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At least 127 records · Page 7Linked to original sources

PubMed1983

Hyperthermic responses to central injections of some peptide and non-peptide opioids in the guinea-pig.

Intracerebroventricular administration of prototype non-peptide opioid receptor (mu, kappa, sigma) agonists, morphine, ketocyclazocine and N-allyl normetazocine (SKF 10,047) and an agonist at both kappa and sigma receptors, pentazocine, induced hyperthermia in guinea-pigs. Similar administration of peptide opioids like beta-endorphin (BE), methionine enkephalin (Met-E), leucine enkephalin (Leu-E) and their synthetic analogues D-ala2-methionine-enkephalinamide (D-ala2-Met-E) and D-ala2-leucine-enkephalinamide (D-ala2-Leu-E) also caused hyperthermia. Of the three anion transport systems (iodide, hippurate and liver-like) present in the choroid plexus, only the liver-like transport system seems to be important to central inactivation of beta-endorphin, D-ala2-Met-enkephalin and D-ala2-Leu-enkephalin since iodipamide (an inhibitor of the liver-like transport system) augmented the hyperthermia. Prostaglandins (PG) and norepinephrine (NE) were not involved in peptide- and non-peptide opioid-induced hyperthermia because a prostaglandin synthesis inhibitor, indomethacin, and an alpha-adrenergic receptor blocker, phenoxybenzamine, had no thermolytic effect. Likewise cAMP was not required since a phosphodiesterase inhibitor, theophylline, did not accentuate the hyperthermia due to administration of peptide and non-peptide opioids. Naloxone-sensitive receptors were involved in the induction of hyperthermia by morphine and beta-endorphin since naloxone attenuated the effect. In contrast, the hyperthermic responses to ketocyclazocine, SKF 10,047, pentazocine, Met-enkephalin, Leu-enkephalin, D-ala2-Met-enkephalin and D-ala2-Leu-enkephalin were not antagonized by naloxone. Lack of antagonism of naloxone on pyrogen, arachidonic acid, PGE2, dibutyryl cAMP and NE-induced hyperthermia indicates that endogenous opioid peptides are not likely to be central mediators of the hyperthermia induced by these agents.

Animals↗

PubMed1996

Characterization of site I on human serum albumin: concept about the structure of a drug binding site.

Human serum albumin (HSA) possesses at least three sites or areas for high-affinity binding of drugs. Of these sites, site I was investigated by series of ultrafiltration and equilibrium dialysis experiments. Three ligands, acenocoumarol, dansyl-L-asparagine (DNSA) and n-butyl p-aminobenzoate (n-butyl p-ABE) were employed as marker ligands. Each ligand binds to a single high-affinity site on HSA, and binding studies with different pairs of the ligands revealed independent high-affinity binding. Preliminary displacement studies performed with the typical site I binding drugs warfarin, phenylbutazone and iodipamide showed different displacement patterns of the three marker ligands. These studies were followed by stringent competition experiments involving all possible combinations of the three test ligands themselves and of these and the three marker ligands. On the basis of the results obtained it seems that the acenocoumarol and DNSA binding regions correspond to the warfarin and azapropazone binding regions, respectively, of site I reported by others (Fehske, Schläfer, Wollert and Müller (1982) Mol. Pharmacol. 21, 387-393). The new binding region, represented by n-butyl p-ABE, is probably located adjacent to the acenocoumarol binding region but apart from that of DNSA. We have elaborated a model for binding site I in which we propose novel nomenclatures, region Ia, Ib, and Ic for the acenocoumarol, DNSA and n-butyl p-ABE binding regions, respectively. Furthermore, the relation between these regions and the high-affinity binding sites for other drugs have been discussed.

Acenocoumarol↗

PubMed1987

A particulate contrast agent with potential for ultrasound imaging of liver.

