[Effect of trimecaine and its quaternary derivative G-103 on myocardial action potentials]. / Vliianie trimekaina i ego chetvertichnogo proizvodnogo Zh-103 na potentsial deistviia miokarda.

The conventional microelectrode technique was used to study the effects of trimecaine and its quaternary derivative G-103 on the action potential in the rat myocardium. G-103 suppressed the maximal rate of the action potential depolarization at lower concentrations than trimecaine although its effect developed slower: t 1/2 = 25 and 5 min, respectively. G-103 abolished the tonic component of trimecaine-induced blockade and failed to alter the rate-dependent component.

Síntesis, controles químicos y radioquímicos del "mebrofenin-Tc-99m": estudios radiofarmacológicos y usos en seres humanos / Synthesis, chemical and radiochemical cotrols of mebrofenin-Tc-99m: radiopharmacological studies and uses in humans

En este trabajo se presenta el estudio químico radiofarmacológico y el uso en seres humanos realizado con el "mebrofeini-Tc-99m". La finalidad del trabajo fue determinar el uso potencial de este radiofármaco en seres humanos portadores de distintas entidades clínico patológicas. Para esto, se sintetizó el producto mejorando el rendimiento de reacción, mediante una modificación en la segunda etapa del camino de síntesis, lo que condujo a elevarlo del 70 al 90%. Se determinó la cinética plasmática mediante la circulación extracorpórea realizada en ratas wistar, mientras que la hepática y renal se llevó a cabo en ratones endocriados. Todos los resultados fueron analizados mediante un procesador, obteniéndose las vidas medias plasmáticas y los máximos tiempos de captación (AU)

Síntesis, controles químicos y radioquímicos del "mebrofenin-Tc-99m": estudios radiofarmacológicos y usos en seres humanos / Synthesis, chemical and radiochemical cotrols of mebrofenin-Tc-99m: radiopharmacological studies and uses in humans

En este trabajo se presenta el estudio químico radiofarmacológico y el uso en seres humanos realizado con el "mebrofeini-Tc-99m". La finalidad del trabajo fue determinar el uso potencial de este radiofármaco en seres humanos portadores de distintas entidades clínico patológicas. Para esto, se sintetizó el producto mejorando el rendimiento de reacción, mediante una modificación en la segunda etapa del camino de síntesis, lo que condujo a elevarlo del 70 al 90%. Se determinó la cinética plasmática mediante la circulación extracorpórea realizada en ratas wistar, mientras que la hepática y renal se llevó a cabo en ratones endocriados. Todos los resultados fueron analizados mediante un procesador, obteniéndose las vidas medias plasmáticas y los máximos tiempos de captación

Clinical experience with the newer hepatobiliary radiopharmaceuticals.

Technetium 99m-labelled hepatobiliary imaging agents provide high resolution images not previously possible with rose bengal labelled with iodine 131. This has prompted a re-examination of the utility of these radioactive pharmaceuticals. We have found that the newer methodology provides a rapid, innocuous and accurate means of excluding acute cholecystitis from the diagnosis in patients with symptoms suggestive of this disease and of assessing surgically altered biliary anatomy. In the presence of moderate bilirubinemia, up to about 85.5 to 103 mumol/L [5 to 6 mg/dL], a definitive distinction can be made between medical and surgical jaundice.

Pharmacokinetics and metabolism of the anilide local anaesthetics in neonates. 11 Etidocaine.

The urinary elimination of etidocaine and several of its metabolites was investigated in neonates whose mothers had received one or more doses of etidocaine during labour. The urine collection period ranged among the neonates from 21.4 to 47.0 h post-partum. The total amounts of etidocaine and its metabolites recovered in neonatal urine represented a mean of 0.12% of the maternal dose. Some differences in the pattern of urinary metabolites were observed between neonates and adults. Mean half-life of elimination of etidocaine calculated from sigma-minus plots of the neonatal urinary data was 6.42 h. This is greater than that previously reported following intravenous administration of etidocaine to adults (2.6 h). The slower rate of elimination in neonates is probably due to an increased neonatal volume of distribution since there is evidence to show that etidocaine is extensively metabolised by the neonate.

