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At least 55 records · Page 3Linked to original sources
PubMed1991

Cyclandelate in diabetic neuropathy. A double-blind, placebo-controlled, randomized, cross-over study.

Cyclandelate has the ability to improve the rheological properties of the blood and therefore may improve blood supply of peripheral nerves. Previous studies in diabetic neuropathy have shown beneficial effects of the drug. We performed a double-blind, placebo-controlled, cross-over study in 40 diabetic patients with cyclandelate in a dose of 1600 mg daily. Motor and sensory nerve conduction velocities, late responses, thermal discrimination thresholds, vibration perception thresholds and pain scores were studied. We were not able to show any positive effect of the drug and therefore conclude that cyclandelate is not effective in the treatment of diabetic neuropathy.

Adult↗
PubMed1991

Bioavailability of cyclandelate from capsules in beagle dogs and dissolution rate: correlations with bioavailability in humans.

The bioavailability in beagle dogs and the dissolution rates of cyclandelate from five capsule preparations commercially available in Japan were measured. One of the capsules that showed an extremely low bioavailability in humans also showed the lowest bioavailability in beagle dogs, although the difference in bioavailability with the highest preparation was smaller than in humans. A significant correlation was obtained between the results of the studies in humans and beagles. However, the power of the test using beagles was extremely low in comparison with that in the human study. Food enhanced the bioavailability of cyclandelate from the capsules having the highest and lowest bioavailability in the fasted state in beagles as observed in the human study previously. The bioinequivalence of the cyclandelate capsules detected in the fasted state disappeared in the fed state in the beagle dog study, while the bioinequivalence still remained in the non-fasted state in human subjects. Thus bioequivalence testing in the fed state led to different results in both species. The most poorly bioavailable capsule in both species in the fasted state showed a slow dissolution rate by several dissolution methods with moderate stirring. In order to obtain a good correlation with in vivo bioavailability, a large volume of test solution and addition of Tween 80 were required. Extensive growth of whiskers (needle-like crystals) was observed in the entire capsule mass having the lowest bioavailability.

Animals↗
PubMed1987

Specific effects of cyclandelate on memory.

In an uncontrolled clinical trial of 6 weeks' duration conducted in 20 male patients, aged 49 to 68 years, with memory disorders, cyclandelate 1200 to 1600 mg daily was found to be effective in improving memory as reflected by psychiatric, psychometric and psychophysiological measurements. Treatment with cyclandelate produced clinical effects which were selective for the Wechsler Memory Scale items of visual reproduction and orientation--indicators of the declarative memory. Moreover, the improvements seen in the average auditory reaction and critical flicker fusion frequency demonstrates its effect on procedural memory. Thus, our results indicate that this drug may be therapeutically useful in memory disorders of various aetiology, and that further exploration of the place of cyclandelate in this clinical area is needed.

Aged↗
PubMed1987

Comparative efficacy of cyclandelate versus flunarizine in the prophylactic treatment of migraine.

In a double-blind, parallel-group randomised trial of 3 months' duration, the efficacy of cyclandelate 800 mg twice daily in migraine prophylaxis was compared with that of flunarizine 5mg daily in 40 patients. In comparison with placebo and baseline values, both drugs significantly relieved symptoms of migraine as assessed by indices of pain total index, headache index, analgesic consumption and number of migraine days. Patients taking flunarizine experienced side effects such as drowsiness, weight gain and asthenia, while the most common complaint reported with cyclandelate was gastric upset. These results suggest that cyclandelate may be a useful alternative in migraine prophylaxis.

Adolescent↗
PubMed1987

Cyclandelate in the treatment of vertigo of circulatory origin. A study in general practice.

A multicentre study with 622 patients has been undertaken to evaluate the efficacy of cyclandelate 1600 mg daily in the treatment of vertigo of circulatory origin in general practice. The characteristics of the patient population were consistent with the diagnosis of vertigo of circulatory origin. Patients with some risk factors, essentially a history of thrombosis and atherosclerotic patients, had more severe symptoms at the onset of the study. During the 3-month period of treatment with cyclandelate, the average global score of vertigo (0-10) decreased from 5.57 to 2.12 and the average scores of frequency, severity and duration of vertigo (0-4) decreased from 2.53, 2.55 and 2.26 to 0.98, 0.89 and 0.84, respectively. Patients previously treated with other anti-ischaemic drugs had similar responses compared to other patients. These results indicate that cyclandelate may be useful in the management of vertigo of circulatory origin in general practice.

Aged↗
PubMed1987

Clinical experience with cyclandelate in insulin-dependent diabetic patients with neuropathy.

