{"doi":"10.3109/00498254.2011.643256","title":"The impact of P-glycoprotein mediated efflux on absorption of 11 sedating and less-sedating antihistamines using Caco-2 monolayers","abstract":null,"journal":"Xenobiotica","year":2012,"id":652755,"datarank":0.5375278407684165,"base_score":3.58351893845611,"endowment":3.58351893845611,"self_citation_contribution":0.5375278407684165,"citation_network_contribution":0.0,"self_endowment_contribution":0.5375278407684165,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":35,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1491311,"name":"Cameron Wright","orcid":"0000-0001-5416-8958","position":1,"is_corresponding":false},{"id":764979,"name":"Andrew Crowe","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"The impact of P-glycoprotein mediated efflux on absorption of 11 sedating and less-sedating antihistamines using Caco-2 monolayers","abstract":"Caco-2 cells were used to compare P-gp mediated efflux and passive permeability using bidirectional transport of 11 antihistamines. An efflux ratio >2 indicated active efflux, with PSC833 and GF120918 used as functional P-gp inhibitors. Antihistamines were measured directly by HPLC or LC/MS. Fexofenadine had an efflux ratio of 37, yet had negligible passive permeability, even in the presence of a pH gradient (0.1 × 10(-6) cm/sec). Its precursor, terfenadine, had an efflux ratio of 2.5, while cetirizine, desloratadine and hydroxyzine were 4, 7 and 14, respectively. After incubation with P-gp inhibitors, these ratios dropped significantly. Loratadine, by contrast, had equivalent transport in both directions and passive permeability was high (24 × 10(-6) cm/sec). Dimenhydrinate was the only other sedating antihistamine to exhibit efflux, with a ratio of 10. Gradient conditions of pH (6/7.4) increased efflux of terfenadine and desloratadine to over 31 and 38 fold respectively, yet this increased efflux was not associated with P-gp. Altering functional P-gp in the gut is likely to influence absorption of some sedating antihistamines such as dimenhydrinate and hydroxyzine and most less-sedating antihistamines except loratadine. In addition, desloratadine exhibits pH dependent efflux which could further induce variable absorption of this antihistamine.","is_dataset_classified":null,"base_score":3.58351893845611,"endowment":3.58351893845611,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"22188412","pmcid":null,"openalex_id":"https://openalex.org/W2007858153","authors":[],"funders":[],"total_grants":0,"fwci":0.3902,"citation_percentile":0.61703918,"influential_citations":0,"citation_trend":[{"year":2013,"count":3},{"year":2015,"count":2},{"year":2016,"count":1},{"year":2017,"count":5},{"year":2019,"count":1},{"year":2020,"count":7},{"year":2021,"count":4},{"year":2022,"count":5},{"year":2023,"count":2},{"year":2024,"count":3},{"year":2026,"count":2}],"oa_status":"green","license":"cc-by","oa_locations":[{"url":"https://figshare.com/articles/journal_contribution/The_impact_of_P-glycoprotein_mediated_efflux_on_absorption_of_11_sedating_and_less-sedating_antihistamines_using_Caco-2_monolayers/22912076","host_type":"repository"},{"url":"https://figshare.com/articles/journal_contribution/The_impact_of_P-glycoprotein_mediated_efflux_on_absorption_of_11_sedating_and_less-sedating_antihistamines_using_Caco-2_monolayers/22912076","host_type":"repository"},{"url":"http://www.tandfonline.com/doi/pdf/10.3109/00498254.2011.643256","host_type":"publisher"},{"url":"https://doi.org/10.3109/00498254.2011.643256","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/22188412","host_type":"repository"},{"url":"http://ecite.utas.edu.au/92571","host_type":"repository"},{"url":"http://hdl.handle.net/20.500.11937/24956","host_type":"repository"}],"fields_of_study":["Drug Transport and Resistance Mechanisms","Advanced Drug Delivery Systems","Neuropeptides and Animal Physiology","ATP Binding Cassette Transporter, Subfamily B, Member 1","Biological Transport","Caco-2 Cells","Cetirizine","Chromatography, High Pressure Liquid","Drug Interactions","Histamine H1 Antagonists","Humans","Hydrogen-Ion Concentration","Intestinal Absorption","Loratadine","Mass Spectrometry","Permeability","Terfenadine"],"mesh_terms":["Biological Transport","Chromatography, High Pressure Liquid","Drug Interactions","Histamine H1 Antagonists","Humans","Hydrogen-Ion Concentration","Intestinal Absorption","Permeability","Mass Spectrometry","Terfenadine","Cetirizine","Loratadine","Caco-2 Cells","ATP Binding Cassette Transporter, Subfamily B, Member 1"],"keywords":["Efflux","P-glycoprotein","Caco-2","Chemistry","Pharmacology","Biochemistry","In vitro","Medicine","Multiple drug resistance"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Clean water and sanitation"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-10T16:52:15.837274Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}