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PubMed2000

Effect of some psychotropic drugs and a barbiturate on mycoplasmas.

The inhibitory effect of selected membrane stabilisers on Mycoplasma pneumoniae, M. hominis and Ureaplasma urealyticum was investigated in vitro. The phenothiazine chlorpromazine (CPZ) and the barbiturate thiopental (Leopental(R)) as well as the stereo-isomeric thioxanthene derivatives; cis(Z)-clopenthixol (Zu-clopenthixol(R))/ trans (E)-clopenthixol and cis (Z)-chlorprothixen (Truxal(R))/trans(E)-chlorprothixen, all have antimycoplasmal effect in the range 3.9-312 mg/l, measured as growth inhibition. It was also demonstrated that the enzymatic functions of the different mycoplasma strains, such as breakdown of glucose, arginine and urea, were abolished by concentrations of CPZ that were sufficiently low to allow multiplication of the organisms. A similar effect was obtained with Leopental(R) although the mycoplasmas were generally only half as sensitive to this drug. Also M. gallisepticum and Acholeplasma laidlawii were inhibited by CPZ and Thiopental. The four thioxanthenes were all inhibitory to mycoplasmal growth and the effect was independent of their stereo-isomeric configuration. The clopenthixol stereoisomers, but not the chlorprothixene isomers, inhibited colour change at concentrations lower than those which inhibited growth. While enzyme activity may continue for some time in vitro when classic antibiotics have inhibited mycoplasmal growth, the reverse effect was observed with phenothiazines and thioxanthenes. The membrane stabilisers may be useful tools in the investigation of microbiological activity on the mycoplasma membrane. From these drugs, new 'antibiotics' might be developed with another action than that of the known antimycoplasmal drugs.

Anti-Bacterial Agents↗
PubMed1994

Determination of zuclopenthixol and its main N-dealkylated metabolite in biological fluids using high-performance liquid chromatography with post-column photochemical derivatization and fluorescence detection.

A highly sensitive high-performance liquid chromatographic (HPLC) method for the assay of cis-(Z)-clopenthixol (zuclopenthixol) in urine and plasma has been developed. Following solid-phase extraction, the samples are chromatographed using reversed-phase ion-pairing HPLC. After separation, the solutes, having a thioxanthene structure, are transformed on-line into thioxanthones in a photochemical reactor. The thioxanthones are highly fluorescent compounds, and therefore, low detection limits are obtained when using fluorescence detection. Detection limits for zuclopenthixol and its N-dealkylated metabolite, in plasma as well as in urine, using fluorescence detection with excitation at 260 nm and emission at 435 nm, were found to be 0.05 ng/ml and 0.2 ng/ml, respectively. The chromatographic system separates the cis-(Z)- and trans-(E)-isomers of clopenthixol from its main dealkylated metabolite. Furthermore, the chromatographic system is very suitable for study of the photochemical reaction, since the chloro-thioxanthone and thioxanthone are well separated from the isomers of clopenthixol.

Chromatography, High Pressure Liquid↗
PubMed1993

Clinical evaluation and serum concentration of zuclopenthixol acetate in psychotic Asian patients: a single-dose preliminary study.

Nineteen acutely disturbed psychotic Asian patients were treated with a single intramuscular injection of 50 mg of zuclopenthixol acetate in Viscoleo. Patients were assessed clinically before and after treatment using the Brief Psychiatric Rating Scale (BPRS). Serum zuclopenthixol and the inactive geometric isomer trans(E)-clopenthixol were determined by high-performance liquid chromatography after intramuscular injection. All patients improved, with the BPRS being significantly reduced (p < 0.001) at 72 h after injection. Adverse effects were generally few. The mean +/- SEM serum zuclopenthixol concentrations at 24, 48, and 72 h were 19.9 +/- 2.8, 31.5 +/- 4.5, and 17.8 +/- 2.9 micrograms/L, respectively. trans(E)-Clopenthixol concentrations ranged from negligible to 39.5 micrograms/L. This study confirms that a single intramuscular injection of 50 mg is adequate for managing severely disturbed psychotic patients for the first 3 days. The serum zuclopenthixol concentrations attained in the Asian patients were higher than those reported in Caucasian psychiatric patients. In some patients, a considerable amount of zuclopenthixol had been transformed to trans(E)-clopenthixol.

Adolescent↗
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↗
PubMedDate not supplied

The role of stereoselectivity of chemosensitizers in the reversal of multidrug resistance of mouse lymphoma cells.

The effect of three different stereoisomer pairs of CNS (central nervous system) active compounds was studied on the activity of human mdr1 p-glycoprotein. The methotrimeprazine, clopenthixol and butaclamol isomers had an antiproliferative effect (ID50) on the mdr1 expressing cells at 0.250 microgram/ml, while the parental cells were less sensitive having ID50 at 0.37-0.69 microgram/ml. Enantiomers of methotrimeprazine and clopenthixol had similar effectivity on the drug efflux of mdr cells. However, (-)butaclamol was found to inhibit mdr efflux-pump activity much more than the CNS active (+) isomer. Based on these results, tricyclic compounds does not seem to have stereoselectivity in methotrimeprazine and clopenthixol on the mdr reversal effect. In general, both active and inactive members of stereoisomers had a similar effect on the drug accumulation of the mdr cells. Therefore, hypothetically the CNS inactive member of stereoisomer pairs can be used as a resistance modifier without any risk in patients suffering from drug resistant cancer.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed2000

Zuclopenthixol acetate in the treatment of acute schizophrenia and similar serious mental illnesses.

