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PubMed1983

Receptor capping in mouse T-lymphoma cells: a Ca2+ and calmodulin-stimulated ATP-dependent process.

The roles that Ca2+, calmodulin, and ATP play in the redistribution of concanavalin A (Con A) binding sites on the surface of mouse T-lymphoma cells were examined. Membranes of cells labeled with fluorescein-conjugated Con A (Fl-Con A) were made permeable ("skinned") to ions and proteins by incubation in a solution containing no added Ca2+, 7 mM EGTA, and ATP. The intracellular ionic and protein concentrations could then be varied, and the degree of Con A receptor capping monitored simultaneously. A graded increase (9.0 to 30%) was found in the number of capped cells with increasing Ca2+ concentration from 10(-6)-10(-4.9) M. Increasing concentrations of trifluoperazine, chlorpromazine, and promethazine (1.5 x 10(-6) to 1.0 x 10(-4) M) in cell suspensions containing 10(-4) M Ca2+ produced graded inhibition of capping in the same order that the drugs bind to calmodulin. Removal of extracellular Ca2+ dissociated (reversed) some of the caps into patches, thus reducing their number (12%). ATP was required for either capping or cap dissociation to occur. Addition of calmodulin (3.9 x 10(-8)-6.3 x 10(-7) M) to the cell suspension increased the Ca2+ sensitivity. These results provide direct evidence that capping of Con A receptors is a reversible process (i) regulated by intracellular Ca2+ concentrations, (ii) requiring ATP as an energy source, and (iii) susceptible to the influence of calmodulin. These findings are consistent with the hypothesis that the collection of surface receptor patches into cap structures is controlled by the interaction of actomyosin filaments, which in turn is regulated by a Ca2+-calmodulin-activated control system.

Adenosine Triphosphate↗
PubMed1986

Potential therapeutic efficacy of inhibitors of human phospholipase A2 in septic shock.

Soluble phospholipase A2 has been implicated in the pathogenesis of local and systemic inflammatory reactions. Elevated levels of circulating phospholipase A2 (PLA2) correlate with the severity of circulatory collapse and pulmonary dysfunction in gram-negative septic shock. Characterization of septic shock serum PLA2 revealed a calcium-dependent enzyme with absolute 2-acyl specificity with a pH optimum of 7.5. We tested a number of therapeutic agents for their ability to inhibit PLA2 from human septic shock serum. Chloroquine, chlorpromazine, dexamethasone base, dexamethasone sodium phosphate, indomethacin, lidocaine, oleic acid, palmitic acid, promethazine, trans-retinoic acid, rutin and dl-alpha-tocopherol were all studied over the range of 10(-2) to 10(-7) M. All agents, with the sole exception of dexamethasone base, inhibited PLA2 activity at concentrations greater than 10(-3) M. PLA2 inhibition by dexamethasone sodium phosphate was factitious, due to the formation of calcium-phosphate complexes. Of the 11 agents studied, chlorpromazine was the most effective, with an IC50 of 7.5 X 10(-5) M, a membrane concentration achievable within its therapeutic range. Inhibition was non-competitive with an apparent Ki of 5 nM. Since serum PLA2 levels correlate with mortality in both experimental endotoxemia and clinical gram-negative septic shock, and chlorpromazine was previously shown to improve survival in these conditions, we postulate that its therapeutic efficacy resides at least in part in its PLA2-inhibitory activity.

Dexamethasone↗
PubMed1979

Inhibition of diamine oxidase by antihistaminic agents and related drugs.

Various drugs were tested as inhibitors of diamine oxidase on the basis of chemical relationships to the enzyme substrates. It was found that serotonine tryptamine and phenformin are good competitive inhibitors while cimetidine and pheniprazine are non-competitive inhibitors. Other antihistaminic drugs like promethazine are less powerful inhibitors.

Amine Oxidase (Copper-Containing)↗
PubMed1983

Specific binding of [3H]mepyramine to histamine H1-receptors in vascular smooth muscle membranes.

