[Blood levels of vincamine. Comparative study of vincamine in delayed and immediate actions].
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Adolescent↗
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[Effects of vincamine on the mesenteric circulation in the rat. Microcirculatory evaluation of the vasodilator activity of vincamine].
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Animals↗
[Disparity in the kinetics of vincamine and vincamine hydrochloride absorption in the rat].
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Animals↗
[Plasma concentrations and renal excretion of vincamine after oral administration in man (author's transl)].
Plasma concentrations and renal excretion of 14,15-dihydro-14beta-hydroxy-(3alpha,16alpha)-eburnamenine-14-carbonic acid methylester (vincamine, Vincapront) were studied in 5 healthy volunteers following the oral intake of 30 or 60 mg vincamine, respectively. After the higher dose (60 mg vincamine), the treatment was continued by the daily intake of 3 X 20 mg vincamine for 5 days. Plasma vincamine levels were determined in the morning prior to the ingestion of the first 20-mg dose and in the evening 2 h after the intake of the third 20-mg dose. Our results prove that vincamine is rapidly liberated and absorbed from the tablet formulation used, the maximum plasma levels being reached 90 min after ingestion and amounting to a mean value of 139 ng/ml after 30 mg and to a mean of 252 ng/ml after 60 mg of vincamine. There was a biphasic elimination of vincamine after both doses indicating a process of distribution influencing also the elimination phase. In the 24-h urine, unchanged vincamine amounted to 5.8% of the applied dose after 30 mg and to 7.3% after 60 mg vincamine. Vincamine did not accumulate during the daily intake of 60 mg for 6 days. Side-effects were not observed in any volunteer during the period of observation.
Administration, Oral↗
Trachealis responses induced by vincamine and vinpocetine; inhibition by indomethacin and Ca2+ dependence.
Vincamine in low concentrations induced a sustained contraction of the isolated guinea pig trachealis with long latency and slow onset and, in high concentrations, it induced relaxation which was potentiated in the precontracted trachealis. Vinpocetine had actions similar to those of vincamine on trachealis, however its relaxant effect was more pronounced. The vincamine-induced trachealis contraction was not changed by substance P desensitization, was reduced by tetrodotoxin, nifedipine and low Ca2+ high Mg2+ solution and increased in nominally Ca2+-free solution. The vincamine-induced relaxation of precontracted trachealis was increased by guanethidine and was not affected by propranolol, high Mg2+-low Ca2+ solution and tetrodotoxin. Vincamine- and vinpocetine-induced trachealis contraction as well as vinpocetine-induced relaxation at basal tension were abolished by indomethacin. Vincamine in a low concentration shifted to the left the concentration-effect curve for CaCl2 in the K+-depolarized trachealis, and shifted it to the right at a high concentration. Our results indicate that the contractile and relaxant actions of vincamine and vinpocetine on the guinea pig trachealis may be due to the generation of prostaglandins and to changes in the membrane Ca2+ fluxes and/or the intracellular Ca2+ distribution.
Acetylcholine↗
Comparative study of the clinical effect of vincamine versus papaverine given parenterally in the acute phase of stroke.
The efficacy of the "oxygenator", vincamine was assessed in comparison to a classic vasodilator, papaverine, after parenteral administration during the first days of an acute thrombo-embolic stroke. All 263 patients admitted to this open trial had a thrombo-embolism of the A. carotis or one of its cerebral branches within the previous 24 h. Patients demonstrating minimal neurological deficit or requiring admission to an intensive care unit, or patients with a suspected hemorrhagic syndrome were excluded. Each patient received i.v. infusions (15 mg X 6) of 6 vials of vincamine per 24 h, or 6 vials of papaverine (40 mg X 6) per 24 h, occasionally in combination with acetylsalicylic acid (ASA), dipyridamol and hydrocortisone. An initial 3-h control was followed by regular surveillance for 5 days, paying special regard to consciousness and motricity. The administration of vincamine alone had a significantly more favourable effect than papaverine alone on consciousness (p less than 0.001). Furthermore, vincamine associated with other drugs was significantly superior (p less than 0.01) to papaverine given in association. A similar tendency was noted for motor recuperation after vincamine compared to papaverine (p less than 0.001). Vincamine and papaverine were well tolerated during the 5-days observation period, only one side effect after vincamine and four after papaverine being noted.
Adult↗
[Alerting effect of vincamine in rats (author's transl)].
The alerting effect of vincamine, an indole alkaloid of Vinca minor, has been demonstrated using three electropharmacological tests: 1) the sleep-wakefulness cycle of freely moving rats implanted with cortical electrodes, 2) the sleep induced by 200 mg/kg i.v. sodium 4-hydroxy-butyrate (GHB) in the curarized rat, 3) the duration of spindle activity in the E.E.G. of curarized rats provoked by an acute asphyxia in which the E.E.G. activity was abolished for 20 sec. Vincamine increased the total duration of wakefulness at the expense of sleep, decreased the number of phases of paradoxical sleep (PS), increased the latency of the first phase of PS, but had no effects on the sleep-wakefulness cycle in a further test 24 hours after administration. Vincamine induced neither stereotyped behavior nor hypermotility. Vincamine also decreased the duration of GHB-induced sleep and the duration of post-asphyxic spindles. All effects observed were dose dependent. By means of these electropharmacological tests we have been able to discover two further agents which have more potent alerting effects than vincamine: desoxyvincaminamide and N-cyclopropyl-desoxyvincaminamide.
