Search

Background: Yellow horn poppy (Glaucium flavum, syn. Chelidonium flavum) in the family Papaveraceae, is growing in many geographical areas; it is mostly native to Northern Africa, Western Asia, and Europe. The plant is well known for its different types of alkaloids, including aporphines, protopines, and phenolic compounds. In Eastern Europe, the HCl and HBr salts of glaucine (the common active constituent in G. flavum) have been approved as cough suppressants, in addition to several therapeutic applications in traditional medicine. The natural products of G. flavum varied according to the geographical habitat, the stage of maturity, and the selected plant organ. Materials and Methods: For the first time, the extraction and isolation of natural products (alkaloids and flavonoids) from dried aerial parts of the Libyan population of yellow horn poppy and testing their biological effects, which include antihistaminic, antiarthritic, and antiobesity effects. Results: Alkaloids (glaucine and isoboldine) and flavonoid constituents (quercetin-7- O -rutinoside and rutin) have been isolated, while the biological activity results showed that quercetin-7- O -rutinoside and rutin showed half-maximal inhibitory concentration (IC50) (µg) = 29.7 and 46.6, 26.2 and 61.3, and 58.8 and 50.1 for antihistaminic, antiarthritic, and antiobesity, respectively, compared with those of glaucine and isoboldine effects, IC50 = 77.4 and 159.3, 61.7 and 118.7, and 237.8 and 157.6, respectively. Conclusion: According to the obtained results, the antihistaminic, antiarthritic, and antiobesity effects of the flavonoid compounds were stronger than those of the alkaloidal constituents of yellow horn poppy. [ABSTRACT FROM AUTHOR]

Allergic rhinitis (AR) is a highly prevalent respiratory condition that carries a heavy burden and can have a significant impact on patient quality of life. AR is caused by seasonal or perennial exposure to outdoor pollens and molds as well as indoor allergic triggers. In this review article, we discuss the factors associated with the development of AR throughout the year and the fact that patients with AR need continuous treatment rather than seasonal treatment. Conventionally, AR has been mainly categorized into seasonal AR and perennial AR, but these classes do not seem to be well-adapted. Climate changes, temperature changes, and high carbon dioxide (CO2) concentration affect the growth of plants and increase the length of pollen seasons and pollen allergenicity. Air pollution aggravates allergic sensitization symptoms in AR sensitized individuals. Due to increased air pollution and indefinite pollen seasons AR symptoms are present throughout the year. Patients with AR often need continuous treatment, which should be considered while making the strategy for treating allergic rhinitis sufferers. Management of AR involves avoiding the allergen, medications for symptomatic relief, anti-inflammatory therapies, and allergy immunotherapy. Although the first-generation H1-antihistamines reduce AR symptoms, they cause sedation and impair cognitive functions; thus, second-generation antihistamines (ie, levocetirizine, loratadine, bilastine, fexofenadine) are preferred. The efficacy and safety of fexofenadine for the treatment of seasonal allergic rhinitis (SAR) symptoms have been demonstrated by numerous clinical studies, irrespective of the season and underlying allergen. In this review, we discuss the allergic rhinitis classification, the role of climate change, air pollution, and factors contributing to year-round symptoms in patients with AR and the need for continuous pharmacological treatment for management.

Background: Asthma is a chronic inflammatory disease characterized by reversible airway obstruction, hyperresponsiveness, and remodeling. Asthma prevalence has increased significantly globally over the last decade, and it remains incurable to this date. Aims and Objectives: The present study evaluated some of the antiasthmatic medicinal plants to assess their mode of action. Materials and Method: Animal models for milk-induced leukocytosis, milk-induced eosinophilia, mast cell degranulation, clonidine-induced catalepsy, and active paw anaphylaxis were used to assess the pharmacological effects of Ammi visnaga, Medicago sativa, and Urtica dioica. Results: Mice pretreated with diazepam, methanolic extract of M. sativa, and U. dioica exhibited significant (P < 0.05) inhibition in milk-induced leukocytosis. However, only M. sativa showed statistically significant (P < 0.05) results. All plants showed a statistically significant (P < 0.05) tendency to decrease milk-induced eosinophilia. Methanolic extracts of all plants significantly (P < 0.05) protected mast cells against degranulation by clonidine. A. visnaga and U. dioica significantly (P < 0.05) protected mice against clonidine-induced catalepsy. An acute treatment by M. sativa potentiated the catalepsy, while it significantly inhibited the catalepsy (P < 0.05) upon chronic treatment. In the allergic inflammation model, methanolic extracts of all plants under study decreased paw thickness in a statistically significant manner (P < 0.05). Conclusion: All the three plants in this study demonstrated anti-inflammatory and antihistaminic effects, as well as decreased paw thickness, validate anti-allergic properties. A. visnaga showed a mast cell-stabilizing effect. A. visnaga and U. dioica inhibited the histamine-mediated clonidine-induced catalepsy from mast cells which proves the antihistaminic activity of these plants.

Abstract Background Treatment with commonly used drugs such as antidepressants (ADs), antipsychotics (APs), and benzodiazepines (BDs) may hamper the use of allergy skin testing due to possible antihistaminic effects. Objective To examine the antihistaminic effect of AD, AP, and BD as measured by the ability of these drugs to suppress the normal wheal reaction caused by skin prick test (SPT). Methods Skin prick test was performed in patients receiving treatment with AD, AP, and/or BD. Double SPT was performed with histamine solutions of 10, 30, and 100 mg/ml and mean wheal diameter calculated. Results A total of 313 patients were included. 236 (75%) patients were treated with one of the examined drugs and 77 (25%) patients with more than one of these drugs. Drugs most frequently used was sertraline (n = 65), citalopram (n = 63), mirtazapine (n = 36), venlafaxine (n = 33), and quetiapine (n = 32). Treatment with mirtazapine and/or quetiapine was associated with negative SPTs in 30/36 (83%) and 22/32 (69%), and the antihistaminic effect of these drugs was dose‐dependent. For patients treated with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (TCAs), serotonin norepinephrine reuptake inhibitors (SNRIs), or BD alone, almost all SPTs were positive (94%, 95%, 100%, and 100%, respectively). Negative SPTs in patients treated with SSRI, TCA, SNRI, or BD and ≥1 other of the examined drugs were associated with simultaneous treatment with mirtazapine or quetiapine in 39/44 (89%) patients. Conclusion Skin testing has little meaning in patients treated with mirtazapine or quetiapine. Treatment with SSRI, SNRI, and BD does not seem to affect the results of SPTs, whereas skin tests in patients treated with TCA should be interpreted with caution.

