Oct 13, 2009

Zoloft (Sertraline)

Pharmacological action:
Antidepressant. Selective inhibitor return capture serotonin. Weak impact on return capture noradrenaline and dopamine makes. In therapeutic doses Zoloft (sertraline, asentra) oppresses also capture serotonin platelets blood of the person. Does not render stimulating, sedative or anticholinergic action. The preparation does not co-operate with m-holino, serotonine, dopamine, histamine, adreno- GABA- and benzodiazepine receptors. At application Zoloft there is no increase in weight of a body; in some cases its decrease is noted. The preparation does not cause mental or physical medicinal dependence. Аntidepressant effect it is marked by the end of the second week of regular reception of a preparation whereas the maximum effect is reached only in 6 weeks.
Zoloft very interesting preparation since is the most powerful inhibitor return capture dopamine with what some delayed stimulating effects of a preparation are connected. It is far not SSRI - it influences many structures, and ability inhibit return capture dopamine does this preparation unique in own way - in narcology is perspective enough, and capacity at it good, I would tell - simply the effect comes extremely slowly but if already comes will not be a little. The preparation is interesting to much: thanking its spectrum of activity, it results immune system of an organism in norm, eliminates some pathologies, but treatment should be long thus. And meanwhile it is powerful enough inhibitor return capture dopamine, only this effect, I will repeat, month and preparation reception develops more later somewhere. But it is not necessary to speak about good shipping... Never met. The first week - GI tract it is literally on the verge at many, the second week - starts to smooth out, and only on the third the expressed effect starts to be shown, but at many it is not present... Very delayed action at zoloft, but amazes a profile. And IMHO all these generics - asentra, stimuloton etc. Strongly concede zoloft on antidepressant effect and are ineffective.

May 23, 2009

Valdoxan (Agomelatine)

Agomelatine - agonist melatonin (MT1 and MT2 receptors)and the antagonist5HT2c.Represents an energizer, active on validate depression models (the test of the learnt feebleness, the despair test, chronic stress of moderate expressiveness), no less than at models with decinhronise a warm rhythm, and also in experimental situations of alarm and stress. It has been shown that Valdoxan does not influence capture monoamines and has no affinity to an alpha - beta-adrenergicheskim, gistaminergic, holinergic, dophaminergic and benzodiazepines to receptors; it explains absence at Valdoxan characteristic for other energizers of collateral actions on a gastroenteric path, sexual functions and cardiovascular system.
Agomelatine, thanks to antagonistic action on 5 HT2c receptors, liberation dophamine and noradrenaline, in particular in area prefrontal strengthens brain barks. In experiments on animals with the simulated syndrome of the braked phase of a dream (Delayed Sleep Phase Syndrome) at blind and old animals it has been shown that Valdoxan restores synchronisation cirkad rhythms through stimulation melatonine receptors. At chronic stress Valdoxan interferes with occurrence "broken off" (fragmented) a dream. In experiences on healthy volunteers Agomelatine did not break normal structure of a dream and well influenced a dream at sick of depression. In therapeutic doses Valdoxan prevented development of a sleeplessness and infringements of memory from the moment of reception of a preparation and till the morning.
Agomelatine does not cause accustoming that has been shown in research on healthy volunteers with use of a visual analogue scale or the Questionnaire of the Research Center on studying of fatal predilections (Addiction Research Center Inventory - ARCI 49 check-list). Valdoxan also investigated about occurrence of a syndrome of cancellation at sick of depression by means of a Questionnaire revealing signs of a syndrome of cancellation (Discontinuation Emergent Signs and Symptoms (DESS)). It was found out that the cancellation syndrome does not develop even at the sharp termination of treatment.
Valdoxan does not influence weight of a body.
During the program of clinical development Valdoxan its efficiency and safety against the big depressive frustration was investigated. In плацебо comparative controllable research 4500 patients from whom 2500 received a preparation from 6 weeks about one year are surveyed. Agomelatine it has appeared statistically significantly more effective in comparison with placebo, thus the antidepressive effect comes within two weeks (disorder of efficiency: from 49,1 % to 61 % against 34,3 % - 46,3 % in group receiving placebo).Also the authentic data about efficiency Valdoxan at patients with heavier forms of depressive frustration (indicators of a scale of Hamilton> 25), two thirds of population making more has been obtained. Researches with the active control have confirmed the received results.
Valdoxan also it was effective at initially high levels of alarm, no less than at a combination of disturbing and depressive frustration. Influence Agomelatine on sexual function sick of depression with remmitic a clinical course was studied. The Scale of studying of influence on sexual sphere (Sex Effects Scale - SEXFX) was used. It has been shown that Agomelatine does not cause sexual infringements and does not influence occurrence of excitation and orgazm. At sick of depression, since second week of treatment, Valdoxan statistically signi/ficantly improved process sleep, without causing thus the subsequent day block.

