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reliable anxiolytic that won't sedate


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#1 doctordog

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Posted 17 June 2009 - 03:40 AM


hi, i'm looking for an anxiolytic that will help with depression/anxiety, because it's becoming increasingly apparent to me that unless i do something to get those two factors under control, i'm not really going to get anywhere; i mean what use is it wasting money on nootropics and stuff when you barely have the wherewithal to face the day. so here's to prioritizing - *toast*.

anything sedating/cognitive dulling is counter-progressive, since what i am looking for is something that will let me return to work while i treat underlying factors. i am interested in having some blood work, cortisol testing + hormonal panels done, but it's impossible to progress when every potential decision is being filtered through an inherently irrational thought process. i can't stick to anything because anxiety demands an instant solution, and will instantly shred any feeble little structures i try to put in place. it's amazing that i've managed to stay on memantine this long; part of that fact can no doubt be attributed to the fact that it's really great at turning the volume down on repetitive thoughts. but my mood really sucks, i can't get refreshing sleep, and i can't really capitalize on the (slightly) improved attention span due to a lack of emotional range. i might try going down to 15mg to see if that helps things, but in the meantime it would help if i could deal with my mood/motivation. i'm in CBT - which helps with general life-structuring - but my feelings are that it's potential is limited, since i think there is a definite chemical/endogenous basis to my problems.

currently at my disposal is one box of brand-name Wellbutrin SR; i understand that, at higher doses, it can have some dumb-drug effects, and also wind people up. but is it possible to get benefits for anxiety + dysthymia at a lower (100/150mg) dose? there is also the added consideration that memantine might potentiate its effect, though i'm a little put off by the fact that both drugs block nACHr receptors (i realise i'm not really in a position to be picky, but like i say, anything that might further dumb me down won't really help; i also seem to be a lot more dysfunctional when over-stimulated. as a little experiment, i took 300mg of N-Acetyl-Tyrosine yesterday morning, and had to suffer through the worst physical/mental tension for the rest of the day).

i am also going to place an order for some Stablon tonight, since it's profile sounds really attractive. i am also going to pick up some SAM-e to try as an adjunct. i've considered going down the herb route but it just doesn't seem all that reliable. i was reminiscing about my experience with St John's Wort, but after taking some bacopa these past couple days - which is great for stress, but leaves me a little fogged out - i recall that i had a similar reaction to SJW.

my GP is in the process of finding me a new pdoc, and also willing to support + supervise any decision i make, but until then, would Stablon or Bupropion be a better band-aid for motivation problems, coupled with mood, sleep + anxiety issues? i also realise bupropion is often contraindicted in anxiety patients, but at the moment most of mine stems from watching my life + potential slip away from me, so anything which promotes functioning could theoretically prove to be anxiolytic

#2 tlm884

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Posted 17 June 2009 - 05:13 AM

Buproprion is not an anxiolytic. It can make anxiety worse. Most SSRI's, TCA's are all sedating even thought they are "stimulating". I would look into the SSRE's and Propranolol or Tenex (if you are in the US)

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#3 FunkOdyssey

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Posted 17 June 2009 - 05:27 AM

I would consider agomelatine (improved sleep, antidepressant, non-sedating anxiolytic), afobazol (highly effective non-sedating anxiolytic), and tianeptine (antidepressant, mild anxiolytic), possibly in some combination.

Bupropion would help with motivation but may make your anxiety worse. Or it may help -- in some studies bupropion is claimed to be anxiolytic, and in some people it really is. Responses are very individual. It definitely won't help with sleep though and may make that worse.

#4 tlm884

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Posted 17 June 2009 - 05:43 AM

I would consider agomelatine (improved sleep, antidepressant, non-sedating anxiolytic), afobazol (highly effective non-sedating anxiolytic), and tianeptine (antidepressant, mild anxiolytic), possibly in some combination.

Bupropion would help with motivation but may make your anxiety worse. Or it may help -- in some studies bupropion is claimed to be anxiolytic, and in some people it really is. Responses are very individual. It definitely won't help with sleep though and may make that worse.


