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PubMed1985

Gas-liquid chromatographic evaluation of bencyclane in biological samples for pharmacokinetic and bioavailability investigations: comparison of two analytical methods.

Analytical conditions that allow bencyclane, a vasodilator, to be evaluated in biological samples for pharmacokinetic and bioavailability investigations are reported. Two gas chromatographic methods were developed, one employing a flame-ionization detector, reaching a sensitivity of 0.5-1 micrograms/ml, and the other employing a thermionic specific detector and reaching a sensitivity of 10 ng/ml. The extraction recovery, reproducibility and specificity were all satisfactory with both methods. The former method is suitable for chemical quality controls and the latter has a sufficient sensitivity and reproducibility for determination of the drug in biological samples as required in pharmacokinetic investigations.

Animals↗
PubMed1980

Pial arteriolar reaction to intravenous administration of bencyclane in the cat.

In a series of 29 experiments in cats, the vasodilatory effect of Bencyclane on pial arterioles was investigated by means of the cranial window technique, using an image-splitting eyepiece, a photometric method or simple microscopic observation. Intravenous injection of 3 mg kg-1 led to vasodilatation in all experiments, yet decreased blood pressure within 30--40 sec until 5--6 min down to 70% of resting pressure. Mean maximal dilatation of arterioles with a 76-micrometers mean resting diameter was 53%. After normalization of blood pressure, arteriolar diameters remained increased by 5--10% for further 10 min, thus indicating increased cerebral blood flow for a total time of about 15 min. During intravenous infusion of 0.2--0.3 mg kg-1min-1 of the drug, pial arterioles dilated by about 10% with blood pressure remaining on resting levels. A higher dosage rate of infusion evoked further vasodilatation, yet parallel decrease of blood pressure.

Animals↗
PubMed1976

In vitro effects of bencyclan on coagulation, fibrinolysis and platelet function.

The in vitro effects of N-3-(1-benzyl-cycloheptyloxy)-propyl-N,N-dimethylammonium-hydrogenfumarate (bencyclan) on clotting, fibrinolytic and platelet function test were investigated by adding the drug to normal human plasma. An anticoagulant activity, mainly of an antithromboplastin nature (directed against later stages of intrinsic thromboplastin formation and against tissue thromboplastin), was observed, while thrombin phase was unaffected. No effect was found in the fibrinolytic system tested (euglobulin lysis, UK-activated fibrinolysis, "hanging clot" method). The drug, although capable of aggregating platelets by itself at very high concentrations, showed a striking inhibitory effect, over a wide range of concentrations, both on platelet aggregation induced by ADP, epinephrine or collagen and on platelet adhesiveness to glass or collagen. Clot retraction was also clearly inhibited. PF3 availability was influenced with a peculiar two-phase behaviour dose-dependently. High concentrations showed a promoting action, while the lower were obviously inhibitory. It is suggested that the effects on platelet function may be due to an influence of the drug on cell membrane.

Bencyclane↗
PubMed1977

[Determination of the KM-value of the fumarase (E.C. 4.2.1.2) with bencyclan-hydrogenfumarate as the substrate (author's transl)].

The Michaelis-Menten constant for fumarase (E.C. 4.2.1.2) has been determined by measuring the enzyme activity by the spectrophotometric method of Racker, which depends on the formation or disappearance of the double bond of fumaric acid. When using Na2-fumarate or bencyclan hydrogenfumarate (Fludilat), respectively, as a substrate, a KM-value of 1.3 X 10(-3) M was found for both substances. In a linked assay where the formation of NADH in the reaction of fumarate leads to malate leads to oxaloacetate was used as a parameter for the reaction rate, a KM-value of 1.35 X 10(-3) M was found.

Animals↗
PubMed1989

[Bencyclane in stage II arterial occlusive disease. Results of a controlled study].

In a single-center, double-blind, randomized study, 19 patients with peripheral arterial occlusive disease stage II Fontaine were treated with bencyclan, and a further 19 patients with buflomedil for 10 weeks after a wash-out phase of 2 weeks. Both groups showed a significant increase in painfree and total walking distances. No significant difference was found between the two groups.

Aged↗
PubMed1976

[The effect of bencyclane hydrogen fumarate (Fludilate) on the adhesion of tumor cells in vivo and in vitro].

Bencyclane hydrogen fumarate (Fludilat) was tested on the stickiness of tumor cells in vivo and in vitro. It was intended to determine whether Fludilat reduced the cancer cell stickiness in vitro, and if the survival time of cancer cell carrying animals can be increased with Fludilat in vivo, or in combination with a cytostatic. For the in vitro trials, concentrations from 0.001 mg/ml to 1 mg/ml medium were chosen. The survival trial on NMRI-mice with Nemeth-Kellner lymphosarcoma was performed in three groups, each with 4-5 sub-groups: Control group--Fludilat 5 mg, 10 mg, 20 mg/kg bodyweight, Bleomycin--50 mg/kg bodyweight, 100 mg/kg bodyweight, 250 mg/kg bodyweight, Bleomycin 50 mg/kg bodyweight + Fludilat 5 mg/kg bodyweight, Bleomycin 100 mg/kg + Fludilat 10 mg/kg bodyweight, Bleomycin 250 mg/kg + Fludilat 20 mg/kg bodyweight. The sequence of deaths was determined, and the 50% survival time was taken as criterium for the effect of the treatment. The in vitro trials showed a complete removal of the monolayer of the tumor cells from the bottom of the culture flask, in doses of 0.01-1 mg/ml medium. In the in vivo trial an increase in the 50% survival time could be achieved in all groups. The results of combined therapy of Fludilat and Bleomycin were striking. In comparison to the control animals, the treated animals showed that the occurrence of solid abdominal metastases from the Nemeth-Kellner lymphosarcoma could be almost completely prevented, especially at high doses. The Ca++-antagonistic effect, in changing the surface of the cells, is discussed as a mechanism of action.

Animals↗
PubMed1984

Quantitative determination of bencyclane in human plasma by capillary gas chromatography/chemical ionization mass spectrometry.

Since 10 years there is a phenomenal increase in the use of mass spectrometry, combined with (capillary-) gas chromatography and dedicated data systems for the rapid, reliable, sensitive and selective determination of xenobiotics (drugs, their degradation/biotransformation products etc.) in biological fluids. This applies especially since the introduction of newer developments in ionization techniques (CI, DCI, FAB) and gas chromatographic column technology (fused silica, bonded phase columns). We employed such a sophisticated method for the quantitative determination of N-[3-(1-benzyl-cycloheptyl-oxy)-propoxy]-N,N'- dimethylammoniumhydrogen fumarate (bencyclane) in human plasma after oral application of a therapeutic doses. Our results clearly show that this approach is the best method available; furthermore the detected plasma levels will lead to discussions with respect to the pharmacokinetic properties of the drug.

Bencyclane↗
PubMed1976

Study of platelet aggregation in vivo i. Effect of bencyclan.

A 20mu diameter pore size screen was inserted into an arterio-venous bypass system in heparinized stumptailed monkeys. ADP and serotonin injection resulted in aggregation of platelets on the screen and consecutive increase in pre-screen pressure and decrease in post-screen pressure. From these changes an "aggregation index" was calculated. Bencyclan in doses of 0.5-15 mg/kg inhibited platelet aggregation in vivo. Doses of 20 mg/kg or above showed some hemolytic effect, no other undesirable effects were seen.

Adenosine Diphosphate↗