The antagonist-sensitive binding of [3H]mepyramine to beef aortic membranes was as expected for binding to histamine H1-receptors. [3H]mepyramine binds rapidly and in saturable fashion to the specific receptor sites, specific binding reaching equilibrium in 3 min at 37 degrees C. SCATCHARD's analysis of the binding data gave a dissociation constant of 3.0 nM for the radioligand-receptor complex and maximal number of binding sites: 31 fmol/mg protein. In the competition studies histamine H1-antagonists are more potent inhibitors of radioligand binding than H2-antagonist. They inhibit [3H]mepyramine binding in the following order: mepyramine greater than triprolidine greater than promethazine much greater than cimetidine. Binding data are in correlation with the previous pharmacological studies.

Aminopyridines↗
PubMed1979

The effects of metiamide and H1 receptor blocking agents on anaphylactic response in guinea-pigs.

The effects of metiamide and of four H1 receptor blocking agents (mepyramine, promethazine, clemastine and ketotifene) on anaphylactic reaction were studied in the guinea-pig. The H1 blockers conferred partial protection which shows that with the experimental protocol utilized (challenge injection with high doses of antigen), histamine plays a lesser role than other mediators released or synthesized. Metiamide (30.0 mg/kg i.v.) noticeably enhanced the increase in pulmonary resistance observed during anaphylactic reaction and reduced the protective effect of the H1 antagonists on this parameter and on histamine release. These effects might be explained by an inhibition - at least partial - of the negative feed-back mechanism through which histamine controls its own release, or by a specific action of metiamide in high doses. The transient tachycardia initially observed in anaphylactic shock is partly related to stimulation of cardiac H2 receptors by the histamine released, since it is suppressed by metiamide.

Airway Resistance↗
PubMed1984

Evaluation of the CNS properties of SCH 29851, a potential non-sedating antihistamine.

SCH 29851 [8-chloro[6,11-dihydro-11-(1-carboethoxy-4-piperidylidene)- 5-H-benzo [5,6]cyclohepta[1,2-b]-pyridine] was discovered as part of a search for a new antihistamine without effects on the central nervous system (CHS). Antihistaminic potency and duration of action of SCH 29851 and other antihistamines were assessed by inhibition of histamine-induced lethality in guinea pigs and histamine-induced paw edema in mice. Evaluation of possible CNS effects included gross observation of mice, rats, dogs and monkeys, prevention of electroshock-induced convulsions, acetic acid-induced writhing and physostigmine-induced lethality in mice and biochemical measures related to sedative liability such as displacement of in vivo 3H-mepyramine binding in mouse brain and in vitro 3H-WB 4101 binding in guinea pig cortex. Comparisons were made to several antihistamines considered to be sedative to varying degrees, including diphenhydramine, promethazine, chlorpheniramine and azatadine and to the newer antihistamines terfenadine and astemizole which are reported to be non-sedating in man at doses that antagonize the effects of histamine peripherally. SCH 29851 had antihistamine activity in the tests used with a potency at least comparable to most standards and was devoid of activity in all the functional and biochemical models used as indices of CNS activity. It is expected that SCH 29851 should be an effective, long acting, antihistamine in man without sedative effects at therapeutic doses.

Animals↗
PubMed1991

Heterogeneity of [3H]-mepyramine binding sites in guinea pig cerebellum and lung.

The nature of histamine receptors in peripheral tissues is still controversial. However, evidence of heterogeneous classes of binding sites for [3H]-mepyramine are reported in the literature. The aim of our study was, therefore, to investigate the nature of this heterogeneity by comparing [3H]-mepyramine binding in a central tissue (cerebellum) and in a peripheral tissue (lung) obtained from guinea pigs and to assess its dependence upon the temperature of incubation. The results revealed that the [3H]-mepyramine interaction in both tissues is temperature-dependent. At 25 degrees C, the interaction between [3H]-mepyramine and the receptors was biphasic in the lung while only a single class of binding site was found in the cerebellum. At 0 degrees C, [3H]-mepyramine interacted with three binding sites in the lung and two in the cerebellum. The behaviour of the reference compounds (clemastine, promethazine and histamine) also supported this temperature-dependence. Moreover, two new compounds (DF 11062 and DF 11113), synthesized in our laboratories and endowed with antihistamine activity, can differentiate between the low affinity site seen at 25 degrees C in the lung and that seen in the cerebellum at 0 degrees C.

