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At least 19 recordsLinked to original sources
PubMed1984

[Therapeutic efficacy of trimecaine in cardiac rhythm disorders and ways of improving it].

The efficacy of antiarrhythmic therapy with trimecain in 5 different regimens was studied in 87 patients, in 146 episodes of various disorders of the cardiac rhythm. On the basis of clinical and experimental (on 14 dogs with ventricular arrhythmia) studies, different schemes of trimecain treatment are compared. It was shown that combination of the intravenous and the subsequent intramuscular administration of trimecain to treat ventricular extrasystole complicating the course of acute myocardial infarction is as effective as prolonged instillation but exerts a longer action and is better tolerated by patients. Using tetrapolar chest rheography the effect of trimecain infused in the maximum single dose on the central hemodynamics and the ECG was studied in subjects without any cardiovascular pathology. It has been established that trimecain does not suppress myocardial contractility and has no hypotensive action.

Acetanilides↗
PubMed1991

[Changes in pharmacokinetics of trimecaine in patients with liver cirrhosis].

Trimecaine (Mesocain, Léciva) an analogous preparation to lidocaine is used as a local anaesthetic, antiarrhythmic and spasmolytic preparation. The purpose of the investigation was to assess the fate of trimecaine in nine patients with compensated cirrhosis of the liver. The pharmacokinetics were evaluated after intravenous infusion of trimecaine administered at a rate of 150-200 mg.h-1. Plasma concentrations of the drug evaluated by gas chromatography indicate a marked retardation of trimecaine elimination in patients with liver damage. In the group of patients with cirrhosis of the liver the total clearance of the drug was lower (8.7 +/- 5.0 1.h-1), as compared with the group of patients without liver damage (34.7 +/- 19.4 1.h-1). In patients with cirrhosis of the liver also a multiple reduction of distribution volumes was observed. The results indicate a high hepatic extraction of

Humans↗
PubMed1983

[Comparative clinical study of the effectiveness of the new anti-arrhythmia agents, trimecaine and pyrromecaine].

The antiarrythmic effects of trimecain and pyromecain were studied in 53 patients with frequent ventricular premature beats. Trimecain was given to 22 patients and pyromecain was given to 31. The efficiency of both intravenous and oral drug administration was considered. Comparative drugs--lidocain, mexityl, procainamid were parallely used. The efficiency criterion was the decrease in mean ventricular premature beats per hour by 50% or more during ECG-monitoring. A positive antiarrhythmic effect of intravenous trimecain was observed in 35.3% of the patients, that of pyromecain was in 18.2% and after administration of a related compound lidocain, it was seen in 30.0% and 26.7%, respectively. Trimecain in tablets proved to be efficacious in 15.4% of the patients in a single dose and in 18.2% after its long-term therapy, while mexityl, a comparative agent was efficacious in 63.6%. Pyromecain in tablets did not lead to decrease in ectopia either during an "acute" test or during the long-term therapy whereas procainamid was effective in 37.3% of the patients studied.

Acetanilides↗
PubMed1982

[Pharmacokinetic characteristics of trimecaine compared to lidocaine in myocardial infarct patients].

The authors studied pharmacokinetics of trimecain and lidocain in 10 and 15 patients with myocardial infarction, respectively, after a single intravenous jet injection in the dose of 80 mg. The groups were comparable as to age, mass and surface of the body. In all patients the dependence of trimecain and lidocain concentrations on time was biexponential. Average individual values of distribution volumes in stationary condition and in the stage of elimination, clearance and half-life differed but insignificantly for trimecain and lidocain. The results obtained justify the conclusion that trimecain and lidocain are identical from the pharmacokinetic point of view.

Acetanilides↗
PubMed1995

[The effect of quaternization on local anesthetic effects of trimecaine].

Effects of the local anaesthetic trimecaine and its quaternary derivative on the isolated rat sciatic nerves were examined. Trimecaine inhibited action potential propagation in the isolated nerve in vitro at four-times lower concentrations than its quaternary derivative. Despite extracellular application, the quaternary derivative inhibited action potential propagation in the sciatic nerve but with a longer half-life in comparison with trimecaine. With increasing external pH, the blocking effect of trimecaine was profound. The blocking potency of the quaternary compound was not consistently changed with the changes in external medium pH.

Action Potentials↗
PubMed2006

Local administration of 2% trimecaine affects the content of fucosylated glycoconjugates in goblet cells in rabbit tracheal epithelium.

