The drug discovery and development process is still long, costly, highly risky. principal attrition factor undetected toxicity, with hepatic cardiac toxicities playing a critical role being the main responsible of safety-related withdrawals from market. Multi Organs-on-Chip (MOoC) represent disruptive solution to study drug-related effects on several organs simultaneously efficiently predict to...

It has been reported that some of H1 receptor antagonists have important effects on cardiovascular system. Terfenadine as a non-sedative H1 receptor antagonist has an arrhythmogenic activity. In this study we have shown the effects of four antihistamine drugs: terfenadine, loratadine, clemastine and diphenhydramine, on the rate and contractions of isolated rat atria. Terfenadine (1-10 μM) cause...

A double blind placebo controlled experiment was conducted measuring the effects of the centrally active antihistamine triprolidine and the peripherally acting antihistamine terfenadine on actual driving performance in a group of experienced women drivers. Triprolidine greatly impaired driving behaviour, whereas terfenadine did not. Triprolidine also impaired subjective and objective measures o...

Terfenadine (4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-(4-tert-butylphenyl)-butan-1-ol) was identified in a biological screening to be a moderate inhibitor (27% inhibition) of the CD81-LEL-HCV-E2 interaction. To increase the observed biological activity, 63 terfenadine derivates were synthesized via microwave assisted nucleophilic substitution. The prepared compounds were tested for their inh...

Testosterone, terfenadine, midazolam, and nifedipine, four commonly used substrates for human cytochrome P-450 3A4 (CYP3A4), were studied in pairs in human liver microsomes and in microsomes from cells containing recombinant human CYP3A4 and P-450 reductase, to investigate in vitro substrate-substrate interaction with CYP3A4. The interaction patterns between compounds with CYP3A4 were found to ...

OBJECTIVE To determine whether better health-related quality of life (HRQL) is achieved by initiating treatment of seasonal (ragweed) rhinoconjunctivitis (hay fever) with a nasal steroid (fluticasone) backed up by a nonsedating antihistamine (terfenadine) or whether it is better to start with the antihistamine and add the nasal steroid when necessary. DESIGN Randomized, nonblind, parallel-gro...