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PubMed1989

The heterogeneity of 3-methoxy-4-hydroxyphenylglycol levels among depressed patients.

A previous report by our group and results published by other research groups have indicated a dichotomy in MHPG levels in depressed patients. This study attempted to characterize phenomena associated with this dichotomy in plasma MHPG levels. First, we have noted, at least in female patients, that homogeneity of MHPG levels, as tested by fitting with a normal curve, can be ruled out. In contrast, in the total population, a dichotomy was less evident in this study; the 2 subgroups, high and low levels of MHPG, partially overlap, and this results in a gaussian distribution. However, based on the hypothesis of a bimodal distribution, as shown by others and not excluded here, it was possible to find some factors associated with heterogeneity. Thus, polarity of depression, sex and age of the patients, age of disease onset and depression score affect MHPG levels. On the other hand, other elements suspected to modify MHPG values, such as the different lengths of the washout period (minimum 10 days), or some medication (chloralhydrate or levomepromazine) required during the washout period, did not show any effect. The aim of this study was to better characterize this peripheral index for its possible use in clinical application.

Adult↗

PubMed1994

Medicine self-poisoning and the sources of the drugs in Lund, Sweden.

The purpose of this study was to investigate the prevalence of toxic agents in attempted and completed suicides. The purpose was also to explore the sources of the drugs taken by suicide attempters. Verbal information on drug intake was collected from 280 suicide attempters during 1987-1990 in the Lund-Orup catchment area. Information on the sources of the drugs was collected from 143 of these attempters. The study also includes toxicological screening from 73 fatal poisonings in southern Sweden during 1989. According to verbal information, the most common drugs used by suicide attempters were benzodiazepines (51%), analgesics (29%) and antidepressants (20%). In suicide attempters, diazepam and levomepromazine were reported more than expected from prescription data. Toxicological screenings of fatal poisonings showed that benzodiazepines were most common (55%), followed by analgesics (38%), mainly propoxyphene (29%) and antidepressants (30%), mainly amitriptyline (22%). Amitriptyline and diazepam were more commonly detected in completed suicides than expected from prescription data. The most common sources of drugs to attempted suicides were physicians, and especially psychiatrists. We therefore conclude that continuous information to physicians on drug overdose is important, and it is also important to introduce alternative strategies to prevent suicidal behaviour.

Adolescent↗

PubMed1995

Long-term treatment of mood disorders in schizophrenia.

Mood disorders in schizophrenia are common and are associated with a poor outcome, an increased risk of relapse and a high rate of suicide. Consequently, treatment strategies need to take mood disorders into account. In depressed and actively psychotic schizophrenic and schizoaffective patients, treatment with neuroleptic plus antidepressant may be less effective than neuroleptic alone. However, patients with post-psychotic depression on maintenance neuroleptics respond well to tricyclic antidepressants. Mood disorders can be caused by neuroleptics and if so will often improve if the dose is reduced or if the drug is changed. Anticholinergics may also help. In schizoaffective disorder, lithium is usually beneficial, especially for patients with classical affective disorder. Carbamazepine may be more effective in patients with schizoaffective and schizophreniform disorders. At doses comparable with those effective in schizophrenia, clozapine may be as good or better than conventional neuroleptics in schizophrenic patients with psychotic mood disorder or schizoaffective disorder. In patients with high BPRS anxiety/depression scores, risperidone (8 mg/day) was more effective than haloperidol (10 mg/day). Risperidone at a mean dose of 8.6 mg/day was also more effective than haloperidol (mean dose 9.2 mg/day) or levomepromazine (methotrimeprazine -- mean dose 125 mg/day) on the Psychotic Anxiety Scale. Mood-related symptoms are therefore amenable to treatment. Risperidone and clozapine appear to be good candidates for the long-term treatment of mood disorders in schizophrenia, although long-term, double-blind, controlled studies are needed to confirm this.

