39 replies to this topic

[Ben]

I gave deprenyl a trial recently and the results were interesting. After about 1 pm I would start feeling very, very sleepy and when going to bed, after having taken it in the morning, I would almost invariably wake up during the night with a ringing in my ears and a with what appeared to be a fast heart rate. I was very cold at night, so that's perhaps why I would wake up.

So who here has experienced something similar to this? I took 1 drop a day of selegiline citrate which is, I think, equivalent to 1 mg.

Edited by Ben - Aus, 16 December 2008 - 01:41 PM.

[yoyo]

Mostly, it makes me horny.

[Lufega]

I am up to two drops a day and the effects are minimal. 1 drop is suggested for "healthy individuals" but I am far from that so I'll experiment with 3 -5 drops a days. The first day I used 5 drops and I felt better than I had in years!

[Wedrifid]

Mostly, it makes me horny.

Horny and organised.

[synaesthetic]

Cyprenil seems to make me sleepier than Selepryl.

[Shepard]

Most people that play around with substances that increase dopamine tend to report sleepinees during the beginning of the run.

[yoyo]

Most people that play around with substances that increase dopamine tend to report sleepinees during the beginning of the run.

it depends on how it increases DA...direct DA agonists mostly are sleep-inducing

[Advanc3d]

Yeb, makes me sleepy and cranky....
i no longer take it anymore unless im taking illicit stimulants

[Shepard]

it depends on how it increases DA...direct DA agonists mostly are sleep-inducing

From anecdotal reports, it does seem that the more powerful agonists produce the worst effects (almost narcoleptic in some cases). But there have also been multiple reports of deprenyl inducing daytime sleepiness in some.

[zoolander]

I've never had a problem with sleepiness. Unfortunately we'll have to recognise that we have responders and we have non-responders. I seem to respond to just about everything I take *smiles* I know by trailing friends and friends of friends on galantamine that there are people that respond in such a way that it really things dramatically for them. I absolutely love helping the responders. On the other hand there are the non-responders who, when asked how they're doing will just respond "what?"...."nothing"...."nada". I have heard of people getting sleepy on seleginine, not me though

[Ben]

it depends on how it increases DA...direct DA agonists mostly are sleep-inducing

From anecdotal reports, it does seem that the more powerful agonists produce the worst effects (almost narcoleptic in some cases). But there have also been multiple reports of deprenyl inducing daytime sleepiness in some.

Could it be because for some people deprenyl is unnecessary and causes an excessive amount of dopamine at the receptors?

[Advanc3d]

it depends on how it increases DA...direct DA agonists mostly are sleep-inducing

From anecdotal reports, it does seem that the more powerful agonists produce the worst effects (almost narcoleptic in some cases). But there have also been multiple reports of deprenyl inducing daytime sleepiness in some.

Could it be because for some people deprenyl is unnecessary and causes an excessive amount of dopamine at the receptors?

It doesnt make sence, doesnt Dopamine also get metabolised in to Norepinephrine?
i would assume it would cause a large increase in NE as well

but it does make me pretty sleepy and if i take it daily for more than 3 weeks i start to get headaches

also my blood pressure is lowered a fair bit which is probably why the headaches occur.. and my sex drive is also lowered after a while of daily use..

im assuming that Deprenyl somehow has an effect on Histamine and/or Adrengic antagonism

[Mixter]

Horny and organised.

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Deprenyl -> Profit!



Deprenyl at 2,5 mg makes me slightly irritable but increases motivation. I'm not going beyond the dose
before age 40 Something that screws with your mood/personality is best used with caution. The dopamine
effects gave me very vivid dreams once or twice, but I don't wake up... Dopamine effects are not that good,
would actually be nice if we could have the mitochondrial protection and anti-aging without dopamine/MAO-B effects.

[bgwithadd]

If you are getting sleepy and irritable or feeling zombie-ish or cold you're taking too much. All there is to it. Deprenyl can sort of be considered amphetamine lite that lasts 24x7, due to the mao-b effects, and it's not something healthy people need a lot of (if any). Coldness and tinnitus are due to vasoconstriction. Unless you want to see the fun effects of bad skin and erectile dysfunction 6 months down the road then I'd recommend you lower your dose.

[bgwithadd]

im assuming that Deprenyl somehow has an effect on Histamine and/or Adrengic antagonism

Yeah, it increases PEA, which will increase histamine.

