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At least 1,207 records · Page 67Linked to original sources
PubMed1975

An evaluation of tilidine hydrochloride in the treatment of pain requiring immediate analgesia.

Problems relating to analgesia in various situations are briefly discussed. A simple working classification for analgesic administration is given. The results of a trial, in which 50 mg of a new analgesic, tilidine, was given sublingually, are presented. The drug was evaluated in cases where immediate analgesia was indicated. The majority of patients had injuries to the hand or head. It was found that tilidine provided a marked analgesic effect in 27 of the 30 patients. The onset of action was rapid, 25 of the 30 patients obtaining complete relief within 6 minutes. It is concluded that tilidine is a powerful analgesic, with a rapid onset of action when it is give in the sublingual drop form. Moreover, it is a drug of choice, in this form, for acute, moderately severe situations (those which require immediate analgesia, but where opinates are not thought to be necessary).

Acute Disease↗
PubMedDate not supplied

Catecholamines concentration in brain and heart tissue of rats and its blood pressure during chronic treatment with a new tricyclic antidepressant 10-(3-dimethylaminopropyl)-7-chlorobenzo-(b), (1,8)-naphthyridone-5 monohydrochloride (IF-C-45).

DA concentration in brain tissue decreased statisticaly after 3, 6 and 9 weeks, NA concentration also statisticaly decreased but after 3 weeks only. The NA concentration in heart tissue decreased statisticaly significant in all investigated animals. There were no statisticaly significant changes in blood pressure.

Adrenal Glands↗
PubMedDate not supplied

The analysis of cardiovascular action of 10-(3-dimethylaminopropyl)-7-chlorobenzo-(b)-(1,8)-naphthyridone-5 monohydrochloride (IF-C-45) with antidepressant properties.

The effects on cardiovascular system of a new compound, 10-(3-dimethylaminopropyl)-7-chlorobenzo-(b)-(1,8)-naphthyridone-5-monohydrochloride (IF-C-45) were investigated in rats, dogs and cats and compared to the effects induced by imipramine. Within the range of the analysis of peripheral cardiovascular effects IF-C-45 acts in a similar way as imipramine does. Its hypotensive and cardiodepressive action is significantly weaker than that of imipramine.

Administration, Oral↗
PubMedDate not supplied

Local anaesthetic activity of some new substituted acylamides II.

Six new substituted acylamides, chemically related to lignocaine were studied for local anaesthetic activity and toxicity in mice, frogs and guinea pigs. Only one of these compounds, w-pyrrolidino 2, 3, 5, 6 tetramethyl acetanilide was found to possess potency comparable to lignocaine with a slightly higher therapeutic index. Study of the S.A.R. of this group indicated that by removal of two methyl groups at position 3 and 5 in the above compound, a local anaesthetic with greater potency than lignocaine may be obtained. Further exploration of the potentialities of a compound having pyrrolidine group as a part of basic side chain is indicated.

Acetanilides↗
PubMed1975

Pharmacokinetic study of maleate acid of 2-(N,N-dimethylaminoethanol-14C1)-cyclohexylpropionate (cyprodenate) and of N,N-dimethylaminoethanol-14C1 in animals.

The localization, distribution, and elimination of maleate acid 2-(N,N-dimethylaminoethanol-14C1)-cyclohexylpropionate (14C-cyprodenate, Actebral) was studied in rats and pigs. Beside this, dimethylaminoethanol-14C (DMAE) was also administered to rats enabling a comparison of the pharmacokinetics of the two 14C-labelled molecules to be made. The study of the localization by autoradiography and the study of the quantitative distribution of the radioactivity showed that cyprodenate, a psychotonic drug, diffused more rapidly than DMAE through the hemo-encephalic barrier. However, it was also observed that the radioactivity found in the brain rises continually as a function of time, regardless of the product administered. The two labelled products were primarily excreted in the urine (30-35 per cent of the dose in 72 h in rats and 6 per cent of the dose in 48 h in pigs) following oral administration of cyprodenate. Radioactivity found in the feces was practically nil and in rats the biliary elimination of the drug was very weak. Thus, whichever animal is used, it was found that 14C-cyprodenate is totally absorbed. Radioactivity expired as 14CO2 was negligible (around 1 per cent of the administered dose in 8 h), however, this value increases as a function of time, becoming 4 per cent in 24 h. In rats the maximum radioactivity in the blood was found at 45 min to 1 h after oral administration of 14C-cyprodenate. These values decrease slowly until 3 h when they begin to increase again. The rising of the blood level values is practically the same for pigs, the maximum being attained at 1 h. Therefore, whatever route of administration, whichever dose or animal, we always found a progressive elevation of the protein binding to the plasma proteins for these two labelled products in vivo.

Animals↗
PubMed2002

[Participation of dexamethasone and E and C vitamins in the modulation of the hepatotoxic effect induced by fomesafen and 2,4-D amino herbicides, in rats ].