Affective Symptoms↗

PubMed1985

The antibacterial effect of selected neuroleptics on Vibrio cholerae.

The present investigation has been undertaken to illustrate the anti-bacterial effect of chlorpromazine, clopenthixol and levomepromazine-maleate. It has been shown that clopenthixol has the strongest antibacterial effect. It is known that chlorpromazine also has an antisecretory activity. The fact that clopenthixol exists in cis(Z)- and trans(E)-isomerical compounds, and that these compounds both have an antibacterial effect, but only the cis-compound has an antisecretory and neuroleptic effect, might suggest the development of more specific pharmaceuticals in these new fields.

Antipsychotic Agents↗

PubMed1986

The antibacterial effect of selected phenothiazines and thioxanthenes on slow-growing mycobacteria.

The aim of the present investigation was to illustrate the antibacterial effect of various phenothiazine and thioxanthene derivatives on mycobacteria in vitro. It was demonstrated that clopenthixol is about twice as potent as chlorpromazine (CPZ) and levomepromazine-maleate is about half as potent as CPZ, measured by the inhibitory effect on the growth of the mycobacterial strains. Measured in the same way the stereoisomeric compounds of flupenthixol are shown to be more potent than the stereo-isomeric compounds of clopenthixol and chlorprothixen. The two last-named compounds are equal in potency. The stereo-isomeric analogs of the thioxanthene derivatives are equal in antibacterial potency against the slow-growing mycobacteria. The mycobacterial strains investigated show no difference in sensitivity between the cis (Z)--and and trans (E)--compounds of the thioxanthenes. It seems particularly promising that also the more resistant mycobacteria other than Mycobacterium tuberculosis, e.g. M. avium and M. intracellulare, are sensitive in the concentration range investigated. Considered as a whole, these results might be a stimulus to investigate the antimicrobial effect of the thioxanthenes in vivo.

Anti-Bacterial Agents↗

PubMed2000

Dopamine D3 receptor binding by D3 agonist 7-OH-DPAT (7-hydroxy-dipropylaminotetralin) and antipsychotic drugs measured ex vivo by quantitative autoradiography.

Because the dopamine D3 receptor is primarily expressed in regions of the limbic system of brain, it was proposed that it may represent a target for antipsychotic drugs that is free of extrapyramidal side effects. An ex vivo receptor binding technique employing [3H]7-OH-DPAT was used to evaluate in vivo occupancy of dopamine D3 receptors in the rat nucleus accumbens by selective D3 agonist 7-OH-DPAT (7-hydroxy-dipropylaminotetralin) and various antipsychotic drugs. With an ID50 value of 0.07 mg/kg, the selective D3 agonist (+)-7-OH-DPAT had the most potent inhibitory effect on ex vivo binding of [3H]7-OH-DPAT among all drugs tested. Clinical doses of phenothiazine drugs, such as chlorpromazine and levomepromazine, induce binding to D3 receptors in vivo, while atypical antipsychotic drugs, such as clozapine, pimozide, and sulpiride, are very weak in inhibiting ex vivo binding of [3H]7-OH-DPAT, indicating that the role of D3 receptors as targets of antipsychotic drugs free of extrapyramidal side effects may not be important.

Animals↗

PubMed1996

Amantadine versus biperiden: a double-blind study of treatment efficacy in neuroleptic extrapyramidal movement disorders.

