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PubMed2000

Determination of nortriptyline in human serum by fully automated solid-phase extraction and on-line high-performance liquid chromatography in the presence of antipsychotic drugs.

A fully automated on-line method for determination of nortriptyline in human serum was developed using an ASPEC XL (Gilson) solid-phase extraction apparatus in combination with high-performance liquid chromatography. Solid phase extraction was performed on cyanopropyl cartridges. HPLC was carried out using a C18 column with a mobile phase of acetonitrile-0.01 M triethylamine (34:66 v/v) buffer, pH 3.0. UV detection was at 242 nm. The Inter-day CV% was <5%. Comparison with liquid-liquid extraction of serum from patients treated with nortriptyline showed good agreement. Studies of analytical interference from coadministered psychoactive drugs revealed that only imipramine and a methotrimeprazine metabolite interfered.

Antidepressive Agents, Tricyclic↗
PubMed1990

Subcutaneous infusions for control of cancer symptoms.

Continuous subcutaneous infusions offer a safe, simple, effective alternative to intravenous or intramuscular injections when oral medications cannot be used. They are extremely useful for cancer patients suffering from pain, vomiting, seizures, and other symptoms. Hydromorphone or morphine may be combined with metoclopramide, methotrimeprazine, or haloperidol (in D5W only), in the same pump to control both pain and nausea. Seizures can be controlled by subcutaneous infusion of phenobarbital or midazolam. If proper doses are prescribed and skin irritation is watched for, they can be used safely in the patient's home.

Analgesics↗
PubMed1993

Biologically active conformers of phenothiazines and thioxanthenes. Further evidence for a ligand model of dopamine D2 receptor antagonists.

Conformational analyses have been performed on several phenothiazine and thioxanthene dopamine antagonists using the MM2-87 program and parameter set. The compounds that were examined are thioridazine (2), methotrimeprazine (3), cis- and trans-chlorprothixene, and a piperidylidene derivative of chlorprothixene. In addition, (+)-2 and (-)-3 were determined by X-ray crystallography to have the R absolute configuration. The above compounds were superimposed onto loxapine, which was used as a template for the previously proposed dopamine D2 receptor ligand model. The conformational properties and receptor affinities of these compounds were found to be entirely consistent with the ligand model. For example, a conformer of (+)-R-2 that is consistent with the ligand model is lower in energy than a consistent conformer for (-)-S-2, which agrees with the higher D2 receptor affinity of the former. Similarly, in agreement with the much higher affinity of (-)-R-3 relative to (+)-S-3, only the former contains a low energy conformer consistent with the ligand model. The ligand model is also consistent with the greater potency of cis-thioxanthenes over the trans isomers. These results emphasize the importance of the correct orientation of the ammonium hydrogen for high affinity at the D2 receptor. The pharmacophore for D2 receptor ligands is compared with a recently proposed pharmacophore for D1 ligands.

Antipsychotic Agents↗
PubMed2004

The role of pharmacotherapy in the management of behaviour disorders in traumatic brain injury patients.

The aim of this paper was to systematically review the research published in English language on the effectiveness of drugs for the treatment of neurobehavioural disorders in patients with traumatic brain injury (TBI). A literature search using Medline, Pre-Medline, Embase, Psychlit and Cochrane Library databases between 1990 and January 2003 as well as a hand search of Brain Injury since 1996 were carried out. Phrases such as 'head injury', 'brain injury', 'drug treatment', 'drug trials' and 'randomized controlled trials' were used. Sixty-three papers were selected for data synthesis. Of these, 13 were randomized controlled trials, eight were prospective observational studies, four were retrospective studies, 25 were case series and 13 were single case studies. There was a dearth of type I-III evidence. There was no strong evidence either way to suggest that drugs are effective in the treatment of behaviour disorders in patients with TBI. However, there was weak evidence, primarily based on case studies that psychostimulants are effective in the treatment of apathy, inattention and slowness; high dose beta-blockers in the treatment of agitation and aggression; anti-convulsants and anti-depressants (particularly SSRIs) in the treatment of agitation and aggression, particularly in the context of an affective disorder; and possibly a specific neuroleptic methotrimeprazine in the treatment of agitation in the post-acute stage of Acquired Brain Injury. Some drugs that are effective in some patients have been shown to be ineffective in others. Some drugs, particularly lithium and dopaminergic drugs could cause adverse effects and deterioration in some patients.

Adrenergic beta-Antagonists↗
PubMed2003

Olanzapine for intractable nausea in palliative care patients.

