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At least 919 records · Page 51Linked to original sources
PubMed1990

Studies on synergism between penicillins and ambodryl (bromodiphenhydramine HCl), an antihistamine with antimicrobial property.

With respect to 31 different selected test bacteria, all sensitive to benzyl penicillin (Pc), ampicillin (Ap), methicillin (Me), ceporan (Ce), cloxacillin (Cx), streptomycin (Sm), kanamycin (Km), gentamicin (Gm), chloramphenicol (Cm), tetracycline (Tc), polymyxin (Pm) as well as ambodryl [Am; an antihistamine (bromodiphenhydramine HCl) with distinct antimicrobial properties], it was found that Am in combination either with Pc, Ap, Ce or Me consistently showed enhancement of antimicrobial effects resulting from synergism. A combination of Am with either Sm, Km, Gm or Tc, on the other hand, showed only additive effects. An interaction of the activities of Am with Pm also resulted in indifference effects. Determination of the area of inhibition zone, calculated from its diameter for the degree of synergism in case of Am and Pc, showed these synergistic effects to be significant (P less than 0.05) in comparison with their individual effects: this was corroborated by the determination of the fractional inhibitory concentration (FIC) index which was found to be less than 0.5. The synergism of Am-Pc combination was confirmed by in vivo studies by challenging mice with a virulent strain of S. typhimurium and looking for protection.

Bacteria↗
PubMedDate not supplied

[The effect of the new Soviet antihistamine and antiserotonin preparation bikarfen on the central nervous system].

The effect of an antiallergic (antihistaminic and antiserotonin) drug bicarphen on the functional state of the central nervous system (CNS) was studied. In experiments on animals bicarphen in contrast to dimedrol (diphenhydramine) exerted predominantly the activating effect on CNS (decreased the hypnotic action of barbamyl, enhanced the summation capacity of CNS and the activity of mice in the escape behavioral test, increased the bioelectrical activity of the brain and the activating effect of antidepressants on the EEG).

Animals↗
PubMedDate not supplied

A large-scale, office-based study evaluates the use of a new class of non-sedating antihistamines. A report from CEN.

The two newest agents in the class of nonsedating antihistamines were studied in a wide variety of family practice patients. In a Phase IV, prospective, alternating sequence, open-label design, patients having allergic rhinitis (AR) were assigned to receive either astemizole (n = 659) or terfenadine (n = 639). The resultant treatment groups, typical of family practices, were comparable for demographics, signs and symptoms of allergic rhinitis, and clinical profile. The groups differed in that astemizole patients had a longer history of AR and a higher frequency of family history of AR. Patients who were treated for 3 to 8 weeks were grouped for analyses. The frequency and severity of the signs and symptoms of AR and patient complaints decreased markedly in both groups. Self-reported improvement in quality of life based on nine measures was the same for each group. No differences were seen between treatments when positive-rated outcomes were combined in the final overall assessment by physicians and patients. In rating the success of therapy, physicians' ratings of "excellent" and patients' ratings of "felt much better" were reported more frequently (P less than 0.05) for astemizole, while physicians' ratings of "good" and patients' ratings of "better" were reported more frequently (P less than 0.05) for terfenadine.

Adult↗
PubMed1990

Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers.

New H1-receptor antagonists are assessed not only for their H1 antihistaminic activity but also for their central nervous system (CNS) side effects. Fifteen healthy subjects received a once daily dose of 5 mg, 10 mg or 20 mg of epinastine, or a twice daily dose of 60 mg of terfenadine or placebo in a randomized double-blind (double-dummy) crossover study. The response to histamine-induced skin wheals was compared. CNS effects were evaluated by a multiple reaction time task, a finger tapping test and a self-rating scale (Bf-S von Zerssen) to assess mood state. Epinastine attenuated the wheal size in response to histamine in a dose-dependent manner. In addition, all epinastine dosages had a distinctly faster onset of action than terfenadine. All active treatments (5 mg, 10 mg, 20 mg epinastine and 60 mg terfenadine) attained their maximum effects 4 h after administration. At this time point and also 12 h after administration, 20 mg of epinastine were significantly more effective than 60 mg of terfenadine. Single 10 mg and 20 mg doses of epinastine were as effective as terfenadine given twice daily, and significantly more effective than placebo 24 h after drug administration (i.e. 12 h after the second dose of terfenadine). The psychometric tests for CNS effects did not reveal any difference among epinastine, terfenadine and placebo. In conclusion, epinastine is one of the most effective peripherally acting H1 antagonist which lacks significant CNS side effects and is suitable as a once daily dosage regimen.