Where do you get afobazol? Is it approved in Canada

#5 doctordog

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Posted 17 June 2009 - 09:52 AM

I would consider agomelatine (improved sleep, antidepressant, non-sedating anxiolytic), afobazol (highly effective non-sedating anxiolytic), and tianeptine (antidepressant, mild anxiolytic), possibly in some combination.

Bupropion would help with motivation but may make your anxiety worse. Or it may help -- in some studies bupropion is claimed to be anxiolytic, and in some people it really is. Responses are very individual. It definitely won't help with sleep though and may make that worse.


thanks. is there any chance you could PM me with reliable sources for picking those up, so i can get my GP to write a script? IAS has stablon, though it's a little pricey; a cheaper alternatively would be appreciated

#6 Lufega

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Posted 17 June 2009 - 12:23 PM

Relora.

It takes the edge off but it's non-sedating. This stuff works really well. I find it calms anxiety even better than magnesium. It's also helped me burn more fat than anything else I've tried. I feel great when I'm on it.

#7 FunkOdyssey

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Posted 17 June 2009 - 04:22 PM

Where do you get afobazol? Is it approved in Canada


Its a novel Russian drug, available from online sources. They are particularly proud of it since western medicine's attempt at a non-sedating anxiolytic (buspirone) was basically a complete failure. It is not acutely effective the way benzodiazepines are to resolve a panic attack, but taken continuously, by the fourth week afobazol is actually more effective than diazepam at controlling anxiety.

#8 k10

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Posted 17 June 2009 - 08:16 PM

Where do you get afobazol? Is it approved in Canada


Its a novel Russian drug, available from online sources. They are particularly proud of it since western medicine's attempt at a non-sedating anxiolytic (buspirone) was basically a complete failure. It is not acutely effective the way benzodiazepines are to resolve a panic attack, but taken continuously, by the fourth week afobazol is actually more effective than diazepam at controlling anxiety.



Does it cause physical dependance or a withdrawal syndrome?

Edited by k10, 17 June 2009 - 08:17 PM.


#9 FunkOdyssey

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Posted 17 June 2009 - 09:08 PM

Not according to the manufacturer. I don't know anyone that has taken it long-term yet, just several people who've been on it for a week or less.

#10 NootropicEU

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Posted 17 June 2009 - 10:25 PM

Institute of Molecular genetics, Russian Academy of sciences have developed a new unique peptide based anxiolytic. It looks promising.

Automatic translation from their website:

SELANK ®
anxiolytic drug action

SELANK - this regulatory peptide, a synthetic analogue of a short fragment of the heavy chain of human immunoglobulin G (tetrapeptid taftsin), extended tripeptidom Pro-Gly-Pro nootropnogo action. SELANK developed at the Institute of Molecular Genetics, Russian Academy of Sciences jointly with the Research Institute of Pharmacology them. VV Zakusova RAMS. SELANK has sustained and nootropnym anxiolytic effect and is effective in the treatment of patients with generalized anxiety disorder. SELANK advantage over the traditional benzodiazepinovyh tranquilizers (relaniuma, alprazolama, fenazepama, etc.) The lack of habituation and side effects (retardation, drowsiness, violations of concentration, memory and coordination of movements). SELANK practically harmless, even at doses 500 times higher than therapeutic. SELANK (0.15% aqueous solution) can be successfully applied to suppress the feelings of fear, anxiety in neurotic patients, to stimulate memory and learning in healthy people, neutralize the effects of stress, as well as for the prevention of mental fatigue and astenonevroticheskih disorders of different genesis.
Has completed phase III clinical trials the drug «Selank-0, 15% solution» in three psychiatric hospitals in Moscow, which take place at this time. Preliminary results of clinical studies confirm the findings of phase II clinical studies. There are currently prepared and submitted for approval by all regulatory documentation for the release of a new drug. A manufacturing base for production of the drug.

Drug «Selank-0, 15% solution» is unique and has no analogues abroad.

Patents:

1. Anxiolytic pharmaceutical composition tool and anxiolytic action.
Patent number 2155065, issued on 27 August 2000.
2. The method of prevention and correction of immunodeficient states.
Patent, a positive decision of 27 June 2007.

Awards:

Gold medal and a diploma at the international salon of innovations. Geneva, April 20, 2007 for peptide drug Selank - anksiolitik with nootropnym effect.

Edited by anony4mous, 17 June 2009 - 10:25 PM.


