Pharmacokinetics
This product is absorbed by oral administration at approximately 90% and by rectal administration at 70%. The pharmacological effect appears 20 to 30 minutes after oral administration, and the duration of action is 3 to 5 hours. The half-life of plasma is 8 to 11 hours. In the body tissues, this drug is mainly metabolized in the liver, and approximately 70% of the drug is eliminated through the kidneys.
In vitro study
Flupirtine blocks the death of cortical neuronal cells in rats induced by NMDA and gp120 HIV-1. When the concentration of Flupirtine is 1-10 mM, it protects primary nerve cells from the toxicity induced by sodium glutamate by reducing the concentration of calcium ions. When the concentration of Flupirtine is 1 or 5μg/mL, it acts on primary neuronal cells and blocks the apoptosis induced by β -amyloid protein (25-35). When Flupirtine at a concentration of 10 μM was applied to PC 12 culture treated with 10 mM L-glutamic acid, it significantly reduced the death of non-receptor-regulated necrotic cells. Meanwhile, Flupirtine acting on PC 12 culture had an antioxidant effect. When the concentration of Flupirtine was 1 μM and 10 μM, it reduced the death of human living brain tissue cultures regulated by TRAIL. Flupiratin activates the inward rectifying potassium ion channels, thereby stabilizing the resting membrane potential at the treatment-related concentration.