Trifluoperazine formation

Chlorpromazine produces a tranquihty characterized by a detached serenity without depression of mental faculties or clouding of consciousness. It depresses the CNS selectively by reducing input directed to the reticular formation through collaterals arriving from the sensory pathways. Chlorpromazine-induced sedation differs from that caused by barbiturates in that the patient can be easily aroused. In practice, the more sedative neuroleptics are often prescribed for agitated, overactive patients, and the less sedative agents are used for apathetic, withdrawn patients. However, sedation is not necessary for its antipsychotic property for two reasons (1) tolerance develops to the sedative effects, and (2) fluphenazine, prochlorperazine, and trifluoperazine are excellent neuroleptics that lack pronounced sedative effects. 

McLean and coworkers have reported that inhibitors of MPT (cyclosporine A and trifluoperazine) inhibited acetaminophen toxicity in rat liver slices and in vivo when administered as a cocktail with fructose (Beales and McLean 1996 Nieminen et al. 1997). Also, Dimova et al. (1995) reported that the MPT inhibitor trifluoperazine decreased acetaminophen-induced hepatotoxicity in the mouse. Masubuchi et al. (2005) reported that Cyclosporine A decreased acetaminophen toxicity in mice. Since hepatic glutathione depletion was the same in acetaminophen-treated and acetaminophen plus cyclosporine A-treated mice, it was concluded that the decrease in toxicity was not mediated by inhibition of NAPQI formation. Moreover, they observed that acetaminophen caused a swelling of liver mitochondria and a decrease in mitochondrial membrane potential, both of which were elinrinated by cotreatment with Cyclosporine A. Collectively, the data indicate that MPT is an important mechanism leading to acetaminophen toxicity. 

Carboxyl group clofibrate, ciprofibrate, etodolac, fenoprofen, ibuprofen, ketoprofen, naproxen (racemic > 5), valproic acid and formation of simvastatin and atorvastatin lactones via an intermediate acyl glucuronide Tertiary amines amitriptyline, chlorpheniramine, chlorpromazine, clozapine, cyproheptadine, diphenylamine, doxepin, imipramine, ketotifen, loxapine, promethazine, tripellenamine, trifluoperazine Aromatic heterocyclic amines croconazole, lamotrigine, nicotine (30X velocity than UGT1A3), 1-phenylimidazole, posaconazole, retigabine Primary and secondary amines ... 

In common with findings with other phenothiazines, sulfoxide formation occurs during trifluoperazine metabolism ... 

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