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At least 343 records · Page 19Linked to original sources

PubMed1990

[Chromatographic purity tests of various phenothiazine derivatives. I. Thin-layer chromatography].

Chromatographic purity tests of four phenothiazine derivatives chlorpromazine, levomepromazine, promethazine and trifluoperazine have been developed. The adsorptive and partition methods are suitable to the separation of the above substances and intermediates as well as side products of their productions. The most common impurities of final products were detected by qualitative purity tests. Densitometric quantitative determinations were carried out on silicagel layer using the solvent system cyclohexanebenzene-diethylamine. Quantity of intermediate impurities were 0.15-0.96%.

Antipsychotic Agents↗

PubMed1990

[Chromatographic purity tests of various phenothiazine derivatives. II. Gas chromatography].

Gas chromatographic purity tests of four phenothiazine derivatives chloropromazine, levomepromazine, promethazine and trifluoperazine have been described. Chromatographic system has been optimized that is suitable to the separation of the above substances and their intermediates as well as their side products. Thermostabilities of phenothiazine derivatives were determined, their thermal decompositions were investigated under gas chromatographic circumstances and the data obtained were completed with data of their thermoanalytical tests. Optimal conditions have been worked out and by applying them thermal decomposition of compounds could be minimized. Authors have drawn attention to formation of artificial products which could not be avoided therefore taking into account requirements of purity tests the application of the method is problematical.

Antipsychotic Agents↗

PubMed1991

The influence of various drugs on the binding of tianeptine to human plasma proteins.

The plasma binding of the atypical tricyclic antidepressant tianeptine was studied in combination with six drugs, at therapeutic concentrations: cyamemazine, levomepromazine, flunitrazepam, oxazepam, diclofenac and salicylic acid. Of these drugs, only salicylic acid at high plasma concentrations impaired tianeptine binding and thus may potentiate its effects.

Anti-Inflammatory Agents, Non-Steroidal↗

PubMedDate not supplied

[Comparative effect of psychotropic agents on orienting-motor responses and cerebral Na,K-ATPase activity in vivo].

Levomepromazine, chlorpromazine (10 and 30 mg/kg), etaperaxine, haloperidol (3 and 10 mg/kg) inhibited the exploratory-motor reactions of rats and the brain Na, K-ATPase activity an hour after their administration. The effects of tranquilizers as well as of antidepressants on the exploratory reactions and on the enzyme activity were not found to stand in a clearcut relation to each other. The stimulating effect of amphethamine (3 mg/kg) was accompanied by activation and suppressive action (10 mg/kg)--by inhibition of the enzyme. It is suggested that the inhibition of the brain Na, K-ATPase activity by psychotropic drugs may play a role in the mechanism of their sedative action.

Amphetamine↗

PubMed1987

Calmodulin and troponin C as targets for drug action.

In this study, ligands from various chemical classes were investigated with respect to their relative affinities to calmodulin (CaM) and troponin C (TnC), using the fluorescent dye 3,3'-dipropylthiocarbocyanine iodide (diS-C3-5'). In parallel, functional tests were carried out determining the effects of the ligands on the CaM activated cyclic nucleotide phosphodiesterase (PDE) activity and the TnC mediated Ca-sensitivity of skinned myocardial fibres and cardiac myofibrils. The following results were obtained: 1) As a rule, most of the ligands tested had higher affinities to CaM than to TnC. 2) Even within one and the same pharmacological class (e.g. phenothiazines) the relative affinities for CaM and TnC varied considerably, trifluoperazine (TFP) or levomepromazine (LMP) showing low or no CaM specificity, methophenazine (MP) on the other hand being highly selective for CaM by a factor of more than 200. 3) In all cases tested, the functional tests were in good quantitative agreement with the binding data, showing inhibition of CaM stimulated PDE activity and Ca-sensitizing effects in concentrations corresponding well with the respective drug affinities to CaM and TnC, respectively. 4) It is concluded that a) interaction of ligands with TnC can lead to Ca-sensitization of the cardiac contractile system and a positive inotropic effect without a concomitant elevation of the intracellular level of activator Ca. This may result in a novel cardiotonic principle avoiding the common side effects of 'classical' positive inotropic agents due to Ca-overload. b) drug selectivity for TnC or CaM appears chemically achievable.

