Fluphenazine , dosing

Fluphenazine 1.2 x oral fluphenazine daily dose, Based on starting dose and Can be administered IM or SC ... 

Midha, K. K. et al. (1988a). Variation in the single dose pharmacokinetics of fluphenazine in psychiatric patients. Psychopharmacology, 96, 206-11. 

For fluphenazine decanoate, an esterified formulation in sesame seed oil, the simplest conversion is the Stimmel method, which uses 1.2 times the oral daily dose for stabilized patients, rounding up to the nearest 12.5-mg interval, administered IM in weekly doses for the first 4 to 6 weeks (1.6 times the oral daily dose for patients who are more acutely ill). Subsequently, fluphenazine decanoate may be administered once every 2 to 3 weeks. Oral fluphenazine may be overlapped for 1 week. 

A side effect, dystonia of the neck muscles, often appeared after the higher doses of 302034 or fluphenazine, usually about 12-16 hours following administration. (This was quickly relieved by 50 mg of Lm benadryl.) Slopes of the dose-response curves were... 

Fluphenazine should be initiated at 5 mg/day to treat schizophrenia and increased as needed. The depot form is administered every 2 weeks in doses from 6.25 to 50mg per dose. The depot form is generally believed to cause less EPS however, some physicians have raised the concern that depot fluphenazine may be prone to dose dumping. Dose dumping means that a significant portion of the depot dose might be prematurely released into the bloodstream. 

Like fluphenazine, haloperidol is available in oral, injectable, and depot forms. In schizophrenia, haloperidol is begun at doses of 5 mg daily and increased as needed. Lower doses are used for most other indications. The depot form of haloperidol is initiated by administration of a 50mg test dose. Depot haloperidol is given monthly at about 20 times the daily dose of the oral form. The maximum depot dose is 200 mg per month. Dose dumping does not seem to be a problem with depot haloperidol. 

Typical Antipsychotics. Low doses of high potency typical antipsychotics such as haloperidol or fluphenazine (0.5-2mg given once or twice daily) are generally quite effective for psychotic symptoms after TBI. Unfortunately, as noted earlier, many post-TBl patients are susceptible to the extrapyramidal side effects of these medicines, especially if there was any injury to brain regions such as the basal ganglia. Low potency antipsychotics are not a viable alternative, because their anticholinergic and sedative effects are equally, if not more, problematic for patients who have suffered TBI. We recommend using typical antipsychotics, even for psychotic symptoms, as briefly as possible and in the lowest effective dose, if at all. Fortunately, there are now alternatives. 

FLUPHENAZINE HYDROCHLORIDE Individualize dosage. The oral dose is approximately 2 to 3 times the parenteral dose. Institute treatment with a low initial dosage increase as necessary. Therapeutic effect is often achieved with doses... 

Poor risk patients - In poor risk patients (known phenothiazine hypersensitivity or with disorders predisposing to undue reactions), cautiously initiate oral or parenteral fluphenazine. When appropriate dosage is established, give equivalent dose of fluphenazine decanoate. 

Fluphenazine (Prolixin, Permitil) [Antipsychotic/ Phenothiazine] Uses Schizophrenia Action Phenothiazine antipsychotic blocks postsynaptic mesolimbic dopamin gic brain receptors Dose 0.5-10 mg/d in % doses PO q6-8h, av age maint 5 mg/d or 1.25 mg IM, then... 

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. 

A high risk of relapse is inherent to schizophrenic psychoses. A relapse is often triggered by emotional stress. It is very important to prevent a relapse by either maintaining low-dose oral medication or by switching to a depot antipsychotic. In some cases, this cannot be avoided. Especially when compliance is a problem, a depot medication may help to keep the patient free of psychotic symptoms. Frequently used depot antipsy-chotics are haloperidol-decanoate, fluphenazine-decanoate, and fluspirilene, which are given in relatively low dosages (see Table 41.4). In EOS, relapse prevention is more important than in adulthood, as the majority of patients have not yet finished school or started a professional career. 

