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Sample records for antihistamines

  1. 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.

  2. 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.

  3. Hypersensitivity to antihistamines.

    Science.gov (United States)

    Shakouri, Alireza A; Bahna, Sami L

    2013-01-01

    Antihistamines are the cornerstone of allergy therapy and are not expected to cause hypersensitivity reactions. We describe two cases, one had urticaria to multiple anti-H1-preparations and the other had anaphylaxis to hydroxyzine. We also provide a review of the English literature on reported reactions regarding causative preparations and manifestations. The latter showed a wide range; most commonly urticaria/angioedema, contact dermatitis, anaphylaxis, and fixed drug eruption (FDE). Most reported cases were young to middle age adults, with apparent predilection to female subjects. The onset of reactions varied from a few minutes for anaphylaxis and urticaria/angioedema, several hours for maculopapular rashes, or longer for contact dermatitis and FDE. Almost all antihistamines have been reported as causing reactions; cetirizine was the most common oral preparation followed by its parent drug, hydroxyzine. Doxepin cream was the most commonly implicated topical preparation in causing contact dermatitis. A causal relationship is often difficult to recognize because the reaction may be similar to the disease being treated with that antihistamine preparation. Reactions to one preparation are likely to occur, but not always, to other members of the same class. Diagnosis is based on clinical suspicion and may be verified by challenge testing. Except for patch testing in contact dermatitis or fixed eruption, other tests have not shown optimal reliability. In most cases, challenge testing with multiple preparations would identify one or more preparations that can be tolerated. Although hypersensitivity to antihistamines seems to be very rare, awareness of the problem would reduce its misdiagnosis.

  4. Pharmacology of Antihistamines

    Science.gov (United States)

    Church, Martin K; Church, Diana S

    2013-01-01

    H1-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 H1-receptors which are members of the G-protein family. The older first generation H1-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 H1-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. PMID:23723474

  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 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.

  7. Repurposing Cationic Amphiphilic Antihistamines for Cancer Treatment

    DEFF Research Database (Denmark)

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

    2016-01-01

    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...

  8. 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.

  9. 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.

  10. Antihistamine activity of Bryophyllum calycinum.

    Science.gov (United States)

    Nassis, C Z; Haebisch, E M; Giesbrecht, A M

    1992-01-01

    1. The juice obtained by pressing the leaves of Bryophyllum calycinum (Crassulaceae) exhibited histamine-blocking activity. 2. The juice contains flavonoid compounds, carbohydrates and mineral salts. A flavonoid fraction (fraction B) obtained by partitioning the juice between n-butanol and water contained the substance responsible for the antihistamine activity. 3. When assayed on the isolated guinea pig ileum, 50 mg/ml juice and 0.15 mg/ml fraction B produced parallel and concentration-dependent rightward displacement of the concentration-response curve to histamine (EC50 (FL): 1.30 (0.26-5.28) x 10(-7) M, 15.80 (5.90-23.30) x 10(-7) M, 12.50 (7.62-14.90) x 10(-7) M, in the absence and presence of 50 mg/ml juice and 12 mg/ml fraction B, respectively) apparently in a competitive manner. The antagonism was specific for histamine, i.e., did not modify the response to acetylcholine, KCl and BaCl2 and was reversible upon washing. Vascular permeability responses of rats to intracutaneous 1.0, 5.0 or 10.0 micrograms histamine were decreased by about 20-25% in animals pretreated with 4 ml/kg of juice or with 12 mg/kg fraction B. The juice (4 ml/kg) protected guinea pigs from death by asphyxia induced by 5 mg histamine and the protection lasted at least 1 h. 4. However, since the juice was ineffective in protecting the gastric mucosa from histamine-induced ulceration, we conclude that the antihistamine effect of the juice and fraction B was produced by blockade of H1 and not H2 receptors.

  11. Bilastine: new insight into antihistamine treatment

    OpenAIRE

    Ridolo, Erminia; Montagni, Marcello; Bonzano, Laura; Incorvaia, Cristoforo; Canonica, Giorgio Walter

    2015-01-01

    Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine epitomizes the evolution of research on antihistamines concerning both efficacy and safety. In AR treatment, a number of large controlled clinical trials documented its efficacy, as assessed by improvement of all nasal and ocular symptoms and quality of life. These outcomes show that bilastine meets current EAACI/ARIA criteria fo...

  12. A Danish Survey of Antihistamine Use and Poisoning Patterns

    DEFF Research Database (Denmark)

    Jensen, Louise; Rømsing, Janne; Dalhoff, Kim

    2017-01-01

    The first-generation antihistamine, promethazine, became a prescription-only drug in Denmark as of December 2014. First-generation antihistamines are known to have a higher toxic potential than second-generation antihistamines. The aim of this study was to provide a nationwide description...... 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...

  13. 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.

  14. 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.

  15. 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 p

  16. 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?

  17. Knowledge and attitude of medical resident doctors toward antihistamines

    Directory of Open Access Journals (Sweden)

    Esha Chainani

    2015-01-01

    Full Text Available Background: Allergic rhinitis and urticaria are chronic persistent allergic conditions that need proper management as they significantly reduce quality of life measures. Of the many pharmacological options of allergic rhinitis and urticaria, second-generation antihistamines are the mainstay of therapy. Aims: This review focuses on the knowledge of medical residents toward prescribing antihistamines, according to the new ARIA and GA2LEN guidelines for allergic rhinitis and urticaria, attempting to find the cause of less prescription of newer second-generation antihistamines by finding out the knowledge and attitude of the doctors prescribing them to the patients. Materials and Methods: The study was carried out among resident doctors at a tertiary care teaching hospital. Primary data from 100 resident doctors, who gave their informed consent, was collected. A prevalidated questionnaire regarding knowledge, attitude and prescribing practice of antihistamines was filled up. The data was then analyzed with suitable statistical tests. Every question was first validated using the Chi-square test, and significance was below 10% hence proving validity of the questions. Results: Out of the doctors surveyed, 82% of doctors said they prescribed second-generation antihistamines, while 18% still prescribed first-generation antihistamines. Out of the 82% that prescribed second-generation antihistamines, 8.9% also prescribed first-generation antihistamines as well. 23% of doctors surveyed had heard about the ARIA and GAL2EN guidelines and their recommendations for prescribing second-generation antihistamines over the older first-generation antihistamines, while 77% of them had not heard of these position papers. Conclusion: First-generation or classic antihistamines are still overused due to the lack of knowledge of various guidelines that have been published. The main reason for not prescribing the second-generation antihistamines was due to the increased

  18. Bilastine: new insight into antihistamine treatment.

    Science.gov (United States)

    Ridolo, Erminia; Montagni, Marcello; Bonzano, Laura; Incorvaia, Cristoforo; Canonica, Giorgio Walter

    2015-01-01

    Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine epitomizes the evolution of research on antihistamines concerning both efficacy and safety. In AR treatment, a number of large controlled clinical trials documented its efficacy, as assessed by improvement of all nasal and ocular symptoms and quality of life. These outcomes show that bilastine meets current EAACI/ARIA criteria for medications used in the treatment of AR. Also in CU, the review of the literature indicates that once-daily treatment with bilastine 20 mg was effective in managing symptoms and improving patient's quality of life. Concerning safety and tolerability, the profile of bilastine is very similar to placebo and in particular the adverse effects on central nervous system are insignificant. The balance of efficacy and safety of bilastine is particularly helpful when dosages higher than standard are needed to control the symptoms, as frequently occurs in patients with urticaria, in whom antihistamines doses up to four times the standard dose may be administered.

  19. 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.

  20. 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.

  1. Histamine and the antiallergic antihistamines: a history of their discoveries.

    Science.gov (United States)

    Emanuel, M B

    1999-07-01

    The paper provides a historical overview of the discovery of both histamine and the H1 antihistamines. The context of these discoveries is provided in relation to the development of medicinal chemistry during the 19th century. Background is provided on the history of discovery of mechanisms of anaphylaxis and allergy and the immunology of hypersensitivity at the end of the 19th and early 20th century. The discovery of histamine and the antihistamines is then discussed in relation to the development of pharmacological receptor theory culminating in the discovery of the first antihistamines in the 1930s and their widespread clinical introduction in the 1940s.

  2. NSAID-sensitive antihistamine-induced urticaria/angioedema.

    Science.gov (United States)

    Cimbollek, S; Ortega Camarero, M; Avila, R; Quiralte, J; Prados, M

    2011-01-01

    We present a case of urticaria caused by antihistamines in a patient with nonsteroidal anti-inflammatory drug (NSAID) sensitivity. A 35-year-old man experienced, on 2 separate occasions, immediate generalized urticaria during treatment with ibuprofen and naproxen, respectively. A single-blind, placebo-controlled oral challenge (SBPCOC) with piroxicam was carried out, and resulted in urticaria and angioedema 3 hours later. Two hours after initial clinical resolution, the patient developed multiple wheals on the trunk and upper limbs. He described similar delayed reactions after oral antihistamine administration on previous occasions. SBPCOCs with acetaminophen and etoricoxib were performed, with good tolerance. Skin prick and patch tests with loratadine and cetirizine were negative. After an SBPCOC with loratadine, the patient developed generalized urticaria 90 minutes after intake. Tolerance to fexofenadine 180 mg was confirmed. We describe the first case of a possible new subset of antihistamine urticaria, and suggest calling this NSAID-sensitive antihistamine-induced urticaria/angioedema.

  3. 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.

  4. 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

  5. H1抗组胺药%H1-antihistamines

    Institute of Scientific and Technical Information of China (English)

    张罗; 韩德民

    2013-01-01

    While histamine plays an important role in the pathogenesis of allergic diseases, such as allergic rhinitis, H1-antihistamines, which have been using in the treatment of allergic diseases for more than 70 years, are considered as the cornerstone of the medication of allergic diseases. In this review, we discuss the history of histamine studies and anti - histamine discovery, the histamine receptors, as well as the mechanisms and the safety of H1-antihistamines.

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

    OpenAIRE

    Cohen, A F; Posner, J

    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 ...

  7. Updosing of nonsedating anti-histamines in recalcitrant chronic urticaria

    OpenAIRE

    Kiran Godse; Prachi Bhattar; Sharmila Patil; Nitin Nadkarni; Manjyot Gautam

    2016-01-01

    Chronic urticaria (CU) is a persistent, debiliating condition that causes severe impairment on the quality of life (QoL) of patient by interrupting work productivity. Current guidelines recommend second-generation (nonsedating) anti-histamines for the treatment for all forms of urticaria. In patients who do not respond adequately to conventional doses of anti-histamines, it is recommended to increase the dose to up to four times to obtain control. But there are only few controlled studies tha...

  8. Knowledge and Attitude of Medical Resident Doctors Toward Antihistamines

    OpenAIRE

    Esha Chainani; Kiran Godse; Shweta Agarwal; Sharmila Patil

    2015-01-01

    Background: Allergic rhinitis and urticaria are chronic persistent allergic conditions that need proper management as they significantly reduce quality of life measures. Of the many pharmacological options of allergic rhinitis and urticaria, second-generation antihistamines are the mainstay of therapy. Aims: This review focuses on the knowledge of medical residents toward prescribing antihistamines, according to the new ARIA and GA2LEN guidelines for allergic rhinitis and urticaria, attemptin...

  9. 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.

    2015-01-01

    Introduction 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. Areas covered 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. Expert opinion 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: (1) selection of appropriate study population; (2) ascertainment of antihistamine exposures; and (3) ascertainment of birth defects 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 defects risk could be made. PMID:25307228

  10. [Antihistamines for the treatment of urticaria in Mexico].

    Science.gov (United States)

    Larenas-Linnemann, Désirée; Sánchez-Borges, Mario; Del Río-Navarro, Blanca Estela; Alonzo-Romero Pareyón, María De Lourdes; Maldonado-García, César Alfonso; Mendoza-López, Enrique; Ortega-Martell, José Antonio; Sienra-Monge, Juan José Luis; Medina-Ávalos, Miguel Alejandro; Rojo-Gutiérrez, María Isabel; Beirana-Palencia, Angélica María; Vargas-Correa, Jorge Bernardo; Báez-Loyola, Carlos; Ramírez-Segura, Ruth Ivonne Mireya; Guzmán-Perea, María Graciela

    2015-01-01

    There are four types of histamine receptors. Allergic symptoms, especially those in rhinoconjunctivitis and urticaria, are mainly caused by activation of histamine receptor 1 (H1). Consequently, oral H1-antihistamines form and integral part of the treatment of these diseases. Antihistamines are inverse agonists that stabilize the non-active configuration of the histamine receptor. First generation H1-antihistamines cause a variety of adverse effects via several mechanisms: sedation (accumulation in the central nervous system), dry mouth, urinary retention, weight gain (low selectivity: stimulation of serotonin/muscarinic/alpha-adrenergic receptors) and drug interactions (substrate of CYP450-3A4). Generally second generation H1-antihistamines have a better safety profile. New guidelines on allergic rhinitis and urticaria recommend second generation H1-antihistamines as first line drugs, with -if necessary- four-times updosing to obtain control in urticaria. The enhanced efficacy of quadruple doses in urticaria, while maintaining a good safety profile, has been shown for bilastine, desloratadine and levocetirizine (rupatadine). For ebastine and fexofenadine only the safety of quadruple doses has been shown till now. Extreme precaution should be taken with astemizol and terfenadine that never should be up-dosed, as high serum concentrations can cause potentially fatal ventricular tachycardia. First generation antihistamines are not recommended as first line treatment and updosing is not safe.

  11. [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.

  12. 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.

  13. H1-antihistamines for chronic spontaneous urticaria.

    Science.gov (United States)

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

    2014-11-14

    Background Chronic spontaneous urticaria (CSU) is characterised by the development of crops of red, itchy, raised weals or hives with no identifiable external cause.Objectives To assess the effects of H1-antihistamines for CSU.Search methods We searched the following databases up to June 2014: Cochrane Skin Group Specialised Register, CENTRAL (2014, Issue 5), MEDLINE(from 1946), EMBASE (from 1974) and PsycINFO (from 1806). We searched five trials registers and checked articles for references to relevant randomised controlled trials.Selection criteria We included randomised controlled trials of H1-antihistamines for CSU. Interventions included single therapy or a combination of H1-antihistamines compared with no treatment (placebo) or another active pharmacological compound at any dose.Data collection and analysis We used standard methodological procedures as expected by The Cochrane Collaboration.Our primary outcome measures were proportion of participants with complete suppression of urticaria: 'good or excellent' response,50% or greater improvement in quality of life measures, and adverse events.We present risk ratios (RR) with 95% confidence intervals(CIs). Main results We identified 73 studies (9759 participants); 34 studies provided data for 23 comparisons. The duration of the intervention was up to two weeks (short-term) or longer than two weeks and up to three months (intermediate-term).Cetirizine 10mg once daily in the short term and in the intermediate term led to complete suppression of urticaria by more participants than was seen with placebo (RR 2.72, 95% CI 1.51 to 4.91). For this same outcome, comparison of desloratadine versus placebo in the intermediate term (5 mg) (RR 37.00, 95% CI 2.31 to 593.70) and in the short term (20 mg) (RR 15.97, 95% CI 1.04 to 245.04)favoured desloratadine, but no differences were seen between 5 mg and 10 mg for short-term treatment.Levocetirizine 20 mg per day (short-term) was more effective for complete suppression of

  14. 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.

  15. 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 ...

  16. 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...

  17. Prescription writing trends of antihistamines at the university health centre

    Directory of Open Access Journals (Sweden)

    Kumar Anil

    2009-01-01

    Full Text Available The aim of the present study was to establish antihistamines drug prescribing pattern in order to improve the rational prescribing of antihistamines by physicians at Panjab University Health Centre. The study was performed in between the months of November 2005 to April 2006. Five hundred out patients were monitored and data was collected on WHO-based prescription-auditing performa. Demographic analysis of this prospective study revealed that out of the 500 patients, 293 (58.6 % were male and 207 (41.4 % were female and maximum patients were in the age group of 21-40 (34.8 %. Chlorpheniramine maleate (235 prescriptions was the highest prescribed among antihistamine prescriptions (36.89 % followed by diphenhydramine hydrochloride (186 prescriptions, 29.19%, cetirizine (175 prescriptions, 27.47 % and promethazine (41 prescriptions, 6.4%. In comparison to generic drugs (169 prescriptions, 26.54%, branded were more prescribed at PUHC. Majority of antihistamines were in form of tablets (414 prescriptions, 64.99% followed by liquid formulations (195 prescriptions, 30.61% and injections (28 prescriptions, 4.40%. The average cost of different antihistamine drugs prescribed was as follows: diphenhydramine hydrochloride Rs. 34.74 followed by promethzine Rs. 22.46, chlorpheniramine maleate Rs. 15.30, and cetirizine Rs. 13.50. Average numbers of drugs prescribed per prescription were 1.27. The average consulting and dispensing time was 4.82 and 3.56 min, respectively. Out of the 500 university patients, 258 (51.6% had the knowledge regarding the medication prescribed and 242 (48.4% were unaware of the medication prescribed.

  18. [Treatment of serous macular retinal detachment with antihistamines].

    Science.gov (United States)

    Kirschfeld, K

    2015-01-01

    The etiology of retinal detachment in central serous retinopathy (CSR) is unknown; however, three facts are generally accepted: (1) the serous exudate which raises the layers of the receptors/pigment epithelium is formed due to hyperpermeability in the choriocapillaries, (2) patients frequently suffer from headaches and (3) stress promotes the incidence of CSR. A high blood plasma histamine concentration can cause the abovementioned symptoms which suggests that histamine might provoke CSR. Within 1 week after administration of the antihistamine loratadin a considerable reduction in the retinal exudate and restoration of vision were observed. This supports the hypothesis that histamine could be involved in the process of retinal detachment. Further investigations and large scale clinical trials should clarify if this hypothesis can be proved or disproved and whether antihistamines can be used for age-related macular degeneration (AMD).

  19. Identification of phenothiazine antihistamines and their metabolites in urine.

    Science.gov (United States)

    Maurer, H; Pfleger, K

    1988-01-01

    Identification of the phenothiazine antihistamines alimemazine, dimetotiazine, isothipendyl, mequitazine, oxomemazine, promethazine, thiethylperazine, triflupromazine and their metabolites in urine is described. After acid hydrolysis of the conjugates, extraction and acetylation the urine samples were analysed by computerized gas chromatography-mass spectrometry. Using ion chromatography with the selective ions m/z 58, 72, 100, 114, 124, 128, 141, and 199 the possible presence of phenothiazine antihistamines and/or their metabolites was indicated. The identity of positive signals in the reconstructed ion chromatograms was confirmed by a visual or computerized comparison of the stored full mass spectra with the reference spectra. The ion chromatograms, reference mass spectra and gas chromatographic retention indices (OV-101) are documented. The procedure presented is integrated in a general screening procedure (general unknown analysis) for several groups of drugs.

  20. 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.

  1. Antihistamines in drivers, aircrew and occupations of risk.

    Science.gov (United States)

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

    2013-01-01

    The most commonly occurring allergic diseases can involve a daytime drowsiness associated with the condition itself. The antihistamines used in their treatment can also have central effects and affect certain occupations concerned with risk, road safety and maritime and air navigation. Cognitive tests, experimental studies and epidemiological data recommend avoiding 1st generation antihistamines for people who must drive regularly and/or professions concerned with safety. Although there are no comparative studies on real driving between 1st and 2nd generation antihistamines, in this type of patients there should be a preference for prescribing those with least possible central effect, especially those which are a good substrate for transmembrane transporter pumps such as P-glycoprotein and therefore have a low capacity for crossing the hematoencephalic barrier, thus allowing a broader window for therapy. In this sense, bilastine is a good P-glycoprotein substrate and shows good tolerance at CNS level, in both psychometric trials and real driving test protocols, even at double the dose recommended in the technical file.

  2. 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.

  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. Excipients in Oral Antihistamines Can Perpetuate Allergic Contact Dermatitis.

    Science.gov (United States)

    Tocci, Elizabeth M; Robinson, Amanda; Belazarian, Leah; Foley, Elizabeth; Wiss, Karen; Silvestri, Dianne L

    2015-01-01

    Propylene glycol is a well-documented causative agent of allergic contact dermatitis (ACD). It is also reported to cause systemic dermatitis after ingestion of foods or medicines containing it and after intravenous injection of a medicine with propylene glycol in its base. We describe two adolescents with sensitivity to propylene glycol confirmed by patch testing whose dermatitis improved dramatically after cessation of oral antihistamines containing propylene glycol. We report these cases to alert providers to the potential for worsening of ACD due to systemic exposure to propylene glycol in patients with a cutaneous sensitivity to the allergen.

  5. [Effect of new antihistaminic preparations on the body's immunologic reactivity].

    Science.gov (United States)

    Mashkovskiĭ, M D; Veksler, I G; Kaminka, M E; Iakimenko, V A

    1981-03-01

    The effect of new antihistaminic drugs, phencarol and bicarphen, on immunologic reactivity of experimental animals was studied in comparison with diphenhydramine. Phencarol and bicarphen inhibited the delayed type allergic reactions to a greater degree than diphenydramine. Unlike diphenhydramine, phencarol and bicarphen injected simultaneously with test-antigen markedly decreased the number of rosette-forming lymphocytes in the immunocompetent organs (spleen, thymus, lymph nodes). Phencarol, bicarphen and diphenhydramine produced the same inhibitory effect on the content of antibody-producing cells in the spleen of mice.

  6. Comparative Effect of Newer Antihistamines on Psychomotor Functions in Indian Population

    Directory of Open Access Journals (Sweden)

    Vivek K. David, Dinesh K. Badyal, Ashish Varghese*, Emy Alexander**

    2010-01-01

    Full Text Available The purpose of the present study was to comparatively evaluate the effect of newer antihistamines onpsychomotor functions in Indian population. Seventy five patient volunteers were included in the study.Volunteers were put into 5 groups based on the type of antihistamine prescribed. Group-1 volunteersincluded those who were prescribed no antihistamine, group-2 were prescribed first generation antihistamines,group 3, 4 & 5 were prescribed second generation antihistamines cetrizine, fexofenadine and loratadinerespectively. A battery of four psychomotor function tests: critical flicker fusion threshold (CFFT, digitsymbol substitution test (DSST, finger tapping (FT and visual analogue scale (VAS for day time sedationwas used in the study. First generation antihistamines impaired psychomotor functions establishing thevalidity of psychomotor function tests chosen for the study. Second generation antihistamines did notsignificantly affect CFFT frequency, but DSST score was significantly reduced. Fexofenadine significantlyreduced FT score. All antihistamines produced sedation except loratadine on VAS. Second generationantihistamines impaired psychomotor performance in Indian patients, however there were individualdifferences evident in respect to the effect of drugs.

  7. 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

  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. CE-MS of antihistamines using nonvolatile phosphate buffer.

    Science.gov (United States)

    Chien, Chiu-Tang; Li, Fu-An; Huang, Ju-Li; Her, Guor-Rong

    2007-05-01

    Antihistamines were analyzed by CE-ESI-MS using phosphate buffer. The separation was performed in an acidic environment so that phosphate ions had a net velocity flowing toward the inlet reservoir instead of the ESI source. To further reduce the effect of ion suppression, the sodium ion in sodium phosphate was replaced with an ammonium ion. Furthermore, with the combination of reducing the concentration of acid added to the sheath liquid and the use of a low-flow interface, phosphoric acid could be added to the sheath liquid. Because of the use of the same counterion (phosphate ion) in running buffer and in sheath liquid, the separation integrity (resolution, elution order, and peak shape) was preserved. In addition, ion suppression was also greatly alleviated because a minimal amount of phosphate flowed into the ESI source.

  10. Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.

    Science.gov (United States)

    Perlmutter, Jessamyn I; Forbes, Lauren T; Krysan, Damian J; Ebsworth-Mojica, Katherine; Colquhoun, Jennifer M; Wang, Jenna L; Dunman, Paul M; Flaherty, Daniel P

    2014-10-23

    Staphylococcus aureus is a rapidly growing health threat in the U.S., with resistance to several commonly prescribed treatments. A high-throughput screen identified the antihistamine terfenadine to possess, previously unreported, antimicrobial activity against S. aureus and other Gram-positive bacteria. In an effort to repurpose this drug, structure-activity relationship studies yielded 84 terfenadine-based analogues with several modifications providing increased activity versus S. aureus and other bacterial pathogens, including Mycobacterium tuberculosis. Mechanism of action studies revealed these compounds to exert their antibacterial effects, at least in part, through inhibition of the bacterial type II topoisomerases. This scaffold suffers from hERG liabilities which were not remedied through this round of optimization; however, given the overall improvement in activity of the set, terfenadine-based analogues provide a novel structural class of antimicrobial compounds with potential for further characterization as part of the continuing process to meet the current need for new antibiotics.

  11. 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.

  12. 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...

  13. 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

  14. 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

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

    OpenAIRE

    Wolthers, Ole D.

    2013-01-01

    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 a...

  16. 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.

  17. 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.

  18. 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.

  19. Photodegradation of the antihistamine cetirizine in natural waters.

    Science.gov (United States)

    Mead, Ralph N; Barefoot, Seth; Helms, John R; Morgan, Jeremy B; Kieber, Robert J

    2014-10-01

    The photodegradation rate of the anti-histamine cetirizine (Zyrtec®) was investigated in various water matrices. The average observed first-order photodegradation rate coefficient (kobs ), obtained by linear regression of the logarithmic-transformed cetirizine concentrations versus irradiation time in simulated sunlight, was 0.024 h(-1) (n = 6; standard deviation ± 0.004) in deionized water corresponding to a half-life of approximately 30 h. There was no statistical difference in the kobs of cetirizine photodegradation in coastal seawater compared with deionized water or deionized water amended with dissolved chromophoric organic matter. The quantum yield of cetirizine photodegradation decreased dramatically with increasing wavelength and decreasing energy of incoming radiation, with the average value ranging from 5.28 × 10(-4) to 6.40 × 10(-3) in the ultraviolet wavelength range (280-366 nm). The activation energy of cetirizine photodegradation was 10.3 kJ mol(-1) with an observed increase in cetirizine photodegradation as temperature increased. This is a significant environmental factor influencing half-life and an important consideration, given that cetirizine has been detected in wastewater and receiving waters from different locations globally.

  20. 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.

  1. Pro-Arrhythmic Potential of Oral Antihistamines (H1): Combining Adverse Event Reports with Drug Utilization Data across Europe

    OpenAIRE

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

    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 clinical data are available on other antihistamines. Aim: To investigate the pro-arrhythmic potential of antihistamines by combining safety reports of the FDA Adverse Event Reporting System (FAERS)...

  2. Histamine H1 Receptor Gene Expression and Drug Action of Antihistamines.

    Science.gov (United States)

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

    2016-11-25

    The upregulation mechanism of histamine H1 receptor through the activation of protein kinase C-δ (PKCδ) and the receptor gene expression was discovered. Levels of histamine H1 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 H1 receptor mRNA in the nasal mucosa was observed in patients with pollinosis. Both scores of nasal symptoms and the level of histamine H1 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 H1 receptor-mediated activation of histamine H1 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 H1 receptor gene expression, suggesting the advantage of therapeutic effect.

  3. Antihistamines and aquatic insects: bioconcentration and impacts on behavior in damselfly larvae (Zygoptera).

    Science.gov (United States)

    Jonsson, M; Fick, J; Klaminder, J; Brodin, T

    2014-02-15

    Because aquatic insects use histamines as neurotransmitters, adverse impacts on aquatic insects living in aquatic environments that receive antihistamines with wastewater effluent are plausible. In this study, we exposed damselfly larvae to low concentrations of two commonly used antihistamines (Hydroxyzine and Fexofenadine, 360 ± 42 and 2,200 ± 43 ng l(-1), respectively), and recorded damselfly larvae behavior before and after exposure. Further, after the second set of behavioral assays was performed, we quantified bioconcentration of the antihistamines in the damselfly bodies. Our results showed significant changes in damselfly behavior following antihistamine exposure. After Hydroxyzine exposure, the damselfly larvae became less active, and they showed reduced fleeing response (i.e. increased boldness) after being exposed to Fexofenadine, the latter also being significantly different from the non-exposed (control) individuals. Further, we found high levels of bioconcentration in the damselflies; Hydroxyzine showed an average bioconcentration factor (BCF) of 2000. As such, our results indicate that low concentrations of antihistamines can have sub-lethal effects on aquatic insects manifested as behavioral changes, and that bioconcentration of these substances can be high. Therefore, the need to investigate the impact of emergent aquatic contaminants also on aquatic insects, and on behaviors that are of ecological importance, is further highlighted.

  4. MODULATION OF ANTI-INFLAMMATORY ACTIVITY OF NSAIDS IN NORMAL RATS TREATED WITH ANTIHISTAMINICS.

    Directory of Open Access Journals (Sweden)

    Nilam Nigam

    2012-10-01

    Full Text Available NSAIDs are frequently used for relief of inflammati on and Antihistaminics are indicated for simultaneous administration for aller gic manifestations. Opioids analgesics have been reported to interact with Antihistaminics. To e xplore the interacting potentiality, in the present study the effects of combined treatment with NSAIDs and antihistaminics were examined in rats. Anti-inflammatory effect was eval uated by Carrageenan induced hind paw oedema in rats. NSAIDs like aspirin, ibuprofen and pir oxicam were selected for study on per se and on concurrent administration with Antihistamini cs such as Promethazine, Cetrizine and Astemizole. All NSAIDs protected animals show anti-i nflammatory activity. Aspirin shows highly significant potentiation of anti-inflammatory effect at all dose level, however ibuprofen and piroxicam show highly significant anti-inflammatory effect at higher doses only and on concurrent administration of antihistaminics, aspiri n, piroxicam and ibuprofen with all antihistaminics produced highly significant potentiat ion except ibuprofen with Cetrizine produced significant potentiation of anti-inflammator y response at higher doses only.

  5. 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.

  6. 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...... was not significantly higher than 1 (OR 1.37 [95% CI: 0.85, 2.23]), whereas the risk estimate calculated after the governmental decision did significantly differ from 1 (OR 4.19 [95% CI: 2.49, 7.05]). CONCLUSIONS: Our data suggest that non-sedating antihistamines might have an increased risk for inducing arrhythmias....... Our findings, however, strongly suggest that the increased risk identified can at least partly be explained by reporting bias as a result of publications about and mass media attention for antihistamine induced arrhythmias....

  7. PREVALANCE OF VARIOUS SKIN DISORDERS AND PRESCRIBING PATTERN OF ANTIHISTAMINES IN TERTIARY CARE HOSPITAL, PUNE

    Directory of Open Access Journals (Sweden)

    Mrs. Manjusha Sajith

    2014-03-01

    Full Text Available Objectives: Dermatological conditions account for up to 2% of consultations in general practice worldwide. Skin diseases in developing countries have a serious impact on quality of life. The objective of the present study is to assess the prevalence of various skin diseases and to assess the drug utilization pattern of antihistamines in Dermatology Outpatient Department. Methods: A prospective study was carried out in Dermatology department of Bharati Hospital and Research Centre, Pune. The data collection form was prepared which includes patient and medication related information. The prescriptions were analyzed for common skin conditions and prescription patterns. Results: During the study period 320 prescriptions were analyzed including males 158 (49.37% and females 162 (50.62%. The maximum number of patients (38.75% were in the age group of adults (20 to 30years and minimum were children (<10 yrs is 6.25%. Most of them were having Acne problems (31.25%, followed by Eczema (8.75. Antibiotics (31.91% were mostly prescribed class of drugs, followed by steroids (20.33% and antihistamines (17.73%. Among antihistamines, Levocetirizine is mostly prescribed (66.66%. Antihistamines were mostly prescribed in skin problems like Urticaria (20.0%, followed by Dermatitis (18.66%. Ranitidine is prescribed along with other antihistamines to treat Urticaria( hives. Conclusion: Most of the patients were having Acne problems. Antihistamines were mostly prescribed in allergic conditions and rashes. Majority of drugs were prescribed in brand names. Periodic evaluation of prescribing pattern is necessary to improve prescribing standards.

  8. 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

  9. 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

    BACKGROUND: First-generation H(1)-antihistamines obtained without prescription are the most frequent form of self-medication for allergic diseases, coughs and colds and insomnia even though they have potentially dangerous unwanted effects which are not recognized by the general public. AIMS...

  10. 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

    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

  11. A study to evaluate prescribing pattern and cost minimization analysis of antihistamines among patients of allergy

    Directory of Open Access Journals (Sweden)

    Ayesha Vaseem

    2016-12-01

    Results: Most commonly prescribed antihistamine is cetrizine followed by levocetrizine and fexofenadine. Conclusions: This study demonstrated a significant price difference, ranging from 4% to 83.75% between the branded and generic version of given drugs. This in turn is leading to an increase in the cost of total treatment. [Int J Basic Clin Pharmacol 2016; 5(6.000: 2500-2503

  12. New patents of fixed combinations of nasal antihistamines and corticosteroids in allergic rhinitis.

    Science.gov (United States)

    Wolthers, Ole D

    2013-09-01

    During the last few years, fixed combinations of intranasal antihistamines and corticosteroids have been introduced for treatment of allergic rhinitis. The aim of this systematic review was to assess recent patents and clinical evidence for fixed combinations of intranasal antihistamines and intranasal corticosteroids in allergic rhinitis. Data base searches revealed that intranasal combinations of the antihistamine azelastine with the corticosteroids mometasone furoate, ciclesonide and fluticasone propionate, respectively, have been patented. Four randomized, double-blinded, parallel-group, placebo-controlled, multicenter trials sponsored by the manufacturer evaluated the fixed combination of intranasal azelastine 125 µg and fluticasone propionate 50 µg administered as one dose per nostril b.i.d. in patients with moderate-to-severe symptomatic allergic rhinitis ≥ 12 years of age. Three of the studies were published as a meta-analysis which found the fixed combination of azelastine and fluticasone propionate statistically significantly more efficacious in reducing baseline total nasal symptom score by 5.7 as compared to azelastine (4.4; P antihistamines and corticosteroids are needed, especially, in primary care settings and in children before fixed combination treatment can be considered first line therapy in allergic rhinitis. Fixed combination treatment of azelastine and fluticasone propionate may offer additional benefit to selected populations of adolescents and adults with moderate-to-severe symptoms.

  13. 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.

  14. 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.

  15. 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.

  16. Second generation antihistamines: assessment of the efficacy of treatment and tolerance of some preparations of this group (preliminary studies

    Directory of Open Access Journals (Sweden)

    Małgorzata A. Czarny-Działak

    2016-04-01

    Full Text Available Introduction : Second generation antihistamines are key medicines in the treatment of allergic diseases such as allergic rhinitis and allergic conjunctivitis. Aim of the research: To compare the effectiveness of selected antihistamines and frequency of side effects in the course of their therapy in the patient opinion. Material and methods : The study was conducted on a group of 40 patients taking rupatadine, bilastine, levocetirizine and fexofenadine. The method of diagnostic survey was used, having the character of a preliminary examination in view of the small number of people involved in the study. Results: Among the 40 patients, side effects of the medicines only appeared in 3 respondents, which is 1.2%. Conclusions : The new generation antihistamines in light of our studies appear to be safe and associated with few side effects. Due to the small number of surveyed people we treat these tests as preliminary to further analysis of the effectiveness of selected antihistamines.

  17. Up-dosing of non-sedating antihistamines in chronic urticaria: Need for well-designed clinical trials in India

    OpenAIRE

    Anant D. Patil

    2014-01-01

    Urticaria is a heterogeneous group of diseases. Chronic urticaria significantly impacts quality-of-life of patients. Second generation, non-sedating antihistamines are recommended as first line treatment for chronic spontaneous urticaria. In patients with inadequate control of symptoms, increase in dosage of non-sedating antihistamines up to four fold has been recommended. This recommendation is based on low cost, good safety and good evidence of efficacy of non-sedating, second generation an...

  18. Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines.