[luv2increase]

Coldness and tinnitus are due to vasoconstriction. Unless you want to see the fun effects of bad skin and erectile dysfunction 6 months down the road then I'd recommend you lower your dose.

Hogwash?



lol



Nuff said...

[Johann]

I gave deprenyl a trial recently and the results were interesting. After about 1 pm I would start feeling very, very sleepy and when going to bed, after having taken it in the morning, I would almost invariably wake up during the night with a ringing in my ears and a with what appeared to be a fast heart rate. I was very cold at night, so that's perhaps why I would wake up.

So who here has experienced something similar to this? I took 1 drop a day of selegiline citrate which is, I think, equivalent to 1 mg.

I've had pretty much the same experience. I'm almost certain I will stop taking it. I didn't know that the coldness was related to deprenyl but I have noticed that feeling definitely.

[Pike]

i wouldn't be surprised deprenyl would make you sleepy at first. it IS an MAOI after all. your body would probably respond to it the same way it would to a dopamine agonist at first and register a LACK of dopamine: hence why it makes you so tired. the super libido that some people report is your brain seeking a dopamine rewarding type of activity --> orgasm does release dopamine.

people have got to become a little more patient with some of these nootropics. most of the pharmaceutical nootropics i've seen take at least 6 weeks to reach clinically significant benefit. from personal experience, i know for damned sure that selegiline, memantine, and bupropion are no exception to this rule. i would EXPECT deprenyl to have the kinds of effects that people are complaining about at first. if they still have those side effects, say, 3 months after use... THEN i would worry.

unless the compound you're taking specifically triggers enhanced dopamine/catecholamine RELEASE (and to some extent, reuptake inhibition), then i really doubt you'd experience any sort of specific stimulant action. off the top of my head (meaning i can't remember where i read it, but it could have been either this forum or the ADHD forum), the stimulant effect of things like amphetamines/DNRIs are registered through the RATE at which their turning out dopamine/cats, not simply the AMOUNT of dopamine/cats. apparently, this is why compounds that inhibit CYP 2D6 (the only p450 enzyme that seems to have an effect on amphetamine metabolization aside from MAO) may extend the duration that amphetamines are felt, but they cut down on the euphoric effects that normal people feel from them.



if my subjective experience is relevant to anyone, after 2 months of deprenyl, it feels a lot like being on 10mg of adderall, but all day long. i kind of prefer it to my prescription amps because it doesn't give me the stimulant blues that amps do. (note: if you DON'T have ADHD, then don't worry about what the stimulant-blues are. it probably doesn't apply to you.)

[Johann]

Pike,
I'm been on just 1mg a day for not even a combined total of a week (3 days on, took 2 days off, then on again).
Do you think that the irritability will cease? The chills will go away?
And what is your view on Wellbutrin? I love the stuff but I believe it is not nicotinic receptor friendly? How about selegiline? It seems that the last few days that I've been on it, the recall
isn't there.

[Pike]

Pike,
I'm been on just 1mg a day for not even a combined total of a week (3 days on, took 2 days off, then on again).
Do you think that the irritability will cease? The chills will go away?
And what is your view on Wellbutrin? I love the stuff but I believe it is not nicotinic receptor friendly? How about selegiline? It seems that the last few days that I've been on it, the recall
isn't there.

heh, buddy, when i started selegiline... if i wasn't sleeping or about to eat my way though my 5/6th meal of the day... "unpleasant" would've be the word to describe me. so, yes, the irritability definitely went away. that's one of the first things that went away (probably around 2nd or 3rd week). drowsiness went away after a month or so. i've always had problems with cold hands/feet, so i wouldn't be able to tell you about the chills.

about Wellbutrin: Wellbutrin was probably one of the best things i ever tried for my ADHD. everyone who takes wellbutrin reports the initial "honeymoon" effect, in that they get a taste of what its full effect will be like 3 months or so down the line. after about 2 weeks of continuous use, the wellbutrin honeymoon seems to go away, but is supposed to return after like 3 months or so (personally, i never got to 3 months). I think it would be a great monotherapy for MILD adhd, but perhaps not for more severe cases. i decided to stop taking it after i discovered that it was a giant CYP 2D6 inhibitor, which is definitely an interaction that i should be worried about until i cease my prescription amphetamine use (but this is probably not an issue for people who aren't on prescrip amphetamines, specifically). as for the nicotinic receptor action: i never noticed much with it. then again, i never reached a full 3 months of continuous use, which is when it's supposed to be at max efficacy.

that first week of selegiline is always the hardest. but if you really want selegiline's full benefit, you've got to stick with it and use it consistently. it takes some determination, but if you can get past that 6 week mark, i bet you'll be home free of any side effects.

hope my input helps!