Nausea is a common problem among palliative care patients, which is often undertreated. Olanzapine, an atypical antipsychotic, possesses a unique neurotransmitter binding profile that is similar to methotrimeprazine, an anti-emetic widely used in Europe for recalcitrant nausea. We report a case series of six patients who suffered nausea which was resistant to initial treatment with traditional antiemetics; each patient exhibited marked improvement when treated with olanzapine.

Aged↗
PubMed2004

Evaluation of laryngeal mask as an alternative to endotracheal intubation in cats anesthetized under spontaneous or controlled ventilation.

OBJECTIVE: To compare the cardiorespiratory effects and incidence of gastroesophageal reflux with the use of a laryngeal mask airway (LMA) or endotracheal tube (ET) in anesthetized cats during spontaneous (SV) or controlled ventilation (CV). STUDY DESIGN: Prospective randomized experimental trial. ANIMALS: Thirty-two adult crossbred cats, weighing 2.7 +/- 0.4 kg. METHODS: The cats were sedated with intramuscular (IM) methotrimeprazine (0.5 mg kg(-1)) and buprenorphine (0.005 mg kg(-1)), followed 30 minutes later by induction of anesthesia with intravenous (IV) thiopental (12.5-20 mg kg(-1)). An ET was used in 16 cats and an LMA in the remaining 16 animals. Anesthesia was maintained with 0.5 minimum alveolar concentration (0.6%) of halothane in oxygen using a Mapleson D breathing system. Cats in both groups were further divided into two equal groups (n = 8), undergoing either SV or CV. Neuromuscular blockade with pancuronium (0.06 mg kg(-1)) was used to facilitate CV. Heart and respiratory rates, direct arterial blood pressure, capnometry (PE'CO2) and arterial blood gases were measured. Gastric reflux and possible aspiration was investigated by intragastric administration of 5 mL of radiographic contrast immediately after induction of anesthesia. Cervical and thoracic radiographs were taken at the end of anesthesia. Data were analyzed using anova followed by Student-Newman-Keuls, Kruskal-Wallis or Friedman test where appropriate. RESULTS: Values for PaCO2 and PE'CO2 were higher in spontaneously breathing cats with the LMA when compared with other groups. Values of PaO2 and hemoglobin oxygen saturation did not differ between groups. Gastroesophageal reflux occurred in four of eight and two of eight cats undergoing CV with ET or LMA, respectively. There was no tracheal or pulmonary aspiration in any cases. CONCLUSIONS AND CLINICAL RELEVANCE: The use of an LMA may be used as an alternative to endotracheal intubation in anesthetized cats. Although aspiration was not observed, gastric reflux may occur in mechanically ventilated animals.

Anesthetics, Intravenous↗
PubMed1958

Inhibition by various substances of oedema formation in the bind-paw of the rat induced by 5-hydroxytryptamine, histamine, dextran, egg-white and compound 48/80.

Of the substances studied for their inhibitory action of the oedema formation in the hind-paw of the rat, the most active was a new derivative of phenothiazine, related to chlorpromazine. It is methotrimeprazine {10-(3-dimethylamino-2-methylpropyl)-2-methoxyphenothiazine; 7044 RP}. This substance possesses potent antihistamine and anti-5-hydroxytryptamine properties, and doses of 0.25 mg./kg. inhibited the blueing and swelling of the foot after injections of histamine, 5-hydroxytryptamine, eggwhite, dextran or compound 48/80 into the feet of rats with sulphan blue (Evan's blue) dye in their circulation. The results indicate that both histamine and 5-hydroxytryptamine play rôles in increasing capillary permeability in the rat.

Animals↗
PubMed2004

Do the second-generation "atypical neuroleptics" have analgesic properties? A structured evidence-based review.

STUDY DESIGN: This is a structured, evidence-based review of all available studies on the potential effectiveness of the atypical neuroleptics for the treatment of pain (analgesia). To determine what evidence, if any, exists for, or against, the effectiveness of the atypical neuroleptics for analgesia. SUMMARY OF BACKGROUND DATA: There has been significant controversy over whether the conventional neuroleptics (non-atypicals) have analgesic properties. A recent review (Patt et al. 1994) did conclude that the evidence for effectiveness was sparse, except for methotrimeprazine. However, that review did not include a new class of neuroleptics: the atypicals such as olazapine, risperidone, quetiapine, etc. METHODS: A computer and manual search for studies relating to the atypicals and their analgesic effectiveness produced 10 studies/reports. These were reviewed in detail, and information relating to the above problem was abstracted and placed into tabular form. Each report was also categorized by the type of study it represented according to the guidelines developed by the Agency for Health Care Policy and Research (AHCPR). The strength and consistency of the evidence represented by the 10 studies were then categorized according to the AHCPR guidelines. Conclusions of this review were based on these results. RESULTS OF DATA SYNTHESIS: Of the 10 studies/reports, four were characterized by AHCPR guidelines as Type II (experimental), two were Type III (quasiexperimental), two were Type IV (nonexperimental), and two were Type V (case reports). Of these studies/reports, 90% indicated that the atypicals did have an analgesic effect. The overall strength and consistency of this evidence using the AHCPR guidelines was, therefore, categorized as B (generally consistent from Type II, Type III, and Type IV studies). CONCLUSIONS: Based on the above results, it was concluded that the reviewed data were generally consistent, suggesting that some of the atypicals may have an analgesic effect. There were, however, few double-blind, placebo-controlled studies, and many of the reports/studies had less than 50 patients. As such, this question requires further research.

