we have also substantiated the choice of necessary auxiliary substances.

  8. Preliminary Validation of a Readiness-to-Fly Assessment Tool for Use in Naval Aviation

    Science.gov (United States)

    2010-05-25

    current industry standard tool. Finally, combining the individual diagnostic power of Flight Fit and PMI Fit 2000 with established group measures such as...hours. (circle all that apply) a. None d. Antihistamines b. Sedatives/Tranquilizers e. Decongestants c. Aspirin /Tylenol/any...on a suite of industry standard fatigue-sensitive measures (e.g., the Psychomotor Vigilance Test) at regular intervals over 25 hours of continual

  9. A comparative study of various therapeutic regimens in urticaria

    Directory of Open Access Journals (Sweden)

    Mukhopadhyay Amiyakumar

    1995-01-01

    Full Text Available 127 patients of urticaria were treated with chlorpheniramine maleate alone and in combination with cyproheptadine hydrochloride, ranitidine and doxepin and levamisole. Chlorpheniramine and doxepin combination showed a satisfactory result in 88.46% of patients. Overall study showed that a combination regimen is better than the antihistaminics alone. Drowsiness was the commonest side effect. Levamisole and chlorpheniramine maleate combination was found to be more effective than the antihimstamine alone.

  10. Icatibant er en ny behandlingsmulighed ved livstruende angiotensinkonverterende enzym-inhibitor-udløst angioødem

    DEFF Research Database (Denmark)

    Fast, Søren; Henningsen, Emil; Bygum, Anette

    2011-01-01

    A 78 year-old woman with life-threatening angiotensin-converting enzyme inhibitor (ACE-i) induced angioedema was unresponsive to conventional treatment with corticosteroids, antihistamines and epinephrine. She was successfully treated with icatibant licensed for treatment of hereditary angioedema...... knowing that both conditions involve bradykinin induced activation of bradykinin B2 receptors. Randomised, controlled trials are warranted to document the efficacy of icatibant in ACE-i angioedema....

  11. Angioedema without urticaria in childhood.

    Science.gov (United States)

    Ertoy Karagol, Hacer I; Yilmaz, Ozlem; Bakirtas, Arzu; Topal, Erdem; Demirsoy, Mehmet S; Turktas, Ipek

    2013-11-01

    There has been no separate study investigating angioedema without urticaria (Aw/oU) exclusively in children so far. The purpose of this study was to investigate the frequency, clinical presentation, etiology, management and follow-up of Aw/oU in children. This is a prospective study that included all consecutive patients with a history of Aw/oU referred to our clinic between January 2011 and May 2012. A standard diagnostic and therapeutic algorithm was applied to all patients. The frequency of Aw/oU was found to be 1.6% during the study period. An etiological factor could be found in only 45 patients (49%). The causes of Aw/oU were infection (21%), allergy (14%), thyroid autoimmunity (TA)-related (8%) and nonsteroid anti-inflammatory drug hypersensitivity (6%), and idiopathic angioedema (51%). There was no hereditary type I, II or acquired type of angioedema or rare syndromes associated with Aw/oU. The median follow-up was 16 months (range: 12-30 months). Antihistamine prophylaxis was initiated at therapeutic doses in 20 patients with frequently recurrent angioedema due to idiopathic and euthyroid TA-related Aw/oU for 3 months. These patients responded to antihistamine prophylaxis for 3 months. Four patients relapsed after cessation of prophylaxis at the end of 3 months. Antihistamine prophylaxis was prolonged to 6 months in three patients and to 9 months in one patient. Angioedema without urticaria in children is a rare condition and no etiology can be identified in half of them. Antihistamine treatment alone is sufficient, and prognosis is good in recurrent non hereditary cases in a short-term follow-up period. © 2013 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  12. Cyclosporine Treatment in a Patient with Concurrent Autoimmune Urticaria and Autoimmune Hepatitis

    OpenAIRE

    Ju, Hye Young; Kim, Hei Sung; Kim, Hyung Ok; Park, Young Min

    2009-01-01

    Patients with autoimmune urticaria show a higher rate of seropositivity for other autoantibodies and often have a history of autoimmune conditions. They also tend to have more severe symptoms and to have a poor response to conventional antihistamine treatment. Autoimmune hepatitis is a chronic inflammatory disorder in which progressive liver injury is thought to be the result of a T-cell-mediated immunologic attack against liver cells in genetically predisposed individuals. While the associat...

  13. Transient hair loss in patients with chronic spontaneous urticaria treated with omalizumab

    DEFF Research Database (Denmark)

    Noshela Ghazanfar, M; Thomsen, S F

    2017-01-01

    Summary: Omalizumab (anti-IgE) is used as add-on therapy for antihistamine refractory chronic urticaria patients. The most commonly reported adverse effects were headache, arthralgia, upper respiratory infections, fatigue, nausea and injection-site reactions. However, lately a few cases of hair...... loss have been reported. We describe a case of transient hair loss in a young female patient after initiating treatment with omalizumab. Despite this side effect, the patient continued with omalizumab treatment for 10 months with good effect....

  14. Efficacy comparison of cetirizine and loratadine for allergic rhinitis in children

    OpenAIRE

    Juliana; Rita Evalina; Lily Irsa; M. Sjabaroeddin Loebis

    2012-01-01

    Background Allergic rhinitis represents a global health problem affecting 10% to more than 40% of the population worldwide. Several studies in recent years have described the efficacy of second-generation antihistamines in younger children. It is not well established whether cetirizine is more effective than loratadine in reducing symptoms of allergic rhinitis. Objective The objective of this study was to compare the efficacy of loratadine with cetirizine for treatment of allergic rhiniti...

  15. Minimal Clinically Important Difference (MCID) in Allergic Rhinitis: Agency for Healthcare Research and Quality or Anchor-Based Thresholds?

    Science.gov (United States)

    Meltzer, Eli O; Wallace, Dana; Dykewicz, Mark; Shneyer, Lucy

    2016-01-01

    In 2013, the Agency for Healthcare Research and Quality (AHRQ) recommended that allergic rhinitis (AR) studies calculate a minimal clinically important difference (MCID) based on an estimated threshold equal to 30% of the maximum total nasal symptom score. Applying this threshold, their data showed no differences between well-established treatments, and a subsequent analysis using prescribing information found no differences between active treatments and placebo controls. The objective of this study was to demonstrate the application of an evidence-based model to determine MCIDs for AR studies, with an absolute value for an anchor-based threshold and validated methods for calculating distribution-based thresholds. Using the same studies as the AHRQ report, anchor- and distribution-based MCID thresholds were determined for 3 clinical comparisons identified by the AHRQ: (1) oral antihistamine+intranasal corticosteroid (INCS) versus INCS, (2) montelukast versus INCS, and (3) intranasal antihistamine+INCS in a single device versus the monotherapies. The outcomes were compared with those reported using the AHRQ threshold. No treatment comparison met the AHRQ-defined MCID threshold; all treatments were determined to be equivalent for all 3 queries. In contrast, the evidence-based model revealed some differences between treatments: INCS > montelukast; intranasal antihistamine+INCS > either monotherapy. No clinically relevant benefit was observed for adding an oral antihistamine to INCS, but some studies were not optimal choices for quantitative determination of MCIDs. Updating the literature search revealed no additional studies that met the AHRQ inclusion criteria. The evidence-based threshold for MCID determination for AR studies should supersede the threshold recommended in the AHRQ report. Copyright © 2016 The Authors. Published by Elsevier Inc. All rights reserved.

  16. Efficacy comparison of cetirizine and loratadine for allergic rhinitis in children

    OpenAIRE

    Juliana Juliana; Rita Evalina; Lily Irsa; M. Sjabaroeddin Loebis

    2012-01-01

    Background Allergic rhinitis represents a global health problem affecting 10% to more than 40% of the population worldwide. Several studies in recent years have described the efficacy of second-generation antihistamines in younger children. It is not well established whether cetirizine is more effective than loratadine in reducing symptoms of allergic rhinitis. Objective The objective of this study was to compare the efficacy of loratadine with cetirizine for treatment of...

  17. Medications for Allergic Rhinitis.

    Science.gov (United States)

    Roditi, Rachel E; Ishman, Stacey; Lee, Stella; Lin, Sandra; Shin, Jennifer J

    2017-01-01

    Objectives Adherence to the allergic rhinitis clinical practice guideline is being considered as a potential focus for national performance metrics. To help inform this discussion, we assessed patient- and clinician-reported medication administration among nationally representative populations of patients with allergic rhinitis. Study Design Cross-sectional analyses. Setting and Subjects Home health assessments, ambulatory visits. Methods Participants in the National Health and Nutrition Examination Survey and the National Ambulatory Medical Care Survey / National Hospital Ambulatory Medical Care Survey were assessed. The primary outcomes were the percentage of patients reporting receipt of antihistamines and/or nasal steroids among those with allergy-related symptoms and the percentage for whom a clinician administered these medications when diagnosing allergic rhinitis. Secondary outcomes included assessments of those with worse quality of life, confirmatory allergy testing, and leukotriene receptor antagonist use. Results Within the National Health and Nutrition Examination Survey, an estimated 29.2 million patients were diagnosed with "hay fever," while 92.2 million were diagnosed with "allergies." Patients with symptoms of allergic rhinitis reported that antihistamines or nasal steroids were prescribed in 21.1% to 24.0% of cases. Leukotriene receptor antagonists were given to 1.7% of those without asthma or use of other allergy medications. Within the National Ambulatory Medical Care Survey / National Hospital Ambulatory Medical Care Survey, observations representing 149.5 million visits for allergic rhinitis demonstrated that nasal steroids were administered in 29.6% of cases, while nonsedating and sedating antihistamines were given in 22.4% and 17.2%, respectively. Conclusions Despite a high prevalence of allergic rhinitis, per patient report and clinician entry, a substantial number of affected patients do not receive antihistamines and nasal steroids.

