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At least 811 records · Page 45Linked to original sources
PubMed1988

Blocking of histamine-induced conjunctivitis by the oral antihistamine, astemizole.

When histamine is applied topically to the eye it produces stinging and inflammation of the caruncle and bulbar and palpebral conjunctiva. This model has been employed in the present study to assess the ability of an oral antihistamine, astemizole, to attenuate the irritation and inflammatory signs. Astemizole 30 mg, taken orally once daily for 1 week, considerably lessened the stinging and significantly lowered the signs of inflammation caused by topically applied histamines.

Administration, Oral↗
PubMed1992

Assessment of the anticholinergic effect of the new antihistamine mizolastine in healthy subjects.

1. Twelve healthy subjects were enrolled in a double-blind placebo controlled cross-over study in order to assess the possible anticholinergic effects of four doses of a new antihistamine compound, mizolastine, compared with hyoscine butylbromide (HBB) used as a reference anticholinergic drug. 2. Although mizolastine, a potent and selective H1-receptor blocker has no affinity for muscarinic receptors and does not antagonize the effects of carbachol in rodents, a study was initiated to investigate its effects on various effectors possessing muscarinic receptors (eye, heart, sweat gland, salivary gland). 3. HBB (40 mg, s.c.) impaired accommodation, decreased salivary flow and inhibited cardiac sinus arrhythmia. Pupil diameter and maximum constriction speed, carbachol-induced skin sweating and Valsalva ratio were unaffected. 4. Mizolastine (5, 10, 20, 40 mg p.o.) did not affect any parameter at any time point, demonstrating a lack of anticholinergic effect.

Adult↗
PubMed1993

Diazepam effects on the performance of healthy subjects are not enhanced by treatment with the antihistamine ebastine.

1. We have given 12 healthy subjects the H1-antihistamine ebastine (20 mg) or placebo in a randomized double-blind and crossover study for 1 week each. The subjects were tested for drug effects on day 6 of each period, and for interactions of ebastine with oral 15 mg diazepam (DZ) on day 7. On both days, the testing runs were at baseline and 1.5, 3, 4.5 and 6 h after intake. 2. The performance was evaluated both objectively (digit symbol substitution, flicker fusion, Maddox wing, simulated driving, body balance) and subjectively (visual analogue scales, questionnaires). Venous blood was sampled daily during the maintenance and during each testing round for the assay of plasma carebastine (the active metabolite of ebastine) by high pressure liquid chromatography and plasma diazepam by radioreceptor assay. Three-way ANOVA, paired t-test, Wilcoxon rank sign test and Fisher's fourfold table test were used for data analysis. 3. Plasma carebastine reached steady levels from day 3 onwards. The mean concentrations in the morning were 82 micrograms l-1 on day 6 and 85 micrograms l-1 on day 7. The rise (+ 150%) in plasma carebastine after an extra 20 mg ebastine was not modified by DZ. Ebastine did not affect performance objectively or subjectively, yet borderline drowsiness was recorded during the first 3 h. On day 7, plasma DZ concentrations peaked (mean 480 micrograms l-1) at 1.5 h after the intake. DZ produced impaired performance in various objective tests, and drowsiness, weakness, clumsiness, mental slowness and poor performance were reported on visual analogue scales.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1995

Lack of interaction between a new antihistamine, mizolastine, and lorazepam on psychomotor performance and memory in healthy volunteers.

1. The possible interaction between a new H1 antihistamine, mizolastine, and lorazepam was assessed in a randomised, double-blind, cross-over, placebo-controlled study involving 16 healthy young male volunteers who received mizolastine 10 mg or placebo once daily for 8 days with a 1 week wash-out interval. The interaction of mizolastine, at steady-state, with a single oral dose of lorazepam or placebo was assessed on days 6 or 8 of each treatment period. 2. Psychomotor performance and cognitive function were evaluated using objective tests (critical flicker fusion threshold, choice reaction time, tapping, arithmetic calculation, body sway) and self-ratings (visual analogue scale, ARCI) before and at 2, 4, 6 and 8 h after dosing. Short-term memory (Sternberg memory scanning immediate free recall of a word list) and long-term memory (delayed free recall and recognition of words and pictures) were assessed before and at 3 h after dosing. Pharmacodynamic interactions were evaluated by repeated measures ANOVA in a 2 x 2 factorial interaction model. 3. Mizolastine, 10 mg once daily, at steady-state, was devoid of sedation and detrimental effect on skilled performance and memory. 4. In contrast, a single 2 mg dose of lorazepam produced marked impairment of psychomotor performance, cognitive functions (significant reduction in flicker fusion threshold, tapping and arithmetic calculation and increase in reaction times and body sway) and subjective sedation from 2 to 8 h after dosing. In addition, lorazepam induced an anterograde amnesia, characterised by a decrease in delayed free recall and recognition, and a deficit in short term memory.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed2006

The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study.