[Johann]

I believe what you're saying about Dep becoming a workable thing several weeks from
now. I've seen many on here take one thing and if they didn't have miraculous results the
very first day, they simply wrote it off for good (racetams in particular).

I do appreciate the extra little bit of motivation that deprenyl gives me. However, I just don't know if I have the inner strength to deal w/ several weeks of what to me is a very unsettling
accommodation period. Even my tinnitus was made louder. Hoping it subsides soon.

If I don't resume the dep, I'll be looking to sell 58 tabs (5mg each) of Deprenyl, LOL. I'll part w/ 'em cheap.

[Pike]

I believe what you're saying about Dep becoming a workable thing several weeks from
now. I've seen many on here take one thing and if they didn't have miraculous results the
very first day, they simply wrote it off for good (racetams in particular).

I do appreciate the extra little bit of motivation that deprenyl gives me. However, I just don't know if I have the inner strength to deal w/ several weeks of what to me is a very unsettling
accommodation period. Even my tinnitus was made louder. Hoping it subsides soon.

If I don't resume the dep, I'll be looking to sell 58 tabs (5mg each) of Deprenyl, LOL. I'll part w/ 'em cheap.

IMHO as a pharmaceutical, i believe the only other thing that would come close to selegiline's impact on life extensionism would be hydergine. in terms of all of the nootropics (non pharmaceuticals included) we know about, selegiline's impact on the life-extension movement might only be rivaled by Centrophenoxine or perhaps the 'Racetams. sure the breaking-in stage is unpleasant, but nothing worth doing was meant to be easy. those first few days you take Sele are probably the days where you'll feel the full 100% side effects. after my first week of consistent (same time every day) dosing, i'd say the side effects dropped to like (if i had to put it quantitatively) 50%. by the end of the second week they were probably around 30%. from then onward until 6 weeks, it was just easier and easier.

if the drowsiness is a little too much to bear and you feel like you just might fall asleep, grab a piece of gum. Human body won't allow itself to fall asleep as long as you're chewing something!

remember: that first week or so of Selegiline is always the hardest. but if you can keep consistent and administer your selegiline at roughly the same time each day, you'll be able to enjoy the the most famous nootropic in all life extension!

[Johann]

I'll probably give it another go after this semester ends in December. I'll be off for several weeks and that way can sleep or whatever.
Do you know much about Dep raising serotonin levels? And if so,
doesn't serotonin sort of work to make one dopey? I ask this because I was having killer results from Aniracetam and Galantamine and it seemed to get blunted while on Deprenyl. Something that will go away in time?

[Pike]

I'll probably give it another go after this semester ends in December. I'll be off for several weeks and that way can sleep or whatever.
Do you know much about Dep raising serotonin levels? And if so,
doesn't serotonin sort of work to make one dopey? I ask this because I was having killer results from Aniracetam and Galantamine and it seemed to get blunted while on Deprenyl. Something that will go away in time?

i mean, unless the amphetamine metabolites in selegiline (which are minimal at that, and in the L-isomer, which aren't anywhere near as potent as the D-isomers) can elicit significant serotonin release, i don't think so. last i checked serotonin was metabolized by MAO-A, and selegiline selectively inhibits MAO-B up to 10mg p/day. so, unless you're taking more than 10mg of dep, no, i don't think it would tinker with your serotonin levels at all.

one reason it could be tinkering with your aniracetam benfits is because, IIRC, desmethylselegiline (the main metabolite) was supposed to be an NMDA receptor antagonist. in theory, an NMDA receptor antagonist would probably put a giant STOP sign in front of aniracetam's ampakine activity and make all of that AMPA receptor modulation useless since your NMDA receptors can't open up and trigger LTP. again, that's just how i think it would blunt the effects.

the racetams are all purported to have ampakine activity, according to one patent i read, and so that's why i never really combine them with a dopaminergic compound that has NMDA receptor activity.