  18. Activation of human erythrocyte glutathione – s – transferase (EC.2.5 ...

    African Journals Online (AJOL)

    Various concentrations (0.05mg%, 0.10mg%, 0.20mg%, 0.30mg%, 0.40mg% and 0.50mg%) of each of the antihistamines – cyproheptadine, chlorpheniramine and klemastin (all H – 1 antagonists), were tested on their possible effect on human erythrocyte (red cell) glutathione – S – transferase (EC. 2.5.1.18) activity.

  19. Long-lasting airplane headache in a patient with chronic rhinosinusitis.

    Science.gov (United States)

    Pfund, Z; Trauninger, A; Szanyi, I; Illes, Z

    2010-04-01

    The authors report long-lasting airplane headache in a patient with non-allergic, chronic rhinosinusitis. Association of mucosal inflammation with compromised sinonasal ventilation and sinus barotrauma created a base for not only the pain but also for the prolongation of symptoms. Effective therapy with antihistamine and nasal decongestant supports the theory that sinonasal barotrauma plays a triggering role in the pathophysiology of airplane headache.

  20. Steroids vs immunotherapy for allergic rhinitis

    DEFF Research Database (Denmark)

    Aasbjerg, Kristian; Backer, Vibeke

    2014-01-01

    Treatment for seasonal allergic rhinitis induced by airborne allergens can be divided into two major groups: symptom-dampening drugs, such as antihistamines and corticosteroids, and disease-modifying drugs in the form of immunotherapy. It has been speculated that depot-injection corticosteroids...... given once or twice a year are a safe and patient-friendly alternative to the time-consuming immunotherapy. Our data indicate otherwise....

  1. Benzodiazepines for psychosis-induced aggression or agitation

    DEFF Research Database (Denmark)

    Zaman, Hadar; Sampson, Stephanie J; Beck, Alison Ls

    2017-01-01

    . OBJECTIVES: To examine whether benzodiazepines, alone or in combination with other pharmacological agents, is an effective treatment for psychosis-induced aggression or agitation when compared with placebo, other pharmacological agents (alone or in combination) or non-pharmacological approaches. SEARCH...... benzodiazepines alone or in combination with any antipsychotics, versus antipsychotics alone or in combination with any other antipsychotics, benzodiazepines or antihistamines, for people who were aggressive or agitated due to psychosis. DATA COLLECTION AND ANALYSIS: We reliably selected studies, quality assessed...

  2. Management of Allergic Rhinitis

    OpenAIRE

    Sausen, Verra O.; Marks, Katherine E.; Sausen, Kenneth P.; Self, Timothy H.

    2005-01-01

    Allergic rhinitis is the most common chronic childhood disease. Reduced quality of life is frequently caused by this IgE-mediated disease, including sleep disturbance with subsequent decreased school performance. Asthma and exercise-induced bronchospasm are commonly seen concurrently with allergic rhinitis, and poorly controlled allergic rhinitis negatively affects asthma outcomes. Nonsedating antihistamines or intranasal azelastine are effective agents to manage allergic rhinitis, often in c...

  3. Effect of histamine H1 receptor antagonists on TARC/CCL17 and MDC/CCL22 production from CD14+ cells induced by antigenic stimulation in vitro.

    Science.gov (United States)

    Shoji, Naruo; Asano, Kazuhito; Furuta, Atsuko; Hirano, Kojiro; Suzaki, Harumi

    2011-01-01

    Thymus- and activation-regulated chemokine (TARC) and macrophage-derived chemokine (MDC) are accepted to be important molecules in the development and maintenance of allergic diseases. Although several types of histamine H(1) receptor antagonist (antihistamine) have been developed and used for the treatment of allergic diseases, the influence of antihistamines on TARC and MDC production is not well understood. The present study was undertaken to examine the influence of antihistamines on TARC and MDC production from CD14+ cells after antigenic stimulation in vitro. CD14+ cells prepared from patients with pollinosis to Japanese cedar pollen were stimulated with specific allergen extracted from Japanese cedar pollen (Cry j 1) in the presence of azelastine (AZE), ketotifen (KET), fexofenadine (FEX) and oxatomide (OXA) for 6 days. TARC and MDC levels in culture supernatants were examined by ELISA. We also examined the influence of FEX on TARC and MDC mRNA expression, phosphorylation of mitogen-activated protein kinases (MAPKs) and transcription factor activation in CD14+ cells after Cry j 1 stimulation. FEX at 250 ng/ml, which is almost equal to therapeutic blood levels, caused a significant inhibition of TARC and MDC production.However, AZE, OXA and KET required higher concentrations than their therapeutic blood levels to suppress production of these factors. FEX at 250 ng/ml also suppressed NF-κB activation, phosphorylation of p38 MAPK and extracellular signal-regulated kinases 1 and 2 and expression of mRNA for TARC and MDC. These results suggest that antihistamines, especially FEX, suppress CC chemokine production from CD14+ cells through interference with antigen-mediated signaling and result in favorable modification of allergic disease states or conditions. Copyright © 2010 S. Karger AG, Basel.

  4. Serum Clusterin as a Prognostic Marker of Chronic Spontaneous Urticaria.

    Science.gov (United States)

    Kim, Ji-Hye; Lee, Hyung-Young; Ban, Ga-Young; Shin, Yoo-Seob; Park, Hae-Sim; Ye, Young-Min

    2016-05-01

    A substantial proportion of patients with chronic spontaneous urticaria (CSU) are refractory to antihistamines. However, identifying the subpopulation whose urticaria is not completely controlled by antihistamines remains difficult. The response of autologous serum skin test (ASST), a clinical test for the detection of basophil histamine-releasing activity upon autoantibodies or autoreactive stimulation, has been suggested as a potential predictor in the control of urticaria. We sought to identify proteins that were differentially expressed in the sera of patients with positive and negative ASST results and to investigate their association with urticaria control.Proteomics analysis was performed using sera from 3 CSU patients with positive ASST results compared with those showing negative ASST results. Seven upregulated and 5 downregulated proteins were identified by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry in the ASST-positive group compared with the ASST-negative group.Proteins that were differentially expressed according to the ASST results in CSU patients were classified into 6 groups: apolipoproteins, glycoproteins, modified albumin, haptoglobulin, plectin, and others. Among these, apolipoprotein J or clusterin was validated using an enzyme-linked immunosorbent assay. Clusterin levels in 69 ASST-positive patients were significantly higher than those in 69 ASST-negative patients and in 86 healthy controls (231.2 ± 44.0 vs 210.2 ± 36.1 vs 118.7 ± 71.9 μg/mL, P urticaria would be refractory to antihistamines. Serum clusterin can be a prognostic marker to determine the responsiveness to antihistamine treatment in patients with CSU.

  5. EFFICACY AND SAFETY FOR THE COMBINATION OF PHENYLEPHRINE, NAPHAZOLINE, CHLORPHENIRAMINE MALEATE, MENTHOL AND CAMPHOR IN PATIENTS OF ALLERGICCONJUNCTIVITIS AND INFLAMMATION OF A NON-INFECTIOUS ORIGIN

    OpenAIRE

    Dr. Mayuresh Dilip Kiran* & Lalit Jeevan Pawaskar

    2017-01-01

    Introduction Allergic conjunctivitis is an inflammatory response caused by an allergen when it interacts with IgE bound mast cells. Ocular redness, ocular itching and ocular discharge are the main symptoms of allergic conjunctivitis. Combination of Phenylephrine and Naphazoline which are vasoconstrictors used for the treatment of ocular redness, Chlorpheniramine maleate as an antihistaminic drugused for the treatment of ocular allergy and Menthol and Camphor used to give cooling effect to...

  6. Analysis of Non-infective Oral Mucosal Lesions with Possible ...

    African Journals Online (AJOL)

    There were 24 (0.2%) patients with possible immune mediated oral mucosal lesions in the study period. The mucosae of the lip (n=7, 29.2%), buccal ... The patients were treated mainly with prednisolone (n=8, 33.3%), anti-histamine (n=8, 33.3%) and warm saline mouth rinse (n=7, 29.2%). Satisfactory healing was observed ...

  7. Role of neurotensin in radiation-induced hypothermia in rats

    Energy Technology Data Exchange (ETDEWEB)

    Kandasamy, S.B.; Hunt, W.A.; Harris, A.H. (Armed Forces Radiobiology Research Institute, Bethesda, MD (USA))

    1991-05-01

    The role of neurotensin in radiation-induced hypothermia was examined. Intracerebroventricular (ICV) administration of neurotensin produced dose-dependent hypothermia. Histamine appears to mediate neurotensin-induced hypothermia because the mast cell stabilizer disodium cromoglycate and antihistamines blocked the hypothermic effects of neurotensin. An ICV pretreatment with neurotensin antibody attenuated neurotensin-induced hypothermia, but did not attenuate radiation-induced hypothermia, suggesting that radiation-induced hypothermia was not mediated by neurotensin.