    Science.gov (United States)

    Gillard, M; Benedetti, M Strolin; Chatelain, P; Baltes, E

    2005-09-01

    The predictive efficacy of drugs in humans is frequently estimated from both a high affinity for their receptor as measured in vitro and a long plasmatic half-life. This is grossly misleading since one key parameter is missing: drug concentration at the receptor site in vivo. As a case study we compared the efficacies of three H(1) antihistamines in inhibiting histamine-induced wheal and flare in humans at two different time points with the above mentioned parameters. It is concluded that estimating in vivo receptor occupancy, which takes into account both the affinity of the drug for the receptor and its free plasma concentration, is a far better predictor for human pharmacodynamics and hence antihistamine potency, than considering in vitro affinity and plasmatic half-life only.

  19. 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%.

  20. 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.

  1. 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.

  2. THE EFFECT OF SOME NEW ANTIHISTAMINES ON THE ANAPHYLACTIC MICROSHOCK OF THE GUINEA-PIG.

    Science.gov (United States)

    HERXHEIMER, H; STRESEMANN, E

    1963-12-01

    The dose/response curves for the protective effects of the new antihistamine compounds trimeprazine, 10-(3-diethylamino-2-methylpropyl)phenothiazine 1,1-dioxide hydrochloride (oxomemazine hydrochloride), cyproheptadine, homochlorcyclizine and methotrimeprazine against the anaphylactic microshock of the guinea-pig were similar to that of promethazine. The first three compounds, however, protected at lower doses than promethazine (5 to 10 mug/kg). The protective effect of cyproheptadine lasted longer than 24 hr.

  3. 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.

  4. Chemometrics optimization of six antihistamines separations by capillary electrophoresis with electrochemiluminescence detection.

    Science.gov (United States)

    Zhu, Derong; Li, Xia; Sun, Jinying; You, Tianyan

    2012-01-15

    This work expanded the knowledge of the use of chemometric experimental design in optimizing of six antihistamines separations by capillary electrophoresis with electrochemiluminescence detection. Specially, central composite design was employed for optimizing the three critical electrophoretic variables (Tris-H(3)PO(4) buffer concentration, buffer pH value and separation voltage) using the chromatography resolution statistic function (CRS function) as the response variable. The optimum conditions were established from empirical model: 24.2mM Tris-H(3)PO(4) buffer (pH 2.7) with separation voltage of 15.9 kV. Applying theses conditions, the six antihistamines (carbinoxamine, chlorpheniramine, cyproheptadine, doxylamine, diphenhydramine and ephedrine) could be simultaneous separated in less than 22 min. Our results indicate that the chemometrics optimization method can greatly simplify the optimization procedure for multi-component analysis. The proposed method was also validated for linearity, repeatability and sensitivity, and was successfully applied to determine these antihistamine drugs in urine.

  5. 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.

  6. Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria.

    Science.gov (United States)

    Wolthers, Ole D

    2013-01-01

    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.

  7. 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.

  8. In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates

    Directory of Open Access Journals (Sweden)

    Moustafa A El-Nakeeb

    2011-09-01

    Full Text Available Antihistaminics are widely used for various indications during microbial infection. Hence, this paper investigates the antimicrobial activities of 10 antihistaminics belonging to both old and new generations using multiresistant Gram-positive and Gram-negative clinical isolates. The bacteriostatic activity of antihistaminics was investigated by determining their MIC both by broth and agar dilution techniques against 29 bacterial strains. Azelastine, cyproheptadine, mequitazine and promethazine were the most active among the tested drugs. Diphenhydramine and cetirizine possessed weaker activity whereas doxylamine, fexofenadine and loratadine were inactive even at the highest tested concentration (1 mg/ml. The MIC of meclozine could not be determined as it precipitated with the used culture media. The MBC values of antihistaminics were almost identical to the corresponding MIC values. The bactericidal activity of antihistaminics was also studied by the viable count technique in sterile saline solution. Evident killing effects were exerted by mequitazine, meclozine, azelastine and cyproheptadine. Moreover, the dynamics of bactericidal activity of azelastine were studied by the viable count technique in nutrient broth. This activity was found to be concentration-dependant. This effect was reduced on increasing the inoculum size while it was increased on raising the pH. The post-antimicrobial effect of 100 fg/ml azelastine was also determined and reached up to 3.36 h.

  9. Postadulticide pulmonary hypertension of canine heartworm disease: successful treatment with oxygen and failure of antihistamines.

    Science.gov (United States)

    Rawlings, C A; Tackett, R L

    1990-10-01

    Postadulticide pulmonary hypertension mechanisms and treatment with antihistamines and supplemental oxygen were studied in eight dogs with heartworm disease. To ensure severe postadulticide thromboembolism, additional heartworms (either 20 or 40 into 4 dogs each) were transplanted into naturally infected dogs before thiacetarsamide treatment. During pentobarbital anesthesia, 2 pulmonary hemodynamic studies were conducted on each dog with a sequence of baseline, hypoxia with FlO2 = 10%, hyperoxia with FlO2 = 100%, a second baseline, treatment with either diphenhydramine (D) or cimetidine (C), and another hypoxia. All dogs were pulmonary hypertensive, with each dog having a mean pulmonary arterial pressure (PPA) greater than 20 mm of Hg. Mean PPA increased from baseline conditions (25.0 +/- 4.5 SD for D and 24.3 +/- 4.4 for C) to hypoxia (28.5 +/- 4.7 for D and 28.4 +/- 3.7 for C), and decreased during hyperoxia (16.9 +/- 3.0 for D and 17.4 +/- 3.0 for C), respectively. Neither antihistamine reduced PPA at normoxia. The degree of pulmonary hypertension when breathing room air increased even more during hypoxia, and this increase was not attenuated by either antihistamine. Histamine did not appear to mediate pulmonary hypertension during postadulticide thromboembolism, nor to modify the hypoxia-mediated pulmonary hypertension at this disease stage. Because baseline PO2 was low (66.6 +/- 11.7 mm of Hg for D and 69.4 +/- 14.2 for C) and because PPA decreased during administration of oxygen, the pulmonary hypertension was mostly hypoxia-induced. In addition to the arterial lesions, much of the pulmonary hypertensive mechanism was an active and reversible vasoconstriction in response to hypoxia caused by the secondary lung disease.(ABSTRACT TRUNCATED AT 250 WORDS)

  10. 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.

  11. 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

    2016-01-01

    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). PMID:26657408

  12. 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).

  13. 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...... 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...... 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....

  14. Liquid chromatography of antihistamines using post-column tris(2,2'-bipyridine) ruthenium(III) chemiluminescence detection.

    Science.gov (United States)

    Holeman, J A; Danielson, N D

    1994-09-23

    The separation and detection of five antihistamine drugs commonly found within over-the-counter allergy and cold pharmaceutical products was performed by HPLC with chemiluminescence (CL) detection. Comparable detection limits at 5-10 pmol were found for the antihistamines by both UV at 214 nm and tris(2,2'-bipyridine) ruthenium(III) CL. However, urine samples were found not to generate as large an unretained peak by CL detection as compared to those peaks by UV detection at 214 and 254 nm. For example, the pheniramine peak representing 0.15 microgram/ml was almost totally obscured at 214 nm. Quantitative results received for three antihistamine commercial samples ranged from 4 to 8% error in accuracy when an internal standard was used to compensate for short term detector drift.

  15. 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.

  16. 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

  17. 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

    Background 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. Aim 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. Methods 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. Results 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. Conclusions Some second-generation antihistamines are associated with signal of torsadogenicity and largely used in most European countries. Although confirmation by

  18. Steroids and antihistamines synergize to inhibit rat's airway smooth muscle contractility.

    Science.gov (United States)

    Liu, Shao-Cheng; Chu, Yueng-Hsiang; Kao, Chuan-Hsiang; Wu, Chi-Chung; Wang, Hsing-Won

    2015-06-01

    Both glucocorticoids and H1-antihistamines were widely used on patients with allergic rhinitis (AR) and obstructive airway diseases. However, their direct effects on airway smooth muscle were not fully explored. In this study, we tested the effectiveness of prednisolone (Kidsolone) and levocetirizine (Xyzal) on isolated rat trachea submersed in Kreb's solution in a muscle bath. Changes in tracheal contractility in response to the application of parasympathetic mimetic agents were measured. The following assessments of the drug were performed: (1) effect on tracheal smooth muscle resting tension; (2) effect on contraction caused by 10(-6) M methacholine; (3) effect of the drug on electrical field stimulation (EFS) induced tracheal smooth muscle contractions. The result revealed sole use of Kidsolone or Xyzal elicited no significant effect or only a little relaxation response on tracheal tension after methacholine treatment. The tension was 90.5 ± 7.5 and 99.5 ± 0.8 % at 10(-4) M for Xyzal and 10(-5) M for Kidsolone, respectively. However, a dramatically spasmolytic effect was observed after co-administration of Kidsolone and Xyzal and the tension dropped to 67.5 ± 13.6 %, with statistical significance (p antihistamines to dramatically relax the trachea smooth muscle within minutes. Therefore, for AR patients with acute asthma attack, combined use of those two drugs is recommended.

  19. Identification of histamine receptors and reduction of squalene levels by an antihistamine in sebocytes.

    Science.gov (United States)

    Pelle, Edward; McCarthy, James; Seltmann, Holger; Huang, Xi; Mammone, Thomas; Zouboulis, Christos C; Maes, Daniel

    2008-05-01

    Overproduction of sebum, especially during adolescence, is causally related to acne and inflammation. As a way to reduce sebum and its interference with the process of follicular keratinization in the pilosebaceous unit leading to inflammatory acne lesions, antihistamines were investigated for their effect on sebocytes, the major cell of the sebaceous gland responsible for producing sebum. Reverse transcriptase-PCR analysis and immunofluorescence of an immortalized sebocyte cell line (SZ95) revealed the presence of histamine-1 receptor (H-1 receptor), and thus indicated that histamines and, conversely, antihistamines could potentially modulate sebocyte function directly. When sebocytes were incubated with an H-1 receptor antagonist, diphenhydramine (DPH), at non-cytotoxic doses, a significant decrease in squalene levels, a biomarker for sebum, was observed. As determined by high-performance liquid chromatography, untreated sebocytes contained 6.27 (+/-0.73) nmol squalene per 10(6) cells, whereas for DPH-treated cells, the levels were 2.37 (+/-0.24) and 2.03 (+/-0.97) nmol squalene per 10(6) cells at 50 and 100 microM, respectively. These data were further substantiated by the identification of histamine receptors in human sebaceous glands. In conclusion, our data show the presence of histamine receptors on sebocytes, demonstrate how an antagonist to these receptors modulated cellular function, and may indicate a new paradigm for acne therapy involving an H-1 receptor-mediated pathway.

  20. Control of nausea and autonomic dysfunction with terfenadine, a peripherally acting antihistamine

    Science.gov (United States)

    Kohl, Randall L.; Calkins, Dick S.; Robinson, Robert E.

    1991-01-01

    Terfenadine (Seldane) was admisistered to 14 male subjects in a randomized, double-blinded, and cross-over design to assess the efficacy of this peripherally active antihistamine as an antimotion sickness drug. Terfenadine possesses practically no central side effects. A staircase profile test was administered 4 h following placebo or a single oral dose of terfenadine (300 mg). The study revealed a statistically significant therapeutic effect from terfenadine (p less than 0.05). This led to a conclusion that, because the drug does not or only poorly crosses the blood-brain barrier, a selective peripheral antihistamine action may be sufficient in the control of motion sickness induced through cross-coupled accelerative semicircular canal stimulation using a rotating chair. This finding implies that other peripherally acting agents might be found that possess even greater antimotion sickness efficacy. The present research raises additional questions regarding current theories on the etiology of motion sickness, its associated autonomic system dysfunction, and the validity of assumptions that effective pharmacological agents must act centrally.

  1. Mast Cell Stabilizing,Antianaphylactic and Antihistaminic Activity of Coccinia grandis Fruits in Asthma

    Institute of Scientific and Technical Information of China (English)

    Dnyaneshwar J Taur; Ravindra Y Patil

    2011-01-01

    Coccinia grandis Linn(Curcubitaceae)is a climber herb cultivated throughout India.In traditional medicine fruits have been used to treat leprosy,fever,asthma,bronchitis and jaundice.In present study,ethanol extract of C.grandis fruit(ECGF)at 100,125 and 150 mg·kg-1,i.p.,was evaluated for mast cell stabilizing,antianaphylactic and antihistaminic activity using egg albumin induced mast cell degranulation in mice;passive cutaneous anaphylaxis in rats and clonidine induced catalepsy in mice respectively.ECGF at(100-150 mg·kg-1,i.p.)significantly protected egg albumin induced degranulations of mast cells and caused reduction of blue dye leakage in passive cutaneous anaphylaxis in dose dependently.The treatment ECGF also inhibited clonidine induced catalepsy in dose dependent manner.Phytochemical studies observed presence of saponin,steroids,alkaloids,flavonoids and glycosides.In conclusion ECGF possesses mast cell stabilizing;anti anaphylactic and antihistaminic potential which might be used in treatment of asthma.

  2. A patient with steroids and antihistaminic drug allergy and newly occurred chronic urticaria angioedema: what about omalizumab?

    Science.gov (United States)

    Kutlu, A; Karabacak, E; Aydin, E; Ozturk, S; Bozkurt, B

    2014-08-01

    In this case report, successful use of omalizumab in the treatment of chronic urticarial and angioedema in a 24-year-old female patient with an allergic reaction history to almost every drug including steroids and antihistamines was presented. She also had allergy against a large number of foods, which were confirmed by oral provocation, specific Immunoglobulin E and allergy skin test.

  3. 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.

    2014-01-01

    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), Univer

  4. 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

  5. Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine

    Directory of Open Access Journals (Sweden)

    Wang XY

    2016-04-01

    Full Text Available Xue Yan Wang,1 Margaret Lim-Jurado,2 Narayanan Prepageran,3 Pongsakorn Tantilipikorn,4 De Yun Wang5 1Department of Allergy, Beijing Shijitan Hospital, Capital Medical University, Beijing, People’s Republic of China; 2St Luke’s Medical Center, Quezon City, Manila, Philippines; 3Department of Otorhinolaryngology, Head & Neck Surgery, University Malaya Faculty of Medicine, Kuala Lumpur, Malaysia; 4Rhinology and Allergy Division, Department of Otorhinolaryngology, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok, Thailand; 5Department of Otolaryngology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore Abstract: Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients’ quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug–drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug’s safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily. The

  6. 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.

  7. 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.

  8. 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.

  9. Validation of a Serum Analysis Method to Analyze Antihistamines by Capillary Electrophoresis

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    J. Peris-Vicente

    2014-01-01

    Full Text Available The validation of an electrophoresis-based analytical method to quantify 17 antihistamines in pharmaceutical formulations and serum is described. Then, whether the methodology provides true values with low uncertainty and is able to detect the concentration range level of analyte usually found in the matrix was evaluated. The analytical method was validated following the recommendations of an official guide to provide more reliability to the results. The ICH Harmonized Tripartite Guideline was selected because it was especially developed for analysis of drugs. The guide and the following required validation parameters, selectivity, calibration range, linearity, limit of detection, limit of quantification, inter- and intraday accuracy and precision, and robustness, were described. The method was inexpensive, fast, simple, environmentally friendly, and useful for routine analysis. The methodology was successfully validated and applied to commercial pharmaceutical formulations and spiked blank serum samples.

  10. Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine.

    Science.gov (United States)

    Wang, Xue Yan; Lim-Jurado, Margaret; Prepageran, Narayanan; Tantilipikorn, Pongsakorn; Wang, De Yun

    2016-01-01

    Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug's safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily). The fourfold higher than standard dose is specified as an acceptable second-line treatment option for urticaria in international guidelines. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity. Based on its pharmacokinetic properties, efficacy, and tolerability profile, bilastine will be valuable in the management of allergic rhinitis and urticaria.

  11. 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

  12. First-Generation H1 Antihistamines Found in Pilot Fatalities of Civil Aviation Accidents, 1990-2005

    Science.gov (United States)

    2007-05-01

    their pharmaceutical formulations and preparations, they are also marketed as prescription drugs . These FGH 1 AIs are available in various tablet...pain reduction, and/or surgical procedures. Whereas, other drugs —for example, antidepressants , cardiovascular agents, sympathomimetics, and even...while other drug (s) and/or ethanol were also present in an additional 235 fatalities. Thirty-five of the 338 fatalities had more than 1 antihistamine

  13. Effect of Disodium Cromoglycate (DSCG) and Antihistamines on Postirradiation Cerebral Blood Flow and Plasma Levels of Histamine and Neurotensin

    Science.gov (United States)

    1988-01-01

    73 6 SOTI UNCLASIFIE ESCURIIY CLASSIFICATION OF Tm-S siki FUNDAMENTAL AND APPLIED TOXICOLOGY 10, 233-242 (1988) Effect of Disodium Cromoglycate (DSCG...given the mast cell stabilizer disodium cromoglycate and the antihistamines mepyramine and cimetidine before Irradiation did not exhibit an abrupt...occur ment with the mast cell stabilizer, disodium with equal frequency in all species, having cromoglycate (DSCG, cromolyn sodium), in- been reported

  14. Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects

    OpenAIRE

    Togawa, Michinori; Yamaya, Hidetoshi; Rodríguez, Mónica; Nagashima, Hirotaka

    2016-01-01

    Background and objectives Bilastine is a novel second-generation antihistamine for the symptomatic treatment of allergic rhinitis and urticaria. The objective of this study was to evaluate the pharmacokinetics, pharmacodynamics, and tolerability of bilastine following single and multiple oral doses in healthy Japanese subjects. The pharmacokinetic and pharmacodynamic profiles were compared with those reported in Caucasian subjects. Methods In a single-blind, randomized, placebo-controlled, pa...

  15. P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec), a second-generation non-sedating antihistamine.

    Science.gov (United States)

    Polli, Joseph W; Baughman, Todd M; Humphreys, Joan E; Jordan, Kelly H; Mote, Angela L; Salisbury, Jo A; Tippin, Timothy K; Serabjit-Singh, Cosette J

    2003-10-01

    Recent in vitro studies have suggested that P-glycoprotein (Pgp) and passive membrane permeability may influence the brain concentrations of non-sedating (second-generation) antihistamines. The purpose of this study was to determine the importance of Pgp-mediated efflux on the in vivo brain distribution of the non-sedating antihistamine cetirizine (Zyrtec), and the structurally related sedating (first-generation) antihistamine hydroxyzine (Atarax). In vitro MDR1-MDCKII monolayer efflux assays demonstrated that cetirizine was a Pgp substrate (B-->A/A-->B + GF120918 ratio = 5.47) with low/moderate passive permeability (PappB-->A = 56.5 nm/s). In vivo, the cetirizine brain-to-free plasma concentration ratios (0.367 to 4.30) were 2.3- to 8.7-fold higher in Pgp-deficient mice compared with wild-type mice. In contrast, hydroxyzine was not a Pgp substrate in vitro (B-->A/A-->B ratio = 0.86), had high passive permeability (PappB-->A + GF120918 = 296 nm/s), and had brain-to-free plasma concentration ratios >73 in both Pgp-deficient and wild-type mice. These studies demonstrate that Pgp-mediated efflux and passive permeability contribute to the low cetirizine brain concentrations in mice and that these properties account for the differences in the sedation side-effect profiles of cetirizine and hydroxyzine.

  16. In vitro antihistamine-releasing activity of a peptide derived from wasp venom of Vespa orientalis

    Institute of Scientific and Technical Information of China (English)

    Jafar Jalaei; Mehdi Fazeli; Hamid Rajaian; Somayeh Layeghi Ghalehsoukhteh; Alireza Dehghani; Dominic Winter

    2016-01-01

    Objective: To investigate the antihistamine-releasing effect of a peptide isolated from wasp venom of Vespa orientalis.Methods: This peptide was separated from crude venom by chromatography methods and mass spectrometry. Then various concentrations(2, 4, 8, 16, 32, 64, 128 and256 mmol/L) of the peptide were incubated with mast cells and lactate dehydrogenase assay was performed.Results: No significant effect was observed in lactate dehydrogenase absorbance under128 mmol/L concentration. This implied that the peptide did not cause cell death in mast cells and consequently, histamine release did not happen. Moreover, the results showed the IC50 of mast cells degranulation at 126 mmol/L, which was approximately high implying that this peptide had high selectivity for normal cells and did not cause histamine release from these cells.Conclusions: This would be a great aim in new drug development, in which an agent acts potentially on its target tissue without activating the immune system.

  17. EFFICACY OF ANTIHISTAMINE AGENTS ON MODEL FOR EXERCISE-INDUCED ASTHMA IN GUINEA PIGS

    Institute of Scientific and Technical Information of China (English)

    TAO Meng-Fei; REN Tao; LIANG Yong-Jie

    2006-01-01

    Objective To investigate the effects of antihistamine agents, loratadine and ketotifen, on the model of exercise-induced asthma in guinea pigs with lipopolysaccharide ( LPS) and metyapone. Methods Nineteen guinea pigs were injected peritoneolly with LPS (1mg/kg, i. p. ) and metyapone ( 50mg/kg, i. p. ). Then they were randomized into 3 groups. The control group ( n =7) did not take any drug, ketotifen group ( n =6) adminisd-1 ) for 4 days. On the fifth day, lung resistance (RL) and dynamic compliance of respiratory system (Cdyn) of 3 groups were measured before and after exercise challenge. The total number of leukocytes in bronchoalveolar lavage fluid (BALF) from 3 groups was counted and differentiated cell type count was measured. Morphometric examination of the animal lungs was performed. Results In control group, RLincreased and Cdyn decreased significantly after exercise challenge. In ketotifen group and loratadine group with no change. There was a significant increase in the number of neutrophils, macrophages and eosinophils in BALF from control group. The infiltration of neutrophils in the bronchial mucosa was shown in control group in the morphometric study. Conclusion Loratadine and ketotifen can inhibit the exercise-indaced bronchoconstriction in guinea pigs pretreated with LPS and metyrapone. Inhibiting the formation of inflammation in airway may be the therapeutic mechanism of these H-1 receptor antagonists.

  18. EVALUATION OF ANTIMICROBIAL AND ANTI-HISTAMINE ACTIVITY OF THE AERIAL PARTS OF TEPHROSIA PURPUREA L.

    Directory of Open Access Journals (Sweden)

    Duraisami Nivedithadevi

    2012-03-01

    Full Text Available Tephrosia purpurea (Fabaceae has been used as a medicinal plant in all over India. This plant is a much branched perennial herb. Roots are given orally against any type of poisoning such as snakebite and the aerial parts were used for hydrophobia, asthma, cough, heart disease and kidney problems. Anti-microbial activity of 50% alcoholic extract with different concentrations were tested against the fungal strains like Aspergillus fumigates, Aspergillus niger, Ganoderma lucida and Candida albicans and bacterial organisms like Escherichia coli, Serratia mercescens, Staphylococcus aureus and Staphylococcus epidermis. The 50% alcoholic extract of Tephrosia purpurea at 5mg, 10mg, and 20mg concentration showed antibacterial activity against Escherichia coli, Serratia marcescens and Staphylococcus. Extracts of Tephrosia purpurea at 5mg, 10mg, and 20mg concentration did not show positive antifungal activities against Aspergillus fumigates, Aspergillus niger, Ganoderma lucida and Candida albicans. Antihistamine activity of 50% alcohol extract of Tephrosia purpurea (TP was evaluated in isolated guinea pig ileum. It was observed that different concentrations (2mg, 4mg and 8mg/ml of TP extract antagonized the contraction of ileum induced by histamine. The extracts at 8mg/ml concentration expected maximum antagonistic. The results obtained with histamine in guinea-pig isolated ileum preparations are sensitive to histamine against like histamine at the lower concentration.

  19. 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.

  20. 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.

  1. 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.

  2. 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.

  3. Interactions of bilastine, a new oral H₁ antihistamine, with human transporter systems.

    Science.gov (United States)

    Lucero, Maria Luisa; Gonzalo, Ana; Ganza, Alvaro; Leal, Nerea; Soengas, Itziar; Ioja, Eniko; Gedey, Szilvia; Jahic, Mirza; Bednarczyk, Dallas

    2012-06-01

    Membrane transporters play a significant role in facilitating transmembrane drug movement. For new pharmacological agents, it is important to evaluate potential interactions (e.g., substrate specificity and/or inhibition) with human transporters that may affect their pharmacokinetics, efficacy, or toxicity. Bilastine is a new nonsedating H₁ antihistamine indicated for the treatment of allergic rhinoconjunctivitis and urticaria. The in vitro inhibitory effects of bilastine were assessed on 12 human transporters: four efflux [multidrug resistance protein 1 (MDR1) or P-glycoprotein, breast cancer resistance protein (BCRP), multidrug resistance associated protein 2 (MRP2), and bile salt export pump) and eight uptake transporters (sodium taurocholate cotransporting polypeptide, organic cation transporter (OCT)1, organic anion transporter (OAT)1, OAT3, OCT2, OATP2B1, OATP1B1, and OATP1B3). Only mild inhibition was found for MDR1-, OCT1-, and OATP2B1-mediated transport of probe substrates at the highest bilastine concentration assayed (300 μM; half-maximal inhibitory concentration: ≥300 μM). Bilastine transport by MDR1, BCRP, OAT1, OAT3, and OCT2 was also investigated in vitro. Only MDR1 active transport of bilastine was relevant, whereas it did not appear to be a substrate of OCT2, OAT1, or OAT3, nor was it transported substantially by BCRP. Drug-drug interactions resulting from bilastine inhibition of drug transporters that would be generally regarded as clinically relevant are unlikely. Additionally, bilastine did not appear to be a substrate of human BCRP, OAT1, OAT3, or OCT2 and thus is not a potential victim of inhibitors of these transporters. On the other hand, based on in vitro evaluation, clinically relevant interactions with MDR1 inhibitors are anticipated.

  4. 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.

  5. Application of antihistamines in special populations%抗组胺药在特殊人群中的应用

    Institute of Scientific and Technical Information of China (English)

    温禾; 姚煦

    2016-01-01

    抗组胺药物是皮肤科治疗过敏性疾病最常见的药物之一,在大部分人群中有着较好的疗效及耐受性.由于其适用范围广泛,安全性显得尤为重要.对于儿童、孕妇、哺乳期妇女、老年人以及肝、肾功能不全的过敏性疾病患者,应用抗组胺药时应充分考虑每一种药物的药效学、代谢特点以及药物之间的相互作用,权衡用药收益和可能带来的不良反应,选择相应的安全性高的抗组胺药物,或者通过减少常规用药剂量、延长用药间隔时间等方法使安全性达到最大.%Antihistamines,a group of drugs most commonly used for the treatment of allergic diseases in dermatology,exert favorable efficacy and are well tolerated in most people.Due to their wide application,the safety of medication is particularly important.When they are used in some special populations with allergic diseases,such as children,pregnant and lactating women,the elderly and people with hepatic or renal insufficiency,their pharmacodynamics,metabolic characteristics and interactions with other drugs should be fully considered,and profits of medication and potential adverse effects should be well weighed before choosing relatively safe antihistamines.In addition,decreasing the routine dose or prolonging intervals between the administration of antihistamines may also be attempted to achieve maximum safety.

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

    Directory of Open Access Journals (Sweden)

    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

  7. 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....... 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 (Purticaria activity score over 7...

  8. 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.

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

    Directory of Open Access Journals (Sweden)

    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

  10. 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.

  11. A clinical study to evaluate the efficacy of the antihistamine doxylamine succinate in the relief of runny nose and sneezing associated with upper respiratory tract infection.

    Science.gov (United States)

    Eccles, R; Van Cauwenberge, P; Tetzloff, W; Borum, P

    1995-12-01

    Antihistamines are widely used in common cold medications, although the role of histamine in the development of common cold symptoms is unclear and the use of antihistamines for the treatment of common cold is controversial. It is clear that antihistamines do not offer a cure for common cold but they may alleviate symptoms of sneezing and runny nose. The present study was designed to investigate the efficacy of an antihistamine, doxylamine, on the symptoms of runny nose and sneezing associated with common cold. We conducted a randomized double-blind study in cold sufferers. One thousand and one volunteers with cold symptoms were screened in four centres (UK, Denmark, Belgium, Germany) and 688 satisfied the entry criteria of the study. The main reasons for excluding subjects were a low nasal secretion weight (secretion weight doxylamine succinate 7.5 mg by mouth four times a day up to nine doses (n = 345) or placebo (n = 343). The principal measurements were prospectively defined as runny nose and sneezing symptom scores. Data were analysed on an intention-to-treat basis, using Cochran-Mantel-Haenszel statistics controlling for baseline symptom scores. A between-group comparison showed that doxylamine-treated volunteers benefited from a significantly greater reduction in runny nose scores (P Doxylamine therapy was well tolerated; the incidence of unexpected side-effects was comparable with placebo. Of the expected side-effects, 13.3% of doxylamine-treated patients reported drowsiness. The incidence of sedative effects was lower than has been reported for other commonly used first-generation antihistamines.

  12. 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)

  13. 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.

  14. Seasonal changes in antibiotics, antidepressants/psychiatric drugs, antihistamines and lipid regulators in a wastewater treatment plant.

    Science.gov (United States)

    Golovko, Oksana; Kumar, Vimal; Fedorova, Ganna; Randak, Tomas; Grabic, Roman

    2014-09-01

    Seasonal changes in the concentration of 21 pharmaceuticals in a wastewater treatment plant (WWTP) in České Budějovice were investigated over 12months. The target compounds were 10 antibiotics, 4 antidepressants, 3 psychiatric drugs, 2 antihistamines and 2 lipid regulators. 272 Wastewater samples (136 influents and 136 effluents) were collected from March 2011 to February 2012 and analyzed using two-dimensional liquid chromatography coupled with tandem mass spectrometry. All studied pharmaceuticals were frequently detected in both the influent and the effluent wastewater samples, except for meclozine, which was only found in the influent. The mean concentration of pharmaceuticals varied from 0.006μgL(-1) to 1.48μgL(-1) in the influent and from 0.003μgL(-1) to 0.93μgL(-1) in the effluent. The concentration of most pharmaceuticals was higher during winter.

  15. Square-Wave Voltammetric Determination of Antihistaminic Drug Hydroxyzine in Pharmaceuticals Using a Boron-doped Diamond Electrode

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    Jessica Scremin

    2016-07-01

    Full Text Available The determination of antihistaminic hydroxyzine using square-wave voltammetry and a cathodically pretreated boron-doped diamond electrode is described. The obtained analytical curve was linear in the hydroxyzine concentration range 0.50 – 20.0 mmol L–1 in 0.1 mol L–1 HCl solution, with a detection limit of 0.43 mmol L–1. Addition and recovery studies in commercial tables and liquid formulations showed excellent recovery values ranging from 94.3 % to 104 %. Furthermore, the proposed method was successfully applied in the determination of hydroxyzine in several pharmaceutical formulations and the results were in a close agreement at a 95 % confidence level with those obtained using an official potentiometric method. DOI: http://dx.doi.org/10.17807/orbital.v8i3.833

  16. Quantitation of antihistamines in pharmaceutical preparations by liquid chromatography with a micellar mobile phase of sodium dodecyl sulfate and pentanol.

    Science.gov (United States)

    Gil-Agustí, M; Monferrer-Pons, L; Esteve-Romero, J; García-Alvarez-Coque, M C

    2001-01-01

    A reversed-phase liquid chromatographic procedure with a micellar mobile phase of sodium dodecyl sulfate (SDS), containing a small amount of pentanol, was developed for the control of 7 antihistamines of diverse action in pharmaceutical preparations (tablets, capsules, powders, solutions, and syrups): azatadine, carbinoxamine, cyclizine, cyproheptadine, diphenhydramine, doxylamine, and tripelennamine. The retention times of the drugs were <9 min with a mobile phase of 0.15M SDS-6% (v/v) pentanol. The recoveries with respect to the declared compositions were in the range of 93-110%, and the intra- and interday repeatabilities and interday reproducibility were <1.2%. The results were similar to those obtained with a conventional 60 + 40 (v/v) methanol-water mixture, with the advantage of reduced toxicity, flammability, environmental impact, and cost of the micellar-pentanol solutions. The lower risk of evaporation of the organic solvent dissolved in the micellar solutions also increased the stability of the mobile phase.

  17. 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

  18. Effects of anti-histamine treatment on liver injury triggered by small intestinal ischemia reperfusion in rats.

    Science.gov (United States)

    Huang, Pin-Jie; Gan, Xiao-Liang; Liu, Jian-Pei; Liu, De-Zhao; Wang, Yan-Ling; Hei, Zi-Qing

    2014-10-31

    Mast cell (MC) degranulation has been implicated in small intestinal ischemia reperfusion (IIR) injury, therein, inhibiting overproduction of histamine released from activated MC may provide promising strategies against IIR-mediated liver injuries. The aim of the present study was to explore whether anti-histamine treatment contribute to attenuating IIR-mediated liver injury. Adult SD rats were randomized into sham-operated group (S group), sole IIR group (IIR group), and IIR treated with Ketotifen, a histamine antagonist (IIR+K group), Cromolyn Sodium, a MC stabilizer (IIR+C group), and Compound 48/80, a MC degranulator (IIR+CP group), respectively. IIR was induced by superior mesenteric artery occlusion for 75 min followed by 4 h of reperfusion. The agents were intravenously administrated 5 min before reperfusion to induce different levels of histamine. Subsequently, serum concentrations of ALT, AST and histamine; levels of LDH,TNF-α, IL-8 and MDA as well as SOD activities in the liver were assessed. Histopathologic changes were also evaluated. IIR resulted in severe liver injury as demonstrated by significant increases in injury scores, with concomitant significant increases in serum ALT, AST and histamine levels, as well as LDH, TNF-α, IL-8, and MDA levels in the liver, accompanied by reduction in SOD activities (all P IIR vs. S). Treatments by Ketotifen and Cromolyn Sodium similarly markedly alleviated IIR-mediated liver injury as confirmed by significant reduction of the above biomedical changes whereas Compound 48/80 further aggravated IIR-mediated liver injury by dramatically enhancing the above biomedical changes. Data of our study suggest that anti-histamine treatments may provide promising benefits in alleviating liver injury triggered by IIR.

  19. 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.

    Science.gov (United States)

    Gesualdo, Francesco; Stilo, Giovanni; D'Ambrosio, Angelo; Carloni, Emanuela; Pandolfi, Elisabetta; Velardi, Paola; Fiocchi, Alessandro; Tozzi, Alberto E

    2015-01-01

    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.

  20. 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.

  1. 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

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    Shokrollah Farrokhi

    2010-12-01

    Full Text Available 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.

  2. 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.

  3. The antihistamines clemastine and desloratadine inhibit STAT3 and c-Myc activities and induce apoptosis in cutaneous T-cell lymphoma cell lines.

    Science.gov (United States)

    Döbbeling, Udo; Waeckerle-Men, Ying; Zabel, Franziska; Graf, Nicole; Kündig, Thomas M; Johansen, Pål

    2013-02-01

    Mycosis fungoides and its leukaemic counterpart Sézary syndrome are the most frequent cutaneous T-cell lymphomas (CTCL), and there is no cure for these diseases. We evaluated the effect of clinically approved antihistamines on the growth of CTCL cell lines. CTCL cell lines as well as blood lymphocytes from patients with Sézary syndrome were cultured with antihistamines, and the cell were analysed for proliferation, apoptosis and expression of programmed death molecules and transcription factors. The two antihistamines clemastine and desloratadine, currently used for symptom alleviation in allergy, induced potent reduction of the activities of the constitutively active transcription factors c-Myc, STAT3, STAT5a and STAT5b in mycosis fungoides and Sézary syndrome cell lines. This inhibition was followed by apoptosis and cell death, especially in the Sézary syndrome-derived cell line Hut78 that also showed increased expression of the programmed death-1 (PD-1) after clemastine treatment. In lymphocytes isolated from Sézary syndrome patients, the CD4-positive fraction underwent apoptosis after clemastine treatment, while CD4-negative lymphocytes were little affected. Because both c-Myc and STAT transcription factors are highly expressed in proliferating tumours, their inhibition by clemastine, desloratadine and other inhibitors could complement established chemotherapies not only for cutaneous T-cell lymphomas but perhaps also other cancers.