Background: Asthma is a chronic inflammatory disease characterized by reversible airway obstruction, hyperresponsiveness, and remodeling. Asthma prevalence has increased significantly globally over the last decade, and it remains incurable to this date. Aims and Objectives: The present study evaluated some of the antiasthmatic medicinal plants to assess their mode of action. Materials and Method: Animal models for milk-induced leukocytosis, milk-induced eosinophilia, mast cell degranulation, clonidine-induced catalepsy, and active paw anaphylaxis were used to assess the pharmacological effects of Ammi visnaga, Medicago sativa, and Urtica dioica. Results: Mice pretreated with diazepam, methanolic extract of M. sativa, and U. dioica exhibited significant (P < 0.05) inhibition in milk-induced leukocytosis. However, only M. sativa showed statistically significant (P < 0.05) results. All plants showed a statistically significant (P < 0.05) tendency to decrease milk-induced eosinophilia. Methanolic extracts of all plants significantly (P < 0.05) protected mast cells against degranulation by clonidine. A. visnaga and U. dioica significantly (P < 0.05) protected mice against clonidine-induced catalepsy. An acute treatment by M. sativa potentiated the catalepsy, while it significantly inhibited the catalepsy (P < 0.05) upon chronic treatment. In the allergic inflammation model, methanolic extracts of all plants under study decreased paw thickness in a statistically significant manner (P < 0.05). Conclusion: All the three plants in this study demonstrated anti-inflammatory and antihistaminic effects, as well as decreased paw thickness, validate anti-allergic properties. A. visnaga showed a mast cell-stabilizing effect. A. visnaga and U. dioica inhibited the histamine-mediated clonidine-induced catalepsy from mast cells which proves the antihistaminic activity of these plants. [ABSTRACT FROM AUTHOR]

Background: Treatment with commonly used drugs such as antidepressants (ADs), antipsychotics (APs), and benzodiazepines (BDs) may hamper the use of allergy skin testing due to possible antihistaminic effects. Objective: To examine the antihistaminic effect of AD, AP, and BD as measured by the ability of these drugs to suppress the normal wheal reaction caused by skin prick test (SPT). Methods: Skin prick test was performed in patients receiving treatment with AD, AP, and/or BD. Double SPT was performed with histamine solutions of 10, 30, and 100 mg/ml and mean wheal diameter calculated. Results: A total of 313 patients were included. 236 (75%) patients were treated with one of the examined drugs and 77 (25%) patients with more than one of these drugs. Drugs most frequently used was sertraline (n = 65), citalopram (n = 63), mirtazapine (n = 36), venlafaxine (n = 33), and quetiapine (n = 32). Treatment with mirtazapine and/or quetiapine was associated with negative SPTs in 30/36 (83%) and 22/32 (69%), and the antihistaminic effect of these drugs was dose-dependent. For patients treated with selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (TCAs), serotonin norepinephrine reuptake inhibitors (SNRIs), or BD alone, almost all SPTs were positive (94%, 95%, 100%, and 100%, respectively). Negative SPTs in patients treated with SSRI, TCA, SNRI, or BD and ≥1 other of the examined drugs were associated with simultaneous treatment with mirtazapine or quetiapine in 39/44 (89%) patients. Conclusion: Skin testing has little meaning in patients treated with mirtazapine or quetiapine. Treatment with SSRI, SNRI, and BD does not seem to affect the results of SPTs, whereas skin tests in patients treated with TCA should be interpreted with caution. [ABSTRACT FROM AUTHOR]

2-piperidone is a six membered heterocyclic compound existing naturally in piperaceae and portulaceae families. The synthetic derivatives of piperidone are promising bioactive molecules. They are antioxidant and antiinflammatory agents. Antihistaminic and anticholinergic studies are used as a part of antiasthmatic study. In the current study antihistaminic and anticholinergic studies were carried out using guinea pig bronchi and ilei in naturally isolated compound 2-piperidone from the plant Talinum portulacifolium. The results indicate that the compound (2 mg/kg 10.81 ± 1.29*** at p<0.001) showed profound antihistaminic activity significantly in histamine induced bronchospasm model than standard drug chlorpheniramine (2 mg/kg 8.77±0.43** at ** p<0.01). The compound can be further studied for antiasthmatic activity by various other ways to establish its mechanism of action as well as drug development studies to render it a novel antiasthmatic drug. [ABSTRACT FROM AUTHOR]

Nowadays, measurement uncertainty is considered an essential parameter for method evaluation. Measurement uncertainty estimation requires a detailed study of all possible sources of uncertainty. The aim of this work was to develop and validate an isocratic reversed-phase high-performance liquid chromatographic method for the simultaneous separation and determination of five antihistamines in pharmaceutical formulations and to establish a procedure to evaluate the measurement uncertainty of values generated by the validated method. A relatively short chromatographic separation time, less than 9 min, was achieved by means of a Waters XBridge C18 (4.6 mm×250 mm, 5 µm) analytical column under isocratic conditions using a mobile phase consisting of sodium perchlorate buffer (pH 3.5; 0.1 mol L−1)–acetonitrile (55:45, v/v) at a flow rate of 1 mL min−1 and UV detection at 235 nm. The selectivity, method linearity, accuracy, precision, limits of detection (LOD) and limits of quantification were examined as parts of the method validation. The described method shows excellent linearity over a range of 30 μg mL−1 to 70 μg mL−1 for all compounds with correlation coefficients higher than 0.995. The standard deviations of the intraday and inter-day precision were all less than 2 %. The LOD of all studied compounds ranged from 0.029 μg mL−1 to 0.03 µg mL−1. Using EURACHEM/CITAC guide and Valid Analytical Measurement (LGC/VAM) protocol, measurement uncertainty associated with precision and standard preparation were the most important contributing for the five antihistamines, accounting for 87.72 % to 91.03 % and 4.05 % to 10.24 % of total uncertainty, respectively, and overall uncertainties obtained were from 0.05 mg to 0.58 mg. Therefore, the proposed method was suitable for the routine analysis of antihistamines in pharmaceuticals formulations with the required accuracy, precision and measurement uncertainty. [ABSTRACT FROM AUTHOR]

