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Studies on antimicrobial effect of the antihistaminic phenothiazine trimeprazine tartrate.

The antibacterial and bactericidal activities of the antihistamine trimeprazine were studied against 243 strains of bacteria which included both Gram positive and Gram negative types. The susceptibility of these bacterial strains to trimeprazine was assessed by determining their minimum inhibitory concentration (MIC) which was found to be between 10 and 100 micrograms/ml. Nineteen strains of Staphylococcus spp. and Salmonella spp. were trimeprazine. Most of the strains belonging to Bacillus spp. and Salmonella spp. were inhibited by less than 100 micrograms/ml. Trimeprazine could also inhibit strains of Shigella spp. Vibrio cholerae and V. parahaemolyticus at 10-100 micrograms/ml. Strains of klebsiella, proteus, pseudomonas and citrobacter were moderately sensitive to trimeprazine. In in vivo studies it was seen that when trimeprazine was used at a concentration of 0.75 and 0.4 micrograms/gm body weight of the mouse both levels offered significant protection to Swiss mice challenged with 50LD50 of virulent strain of S. typhimurium 74. Statistical analysis of the data was found to be significant, p < 0.001 according to chi 2 test.

Animals↗

Central effects of the H1-antihistamine, cetirizine.

BACKGROUND: Effects of the H1-antihistamine, cetirizine, were studied on daytime alertness and performance to establish whether the drug would be suitable for use by air personnel and others involved in skilled activity. METHODS: The investigation was carried out in six healthy volunteers, and the effects of the drug (5, 10, and 15 mg) were studied on sleep latency, subjective sleepiness, digit symbol substitution, tracking and vigilance from 0.5 h to 7.5 h after ingestion. The study was placebo-controlled and double-blind with a six-way cross-over design. Promethazine (10 mg) was used as an active control to establish the sensitivity of the experimental procedures. RESULTS: Promethazine (10 mg) decreased the mean level of vigilance over the day, increased objective and subjective sleepiness from 1.5 to 5.5 h, and impaired tracking 5.5 h after ingestion. Cetirizine (10 and 15 mg) led to shortened sleep latencies over the day, and at 7.5 h sleep latencies were shorter with 10 mg cetirizine than with placebo. Subjective sleepiness with cetirizine was increased compared with placebo after 5 mg at 1.5 h, 10 mg at 7.5 h, and 15 mg at 5.5 h and when meaned over the day. Tracking was impaired with 5 and 15 mg cetirizine 0.5 h after ingestion. CONCLUSION: The study failed to establish dose-response effects of cetirizine, but it is evident that cetirizine is not free of central activity over the therapeutic range, and so its use by air personnel is not recommended.

Administration, Oral↗

[A pilot phase II study of combination therapy with oxatomide, an antihistamine, plus dextromethoraphan and bakumondo-to, an herbal drug, in patients with postinfectious persistent cough].

Previously, we reported the effectiveness of treatment with oxatomide (O), an antihistamine, plus dextromethorphan (D), and that of Bakumondo-to (B), an herbal drug that inhibits the activation of C-fibers, in patients with persistent coughing after upper-airway infection. In this study, we evaluated the efficacy and side effects of combination therapy (O + D + B) in patients with postinfectious persistent cough. Patients who had been coughing for more than three weeks and had a history of upper-airway infection took part in the study. None had any history of nasal disease, gastroesophageal reflux, bronchial asthma, or other chronic pulmonary disease. All patients were non-smokers, and none used angiotensin converting enzyme (ACE) inhibitors. All had normal chest roentgenograms and normal pulmonary function. The following hematological data were obtained before treatment: peripheral eosinophil counts. CRP levels, serum IgE concentrations, and titers of cold agglutinins and antibodies to Mycoplasma pneumoniae. The effects of one week of treatment with O + D + B on the severity of coughing, as estimated with a cough diary, were examined. Thirty-six patients entered the study, but only 18 with normal hematological findings who satisfied the study criteria were eligible for efficacy and side-effect analyses. Cough scores decreased significantly from 5.1 +/- 2.4 (range, 2-9) to 1.2 +/- 1.9 (range, 0-6), and the rate of cough disappearance was 50%. Two patients reported slight drowsiness. Therapy with O + D + B reduced perception of coughing as estimated with a cough diary. These results suggest that this therapy (O + D + B) may be useful in patients with postinfectious persistent cough.

Adrenergic beta-Agonists↗

[The influence of antihistamine agents on reaction time].

Authors carried out the study of reaction time on auditory stimulus in a group of 200 patients taking a single dose of: Clemastin, Phenazolinum, Zyrtec, Astemizol, Claritin, Disophrol and placebo. The results indicate the prolongation of reaction time after the administration of either first or second generation antihistaminics.

Adolescent↗