Double-blind comparison of lidocaine and etidocaine during continuous epidural anesthesia for vaginal delivery.

Etidocaine 0.5% plain, etidocaine 0.5% with epinephrine 1:200,000 and lidocaine 1% with epinephrine 1:200,000 were compared in a series of patients receiving epidural anesthesia for vaginal delivery. Results, based on data from 48 patients, showed a significant increase in the duration of action (P is less than .01%), the degree of sensory analgesia (P is less than .02%) and the degree of motor blockade (P is less than .01%) in the group that received etidocaine with epinephrine compared to the remaining groups. There were no significant differences in the duration of labor or the number of complications. It was concluded that etidocaine and lidocaine in the concentrations used were unsatisfactory for labor and delivery.

Effect of p-hydroxyacetanilide, sodium sulfate, and L-methionine on the leukemogenicity of N-[4-(5-nitro-2-furyl)-2-thiazolyl]acetamide.

Dietary administration of N-[4-(5-nitro-2-furyl)-2-thiazolyl]acetamide to mice for 14 weeks followed by 16 weeks of control diet resulted in a high incidence of lymphocytic leukemia and a low incidence of forestomach squamous cell papillomas. The coadministration of p-hydroxyacetanilide at a dose of 1.0% with either 250 or 500 ppm of N-[4-(5-nitro-2-furyl)-2-thiazolyl]acetamide resulted in inhibition of leukemogenesis, whereas when p-hydroxyacetanilide was coadministered with 1000 ppm of N-[4-(5-nitro-2-furyl)-2-thiazolyl]acetamide the leukemia incidence was not significantly reduced, but the latent period was prolonged. When sodium sulfate was administered with p-hydroxyacetanilide and N-[4-(5-nitro-2-furyl)-2-thiazolyl]acetamide, leukemogenesis was partially restored. L-Methionine, fed in place of sodium sulfate, unblocked leukemogenicity inhibition by p-hydroxyacetanilide. None of these chemicals, p-hydroxyacetanilide, sodium sulfate, or L-methionine, significantly affected the incidence of forestomach papillomas induced by N-[4-(5-nitro-2-furyl)-2-thiazolyl]acetamide, although tumor incidences in all groups were low. p-Hydroxyacetanilide and sodium sulfate had no significant effect on the high incidence of stomach tumors induced by formic acid 2-[4-(5-nitro-2-furyl)-2-thiazolyl]hydrazide or bladder tumors induced by N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide.

Hepato-biliary scintigraphy and hepatography with Tc-99m diethyl-acetanilido-iminodiacetate in obstructive jaundice.

Tc-99m diethyl-IDA was used for combined serial hepato-biliary scintigraphy and processing of hepatographic curves, using a scintillation camera and an image-processing system. Patients with obstruction of the common bile duct, proven by operation, were investigated. Hepatograms from an area of interest corresponding to the periphery of the right liver lobe varied predictably with changes in the serum levels of alkaline phosphatase and bilirubin. Both anatomical and functional information was obtained. The investigation could be carried out even under reduced liver function. Hepatic uptake of the agent was noted at serum alkaline phosphatase levels up to 1000 U/l and serum bilirubin levels up to 170 mumol/l.

[Anti-arrhythmic activity of trimecaine under experimental and clinical conditions]. / Protivoaritmicheskaia aktivnost' trimekaina v eksperimente i klinike.

The antiarrhythmic properties of trimecaine, a local anesthetic, were studied. Tests on cats and rats with arrhythmia induced by stimulation with electric current and injection of aconitine, barium chloride, and calcium chloride as well as on a cell model of aconitine arrhythmia have shown that trimecaine possesses marked antiarrhythmic properties. It is more active and less toxic than procainamide hydrochloride or quinidine. Oral administration of 0.35% trimecaine solution had a favourable therapeutic effect in extrasystole in patients with complex heart valvular diseases and circulatory disorders. It is presumed that parenteral injection will produce a more rapid and prolonged antiarrhythmic effect.

