Tripelennamine (citrate)

Tripelennamine citrate is a histamine H1-receptor antagonist. Tripelennamine citrate effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine citrate does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine citrate exhibits local and central analgesic activity. Tripelennamine citrate can be used in studies related to emphysema, urticaria and acute laminitis^[1][2][3]. In Vitro:Tripelennamine (1.0 μg/mL) citrate exhibits 83.4% protein binding in healthy Arabian camel serum and 73.6% protein binding in healthy horse serum, with no significant difference between the two species^[2]. In Vivo:Single administration of tripelennamine citrate (1.10 mg/kg; i.v.; 15 min prior to exercise) does not significantly alleviate exercise-induced arterial hypoxemia in exercise-trained thoroughbred horses during high-intensity exercise^[1].