Animals↗
PubMed1993

Effects of antipsychotic drugs on latent inhibition: sensitivity and specificity of an animal behavioral model of clinical drug action.

Latent inhibition (LI) of a conditioned emotional response (CER) has been proposed as a quantitative measure of selective attention. We have assessed the parallels of the pharmacology of LI in rats with the clinical pharmacology of schizophrenia. Drug and vehicle treated rats were divided into groups and preexposed 20 times to cage illumination as a CS, or not preexposed. All groups were conditioned with 2 CS-footshock pairings. The following day CER, as measured by interruption of drinking in response to CS presentation, was recorded. LI was observed as a decreased CER in preexposed relative to non-preexposed animals. LI was enhanced by haloperidol 0.3 mg/kg after 7 or 14 daily treatments, but not after a single acute dose. Haloperidol doses of 0.3 and 0.03 mg/kg enhanced LI, while doses of 0.003 and 3.0 mg/kg had no effect. Haloperidol enhancement of LI was unaffected by the coadministration of the anticholinergic agent trihexyphenidyl. Enhancement of LI is exhibited by the antipsychotic drugs fluphenazine, chlorpromazine, thiothixene, thioridazine, mesoridazine, and metoclopramide but not clozapine. The non-antipsychotic drugs pentobarbital, imipramine, chlordiazepoxide, trihexyphenidyl, and promethazine failed to enhance LI. LI exhibits striking parallels to the clinical pharmacology of schizophrenia.

Animals↗
PubMed1995

The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis.

Investigations conducted over the past 3 decades have demonstrated that serotonergic receptors, specifically the 5-HT2A and 5-HT2C subtypes, play an important role in the behavioral effects of hallucinogenic compounds. The present study was designed to determine the respective significance of these two receptors in the stimulus effects of LSD and (-)DOM in the rat. Specifically, the interactions of a series of serotonergic antagonists (risperidone, pirenpirone, metergoline, ketanserin, loxapine, LY53857, pizotyline, spiperone, cyprohepatadine, mesulergine, promethazine, and thioridazine) with the LSD stimulus and the (-)DOM stimulus in LSD-trained subjects was defined. From these data, IC50 values were determined for the inhibition of the LSD-appropriate responding elicited by either 0.1 mg/kg LSD (15-min pretreatment time) or 0.4 mg/kg (-)DOM (75-min pretreatment). In addition, the affinities of these antagonists for 5-HT2A and 5-HT2C receptors were determined in radioligand competition studies, 5-HT2A affinity correlated significantly with IC50 values for the blockade of the LSD (r = +0.75, P < 0.05) and (-)DOM (r = +0.95, P < 0.001) stimuli in the LSD trained subjects. 5-HT2C affinity did not correlate significantly with either series of IC50 values. These data indicate that (1) the stimulus effects of LSD, and (2) the substitution of (-)DOM for the LSD stimulus are mediated by agonist activity at 5-HT2A receptors.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗
PubMed1991

Elimination of plasmids pKM 101 and F'lac from Salmonella typhimurium and Escherichia coli by bisammonium salt. The effect of outer membrane pattern.

Plasmid-curing activity of N,N'-bis(decyldimethyl)-1,6-hexanediammonium dibromide, BDHD, was tested on six different plasmids in E. coli and plasmid pKM 101 in S. typhimurium. BDHD eliminated the F'lac plasmid from E. coli cells only with a low efficiency. Plasmid pKM 101 was eliminated from S. typhimurium cells significantly and this effect was dependent on an outer membrane pattern. A deep-rough mutant of S. typhimurium is completely resistant to curing activity of BDHD, while part-rough and smooth cells are susceptible to it. In contrast to pKM 101, a cryptic plasmid being present in S. typhimurium cells was not eliminated by BDHD. The curing activity of sodium dodecyl sulfate, acridine orange, crystal violet, and promethazine was also affected by the outer membrane pattern of S. typhimurium cells.

