Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C1323099 (sympathomimetic)
 2,957 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

1. We investigated the effects of the chronic administration of a sympathomimetic agent on energy expenditure, protein metabolism and levels of thyroid hormones and catecholamines in 10 obese subjects after a 6-week very-low-calorie-diet programme (1965 kJ, 60 g of protein, 45 g of carbohydrates). L-(-)-Ephedrine hydrochloride (50 mg three times a day by mouth) or placebo were administered during 2-week periods (weeks 2-5 of the VLCD programme) in a randomized, double-blind, cross-over design. Five subjects began with ephedrine and five with placebo. 2. The results were analysed separately in the two groups. No difference was found between them as regards weight loss during the very-low-calorie diet and drug treatments. Conversely, ephedrine therapy induced a significantly lower daily urinary excretion of nitrogen (and, consequently, a better nitrogen balance) with respect to placebo, independently of the drug sequence. Daily urinary levels of 3-methylhistidine during ephedrine and placebo treatments were similar. The fasting resting metabolic rate (oxygen consumption, ml STP/min) fell significantly during the very-low-calorie diet in both groups, but this effect was partially and significantly prevented by administration of ephedrine. Diet therapy significantly reduced 24 h urine levels of vanillylmandelic acid and homovanillic acid, which, however, increased to pretreatment values during ephedrine treatment. No significant effects were shown on 24 h urinary concentrations of adrenaline, noradrenaline and dopamine during the very-low-calorie diet and/or ephedrine treatment.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effects of chronic administration of ephedrine during very-low-calorie diets on energy expenditure, protein metabolism and hormone levels in obese subjects. 131 Sep 22

Hexoprenaline is a selective beta 2-mimetic drug used in tocology for the prevention of premature labor and immature birth. From clinical application of the drug in bronchospasm therapy its selectivity, which is due to the elongated nitrogen substituent, is well-known. Because of the relatively small stimulation of cardiac beta 1-receptors the side-effects related therewith are less pronounced than with other beta-mimetics. The extent of tachycardia depends on the initial sympathomimetic condition of the patients. The success rate for hexoprenaline tocolyses is 34-78%, dependent on the initial tocological condition. The advantage of hexoprenaline compared with other tocolytics on the basis of experience made so far seems to relate to the smaller increase in chronotropy and the better tolerability.
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PMID:[Hexoprenaline--a new tocolytic for treatment of premature labor]. 299 31

To investigate metabolic and endocrine changes in the fetus during prolonged maternal tocolysis with beta sympathomimetic drugs, ritodrine hydrochloride (2.1 micrograms/kg per minute) was infused into pregnant sheep near term. Confirming earlier studies, maternal plasma metabolite and hormone levels changed greatly during the first six to eight hours of infusion. Changes in the fetus paralleled these closely: glucose, lactate, and insulin increased sharply, but glucagon and alpha-amino acid nitrogen decreased. After this, most maternal and fetal plasma metabolite and hormone levels returned to the normal range and were unchanged by infusion for 72 to 96 hours. Fetal lactate levels, however, remained elevated. Similar changes occurred during interrupted maternal infusions of ritodrine. Prolonged infusion of ritodrine leads to diminished responsiveness in beta-adrenergic mechanisms regulating maternal plasma metabolite and hormone levels. Comparable unresponsiveness of fetal beta-adrenergic mechanisms, though less certain, could increase hazards during delivery and adaptation to postnatal life.
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PMID:Maternal and fetal metabolic effects of prolonged ritodrine infusion. 393 9

Albumin, total protein, total bilirubin, glucose, cholesterol, triglycerides, blood urea nitrogen, alkaline phosphatase and glutamic oxaloacetic transaminase levels were determined in the serum of cord blood of neonates born to mothers previously treated with the betamimetic drug fenoterol. The results were compared with those of untreated controls. More deviations from the control were found if the interval between termination of treatment and delivery was shorter than 48 hours. A longer drug-free interval seems more favourable for the metabolic balance of the newborns. Newborns whose mother has received beta-sympathomimetic tocolytic treatment need careful supervision.
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PMID:The effect of fenoterol on fetal metabolism: cord blood studies. 398 50