  4. 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.

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

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    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.

  6. 2008-2011年我院口服抗组胺药利用分析%Utilization analysis of oral antihistamines in our hospital from 2008 to 2011

    Institute of Scientific and Technical Information of China (English)

    黄蔚; 郭燕萍; 陈妙英; 王斌; 钟明康

    2012-01-01

    AIM To evaluate the utilization status and development tendency of oral antihistamines in our hospital. METHODS Data about clinical application of oral antihistamines in our hospital during 2008 to 2011 were analyzed statistically in terms of drug varieties, consumption sum and DDDs. RESULTS The consumption sum of oral antihistamines was decreased year by year. The consumption of 2nd generation oral antihistamine and improved 2nd generation oral antihistamine was far greater than the first generation, accounting for more than 96% of the total. Cetirizine and lev-ocetirizine had been at the first two DDDs sort,and mizolastine up to three. CONCLUSION The 2nd generation oral antihistamine and improved 2nd generation oral antihistamine have become the dominant antiallergic drugs due to their advantages of safety, high efficacy and less interaction with other drugs. The choice of antihistamines is in line with rational drug use in our hospital. The study on modified dosage form of the traditional antihistamines and the antihistamines with more reliable safety remains to be done.%目的 评价我院口服抗组胺药应用情况及趋势.方法 对我院2008-2011年口服抗组胺药应用品种、用药金额、用药频度(DDDs)等进行统计、分析.结果 我院口服抗组胺药用药金额逐年下降.第2代口服抗组胺药及其改良品种的使用最远远大于第1代,占到总额的96%以上.2008-2011年西替利嗪和左西替利嗪一直位于DDDs排序的前2位,咪唑斯汀由2008年第5位上升至2011年第3位.结论 我院主要选择安全、高效、与其他药物相互作用少的第2代口服抗组胺药及其改良品种作为抗过敏治疗的主导药物,符合临床合理用药的要求.传统抗组胺药的改良剂型以及安全性更可靠的抗组胺药是研究方向.

  7. Utility of NBD-Cl for the spectrophotometric determination of some skeletal muscle relaxant and antihistaminic drugs

    Science.gov (United States)

    Saleh, Hanaa M.; EL-Henawee, Magda M.; Ragab, Gamal H.; El-Hay, Soad S. Abd

    2007-08-01

    A simple, accurate, precise and sensitive colorimetric method for the determination of some skeletal muscle relaxant drugs, namely orphenadrine citrate ( I), baclofen ( II), antihistaminic drugs as acrivastine ( III) and fexofenadine hydrochloride ( IV) is described. This method is based on the formation of charge transfer complex with 4-chloro-7-nitro-2,1,3-benzoxadiazole (NBD-Cl) in non-aqueous medium. The orange color products were measured at 472, 465, 475 and 469 nm for drugs I, II, III and IV, respectively. The optimization of various experimental conditions was described. Beer's Law was obeyed in the range (2.5-17.5), (5-70), (2.5-25) and (10-50) μg/ml for drugs I, II, III and IV, respectively. The molar absorptivity ( ɛ), sandell sensitivity, detection (LOD) and quantitation limits (LOQ) are calculated. The procedure was favorably applied for determination of certain pharmaceutical dosage forms containing the studied drugs. The obtained results were compared with the official and reported methods. There were no significant differences between proposed, reported and the official methods.

  8. Use of Oral Antihistamine Agents in Beijing, Shanghai and Guangzhou in 2013%2013年北京、上海、广州地区医院口服抗组胺药应用分析

    Institute of Scientific and Technical Information of China (English)

    曹媛; 罗美娟; 邓蓉蓉; 夏延哲

    2014-01-01

    目的:了解2013年北京、上海和广州地区医院口服抗组胺药的应用情况,促进合理用药。方法:采用《医院处方分析》课题数据库,调查2013年北京、上海、广州地区医院口服抗组胺药的用药频度( DDDs )、限定日费用( DDC )、销售总金额、排序比( B/A)、药物利用指数( DUI)以及各代口服抗组胺药处方数和取药数量占比,并进行回顾性统计、分析。结果:2013年北京、上海和广州地区医院口服抗组胺药使用频率和销售总额排序居首位的分别为西替利嗪、左西替利嗪和地氯雷他定;抗组胺药的DUI均≤1;应用最多的抗组胺药为第2代抗组胺药。结论:北京、上海和广州地区医院使用口服抗组胺药较合理,第2代抗组胺药成为临床上治疗过敏性疾病的常用药物。%OBJECTIVE:To investigate the use of antihistamine agents of in Beijing, Shanghai and Guangzhou in 2013 and its rationality. METHODS:The use of antihistamine agents of in Beijing, Shanghai and Guangzhou in 2013 was investigated retrospectively in respect of DDDs, daily drug cost(DDC), consumption sum, order ratio, drug utilization index( DUI) and the ratio of the number of prescriptions to consumption quantity of antihistamine agents by taking the Project of Hospital Prescription Analysis. RESULTS:The leading antihistamine agents in terms of DDDs and consumption sum in Beijing, Shanghai and Guangzhou in 2013 were Cetirizine, Levocetirizine and Desloratadine respectively. The DUIs of antihistamine agents were all less than 1. The second generation antihistamines were the most frequently used antihistamines. CONCLUSIONS:The use of antihistamine agents in Beijing, Shanghai and Guangzhou was rational and the second generation of antihistamine agents have become the common medications for allergic reactions.

  9. 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.

  10. 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.

  11. 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

    Directory of Open Access Journals (Sweden)

    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.

  12. 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.

  13. 第二代抗组胺药物的种类及应用策略%Types and application strategy of the second-generation antihistamines

    Institute of Scientific and Technical Information of China (English)

    吴建华

    2012-01-01

    The second-generation antihistamines possess different structures and types, with various efficacy and metabolic characteristics. For allergic diseases of different degrees, either an increased dosage or a combination of different drugs could be used in the treatment. For patients with chronic allergic diseases, gradual withdrawal of drugs generally follows a pattern in top-down order, e. g. from medication every other day to intermittent medication. In case of children, pregnant women, lacta-tional women, hepatic or renal insufficiency patients with allergic diseases, relatively safer antihistamines should be chosen.%第二代抗组胺药结构和种类不同,药效和代谢特点各不相同.对于不同程度的过敏性疾病可采用加大剂量或联合用药的方法治疗;对于慢性过敏性疾病,一般采用隔日服药至间断服药等降阶梯方式逐渐停药;对于儿童,孕妇,哺乳期妇女,肝、肾功能不全的过敏性疾病病人,应该选择相应的安全性高的抗组胺药.

  14. Computational Evaluation of 2-Phenyl-4H-chromen-4-one Analogues as Antihistamines: Potential Histamine N-Methyltransferase (HMT Inhibitors

    Directory of Open Access Journals (Sweden)

    Shikha S. Dave

    2009-01-01

    Full Text Available Abnormal release of histamine, which is present in relatively high concentration in the lungs, causes serious allergic vasoconstriction and anaphylactic manifestation in human beings. In mammals, a major pathway of histamine metabolism in the lungs is mediated by histamine N-methyl transferase (HMT and diamine oxidase. The need to design a strategy of mechanistic computational evaluation of protein-ligand affinity i.e. HMT- 2-phenyl-4H-chromen-4-ones, protein complex binding energy has been established. A library of synthesized 2-phenyl-4H-chromen-4-ones was docked into the active site cavity of target protein, HMT (Pdb: 2aot. The high-resolution crystal structure of HMT complex with the competitive inhibitor N [2 (benzhydryloxyethyl] N N-Dimethylamine (Diphenhydramine revealed a protein with a highly confined binding region that could be targeted in the design of specific anti-histamines. The validation of docking programme by Potential Mean Force was compared with binding energy results of known ligands in the active sites of HMT, diphenhydramine / benadryl, promethazine, cyproheptadine, trimeton / avil etc. All the synthesized chromone derivatives showed comparable negative binding energies pointing towards the fact that these molecules could be potent antihistamines.

  15. 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.

  16. 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 ...

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

    Directory of Open Access Journals (Sweden)

    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

  18. 宜宾市第一人民医院2008~2010年抗组胺药应用分析%Analysis of antihistamine drugs used in the First People's Hospital of Yibin from 2008 to 2010

    Institute of Scientific and Technical Information of China (English)

    赵大贵

    2012-01-01

    目的 分析我院抗组胺药的应用状况和发展趋势.方法 采用金额排序和应用频度分析法对我院2008~2010年度抗组胺药的使用情况进行统计分析.结果 2008~2010年我院抗组胺药销售金额和用药频度(DDDs)逐年上升,DDDs排序前3位依次是左西替利嗪、依巴斯汀、咪唑斯汀,占抗组胺药销售总额的80%以上.用药金额2009年较2008年增长45.09%,2010年较2009年增长12.50%.结论 安全、高效的第二、三代抗组胺药成为我院抗过敏治疗的主要药物.%Objective To study the current situation and future trend of antihistamine drugs in our hospital. Methods According to the order of sales amount and DDDs,the medication of antihistamine drugs used in our hospital from 2008 to 2010 was analyzed. Results Sales amount and drug use frequency of antihistamine drugs rose year by year from 2008 to 2010. Drugs with the top 3 DDDs were Levocetirizine Hydrochloride, Ebastine and Mizolastine respectively. The sales amount of the 3 drugs accounted for more than 80% of total sales of antihistamine drugs. The sales amount of medicine increased by 45. 09% from 2008 to 2009, and that increased by 12. 50% from 2009 to 2010. Conclusion The second and third generation antihistamine drugs are expected to become the dominant anti-allergic medicines in our hospital in virtue of their safety and efficacy.

  19. 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

  20. Analysis of combined use of oral Antihistamines with orhter medicines%我院口服抗组胺药物与其他药物联合应用分析

    Institute of Scientific and Technical Information of China (English)

    车斌; 郭晶

    2009-01-01

    Objective To observe combined use of antihistamines on the treatment of allergy-related and itch dermatoses. Methods H1-R antagonists combined with other anti-inflammatory drug were use for OPD from July 2007 to June 2008. Results The combined use of H1-R antagonists, corticosteroids,first -generation and second-generation antihistamines of combined use were mostly used and single-use antihistamines were only 8.44%. Conclusion The combined use of antihistamines prevents allergy-related and itch dermatoses.%目的 探讨抗组胺药物的联合应用在治疗变态反应相关性皮肤病及瘙痒性皮肤病中的机制.方法 采用我院门诊日处方查询系统,分析我院2007年7月至2008年6月每月的第一个星期一门诊处方中,H1受体(H1-R)拮抗剂与其他抗炎性反应介质药物的联合使用情况.结果 我院H1-R拮抗剂与肾上腺皮质激素、第一代与第二代H1-R拮抗剂联合应用的情况较多,单用H1-R拮抗剂只占我院口服抗组胺药物处方中的8.44%.结论 口服抗组胺药物的联合应用,对变态反应相关性皮肤病及瘙痒性皮肤病有早期干预作用,可以阻止炎性级联反应的发展.

  1. 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.

  2. Thin layer chromatography-densitometric determination of some non-sedating antihistamines in combination with pseudoephedrine or acetaminophen in synthetic mixtures and in pharmaceutical formulations.

    Science.gov (United States)

    El-Kommos, Michael E; El-Gizawy, Samia M; Atia, Noha N; Hosny, Noha M

    2014-03-01

    The combination of certain non-sedating antihistamines (NSA) such as fexofenadine (FXD), ketotifen (KET) and loratadine (LOR) with pseudoephedrine (PSE) or acetaminophen (ACE) is widely used in the treatment of allergic rhinitis, conjunctivitis and chronic urticaria. A rapid, simple, selective and precise densitometric method was developed and validated for simultaneous estimation of six synthetic binary mixtures and their pharmaceutical dosage forms. The method employed thin layer chromatography aluminum plates precoated with silica gel G 60 F254 as the stationary phase. The mobile phases chosen for development gave compact bands for the mixtures FXD-PSE (I), KET-PSE (II), LOR-PSE (III), FXD-ACE (IV), KET-ACE (V) and LOR-ACE (VI) [Retardation factor (Rf ) values were (0.20, 0.32), (0.69, 0.34), (0.79, 0.13), (0.36, 0.70), (0.51, 0.30) and (0.76, 0.26), respectively]. Spectrodensitometric scanning integration was performed at 217, 218, 218, 233, 272 and 251 nm for the mixtures I-VI, respectively. The linear regression data for the calibration plots showed an excellent linear relationship. The method was validated for precision, accuracy, robustness and recovery. Limits of detection and quantitation were calculated. Statistical analysis proved that the method is reproducible and selective for the simultaneous estimation of these binary mixtures.

  3. Assessment of cetirizine, an antihistamine, to prevent cutaneous reactions to nevirapine therapy: results of the viramune-zyrtec double-blind, placebo-controlled trial.

    Science.gov (United States)

    Launay, O; Roudière, L; Boukli, N; Dupont, B; Prévoteau du Clary, F; Patey, O; David, F; Lortholary, O; Devidas, A; Piketty, C; Rey, E; Urbinelli, R; Allaert, F A; Tréluyer, J M; Caumes, E

    2004-04-15

    We conducted a 12-week, multicenter, randomized, double-blind, placebo-controlled trial of cetirizine to assess the ability of antihistamines to prevent nevirapine-associated rash in patients infected with human immunodeficiency virus type 1. Patients initiating treatment with nevirapine were randomized to receive either cetirizine, 10 mg q.d. (104 patients), or placebo (96 patients) during the first 6 weeks of therapy. Rash occurred in 22 (11%) of 200 patients; 10 (9.6%) were in the cetirizine group and 12 (12.5%) were in the placebo group (odds ratio [OR], 0.75; 95% confidence interval [CI], 0.31-1.81; P=.5). Five of 22 rashes were cases of hypersensitivity syndrome. The rate of nevirapine discontinuation due to rash was similar in the 2 groups (7.7% and 6.25% in the cetirizine and placebo groups, respectively; P=.4). Multivariate analysis showed no treatment-group effect but indicated that age >40 years (OR, 3.83; 95% CI, 1.4-10.46; P=.008) was associated with an increased risk of rash. Cetirizine has no preventive effect on nevirapine-associated rash.

  4. 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.

  5. 抗组胺药非索非那定的研究进展%Research progress of the anti-histamine drug fexofenadine

    Institute of Scientific and Technical Information of China (English)

    杨云; 颜耀东; 刘茵; 马长勇

    2012-01-01

    非索非那定是第二代H1抗组胺药,对H1受体有高度选择性,有直接的抗炎活性,起效快、作用维持时间长且长期使用不易出现耐药性.非索非那定的代谢动力学易受几种转运蛋白诱导剂或抑制剂的影响,但未见需调整剂量的报道,转运蛋白对非索非那定代谢的机理有待进一步的研究.临床用于治疗变态反应性疾病,如过敏性鼻炎、荨麻疹、过敏性哮喘、遗传性过敏性斑秃等,且联合其他药物疗效显著.目前,非索非那定微球的鼻内给药制剂正在研发中.非索非那定不良反应少见,无论是单独应用还是联合其他药物使用,都未见严重的心血管事件,不影响胆碱能活性.非索非那定不能透过血脑屏障、不进入中枢神经系统,被推荐于从事安全相关作业人员使用.%Fexofenadine is a second-generation H,-antihistamine with a high selectivity to H, receptor, direct anti-inflammatory effect, rapid onset, long-acting activities, and no tolerance even applied after a long time. The pharmacokinetics can be changed by several transport proteins which was induced or depressed by other drugs, but there was no report about changing the doses. The mechanism affected by transport proteins needs to be further researched. It is used for allergic disease, such as allergic rhinitis, urticaria, allergic asthma, atopic alopecia areata and so on and the effectiveness is better when co-administered with other drugs. The microspheres for intranasal delivery of fexofenadine hydrochloride with quick-acting is in development. The adverse reactions are rare. Fexofenadine does not have any major cardiovascular side effects either administered alone or co-administered with other drugs. It has no effect on the cholinergic activities. Fexofenadine can not permeate the CNS through blood brain barrier and is recommended to use in safety-critical filed patients.

  6. Development and validation of a rapid stability indicating HPLC-method using monolithic stationary phase and two spectrophotometric methods for determination of antihistaminic acrivastine in capsules

    Science.gov (United States)

    Gouda, Ayman A.; Hashem, Hisham; Jira, Thomas

    2014-09-01

    Simple, rapid and accurate high performance liquid chromatographic (HPLC) and spectrophotometric methods are described for determination of antihistaminic acrivastine in capsules. The first method (method A) is based on accurate, sensitive and stability indicating chromatographic separation method. Chromolith® Performance RP-18e column, a relatively new packing material consisting of monolithic rods of highly porous silica, was used as stationary phase applying isocratic binary mobile phase of ACN and 25 mM NaH2PO4 pH 4.0 in the ratio of 22.5:77.5 at flow rate of 5.0 mL/min and 40 °C. A diode array detector was used at 254 nm for detection. The elution time of acrivastine was found to be 2.080 ± 0.032. The second and third methods (methods B and C) are based on the oxidation of acrivastine with excess N-bromosuccinimide (NBS) and determination of the unconsumed NBS with, metol-sulphanilic acid (λmax: 520 nm) or amaranth dye (λmax: 530 nm). The reacted oxidant corresponds to the drug content. Beer’s law is obeyed over the concentration range 1.563-50, 2.0-20 and 1.0-10 μg mL-1 for methods A, B and C, respectively. The limits of detection and quantitation were 0.40, 0.292 and 0.113 μg mL-1 and 0.782, 0.973 and 0.376 μg mL-1 for methods A, B and C, respectively. The HPLC method was validated for system suitability, linearity, precision, limits of detection and quantitation, specificity, stability and robustness. Stability tests were done through exposure of the analyte solution for four different stress conditions and the results indicate no interference of degradants with HPLC-method. The proposed methods was favorably applied for determination of acrivastine in capsules formulation. Statistical comparison of the obtained results from the analysis of the studied drug to those of the reported method using t- and F-tests showed no significant difference between them.

  7. Controlled-release formulation of antihistamine based on cetirizine zinc-layered hydroxide nanocomposites and its effect on histamine release from basophilic leukemia (RBL-2H3 cells

    Directory of Open Access Journals (Sweden)

    Hussein Al Ali SH

    2012-07-01

    Full Text Available Samer Hasan Hussein Al Ali,1 Mothanna Al-Qubaisi,2 Mohd Zobir Hussein,1,3 Maznah Ismail,2,4 Zulkarnain Zainal,1 Muhammad Nazrul Hakim51Department of Chemistry, Faculty of Science, 2Laboratory of Molecular Biomedicine, Institute of Bioscience, 3Advanced Materials and Nanotechnology Laboratory, Institute of Advanced Technology (ITMA, 4Department of Nutrition and Dietetics, Faculty of Medicine and Health Science, Universiti Putra, Malaysia; 5Department of Biomedical Science, Faculty of Medicine and Health Science, Universiti Putra Malaysia, Selangor, MalaysiaAbstract: A controlled-release formulation of an antihistamine, cetirizine, was synthesized using zinc-layered hydroxide as the host and cetirizine as the guest. The resulting well-ordered nanolayered structure, a cetirizine nanocomposite "CETN," had a basal spacing of 33.9 Å, averaged from six harmonics observed from X-ray diffraction. The guest, cetirizine, was arranged in a horizontal bilayer between the zinc-layered hydroxide (ZLH inorganic interlayers. Fourier transform infrared spectroscopy studies indicated that the intercalation takes place without major change in the structure of the guest and that the thermal stability of the guest in the nanocomposites is markedly enhanced. The loading of the guest in the nanocomposites was estimated to be about 49.4% (w/w. The release study showed that about 96% of the guest could be released in 80 hours by phosphate buffer solution at pH 7.4 compared with about 97% in 73 hours at pH 4.8. It was found that release was governed by pseudo-second order kinetics. Release of histamine from rat basophilic leukemia cells was found to be more sensitive to the intercalated cetirizine in the CETN compared with its free counterpart, with inhibition of 56% and 29%, respectively, at 62.5 ng/mL. The cytotoxicity assay toward Chang liver cells line show the IC50 for CETN and ZLH are 617 and 670 µg/mL, respectively.Keywords: cetirizine hydrochloric acid

  8. 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

  9. 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.

  10. Synthesis and Antihistaminic Activity of Diarylmethylpiperazine Derivatives%二芳甲基哌嗪衍生物合成及其抗组胺活性的研究

    Institute of Scientific and Technical Information of China (English)

    邓娜; 尹卓; 汪濛

    2011-01-01

    Objective The diarylmethylpiperazine moiety as active group frequently existing in the structures of H1 receptor antagonists and chromone-2-carboxylic acid moiety as active structure existing in leukotriene receptor antagonists were spliced on the basis of isostere and mosaic theory, and a series of diarylmethylpiperazine derivatives were synthesized and their antihistaminic activities were explored. Methods The lydroxyl-substituted chromone2-carboxylic ester contained an aliphatic chain-linked to diarylmetlylpiperazine to produce diarylmethylpiperazine derivatives. The antihistaminic activities of diarylmethylpiperazine derivatives were measured. Results The structures of diarylmethylpiperazine derivatives were identified by MS and H NMR spectra.%目的 利用电子等排和拼合原理,选择H1受体拮抗剂的活性部分二芳甲基哌嗪与白三烯受体拮抗剂的活性结构色酮-2-羧酸拼接,设计合成二芳甲基哌嗪衍生物,并且考察其抗组胺活性.方法 以羟基取代的色酮-2-羧酸酯为母体,将羟基与二芳甲基哌嗪通过脂肪链相连,得二芳甲基哌嗪衍生物,并测定化合物的抗组胺活性.结果 目标化合物的组成和结构经质谱和核磁共振氢谱确认.

  11. Evaluation of Three Kinds of Antihistamines Curative Effect for the Treatment of Chronic Idiopathic Urticarial%评价3种抗组胺药治疗慢性特发性荨麻疹的疗效

    Institute of Scientific and Technical Information of China (English)

    陈海兵

    2015-01-01

    目的:评价3种抗组胺药治疗慢性特发性荨麻疹的疗效。方法选取于我院就诊的慢性特发性荨麻疹患者90例作为研究对象,随机分为三组,每组各30人,分别给予西替利嗪药物治疗、氯雷他定药物治疗、依巴斯丁药物治疗。结果第7天、14天、28天三组有效率为:氯雷他定组分别为70.00%、83.33%、93.33%;西替利嗪组分别为66.67%、86.67%、90.00%;依巴斯丁组分别为76.67%、86.67%、96.67%。结论三种抗组胺药物在临床治疗慢性特发荨麻疹上都具有较好的效果,具有临床应用价值。%Objective To evaluate three kinds of antihistamines curative effect for the treatment of chronic idiopathic urticaria. Methods 90 patients with chronic idiopathic urticaria were selected from our hospital as research object, randomly dividing into three groups (30 people a group). Cetirizine group was given cetirizine medication, loratadine group was given loratadine drug therapy, by buss butyl group was given by buss butyl drug therapy. Results 7 days, 14 days, the effective rate of 28 days three groups:loratadine group was 70.00%, 83.33%and 70.00%respectively. Cetirizine group was 66.67%, 86.67%and 66.67%respectively. By bass butyl group 76.67%, 86.67, 96.67, respectively. Conclusion The three kinds of antihistamines in clinical treatment of chronic idiopathic urticaria had good effect, had clinical application value.

  12. 固相萃取/高效液相色谱法测定化妆品中5种抗组胺药物残留%Determination of Five Antihistamine Residues in Cosmetics by SPE/HPLC

    Institute of Scientific and Technical Information of China (English)

    车文军; 张征; 徐春祥; 王莉; 卢剑; 王燕芹; 邹洁; 武中平

    2012-01-01

    建立了固相萃取/高效液相色谱( SPE/HPLC)测定化妆品中5种抗组胺药物(多西拉敏、曲吡那敏、溴苯那敏、苯海拉明、氯苯沙明)残留的分析方法.试样经三氯乙酸溶液超声提取,PCX柱净化后,以甲醇-磷酸盐缓冲溶液为流动相,经C18柱分离后进行HPLC检测.5种抗组胺药物在5.0~ 100 mg/L范围内均呈良好的线性关系,线性系数均大于0.999.在5.0、10.0、25.0 mg/kg 3个加标水平下的平均回收率为92%~ 108%,相对标准偏差(RSD,n=6)为2.1%~4.2%,检出限为0.5~1.0 mg/L.该方法灵敏度高、重现性好、定量准确.%A solid phase extraction coupled with high performance liquid chromatography ( SPE/ HPLC) was developed for the determination of five antihistamines, e. g. doxylamine, tripelen-namine, brompheniramine, diphenhydramine, chlorphenoxamine, in cosmetics. The samples were extracted with trichloroacetic acid solution under ultrasonication, and cleaned up with PCX solid phase extraction. The separation of five antihistamines was carried out on a C18 column using metha-nol - phosphate buffer as mobile phase. The calibration curves of five drugs were linear in the range of 5. 0 - 100 mg/L, with correlation coefficients more than 0. 999. The mean recoveries at spiked levels of 5.0, 10.0, 25. 0 mg/kg were in the range of 92% -108% with RSDs(n =6)of 2. 1% -4. 2% . The limits of detection were in the range of 0. 5 -1.0 mg/L. The method was sensitive, reproducible and accurate.

  13. Antihistamine drugs usage analysis of outpatient pharmacy of skin disease hospital from 2010 to 2012%皮肤病医院2010-2012年门诊药房抗组胺药物使用情况分析

    Institute of Scientific and Technical Information of China (English)

    李志林

    2014-01-01

    Objective To explore application and problems of antihistamine drugs usage of outpatient pharmacy of our hospital from 2010 to 2012.Methods With hospital information system (HIS),extracted the data of antihistamines usage,including drug name,specification,quantity,sales etc.in outpatient pharmacy of our hospital from 2010 to 2012.At the same time,a retrospective analysis of 3000 copies of dermatology prescription for allergic skin disease and skin itching of outpatient department was issued,evaluated antihistamines usage.Results The use of antihistamines of the out-patient service pharmacy was reasonable.Usage and dosage in part of prescriptions had shortcomings,mainly the larger dose and the longer course of treatment; the combination treatment was also not reasonable,too much emphasis on efficacy,while ignoring the poisonous side effect.Conclusion Outpatient department should strengthen the rational use of antihistamine drugs,reduce side effects of drugs and ensure patient health.%目的 分析和了解2010至2012年间我院门诊药房抗组胺药物的使用情况及存在问题.方法 利用医院信息系统(HIS),提取我院在2010至2012年门诊药房抗组胺药物的使用情况数据,包括药物名称、药品规格、使用量、销售量等.同时,结合皮肤科对门诊过敏性皮肤病、瘙痒性皮肤病所开具的处方3000份,并进行回顾性分析,评价抗组胺药物的使用情况.结果 门诊药房抗组胺药物的使用情况基本合理,部分处方中用法用量有不足之处,主要表现为剂量较大而且疗程较长,其中联合用药也有不合理之处,过分注重疗效而忽视了抗组胺药物的毒副作用.结论 门诊部门应加强对抗组胺药物的合理使用,降低药物的毒副作用,保证病人身体健康.

  14. 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.

  15. Health technology assessment of four non-sedating antihistamines for allergic diseases%四种第二代抗组胺药物的卫生技术评估

    Institute of Scientific and Technical Information of China (English)

    孙鑫; 曹立亚; 马涛; 兰奋; 李夏; 肖爱丽; 陈心足; 李幼平

    2003-01-01

    Objectives This review compared clinical effectiveness, cardiac safety and economics of astemizole, lorata dine, cetirizine and terfenadine to provide evidence for adjustment of Essential Drug List in China. Search strategy We searched Medline, Cochrane Library, Embase and Chinese Biomedical Database. Fourteen databases for drug safety and pharmaceutical economics were additionally searched. Selection Criteria Randomized controlled trials and systematic reviews, published in English and Chinese and comparing two or more of these four antihistamines for allergic rhinitis and urticaria were included for study of effectiveness. Non-randomized clinical trials were additionally included for eco nomic evaluation. Cardiac safety studies of antihistamines for allergic diseases of any type were included. Quality Appraisal Jadad scale was primarily applied to randomized controlled trials. Allocation concealment and intention-to treat analysis were also appraised. The QUOROM statement was applied to systematic reviews and meta-analysis. Data extraction and analyses For the study of effectiveness, composite data were primarily extracted and analyzed by fixed effect model. Sensitivity analysis was done to explore the heterogeneity. For the study of cardiac safety, cases of adverse drug reactions and death were summarized. Difference of occurrence rate in sex and age were analyzed if possible.Electrocardiography and clinical symptoms were summarized. Results No studies on economic evaluation were identified. 27 and 6 randomized controlled trials, including 3 227 participants, for allergic rhinitis and urticaria were identified.Cetirizine was superior to loratadine (n=709) in symptom score and onset of action, superior to terfenadine (n=645) in Quality of Life and superior to astemizole (n=498) in patient satisfaction and onset of action. 73 h-ADR cases were identified in astemizole, 27 cases in terfenadine, 1 case in loratadine and none in cetirizine. No deaths were identified

  16. Antihistamines as neuroprotective agents / Hester Elizabeth Badenhorst

    OpenAIRE

    2004-01-01

    Biomolecules are continuously exposed to potentially harmful oxidative stress as a consequence of free radical formation. Increased free radical generation has been associated with aging as well as neurodegenerative disorders. Antioxidants affect processes associated with oxidative stress by quenching free radicals and acting as oxygen scavengers. Parkinson's disease results from a deficiency in the neurotransmitter, dopamine and it is also evident that damage caused by free ra...

  17. Complex Cognitive Performance and Antihistamine Use

    Science.gov (United States)

    1990-04-01

    respiratory edema, atopic dermatitis or eczema , seasonal rhinitis (hay fever), bronchial asthma (especially those with an allergic component), motion 6 7...0.0 Diarrhea 0.9 2.1 Rash 1.2 0.3 Eczema 0.4 1.2 Increased appetite 0.5 0.6 Increased weight 0.4 0.3 11 TABLE 5 Incidence (%) of Adverse Effects...Hendrickx, J., Lauwers, W., Hurkmans, R., Swysen, E., Heykants, J. (1986). Excretion and biotransformation of astemizole in rats, guinea-pigs, dogs

  18. Caffeoylquinic acid derivatives from Bidens parviflora and their antihistamine release activites%小花鬼针草中咖啡酰奎宁酸类成分及其抑制组胺释放活性

    Institute of Scientific and Technical Information of China (English)

    王珏; 王乃利; 姚新生; 北中進

    2006-01-01

    目的研究小花鬼针草Bidens parviflora全株的化学成分,并通过抑制组胺释放活性方法寻找生物活性化合物.方法采用硅胶、Sephadex LH-20和ODS柱色谱分离化合物,运用1D NMR,2D NMR等波谱法鉴定了化学结构,通过组胺抑制实验探讨抗炎活性.结果分离鉴定6种咖啡酰奎宁酸类化合物及其甲酯,分别是3,5-二氧咖啡酰奎宁酸(3,5-di-O-caffeoylquinic acid,Ⅰ)、3,4-二氧咖啡酰奎宁酸(3,4-di-O-caffeoylquinic acid,Ⅱ)、4,5-二氧咖啡酰奎宁酸(4,5-di-O-caffeoylquinic acid,Ⅲ)、4-氧-咖啡酰奎宁酸(4-O-caffeoylquinic acid,Ⅳ)、5-氧-咖啡酰奎宁酸(5-O-caffeoylquinic acid,Ⅴ)、4-[3-(3,4-二羟基苯基)-丙烯酰氧基]-2,3-二羟基-2-甲基-丁酸{4-[3-(3,4-dihydroxy-phenyl)-acryloyloxy]-2,3-dihydroxy-2-methyl-butyric acid,Ⅵ}.结论所有化合物均为首次从该植物中分得,化合物Ⅵ为新化合物.这些化合物显示一定的抑制组织胺释放活性.%Objective Based on the activities of antihistamine release to study the compounds from Bidens parvi-flora and find biological active compounds. Methods The chemical constituents from B.parviflora were isolated by silica gel and Sphadex LH-20 column chromatographies and purified by preparative HPLC. The chemical structures had been identified by physiochemical properties and spectroscopic methods. Results Six caffeoylquinic acid derivatives were identified as 3, 5-di-O-caffeoylquinic acid ( Ⅰ ),3, 4-di-O-caffeoylquinic acid ( Ⅱ ), 4, 5-di-O-caffeoylquinic acid ( Ⅲ ), 4-O-caffeoylquinic acid ( Ⅳ ), 5-O-caffeoylquinic acid ( Ⅴ ), 4-[3-(3, 4-dihydroxy-phenyl)-acryloyloxy]-2, 3-dihydroxy-2-methyl-butyric acid ( Ⅵ ). Conclusion Compounds Ⅰ - Ⅵ are first obtained from B. parviflora and Ⅵ is new one. Some of the compounds exhibit the activities in antiallergic assays. Moreover, the structure-activity relationships of these compounds have been also discussed in this paper.

  19. [Epidemiologic features in patients with antihistamine-resistant chronic urticaria].

    Science.gov (United States)

    Sánchez Borges, Mario; Tassinari, Stefano; Flores, Adriana

    2015-01-01

    Antecedentes: en la actualidad, la información disponible acerca de las características particulares de los pacientes que padecen urticaria crónica espontánea resistente a tratamiento es muy limitada. Objetivo: investigar las características demográficas y clínicas de los pacientes con urticaria crónica espontánea resistente a tratamiento. Material y método: estudio descriptivo, retrospectivo, de la información clínica y demográfica de pacientes que consultaron en los servicios de Alergología de dos hospitales de Caracas, Venezuela, que padecían urticaria espontánea de más de seis semanas de evolución y que no habían respondido a por lo menos un curso de tratamiento con antihistamínicos. Resultados: la urticaria crónica espontánea resistente a tratamiento fue más frecuente en pacientes de sexo femenino, de edades entre 20 y 59 años, de raza caucásica americana, con predominio de síntomas moderados, duración de las lesiones individuales de menos de tres horas y diámetro de los habones entre 1 y 3 cm. El angioedema solo o asociado con urticaria afectó a 14% de los pacientes. Las enfermedades asociadas con mayor frecuencia fueron: asma, rinitis y rinosinusitis, enfermedades tiroideas e hipertensión arterial. Conclusión: la urticaria crónica espontánea resistente a tratamiento constituye un subgrupo muy frecuente de urticaria crónica y representa un importante desafío terapéutico. En este estudio no se demostraron características diferenciales en comparación con las de los pacientes con urticaria crónica espontánea que responden al tratamiento con antihistamínicos.

  20. Tricin from a malagasy connaraceous plant with potent antihistaminic activity.

    Science.gov (United States)

    Kuwabara, Hidenori; Mouri, Kyoko; Otsuka, Hideaki; Kasai, Ryoji; Yamasaki, Kazuo

    2003-09-01

    The bioassay-guided separation of a Malagasy plant, Agelaea pentagyna, led to the isolation of a flavonoid, tricin (1), with potent inhibitory activity toward exocytosis from antigen-stimulated rat leukemia basophils (RBL-2H3). The structure-activity relationships among structurally related natural and synthetic flavonoids are also discussed.

  1. 21 CFR 341.72 - Labeling of antihistamine drug products.

    Science.gov (United States)

    2010-04-01

    ... citrate, diphenhydramine hydrochloride, or doxylamine succinate identified in § 341.12(f), (g), and (h... diphenhydramine citrate, diphenhydramine hydrochloride, or doxylamine succinate identified in § 341.12(f), (g... 6 years of age: consult a doctor. (8) For products containing doxylamine succinate identified...