The fomesafen and 2,4-D amine herbicide induce cytotoxic effects at hepatic level in rats, such as: hepatomegaly, hyperplasia and increase in the enzymes activity which participate in the processes of peroxisomal beta-oxidation of fatty acids. In this work, the effect of vitamin E and C was evaluated, as well as, the dexamethasone in the modulation of these hepatotoxic effects. Sprague-Dawley rats were treated with the herbicides and with the agents to be evaluated. The different treatments were given during 15 days orally route. The herbicides combined with the dexamethasone and antioxidant agents were administrated only and simultaneously with the herbicides. Once concluded the different treatment, the rats were weighed and sacrificed. It was evaluated the liver size and liver fragments were obtained to determine the enzymatic activity of Fatty Acyl CoA-oxidase (FACO) and cellular number. The results showed that the hepatomegaly induced by fomesafen was inhibited by the vitamins and by the dexamethasone, while any effect was not observed in the group of rats treated with 2,4-D amine. None of the agents modulated the FACO activity induced by herbicides in treated rats. However, the dexamethasone showed a protective effect in the hyperplasia induced by two herbicides. The hepatotoxic effects induced by the herbicides responded to a different mechanism due to the differences of the effects observed at the antioxidant agents. On the other hand, the inhibition of the cellular proliferation by the dexamethasone does not keep relation with the responsible mechanisms of inducing the oxidant stress into FACO activity. Under experimental conditions of this study, the use of these agents does not guarantee protection against the hepatotoxic effects induced by the herbicides.

2,4-Dichlorophenoxyacetic Acid↗
PubMed2003

Characteristics of coagulation-flocculation of humic acid with effective performance of polymeric flocculant and inorganic coagulant.

Ferric chloride and aluminium sulphate as coagulants and positive charged flocculants PDDMAC ((PDDMAC = poly (diallyldimethylammonium chloride) were used for pre-treatment of water and wastewater for removing humic substance prior to RO membrane filtration. It was found that a combination of flocculant and coagulant enhanced the coagulation-flocculation process and humic acid removal. The optimum conditions of coagulation-flocculation were established in reference to the ratio of humic acid and coagulant. Zeta potential and the ratio of E4/E6 were investigated to explore the possible micro-mechanisms of coagulation-flocculation. The ratios of E4/E6 show the molecular size variations using different coagulants and flocculants, which are expected to benefit membrane-fouling control.

Dimethylamines↗
PubMed1992

[Immunochemical changes in the outer membrane of Escherichia coli adapted to amine oxides].

Resistant strains of Escherichia coli were obtained by stepwise cultivation in subinhibitory concentrations of two antimicrobially active amine oxides. Changes in the chemical composition of the outer membrane of the resistant strains were accompanied also by different antigenic reactions. New precipitation lines were revealed by double immunodiffusion and immuno-electrophoretic methods. The results of immunochemical analysis confirm the findings that the resistance to amphiphilic compounds is associated with the outer membrane which limits the access of antimicrobially active molecules to their sites of action in the cytoplasmic membrane.

Antigens, Bacterial↗
PubMed1992

Pharmacological evaluation of JO 1870: relation to the potential treatment of urinary bladder incontinence.

The effect of p.o. administered JO 1870 [(-)-1-(p-chlorophenyl)-N,N- dimethyl-1-ethyl(4-phenyl)-but-3-en-1-ylamine, hydrochloride] on the urinary bladder cystometrogram has been investigated in the unanesthetized rat. The effects of JO 1870 have been compared with those of morphine and reference drugs currently used for the treatment of urinary incontinence in humans. JO 1870 (2.5-25 mg/kg) dose-dependently increased the bladder capacity and the threshold pressure responsible for urination. These effects were antagonized by the i.v. administration of naloxone (0.2 mg/kg). In comparison, morphine (2.5-25 mg/kg) moderately increased urinary volume and threshold pressure. Different anticholinergic drugs (propantheline bromide, 10 mg/kg; terodiline, 25 mg/kg; dicyclomine, 25 mg/kg) had no significant effects on either parameter and the antidepressant clomipramine (25 mg/kg) decreased both. In vitro, JO 1870 specifically displaced [3H]-[D-Ala2,MePhe4,Gly5-(ol)]enkephalin from binding sites in guinea pig whole-brain membranes and rat thalamus; the sodium shift ratio obtained from [3H]naloxone binding was 16. These results suggest that JO 1870 has some opioid agonist activity. JO 1870 (2.5-300 mg/kg) had few effects on cardiorespiratory, gastrointestinal or nociceptive systems in rats. Together, these results indicate that JO 1870 is a nonanticholinergic agent that potently increases bladder capacity, likely through an opioid mechanism, and may have potential use in the treatment of urinary incontinence.

Animals↗
PubMedDate not supplied

Distribution of TNF endogenously induced by various immunopotentiators and Lactobacillus casei in mice.

Intravenous administration of heat-killed Lactobacillus casei YIT 9018 (LC) elicited endogenous cytotoxic factor (CF) production in ICR mice, peaking in serum after 2 h and declining gradually to basal level at 23 h. The endogenous CF production was significantly enhanced by priming with high molecular-weight lignins and glucans, but not by phenylpropenoid precursors or partially hydrolyzed products of glucans. The extent of stimulation of CF production by these priming agents was positively related to that of tumor necrosis factor (TNF) production, as judged by enzyme-linked immunosorbent assay. Endogenously produced TNF was concentrated more in liver, lung and intestine, as well as in serum, than in other organs. Histochemical examination revealed a significant increase in the number and swelling of Kupffer cells and sinusoidal endothelium in the liver of the treated mice.

Adjuvants, Immunologic↗