Animals↗

PubMed1989

Zuclopenthixol and haloperidol/levomepromazine in the treatment of elderly patients with symptoms of aggressiveness and agitation: a double-blind, multi-centre study.

A double-blind study was carried out in 48 hospitalized, elderly demented patients with key symptoms of aggressiveness and agitation to evaluate the efficacy and tolerability of zuclopenthixol compared with that of haloperidol/levomepromazine. Patients were allocated at random to receive initial doses of either 4 mg zuclopenthixol daily or 1 mg haloperidol in the morning and 5 mg levomepromazine in the evening over a period of 4 weeks. In Week 4, the mean daily dose was 4.8 mg zuclopenthixol and 1.6/7.6 mg haloperidol/levomepromazine, respectively. After 1 week, the severity of illness was already significantly reduced, and was further reduced after 2 and 4 weeks of treatment in both groups: the reduction, however, was most pronounced in the zuclopenthixol group and after 2 weeks this difference was significant. Side-effects were few. The results of the study indicate that, whilst both zuclopenthixol and haloperidol/levomepromazine were effective and well tolerated in these elderly patients with aggressiveness and agitation, onset of therapeutic effect appeared more rapidly with zuclopenthixol, which furthermore provides the practical advantage that it may be administered once a day.

Aged↗

PubMed1987

[The beta-adrenergic receptor and adenylate cyclase of rat reticulocytes as a test system for screening pharmacologic preparations].

The effect of cardio- and neurotropic drugs was studied on beta 2-adrenergic receptors and coupled adenylate cyclase (AC) from rat reticulocytes. Trifluperazine, chlorpromazine, levomepromazine, metaphenazine, haloperidol, (+) and (-) isomers of butaclamol, as well as imipramine, vinblastine and verapamil, at a concentration of 10(-4) M failed to influence AC stimulation by isoproterenol. Thioproperazine and trifluperidol inhibited isoproterenol-stimulated AC with Ki = 4.0.10(-5) M and Ki = 4.5.10(-5) M, respectively. This inhibitory effect was due to the direct action of thioproperazine and trifluperidol on the beta-adrenergic receptors, since this drugs displace the receptor-bound (3H) dihydroalprenolol with Ki = 5.10(-6) M and 9.10(-6) M, respectively. The results obtained suggest that adrenolytic effect of trifluperidol and thioproperazine might play a significant role in their side effects.

Adenylyl Cyclases↗

PubMed1985

[Neuroleptics in psychogeriatrics. A proposal for a more rational prescription policy].

All neuroleptics have a cerebral dopamine receptor blocking effect. This is the best documented explanation for their anti-psychotic effect. Furthermore, they act to a widely differing extent in a blocking manner to other central neurotransmitters, such as noradrenaline, acetylcholine, histamine, and serotonin. During the last couple of years quantitative data have been produced, enabling a more rational choice of neuroleptics. Based on these data and a number of pharmacokinetic considerations, a provisional scheme has been elaborated for the choice of neuroleptics in some clinical situations in psychogeriatrics. Our own experiences with this scheme are promising. It allowed us to restrict the use of neuroleptics to five drugs. The neuroleptics with a strong sedative and anticholinergic action, such as alimemazine, promazine and levomepromazine, being potentially dangerous to particularly elderly patients, are no longer used.

Aged↗

PubMed1986

[Seasonal changes in the behavioral effects of neuroleptics on white rats].

Summarized results of the experiments (conducted in 1981-1984) demonstrate seasonal rhythms of some behavioural effects (catalepsy and depression of locomotor activity) of haloperidol (0.5 mg/kg) and levomepromazine (5 mg/kg) in white rats. In intact rats neuroleptics were more effective in depressing high than low motor activity. Catalepsy induced by single administration of neuroleptics was more pronounced in spring and autumn months. A certain negative correlation exists between seasonal variations of neuroleptic catalepsy and the speed of monoamine (dopamine and serotonin) metabolism in the brain of intact rats.