  2. Safety profile of bilastine: 2nd generation H1-antihistamines.

    Science.gov (United States)

    Scaglione, F

    2012-12-01

    Bilastine is a new H1 antagonist with no sedative side effects, no cardiotoxic effects, and no hepatic metabolism. In addition, bilastine has proved to be effective for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. Pharmacological studies have shown that bilastine is highly selective for the H1 receptor in both in vivo and in vitro studies, and with no apparent affinity for other receptors. The absorption of bilastine is fast, linear and dose-proportional; it appears to be safe and well tolerated at all doses levels in healthy population. Multiple administration of bilastine has confirmed the linearity of the kinetic parameters. The distribution in the brain is undetectable. The safety profile in terms of adverse effects is very similar to placebo in all Phase I, II and III clinical trials. Bilastine (20 mg), unlike cetirizine, does not increase alcohol effects on the CNS. Bilastine 20 mg does not increase the CNS depressant effect of lorazepam. Bilastine 20 mg is similar to placebo in the driving test. Therefore, it meets the current criteria for medication used in the treatment of allergic rhinitis and urticaria.

  3. 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

    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...

  4. [Mutagenesis of the human histamine H1 receptor and design of new antihistamine agents].

    Science.gov (United States)

    Differding, E; Gillard, M; Moguilevsky, N; Varsalona, F; Noyer, M; Daliers, J; Goldstein, S; Neuwels, M; Lassoie, M A; Guillaume, J P; Bascour, M; Bollen, A; Hénichart, J P

    1996-01-01

    The binding cavity of histamine and histamine antagonists is explored using site directed mutagenesis of the human histamine H1 receptor and the amino acids involved in ligand binding are identified. Whereas Asp107 and Phe199 are important for both agonists and antagonists, two additional amino acids (Asn198 and Trp103) are required for efficient histamine binding. The binding site of antagonists is best defined as resulting from a strong ionic bond to Asp107, an orthogonal interaction between one of the aromatic rings with Phe199, and probably a hydrophobic interaction between the second aromatic ring and the lipophilic amino acids of the upper part of TMIV and TMV. This is consistent with structure-activity data of most described antagonists.

  5. Effects of antidepressants and antihistaminics on catalepsy induced by intracerebroventricular administration of histamine in mice.

    Science.gov (United States)

    Onodera, K

    1991-01-01

    The intracerebroventricular (icv) administration of histamine but not N-telemethylhistamine and 1-methyl-4-imidazole acetic acid induced catalepsy in mice. Histamine H1-receptor blockers such as cyproheptadine, mepyramine and diphenhydramine reduced histamine-induced catalepsy. However, astemizole which is known to be without central effects, did not reduce histamine-induced catalepsy. The icv pretreatment with histamine H2-receptor blockers, such as metiamide and cimetidine, also had no effect. Moreover, various antidepressants, both imipramine- and atypical-type drugs antagonized histamine-induced catalepsy to various degrees in this experiment. Thus, the induction of catalepsy by icv administration of histamine was mediated through histamine H1-receptors, and suggested that antidepressants reduced histamine-induced catalepsy via this mechanism. Histamine-induced catalepsy is a possible new animal model of depression which can also be used for evaluation of atypical antidepressants.

  6. 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.

  7. Effects of antihistamine and anti-inflammatory medication use on risk of specific glioma histologies

    OpenAIRE

    Scheurer, Michael E.; Amirian, E. Susan; Davlin, Stacy L.; Rice, Terri; Wrensch, Margaret; Melissa L. Bondy

    2011-01-01

    Several studies have shown a decrease in glioma risk associated with a personal history of allergic conditions and the medications used to treat the symptoms. However, few studies have been able to examine risk within histological subgroups of glioma. Case-control data from M. D. Anderson Cancer Center and University of California, San Francisco were pooled to conduct the analysis stratified by histological subtype. A risk prediction model considering inflammation-related variables and antihi...

  8. Advancement of antihistamine drugs application%抗组胺药物应用进展

    Institute of Scientific and Technical Information of China (English)

    杨森; 张学军

    2002-01-01

    抗组胺药物治疗过敏性疾病已广泛地应用于临床.由于第1代抗组胺药物嗜睡的不良反应而影响了它的临床应用,20世纪80年代后生产的第2代抗组胺药物具有H1受体选择性高、无镇静作用、与组胺作用分离等特点,称非镇静抗组胺药(NSA) .但第2代抗组胺药仍有一些不良反应,尤以心脏的毒性作用,这与抗组胺药物相互作用、药动学、以及药物的分子结构有关.1997年新型抗组胺药物--非索非那定(fexofenadine)问世,它是作用快、疗效高、相对安全低毒的抗组胺药.非索非那定的开发,为寻找既无中枢镇静作用,也无心脏毒性的抗组胺药物开辟了新的途径.

  9. 抗组胺药研究进展%Advances in antihistamines

    Institute of Scientific and Technical Information of China (English)

    刘永贵; 于鹏; 徐颂; 贺星; 田红; 陈常青

    2010-01-01

    组胺是引起炎症和过敏性疾病的一类物质,是速发型过敏反应(临床最常见Ⅰ型变态反应疾病)的重要的化学介质之一.因而,在过去的70多年中,抗组胺药物出现了第一代、第二代,以及第二代的改良品种,在临床上被广泛应用.尤其是在非处方药方面,该类药常与其他药物,如解热镇痛剂、去鼻塞剂等组成复方制剂用于感冒发热等,深受医生和患者的欢迎.现对抗组胺药物(以组胺H1受体拮抗剂为主)的研发进展做一介绍.

  10. Radiation-Released Histamine in the Rhesus Monkey as Modified by Mast Cell Depletion and Antihistamine

    Science.gov (United States)

    1975-06-01

    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.

  11. Spectrophotometric Determination of Some Non-Sedating Antihistamines Using Erythrosine B

    OpenAIRE

    Noha N. Atia; Noha M. Hosny; Michael E. El-Kommos; Samia M. El-Gizawy

    2013-01-01

    A simple and sensitive spectrophotometric method has been developed for the determination of cetirizine (I), ebastine (II), fexofenadine (III), ketotifen (IV), and loratadine (V) based on ion-pair complex formation with erythrosine B. The pink color of the produced complex was measured at 550 nm without solvent extraction. Appropriate conditions were established by studying the color reaction between erythrosine B and the studied drugs to obtain the maximum sensitivity. Beer-Lambert's law is ...

  12. EVALUATION OF ANTIMICROBIAL AND ANTI-HISTAMINE ACTIVITY OF THE AERIAL PARTS OF TEPHROSIA PURPUREA L.

    OpenAIRE

    Duraisami Nivedithadevi; Paramasivam Manivannan; Ramamurthy Somasundaram

    2012-01-01

    Tephrosia purpurea (Fabaceae) has been used as a medicinal plant in all over India. This plant is a much branched perennial herb. Roots are given orally against any type of poisoning such as snakebite and the aerial parts were used for hydrophobia, asthma, cough, heart disease and kidney problems. Anti-microbial activity of 50% alcoholic extract with different concentrations were tested against the fungal strains like Aspergillus fumigates, Aspergillus niger, Ganoderma lucida and Candida alb...

  13. FORMULATION DEVELOPMENT AND EVALUATION OF CHEWABLE TABLETS CONTAINING NON- SEDATING ANTIHISTAMINE

    Directory of Open Access Journals (Sweden)

    Jayadev Patil

    2012-06-01

    Full Text Available Various formulations of Loratadine Chewable tablets containing different pharmaceutical compositions with simple manufacturing procedures were developed by using different excipients. The excipients used here are Lactose, Mannitol, Ethyl cellulose, microcrystalline cellulose, Maize Starch, Citric Acid, Aspartame, Colloidal silicon dioxide, Magnesium Stearate, D & C Yellow No 10 and Raspberry flavour. Oral chewable tablets are the most preferred among the conventional dosage forms due to its aesthetic appeal and ease of administering to children, which has entered the market. Loratadine is formulated into chewable tablets by wet granulation method using suitable excipients as mentioned earlier, which are evaluated by using simple analytical equipments. The chewable tablet was better presented using artificial sweetener Aspartame and Raspberry flavour as flavouring agent. The chewable tablets are prepared to ensure that they are easily crushed by chewing. The tablets were evaluated for weight variation, hardness, friability; drug content and mouth feel along with in-vitro dissolution. As per monograph, the chewable tablets are not required to comply with disintegration test. Wet granulation process using Mannitol, Lactose, Micro crystalline cellulose (Avicel-CE 15, Ethyl cellulose and Sweeteners and Flavors were found to be simple and robust method to prepare chewable tablets.

  14. 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.

  15. Determination of some antihistaminic drugs by atomic absorption spectrometry and colorimetric methods.

    Science.gov (United States)

    El-Kousy, N; Bebawy, L I

    1999-08-01

    Atomic absorption spectrometry (AAS) and colourimetric methods have been developed for the determination of pizotifen (I), ketotifen (II) and loratadine (III). The first method depends on the reaction of the three drugs (I); (II) and (III) with cobalt thiocyanate reagent at pH 2 to give ternary complexes. These complexes are readily extracted with organic solvent and estimated by indirect atomic absorption method via the determination of the cobalt content in the formed complex after extraction in 0.1 M hydrochloric acid. It was found that the three drugs can be determined in the concentration ranges from 10 to 74, 12 to 95 and 10 to 93 microg ml(-1) with mean percentage recovery of 99.71+/-0.87, 99.70+/-0.79 and 99.62+/-0.75%, respectively. The second method is based on the formation of orange red ion pairs as a result of the reaction between (I); (II) and (III) and molybdenum thiocyanate with maximum absorption at 469.5 nm in dichloromethane. Appropriate conditions were established for the colour reaction. Under the proposed conditions linearity was obeyed in the concentration ranges 3.5-25, 5-37.5 and 2.5-22.5 microg ml(-1) with mean percentage recovery of 99.60+/-0.41, 100.11+/-0.43 and 99.31+/-0.47% for (I): (II) and (III), respectively. The third method depends on the formation of radical ion using 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ). The colour formed was measured at 588 nm for the three drugs (I); (II) and (III), respectively. The method is valid in concentration range 10-80 microg ml(-1) with mean percentage recovery 99.75+/-0.44, 99.94+/-0.72 and 99.17+/-0.36% for (I); (II) and (III), respectively. The proposed methods were applied to the analysis of pharmaceutical preparations. The results obtained were statistically analysed and compared with those obtained by applying the official and reference methods.

  16. 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....

  17. Medicines to Treat Allergies

    Science.gov (United States)

    ... antihistamines . Some examples of brand- name antihistamines are Zyrtec and Claritin . You can buy antihistamines with or ... generic antihistamines as the best for most people:  Cetirizine (tablets)  Loratadine (tablets, dissolving tablets, or liquid)  Alavert ( ...

  18. A New Marmoset P450 4F12 Enzyme Expressed in Small Intestines and Livers Efficiently Metabolizes Antihistaminic Drug Ebastine.

    Science.gov (United States)

    Uehara, Shotaro; Uno, Yasuhiro; Yuki, Yukako; Inoue, Takashi; Sasaki, Erika; Yamazaki, Hiroshi

    2016-06-01

    Common marmosets (Callithrix jacchus) are attracting attention as animal models in preclinical studies for drug development. However, cytochrome P450s (P450s), major drug-metabolizing enzymes, have not been fully identified and characterized in marmosets. In this study, based on the four novel P450 4F genes found on the marmoset genome, we successfully isolated P450 4F2, 4F3B, 4F11, and 4F12 cDNAs in marmoset livers. Deduced amino acid sequences of the four marmoset P450 4F forms exhibited high sequence identities (87%-93%) to the human and cynomolgus monkey P450 4F homologs. Marmoset P450 4F3B and 4F11 mRNAs were predominantly expressed in livers, whereas marmoset P450 4F2 and 4F12 mRNAs were highly expressed in small intestines and livers. Four marmoset P450 4F proteins heterologously expressed in Escherichia coli catalyzed the ω-hydroxylation of leukotriene B4 In addition, marmoset P450 4F12 effectively catalyzed the hydroxylation of antiallergy drug ebastine, a human P450 2J/4F probe substrate. Ebastine hydroxylation activities by small intestine and liver microsomes from marmosets and cynomolgus monkeys showed greatly higher values than those of humans. Ebastine hydroxylation activities by marmoset and cynomolgus monkey small intestine microsomes were inhibited (approximately 60%) by anti-P450 4F antibodies, unlike human small intestine microsomes, suggesting that contribution of P450 4F enzymes for ebastine hydroxylation in the small intestine might be different between marmosets/cynomolgus monkeys and humans. These results indicated that marmoset P450 4F2, 4F3B, 4F11, and 4F12 were expressed in livers and/or small intestines and were functional in the metabolism of endogenous and exogenous compounds, similar to those of cynomolgus monkeys and humans.

  19. 抗组胺药的药物相互作用%Drug-drug interactions of antihistamines

    Institute of Scientific and Technical Information of China (English)

    孙平华; 姚志红; 孙铁民

    2006-01-01

    介绍了抗组胺药物和其他临床常用药物的相互作用,为患者安全用药提供参考.第一、二代抗组胺药易与多种药物发生相互作用而致心脏毒性等不良反应,第三代抗组胺药联用时不会导致严重的不良反应.所以抗组胺药作为临床和OTC常用抗过敏药,应对其药物相互作用及产生的不良反应引起注意.

  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. 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

    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.......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....

  2. Taste Masked Orally Disintegrating Pellets of Antihistaminic and Mucolytic Drug: Formulation, Characterization, and In Vivo Studies in Human.

    Science.gov (United States)

    Taj, Yasmeen; Pai, Roopa S; Kusum Devi, V; Singh, Gurinder

    2014-01-01

    The main aim of the present study was to evaluate the potential of orally disintegrating pellets (ODPs) as an approach for taste masking of bitter drugs, namely, Ambroxol hydrochloride (A-HCl) and Cetirizine dihydrochloride (C-DHCl). Pellets were prepared by extrusion/spheronization with Eudragit EPO, kyron T-134, Kyron T-314, mannitol, sorbitol, MCC (Avicel PH-101), sucralose, chocolate flavor, and 5% xanthum gum. The prepared pellets were characterized for percentage yield, drug content, particle size, in vitro drug release, and in vivo evaluation on humans for taste, mouth feel, and in vivo disintegration time. The results revealed that the average size of pellets was influenced greatly by the percentage of binder and extrusion speed. The optimized ODPs disintegrated in less than 20 s and showed more than 98% of drugs in ODPs dissolved within 15 min. Taste perception study was carried out on human volunteers to evaluate the taste masking ability of ODPs for taste, mouth feel, and in vivo disintegration time. Crystalline state evaluation of drugs in the optimized ODPs was conducted for X-ray powder diffraction. In conclusion, the study confirmed that ODPs can be utilized as an alternative approach for effective taste masking and rapid disintegration in the oral cavity.

  3. [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.

  4. Potentiometric determination of antihistaminic diphenhydramine hydrochloride in pharmaceutical preparations and biological fluids using screen-printed electrode.

    Science.gov (United States)

    Frag, Eman Y Z; Mohamed, Gehad G; El-Sayed, Wael G

    2011-10-01

    The performance characteristic of sensitive screen-printed (SPE) and carbon paste (CPE) electrodes was investigated for the determination of diphenhydramine hydrochloride (DPH) drug in pure, pharmaceutical preparations and biological fluids. Different experimental conditions namely types of materials used to prepare the working electrode (plasticizer), titrant, pH, temperature and life time were studied. Under these conditions, the SPE shows the best performance than CPE with respect to total potential change and potential break at the end point. The SPE and CPE exhibit suitable response to DPH in a concentration range of 1.0.10(-2) to 1.0.10(-6) mol/L with a limit of detection 9.70.10(-7) and 9.80.10(-7) mol/L, respectively. The slope of the system was 55.2±1.0 and 54.7±1.0 mV/decade over pH range 3.0-8.0 and 3-7 for SPE and CPE, respectively. Selectivity coefficients for DPH relative to a numbers of potential interfering substances were investigated. The SPE and CPE show a fast response time of 10 and 16s and were used over a period of 2 months with a good reproducibility. The sensors were applied successfully to determine DPH in pharmaceutical preparations and biological fluids. The results are compared with the official method.

  5. Taste Masked Orally Disintegrating Pellets of Antihistaminic and Mucolytic Drug: Formulation, Characterization, and In Vivo Studies in Human

    Science.gov (United States)

    Taj, Yasmeen; Pai, Roopa S.; Kusum Devi, V.; Singh, Gurinder

    2014-01-01

    The main aim of the present study was to evaluate the potential of orally disintegrating pellets (ODPs) as an approach for taste masking of bitter drugs, namely, Ambroxol hydrochloride (A-HCl) and Cetirizine dihydrochloride (C-DHCl). Pellets were prepared by extrusion/spheronization with Eudragit EPO, kyron T-134, Kyron T-314, mannitol, sorbitol, MCC (Avicel PH-101), sucralose, chocolate flavor, and 5% xanthum gum. The prepared pellets were characterized for percentage yield, drug content, particle size, in vitro drug release, and in vivo evaluation on humans for taste, mouth feel, and in vivo disintegration time. The results revealed that the average size of pellets was influenced greatly by the percentage of binder and extrusion speed. The optimized ODPs disintegrated in less than 20 s and showed more than 98% of drugs in ODPs dissolved within 15 min. Taste perception study was carried out on human volunteers to evaluate the taste masking ability of ODPs for taste, mouth feel, and in vivo disintegration time. Crystalline state evaluation of drugs in the optimized ODPs was conducted for X-ray powder diffraction. In conclusion, the study confirmed that ODPs can be utilized as an alternative approach for effective taste masking and rapid disintegration in the oral cavity. PMID:27379290

  6. Taste Masked Orally Disintegrating Pellets of Antihistaminic and Mucolytic Drug: Formulation, Characterization, and In Vivo Studies in Human

    OpenAIRE

    Taj, Yasmeen; Pai, Roopa S.; V. Kusum Devi; Singh, Gurinder

    2014-01-01

    The main aim of the present study was to evaluate the potential of orally disintegrating pellets (ODPs) as an approach for taste masking of bitter drugs, namely, Ambroxol hydrochloride (A-HCl) and Cetirizine dihydrochloride (C-DHCl). Pellets were prepared by extrusion/spheronization with Eudragit EPO, kyron T-134, Kyron T-314, mannitol, sorbitol, MCC (Avicel PH-101), sucralose, chocolate flavor, and 5% xanthum gum. The prepared pellets were characterized for percentage yield, drug content, pa...

  7. Drug: D03360 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 26 Epidermides 264 Analgesics, anti-itchings, astringents, anti-inflammatory agents 2642 Antihistamine...ICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamine... Tract/Pulmonary Agents Antihistamines Diphenhydramine D03360 Diphenhydramine laurylsulfate (JAN) Target-bas...Antiparkinson Agents Anticholinergics Diphenhydramine D03360 Diphenhydramine laurylsulfate (JAN) Respiratory

  8. Drug: D03285 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for top...ical use D04AA32 Diphenhydramine D03285 Diphenhydramine tannate (JP16) R RESPIRATOR

  9. Drug: D07197 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available CS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topi...cal use D04AA15 Bamipine D07197 Bamipine (INN) R RESPIRATORY SYSTEM R06 ANTIHISTAMI

  10. Drug: D07790 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available STEMIC USE R06AX Other antihistamines for systemic use R06AX16 Deptropine D07790 ...ssification [BR:br08303] R RESPIRATORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SY

  11. Drug: D08432 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available L. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topical use D04AA10 Promethazine D08432 Promet...e Respiratory Tract/Pulmonary Agents Antihistamines Promethazine D08432 Promethazine maleate Target-based cl

  12. Drug: D02419 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available , INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topical use D0... Diphenhydramine D02419 Diphenhydramine salicylate (JAN) Respiratory Tract/Pulmonary Agents Antihistamines D

  13. Drug: D00494 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available TC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamine...Antiemetics, Other Promethazine D00494 Promethazine (JAN/INN) Respiratory Tract/Pulmonary Agents Antihistamine

  14. Drug: D07853 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04 ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihis...tamines for topical use D04AA13 Dimetindene D07853 Dimetindene (INN) R RESPIRATORY

  15. Drug: D01242 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available NES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamine...Respiratory Tract/Pulmonary Agents Antihistamines Promethazine D01242 Promethazine teoclate (JAN/INN) Target

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

    Directory of Open Access Journals (Sweden)

    Miloš Jeseňák

    2014-01-01

    Full Text Available Complementary and alternative medicine is surviving across the decades and also in the medicine of 21st century. The physicians are meeting different preparations during their praxis and the challenge for them is to find the right way how to navigate the patients in the middle of thousands of preparations and methods. Complementary and alternative medicine is considered to be the therapeutic approaches and methods which are not involved in the standard conventional treatment schema.

  17. The efficacy and safety of the third generation antihistamine desloratadine in clinical use%第三代抗组胺药地氯雷他定

    Institute of Scientific and Technical Information of China (English)

    徐道华

    2005-01-01

    地氯雷他定是氯雷他定在体内主要的活性代谢产物,为一种口服非镇静抗组胺药.在美国和欧洲用于治疗过敏性鼻炎和慢性荨麻疹,起效快,不良反应小,尤其对儿童患者安全性好.对其药理作用、临床应用及安全性进行评价.

  18. 抗组胺新药非索非那定的合成和应用%Synthesis and Application of a New Antihistamine Drug--Fexofenadine

    Institute of Scientific and Technical Information of China (English)

    刘斌; 容如滨; 袁华; 喻宗沅

    2005-01-01

    非索非那定是新一代的抗组胺药,用于治疗过敏性疾病,无镇静和嗜睡感,毒副作用小.综述了抗组胺新药非索非那定的合成方法,比较了它们的优缺点,并对其应用前景作了展望.

  19. 我院抗组胺药应用动态分析%Dynamic Andlysis of Antihistamine Drugs in Our Hospital from 2001 to 2003

    Institute of Scientific and Technical Information of China (English)

    尹艳莲

    2005-01-01

    目的:分析我院抗组胺药的应用现状及趋势预测,引导临床合理用药.方法:采用用药金额和用药频度排序法,对我院2001~2003年抗组胺药应用情况进行统计分析.结果:第一代抗组胺药的用药频度呈下降趋势,第二代稳步上升.结论:毒副作用小,服用方便,经济高效的抗组胺药是医生患者的首选.

  20. Utilization Analysis of Antihistamines in Our Hospital from 2006 to 2008%2006~2008年我院抗组胺药应用分析

    Institute of Scientific and Technical Information of China (English)

    李岚; 王晓玲

    2010-01-01

    目的:了解抗纽胺药在我院的应用情况和发展趋势.方法:采用金额排序和使用频度分析法时我院2006~2008年抗组胺药的使用情况进行统计分析.结果:左西替利嗪片、西替利嗪滴剂、氯雷他定糖浆的用药频率一直保持领先.结论:安全、有效的第2、3代抗组胺药将成为抗过敏治疗的主要药物.

  1. 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.

  2. Clinical application of antihistamines in children allergic rhinitis%抗组胺药在儿童变应性鼻炎治疗中的应用

    Institute of Scientific and Technical Information of China (English)

    孟立新

    2013-01-01

    儿童变应性鼻炎(AR)的临床诊治受到耳鼻喉科、变态反应科、呼吸科和儿科等相关学科的关注,权威AR指南的药物治疗规范都强调抗组胺药的重要性.本文综述抗组胺药在儿童AR中的应用.

  3. 小青龙汤和麻黄汤抗组胺作用%Antihistamine Action of Small - blue - dragon Decoction and Mahuang Decoction

    Institute of Scientific and Technical Information of China (English)

    阮岩; 李笋; 封彦蕾; 陈蔚

    2006-01-01

    目的利用组胺皮肤试验了解中药抗组胺机理,比较中西药抗组胺作用的异同.方法将45例健康志愿者分为小青龙汤组,麻黄汤组,氯雷他定组和安慰剂组,各组在用药前及用药后2,5,24 h进行不同浓度的组胺皮肤试验,皮试后15 min观察并记录风团及红晕的面积,绘制剂量-反应曲线.结果风团和红晕面积比较,小青龙汤、麻黄汤组服药后2,5,24 h和服药前差异无显著性(P>0.05).氯雷他定组服药后2,5,24 h和服药前差异有显著性(P<0.05).结论小青龙汤和麻黄汤不能直接抑制组胺,而可能是抑制肥大细胞脱颗粒作用,减少组胺的分泌.

  4. Heart Damage by Combination of Erythromycin and Antihistamine Drug%琥乙红霉素与抗组胺药合用引起心脏损害

    Institute of Scientific and Technical Information of China (English)

    林琴; 余更生

    2006-01-01

    琥乙红霉素(利君沙)联合抗组胺药[富马酸酮替芬或曲普利啶(克敏)],引起心脏损害少见,尤其是引起心脏迷走神经张力增高,导致窦性心动过缓、显著窭性心律不齐、窦房结游走心律未见报告,易误诊误治,现报告2例。

  5. 我院口服抗组胺药物应用分析%Analysis of Antihistamines Used in Our Hospital During the Period 2001 ~ 2002

    Institute of Scientific and Technical Information of China (English)

    张平; 吴祥元; 宋湘芝; 林焯英; 黄师菊

    2003-01-01

    目的:了解口服抗组胺药物在我院的应用情况和发展趋势.方法:采用金额排序和应用频度分析法对我院2001年1月~2002年12月常用口服抗组胺药进行统计、分析.结果:用药金额及用药频度(DDDs)逐年提高,2002年用药金额及DDDs分别是2001年的1.34倍和1.38倍.结论:氯雷他定是抗过敏药物首选.我国制药企业应抓住机遇,开发国产的长效、安全、经济的口服抗组胺药物.

  6. 抗组胺药对认知功能和执行能力的影响%The effect of antihistamines on human recognition and performance

    Institute of Scientific and Technical Information of China (English)

    支玉香; 张宏誉

    2003-01-01

    抗组胺药是治疗过敏性疾病十分有效的药物,其对中枢神经系统的镇静作用主要表现为认知功能和执行能力的下降,因此,对该药治疗指数或益处/风险比值的评估十分重要.笔者将对评估方法及结果加以综述.

  7. 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).

  8. Circulating histamine and neutrophil chemotactic activity during allergen-induced asthma: the effect of inhaled antihistamines and anti-allergic compounds.

    Science.gov (United States)

    Morgan, D J; Moodley, I; Cundell, D R; Sheinman, B D; Smart, W; Davies, R J

    1985-07-01

    Plasma histamine and serum neutrophil chemotactic activity (S-NCA) were measured in ten atopic asthmatic patients on four separate occasions after allergen bronchial provocation testing (BPT). Single doses of inhaled sodium cromoglycate (SCG; 20 mg), clemastine (0.5 mg), ketotifen (0.5 mg) and isotonic saline (0.9% NaCl) placebo were administered 30 min before bronchial provocation testing in random order and double-blind. The airflow obstruction after BPT was monitored by measurement of forced expiratory volume in 1 s (FEV1). Plasma histamine was measured by the double-isotope radioenzymatic assay and S-NCA by a modified Boyden chamber technique. A highly significant decrease in FEV1 after BPT occurred on the placebo pre-treatment visit (P less than 0.001). Prior administration of inhaled SCG, clemastine and ketotifen significantly reduced the decrease in airflow obstruction seen after BPT when compared with placebo treatment (P less than 0.01, P less than 0.02, P less than 0.05 respectively). No significant alteration in plasma histamine was detected during allergen-induced airflow obstruction. Levels of S-NCA were significantly higher 5, 10 and 15 min after BPT when compared with the pre-challenge level (P less than 0.01, P less than 0.01, P less than 0.001 respectively). These levels were not significantly decreased when airflow obstruction was inhibited by the prior inhalation of SCG, clemastine or ketotifen.

  9. Development, Validation and Application of RP-HPLC Method: Simultaneous Determination of Antihistamine and Preservatives with Paracetamol in Liquid Formulations and Human Serum

    Science.gov (United States)

    Hasan, Najmul; Chaiharn, Mathurot; Toor, Umair Ali; Mirani, Zulfiqar Ali; Sajjad, Ghulam; Sher, Nawab; Aziz, Mubashir; Siddiqui, Farhan Ahmed

    2016-01-01

    In this article we describe development and validation of stability indicating, accurate, specific, precise and simple Ion-pairing RP-HPLC method for simultaneous determination of paracetamol and cetirizine HCl along with preservatives i.e. propylparaben, and methylparaben in pharmaceutical dosage forms of oral solution and in serum. Acetonitrile: Buffer: Sulfuric Acid (45:55:0.3 v/v/v) was the mobile phase at flow rate 1.0 mL min-1 using a Hibar® Lichrosorb® C18 column and monitored at wavelength of 230nm. The averages of absolute and relative recoveries were found to be 99.3%, 99.5%, 99.8% and 98.7% with correlation coefficient of 0.9977, 0.9998, 0.9984, and 0.9997 for cetirizine HCl, paracetamol, methylparaben and Propylparaben respectively. The limit of quantification and limit of detection were in range of 0.3 to 2.7 ng mL-1 and 0.1 to 0.8 ng mL-1 respectively. Under stress conditions of acidic, basic, oxidative, and thermal degradation, maximum degradation was observed in basic and oxidative stress where a significant impact was observed while all drugs were found almost stable in the other conditions. The developed method was validated in accordance with ICH and AOAC guidelines. The proposed method was successfully applied to quantify amount of paracetamol, cetirizine HCl and two most common microbial preservatives in bulk, dosage form and physiological fluid. PMID:27651840

  10. Drug: D00480 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available fecting cellular function 44 Allergic agents 441 Antihistamines 4413 Phenothiazin... ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topical use D04AA10 P...azine D00480 Promethazine hydrochloride (JP16/USP) Respiratory Tract/Pulmonary Agents Antihistamine

  11. Drug: D03854 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Tract/Pulmonary Agents Antihistamines Diphenhydramine D03854 Diphenhydramine citrate (USP) Target-based cla...ANTIHISTAMINES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihi...stamines for topical use D04AA32 Diphenhydramine D03854 Diphenhydramine citrate (US...(USP) Antiparkinson Agents Anticholinergics Diphenhydramine D03854 Diphenhydramine citrate (USP) Respiratory

  12. Drug: D00300 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 26 Epidermides 264 Analgesics, anti-itchings, astringents, anti-inflammatory agents 2642 Antihistamine... D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines...s Diphenhydramine D00300 Diphenhydramine (JP16/INN) Respiratory Tract/Pulmonary Agents Antihistamines Diphen

  13. Drug: D04447 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 6 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AB Substituted alkylamines R06AB54 Chlorphenamine, combinat...ions D04447 Betamethasone - d-chlorpheniramine maleate mixt PubChem: 17398108 ...

  14. Drug: D07407 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available histamines for systemic use R06AX28 Rupatadine D07407 Rupatadine (INN) Target-based...SPIRATORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other anti

  15. Drug: D07196 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 12 Anatomical Therapeutic Chemical (ATC) classification [BR:br08303] D DERMATOLOGICALS D04 ANTIPRURITICS, IN...CL. ANTIHISTAMINES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Anti

  16. Chronic Idiopathic Cough and Chronic Cough in Idiopathic Pulmonary Fibrosis | EU Clinical Trials Register [EU Clinical Trials Register

    Lifescience Database Archive (English)

    Full Text Available nhaled corticosteroids, benzonatate, dextromethorphan, carbetapentane, H1 antihistamines, leukotriene modifi...eeks of the Screening Visit: Prednisone, narcotic antitussives, baclofen, gabapentin, inhaled corticosteroids, benzonatate, dextromet...horphan, carbetapentane, H1 antihistamines, leukotriene

  17. Sleep disturbances in allergic rhinitis: disease and/or the drug?

    OpenAIRE

    Anant D. Patil

    2013-01-01

    Allergic rhinitis is a common chronic disease in adults as well as children. Allergic rhinitis has negative impact on sleep and quality of life of the patient. Antihistamines are widely used in the management of allergic rhinitis. First generation antihistamines cause sedation and drowsiness. Second generation antihistamines cause minimal or no sedation. There is difference in propensity to cause sedation amongst second generation antihistamines. As sleep is important for physical as well as ...

  18. Drug: D07482 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tion [BR:br08303] R RESPIRATORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other antihista...mines for systemic use R06AX09 Azatadine D07482 Azatadine (INN) Target-based classi

  19. Drug: D07458 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available YSTEMIC USE R06AX Other antihistamines for systemic use R06AX05 Antazoline D07458...ids R01AC04 Antazoline D07458 Antazoline (INN) R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR S

  20. Drug: D07900 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available tion [BR:br08303] R RESPIRATORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other antihista...mines for systemic use R06AX24 Epinastine D07900 Epinastine (INN) S SENSORY ORGANS

  1. Drug: D07493 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available TORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other antihista...mines for systemic use R06AX01 Bamipine D07493 Bamipine lactate Target-based classi

  2. Drug: D08353 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ication [BR:br08303] R RESPIRATORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other antihi...stamines for systemic use R06AX04 Phenindamine D08353 Phenindamine (INN) Target-bas

  3. Drug: D00669 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available cellular function 44 Allergic agents 441 Antihistamines 4411 Diphenhydramines D00...TIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topical use D04AA32 Diph...ticholinergics Diphenhydramine D00669 Diphenhydramine hydrochloride (JP16/USP) Respiratory Tract/Pulmonary Agents Antihistamine

  4. Drug: D03535 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topical use D04AA14 Cl...(USAN) USP drug classification [BR:br08302] Respiratory Tract/Pulmonary Agents Antihistamines Clemastine D03

  5. Drug: D03290 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available nction 44 Allergic agents 441 Antihistamines 4413 Phenothiazines D03290 Promethazine methylenedisalicylate (... ANESTHETICS, ETC. D04AA Antihistamines for topical use D04AA10 Promethazine D03290 Promethazine methylenedi...90 Promethazine methylenedisalicylate (JAN) Respiratory Tract/Pulmonary Agents Antihistamines Promethazine D

  6. 小花鬼针草中的苯丙苷类成分及抑制组胺释放活性%Phenolic glucosides from Bidens parviflora and their anti-histamine activities

    Institute of Scientific and Technical Information of China (English)

    王珏; 王乃利; 姚新生; 北中進

    2007-01-01

    目的 研究小花鬼针草Bidens parviflora全株的化学成分,并通过组胺抑制实验寻找活性成分.方法 采用硅胶、Sephadex LH-20和ODS柱色谱分离化合物,运用1D NMR、2D NMR波谱学方法鉴定了化合物的结构,通过组胺抑制实验测定化合物抗过敏活性.结果 分离鉴定了4个苯丙苷类及1个苯甲醇苷成分:4-羟基-3-甲氧基苯丙三醇8-O-β-D-葡萄糖苷(guaiacyl glycerol 8-O-β-D-glucoside Ⅰ)、丁香酚苷(syringin,Ⅱ)、4-烯丙基-2-甲氧基苯酚-O-(6-O-β-D-芹糖基)-β-D-葡萄糖苷[4-allyl-2-methoxyphenol-O-(6-O-β-D-apiofuranosyl)-β-D-glucoside,Ⅲ]、5,7-二羟基色原酮-7-O-β-D-葡萄糖苷(5,7-dihydroxy chromone 7-O-β-D-glucoside,Ⅳ)、苄醇-O-β-D-葡萄糖苷(benzyl alcohol-O-β-D-glucoside,Ⅴ).化合物Ⅰ~Ⅴ抑制组胺释放,IC50分别为70、61、>100、52、>100 μg/mL.结论 化合物Ⅰ~Ⅴ首次从本植物中分得,Ⅲ为未见文献报道的新化合物,命名为鬼针草酚葡萄糖苷(bidenphenol glucoside).化合物Ⅰ~Ⅴ具有抑制组胺释放的活性.