AIMS: To determine the effect of gender and the genetic polymorphisms of CYP2J2, CYP3A4, CYP3A5 and MDR1 on the urinary excretion of the H(1) antihistamine ebastine in healthy subjects. METHODS: Eighty-nine Caucasians were studied. The presence of polymorphisms in genes known to be involved in ebastine metabolism and transport (CYP2J2*2,*3,*4,*6,*7, CYP3A4*1B, CYP3A5*3, *6 and MDR1(ABCB1)(C3435T)) was assessed by means of PCR-restriction fragment length polymorphism and sequencing methods. Genotype was correlated with the urinary excretion of the main ebastine metabolites (desalkylebastine and carebastine) under basal conditions and after administration of grapefruit juice. RESULTS: Women excreted statistically greater amounts of desalkylebastine in urine (mean +/- SD (95% confidence intervals, 95% CI), 23.0 +/- 19.5 (18.1, 27.9) micromol) than men (12.4 +/- 11.0 (7.9, 16.9)), (mean difference: 10.6 (2.4, 18.7), P < 0.005). The CYP2J2, CYP3A4 and CYP3A5 analysed polymorphisms did not greatly affect ebastine metabolite excretion. The MDR1(C3435T) polymorphism was found to affect both the urinary excretion of the active metabolite carebastine (32.3 +/- 18.3 (23.1, 41.4), 22.8 +/- 14.7 (18.6, 27.0) and 21.5 +/- 15.3 (14.7, 28.3) for CC, CT and TT carriers, respectively; P < 0.05) and the grapefruit juice-induced inhibition of its transport/formation (mean fold-decrease +/- SD (95% CI), 1.5 +/- 0.8 (1.0, 2.0), 1.1 +/- 0.9 (0.7, 1.4) and 0.9 +/- 0.4 (0.6, 1.2) for CC, CT and TT carriers, respectively; P = 0.01). CONCLUSIONS: Gender and the presence of the MDR1(C3435T) polymorphism both influence the excretion of ebastine metabolites in urine.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1993

A corticosteroid, a non-steroidal anti-inflammatory drug and an antihistamine modulate in vivo vascular reactions before and during post-occlusive hyperaemia.

Post-occlusive reactive hyperaemia is the temporary increase of blood flow in a tissue following transient vascular obstruction, and has recently been proposed as an in vivo method for ranking topical corticosteroid potency. We investigated in vivo vascular reactions before and during post-occlusive hyperaemia using laser-Doppler flowmetry and reflectance spectroscopy (RS). RS enables resolution of in vivo erythema into deoxygenated (venous) [DOH] and oxygenated (arterial) haemoglobin (OH) components (expressed in arbitrary units, AU). Using a randomized 24-h occlusive exposure in 10 healthy volunteers the effects of a corticosteroid (betamethasone-17-valerate), a non-steroidal anti-inflammatory drug (NSAID) [indomethacin], an antihistamine (diphenhydramine), or vehicle, were studied before and during post-occlusive hyperaemia. The 24-h vehicle exposure decreased total haemoglobin (composed of a small increase in OH [P < 0.001] and a greater decrease in DOH [P < 0.005], [OH, 0.23 +/- 0.18 AU; DOH, 0.28 +/- 0.12 AU]). The blood flow increased 7.1% to 28 +/- 8 AU (P > 0.05). Betamethasone-17-valerate exposure decreased total haemoglobin further (OH, 0.10 +/- 0.09 AU [P < 0.005]; DOH, 0.18 +/- 0.08 AU [P < 0.05]), which corresponded to a 15% blood flow decrease (P < 0.05). Indomethacin reduced OH to 0.18 +/- 0.12 AU (P < 0.02) and increased DOH slightly, with a trend towards decreased blood flow (P > 0.05). Diphenhydramine caused no significant changes in RS or laser-Doppler flowmetry readings before post-occlusive hyperaemia. Post-occlusive hyperaemia increased total haemoglobin maximally at the first observation time (OH, 0.63 +/- 0.13 AU; DOH, 0.31 +/- 0.11 AU [P < 0.001]).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1976

Intranasal steroid aerosol in perennial rhinitis: comparison with an antihistamine compound.

