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Adaptol (mebicar)


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#1 medievil

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Posted 04 September 2010 - 12:12 AM


Adaptal looks pretty interesting, its also dirt cheap so worth giving a try.

Here we go:

Zh Nevrol Psikhiatr Im S S Korsakova. 2010;110(2):45-9.
[Adaptol in the treatment of anxiety disorders in children with school maladaptation]
[Article in Russian]

[No authors listed]

Abstract
We examined 336 children, aged 7-14 years, with signs of school maladaptation (SM). Anxiety disorders were found in 167 (49.7%), including generalized anxiety disorder - 87 children (25.9%), phobic disorder - 40 children (11.3%), anxiety disorder - 14 (4.2%), social anxiety disorder - 26 (7.7%). These indices differed significantly from those in the comparison group of children without SM. The children with generalized anxiety disorder were treated with adaptol (1000 mg/d during 30 days). The clinical and psychological examination revealed the high efficacy of this drug. Adaptol was well-tolerated, with no side-effects observed.

Zh Nevrol Psikhiatr Im S S Korsakova. 2009;109(8):45-8.
[Adaptol in the treatment of ADHD.]
[Article in Russian]

Chutko LS, Surushkina SIu, Nikishena IS, Iakovenko EA, Anisimova TI, Sergeev AV.

Abstract
Effectiveness of adaptol, a non-benzodiazepine tranquilizer, in the treatment of ADHD has been studied. The use of adaptol in dosage 500 mg 2 times daily during one month resulted in the decrease of hyperactivity and impulsivity and did not exert any influence on attention and reaction time. The authors emphasize the importance of this fact due to its relation to side-effects which are often seen in the treatment with benzodiazepine tranquilizers. It has been concluded that adaptol may be used in the treatment of ADHD as a monotherapy in cases with predominance of hyperactivity/impulsivity and as a complex therapy in other diseases especially in the combination of ADHD and anxiety disorders.

Farmakol Toksikol. 1988 Jan-Feb;51(1):21-3.
[Clinical and experimental validation of the use of the tranquilizer mebikar as a corrective of the neuroleptic syndrome]
[Article in Russian]

Zimakova IE, Semenikhin DG, Karpov AM, Kirshin SV.

Abstract
The results of the experimental and clinical studies showed that administration of mebikar in combination with neuroleptics reduced the degree of side effects of the neuroleptics without decreasing their antipsychotic effect.

[Evaluation of the nootropic effect of mebikar in clinical practice]
[Article in Russian]

Zimakova IE, Makarchikov NS, Karpov AM.

Abstract
Mebicar therapy resulted in a reduction of the degree of deficient disorders of thinking in 27 of 50 patients with paranoid schizophrenia and normalization of indices of mental working capacity, attention and memory, shortening of the time of visual-motor disjunctive reaction in 50 patients with borderline states. Mebicar was shown to possess a nootropic effect which differs qualitatively from that of piracetam.

[Effect of tranquilizers on the course of myocardial ischemia and on myocardial resistance to hypoxia in coronary artery occlusion]
[Article in Russian]

Kovalev GV, Gurbanov KG, Tiurenkov IN, Naĭdenov SI.

Abstract
It was shown that meprobamate and phenazepam protect the myocardium from hypoxia and decrease myocardial ischemia during coronary occlusion. Phenibut and mebicar reduce the tolerance to ischemia and increase the degree of ischemic injury to the heart. Diazepam has no effect on these processes.

[Effect of tranquilizing agents on the blood level of endogenous ethanol in alcoholics]
[Article in Russian]

Burov IuV, Treskov VG, Drozdov ES, Kovalenko AE.

Abstract
Experiments on alcohol addicts blood were made to study the time course of the endogenous ethanol level after a single administration of mebicar (1.5 g), a derivative of bicyclic bisuria, 50 ml of 5% sodium hydroxybutyric syrup, a derivative of gamma-hydroxybutyric acid, and 20 mg diazepam, a derivative of 1,4-benzodiazepines. The clinical effect was recorded simultaneously. It was established that different tranquilizers stimulate the increase in the endogenous ethanol level as regards the spectrum of psychotropic activity. This effect was the most pronounced with mebicar and to a less measure with diazepam.

[Comparative analysis of the behavioral, neurochemical and autonomotropic effects of mebikar and diazepam]
[Article in Russian]

Zimakova IE, Kirshin SV, Kamburg RA.