[Johann]

alright.. that is beginning to make sense..
I just posted on Naltrexone's hypothetical effects on NDMA receptors.. wasn't for sure which
one was messing w/ my nootropical zenith.

[Pike]

hmm.... from what it seems, all of the neuroprotective/life-enhancing effects of selegiline can be mainly attributed to its desmethylselegiline metabolite, while MAO-B and CAE activity can mostly be attributed to the parent compound (but DMS also has mao-b inhibition properties).

For anyone interested, this is the patent claiming that ALL racetams, not just ani, have ampakine activity.

uh oh, looks like selegiline could be a real contender for NMDA receptor antagonism because here, it seems to blunt NMDA damage WITHOUT interfering with the AMPA-NMDA long-term-potentiation cycle!

which means that maybe your reversal of benefits from ani+galantamine could be attributed to something else! then again, it could simply be that you don't FEEL like you're firing your pistons with the increased acetylcholine levels because you have the enhanced dopamine from selegiline to balance out that ACh-DA "seesaw"

Edited by Pike, 16 November 2009 - 11:30 PM.

[Johann]

Interesting about all the 'tams having AMPA effects.. can you summarise how that works?

Also, about the Selegiline, what I will do is offer myself as an experiment. I will take nothing but the Low Dose Naltrexone for a couple of weeks and see how that goes and not the Deprenyl. Another hypothesis is that since in the
early going w/ LDN, the sleep is drastically affected -- the REM in particular. This has to do with opiod regulation and whatnot. That is possibly what could have been affecting me.

Also, I'm thinking of getting some Piracetam, 3 KG from SP. Great price and if it affects AMPA as well.. I will be happy.

[Pike]

the ampakine activity, in terms of what you get from 'racetams, is kinda like having someone at the front of your AMPA receptor to "hold the door open," so to speak, for your glutamate. that way, when glutamate comes around, it gets a nice helping hand to in binding to the receptor. thus, your AMPA receptors fire off a lot easier, making more of their little AMPA receptor buddies. from that, the collective boost in AMPA receptors will make it a lot easier to both "disarm" your NMDA receptors and will make LTP formation a lot easier.


but you gotta be careful when mixing your dopaminergics with things that act on the AMPA/NMDA receptors because dopamine receptor stimulation can elicit calcium release, and calcium influx is the basis of glutamate mediated neurotoxicity. but, i guess in the case of selegiline, it might be safer given it's NMDA protective features. still, though, it's best to play it safe.

also, 3kg of piracetam is a lot! i was able to make 600+ capsules all in the ballpark of 800mg from just the half-kilogram size. don't get me wrong, the 3kg deal is a great deal, but stick to the half-kilo unless you plan on using piracetam in megadoses (which i still don't think is all that warranted even though some people tinker in dosages of 10g+).

[protoject]

With chronic dosing of selegiline, what are the resulting levels of the parent substance and metabolites, especially in regards to the MAO-B inhibiting compounds, and how does this bear on MAO-A inhibition?

What I'm getting at is... that selegiline's elimination half-life during chronic dosing is 9 hrs... and we know that with a longer half life the doses may be building up in the system over time. So if we take 10mg a day, after a meal, I assume that:

- we'd be getting 2mg of that 10mg because selegiline is 20% bioavailible that way
- the 2mg, which we took at 12:00 noon, with chronic dosing would be half gone from being active in the system after 9 hrs [9 PM], 1 mg would remain
- for the next 9 hours that 1mg would break down into 0.5 mg. so at 6am, 0.5 mg is still active in the system.
- come your next dose at 12 noon , that 0.5mg has broken down into 0.08mg, which is added on to your next dose.

So is there eventually a time when the concentration in the blood/ wherever has completely fulfilled MAO-B inhibiting capacity , and starts leaking over into MAO-A inhibiting?
Does it even work like that? I mean, does the selegiline inhibit all the MAO-B and that's when it starts inhibiting MAO-A, or does it simply lose selectivity for mao-b for some other reason that I'm not aware of? How does it work?

Also, isn't it true that in the body, selegiline's half life depends on some factors other than MAO-B [i.e. P450 enzymes] , and that when it comes to it's half life under the context of being an MAO-B substrate that the half life is more specific in that case?

[Steve_86]

Pike:
What dose of Deprenyl do you take/recommend for ADHD?

Does anyone know the dosing at which deprenyl would become harmful to ones health or lifespan?