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At least 1,081 records · Page 60Linked to original sources
PubMed1980

The effect of the steroid muscle relaxant pipecurium bromide on the acetylcholinesterase activity of red blood cells in vitro.

The acetylcholinesterase (AchE) inhibitory effect of a muscle relaxant 2 beta,16 beta-bis-(4'-dimethyl-1'-piperazino)-3 alpha,17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), was studied in vitro. The inhibition of AchE activity of human red blood cells, expressed as pI50, was 3.99, whereas that of serum cholinesterase (ChE) was 4.33. The AchE inhibitor action was reversible. The inhibition was not influenced by the combined administration of promethazine or atropine. The combined effect of pipecurium bromide and of some other diamino-azasteroid agent proved to be additive. Pipecurium bromide showed mixed-type inhibitory effect both on AchE and ChE.

Acetylcholinesterase↗
PubMed1984

[Experience with psychotropic agents Pyrethia and Contomin in the terminal care of lung cancer patients].

Among patients with lung cancer, those having PS 4 ( Performance Status 4) and cancer pain received " Pyrecon ", a psychotropic agent, consisting of promethazine hydrochloride ( Pyrethia ) and chlorpromazine hydrochloride ( Contomin ). A mixture of 125 mg of Pyrethia and 50 mg of Contomin was diluted in 500 ml of regular IV solution and given through the central vein at a rate of 20 ml/hr. Pyrecon was found to be effective in patients with severe cancer pain in whom Brompton cocktail was ineffective. Pyrecon was also effective in patients whose daily life rhythm was unsteady due to insomnia caused by anxiety or unrest. We suggest that Pyrecon is effective in the treatment of cancer pain.

Adult↗
PubMed1983

[Biotransformation of fentanyl. III. Effect of chronic drug exposure on the distribution, metabolism and excretion in the rat].

In male Wistar rats, tissue distribution and excretion of fentanyl and its metabolites were studied after intravenous of intramuscular injection. Oxidative desalkylation leading to phenylacetic acid and norfentanyl proved to be the main degradation pathway in-vivo, whereas other metabolites, including the pharmacologically still active p-hydroxy(phenethyl)fentanyl were formed only in minor quantities. All compounds could be detected in any tissue under study (brain, lung, liver, kidney, muscle and fat) as well as in the gastric contents, the amount of fentanyl in the latter cumulating to about 2% of the total dose 60 min after injection, compared with about 10% in the fat. In rats chronically treated with ethanol, nicotine, morphine, phenobarbital, promethazine or diazepam, major differences in in-vitro fentanyl metabolism by liver homogenates were observed including both inhibition and induction. Phenobarbital pretreatment also induced extrahepatic biotransformation in kidney, adrenals and intestinal mucosa. On the other hand, tissue concentrations of fentanyl and its metabolites did not clearly reflect the in-vitro changes in metabolic activity. Fentanyl brain levels were found to be lower in the treatment groups but seemed not to correlate with pharmacodynamics, less effects following injection being observed only after ethanol and morphine. The in-vitro metabolic drug interaction proved to be of less importance than changes in diuresis and/or urinary pH when excretion products were analysed. As a conclusion, it is suggested that altered sensitivity of brain tissue rather than changes in bioavailability must explain variations in dose-response relationship which are frequently believed to be seen when fentanyl is used in patients with chronic drug administration.

Animals↗
PubMedDate not supplied

Inhibition of Escherichia coli haemagglutination by phenothiazines.

The enterotoxigenic Escherichia coli strain H-10407 (078-H11) of Evans, possessing a colonization factor antigen (CFA/I) and haemagglutinating in the presence of mannose, was tested as to its ability to cause haemagglutination in the presence of phenothiazines. The phenothiazines (chlorpromazine, thioridazine, prochlorperazine, triethylpiperazine, promethiazine and promazine) were able to inhibit E. coli haemagglutination when added to the complex E. coli-erythrocytes. The most potent inhibitors were prochlorperazine and thioridazine, which inhibited E. coli haemagglutination in 1 min at a concentration of 1.5 mg/ml. The less potent was promethazine that inhibited haemagglutination at 6 mg/ml. Once haemagglutination had occurred the phenothiazines were able to reverse it, to "unhood" the E. coli from the erythrocytes. Prochlorperazine at a concentration of 0.4 mg/ml could reverse haemagglutination after 1 h contact with the E. coli erythrocytes complex. E. coli H-10407 grown in the presence of phenothiazines lost its haemagglutinating activity. The resulting non haemagglutinating E. coli recovered its haemagglutinating activity when recultured in a prochlorperazine free medium.