#11 NootropicEU

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Posted 17 June 2009 - 10:30 PM

Intranasal administration of the peptide Selank regulates BDNF expression in the rat hippocampus in vivo.

[Effects of heptapeptide selank on genetically-based and situation-provoked symptoms of depression in behavior in WAG/Rij and Wistar rats, and in BALB/c mice]

[Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia]

Edited by anony4mous, 17 June 2009 - 10:36 PM.


#12 okok

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Posted 19 June 2009 - 04:30 PM

before taking medications with side effects, why not consider st. johns wort? Hypericum taken in the long term is very effective with anxiety/sleep. Get the tea, no hypericum pills, no tea bags, ~2 tbl spoons/infusion, not before bedtime.

#13 FunkOdyssey

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Posted 19 June 2009 - 05:26 PM

before taking medications with side effects, why not consider st. johns wort? Hypericum taken in the long term is very effective with anxiety/sleep. Get the tea, no hypericum pills, no tea bags, ~2 tbl spoons/infusion, not before bedtime.


The side effect profile of agomelatine is better than st. john's wort and it is also much safer to combine with other substances. St John's wort has a list of drug interactions longer than my arm. Tianeptine is also safer, but does have some side effects that are probably comparable to St John's wort incidence and severity-wise. Afobazol is a bit of an unknown unless you can read Russian.

#14 doctordog

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Posted 19 June 2009 - 11:19 PM

I'm beginning to think that sleep quality may be one of the governing issues here. I try to stick to a pretty strict 8 hours, but still never feel refreshed; what's more, while on Memantine, I feel like my mind is constantly switched 'on'. That sensation, combined with sleep deprivation, has left me feeling pretty loopy- physically, I'm completely calm, but my mind is constantly going around and around in circles, and I have pretty much zero working memory. Diazepam didn't do anything to mitigate sleep quality - in fact, it felt like the Memantine blocked its effect entirely -, though for a couple of days I had a lot of success using Bacopa, which makes me think that the Memantine dose might be too high (cf. its action as a serotonin antagonist). For the next week I've decided to try restricting exercise and caffeine intake during the evenings (I usually exercise after work), as well as lower the Memantine dose to 15mg or possibly 10mg. There have been some days when the Memantine worked and I felt completely normal, so it definitely seems worth pursuing; my doctor thought it might be a placebo effect, but I doubt it. I just wished I had kept a more thorough journal, so I could see what conditions it was helping under. I've booked myself in for a sleep study next week, since from memory, sleep quality has been an issue for a while. I couldn't afford to have one in which I'm monitored in-house (~$1000), but I found a guy who uses a take-home machine, and charges ~$200. I'm just wondering how effective (if at all) the latter method is.

#15 niner

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Posted 20 June 2009 - 03:30 AM

For the next week I've decided to try restricting exercise and caffeine intake during the evenings (I usually exercise after work), as well as lower the Memantine dose to 15mg or possibly 10mg.

Considering the half life of caffeine, you might want to try cutting it out entirely for a while as an experiment. I mean really cutting it (and its various friends and congeners) out, meaning not only coffee but tea, colas, chocolate, and certain extracts. If you are a fast metabolizer of caffeine, this may or may not help. I'm a slow metabolizer, so if I have a lot of coffee, even in the morning, I may end up taking a couple mg of Ambien if I want to get to sleep at a decent hour.

#16 doctordog

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Posted 20 June 2009 - 05:15 AM

Considering the half life of caffeine, you might want to try cutting it out entirely for a while as an experiment. I mean really cutting it (and its various friends and congeners) out, meaning not only coffee but tea, colas, chocolate, and certain extracts. If you are a fast metabolizer of caffeine, this may or may not help. I'm a slow metabolizer, so if I have a lot of coffee, even in the morning, I may end up taking a couple mg of Ambien if I want to get to sleep at a decent hour.


I was referring more to caffeine-lite stuff like green tea, which I'll drink, for example, during dinner at a Japanese restaurant. I never touch coffee, sodas, etc. though I do eat a lot of dark chocolate ... hmm ...