  7. Clinial Analysis of Compound Glycyrrhizin and Antihistamine in Treating Drug Eruption%复方甘草酸苷联合抗组胺药治疗药疹临床分析

    Institute of Scientific and Technical Information of China (English)

    袁星海; 姚新民; 王豫平

    2005-01-01

    目的评价复方甘草酸苷联合西替利嗪治疗猩红热样及麻疹样型药疹的疗效.方法治疗组53例用复方甘草酸苷联合西替利嗪治疗,同时以葡萄糖酸钙注射液联合西替利嗪治疗35例患者作为对照.结果治疗组治愈率(90.6%),显著高于对照组(60.0%)(P<0.05).结论复方甘草酸苷联合西替利嗪治疗猩红热样及麻疹样型药疹安全、有效.

  8. ANALYZE THE STATUS OF APPLICATION OF ANTIHISTAMINE DRUGS IN A HOSPITAL FROM 2009 TO 2012%某院2009~2012年抗组胺类药物使用情况分析

    Institute of Scientific and Technical Information of China (English)

    梁玉屏

    2013-01-01

    目的 评价分析某院抗组胺类药物的应用状况和发展趋势.方法 采用金额排序和使用频度分析法对近三年来某院抗组胺类药物的使用情况进行统计分析.结果 地氯雷他定片、氯苯那敏片、氯雷他定片、赛庚定片的用药频率一直处于该类药物前四位.结论 目前价格适中的第三代抗组胺药应用广泛且适宜性好.

  9. 某综合型医院门诊新型抗组胺药的回顾性处方点评%Retrospective Comments on Prescription of New Type of Oral Antihistamine Drugs for Outpatients in A General Hospital

    Institute of Scientific and Technical Information of China (English)

    万正兰; 郭新铭; 李飞

    2011-01-01

    目的 了解本院新型抗组胺药的临床应用情况和存在的问题.方法 利用医院HIS系统分析门诊2009-12-14~22日含新型第2代、第3代抗组胺药的所有处方.结果 本院的新型抗组胺药应用总体较为合理,但有些处方的适应症及用法用量不适宜,联合用药方面也值得商榷.结论 临床医师应对药品说明书有更多的了解,药师应为临床提供及时的最新用药信息,协助医师提高合理用药水平.

  10. 抗组胺新药枸地氯雷他定研究综述%A Review of the Research on Desloratadine Citrate Disodium, a New Antihistamine Drug

    Institute of Scientific and Technical Information of China (English)

    刘为中; 何广卫; 崔进

    2014-01-01

    枸地氯雷他定是一种可以口服的抗组胺新药,系列的药理、药效、毒理、药代动力学和临床研究证明了枸地氯雷他定缓解慢性特发性荨麻疹及常年性过敏性鼻炎的全身及局部症状的安全和有效性.

  11. 长江流域146家医院抗组胺药用药情况分析%Investigation and Analysis of the Antihistamine Drugs in 146 Hospitals of Drainage Area of the Yangtse River

    Institute of Scientific and Technical Information of China (English)

    王建平; 金大源; 田小宁

    2004-01-01

    目的:分析抗组胺药用药现状和趋势.方法:调查了6城市146家医院2000~2002年抗组胺药的使用金额,分析其临床用药情况.结果:抗组胺药的用药金额2000,2001,2002年分别为人民币4 171.43万,4 382.91万,3908.67万元,2001年较2000年增长4.83%,2002年较2001年减少12.13%.结论:西替利嗪和氯雷他定是首选抗组胺药,此类药物有心脏毒性作用,发生率虽低,但应予以警惕.

  12. 抗组胺药物在儿童和妊娠期妇女中的合理应用%Reasonable Application of Antihistamine Drugs in Children and Pregnant Women

    Institute of Scientific and Technical Information of China (English)

    曹红; 李玫; 徐埏; 李天平; 唐尧

    2008-01-01

    综述了抗组胺药物的分类及其作用特点.通过分析儿童和妊娠期妇女药物代谢动力学的特点,为其选用安全有效的治疗药物,促进抗组胺药物在儿童和妊娠期妇女中的合理应用提供参考.

  13. Retrospective Analysis on the Adverse Drug Reactions(ADR)Induced by Second Generation Antihistamine Drugs%第2代抗组胺药不良反应回顾性分析

    Institute of Scientific and Technical Information of China (English)

    徐珽; 吴逢波; 杨梅; 唐尧

    2007-01-01

    目的:分析第2代抗组胺药所致不良反应的临床特征、相关因素,为临床用药提供参考依据.方法:检索1986~2006年国内文献库收载的第2代抗组胺药的不良反应资料,得到符合标准的病例128例,并按世界卫生组织(WHO)国际药品监测合作中心的不良反应分类方法进行分类、研究.结果:128例ADR报告中女性明显多于男性;不良反应以心血管系统损害最多(38例,占29.69%),其次为皮肤及其附件损害(36例,占28.13%)和全身性损害(20例,占15.63%);不良反应预后较好.结论:患者的性别、体质、合并用药等因素均能影响不良反应的发生,对于引起过敏性休克和心律失常的不良反应临床应提高警惕.

  14. 2008-2010年我院抗组胺药应用分析%Utilization of Antihistamine Drugs in Institute of Dermatology of Chinese Academy of Medical Sciences in Our Hospital During the Period 2008-2010

    Institute of Scientific and Technical Information of China (English)

    龚春燕; 申国庆; 蔡果; 江丽

    2011-01-01

    目的:分析中国医学科学院皮肤痛研究所抗组胺药的应用状况和趋势,为临床合理用药提供参考.方法:利用医院数据库,对我院2008-2010年抗组胺药的用药金额、用药频度(DDDa)和限定日费用(DDC)等进行统计分析.结果:我院抗组胺药用药金额呈逐年上升趋势,2008-2010年,我院抗组胺药用药金额分别为1147、1180和1217万元,2009年和2010年较上年增幅分别为2.88%和3.14%;第2代抗组胺药占据用药金额排序首位,其金额为20272 839.14元,构成比为57.20%.以盐酸左西替利嗪为代表的第3代抗组胺药连续3年居DDDs排序首位,3年来构成比分别为43.1%、38.5%和38.9%;第1代抗组胺药富马酸酮替芬因价格低廉、疗效确切,其用药频度也连续3年位居第3位;国产抗组胺药用药金额逐年上升,3年用药金额分别为575、616和660万元,其构成比分别为50.1%、52.2%和54.3%.结论:抗组胺药在我院临床应用基本合理,第2、3代新型抗组胺药在临床占主导地位.

  15. 抗组胺药敏感性的细胞色素P450研究进展%Study advances of cytochome P450 sensitive to antihistamine drugs

    Institute of Scientific and Technical Information of China (English)

    张毅民; 王乃平

    2005-01-01

    HP450具有细胞色素P450特征和抗组胺药敏感的双重性,它在不同的大鼠肝脏疾病模型中有明显的变化规律,与肝脏疾病的发展具有一定的相关性,在肝癌发生过程中HP450基因的转录及表达均发生了变化.HP450有可能作为诊断肝癌的新指标,在预防和治疗肝癌中可能作为一个新靶点.

  16. 我院2004~2006年抗组胺药应用分析%Use of Antihistamine Agents in Our Hospital During the Period 2004~2006

    Institute of Scientific and Technical Information of China (English)

    赵银安; 颜艳; 燕洪平

    2007-01-01

    目的:了解我院抗组胺药应用现状及趋势,并分析其合理性.方法:调查2004年~2006年我院应用抗组胺药的品种、剂量、消费金额、用药频度(DDDs)和每日平均药费(DDC)等情况.结果:2004年~2006年共应用抗组胺药11个品种;2004年、2005年、2006年的用药金额分别为421 292、459 349和561 942元,年平均增长率为15.50%.DDDs分别为206 747、246 687和230 267,年平均增长率为5.54%,3年之中DDC无差异.结论:分析、掌握药品消费金额和用药频度、对抗组胺药的供应管理至关重要.药品消费结构不够合理,提高合理用药水平有助于降低药费支出.

  17. ADRs in Cardiovascular System Induced by Second Generation Antihistamine Drugs: A Retrospective Analysis%第2代抗组胺药引起心血管系统不良反应的回顾性分析

    Institute of Scientific and Technical Information of China (English)

    李健; 徐珽; 吴蓬波; 唐尧

    2008-01-01

    目的:分析第2代抗组胺药引起心血管系统不良反应的临床特征、相关因素,为不良反应的防治提供参考依据.方法:检索1986.2007年国内文献源第2代抗组胺药引起心血管系统不良反应的资料.不良反应按世界卫生组织(WHO)国际药品监测合作中心的分类方法分类.结果:38例心血管系统不良反应报告中女性明显多于男性;引起不良反应的主要药物是特非拉定(22例)和阿司咪唑(11例);不良反应预后较好.结论:患者的性别、合并用药等因素能影响不良反应的发生,对心血管系统不良反应应提高警惕,减少不良反应的发生.

  18. Sleep disturbances in allergic rhinitis: disease and/or the drug?

    Directory of Open Access Journals (Sweden)

    Anant D. Patil

    2013-12-01

    Full Text Available Allergic rhinitis is a common chronic disease in adults as well as children. Allergic rhinitis has negative impact on sleep and quality of life of the patient. Antihistamines are widely used in the management of allergic rhinitis. First generation antihistamines cause sedation and drowsiness. Second generation antihistamines cause minimal or no sedation. There is difference in propensity to cause sedation amongst second generation antihistamines. As sleep is important for physical as well as mental health, present article reviews impact of allergic rhinitis and antihistamines on sleep. [Int J Basic Clin Pharmacol 2013; 2(6.000: 668-670

  19. 75 FR 51984 - Federal Advisory Committee; Meeting of the Uniform Formulary Beneficiary Advisory Panel

    Science.gov (United States)

    2010-08-24

    ... Stabilizers, Steroids, and Antihistamines), Renin-Angiotensin Antihypertensives (RAAS), pertinent utilization management issues, drugs recommended for non-formulary placement due to non-compliance with the...

  20. Drug: D08161 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available histamines for systemic use R06AX15 Mebhydrolin D08161 M...ification [BR:br08303] R RESPIRATORY SYSTEM R06 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other anti

  1. 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

  2. Drug: D07307 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07307 Drug Cyamemazine (INN); Tercian (TN) C19H21N3S 323.1456 323.4551 D07307.gif Neuroleptic; Antihistamin...ic ATC code: N05AA06 Anatomical Therapeutic Chemical (ATC) classification [BR:br083

  3. Drug: D02599 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D02599 Drug Orphenadrine hydrochloride; Disipal (TN) C18H23NO. HCl 305.1546 305.8423 D02599.gif Antihistamin...ic; Relaxant [skeletal muscle] ATC code: N04AB02 muscarinic cholinergic receptor an

  4. Drug: D09705 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ent of ocular itching, Antihistaminic second-generation antihistamine drug H1-receptor antagonist [HSA:3269]...D09705 Drug Bepotastine (USAN/INN) C21H25ClN2O3 388.1554 388.8878 D09705.gif Treatm

  5. Drug: D03963 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03963 Drug Efletirizine dihydrochloride (USAN) C21H24F2N2O3. 2HCl 462.1289 463.3455 D03963.gif Antihistamin...ic CAS: 225367-66-8 PubChem: 47205949 LigandBox: D03963 ATOM 30 1 X Cl 39.4073 -21.

  6. The safety and efficacy of subcutaneous birch pollen immunotherapy - a one-year, randomised, double-blind, placebo-controlled study

    DEFF Research Database (Denmark)

    Bødtger, Uffe; Poulsen, L K; Jacobi, H H;

    2002-01-01

    was conducted as a clustered regimen and was performed in a specialist unit. Symptom scores from nose, eyes, and lungs, and use of oral and topical antihistamines, beta-2-agonists, and oral corticosteroids were recorded daily during the season of 2000. Sensitivity to allergen provocation in skin, conjunctiva...... antihistamines (P

  7. Drug: D02234 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available erapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 44 Allergic agents 441 Antihistamine...adine D02234 Cyproheptadine hydrochloride (JP16/USP) USP drug classification [BR:br08302] Respiratory Tract/Pulmonary Agents Antihist...amines Cyproheptadine D02234 Cyproheptadine hydrochlorid

  8. 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 performan

  9. Analysis on the Utilization of Antihistamine Drugs in Guangxi Zhuang Nationality Autonomous Region Dermatological Hospital from 2006 to 2010%2006-201O年广西壮族自治区皮肤病医院抗组胺药应用分析

    Institute of Scientific and Technical Information of China (English)

    黄琳

    2011-01-01

    目的:了解广西壮族自治区皮肤病医院抗组胺药应用情况和发展趋势,探讨抗组胺药的合理应用问题.方法:采用用药频度(DDDs)、日均费用(DDC)、DDDs排序、金额排序及排序比(B/A),结合处方点评结果,分析我院2006-2010年抗组胺药应用情况.结果:我院抗组胺药的用药金额、DDDs呈逐年增长态势.结论:安全、有效、应用方便的第2、3代抗组胺药是我院临床应用的主要药物,价格低廉但作用肯定的第1代抗组胺药仍发挥其独特效应,医疗机构应加强抗组胺药管理,提高药物治疗水平.

  10. Forty-Nine Cases with Chronic Urticaria Treated with Blood-Nourishing and Wind-Expelling Prescription Combined with Antihistamine Drugs%养血祛风方联合抗组胺药治疗慢性荨麻疹49例

    Institute of Scientific and Technical Information of China (English)

    吴忠珍

    2016-01-01

    目的:观察养血祛风方联合抗组胺药治疗慢性荨麻疹的临床疗效.方法:选取2011年12月—2012年12月在本院诊疗的慢性荨麻疹患者98例,随机分为观察组和对照组,每组49例.对照组给予常规抗组胺药治疗,观察组在对照组治疗的基础上加用养血祛风方治疗.结果:观察组有效率95.9%,对照组有效率85.7%,观察组优于对照组(P<0.05);治疗后,观察组患者血清IgE、IL-4、IFN-γ水平优于对照组(P<0.05).结论:养血祛风方联合抗组胺药治疗慢性荨麻疹疗效确切,能有效降低血清荨麻疹相关细胞因子的表达.

  11. Safety,therapeutic effect and correlative issues of using Antihistamine drug in pregnant,lactational and infant patients%妊娠、哺乳期及婴幼儿患者抗组胺药物应用的安全性、疗效及相关问题

    Institute of Scientific and Technical Information of China (English)

    刘宏杰; 郭在培

    2009-01-01

    抗组胺药物广泛应用于各种变应性疾病、瘙痒性皮肤病的治疗及预防,其疗效肯定,耐受性好.文中就近10年来妊娠、哺乳期及婴幼儿患者抗组胺药物应用的安全性、疗效及相关问题进行了综述.

  12. 1999年~2001年上海市47家医院抗组胺药应用分析%Analysis of the Use of Antihistamine Agents in 47 Hospitals of Shanghai During the 1999~ 2001 Period

    Institute of Scientific and Technical Information of China (English)

    归成; 徐红冰; 席宇飞

    2002-01-01

    目的:分析上海市47家医院抗组胺药的应用情况,供生产、营销、应用等部门参考.方法:调查上海市47家医院1999年~2001年抗组胺药主要品种、用量、金额、DDDs以及临床的评价和不良反应.结果与结论:抗组胺药品种变化不大,用量2001年有所下降,目前最常用的为西替利嗪、氯雷他定和酮替芬等.报道的心脏毒性发生率虽然极低,亦应警惕.

  13. Comparative Activity of Antihistamines on Area Under Dose-response Curve from Histamine-induced Wheal and Flare Responses in Human Skin%组胺点刺皮肤试验的剂量--反应曲线下面积比较抗组胺药物的活性

    Institute of Scientific and Technical Information of China (English)

    王瑞琦; 张宏誉

    2004-01-01

    目的应用组胺点刺皮肤试验的剂量-反应曲线下面积(AUDRC)比较抗组胺药物(咪唑斯汀和氯雷他定)的抗组胺活性.方法90名健康志愿者及60例过敏性疾病患者,按随机、双盲的方法单次口服咪唑斯汀10 mg,氯雷他定10 mg或安慰剂1片.服药前及服药后2、4和24h分别进行组胺皮肤滴定试验,记录风团及红晕反应面积,计算AUDRC.结果健康志愿者和过敏患者在服药前及服药后2、4和24 h的风团及红晕反应差异均无显著性.服药前,咪唑斯汀、氯雷他定和安慰剂3组的AUDRC2.7-54.3mmol/L差异无显著性.服药后,咪唑斯汀组和氯雷他定组的AUDRC2.7-54.3mmol/L均比服药前明显下降,且咪唑斯汀组的AUDRC2.7-54.3mmol/L下降幅度较大(P<0.01).结论依据抗组胺药物对组胺点刺皮肤试验的抑制作用可建立药效动力学模型,AUDRC可作为比较抗组胺药物药效动力学活性的一个指标.

  14. Neuropatía hemorrágica tóxica aguda y fallo multiorgánico tras intoxicación por anticoagulantes, disolventes, AINES y antihistamínicos: A propósito de un caso fatal Acute toxic haemorrhagic neuropathy and multiorganic failure following poisoning by anticoagulants, solvents, nsaids and antihistaminic drugs: Report of a fatal case

    Directory of Open Access Journals (Sweden)

    A. Garfia

    2002-01-01

    Full Text Available Se presenta un caso de intoxicación mortal por ingestión del raticida Brodifacum, un anticoagulante superwarfarínico, junto con otros fármacos, entre los que se incluían antiinflamatorios no esteroideos y un disolvente orgánico de uso doméstico. El sujeto falleció en la UCI, con un cuadro de insuficiencia respiratoria aguda, seguida de fallo hepático y renal. En la autopsia se pusieron de manifiesto lesiones hemorrágicas circunferenciales que afectaban a diversos tejidos, entre los que se encontraban la grasa mesentérica, el epicardio, y la grasa perirrenal. El estudio microscópico demostró la existencia de una típica lesión hemorrágica aguda, circunferencial, en los nervios vegetativos epicárdicos y del área del esplácnico. La explicación de porqué los nervios periféricos vegetativos se constituyen en diana de los efectos tóxicos se atribuye a la acción combinada de los disolventes y de los anticoagulantes, sobre el sistema nervioso periférico. Se sabe que los disolventes orgánicos producen una lesión neuronal aguda, consistente en tumefacción axonal y del soma neuronal, que conlleva a la alteración del sistema de transporte a lo largo del axón. Creemos que -desde el punto de vista fisiopatológico- la vasodilatación reactiva de los vasa nervorum, producida a consecuencia de la lesión neuronal aguda inducida por los disolventes, unida al estado de hipocoagulabilidad sanguínea -dependiente de la ingestión de Brodifacum (superwarfarina y potenciada por los antiinflamatorios no esteroideos- constituyen los mecanismos íntimos que podrían explicar esta peculiar Neuropatía Hemorrágica Aguda Tóxica de los nervios periféricos del Sistema Nervioso Neurovegetativo. Desconocemos si los nervios periféricos mixtos se encontraban afectados por esta lesión, al carecer de muestras para un estudio definitivo.In this paper we describe a case of mortal poisoning by ingestion of the rodenticide Brodifacoum, a superwarfarin anticoagulant, together with other drugs, among which were non steroid anti-inflammatory drugs and a domestic organic solvent. The individual died in the Intensive Care Unit, with acute respiratory insufficiency, followed by hepatic and renal failure. At autopsy round haemorrhagic lesions were seen, which affected several tissues, among which were mesenteric fat, the epicardium, and the peri-renal fat. Microscopic study revealed the existence of a typical acute haemorrhagic lesion, located around the epicardial vegetative nerves and those found in the splanchnic beds. The reason why the peripheral vegetative nerves constitute the target of the toxic effects is attributed to the combined action of the solvents together with the superwarfarin drug, on the Peripheral Nervous System. It is known that organic solvents produce an acute neuronal lesion, consisting in tumefaction of the axon and the neuronal soma, which leads to the alteration of the system of transport (neurotubules along the axon. We believe that - from a physiological point of view - the reactive vascular congestion of the vasa-nervorum, produced as a consequence of the acute neuronal lesion induced by the solvents, together with the state of hipocoagulability of the blood - due to the ingestion of the superwarfarin (Brodifacoum and potentiated by the the anticoagulant action of the non steroid anti-inflammatory drugs - make up the intimate mechanisms which could explain this characteristic Acute Toxic Haemorrhagic Neuropathy of the peripheral nerves of the Neurovegetative Nervous System. We do not know if the mixed peripheral nerves were affected by this lesion, due to absence of samples for a more definitive study.

  15. Neuropatía hemorrágica tóxica aguda y fallo multiorgánico tras intoxicación por anticoagulantes, disolventes, AINES y antihistamínicos: A propósito de un caso fatal Acute toxic haemorrhagic neuropathy and multiorganic failure following poisoning by anticoagulants, solvents, nsaids and antihistaminic drugs: Report of a fatal case

    OpenAIRE

    2002-01-01

    Se presenta un caso de intoxicación mortal por ingestión del raticida Brodifacum, un anticoagulante superwarfarínico, junto con otros fármacos, entre los que se incluían antiinflamatorios no esteroideos y un disolvente orgánico de uso doméstico. El sujeto falleció en la UCI, con un cuadro de insuficiencia respiratoria aguda, seguida de fallo hepático y renal. En la autopsia se pusieron de manifiesto lesiones hemorrágicas circunferenciales que afectaban a diversos tejidos, entre los que se enc...

  16. Fatigue

    Science.gov (United States)

    ... Taking certain medicines, such as antidepressants, antihistamines, and medicines for nausea and pain Having medical treatments, like chemotherapy and radiation Recovering from major surgery Anxiety, stress, or depression Staying up too late Drinking too much alcohol ...

  17. 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 ...

  18. Weekly injection of histaglobulin produces long-term remission in chronic urticaria: A prospective clinical study

    Directory of Open Access Journals (Sweden)

    Gurumoorthy Rajesh

    2016-01-01

    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.

  19. 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.

  20. Nosebleeds (For Parents)

    Science.gov (United States)

    ... and Remedies Tips for Preventing Nosebleeds en español Hemorragias nasales Nosebleeds are common in kids 3 to ... prescribe medicine (such as antihistamines or decongestants) to control an itchy, runny, or stuffy nose. The medicine ...

  1. Nosebleeds

    Science.gov (United States)

    ... Nosebleeds Causes and Remedies Preventing Nosebleeds en español Hemorragias nasales Sitting in science class one afternoon, you ... prescribe medicine such as antihistamines or decongestants to control an itchy, runny, or stuffy nose. The medicine ...

  2. Temsirolimus

    Science.gov (United States)

    ... your doctor if you are allergic to temsirolimus, sirolimus, antihistamines, any other medications, polysorbate 80, or any ... Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), and sertraline (Zoloft); sirolimus (Rapamune, Rapamycin); sunitinib (Sutent); and telithromycin (Ketek). Many ...

  3. A randomized, double-blind, placebo-controlled study of latrepirdine in patients with mild to moderate Huntington disease

    DEFF Research Database (Denmark)

    Hjermind, Lena Elisabeth

    2013-01-01

    BACKGROUND Latrepirdine is an orally administered experimental small molecule that was initially developed as an antihistamine and subsequently was shown to stabilize mitochondrial membranes and function, which might be impaired in Huntington disease. OBJECTIVE To determine the effect of latrepir...

  4. Treatment of the Hyperactive Child

    Science.gov (United States)

    Wunderlich, Ray C.

    1973-01-01

    Described individually are the following forms of medical treatment for the hyperactive child: stimulants, tranquilizers, megavitamins, corticosteroids, antihistamines, anticonvulsants, food elimination, air filtration, allergic desensitization, perceptual motor training, and behavioral counseling. (DB)

  5. Drug: D01782 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available antagonists Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 44 Allergic agents 441 Antihista...mines 4412 Tripelennamines D01782 Triprolidine hydrochloride hydrate (JAN); Triprol

  6. Drug: D01172 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available r antagonists Therapeutic category of drugs in Japan [BR:br08301] 4 Agents affecting cellular function 44 Allergic agents 441 Antihis...tamines 4415 Diphenylpyralines D01172 Diphenylpyraline hydrochloride (JAN) Anatomic

  7. Development of a C3 generic workstation: System overview

    Science.gov (United States)

    Strome, David R.

    1988-01-01

    A command, control, and communications (C3) environment is described which will be applied to the evaluation of performance of aircrews, particularly in situations in which they are subjected to chemical defense protection drugs and antihistamines.

  8. Seasonal Allergies: Symptoms, Diagnosis, and Treatment

    Science.gov (United States)

    ... usually used in combination with antihistamines. Long-term usage of spray decongestants can actually make symptoms worse, ... Contact Us | Viewers & Players Friends of the National Library of Medicine (FNLM)

  9. Seasonal Allergies: Diagnosis, Treatment & Research

    Science.gov (United States)

    ... usually used in combination with antihistamines. Long-term usage of spray decongestants can actually make symptoms worse, ... Contact Us | Viewers & Players Friends of the National Library of Medicine (FNLM)

  10. Pyridoxine (Vitamin B6)

    Science.gov (United States)

    ... B6 (pyridoxine) and a sleep-inducing antihistamine called doxylamine. The makers of Bendectin took it off the ... by pregnancy. Vitamin B6 (pyridoxine) plus the medication doxylamine is recommended for women who do not get ...

  11. 21 CFR 310.545 - Drug products containing certain active ingredients offered over-the-counter (OTC) for certain uses.

    Science.gov (United States)

    2010-04-01

    ...), anticholinergic, antihistamine, oral antitussive, or stimulant active ingredient. (7) Dandruff/seborrheic... Mono- and di-glycerides Niacinamide Organic vegetables Pancreatin Pantothenic acid Papain Papaya... blue Natural estrogenic hormone Niacinamide Nutmeg oil (oil of nutmeg) Oil of erigeron...

  12. Comparative evaluation of H1 receptor blocking activity and safety of newer H1antagonist mizolastine with loratadine and placebo: a randomized double blind three way crossover study

    Directory of Open Access Journals (Sweden)

    K. Swarnalatha

    2016-06-01

    Conclusions: Mizolastine has good antihistaminic activity than loratadine. Neither drug causes any psychomotor impairment or has anti-cholinergic action. [Int J Basic Clin Pharmacol 2016; 5(3.000: 661-675

  13. Recurrent facial urticaria following herpes simplex labialis.

    Science.gov (United States)

    Zawar, Vijay; Godse, Kiran

    2012-03-01

    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.

  14. Recurrent facial urticaria following herpes simplex labialis

    OpenAIRE

    Vijay Zawar; Kiran Godse

    2012-01-01

    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.

  15. Isolation of stigmast-5,24-dien-3-ol from marine brown algae Sargassum tenerrimum and its antipredatory activity

    Digital Repository Service at National Institute of Oceanography (India)

    Majik, M.S.; Adel, H.; Shirodkar, D.; Tilvi, S.; Furtado, J.

    - diabetic,13 antihistaminic, and anticholinergic.14 Additionally, Vahouny et al. reported that fucosterol reduces the gastrointestinal absorption of cholesterol15 and Hagiwara et al. observed that, fucosterol decreases angiotensin converting enzyme levels...

  16. Effect of bilastine upon nasal obstruction.

    Science.gov (United States)

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

    2011-01-01

    H1 antihistamines constitute one of the main references for the treatment of allergic rhinitis. Classically, these drugs have been considered effective in controlling sneezing, rhinorrhea and itching, though they have not been regarded as particularly effective in application to nasal obstruction. The most recent studies, involving second-generation H1 antihistamines (desloratadine, fexofenadine, levocetirizine, rupatadine), have shown these drugs to offer effects upon nasal obstruction significantly superior to those of placebo. The present review examines the effect of bilastine, a new, potent and highly specific H1 antihistamine without sedative effects or cardiac toxicity, upon nasal obstruction. The analysis of the data from the different clinical trials indicates that in patients with allergic rhinitis, the effect of bilastine upon nasal obstruction is superior to that of placebo and similar to that of other second-generation H1 antihistamines, manifesting within 24 hours after the start of treatment.

  17. What Is Atopic Dermatitis?

    Science.gov (United States)

    ... an insect bite). Nummular eczema. The skin has coin-shaped spots of irritation. The spots can be ... reactions Corticosteroids Antibiotics to treat infections caused by bacteria Antihistamines that make people sleepy to help stop ...

  18. Aspirin to Zoloft: Ways Medicines Work

    Science.gov (United States)

    ... View All Articles | Inside Life Science Home Page Aspirin to Zoloft: Ways Medicines Work By Emily Carlson ... biology of how cancer cells grow. Antihistamines, Antidepressants, Aspirin Adrenergic receptor with carazolol, a beta-blocker. View ...

  19. Hives (Urticaria)

    Science.gov (United States)

    ... Loss Surgery? A Week of Healthy Breakfasts Shyness Hives (Urticaria) KidsHealth > For Teens > Hives (Urticaria) A A A ... prescribed an antihistamine to treat it. What Is Urticaria? The medical name for hives is urticaria . It's ...

  20. 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.

  1. Drug: D07403 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07403 Drug Pyrrobutamine (BAN) C20H22ClN 311.1441 311.8484 D07403.gif ATC code: R0...NES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other antihistamines for systemic use R06AX08 Pyrrobutamine D07403... Pyrrobutamine (BAN) CAS: 91-82-7 PubChem: 51091739 LigandBox: D07403

  2. Buclizine- old wine in new bottle?

    OpenAIRE

    Rakesh C. Chaurasia; Sandhya Chandra

    2012-01-01

    Buclizine is a first generation antihistaminic with some anticholinergic potential. This drug has specific pharmacological indications in allergy, morning sickness, migraine, motion sickness and insomnia with some or doubtful success. It is an obsolete drug of decline use due to better availability of second and third generation antihistamines. Buclizine, a forgotten drug used in past is now re-introduced as an appetite stimulant. Previously one of the counterpart “cyproheptadine”...

  3. Pharmacology of Nasal Medications: An Update

    OpenAIRE

    Martin, G. F.

    1988-01-01

    The author of this article reviews the pharmacology of nasal medication, focusing on the indications and side-effects. The newer group of non-sedating antihistamines proves to be a useful supplement to disodium cromoglycate and the traditional antihistamines in the treatment of allergic rhinitis. The topical steroids (flunisolide and beclomethasone dipropionate) did not produce a significant incidence of adrenal suppression, mucosal atrophy, or nasal candidiasis. The anticholinergic ipatropiu...

  4. Promethazine as a Novel Prophylaxis and Treatment for Nerve Agent Poisoning

    Science.gov (United States)

    2008-12-01

    21010-5400 ABSTRACT The present study evaluated promethazine, an FDA-approved antihistamine , for treating the toxic effects of soman (GD...adjunct or alone is an effective countermeasure against GD poisoning. Moreover, as an FDA-approved drug , promethazine could be transitioned quickly...these findings suggest that antihistamine treatment could be beneficial in reducing the incidence of HPE and mortality following GD poisoning. The

  5. Effects of a single dose of Bilastine 20mg on flying ability in healthy volunteers under conditions of simulated cabin pressure

    OpenAIRE

    Valk, P.J.L.; Jetten, A. M.; M. Simons

    2015-01-01

    Background : Optimal physical and mental fitness of pilots is a prerequisite for flight safety. Pilots suffering from allergic rhinoconjuctivitis or other allergic upper airway diseases are not allowed to fly because ambient pressure changes may aggravate the symptoms and some antihistaminic medication may interfere with flight safety, probably due to their sedative effects. Bilastine is a new second-generation highly selective H1 antihistamine that has been developed for the treatment of all...

  6. Molecular determinants responsible for sedative and non-sedative properties of histamine H₁-receptor antagonists.

    Science.gov (United States)

    Uesawa, Yoshihiro; Hishinuma, Shigeru; Shoji, Masaru

    2014-01-01

    There is argument whether non-sedative properties of histamine H1-receptor antagonists (antihistamines) are determined by their active extrusions from the brain via P-glycoprotein or their restricted penetration through the blood-brain barrier. We have reported that sedative and non-sedative antihistamines can be well discriminated by measuring changes in their binding to H1 receptors upon receptor internalization in intact cells, which depends on their membrane-penetrating ability. In this study, molecular determinants responsible for sedative and non-sedative properties of antihistamines were evaluated by quantitative structure-activity relationship (QSAR) analyses. Multiple regression analyses were applied to construct a QSAR model, taking internalization-mediated changes in the binding of antihistamines as objective variables and their structural descriptors as explanatory variables. The multiple regression model was successfully constructed with two explanatory variables, i.e., lipophilicity of the compounds at physiological pH (logD) and mean information content on the distance degree equality (IDDE) (r(2) = 0.753). The constructed model discriminated between sedative and non-sedative antihistamines with 94% accuracy for external validation. These results suggest that logD and IDDE concerning lipophilicity and molecular shapes of compounds, respectively, predominantly determine the membrane-penetrating ability of antihistamines for their side effects on the central nervous system.

  7. Re-analysis of safety data supporting doxylamine use for nausea and vomiting of pregnancy.

    Science.gov (United States)

    Chin, Jessica W S; Gregor, Sarah; Persaud, Navindra

    2014-09-01

    Antihistamines are commonly used to treat nausea and vomiting of pregnancy (NVP). We re-analyzed the 24 primary studies cited in a 1997 meta-analysis that concluded antihistamine use for NVP was safe as they had been studied in more than 200,000 participating women and the pooled odds ratio for congenital malformations was 0.76 (95% confidence interval [CI]: 0.60-0.94). Our analysis of this meta-analysis showed that 139,414 women were included in 22 original studies involving antihistamines, 129,108 of which were in studies involving doxylamine. In these studies, 23,485 women were exposed to antihistamines, 14,624 of which were exposed to doxylamine. The summary relative risk (cohort studies) and odds ratio (case-control studies) for congenital malformations from antihistamine exposure were 1.09 (95% CI: 1.01-1.18) and 1.04 (95% CI: 0.91-1.19), and for doxylamine exposure, the summary relative risk and odds ratio were 0.94 (95% CI: 0.80-1.10) and 1.07 (95% CI: 0.93-1.23), respectively. Although not a new systematic review, our re-analysis demonstrates that the safety data for antihistamines, and doxylamine in particular, are based on many fewer than 200,000 participating women and exposures, and that doxylamine use is not associated with a decreased risk of malformations as previously reported.

  8. 中药内服、外洗并联合抗组胺药物治疗慢性肾功能不全非透析患者瘙痒症状随机对照研究%Randomized Controlled Trail on Internal and External Application of TCM Drugs Combined with Antihistamine in Treatment of Non-Dialysis Patients With Chronic Renal Failure and Pruritus

    Institute of Scientific and Technical Information of China (English)

    陈肖蓉; 孔祥栋

    2013-01-01

    目的:探讨中药内服、外洗并联合抗组胺药物治疗慢性肾功能不全非透析患者瘙瘁的疗效.方法:选择90例慢性肾功能不全合并皮肤瘙瘁症的患者,随机分为3组,每组30例,A组予抗阻胺药物治疗,B组予中药内服、外洗治疗,C组患者予中药内服、外洗联合抗组胺药物治疗,观察三组患者治疗前后生化指标及皮肤瘙痒缓解程度的变化.结果:治疗后C组瘙痒程度积分明显低于其他两组(P<0.05);C组的BUN、P、iPTH水平的下降以及Ca上升的改善均较A组、B组高,B组较A组高,且差异有统计学意义(P均<0.05).结论:中药内服、外洗加药物口服治疗慢性肾功能不全伴有瘙痒患者,能明显减轻瘙痒症状.

  9. Effects of single therapeutic doses of promethazine, fexofenadine and olopatadine on psychomotor function and histamine-induced wheal- and flare-responses: a randomized double-blind, placebo-controlled study in healthy volunteers.