Apr 4, 2009


Itself Zoloft it is very quite good, but all these generics etc. Strongly concede on antidepressant effect and are ineffective. From sportsmen heard that they accept Zoloft during a diet, patiently transferring side effects as from it the weight does not increase.
Zoloft rather interesting preparation, it is the most powerful inhibitor return capture dopamine with what some delayed stimulating effects of a preparation are connected. It is far not SSRI - it influences many structures, and ability inhibit return capture dopamine does this preparation unique in own way - in narcology is perspective enough, and capacity at it not weak, I would tell simply the effect comes extremely slowly but if already comes will not be a little. The preparation is interesting to much: thanking its spectrum of activity it results in norm immune system of an organism, eliminates some pathologies, but treatment should be long thus. One of the few antidepressants by which it is treated coaxile toxicomania after removal algic and psyhotics symptoms - neither Cipralex, nor Paxil will not give in this case such result and as business apparently in range actions Zoloft and abilities to influence return capture dopamine about what in instructions to a preparation it is not told was found out, and meanwhile it is powerful enough IRCD, only effect this, I will repeat, month and preparation reception develops
more later somewhere. But here speak about good shipping - never met. The first week - G.I. tract it is literally on the verge at many, the second week - starts to smooth out, and only on the third starts to be shown expressed effect, but at many it is not present... Very delayed action IMHO at Zoloft, but amazes a profile.

Feb 28, 2009

Koaksil (Tianeptine, Coaxil): drug abuse

If you drink this product in a single year on the traditional pattern - 3 pills a day, no habit is not observed, but the higher the dosage of tianeptine - the stronger the narcotic effects from it.
In high doses, drugs acting as heroin + cocaine + MDMA. Hyperstimulation dopamine receptors, strong tranquilizing action, retardation enkephalinase, effects on GABA receptors, and many others led to a clear effect of drugs that people are familiar with the action of opioids, is associated with the heroin + cocaine, and the ordinary people to the large doses of tianeptine effect very similar to MDMA.
After half an hour, hour after administration of toxic doses of a strong euphoria, the desire to say, enjoy life etc. But this is a short - after the termination, there is very pronounced dysphoria, and people who were so stupid that took large doses of long-term development abstinenty syndrome, in which even the introduction of heroin intravenously only briefly addresses a meal.
Patients should be very well remembered: Koaksil - this is worse than heroin, crack etc., The drug did not go "of their victims... And everything starts with three pills a day... And ends with opioids, disabled life, limb amputations, with abscesses, where the dirty solution is injected intravenously 10-20 tablets and get past the...
Those who drink tablets reach the 60-120 or more tablets per day. Even a year or more sobriety and isolation of koaksila with physical exertion - no result - at the earliest possible drug run to a pharmacy for their antidepressants...

Lerivon side effects

1) Lerivon severe impact on the function of bone marrow - requires periodic monitoring of blood picture.
2) during the course of lerivon, on second - third week could be quite dramatic shift in gypo-and manic state, the drug should be immediately repealed.
3) For depleted patients lerivon is fairly heavy medication, and I frequently observed side effects in the form of infection in the mouth (candidiasis), and generally megascopic immunosuppressive effects - worsening of associated infectious diseases, and anemia.
4) Violation of swallowing reflex after about an hour after ingestion.
5) Increased salivation.
6) Increase of appetite.

