Résumé
The optimal treatment of schizophrenia poses a challenge to develop more effective treatments and safer drugs, to overcome poor compliance, discontinuation and frequent switching with available antipsychotics. Iloperidone is a new antipsychotic developed to overcome some of the limitations in the drug treatment of schizophrenia. It has been approved by regulating agencies for use in treatment of adult schizophrenia.
Sujets)
Adulte , Neuroleptiques/pharmacocinétique , Neuroleptiques/usage thérapeutique , Humains , Isoxazoles/analogues et dérivés , Isoxazoles/pharmacocinétique , Isoxazoles/usage thérapeutique , Pipéridines/analogues et dérivés , Pipéridines/pharmacocinétique , Pipéridines/usage thérapeutique , Schizophrénie/traitement médicamenteuxSujets)
Humains , Pipérazines/administration et posologie , Pipérazines/analogues et dérivés , Pipérazines/pharmacocinétique , Pipérazines/pharmacologie , Pipérazines/administration et posologie , Pipéridines/analogues et dérivés , Pipéridines/pharmacocinétique , Pipéridines/pharmacologie , Pipéridines/usage thérapeutique , Schizophrénie/traitement médicamenteuxRésumé
Multidrug resistance [MDR] was circumvented by a large number of compounds including verapamil and a newly synthesized triazinoaminopiperidine derivative S9788 [Servier 9788]. S9788 was found to overcome multidrug resistance both in vitro and in vivo. The mode of action of these chemosensitizers is thought to involve interaction on P-glycoprotein, a membrane-bound efflux transport protein for cytotoxic drugs. On the other hand, verapamil binds strongly to alpha 1-acid glycoprotein [AGP] in serum or solutions and AGP can modulate the chemosensitizing action of verapamil in MDR in vitro. The interaction of S9788 with [3H] vincristine was measured at binding sites on alpha 1-acid glycoprotein in vitro using equilibrium dialysis [Dianorm] and clinically relevant concentrations of ligands and protein