摘要:

AbstractThe pharmacokinetics of 2‐pivaloylindan‐1,3‐dione (Pival±) after administration of a single dose was investigated in dogs. The plasma concentration graph can be described by a one compartment open model. The drug is fairly well absorbed (67%) and the excretion is extremely slow with a half‐life of nearly five days. These kinetics can be explained by the physicochemical properties of the drug, such as strong binding to canine plasma protein, high lipophility and the lack of transformation to polar metabolites. A single oral dose of 5 mg/kg must be regarded as lethal to dogs and the LD50 is assumed to be approximately 4 mg/kg in this

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02173.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractThe mechanism of the prolonged effect of dextran on the duration of local anaesthesia has been studied. Using radio‐active mepivacaine it was found that dextran prolonged the duration of infiltration anaesthesia in guinea‐pigs by delaying the absorption of the local anaesthetic agent. Experimentsin vitroindicate that molecular complexes between the local anaesthetic and dextran may be formed and it is assumed that the delayed absorption might be due to the formation of such molecular complexes. This hypothesis was strengthened by experiments in which dental infiltration anaesthesias were performed in healthy volunte

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02174.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractThe intravenous injection into rats of dextran (average M W 70,000) 10 mg/100 g caused marked hypotension after a delay of about 5 minutes. Blood samples collected by cardiac puncture at this time were tested for the amounts of prekallikrein activator (PKA) and kallikrein after acetone‐ and then kaolin activation of the plasminogen‐free plasma. PKA was assayed by measuring the initial rate of release of benzoyl arginine esterase (BAEe) activity in a preparation of partially purified human prekallikrein, and kallikrein was assayed by measuring the BAEe esterase activity. Significant reductions of both parameters were registered, and the amount of high molecular weight kininogen (HMWK) present in the plasma was also reduced. Pretreatment of the rats with ε‐aminocaproic acid intraperitoneally (200–300 mg/100 g) abolished the dextran‐caused decreases in the plasma levels of the above mentioned factors, and reduced the fall in blood pressure. The addition of purified human HMWK to the plasma before the acetone activation procedure was started, increased the yield of PKA activity in the final enzyme preparation. When PKA was assayed after kaolin activation of plasma at 0° using the method developed by Laake&Vennerød (1973a&b) for the determination of PKA (activated factor XII) in human plasma, no differences were registered between plasma from rats treated with dextran and plasma obtained from control rats. It is suggested that the low PKA activity of the acetone activated enzyme preparation from plasma of rats treated with dextran was due to the loss of HMWK or a frac

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02175.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractGranulation tissue was produced in rats by subcutaneous implantation of viscose cellulose sponges. Treatment with cyclophosphamide in a dose of 10 mg/kg/day for 14 days caused an increase in acid soluble OH‐proline and a decrease in alpha/beta ratio of acid soluble collagen of granulation tissue. Forty‐two days of continuous cyclophosphamide treatment caused a decrease in dry weight, in free OH‐proline, and in salt soluble OH‐proline in granulation tissue. These findings are in accordance with previous observations of a decreased collagen synthesis and an inhibited collagen degradation in granulation tissue after cyclophosphamide treatment. In skin, the only change after cyclophosphamide was a decrease in total content of OH‐proline and an increase in alpha/beta ratio of acid soluble collagen after 42 days of treatment. No effect of the subcutaneous sponge implantation was observed on the collagen variables in the skin. In comparison with unstarved controls, a reduction in dry weight and in free OH‐proline in granulation tissue, as well as an increase in salt soluble OH‐proline in the skin were observed 28 days after a 14‐day treatment with cyclophosphamide. These observations indicate a sustained effect of cyclophosphamide on collagen 28 days after cessation of treatment. In addition the thermal stability of rat tail tendons was decreased 28 days after withdrawal of cyclophosphamide to the same extent as after starvation for 42 days and after 42 days of continuous cyclophosphamide treatment. It is concluded that the cyclophosphamide‐induced collagen alterations, which may be of importance in the anti‐inñammatory action of cyclophosphamide, are only in part reversible, 28 days after cessation of 14 days of cyclop