Most conventional antipsychotics are associated with a dose-depen-dent risk of a lowered seizure threshold, although the incidence of seizures with most of these drugs is quite small (Devinsky et al. 1991). Of all the conventional antipsychotics, molindone and fluphenazine have been shown most consistently to have the lowest potential for this side effect (ltd and Soldatos 1980 Ohver et al. 1982). The atypical antipsychotic clozapine is associated with a dose-dependent risk of seizure. 

Fluphenazine enanthate and decanoate are similar in potency, efficacy, and adverse effects. They differ only in that the decanoate preparation is slightly more potent and slightly longer acting, requiring lower doses and less frequent administrations. Because the decanoate form manifests marginally fewer adverse effects, it is probably preferable. 

Fluphenazine decanoate may cause more acute EPS than haloperidol decanoate due to a phenomenon known as dose dumping. Here, a small amount of depot formulation is released into the systemic circulation shortly after an injection. There may be a tendency for haloperidol to be more effective for a subset of schizophrenic symptoms, less depressogenic, and slightly less likely to exacerbate extrapyramidal symptoms. These effects, however, are not large, may not be clinically significant, and are not consistently evident in all studies. 

Lower potency neuroleptics, such as thioridazine and chlorpromazine, have a decreased incidence of EPS when compared with higher potency agents, such as haloperidol or fluphenazine. Novel agents, such as clozapine and quetiapine, are virtually devoid of EPS effects when given at their recommended dosing range. 

Marder SR, Van Putten T, Mintz J, et ai. Low- and conventional-dose maintenance therapy with fluphenazine decanoate. Two-year outcome. Arch Gen Psychiatry 1987 44 518-521. 

Hogarty GE, McEvoy JP, Munetz M, et ai. Dose of fluphenazine, familial expressed emotion, and outcome in schizophrenia. Results of a two-year controlled study. Arch Gen Psychiatry 1988 45 797-805. 

Weizman A, Tyano S, Wijsenbeek H, et al. High dose diazepam treatment and its effect on prolactin secretion in adolescent schizophrenic patients. Psychopharmacology 1984 82 382-385. Wolkowitz OM, Breier A, Doran A, et al. Alprazolam augmentation of the antipsychotic effects of fluphenazine in schizophrenic patients. Arch Gen Psychiatry 1988 45 664-671. 

If these measures fail, clonidine, fluphenazine, clonazepam, or carbamazepine should be tried. The pharmacologic properties of these drugs are discussed elsewhere in this book. Clonidine reduces motor or vocal tics in about 50% of children so treated. It may act by reducing activity in noradrenergic neurons in the locus coeruleus. It is introduced at a dose of 2-3 mcg/kg/d, increasing after 2 weeks to 4 mcg/kg/d and then, if required, to 5 mcg/kg/d. It may cause an initial transient fall in blood pressure. The most common adverse effect is sedation other adverse effects include reduced or excessive salivation and diarrhea. Phenothiazines such as fluphenazine sometimes help the tics, as do dopamine... 

Well-tolerated parenteral forms of the high-potency older drugs haloperidol and fluphenazine are available for rapid initiation of treatment as well as for maintenance treatment in noncompliant patients. Since the parenterally administered drugs may have much greater bioavailability than the oral forms, doses should be only a fraction of what might be given orally, and the manufacturer s literature should be consulted. Fluphenazine decanoate and haloperidol decanoate are suitable for long-term parenteral maintenance therapy in patients who cannot or will not take oral medication. 

Flupenthixol and procyclidine Fluphenazine Prednisone and salbutamol Betal nut (Areca catechu) Rigidity, bradykinesia, jaw tremor Betal contains arecoline, a cholinergic alkaloid Tremor, stiffness, akithesia Inadequate control of asthma Arecoline challenge causes dose-related bronchoconstriction in patients with asthma... 

CPZ (9), triflupromazine (11), and fluphenazine (3) inhibited HIT-T15 pancreatic (3-cell ATP-sensitive potassium channels in a dose-dependent manner [254], Reversible inhibition of these channels was observed when they were activated by ATP depletion or by treatment with the channel opener diazoxide. The IC50 values for CPZ (9), triflupromazine (11), and fluphenazine (3) were 1, 4, and 6 xM, respectively. 

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