The disposition and metabolism of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801), a new agent with potent anticonvulsant, central sympathomimetic, and apparent anxiolytic properties, was studied in rats, dogs, and rhesus monkeys. [3H]benzene-MK-801 was administered orally at a dose of 1 mg/kg. MK-801 was measured in plasma by GLC using a nitrogen detector; the overall sensitivity of the method was 3 ng/ml. Radioactivity was excreted mainly in urine of dogs and monkeys but fecal excretion in rats was also extensive. The apparent plasma t1/2 of MK-801 in the rat and dog was approximately 1 hr. Maximal plasma levels of MK-801 in the rat, dog, and monkey were 46 (0.5 hr), 16 (0.25 hr), and 10 (2 hr) ng/ml, respectively. Radioactivity was extensively excreted in rat bile and was widely distributed among various tissues. Major metabolites of the drug in rat and dog urine were the 2- and 8-hydroxy analogs (rat) and the N-hydroxy derivative (dog).
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PMID:Disposition and metabolism of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imine in rats, dogs, and monkeys. 613 97

In previous papers dealing with the study of the conformations and the biopharmacological activity of conformationally restrained analogs of sympathomimetic catecholamines (NE and ISO), proposals were advanced for the three-dimensional molecular models A, B, and C; these models provided information about the steric requirements for the direct activation of alpha 1, alpha 2,beta 1, and beta 2 adrenoceptors, respectively. The 1-(aminomethyl)-6,7-dihydroxyisochromans 11 and 12 and the 1-(aminomethyl)-5,6-dihydroxyisochromans 13 and 14 (1-AMDICs) are two different types of semirigid analogs of NE and ISO. The alpha 1, alpha 2, beta 1, and beta 2 adrenergic properties of the 1-AMDICs 11-14 were evaluated in vitro, both by radioligand binding assays and by functional tests on isolated preparations, and were compared with those of their parent compounds (NE and ISO). The results of a conformational study carried out by means of both 1H NMR spectrometry and theoretical calculations indicated that, in these 1-AMDICs, the presumed active groups (aryl moiety, amine nitrogen and benzylic ethereal oxygen) are in a spatial relationship corresponding to the one found for NE and ISO in their preferred conformations, which also proved to be the pharmacophoric conformation in the models A-C. By means of a comparison of the stereostructures of the 1-AMDICs 11-14 with their biopharmacological properties, it was possible to obtain a further definition of the model B with respect to the activation of the alpha 2 adrenoceptors; the superimposition of the 1-AMDICs 11 and 12 with the molecular model C made it possible to detect an area of the beta-adrenergic receptors which might hinder the fit of adrenergic drugs that are analogs of catecholamines with these receptors.
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PMID:Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives. 823 93

Methylephedrine is a sympathomimetic amine that appears in many over-the-counter cough and cold medications throughout the world. The abuse of methylephedrine-containing medications has been reported in Japan. Although methylephedrine is not available in the United States, it was identified in 15 cases received by the Forensic Toxicology Laboratory, Division of Forensic Toxicology, Office of the Armed Forces Medical Examiner, Armed Forces Institute of Pathology over a two-year period; 12 of the 15 cases were collected from patients or decedents located within the confines of the continental United States. Methylephedrine was identified in each case by gas chromatography-nitrogen-phosphorus detection following an alkaline extraction and subsequently confirmed using full scan electron impact mass spectrometry. Quantitation of underivatized methylephedrine was performed using the same technique. Blood methylephedrine concentrations ranged from less than 0.05 to 0.28 mg/L (n = 14), and the mean methylephedrine concentration in urine was 1.6 mg/L (range, 0.15-6.8, n = 11 [excluding case 6]). A literature search revealed little information pertaining to the interpretation of methylephedrine concentrations in the blood. Six of the 15 cases presented here were positive for methylephedrine in the blood. Three of these cases were postmortem cases, and the other three cases were nonfatal aircraft mishaps. There is no evidence in any of these cases that methylephedrine was present at toxic concentrations; therefore, it appears from the cases reviewed in this study that blood methylephedrine concentrations less than 0.3 mg/L are not associated with significant toxicity.
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PMID:Methylephedrine concentrations in blood and urine specimens. 968 34