Ultrasonic backscatter and attenuation coefficients of a medium can be increased by the addition of solid, micron sized inhomogeneities. A potentially useful agent for ultrasonic contrast of liver images has been identified. Iodipamide ethyl ester (IDE) particles can be produced in the form of dense, relatively incompressible solids with high impedance mismatch to water. The chemical, biomechanical, and pharmacological properties of the small, uniform diameter IDE particles permit safe intravenous injection followed by rapid accumulation by reticuloendothelial (RE) cells of the liver and spleen, and later elimination from these organs. Since the particles are phagocytized by RE cells, present in normal liver but not in tumors and many lesions, the selective enhancement of ultrasonic backscatter should improve detectability of lesions which are hypo- or iso-echoic compared to surrounding tissue. The mechanisms of particle-ultrasound interaction may be described by relative motion attenuation, and scattering from a cloud of dense, incompressible spheres for the case of IDE particles in agar. Thus, values of attenuation and backscatter can be controlled by choice of ultrasound frequency and particle concentration and size. When the particles are accumulated in rat livers, additional mechanisms induce attenuation and backscatter in excess of that predicted by IDE in agar. This preliminary work demonstrates that solid, biocompatible particles may be useful as an ultrasonic contrast agent.

Animals↗

PubMed1976

Single bolus versus drip infusion for intravenous cholangiography.

Biliary tract visualisation in 50 patients examined by infusion of methylglucamine iodipamide was compared, by double-blind technique, to cholangiograms obtained in 50 other patients by a single bolus injection. The infusion technique did not give better results than the single bolus method. In another group of 20 patients, each individual was examined by both methods. The radiographs, read in a double-blind manner, showed both methods to be comparable in demonstrating the biliary system. It seems that other means have to be designed and employed in order to improve the radiographic delineation of the biliary tract.

Cholangiography↗

PubMed1981

Intravenous cholangiography by bolus injection of meglumine iotroxamate and meglumine iodoxamate: a comparative trial of two new contrast media.

The meglumine salts of iodoxamic and iotroxamic acids are recently developed intravenous cholangiographic media. In several studies these two media have been shown to be significantly better than meglumine iodipamide and meglumine ioglycamate for opacification of the biliary tree and incidence of adverse effects. As part of a multi-centre double-blind trial 100 patients were given iodoxamate or iotroxamate. Comparisons of opacification, side effects and renal excretion of contrast were made. The results showed no statistically significant difference in biliary tree opacification; more frequent renal excretion of contrast with iodoxamate; and contrary to previous reports a slightly higher incidence of side effects with iotroxamate.

Biliary Tract↗

PubMedDate not supplied

Preclinical evaluation of an iodinated particulate contrast agent for use during angiography: work in progress.

PURPOSE: To study the feasibility of using an iodinated particulate contrast agent, iodipamide ethyl ester (IDE), for angiography. MATERIALS AND METHODS: IDE at doses of 40-100 mg of iodine per kilogram was diluted to a total volume of 5-20 mL and used for digital subtraction angiography in nine dogs under general anesthesia. Equivalent images were obtained by using water-soluble contrast medium (WSCM) for comparison (iohexol) in seven animals. All images were reviewed by blinded reviewers and graded subjectively on a five-point scale. RESULTS: Angiographic studies of multiple vascular territories performed with IDE yielded images of slightly lower overall quality compared with images obtained with WSCM (P = .14, Mann-Whitney U test). Arterial phase images were subjectively superior with WSCM when compared with IDE (P < .0001, chi 2.) Depiction of the corresponding veins during the venous phase on the IDE angiograms was superior to that on WSCM angiograms in 12 of 21 cases, although this did not reach statistical significance (P > .05 chi 2). Images of the renal vein and portal vein achieved with IDE were graded as superior to those achieved with WSCM in eight of 10 reviews. CONCLUSION: Angiography is feasible with IDE. Compared with WSCM, IDE produced images of lesser quality during the arterial phase, but of equal or superior quality in the venous phase depending on the vessel studied. Because it is excreted slowly in bile and is isotonic, it may prove useful in patients with renal insufficiency, diabetes, multiple myeloma, or severe coronary disease.