Cell Membrane↗
PubMed1981

Pre-anaesthetic medication in paediatric day-care surgery.

Pre-anaesthetic medication has the primary aim of making the whole process of anaesthesia smooth and agreeable. This prospective blind study was planned to compare the efficacy of three active drugs and a placebo as premedication in a paediatric population undergoing operation on a day care basis. One hundred and fifty-nine patients between one and 12 years of age were assigned randomly to one of four groups who received either hydroxyzine 0.5 mg . kg-1 (n - 43) promethazine 0.5 mg . kg-1 (n 40) diazepam 0.1 mg . kg (n - 378) or placebo (n - 36) by mouth, 60 minutes before operation. Observations in the operating room included the emotional state of the patient on arrival, quality of induction and complications. In the recovery room time for emergence from anaesthesia, complications and requirements for analgesia were recorded. The parents were asked for return a questionnaire detailing psychological and physical complications during three postoperative days. There was no difference between the groups in any of the factors examined. From this study we conclude that children undergoing surgical operations and anaesthesia on a day care basis should not receive pharmacological premedication, not because of overwhelming risk from its use, but because of the absence of any benefit.

Ambulatory Surgical Procedures↗
PubMed1980

Anaesthetic management of a patient with carcinoid tumor undergoing myocardial revascularization.

Carcinoid tumors with hepatic involvement can produce intense flushing, tachycardia, hypotension or hypertension and diarrhoea. Patients with limited cardiac reserve may not tolerate these effects under anaesthesia. Valvular heart disease associated with carcinoid tumors has been reported, but there is no record in the literature of such an association with coronary artery disease. This report presents the anaesthetic management of a patient with coronary artery disease and carcinoid tumor undergoing myocardial revascularization. Emphasis is placed on the rational use of anaesthetic and adjunctive agents which will minimize the incidence of carcinoid symptons. The salient features of the management are prevention of release of vasoactive substances by the use of promethazine hydrochloride during operation, the avoidance of stropine, prophylactic administration of corticosteroids and smooth induction of anaesthesia by the use of diazepam and dimethyl-tubocurarine iodide (Metocurine).

Aged↗
PubMed1998

Anaesthetic considerations in a patient with lepromatous leprosy.

PURPOSE: To consider the anaesthetic problems in a patient with lepromatous leprosy undergoing general anaesthesia. CLINICAL FEATURES: A 52 yr old man with lepromatous leprosy for five years was booked for elective radical nephrectomy. He received 100 mg dapsone per day po. The patient was asymptomatic for cardiovascular disease but his electrocardiogram showed complete left bundle branch block, inferior wall ischaemia with echocardiogram findings of 58% ejection fraction and left ventricular diastolic dysfunction. Other preoperative investigations (haemogram, serum urea and creatinine, liver function tests and chest X-ray) were normal. After premedication with diazepam, meperidine and promethazine, the patient received glycopyrrolate and anaesthesia was induced with thiopentone. Atracurium was given to facilitate tracheal intubation. Anaesthesia was maintained with intermittent positive pressure ventilation using N2O in oxygen with halothane. Anaesthesia and surgery were uneventful except that the patient had a fixed heart rate that remained unchanged in response to administration of anticholinergic, laryngoscopy, intubation and extubation. CONCLUSION: Patients with lepromatous leprosy may have cardiovascular dysautonomia even when they are asymptomatic for cardiovascular disease.

Adjuvants, Anesthesia↗
PubMed1999

Intubation via LMA in pediatric patients with difficult airways.