A method was developed that permitted rapid identification in urine of the following sympathomimetic amines: amphetamine, benzphetamine, cathinone, desmethylsegiline, diethylpropion, ephedrine, fenfluramine, mazindol, methylenedioxyamphetamine, methylenedioxyethylamphetamine, methylenedioxymethamphetamine, mescaline, methamphetamine, methcathinone, methylaminorex, methylphenidate, pemoline, phendimetrazine, phenylepherine, phentermine, phenylpropanolamine, pseudoephedrine, and selegiline. In addition, two alpha-phenylethylamine-like monoamine oxidase inhibitors, phenelizine and tranylcypromine, were studied. Those sympathomimetic amines containing a primary or secondary amine, a hydrazine, and/or hydroxyl (except mazindol) functional groups were derivatized effectively using an on-column derivatization technique that used a reagent consisting of 10% fluoroanhydride in hexane, whereas the other sympathomimetic amines, including mazindol, were analyzed underivatized. Three different fluoroanhydrides, trifluoroacetic (TFAA), pentafluoropropionic (PFPA), and heptafluorobutyric (HFBA), and three different injection-port temperatures (160, 200, and 260 degrees C) were investigated. Both TFAA and PFPA gave sympathomimetic amine derivatives with essentially identical retention times, whereas HFBA gave longer retention times and better separation of individual compounds. The base fragmentation ion was noted to increase 50 amu (CF2) for each derivatized sympathomimetic amine as the length of the carbon-fluorine chain increased. Fragmentation ion abundance was maximized at an injection-port temperature of 260 degrees C, and this enhanced sensitivity coupled with the better chromatographic resolution of the individual sympathomimetic amines prompted the selection of HFBA as the derivatizing agent of choice. Assignments were made for the fragmentation ions produced by each derivatized drug. The developed method was adapted to analyze urine specimens that might be encountered in emergency toxicology testing. For identification of sympathomimetic amines requiring derivatization, 0.1 mL of the patient specimen had amphetamine-d5 and methamphetamine-d5 added as internal standard followed by adjustment of pH to 9.3 with borate buffer, extraction with 9:1 chloroform/isopropanol, centrifugation and separation of the organic phase, addition of 10% methanolic HCI and evaporation under nitrogen, reconstitution with HFBA reagent, and on-column derivatization during gas chromatographic-mass spectrometric (GC-MS) analysis. For those sympathomimetic amines not requiring derivatization, 1.0 mL of urine specimen had diazepam-d5 added as internal standard followed by the same extraction procedure and reconstitution accomplished with ethyl acetate. Because precolumn derivatization was eliminated and only 8 min was required for GC-MS analysis, complete analysis time was approximately 30 min, making the method suitable for clinical emergency toxicology purposes.
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PMID:GC-MS identification of sympathomimetic amine drugs in urine: rapid methodology applicable for emergency clinical toxicology. 1077 41

The elimination of Xe133 from a deposit in the subcutaneous adipose tissue adjacent to the anterior tibial muscle was recorded by an external scintillation detector in 16 human subjects in sitting and in supine body position in a neutral environmental temperature (28 degrees C). The xenon clearance rate was increased in supine compared to sitting body position by a mean of 33%. I also studied the effect of a sympathomimetic beta 2-receptor stimulating agent using the same technique in 16 supine subjects. A perorally administered ester of terbutaline increased the xenon-elimination rate by a mean of 103%. The increased xenon-elimination rates in the supine body position and after the drug administration may reflect corresponding increases in adipose-tissue blood flow. The findings are in accordance with earlier measurements of an increase in central and peripheral blood flow and an increased whole-body, nitrogen-elimination rate during supine body position. The results might be of importance in decompression routines and in the treatment of decompression sickness.
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PMID:The effects of body position and a vasodilator on xenon133 elimination from human subcutaneous fat. 1089 64

The application of liquid nitrogen to the skin induces inflammation and pain. However, there is little data on the role of inflammatory mediators in the production of these symptoms. We have developed an experimental model to study some aspects of the inflammatory response and its mediators following the application of cold. We have applied liquid nitrogen jets to subcutaneous air pouches in the dorsal skin of rats to study the kinetics of the migration of inflammatory cells; also to the ear for histopathological analysis and on the paws for edema and pain. Inflammatory mediators were identified by pharmacological means. The results showed that the cellular inflammatory response was characterized by persistent cell migration, mainly of granulocytes. Histopathology of the ears confirmed these findings. Histamine and sympathomimetic mediators were mainly responsible for the resultant swelling. However, the hypernociception that resulted involved other mediators including IL-1 and eicosanoids. These data suggest that interference with the release of inflammatory mediators might reduce the side effects of cryosurgery and prevent hyperalgesia and inflammation at the site of application of cold.
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PMID:Different inflammatory mediators induce inflammation and pain after application of liquid nitrogen to the skin. 1700 73


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