  8. Urticaria multiforme er en variant af urticaria, som imiterer erythema multiforme

    DEFF Research Database (Denmark)

    Authried, Georg; Bracher, Linda; Bygum, Anette

    2013-01-01

    A 21-month-old boy developed urticaria multiforme during the course of a presumed pneumonia, which was treated with imacillin. At admission to hospital he was initially considered to have erythema multiforme, but the correct diagnosis was soon established as urticaria multiforme. He had a good re...... response to antihistamines. The diagnostic differences between urticaria multiforme and erythema multiforme are presented in this case report....

  9. A positive serum basophil histamine release assay is a marker for ciclosporin-responsiveness in patients with chronic spontaneous urticaria

    DEFF Research Database (Denmark)

    Iqbal, Kamran; Bhargava, Kapil; Skov, Per Stahl

    2012-01-01

    ABSTRACT: The electronic records of 398 patients with chronic spontaneous urticaria (CSU) who had had a serum basophil histamine release assay (BHRA) performed as a marker of functional autoantibodies were audited. The BHRA was positive in 105 patients (26.4%). Fifty eight were treated with ciclo...... with ciclosporin because they were H1 anti-histamine unresponsive. CSU patients with a positive BHRA were more likely to respond clinically (P...

  10. Comparative efficacy of levocetirizine, desloratidine and fexofenadine by histamine wheal suppression test

    Directory of Open Access Journals (Sweden)

    Dhanya N

    2008-01-01

    Full Text Available Background: Histamine is the major mediator of allergic reactions. Newer H1 antihistaminics like levocetirizine, fexofenadine, and desloratadine are used in the treatment of seasonal and perennial allergic rhinitis and urticaria. The ability to block the cutaneous response to intradermal histamine is used to evaluate the potential of antihistamines. Aims: To compare the potency, onset, and duration of action of the commonly used antihistamines-levocetirizine, fexofenadine, and desloratadine Methods: Thirty volunteers were given three single doses of levocetirizine, fexofenadine and desloratadine at weekly intervals. A pretest was performed by using the intradermal histamine prick test. After administration of the drugs, the intradermal test was repeated at ½, 1, 2, 3, 6 and 24 h, and the sizes of the wheal were measured. The mean values were taken and were compared by using Levene′s t-test. Results: At 30 min, fexofenadine showed a statistically significant suppression of wheal size compared to levocetirizine and desloratadine. Two and three hours after administration, levocetirizine and fexofenadine showed statistically significant inhibition of wheal size while only levocetirizine had this effect after six hours when compared to desloratadine. Desloratadine showed greater inhibition of wheal size at the end of 24 h when compared to levocetirizine and fexofenadine but this was not statistically significant. Conclusions: Fexofenadine had the earliest onset of action while levocetirizine showed maximum inhibition of wheal response after three and six hours.

  11. Cytokine production by PBMC and serum from allergic and non-allergic subjects following in vitro histamine stimulation to test fexofenadine and osthole anti-allergic properties.

    Science.gov (United States)

    Kordulewska, Natalia Karolina; Kostyra, Elżbieta; Cieślińska, Anna; Fiedorowicz, Ewa; Jarmołowska, Beata

    2016-11-15

    FXF is a third-generation antihistamine drug and osthole is assumed a natural antihistamine alternative. This paper compares peripheral blood mononuclear cell (PBMC) incubation with FXF and osthole, by studying FXF, osthole and histamine cytokine secretion in PBMC in vitro cultures. Mabtech kits determined the interleukins IL-1β, IL-4, IL-10, IL-13 and TNF-α. The influence of the above active substances on cytokine secretion in PBMC's and serum was assessed: cytokines were IL-1β, IL-4, IL-10, IL-13 and TNF-α; and cytokine levels secreted by untreated PBMCs in pure culture medium formed the absolute control (ctrl). We determined that osthole affects PBMC cytokine secretion to almost precisely the same extent as FXF (IL-1β, IL-4, IL-10 and TNF). In addition osthole had greater IL-13 blocking ability than FXF. Moreover, we observed significantly decreased IL-4 level in histamine/osthole theatment compared to histamine alone. Meanwhile, FXF not significantly decrease the level of IL-4 increased by histamine. This data indicates osthole's strong role in allergic inflamation. All results confirm our hypothesis that osthole is a natural histamine antagonist and therefore can be beneficially used in antihistamine treatment of conditions such as allergies. Copyright © 2016 Elsevier B.V. All rights reserved.

  12. Omalizumab for treating chronic spontaneous urticaria: an expert review on efficacy and safety.

    Science.gov (United States)

    Giménez-Arnau, Ana M

    2017-03-01

    Chronic spontaneous urticaria (CSU) is characterized by the recurrence of itchy hives and/or angioedema for greater than six weeks, with no known external trigger. Omalizumab, a humanized, recombinant, monoclonal anti-IgE antibody, is the only approved add-on therapy for H1-antihistamine refractory CSU patients. Areas covered: The objective of this article is to discuss the mechanism of action, pharmacokinetics and pharmacodynamics of omalizumab for the treatment of CSU. The review also summarizes efficacy and safety data from proof-of-concept, phase II (X-CUISITE, MYSTIQUE), and pivotal phase III omalizumab studies (ASTERIA I, ASTERIA II, and GLACIAL). Expert opinion: Omalizumab is a clinically effective and safe biological therapy for treating H1-antihistamine refractory CSU patients. It significantly reduces CSU symptoms (hives, itch and angioedema), and improves patient health-related quality of life. While omalizumab is already integral to the treatment of antihistamine refractory CSU, widespread use will depend on legal and economic factors, as well as improvements in the early and accurate diagnosis of CSU patients who would benefit from treatment.

  13. Role of biologics in intractable urticaria

    Directory of Open Access Journals (Sweden)

    Cooke A

    2015-04-01

    Full Text Available Andrew Cooke,1 Adeeb Bulkhi,1,2 Thomas B Casale1 1Department of Internal Medicine, Division of Allergy and Immunology, University of South Florida, Tampa, FL, USA; 2Department of Internal Medicine, College of Medicine, Umm Al-Qura University, Makkah, Saudi Arabia Abstract: Chronic urticaria (CU is a common condition faced by many clinicians. CU has been estimated to affect approximately 0.5%–1% of the population, with nearly 20% of sufferers remaining symptomatic 20 years after onset. Antihistamines are the first-line therapy for CU. Unfortunately, nearly half of these patients will fail this first-line therapy and require other medication, including immune response modifiers or biologics. Recent advances in our understanding of urticarial disorders have led to more targeted therapeutic options for CU and other urticarial diseases. The specific biologic agents most investigated for antihistamine-refractory CU are omalizumab, rituximab, and intravenous immunoglobulin (IVIG. Of these, the anti-IgE monoclonal antibody omalizumab is the best studied, and has recently been approved for the management of CU. Other agents, such as interleukin-1 inhibitors, have proved beneficial for Schnitzler syndrome and cryopyrin-associated periodic syndromes (CAPS, diseases associated with urticaria. This review summarizes the relevant data regarding the efficacy of biologics in antihistamine-refractory CU. Keywords: chronic urticaria, omalizumab, intravenous immunoglobulin, anakinra, canakinumab

  14. Position statement for the use of omalizumab in the management of chronic spontaneous urticaria in Indian patients

    Directory of Open Access Journals (Sweden)

    Kiran Godse

    2016-01-01

    Full Text Available Chronic spontaneous urticaria (CSU affects 1% of the world population and also their quality of life, and 50% of these patients are refractory to H1-antihistamines. Omalizumab is a humanized monoclonal anti-IgE antibody that binds with free IgE antibodies and reduces the circulating levels of free IgE. This reduction in free IgE prevents mast-cell degranulation. The EAACI/GA2LEN/EDF/WAO guidelines recommend omalizumab as the third-line of therapy as an add-on to antihistamines. The recommended dose of omalizumab is 300 mg, 4 weekly in the management of CSU refractory to standard of care with H1-antihistamines in adults and adolescents ≥12 years of age. In some patients, a dose of 150 mg may be acceptable. Omalizumab has a good safety profile. However, due to the biologic nature of the drug, all patients administered omalizumab must be observed for 2 h after administration for anaphylactoid reactions. There have been no studies on the effect of impaired renal or hepatic function on the pharmacokinetics of omalizumab. While no particular dose adjustment is recommended, omalizumab should be administered with caution in these patients.

  15. The effectiveness of levocetirizine in comparison with loratadine in treatment of allergic rhinitis--a meta-analysis.