Animals↗

PubMed1978

[Effects of psychotropic drugs on the spinal ventral root reflexes in cats. A comparison of the depressant actions in intact and spinal preparations (author's transl)].

Effects of the typical psychotropic drugs such as neuroleptics, tricyclic antidepressants and benzodiazepines on the monosynaptic reflex (MSR) and polysynaptic reflex (PSR) were investigated using intact and spinal cats. Drugs used were chlorpromazine, levomepromazine, perphenazine, prochlorperazine, droperidol, haloperidol, amitriptyline, imipramine, diazepam and flurazepam. Neuroleptics depressed the ventral root reflexes markedly to slightly in both preparations. The inhibitory effects of these drugs on MSR of intact cats were stronger than those on MSR of spinal cats, and the activity was slightly higher than that of PSR depression in intact preparations. In intact cats, those depressants effects of neuroleptics on PSR produced various characteristic action patterns in comparison with MSR inhibition. Tricyclic antidepressants were similar in the mode of action to the dimethylamino side-chain groups in phenothiazines, but the inhibitory effects of ventral root reflexes were distinctly weaker than that of neuroleptics. Benzodiazepines depressed only PSR without MSR inhibition, especially in spinal cats. Thus, it is suggested that the structure-activity relationship considered, a classification of the psychotropic drugs can be given according to the inhibitory activities on spinal ventral root reflexes in intact and spinal cats.

Action Potentials↗

PubMedDate not supplied

The influence of neuroleptics on the behavioural effect of 5-hydroxytryptophan.

The antagonism of neuroleptics of various groups (chlorpromazine, chlorprothixene, clopenthixol, clozapine, flupenthixol, fluphenazine, haloperidol, levomepromazine, mepazine, perazine, perphenazine, pimozide, prochlorperazine, promazine, spiperone, thiopromazine, thioridazine, trifluperazine, trifluperidol, triflupromazine) towards L-5-hydroxytryptophan (5-HTP) was assessed on the basis of inhibition of characteristic head-twitches. ED50 was assayed in mice and rats. The results indicate that all investigated neuroleptics inhibit the action of 5-HTP and their ED50 values are, as a rule, lower than the values of ED50 for catalepsy. That action is for the majority of neuroleptics more pronounced in mice than in rats. The present paper disucsses possible serotonergic, dopaminergic and also noradrenergic mechanism of action of neuroleptics in the 5-HTP test.

5-Hydroxytryptophan↗

PubMed1987

[Priapism in neuroleptic therapy].

The case of a 47-year old schizophrenic patient, who developed priapism on the fourth day of treatment with 40 mg Haloperidol and 50 mg Levomepromazin daily, is presented. Clinical aspects and possible mechanisms of pathogenesis are discussed.

Drug Therapy, Combination↗

PubMedDate not supplied

The influence of chronic treatment with antidepressant neuroleptics on the central serotonin system.

Chronic administration of antidepressant neuroleptics chlorprothixene (CPX) and levomepromazine (LMZ) increases the sensitivity of one kind of serotonergic receptors in CNS-5-HT2 receptors (which are involved in such behavioral responses as head-twitches and hyperthermia in heat adapted rats), but do not change 5-HT1 receptor population (responsible for the rate of serotonin synthesis). These results confirm once more the hypothesis about the existence of at least two types of serotonin receptors in the CNS. They also indicate that antidepressant neuroleptics, which are potent serotonin 5-HT2 and alpha 1-adrenergic blocking agents, after chronic administration affect the serotonin system in a manner similar to that produced by chronic treatment with classical antidepressant drugs.

Amitriptyline↗

PubMed1985

[An anesthetic technic in dogs for studying the arrhythmogenic effects of acute coronary occlusion].