Abstract
It has been shown that the tranquilizers, diazepam (a 1,4-benzodiazepine derivative) and mebicar (a derivative of bicyclic bisureas) produce one-line inhibition of the production of the conditioned reflex of active avoidance in rats and of their "open-field" motor activity. Both the drugs change the balance of neuroactive amino acids in the animals' brain. However they produce different changes: diazepam increases the content of asparaginic and glutamic acids, while mebicar raises that of gamma-butyric acid. No interrelationship was found between psychotropic and vegetotropic effects of the tranquilizers.

Farmakol Toksikol. 1982 Jul-Aug;45(4):16-9.
[Protective effect of the psychotropic preparations diazepam, sodium oxybutyrate and mebikar in experimental arrhythmias]
[Article in Russian]

Kamburg RA, Zimakova IE.

Abstract
It was shown that the psychotropic agents diazepam (1-2 mg/kg), sodium hydroxybutyrate (50-100 mg/kg) and mebicar (250-500 mg/kg) exert a protective action in experimental arrhythmias. This effect is determined by the ability of the drugs to reduce intoxication phenomena, as well as by their antihypoxic and stress-protective properties. On the other hand, the drugs exert an antiarrhythmic effect proper, interfering with potassium ion balance. The protective effects of diazepam, sodium hydroxybutyrate and mebicar enable their application in combined therapy of arrhythmias of varying genesis.

[GABA-ergic component in the action of the tranquilizing agent mebikar]
[Article in Russian]

Kirshin SV, Zimakova IE.

Abstract
The paper is concerned with studies into the effect of the tranquilizer mebicar, a derivative of tetra-N-alkyl bicyclic bisureas, on the GABA-ergic system. The drug in doses of 250-1500 mg/kg (1/15-1/2 LD50) increased the preconvulsive period upon thiosemicarbazide administration, inconsistently changed the effects of picrotoxin and displayed antagonism in regard to bicucullin. Upon 2-week administration the drug reduced the GABA content in the rat brain. A hypothesis is advanced of mebicar-associated facilitation of the inhibitory GABA-ergic transmission.


Edited by medievil, 04 September 2010 - 12:25 AM.

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#2 medievil

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Posted 04 September 2010 - 12:12 AM

Farmakol Toksikol. 1981 Nov-Dec;44(6):654-7.
[Adaptogenic effect of mebikar in emotional stress, physical exertion and hypoxia]
[Article in Russian]

Kozlovskaia MM, Ostrovskaia RU, Kleĭmenova NN, Kamysheva VA, Sudareva SN.

Abstract
Adaptogenic effect of mebikar was revealed in experiments on cats, mice and rats. The drug was shown to decrease the emotional stress and to completely remove the stupor-like state in cats induced by stress situation and pain stimulation. The drug slightly increased the lifespan of animals under hypoxic hypoxia and raised the limits of maximum tolerable physical load. It lowered the accumulation of hypoxic lactate. Electron microscopy and biochemical analysis revealed the mebikar-induced increase in glycogen content in muscle cells of the myocardium and in skeletal muscles. The data obtained indicate that mebikar is conducive to optimization of the behavior and some processes of energy metabolism in animals exposed to emotional stress, exercise and hypoxic hypoxia.

Vestn Khir Im I I Grek. 1981 Jul;127(7):81-5.
[Effect of mebikar on the experimental and clinical course of traumatic shock]
[Article in Russian]

Bazarevich GIa, Zimakova IE, Kharin GM, Katkovskiĭ GB, Lazareva LV.

Abstract
The effect of mebikar upon the course of traumatic shock was studied on the basis of experimental investigations and clinical observations. The authors have found a positive effect of the drug on indices of acid-base state, histostructure and cellular composition of the liver whose disturbance has a great pathogenetic significance in shock. The application of mebikar considerably improved the results of treatment in clinic and reduced lethality in experiment. It was supposed that the positive effect of the drug was associated with prevention of the development of circulatory disorders and with the maintenance of oxidation-reduction process and the histostructure of tissues.

[Effect of mebikar on focal epileptic activity]
[Article in Russian]

Rekhtman MB, Torshin VI, Darinskiĭ NV.