Objective: The main objective of this research is to develop an immediate release Rupatadine fumarate 10 mg tablets formulation by direct compression, through a Quality by Design approach in Costa Rica. Methods: According to a Quality by Design approach; Target Product Profile, Quality Target Product Profile, and the Critical Quality Attributes were defined. In the preformulation study, compatibility tests were carried out between the raw materials. The Critical Material Attributes were established using Quality Risk Management. Three formulation prototypes were prepared by direct compression and its Critical Process Parameters were defined. The analysis of the prototypes was realized in terms of organoleptic properties, identification, potency, content uniformity, dissolution, disintegration, friability and loss by drying. Results: All the prototypes showed a white or slightly pink surface, potency between 90.0 –110.0 % of the labeling, an acceptance value for the content uniformity lower than the specification (AV < 15), the dissolved amount of active pharmaceutical ingredient was greater than 85.0 % at 30 minutes, friability less than 1.0 %, a disintegration time less than 15 minutes and moisture content less than 2.0 %. Conclusions: The approaching of a Quality by Design model to the current development allowed to obtain satisfactory results in the three formulation prototypes. The excipients to be used can be lactose monohydrate, microcrystalline cellulose, sodium croscarmellose, pregelatinized starch, magnesium stearate, stearic acid, and PVP K-30. [ABSTRACT FROM AUTHOR]

• The multi-targeted 4-quinolone hybrids are designed, synthesized and characterized for the treatment of allergic asthma. • Asthma-associated antihistaminic activity, COX-2, LOX and PED-4 inhibitory activity have been performed to identify the potentiators. • In-silico physicochemical and pharmacokinetic parameters are analysed by Pass software and oral toxicity has been performed according to OECD-420 guidelines (in-vivo). • A 4-quinolone hybrid is found to be pharmacologically more effective and safer than standard (Azelastine hydrochloride). The multi-targeted hybrids can promise tools to fight against multifaceted diseases like allergic asthma by blocking the various mediators which are associated with allergic asthma. Therefore, the multi-targeted therapeutic hybrids have been designed from the combination of two bioactive pharmacophores like quinolone and piperazines. These hybrids have been synthesized and characterized by sophisticated spectroscopic techniques (1HNMR and 13CNMR). Histamine is a more prominent mediator for the progression of allergic asthma. Therefore, all 40 hybrids were screened for their H 1 -antihistaminic activity (in vitro) by histamine-induced contraction in the GPI model. The most active compounds 26c, 28a and 30c were elected for bronchodilatory activity. The two compounds 26c and 28a were found to be more active with 48.72% and 42.62% with significant bronchoprotection (in-vivo) against histamine contraction respectively. Other targets have been predicted for the best compounds by in silico target prediction study using pass online tool. Pass predicted different targets among them. We have selected major associated targets of allergic asthma. Best compounds have been evaluated against other selective targets like prostaglandin-endoperoxide synthase-2 (COX-2), lipoxygenases (LOX) and phosphodiesterase-4 (PDE-4). Both compounds (26c and 28a) manifested good COX-2, LOX and PED-4 inhibitory activities. In silico predictions of pharmacokinetic and oral toxicity parameters were also implemented for the best compounds. In addition to the above, single acute toxicity study for the best compound (26c) has been accomplished at the dose of 300 mg/kgbw to the identification of the Off-target adverse effects. No signs of toxicity and mortality were exhibited during the experiment as per guidelines OCED-420. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract: Antivenoms or antitoxins have been effectively used for more than a century. During this time, these products have always proven to be highly effective in the treatment of infections and envenomations. However, antivenoms did not exhibit good safety results in their initial applications. After many improvements, antivenoms have substantially better safety profiles but still have some side effects. Due to the occurrence of adverse reactions, the practice of using premedication with the intent to decrease side effects has become accepted or mandatory in many countries. The drugs used for premedication belong to the histamine H1 antagonist, glucocorticoid and catecholamine groups. Currently, this practice is being questioned due to low or controversial efficacies in clinical assays. In this article, we discuss the causes of adverse reactions, the mechanisms of drugs that block the undesired effects and the results obtained in clinical trials. Although these three families of drugs could have positive effects on reducing adverse reactions, only adrenaline has demonstrated positive results in clinical assays.

Urticaria is a common skin disease that is characterized by itchy and edematous plaques that appear suddenly and disappear spontaneously within the same day. About half of all cases of urticaria in children are attributed to infections, and they usually do not require routine diagnostic tests. An eight-year-old girl who presented with acute urticaria had signs of respiratory tract infection, and urticaria did not respond to antihistamines. A subsequent test revealed a Mycoplasma pneumoniae infection, which was treated with azithromycin. In patients presenting with acute urticaria together with signs of respiratory tract infection, the possibility of Mycoplasma infection should be considered in the differential diagnosis, especially if urticaria does not respond to antihistamine therapy [ABSTRACT FROM AUTHOR]

Objective: This study assessed and compared in vivo anti-inflammatory activity of Hippophae rhamnoides (HR) and Hippophae salicifolia (HS) seed oil. Materials and Methods: HR and HS seed oil was extracted by Soxhlet apparatus and characterized using gas chromatography mass spectroscopy. Wistar rats were used for predicting anti-inflammatory activity. Results: HR and HS (2 and 4 ml/kg, respectively) exhibited dose-dependent inhibition of carrageenan-, histamine-, prostaglandin-, bradykinin-, and arachidonic acid (AA)-induced paw edema. Significant leukotriene-induced inhibition was observed in HR. Myeloperoxidase (MPO) and lipid-peroxidase (LPO) assays were performed and HR and HS seed oil significantly decreased the level of MPO and LPO at 4 ml/kg dose (P < 0.001). Conclusion: Dual inhibition of AA metabolism in HR and cyclooxygenase inhibition in HS was observed that might be attributed to the presence of polyunsaturated fatty acids (PUFAs), specifically, a correct balance of n-3 and n-6 PUFAs. However, the findings should be interpreted in the light of limitation of this study. Detailed experimentation at enzymatic levels would further help in substantiating the results inferred in this study. Abbreviations Used: AA: Arachidonic acid, ALA: Alpha linolenic acid, COX: Cyclooxygenase, EPA: Eicosapentaenoic acid, GCMS: Gas chromatography-mass spectroscopy, HR: Hippophae rhamnoides, HS: Hippophae salicifolia, ip: Intraperitoneal, LOX: Lipoxygenase, LPO: Lipid peroxidase, LTB4: Leukotriene B4, LTs: Leukotrienes, MPO: Myeloperoxidase, PGE2: Prostaglandin E2, PGs: Prostaglandins, PUFA: Poly unsaturated fatty acid, SBT: Seabuckthorn [ABSTRACT FROM AUTHOR]

