Trifluoperazine effects

The multidrug resistance (mdr) reversing effect of the new phenothiazine complexes were tested on mouse T cell lymphoma cell lines. Trifluoperazine (TFP) was much more effective at the same concentration than verapamil. The efficacy of some metal coordination complexes [TFP-Cu(ll) and TFP-V(IV)] exceeded the action of TFP alone. Chlorpromazine (CPZ) or CPZ-Pt(ll) complex had the same or less effect than verapamil or promethazine (Pz) used as a control. 

Whatever the underlying causes may be, neuroleptic medications are the most effective treatment for schizophrenia. All antipsychotic medications have some form of dopamine receptor antagonism and they are distinguished by their chemical class. The phenothiazines include chlorpromazine (Thorazine), thioridazine (Mellaril), mesoridazine (Serentil), trifluoperazine (Stelazine), fluphenazine (Prolixin), and prochlorperazine (Compazine). The thioxanthenes include chlorprohixine (Taractan) and thiothixene (Navane). Butyrophenones are represented by haloperidol (Haldol). Loxapine (Loxitane) is a dibenzoxapine, and molindone (Moban) is a dihydroindolone. 

Trifluoperazine is one of the most active antipsychotic drugs. A moderate stimulatory effect accompanies the neuroleptic effect. Trifluoperazine is unique in that, patients instead of the usual stiffness and weakness characteristic of phenothazine derivatives, become more lively. This drug has a strong anticonvulsant activity. It is widely used in psychiatry for treating schizophrenia and other mental illnesses. The most common synonyms are mobadid, triftazin, stelazine, cahnazin, and others. 

TRIFLUOPERAZINE Individualize dosage. Increase dosage more gradually in debilitated or emaciated patients. When maximum response is achieved, reduce dosage gradually to a maintenance level. Use the lowest effective dosage. Patients may be controlled with once- or twice-daily administration. 

Bernacchi AS, Fernandez G, Villarruel MC, et al. 1988. Further studies on the late preventive effects of the anticalmodulin trifluoperazine on carbon tetrachloride-induced liver necrosis. Exp Mol Pathol 48 286-300. 

The piperazines include fluphenazine, trifluoperazine, prochlorperazine, perazine and perphenazine. They are agents with a high antipsychotic potency with less pronounced anticholinergic effects. However their potential to produce extrapyramidal effects is more pronounced. 

A variety of relatively uncommon dermatological side effects have been noted to be associated with antipsychotic agents. These include maculopapular rashes, urticaria, and erythema multiforme (Arana, 2000). Photosensitivity and skin pigmentation can also occur during treatment with these drugs. Although skin pigmentation has been most frequently reported with chlorpromazine, this can occur with thioridazine and trifluoperazine (Harth and Rapoport, 1996). In addition, treatment-induced alopecia has been reported for haloperidol, olanzapine, and risperidone (Mercke et ah, 2000). 

Fluphenazine, a typical neuroleptic of the phenothi-azine class, has been less widely used for treatment of tics than haloperidol or pimozide. A controlled trial of haloperidol, fluphenazine, and trifluoperazine found comparable tic-reducing efficacy, but greater sedation and extrapyramidal side effects for haloperidol fluphenazine was the best tolerated (Borison et al., 1982). In an open-label trial with 21 subjects who had an unsatisfactory response to haloperidol, fluphenazine had a superior side effect profile to that of haloperidol in the dose range employed (mean dose of fluphenazine, 7 mg/day, range 2-15 mg/day) (Goetz et al., 1984). In this group selected for an unsatisfactory response to haloperidol, 11 of the 21 subjects (52%) had a better response to fluphenazine than haloperidol, 6 subjects had a comparable response, and 2 subjects preferred haloperidol. 

TABLE 5-10. Effectiveness of other neuroleptics compared with chlorpromazine, thioridazine, and trifluoperazine... 

Further, it is best to start with a very low dose and titrate up slowly in a hospital setting to carefully monitor clinical response, temperature, and neurological and mental status. Using low doses will not necessarily jeopardize chances for an adequate clinical response. We found, for example, evidence for a therapeutic effect with low-dose trifluoperazine (285). This finding is consistent with the growing recognition that less may indeed be more when it comes to the dose of an antipsychotic. 

Trifluoperazine has potent anti-emetic effects but also causes marked sedation and extrapyramidal effects and is not used commonly as an anti-emetic. 

The neuroleptics that are widely available may be divided into two general categories, those with low potency (such as chlorpromazine and thioridazine) and those with high potency (exemplified by haloperidol, trifluoperazine and pimozide). The former groups have a lower propensity to cause extrapyramidal side effects but are more sedative and likely to cause postural hypotension and have anticholinergic side effects. In vitro studies have shown that chlorpromazine has an affinity for all five types of dopamine receptor and has some preference for D2 and D3 receptors. By contrast, haloperidol is more potent than chlorpromazine for the D2, D3 and D4 receptors with a low affinity for the D and D5 receptors. 

Piperazine compounds, such as trifluoperazine or fluphenazine, are the most selective dopamine receptor antagonists. They have the least sedating action and they are the most likely producer of extra pyramidal effects. 

Table 15 Effect of trifluoperazine on survival of mice challenged with Salmonella ty-phimurium...

Mucsi et al. [78] reported that trifluoperazine, chlorpromazine, and promethazine were effective against herpes simplex virus. Certain benzo[a]-phenothiazines also produced identical results against herpes virus [78]. Some structurally related phenothiazines exhibited photodynamic activity against the pseudorabies virus [33]. The inhibitory effect of the phenothiazines was investigated on the multiplication of several viruses. 

Itil TM, Polvan N, Ucok A, Eper E, Guven F, Hsu W. Comparison of the clinical and electroencephalographical effects of molindone and trifluoperazine in acute schizophrenic patients. Behav Neuropsychiatry 1971 3(5) 25-32. 

INDIRECT ANTIPSYCHOTICS 1. Case reports of paralytic ileus with trifluoperazine and methylphenidate 2. Case report of acute dystonias with haloperidol and dexamfetamine 3.1 efficacy of chlorpromazine when dexamfetamine was added 1. Additive anticholinergic effect 2. Uncertain possibly due to t dopamine release 3. Uncertain 1. Watch for signs of altered bowel habit 2. Warn patients of this rare interaction 3. Avoid co-administration... 

However, long-term polypharmacy with a combination of a conventional antipsychotic such as trifluoperazine with an atypical antipsychotic may combine their side effects without clearly augmenting the efficacy of either... 

Holmsen H, Daniel JL, Dangelmaier CA. Molish I, Rigmaiden M, and Smith JB. (1984). Differential effects of trifluoperazine on arachidonate liberation, secretion and myosin jdiosphotylation in intact platelets. Thromb. Res. 36,419-428. 

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