    Science.gov (United States)

    Mösges, Ralph; König, Volker; Köberlein, Juliane

    2011-12-01

    Oral antihistamines are considered the gold standard therapy for allergic rhinitis to date. The goal of this investigation is to make an indirect comparison between loratadine, an oral antihistamine available over-the-counter (OTC) in the USA, and the more modern antihistamine levocetirizine. Only double-blind, placebo-controlled (DBPC) studies involving monotherapy with the active substances levocetirizine and loratadine were included in the meta-analysis. The medical databases EMBASE and Medline were searched systematically for all relevant studies completed by the end of 2009. Only DBPC studies conducted in normal environmental settings were included. Furthermore, the Jadad scale was used to guarantee the quality of the studies involved. The "standardized mean difference" (SMD) method was applied for calculating the study-specific effects to neutralize the variability between studies. The results of a total of seven published DBPC studies met all criteria for inclusion in meta-analysis. The meta-analysis showed that levocetirizine was significantly more effective than loratadine in improving the total symptom score (TSS) (p allergic symptoms when compared to treatment with loratadine.

  16. Levocetirizine as treatment for symptoms of seasonal allergic rhinitis.

    Science.gov (United States)

    Jorissen, M; Bertrand, B; Stiels, B; Vandenbulcke, K

    2006-01-01

    The aim of this study was to assess the effectiveness and safety of levocetirizine in the treatment of the symptoms of seasonal allergic rhinitis (SAR) in patients consulting their primary care doctor. Open-label uncontrolled and non-randomised multi-centre study including patients presenting symptoms of SAR and treated with levocetirizine tablets, 5 mg OD, for 4 weeks. patients with nasal symptoms who were not on treatment or not responsive to treatment, or affected by excessive adverse events due to the antihistamines used previously. There were two visits (initial and after four weeks). Primary end point: efficacy as measured by T4SS (combined score of sneezing, rhinorrhoea, nasal and ocular pruritus, ranging from 0 to 12 recorded by the patient); change in Clinical Global Impression (CGI-c) as rated by the general practitioner, subjective satisfaction with and preference for levocetirizine. Secondary end points: treatment-related adverse events. 1290 patients were evaluated. Before the start of the study, 61.2% did not use any medication, 36.4% took anti-histamines which were not effective, and 27.0% of those previously treated patients experienced excessive adverse events. Statistically significant decreases (p comparison with previous treatments after levocetirizine was used. Levocetirizine showed an improvement in symptom control for SAR and was preferred by patients compared to the antihistamines they had taken previously. Levocetirizine was well tolerated.

  17. The Effect of Schinus terebinthifolius Raddi (Anacardiaceae) Bark Extract on Histamine-Induced Paw Edema and Ileum Smooth Muscle Contraction

    Science.gov (United States)

    Nunes-Neto, Paulo Alexandre; da Silva Júnior, Edilson Dantas; Leopoldina da Silva, Jamilka; Rodrigo da Silva Oliveira, Alisson; Pupo, André Sampaio; Araújo, Alice Valença

    2017-01-01

    Schinus terebinthifolius Raddi (Anacardiaceae), popularly known as red aroeira, is used in traditional medicine to treat inflammatory, gastric, and respiratory disorders. The aim of this study was to evaluate the antihistaminic activity of S. terebinthifolius (St) bark extract by using in vivo and in vitro experimental models. The effects of St were investigated on contractions induced by histamine, carbachol, and potassium chloride in isolated guinea pig ileum. St was also studied in response to hind paw edema induced by histamine in rats. Experiments revealed that although St (250, 500, and 1,000 µg/mL) reduced the histamine-induced contractions by 9.1 ± 1.8, 50.2 ± 2.0, and 68.9 ± 2.0%, respectively, it did not inhibit contractions induced by carbachol or KCl. The association of St (250 and 500 µg/mL) with hydroxyzine, an H1-antihistamine (0.125 and 0.250 µM), increased the inhibitory effect to 67.0 ± 3.2 and 85.1 ± 2.1%, respectively. Moreover, St (100, 200, and 400 mg/kg) decreased paw edema from its peak by 33.9, 48.4, and 54.8%, respectively, whereas hydroxyzine (70 mg/kg) inhibited the peak edema by 56.5%. Altogether, the results suggest that the bark extract of S. terebinthifolius has an antihistaminic effect (H1). PMID:28928787

  18. The Effect of Schinus terebinthifolius Raddi (Anacardiaceae Bark Extract on Histamine-Induced Paw Edema and Ileum Smooth Muscle Contraction

    Directory of Open Access Journals (Sweden)

    Paulo Alexandre Nunes-Neto

    2017-01-01

    Full Text Available Schinus terebinthifolius Raddi (Anacardiaceae, popularly known as red aroeira, is used in traditional medicine to treat inflammatory, gastric, and respiratory disorders. The aim of this study was to evaluate the antihistaminic activity of S. terebinthifolius (St bark extract by using in vivo and in vitro experimental models. The effects of St were investigated on contractions induced by histamine, carbachol, and potassium chloride in isolated guinea pig ileum. St was also studied in response to hind paw edema induced by histamine in rats. Experiments revealed that although St (250, 500, and 1,000 µg/mL reduced the histamine-induced contractions by 9.1±1.8, 50.2±2.0, and 68.9±2.0%, respectively, it did not inhibit contractions induced by carbachol or KCl. The association of St (250 and 500 µg/mL with hydroxyzine, an H1-antihistamine (0.125 and 0.250 µM, increased the inhibitory effect to 67.0±3.2 and 85.1±2.1%, respectively. Moreover, St (100, 200, and 400 mg/kg decreased paw edema from its peak by 33.9, 48.4, and 54.8%, respectively, whereas hydroxyzine (70 mg/kg inhibited the peak edema by 56.5%. Altogether, the results suggest that the bark extract of S. terebinthifolius has an antihistaminic effect (H1.

  19. The Effect ofSchinus terebinthifoliusRaddi (Anacardiaceae) Bark Extract on Histamine-Induced Paw Edema and Ileum Smooth Muscle Contraction.

    Science.gov (United States)

    Nunes-Neto, Paulo Alexandre; Peixoto-Sobrinho, Tadeu José da Silva; da Silva Júnior, Edilson Dantas; Leopoldina da Silva, Jamilka; Rodrigo da Silva Oliveira, Alisson; Pupo, André Sampaio; Araújo, Alice Valença; da Costa-Silva, João Henrique; Wanderley, Almir Gonçalves

    2017-01-01

    Schinus terebinthifolius Raddi (Anacardiaceae), popularly known as red aroeira, is used in traditional medicine to treat inflammatory, gastric, and respiratory disorders. The aim of this study was to evaluate the antihistaminic activity of S. terebinthifolius (St) bark extract by using in vivo and in vitro experimental models. The effects of St were investigated on contractions induced by histamine, carbachol, and potassium chloride in isolated guinea pig ileum. St was also studied in response to hind paw edema induced by histamine in rats. Experiments revealed that although St (250, 500, and 1,000  µ g/mL) reduced the histamine-induced contractions by 9.1 ± 1.8, 50.2 ± 2.0, and 68.9 ± 2.0%, respectively, it did not inhibit contractions induced by carbachol or KCl. The association of St (250 and 500  µ g/mL) with hydroxyzine, an H 1 -antihistamine (0.125 and 0.250  µ M), increased the inhibitory effect to 67.0 ± 3.2 and 85.1 ± 2.1%, respectively. Moreover, St (100, 200, and 400 mg/kg) decreased paw edema from its peak by 33.9, 48.4, and 54.8%, respectively, whereas hydroxyzine (70 mg/kg) inhibited the peak edema by 56.5%. Altogether, the results suggest that the bark extract of S. terebinthifolius has an antihistaminic effect (H 1 ).

  20. Effects of fexofenadine and hydroxyzine on brake reaction time during car-driving with cellular phone use.

    Science.gov (United States)

    Tashiro, Manabu; Horikawa, Etsuo; Mochizuki, Hideki; Sakurada, Yumiko; Kato, Motohisa; Inokuchi, Takatoshi; Ridout, Fran; Hindmarch, Ian; Yanai, Kazuhiko

    2005-10-01

    Antihistamines are a mainstay treatment for allergic rhinitis; however, many older agents cause adverse events, including sedation and central nervous system (CNS) impairment. Research has shown sedating effects of antihistamines on driving; currently, no known study has examined whether cellular phone usage while driving further compounds impairment in individuals administered antihistamines. The aim of this study was to examine this endpoint. In a randomized, double-blind, placebo-controlled, three-way crossover study, healthy volunteers received fexofenadine HCl 120 mg, hydroxyzine HCl 30 mg and placebo. Brake reaction time (BRT) was used to examine driving performance across four conditions: driving only; driving while completing simple calculations; complex calculations; and conversing on a cellular phone. Subjective sedation assessments were also conducted. Brake reaction time with and without cellular phone usage in fexofenadine-treated subjects did not differ significantly from placebo in any condition. In contrast, hydroxyzine-treated subjects were significantly more sedated and had slower BRTs, suggesting slower hazard recognition and brake application, compared with the fexofenadine and placebo groups in all conditions. Importantly, cellular phone operation was an additive factor, increasing BRTs in hydroxyzine-treated volunteers. Fexofenadine did not impair CNS function in subjects involved in a divided attention task of driving and cellular phone operation. Copyright (c) 2005 John Wiley & Sons, Ltd.