Chlorpromazine↗
PubMed1978

Toxic psychosis induced by phenothiazine administration in patients with chronic renal failure.

Adverse reactions to phenothiazines have not been commonly recognized in patients with chronic renal failure. We wish to report a characteristic acute psychosis as a complication of phenothiazine use in such individuals. Four patients with chronic renal failure requiring hemodialysis were given doses of chlorpromazine ranging from 100--1000 mg over time intervals varying from 2--7 days. All developed extreme restlessness, auditory and visual hallucinations, and episodes of belligerent behavior. A fifth patient treated with promethazine developed a similar psychosis. Each became ill shortly after the initiation of phenothiazine therapy. All improved slowly after cessation of the drug. Hemodialysis in four patients did not appear to affect the course of the illness. The use of phenothiazines in patients with chronic renal failure is cautioned.

Aged↗
PubMed1978

The effect of premedicants upon the lower oesophageal sphincter.

The barrier function of the lower oesophageal sphincter is of great practical importance in the prevention of regurgitation and aspiration. The action of seven most commonly used premedicants upon the lower oesophageal sphincter was studied in ten healthy volunteers. The results were compared with a placebo injection in eight volunteers. Sodium pentobarbital, droperidol and triflupromazine increased the presenting pressure of the lower oesophageal sphincter. Decreases were observed after promethazine, pethidine, the combination of droperidol plus fentanyl and atropine.

Adjuvants, Anesthesia↗
PubMed1978

[Influence of mediators on plasminogen activator release].

The influence of substances known as low molecular weight mediators such as biogenic amines, peptides and prostaglandins on the plasminogen activator release was studied in the isolated perfused pig ear. Among the substances tested, histamine and the plasma kinins bradykinin and kallidin were found to possess a dose-dependent activator-releasing effect, which in case of histamine can be suppressed by an antihistamine (promethazine). Serotonin and the prostaglandins at concentrations up to 10(-5)M possess no significant activator-releasing effect. Compared with the biogenic peptides angiotensin, oxytocin, vasopressin, and eledoisin, only the latter was found to release plasminogen activator. Studies on the influence of the substances tested on the capillary permeability showed that enhanced permeability is caused only by those mediators which cause also increased activator release.

Animals↗
PubMed1995

[Plasma catecholamine level and clinical parameters--quality criteria for premedication in childhood].

Stress hormones noradrenaline and adrenaline were measured in plasma before and after premedication to objectivate the anxiolytic potency of different premedication methods in children. In addition indirect signs of sympathoadrenergic activity (heart rate and blood pressure) as well as children's behavior and reaction to face mask were documented. Each group consisted of 16 children (aged 3 to 15 years). One group was prepared only psychologically, the second group received 0.1 mg/kg midazolam intravenously and the third group was given 1 mg/kg promethazine orally. Blood pressure and heart rate decreased after premedication, mainly in the midazolam group. After mask exposition in all groups noradrenaline and adrenaline levels increased with the exception of adrenaline in the midazolam-group, where the levels remained low. Mask acceptance and anxiolysis were better in the midazolam-group than in other groups. Reduction in heart rate and blood pressure, catecholamines in plasma, anxiolysis and a high mask acceptance indicate that intravenous administration of midazolam is very effective in premedicating children.

Adjuvants, Anesthesia↗
PubMed1995

Features of memory on novel situation and avoidance response: evidence from comparisons between open-field behavior and step-through task.