Jan 27, 2009

Tianeptine (Coaxil)

Weak antidepressant without side effects. A well-tolerated. Addressed to light subdepressivnym states. Pronounced anksiolitic component of the drug.

Especially shown in gerontology, as has the perfect profile portability: poststroke, with dementia its. Showed people with suicidal tendencies, when you need to quickly stop melancholic syndrome - was a successful event. As AD is very active, by the way, just its own specific actions - need to drink quite a long time (60 days - at least).

In Narcology was indispensable for the treatment codeinizm as monotherapy in effect in a dose 1t 2 times a day + benzodiazepines and sleeping pills (sometimes). Is irreplaceable in the
subjects, likes dissociative drugs (dextromethorphan, especially in syrup, with gvayafenezin). A powerful gedonicheskim potential drug should be able to enjoy, it is now difficult. Cancer patients are responding well, there already, and large doses can be given (analgesia develops quite clearly against the background of redeminesation and the return of some optimism).

The positive side coaxil - diversity of action, the speed of the initial activation effect
neyroplasticity, low toxicity, the absence of numerous side effects, increasing libido its. The negative side - narkogen potential, but expressed only at high doses, that is, if properly to the patient, there is usually no problem. But history should be taken into account. Do not underestimate the coaxil - a unique product of its kind, but requires more care in the appointment.

Paroxetine (Paxil, Seroxat)

Good antidepressant SSRI. Used 1 times a day. So attractive that builds a dream (you can take and at night!) Without side effects.

More paxil renowned for its powerful syndrome lifting, so you need to repeal the drug VERY smoothly and, of course, under the supervision of a doctor. Himself the product, of course, one of the best of a group of SSRI.

In some countries it is forbidden due to toxicity, and because of the express repeal syndrome, which really did not write the instructions, and about large dosages and long-term, with the lifting of the drug should be very careful - to reduce the dose to the most minimum number mg a week or two, and then, even with a very smooth cessation of treatment, the syndrome is still occasionally lifting there, even some time later, a seemingly well-being.

Paroxetine abused many - he, unlike the other SSRI, gives expression anxiolytic effect, and later - pleasant activation in healthy people. Often the patients provoke suicidal actions. In small doses and short course, all this smoothed, but in other cases, where applicable paxil long and in high doses, to cancel it just so rarely, and often had to resort to other drugs (benzodiazepines, nootropics, hypnotics).

Paxil - one of the favorite drug, drugs, because in addition to its own euphoria in some cases, actions, even able to eliminate the effects of MDMA, returning to the central nervous system are more or less normal.

By lifting Syndrome - the worst drug. I already laugh - anything that ends with "aksil" - is evil: "Coaxil", "Paxil" When treatment with this drug, you need to observe very carefully, and before the appointment to make sure that the patient is not responding to therapy safer drugs. The impact on sexual function of the SSRI is typically transient in nature, but about paxil I've heard sad stories ...

Jan 23, 2009

Amitriptyline (Elavil, Endep)

Amitriptyline - a strong antidepressant threecycles nature. Currently, one of the strongest. Unfortunately due to side effects are limited and applied gradually being replaced by new class of antidepressants SSRI and double-acting antidepressants. There are strong sedative component of the drug.

Meanwhile, recall that some of the negative SE product can be significantly reduced. If I am not mistaken, this AD introduced in the list of essential medicines, and rightly so: there are often cases where the "save" the drug; ampul amitriptyline once was successfully used by ambulance in critical situations have occurred or exacerbation of depressive phase of MDP, or aggravate major depression with agitation, and the patient is literally dragged out of the windows of four people, and after the introduction of amitriptyline occurred at rest, and later at a hospital after treatment by other AD and drugs, the patient returned home in full remission - I know cases where this TCA truly and literally saved the lives of people.

If we talk about drug abuse, until very recently, amitriptyline, along with imipramine in different clinical cases was not only the leading AD in the treatment of opioid dependence syndrome, but often helped "not falling" in postabstinent period and in addition, also literally saved when This rare but very dangerous in terms of provocation, syndrome, as "psevdoabstinent syndrome". As I wrote in another article, this drug, if you use it well, you can remove the withdrawal symptoms of moderate (joint application with nootropil).