Angiography, Digital Subtraction↗

PubMed1995

Comparison of patient reactions and diagnostic quality for hysterosalpingography using ionic and nonionic contrast media.

RATIONALE AND OBJECTIVES: We compared adverse reactions and image quality for hysterosalpingography (HSG) performed with ionic (diatrizoate meglumine combined with iodipamide meglumine [DM + IM]) and nonionic (iohexol) contrast media. METHODS: We performed a study of 95 patients who had HSG and were randomly selected to receive DM + IM or iohexol. Patients reported episodes of abdominal pain and other adverse reactions immediately and 24 hr after the procedure and categorized severity of symptoms on a subjective scale. Two radiologists evaluated image quality for diagnosis. RESULTS: Prevalence of abdominal pain and other reactions both immediately and 24 hr after HSG was lower in patients who received iohexol than in patients who received DM + IM. Moderate or severe abdominal pain was significantly lower in the iohexol group than in the DM + IM group (p < .05). Visualization of the uterine cavity and ampullary rugae was judged excellent with both contrast media (87% with iohexol and 92% with DM + IM). CONCLUSION: Iohexol and DM + IM are excellent contrast media for use during HSG; iohexol 300 may cause fewer episodes of more severe and prolonged abdominal pain.

Abdominal Pain↗

PubMed1995

Lesion visualization by targeted computed tomography liver enhancement in dogs.

RATIONALE AND OBJECTIVES: We conducted a pilot study to determine the potential advantages of using liver-specific targeted computed tomography (CT) contrast agents for lesion detection. METHODS: Eight dogs had liver infarcts created by percutaneous injections of ethanol. Each dog underwent CT scans with four imaging techniques: unenhanced, intravenous contrast enhanced (IVCE), CT arterial portography (CTAP), and targeted liver enhancement with iodipamide ethylester (IDE) particles. Lesions were assessed quantitatively to determine liver-to-lesion density differences and the drop in density across liver edge as a quantitative measure of edge sharpness. Expert readers subjectively analyzed data to determine lesion visibility and edge sharpness. RESULTS: Liver-to-lesion density differences were greatest with CTAP (56.4 +/- 35.5 Hounsfield units [H]) followed by IDE (41.1 +/- 7.0 H), i.v. (22.7 +/- 6.0 H), and unenhanced scans (13.6 +/- 4.1 H; ps < .05 for CTAP versus unenhanced and IDE versus unenhanced). Edges were best defined both subjectively and quantitatively on IDE-enhanced scans. CONCLUSION: Targeted liver-specific contrast agents have potential to increase lesion visibility when compared with standard i.v. contrast enhancement of the liver by increasing lesion edge definition and liver-to-lesion attenuation differences. Further work in animal tumor models, and clinical trials as agents become available, appears justified.

Animals↗

PubMed1978

Pharmacocholangiography.

The effect of ouabain and atropine on bile flow and bile iodine concentration in intravenous cholangiography was investigated in 4 cholecystectomized dogs (20 experiments) with complete bile diversion under general anesthesia and compared to the effect of sodium taurocholate. Iodipamide was administered intravenously with an initial priming dose of 50 mg per kg followed by a constant infusion of 2 mg per min per kg. Ouabain in stepwise increasing infusion rates, .0625 to .25 microgram per min per kg, had no significant effect. Atropine infusion rates from 1 to 8 microgram per min kg increased the bile iodine concentration up to 19% but already a 14% increase with a 5% reduction in bile flow was found with the smallest atropine dose. The lowest taurocholate infusion rate resulted in the highest bile iodine concentration and lowest bile flow. It is suggested that atropine premedication and low bile salt plasma levels might improve the opacification of the biliary tree particularly in hepatic dysfunction by reducing selectively specific fractions of the basal bile flow.