AIM: To study the features of memory on novel situation and avoidance response in mice. METHODS: Open-field activity and step-through latency were used to determine the memory of mice on a new environment and avoidance, respectively. RESULTS: The open-field memory was only observed 24 and 48 h after acquisition session. The avoidance memory still existed 72 and 96 h after training session. On d 1 mice were allowed to remain on open-field and step-through for 0.5, 1, 3, and 5 min. On d 2 the retention latencies in 0.5- and 1-min groups were shorter than those in 3- and 5-min groups, while the recall activities in open-field were indifferent between these groups. Scopolamine (1 mg.kg-1) and caffeine (200 mg.kg-1) injected ip 15 min before the first session inhibited the avoidance response and the adaptation to open-field environment in mice. Chlorpromazine, promethazine, picrotoxin and pentobarbital impaired the avoidance memory, but not impaired the open-field memory. CONCLUSION: These results supported the hypothesis that the adaptation of mice on open-field was a short or medium term memory.

Animals↗
PubMedDate not supplied

[Prevention of allergic reactions to X-ray contrast media. Description of the technique].

The technique of phophylaxis for allergic reactions due to contrast test in X-rays was applied in a group of 101 patients (20-60 years old). An antihistaminic (Promethazine 25 mg) and a corticosteroid (Hydrocortizone 100 mg or prednisol 60) were administered intravenously before the test. The prophylactic technique is described and satisfactory results are shown in all patients undergoing the contrast test. Undesirable effects of iodine substances in patients without an iodine allergy history were avoided with the use of this method in tests such as descending urogram, cytography, fistulography, etc. The use of drugs in the symptomatic treatment of undesirable effects of iodine in contrast test is suggested in some medical literature. This paper is the result of an experiment of a medical team from CIMEQ.

Adrenal Cortex Hormones↗
PubMed1995

Identification of potential problems for elderly outpatients after preoperative medication: a case study.

Meperidine and promethazine are preoperative medications ordered frequently for outpatient and inpatient surgical procedures in this facility. Although all medications have the potential to cause adverse reactions, the case studies presented in this article suggest a relationship between the use of one or both of these drugs and the cancellation of surgery, ie, two surgical procedures were cancelled because of the patients' behavior after administration of preoperative medication. Nurses are advised of the potential for reactions, especially in the elderly patient. Further examination of this topic is essential to prevent other episodes of adverse drug reaction or cancellation of surgical procedure and to add to the current knowledge base of effective preoperative medications.

Aged↗
PubMed1994

Detection of photoreactivity demonstrated in a modified local lymph node assay in mice.

Photoallergic and phototoxic reactions are an increasing problem in dermatologic practice. Currently available test models are heterogeneous and do not allow differentiation between photoallergic and phototoxic reactions. We have modified the local lymph node assay to screen for photoreactive compounds. We found an ultraviolet A (UVA) irradiation-dependent increase in the weights and cell counts of the auricular lymph nodes after application of 8-methoxypsoralen, tribromosalicylanilide, trichlorosalicylanilide, chlorpromazine and promethazine. In contrast to these photoreactive compounds, contact sensitizers did not produce any reaction to UVA irradiation in the local lymph node assay. This assay system has the advantage of being less expensive and less time-consuming and might even be able to differentiate between phototoxic, photoallergic and contact allergic reactions.

Allergens↗
PubMed1978

[Inhibition of non-cytotoxic histamine liberation from isolated rat mast cells by antihistaminic preparations].

Phenothiazines (chlorpromazine and promethazine) and antihistaminic quinuclidine derivatives [phencarol, quinuclidyl-3-di-(o-tolyl) carbinol, hydrochloride quinuclidyl-3-di-(o-methoxyphenyl) carbinol--HQMC] at concentrations preceding the histamine-releasing ones inhibited the compound 48/80-induced histamine release from the isolated rat mast cells. HQMC inhibited histamine release induced by selective liberators (compound 48/80, MCD-peptide, specific antigen), but potentiated histamine release induced by nonselective liberators (chlorpromazine, tryton X-100). The inhibition by HQMC of histamine release induced by compound 48/80 increased during 1 min and was reversible. The inhibitory effect of all the compounds tested was partially counteracted by glucose.

Animals↗
PubMed1994

Effects of a combined drug regimen on tumour necrosis factor and plasma kallikrein activity in experimental endotoxaemia.