Intranasal betamethasone valerate aerosol, given for 28 days, was compared with an oral antihistamine compound in a couble-blind, double-dummy, cross-over trial involving thirty patients with perennial rhinitis. The steroid aerosol was more effective in reducing symptoms and was preferred by the patients (P less than 0-01). Nasal blockage index, calculated from oral and nasal peak expiratory flow measurements, did not provide useful or additional information. There were no side effects from the steroid and Candida albicans was not cultured from nasal swabs. It is concluded that beta-methasone valerate aerosol is a suitable short-term alternative for patients whose perennial rhinitis fails to respond to conventional therapy.

Administration, Intranasal↗
PubMed1990

Does the clinical experience with non-sedating H1-antagonists justify a reassessment of antihistamines in allergy treatment?

Although antihistamines were usually considered as ineffective in asthma, the appearance of new more potent anti-'1-antagonists with no or less side-effects leads to a reassessment of their use. Although mediators and mechanisms other than histamine are involved in natural or provoked reactions to allergens in the skin, the nose or the lungs, the new anti-H1-antagonists have been shown to be effective. For some of these drugs, the effect may go beyond a mere H1-receptor blockade and involve impairment of mediator release from mast cells and/or an inhibiting effect on other cell types (e.g. eosinophils) implicated in the late-phase reactions. Quantitative kinetics evaluation of late-phase reactions in the skin and of their inhibition by anti-allergic drugs will be helped considerably by the development of telethermography, a new skin evaluation technique.

Asthma↗
PubMed1994

Comparison of a new antihistaminic and antiallergic compound KW 4679 with terfenadine and placebo on skin and nasal provocation in atopic individuals.

The effects of three oral doses of a new compound KW 4679 thought to have both antihistaminic and antiallergic properties were compared with terfenadine and placebo in a double-blind cross-over trial in 15 volunteers with seasonal allergic rhinitis. Comparison of the effect of the treatments with either 2.5, 5 or 10 mg b.i.d. of KW 4679, 60 mg b.i.d. of terfenadine or placebo was made on the response to histamine and grass pollen skin-prick testing. Nasal provocation testing with grass pollen was performed on the eighth day of treatment. Nasal airway resistance (NAR) was measured using active posterior rhinomanometry and the dose of grass pollen which caused a 200% increase in NAR was determined. The number of sneezes in the first 12 min was counted. Compared with placebo all doses of KW 4679 and terfenadine significantly inhibited the skin weal response to histamine and grass pollen (P < 0.001). The inhibitory effect of KW 4679 on both histamine and allergen induced skin weals was significantly greater than that of terfenadine (P = 0.001 and P = 0.049 respectively). The results of nasal challenges with grass pollen showed that all doses of KW 4679 and terfenadine were effective in reducing sneeze counts (P < 0.001), though there were no significant effects on allergen induced increase in NAR. All three doses of KW 4679 were generally well tolerated. Drowsiness was reported by some of the volunteers on KW 4679 and one volunteer reported drowsiness whilst taking placebo. Slight and reversible rises in AST and ALT concentrations were observed; these were not considered clinically significant.

Adult↗
PubMed2005

A new antihistamine levocetirizine inhibits eosinophil adhesion to vascular cell adhesion molecule-1 under flow conditions.