Abstract
Effect of mebicar on the epileptic activity (EA) and frequency of interepileptic activity discharges (IEAD) was studied in experimental focal cortical epilepsy induced by penicillin application to the sensomotor cortex of conscious rats. Mebicar in a dose of 300--100 mg/kg induced a dose-dependent suppression of EA in the presence of the increased frequency of IEAD. During rhythmic stimulation of some areas of the thalamus mebicar completely abolished high-frequency EA, promoting consecutive alternating on the electrocorticogram of periods of responses to each stimulus with dead bands. The antiepileptic effect of mebicar was compared with that of diazepam in the similar model of epilepsy. It is suggested that the action of mebicar on the focus of epileptic activity in the cerebral cortex is related to the potentiation of synaptic inhibition of the neurons in the focus of epileptic activity.

[Correlation between the stress-protective and vegetotropic action of mebikar]
[Article in Russian]

Val'dman AV, Zaikonnikova IV, Kozlovskaia MM, Zimakova IE, Bravkov MF.

Abstract
Mebicar, a tranquilizer of the group of tetra-N-alkyl bicyclic bis-ureas, under acute emotional stress in cats (confrontation with a dog), simultaneously with tranquilizing effect on behavior also improves central baroreflex control and reduces hypertensive reaction of the arterial pressure. In rats, it normalizes disorders of individual and intraspecies behavior induced by the stress of a long-term social isolation. It decreases the degree of ulcer injury of the stomach during the immobilization stress.

[Effect of mebikar on the state of animals under extreme conditions]
[Article in Russian]

Zimakova IE, Kamburg RA, Kirshin SV.

Abstract
A new original tranquilizer mebicar exerts a protective action on some parameters of body function under the influence of extreme conditions (stress, hypoxia). Antihypoxic effect of the drug manifests within a wide dosage range (100-1000 mg/kg) and compares favourably with the effect of sodium hydroxybutyrate. Mebicar does not affect the muscle tone, movement coordination or working capacity of the animals. It is suggested that the normalizing action of mebicar as tranquilizer and antihypoxic agent may be related to its involvement in metabolism.

[Characteristics of the psychotropic spectrum of action of mebicar]
[Article in Russian]

Val'dman AV, Zaikonnikova IV, Kozlovskaia MM, Zimakova IE.

Abstract
Under group interaction in cats, a new Soviet tranquilizer mebicar eliminates fear-alarm induced by stimulatin of the emotiogenic zone of the hypothalamus. This action is not associated with myorelaxant or hypnotic action. Mebicar decreases the brain noradrenaline level, exerts no effect on the dopaminergic systems, increases the brain serotonin level, and does not elicit cholinolytic action.

Farmakol Toksikol. 1977 Nov-Dec;40(6):684-7.
[Pharmacological effects of the new psychotropic preparation, mebikar]
[Article in Russian]

Zimakova IE.

Abstract
By its effects mebicar -- a derivative of bicyclic bis-ureas -- may be refered to psychotropic drugs occupying a middle position between tranquilizers and neuroleptics. The drug inhibits the orientation reaction in albino mice, potentiates the action of narcotic hypnotics, abolishes the conditioned reflex reaction of avoidance, displays central adrenolytic activity, interferes with the norepinephrine metabolism in the brain stem and modifies the permeability of the blood-encephalic barrier, like this is done by the known neuroleptics. The substance is little toxic, does not exert any direct spasmolytic action on the isolated organs.


And 2 anecdotal reports ive found online, perhaps we could find more with google translate and then look around on a couple of russian fora.

So i order this med i run across,adaptol(mebicar)

Sounded great,but saw price at 10 dollers and said eh ill try it but much hope was lost.

In fact i had it sitting around a while,ten dollers threw me off.

Well i take it one night,and it was the most potent tranqulizer i had taken in a long time.

I just today took delivery of a russian tranquiliser drug called 'adaptol' also known as 'mebicar' and took a dose that was 'recommended' and it put me out very quickly... after the acute effects wore off however it has turned out to be even more effective than verapamil although it seems to also be reducing the more apparent effects of the MDPV when I consider it a little longer I think that it is simply that I am not used to such a diminished response to MDPV's sympathomimetic effects.