PURPOSE: To report two cases of successful tracheal intubation in difficult pediatric airways using a conventional laryngeal mask airway (LMA) with an extended polyvinyl chloride (PVC) tube after laryngeal assessment with a fibreoptic device. CLINICAL FEATURES: Two cases, Dandy-Walker and Pierre Robin syndromes, were scheduled for surgery. They were premedicated with 0.5 mg x kg(-1) promethazine p.o. 90 min before surgery. Both patients arrived in the operating room sedated, with dry mouth, and without evidence of increased intracranial tension or airway obstruction. Inhalational induction with isoflurane 0.5-3% was commenced. Conventional tracheal intubation was impossible in both cases. In each an LMA was inserted to maintain ventilation, anesthesia, and to facilitate intubation. Fibreoptic bronchoscopy was used to assess the larynx, followed by blind intubation via the LMA using extended PVC tracheal tube (TT). Anesthesia was maintained during intubation using Mapleson F anesthesia circuit attached to a connector with fibreoptic bronchoscope adapter. CONCLUSION: This report describes the assessment of the airway with fibreoptic bronchoscopy after LMA insertion facilitated blind tracheal intubation in two children with difficult airways.

Anesthesia, Inhalation↗
PubMed2001

[Factitious disorders. Hematologic, neurologic and dermatologic symptoms in a physician with factitious disorder].

HISTORY AND FINDINGS: A 38-year-old female physician was admitted with the suspected diagnosis of a myelodysplastic syndrome. The self-reported history was inconsistent and incoherent. On physical examination neurological and dermatological disorders could be found. EXAMINATIONS: A bone marrow puncture revealed a toxicity-induced bone marrow damage. Extensive examinations to evaluate the neurological symptoms did not show any pathological findings. A toxicological screening identified opioids, benzodiazepines and promethazine. TREATMENT AND COURSE: Because of the inconsistent history and the contradictory results of our clinical tests, we asked in other hospitals for past admissions and were thus able to have insight into a hospital career that grasped numerous different admission diagnoses. All presented symptoms, especially the bone marrow damage, were self-induced by the patient. CONCLUSIONS: For the first time in this patient's history, a factitious disorder was diagnosed after a hospital career of almost 10 years. In this publication, the case is thoroughly presented. Additionally, the current literature is reviewed with latest recommendations for therapeutic strategies about this poorly understood disorder.

Adult↗
PubMed1999

High concentrations of histamine stimulate equine polymorphonuclear neutrophils to produce reactive oxygen species.

OBJECTIVE AND DESIGN: Because high concentrations of histamine are locally released in inflammation, we investigated the effects of supraphysiological doses of histamine on the production of reactive oxygen species (ROS) by neutrophils. MATERIALS AND METHODS: Isolated equine neutrophils were activated by 10(-4) to 5 x 10(-3) M histamine. The production of ROS and free radicals was estimated by luminol-enhanced chemiluminescence (CL) and electron spin resonance (ESR) with spin trapping technique. In this model of histamine-stimulated neutrophils, we tested the antagonists of H1 and H2 histamine receptors, the role of Ca2+ and Mg2+, the role of staurosporine and pertussis toxin (inhibitors of protein kinase C and proteins G) and the effects of superoxide dismutase, catalase, hydroxyl radical scavengers (phenylalanine and mannitol) and N(G)-monomethyl-L-arginine (L-NMMA), inhibitor of NO-synthase. RESULTS: Histamine (from 10(-5) to 10(-3) M) stimulated neutrophils to produce CL and ESR signals characterized by spin adducts of superoxide anion and/or hydroxyl radicals. The CL response was inhibited by 10(-4) and 10(-3) M H1 receptor antagonists (promethazine, pyrilamine, and diphenhydramine), by Ca2+ and Mg2+ depletion and by 10 nmoles staurosporine. CL was partially inhibited by pertussis toxin (4 microg/ mL). The ESR signals were practically suppressed by pyrilamine (an H1 receptor antagonist) and superoxide dismutase, and partially inhibited by catalase, hydroxyl radical scavengers and L-NMMA (respectively 59, +/- 30% and 68% inhibition). CONCLUSIONS: High concentrations of histamine stimulated the neutrophils to product ROS and free radicals via H1 receptors and the NADPH-oxidase pathway.

Animals↗
PubMed1996

[Comparison of sufentanil-propofol-anesthesia with fentanyl-propofol in major abdominal surgery].