Anticholinergic treatment of neuroleptic extrapyramidal movement disorders (EPS) has been associated with induction of tardive dyskinesia. Also an increasing abuse of anticholinergics by schizophrenic patients is noted. Since as early as 1976, positive effects of amantadine (AMA) on neuroleptic EPS have been described, therefore a controlled study of these reports seemed worthwhile. Forty-two schizophrenic patients (of which 7 were dropouts) of three centers entered the study and were treated for EPS in a double-blind design: 18 (11 m, 7 f) with AMA and 17 (8 m, 9 f) with biperiden (BIP). Identical preparations of AMA 100 mg, tid) and BIP (2 mg, tid) were used in treatment of haloperidol-induced EPS (AMA, mean 22.4 mg haloperidol; BIP, mean 19.6 mg haloperidol). Effects of treatment and possible side effects were rated: EPS for the intensity of EPS, BPRS for quantification of psychotic symptoms, FSUCL for rating the side effects and KUSTA to document patients' mood. Ratings were recorded on days 0, 3, 7, 14, 28 and at discontinuation, respectively. All patients were treated with haloperidol and levomepromazine (for tranquilization/sleep induction) and the respective antiparkinsonian agent for 14 days. Patient characteristics did not differ significantly in either groups. In the AMA treatment group, 2 patients dropped out for noncompliance, in the BIP group, 5 (3 no effect, 1 noncompliance, 1 agitation). All results as recorded with the different rating instruments showed a significant (p < 0.01) overall improvement, whereas no significant differences between treatment groups could be determined, notably the treatment effect of both drugs on EPS was similar. Thus, the application of AMA in cases of neuroleptic EPS seems justified and is a useful alternative of anticholinergic drugs. Certain advantageous aspects of AMA treatment of EPS with regard to the glutamate hypothesis of schizophrenia and tardive dyskinesia are discussed.

Amantadine↗

PubMed1977

The different influence of predominantly antiadrenergic and antidopaminergic neuroleptics on the estrous cycle in rats.

In experiments performed on rats, single subcutaneous doses of predominantly antidopaminergic neuroleptics (fluspirilene, pimozide, and thioproperazine in large doses) elicited persistent diestrus, i.e. pseudopregnancy. Neuroleptics with predominantly antiadrenergic action (levomepromazine, thioridazine, chlorpromazine) as well as phenoxybenzamine injected intraventricularly induced mainly prolonged estrus, i.e. blocking of ovulation. Since pseudopregnancy implies a rise of prolactin secretion, our results indirectly indicate that PIF secretion is stimulated by dopamine. The antiovulatory effect of the antiadrenergic agents, which involves an inhibition of the proestral LH surge, suggests that the discharge of LRF is mediated by an adrenergic mechanism.

Animals↗

PubMed1997

Phototoxic properties of neuroleptic drugs.

BACKGROUND: Photo-induced eruptions are well-known adverse effects of some neuroleptic drugs, particularly chlorpromazine. OBJECTIVE: By a photohemolysis test we assessed in vitro the phototoxic properties of 12 phenothiazines (chlorpromazine, dixyrazine, fluphenazine, levomepromazine, perazine, perphenazine, promazine, promethazine, prothipendyl, thioridazine, trifluoperazine, triflupromazine) and 5 thioxanthenes (chlorprothixene, clopenthixol, flupenthixol, thiothixene, zuclopenthixol). METHODS: Human erythrocytes from 3 donors were incubated with the compounds and irradiated with light sources rich in UVA or UVB, respectively. Doses were up to 100 J/cm2 UVA or up to 1,600 mJ/cm2 UVB. Photo-induced hemolysis was calculated as percentage of complete hemolysis. RESULTS: Photo-induced hemolysis >10% due to radiation rich in UVA was found with chlorpromazine (maximal median: 98%), dixyrazine (100%), fluphenazine (84%), perazine (100%), perphenazine (100%), promazine (16%), promethazine (25%), prothipendyl (96%), trifluoperazine (100%), triflupromazine (76%), chlorprothixene (100%) and thiothixene (31%). UVB-rich radiation induced hemolysis only with chlorpromazine (73%), dixyrazine (45%) and perazine (60%). CONCLUSION: Most neuroleptics are strongly phototoxic in vitro indicating a potential risk for photo-induced reactions also to occur in patients treated with these drugs.

Antipsychotic Agents↗

PubMed1995

Disposable devices for the dispensing of oral drops. Study of photoprotectiveness and compatibility.

