Pharmaceutical Sciences and Health Technologies 4.
Dr. Aljazmaty, Haya
XOUTUQ
Institute of Pharmacodynamics and Biopharmacy, University of Szeged
0036300102692
aljazmatyhaya@gmail.com
Investigation of Pregnancy-Induced Changes in Loratadine Pharmacokinetics Using a Rat Model
Dr. Haya Aljazmaty1, Prof. Gáspár Róbert2, Dr. Anita Sztojkov-Ivanov1
1: Institute of Pharmacodynamics and Biopharmacy, University of Szeged
2: Department of Pharmacology and Pharmacotherapy, Albert Szent-Györgyi Medical School, Faculty of Medicine, University of Szeged
Szóbeli
Pharmaceutical Sciences and Health Technologies 4.
English
Pharmaceutical Sciences and Health Technologies
Allergic diseases affect around one-third of pregnancies, frequently demanding antihistamine therapy. Pregnancy- induced physiological changes can modify drug pharmacokinetics (PK), potentially compromising both efficacy and safety. Despite the widespread use of loratadine, data on the disposition of the parent drug and its metabolite, desloratadine, during pregnancy remain limited. This study examines the PK alterations of loratadine and desloratadine in late pregnant rats and assesses fetal exposure.
A single oral dose (20 mg/kg) of loratadine was given to female Sprague-Dawley rats: non-pregnant controls and a gestation day 21 (GD21) group. Maternal and fetal blood samples were withdrawn at predetermined time points, and analytes concentrations were measured using a validated high-performance liquid chromatography (HPLC) method with UV detection, with a Phenomenex Luna 5 µm CN column. PK parameters were derived using PKSolver 2.0, GraphPad Prism 11 was used for statistics.
The PK profile of loratadine at GD21 was significantly altered versus controls, showing elevated plasma concentrations, increased area under the curve (AUC), diminished apparent oral clearance (CL/F), and an extended elimination half-life (t1/2). Desloratadine formation was markedly delayed at GD21, indicated by elevated loratadine concentrations and prolonged metabolite exposure. Both loratadine and desloratadine passed the placental barrier; nevertheless, fetal plasma concentrations remained lower than maternal ones.
The increased systemic exposure may be attributed to enhanced intestinal perfusion or altered transporter expression. As loratadine is primarily eliminated via hepatic metabolism, reduced CL/F likely reflects decreased hepatic metabolic capacity or transporter activity in late pregnancy. The delayed formation and prolonged exposure of desloratadine suggest altered metabolic conversion, supported by a temporal dissociation between loratadine and desloratadine profiles.
Eventually, these results underline the need for gestation-specific PK studies to optimize dosing and minimize maternal and fetal hazards.
Funding: supported by the Ministry of Culture and Innovation of Hungary from the National Research, Development and Innovation Fund, under TKP2021-EGA funding scheme.
University of Szeged
Prof. Gáspár Róbert, Dr. Anita Sztojkov-Ivanov
I do not give consent to the publication of my abstract on the website of the congress.
in doctoral studies after complex exam (PhD)
Szabad
elfogadva
szóbeli
nem rendelkezett róla
9771
17:00
17:10