OBJECTIVE: To clarify the relationship between changes in haemodynamics, liberation of tumour necrosis factor and generation of plasma kallikrein, and to see if treatment with a combination of drugs was successful in preventing activation of tumour necrosis factor and plasma kallikrein in experimental endotoxic shock. DESIGN: Controlled study. MATERIAL: 22 juvenile pigs. INTERVENTIONS: 15 animals received 0.01 mg/kg endotoxin infusion, the rest being given the same volume of saline. 10 received no treatment, and 5 were given a combination of methylprednisolone, naloxone, ketanserin, promethazine, C1 esterase inhibitor, antithrombin III and aprotinin. MAIN OUTCOME MEASURES: Assessment of the liberation of tumour necrosis factor, generation of plasma kallikrein, and haemodynamic and cellular effects of endotoxaemia. RESULTS: There was a linear statistical relationship between decreases in cardiac output and increases in packed cell volume, and between increases in packed cell volume and plasma kallikrein activity. The combination treatment totally blocked all the effects of the infusion of endotoxin. CONCLUSION: Endotoxin affects several mediators, but combination treatment can prevent some of these effects.

Animals↗
PubMed1976

Antibacterial effect of some phenothiazine compounds and R-factor elimination by chlorpromazine.

Chlorpromazine, levopromazine and promethazine exerted a bacteriostatic effect on Gram-positive bacteria at 20-60 mug/ml, on Gram-negative bacteria at 130-180 mug/ml concentration. Of the three compounds, chlorpromazine had the most marked bactericidal effect on cultures of Bacillus anthracis growing in minimal medium. In addition, chlorpromazine had a significant bactericidal effect on the resting cells of Escherichia coli suspended in saline. Pseudomonas aeruginosa was resistant to phenothiazines. Experiments have failed to derive resistant mutants from the highly sensitive B. anthracis. An effective R-factor elimination was observed at chlorpromazine concentrations of 50 mug/ml, practically not affecting the growth of multiple resistant E. coli.

Bacillus anthracis↗
PubMed1993

Histamine induces a gene-specific synthesis regulation of secretogranin II but not of chromogranin A and B in chromaffin cells in a calcium-dependent manner.

The effect of histamine on steady-state mRNA levels of three soluble secretory proteins from chromaffin granules was investigated in cultured bovine adrenal medullary cells. Histamine stimulated secretogranin II mRNA 4-fold, with no or only slight effects on chromogranin A and B transcription. After an initial lag phase, secretogranin II mRNA increased markedly between 4 and 12 h followed by a plateau phase up to 48 h. The effect of histamine on secretogranin II gene-expression was abolished by the H1 receptor antagonist promethazine but not by the H2 blocker cimetidine. The histamine-induced elevation of secretogranin II mRNA was partially reduced by the L-type calcium channel blocker nifedipine, indicating a contribution of extracellular calcium in the second messenger signaling pathway involved. At present, the H1 histaminergic receptor is the first membrane receptor found regulating secretogranin II biosynthesis in chromaffin cells. The selective up-regulation of secretogranin II mRNA but not of chromogranin A and B by histamine is another example illustrating that the synthesis regulation of secretory components co-stored in large vesicles of neuroendocrine cells is specific to the individual gene. Together with results obtained earlier, our data demonstrate a marked variation in the relative composition of peptides secreted from adrenal medulla into circulation following different physiologic conditions.

Adrenal Medulla↗
PubMed1996

Oral premedications in paediatric day surgery.

The degree of sedation in 191 day-stay children after oral premedication were compared. One hundred and forty-six were 1-5 years old (Group 1) and were randomised to receive either chloral 40 mg/kg, midazolam 0.2 mg/kg, promethazine 1 mg/kg, trimeprazine 3 mg/kg or placebo. Forty-five were 5-12 years old and were randomised to receive either trimeprazine 3 mg/kg, midazolam 0.2 mg/kg or placebo (Group 2). The children were assessed using four categories: asleep or drowsy, awake but calm, crying or anxious and oversedated or obstructed airway. They were assessed on leaving the ward, at separation from the parents, at induction, in the recovery room and one and two hours after returning to the ward. In Group 1, it was found that chloral and trimeprazine gave the best degree of sedation but the sedative effect of trimeprazine lasted longer into the post operative period. In Group 2, it was found that the children did not require deep sedation and the anxiolysis obtained with midazolam was adequate.

Administration, Oral↗