Amber-coloured syringes designed for the distribution of unit-doses of oral drops were studied for the efficiency of the photoprotectiveness and the possible binding of eleven phenothiazine neuroleptics: alimemazine, chlorpromazine, cyamemazine, fluphenazine, levomepromazine, periciazine, pipotiazine, prochlorperazine, thioproperazine, thioridazine, and trifluoperazine, all very easily oxidized in solution in daylight. Spectrofluorimetry made it possible, in one operation, to determine the remaining concentrations of drugs after storage and to verify the absence of photo-oxidation. The storage was performed up to 13 days at 25 +/- 3 degrees C and without any precaution from daylight. All the drugs studied were stable and none bound on the syringes. However, the stability appeared to be due to the antioxidants in the drug preparations, and not to the coloured material, since oral drops were also stable in uncoloured syringes designed for injection. Nevertheless, the amber-coloured syringes efficiently protect the active principles in pure aqueous solutions, without preservative, and thus this physical protection reinforces the chemical one of the galenical formulation.

Administration, Oral↗

PubMedDate not supplied

Citalopram causes no significant alterations in plasma neuroleptic levels in schizophrenic patients.

Steady-state plasma concentrations of commonly used neuroleptic drugs were measured in 90 schizophrenic patients before and after adding placebo or citalopram (40 mg/day) to their treatment regimen. Plasma concentrations of citalopram and its main metabolite, desmethylcitalopram, were also measured. In addition, patients with exceptionally high neuroleptic levels or an increase in adverse effects during the 12-week study period were evaluated for their debrisoquine/sparteine hydroxylase (CYP2D6) genotype, an enzyme responsible for oxidative metabolism of several neuroleptics and selective serotonin re-uptake inhibitors. There were no significant changes in plasma concentrations of haloperidol, chlorpromazine, zuclopenthixol, levomepromazine, thioridazine or perphenazine during the study. Plasma concentrations of citalopram and desmethylcitalopram were well within the levels reported previously with monotherapy, and remained stable throughout the study. None of the 15 patients analysed for the CYP2D6 genotype was a poor metabolizer. It is concluded that clinically important pharmacokinetic drug interactions do not play a crucial role when citalopram is used as an augmentation therapy in neuroleptic-treated schizophrenic patients.

Adult↗

PubMed1992

Zuclopenthixol, melperone and haloperidol/levomepromazine in the elderly. Meta-analysis of two double-blind trials at 15 nursing homes in Norway.

A meta-analysis was carried out of the data from two double-blind, multi-centre studies with identical methodology which compared the effectiveness of treatment of elderly patients with zuclopenthixol and with other antipsychotic drugs. In one study, patients were treated for 4 weeks with either zuclopenthixol or melperone; in the other, with either zuclopenthixol or a combination of haloperidol and levomepromazine. The meta-analysis evaluated the results of 96 patients, 49 in the zuclopenthixol group and 47 in the comparison group. Doses, which were adjusted to individual patient's needs, were low as shown by the percentages of defined daily doses for each of the study drugs. The results indicated that all three treatment alternatives were effective in the treatment of elderly patients with symptoms of agitation and hostility/aggressiveness. There was a trend, however, for zuclopenthixol to have a more rapid onset of effect. Zuclopenthixol also has the advantage for both patients and nursing staff that dosage is once daily. Only few and mild side-effects were reported with the three drug regimens.

Aged↗

PubMed2001

Drugs and syringe drivers: a survey of adult specialist palliative care practice in the United Kingdom and Eire.