Objective: This study was conducted to investigate nasal nitric oxide (nNO) and its metabolites nasal nitrite-nitrate (nNOx) in patients with allergic rhinitis (AR), the effects of two different drugs (oral antihistamine and intranasal steroid) on nNOx and the presence of a correlation between nNOx and clinical parameters. Methods: Sixty patients with active symptoms of perennial AR and 25 healthy adults as a control group were enrolled. The patients were randomized into two groups. Half of the patients received fexofenadine 1x120 mg/day orally, and the other half received triamcinolone acetonide 1 x2 puff/day intranasally for one month. The amount of nNOx in nasal lavage fluid was measured by using a commercially available kit and the photometric endpoint determination method. Results: Pre-treatment levels of NOx in the nasal lavage fluids (1.92± 1.20 mg/l) of patients with AR were found to be significantly higher when compared with nasal lavage fluid NOx levels of healthy adults (1.38±0.78 mg/l) (p=0.04). The post-treatment nNOx level (1.52±0.85 mg/l) was significantly lower when compared with the pre-treatment value (p=0.028). Conclusion: Nasal nitric oxide metabolites were shown to be good biomarkers for AR, and that oral fexofenadine significantly decreased nNOx levels. [ABSTRACT FROM AUTHOR]

Résumé L’anaphylaxie est une urgence allergique dont la fréquence augmente constamment. Son management repose sur l’administration d’adrénaline et la coordination entre urgentistes et allergologues. L’objectif de l’étude était de déterminer l’incidence de l’anaphylaxie en 2015, d’en décrire les principales caractéristiques et d’évaluer les pratiques. Quatre centres hospitaliers lorrains ont été sélectionnés. Les dossiers médicaux informatiques des patients admis aux urgences adultes ou pédiatriques entre le 1 er janvier et le 31 décembre 2015 ont été interrogés sur leurs motifs de recours et code diagnostique. Les dossiers dont le codage était susceptible de correspondre à une réaction anaphylactique (95 codes sélectionnés) étaient revus individuellement par un investigateur allergologue, puis inclus en cas de confirmation. Un questionnaire standardisé a permis le recueil des données épidémiologiques, caractéristiques cliniques et prise en charge des patients. L’anaphylaxie représente 0,16 % des passages aux urgences pour 2015, avec une incidence de 34 pour 100 000 personnes-année en Lorraine. La présentation clinique est influencée significativement par l’âge, le facteur étiologique, certains cofacteurs (asthme, comorbidité cardiovasculaire, médications), et la gravité de la réaction. En cas d’anaphylaxie sévère, le recours à l’adrénaline n’était que de 32,4 % (48/148), et 4 fois sur 10 la durée de surveillance hospitalière était inférieure à 6 heures. Une orientation vers l’allergologue était proposée chez 57,9 % (187/323) des patients. L’anaphylaxie est une cause non exceptionnelle d’admission aux urgences. Les recommandations sont encore trop peu appliquées, et une meilleure connaissance de la pathologie et de sa prise en charge est nécessaire pour les professionnels gérant l’urgence. Anaphylaxis is an allergic emergency, and its frequency increases in all countries since the 2000s. Epinephrine administration and allergist-emergency room interactions are the key points of its management. The objective of the study was to determine the incidence of anaphylaxis in 2015, to describe its main characteristics and to evaluate practices in Lorraine for this period. Four hospitals in Lorraine were selected. Medical records from each center's adult and pediatric emergency rooms, from 1st January to 31th December 2015, were classified based on their admission cause and diagnosis code. When data were consistent for an anaphylaxis (95 selected ICD-10 codes) record was analyzed by an allergist practitioner and included if confirmed. Epidemiological data, clinical characteristics, management assessment and orientation were provided through a standardized questionnaire. Anaphylaxis is responsible for 0.16% emergency rooms’ admissions in the participating centers in 2015; the estimated incidence in Lorraine is 34 per 100,000 person-years. Clinical presentation depends on age, etiologic agent, several cofactors (asthma, cardiovascular comorbidities, treatments) and reaction's gravity. When anaphylaxis was serious (Ring-Messmer's grade ≥ 3), epinephrine use was only 32.4% (48/148) and observation duration was less than 6 hours 4 times on 10. An allergist referral was proposed in 57.9% (187/323) patients. Anaphylaxis is not a rare cause for emergency rooms’ admission in Lorraine. Therefore guidelines are insufficiently followed and a better knowledge of the pathology and its management is necessary for emergency healthcare practitioners. [ABSTRACT FROM AUTHOR]

The present work deals with the pharmacological screening of some newly synthesized triazoles. A series of 1,2,4-triazoles have been synthesized using benzoic acid or 4-chloro benzoic acid as the starting materials. The synthesized compounds were characterized by physical and spectral analysis viz., Fourier transform infrared spectroscopy, H nuclear magnetic resonance, C nuclear magnetic resonance, Gas Chromatography-Mass Spectrometry and elemental analysis Carbon, Hydrogen and Nitrogen analysis in order to confirm the structure. Acute toxicity studies were carried out in accordance with the Organization for Economic Co-operation and Development guideline 425. The compounds were not found to be lethal even at a dose level of 2000 mg/kg. Pharmacological evaluation was done following three intact animal experiments and one experiment on the isolated tissue. Results of the study indicated that the compound 7bi and 7bj protected up to 60% against histamine-induced dyspnea. Antihistaminic nature of the test compounds 7bi, 7bj, 7ai, and 7bk were also confirmed by the loss of catalepsy after the administration of clonidine (1%, s.c.). During experiments on isolated tissue, suppression of dose-response curve of histamine indicates a noteworthy denouement in favor of the said effect. [ABSTRACT FROM AUTHOR]

Background: The use of anti-histaminic agents has been increased significantly from last decades and till now no method is available for quantitation of ALZ in human plasma which can be applied in a bioequivalence study using LC-MS/MS. Objective: The present study is concerned with the development and validation of ALZ in human plasma by high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS). Materials and Methods: Sample preparation involved the extraction with liquid-liquid extraction method by using ethyl acetate as an organic solvent. Chromatographic separation was performed on Atlantis; T3 5 ΅m 4.6 mm Χ 150 mm column with the mobile phase consisting of acetonitrile: (10 mm ammonium formate buffer: Formic acid: 99.9:00.1 v/v) 50:50 v/v. The interface used with the application programming interface 4000 LC-MS/MS was a turbo ion spray in which positive ions were measured in multiple reaction monitoring mode. The precursor to product ions transition of m/z 299.30 → 100.20 amu and 305.30 → 106.30 amu were used for ALZ and ALZ D6 respectively. Results: The method was validated over the concentration range of 20.013-10006.551 pg/mL. The mean percent recovery of ALZ was found 77.771% with a precision of 7.71% and the lower limit of quantification was 20.013 pg/mL. The intra- and inter-day precision of the method at three concentrations was 0.98-4.50% and 1.57-5.72% while the intra- and inter-day % accuracy was 99.02-93.82% and 101.78-106.96%. Stability of compounds was established in a series of stability studies. The application of this method was demonstrated in the bioequivalence study and was found suitable in a study of sample size as big as 30 enrolled volunteers. Conclusion: For the very first time, a sensitive, selective and robust Liquid Chromatography- Mass Spectrometry method for the determination of alimemazine (ALZ) in human plasma has been developed and validated using ALZ D6 as an internal standard.