Effect of diamfenetide on experimental infections of Fasciola hepatica in lambs: anthelmintic and clinical investigations.

The activity of diamfenetide (N,N'-[oxybis(2,1-ethan diyloxy-4,1-phenylene)] bis acetamide) was studied in lambs experimentally inoculated with Fasciola hepatica. The drug was given orally at a dose level of 100 mg/kg either 1,3,5,7, or 9 weeks postinoculation. It was 100% effective 1, 3, and 5 weeks postinoculation, 73% effective 7 weeks postinoculation, and 57% effective 9 weeks postinoculation. Serum gamma-glutamyl transpeptidase activity remained normal in all lambs for 5 weeks after infection; it then began to increase in infected, untreated lambs at 6 weeks, and had increased 5- to 6-fold 9 weeks postinoculation in infected lambs. This enzyme activity was the most sensitive hematologic parameter used in this test to detect hepatobiliary damage by the parasite. The drug was well tolerated at the dose level used.

Effects of adrenaline and the concentration of solution on extradural block with etidocaine.

Forty patients allocated to four groups received extradural injections of etidocaine for the performance of lower abdominal surgery. Twenty millilitre of the 1% or 1.5% solutions with or without adrenaline (1:200 000) was given in a double-blind manner. The addition of adrenaline to etidocaine did not significantly prolong the duration of analgesia, but it produced significant more motor block. Etidocaine 1.5% caused significantly longer durations of analgesia and more motor block than the 1% solution. The spread of sensory analgesia was similar with all four solutions of local anaesthetic agent.

The influence of alachlor, trifluralin, and diazinon on the development of endogenous mycorrhizae in soybeans.

Preplant incorporated treatments of 2 and 4 kg/ha of trifluralin and diazinon had no significant effect on growth, P accumulation or root colonization by mycorrhizal fungi in soybeans planted in an Andover clay loam. At 4 kg/ha, alachlor and trifluralin inhibited root development of 25 day-old plants. The 4 kg/ha alachlor treatment reduced shoot weight of 25 day old plants significantly and suppressed mycorrhizal development of 25 to 60 day old plants. At currently used commercial rates neither alachlor, trifluralin, nor diazinon affected mycorrhizal development under the conditions of the experiment.

Nonvisualization of the gallbladder by 99mTc-HIDA cholescintigraphy as evidence of cholecystitis.

Cholescintigraphy with N-substituted iminodiacetic acid (HIDA) labelled with technetium-99m is a new noninvasive technique for evaluation of the hepatobiliary system. The significance of nonvisualization of the gallbladder by this method in comparison with standard radiologic examinations was studied. In 43 healthy subjects the gallbladder was visualized by the two methods. By contrast, all 27 patients in whom the gallbladder was not visualized by cholescintigraphy had cholecystitis. When visualization failed to occur, a repeat cholescintigraphic study after an injection of cholecystokinin demonstrated the status of the cystic duct. Visualization excludes cystic duct obstruction and acute cholecystitis, whereas persistent nonvisualization indicates cystic duct obstruction.

The efficiency of diamphenethide in controlling natural infestations of Fasciola hepatica in lambs.

The activity of diamphenethide against natural infestations of Fasciola hepatica in fattening lambs was assessed on a farm with a noted history of fascioliasis. The main experimental groups, two treated and one control, grazed known contaminated pastures for a twelve week period after which they were removed to fluke-free areas to await slaughter. Three groups of four tracer lambs were each grazed for three successive four week periods with the main flock to determine continuity of infection. A single treatment with diamphenethide at 110 mg/kg bodyweight given when the sheep were removed from the trial area was 96.7% effective against the sub-chronic disease which had developed by this time. Three treatments at 110 mg diamphenethide/kg bodeweight given at intervals of four weeks during the grazing period proved to be 100% effective in preventing the establishment of the disease. Significant benefits in terms of weight gain were exhibited by the treated lambs.