Subcutaneous delivery of drugs using a syringe driver is common practice within specialist palliative care units. There is, however, little documented information regarding clinical practice. A survey performed in 1992 reported that at least 28 drugs were used in combination with others in a single syringe driver. The aim of the present study was to reassess practice in this field and to enquire more specifically about newer drugs. Postal questionnaires were sent to all adult specialist palliative care in-patient units in the UK and Eire (n = 208). One hundred and sixty-five units (79%) responded. The most common syringe driver in use was the Graseby 26 (61% of responding units). Most units delivered the contents of the syringe over 24 h, and water was usually used as the diluent in 90% of cases. The maximum number of drugs that respondents were prepared to mix in a single syringe was usually three (51%) or four (35%). In the UK, all units used diamorphine in doses from 2.5 mg/24 h upwards. All respondents also used haloperidol, in doses from 0.5 to 60 mg/24 h. A total of 28 different drugs were used in syringe drivers. The most common combinations were diamorphine and midazolam (37%), diamorphine and levomepromazine (35%), diamorphine and haloperidol (33%), and diamorphine and cyclizine (31%). In conclusion, there is much in common with regard to the way in which drugs are delivered in syringe drivers. However, a wide variety of drugs and drug combinations are still in use.

Adult↗

PubMed2006

Effects of therapeutic agents on cellular respiration as an indication of metabolic activity.

Animal experiments are indispensable in the investigation of the toxicity of drugs on cells, but may not be preferred for ethical reasons and sensitivity. As an alternative procedure, we investigated the susceptibility of cells to drugs using the effect on cellular respiration as an indicator of cell activity (toxicity). The primary cultures (cell lines) used in this study included human fetal myocardial cells, skeletal muscle cells, nerve cells, hypophyseal cells, epithelial cells of gastric mucosa, lymphocytes, hepatocytes, pancreatic (exocrine) cells, renal tubular epithelial cells and fetal adrenal cortex cells, which were obtained from the American Type Culture Collection (ATCC). The drugs used were diazepam, haloperidol and levomepromazine maleate (psychoactive drugs), cisplatin and doxorubicin hydrochloride (anticancer agents). The cells were used at a density of 2 x 10(6) cells/2 mL of growth medium and, to test the susceptibility, each drug was prepared at a concentration of 10 g/mL. Experiment results indicated that, even with the same drug, sensitivity was markedly different depending on the cell lines. Cardiac muscle cells showed the strongest respiratory inhibition by Serenace and were least inhibited by Hirnamin. The highest sensitivity to Cercine was noted for neurons, while gastric mucosa cells had almost no sensitivity. Sensitivity to Serenace, which was expected to have a strong nerve action, was higher in myocardial cells instead. In the present study, we suggested the possibility of studying individual differences in drug sensitivity through investigation of toxicity in each organ as opposed to toxicity in the individual. In addition, Serenace, which was developed as a neurotopic agent, showed a higher toxicity in cardiac muscle cells than in neurons. This finding appeared noteworthy, not only for forensic toxicology, but also for clinical practice and drug development.

Cell Count↗

PubMed2004

Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates.

The pharmacokinetics of antipsychotic drugs has become an integral part in understanding their pharmacodynamic activity and clinical effects. In addition to metabolism aspects, carrier-mediated transport, particularly secretion by ABC transporters, has been discussed as potentially relevant for this group of therapeutics. In this study, the psychoactive compounds perphenazine, flupentixol, domperidone, desmethyl clozapine, haloperidol, fluphenazine, fluvoxamine, olanzapine, levomepromazine, perazine, desmethyl perazine, clozapine, quetiapine and amisulpride were characterized in terms of P-glycoprotein (P-gp) affinity and transport. Experimental methods involved a radioligand displacement assay with [3H]talinolol as radioligand and transport--as well as transport inhibition--studies of the P-gp substrate [3H]talinolol across Caco-2 cell monolayers. In addition, the physicochemical descriptors log P and deltalog P were determined to test potential correlations between transporter affinity and lipophilicity parameters. All of the tested antipsychotics showed affinity to P-gp albeit their IC50 values (concentration of competitor that displaced 50% of the bound radioligand) differed by a factor exceeding 1000, when compared using the transport inhibition assay. From the group of P-gp substrates, amisulpride and fluphenazine were selected for in-vivo drug-drug interaction studies in rats to demonstrate the in-vivo relevance of the in-vitro findings. Compounds were administered by intraperitoneal injection either alone or in combination with 50 mg kg(-1) ciclosporin. The concentration versus time profiles for both drugs were followed in serum as well as in brain tissues. Significant differences between the treatments with the antipsychotic alone versus the combination of antipsychotic with ciclosporin were found for amisulpride. The distribution of amisulpride to the brain was increased and systemic serum levels were likewise increased indicating decreased systemic clearance for the combination regimen. For fluphenazine, systemic levels with and without co-administration of ciclosporin were comparable while higher brain-to-serum concentration ratios were found after co-administration of ciclosporin. The findings are explained on the basis of the limited contribution of P-gp-mediated transport to the elimination of fluphenazine and to a direct effect with respect to its distribution into the brain.