Allergy and infections are the most common causes of rhinosinusitis both in adults and children. Guidelines for the diagnosis and management of these diseases are systematically developed by panels of world-class experts and published in the form of consensuses like ARIA (Allergic Rhinitis and its Impact on Asthma) or EPOS (European Position Paper on Rhinosinusits and Nasal Polyps). Even though symptoms of rhinitis are the same regardless of etiology (nasal congestion and rhinorrhea), a number of concomitant characteristics (e.g. seasonal nature of symptoms in case of seasonal allergic rhinitis, chronic nature of symptoms, headache, purulent secretion in case of chronic bacterial rhinosinusits) sets the diagnosis on the right course. The paper describes groups of medications used in treatment of allergic and non-allergic rhinitis, presents data on their effectiveness and discusses treatment strategies developed by the authors in ARIA and EPOS. In allergic rhinitis particular attention is paid to antihistamines and nasal glucocorticosteroids. In non-allergic rhinitis recommendations for nasal glucocorticosteroid treatment and the indications for antibiotic treatment are highlighted. Other medicinal products which could prove effectiveness in treatment of rhinosinusitis are presented. [ABSTRACT FROM AUTHOR]

Asthma is a common disease that is rising in prevalence worldwide with the highest prevalence in industrialized countries. Asthma affects about 300 million people worldwide and it has been estimated that a further 100 million will be affected by 2025. Ayurveda, Siddha, Unani and Folk (Tribal) medicines are the major systems of indigenous medicines. Over three-quarters of the world population relies mainly on plants and plant extracts for health care. Unlike many diseases, which can be attributed to the life style of modern man, asthma is an ancient illness. There are number of medicinal plants have been reported for antihistaminic/anti-asthmatic activities like Achyranthes aspera, Tephrosia purpurea, Dolichos lablab, Eclipta alba, Jasminum sambac, Balanites aegyptiaca, Viscum album, Tridex procumbens, Glycyrrhiza glabra and Cassia fistula. Present review is focused on used of medicinal plants for treatment of asthama. It is suggested that formulation and patent of the reported medicinal plants is mandatory for further use against asthma and if possible, clinical trials should be done of these plants for their appropriate use. [ABSTRACT FROM AUTHOR]

Cinnarizine is a piperazine derivative with antihistaminic, antiserotonergic, antidopaminergic, and calcium channel-blocking activities. A comprehensive profile was performed on cinnarizine including its description and the different methods of analysis. The 1H NMR and 13C one- and two-dimensional NMR methods were used. In addition, infrared and mass spectral analyses were performed which all confirmed the structure of cinnarizine [ABSTRACT FROM AUTHOR]

A series of new 10-(alkylamino)-8-methyl-2,6-dihydroimidazo[1,2-c]pyrimido[5,4-e]pyrimidine-5(3H)-thiones (4a-g) were subjected to molecular property prediction (drug-likeness, lipophilicity and solubility parameters) using Osiris Property Explorer, ALOGPS 2.1, Molinspiration and ACD/Chemsketch 12.0 software programmes. The calculated drug-related properties of the designed molecules were similar to those found in most marketed drugs. Amongst the proposed analogues, four promising candidates were chosen (4a-d) for synthesis on the basis of Lipinski's 'Rule of Five' and drug-likeness scores. The significant biological activity of the test compounds in two in vitro modes (isolated guinea pig tracheal chain preparation, isolated guinea pig ileum) supports the promise and accuracy of the prediction. Among them, 4a was the most potent antihistaminic (IC50 value of 30.2 µM; standard, chlorpheniramine maleate showed an IC50 of 14.1 µM). [ABSTRACT FROM AUTHOR]

Background: Levocetirizine, an active enantiomer of cetirizine is third generation antihistaminic agent used for treating various allergies like atopic dermatitis, chronic idiopathic urticaria and allergic rhinitis. Objective: Development of novel topical formulation of levocetirizine based on flexible vesicles (FVs) with an aim to have targeted peripheral antihistaminic effect. Materials and methods: The FVs were prepared by thin film hydration method and characterized for drug content, entrapment efficiency, pH, vesicular size, spreadability, morphological characteristics and drug leakage studies. Franz diffusion cell assembly was used to carry out the ex vivo permeation studies through mice skin and the permeation profile of the developed FV formulation was compared with conventional formulations of levocetirizine. Results and discussion: The ex vivo permeation studies revealed 1.78-fold increase in percent permeation of levocetirizine from FV formulation as compared to conventional formulations of levocetirizine in 8 h. Further, oxazolone induced atopic dermatitis murine model was selected to study the in vivo pharmacodynamic activity. The developed formulation was evaluated for scratching score, erythema score and histological evaluation. There was marked reduction in scratching score from 15.25 scratches/20 min with conventional levocetirizine cream to 6.75 scratches/20 min with application of levocetirizine FV formulation. Also, there was significant reduction in erythema score as well as dermal eosinophil count. Results of skin sensitivity and toxicity studies suggest that the developed formulation was dermally safe and nontoxic. Conclusion: A novel FVs based topical formulation of levocetirizine was successfully developed for treatment of atopic dermatitis. [ABSTRACT FROM AUTHOR]

We have planned to demonstrate histopathologic effects of mid- or long-term oral use of desloratadine and cetirizine HCl molecules on middle ear mucosa of rats. Thirty-six rats were randomized equally into six groups. Desloratadine groups received once daily doses of 1 mg/ml desloratadine for 30 (D30 Group) or 60 (D60 Group) days. The Cetirizine study groups were given once daily doses of 1 mg/ml cetirizine for 30 (S30 Group) or 60 (S60 Group) days. Control groups were given 2 cc physiologic saline using orogastric gavage method through a 12 G gavage catheter for 30 (K30 Group) or 60 (K60) days. At the end of 30 days, D30, S30 and K30 Groups were sacrificed. Tissue samples harvested from groups were evaluated between 1 and 4 Grades for histological characteristics of middle ear canal, eardrum, middle ear epithelium and connective tissue, edema, vascular congestion and inflammatory cells. In the control group no pathological finding was encountered in rats sacrificed on 30 and 60 days. No statistical difference was observed when groups were compared on external ear epithelial tissue, external ear sebaceous gland, middle ear inflammation, and middle ear capillary dilatation both on 30 and 60 days. Tympanic membrane collagen was more evident in D30 and D60 groups when compared with C30 and C60 groups. Comparison of histopathological grading results between 30 and 60 days revealed no significant changes. In conclusion, oral intake of cetirizine and desloratadine preparations has effects of tympanic membrane collagen, degrees of edema and vascular congestion being more prominent with desloratadine molecule. [ABSTRACT FROM AUTHOR]

Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes. [ABSTRACT FROM AUTHOR]

Background: The global prevalence of allergic rhinitis is high. International Study of Asthma and Allergies in Childhood (ISAAC) Phase III reports a total estimated prevalence of 4.6% in Mexico. There is evidence based on allergic rhinitis Clinical Practice Guidelines (CPG), but its promotion, acceptance and application is not optimal or adequate in Mexico. Objective: To generate a guideline for the treatment of allergic rhinitis and its impact on asthma by adaptating the 2010 ARIA Guideline to Mexican reality, through a transculturation process applying the ADAPTE methodology. Material and method: Using the ADAPTE Methodology, the original 2010 ARIA CPG recommendations were evaluated by the guideline development group (GDG) into which multiple medical specialities managing patients with allergic rhinitis were incoorporated. The GDG valorated the quality of 2010 ARIA, checked and translated key clinical questions. Moreover, the GDG adjusted recommendations, patient preferences and included comments in the context of the Mexican reality (safety, costs and cultural issues). To accomplish this, we ran Delphi panels with as many rounds as necessary to reach agreement. One extra question, not included in the original 2010 ARIA, on the use of Nasal Lavages for AR was created sustained by a systematic literature review. Results: A total of 45 questions from the original 2010 ARIA were included and divided into six groups covering prevention, medical treatment, immunotherapy and alternative medicine to treat patients with allergic rhinitis with or without asthma. Most of the questions reached agreement in one or two rounds; one question required three rounds. Conclusions: An easy-to-use, adaptated, up-to-date and applicable allergic rhinitis guideline for Mexico is now available. [ABSTRACT FROM AUTHOR]

Background: The use of anti-histaminic agents has been increased significantly from last decades and till now no method is available for quantitation of ALZ in human plasma which can be applied in a bioequivalence study using LC-MS/MS. Objective: The present study is concerned with the development and validation of ALZ in human plasma by high performance liquid chromatography tandem mass spectrometry (HPLC-MS/ MS). Materials and Methods: Sample preparation involved the extraction with liquid-liquid extraction method by using ethyl acetate as an organic solvent. Chromatographic separation was performed on Atlantis® T3 5 μm 4.6 mm × 150 mm column with the mobile phase consisting of acetonitrile: (10 mm ammonium formate buffer: Formic acid: 99.9:00.1 v/v) 50:50 v/v. The interface used with the application programming interface 4000 LC-MS/MS was a turbo ion spray in which positive ions were measured in multiple reaction monitoring mode. The precursor to product ions transition of m/z 299.30 → 100.20 amu and 305.30 → 106.30 amu were used for ALZ and ALZ D6 respectively. Results: The method was validated over the concentration range of 20.013-10006.551 pg/mL. The mean percent recovery of ALZ was found 77.771% with a precision of 7.71% and the lower limit of quantification was 20.013 pg/mL. The intra- and inter-day precision of the method at three concentrations was 0.98-4.50% and 1.57-5.72% while the intra- and inter-day % accuracy was 99.02-93.82% and 101.78-106.96%. Stability of compounds was established in a series of stability studies. The application of this method was demonstrated in the bioequivalence study and was found suitable in a study of sample size as big as 30 enrolled volunteers. Conclusion: For the very first time, a sensitive, selective and robust Liquid Chromatography- Mass Spectrometry method for the determination of alimemazine (ALZ) in human plasma has been developed and validated using ALZ D6 as an internal standard. [ABSTRACT FROM AUTHOR]

This work reviews the neuropharmacology of the vestibular system, with an emphasis on the mechanism of action of drugs used in the treatment of vestibular disorders. Clinicians are confronted with a rapidly changing field in which advances in the knowledge of ionic channel function and synaptic transmission mechanisms have led to the development of new scientific models for the understanding of vestibular dysfunction and its management. In particular, there have been recent advances in our knowledge of the fundamental mechanisms of vestibular system function and of drug action. In this work, drugs acting on vestibular system have been grouped into two main categories according to their primary mechanisms of action: those with effects on neurotransmitters and neuromodulators dynamics and those that act on voltage-gated ion channels. Particular attention is given in this review to drugs that may provide additional insight into the pathophysiology of vestibular diseases. The critical analysis of the literature reveals that there is a significant lack of information defining the real utility of diverse drugs used in clinical practice. The development of basic studies addressing drug actions at the molecular, cellular and systems level, combined with reliable and well controlled clinical trials, would provide the scientific basis for new strategies for the treatment of vestibular disorders. [ABSTRACT FROM AUTHOR]

Abrus precatorius Linn (Fabaceae) is a climbing shrub; leaves are pinnate with many pairs of leaflets. Leaves 5-10 cm long, leaflets 10-20 pairs, opposite, flowers are pink clustered. The roots, stems, and leaves contain glycyrrhizin, sweet in taste. Leaves are traditionally have been used in the treatment of fever, asthma and caries of teeth. Clonidine induces catalepsy by releasing histamine from mast cells which is responsible for different asthmatic conditions. The leaves of A. precatorius traditionally used for asthma, hence objective of present study was to evaluate antihistaminic activity of A. precatorius using clonidine induced catalepsy in mice. In present study ethanol extract of A. precatorius leaves (EAPL) at doses 100, 125, 150 mg/kg i.p were evaluated for antihistaminic activity using clonidine and haloperidol induced catalepsy in mice. Finding of investigation showed that chlorpheniramine maleate (CPM) and EAPL inhibit clonidine induced catalepsy significantly P < 0.001 when compare to control group, while CPM fail to inhibit haloperidol induced catalepsy. Present study concludes that EAPL possesses antihistaminic activity. [ABSTRACT FROM AUTHOR]