The proportion of fucosylated glycoconjugate-containing rabbit tracheal goblet cells after intratracheal application of trimecaine was studied to evaluate its possible unfavourable effects. This lapine model is comparable with diagnostic findings in humans because airway epithelia in humans and rabbits are similar; tracheal epithelium is also practically identical to bronchial epithelium in both species. Local trimecaine anaesthesia caused a proportional decrease in percentage of the tracheal goblet cells containing both alpha(1-2)- and alpha(1-6)-, alpha(1-3)- and alpha(1-4)-fucosylated glycoconjugates as revealed 10 min postexposure using lectin histochemistry. In previous studies, only mild ultrastructural damage to the airway's epithelium was revealed, but a conspicuous decrease in sialylated glycoconjugate-containing tracheal goblet cells and the dominance of acidic sulphated glycoconjugates were observed as after-effects of the same treatment. Glycoconjugate changes can influence the inner environment of airways (e.g. viscoelastic properties of the airways' mucus and mucosal barrier functions) and thus the patient's defence barriers in airways may be weakened. Concurrently, the histochemical properties of goblet cells can be altered in bronchoscopic specimens. Since trimecaine is widely used as local anaesthesia in airways in bronchoscopy, it is necessary to heed these aforementioned effects.

Administration, Topical↗
PubMedDate not supplied

[The anti-arrhythmia activity of amino acid-containing trimecaine derivatives on models of early occlusive and reperfusion arrhythmias in cats].

Experiments were conducted on models of early occlusion and reperfusion arrhythmias in cats to study the antiarrhythmic activity of trimecain, its morpholine analogue (MPT), and MPT derivatives containing glycine, magnesium salt of aspartic acid, and N-acetylglutaminic acid. All the compounds were injected in doses of 5% of LD50. A 22.5 mg/kg dose of trimecain prevented cardiac rhythm disorders after occlusion of the coronary arteries as well as after restoration of the coronary blood flow. Replacement of the diethyl group in the structure of trimecain by the morpholine ring led to diminution of antiarrhythmic activity, and MPT in a dose of 28.0 mg/kg, in distinction from the former, had no effect on the frequency of the occurrence of early occlusion arrhythmias and the duration of reperfusion arrhythmias. Introduction of amino acids as an anion into the MPT structure raised the antiarrhythmic activity of the last named.

Amino Acids↗
PubMedDate not supplied

[The antiarrhythmic activity of the trimecain ammonium derivative in myocardial ischemia].

The results of experiments on cats and dogs showed that quaternidine, a quaternary ammonium derivative of trimecaine, exceeds the structural precursors (trimecaine and lidocaine), as well as the reference drugs quinidine and propranolol, in intensity of the antiarrhythmic action upon single administration on the occlusive and reperfusive arrhythmia models. The therapeutic effect of quaternidine in animals with acute myocardial ischemia lasts for about 8 h, which more than 20 times longer as compared to the duration of action of both lidocaine and trimecaine.

Animals↗
PubMedDate not supplied

[Effect of trimecaine and its quaternary derivative G-103 on myocardial action potentials].

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.

Acetanilides↗
PubMed1989

[Effect of trimecaine on myocardial contractility and the rhythmoinotropic properties of the myocardium in hypoxia].

In the papillary muscles from 14 adult rats and myocardial specimens from 14 newborn ones, trimecaine in doses of 1.10(-6) and 5.10(-6) g/ml produced a dose-dependent negative inotropic effect, reversed the rhythmoinotropic correlation into a negative one and minimized the efficiency of postextrasystolic potentiation. Trimecaine in the former dose reduced hypoxic damage of myocardial specimens in the both groups as reflected by a smaller amplitude of hypoxic contracture and better contractility recovery following a hour hypoxia. It is suggested that reduction in hypoxic contracture and damage to the myocardium occur in the presence of trimecaine from limited Ca2+ entry into myocytes via the Na-Ca turnover mechanism.

Acetanilides↗
PubMed1980

[Comparative clinical study of trimecaine and lidocaine as anti-arrhythmia agents in myocardial infarct].

The article discusses the comparative antiarrhythmic effectiveness of trimecaine and lidocaine in patients with acute myocardial infarction in the first 24 hours of the disease. The 45 patients included in the study were separated into 3 groups: the 1st (control) group consisted of 15 patients with acute myocardial infarction who were not given antiarrhythmic or arrhythmogenic agents; the 2nd group was formed of 15 patients who from the time of admission were given trimecaine by intravenous drip at a rate of 2 mg/min for purposes of prevention after preliminary jet-injection of 80 mg of the drug; the 3rd group consisted of 15 patients given lidocaine by the same schedule. An antiarrhythmic effect was noted in 60% of group 2 patients and in 87% of group 3 patients. No antiarrhythmic effect was produced in 40% of patients treated with trimecaine and in 13% of those given lidocaine.