ATP Binding Cassette Transporter, Subfamily B↗

PubMed2004

Coloration of phenothiazines with metal-containing drugs.

We studied the color change of phenothiazines and metal-containing drugs after compound formation, followed by use of FT-Raman spectrocopy to observe any structural changes in them. When 6 phenothiazines (thioridazine hydrochloride, prochlorperazine maleate, levomepromazine maleate, chlorpromazine phenolphthalinate, fluphenazine maleate and perphenazine fendiate) formed compounds with natural aluminum silicate, the color change was accompanied by a shift of FT-Raman signals. These changes could be attributed to the structural changes of phenothiazines. This present observation can be then used in advance to avoid coloration of phenothiazines during preparative procedures with metal-containing drugs such as antacids.

Aluminum Silicates↗

PubMed1983

Effect of zotepine and various drugs on apomorphine- and methamphetamine-induced rotational behaviour in rats with unilateral lesions of the substantia nigra.

The effect of zotepine (2-chloro-11-(2-dimethyl-aminoethoxy) dibenzo [b, f] thiepin), a new neuroleptic, and other neuroleptics, minor tranquilizers, antidepressants, anticholinergic drugs, antihistamine drugs, antiparkinsonian drugs, alpha-, beta-adrenergic blocking agents, hypnotics and central muscle relaxants on apomorphine (APM)- and methamphetamine (MAP)-induced rotational behaviour was investigated in rats with unilateral lesions of the substantia nigra. Only the neuroleptics dose-dependently depressed both rotational behaviours. The minor tranquilizers also depressed both behaviours, but their effect was non-specific. The neuroleptics could be divided into two groups according to their relative effect on the APM- and MAP-induced rotational behaviour. The high-ratio group (fluphenazine, haloperidol, perphenazine, pimozide and zotepine) depressed the MAP-induced rotational behaviour more strongly than the APM-induced one, whereas the depressive effect of the low-ratio group (chlorpromazine, levomepromazine, thioridazine and clozapine) was the reverse. Zotepine, while belonging to the high-ratio group, was markedly lower in ratio than the other neuroleptics in this group. The correlation between the different effect of the two groups of neuroleptics and their clinical effect is discussed.

Animals↗

PubMedDate not supplied

Effect of some psychotropic drugs on luminol-dependent chemiluminescence induced by O2-, *OH, HOCl.

We studied antioxidant activity of six neuroleptics (chlorpromazine, levomepromazine, promethazine, trifluoperazine and thioridazine) and two antidepressants (imipramine and amitriptyline) in the range of concentration of 10(-7)-10(-4) M. We applied luminol-dependent chemiluminescence to test the ability of these drugs to scavenge the biologically relevant oxygen-derived species: hydroxyl radical, superoxide radical, hypochlorous acid in vitro. We found that the phenothiazines were powerful scavengers of hydroxyl and superoxide radicals. Chlorprothixene, amitriptyline and imipramine had no scavenge activity to the superoxide radical. All drugs showed a moderate scavenger effect on hypochloric anion.

Antidepressive Agents↗