  1. Double-blind placebo-controlled study of bepotastine besilate in pediatric patients with perennial allergic rhinitis.

    Science.gov (United States)

    Okubo, Kimihiro; Ichimura, Masahiko; Koyama, Tomoya; Susuta, Yutaka; Izaki, Hitoshi

    2015-01-01

    Although second-generation antihistamines, such as bepotastine besilate, are recommended as a first-line treatment option for adult perennial allergic rhinitis (PAR), few non-sedating second-generation antihistamines are safe for children. A double-blind, placebo-controlled, comparative study of 473 pediatric PAR patients (7 - 15 years old) to determine the superiority and safety of bepotastine besilate (10 mg twice daily) relative to placebo for improved total and individual nasal symptom scores compared with baseline. Subjects were randomized to placebo (n = 233) or bepotastine besilate (n = 240, 10 mg orally twice daily for 2 weeks). Interference of daily life by PAR was assessed by measuring change in individual nasal symptom scores from baseline. Bepotastine besilate was superior to placebo in terms of total nasal symptom scores, with improved overall nasal symptoms of PAR compared with baseline values. Subgroup analyses demonstrated bepotastine besilate was effective irrespective of age, sex or body weight. No clinically significant adverse drug reactions often observed with first-generation antihistamines were reported and no difference in adverse events between groups was observed. Bepotastine besilate is effective and safe for pediatric PAR patients aged 7 - 15 years, and has a significant clinical impact on PAR. ClinicalTrials.gov identifier: NCT01861522 ( https://clinicaltrials.gov/ct2/show/NCT01861522 ).

  2. Impact of fexofenadine, osthole and histamine on peripheral blood mononuclear cell proliferation and cytokine secretion.

    Science.gov (United States)

    Karolina Kordulewska, Natalia; Kostyra, Elżbieta; Matysiewicz, Michał; Cieślińska, Anna; Jarmołowska, Beata

    2015-08-15

    This paper compares results of peripheral blood mononuclear cell (PBMC) incubation with fexofenadine (FXF) and osthole. FXF is a third-generation antihistamine drug and osthole is assumed a natural antihistamine alternative. To our best knowledge, this is the first comparative study on FXF, osthole and histamine cytokine secretion and cytotoxicity in PBMC in vitro cultures using cell proliferation ELISA BrdU. The cultures were treated 12, 42, 48 and 72h with FXF and osthole at 150, 300 and 450ng/ml concentrations and histamine at 50, 100 and 200ng/ml. Our study results confirm that FXF, osthole and histamine exert no cytotoxic effect on PBMCs and that IL-6, IL-10 and TNF-α cytokine secretion following osthole cell stimulation was similar to that by FXF stimulation.This confirms our hypothesis that osthole is a natural histamine antagonist, and can therefore be beneficially applied in antihistamine treatment. Copyright © 2015 Elsevier B.V. All rights reserved.

  3. Weekly injection of histaglobulin produces long-term remission in chronic urticaria: A prospective clinical study

    Science.gov (United States)

    Rajesh, Gurumoorthy; Keerthi, Subramaniam; Karthikeyan, Kaliaperumal; Venkatesan, Murugan

    2016-01-01

    Objective: Treatment of chronic urticaria (CU) can be difficult in many patients. Achieving long-term remission and reducing the requirement of antihistamines are vital in CU. The objective of this study was to assess the effectiveness of injection histaglobulin, a complex of histamine and human immunoglobulin, in producing relief in patients with CU. Materials and Methods: Fifty-one patients with CU were enrolled into this prospective clinical study. Patients were administered 1 ml of injection histaglobulin subcutaneous for 8 consecutive weeks. They were also prescribed tablet levocetirizine 5 mg to be taken when required (but not more than the permitted dosage). Efficacy was assessed using urticaria activity score (UAS) which has a maximum score of 33/day, during each weekly visit. Final assessment was done after 24 weeks. Results: Twenty-nine patients had completed the entire 8-week drug regimen. Mean basal UAS was 18.9 ± 6.3 and it reduced to 80.4% by 8 weeks. The angioedema sub-score reduced by 89.8%. Anti-histamine pill burden also reduced significantly. By 24 weeks of starting the therapy, 23 patients (45%) had attained complete remission. No adverse effects to the drug were observed. Conclusions: Histaglobulin was found to be effective in producing long-term remission and it reduced the antihistamine requirement as well. Thus, it can serve as an effective alternative to existing treatment modalities. PMID:27298500

  4. Omalizumab for the treatment of chronic urticaria.

    Science.gov (United States)

    Zuberbier, Torsten; Maurer, Marcus

    2015-02-01

    Urticaria is a common and often debilitating dermatological condition defined by the sudden appearance of wheals, angioedema or both. It is further classified into specific subtypes based on duration and specific triggers. Awareness and understanding of urticaria are important to ensure a correct initial diagnosis and initiate appropriate guideline-based treatment outlining a stepwise approach. However, in chronic urticaria, approximately 50% of patients are refractory to the first step, the use of licensed doses of second-generation H1-antihistamines. If the second step, an increase in the dose of the second-generation H1-antihistamines, is also not successful, in the third step omalizumab (Xolair™, Novartis Pharma AG(©)/Genentech, Inc.(©)), an anti-IgE therapy, is recommended as an add-on. Of all alternative treatments mentioned in the guidelines, omalizumab is currently the only licensed treatment for H1-antihistamine-refractory chronic spontaneous urticaria, has a favorable risk/benefit ratio and was well tolerated in clinical studies.

  5. [Urticaria: diagnosis and treatment].

    Science.gov (United States)

    Soria, A; Francès, C

    2014-09-01

    Urticaria is a common inflammatory skin disease. It is clinically defined as the occurrence of transient papular skin and/or mucosal lesions or subcutaneous lesions called angioedema. Chronic urticaria is defined as a clinical course over more than 6weeks. Different clinical forms of urticaria can coexist in the same patient. Urticaria results of mast cell activation. The diagnosis of urticaria is based on clinical examination. An allergic etiology for acute urticaria, although rare, is always to find and remove. Chronic urticaria is not allergic. Diagnosis is based on questioning and a careful clinical examination to rule out differential diagnoses. Few diagnostic tests are necessary for diagnosis and management, and are especially useful in case of doubtful diagnosis. The treatment of urticaria is symptomatic and based on anti-H1 second generation antihistamines as first-line therapy. In some chronic urticarial, antihistamines up dosing may be necessary. In the majority of patients, this treatment is sufficient to control chronic urticaria. In case of antihistamines failure, other treatment particularly immunomodulatory treatments can be offered in specialized departments. Copyright © 2014 Société nationale française de médecine interne (SNFMI). Published by Elsevier SAS. All rights reserved.

  6. Updates in the treatment of ocular allergies

    Directory of Open Access Journals (Sweden)

    Osmo Kari

    2010-11-01

    Full Text Available Osmo Kari1, K Matti Saari21Department of Allergology, Skin and Allergy Hospital, Helsinki University Central Hospital, Helsinki, Finland; 2Department of Ophthalmology, University of Turku, Turku, FinlandAbstract: Allergic diseases have greatly increased in industrialized countries. About 30% of people suffer from allergic symptoms and 40%–80% of them have symptoms in the eyes. Atopic conjunctivitis can be divided into seasonal allergic conjunctivitis (SAC and perennial allergic conjunctivitis (PAC. The treatment of SAC is simple; antihistamines, anti-inflammatory agents, or chromoglycate. In severe cases of SAC, subcutaneous or sublingual immunotherapy is helpful. PAC needs longer therapy, often year round, with mast cell stabilizers, antihistamines, and sometimes local steroids. Atopic keratoconjunctivitis is a more severe disease showing chronic blepharitis often connected with severe keratitis. It needs, in many cases, continuous treatment of the lid eczema and keratoconjunctivitis. Blepharitis is treated with tacrolimus or pimecrolimus ointment. Conjunctivitis additionally needs corticosteroids and, if needed, cyclosporine A (CsA drops are administered for longer periods. Basic conjunctival treatment is with mast cell-stabilizing agents and in addition, antihistamines are administered. Vernal keratoconjunctivitis is another chronic and serious allergic disease that mainly affects children and young people. It is a long-lasting disease which commonly subsides in puberty. It demands intensive therapy often for many years to avoid serious complicating corneal ulcers. Treatment is mast cell-stabilizing drops and additionally antihistamines. In relapses, corticosteroids are needed. When the use of corticosteroids is continuous, CsA drops should be used, and in relapses, corticosteroids should be used additionally. Nonallergic eosinophilic conjunctivitis (NAEC is a less known, but rather common, ocular disease. It affects mostly middle-aged and

  7. A four arm, double blind, randomized and placebo controlled study of pregabalin in the management of post-burn pruritus.

