MILDRONĀTS GRINDEKS 250 mg hard capsules, 60 pcs.
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20.50 €
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Expiration date: 2029-06-30
Meldonium is used as part of combination therapy in the following cases:
– reduced work capacity and physical overload;
– during the recovery period after cerebrovascular disorders or head injuries.
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Meldonium (Mildronāts-Grindeks) is a structural analogue of gamma-butyrobetaine (GBB), the precursor of carnitine, in which one carbon atom is replaced by a nitrogen atom. Its effects on the body can be explained in two ways.
▪ Influence on carnitine biosynthesis
Meldonium, by reversibly inhibiting gamma-butyrobetaine hydroxylase, reduces carnitine biosynthesis and therefore disrupts the transport of long-chain fatty acids across cell membranes, preventing the accumulation of powerful detergents — activated, non-oxidised fatty acids — inside cells. This helps prevent damage to cell membranes.
As carnitine concentration decreases under ischemic conditions, β-oxidation of fatty acids is suppressed and oxygen consumption in cells is optimised, glucose oxidation is stimulated, and ATP transport from sites of biosynthesis (mitochondria) to sites of utilisation (cytosol) is restored. In essence, cells are supplied with nutrients and oxygen, and their utilisation becomes more efficient.
At the same time, increased biosynthesis of the carnitine precursor GBB activates NO-synthase, which improves blood rheology and reduces peripheral vascular resistance.
As the concentration of meldonium decreases, carnitine biosynthesis gradually increases again, and the amount of fatty acids in cells is restored. It is believed that the effectiveness of meldonium is based on increasing the tolerance of cells to load when fatty acid levels fluctuate.
▪ Mediator function in the hypothetical GBB-ergic system
A hypothesis has been proposed that a neural signalling system — the GBB-ergic system — exists in the body, responsible for transmitting nerve impulses between somatic cells. The mediator of this system is the ester of GBB, the last precursor of carnitine.
Through the action of GBB-esterase, the mediator donates an electron to the cell, transmitting the electrical impulse, and is converted into GBB. The hydrolysed GBB is then actively transported to the liver, kidneys, and testes, where it is transformed into carnitine. In response to stimuli, somatic cells synthesise new GBB molecules, ensuring further signal propagation.
As carnitine concentration decreases, GBB synthesis is stimulated, increasing the concentration of GBB ester.
Meldonium, being a structural analogue of GBB, is capable of acting as a “mediator.” However, GBB-hydroxylase does not recognise meldonium; therefore, carnitine concentration decreases rather than increases. By replacing the mediator and promoting an increase in GBB concentration, meldonium enhances the development of the body’s adaptive responses. As a result, overall metabolic activity increases in other systems as well, including the central nervous system (CNS).
Influence on the CNS
Animal studies have demonstrated the antihypoxic effect of meldonium and its ability to improve cerebral circulation. Meldonium optimises redistribution of blood flow in favour of ischemic areas of the brain and increases neuronal resistance under hypoxic conditions.
Meldonium also exhibits CNS-stimulating properties — increased motor activity, enhanced physical performance, stimulation of behavioural responses, and anti-stress effects.
Effectiveness in cerebrovascular and neurological disorders
The influence of meldonium on the rehabilitation process in patients with neurological disorders (after cerebrovascular diseases, brain operations, trauma) has been studied.
Results of clinical evaluation of meldonium demonstrate a positive effect on patients’ physical performance and the restoration of functional independence during the recovery period, depending on the dose used.
Analysis of individual and overall cognitive function changes after treatment showed a positive effect on cognitive recovery during rehabilitation.
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Product details
Meldonium (Mildronāts-Grindeks) is a structural analogue of gamma-butyrobetaine (GBB), the precursor of carnitine, in which one carbon atom is replaced by a nitrogen atom. Its effects on the body can be explained in two ways.
▪ Influence on carnitine biosynthesis
Meldonium, by reversibly inhibiting gamma-butyrobetaine hydroxylase, reduces carnitine biosynthesis and therefore disrupts the transport of long-chain fatty acids across cell membranes, preventing the accumulation of powerful detergents — activated, non-oxidised fatty acids — inside cells. This helps prevent damage to cell membranes.
