[Effect of fluvastatin on serum lipid levels in essential hypertension]. / A fluvastatin hatása a szérum lipid szintekre esszenciális hipertóniás betegekben.

The efficacy and safety of the HMG-CoA reductase fluvastatin was investigated in a multicenter, open label clinical therapeutic trial in the treatment of hypercholesterinaemia in hypertensive patients (WHO I-II.). 49 patients were involved, 6 patients were dropped out because of th lack of compliance, 43 patients were investigated (mean age: 57.6 +/- 9.4 years, mean blood pressure: 146 +/- 16/88+/- g mmHg (systolic/diastolic). The antihypertensive treatment was unchanged during the study. An 8 weeks low-lipid diet was started if the fasting total cholesterol (TC) level was equal or higher than 6.5 mM/L and the triglyceride level was lower than 4.6 mM/L. After the dietary period fluvastatin treatment was started (20 mg o.d.), if the level of LDL-C was higher than 4,1 mM/L. Blood pressure, heart rate, TC, HDL-C (HDL2-C, HDL3-C), apoA1, apoB, TG were measured at the 4th, 8th, 12th weeks of treatment. LDL-C was calculated with Fridewald equation. The daily dose of fluvastatin was increased to 40 mg, if LDL-C level was higher than 3.5 mM/L after 4 weeks of treatment. 36 patients completed the study (Group B). 7 patients were dropped out at the end of the dietary period, because of the significant decrease of TC and LDL-C levels (Group A). In Group B fluvastatin significantly reduced the level of TC (from 7.22 +/- 0.88 to 5.99 +/- 0.98 mM/L), of LDL-C (from 5.13 +/- 0.71 to 3.95 +/- 0.88 mM/L), and the level of ApoB (from 0.97 +/- 0.26 to 0.85 +/- 0.15 mM/L), but did not influence significantly the level of HDL-C, ApoA1 and TG. The diastolic blood pressure decreased significantly during the dietary period, while after beginning the fluvastatin treatment the decrease of the systolic blood pressure became significant. There was no change in the heart rate. Only minor side effects were observed in 3 patients (dysuria, constipation, lack of appetite). Fluvastatin proved to be an effective and well-tolerated drug in the treatment of hypercholesterinaemia in hypertensive patients.

Interaction of taxol and other anticancer drugs with alpha-cyclodextrin.

The interaction between 23 anticancer drugs and alpha-cyclodextrin (alpha-CD) was studied by reversed-phase charge-transfer thin-layer chromatography and the relative strength of interaction was calculated. As alpha-CD has smaller cavity than beta- and tau-CD it interacted only with 10 anticancer drugs proving the relatively poor complex forming capacity of alpha-CD. The hydrophobicity of host-guest inclusion complex was always different from that of the uncomplexed drug suggesting that the complex formation may influence the uptake, absorption, half-life etc. of the original drug. The inclusion forming capacity of drugs differed considerably according to their chemical structure. The intensity of interaction significantly depended on the hydrophobicity of the guest molecule proving the preponderant role of hydrophobic interactions in inclusion complex formation.

Hungarian Isradipine Study (HIS): long-term (3-year) effects on blood pressure and plasma lipids.

These are the preliminary data of an open multicenter trial of antihypertensive treatment with isradipine as monotherapy (dose, 4.55 +/- 0.56 mg twice daily; n = 11) or isradipine (7.5 +/- 0.63 mg twice daily) in combination with bopindolol (1.16 +/- 0.12 mg once daily; n = 30) administered for 3 years to patients with essential hypertension (WHO classification I or II). Blood pressure was significantly decreased in both treatment groups and there was no indication of resistance to therapy. Plasma levels of total cholesterol and triglycerides were decreased by the end of the second year of treatment, and there was a tendency toward increase in plasma levels of high-density lipoprotein cholesterol (HDL2 or HDL3). The atherogenic index (ratio between total cholesterol and HDL2 plus HDL3) was also decreased. Blood glucose levels remained unchanged in both normoglycemic patients and those with non-insulin-dependent diabetes mellitus (NIDDM) during 3 years of therapy. It is concluded that isradipine is safe and effective when administered long-term in the treatment of hypertensive patients with either hyperlipidemia or NIDDM.

Interaction of amino acids with a non-homologous series of anticancer drugs.

The interaction of amino acids with 14 commercial anticancer drugs was studied by charge-transfer reversed-phase thin-layer chromatography and the retention matrix was evaluated by principal component analysis. The majority of amino acids had a negligible effect on the retention of anticancer drugs. Only dicarboxy amino acids and Trp exerted a considerable impact on the retention of drugs, indicating the involvement of hydrophilic forces (probably hydrogen bond formation) and stacking interactions in the binding of drugs to amino acids. Stepwise regression analysis proved that both the pI value of amino acids and the pK value of the amino acid side chain significantly influence the strength of interaction. The findings support the hypothesis that the binding of anticancer drugs to proteins may involve both hydrophilic forces occurring between the corresponding polar sub-structures of drugs and amino acids and stacking interactions between the various ring structures. The relative importance of these interactions depends on the character of the amino acid residue and the chemical structure of drugs.

Long-term antihypertensive therapy with guanfacine.