Acetanilides↗
PubMed1978

[Anti-arrhythmic activity of trimecaine under experimental and clinical conditions].

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.

Acetanilides↗
PubMed1984

[Local anesthetic properties of a polymeric compound of trimecaine].

Original techniques were used in experiments on rabbits and rats to explore the activity and duration of a local anesthetic action of a new trimecaine polymer as compared with trimecaine hydrochloride. The polymer effect was found to be 1.5-2 times longer as compared to that of its low-molecular analog, which was discovered in experimental terminal, conduction and infiltration anesthesia in particular. According to the data obtained, the prolongation of the effect of the new drug is determined by slow separation of trimecain from the polymer.

Acetanilides↗
PubMedDate not supplied

[The effect of trimecaine on allergic reactions in rabbits].

The topical anesthetic trimecaine given to rabbits in a dose of 10 mg/kg attenuated the severity of anaphylaxis, lowered the anaphylactic index, substantially reduced the rates of animals' death from anaphylactic shock. The drug used in a dose of 1 mg/kg slightly had effects on experimental anaphylaxis. Trimecaine affected the rabbit total lipid/phospholipid ratio which had its own specific features in intact, sensitized and anaphylactic animals. It is suggested that the antiallergic effects of trimecaine are associated with the ability of the agent to change the receptor characteristics of target cells in allergy enhanced by its interaction with lipid complexes of the cell membrane.

Anaphylaxis↗
PubMedDate not supplied

[The antiarrhythmic activity of the polymeric forms of quinidine, trimecaine, etatsizin, propranolol and verapamil].

The antiarrhythmic activity and acute toxicity of polymeric formulations of quinidine, trimecaine, ethacizine, propranolol, verapamil which had been immobilized on a cellulose carrier (monocarboxylcellulose) and low molecular analogues were studied in various experimental animals (rats, mice, dogs). The polymeric formulations of trimecaine and verapamil were found to have a higher antiarrhythmic activity in different arrhythmia models than trimecaine and verapamil. The toxicity of all new compounds was no more than the values of conventional antiarrhythmic drugs.

Animals↗
PubMed1976

[Decrease in the maximum sodium permeability and slow sodium inactivation in Ranvier's nodes treated with trimecaine].

The effect of local anesthetic trimecaine on sodium permeability was studied in voltage clamped nerve fibres of the frog. Trimecaine affected PNa by means of two different mechanisms: potential independent block (reduction of PNa) and slow inactivation imposed by prolonged depolarization. Trimecaine induced slow inactivation appeared to be qualitatively similar to that produced by externally applied procaine or high external potassium. According to dose-effect curves one molecule of drug per channel reaction is involved for both mechanisms. The drug molecule has greater affinity for the receptor site responsible for slow inactivation.

Acetanilides↗
PubMedDate not supplied

[Antiarrhythmic activity of trimecaine in experimental arrhythmia and its effect on the heart conduction system].

The anesthetic trimecaine is shown to be capable of eliminating the flutter of atria in dogs simulated by an electric stimulation of the myocardium and atrial fibrillation in cats induced with aconitin and precludes ventrical fibrillation in rats arising due to intoxication with calcium chloride. Trimecaine noticeably mitigates the toxic effect of strophanthin. While depressing the automatism of the sinoatrial node the drug does not affect the conduction function.

Acetanilides↗
PubMedDate not supplied

[The effect of premedication using promedol and galanthamine on the course of epidural anesthesia with trimecaine].

The course of epidural anesthesia with a 2% trimecaine solution has been studied in 93 patients (mean age 56.5 years) upon premedication with promedol (20 mg) and galanthamine (10 mg). It has been established that promedol promotes mainly to a reduction in the time of anesthesia onset (by 26.5%) and to the enhancement of the antihypertensive reaction (by 15.7%). Premedication with galanthamine is accompanied by a 13% decrease in the initial anesthetic dose, a 34.5% shortening of the time of anesthesia onset and the attenuation of negative hemodynamic shifts. Upon premedication with both drugs, the total trimecaine expenditure decreases by 25% and the time of anesthesia onset shortens more than by half.

Adult↗