#17 Lufega

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Posted 20 June 2009 - 01:41 PM

Effect of a proprietary Magnolia and Phellodendron extract on stress levels in healthy women: a pilot, double-blind, placebo-controlled clinical trial.
Kalman DS, Feldman S, Feldman R, Schwartz HI, Krieger DR, Garrison R.

Director, Nutrition, Miami Research Associates, Miami, FL, USA. dkalman@miamiresearch.com

BACKGROUND: Recent research has established correlations between stress, anxiety, insomnia and excess body weight and these correlations have significant implications for health. This study measured the effects of a proprietary blend of extracts of Magnolia officinalis and Phellodendron amurense (Relora) on anxiety, stress and sleep in healthy premenopausal women. METHODS: This randomized, parallel, placebo controlled clinical study was conducted with healthy, overweight (BMI 25 to 34.9), premenopausal female adults, between the ages of 20 and 50 years, who typically eat more in response to stressful situations and scores above the national mean for women on self-reporting anxiety. The intervention was Relora (250 mg capsules) or identical placebo 3 times daily for 6 weeks. Anxiety as measured by the Spielberger STATE-TRAIT questionnaires, salivary amylase and cortisol levels, Likert Scales/Visual Analog Scores for sleep quality and latency, appetite, and clinical markers of safety. The study was conducted by Miami Research Associates, a clinical research organization in Miami, FL. RESULTS: The intent-to-treat population consisted of 40 subjects with 26 participants completing the study. There were no significant adverse events. Relora was effective, in comparison to placebo, in reducing temporary, transitory anxiety as measured by the Spielberger STATE anxiety questionnaire. It was not effective in reducing long-standing feelings of anxiety or depression as measured using the Spielberger TRAIT questionnaire. Other assessments conducted in this study including salivary cortisol and amylase levels, appetite, body morphology and sleep quality/latency were not significantly changed by Relora in comparison to placebo. CONCLUSION: This pilot study indicates that Relora may offer some relief for premenopausal women experiencing mild transitory anxiety. There were no safety concerns or significant adverse events observed in this study.


Anxiolytic properties of botanical extracts in the chick social separation-stress procedure.
Sufka KJ, Roach JT, Chambliss WG Jr, Broom SL, Feltenstein MW, Wyandt CM, Zeng L.

Department of Psychology, University of Mississippi, Oxford 38677, USA. pysufka@olemiss.edu

RATIONALE: The recent growth in sales of natural products labeled as dietary supplements in the United States has renewed scientific interest in the study of the therapeutic effects of multi-component botanical products. OBJECTIVES: This study sought to determine whether botanical extracts derived from the Rutaceae family, Acori graminei, the Magnoliaceae family, Alchemilla vulgaris and Primula veris, which had previously been identified in bioassays as having potential anxiolytic activity, were active in the chick social separation-stress procedure. METHODS: Eight-day-old chicks received IP injections of test articles 30 min before being tested in the presence of two social companions or in isolation for a 3-min observation period. Dependent measures were: a) latency to adopt a ventral recumbent posture to index sedation, b) number of vocalizations to index separation-distress and c) a composite pain score (comprised of footlift frequency and footlift duration in response to 50 microl of 0.10% formalin injected into the plantar surface of the foot) to index stress-induced analgesia. RESULTS: Proprietal extracts NPS00033 from the Rutaceae plant family and NPS00039 (Relora) from the Magnoliaceae plant family screened positive in this chick model without causing sedation. CONCLUSIONS: These results suggest that botanical extracts Relora and NPS00033 may be useful in modulating anxiety states.



#18 jackinbox

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Posted 20 June 2009 - 02:52 PM

before taking medications with side effects, why not consider st. johns wort? Hypericum taken in the long term is very effective with anxiety/sleep. Get the tea, no hypericum pills, no tea bags, ~2 tbl spoons/infusion, not before bedtime.


The side effect profile of agomelatine is better than st. john's wort and it is also much safer to combine with other substances. St John's wort has a list of drug interactions longer than my arm. Tianeptine is also safer, but does have some side effects that are probably comparable to St John's wort incidence and severity-wise. Afobazol is a bit of an unknown unless you can read Russian.


As far as I know Agomelanine is not available yet. Do you know any source for it?

#19 jackinbox

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Posted 20 June 2009 - 02:55 PM

Tianeptine (stablon) is nice for anxiety but I have constipation issue when taking it. It definitely make my IBS worse.