Twenty patients with essential hypertension were treated with guanfacine given in single 1-5 mg daily doses over a period of 24 weeks. Compared with the initial values at the end of the first washout period, there was a significant decrease in blood pressure and heart rate. The most common side effect, dryness of the mouth, usually disappeared after 8-10 weeks of treatment. No changes in laboratory values were seen. In the post-treatment placebo period there were significant increases in blood pressure and heart rate compared with the last readings during the treatment period. However, these never exceeded the pretreatment values. In a second series guanfacine (1-5 mg daily) was abruptly discontinued in 11 patients after 6-20 weeks of treatment. Blood pressure was measured twice a day, in lying and standing positions, during the 4 days preceding abrupt withdrawal of guanfacine and for 7 days after discontinuation. Clopamide was given concurrently to two patients, and this was continued after withdrawal of guanfacine. Only in two patients did the blood pressure rise to values above the initial levels (30 mmHg systolic and 10 diastolic), but no clinical symptoms were observed during the withdrawal. A transitory increase in heart rate between 10 and 30 bpm was observed in five patients after abrupt discontinuation of the drug.

Antihypertensive effect of guanfacine: long-term 'once-a-day' treatment and sudden withdrawal.

1. Twenty patients with essential hypertension were treated with guanfacine given in single daily doses of 1--5 mg over a period of 24 weeks. Compared with the initial values at the end of the first wash-out period, there was a significant decrease of blood pressure and heart rate. The most common side effect, dryness of the mouth, usually disappeared after 8--10 weeks of treatment. No changes in laboratory values were seen. In the post-treatment placebo period there were significant increases in blood pressure and heart rate compared with the last readings during the treatment period. However, these never exceeded the pretreatment values. 2. In a second trial guanfacine (1--5 mg daily) was abruptly discontinued in 11 patients after 6--20 weeks' treatment. Blood pressure was measured twice a day, in lying and standing positions, during the 4 days before abrupt withdrawal of guanfacine and for 7 days after discontinuation. Clopamide was given concurrently to two patients, and this was continued after withdrawal of guanfacine. Only in two patients did the blood pressure rise to values above the initial levels (30 mmHg systolic and 10 mmHg diastolic), but no clinical symptoms were observed during the withdrawal. A transitory increase of heart rate of between 10 and 30 beats/min was observed in five patients after abrupt discontinuation of the drug.

Denitrification and removal of heavy metals from waste water by immobilized microorganisms.

Pseudomonas fluorescens, immobilized on soft polyvinyl chloride granules containing up to 35% softeners as carbon source, was used for simultaneous removal of nitrate and heavy metals. In typical continuous column operation, a 100 mg/L nitrate input solution was reduced to a 20 mg/L output at a feeding rate of 1500 mL/h, with a capacity of 14 kg/day/m(3), and with an efficiency of 79%. In the same column, Pb(NO3)2 concentration was reduced from 1.0 to 0.05-0.1 mg/L and ZnSO4 concentration was reduced from 10 to 5 mg/L.Pseudomonas aeruginosa immobilized on an O2 plasma-treated melt blown polypropylene web was used for removing 95% of a 1.7 nCi PuCl4 activity from a nuclear plant waste water in a batch operation.

[Electrodynamic discrepancy of the heart]. / Uber die elektrodynamische Herzdiskrepanz.

Electrodynamic discrepancy was observed in the hearts of 15 out of 144 patients with myocardial infarction who died on account of various complications. Autopsy revealed cardiac rupture with pericardial tamponade in each of the 15 cases. If the ECG shows no typical signs of a myocardial infarction, then with great probability an aortic rupture is present. The pathomechanism of electrodynamic discrepancy of the heart may be explained with the help of Laplace's law and "neuropraxia", "Afterload" and "preload" are reduced to practically nil, the tension of the myocardial walls falls, the effective work of the heart muscle stops and with the considerably lower oxygen requirement of the myocardium the bioelectric activity of the heart is still maintained for 12-30 minutes.

[Bouquet qualification of wines by gas chromatography. 2. Development of measuring unit for bouquet qualification by determination of relationship of chromatographic peak areas and conditions of application]. / Uber die gaschromatographische Duftqualifizierung von Weinen 2. Mitt. Entwicklung einer Masszahl zur Qualifizierung des Duftes durch Bestimmung des Zusammenhanges mit den Peakflächen und Anwendungsbedingungen

In a previous paper we described a method by which routine head-space analysis of wines can be performed with sufficiently accurate results by means of gas chromatography. From the results thus obtained, with application of organoleptic data, chemical and classical analytical parameters of aromatic changes during seasoning and storing wines as well as mathematical-statistical data of the method elaborated, a mathematical relationship has been derived between gas chromatographic peak areas characteristic of different aroma components and the bouquet of wine. Reliability of the method has been verified by the fact that, in spite of the small number of samples, the bouquet of seven different types of wine could be discriminated in 95,45% probalility. The method allows arbitrary choice in the number of samples and in the degree of reliability required, in investigating the quality of a wine. For this purpose, another mathematical relationship has been set up to provide criteria for the distinction of the quality of bouquets. By this method, the bouquet of various types of wines or within an identical type, the bouquet of different vintages and/or bottlings can be determined.

[Bouquet qualification of wines by gas chromatography. 1. Experimental method for gas phase analysis]. / Uber die gaschromatographische Duftqualifizierung von Weinen 1. Mitt. Versuchsmethode zur Gasphasenanalyse

In the course of our investigations we tried to find a method for the bouquet qualification of wines by gas chromatography. For this purpose, instead of aroma research studies requiring complex equipment and laboursome precise laboratory work, we developed a method for head space analysis functioning with simple experimental instruments and being sufficiently fast for serial routine work. By the method developed, the head space of a great number of samples taken from 7 different wine-types have been successfully examined. Errors of measurement were checked by standard deviation analysis and the values obtained (3,23%) were found satisfactory. According to the above, our head space analysis may provide a satisfactory basis for elaborating a method for the instrumental bouquet qualification of wines.