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    Ahuja, Rajeev B; Gupta, Gaurav K

    2013-02-01

    Post-burn itch is a distressing symptom in burns rehabilitation and its treatment often proves frustrating for the patient and the multidisciplinary burns team. Traditionally, the mainstay of antipruritic therapy for decades has been antihistamines and massage with emollients. With a better understanding of the neurophysiology of itch emerged a new dimension in the treatment of post-burn pruritus. Gabapentin, a centrally modulating anti-epileptic agent and α2δ ligand, proved in clinical trials to be immensely better in the treatment of post-burn pruritus. Pregabalin is a newer structural analog of gabapentin. It has a much better anxiolytic effect and pharmacokinetic profile as compared to gabapentin. The current study was initiated to specifically study the role of pregabalin in relieving post-burn itch as this has never been investigated before. This double blind, randomized and placebo controlled study had four arms and was carried out on 80 adult patients (20 each). The four arms were: pregabalin, cetirizine with pheniramine maleate, combination of pregabalin, cetirizine and pheniramine maleate, and placebo (vit. B comp.). Massage with coconut oil was integral to all groups. Drug dosage was determined by initial VAS (visual analog scale) scores. All groups matched in demographic data and initial VAS scores. VAS scores were evaluated over next 28 days (days 3, 7, 14, 21 and 28). In patients with mild itch (VAS scores 2-5) or moderate itch (VAS scores 6-8) near complete remission of itch was seen in combination group and pregabalin group where the response was comparable and close to 95%. This was significantly better response than antihistaminic combination or massage alone. However, massage alone was sufficient in decreasing mean scores in mild itch, in a large percentage of patients. Amongst the patients with severe itch (VAS scores 9-10), 3/6 and 6/7 patients dropped out of trial in the antihistaminic and placebo groups, respectively. Combination therapy

  8. Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis

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    Santa J Ono

    2011-02-01

    Full Text Available Santa J Ono1, Keith Lane21Emory University School of Medicine and Emory Eye Center, Dobbs Ocular Immunology Laboratories, Atlanta, GA, USA; 2Ora Inc., 300 Brickstone Square, Andover, MA, USABackground: Antihistamines constitute the first line of therapy for allergic conjunctivitis, and are safe and effective in relieving the signs and symptoms of ocular allergy. Despite this, they are less effective than some other drugs in relieving delayed symptoms of allergic conjunctivitis. Recent evidence suggests that changes in the conjunctival epithelium may underlie aspects of delayed reactions. In this study we compared two antihistamines, olopatadine and alcaftadine, for their ability to modify epithelial cell changes associated with allergic conjunctivitis at time points selected to reflect late-phase reactions.Methods: Studies employed a modified conjunctival allergen challenge model. Sensitized mice were challenged with topical allergen with or without drug treatments. Treatment groups were assayed for acute-phase (15 minutes and delayed-phase (24 hours responses. Groups were scored for allergy symptoms (redness, itch, tearing, and edema and for conjunctival mast cell numbers. Delayed-phase groups were also examined for eosinophil numbers and for tight junctional protein expression.Results: Olopatadine-treated and alcaftadine-treated animals had similar efficacy profiles and mast cell numbers, suggesting both were effective at ameliorating symptoms of the acute phase. In contrast, alcaftadine-treated animals had significantly lower conjunctival eosinophil infiltration than either controls or olopatadine-treated animals. Allergen challenge caused a significant decrease in expression of the junctional protein, ZO-1, and this decrease was prevented by alcaftadine but not by olopatadine.Conclusion: Alcaftadine displays therapeutic properties beyond its antihistamine action. These include an ability to reduce conjunctival eosinophil recruitment, and a

  9. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria

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    Sadaba B

    2013-05-01

    Full Text Available Belen Sadaba, Jose Ramon Azanza, Almundena Gomez-Guiu, Raquel RodilClinical Pharmacology Service, Clinica Universidad de Navarra, Navarra, SpainAbstract: Bilastine is a second generation antihistamine indicated for the treatment of seasonal or perennial allergic rhinoconjunctivitis and chronic urticaria with a daily dose of 20 mg, in adults and children over 12 years of age. The efficacy of bilastine has been shown to be similar to that of the comparator drugs for the control of the nasal and nonnasal symptoms of allergic rhinoconjunctivitis, while also showing a subjective improvement in the quality of life and in overall clinical impression. For chronic urticaria the symptoms (itching and the development of papules lessens from the second day of treatment onwards, in a similar way to other antihistamines used as comparators. Bilastine should not be administered at meal times to avoid interference with the absorption process. It is not distributed to the central nervous system, is scarcely metabolized, and elimination is through the kidneys and feces, with a 14-hour elimination half-life. It has no effect on cytochrome P450. During clinical development, bilastine was shown to be a drug that is adequately tolerated, with a similar effect to placebo with regard to drowsiness and changes in heart rate. In relation to its use, headaches were the most frequent adverse effect to be reported. No cardiotoxic effects have been observed, and the therapeutic dose does not alter the state of alertness.Keywords: bilastine, allergic rhinoconjunctivitis, chronic urticaria, second generation antihistamine, drowsiness, CYP450

  10. Angioedema in the omalizumab chronic idiopathic/spontaneous urticaria pivotal studies.

    Science.gov (United States)

    Zazzali, James L; Kaplan, Allen; Maurer, Marcus; Raimundo, Karina; Trzaskoma, Benjamin; Solari, Paul G; Antonova, Evgeniya; Mendelson, Meryl; Rosén, Karin E

    2016-10-01

    Angioedema, present in some patients with chronic idiopathic/spontaneous urticaria (CIU/CSU), may have a negative effect on patient quality of life. To describe patient-reported angioedema and its management in the pivotal omalizumab studies (ASTERIA I, ASTERIA II, GLACIAL). Enrolled patients with CIU/CSU remained symptomatic despite treatment with histamine 1 (H 1 )-antihistamines at licensed doses (ASTERIA I, ASTERIA II) or H 1 -antihistamines at up to 4 times the approved dose plus H 2 -antihistamines and/or a leukotriene receptor antagonist (GLACIAL). All studies administered omalizumab (75, 150, or 300 mg in ASTERIA I and ASTERIA II; 300 mg in GLACIAL) or placebo subcutaneously every 4 weeks for at least 12 weeks. Urticaria Patient Daily Diary entries were completed by patients and summarized. At baseline, angioedema prevalence was higher in GLACIAL (53.1%) than in ASTERIA I (47.5%) or ASTERIA II (40.7%). The mean proportion of angioedema-free days during weeks 4 to 12 was greater for patients treated with 300 mg of omalizumab than placebo in ASTERIA I (96.1% vs 88.2%, P angioedema was managed by low-intensity interventions (doing nothing or taking medication). Treatment with 300 mg of omalizumab was efficacious in reducing patient-reported angioedema. Low-intensity interventions were generally used to manage angioedema episodes. clinicaltrials.gov Identifiers: NCT01287117 (ASTERIA I), NCT01292473 (ASTERIA II), and NCT01264939 (GLACIAL). Copyright © 2016 The Authors. Published by Elsevier Inc. All rights reserved.

  11. Profile of omalizumab in the treatment of chronic spontaneous urticaria

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    Labrador-Horrillo M

    2015-08-01

    Full Text Available Moises Labrador-Horrillo,1 Marta Ferrer2 1Allergy Section, Internal Medicine Department, Vall d’Hebron Hospital, Universitat Autònoma de Barcelona, Barcelona, 2Department of Allergy and Clinical Immunology, Clínica Universidad de Navarra, IDISNA, Instituto de Investigación de Navarra, Pamplona, Spain Abstract: Chronic spontaneous urticaria (CSU is a disease with significant morbidity and relative prevalence that has important effects on the quality of life (QoL of those who suffer from it. Omalizumab is a recombinant humanized anti-immunoglobulin E (IgE antibody that binds to the Cε3 domain of the IgE heavy chain and prevents it from binding to its high-affinity receptor FcεRI. It has been largely studied in the field of asthma and is currently approved for the treatment of both adult and pediatric (children; >6-year-old patients. In addition, in recent, well-controlled clinical trials in patients with CSU resistant to antihistamines, add-on therapy with subcutaneous omalizumab significantly reduced the severity of itching, and the number and size of hives, and increased patients’ health-related QoL and the proportion of days free from angioedema compared with placebo, with an excellent tolerance. Thus, omalizumab is an effective and well-tolerated add-on therapy for patients with CSU who are symptomatic despite background therapy with H1 antihistamines. In this review, we cover the following points: epidemiology, pathogenesis, assessment of activity, impact on QoL, and treatment of CSU, and finally, we focus on omalizumab in the treatment of CSU including the pharmacokinetic properties and mechanism of action, and use in pregnant women, nursing infants, and children. Keywords: omalizumab, chronic spontaneous urticaria, antihistamines, subcutaneous administration, add-on therapy

  12. The Turkish Guideline for the Diagnosis and Management of Urticaria-2016

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    Emek Kocatürk Göncü

    2016-09-01

    Full Text Available Background and Design: Albeit an easily recognized disease, urticaria features many diverse approaches which rationalize the need for an algorithm for the diagnosis, classification, etiopathogenesis, diagnostic evaluation and therapeutic approach. Therefore, authors from Dermatoallergy Working Group of the Turkish Society of Dermatology and the Turkish Dermatoimmunology and Allergy Association aimed to create an urticaria guideline for the diagnosis, treatment and followup of urticaria. Materials and Methods: Each section of the guideline has been written by a different author. The prepared sections were evaluated in part by e-mail correspondence and have taken its final form after revision in the last meeting held by the participation of all authors. Results: The guideline includes the description, classification, pathophysiology as well as diagnosis and treatment of urticaria. Urticaria is classified into two main types: acute urticaria and chronic urticaria while chronic urticaria is further subdivided into spontaneous urticaria and inducible urticaria. The first step of treatment includes standard doses of H1-blockers. In patients who do not respond to the first step, antihistamine dose is increased up to four times; if unsuccessful, another second-generation antihistamine is given in the same dose. In antihistamine-resistant cases, introduction of omalizumab is required. Omalizumab dose may be increased in patients failing to respond to the standard dose. In patients unresponsive to omalizumab, cyclosporine-A may be given. Routine diagnostic tests are not recommended in acute urticaria. In chronic urticaria, erythrocyte sedimentation rate, differential blood count and C-reactive protein testing are the only investigations that are needed routinely. Conclusion: Chronic urticaria is a disease that can be challenging for the physician in terms of treatment and follow-up. Depending on evidence-based data (and individual experiences, this