Administration, Oral↗
PubMed1990

[Investigation, identification and dosage of local anesthetics and antihistaminics in cosmetic products].

A rapid and accurate reversed-phase HPLC method for separation and simultaneous quantitation of some local anesthetics, antihistamines and preservatives in skin cosmetics is described. The investigated compounds (procaine, lidocaine, mepivacaine, bupivacaine, benzocaine, brompheniramine, benzoic acid, methyl, ethyl and propyl p-hydroxybenzoate, o-phenylphenol) are extracted by ultrasonic treatment in methanol from cosmetic form. Methanol-aqueous orthophosphoric acid (pH 2.8) containing 0.9% dibutylamine has been used as eluent. The influence of different percentages of methanol on chromatographic behaviour has been studied using both isocratic conditions and gradient elution program. The gradient program allows a rapid resolution and quantitation also for acidic preservatives.

Anesthetics, Local↗
PubMed1975

A new antihistamine hc20-511 compared with dimetinden (fenistil retard) in the treatment of chronic urticaria and other pruritic dermatoses.

The new antihistamine, HC20-511 (Sandoz), was compared with Dimetinden (Fenistil retard) in a single-blind comparative study in 42 patients with dermatoses, 28 of whom suffered from chronic urticaria. HC20-511 had a better effect, especially in chronic urticaria, where pruritus, erythema and papules quickly disappeared. The effect appeared somewhat faster than and lasted as long as that of Dimetinden, although HC20-511 is not a retard-preparation unlike the Dimetinden preparation used for comparison. HC20-511 also caused less side effects.

Adolescent↗
PubMed1975

Biologically active substances in oak gall extracts. Part 1: Isolation and chemical identification of a substance exerting antihistamine-like activity (KC-18).

The previously reported antihistamine-like activity of partially purified oak gall extracts has been confirmed. Isolation of the active principle was achieved through the use of organic solvent extractions and column chromatographic (Sephadex LH-20 and silica gel) procedures. Preliminary investigation on the structure of this chemically pure substance using mass spectrometry, thin layer chromatography, base hydrolysis and electrophoresis indicated that it is most probably an ester of piperonylic acid. KC-18, given intraperitoneally in doses of 4 mg/kg to guinea pigs 5 hours prior to an exposure to a 0.15 per cent histamine aerosol, significantly reduced the bronchoconstrictor effect of histamine.

Animals↗
PubMed1975

Biologically active substances in oak gall extracts. Part 11. The antihistamine-like activity of a substance (KC-18) isolated from oak gall extracts.

The effects of the newly isolated antihistamine (KC-18) from the Hungarian oak gall extracts on some actions of histamine have been investigated. Intraperitoneally administered KC-18 into guinea pigs and cats in doses of 2.5-16 mg/kg exerted a significant dose-related inhibition of histamine-induced bronchoconstriction, increase in capillary permeability and hypotension. In guinea pigs, actively sensitized with ovalbumin, 4 mg/kg KC-18 administered intraperitoneally prevented the development of anaphylactic shock following antigenic challenge. Histamine-induced gastric acid secretion in the rat was also dose-relatedly reduced by the intravenous administraton of 72 and 120 mg/kg KC-18. However, KC-18 in doses up to 100 mug/ml did not modify the histamine-induced contraction of the isolated guinea pig ileum.