Analgesics↗
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↗
PubMed2003

In vitro human plasma leucine(5)-enkephalin degradation is inhibited by a select number of drugs with the phenothiazine molecule in their chemical structure.

A number of drugs with the phenothiazine molecule in their chemical structure inhibit in a dose-dependent manner human plasmatic aminopeptidase leucine(5)-enkephalin (LEU) metabolism. Half-life peptide degradation was significantly increased by thioridazine > fluphenazine > As-1397 [10-(alpha-diethylaminopropionyl)phenothiazine] >/= promethazine >/= chlorpromazine (final drug conc. 10(-4) M); t1/2 (+/- SD) 21.2 +/- 1.1, 19.6 +/- 1.0, 17.2 +/- 0.9, 17.1 +/- 1.0, and 17.1 +/- 1.1 min, respectively. Control and bacitracin (known aminopeptidase inhibitor) values were 11.8 +/- 1.0 and 31.3 +/- 1.7 min, respectively. These drugs significantly decreased (listed in the same order) LEU degradation initial velocity; Iv (+/- SD) 0.77 +/- 0.2, 0.82 +/- 0.2, 0.92 +/- 0.3, 0.93 +/- 0.2, 0.94 +/- 0.3 pg LEU/min, respectively. Control and bacitracin 1.10 +/- 0.3 and 0.20 +/- 0.1 pg LEU/min, respectively. Values represent results from 5 samples, each obtained by pooling 6 individual plasmas (4 male and 2 female; n = 30 healthy, drug-free volunteers). However, neither the phenothiazines ethopropazine, methotrimeprazine, prochlorperazine and trifluoperazine nor the various commonly used heterocyclic antipsychotics tested, e.g., molindone, loxapine, clozapine, haloperidol, sulpiride and thiothixene inhibited plasma LEU degradation kinetics. Our results failed to show correlations between chemical structure, antipsychotic properties and ability to inhibit plasmatic aminopeptidase LEU degradation. Whereas, presence of the phenothiazine molecule appears to be necessary for enzyme inhibition, only five out of nine substituted phenothiazines tested exhibited this effect. Furthermore, there was a lack of correlation between phenothiazines antipsychotic properties and their capacity to inhibit aminopeptidase activity, a property shown by promethazine (antihistaminic) and As-1397 (selective butyrylcholinesterase inhibitor) but lacking in prochlorperazine and trifluoperazine. Our results provide information which could lead to the rational design of agents capable to modulate the bioavailability of enkephalin and other endogenous aminopeptidase-degraded peptides believed to be involved in the etiology and/or pathophysiology associated with various disease conditions. Whether their development could find useful pharmacological applications remains to be explored.

Adult↗
PubMed1998

Sedation for intractable distress in the dying--a survey of experts.

Terminal sedation is a phrase that has appeared in the palliative care literature in the last few years. There has not been a clear definition proposed for this term, nor has there been any agreement on the frequency with which the technique is used. A postal survey of 61 selected palliative care experts (59 physicians, two nurses) was carried out to examine their response to a proposed definition for 'terminal sedation', to estimate the frequency of this practice and the reasons for its use, to identify the drugs and dosages used, to determine the outcome, and to explore the decision-making process. Opinions on physician-assisted suicide and voluntary euthanasia were also sought. Eighty-seven per cent of the experts responded from eight countries, although predominantly from Canada and the United Kingdom. Forty per cent agreed unequivocally with the proposed definition, while 4% disagreed completely. Eighty-nine per cent agreed that 'terminal sedation' is sometimes necessary and 77% reported using it in the last 12 months--over half of these for up to four patients. Reasons for using this method included various physical and psychological symptoms. The most common drugs used were midazolam and methotrimeprazine. Decision making usually involved the patient or family, and varied with respect to the ease with which the decision was made. The use of sedation was perceived to be successful in 90 out of 100 patients recalled. Ninety per cent of respondents did not support legalization of euthanasia. In conclusion, sedating agents are used by palliative care experts as tools for the management of symptoms. The term 'terminal sedation' should be abandoned and replaced with the phrase 'sedation for intractable distress in the dying'. Further research into the management of intractable symptoms and suffering is warranted.