The steroids 3,6,17-trihydroxy-stigmasta-4,7,24(28)-triene (A) and 14,15,18,20-diepoxyturbinarin (B) were isolated from the cyclohexane extract of brown alga, Turbinaria conoides (J. Agardh) Kutzing, and have been reported for their antimicrobial activity by us. In this study, the isolated compounds were evaluated for comprehensive antihistaminic, antiviral and cytotoxicity screening. The antihistaminic study was performed using in vitro standard animal models. Evaluation of the potency (EC50), affinity (pA2) and the maximal response (Emax) of the histamine alone and in the presence of the compounds were determined. Antiviral activity and cytotoxicity were performed in Crandell-Rees feline kidney (CRFK) cells by a colorimetric formazan-based MTS assay. No significant antiviral activity or cytotoxicity were observed for the compounds in the CRFK cells. Compound A inhibited the histamine-induced concentration at 20 µg mL-1(p < 0.05). The most significant inhibition (97%) was observed for compound B (p < 0.01) at the same concentration, which was comparable to that of the positive control chlorpheniramine maleate (10 µg mL-1). This potentiality suggests that 14,15,18,20-diepoxyturbinarin (B) can be developed as a new lead antihistaminic agent. [ABSTRACT FROM AUTHOR]

The aim of the study was to evaluate the antiulcer activity of Linum usitatissimum fixed oil against aspirin-, indomethacin-, ethanol-, reserpine-, serotonin- and stress-induced gastric ulceration in rats and histamine-induced gastric ulceration in guinea pigs. Attempts were also made to evaluate the in vitro anticholinergic and antihistaminic activity and in vivo antisecretary and antiulcer activity of oil following pylorus ligation in rats. L. usitatissimum fixed oil exhibited significant antiulcer activity against different ulcerogens in experimental animal models. The fixed oil significantly inhibited acetylcholine- and histamine-induced contraction of guinea pig and rat ileums, respectively, suggesting its anticholinergic and antihistaminic activity. The oil also exhibited significant inhibitory effect on gastric secretion/total acidity and aspirin-induced gastric ulceration in pylorus-ligated rats. The lipoxygenase inhibitory, histamine antagonistic and antisecretory (anticholinergic) effects of the oil could probably have contributed towards antiulcer activity. L. usitatissimum fixed oil may be considered to be a drug of natural origin which possesses significant antiulcer activity. The present observation is the first experimental data showing antiulcer activity of L. usitatissimum fixed oil. [ABSTRACT FROM AUTHOR]

Punica granatum Linn. (Punicaceae) flower buds are used in the treatment of asthma traditionally, so the present work was undertaken to prove it scientifically using suitable animal models. Antihistaminic principles are useful in the treatment of asthma,;hence, in present work antihistaminic activity of various extracts of P. granatum flower buds was checked using clonidine-induced catalepsy and haloperidol-induced catalepsy in Swiss albino mice at the dose of 50 and 100 mg/kg, p.o. The results showed that ethanol extracts (100 mg/kg, p.o.) are having significant antihistaminic activity amongst other extracts. Thus, it can be concluded that tannins from the flower buds of P. granatum may be responsible for antihistaminic activity and may have potential role in the treatment of asthma. [ABSTRACT FROM AUTHOR]

This study investigated the effect of an aqueous extract of Tinospora cordifolia (Willd.) Miers (Menispermaceae) stem on mast cell mediated allergic reactions in vivo and in vitro and studied its possible mechanism. T. cordifolia (125 to 1000 mg/kg) dose-dependently inhibited compound 48/80 induced lethality in rats, histamine induced paw edema in mice and histamine induced bronchial asthma in guinea pigs. T. cordifolia significantly (p < 0.001) inhibited the cutaneous anaphylaxis reaction activated by histamine in a rat model and compound 48/80 induced ear swelling response in mice. T. cordifolia (2.5-160 μg/mL) also showed significant (p < 0.001) inhibition of histamine induced contraction of guinea-pig ileum in vitro implying the H1 antihistamine activity. T. cordifolia (0.01 to 10 mg/mL) significantly (p < 0.001) inhibited the histamine release from rat peritoneal mast cells activated by compound 48/80. In addition, T. cordifolia (0.01 to 10 mg/mL) significantly (p < 0.001) inhibited the secretion of tumor necrosis factor-α (TNF-α) in antidinitrophenyl (DNP) IgE-stimulated rat peritoneal mast cells. The level of cAMP in RPMC transiently and significantly increased compared with that of control cells when T. cordifolia was incubated with mast cells. T. cordifolia (0.01 to 10 mg/mL) showed concentration-dependent inhibition in compound 48/80 induced reactive oxygen species (ROS) generation. In addition, T. cordifolia decreased intracellular calcium levels of activated mast cells. These results show that T. cordifolia may be beneficial in the treatment of acute and chronic allergic disorders. [ABSTRACT FROM AUTHOR]

Barbiturates represent an important group of central nervous system depressant drugs derived from barbituric acid by replacement of the hydrogen atoms on C5 by alkyl or aryl groups or by substitution of S for O on C2. They are administered orally as sedatives or intravenously as anaesthetics. Some are also effective in treating epilepsy. Barbiturates induce a repose analoguos with narcosis (remove dreaming/ paradoxa; repose phases). They represent a sedative and hypnotic medicine group with the largest utilisation among this type of classic medicine. [ABSTRACT FROM AUTHOR]

The aim of this study was to assess the possible protective effects of Nigella sativa (NS) and its constituent, thymoquinone (TQ) on ethanol-induced gastric mucosal damage in an experimental model. Forty male rats aged four months were divided into four groups (each group containing ten animals); the control group received physiologic saline (10 ml kg−1) and the ethanol group had taken 1 ml (per rat) absolute alcohol by gavage. The third and fourth groups also received NS (500 mg kg−1) and TQ (10 mg kg−1) by gavage 1 h before alcohol administration, respectively. Both drugs (NS and TQ) could protect the gastric mucosa against the injurious effect of absolute alcohol and promote ulcer healing as evidenced from the ulcer index values. Gastric damage was confirmed histomorphometrically by significant increases in the number of mast cells (MC) and gastric erosions in ethanol treated rats. The NS treatment significantly decreased the number of MC and reduced the area of gastric erosions. Likewise, TQ treatment was also able to reduce the number of MC and the gravity of gastric mucosal lesions, but to lesser extent compared to NS. Gastric tissue histamine levels and myeloperoxidase activities were found to be increased in ethanol treated rats, and NS or TQ treatment reversed these increases. Results obtained from this study suggest that both drugs, particularly NS could partly protect gastric mucosa from acute alcohol-induced mucosal injury, and these gastroprotective effects could be due to their antiperoxidative, antioxidant and antihistaminic effects. [ABSTRACT FROM AUTHOR]