Intramuscular injection of levomepromazine (0.5 mg/kg) 30 min before intravenous injection of 10 mg/kg pentobarbital sodium induces a good surgical anaesthesia in dogs artificially ventilated with 50% N2O and 50% O2 and given 0.01 mg/kg atropine and 0.1 mg/kg pancuronium intravenously before left thoracotomy. This protocol is suitable for the study of the arrhythmogenic effects of acute one-stage coronary artery ligation in anaesthetized dogs. In fact, minor interference with the autonomic nervous system appears to be involved since heart rate is maintained slow and mean aortic pressure is kept within normal limits, as pH, PaO2, anc PaCO2 during subsequent periods. Acute circumflex coronary arterio-venous pedicle ligation close to the left main trunk division resulted in this model in a high incidence of ventricular fibrillation (10 out of 15 dogs) early (7 +/- 4 min) after occlusion. Specific interventions aimed at reducing the incidence of early post-ischemic life-threatening ventricular arrhythmias might be tested in this model.

Anesthesia, General↗

PubMed1979

[Therapy of acute schizophrenic attacks. High dosage haloperidol therapy compared with a two component treatment].

In a controlled open study 18 patients were treated with high doses of haloperidol (Haldol-Janssen) from 50 to 100 mg daily and 15 patients with a combined therapy of 10 mg haloperidol and 150 to 300 mg levomepromazin (Neurocil). The high-dosed sample a significantly rapid decrease of the productive symptoms and improvement of the general condition were found. The medians of the rating scales and self-rating scales showed similar courses. Within the high-dosage group especially after the beginning of therapy, there was an unexpected significant increase in extrapyramidal signs (dyskinesias), which did not appear any more after starting with an initial dose of at least 50 mg Haldol-Janssen. Other side effects could not be found, the tolerance was good.

Anxiety↗

PubMed1980

Antagonistic effects of psycholeptic drugs on stress-induced analgesia.

Stress-induced analgesia was significantly antagonized by naloxone and was dose-dependently reduced by diazepam, chlordiazepoxide, flurazepam, medazepam, nitrazepam, estazolam, phenobarbital, chlorpromazine, levomepromazine, haloperidol and propranolol. In contrast to psycholeptics, morphine substantially increased in threshold of nociceptive response in the post-stress session. Centrally acting muscle relaxants, tolperisone and carosiprodol had no substantial anti-stress effects. These results suggest that the stress-induced analgesia is probably mediated through endogenous opioids in the central nervous system. The approach used in our study provides a simple method for assessing the anti-stress action of psycholeptics.

Analgesia↗

PubMedDate not supplied

[Neuroleptics as antagonists of gamma-aminobutyric acid].

Experiments on the neurons of isolated spinal cord of rats aged 9-14 days have revealed that like picrotoxin, the neuroleptics reduce the GABA-induced depolarization of primary afferents, hyperpolarization of the motoneurons and inhibition of the function of the interneurons which exercise the inhibitory control of motoneuronal activity. The highest GABA-lytic activity was displayed by the butirophenon derivatives (droperidol and haloperidol). Triphthazin slightly yields to these drugs as regards the activity. Aminazin and levomepromazin have a moderate GABA-lytic activity, whereas thioridazin and ftorphenazin have none. A possible role of the GABA-lytic activity of the neuroleptics in their antipsychotic action is discussed.

Animals↗

PubMed1984

Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action.

The relative potencies of a variety of neuroleptic drugs and antidepressant agents in competing for the binding of 3H-clonidine and 3H-yohimbine to alpha 2-adrenergic receptors of the rat cerebral cortex were quantified. The rank order of potencies of neuroleptics tested in competing for both ligand bindings is: clocapramine, carpipramine much greater than perphenazine, fluphenazine, alpha,beta-flupentixol greater than propericiazine, levomepromazine greater than chlorpromazine, pimozide greater than moperone much greater than haloperidol, sulpiride. Among the antidepressants, mianserin is the most potent antidepressant. Amitriptyline has a substantial affinity, while desipramine, imipramine, and clomipramine are the least potent. It is concluded that a number of neuroleptics and antidepressant agents display a potent or moderate affinity to alpha 2-receptor sites. These findings support the suggestion that some neuroleptics enhance the release of norepinephrine (NE) mainly by acting on presynaptic alpha 2-receptors, and that the alpha 2-receptor blocking property may have an important role in the mechanism of the antidepressant effect of some neuroleptic compounds.

Animals↗