Aerosols↗
PubMed1988

Effect of antihistamines on interferon production by leukocytes from sensitized and non-sensitized mice.

The effect of four antihistamines (Intal, Zaditen, Tavegyl, Benzhydramine) on interferon production in mice was investigated. The agents were administered in vivo to ovalbumin-sensitized and non-sensitized mice, or in vitro to isolated peritoneal cell cultures. The cells were induced for interferon production with Newcastle virus. It was shown that Tavegyl and Benzhydramine, both after in vivo and in vitro administration, inhibit interferon production, while Intal and Zaditen had no effect.

Animals↗
PubMedDate not supplied

"In vivo" and "in vitro" evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine).

A group of 32 patients with perennial allergic rhinitis sensitized exclusively to house dust and mites were evaluated for "in vivo" modifications (skin tests for histamine, house dust and mites) and "in vitro" alterations (seric IgE, specific IgE, histamine release curve to different concentrations of Dermatophagoides pteronyssinus and histamine release curve to this pneumoallergen after incubation with H1 receptor antagonists) to four antihistamines (astemizole, azatadine, mequitazine and terfenadine). The patients were divided into 4 groups of 8 and the "in vivo" and "in vitro" tests were performed on days -1, +15 and +30 of administration of these drugs. The reduction in the size of the wheal (prick test) for histamine when comparing days -1 and +15 and -1 and +30 was 69% and 79% (astemizole), 64% and 71% (azatadine), 69% and 64% (mequitazine) and 61% and 64% (terfenadine), respectively. The difference in the mean size of the wheal in mm2 for house dust, Dermatophagoides pteronyssinus and farinae was statistically significant (p less than 0.001) except when comparing the results obtained for mequitazine on days -1 and +15. This was also the case on days -1 and +30 for terfenadine. The values of the serum IgE and specific IgE did not attain statistical significance (p greater than 0.05) in the various tests carried out. After incubation with H1 receptor antagonists an inhibition curve of the histamine release in the presence of Dermatophagoides pteronyssinus was obtained. The inhibition of this curve on day -1 was higher for terfenadine and mequitazine than for azatadine and astemizole.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMedDate not supplied

[The effect of antihistamine preparations on the contraction of the isolated guinea pig ureter].

The effect of antihistaminics on contractions of the isolated guinea pig ureter was studied. The ureter contractions induced by histamine were prevented by H1-blockers: pipolphen (promethazine), dimedrol (diphenhydramine), phencarol (quifenadine), suprastin (chloropyramine), cyproheptadine and H2-blockers: cimetidine, ranitidine. Electric stimulation-induced contractions were prevented by suprastin. Phencarol, tavegil, cimetidine, ranitidine didn't act on the contractions. The electrically induced contractions were potentiated by pipolphen, dimedrol, cyproheptadine.

Animals↗
PubMed1989

The effectiveness of the nonsedating antihistamine loratadine plus pseudoephedrine in the symptomatic management of the common cold.

A multicentered trial compared the effects of the non-sedating antihistamine, loratadine, 5 mg plus pseudoephedrine 120 mg with a placebo on the signs and symptoms of the common cold. One hundred forty-two (142) subjects were treated with the loratadine/pseudoephedrine combination and 141 subjects were treated with placebo twice daily for five days. Evaluations by both subjects and physicians suggest that this antihistamine/decongestant combination is superior to placebo in relieving symptoms of the common cold. Specific differences were found in symptoms including nasal congestion, sneezing, postnasal drainage, and nasal discharge. Differences between groups for the following side effects were found: dry mouth (9% for the combination vs 2% for placebo), insomnia (6% vs 3%), and nervousness (4% vs 2%). There were no differences between groups for the frequency of drowsiness.

Adolescent↗
PubMed1989

The European experience with antihistamines in asthma.