  13. Treatment of congestion in upper respiratory diseases

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    Eli O Meltzer

    2010-02-01

    Full Text Available Eli O Meltzer1, Fernan Caballero2, Leonard M Fromer3, John H Krouse4, Glenis Scadding51Allergy and Asthma Medical Group and Research Center, San Diego, CA and Department of Pediatrics, University of California, San Diego, USA; 2Allergy and Clinical Immunology Service, Centro Medico-Docente La Trinidad, Caracas, Venezuela; 3David Geffen School of Medicine, University of California, Los Angeles, USA; 4Wayne State University School of Medicine, Detroit, Michigan, USA; 5Department of Allergy and Rhinology, Royal National TNE Hospital, London, UKAbstract: Congestion, as a symptom of upper respiratory tract diseases including seasonal and perennial allergic rhinitis, acute and chronic rhinosinusitis, and nasal polyposis, is principally caused by mucosal inflammation. Though effective pharmacotherapy options exist, no agent is universally efficacious; therapeutic decisions must account for individual patient preferences. Oral H1-antihistamines, though effective for the common symptoms of allergic rhinitis, have modest decongestant action, as do leukotriene receptor antagonists. Intranasal antihistamines appear to improve congestion better than oral forms. Topical decongestants reduce congestion associated with allergic rhinitis, but local adverse effects make them unsuitable for long-term use. Oral decongestants show some efficacy against congestion in allergic rhinitis and the common cold, and can be combined with oral antihistamines. Intranasal corticosteroids have broad anti-inflammatory activities, are the most potent long-term pharmacologic treatment of congestion associated with allergic rhinitis, and show some congestion relief in rhinosinusitis and nasal polyposis. Immunotherapy and surgery may be used in some cases refractory to pharmacotherapy. Steps in congestion management include (1 diagnosis of the cause(s, (2 patient education and monitoring, (3 avoidance of environmental triggers where possible, (4 pharmacotherapy, and (5 immunotherapy

  14. An open-label prospective clinical study to assess the efficacy of increasing levocetirizine dose up to four times in chronic spontaneous urticaria not controlled with standard dose.

    Science.gov (United States)

    Sharma, Vinod Kumar; Gupta, Vishal; Pathak, Mona; Ramam, M

    2017-09-01

    The EAACI/GA 2 LEN/EDF/WAO recommendation of increasing antihistamines' dose up to four times in urticaria not adequately controlled with the standard dose is largely based on expert opinion. The objective of this study is to test the current urticaria guidelines of up-dosing antihistamines as second-line treatment. This was an open-label study conducted prospectively on 113 patients with chronic spontaneous urticaria. All patients were treated with sequentially increasing doses of levocetrizine (5 mg, 10 mg, 15 mg and 20 mg/day) every week till the patients became completely asymptomatic or dose of 20 mg/day reached. Urticaria Activity Score (UAS)-7, urticaria-related quality-of-life (CU-Q2oL) and patients' global assessment were used to assess treatment response. Twenty-one (18.58%) patients became asymptomatic with levocetirizine 5 mg/day, while 50 required higher doses of levocetirizine for complete control: 29/92 (31.52%), 6/63 (9.52%) and 15/57 (26.31%) with 10 mg, 15 mg and 20 mg/day, respectively. The percentage of patients experiencing >75% improvement increased with increasing doses of levocetirizine: 26.54%, 53.98%, 60.17% and 69.91% with 5 mg, 10 mg, 15 mg and 20 mg/day, respectively. Sequential up-dosing of levocetirizine produced a progressive improvement in both urticaria control (UAS-7) and quality-of-life (CU-Q2oL) without significantly increasing somnolence. Our results support the current recommendations of increasing antihistamines up to four times the standard dose in patients who fail the first-line treatment.

  15. Probiotics and refractory chronic spontaneous urticaria.

    Science.gov (United States)

    Nettis, E; Di Leo, E; Pastore, A; Distaso, M; Zaza, I; Vacca, M; Macchia, L; Vacca, A

    2016-09-01

    Background. In chronic spontaneous urticaria (CSU) first-line therapy with an antihistamine-based regimen may not achieve satisfactory control in patients. Thus, a continuing need exists for effective and safe treatments for refractory CSU. Aim. To evaluate the clinical efficacy and safety of an intake of a combination of 2 probiotics (Lactobacillus salivarius LS01 and Bifidobacterium breve BR03) in patients with CSU who remain symptomatic despite concomitant H1-antihistamine therapy. Methods. This report analyzes the effects of therapy with two probiotic strains on the clinical progress of 52 unselected patients with difficulty to treat CSU underwent to medical examination in two Italian specialist urticaria Clinics between September 2013 and September 2014. A mixture of Lactobacillus LS01 and Bifidobacterium BR03 were administered in each patient twice daily for 8 weeks. To evaluate patients' improvement with probiotics, urticaria activity score over 7 days (UAS7) was used at baseline and at week 8 in addition to a 5-question urticaria quality of life questionnaire. Results. Fifty-two patients with CSU were included in this study (10 male and 42 female, age range 19-72 years). Mean disease duration was 1.5 years. Fourteen patients discontinued treatment, so evaluable population consisted of 38 patients. Nine of the 38 patients experienced mild clinical improvement during probiotic treatment (23.7%); one patient reported significant clinical improvement (2.6%) and one patient had complete remission of urticaria (2.6%). Twenty-seven patients did not have improvement in symptoms (71.1%). No side effects during the course of therapy were reported. Conclusions. A combination of Lactobacillus salivarius LS01 and Bifidobacterium breve BR03 administered twice daily for 8 weeks might reduce the symptoms scores and improve quality of life scores in a part of patients with CSU who remained symptomatic despite treatment with H1 antihistamine mostly in subjects with allergic

  16. Clinical practice guideline for diagnosis and management of urticaria.

    Science.gov (United States)

    Kulthanan, Kanokvalai; Tuchinda, Papapit; Chularojanamontri, Leena; Chanyachailert, Pattriya; Korkij, Wiwat; Chunharas, Amornsri; Wananukul, Siriwan; Limpongsanurak, Wanida; Benjaponpitak, Suwat; Wisuthsarewong, Wanee; Aunhachoke, Kobkul; Wessagowit, Vesarat; Chatchatee, Pantipa; Wattanakrai, Penpun; Jirapongsananuruk, Orathai; Klaewsongkram, Jettanong; Noppakun, Nopadon; Vichyanond, Pakit; Suthipinittharm, Puan; Ruxrungtham, Kiat; Singalavanija, Srisupalak; Ngamphaiboon, Jarungchit

    2016-09-01

    Urticaria is a common skin condition that can compromise quality of life and may affect individual performance at work or school. Remission is common in majority of patients with acute spontaneous urticaria (ASU); however, in chronic cases, less than 50% had remission. Angioedema either alone or with urticaria is associated with a much lower remission rate. Proper investigation and treatment is thus required. This guideline, a joint development of the Dermatological Society of Thailand, the Allergy, Asthma, and Immunology Association of Thailand and the Pediatric Dermatological Society of Thailand, is graded and recommended based on published evidence and expert opinion. With simple algorithms, it is aimed to help guiding both adult and pediatric physicians to better managing patients who have urticaria with/without angioedema. Like other recent guideline, urticaria is classified into spontaneous versus inducible types. Patients present with angioedema or angioedema alone, drug association should be excluded, acetyl esterase inhibitors (ACEIs) and non-steroidal anti-inflammatory drugs (NSAIDs) in particular. Routine laboratory investigation is not cost-effective in chronic spontaneous urticaria (CSU), unless patients have clinical suggesting autoimmune diseases. Non-sedating H1-antihistamine is the first-line treatment for 2-4 weeks; if urticaria was not controlled, increasing the dose up to 4 times is recommended. Sedating first-generation antihistamines have not been proven more advantage than non-sedating antihistamines. The only strong evidence-based alternative regimen for CSU is an anti-IgE: omalizumab; due to very high cost it however might not be accessible in low-middle income countries. Non-pharmacotherapeutic means to minimize hyper-responsive skin are also important and recommended, such as prevention skin from drying, avoidance of hot shower, scrubbing, and excessive sun exposure.