    Science.gov (United States)

    Kamei, Hiroyuki; Isaji, Ami; Noda, Yukihiro; Ishikawa, Kazuhiro; Senzaki, Koji; Yamada, Kiyofumi; Sugiura, Kazumitsu; Tomita, Yasushi; Nabeshima, Toshitaka

    2012-05-01

    Since most first-generation antihistamines have undesirable sedative effects on the central nervous systems (CNS), newer (second-generation) antihistamines have been developed to improve patients' quality of life. However, there are few reports that directly compare the antihistaminic efficacy and impairment of psychomotor functions. We designed a double-blind, placebo controlled, crossover study to concurrently compare the clinical effectiveness of promethazine, a first-generation antihistamine, and fexofenadine and olopatadine, second-generation antihistamines, by measuring their potency as peripheral inhibitors of histamine-induced wheal and flare. Further, we investigated their sedative effects on the CNS using a battery of psychomotor tests. When single therapeutic doses of fexofenadine (60 mg), olopatadine (5 mg) and promethazine (25 mg) were given in a double-blind manner to 24 healthy volunteers, all antihistamines produced a significant reduction in the wheal and flare responses induced by histamine. In the comparison among antihistamines, olopatadine showed a rapid inhibitory effect compared with fexofenadine and promethazine, and had a potent effect compared with promethazine. In a battery of psychomotor assessments using critical flicker fusion, choice reaction time, compensatory tracking, rapid visual information processing and a line analogue rating scale as a subjective assessment of sedation, promethazine significantly impaired psychomotor function. Fexofenadine and olopatadine had no significant effect in any of the psychomotor tests. Promethazine, fexofenadine and olopatadine did not affect behavioral activity, as measured by wrist actigraphy. These results suggest that olopatadine at a therapeutic dose has greater antihistaminergic activity than promethazine, and olopatadine and fexofenadine did not cause cognitive or psychomotor impairment.

  10. 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...

  11. 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

  12. 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.

  13. Drug: D08183 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08183 Drug Mepyramine (INN) C17H23N3O 285.1841 285.384 D08183.gif Antiallergic; Hi...A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AA Antihistamines for topical use D04AA02 Mepyramine D08183... USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AC Substituted ethylene diamines R06AC01 Mepyramine D08183 Mepy...Histamine H1-receptor [HSA:3269] [KO:K04149] Mepyramine [ATC:D04AA02 R06AC01] D08183... Mepyramine (INN) CAS: 91-84-9 PubChem: 96024873 LigandBox: D08183 NIKKAJI: J4.645K ATOM 21 1 C8x C 20.51

  14. Doxylamine overdose as a potential cause of rhabdomyolysis.

    Science.gov (United States)

    Leybishkis, B; Fasseas, P; Ryan, K F

    2001-07-01

    Doxylamine succinate, an over-the-counter antihistamine, is commonly used as a nighttime sleep aid in the short-term management of insomnia. It is also used in combination with antitussive and decongestant agents for the temporary relief of common cold symptoms. Doxylamine is frequently involved in accidental and intentional overdoses. Rhabdomyolysis and secondary acute renal failure are rare but potentially serious complications, making early recognition and treatment essential. With the large number of nonprescription antihistamines and sleep aids available to the general public, it is important to keep in mind that overdose is a potential problem. The complications associated with overdose of these medications are just as life threatening as those associated with prescription drugs. A high index of suspicion and evaluation of rhabdomyolysis is warranted in antihistamine toxicity. We report an observation of severe rhabdomyolysis associated with doxylamine overdose.

  15. 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.

  16. A Review of International Recommendations for the Diagnosis and Management of Chronic Urticaria.

    Science.gov (United States)

    Beck, Lisa A; Bernstein, Jonathan A; Maurer, Marcus

    2017-02-08

    Both spontaneous and inducible forms of chronic urticaria pose a significant economic burden and have an adverse effect on patients' quality of life. The international guidelines and US practice parameters for the diagnosis and management of chronic urticaria both recommend performing a thorough patient history and physical examination, conducting limited routine laboratory testing, and taking a stepwise approach to treatment. These documents differ in several areas, such as the order of diagnostic procedures and the treatment for patients non-responsive to standard dose H1-antihistamines. Patients with chronic urticaria who visit a specialist have typically been treated with second-generation H1-antihistamines - the recommended first-line treatments. The advantages and disadvantages of each treatment option should be taken into consideration when selecting therapies beyond H1-antihistamines. Greater awareness of the international guidelines and US practice parameters will likely improve the quality of care for patients with chronic urticaria.

  17. 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...

  18. Pre-hospital treatment of bee and wasp induced anaphylactic reactions

    DEFF Research Database (Denmark)

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

    2017-01-01

    was assessed according to Sampson's severity score and Mueller's severity score. Treatment was evaluated in relation to administration of adrenaline, glucocorticoids and antihistamine. RESULTS: We identified 273 cases (Odense 2008 n = 14 and Region of Southern Denmark 2009-2014 n = 259) of bee and wasp induced...... could not be graded according to Mueller's severity score. Adrenaline was administrated in 54% (96/177) of cases with moderate to severe anaphylaxis according to Sampson's severity score, compared to 88% receiving intravenous glucocorticoids (p antihistamines (p...

  19. 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....

  20. Drug: D07662 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07662 Drug Cetirizine (INN); Cetiderm (TN) C21H25ClN2O3 388.1554 388.8878 D07662.g...FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AE Piperazine derivatives R06AE07 Cetirizine D07662 Cetirizine...y Agents Antihistamines Cetirizine D07662 Cetirizine (INN) Target-based classification of drugs [BR:br08310]... G Protein-coupled receptors Rhodopsin family Histamine H1-receptor [HSA:3269] [KO:K04149] Cetirizine [ATC:R06AE07] D07662 Cetirizine... (INN) USP drug classification [BR:br08302] Respiratory Tract/Pulmonar

  1. Drug: D08497 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08497 Drug Rupatadine fumarate; Rinialer (TN) C26H26ClN3. C4H4O4 531.1925 532.0299...SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AX Other antihistamines for systemic use R06AX28 Rupatadine D08497 Ru...patadine fumarate Target-based classification of drugs [BR:br08310] G Protein-coupled receptor...s Rhodopsin family Histamine H1-receptor [HSA:3269] [KO:K04149] Rupatadine [ATC:R06AX28] D08497 Ru

  2. Advertisements impact the physiological efficacy of a branded drug.

    Science.gov (United States)

    Kamenica, Emir; Naclerio, Robert; Malani, Anup

    2013-08-06

    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.

  3. Factitious urticaria (dermographism): treatment by cimetidine and chlorpheniramine in a randomized double-blind study.

    Science.gov (United States)

    Kaur, S; Greaves, M; Eftekhari, N

    1981-02-01

    The HI-antihistamine chlorpheniramine and the H2-antihistamine cimetidine, given alone and in combination, have been compared with placebo in twenty patients with factitious urticaria (dermographism), in a double-blind, randomized cross-over trial. Of these regimes, the combination was the only treatment which significantly reduced weal size, flare size and duration of weal, compared with placebo, although other treatments approached statistical significance. Continuation of the most effective of the four treatments in nineteen of the patients for a further 3 months without breaking the randomization code provided further evidence of the great effectivness of combined cimetidine and chlorpheniramine. No significant side effects were note.

  4. ASSURE-CSU : A real-world study of burden of disease in patients with symptomatic chronic spontaneous urticaria

    NARCIS (Netherlands)

    Weller, Karsten; Maurer, Marcus; Grattan, Clive; Nakonechna, Alla; Abuzakouk, Mohamed; Bérard, Frédéric; Sussman, Gordon; Giménez-Arnau, Ana M.; Ortiz De Frutos, Javier; Knulst, André; Canonica, G. Walter; Hollis, Kelly; McBride, Doreen; Balp, Maria Magdalena

    2015-01-01

    BACKGROUND: Chronic spontaneous urticaria (CSU) formerly known as chronic idiopathic urticaria (CIU) is a severe and distressing skin condition that remains uncontrolled in approximately one half of patients, despite the use of licensed, recommended doses of modern, second-generation H1-antihistamin

  5. Adverse Reaction to Omalizumab in Patients with Chronic Urticaria: Flare Up or Ineffectiveness?

    Science.gov (United States)

    Ertaş, Ragıp; Özyurt, Kemal; Yıldız, Sinem; Ulaş, Yılmaz; Turasan, Abdullah; Avcı, Atıl

    2016-02-01

    Omalizumab is a recombinant humanized anti-Ig E monoclonal antibody used as the third line treatment of chronic spontaneous urticaria (CSU). We report four patients with severe antihistamine-resistant CSU, who developed angioedema, anaphylaxis and/or flare up of urticaria at different times following omalizumab therapy.

  6. 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 ...

  7. Pyrimidine as antiinflammatory agent: A review

    Directory of Open Access Journals (Sweden)

    Amir M

    2007-01-01

    Full Text Available Pyrimidine nucleus exhibited remarkable pharmacological activities. Literature indicates that compounds having pyrimidine nucleus have wide range of therapeutic uses that include antiinflammatory, antibacterial, anticancer, antiviral, antiHIV, antimalarial, antihypertensive, sedatives and hypnotics, anticonvulsant and antihistaminic. The present review provides a broad view of the antiinflammatory activity possessed by compounds having a pyrimidine nucleus.

  8. [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.

  9. Hyperemesis gravidarum

    DEFF Research Database (Denmark)

    Schouenborg, L O; Honnens de Lichtenberg, M; Djursing, H;

    1992-01-01

    of the pregnancy usually runs a normal course. All of the forms of treatment are dominated by the tendency to spontaneous remission and great placebo effect. Antihistamines, antiemetics, ginger, change of environment, hypnotherapy and psychotherapy appear to be the best forms of treatment....

  10. Drug: D04046 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available STEM N02 ANALGESICS N02B OTHER ANALGESICS AND ANTIPYRETICS N02BA Salicylic acid and derivatives N02BA55 Salicylamide, combinations...TEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AD Phenothiazine derivatives R06AD52 Promethazine, combinations

  11. Drug: D04044 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available EM N02 ANALGESICS N02B OTHER ANALGESICS AND ANTIPYRETICS N02BA Salicylic acid and derivatives N02BA55 Salicylamide, combinations...6A ANTIHISTAMINES FOR SYSTEMIC USE R06AB Substituted alkylamines R06AB54 Chlorphenamine, combinations D04044

  12. Drug: D01358 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 93 300.8257 D01358.gif Serotonin inhibitor; Antihistaminic Therapeutic category: 1179 ATC code: N06AX03 Tetracyclic antidepressant...peutic Chemical (ATC) classification [BR:br08303] N NERVOUS SYSTEM N06 PSYCHOANALEPTICS N06A ANTIDEPRESSANTS N06AX Other antidepressa...nts N06AX03 Mianserin D01358 Mianserin hydrochloride (JA

  13. 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

    1993-01-01

    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

  14. 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...

  15. 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...

  16. 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...

  17. Drug: D02327 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D02327 Drug Doxylamine succinate (USP); Decapryn (TN) C17H22N2O. C4H6O4 388.1998 388.4574 D02327.gif Antihis...taminic Same as: C19414 ATC code: R06AA09 H1-receptor antagonist [HSA:3269] [KO:K04

  18. Drug: D00234 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 0234.gif Anti-allergic; Antihistaminic Same as: C06832 ATC code: R06AX11 H1-receptor antagonist [HSA:3269] [...D00234 Drug Astemizole (JAN/USP/INN); Hismanal (TN) C28H31FN4O 458.2482 458.5703 D0

  19. Drug: D08768 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08768 Drug Promethazine hibenzate; Hiberna (TN) C17H20N2S. C14H10O4 526.1926 526.6459 D08768.gif Antihistam...inic Therapeutic category: 4413 ATC code: D04AA10 R06AD02 H1-receptor antagonist [H

  20. Drug: D00663 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 41 435.3116 D00663.gif Antihistaminic ATC code: R06AB01 H1-receptor antagonist [HSA:3269] [KO:K04149] hsa040...D00663 Drug Brompheniramine maleate (USAN); Dimetane (TN) C16H19BrN2. C4H4O4 434.08

  1. Drug: D07756 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 07756.gif Neuroleptic; Antihistaminic ATC code: N05AA06 Anatomical Therapeutic Chemical (ATC) classification...D07756 Drug Cyamemazine tartrate; Tercian (TN) C19H21N3S. C4H6O6 473.1621 473.542 D

  2. Drug: D05660 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D05660 Drug Pyrilamine maleate (USP); Pymafed (TN) C17H23N3O. C4H4O4 401.1951 401.4562 D05660.gif Antihistam...inic ATC code: D04AA02 R06AC01 Pyrilamine is called Mepyramine in INN. H1-receptor

  3. Drug: D00662 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00662 Drug Azatadine maleate (USP); Optimine (TN) C20H22N2. (C4H4O4)2 522.2002 522.5464 D00662.gif Antihist...aminic ATC code: R06AX09 H1-receptor antagonist [HSA:3269] [KO:K04149] hsa04020(326

  4. Rituximab chimeric anti-CD20 monoclonal antibody treatment for adult refractory idiopathic thrombocytopenic purpura

    DEFF Research Database (Denmark)

    Braendstrup, Peter; Bjerrum, Ole W; Nielsen, Ove J;

    2005-01-01

    with a dose regimen of 375 mg/m2 i.v. approximately once weekly for 4 consecutive weeks. Six patients received a fixed dose of 500 mg disregarding their weight supplemented by 100 mg of methylprednisone i.v. or 50-100 mg of Pred given as premedication together with an antihistamine just before infusion...

  5. 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...

  6. 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...

  7. Omalizumab for Urticarial Vasculitis

    DEFF Research Database (Denmark)

    Ghazanfar, Misbah Nasheela; Thomsen, Simon Francis

    2015-01-01

    include oral antihistamines, oral corticosteroids, dapsone, colchicine or hydroxychloroquine. We describe a male patient with urticarial vasculitis who was treated with omalizumab (anti-IgE) with convincing results and provide a review of previous reports of patients with urticarial vasculitis treated...

  8. Aktinsk prurigo

    DEFF Research Database (Denmark)

    Stockbridge, Eva Boné; Deleuran, Mette Søndergaard; Steiniche, Torben

    2008-01-01

    to the conclusion that the patient suffered from Actinic Prurigo. The disease was very severe and there was a lack of response to treatment with oral prednisolone, antihistamines and pentoxyfyllin. Therefore the patient was treated with Thalidomide 50 mg/25 mg daily (alternating). This resulted in the complete...

  9. Effects of a single dose of Bilastine 20mg on flying ability in healthy volunteers under conditions of simulated cabin pressure

    NARCIS (Netherlands)

    Valk, P.J.L.; Jetten, A.M.; Simons, M.

    2015-01-01

    Background : Optimal physical and mental fitness of pilots is a prerequisite for flight safety. Pilots suffering from allergic rhinoconjuctivitis or other allergic upper airway diseases are not allowed to fly because ambient pressure changes may aggravate the symptoms and some antihistaminic medicat

  10. Drug: D08769 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08769 Mixture, Drug Diphenhydramine hydrochloride - calcium bromide mixt; Rescalmi...n (TN) Diphenhydramine hydrochloride [DR:D00669], Calcium bromide [DR:D01723] Therapeutic category: 4419 The... Antihistamines 4419 Others D08769 Diphenhydramine hydrochloride - calcium bromide mixt PubChem: 96025452 ...

  11. Medication impairing safe driving: knowledge, attitude and behaviour of consumers and patients.

    NARCIS (Netherlands)

    Vervloet, M.; Dijk, L. van

    2007-01-01

    Background: Promoting road safety is one of the aims of the Dutch road safety policy. The role of medication impairing safe driving (tranquilizers, sleep medication, tricyclic antidepressants and first generation antihistamines) in traffic accidents is underexposed and not well known. Previous resea

  12. 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...

  13. 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

  14. 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...

  15. Dyslexia and Learning Disabilities: Medical Diagnosis with Educational Therapy.

    Science.gov (United States)

    Westerman, S. Thomas; And Others

    1982-01-01

    Ways of diagnosing dyslexia are discussed along with the developmental symptoms, which include balancing and hearing deficiencies, reversal of letters or words and unusual posture. Medical treatment with antihistamines and other drugs is described. Approximately 75 percent of individuals are shown to respond favorably to therapy. (CM)

  16. 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

  17. 77 FR 29307 - Control of Alcohol and Drug Use: Addition of Post-Accident Toxicological Testing for Non...

    Science.gov (United States)

    2012-05-17

    ... prohibited or strictly regulated because of their potential for abuse or addiction. The Drug Enforcement... sedating antihistamines. Of the 150 re-tested samples, 14 (9.3 percent) tested positive for at least one... number of positive post-accident test results should FRA decide to report tramadol or...

  18. Doxylamine and Pyridoxine

    Science.gov (United States)

    The combination of doxylamine and pyridoxine is used to treat nausea and vomiting in pregnant women whose symptoms have not improved after changing their diet or using other non-medicine treatments. Doxylamine is in a class of medications called antihistamines. ...

  19. 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.

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

    Medline Plus

    Full Text Available ... counter oral antihistamine. To reduce swelling , apply an ice pack to the bite. If you experience any serious symptoms after a bug bite, such as a rash, fever, or body aches, see your doctor or a board-certified dermatologist immediately. Make sure you tell the doctor about your recent ...

  1. Drug: D01801 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available l 322.156 322.833 D01801.gif Antiallergic; Histamine, H1-receptor antagonist; Antihistaminic ATC code: D04AA...RATIONS FOR TOPICAL USE R01AC Antiallergic agents, excl. corticosteroids R01AC06 Thonzylamine D01801 Thonzyl

  2. Drug: D02249 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available C4H4O4)2 534.2326 534.5589 D02249.gif Antihistaminic, H1-receptor; Asthma prophylactic; Anti-allergic Therap...RGANS S01 OPHTHALMOLOGICALS S01G DECONGESTANTS AND ANTIALLERGICS S01GX Other antiallergics S01GX06 Emedastin

  3. 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.

  4. Suplatast tosilate alleviates nasal symptoms through the suppression of nuclear factor of activated T-cells-mediated IL-9 gene expression in toluene-2,4-diisocyanate-sensitized rats.

    Science.gov (United States)

    Mizuguchi, Hiroyuki; Orimoto, Naoki; Kadota, Takuya; Kominami, Takahiro; Das, Asish K; Sawada, Akiho; Tamada, Misaki; Miyagi, Kohei; Adachi, Tsubasa; Matsumoto, Mayumi; Kosaka, Tomoya; Kitamura, Yoshiaki; Takeda, Noriaki; Fukui, Hiroyuki

    2016-03-01

    Histamine H1 receptor (H1R) gene is upregulated in patients with pollinosis; its expression level is highly correlated with the nasal symptom severity. Antihistamines are widely used as allergy treatments because they inhibit histamine signaling by blocking H1R or suppressing H1R signaling as inverse agonists. However, long-term treatment with antihistamines does not completely resolve toluene-2,4-diisocyanate (TDI)-induced nasal symptoms, although it can decrease H1R gene expression to the basal level, suggesting additional signaling is responsible for the pathogenesis of the allergic symptoms. Here, we show that treatment with suplatast tosilate in combination with antihistamines markedly alleviates nasal symptoms in TDI-sensitized rats. Suplatast suppressed TDI-induced upregulation of IL-9 gene expression. Suplatast also suppressed ionomycin/phorbol-12-myristate-13-acetate-induced upregulation of IL-2 gene expression in Jurkat cells, in which calcineurin (CN)/nuclear factor of activated T-cells (NFAT) signaling is known to be involved. Immunoblot analysis demonstrated that suplatast inhibited binding of NFAT to DNA. Furthermore, suplatast suppressed ionomycin-induced IL-9 mRNA upregulation in RBL-2H3 cells, in which CN/NFAT signaling is also involved. These data suggest that suplatast suppressed NFAT-mediated IL-9 gene expression in TDI-sensitized rats and this might be the underlying mechanism of the therapeutic effects of combined therapy of suplatast with antihistamine.

  5. Bilastine and the central nervous system.

    Science.gov (United States)

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

    2011-01-01

    Antihistamines have been classifed as first or second generation drugs, according to their pharmacokinetic properties, chemical structure and adverse effects. The adverse effects of antihistamines upon the central nervous system (CNS) depend upon their capacity to cross the blood-brain barrier (BBB) and bind to the central H1 receptors (RH1). This in turn depends on the lipophilicity of the drug molecule, its molecular weight (MW), and affinity for P-glycoprotein (P-gp) (CNS xenobiotic substances extractor protein). First generation antihistamines show scant affinity for P-gp, unlike the second generation molecules which are regarded as P-gp substrates. Histamine in the brain is implicated in many functions (waking-sleep cycle, attention, memory and learning, and the regulation of appetite), with numerous and complex interactions with different types of receptors in different brain areas. Bilastine is a new H1 antihistamine that proves to be effective in treating allergic rhinoconjunctivitis (seasonal and perennial) and urticaria. The imaging studies made, as well as the objective psychomotor tests and subjective assessment of drowsiness, indicate the absence of bilastine action upon the CNS. This fact, and the lack of interaction with benzodiazepines and alcohol, define bilastine as a clinically promising drug with a good safety profile as regards adverse effects upon the CNS.

  6. Effects of Aminoguanidine on Pre- and Post-Irradiation Regional Cerebral Blood Flow, Systemic Blood Pressure and Plasma Histamine Levels in the Primate,

    Science.gov (United States)

    1991-01-01

    respiration rate, blood pH, and pie, one group (using a method with less sensitivity peripheral reflexes. A femoral arterial catheter was to HA than the one...and *,vidas.. st’te during acute intestinal in hernia in pigs. dopg% antihistamine. Experientia 33. 1047 1048 (1977). and rabbits: Evidencee fo~r a

  7. Acute onset of generalised pruritus as presenting symptom of Klatskin tumour.

    Science.gov (United States)

    Tobbia, Patrick; Norris, Leslie A; Karimova, Nodira

    2012-08-08

    A 60-year-old Korean woman presented with generalised pruritus and abdominal pain. She was initially treated with oral antihistamine therapy, but upon progression of symptoms and jaundice involvement, she was found to have a Klatskin tumour. The patient was not a candidate for surgical resection and is currently undergoing palliative care.

  8. THE NEGATIVE EFFECTS OF SOME COSMETIC PROCEDURES: PROTECTION POSSIBILITIES, MEDICAL AND PREVENTIVE AGENTS (REVIEW

    Directory of Open Access Journals (Sweden)

    A. V. Majorova

    2016-01-01

    Full Text Available The article describes the possible side responses on cosmetic procedures. There is a review of pharmaceutical and cosmeceutical agents for external use to treat and prevent the complications. We have described the reasonability of the external dosage forms use of anti-histaminic action.

  9. Drug: D00739 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ) C17H27NO3. HCl 329.1758 329.8621 D00739.gif Anesthetic [topical] ATC code: C05AD07 D04AB07 Anatomical Ther...HISTAMINES, ANESTHETICS, ETC. D04A ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AB Anesthetics for topica

  10. Drug: D00551 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 264.3633 D00551.gif Anesthetic [topical] Same as: C07526 ATC code: C05AD02 D04AB06 N01BA03 S01HA03 voltage-... INCL. ANTIHISTAMINES, ANESTHETICS, ETC. D04AB Anesthetics for topical use D04AB06 Tetracaine D00551 Tetraca

  11. Drug: D01768 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available oxil (TN) C17H28N2O3. HCl 344.1867 344.8768 D01768.gif Anesthetic [topical] Therapeutic category: 1313 ATC c...ANTIHISTAMINES, ANESTHETICS, ETC. D04AB Anesthetics for topical use D04AB03 Oxybuprocaine D01768 Oxybuprocai

  12. Fatal overdose from Bendectin.

    Science.gov (United States)

    Bayley, M; Walsh, F M; Valaske, M J

    1975-05-01

    A three-year old male ingested approximately 100 tablets of Bendectin. He developed tonic-clonic seizures followed by cardiac arrest. Toxicologic analysis yielded high levels of doxylamine, dicyclomine, and pyridoxine in blood, peritoneal fluid, and tissue homogenates. The antihistamine, doxylamine succinate appears to be the toxic constituent. Analytical methods used to document the case are herein described.

  13. 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 g...

  14. 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 with ...... of choice instead of antiallergic medications, which have no proven efficacy in this condition....

  15. 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

  16. 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.

  17. Fixed drug eruption due to levocetirizine

    Directory of Open Access Journals (Sweden)

    Ratinder Jhaj

    2016-01-01

    Full Text Available A fixed drug eruption (FDE is a cutaneous adverse drug reaction due to Type IV or delayed cell-mediated hypersensitivity. Antihistamines, which antagonize the action of histamine during an allergic reaction by blocking the H 1 histamine receptors, are used routinely for the treatment of various allergic disorders such as urticaria, eczemas, and also in itchy lesions of skin like scabies.Levocetirizine, an active (R-enantiomer of cetirizine, is a newer or second generation antihistamine, with more specific actions and fewer side effects, including cutaneous reactions. FDE due to levocetirizine as well as with cetirizine are rare. We report a case of levocetirizine induced FDE in a 49-year-old male patient with scabies. The patient had a history of cetirizine induced FDE in the past.

  18. 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......, 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...... and a significant increase in the levels of histamine and tryptase. The challenge of subjects not allergic to pollen produced no such response. Azelastine and cetirizine significantly reduced allergen-induced sneezing and the associated increase in histamine and tryptase levels. No significant differences were...

  19. Diphenhydramine-induced acute dystonia.

    Science.gov (United States)

    Etzel, J V

    1994-01-01

    A 45-year-old woman was administered oral and intravenous diphenhydramine 25 mg for the treatment of an allergic reaction. Within 2 minutes she rapidly developed trismus, dysarthria, tremors of the upper extremities, left-sided weakness, and diminished consciousness. She was treated with intravenous diazepam and benztropine with good response. After approximately 12 hours the patient's condition was completely resolved except for minor subjective weakness of her left extremities. Her hospital stay was uneventful, and she was discharged after 4 days after refusing rechallenge with the drug. Several cases of acute dystonic reactions secondary to antihistamines have been reported in the literature, four of which involved diphenhydramine. Such reactions may occur after short- or long-term therapy. Most patients experienced rapidly developing trismus, facial dystonia, dysarthria, and occasionally, decreases in consciousness, motor incoordination, and weakness. Because of the widespread availability of diphenhydramine and other antihistamines to the general public, awareness of this effect is of great importance.

  20. 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...

  1. 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.

  2. 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.

  3. 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.

  4. 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.

  5. Paroxysmal hypnogenic dyskinesia responsive to doxylamine: a case report.

    Science.gov (United States)

    Williams, Daniel M

    2012-01-01

    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.

  6. Some medicinal plants with antiasthmatic potential:a current status

    Institute of Scientific and Technical Information of China (English)

    Dnyaneshwar J Taur; Ravindra Y Patil

    2011-01-01

    Asthma is a common disease that is rising in prevalence worldwide with the highest prevalence in industrialized countries. Asthma affect about 300 million people worldwide and it has been estimated that a further 100 million will be affected by 2025. Since the ancient times, plants have been exemplary sources of medicine. Current asthma therapy lack satisfactory success due to adverse effect, hence patients are seeking complementary and alternative medicine to treat their asthma. Ayurveda and other Indian literature mention the use of plants in various human ailments. India has about 45 000 plant species and among them several thousand are claimed to possess medicinal properties. Researches conducted in the last few decades on the plants mentioned in ancient literature or used traditionally for asthma have shown antiasthmatic, antihistaminic and antiallergic activity. This review reveals that some plants and their extract have antiasthmatic, antihistaminic, anticholinergic and antiallergic activity.

  7. Preclinical and human surrogate models of itch

    DEFF Research Database (Denmark)

    Hoeck, Emil August; Marker, Jens Broch; Gazerani, Parisa;

    2016-01-01

    Pruritus, or simply itch, is a debilitating symptom that significantly decreases the quality of life in a wide range of clinical conditions. While histamine remains the most studied mediator of itch in humans, treatment options for chronic itch, in particular antihistamine-resistant itch, are lim...... currently applied in animals and humans. This article is protected by copyright. All rights reserved.......Pruritus, or simply itch, is a debilitating symptom that significantly decreases the quality of life in a wide range of clinical conditions. While histamine remains the most studied mediator of itch in humans, treatment options for chronic itch, in particular antihistamine-resistant itch......, are limited. Relevant preclinical and human surrogate models of non-histaminergic itch are needed to accelerate the development of novel antipruritics and diagnostic tools. Advances in basic itch research have facilitated the development of diverse models of itch and associated dysesthesiae. While...

  8. Virus and bacteria enhance histamine production in middle ear fluids of children with acute otitis media.

    Science.gov (United States)

    Chonmaitree, T; Patel, J A; Lett-Brown, M A; Uchida, T; Garofalo, R; Owen, M J; Howie, V M

    1994-06-01

    Histamine levels were measured in 677 middle ear fluid (MEF) samples from 248 children (aged 2 months to 7 years) with acute otitis media (AOM); of these, 116 (47%) had documented viral infection. Histamine content was higher in bacteria-positive than in bacteria-negative MEF samples (P = .007) and higher in samples from patients with viral infection than in those from patients with no viral infection (P = .002). Bacteria and viruses together had an additive effect on histamine content in MEF. Histamine concentration in the initial MEF sample tended to be higher in patients with persistent otitis than in those with good response to treatment (P = .14). Results suggest that viruses, bacteria, or both induce histamine production, which leads to increased inflammation in the middle ear. Antihistaminic drugs may be beneficial. Large, prospective, controlled trials of the effects of antihistamine as an adjunct therapy in bacterial and viral AOM are required before recommendations can be made.

  9. Urticaria and angioedema

    OpenAIRE

    Kanani Amin; Schellenberg Robert; Warrington Richard

    2011-01-01

    Abstract Urticaria (hives) is a common disorder that often presents with angioedema (swelling that occurs beneath the skin). It is generally classified as acute, chronic or physical. Second-generation, non-sedating H1-receptor antihistamines represent the mainstay of therapy for both acute and chronic urticaria. Angioedema can occur in the absence of urticaria, with angiotensin-converting enzyme (ACE) inhibitor-induced angioedema and idiopathic angioedema being the more common causes. Rarer c...

  10. Antinauseants in Pregnancy: Teratogens or Not?

    OpenAIRE

    Biringer, Anne

    1984-01-01

    Nausea and/or vomiting affect 50% of all pregnant women. For most women, this is a self-limited problem which responds well to conservative management. However, there are some situations where the risk to the mother and fetus posed by the illness are greater than the possible risks of teratogenicity of antinauseant drugs. Antihistamines have had the widest testing, and to date, there has been no evidence linking doxylamine, dimenhydrinate or promethazine to congenital malformations. Since no ...

  11. Study of drug use in outdoor pediatric patients of upper respiratory tract infections in a tertiary care hospital

    Directory of Open Access Journals (Sweden)

    Usha Joshi

    2015-10-01

    Conclusions: The study revealed that the majority of children were below 5 years of age. The most common class of drugs prescribed was antihistaminics and expectorant combinations followed by analgesics and antipyretics. Although the majority of the patients received antibiotics, 40.55% of patients received symptomatic treatment. This is a welcome step as inappropriate use of the antibiotics can potentiate to the increasing trend of antimicrobial resistance. [Int J Basic Clin Pharmacol 2015; 4(5.000: 1004-1008

  12. 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.

  13. Effects of Terfenadine and Diphenhydramine on Brain Activity and Performance in a UH-60 Flight Simulator

    Science.gov (United States)

    1992-09-01

    inability to sleep . In some situations, sedation and other CNS depressant effects may be clinically useful. However, in many instances, these effects...pharmacokinetics data suggest a polyphasic elimination (Carruthers et al., 1978). Diphenhydramine is considered characteristic of the antihistamines with...previously. In one study (Carruthers et al., 1978), 50 mg of diphenhydramine produced sleep in approximately half of the subjects during the first hour

  14. The Role of Histamine H1 and H4 Receptors in Atopic Dermatitis: From Basic Research to Clinical Study

    Directory of Open Access Journals (Sweden)

    Yusuke Ohsawa

    2014-01-01

    Although the oral administration of H1R antagonists is widely used to treat AD, it is not very effective. In contrast, JNJ39758979, a novel H4R antagonist, had marked effects against pruritus in Japanese patients with AD in a phase II clinical trial. Next generation antihistaminic agents possessing H1R and H4R antagonistic actions may be a potent therapeutic drug for AD.

  15. 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.

  16. 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.

  17. 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...

  18. 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....

  19. Maternal use of Loratadine during pregnancy and risk of hypospadias in offspring

    Directory of Open Access Journals (Sweden)

    2006-01-01

    Full Text Available To examine the risk of hypospadias after exposure to loratadine and other antihistamines during pregnancy, we conducted a population-based case-control study in four Danish counties, which account for 30% of the Danish population (~1.6 M. We obtained data on maternal use of antihistamines from prescription databases, and data on birth outcomes from the Danish Medical Birth Registry (MBR and the Hospital Discharge Registry (HDR. A total of 65,383 male births with a full prescription history of the mother in the study period from 1989-2002 were available for analysis. Within this cohort, we identified cases with a diagnosis of hypospadias, and 10 selected controls per case without such a diagnosis (matched on birth month, gender and year of birth. We identified 227 cases of hypospadias recorded in the HDR within six months postpartum and 2270 controls. One case (0.4% and eight (0.4% controls were exposed to loratadine in the first trimester and up to 30 days before the time of conception. The adjusted odds ratio (OR for hypospadias among users of loratadine relative to non-users was 1.4 (95% CI: 0.2-11.2 and the corresponding OR for other antihistamines was 1.9 (95% CI: 0.7-5.7. In this study, maternal exposure to loratadine did not appear to be associated with an increased risk of hypospadias when compared with other antihistamines, although it should be noted that the statistical precision of the risk estimates might be limited.

  20. Lacosamide-induced rash.

    Science.gov (United States)

    Koubeissi, Mohamad Z; Vismer, Marta; Ehrlich, Alison

    2014-09-01

    Cutaneous eruptions and hypersensitivity represent frequently reported side effects of anti-seizure medications. However, these side-effects have rarely been previously reported for lacosamide, a newer-generation anti-seizure medication with a novel mechanism of action. Here, we report a case of diffuse skin eruption in a patient with history of epilepsy soon after initiation of lacosamide. The rash resolved after discontinuation of lacosamide and use of antihistamines and steroids. We also review the information on drug hypersensitivity syndrome.

  1. Food allergy as seen by a paediatric gastroenterologist

    DEFF Research Database (Denmark)

    Husby, Steffen

    2008-01-01

    diagnosis of food allergy and the causative food is important because the condition is present in only about one third of patients with suspected food allergy, may be due to foods other than those originally suspected, and elimination diets may be detrimental to the child's health. Differential diagnosis...... is important to rule out upper and/or lower gastrointestinal disorders. Food allergy is generally treated with a hypoallergenic diet; antihistamines and leukotriene receptor antagonists may be used in specific conditions....

  2. 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....

  3. Survey in the Emergency Department of Parents’ Understanding of Cough and Cold Medication Use in Children Younger Than 2 Years

    Science.gov (United States)

    2012-09-01

    children gave various drug classes including analgesics, antihistamines , antipyretics, cough suppressants, expectorants, and decongestants. One hundred...FACEP,*Þ Vikhyat S. Bebarta, MD, FACEP, FACMT,*þ Rebecca L. Pitotti, MSN, RN,§ and Toni E. Vargas, PA-C§ Objectives: In August 2007, the Food and Drug ...CCM use in children younger than 2 years. Most thought CCMs were safe and effective. KeyWords: cough and cold medications, Food and Drug

  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. Journal of Special Operations Medicine, Volume 3, Edition 3

    Science.gov (United States)

    2003-01-01

    These medications, known by their trade names Tagamet® (cimetidine), Pepcid® (famotidine), Axid® (nizatidine), and Zantac® ( ranitidine ) selectively...Claritin Reditabs®) as the first non-sedat- ing antihistamine available in the United States with- out a prescription. Its formulation and dosing are the...the Special Forces Medic. The Chief Medical Aidman’s Course, formulated by 1st Lt Elliott, was specifically designed for Special Forces Medics. Once

  6. Development of screening assays to test novel integrin antagonists in allergic inflammation

    OpenAIRE

    Spartà, Antonino Maria

    2009-01-01

    Aim of the research: to develop a prototype of homogeneous high-throughput screening (HTS) for identification of novel integrin antagonists for the treatment of ocular allergy and to better understand the mechanisms of action of integrin-mediated levocabastine antiallergic action. Results: This thesis provides evidence that adopting scintillation proximity assay (SPA) levocabastine (IC50=406 mM), but not the first-generation antihistamine chlorpheniramine, displaces [125I]fibronectin (F...