I also seemed to have an allergic reaction to the mebicar which seemed to be mostly ameliorated by taking a moderate dose of ascorbic acid (1500mg or so) and I am hoping will not be present when I take much lower doses of mebicar, I did take it on an empty stomach, the first 300mg, and redosed about 90 minutes later with 150mg shortly after which I was unable to sit upright due to being rather wobbly. Upon waking I had visual disturbances and difficulty recognising what objects were. I plan to take the dose down to 150mg next time I dose it to see whether it still has this calming stimulant side effect reduction effect at the lower dose. I often have odd reactions to various drugs but I think after this experience in future I will stick to dosing at a rate of half the recommended minimum especially in the case of tranquiliser type drugs because I am generally sensitive to them, 5mg of diazepam knocks me out for about 4-5 hours, whereas most people just get mildly drowsy.

Same person:

not sure if it was just a glitch, the initial sedating effect from taking 450mg of mebicar but 300mg on top of about 6mg of desoxypipradrol completely eliminated the anxiety and paranoia (dosed 4mg then about another 2mg 7 hours later and found the effects too strong and bad effects too much but the mebicar worked a treat).

desoxy is weird stuff, so not used to the thing of only having one dose a day, makes me forget i need to redose the verapamil and mebicar to keep up with it.

Those reports are pretty vague tough.

Edited by medievil, 04 September 2010 - 12:25 AM.


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#3 Temp

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Posted 04 September 2010 - 12:26 AM

1


Ok first of all 80% of those "Reports" the person Zimakova is either the primary author or the senior scientist (last author) or just a co-author. So basically it's the same institution most likely sharing the same grant trying to publish or perish in order to maintain the grant.

Edited by Temp, 04 September 2010 - 01:21 AM.


#4 medievil

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Posted 05 September 2010 - 01:20 PM

1


Ok first of all 80% of those "Reports" the person Zimakova is either the primary author or the senior scientist (last author) or just a co-author. So basically it's the same institution most likely sharing the same grant trying to publish or perish in order to maintain the grant.

Yeah can be true, still interested in giving it a try :cool:

#5 Ben

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Posted 27 October 2010 - 12:49 PM

What is mebikar? Has anyone any information on its pharmacology?

#6 tjcbs

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Posted 21 December 2010 - 12:15 AM

anyone try this?

#7 kikai93

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Posted 21 December 2010 - 01:08 AM

What is mebikar? Has anyone any information on its pharmacology?


Previous studies by the present inventor and colleagues have shown that mebicar exerts a protective action on some parameters of body function under the influence of extreme conditions such as stress and hypoxia, within a wide dosage range (100-1000 mg/kg), without affecting the muscle tone, movement coordination or working capacity of tested animals (Zimakova et al., 1980). Mebicar was also shown to change the balance of neuroactive amino acids in the animal’s brain by raising the content of gamma-butyric acid (Zimakova et al., 1982), and to exhibit a protective action in experimental arrhythmias (Kamburg and Zimakova, 1982). Mebicar was further shown to produce an antishock action and to normalize acid-base and oxygen homeostasis (Zimakova et al., 1984). Mebicar was also shown to increase the myocardial contractility, to exert a slight effect on the cardiac rhythm and to dilate the peripheral arteries, and the cardiac stimulating effects were attributed to the involvement of mebicar in the myocardial metabolism (Kamburg, 1990). Authors have developed experiment using mebicar (2,4,6,8-tetramethyl-2,4,6,8-tetraazabicyclo[3.3.0]-octane-3,7-dione) in form of generic formulation Cereprotex.

The present study describes the neuroprotective effects of Cereprotex (2,4,6,8-tetramethyl-2,4,6,8-tetraazabicyclo[3.3.0]-octane-3,7-dione) a well known formulation of mebicar used as tranqualisers since late 1970-s. Models of traumatic and hypoxic brain injury in mice and rats were used to assesses these effects.



So, if you're looking for a full-on tranq... I suppose go for it?


#8 medievil

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Posted 19 April 2012 - 10:43 AM

Bump its damn cheap and looks very promosing; im looking for a anxiolytic to add to my stimulants and may try this.

#9 medievil

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Posted 08 March 2013 - 02:16 AM

bump
Its so cheap, and effective anxiolytic, so why nobody try.

#10 Dinvestor

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Posted 29 July 2013 - 04:27 PM

Just trying to update...Is there anybody out there that has experience with this compound?

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#11 MangekyōPeter

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Posted 29 July 2013 - 09:50 PM

My mom uses it and it helps her with her anxiety, she feels more in control in anxiety-producing situations... Can't report first hand , but could give it a try.




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