As carnitine concentration decreases under ischemic conditions, β-oxidation of fatty acids is suppressed and oxygen consumption in cells is optimised, glucose oxidation is stimulated, and ATP transport from sites of biosynthesis (mitochondria) to sites of utilisation (cytosol) is restored. In essence, cells are supplied with nutrients and oxygen, and their utilisation becomes more efficient.
At the same time, increased biosynthesis of the carnitine precursor GBB activates NO-synthase, which improves blood rheology and reduces peripheral vascular resistance.
As the concentration of meldonium decreases, carnitine biosynthesis gradually increases again, and the amount of fatty acids in cells is restored. It is believed that the effectiveness of meldonium is based on increasing the tolerance of cells to load when fatty acid levels fluctuate.
▪ Mediator function in the hypothetical GBB-ergic system
A hypothesis has been proposed that a neural signalling system — the GBB-ergic system — exists in the body, responsible for transmitting nerve impulses between somatic cells. The mediator of this system is the ester of GBB, the last precursor of carnitine.
Through the action of GBB-esterase, the mediator donates an electron to the cell, transmitting the electrical impulse, and is converted into GBB. The hydrolysed GBB is then actively transported to the liver, kidneys, and testes, where it is transformed into carnitine. In response to stimuli, somatic cells synthesise new GBB molecules, ensuring further signal propagation.
As carnitine concentration decreases, GBB synthesis is stimulated, increasing the concentration of GBB ester.
Meldonium, being a structural analogue of GBB, is capable of acting as a “mediator.” However, GBB-hydroxylase does not recognise meldonium; therefore, carnitine concentration decreases rather than increases. By replacing the mediator and promoting an increase in GBB concentration, meldonium enhances the development of the body’s adaptive responses. As a result, overall metabolic activity increases in other systems as well, including the central nervous system (CNS).
Influence on the CNS
Animal studies have demonstrated the antihypoxic effect of meldonium and its ability to improve cerebral circulation. Meldonium optimises redistribution of blood flow in favour of ischemic areas of the brain and increases neuronal resistance under hypoxic conditions.
Meldonium also exhibits CNS-stimulating properties — increased motor activity, enhanced physical performance, stimulation of behavioural responses, and anti-stress effects.
Effectiveness in cerebrovascular and neurological disorders
The influence of meldonium on the rehabilitation process in patients with neurological disorders (after cerebrovascular diseases, brain operations, trauma) has been studied.
Results of clinical evaluation of meldonium demonstrate a positive effect on patients’ physical performance and the restoration of functional independence during the recovery period, depending on the dose used.
Analysis of individual and overall cognitive function changes after treatment showed a positive effect on cognitive recovery during rehabilitation.
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1231220
MILDRONĀTS GRINDEKS 250 mg cietās kapsulas, 60 gab.
https://e-menessaptieka.lv/en/p/mildronats-r-grindeks-cietas-kapsulas-250-mg-n60-1231220
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MILDRONĀTS GRINDEKS
20.5
Meldonijs (Mildronāts-Grindeks) ir karnitīna priekšteča gamma butirobetaīna (GBB) struktūranalogs, kurā viens no oglekļa atomiem aizvietots ar slāpekļa atomu. Tā iedarbību uz organismu var izskaidrot divējādi.
▪
Ietekme uz karnitīna biosintēzi
SASKAŅOTS ZVA 18-02-2025
Meldonijs, atgriezeniski inhibējot gamma butirobetaīnhidroksilāzi, mazina karnitīna biosintēzi un līdz ar to traucē garķēžu taukskābju transportu caur šūnu apvalkiem, tādējādi novēršot spēcīgu deterģentu – neoksidēto taukskābju aktivēto formu uzkrāšanos šūnās. Šādi tiek novērsti šūnu membrānu bojājumi.