Previous trials have demonstrated a clinical and electrophysiological improvement of diabetic peripheral polyneuropathy in diabetic patients treated with cyclandelate at a dosage of 1600 mg/day. Hence, a double-blind randomised trial was started in 16 insulin-dependent diabetic patients presenting with symptoms of neuropathy, an increased vibration perception threshold (VPT), disturbed tendon reflexes at lower limbs and an EMG showing a significantly decreased motor nerve conduction velocity (MCV) of the peroneal nerves. The placebo-treated group and the cyclandelate-treated group were not significantly different regarding age, duration of diabetes and level of metabolic control (measured as total HbA1), which remained unchanged during the year of observation. In the cyclandelate-treated group, pathological sensation improved significantly in 7 of 8 patients. MCV, measured under standardised conditions, increased significantly during the first 6 months of treatment, while mean VPT did not change. In the placebo group 3 of 8 patients showed an improvement of sensation, 3 did not feel any change and 2 worsened. Neither mean MCV nor VPT changed significantly. No severe side effects were observed during the study period.

Adult↗
PubMed1994

[Evidence of a pharmacokinetic-pharmacodynamic relationship between pharmaco-EEG in healthy subjects after administration of cyclandelate].

In an open randomized cross-over study 800 mg cyclandelate (Natil, CAS 456-59-7) was applicated to 24 young, male volunteers. Before and during 24 h after application of a single dose a 17-channel, quantitative topographical pharmaco-EEG was recorded. A significant increase of the spectral power density was observed in the alpha 2, beta 1 and beta 2 frequency bands starting 2 h after application until 4.5 h. The increase in beta 1 and beta 2 power was observed in the parietocentral area of the cortex. The difference between the circadian development of the EEG power and the development after medication was obvious after 3 until 4.5 h. For the beta frequencies only a weak statistical confirmation could be obtained, but for the alpha 2 frequency a significant difference between the circadian and the EEG power under cyclandelate was found using the sign test. Altogether a quantitative effect on brain activity was detected after oral application of cyclandelate, reaching its maximum before the blood concentration of the metabolites cyclandic glucuronide and mandelic acid reached their peak heights.

Adult↗
PubMed1983

The inhibition of hepatic S-3-hydroxy-3-methylglutaryl-CoA reductase by 3,3,5-trimethylcyclohexanol and its mandelic acid ester, cyclandelate.

Rat hepatic HMGCoA reductase was found to be at least 50% inhibited 17 hr after administration of a single oral dose of 3,3,5-trimethylcyclohexanyl mandelate (cyclandelate), a vasoactive substance. This inhibition was also found in rats given the 3,3,5-trimethylcyclohexanol component but only slight inhibition was seen after an equimolar dose of mandelate. The inhibition of HMGCoA was observed both around the high point and near the low point of the diurnal activity cycle. The effect did not persist to 41 hr after treatment. There was no direct inhibition of HMGCoA reductase by trimethylcyclohexanol when added to the assay system in vitro. The in vivo effect of these inhibitors was specific for HMGCoA reductase. There was no change, neither elevation nor depression, of the amount of microsomal membrane components cytochromes b5 and P-450, not was the activity of another microsomal enzyme, arylesterase, affected by dosing with cyclandelate or trimethylcyclohexanol.

Administration, Oral↗
PubMed1993

The inhibition of cholesterol esterification by cyclandelate in transformed mouse macrophages.

Cyclandelate (trimethylcyclohexanyl mandelate) inhibited cholesterol esterification in a transformed mouse macrophage cell line (J774) with a concentration of approximately 20 microM being required for half-maximal inhibition. The intact drug was required for its inhibitory action since neither of its hydrolysis products, trimethylcyclohexanol and mandelic acid, caused any inhibition even at high concentrations. The drug entered the cells very rapidly with inhibition being apparent within the shortest time possible to measure esterification (15 min after drug addition). The rate of cholesterol esterification returned to control values when drug-inhibited cells were incubated in drug-free medium indicating a rapid loss of drug from the cells. Loading of cells with cholesterol had no effect on the inhibitory action of cyclandelate, and the inhibition of esterification of cholesterol appeared to be specific, since the syntheses of phospholipid and triacylglycerol (which also involve the action of acyltransferases) were not affected by the drug. Similar inhibitions of cholesterol esterification were seen in four other cell lines, a human osteosarcoma, Chinese hamster ovary cells, a human transformed macrophage cell line (U937) and human umbilical cord vein endothelial cells, as well as in slices of pig aorta, indicating a general action in extra-hepatic tissues where the drug is not hydrolysed.

Animals↗
PubMed1981

Simultaneous determination of cyclandelate and its metabolite in human plasma by capillary column gas-liquid chromatography.