  7. Severe rhabdomyolysis after doxylamine overdose.

    Science.gov (United States)

    Soto, L F; Miller, C H; Ognibere, A J

    1993-06-01

    Clinicians should be aware of the complications of rhabdomyolysis in patients who ingest doxylamine succinate and other over-the-counter antihistamines. The easy availability of these substances increases the potential not only for intentional overdose by adults but also for inadvertent ingestion by children. Prompt intervention and careful assessment of renal function, urinary output, and serum creatine kinase levels may represent the difference between an uncomplicated course and acute renal failure.

  8. Food Effects on the Pharmacokinetics of Doxylamine Hydrogen Succinate 25 mg Film-Coated Tablets

    OpenAIRE

    Videla, Sebastián; Lahjou, Mounia; Guibord, Pascal; Xu, Zhengguo; Tolrà, Carles; Encina, Gregorio; Sicard, Eric; Sans, Artur

    2012-01-01

    Background Doxylamine succinate, an ethanolamine-based antihistamine, is used in the short-term management of insomnia because of its sedative effects. The data available on the pharmacokinetic profile of doxylamine in humans are limited, notwithstanding that this drug has been marketed in European countries for more than 50 years. In fact, no data on the effect of food on the pharmacokinetic parameters of doxylamine are available. Objective The objective of this study was to evaluate the pha...

  9. Acute pancreatitis and acute renal failure complicating doxylamine succinate intoxication.

    Science.gov (United States)

    Lee, Yang Deok; Lee, Soo Teik

    2002-06-01

    Doxylamine succinate is an antihistaminic drugwith additional hypnotic, anticholinergic and local anesthetic effects first described in 1948. In Korea and many other countries, it is a common-over-the counter medication frequently involved in overdoses. Clinical symtomatology of doxylamine succinate overdose includes somnolence, coma, seizures, mydriasis, tachycardia, psychosis, and rhabdomyolysis. A serious complication may be rhabdomyolysis with subsequent impairment of renal function and acute renal failure. We report a case of acute renal failure and acute pancreatitis complicating a doxylamine succinate intoxication.

  10. Doxylamine toxicity: seizure, rhabdomyolysis and false positive urine drug screen for methadone

    OpenAIRE

    Syed, Husnain; Som, Sumit; Khan, Nazia; Faltas, Wael

    2009-01-01

    The present report highlights the possible adverse effects of doxylamine, a common over the counter sleep aid. Doxylamine is an antihistamine that at toxic doses can cause anticholinergic effects, including seizures, rhabdomyolysis and death. The following case describes a patient with doxylamine toxicity who presented with seizure and confusion. Our patient was managed symptomatically, and remained otherwise stable throughout his hospitalisation. This case is atypical in terms of a delayed r...

  11. Syndrome of inappropriate antidiuresis in doxylamine overdose

    OpenAIRE

    Carrascosa, Miguel F; Caviedes, José-Ramón Salcines; Lucena, M. Isabel; Cuadrado-Lavín, Antonio

    2012-01-01

    Doxylamine succinate, an H1-antihistamine drug, is commonly used as sleep-inducing agent as well as therapy for nausea and vomiting in pregnancy. At usual doses, it may cause impairment of cognitive and psychomotor performance, anticholinergic effects, agitation and postural hypotension. Besides, since this drug is frequently involved in either accidental or intentional overdoses, it seems relevant to bear in mind other possible toxic effects. We report a case of acute severe hyponatremia in ...

  12. AFRRI (Armed Forces Radiobiology Research Institute) Reports, January, February and March 1988. First quarter 1988

    Science.gov (United States)

    1988-05-01

    8217 ond experimnrt a, potassium Icrrocyanide solution (0. 1 M ) containing MNP (00 M ) and glycylglycine (0. 1 M ) were photolyzed generating tile F.SR...and antihistamine. Ex.perientia 33, MD. 1047-1048. CHAPUT. R. L., AND WISE. D. (1969). Miniature Pig In- DUPONT., A.. AND) MERANt). Y. (1978). Enzyme ...decarboxylase. the enzyme that converts histidine to histamine. is localized in different regions ofthe brain (23): histamine activates adenylate cyclase

  13. Effects of bilastine on T-wave morphology and the QTc interval

    DEFF Research Database (Denmark)

    Graff, Claus; Struijk, Johannes; 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....

  14. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria

    OpenAIRE

    Sadaba B; Azanza JR; Gomez-Guiu A; Rodil R

    2013-01-01

    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...

  15. Evaluation of the Single-dose Pharmacokinetics of Bilastine in Subjects with Various Degrees of Renal Insufficiency

    OpenAIRE

    Lasseter, Kenneth C.; Sologuren, Ander; La Noce, Anna; Dilzer, Stacy C.

    2013-01-01

    Background Bilastine is a novel second-generation H1 antihistamine, which has not shown sedative or cardiotoxic effects in clinical trials and in post-marketing experience so far, developed for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. It has recently been granted marketing authorization for these therapeutic indications in adults and adolescents at a once-daily oral dose of 20 mg in several European countries. Objective This study was conducted to determine the...

  16. Efficacy and safety of bilastine in Japanese patients with perennial allergic rhinitis: A multicenter, randomized, double-blind, placebo-controlled, parallel-group phase III study

    OpenAIRE

    Kimihiro Okubo; Minoru Gotoh; Mikiya Asako; Yasuyuki Nomura; Michinori Togawa; Akihiro Saito; Takayuki Honda; Yoshihiro Ohashi

    2017-01-01

    Background: Bilastine, a novel non-sedating second-generation H1 antihistamine, has been approved in most European countries since 2010. This study aimed to evaluate the superiority of bilastine over placebo in Japanese patients with perennial allergic rhinitis (PAR). Methods: This randomized, double-blind, placebo-controlled, parallel-group, phase III study (trial registration number JapicCTI-142600) evaluated the effect of a 2-week treatment period with bilastine (20 mg once daily), fexo...

  17. PENGUKURAN KANDUNGAN SKOPOLETIN PADA BEBERAPA TINGKAT KEMATANGAN BUAH MENGKUDU (Morinda citrifolia Linn) DENGAN METODE KLT DENSITOMETRI

    OpenAIRE

    Diana Nurus Sholehah

    2010-01-01

    Morinda citrifolia fruit has been used as remedies in Indonesia because many diseases could be healed. Scopoletin, one of major component of Morinda citrifolia was chosen as  marker compound because of  its various activites such as  hypotensive, antiinflamatory and antihistamine. The research aimed to determinate scopoletin in some maturations stage of Morinda citrifolia fruit in order to get best fruit for traditional medicine and phytopharmaca with optimal therapeutical effect . A simple a...

  18. Spasmogenic activity of chemotactic N-formylated oligopeptides: identity of structure--function relationships for chemotactic and spasmogenic activities.

    OpenAIRE

    Marasco, W. A.; Fantone, J. C.; Ward, P. A.

    1982-01-01

    The chemotactic N-formylated oligopeptides are potent spasmogenic agents for guinea pig ileum. Structure-activity studies with various N-formylated peptides suggest the presence of a specific receptor that resembles in specificity the formyl peptide receptor on leukocytes. A competitive antagonist of the formyl peptide receptor on leukocytes also inhibits formyl peptide-induced ileum contraction, whereas the antihistamine diphenhydramine is without effect. The contractile response caused by t...

  19. Urticaria after methyl aminolevulinate photodynamic therapy in a patient with nevoid basal cell carcinoma syndrome.

    Science.gov (United States)

    Wolfe, Christopher M; Green, W Harris; Hatfield, H Keith; Cognetta, Armand B

    2012-11-01

    Methyl aminolevulinate photodynamic therapy (MAL-PDT) is utilized in several countries for the treatment of basal cell carcinoma, but allergic sensitization has been reported by the manufacturer. To the best of our knowledge, we report the first case of urticaria following MAL-PDT in a patient with nevoid basal cell carcinoma syndrome. Prophylactic use of antihistamines may allow continued use of MAL-PDT in this setting.

  20. Ciguatera poisoning in the Cook Islands.

    Science.gov (United States)

    Bailey, Stephanie; Withers, Tristan

    2014-06-25

    This case report presents two British medical students who contracted ciguatera poisoning while on elective in the Cook Islands. Thirty-six hours after consuming two reef fish they developed paraesthesia of the mouth, hands and feet, myalgia, pruritis and cold allodynia. Neurological examination was normal. Diagnosis of ciguatera poisoning was made on history of reef fish consumption and classical clinical presentation. Management was symptomatic (antihistamines) and both students made a full recovery within 10 weeks.

  1. Ciguatera poisoning in the Cook Islands

    OpenAIRE

    Bailey, Stephanie; Withers, Tristan

    2014-01-01

    This case report presents two British medical students who contracted ciguatera poisoning while on elective in the Cook Islands. Thirty-six hours after consuming two reef fish they developed paraesthesia of the mouth, hands and feet, myalgia, pruritis and cold allodynia. Neurological examination was normal. Diagnosis of ciguatera poisoning was made on history of reef fish consumption and classical clinical presentation. Management was symptomatic (antihistamines) and both students made a full...

  2. Urticaria and dermographism in patients with adult-onset Still's disease.

    Science.gov (United States)

    Criado, Paulo Ricardo; de Carvalho, Jozélio Freire; Ayabe, Liliane Akemi; Brandt, Hebert Roberto Clivati; Romiti, Ricardo; Maruta, Celina W

    2012-08-01

    Adult-onset Still's disease (AOSD) patients typically present with arthralgia, fever, lymphadenopathy and a transient salmon maculopapular rash. Only approximately 25 cases of AOSD with urticaria were described in the literature. In this article, the authors report three additional cases of AOSD with urticarial and dermographic lesions who had a good clinical response to glucocorticoid and antihistamines. A review of the literature concerning this issue is also herein written.

  3. Drug: D07400 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D07400 Drug Histapyrrodine (INN) C19H24N2 280.1939 280.4073 D07400.gif ATC code: R0...NES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AC Substituted ethylene diamines R06AC02 Histapyrrodine D07400... Histapyrrodine (INN) CAS: 493-80-1 PubChem: 51091736 LigandBox: D07400

  4. Synthesis and pharmacological evaluation of (6-substituted 4-Oxo-4 H -chromene-3 yl methyl N-substituted aminoacetates

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    Gajbhiye Asmita

    2008-01-01

    Full Text Available A series of the title compounds were synthesized and characterized by spectral data. All the compounds were evaluated for in vitro antihistaminic activity by inhibition of isotonic contractions induced by histamine on isolated guinea pig ileum and the compound 6-k showed significant activity. A few compounds have also been screened for in vivo bronchodilatory activity. These compounds exhibited significant protection against histamine-induced convulsions in guinea pig at the dose of 50 µmol.

  5. 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.

  6. [Argentine guidelines for urticaria and angioedema].

    Science.gov (United States)

    Máspero, Jorge; Cabrera, Hugo; Ardusso, Ledit; De Gennaro, Mónica; Fernández Bussy, Ramón; Galimany, José; Galimberti, Daniel; Label, Marcelo; La Forgia, Marta; Medina, Iris; Neffen, Hugo; Troielli, Patricia

    2014-01-01

    This interdisciplinary paper summarizes the news in the diagnosis and treatment of chronic urticaria (CU), and provides concepts, definitions and evidence-based suggestions for its management. Urticaria occurs in at least 20% of the population at some point in their lives. Acute urticaria (less than 6 weeks' duration), differs from CU in its etiology, but the onset of this disease is always acute. CU may occur as spontaneous (SCU) or induced (ICU). The diagnosis is simple, although a careful evaluation is necessary for differential diagnosis. ICU's diagnosis is mainly clinical, even if provocation tests can be useful. Supplementary studies should be limited and based on the clinical suspicion. Treatment may be divided into three approaches: avoidance, elimination or treatment of the cause, and pharmacological treatment. Recently treatment has been modified with the use of second-generation antihistamines as first-line and increased doses of nonsedating H1 antihistamines, up to 4 times, as second line. Antihistamines are essential to treat CU; however, 40% of patients do not achieve good control despite increased doses and require additional treatment. The most recent evidence indicates a group of drugs to be used as third line in these cases, to improve quality of life and to limit toxicity from frequent or chronic use of systemic steroids. Only 3 drugs are recommended as third line: omalizumab, cyclosporin A or anti-leukotrienes.

  7. Comparative efficacy of levocetirizine, desloratidine and fexofenadine by histamine wheal suppression test

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    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.

  8. The use of New Generation H1 Receptor Blockers and Advantages in Terms of Reliability

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    Muhammed Yayla

    2013-10-01

    Full Text Available H1 receptor blockers are one of the most commonly prescribed medications in the treatment of allergic disorders. These disease have reduced life quality of people and prevalent in the world. H1 receptor blockers has been used since 1940 and lead to some adverse effects such as sedation because of their chemical and pharmacological properties. Therefore new generations have been studied for reduced their adverse effect. The aims of this review are to exhibit advantages of new produced H1 receptor blockers compared to classical antihistamines and demonstrate efficacies of clinical uses of new produced H1 antihistamines. New generation H1 receptor blockers which have been developed after 1980s has less lipophilic properties and their sedative effects are minimized compared to classical antihistamines. Also, their specificity, affinity for H1 receptors and antihistaminergic effects are higher than classical H1 receptor blockers. Although new generation H1 receptor blockers are better tolerated than classical H1 receptor blockers, some of them lead to potential cardio toxicity. Consequently new generation H1 receptor blockers are reliable and efficient drugs, they provide convenience in the treatment of allergic disorders and prevent development of phobia against drugs.

  9. Position statement for the use of omalizumab in the management of chronic spontaneous urticaria in Indian patients

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    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.

  10. Diagnosis and management of rhinitis: complete guidelines of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology. American Academy of Allergy, Asthma, and Immunology.

    Science.gov (United States)

    Dykewicz, M S; Fineman, S; Skoner, D P; Nicklas, R; Lee, R; Blessing-Moore, J; Li, J T; Bernstein, I L; Berger, W; Spector, S; Schuller, D

    1998-11-01

    This document contains complete guidelines for diagnosis and management of rhinitis developed by the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology, representing the American Academy of Allergy, Asthma and Immunology, the American College of Allergy, Asthma and Immunology and the Joint Council on Allergy, Asthma and Immunology. The guidelines are comprehensive and begin with statements on clinical characteristics and diagnosis of different forms of rhinitis (allergic, non-allergic, occupational rhinitis, hormonal rhinitis [pregnancy and hypothyroidism], drug-induced rhinitis, rhinitis from food ingestion), and other conditions that may be confused with rhinitis. Recommendations on patient evaluation discuss appropriate use of history, physical examination, and diagnostic testing, as well as unproven or inappropriate techniques that should not be used. Parameters on management include use of environmental control measures, pharmacologic therapy including recently introduced therapies and allergen immunotherapy. Because of the risks to patients and society from sedation and performance impairment caused by first generation antihistamines, second generation antihistamines that reduce or eliminate these side effects should usually be considered before first generation antihistamines for the treatment of allergic rhinitis. The document emphasizes the importance of rhinitis management for comorbid conditions (asthma, sinusitis, otitis media). Guidelines are also presented on special considerations in patients subsets (children, the elderly, pregnancy, athletes and patients with rhinitis medicamentosa); and when consultation with an allergist-immunologist should be considered.

  11. Treatment of allergic rhinoconjunctivitis: a review of the role of topical levocabastine

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    R. Gerth van Wijk

    1995-01-01

    Full Text Available Lcocabastine is an extremely potent and highly selective H1-receptor antagonist which has been specifically developed as eye drops and nasal spray for the treatment of allergic rhinoconjunctivitis. Clinical experience to date suggests that this topical antihistamine is at least as effective as other current first-line therapeutic approaches for the treatment of this condition, including oral H1-receptor antagonists and sodium cromoglycate. Onset of action is rapid, with clinical effects apparent within minutes of instillation. Moreover, duration of action is sufficiently long to permit a convenient twice-daily dosing regimen. Topical levocabastine is well tolerated with an adverse-effect profile comparable with that of placebo and sodium cromoglycate. As might be expected from the route of drug administration, application site reactions are the most frequent adverse effect associated with levocabastine eye drops and nasal spray with an incidence comparable with that seen in placebotreated controls. The availability of effective and well-tolerated topical antihistamines, such as levocabastine, is an important advance which broadens the range of therapeutic approaches available for the clinical management of allergic rhinoconjunctivitis. Levocabastine appears to be an attractive alternative to oral antihistamines as a first-line therapeutic option for the treatment of this atopic condition.

  12. Role of bilastine in the management of allergic rhinitis and urticaria: an Asia-Pacific consensus statement.

    Science.gov (United States)

    Mösges, Ralph; Lee, Dennis Lip Yen; Abong, Jovilia; Siasoco, Bella; Chow, Steven Kw; Leong, Jern-Lin; Singh, Harvinder; Kuljit, S; Campomanes, Benjamin

    2016-01-01

    The prevalence of allergic diseases is increasing globally, most particularly in middle- to low-income countries. This article examines the burden of allergic rhinitis and chronic urticaria in the Asia-Pacific region, unmet clinical needs, and the potential role of bilastine in the management of these conditions. An International Advisory Group meeting was convened in association with the Asian Pacific Society of Respirology Annual Congress in November 2014, followed by a literature review, and consensus-based outcomes from the meeting and literature review are described. Regional estimates of the prevalence of allergic rhinitis range from 10% to 50%, while little is known regarding the burden of urticaria in the Asia-Pacific region. A survey of allergy patients in the region identified fast, complete, and long-lasting symptom relief as the medication attributes most important to patients. International treatment guidelines for allergic rhinitis and urticaria advocate the first-line use of second-generation, no-sedating H1-antihistamines, such as bilastine, over their first-generation counterparts and a range of these agents are available to Asia-Pacific patients. The newer agents possess many of the properties of an "ideal" antihistamine (once daily administration, rapid and complete symptom relief, limited potential for drug-drug interactions, minimal side effects). The burgeoning prevalence of allergic diseases in the Asia-Pacific region and the uncontrolled symptoms that these patients experience demand a new antihistamine that offers the highest number of positive features according to the international guidelines.

  13. Current challenges and controversies in the management of chronic spontaneous urticaria.

    Science.gov (United States)

    Asero, Riccardo; Pinter, Elena; Marra, Alessandro Maria; Tedeschi, Alberto; Cugno, Massimo; Marzano, Angelo Valerio

    2015-01-01

    Chronic spontaneous urticaria (CSU) is characterized by the recurrence of itchy wheals for at least 6 weeks, affects up to 1% of the general population and may severely impair quality of life. H1-antihistamines are the cornerstones of treatment, but in about 10% of cases they fail to control the disease even at higher than licensed doses. In these patients, short courses of oral steroids may induce a remission in about 50% of cases. Omalizumab, a monoclonal anti-IgE, is effective in antihistamine-unresponsive patients although optimal treatment duration needs to be defined. Immunosuppressive treatment with cyclosporine is also effective in the majority of antihistamine-resistant chronic spontaneous urticaria (CSU) patients, but its use is limited by potential side effects. In refractory patients, other approaches include intravenous immunoglobulin, rituximab, dapsone and anticoagulants. The present review looks with particular interest at the prevalence of treatment failures with the main third-level treatments (corticosteroids, omalizumab and cyclosporine) and discusses them in light of the possible different pathogenic mechanisms underlying chronic spontaneous urticaria.

  14. Unique immunomodulatory effects of azelastine on dendritic cells in vitro.

    Science.gov (United States)

    Schumacher, S; Kietzmann, M; Stark, H; Bäumer, W

    2014-11-01

    Allergic contact dermatitis and atopic dermatitis are among the most common inflammatory skin diseases in western countries, and antigen-presenting cells like dendritic cells (DC) are key players in their pathophysiology. Histamine, an important mediator of allergic reactions, influences DC maturation and cytokine secretion, which led us to investigate the immunomodulatory potential of the well-known histamine H1 receptor antagonists: azelastine, olopatadine, cetirizine, and pyrilamine. Unlike other H1 antihistamines, azelastine decreased lipopolysaccharide-induced tumor necrosis factor α and interleukin-12 secretion from murine bone marrow-derived DC. This effect was independent of histamine receptors H1, H2, or H4 and may be linked to inhibition of the nuclear factor kappa B pathway. Moreover, only azelastine reduced proliferation of allogenic T cells in a mixed leukocyte reaction. We then tested topical application of the H1 antihistamines on mice sensitized against toluene-2,4-diisocyanate, a model of Th2-mediated allergic contact dermatitis. In contrast to the in vitro results, all investigated substances were efficacious in reducing allergic ear swelling. Azelastine has unique effects on dendritic cells and T cell interaction in vitro. However, this did not translate into superior in vivo efficacy for Th2-mediated allergic dermatitis, possibly due to the effects of the antihistamines on other cell types involved in skin inflammation. Future research will have to clarify whether these properties are relevant to in vivo models of allergic inflammation with a different T cell polarization.

  15. The history and progression of treatments for allergic rhinitis.

    Science.gov (United States)

    Ostrom, Nancy K

    2014-01-01

    This article intends to place new treatments in the context of allergic rhinitis (AR) treatment history. The medical literature was searched for significant advances and changes in AR treatment. Historical data on AR treatment options and management were selected. Reviews of AR management published throughout the 20th century were included to provide context for treatment advances. Modern AR treatment began in the early 20th century with immunotherapy and was soon followed by the emergence of antihistamine therapy in the 1930s. Numerous treatments for AR have been used over the ensuing decades, including decongestants, mast cell stabilizers, and leukotriene receptor antagonists. Topical corticosteroid options were developed the 1950s, and, added to baseline antihistamine therapy, became the foundation of AR treatment. Treatment options were significantly impacted after the 1987 Montreal Protocol, which phased out the use of chlorofluorocarbon propellant aerosols because of environmental concerns. From the mid-1990s until recently, this left only aqueous solution options for intranasal corticosteroids (INSs). The approval of the first hydrofluoroalkane propellant aerosol INSs for AR in 2012 restored a "dry" aerosol treatment option. The first combination intranasal antihistamine/INSs was also approved in 2012, providing a novel treatment option for AR. Treatment of AR has progressed with new therapeutic options now available. This should continue to move forward with agents to alter the allergic mechanism itself and impact the disease burden that has a significant impact on patient outcomes.

  16. [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.

  17. 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

  18. 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.

  19. Updates in the treatment of ocular allergies

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    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

  20. AB037. Drug-related costs of rhinitis in Australia: a NostraData cross-sectional study of pharmacy ​​purchases​

    Science.gov (United States)

    Carney, A. Simon; Price, David B.; Smith, Pete; Harvey, Richard; Bosnic-Anticevich, Sinthia; Christian, Louise; Skinner, Derek; Carter, Victoria; Durieux, Alice M. S.

    2016-01-01

    Background Intranasal corticosteroids (INS) are a first-line therapy for rhinitis according to all international clinical guidelines for rhinitis. Although many added treatments are not recommended, the use of multiple therapies to control symptoms is frequent, as patients often continue to experience debilitating symptoms while on medication. Previous estimates of multiple therapy prescriptions may have been too conservative, as most rhinitis therapies are also available over-the-counter (OTC). This may affect the cost burden of rhinitis treatment. To investigate the extent of multiple therapy use to treat rhinitis in Australia, using doctor prescriptions and OTC medication; and to assess the additional cost incurred by multiple therapy use. Methods This was a historical cohort study of pharmacy-related claims from NostraData, Australia. We examined all rhinitis therapy purchases (antihistamines, INS, combination treatments of both such as Dymista, non-steroidal nasal sprays, leukotriene receptor antagonists (LTRA), eye drops for allergic conjunctivitis, oral steroids and systemic steroids) from 909 pharmacies, including OTC and prescription drugs. We used therapies purchased at the same transaction to assess the proportion of multiple therapy purchases and their cost. Results A total of 4,247,193 pharmacy transactions including rhinitis therapies were analysed; 4% of transactions included multiple rhinitis therapy classes. The average transaction cost was 12.82 EUR for single therapy purchases and 26.72 EUR for multiple therapy purchases. 15% of single therapy purchases were INS, for an average cost of 20.68 EUR. The most frequent additions to INS therapy were antihistamine (74%) and non-steroidal nasal spray (10%). About 94% of antihistamine and 97% of non-steroidal nasal spray purchased as add-on therapy to INS were bought over-the-counter. The average cost of INS & antihistamine and INS & non-steroidal nasal spray transactions was 30.65 and 26.57 EUR

  1. 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

  2. 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

  3. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria

    Directory of Open Access Journals (Sweden)

    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

  4. Treatment of congestion in upper respiratory diseases

    Directory of Open Access Journals (Sweden)

    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

  5. 荨麻疹的分层次治疗%Layered treatmention urticaria

    Institute of Scientific and Technical Information of China (English)

    陈年; 成琼辉; 孙仁山; 伍津津

    2014-01-01

    The urticarial guidelines in multiple regions and countries of Europe and Asia referred a four-level medicine treatments on urticaria.The ifrst-level medicine treatment of urticaria is new generation, nonsedating H1-antihistamines. The second-level medicine treatment is increasing the dosage of nonsedating H1-antihistamines up two to four-fold. The third-level medicine treatment is antihistamines and leukotriene antagonist or short courses of systemic steroids. The fourth-level medicine treatment is to add the following drugs including cyclosporine, omalizumab ordapsone based on the ifrst-level medicine treatment. Clinicians should select appropriate treatments based on individual circumstances.%欧洲和亚洲等多个地区和国家的荨麻疹指南中均提到荨麻疹的4层次治疗。荨麻疹的第1层次治疗为非镇静的H1受体拮抗剂;第2层次治疗使用非镇静的H1受体拮抗剂为常规剂量的2~4倍;第3层次治疗为抗组胺药物联合白三烯受体拮抗剂或短时间的系统使用糖皮质激素;第4层次治疗是在第1层次治疗的基础上联合环孢素、奥马株单抗或氨苯砜等药物。临床医师应根据个体情况,选择合适的治疗方案。

  6. Comparison of effects of alcaftadine and olopatadine on conjunctival epithelium and eosinophil recruitment in a murine model of allergic conjunctivitis

    Directory of Open Access Journals (Sweden)

    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

  7. Facial hormone-dependent dermatitis: a clinical analysis of 68 cases%面部激素依赖性皮炎临床分析及其治疗效果

    Institute of Scientific and Technical Information of China (English)

    黄静

    2010-01-01

    Objective To explore the incidence of facial hormone-dependent dermatitis, and to raise the healing rate of it. Methods We applied non-steroid drug topically, cold compress combined with anti-histamine agents to treat facial hormone-dependent dermatitis in 68 cases. The results were compared before and after the treatment. Results There were significantly clinical effects of non-steroid drug topically, cold compress combined with antihistamine agents on facial hormone-dependent dermatitis, with healing rate of 82. 4 % , and effective rate of 100 %. Conclusions In order to reduce the incidence of facial hormone-dependent dermatitis, we should follow the principal of applying steroid agent strictly to treat facial dermatitis. Meanwhile, there is significantly clinical effects of non-steroid drug with topical use and cold compress combined with antihistamine agents on facial steroid-dependent dermatitis.%目的 探讨减少面部激素依赖性皮炎的发生率和提高治愈率.方法 对68例面部激素依赖性皮炎治疗采用外用冷敷收敛联合内服抗组胺药,并对治疗效果进行对比分析.结果 采用外用、冷敷收敛联合抗组胺药取得满意疗效,痊愈率82.4%,有效率100%.结论 在使用糖皮质激素时,应严格掌握外用药物使用原则,减少面部激素依赖性皮炎的发生.采取内服、外用药物的综合治疗方法 ,对面部激素依赖性皮炎可以取得较好的临床疗效.

  8. Angioedema - a rare cause of acute episodic dysuria: Case report and review of literature

    Directory of Open Access Journals (Sweden)

    Panicker Radhakrishna

    2007-01-01

    Full Text Available The presentations of acute angioedema vary and depend upon the organs involved. Acute episodes of angioedema can be life-threatening if it involves the larynx leading to the obstruction of upper airways and it is a major cause of death. Angioedema involving the lips, cheek and tongue are common with bizarre presentations. Angioedema of the gastro intestinal tract frequently mimic an acute abdomen resulting in unnecessary surgical intervention and increased morbidity. Here we present an unusual case of angioedema involving the external urethra resulting in severe discomfort and burning sensation during micturition. He was later investigated and diagnosed as idiopathic urticaria with angioedema and promptly responded to antihistamines.

  9. [Histaminergic angioedema and chronic urticaria].

    Science.gov (United States)

    Hacard, Florence; Nosbaum, Audrey; Bensaid, Benoit; Nicolas, Jean-François; Augey, Frédéric; Goujon, Catherine; Bérard, Frédéric

    2015-01-01

    Most angioedemas are histaminergic and correspond to deep urticarial swelling. Recurrent histaminergic angioedema led to the diagnosis of chronic urticaria, even when there are no superficial associated hives. Chronic urticaria is a benign disease, and autoimmune in 40 % of cases. The occurrence of angioedema in chronic urticaria is not a sign of severity. The occurrence of angioedema in chronic urticaria is associated with a longer duration of urticarial disease. NSAIDs and/or systemic corticotherapy are classic triggers of angioedema in chronic urticaria. In the absence of clinical endpoints, there is no need to make further assessment in chronic urticaria good responders to antihistamines.

  10. Urticaria and Allergy-Mediated Conditions.

    Science.gov (United States)

    Jafilan, Lena; James, Charis

    2015-12-01

    Urticaria is a common condition that involves pruritic, raised skin wheals. Although urticaria is a benign, self-limiting condition, it may cause frustration for patients, often because of its chronicity and its tendency to recur. It can also be a life-threatening allergic reaction. Diagnosis is made clinically. It affects 20% of the general population. The first-line treatment for nonremitting cases includes H-1anti-histamines. However, other therapies may be employed. Other allergy-mediated skin conditions include angioedema, contact dermatitis, and atopic dermatitis. Diagnosis is clinical, and management focuses on prevention, avoiding triggers, and treating the itching and inflammation that accompany these conditions.

  11. Biochemical fingerprint and pharmacological applications of Barleria noctiflora L.f. leaves.

    Science.gov (United States)

    Alagar Yadav, Sangilimuthu; Ramalingam, Sathishkumar; Jebamalairaj, Anitha; Subban, Ravi; Sundaram, Karpagavalli Mennakshi

    2016-12-01

    Background Antioxidant and antihistamine agents from Barleria noctiflora L.f. as natural source due to the existing modern medicine give various adverse effects to overcome these problems with natural products. MethodsB. noctiflora leaves extract was 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 mass spectrometry spectral studies. The volatile phytoconstituents of B. noctiflora extract were analysed by gas chromatography-mass spectrometry. Phytoconstituents from B. noctiflora leaves extract were screened for their antioxidant and antihistamine potential in vitro (2,2-diphenyl-1-picrylhydrazyl radical scavenging activity, 2,2'-azinobis-3-ethylbenzothiozoline-6-sulfonic acid radical decolouration assay, nitric oxide radical scavenging activity, superoxide radical scavenging activity and hydrogen peroxide radical scavenging activity) and in silico (molecular docking), respectively. Results Antioxidant and antihistamine barlerinoside has been isolated and characterized from the leaves of B. noctiflora L.f. Barlerinoside revealed their free-radical scavenging ability on OH-, OH•, NO-, O2- and H2O2 radicals and found high percentage inhibition against OH- radical at the IC50 value of 50.45±2.52  µg. The methanol (MeOH) extract of B. noctiflora leaves contains cyclotene; N,N-dimethylglycine; tetrahydrocyclopenta [1,3] dioxin-4-one; phenol, 2-methoxy-; benzofuran, 2-methyl-; 1,4:3,6-dianhydro-α-d-glucopyranose; 2-methoxy-4-vinylphenol; 1,3;2,5-dimethylene-l-rhamnitol; levoglucosan and bicyclo[2.2.2]oct-7-ene-2,5-dione as being the major compounds. Among phytoconstituents present in the extract, the hexestrol; 1,2-benzenedicarboxylic acid, bis(2-methylpropyl) ester; 1-(3,6,6-trimethyl-1,6,7,7a-tetrahydrocyclopenta[c]pyran-1-yl) ethanone; megastigmatrienone; furan interacted with histamine H1 receptor and bind at GLU-177 and ASP

  12. Sjögren-Larsson syndrome: importance of early diagnosis and aggressive physiotherapy.

    Science.gov (United States)

    Kathuria, Sushruta; Arora, Shikha; Ramesh, V

    2012-09-15

    Sjögren-Larsson syndrome (SLS) is a congenital ichthyotic disorder with spasticity. We describe a case of a 5-year-old boy with SLS diagnosed clinically based on congenital ichythosis, quadriplegia, and mental retardation. The child responded well to emollients and antihistamines. His quadriplegia was managed by aggressive physiotherapy and mental retardation by stimulation techniques. After a 3-year follow up, significant improvement was seen in his motor and mental disability. This case highlights the importance of clinical diagnosis and early intervention for such a disabling disorder.

  13. Antinauseants in Pregnancy: Teratogens or Not?

    Science.gov (United States)

    Biringer, Anne

    1984-01-01

    Nausea and/or vomiting affect 50% of all pregnant women. For most women, this is a self-limited problem which responds well to conservative management. However, there are some situations where the risk to the mother and fetus posed by the illness are greater than the possible risks of teratogenicity of antinauseant drugs. Antihistamines have had the widest testing, and to date, there has been no evidence linking doxylamine, dimenhydrinate or promethazine to congenital malformations. Since no available drugs have official approval for use in nausea and vomiting of pregnancy the physician is left alone to make this difficult decision. PMID:21279128

  14. Acquired Form of Angioedema of the Head and Neck Related to a Deficiency in C1-Inhibitor: A Case Report with a Review of the Literature

    Directory of Open Access Journals (Sweden)

    Bassel Hallak

    2012-01-01

    Full Text Available Angioedema related to a deficiency in the C1-inhibitor protein is characterized by its lack of response to therapies including antihistamine, steroids, and epinephrine. In the case of laryngeal edema, mortality rate is approximately 30 percent. The first case of the acquired form of angioedema related to a deficiency in C1-inhibitor was published in 1972. In our paper, we present a case of an acquired form of angioedema of the oropharyngeal region secondary to the simultaneous occurrence of two causative factors: neutralization of C1-inhibitor by an autoantibody and the use of an angiotensin convertin enzyme inhibitor.

  15. MISCELLANEOUS

    Institute of Scientific and Technical Information of China (English)

    1993-01-01

    930204 Randomized clinical controlled cross-over trial(RCT)in the prevention of blood transfusion febrile reactions with small dose ofhydrocortisone versus antihistamines.WANGJuesheng(王觉生),et al.Dept Intern Med,West-China Med Univ,610041.Chin J InternMed 1992;31(9):536—538.RCT was used in 73 patients who had experi-enced blood transfusion febrile reactions.Forfurther two transfusions Benadryl was used be-fore the first transfusion and hydrocortisone be-

  16. Creutzfeldt-Jacob’s Disease Presenting with Psychiatric Symptomsand Severe Itching

    Directory of Open Access Journals (Sweden)

    Emine Rabia Koç

    2013-03-01

    Full Text Available Creutzfeldt-Jakob disease is a rare and fatal neurodegenerative disease that is characterized by the accumulation of abnormal prion-like proteins in the central nervous system. Clinical features, electroencephalography, brain magnetic resonance imaging and protein 14.3.3 is useful in diagnosis. Protein 14.3.3 may be negative in the early or late stages of the disease. Presentation with psychiatric symptoms and itching is not typical in the beginning of the disease In this paper, we present a patient who was first accepted to the pschiatry ward because of his psychiatric symtpoms and had severe itching, resistant to antihistaminic drugs.