Animals↗
[The effect of vincamine on cerebral blood flow as a function of application rate (author's transl)].
The effect of infusions of 14,15-dihydro-14beta-hydroxy-(3alpha, 16alpha)-eburamenine-14-carbonic acid methylester (vincamine; Vincopront) on cerebral blood flow (CBF) was investigated by the xenon clearance method. In 12 patients receiving 30 mg vincamine within 35--40 min no significant changes in hemispheric or regional CBF were observed. 14 patients received 40 mg vincamine within 35--40 min: in this group hemispheric CBF was significantly increased (p less than 0.01) when compared to the spontaneous changes observed in a control group. The increase was particularly prominent in poorly supplied brain regions. This effect was proved statistically by regression analysis. In a patient with astrocytoma the tumor-hyperperfusion was diminished by vincamine while the flow to the surrounding brain improved. The results indicate the dependency of the vincamine effect on the rate of application and thereby on the plasma concentration of the drug.
Adult↗
[Metabolism of vincamine in the rat].
The metabolism of vincamine hydrochloride was studied in the rat after oral administration of the drug. Vincamine is almost completely metabolized, only a small fraction of the original compound being excreted in the urine. The metabolites detected in blood, urine and tissues were purified by preparative thin layer and column chromatography in several solvent systems, and analyzed by mass spectrometry. It was found that the main urinary metabolites were vincamine conjugates (sulphates and glucuronides). Two new metabolites were detected in all the biological fluids and specimens analyzed: these compounds are more polar than vincamine and their structure was characterized by mass spectrometry, I.R. and U.V. spectroscopy and confirmed by synthesis in our laboratory.
Animals↗
[Demonstrating the effectiveness of cerebroactive drugs in aged patients. Results of a randomized double-blind study of a vincamine containing special preparation].
The neuropsychiatric symptoms of old patients with disturbed cerebral metabolism or blood flow mostly lead to great individual difficulties and make those patients difficult to handle: in the family as well as in hospital such patients develop alienation, isolation and therefore adaptation to a social structure deteriorates with time. In the course of a test program for medicinal therapy of this syndrome we studied the efficacy of a vincamine containing formulation (Pervincamin forte retard or Pervincamin ampoules, respectively) on the symptoms of a chronical brain disturbance. The study was randomised double-blind. We found that under the influence of the vincamine formulation the subjective symptoms, such as lack of interest, apathy, aggressiveness, raging, psychomotoric retardation, lack of concentration, dysmnesia, decreased with a statistical significance (p less than or equal to 0.05). Also the subjective symptoms, reported by the patients, such as tinnitus and vertigo decreased significantly under the treatment with the vincamine preparation. Therefore some of the parameters important for resocialisation and revitalisation of old patients could be influenced in a favourable way. Basing on the good results of our investigations, the treatment of psychiatric disturbances in old patients with vincamine containing drugs seems to be justified.
Aged↗
[Vincamine concentrations in plasma and cerebrospinal fluid in patients following intravenous infusion (author's transl)].
The pharmacokinetic characteristics of 14,15-dihydro-14beta-hydroxy-(3alpha,16alpha)-eburnamenine-14-carbonic acid methylester (vincamine; Vincapront) were studied after i.v. infusion (30 or 40 mg vincamine-hydrochloride within 28--40 min, respectively) in 6 patients with cerebrovascular diseases. At the end of the infusion, maximum plasma levels ranged between 607 and 999 ng/ml. The decline of the plasma concentrations after the end of the infusion could be described using a two-compartment open model. After a phase of distribution lasting 1--2 h there was a linear elimination of vincamine in the semilogarithmic plot. The mean half-life for the beta-slope was 2 h. In four patients we measured the vincamine concentration in the cerebrospinal fluid 2 h after the end of the infusion. It amounted to only 5--24% of the simultaneously estimated plasma concentration.
Adult↗
[The influence of vincamine on global and regional cerebral blood flow in acute and subchronic human cerebral ischimia (author's transl)].
The alterations in global and regional cerebral blood flow (CBF) following i.v. application of 14,15-dihydro-14beta-hydroxy-[13alpha,16alpha]-eburnamenine-14-carbonic acid methylester (vincamine) were studied in 18 patients suffering from acute or subchronic cerebral ischemia. CBF measurements were made after intra-arterial injection of 133Xe using a multi-detector measuring instrument. 30 sec after a single i.v. application of 30 mg/20 min vincamine a statistically significant increase of CBF by 1.5 ml/100 g/min was found, corresponding to 6.1% (p less than 0.01). The regional CBF was influenced to a varying degree, the areas marked by an insufficient blood supply showing a mean increase by 13.4% and the areas marked by normal basic values showing a mean increase by 5.3%. This difference in alteration is statistically significant (p less than 0.02) comparing the differences as percent. The duration of the action of vincamine on the CBF, after a single dose of 30 mg/20 min i.v., was determined for a maximum of 15 min. The CBF values measured within 15 min after the completed i.v. application of vincamine showed a mean decline in blood flow values by --2.5 ml +/- 7.4%, which is statistically insignificant.