Summary: The antipsychotic drug prochlorperazine was screened in vitro for possible antimicrobial property against 157 strains of bacteria, belonging to Gram positive and Gram negative genera. The minimum inhibitory concentration (MIC) of prochlorperazine was determined by agar dilution method, which ranged from 25 to 200μg/ml with respect to most of the strains. Based on such findings, a further study was undertaken to determine whether the efficacy of this drug could be enhanced in the presence of an antihistaminic agent methdilazine, reported to have remarkable antimicrobial action. Four bacterial strains, sensitive to prochlorperazine as well as to three antibacterial chemotherapeutics, viz., methdilazine, fluphenazine and thioridazine were chosen. Disc diffusion tests with prochlorperazine and methdilazine revealed marked synergism between the combination, compared to their individual effects. The synergism was found to be statistically significant (p&#60;0.01). To assess the degree of synergism, the checkerboard analysis was performed. The FIC index of this combination turned out to be 0.37, which confirmed synergism. Therefore, this synergistic drug combination might open a new therapeutic approach to combat drug-resistance in bacterial infections. [Copyright &y& Elsevier]

Objective: This study was undertaken to test that uterine mast cell degranulation alters human myometrial contractility in vitro and to define what mediators are involved in this process. Study design: Longitudinal myometrial strips prepared from biopsy specimen obtained from the lower uterine segment of women at preterm and term gestation (with and without labor) were studied. Contractile responses to compound 48/80, a mast cell degranulator, were compared in the absence or presence of a mast cell stabilizer, H1 and H2 receptor antagonists, cyclooxygenase, and lipoxygenase inhibitors. Results: Compound 48/80 increased myometrial contractility in all groups. The mast cell stabilizer cromolyn inhibited contractility, whereas the cyclooxygenase inhibitor ibuprofen, the H1-receptor antagonist S(+)-chlorpheniramine maleate, but not the H2 antagonist cimetidine, only slightly attenuated this effect. The lipoxygenase inhibitor linoleyl hydroxamic acid augmented the responses to compound 48/80 in the preterm but not in the term group. Conclusion: Uterine mast cell degranulation, or the effects of their mediators, can modulate uterine contractility during pregnancy. [ABSTRACT FROM AUTHOR]

The aim of present research was to develop a fast releasing oral polymeric film, with good mechanical properties, instant disintegration and dissolution, producing an acceptable taste when placed on tongue. Solvent casting method was used to prepare oral films. Levocetirizine dihydrochloride, an antihistaminic was incorporated to relieve the symptoms of allergic rhinitis. The polymers selected were HPMC E 15 and PVA. Propylene glycol was the plasticizers used. Nine batches of films with drug were prepared using different combinations of polymers and plasticizer concentration. The resultant films were evaluated for weight variation, content uniformity, folding endurance, thickness, surface pH, in vitro disintegration and in vitro dissolution. The optimized films which disintegrated in less than 30 sec, releasing 85-98% of drug within 2 minutes. The percentage release was varying with concentration of plasticizer and polymer. The films made with HPMC: PVA (1:2) released 96% of drug in 1 min, which was the best release amongst all.

This study was designed to evaluate antihistaminic and anticholinergic activities of Murraya koenigii leaves. To observe the activities ethanolic (Mk.Eth) and aqueous (Mk.Aq) extracts of M. koenigii through in vitro analysis, isolated guinea pig ileum, rabbit trachea and jejunum tissues were used and tissues responses were recorded by Power Lab data acquisition system connected with isotonic or isometric transducers. Mk.Eth and Mk.Aq showed rightward shift in histamine concentration response curves at 0.1-0.3mg/ml, when tested on isolated guinea pig ileums. Both extracts also relaxed carbachol (1µM) induced pre contracted isolated rabbit trachea and jejunum tissue, dose dependently but a more potent effect was observed with aqueous extract of M. koenigii. Keeping in view all the results, presence of antihistaminic and anticholinergic activities in aqueous and ethanolic extracts of M. koenigii leaves can be strongly suggested that provides sound basis for application of M. koenigii in airways and gastrointestinal disorders. [ABSTRACT FROM AUTHOR]

The effects of 7-[3-[4-(2-quinolinylmethyl)- 1-piperazinyl]propoxy]-2,3-dihydro-4H-1,4- benzothiazin-3-one (VUF-K-8788) on experimental asthmatic reactions in guinea pigs were investigated. VUF-K-8788 inhibited histamine-induced bronchoconstriction at the doses of 0.3 and 1 mg/kg per os (p.o.). VUF-K-8788 inhibited anaphylactic bronchoconstriction at doses between 0.01 and 1 mg/kg in passively sensitized guinea pigs. Terfenadine used as a reference drug also inhibited an antigen-induced bronchoconstriction. VUF-K-8788 at the doses of 0.3 and 1 mg/kg inhibited immediate- and late-phase asthmathic reactions in actively sensitized guinea pigs. Terfenadine inhibited only the immediate phase reaction. Moreover, VUF-K-8788 inhibited the infiltration of eosinophils and macrophages into bronchoalveolar lavage fluid in guinea pigs. These results indicate that VUF-K-8788 may be useful for the treatment of bronchial asthma. [ABSTRACT FROM AUTHOR]

The use of systemic and topical steroids, amiodarone, and phenothiazines has been established as risk factors for the development of cataract. Antihistaminics are commonly prescribed drugs for a wide range of allergic disorders but have rarely been associated with cataract formation. We herewith report cases of two young males who were on long-term antihistaminics for allergic conditions and presented with blurring of vision. Slit lamp examination revealed bilateral posterior subcapsular cataract. The patients did not have any other systemic or ocular condition predisposing for cataract formation; hence, a diagnosis of antihistaminic-induced cataract was made. [ABSTRACT FROM AUTHOR]

Bauhinia racemosa Lam. (Caesalpiniaceae) leaves have been used in the treatment of asthma traditionally and we therefore undertook this study to scientifically validate its benefit in asthma using suitable animal models. Antihistaminic principles are known to be useful in the treatment of asthma; hence, in the present work, the antihistaminic activity of an ethanol extract of B. racemosa (at a dose of 50 mg/kg, i.p.) was assessed using clonidine-induced catalepsy and haloperidol-induced catalepsy in Swiss albino mice. The results showed that the ethanol extract inhibits clonidine-induced catalepsy but there is no effect on haloperidol-induced catalepsy. This suggests that the inhibition is through an antihistaminic action and that there is no role of dopamine. Hence, we concluded that the ethanol extract has significant antihistaminic activity. The polar constituents in the ethanol extract of leaves of B. racemosa may be responsible for the antihistaminic activity and B. racemosa may therefore have a role in the treatment of asthma. [ABSTRACT FROM AUTHOR]