  17. Outcomes of premedication for non-ionic radio-contrast media hypersensitivity reactions in Korea

    International Nuclear Information System (INIS)

    Kim, Sae-Hoon; Lee, So-Hee; Lee, Sang-Min; Kang, Hye-Ryun; Park, Heung-Woo; Kim, Sun-Sin; Cho, Sang-Heon

    2011-01-01

    Background: Radio-contrast media (CM)-related adverse reactions are important clinical problems that may cause fatal anaphylaxis. Accordingly, it has been common practice to premedicate patients who have had previous reactions to CM with corticosteroids, antihistamines, and H2 blockers to prevent hypersensitive reactions. However, the effectiveness of premedication has not been properly demonstrated, especially in cases related to non-ionic CM. In this study, we evaluated the effectiveness of premedication at preventing of non-ionic CM immediate-type hypersensitivity reactions. Methods: A total of 30 patients who had been pretreated with corticosteroid and H1 antihistamines and/or H2 blockers in a 3-year period were enrolled. The results of premedication were evaluated in terms of clinical characteristics and the features of breakthrough reactions. Results: Hypersensitivity reactions were not prevented in 5 of the 30 patients who had experienced prior CM reactions (overall recurrence rate after premedication 16.7%; 4/17 patients with mild previous reactions, and 1/13 patients with severe previous reactions). The recurrence rate after premedication was significantly higher in patients with mild previous reactions than in those with severe reactions (23.5% vs. 7.7%; p < 0.001). The breakthrough reactions were similar to the prior reactions in terms of severity and clinical manifestations. Conclusion: Premedication with corticosteroid and H1 antihistamines and/or H2 blockers effectively prevent non-ionic CM-related adverse events in most patients who have had severe previous reactions to CM. However, physicians should be aware of the possibility of premedication failing and of breakthrough reactions, even in cases in which the previous reactions were mild.

  18. Outcomes of premedication for non-ionic radio-contrast media hypersensitivity reactions in Korea

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Sae-Hoon, E-mail: imimdr@yahoo.co.kr [Department of Internal Medicine, Seoul National University College of Medicine, Seoul (Korea, Republic of); Institute of Allergy and Clinical Immunology, Seoul National University Medical Research Center, Seoul (Korea, Republic of); Department of Internal Medicine, Seoul National University Bundang Hospital (Korea, Republic of); Lee, So-Hee, E-mail: lshsophia@hanmail.net [Department of Internal Medicine, Seoul National University College of Medicine, Seoul (Korea, Republic of); Institute of Allergy and Clinical Immunology, Seoul National University Medical Research Center, Seoul (Korea, Republic of); Lee, Sang-Min, E-mail: sangminlee77@naver.com [Department of Internal Medicine, The Korean Armed Force Capital Hospital, Seongnam (Korea, Republic of); Kang, Hye-Ryun, E-mail: helenmed@hanmail.net [Department of Internal Medicine, Seoul National University College of Medicine, Seoul (Korea, Republic of); Institute of Allergy and Clinical Immunology, Seoul National University Medical Research Center, Seoul (Korea, Republic of); Park, Heung-Woo, E-mail: guineapark@snu.ac.kr [Department of Internal Medicine, Seoul National University College of Medicine, Seoul (Korea, Republic of); Institute of Allergy and Clinical Immunology, Seoul National University Medical Research Center, Seoul (Korea, Republic of); Kim, Sun-Sin, E-mail: ssksting@hanmail.net [Department of Internal Medicine, Seoul National University College of Medicine, Seoul (Korea, Republic of); Institute of Allergy and Clinical Immunology, Seoul National University Medical Research Center, Seoul (Korea, Republic of); Cho, Sang-Heon, E-mail: shcho@plaza.snu.ac.kr [Department of Internal Medicine, Seoul National University College of Medicine, Seoul (Korea, Republic of); Institute of Allergy and Clinical Immunology, Seoul National University Medical Research Center, Seoul (Korea, Republic of)

    2011-11-15

    Background: Radio-contrast media (CM)-related adverse reactions are important clinical problems that may cause fatal anaphylaxis. Accordingly, it has been common practice to premedicate patients who have had previous reactions to CM with corticosteroids, antihistamines, and H2 blockers to prevent hypersensitive reactions. However, the effectiveness of premedication has not been properly demonstrated, especially in cases related to non-ionic CM. In this study, we evaluated the effectiveness of premedication at preventing of non-ionic CM immediate-type hypersensitivity reactions. Methods: A total of 30 patients who had been pretreated with corticosteroid and H1 antihistamines and/or H2 blockers in a 3-year period were enrolled. The results of premedication were evaluated in terms of clinical characteristics and the features of breakthrough reactions. Results: Hypersensitivity reactions were not prevented in 5 of the 30 patients who had experienced prior CM reactions (overall recurrence rate after premedication 16.7%; 4/17 patients with mild previous reactions, and 1/13 patients with severe previous reactions). The recurrence rate after premedication was significantly higher in patients with mild previous reactions than in those with severe reactions (23.5% vs. 7.7%; p < 0.001). The breakthrough reactions were similar to the prior reactions in terms of severity and clinical manifestations. Conclusion: Premedication with corticosteroid and H1 antihistamines and/or H2 blockers effectively prevent non-ionic CM-related adverse events in most patients who have had severe previous reactions to CM. However, physicians should be aware of the possibility of premedication failing and of breakthrough reactions, even in cases in which the previous reactions were mild.

  19. Palonosetron and hydroxyzine pre-treatment reduces the objective signs of experimentally-induced acute opioid withdrawal in humans: a double-blinded, randomized, placebo-controlled crossover study.

    Science.gov (United States)

    Erlendson, Matthew J; D'Arcy, Nicole; Encisco, Ellen M; Yu, Jeffrey J; Rincon-Cruz, Lorena; Peltz, Gary; Clark, J David; Chu, Larry F

    2017-01-01

    Treatments for reducing opioid withdrawal are limited and prone to problematic side effects. Laboratory studies, clinical observations, and limited human trial data suggest 5-HT3-receptor antagonists and antihistamines may be effective. This double-blind, crossover, placebo-controlled study employing an acute physical dependence model evaluated whether (i) treatment with a 5-HT3-receptor antagonist (palonosetron) would reduce opioid withdrawal symptoms, and (ii) co-administration of an antihistamine (hydroxyzine) would enhance any treatment effect. At timepoint T = 0, healthy (non-opioid dependent, non-substance abuser) male volunteers (N = 10) were pre-treated with either a) placebo, b) palonosetron IV (0.75 mg), or c) palonosetron IV (0.75 mg) and hydroxyzine PO (100 mg) in a crossover study design. This was followed at T = 30 by intravenous morphine (10 mg/70kg). At T = 165, 10 mg/70kg naloxone IV was given to precipitate opioid withdrawal. The objective opioid withdrawal score (OOWS) and subjective opioid withdrawal score (SOWS) were determined 5 and 15 minutes after naloxone administration (T = 170, 180, respectively). Baseline measurements were recorded at T = -30 and T = -15. Comparison of average baseline OOWS scores with OOWS scores obtained 15 minutes after naloxone was significant (p = 0.0001). Scores from 15 minutes post-naloxone infusion showed significant differences in OOWS scores between treatment groups: placebo, 3.7 ± 2.4; palonosetron, 1.5 ± 0.97; and palonosetron with hydroxyzine, 0.2 ± 0.1333. Pretreatment with palonosetron significantly reduced many signs of experimentally-induced opioid withdrawal. Co-administration with hydroxyzine further reduced opioid withdrawal severity. These results suggest that 5-HT3 receptor antagonists, alone or in combination with an antihistamine, may be useful in the treatment of opioid withdrawal.

  20. Analysis of comorbidities and therapeutic approach for allergic rhinitis in a pediatric population in Spain.

    Science.gov (United States)

    Ibáñez, María Dolores; Valero, Antonio Luis; Montoro, Javier; Jauregui, Ignacio; Ferrer, Marta; Dávila, Ignacio; Bartra, Joan; Del Cuvillo, Alfonso; Mullol, Joaquim; Sastre, Joaquín

    2013-11-01

    Allergic rhinitis (AR) is the most common chronic disease in children. The main objective of this study was to analyze the comorbidities and therapeutic approaches for AR in a Spanish pediatric population. Children aged 6 to 12 years with AR were included in an observational, cross-sectional, multicenter study. 1,275 children were recruited from 271 centers. AR was intermittent in 59.5% of cases, persistent in 40.5%, seasonal in 60.7%, and perennial in 39.3% of patients. The most frequent comorbidities were conjunctivitis (53.6%), asthma (49.5%), atopic dermatitis (40%), rhinosinusitis(26.1%), otitis media (23.8%), and adenoid hypertrophy (17.3%). Overall, patients with persistent, moderate or severe, AR were more likely to present comobidities, except for food allergy and urticaria. The most common drugs used for treatment of AR were oral antihistamines(76%), nasal corticosteroids(49%) and a combination of both (45%). Antihistamines and nasal corticosteroids were used on demand (<18 days) in 38 and 41% of patients, respectively; for 18-30 days in 22 and 27%; for 1-3 months in 31 and 29%; and for more than 3 months in 8 and 3%, respectively. Eye drops were used in 32% and specific immunotherapy in 21% of patients. Comorbidities are frequent in children with AR, supporting the notion of allergy as a systemic disease. Severity and duration of AR were significantly associated with presence of most of comorbidities. The most common drugs used for AR treatment were oral antihistamines, followed by nasal corticosteroids and a combination of both used on demand. © 2013 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.