It's why something like this first treecyclic antidepressants ... I do not know, perhaps an old school, as they say, but these drugs have been predictable, the mechanism of action enough studied in medicine: amitriptyline, imipramine, azafen, sydnofen, pirazidol, inkazan, sydnocarb even indopan - and missed it ...

Amitriptyline in my "golden list" is, strangely enough - if properly used, is indeed able to perform miracles! Many do not know that, in addition to use in rare cases, half-quarter of tablets as tranquilizers and sleepings and antigastric-ulcer, not only amitriptyline, imipramine and still used in microdoses (1 / 7 - 1 / 10 tablets) syndrome quick feet, if not mistaken - once read an american work, where he was surprised that the use of amitriptyline ...


Venlafaxine is racemates R-and S-enantiomers, both have pharmacological activity. The main metabolite - O-desmetilvenlafaksin that are in the blood plasma than venlafaksine - has similar antidepressive activity, which may soon be presented as a separate product.

Venlafaxine inhibits serotonin transporter protein, but in high doses - as norepinephrine transporter. This drug has no affinity to muscarinic, adrenergic, histamine, 5-HT1-and 5-HT2-serotonin receptors.

T1 / 2 venlafaxine is 5 h, O-desmetilvenlafaksin - 11 h. Binding venlafaxine with plasma protein is 27%, significantly lower than that of SSRI (for example, fluoxetine - 94%, paroxetine - 95%). Since venlafaxine inhibit CYP2D6, it may impede the normal metabolism of other drugs, metabolic this proferment.

Most studies have shown similar efficacy venlafaxine and other antidepressants. In comparison with sertralin and estsitalopram, venlafaxine demonstrated similar effectiveness of these drugs in treating patients with severe depression and in improving their quality of life. A meta-analysis showed an advantage over venlafaksin SSRI, but the analysis had been included only studies with the use of fluoxetine and paroxetine, and the results can not be extrapolated to all SSRI. Large meta-analysis combined the results of 33 RKI involving patients with deep depression that took venlafaxine, fluoxetine, paroxetine and fluvoxamin. The level of remission when receiving venlafaxine was 45%, while taking SSRI - 35%, and placebo control group - 25%. Similar results (more efficiency venlafaxine compared with SSRI) has been demonstrated in other large meta-analysis.

Meta-analysis was criticized because it venlafaksin compared with SSRI in low doses, which could not affect the results. This has led the authors of a new, more accurate studies, but the result was the same. The depth of the effect and the frequency of remission was higher in the application venlafaxine. It was concluded that venlafaxine is really more effective antidepressant compared with SSRI. In parallel, there were reports that there is no significant difference in performance between the second generation of antidepressants, and only minor (but statistically reliable) venlafaxine advantages and sertralin compared with fluoxetine. The decisive criterion in such situations has become controversial speed the onset of clinically significant effect, and venlafaxine in this regard has obvious advantages. In particular, the effect when receiving high-dose venlafaxine occur 1-2 weeks after admission (compared with placebo). The scheme with the rapid build-up of a daily dose venlafaxine to 375 mg / day to achieve strong clinical effect is already over 1 week of therapy.

The same is not enough data on the duration of remission in treatment venlafaxine compared with SSRI. A long reception venlafaxine (12 months), only 22% of patients moved relapse of depression, while in the placebo group the rate was 55% (p <0001), which favors the use of drugs for maintenance therapy to prevent relapse of depression.

Interestingly, in a meta-analysis, together 3 273 patients in the group venfalaxine of SSRI group and 932 patients in the placebo group, demonstrated the effectiveness of preferential venlafaxine in the reduction of somatic symptoms on a scale of HAM-D compared with SSRI and placebo. Profile portability venlafaxine reflects its pharmacodynamics: on the one hand, there are serotoninenergic (nausea, vomiting, sexual dysfunction, etc.), on the other - noradrenergic (sweating, dry mouth, increased heart rate and blood pressure). It is noted that the increase of blood pressure are about 3% of patients, and this effect is likely to be dose dependent.