BACKGROUND: People with schizophrenia or other psychotic illnesses may have delusions or hallucinations that may lead them to be aggressive or violent to themselves or others. Medication that is used in this context require the properties of rapid onset of effect (tranquillisation or at least initial sedation in order to quell aggressive or disorganised behaviour, but also antipsychotic effect), low frequency of administration and low levels of side effects, such as cardiological or neurological side effects, or pain at the injection site. Zuclopenthixol is the cis(Z)-isomer of clopenthixol, a neuroleptic of the thioxanthene group, used for treating people with psychotic symptoms. There is one oral preparation and two depot forms: zuclopenthixol acetate and zuclopenthixol decanoate. The acetate version does not stay in the body for very long (a single dose persists for only 72 hours) and is said to have these properties. OBJECTIVES: To estimate the effectiveness of zuclopenthixol acetate for the acute treatment of serious mental illnesses in comparison to other neuroleptic drugs. SEARCH STRATEGY: Searches of the Cochrane Schizophrenia Group's Register of Trials, The Cochrane Library, MEDLINE, abstracts of congresses and trial reference lists were performed. Appeals for unpublished data to the research community and to the Medical Information Department of Lundbeck Limited were also made. Attempts were made to contact relevant authors. SELECTION CRITERIA: Two reviewers independently assessed citations or papers and selected all randomised trials that included people with serious mental illnesses and compared zuclopenthixol acetate with other drug regimes. DATA COLLECTION AND ANALYSIS: Data were extracted independently by two reviewers. Attempts were made to contact authors for additional or missing information. Odds-ratios (OR) and 95% confidence intervals (CI) were estimated for binary data. Where possible, OR were pooled using Peto method and intention-to-treat analysis undertaken. Mean differences were used for continuous variables. MAIN RESULTS: Pooled data shows no difference for the outcome 'no important improvement' in psychotic symptoms at the end of the follow-up period (OR 0.84 CI 0. 34-2.05). Sedation was evaluated using different instruments. Only one study presented data which suggested an earlier and more intense sedation in zuclopenthixol acetate users at 4 hours (OR 0.18 CI 0. 04-0.93). Use of additional antipsychotic medication was not avoided in the zuclopentixol acetate group (OR 2.18, CI 0.64-7.42) and data on total number of administrations was not obtainable. Side effect data were poorly reported but there is no evidence of a consistent difference between zuclopenthixol acetate and other 'standard drugs' for either the pattern of side effects or the wish to leave the study early. Hospital and service outcomes, number of aggressive incidents, satisfaction with care and economic outcomes were not addressed by any study. REVIEWER'S CONCLUSIONS: Recommendations on the use of zuclopenthixol acetate for the management of psychiatric emergencies in preference to 'standard' treatment have to be viewed with caution. Most trials present important methodological flaws and findings are poorly reported. This review did not find any suggestion that zuclopenthixol acetate is more effective in controlling aggressive/disorganised behaviour, acute psychotic symptoms, or preventing side effects. There were no data directly related to tranquillisation, but it may produce more earlier and intense sedation than oral haloperidol. Well conducted randomized controlled trials are needed to confirm claims related to the use of zuclopenthixol acetate in emergency psychiatry.

Acute Disease↗
PubMed1994

QEEG alpha 1 changes after a single dose of high-potency neuroleptics as a predictor of short-term response to treatment in schizophrenic patients.

Baseline quantitative electroencephalographic (QEEG) characteristics and their changes after a single test dose of either haloperidol or clopenthixol were investigated in a group of 29 schizophrenics as possible predictors of short-term response to those drugs. On baseline QEEG assessment, responders (R) to subsequent treatment showed fewer slow and more fast activities than nonresponders (NR). A large overlap between R and NR with respect to these measures was observed, however, revealing their practical inadequacy to predict short-term response in individual patients. On the contrary, changes in alpha 1, observed 6 hr after the administration of a single test dose of either haloperidol or clopenthixol, discriminated to a very large extent between R and NR, correctly identifying 17 out of 18 R and 8 out of 10 NR. The QEEG test dose procedure might be used in the selection of the most appropriate antipsychotic drug for individual schizophrenic patients.

Adolescent↗
PubMed1985

Hyperactivity induced by stimulation of separate dopamine D-1 and D-2 receptors in rats with bilateral 6-OHDA lesions.

The effects of DA agonists and antagonists with different dopamine (DA) D-1 and D-2 receptor selectivity have been studied in rats with bilateral 6-OHDA lesions. The D-1 agonist SK & F 38393, the D-2 agonist pergolide and the mixed agonist apomorphine all induced marked hyperactivity in lesioned rats in doses which were without stimulant effect in sham-operated animals. The hyperactivity induced by SK & F 38393 was blocked by the DA D-1 antagonist SCH 23390, but unaffected by the D-2 antagonists spiroperidol or clebopride. Pergolide-induced hyperactivity showed the reverse selectivity. The mixed D-1/D-2 antagonists, cis(Z)-flupentixol and cis(Z)-clopenthixol, however blocked the effect of both agonists. Apomorphine-induced hyperactivity was neither blocked by selective D-1 nor D-2 antagonists, but was dose-dependently inhibited by cis(Z)-flupentixol and cis(Z)-clopenthixol. Potent blockade was also obtained by combined treatment with SCH 23390 and spiroperidol, indicating the need of blocking both D-1 and D-2 receptors simultaneously. The results indicate that D-1 and D-2 receptor function can be independently manipulated in denervated rats and they confirm similar results obtained in rats with unilateral 6-OHDA lesions using circling behaviour.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