Anesthesia, General↗

PubMedDate not supplied

Effect of endotoxemia on contrast media reactions.

Since complement activation is sharply temperature-dependent, we have examined the effects of fever produced by a very small dose of endotoxin on contrast media lethality in rabbits. After the injection of 8.2 ml/kg of 52% methylglucamine iodipamide, a group of rabbits exhibiting an average temperature elevation of 1.5 degrees C had a 100% mortality rate. This was contrasted to a 30% mortality in control rabbits receiving contrast alone, and no mortality in rabbits receiving endotoxin alone. The rabbits with fever and increased mortality exhibited increased activation of serum complement. From this preliminary data it appears that caution should be observed in performing a contrast examination in a patient with endotoxemia and/or a fever.

Animals↗

PubMedDate not supplied

Uptake of contrast materials by experimental acute myocardial infarctions: a preliminary report.

The concentration of iodine within infarcted and normal myocardium after intravenous administration of contrast material was determined by fluorescence excitation analysis in seven dogs at 48 hours after coronary arterial ligation. The iodine concentration of infarcted myocardial tissue was several times greater than normal myocardium after administration of meglumine/sodium diatrizoate, iodipamide, and an experimental polymer of iothalamic acid.

Acute Disease↗

PubMedDate not supplied

Glucocorticoid-induced elevations of C1-esterase inhibitor: a mechanism for protection against lethal dose range contrast challenge in rabbits.

Rabbits pretreated with methylprednisolone acquired significant protection against an intravenous challenge of meglumine iodipamide. In comparison to controls, the pretreated rabbits showed moderate elevations of Factor XII, and rather striking elevations of C1-esterase inhibitor. Treated rabbits also showed significantly less granulocytosis. It is believed that the protective effect can be ascribed to the modulation of acute phase reactants by increased concentrations of C1-esterase inhibitor.

Animals↗

PubMedDate not supplied

Release of serotonin from human platelets in vitro by radiographic contrast media.

Both ionic and nonionic, monomeric and dimeric contrast media were found to release serotonin from intact human platelets in vitro. The monomeric contrast media were compared at the concentration range of 25 mg I/ml. Iothalamate was the strongest and the statistically equal metrizamide iopamidol, and P-297 were the weakest releasers. Monomeric and dimeric contrast media were compared at concentration ranges of 50 and 100 mg I/ml. They ranked, in descending order of serotonin releasing potency: iodipamide, iothalamate, P-127, iopamidol, and a statistically indistinguishable group of the monoacid dimer P-286, the nonionic dimer ZK 74 435, and metrizamide. The capability of contrast media to release serotonin seems to be a composite result of their specific physical and molecular structural properties.

Adult↗

PubMed1985

Digital radiographic evaluation of the bile ducts.

This study compares digital radiographic images of the bile ducts in dogs with images obtained using routine radiography. The dogs were infused with iodipamide (2 ml/minute for 30 minutes), and the bile ducts were imaged at 60 minutes using plain radiograph and five digital techniques: (1) dual-energy, (2) DSA-hybrid prepixel shift, (3) DSA-hybrid postpixel shift, (4) a dual-energy film system--Digirad, and (5) scan projection radiography using hybrid subtraction. Six radiologists who were not familiar with digital radiography evaluated the six different studies. The images were presented in a randomized order and each image was evaluated on a five-point scale. There was no difference between the plain radiographs and the dual-energy images. Both of these studies were rated significantly better (P less than .001) than the other four digital images. These results suggest that digital radiography during direct cholangiography may be easily accomplished using a 10% to 15% iodine solution.

Animals↗

PubMed1988

Particulate suspensions as ultrasonic contrast agents for liver and spleen.