UNLABELLED: Major abdominal surgery often leads to a marked sympathoadrenal stress response with high concentrations of plasma catecholomines, hypertension, and tachycardia. We compared the effects of sufentanil-propofol with fentanyl-propofol anaesthesia in a controlled, randomised, double-blind study of 18 ASA I-II patients aged 23-64 years undergoing major abdominal surgery. Study parameters were haemodynamics (heart rate [HR], arterial [ABP], central venous, and pulmonary arterial pressures, cardiac index [CI]), arterial catecholamine concentrations, and the median frequency of the electroencephalogram (EEG) power spectrum. METHODS: After premedication with flunitrazepam 1-2 mg, promethazine 25-50 mg, and piritramide 7.5-15 mg, a five-lead electrocardiograph and a Lifescan brain activity monitor were attached and indwelling cannulae were inserted into the radial artery and two forearm veins. A thermodilution catheter was placed in the pulmonary artery via the right internal jugular vein. Anaesthesia was induced with either fentanyl 7 micrograms/kg followed by 5 micrograms/kg.h or sufentanil 1 microgram/kg followed by 0.7 microgram/kg.h up to the end of surgery. Additional boli of the opioids were given according to set criteria, resulting in an average consumption of 9.03 micrograms/kg.h fentanyl or 1.22 micrograms/kg.h sufentanil. Propofol 2 mg/kg was given followed by 6 micrograms/kg.h up to the end of surgery. Relaxation was obtained with pancuronium 0.025-0.05 mg/kg before and after induction, after tracheal intubation, before and after skin incision, after opening of the peritoneum, and at the end of surgery. RESULTS: No significant differences were observed between the two groups with regard to the study parameters. The duration of surgery and blood loss were similar in both groups, as were patient characteristics. After induction 2 patients in each group developed thoracic rigidity, which was reversible after muscle relaxation. HR, ABP, and CI decreased significantly before skin incision; after surgical stimulation the baseline values were again reached. but not exceeded. No patient developed tachycardia (> 100/min) or hypertension (> 15% higher than baseline pressure) for longer than 10 min during the study period until the end of surgery. The plasma concentrations of epinephrine and norepinephrine decreased significantly during anaesthesia, and under maximum surgical stimulation did not increase higher than the physiological baseline concentrations. The EEG median frequencies decreased after induction, and during the entire anaesthetic period the main activity was in the delta and theta frequency bands. CONCLUSIONS: With both regimens, the sympathoadrenal stress response to major abdominal surgery was nearly completely suppressed, resulting in stable haemodynamics during the operations. Sufentanil and fentanyl were equally well suited as analgesic components of total i.v. anaesthesia with propofol.

Abdomen↗
PubMed1998

[Premedication and preoperative fasting in pediatric anesthesia. Results of a survey].

This study evaluates the current practice of premedication and preoperative fasting in pediatric anaesthesia in Germany. A total of 90 questionnaires were mailed to randomly selected hospitals with departments or sections of anaesthesiology and pediatric surgery. 71 questionnaires were returned and analysed (reply rate 79%). 60% of the responding hospitals start premedication between the ages of 3 and 12 months and 32% between 1 and 2 years of age. Premedication ist most often given orally (64%), followed by rectal (29%) and intranasal (3%) routes. Midazolam is used by 96% of the respondents as the primary sedative premedication. Alternatively, promethazine and chloraldhydrate are most frequently used. Anticholinergic drugs are given routinely by 21% of the respondents. For the apprehensive child intramuscular ketamine is most often used (33%), followed by intranasal midazolam (22%), rectal midazolam (19%) and rectal thiopentone or methohexitone (13%). For children less than 1 year of age 63% of the hospitals restrict clear liquids 2 hours and 34% 3 or 4 hours before anaesthesia. 64% of the respondents require abstinence from milk for 4 hours and 30% for 6 hours prior to surgery. For children older than one year of age fasting period requirements for clear liquids were 2 hours (34%), 3 hours (27%), 4 hours (30%) and 6 hours (9%). For children over 1 year of age the majority allow solid food or milk up to 6 hours prior to anaesthesia (68% and 63%, respectively). The survey shows that premedication is started during the first two years of age by nearly all responding hospitals. Oral or rectal midazolam is the most frequently used premedication regimen. Preoperative fasting guidelines vary.

Adjuvants, Anesthesia↗