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13 recordsLinked to original sources
PubMed1976

Effect of ethyl apovincaminate on the cerebral circulation. Serial angiography and regional cerebral circulation studies in neurosurgical patients.

The effect of ethyl apovincaminate (RGH-4405, Cavinton) on the cerebral circulation has been studied with two methods in a series of neurosurgical patients. Regional circulation was studied with the H2 clearance method in five patients in whom deep electrodes were lodged in various cerebral structures with stereotactic surgery performed for the underlying disease. In connection with serial angiography of 25 patients 10 mg Cavinton was injected i.v.; circulation time of the contrast medium, arterial circulation time, changes of normal and pathological filling were appraised. Registered 15 min after administration, regional circulation showed significant increase, but slight increase was demonstrable in every structure investigated. The change was more marked in two elderly patients over 60 years. In eight cases of serial angiography marked difference was seen in filling by normal and pathological vessels on Cavinton effect; arterial circulation time changed in three cases, contrast medium circulation time did not in any of the cases. The most marked changes occurred in three cases of cerebral vascular disease. In two cases of glioma vascularization of the tumour was visualized by Cavinton.

Brain Diseases↗
PubMed1976

Radiocirculographic study of the effect of ethyl apovincaminate on the cerebral circulation.

The effect of ethyl apovincaminate (RGH-4405, Cavinton) on cerebral circulation has been studied with radiocirculography (rc) in 12 healthy individuals and 17 patients suffering from cerebrovascular diseases. It was shown that acute Cavinton effect produced prolongation of circulation time both in healthy individuals and in more than half of our patients. Shortening of circulation time was observed in one case. On long-term Cavinton treatment circulation time was prolonged in 7 cases, not changed in 7, while in 3 cases it was shortened. The circulation times measured by rc did not reflect changes in the clinical picture.

Adult↗
PubMed1976

Biochemical effects of ethyl apovincaminate.

Some cerebrobiochemical effects of a new cerebrovasodilatory agent, ethyl apovincaminate (RGH-4405, Cavinton) have been studied. Changes of biogenic amines, 5-hydroxyindole acetic acid (5-HIAA) levels, serotonin (5-HT) turnover rate, furthermore effect on 3',5'-cyclic nucleotide phosphodiesterase (PDE; E.C.3.1.4.c) activity, isolated from different tissues, were determined. Lasting increase of cerebral 5-HIAA level was observed after treatment with the compound, 5-HT levels were transitorily enhanced 2 h following i.p. treatment. At later periods (4-6h) after treatment catecholamine levels were significantly raised. 5-HT turnover was practically uninfluenced by the compound. Activities of PDE preparations isolated from cerebral tissues were markedly inhibited. Various hypotheses are suggested in order to explain the biochemical mechanism of action of the compound.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1979

Kinetic metabolism of vinpocetine in the rat.

The pharmacokinetics of vinpocetine (Cavinton), a new potent vasodilator, and of its main metabolite have been studied in rats by specific extraction and radio thin-layer chromatography following i.v. and p.o. administration. The drug is rapidly eliminated, its half-life was found to be 125 min. The apparent volume of distribution was 3.8 l/kg and the clearance rate 33 ml/min/kg. From the equation describing the concentration-time curve a two-compartement open model was computed. Bioavailability of vinpocetine after p.o. administration was about 50%. The main metabolite, free apovincaminic acid, is formed very rapidly in rats and is eliminated from plasma with a half-life of 360 min.

Administration, Oral↗
PubMed1979

Pharmacokinetics of vinpocetine in humans.

The pharmacokinetics of ethyl-apovincaminate (vinpocetine, Cavinton), a new vincamine derivative has been studied in volunteers after p.o. and i.v. administration. The concentration of the drug was determined by mass-fragmentography in human plasma. There was a biphasic elimination of the substance after i.v. injection with a T1/2 alpha of 0.136 h and with a T1/2 beta of 4.83 h. The value of Vdss (2.1 l/kg) shows a high adsorption of the drug by tissue proteins. The clearance rate of elimination was 0.366 l/h/kg. Oral administration of the drug resulted in maximum plasma concentration 1--1.5 h after the administration with values of 20--62 ng/ml. The bioavailability of the drug--calculated from the ratio of the areas under the concentration-time curves--proved to be 56.6 +/- 8.9%. Unchanged vinpocetine could not be detected in urine. From the results two-compartment open models were constructed and the steady state concentrations after multiple dosing were computed.

Administration, Oral↗
PubMed2026

Add-on treatment with vinpocetine reduces seizure frequency and improves comorbidities in patients with loss-of-function γ-aminobutyric acid type A receptor variants.

OBJECTIVE: The semisynthetic compound vinpocetine has gained attention as a potential precision medicine for developmental and epileptic encephalopathies caused by loss-of-function (LoF) variants in γ-aminobutyric acid type A (GABAA) receptor genes. As a positive allosteric modulator of GABAA receptors, case reports suggest that vinpocetine can reduce epileptiform activity and seizure frequency, while improving cognitive function in patients with GABAA receptor-related epilepsies. Here, we extend these observations with a retrospective observational study evaluating the response to vinpocetine in an additional seven patients. METHODS: Patients initiated treatment with vinpocetine between 2018 and 2025 at the Danish Epilepsy Centre or abroad. Clinical data were collected from medical records, seizure diaries, and neuropsychological assessments. The modulatory efficacy of vinpocetine was investigated using electrophysiological studies. RESULTS: Nine patients harboring eight GABAA receptor LoF variants were given add-on vinpocetine treatment. Electrophysiological analyses confirmed dose-dependent positive modulation by vinpocetine across tested variants. Six patients with a median age of 15.5 years (range = 6-29) continued treatment for a median of 24 months (range = 12-90), whereas three discontinued due to adverse effects (AEs) or lack of efficacy. The patients' level of function ranged from normal to moderate intellectual disability, psychiatric comorbidities, and behavioral disturbances. Four patients initiated vinpocetine due to uncontrolled seizures. One became seizure-free, and two experienced a 50%-55% reduction. Electroencephalograms demonstrated improved spike-wave indexes in four patients. Six showed improvement in nonseizure factors, and caregivers reported reduced aggressivity and better vocabulary in one. Vinpocetine was well tolerated, with only mild and reversible AEs reported. SIGNIFICANCE: Adjunctive vinpocetine shows promise as a targeted therapy for patients with GABAA receptor LoF variants, decreasing seizure frequency and positively impacting nonseizure factors, with only mild AEs reported. Vinpocetine may be a safe and effective therapy for patients with GABAA receptor-related epilepsies, which should be investigated further in future N-of-1 trials.

Humans↗