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02176.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractMale rats were exposed to 0,10 and 130 p.p.m. cadmium administered in 0.5% saline drinking water for 71 days. Biweekly records of ECGs, Hct, body weight and blood levels of cadmium were made. Rats exposed to 130 p.p.m. cadmium showed slower growth rates and declining Hct indicative of acute cadmium poisoning. At the end of the experimental period, carotid artery blood pressures and whole heart cadmium levels were determined. Although no significant blood pressure changes were observed in the experimental groups, the cadmium content of the hearts of the higher dose group was significantly higher than in the hearts of the lower dose group. The PR interval of the ECG was lengthened progressively and to the same extent in both experimental groups with continued cadmium feeding. These experiments offer evidence that the accumulation of even moderate amounts of cadmium will be manifested in marked changes in cardiac conduction without overt signs of cadmium poisoning.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02177.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractOsmotically balanced solutions of glucose (0.5–300 mM) and sodium chloride, containing cetrimonium bromide (cetrimide, 0.8–4.1 mM), were instilled into the jejunum, ileum and colon of anaesthetized rats. Net transport of glucose, sodium and potassium was studied by their disappearance from, or accumulation into the intestinal lumen during 15 min incubation. Cetrimide caused the following shifts in normal jejunal and ileal glucose absorption: Atlowluminal glucose levels, absorption was strongly depressed and may be converted to net secretion. Atintermediatelevels, inhibition was less pronounced, and athighluminal glucose levels absorption was enhanced. Similar changes were seen in the colon. Furthermore, cetrimide caused a threefold change in the regression lines relating net sodium fluxes to the initial sodium concentration: The lines became steeper, the correlation was improved and the sodium concentration value corresponding to zero net transport was elevated. Net potassium secretion was increased. — These changes are all consistent with the view that surfactants cause an increase in passive epithelial permeability. Quantitatively, the effect of cetrimide increased with localization in the order colon>ileum>jejunum. Benzalkonium chloride (0.5–1.7 mM) was tested in the ileum only, and caused quite similar

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02178.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractThe diurnal rhythm of oral temperature was studied in 55 lithium treated patients, 51 other psychiatric patients, and 58 healthy subjects. The lithium treated patients had a higher temperature than the normal controls during the 24‐hour period and their temperature maximum was shifted towards an earlier time. When the lithium intake was postponed for 12 hours, temperature temporarily decreased to control values, but returned to the higher level after the lithium dose. The temperature results are discussed in relation to lithium induced changes in electrolyte metabolis

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02179.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractThe effects of 5 and 10 mg oral nitrazepam doses on manual skills, grip strength, and reaction time 8 hours after ingestion of the drugs were studied in 34 healthy female volunteers aged 19–22 years. 5 mg nitrazepam caused a slight but insignificant decrease in psychomotor skills. With 10 mg psychomotor skills were influenced significantly. Grip strength and reaction time were not influenced either by the 5 or 10 mg doses. The investigators corroborate the value of the established effects of nitrazepam as a hypnotic, but recommend that caution should be exercised in prescribing the drug as a hypnotic (especially in doses exceeding 5 mg) to work‐aged subjects as there is a risk of significant effect on the psychomotor skills. Furthermore, the drug may cause fati

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02180.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractDiethylmaleate, cyclohexene oxide and acrylamide administered intraperitoneally to rats, have been shown markedly to inhibit biliary excretion of methyl mercury. Simultaneously the sulphhydryl and sulphide content of the bile decreases. These results probably reflect the conjugation of acrylamide, diethylmaleate and cyclohexene oxide to glutathione in the liver, thereby blocking the biliary excretion of methyl mercury. A high concentration of liver glutathione seems to be a prerequisite for the normal translocation of methyl mercury from liver to bile. These results indicate that methyl mercury is transported from liver to bile as a glutathione complex.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02181.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY

摘要:

AbstractStudies on absorption and excretion of chromium in the rat exposed to known atmospheric concentrations of zinc chromate in an inhalation chamber and the influence of diurnal variations in physical activity have been carried out. Chromium analyses were performed on samples of blood, urine and faeces using a method for determining chromium in small samples of biological material based on flameless atomic absorption spectrometry. Zinc chromate is absorbed quickly during exposure and excreted mainlyviaurine. An accumulation of chromium in blood was observed, followed by a slow elimination. It is suggested that chromium from zinc chromate enters the blood in the hexavalent state.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1978.tb02182.x

出版商:Blackwell Publishing Ltd    

年代:1978

数据来源: WILEY