BACKGROUND: We previously demonstrated that low concentrations of a new antihistamine levocetirizine inhibited eosinophil transmigration through human microvascular endothelial cells. OBJECTIVE: Here, the inhibitory effect of levocetirizine on eosinophil adhesion to recombinant human vascular cell adhesion molecule-1 (rhVCAM)-1 was examined under conditions of shear stress using an in vitro model of the post-capillary venules. METHODS: Eosinophils isolated from normal subjects were pre-incubated with a concentration range of levocetirizine (10(-6)-10(-10) m) or negative dilution control. Resting or granulocyte macrophage-colony stimulating factor (GM-CSF)-stimulated cells were pumped through rhVCAM-1 (10 microg/mL) coated capillary tubes using a microfluidic syringe pump at a precise and constant flow rate (1 dyn/cm(2)). Images of rolling and firmly adherent eosinophils were captured using real-time video microscopy. RESULTS: Levocetirizine significantly inhibited resting eosinophil adhesion to rhVCAM-1 with maximal effect at 10(-8) M with an EC(50) of 10(-9) m. Levocetirizine almost abolished resting eosinophil adhesion by the 15 min time-point. GM-CSF significantly enhanced eosinophil adhesion and their ability to flatten on rhVCAM-1. Both phenomena were inhibited by levocetirizine in a dose-dependent manner, at both 5 and 15 min (optimal concentration of 10(-8) m with an EC(50) of 10(-9) m). Real-time imaging revealed that the effect of levocetirizine on post-adhesion behaviour (detachment, flatness) contributed to its inhibitory action on eosinophil adhesion to rhVCAM-1. In contrast, very late antigen (VLA)-4 mAb inhibited eosinophil adhesion to rhVCAM-1 from the earliest time-points. CONCLUSION: Physiologically relevant concentrations of levocetirizine inhibit resting and GM-CSF-stimulated firm eosinophil adhesion to rhVCAM-1 under flow conditions.

Antibodies, Monoclonal↗
PubMed1991

Efficacy of an oral antihistamine, loratadine, as compared with a nasal steroid spray, beclomethasone dipropionate, in seasonal allergic rhinitis.

The aim of the study was to compare the efficacy and side-effects of oral antihistamine and nasal glucocorticoid therapy in seasonal allergic rhinitis. In a double-blind, double-dummy, group-comparative study, 60 birch and grass pollen allergic patients were treated with either loratadine (10 mg daily) or beclomethasone dipropionate (BDP) (100 micrograms in each nostril twice daily) during a 3 weeks' study period. Grading of 4 nasal and 3 non-nasal symptoms was performed at 4 weekly visits, and patients recorded daily symptoms and possible adverse experiences in a diary. Patients treated with BDP showed significantly less nasal blockage than those receiving loratadine (P less than 0.05), but there was no difference (P greater than 0.05) in other nasal symptoms (sneezing, itching and discharge). Patients treated with loratadine showed a statistically significantly greater relief in eye symptoms as compared with BDP (P less than 0.05). The side-effects caused by the 2 treatments were few and insignificant. We conclude that loratadine and intranasal BDP were effective in the treatment of seasonal allergic rhinitis, but the spectrum of individual symptoms controlled was different for the 2 drugs.

Administration, Intranasal↗
PubMed2006

A randomized comparative clinical trial of recombinant canine interferon-gamma (KT-100) in atopic dogs using antihistamine as control.

Recombinant canine interferon-gamma (KT-100) or topical antihistamine (diphenhydramine: DH) was administered to dogs with atopic dermatitis (AD) for 4 weeks and their efficacies were compared using pruritus, excoriation, erythema and alopecia as evaluation criteria. Clinical studies on 92 atopic dogs (KT-100 group: 63, DH group: 29) were conducted at 18 animal hospitals in Japan. KT-100 was administered subcutaneously once a day three times a week on alternating days for 4 weeks. DH was administered topically twice daily for 4 weeks. The efficacy rates of the KT-100 group on day 28 were 72.1% for pruritus, 73.8% for excoriation, 75.4% for erythema and 60.7% for alopecia, which were significantly higher than those of the DH group (20.7% for pruritus, 27.6% for excoriation, 24.1% for erythema and 24.1% for alopecia).

Administration, Topical↗
PubMed1983

The effect of antihistamines on ultraviolet-light-induced erythema.

Because of the possible role of histamine as an early mediator of ultraviolet light induced erythema, we studied a group of volunteers treated with both H1 and H2 blockers, alone and in combination, before and at various time intervals after, UVL irradiation. No difference was found in the degree of erythema produced by any of the antihistamines used, whether alone or in combination, when compared with the saline control.

Erythema↗
PubMed1977

Comparison of a new antihistamine HC 20-511 with cyproheptadine (Periactin) in chronic urticaria.