Venlafaxine does not cause sedation and antiholinergic appearance. The number of interrupt treatment is the same as other antidepressants in the treatment of the second generation. One of the most dangerous complication is a severe hyponatremia (occurs very rarely), which leads to the syndrome of inadequate giperprodukt antidiuretic hormone, especially if the initially low levels of sodium (for example, in the accompanying admission diuretics).

Good medicine with proven effectiveness.

Jan 22, 2009

Cymbalta (Duloxetine)

Preparation of cymbalta, experience of its application... On degree reaptake serotonin it on the second place after paroxetine. The preparation possesses central analgetic action. On degree of expressiveness of antidepressive effect concedes Ixel. But also adverse less. Causes equal enough condition. Inversion of affect and transition in a hypomaniacal condition it is improbable. However duloxetine - not such harmless and weak: it is shown in the USA at the big depression, at patients are often marked SE from outside CNS and not only. Once again coming back to new the AD-SSRIs, it turns out that most "counterbalanced" on influence on monoamins is milnacipran - it and strongest of all (not including resistant), on the second place - venlafaxine, is more toxic and hardly is less active, dosedependent, well and duloxetine - the softest, difficult structure. Apparently concedes two above named the AD, but it is better transferred, though and not such active. Unless such the inactive? It to all a question, would be desirable to hear opinions dealing with it: after all when said that the same tianeptine is weak, there specificity - the preparation is drunk at once on one т. Three times day, and a course should be long for revealing of all capacity of a preparation - it helps and at heavy depressions... It is a pity, it is a pity that now so with it - much elderly, somatic the patient is excellent went, without SE... Here for what I hate these addicts chemist's - well there the potion it is clear, but what for to be perverted by what a drug is not? How many people were rescued by this preparation, and many has killed and kills... Are Now very necessary for psychiatry SSRIs, but soft, without expressed SE, strong as Ixel and with SE smaller than at duloxetine - these preparations indirectly influence on D2 - D3, there are some data, but the fact what exactly these preparations are most shown at coaxilizm - undoubtedly! Only are necessary such the AD that were transferred exhausted - duloxetine like as approaches, and on anxiolytic activity. We will look that will be further...

Jan 21, 2009

Ixel (Milnacipran)

Milnacipran - rather and rather interesting preparation: from all three now known SSRIs, only Ixel the balanced impact on reaptake serotonin makes and noradrenalin, thus it is necessary to consider and that remarkable fact that Ixel is capable somewhat inhibit return capture dopamine. Expressed timoanaleptic preparation action is accompanied by the strongly pronounced anaesthetising action so expressed that this preparation in a number of the countries is registered as analgetic at fibromyalgia and similar conditions.

It is important to understand that a preparation often register in doses 25мг twice a day; in a dose 50мг twice a day and 150-200 and more mg twice a day. The first variant often appears insufficient for depression overcoming, and a dose in limits 100мг - 200мг twice a day DO NOT RAISE ANTIDEPRESSIVE EFFECTS of the PREPARATION, BUT OFTEN CONDUCT To DEVELOPMENT SE, therefore most good the dosage 50мг twice a day long enough course is. At this dosage Ixel shows balanced enough action both on braked, and on agitation depressions though the activating component prevails, but not so that it was impossible to fall asleep, moreover against reception of such powerful BD as fenazepam or clonazepam - I will tell more: Similar combinations create preconditions for abusing as Milnacipran, and a BD and their mix, therefore from a BD it is necessary to be rather accurate - I often say that fenibut or mexidol are here alternative of a BD, and promote improvement cognitive f-tsy. Pirazidol possesses balanced enough action and around doses 400мг-600мг under condition of good shipping, renders expressed enough tranquilizing action. With account SE pirlindole pertinently to combine it with mexidol, if necessary appointing in the first days of a BD or neuroleptic though this period it is possible to "endure and wait disclosings" of effects pirlindole, quickly increasing doses (50mg/days - the first and second days; 100mg/days - in following two days and so to a necessary dose which for pirazidol makes 200-600мг - at a dosage in 400мг both more the preparation is rather active and influences a dream a little - there is an improvement slipping.