#20 k10

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Posted 21 June 2009 - 05:48 AM

So since stablon is a serotonin reuptake enhancer, does that essentially mean that it is LOWERING serotonin in the brain? This drug confuses me.

#21 Chaos Theory

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Posted 22 June 2009 - 06:18 PM

I have had some anxiety issues for a long time myself. Bupropion(Wellbutrin) actually has a calming effect on me at doses of 150-300mg/day. It did cause some anxiety in the first week or two taking it, but after I adapted to it I actually felt more calm on it.

#22 doctordog

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Posted 22 June 2009 - 11:29 PM

I have had some anxiety issues for a long time myself. Bupropion(Wellbutrin) actually has a calming effect on me at doses of 150-300mg/day. It did cause some anxiety in the first week or two taking it, but after I adapted to it I actually felt more calm on it.


do you still find it effective as a psychostimulant (for mood, motivation, socialization) despite its calming effect? were i to try it, my plan was to not really exceed the doses you mention anyway

#23 jackinbox

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Posted 23 June 2009 - 12:06 AM

So since stablon is a serotonin reuptake enhancer, does that essentially mean that it is LOWERING serotonin in the brain? This drug confuses me.


Yes but like pretty much every drugs, the mechanism aren't fully understood.

#24 wiserd

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Posted 23 June 2009 - 05:48 AM

Theanine is a mild anxiolytic extract of tea. My ex, who has fibromyalgia, used it to get to sleep but it's good during the day too. It doesn't seem to be addictive at all, unlike most GABAergics (except possibly the kavalactones), though you do build a tolerance to it and have to cycle off it for a while.

#25 FunkOdyssey

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Posted 23 June 2009 - 03:36 PM

before taking medications with side effects, why not consider st. johns wort? Hypericum taken in the long term is very effective with anxiety/sleep. Get the tea, no hypericum pills, no tea bags, ~2 tbl spoons/infusion, not before bedtime.


The side effect profile of agomelatine is better than st. john's wort and it is also much safer to combine with other substances. St John's wort has a list of drug interactions longer than my arm. Tianeptine is also safer, but does have some side effects that are probably comparable to St John's wort incidence and severity-wise. Afobazol is a bit of an unknown unless you can read Russian.


As far as I know Agomelanine is not available yet. Do you know any source for it?


Search Google Groups for "agomelatine psychonauts".

#26 bgwithadd

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Posted 23 June 2009 - 05:48 PM

Memantine is great for anxiety and depression and won't sedate. Guanfacine will physically sedate you some, but mentally makes you more clear. Fantastic for anxiety. For supplements theanine and high dose inositol work well for anxiety.

#27 doctordog

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Posted 23 June 2009 - 10:21 PM

Memantine is great for anxiety and depression and won't sedate. Guanfacine will physically sedate you some, but mentally makes you more clear. Fantastic for anxiety. For supplements theanine and high dose inositol work well for anxiety.


I use inositol at night for sleep; during the day, it just leaves me spacey. I'm also taking Memantine at the moment, which helps with anxiety, but is either making my concentration worse or not helping it at all. i'm playing around with the dose to see if a lower one might help.

#28 jackinbox

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Posted 24 June 2009 - 12:41 AM

Memantine is great for anxiety and depression and won't sedate. Guanfacine will physically sedate you some, but mentally makes you more clear. Fantastic for anxiety. For supplements theanine and high dose inositol work well for anxiety.


I would really like to get guanfacine but it's not available in Canada and every online pharma ask for a prescription. :(

#29 k10

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Posted 24 June 2009 - 02:12 AM

So since stablon is a serotonin reuptake enhancer, does that essentially mean that it is LOWERING serotonin in the brain? This drug confuses me.


Yes but like pretty much every drugs, the mechanism aren't fully understood.


Does anyone know if Stablon could induce serotonin syndrome by some weird mechanism when combined with other antidepressants? Or is there basically no chance of that with Stablon?

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#30 dachshund

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Posted 24 June 2009 - 02:33 AM

Sedating anxiolytic drugs is a pain point in the industry. Researchers are working on this problem with new chemistries.

http://www.physorg.c...s164988676.html




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