Samazinoties karnitīna koncentrācijai išēmijas apstākļos, tiek kavēta taukskābju -oksidācija un optimizēts skābekļa patēriņš šūnās, stimulēta glikozes oksidācija un atjaunots ATF transports no tā biosintēzes vietām (mitohondrijos) uz patēriņa vietām (citosolā). Būtībā šūnas tiek apgādātas ar barības vielām un skābekli, kā arī tiek optimizēta šo vielu izmantošana.
Savukārt, pastiprinoties karnitīna priekšteča, t. i., GBB, biosintēzei, tiek aktivizēta NO-sintetāze, tā rezultātā uzlabojas asins reoloģiskās īpašības un samazinās asinsvadu perifēriskā pretestība.
Meldonija koncentrācijai samazinoties, karnitīna biosintēze atkal pastiprinās, un šūnās pamazām atjaunojas taukskābju daudzums.
Uzskata, ka meldonija darbības efektivitātes pamatā ir šūnu slodzes (mainoties taukskābju daudzumam) tolerances paaugstināšana.
▪
Mediatora funkcija hipotētiskajā GBB-erģiskajā sistēmā
Izvirzīta hipotēze, ka organismā eksistē neirālo signālu pārnešanas sistēma – GBB-erģiskā sistēma, kas nodrošina nervu impulsu pārnesi somatisko šūnu starpā. Šīs sistēmas mediators ir karnitīna pēdējā priekšteča – GBB esteris. GBB-esterāzes darbības rezultātā mediators atdod šūnai elektronu, tādējādi pārnesot elektrisko impulsu, bet pats pārvēršas par GBB. Pēc tam GBB hidrolizētā forma tiek aktīvi transportēta uz aknām, nierēm un sēkliniekiem, kur tā transformējas par karnitīnu. Somatiskās šūnas, atbildot uz kairinājumu, sintezē atkal jaunas GBB molekulas, nodrošinot signāla izplatību.
Samazinoties karnitīna koncentrācijai, tiek stimulēta GBB sintēze, tā rezultātā palielinās GBB estera koncentrācija.
Meldonijs, kā norādīts iepriekš, ir GBB struktūranalogs, un tas spēj pildīt „mediatora” funkcijas. Turpretim GBB-hidroksilāze „neatpazīst” meldoniju, līdz ar to karnitīna koncentrācija nevis pieaug, bet samazinās. Tādējādi meldonijs, gan pats aizvietojot „mediatoru”, gan sekmējot GBB koncentrācijas pieaugumu, veicina organisma atbildes reakciju attīstību. Rezultātā pieaug vispārējā metaboliskā aktivitāte arī citās sistēmās, piemēram, centrālajā nervu sistēmā (CNS).
Ietekme uz CNS
Pētījumos ar dzīvniekiem novērota meldonija antihipoksiskā un smadzeņu asinsriti veicinošā darbība. Meldonijs optimizē smadzeņu asinsplūsmas pārdales apjomu par labu išēmiskiem perēkļiem, paaugstina neironu izturību hipoksijas apstākļos.
Meldonijam piemīt CNS stimulējoša darbība – kustību aktivitātes un fizisko darbaspēju pieaugums, uzvedības reakciju stimulācija, kā arī pretstresa iedarbība.
Efektivitāte smadzeņu asinsrites traucējumu un neiroloģisku slimību gadījumā
Pētīta meldonija ietekme uz rehabilitācijas procesu pacientiem ar neiroloģiska rakstura traucējumiem (pēc pārslimotām galvas smadzeņu asinsvadu slimībām, galvas smadzeņu operācijām, traumām).
Meldonija terapeitiskās efektivitātes pārbaudes rezultāti liecina par to pozitīvu iedarbību uz pacientu fizisko darbaspēju un funkcionālās neatkarības atjaunošanos atveseļošanās periodā atkarībā no zāļu devas.
Analizējot atsevišķās un summārās intelektuālo funkciju izmaiņas pēc zāļu lietošanas, konstatēta pozitīva iedarbība uz intelektuālo funkciju atjaunošanās procesu atveseļošanās periodā.
Menessaptieka/Visas preces/Medikamenti/Slikta pašsajūta
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Meldonium dihydricum
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