Adult↗
PubMed2006

Systematic review of antipsychotics for the treatment of hospital-associated delirium in medically or surgically ill patients.

OBJECTIVE: To determine which antipsychotic is associated with the greatest efficacy and safety when used for the pharmacotherapeutic management of delirium in medically or surgically ill patients. DATA SOURCES: MEDLINE, Current Contents, Cumulative Index of Nursing and Allied Health Literature, PsycINFO, Biological Abstracts, Cochrane Central Register of Controlled Trials, and EMBASE databases (all to July 2006) were searched for trials evaluating the pharmacologic treatment of delirium in medically or surgically ill patients. The key terms used included delirium, agitation, or acute confusion, and antipsychotics, phenothiazine, butyrophenone, perphenazine, fluphenazine, clozapine, trifluorophenazine, loxapine, thioridazine, pimozide, molindone, haloperidol, methotrimeprazine, chlorpromazine, prochlorperazine, droperidol, risperidone, quetiapine, ziprasidone, amisulpride, or olanzapine. STUDY SELECTION AND DATA EXTRACTION: Prospective, randomized, controlled trials comparing the clinical effects of antipsychotic therapy with placebo or comparing 2 antipsychotic treatments in an acute care setting were selected. Studies involving dementia-associated delirium, Alzheimer's disease-associated delirium, emergency department-associated acute agitation, acute brain trauma-associated agitation, or agitation secondary to underlying psychiatric afflictions such as depression or schizophrenia were excluded. All studies were evaluated independently by the 3 authors using a validated evaluation tool. Outcomes related to both efficacy and safety were collected. Four prospective trials were included in this systematic review. DATA SYNTHESIS: Antipsychotic agents, either atypical or typical, were effective compared with baseline for the treatment of delirium in medically or surgically ill patients without underlying cognitive disorders. Oral haloperidol was associated with more frequent extrapyramidal side effects, but overall, all agents were well tolerated. Interpretation of the published evidence is limited by the small sample sizes, varied patient populations, and comparative agents of the studies reviewed. CONCLUSIONS: The comparative studies evaluated here suggest that antipsychotic drugs are efficacious, when compared with baseline, and safe for the treatment of delirium. Haloperidol remains the most studied agent. Recommendation of one antipsychotic over another as a first-line pharmacologic intervention in the treatment of hospital-associated delirium is limited by the quality and quantity of data available. Better designed and larger studies evaluating the addition of antipsychotic agents to nonpharmacologic treatments are needed to measure the true effect of pharmacologic treatment.

Antipsychotic Agents↗
PubMed2002

In vitro chloroquine resistance modulation study on fresh isolates of Brazilian Plasmodium falciparum: intrinsic antimalarial activity of phenothiazine drugs.

Phenothiazine drugs - fluphenazine, chlorpromazine, methotrimeprazine and trifluoperazine - were evaluated as modulating agents against Brazilian chloroquine-resistant fresh isolates of Plasmodium falciparum. Aiming to simulate therapeutic schedules, chloroquine was employed at the concentration used for sensitive falciparum malaria treatment and anti-psychotic therapeutic concentrations of the phenothiazine drugs were adopted in two-fold serial dilutions. The in vitro microtechnique for drug susceptibility was employed. Unlike earlier reported data, the phenothiazine modulating effect was not observed. However, all the drugs demonstrated intrinsic antiplasmodial activity in concentrations lower than those described in the literature. In addition, IC50 estimates have been shown to be inferior to the usual anti-psychotic therapeutic concentrations. Statistical analysis also suggested an increase in the parasitaemia rate or, even, a predominant antiparasitic effect of phenothiazine over chloroquine when used in combination.

Adult↗
PubMedDate not supplied

Interaction of protonated anticancer thiazines with water-insoluble phospholipids and antineoplastic agents.