Ultrasonic backscatter and attenuation coefficients of a medium can be increased by the addition of solid, micron-size inhomogeneities. A potentially useful agent for ultrasonic contrast of liver images has been identified. Iodipamide ethyl ester (IDE) particles can be produced in the form of dense, relatively incompressible solids with high impedance mismatch to water. The chemical, biochemical, and pharmacologic properties of the small, uniform diameter IDE particles permit safe intravenous injection followed by rapid accumulation of reticuloendothelial (RE) cells of the liver and spleen, and later elimination from these organs. Since the particles are phagocytized by RE cells, present in normal liver but not in tumors and many lesions, the selective enhancement of ultrasonic backscatter should improve detectability of lesions that are hypoechoic or isoechoic compared with surrounding tissue. The mechanisms of particle-ultrasound interaction may be described by relative motion attenuation, and scattering from a cloud of dense, incompressible spheres for the case of IDE particles in agar. Thus, values of attenuation and backscatter can be controlled by choice of ultrasound frequency and particle concentration and size. When the particles are accumulated in rat and rabbit livers, additional mechanisms induce attenuation and backscatter in excess of that predicted by IDE in agar. This preliminary work demonstrates that solid, biocompatible particles may be useful as an ultrasonic contrast agent.

Animals↗

PubMed1994

Fractal analysis of renal cortical perfusion.

RATIONALE AND OBJECTIVES: Contrast-enhanced computed tomography (CT) images of canine renal cortex were analyzed to determine if the heterogeneous pixel intensity patterns met the requirements for fractal analysis and if the heterogeneity could be quantified by a fractal dimension, Df. METHODS: Contrast-enhanced CT images were obtained after injection of iodipamide ethyl ester (IDE), a vascular marker, or iohexol, a freely filtered interstitial marker, into the catheterized renal artery of an anesthetized dog. Images were mounted on a graphics workstation for analysis. A computer program was written to determine the fractal dimension of the pixel-intensity pattern within selected regions. RESULTS: All regions of renal cortex examined met the requirements for fractal analysis. Three seconds after injection of IDE, the mean fractal dimension decreased significantly from 1.21 +/- 0.05 to 1.12 +/- 0.06 (P < .05). Although the mean fractal dimensions were not significantly different, the variation in the fractal dimension around the renal cortex was significantly different with IDE as compared with iohexol at 3 seconds (P < .05). Differences in the change in fractal dimension over time were also observed with IDE as compared with iohexol. CONCLUSIONS: Fractal dimension measurement provides a new means to examine the in-vivo organization of renal vascular perfusion by quantifying pixel heterogeneity in contrast-enhanced CT. This may prove useful in understanding and quantifying the pathophysiologic changes in renal disease.

Animals↗

PubMed1977

Selectivity of food colours for different organic acid transport systems in rat renal cortex.

Seventeen food colours were tested as inhibitors of the simultaneous uptake of labelled o-iodohippurate and iodipamide into slices of rat renal cortex. The results have been interpreted in terms of inhibition of two different aniontransport systems: the hippurate of H-system and the liver-like L-system. No clearcut relation was found between inhibition ability and system specificity on the one hand and moleculr weight or structure on the other. However, most disulphonic azo dyes and quinoline yellow show an L-system affinity while tri-and tetra-sulphonic azo dyes, triarylmethanes and erytrosine show very little predilection for either of the two systems.

Animals↗

PubMed1979

Organic anion and cation transport in vitro by dog choroid plexus: effects of neuroleptics and tricyclic antidepressants.

Dog lateral choroid plexus accumulates the cation 14C-emepronium and the divalent anion 125I-iodipamide in vitro. At 10 micron, high potency neuroleptics with a substituted piperazine side chain and also haloperidol depress only the uptake of the cation and even stimulate the uptake of the anion. In contrast, at 1--10 micron, the accumulation of both test substances is inhibited by neuroleptics and tricyclic antidepressants with an aliphatic side chain. Such unspecific effects on seemingly unrelated transport systems at concentrations reached clinically in the CSF might explain some side actions of low potency neuroleptics and antidepressants.

Animals↗