Acute Disease↗
Influence of vincamine and piracetam on sleep--waking pattern of the cat.
The effect of Vincamine and Piracetam, two geriatric drugs, on sleep behavior of the laboratory cat was studied. The animals were chronically prepared for recording of the EEG of the cerebral cortex, the lateral geniculate body, and the hippocampus, and for recording of eye movements, the muscular tonus and respiration. During the experiment, sleep and waking behavior were monitored by the above mentioned telemetrically transmitted indicators and also through observation via closed-circuit television. Both Vincamine and Piracetam in doses of 1 and 300 mg/kg p.o., respectively, enhance absolute and relative amounts of paradoxical sleep (PS). Smaller doses have a lesser or no effect on PS. Larger doses again have little effect or else, in the first few hours after application, reduce PS and total amount of sleep. Both drugs have little effect on slow wave and total sleep. Piracetam, but not Vincamine, reduces the prominent frequency of the theta band in hippocampus during PS. The PS-enhancing effect of the two geriatric drugs may be related to their memory-improving influence.
Animals↗
Comparative study of the clinical effects of vincamine + glycerol versus glycerol + placebo in the acute phase of stroke.
The treatment of the acute phase of stroke creates a difficult problem to the clinician. The presently used drugs lead to controversial results. The progress in knowledge of the pathogenesis of cerebral damage underlines the determinant role of the metabolic deficits in the ischemic areas. The effect on the clinical symptomatology of patients in the acute phase of stroke was studied during a double-blind comparative clinical trial with an alcaloid of Vinca minor (Pervincamine) which acts favorably against disturbances of oxydative glucose metabolism and of cerebral microcirculation. 20 patients divided into two homogeneous groups received during 5 days either Pervincamine (4 ampoules of 3 ml = 60 mg vincamine p.d.) + glycerol, or glycerol + placebo administered by i.v. infusion. Clinically the results indicate a greater improvement of the neurological status (objectivated by a neurological scale) with vincamine treatment than with placebo. Statistically the analysis confirms the highly significant effect of vincamine on motility of lower and upper limbs (p less than 0.02) and the significant effect on cranial nerves (homonymous hemianopsia and conjugated deviation of eyes) (p less than 0.05) and on the sphincter control level (p less than 0.05).
Adult↗
Effects of vincamin on cerebral metabolism.
In this study the effects of vincamin (Pervincamine) on cerebral metabolism were investigated. 60 subjects were tested. Vincamin was administrated to 36, aminophillin to 12. No drug was given to the remaining 12 subjects who were used as controls. A definite increase in cerebral metabolism was observed in patients receiving vincamin either by intravenous or intramuscular injection. Practically no change in cerebral metabolism was detected in subjects treated with aminophyllin.
Adolescent↗
[Vincamine in patients with cerebral vascular insufficiency].
The effects of the treatment with vincamine in 20 patients with cerebral vascular insufficiency are reported. The patients were previously submitted to the following tests: neurologic examination, electroencephalography, laboratory tests, psychometry (memory, intellective capability, concentrated attention, abstract reasoning and personality tests). Patients were medicated with vincamin in a 40 mg dose within 24 hours during approximately a 150 days period, after which were again submitted to an identical analysis. The results obtained revealed that in a reasonable percentage of the cases vincamin is an useful medication in controlling the clinical manifestations of the cerebral vascular insufficiency, an improvement being demonstrated in the retrograde and anterograde deficit rate observed in objective tests. An improvement was also noticed in the electroencephalograpric pattern of a few patients.
Adult↗
[Effect of vincamine, vinervine and serotonin on the sexual cycle in rats].
With a prolonged enteral introduction indole alkaloids vincamine (5--20 mg/kg), vinervine (5 mg/kg) and serotonin (2 mg/kg) significantly lengthen the duration of the sex cycle through extending the estrus cycle (vincamine, vinervine and serotonin) and diestrus (serotonin). Without changing the weight of the uterus the studied alkaloids tend to significantly increase the weight of the ovaries and the number of follicles therein. In test with sexually mature castrated and also sexually immature (both alkaloids) and hypophysectomized (vincamine) animals these alkaloids fail to display any estrogenic action.
Animals↗
[A cholinergic participation in the increase of cerebral cortical blood flow induced by vincamine (rat) (author's transl)].
The effect of vincamine on cortical blood flow was tested in control rats and after atropine administration. Cortical blood flow was measured in urethanized rats by means of the hydrogen clearance method. A significative increase in cortical blood flow and decrease in blood pressure and cortical vascular resistance was produced by vincamine iv administration in control animals. In atropinized rats significative cortical blood flow changes were not observed although some tendency to increase was detected. It is suggested that increase in cortical blood flow induced by vincamine may be due to direct action on the vascular smooth muscle and, partially, through a cholinergic mechanism.
Administration, Topical↗