If to speak for Ixel this preparation is distinct from pirazidol that pirazidol is more active under the relation of braking of disintegration and reaptake noradrenalin, than serotonin, and to dopamin it is absolutely indifferent. Milnacipran renders and the balanced action on reaptake as 5HT and NA, slightly influencing on reaptake dopamin. Therefore in doses 50мг twice a day, at reception together with meal, SE a preparation are minimum, actually comparable with placebo while powerful and rather unique antidepressive effect milnacipran gradually develops. Good-quality hyperplasia a bladder is RELATIVE contra-indication for milnacipran, but only in adequate doses. There is a weight of works where efficiency Ixel is shown at ОКR, fibromyalgia, HBS a various aetiology, and, actually, powerful BALANCED timoanaleptic action without expressed SE whereas, I will repeat, dose escalating even on 25-50мг a day does not raise activity of a preparation, but does obvious SE a preparation. Therefore banal updating of a dose and if on a dose per 100mg/days in two steps the answer will not follow in a current of month is necessary, there is a sense to think of preparation change. The same pirlindole - quite good alternative In some cases for those who has not answered therapy milnacipran. To RAISE the DOSAGE of THIS PREPARATION of ANY SENSE HAS no! IT WILL cause ONLY DISTINCT SE And WILL demand APPLICATION POWERFUL HYPNOTICS When In ADEQUATE DOSES MILNACIPRAN POSITIVELY INFLUENCES the DREAM. And here in a case with pirlindole affairs are absolutely otherwise: the above a dose, The expressed and balanced effect of it the AD. Again we have a situation when psychiatrists are not able to address about the AD. It already starts to bother on the sly...

Jan 20, 2009

Lerivon (Mianserin)

Excellent preparation! As well as mitrazapine from this "Organon" it is quite good at the big depressions, but, as well as all the AD, not always yields so positive results, unfortunately. There are patients with heavy depression, but exhausted by illness so that at appointment mianserin along with bad shipping, often enough it is possible to observe and "other party of a medal", unfortunately... For the exhausted patients mianserin is heavy enough preparation, and I often enough observed side effects in the form of infection occurrence in a mouth (candidiasis), and in general visible with the naked eye imunodepression effect both lerivon, and mianserin: that "grippe similar syndrome", an aggravation of accompanying infectious diseases and an anaemia. As it is frequent enough from lerivon there is a transition in hypomania that interferes with the further use of this preparation. From many people it was possible to hear enthusiastic exclamations about lerivon that is connected with the sedative in some cases sedative and somnolent effects and fast enough improvement of mood at application of it the AD.

I only am glad for success in this case, but consider not out of place to remind about unbeneficial enough influence mianserin on marrow function - the neglect this fact can sometimes lead to the most undesirable consequences. I somewhere wrote already, communicating with Atroposom that starting with a chemical structure, lerivon it is possible to consider as typical TTSA-DERIVATIVE dibenz [b, e] azepin with the limited quantity konformation for the basic lateral chain that provides the best complementarity to receptor complex and sharp increase of activity as to a consequence of it; "Braided" in a cycle the lateral chain changes, certainly farm. profile the AD and minimize collateral cholinolytic effects peculiar classical TCA, but the AD in global sense is "easier", from it does not become, unfortunately... Lerivon also has analgetic effect of the central character; mitrazapine, and, it is visible lerivon also, have affinity to kappa-opioid to receptors, than partly it is possible to explain often enough meeting at use organons preparations of some mental infringements and transitions in mania, well and stimulation adrenergic processes quickly causes condition improvement though in certain cases it can appear undesirable.

Sum up experience of application of these preparations, their structure and action mechanisms, it is necessary to rejoice that in most cases the price justifies effect, but practice shows that to the patients accepting both lerivon, and remeron, the rigid control from outside the medical personnel with periodic monitoring of a picture of blood is required. Often at course passage lerivon, on the second-third week there can be sharply enough a transition in hypo- and maniacal conditions that is at the bottom of preparation and transition cancellation as I already also wrote, on older TCA in a complex with nootrops, a BD and other means. And knowing that fact that many these apply the AD in self-treatment, I consider inadmissible as over-the-counter of these the AD from drugstores, and actually their out-patient appointment.