Disease relevance of Emergil

• A prospective study was undertaken on 374 out-patients receiving depot fluphenazine or depot flupenthixol to determine the incidence of tardive dyskinesia [1].
• Six additional cases of generalized chorea were all receiving flupenthixol [1].
• 1. A number of controlled as well as uncontrolled studies indicate that flupenthixol in a low-dose regimen is effective in treating syndromes with depression, anxiety, and psychosomatic disorders [2].
• Flupenthixol augmented the duration of the lordosis posture [3].
• In contrast to the hypothesis, flupenthixol did not reduce, but was associated with more, relapses [4].

Psychiatry related information on Emergil

• No evidence was found that flupenthixol is specifically useful in "activating" chronic patients or in alleviating affective symptoms [5].
• A double-blind cross-over trial of depot flupenthixol in recurrent manic depressive psychosis was carried out [6].
• Acute and maintenance ECT with flupenthixol in refractory schizophrenia: sustained improvements in psychopathology, quality of life, and social outcomes [7].
• Behavioral effects produced by long-term administration of a neuroleptic drug (flupenthixol) upon social interaction in a group of eight rats [8].
• In an open, uncontrolled trial flupenthixol was administered to 45 patients with endogenous depression [9].

High impact information on Emergil

• Ten outpatient crack cocaine smokers with poor prognoses were administered flupenthixol decanoate in an open-label, open-ended trial [10].
• The stereoselective antagonism of the flupenthixol isomers on several putative cellular targets was studied to explore the mechanism of their chemosensitizing activity. cis- and trans-flupenthixol were equally active inhibitors of protein kinase C and calmodulin [11].
• Drug substrates that either enhance (calcein acetoxymethyl ester, demecolcine, and vinblastine) or inhibit (cyclosporin A and trans-(E)-flupentixol) ATPase activity of Cys-less or untreated mutant I306C P-glycoprotein did not affect the activity of MTS-verapamil-treated mutant I306C [12].
• The neuroleptic flupenthixol reduces the expression in rats of the gene coding for NADH-cytochrome b5 reductase as measured by in situ hybridisation and its enzymic manifestation [13].
• Moreover, drug resistance of KB-8-5 epidermoid cancer cells, which express the wild-type MDR1 gene at levels comparable to clinical specimens from multidrug-resistant cancers, was fully overcome in the presence of trans-(E)-flupentixol [14].

Chemical compound and disease context of Emergil

• Amisulpride 400 to 800 mg/day was more effective than haloperidol, risperidone and flupenthixol in controlling affective symptoms in these patients [15].
• A double-blind trial of flupenthixol, nortriptyline and diazepam in neurotic depression using flexible dose schedules suggested that each drug is an efficient treatment for this category of depression although the patterns of response and prevalence of side-effects varied [16].
• Efficacy and tolerability of flupenthixol decanoate in the treatment of depression and psychosomatic disorders: a multicenter trial in general practice [2].
• Psychosomatic disorders in general practice: comparisons of treatment with flupenthixol, diazepam and sulpiride [17].
• Twelve patients with trigeminal neuralgia were treated with a daily dose of 2 mg Melitracen and 40 mg Flupenthixol [18].

Biological context of Emergil

• Flupenthixol did not have any effect on food intake [19].
• The present review analyses the available data on the kinetics and metabolism of fluphenazine, perphenazine, thiothixene, flupenthixol, clopenthixol, haloperidol, pimozide, penfluridol, sulpiride and clozapine [20].
• Regardless of whether the specific binding of [3H]-S-sulpiride was defined with spiperone or the active isomers of butaclamol or flupenthixol, a single homogeneous++ population of binding sites (rat: Kd = 5.6 nM, maximum binding = 590 fmol/mg of protein; rabbit: Kd = 8.3 nM, maximum binding = 540 fmol/mg of protein) was detected [21].
• Stereospecific effect of flupenthixol on neuroreceptor gene expression [22].
• A double-blind crossover trial was carried out in the general practice to compare the effectiveness of flupenthixol and placebo in 43 patients with mild to moderate anxiety/depression states [23].

Anatomical context of Emergil

• In the presence of 2 microM trans-(E)-flupentixol chemoresistance to daunomycin was circumvented only in K562 cells transduced with wild-type, but not with mutant, MDR1 [14].
• The number of nerve cells in two different areas of the corpus striatum (i.e., ventrolateral and dorsomedial) was estimated in rat brain after long-term (36 weeks) treatment with the neuroleptic flupenthixol [24].
• The actions of flupenthixol upon 5-hydroxytryptamine-induced aggregation and the uptake of 5-hydroxytryptamine and dopamine by human blood platelets [25].
• Opposite effects of prefrontal cortex and nucleus accumbens infusions of flupenthixol on stimulant-induced locomotion and brain stimulation reward [26].
• Flupenthixol also antagonized the facilitative effects of apomorphine injections into the medial preoptic area [27].

Associations of Emergil with other chemical compounds

• Sixty-eight depressed out-patients were allocated to treatment with either oral amitriptyline (75-225 mg/day) or intramuscular flupenthixol decanoate (10-30 mg every 14 days) in flexible dosage for 12 weeks under double-blind procedures [28].
• Depressive and extrapyramidal symptoms and clinical effects: a trial of fluphenazine versus flupenthixol in maintenance of schizophrenic out-patients [29].
• To test this hypothesis, in experiment 1, schizophrenic outpatients receiving haloperidol or flupenthixol and matched controls were tested on tasks involving incentive or s-s learning [30].
• 3-Methoxy-4-hydroxyphenylglycol excretion in acutely schizophrenic patients during a controlled clinical trial of the isomers of flupenthixol [31].
• Similarly, intra-NAS flupenthixol or SCH 23390 attenuated the analgesia induced by intra-VTA DiMe-C7 [32].

Gene context of Emergil

• Flupenthixol treatment initially raised the prolactin levels about two- or threefold, and a subsequent decline during months 3 and 6 occurred [33].
• We report here that retroviral vectors encoding a mutant P-glycoprotein (MDR1-F983A) protect hematopoietic cells from anticancer drugs even in the presence of trans-(E)-flupentixol, an inhibitor of P-glycoprotein [14].
• Forty-five patients with acute schizophrenic illnesses (defined by PSE criteria) were assessed in clinical, cognitive and social terms before being entered in a four week study of the isomers of flupenthixol and placebo [34].
• CONCLUSION: ECT and MECT combined with flupenthixol were effective in improving psychopathology in patients refractory to antipsychotic medication alone [7].
• Effect of flupenthixol and butaclamol isomers on prolactin secretion in rats [35].

Analytical, diagnostic and therapeutic context of Emergil

• Radioimmunoassay for flupenthixol in plasma [36].
• The combination of flupenthixol (0.018 mg/kg/day) + quadazocine (0.18 mg/kg/day) significantly reduced speedball self-administration in comparison to the saline treatment baseline (p < .05), whereas, the same doses of each antagonist alone had no significant effect on speedball-maintained responding [37].
• The efficacy of pharmacotherapy in reducing suicide attempts in patients with a history of repeated suicidal behavior has been shown with low doses of the neuroleptic agent flupenthixol compared with placebo [38].
• Thorough neurological examinations of the animals just preceeding the retesting period also revealed some deficits in the flupenthixol-treated animals [39].
• Comparative double-blind study of flupenthixol decanoate and fluphenazine decanoate in the treatment of patients relapsing in a schizophrenic symptomatology [40].

References