  17. Molecular design of synthetic benzimidazoles for the switchover of the duplex to G-quadruplex DNA recognition.

    Science.gov (United States)

    Maji, Basudeb; Bhattacharya, Santanu

    2013-01-01

    Benzimidazole derivatives are well known for their antibacterial, antiviral, anticonvulsant, antihistaminic, anthelmintic and antidepressant activities. Benzimidazole's unique base-selective DNA recognition property has been studied widely. However, most of the early benzimidazole systems have been targeted towards the binding of duplex DNA. Here we have shown the evolution and progress of the design and synthesis of new benzimidazole systems towards selective recognition of the double-stranded DNA first. Then in order to achieve selective recognition of the G-quadruplex DNA and utilize their potential as future anti-cancer drug candidates, we have demonstrated their selective cytotoxicity towards the cancer cells and potent telomerase inhibition ability.

  18. XXIV World Allergy Congress 2015

    OpenAIRE

    Lee, Heung-Man; Park, Il-Ho; Shin, Jae-Min; Zeher, Margit; Matsui, Katsuhiko; Tamai, Saki; Ikeda, Reiko; Suri, Drsushil; Suri, Dranu; Arani, Marzieh Heidarzadeh; Lubis, Azwin; Endaryanto, Anang; Koga, Shinichiro; Tsuzuki, Yasunobu; Jin, Shan

    2016-01-01

    Table of Contents A1 Pirfenidone inhibits TGF-b1-induced extracellular matrix production in nasal polyp-derived fibroblasts Jae-Min Shin, Heung-Man Lee, Il-Ho Park A2 The efficacy of a 2-week course of oral steroid in the treatment of chronic spontaneous urticaria refractory to antihistamines Hyun-Sun Yoon, Gyeong Yul Park A3 The altered distribution of follicular t helper cells may predict a more pronounced clinical course of primary sjögren’s syndrome Margit Zeher A4 Betamethasone suppresse...

  19. St Anne's Private Nursing Home, Sonnagh, Charlestown, Mayo.

    LENUS (Irish Health Repository)

    Szarvas, Szilvia

    2012-02-03

    When intrathecal and epidural opioids are administered, pruritus occurs as an unwanted and troublesome side effect. The reported incidence varies between 30% and 100%. The exact mechanisms of neuraxial opioid-induced pruritus remain unclear. Postulated mechanisms include the presence of an "itch center" in the central nervous system, medullary dorsal horn activation, and antagonism of inhibitory transmitters. The treatment of intrathecal opioid-induced pruritus remains a challenge. Many pharmacological therapies, including antihistamines, 5-HT(3)-receptor antagonists, opiate-antagonists, propofol, nonsteroid antiinflammatory drugs, and droperidol, have been studied. In this review, we will summarize pathophysiological and pharmacological advances that will improve understanding and ultimately the management of this troublesome problem.

  20. Histamine release and endothelial leakage from an intravascular contrast medium

    Energy Technology Data Exchange (ETDEWEB)

    Raininko, R.

    1981-04-01

    The endothelial injury produced by meglumine iodamide was studied in the rat aorta. A mixture of blood and contrast medium was more toxic to the endothelium than the pure contrast agent. This difference disappeared after premedication with antihistamine, which did not affect the injury produced by the pure contrast agent. Meglumine iodamide appears to cause a release of histamine from blood but not from the aortic endothelium nor from surrounding tissues in amounts demonstrable by this method. Leucocytes are a source of histamine after intravascular contrast medium administration.

  1. Synthesis of pyrilamine-d/sub 6/

    Energy Technology Data Exchange (ETDEWEB)

    Bird, I.; Shuker, D.E.G. (Medical Research Council, Carshalton (UK))

    1985-02-01

    The antihistamine drug pyrilamine-d/sub 6/(N-((4-methoxyphenyl)methyl)-N',N'-di(/sup 2/H/sub 3/ )methyl-N-2-pyridinyl-1,2-ethanediamine) was synthesised from N-2-((4-methoxyphenyl)methyl)-aminopyridine and 2-(N,N-di(/sup 2/H/sub 3/)methylamino)ethyl chloride in 83% yield. The alkyl chloride was prepared in 37% overall yield in a three step reaction from toluene-4-sulphondi(/sup 2/H/sub 3/)methylamide.

  2. Bilateral angioedema of eye with single dose of cetirizine

    Directory of Open Access Journals (Sweden)

    Lakhan Majhee

    2015-12-01

    Full Text Available The H1-antihistamine cetirizine is considered to be one of the safest drugs with well-established safety and efficacy. Very rarely cetirizine can cause adverse drug reaction in the form of dose-dependent somnolence, dizziness, or fatigue. We report a case of 27-year-old female patient with isolated angioedema on both the eye due to the administration of single dose of cetirizine 10 mg for hemorroids with pruritus ani. The mechanism of reaction remains unclear. [Int J Basic Clin Pharmacol 2015; 4(6.000: 1296-1298

  3. Sorafenib-induced hand-foot syndrome in a patient of renal cell carcinoma

    Directory of Open Access Journals (Sweden)

    Amrita Sil

    2014-01-01

    Full Text Available Sorafenib, a multikinase inhibitor, is approved for treatment of renal cell cancer and hepatocellular cancer. Hand-foot syndrome (HFD is a condition where erythema, scaling, and bullous lesion affect the hand and feet. In this case, a post-nephrectomy renal carcinoma patient prescribed sorafenib developed HFD 1 week after the drug usage. All laboratory parameters were within normal limits. The dose of sorafenib was reduced and topical corticosteroids, antihistamines, and emollients were prescribed. The reaction reduced after 2 weeks of therapy, only to reappear again when the second cycle of sorafenib-targeted therapy was started. The case was diagnosed as sorafenib-induced HFD.

  4. Brakioradial pruritus behandlet effektivt med gabapentin

    DEFF Research Database (Denmark)

    Uldall Pallesen, Kristine Appel; Bygum, Anette

    2012-01-01

    Brachioradial pruritus is a characteristic clinical condition with a deep intense itching, tingling or burning sensation localized to the dorsolateral part of the upper extremities. The symptoms occur primarily in the late summer in fair skin type people who are extensively sun-exposed. The condi......-exposed. The condition is difficult to treat and does not respond to topical steroids and antihistamines. We describe a 57-year-old woman with longstanding brachioradial itching due to cervical radiculopathy and sun exposure, which was successfully treated with gabapentin....

  5. Severe anaphylactic reaction to mediterranean jellyfish (Ropilhema nomadica envenomation: Case report

    Directory of Open Access Journals (Sweden)

    Nadav Friedel

    2016-01-01

    Full Text Available We present a 15-year-old female patient with an anaphylactic reaction to a jellyfish sting, sustained while surfing in the Mediterranean Sea. She experienced immediate difficulty in breathing, hoarseness and itching and was taken by ambulance to the emergency department, receiving intramuscular adrenaline on the way. She presented with periorbital swelling and facial edema and improved with systemic steroids and antihistamines. She was discharged 2 days later with allergy service follow up at our institution. This is the first case report documenting anaphylaxis due to Mediterranean jellyfish envenomation.

  6. Treatment of refractory chronic urticaria

    Directory of Open Access Journals (Sweden)

    Aayushi Mehta

    2015-01-01

    Full Text Available Chronic spontaneous urticaria is a distressing disease encountered frequently in clinical practice. The current mainstay of therapy is the use of second-generation, non-sedating antihistamines. However, in patients who do not respond satisfactorily to these agents, a variety of other drugs are used. This article examines the available literature for frequently used agents including systemic corticosteroids, leukotriene receptor antagonists, dapsone, sulfasalazine, hydroxychloroquine, H2 antagonists, methotrexate, cyclosporine A, omalizumab, autologous serum therapy, and mycophenolate mofetil, with an additional focus on publications in Indian literature.

  7. Management of difficult urticaria

    Directory of Open Access Journals (Sweden)

    Yadav Sudha

    2009-01-01

    Full Text Available Chronic urticaria, a major health problem causing patient′s distress, induces often physicians′ dilemma while dealing with its etiology, investigations and management. Clinical approach of such cases should include apart from clinical history and physical examination laboratory investigations like routine blood test, thyroid profile, etc. as well as sometimes special test like autologous serum skin test. Management includes reassurance, avoidance of precipitating factors, treatment of underlying disorders, and non-pharmacological approach along with pharmacotherapy. First line drug therapy comprises non-sedative and sedative antihistamines, second line doxepin, nifedipine, leukotriene-inhibitors, sulfasalazine, etc. and third line cyclosporine, dapsone, colchicin, etc.

  8. The Link between Allergic Rhinitis and Asthma: A Role for Antileukotrienes?

    Directory of Open Access Journals (Sweden)

    H Kim

    2008-01-01

    Full Text Available Allergic rhinitis and asthma are both chronic heterogeneous disorders, with an overlapping epidemiology of prevalence, health care costs and social costs in quality of life. Both are inflammatory disorders with a similar pathophysiology, and both share some treatment approaches. However, each disorder has an array of treatments used separately in controlling these atopic disorders, from inhaled corticosteroids, beta2-agonists and antihistamines to newer monoclonal antibody-based treatments. The present article reviews the shared components of allergic rhinitis and asthma, and examines recent evidence supporting antileukotrienes as effective agents in reducing the symptoms of both diseases.

  9. Use of lenalidomide in treating refractory prurigo nodularis.

    Science.gov (United States)

    Liu, Hannah; Gaspari, Anthony A; Schleichert, Rachel

    2013-03-01

    Prurigo nodularis is a chronic, relapsing neurodermatitis that is often resistant to standard therapies with topical corticosteroids and oral antihistamines. Thalidomide, while efficacious in treating recalcitrant cases of prurigo nodularis, causes significant toxicity. Thalidomide-induced peripheral neuropathy frequently results in drug discontinuation. Lenalidomide (Revlimid; Celgene Corporation, Summit, NJ) is a derivative of thalidomide with less neurotoxicity approved for the treatment of multiple myeloma and myelodysplastic syndromes that has not been widely studied in dermatologic disorders. Here, we report a case of refractory prurigo nodularis effectively treated with lenalidomide. Given its favorable side-effect profile, lenalidomide may offer a superior alternative to thalidomide in the treatment of this condition.

  10. Toxic Epidermal Necrolysis induced by rarely implicated drugs

    Directory of Open Access Journals (Sweden)

    Sujit Rajagopalan

    2012-01-01

    Full Text Available Toxic Epidermal Necrolysis (TEN and Steven-Johnson Syndrome (SJS are serious disorders commonly caused as idiosyncratic reactions to drugs, the most common ones being oxicams, anticonvulsants, allopurinol, and sulfonamides. We present a case of TEN in a patient who developed the lesions after ingesting multiple drugs including paracetamol, metoclopramide, antihistamines, and multivitamins. These drugs have rarely been implicated in this disorder. The suspected drugs in this case were paracetamol and metoclopramide. However, the role of other drugs could not be ruled out definitely. The patient was managed with antibiotics, corticosteroids, and parenteral fluids and recovered well.

  11. Exanthema after a stress Tc-99m sestamibi study: continue with a rest sestamibi study?

    DEFF Research Database (Denmark)

    Hesse, Birger; Vinberg, Niels; Mosbech, Holger

    2011-01-01

    of a further reaction. Material and methods:  A patient experienced a maculo-papular exanthema, i.e. a mild, probably allergic, adverse event (AE) after a stress MPI including administration of a dose of Tc-99m sestamibi. A rest MPI was needed to decide whether coronary bypass surgery should be performed....... After prophylactic treatment with antihistamine and corticosteroid, an uneventful rest MPI was performed. Discussion and conclusion:  International recommendations or guidelines related to treatment of AEs after nuclear medicine studies do not exist. Serious AEs in nuclear medicine are very rare...

  12. Use of intranasal corticosteroids in the management of congestion and sleep disturbance in pediatric patients with allergic rhinitis.

    Science.gov (United States)

    Lanier, Bob Q

    2008-06-01

    Allergic rhinitis affects a large number of children and exerts a considerable socioeconomic impact. It is underdiagnosed and inadequately treated, which predisposes children to potentially serious comorbidities. Allergic rhinitis symptoms may create nighttime breathing problems and sleep disturbances and have a negative effect on a child's ability to learn in the classroom. Although antihistamines have shown efficacy in relieving many symptoms, they have little effect on nasal congestion. This article summarizes the advantages of intranasal corticosteroids, including their effectiveness against congestion and excellent safety profile. Intranasal corticosteroids with minimal systemic bioavailability provide topical drug delivery that minimizes the potential for systemic side-effects.

  13. Drug: D00664 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00664 Drug Cetirizine hydrochloride (JP16/USAN); Zyrtec (TN) C21H25ClN2O3. 2HCl 46...Japan [BR:br08301] 4 Agents affecting cellular function 44 Allergic agents 449 Miscellaneous 4490 Miscellaneous D00664 Cetirizine...S FOR SYSTEMIC USE R06AE Piperazine derivatives R06AE07 Cetirizine D00664 Cetirizine hydrochloride (JP16/USA...N) USP drug classification [BR:br08302] Respiratory Tract/Pulmonary Agents Antihistamines Cetirizine... D00664 Cetirizine hydrochloride (JP16/USAN) Target-based classification of drugs [BR:br0

  14. Anaphylaxis.

    Science.gov (United States)

    Hernandez, Lorenzo; Papalia, Sarah; Pujalte, George G A

    2016-09-01

    Anaphylaxis is an acute, systemic reaction mediated by immunoglobulin E hypersensitivity. Release of bioactive factors causes vasodilation and bronchiole constriction that can lead to hypotensive shock and asphyxiation. Differential diagnosis includes acute asthma, localized angioedema, syncope, and anxiety/panic attacks. Diagnostic tests lack specificity. Clinical diagnosis is based on demonstration of specific airway or cardiovascular compromise within proximity of allergen exposure. Treatment includes epinephrine, antihistamines, fluid resuscitation, and airway management. Prevention focuses on awareness/avoidance of triggers, implementation of personalized action plans, as well as immune modulation by desensitization in a closely controlled setting where available.

  15. [Allergy-related emergencies].

    Science.gov (United States)

    Kaufman, E; Garfunkel, A; Galili, D; Zusman, S P; Malamed, S F; Findler, M; Elad, S

    2002-01-01

    Allergic reactions can develop to any of the drugs or materials commonly used in dentistry. They exhibit a broad range of clinical signs and symptoms ranging from mild, delayed reactions to immediate and life-threatening reactions developing within seconds. Allergies usually manifest themselves in reactions that are related to histamine release in one of three ways: skin reactions, respiratory problems and anaphylaxis. Anaphylaxis is the most critical allergic reaction in the dental environment. Measures such as airway management, oxygen supplementation, antihistamine, adrenaline and corticosteroid medication, cardiopulmonary resuscitation and evacuation to the emergency room, may be necessary.

  16. Mania after misuse of dextromethorphan: a case report and brief review of "robotripping".

    Science.gov (United States)

    Stanciu, Cornel N; Penders, Thomas M

    2015-01-01

    Dextromethorphan (DXM) in combination with antihistamines and/or pseudoephedrine is widely available as an over-the-counter remedy commonly used for relief of colds and cough. In supratherapeutic amounts, DXM can be extremely activating. These cough preparations have been adopted by many young users of recreational drugs for their psychoactive effects. When used in amounts exceeding those recommended, this practice, known as "robotripping," may result in a manic toxidrome of psychomotor agitation, hostility, grandiose behavior, hallucinations, paranoia, and panic. A case illustration of this phenomenon is described and implications of this phenomenon discussed. There are few reports associating DXM use with bipolar symptomatology.

  17. A rare case of isoniazid-induced erythroderma

    Directory of Open Access Journals (Sweden)

    Yashika Garg

    2015-01-01

    Full Text Available Tuberculosis is a common infectious disease in developing countries. Isoniazid is established the first-line antitubercular drug and an essential component of all antitubercular regimens. Erythroderma caused by isoniazid is an uncommon but serious adverse drug reaction. We report here a case of a 63-year-old female patient who presented with generalized redness and scaling with itching after 8 weeks of antitubercular treatment (ATT. ATT was stopped immediately, and antihistaminics were started. The patient improved over a period of 2 weeks. On sequential rechallenge, she developed similar lesions all over the body with isoniazid, hence confirming the diagnosis of isoniazid-induced erythroderma.

  18. Pharmacokinetic Dose Proportionality Between Two Strengths (12.5 mg and 25 mg) of Doxylamine Hydrogen Succinate Film-Coated Tablets in Fasting State: A Single-Dose, Randomized, Two-Period Crossover Study in Healthy Volunteers

    OpenAIRE

    Videla, Sebastián; Cebrecos, Jesús; Lahjou, Mounia; Wagner, France; Guibord, Pascal; Xu, Zhengguo; Cabot, Anna; Encabo, Mercedes; Encina, Gregorio; Sicard, Eric; Sans, Artur

    2013-01-01

    Background Doxylamine succinate, an ethanolamine-based antihistamine, is used in the short-term management of insomnia because of its sedative effects. No data on the dose proportionality of the pharmacokinetics of doxylamine are available, although this drug has been marketed in European countries for more than 50 years. Objective The objective of this study was to evaluate and compare the dose proportionality between two marketed strengths (12.5 mg and 25 mg) of doxylamine hydrogen succinat...

  19. Suicide through doxylamine poisoning.

    Science.gov (United States)

    Bockholdt, B; Klug, E; Schneider, V

    2001-06-01

    Doxylamine is an antihistamine of the ethanolamine class. It is used primarily as a sleep-inducing agent. Only a few reports can be found in the literature about lethal intoxications with doxylamine, but many with combined intoxications. Doxylamine is, aside from diphenhydramine, the only chemically defined active ingredient in some sleeping medications which is available without a prescription in the Federal Republic of Germany. Two cases of doxylamine poisoning are presented, in which high doxylamine concentrations were found in the blood and organs.

  20. Poison ivy, oak, and sumac dermatitis identification, treatment, and prevention.

    Science.gov (United States)

    Garner, L A

    1999-05-01

    Allergic contact dermatitis from poison ivy, oak, or sumac is common among people who work or exercise outdoors. The plants, classified in the genus Rhus or Toxicodendron, contain allergens that can cause reactions ranging from mild pruritus to severe urticaria or generalized maculopapular eruptions. Initial management includes cleansing, cold compresses, and, possibly, oral antihistamines for symptomatic relief. Topical corticosteroids are given for localized nonfacial eruptions; systemic corticosteroids are used for severe eruptions. Prevention involves avoiding contact with the plants and washing exposed skin within 2 hours.

  1. Omalizumab for Urticarial Vasculitis: Case Report and Review of the Literature

    Directory of Open Access Journals (Sweden)

    Misbah Nasheela Ghazanfar

    2015-01-01

    Full Text Available Urticarial vasculitis is characterised by inflamed itching or burning red patches or wheals that resemble urticaria but persist for greater than 24 hours. It is often idiopathic but is sometimes associated with collagen-vascular disease, particularly systemic lupus erythematosus. Treatment options include oral antihistamines, oral corticosteroids, dapsone, colchicine or hydroxychloroquine. We describe a male patient with urticarial vasculitis who was treated with omalizumab (anti-IgE with convincing results and provide a review of previous reports of patients with urticarial vasculitis treated with omalizumab.

  2. [The marketing analysis of assortment of market of pharmaceuticals applied in treatment of psoriasis in Ukraine].

    Science.gov (United States)

    Kotvitskaya, A A; Karlo, V V

    2013-01-01

    The analysis of assortment of pharmaceuticals for treatment of psoriasis recommended by Minzdrav of Ukraine and present at the national pharmaceutical market is made. The characteristics of distribution of national and foreign producers of antihistamine and anti-psoriatic pharmaceuticals are established The availability of particular medicinal forms of various producers is analyzed too. The characteristics and tendencies in consumption of these groups of pharmaceuticals in natural and monetary units are analyzed including dynamics of changes of mean wholesale prices during the analyzed period.

  3. Experimenteller Nachweis der Symptomreduktion bei Patienten mit Kältekontakturtikaria durch Dosissteigerung von Bilastin

    OpenAIRE

    Spohr, Adrian

    2014-01-01

    Background: Cold contact urticaria (CCU) is characterized by itchy wheal and flare responses due to the release of histamine and other pro-inflammatory mediators after exposure to cold. The treatment of choice in CCU are non-sedating H1 antihistamines. If patients cannot be sufficiently controlled with standard dosages, the current EAACI/GA2LEN/EDF/WAO-guideline for the management of urticaria recommends high-dose H1 blockers up to 4 times the standard dose. Objective: Aim of the study is...

  4. Up-dosing with bilastine results in improved effectiveness in cold contact urticaria

    OpenAIRE

    Krause, K; Spohr, A.; Zuberbier, T.; Church, M. K.; Maurer, M.

    2013-01-01

    Background Cold contact urticaria (CCU) is characterized by itchy wheal and flare responses due to the release of histamine and other pro-inflammatory mediators after exposure to cold. The treatment of choice is nonsedating antihistamines, dosages of which may be increased up to fourfold if standard doses are ineffective. Here, we assess the effects of a standard 20 mg dose and up-dosing to 40 and 80 mg of bilastine in reducing the symptoms of CCU and inflammatory mediator release following c...

  5. Triprotic acid-base microequilibria and pharmacokinetic sequelae of cetirizine.

    Science.gov (United States)

    Marosi, Attila; Kovács, Zsuzsanna; Béni, Szabolcs; Kökösi, József; Noszál, Béla

    2009-06-28

    (1)H NMR-pH titrations of cetirizine, the widely used antihistamine and four related compounds were carried out and the related 11 macroscopic protonation constants were determined. The interactivity parameter between the two piperazine amine groups was obtained from two symmetric piperazine derivatives. Combining these two types of datasets, all the 12 microconstants and derived tautomeric constants of cetirizine were calculated. Upon this basis, the conflicting literature data of cetirizine microspeciation were clarified, and the pharmacokinetic absorption-distribution properties could be interpreted. The pH-dependent distribution of the microspecies is provided.

  6. Flushing syndrome due to mahimahi (scombroid fish) poisoning.

    Science.gov (United States)

    Kim, R

    1979-08-01

    Scombroid fish poisoning, one of the most common adverse reactions to fish, is also probably one of the most common causes of a flushing syndrome. The reaction usually involves fishes of the Scombridae family but, in Hawaii, the reaction is most often due to mahimahi (Coryphaena hippurus). Onset of the reaction is usually abrupt and commonly associated with a prominent flush resembling a sunburn. Headache, tachye to a toxin with histamine-like properties, which is formed because improper refrigeration enables endogenous bacteria to decarboxylate histidine normally present in dark-meat fishes. Symptoms are usually promptly relieved by parenteral antihistamine therapy.

  7. Bullous Mastocytosis Mimicking Congenital Epidermolysis Bullosa

    Directory of Open Access Journals (Sweden)

    Julio Cesar Salas-Alanis

    2014-05-01

    Full Text Available A 2-month-old female infant was referred to DebRA Mexico from the Regional Children's Hospital because of a generalized dermatosis from birth characterized by multiple blisters and erosions on the trunk, face and limbs, associated with minor trauma. A skin biopsy showing subepidermal blisters associated with a dermal infiltrate of Giemsa-positive cells and CD117-positive antibody was consistent with the diagnosis of bullous mastocytosis. Treatment with oral antihistamines, topical steroids, and antibiotics was initiated, leading to a remission of the lesions.

  8. Clinico-Pathological aspects of Shock

    Directory of Open Access Journals (Sweden)

    Kulkarni M.D.

    2009-08-01

    Full Text Available Shock can be defined as “a common grave medical emergency characterised basically by reduction in the effective circulating blood volume and blood pressure”. (Robbins or as “Disparity between the volume of blood and the volume capacity of the vascular system” which cause inability of body tissue to metabolise nutrients due to inadequate oxygen supply. Shock can be classified into: Primary and Secondary.Cardiogenic, Vasogenic, Hematogenic, Neurogenic and Electrocution. The therapy includes Blood, Plasma, Saline transfusion, antibiotic, antihistaminic, hyperimmune serum, vasoconstrictor according to the cause of the shock. [Vet. World 2009; 2(4.000: 163-165

  9. Neuraxial opioid-induced pruritus: a review.

    LENUS (Irish Health Repository)

    Szarvas, Szilvia

    2012-02-03

    When intrathecal and epidural opioids are administered, pruritus occurs as an unwanted and troublesome side effect. The reported incidence varies between 30% and 100%. The exact mechanisms of neuraxial opioid-induced pruritus remain unclear. Postulated mechanisms include the presence of an "itch center" in the central nervous system, medullary dorsal horn activation, and antagonism of inhibitory transmitters. The treatment of intrathecal opioid-induced pruritus remains a challenge. Many pharmacological therapies, including antihistamines, 5-HT(3)-receptor antagonists, opiate-antagonists, propofol, nonsteroid antiinflammatory drugs, and droperidol, have been studied. In this review, we will summarize pathophysiological and pharmacological advances that will improve understanding and ultimately the management of this troublesome problem.

  10. Intolerance to topical products may be due to dermographism.

    Science.gov (United States)

    Watsky, Kalman L; McGovern, Thomas

    2003-03-01

    Patients with reactions to topical products may be eliciting a physical urticaria, dermographism, by rubbing. These reactions may be misinterpreted as allergic, and three cases demonstrating this phenomenon were reviewed. All patients with reactions to topical products due to dermographism improved with counseling and antihistamine therapy. Repeat open application testing confirmed the safety of previously suspect medications in two of the three cases, preventing unnecessary changes in the medication regimens and inaccurate diagnoses of medication allergy. We observe that intolerance to topical medications due to dermographism can usually be managed without extensive testing or treatment.

  11. [Dermatitis from contact with Agave americana].

    Science.gov (United States)

    Golan, H; Landau, M; Goldberg, I; Brenner, S

    2000-10-01

    Various plants induce dermatitis in man. There have been only a few published cases of contact dermatitis caused by Agave americana (AA). We report intentional exposure to AA in a soldier seeking sick leave, and review our previously reported cases. Treatment with oral antihistamines and topical saline compresses resulted in subsidence of the systemic symptoms within 24 h and regression of cutaneous manifestations in 7-10 days. Physicians should be alert to the possibility of self-inflicted contact dermatitis induced by exposure to plants, especially to A. americana. Systemic signs may accompany the cutaneous lesions.

  12. Pityriasis rosea-like eruptions due to mustard oil application

    Directory of Open Access Journals (Sweden)

    Zawar Vijay

    2005-01-01

    Full Text Available A young man employed in a construction company, presented with cutaneous lesions clinically simulating pityriasis rosea. Satisfactory and complete response to corticosteroids and antihistamines was followed by recurrence. Multiple recurrences within a short span of time arose a suspicion of alternative diagnosis. Site visit helped us to rule out occupational contact dermatitis. Further history taking revealed that he was recently using mustard oil for body massage. Subsequent patch testing confirmed contact hypersensitivity to mustard oil. Avoidance of the contact with mustard oil arrested appearance of further skin lesions. We stress the importance of taking a good history in clinical practice in disclosing a possible contactant.

  13. The clinical management of hyperemesis gravidarum.

    Science.gov (United States)

    Sonkusare, Shipra

    2011-06-01

    Hyperemesis gravidarum is a severe and disabling condition with potentially life-threatening complications. It is likely to have a multifactorial etiology which contributes to the difficulty in treatment. Treatment is supportive with correction of dehydration and electrolyte disturbance, antiemetic therapy, prevention and treatment of complications like Wernicke's encephalopathy, osmotic demyelination syndrome, thromboembolism, and good psychological support. There are abundant data on the safety of antihistamines, phenothiazines, and metoclopromide in early pregnancy and treatment should therefore not be withheld on the basis of teratogenicity concerns. Thiamine replacement is indicated in hyperemesis gravidarum to prevent development of Wernicke's encephalopathy.

  14. KALANCHOE PINNATA : PHYTOCHEMICAL AND PHARMACOLOGICAL PROFILE

    Directory of Open Access Journals (Sweden)

    Seema V. Pattewar

    2012-03-01

    Full Text Available The main objective of this review is to provide advance information for the drug discovery research from the divine herb Kalanchoe pinnata, which contains a wide range of active compounds, including alkaloids, triterpenes, glycosides, flavonoids, steroids, bufadienolides, lipids and organic acids. The pharmacological studies are reviewed and discussed, focussing on activities as immunomodulator, CNS depressant, analgesic, antimicrobial, antiinflammatory, antiallergic, antianaphylactic, antileishmanial, antitumorous, antiulcerous, antibacterial, antifungal, antihistamine, antiviral, febrifuge, gastroprotective, immunosuppressive, insecticidal, muscle relaxant, sedative, anticancer. Now it becomes endangered plant which needs to be conserved as well as explored for its significant green chemistry.

  15. Management of urticaria and angioedema in children: new trends.

    Science.gov (United States)

    Oranje, A P

    2010-12-01

    Urticaria in childhood is a common problem. History of development of urticaria should be carefully taken from a written history/information list. For urticaria, the EAACI/GALEN/EDF consensus guidelines on definition, classification, diagnosis and management of urticaria should be considered. Soon an updated version of a new consensus will appear. The new classification of urticaria includes 3 main groups: spontaneous or idiopathic urticaria (divided in acute urticaria ≥6 weeks), physical urticaria (cold contact urticaria, delayed pressure urticaria) and other urticaria disorders such as aquagenic urticaria. In general aspects, there is no difference between children and adults, except some details. In children most urticaria are acute idiopathic or physical of character. Also, urticarial flares in atopic dermatitis in young children are common as manifestation of food allergy First step of treatment is directed to the cause (that is difficult in chronic urticaria) and triggering factors. The currently recommended first line treatment is application of oral nonsedating H1 antihistamines. If needed, the dosage of antihistamines should be up to two-fold (in adults four-fold), although evidence is lacking for this, whereas alternative treatment should be reserved as add-on therapy for unresponsive patients.

  16. Implementation of anaphylaxis management guidelines: a register-based study.

    Directory of Open Access Journals (Sweden)

    Linus Grabenhenrich

    Full Text Available BACKGROUND: Anaphylaxis management guidelines recommend the use of intramuscular adrenaline in severe reactions, complemented by antihistamines and corticoids; secondary prevention includes allergen avoidance and provision of self-applicable first aid drugs. Gaps between recommendations and their implementation have been reported, but only in confined settings. Hence, we analysed nation-wide data on the management of anaphylaxis, evaluating the implementation of guidelines. METHODS: Within the anaphylaxis registry, allergy referral centres across Germany, Austria and Switzerland provided data on severe anaphylaxis cases. Based on patient records, details on reaction circumstances, diagnostic workup and treatment were collected via online questionnaire. Report of anaphylaxis through emergency physicians allowed for validation of registry data. RESULTS: 2114 severe anaphylaxis patients from 58 centres were included. 8% received adrenaline intravenously, 4% intramuscularly; 50% antihistamines, and 51% corticoids. Validation data indicated moderate underreporting of first aid drugs in the Registry. 20% received specific instructions at the time of the reaction; 81% were provided with prophylactic first aid drugs at any time. CONCLUSION: There is a distinct discrepancy between current anaphylaxis management guidelines and their implementation. To improve patient care, a revised approach for medical education and training on the management of severe anaphylaxis is warranted.

  17. A report of acute atrial fibrillation induced by misapplication of epinephrine

    Directory of Open Access Journals (Sweden)

    Yu-Jang Su

    2015-06-01

    Full Text Available Urticaria is a systemic allergic reaction leading to wheal formation with skin itching. Occasionally we come across some intractable cases, in which we may administrate epinephrine infusion besides steroid and anti-histamine. A 19 year-old man suffered from intractable urticaria for 2 days, although anti-histamine and steroids were used. Titration of adrenaline was considered in the treatment of intractable urticaria. He was administrated 1 mg epinephrine intravenous bolus due to mis-dilution by the nurse. Transient atrial fibrillation with cardiac ischemia occurred. After 12.5 mg labetalol i.v., and 11-hour observation in the emergency room, he gradually recovered to normal sinus rhythm without ST-T change. In the past, ventricular tachycardia, hypertension, chest pain, pulmonary edema, the need to intubate, renal failure requiring renal transplant, coronary artery spasm, myocardial ischemia/infarction and hypokalemia have been reported after mis-diluted or excessive doses of epinephrine in treating anaphylaxis. To our knowledge, our case is the first worldwide to describe transient atrial fibrillation after epinephrine overdose, and the patient was successfully resuscitated by 12.5 mg labetalol. It is important to know how to rescue accidental epinephrine intravenous injection patients.

  18. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria.

    Science.gov (United States)

    Sadaba, Belen; Azanza, Jose Ramon; Gomez-Guiu, Almundena; Rodil, Raquel

    2013-01-01

    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.

  19. Differences of promethazine and terfenadine on ion channels in guinea pig ventricular myocytes

    Institute of Scientific and Technical Information of China (English)

    LI Xue-wen; NIU Shuan-cheng; ZHANG Xuan-ping; L(U) Ji-yuan; BAI Feng; ZHANG Ling; WU Bo-wei

    2006-01-01

    @@ Promethazine, a first generation antihistamine,has an antiarrhythmic effect on ischemia-reperfusion inducing arrhythmias1 and experimental arrhythmias.2 However, terfenadine as a second generation of antihistamine, has been reported to elicit hypotension, bradycardia, prolongation of the QTc interval and torsades de pointes (TdP) like ventricular arrhythmia.3 This may be due to the blockage on rectifier postassium current (Ik) of terfenadine, resulting in the prolongation of the action potential duration (APD) and dispersion of the repolarization duration, which might provoke a specific form of polymorphic ventricular tachydysrhythmia, i.e. TdP.4 In clinical practice,however, the class Ⅲ antiarrhythmic agents, which target on the Ik and prolong the action potential duration and QTc interval, rarely lead to arrhythmias.Other actions must be considered to underlie the arrhythmogenic tendency of terfenadine besides its inhibition on Ik. Though both promethazine and terfenadine block the H1 receptor, there must be a different pharmacology profile between the two compounds on ion channels of cardiac myocytes.Whole-cell patch clamp technique was used to investigate the effects of these two antagonists of the H1 receptor on the main ion currents in cardiac electrical activities.

  20. A report of acute atrial fibrillation induced by misapplication of epinephrine

    Institute of Scientific and Technical Information of China (English)

    Yu-Jang Su

    2015-01-01

    Urticaria is a systemic allergic reaction leading to wheal formation with skin itching. Occasionally we come across some intractable cases, in which we may administrate epinephrine infusion besides steroid and anti-histamine. A 19 year-old man suffered from intractable urticaria for 2 days, although anti-histamine and steroids were used. Titration of adrenaline was considered in the treatment of intractable urticaria. He was administrated 1 mg epinephrine intravenous bolus due to mis-dilution by the nurse. Transient atrial fibrillation with cardiac ischemia occurred. After 12.5 mg labetalol i.v., and 11-hour observation in the emergency room, he gradually recovered to normal sinus rhythm without ST-T change. In the past, ventricular tachycardia, hypertension, chest pain, pulmonary edema, the need to intubate, renal failure requiring renal transplant, coronary artery spasm, myocardial ischemia/infarction and hypokalemia have been reported after mis-diluted or excessive doses of epinephrine in treating anaphylaxis. To our knowledge, our case is the first worldwide to describe transient atrial fibrillation after epinephrine overdose, and the patient was successfully resuscitated by 12.5 mg labetalol. It is important to know how to rescue accidental epinephrine intravenous injection patients.