A method was developed for the simultaneous determination of cyclandelate and mandelic acid concentrations in plasma, involving extraction from plasma followed by trimethylsilylation and chromatography of the derivatives on a glass capillary column with hydrogen flame-ionization detection. Calibration graphs were linear down to at least 20 microgram/ml for each substance. The precision was excellent with a pooled relative standard deviation of 6.3% and 6.4% for cyclandelate and mandelic acid serum samples, respectively. Concentrations below 500 ng/ml of each substance could be detected in human plasma. The method was developed for use in bioavailability and metabolism studies.

Animals↗
PubMed1977

Cyclandelate: effect on circulatory measurements and exercise tolerance in chronic arterial insufficiency of the lower limbs.

Thirty-nine patients with arterial insufficiency of the lower limbs were treated with cyclandelate or placebo in a double-blind cross-over study, to evaluate the effect of this drug on symptomatic and physiologic indicators of circulatory status. The following measurements were used: skin temperature of the big toe and dorsum of the foot; blood flow in the calf at rest and after exercise on a foot ergometer to the point of claudication; walking distance to the development of claudication; exercise tolerance on a foot ergometer; and reflex vasoconstriction on the skin of the toe in response to cooling of the upper extremities. During treatment with cyclandelate, significant improvement occurred in each of these measures of circulatory efficiency.

Adult↗
PubMed1977

Treatment of early diabetic retinopathy with cyclandelate.

In order to assess the effect of cyclandelate on the abnormal permeability of the blood-retinal barrier which occurs in diabetic patients before any other lesions are apparent in the retina a well-controlled, double blind, and paired trial was carried out in 22 patients. The treatments were randomised. The permeability of the blood-retinal barrier was assessed by vitreous fluorophotometry. Each patient was examined before being involved in the trial and then another 3 times with 1 month's interval. The total duration of treatment was 3 months. The results showed that the breakdown of the blood-retinal barrier as evidenced by the degree of abnormal fluorescein penetration into the vitreous suffered a significant decrease in the diabetic patients treated with cyclandelate when compared to the patients submitted to placebo administration, and this effect is particularly apparent in the third month of treatment.

Adult↗
PubMed1987

Calcium modulation and clinical effect. Profile of cyclandelate.

Since its original development as a vasodilator, cyclandelate has been shown to possess a pharmacological profile which reflects its primary mechanism of action-calcium modulation. Thus, the ability of the drug to improve the rheological properties of blood by maintaining red blood cell deformability and inhibiting platelet aggregation may be explained by its effects on the influx of extracellular calcium. Since elevated intracellular calcium concentrations are known to contribute to pathological changes in conditions of local cerebral ischaemia, the clinical implications for the use of cyclandelate in the treatment of such diseases are clear.

Calcium↗
PubMed1991

[Cyclandelate Reference Standard (Control 901) of National Institute of Hygienic Sciences].

The raw material of cyclandelate was examined for preparation of the "Cyclandelate Reference Standard". Analytical data obtained were as follows: melting point, 60 degrees C; ultraviolet spectrum, lambda max = 252, 258 and 264 nm E1%1cm = 6.1 (252 nm), 7.5 (258 nm), 5.9 (264 nm); infrared spectrum, 3454, 2948, 1730, 1453, 1202, 737, 695 cm-1; thin-layer chromatography, no impurities were detected until 1000 micrograms; high-performance liquid chromatography (HPLC), one impurity was detected, loss on drying, 0.00%. Based on the above results, this raw material was authorized to be the Reference Standard of the National Institute of Hygienic Sciences.

Chromatography, High Pressure Liquid↗
PubMed1987

Cyclandelate in the treatment of multi-infarct dementia. Interim findings from a multicentre study in general practice.

An open, multicentre clinical trial conducted in general practice was undertaken to investigate the effects of treatment with cyclandelate 800 mg twice daily in elderly patients with multi-infarct dementia. Interim findings in 303 patients demonstrate significant improvements after 12 weeks' treatment in mean scores of cognitive functions, orientation, verbal communications, social behaviour and interest in others and in the environment as assessed by the Blessed Dementia Scale and Parkside Behavioural Scale. Although a placebo response cannot be excluded because of the uncontrolled design of the study, these findings appear to warrant further investigation in well-designed controlled clinical trials in patients with multi-infarct dementia.

Aged↗
PubMed1982

[Efficacy of an etofylline-cyclandelate combination in age-dependent cerebrovascular insufficiency].

The pharmaceutical preparation Eucebral-N contains 80 mg etofylline and 100 mg cyclandelate. The drug is used curatively and preventively for peripheral and central circulatory disturbances. This report describes a study in which subjective statements of old patients from a home for the aged have been objectivated and evaluated. The results of the study, evaluated with usual statistical methods are: the communication ability, the state of confusion as well as the psychomotorical retardation could be improved significantly after 4 weeks', administration of the drug.

Aged↗