A series of neuroleptic protonated phenothiazine derivatives (promethazine, promazine, triflupromazine, methotrimeprazine, propiomazine, trifluoperazine and fluphenazine), some with known anticancer properties, were complexed with water-insoluble antineoplastice agents such as 5-fluorouracil (5FU), methotrexate (MTX) and sulindac, as well as with components of biomembrane and synthetic phospholipids as possible models of cancer and microbial cells. In all cases water-soluble micellar inclusion adducts were formed exhibiting electron charge transfer complex behaviour, with the appearance of thazine free radicals. The thiazines sequestered the drugs and phospholipids in well-defined molar ratios (MR) parabolically-dependent on the dipole moments (mu) of the protonated phenothiazine derivatives. pH comparisons showed that the inclusion adducts followed a model in which the compounds were enveloped in the lipophilic interior of the thiazine aggregates, while the side-chains of the latter faced the aqueous environment. In the model experiment, interaction of the thiazines and the 5FU adducts with E. coli F' lac was additive to marginally synergistic, confirmed by the checkerboard technique. The parabolic dependence of the molar minimum inhibitory concentration of the thiazines and thiazine/5FU adducts on the thiazine dipole moments suggests that their primary loci of interaction are the cell wall or membrane phospholipid components. Thiazines, especially those with dipole moments centered on about 6 D, near which the lowest MR occurs, can act as effective carriers for insoluble or sparsely soluble drugs. Any new thiazine drug for use alone or as a carrier in anticancer therapy should be designed with this criterion in mind.

Antineoplastic Agents↗
PubMedDate not supplied

Preliminary studies on phenothiazine-mediated reversal of multidrug resistance in mouse lymphoma and COLO 320 cells.

The ability of phenothiazine derivatives to inhibit the transport activity of P-glycoprotein in resistant mouse lymphoma and MDR/COLO 320 cells was studied. A rhodamine 123 efflux from the above-mentioned neoplastic cells in the presence of tested compounds was examined by flow cytometry. Two of the phenothiazine derivatives, namely perphenazine and prochlorperazine dimaleate, proved to be effective inhibitors of the rhodamine efflux. Other tested phenothiazine derivatives (promethazine hydrochloride, oxomemazine, methotrimeprazine maleate, trifluoropromazine hydrochloride, trimeprazine) also modulated the intracellular drug accumulation in both resistant cell lines, however, they exerted additional cytotoxic effects. The differences observed between the effects of the test compounds on intracellular drug accumulation could be the outcome of differences in phenothiazine's chemical structure, which is crucial for drug-cell membrane interactions. The results of this study provide information about a new group of compounds that offer promise in multidrug resistance reversal in tumor cells.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1985

Agranulocytosis in the course of phenothiazine therapy: case reports.

Agranulocytosis developed in three patients subsequent to chlorpromazine therapy and in one patient following treatment with methotrimeprazine and trifluoperazine. Although three of these four patients developed agranulocytosis within the expected time lapse (6 weeks), one patient developed the condition 12 years after the initiation of therapy. In one patient there was a recurrence of the agranulocytosis following reinstitution of chlorpromazine therapy. The subsequent treatment of psychosis is safer if another neuroleptic is substituted for the one that caused the agranulocytosis.

Adult↗
PubMedDate not supplied

Propranolol-induced depression and psychosis.

Episodes of depression and acute psychosis in two patients receiving propranolol hydrochloride are described, and the literature on propranolol-induced depression and psychosis is reviewed. A 42-year-old woman developed severe depression, marked apathy, social withdrawal, and anorexia after taking propranolol hydrochloride (80 mg/day) for three months to control her hypertension. Five days after the dose was reduced to 40 mg/day, there was a major improvement in her depressive symptoms, with a complete resolution in eight days. Upon rechallenge with 80 mg/day of propranolol, she again experienced depressive symptoms. Atenolol 50 mg/day was substituted for the propranolol therapy, and she exhibited a complete remission of her depression. The second patient was a 63-year-old man who had been taking propranolol hydrochloride 160 mg/day for three months without incident. Because of an increased frequency of anginal attacks, the dosage was increased to 240 mg/day. Within two days, he demonstrated such agitation, excitement, and combativeness that he had to be controlled with a 25-mg dose of methotrimeprazine. When the propranolol dose was reduced to 160 mg/day, his psychotic symptoms rapidly cleared. However, when the dose was subsequently increased to 200 mg/day, he again showed increased agitation. After substituting atenolol 100 mg/day for propranolol, the patient's mental status returned to normal. Both of these patients experienced symptoms that were temporarily associated with propranolol. Both patients were subsequently controlled without symptoms with atenolol therapy. Propranolol is a highly lipophilic beta blocker that achieves high concentrations in the brain. When continued beta-blocking therapy is necessary or beta blockade is indicated, a weakly lipophilic agent such as atenolol is indicated.

Adult↗