The effect and tolerance of a new antihistamine, HC 20-511, in daily doses of 2 and 4 mg was compared with cyproheptadine (Periactin) 8 mg daily in 50 cases of chronic urticaria. HC 20-511 4 mg daily proved to be the most effective, rapid and long-lasting. HC 20-511 had less sedative effect than cyproheptadine, but both possessed the same appetite-stimulating effect. However, this was not noted with the smaller dosage of HC 20-511.

Adult↗
PubMed1982

Effect of the H1 antihistamine chlorpheniramine maleate on histamine-induced symptoms in the human conjunctiva. Indirect evidence for nervous H1 receptors.

Earlier studies have shown that intranasal chlorpheniramine (0.77%) can inhibit histamine-induced tickling, sneezing, and hypersecretion by a local effect on nerve fibres. The aim of the present study was to examine whether this solution had local anaesthetic of parasympatholytic properties. If neither of these properties are present it suggests that the anti-pruritic effects of the solution are caused by inhibition of H1 receptors, which in turn is indirect evidence for the presence of H1 receptors on nerve fibers. In a double-blind design 15 normal subjects were provoked with histamine in the eye after pretreatment with chlorpheniramine or with a local anaesthetic, oxybuprocain. Both drugs inhibited itching, but the H1 antihistamine was significantly more effective than the local anaesthetic (P less than 0.01). Corneal sensitivity was measured by an esthesiometer, and pupil difference was used as a measure for atropine activity. Chlorpheniramine had neither a local anaesthetic nor a parasympatholytic effect. This study has therefore strengthened the hypothesis that there are nervous H1 receptors in the mucous membranes of the eye and airways and has extended its application in animals to also include man.

Adult↗
PubMed1988

Duration of the inhibitory activity on histamine-induced skin weals of sedative and non-sedative antihistamines.

The inhibitory effect of orally administered dexchlorfeniramine (4 mg/day), cyproheptadine (8 mg/day), astemizole (20 mg/day), loratadine (40 mg/day) and terfenadine (120 mg/day) on the size of histamine-induced weals was tested by skin prick test with histamine in an open study including 23 healthy individuals. The antihistamines were administered for 2 days in the nationally recommended therapeutic doses. For all drugs the maximal weal suppression with the dosage chosen was recorded the day after the last dosage, being 29% (for dexchlorfeniramine), 72% (for cyproheptadine), 50% (for astemizole), 62% (for loratadine), and 56% (for terfenadine) of the baseline value. For the drugs in the same order the duration of the inhibitory effect of the drugs after the last dose administered was between 3-4, 7-11, 17-28, 4-7, and 4-7 days, respectively.

Female↗
PubMed1990

Treatment of hay fever with loratadine--a new non-sedating antihistamine.

The efficacy and safety of loratadine, a new orally active specific H1-receptor blocking antihistamine with poor penetration into the CNS, was evaluated in a double blind comparative study. One hundred and seven hay fever patients, sensitive to birch pollen, were randomized into three parallel groups receiving loratadine 40 mg once daily, clemastine 1 mg twice daily, or placebo during the birch pollen season. Both active treatments showed reduction of symptoms in comparison with placebo, but the results were more pronounced with loratadine treatment, which significantly reduced the overall allergic condition as well as all separate allergic rhino-conjunctivitis symptoms except nasal stuffiness. Compared with placebo the sedation rate was significantly higher with clemastine treatment (P less than 0.05) but not with loratadine. Loratadine was thus concluded to be efficacious in hay fever treatment with a sedation rate not differing from placebo.

Clemastine↗
PubMed1992

Evaluation of antihistamine-related daytime sleepiness. A double-blind, placebo-controlled study with terfenadine.

The daytime sleepiness potentially associated with antihistamines was evaluated by the multiple sleep latency test (MSLT) in a study comparing terfenadine with placebo. According to a double-blind, randomized, cross-over design, 12 healthy men were given either 120 mg terfenadine or placebo once daily in the morning, for 3 consecutive days with a 5-day interval. EEG-polygraphic recordings were made each study day at 9:30 and 11:30 a.m., and 1:30, 3:30, and 5:30 p.m., and the tendency to fall asleep was measured. All mean stage-1 sleep latencies throughout the study failed to show any significant difference between terfenadine and placebo. Accordingly, psychomotor performance assessed by visual and auditory reaction time did not change after treatment. The results of this study confirmed that terfenadine does not induce daytime sleepiness as objectively measured by MSLT.

Adult↗