Until the appearance of nonsedating antihistamines such as terfenadine and astemizole, clinical studies of H1 antagonists in the treatment of asthma yielded disappointing results. The author reviews recent European studies that demonstrate terfenadine's effectiveness in reducing symptoms and improving bronchodilation in patients with mild atopic asthma.

Asthma↗
PubMed1978

A repeated dose comparison of the side effects of five antihistamines on objective assessments of psychomotor performance, central nervous system arousal and subjective appraisals of sleep and early morning behaviour.

The side effects of five antihistamines (chlorpheniramine maleate, mebhydrolin, clemastine hydrogen fumarate, Tavegil; ketotifen, and promethazine hydrochloride) were measured on subjective assessments of sleep and the integrity of early morning behaviour and objective assessments of complex psychomotor behaviour and central nervous system arousal. Fifty consenting volunteers each received one of the five preparations for a period of four days with the subjective effects being reported on a set of 10 cm line visual analogue scales and the objective assessments being made via a computer assisted reaction time task and critical flicker fusion thresholds. Chlorpheniramine, 4 mg t.d.s. for four days, produces a significant impairment in critical flicker fusion thresholds with respect to pretreatment baselines but none of the preparations showed any significant impairment in complex reaction time assessments. The subjective assessments of sleep and early morning hangover showed mebhydrolin and clemastine to be free from detrimental side effects, but promethazine and chlorpheniramine produce significant impairments in the integrity of early morning behaviour.

Adult↗
PubMedDate not supplied

[Pharmacokinetics of the new Soviet, tritium-labelled, antihistamine preparation, phencarol].

As evidenced no less than 45 per cent of tritium-labelled antihistaminic drug phencarol (quinuclidine-3-diphenylcarbinol hydrochloride) introduced intragastrically to rats is absorbed. The maximal radioactivity in various organs is reached in 1--3 hours, with high specific radioactivity being recorded in the lungs and liver and low--in the brain. The drug or radioactive products of its tranformation are eliminated largely via the gastrointestinal tract and kidneys.

Animals↗
PubMedDate not supplied

[Experimental study of the antiedema activity of antihistamine preparations compared to the dynamics of their concentration in the blood serum].

The time-course of the antiexudative effect of the antihistaminic drugs diphenhydramine, phencarol and suprastin was studied in experimental dextran edema of the rat hind limb after intragastric administration of the drugs in a dose of 50 mg/kg. The data obtained were correlated to the time-course of the blood serum drug concentration measured by high pressure liquid chromatography. The relationship between the pharmacological action of the drugs and the mean maintenance dose was depicted by means of computer. It has been shown that the antiexudative activity of diphenhydramine and phencarol is approximately identical, whereas the efficacy of suprastin is several times less.

Animals↗
PubMed1985

[Hismanal--a non-sedating H1 antihistaminic].

The intake of antihistamines with CNS depressing side effects leads to a multiple increase of risk for accidents with lethal results in traffic. 12 special pharmacopsychological trials, e.g. at the Royal Air Force Institut, Great Britain; at the Association for Research into Accident Causes, Cologne; and the Department of Pharmacotherapy (Drugs and Driving Research Group), University of Utrecht, Netherlands, showed Hismanal to have neither sedation nor performance reducing side effects.

Arousal↗
PubMed1985

Central effects of H1 and H2 antihistamines.

H1-antihistamines are usually associated with impairment of central nervous functions, but unacceptable decrements in performance may not be an inevitable sequel of their use. Effects are dependent on the ability of a particular drug to cross the blood brain barrier, and so compounds which cross so slowly that tolerance of the central nervous system can develop gradually without any immediate changes in performance are of interest. However, sustained release formulations and compounds which have a selective affinity for the peripheral receptor may also have their part to play in the management of allergic states in those involved in skilled activity. As far as H2-antagonists are concerned, it is likely that as they are less liposoluble they would be free of central effects. Studies on the central effects of H1 and H2 antagonists are reviewed, and tentative recommendations are made in respect of these findings concerning the possible use of these drugs in aircrew.

Aerospace Medicine↗