T Nation

Selegeline Questions

I just got my selegiline here! Im trying to check and see what supps you can and cant take with it. I`m cutting right now and use the following everyday:

caffine (2-500mg daily)
dmae (500mg usually once a day)
vinpocetine (only on training days, one 10mg cap
ephedrine (only on training days, 24mg)
clen (Im up to 50ish mcg daily now) yohimbe (only 2.5 mg twice a day, sometimes less) geranium caps (25mg twice a day max, usually once) dhea transdermal (30 mg twice a day) fish oil caps (6-8 per day) multi-vitamin vitamin D (extra 4000ius)

Those are most of my day time supps. At night I take all of or a combination of these:

valerian root (usually only on weekends)
st john`s wort
5htp
gaba

Is there anything you see here that shouldnt be used with selegiline? I plan on using 2.5 mg daily or eod. For sure l-tyrosine has to be taken out as its a dopamine agonist, so I didn`t even list it… Do you take it empty or full stomach, is it liposoluble?

Anyone used aniracetam, oxiracetam or sulbutiamine with selegiline also? For now these are the supps I use the least but may change soon.

Heavy question for sure, but would really appreciate some feedback as I know some guys here have some experience with selegiline.

Thanks!

Not sure this answers you but I do know cabergoline [a dopamine agonist] can be taken with selegiline. Mention this only because you were ruling out l-tyrosine for this reason but caber and selegiline have different pathways. 2.5mg ED/EOD seems like a good mild starter dose 5mg EOD is what I consider default. So unless you wanna split the pills and take them daily 5mg EOD is fine

I just found this on yohimbe:

Yohimbe combined with deprenyl

Version 1.0, October 2009

I have also tried deprenyl (selegeline, Jumex) with yohimbe. Deprenyl is a MAO inhibitor, and I had read that MAO inhibitors don’t go well with yohimbe, so I was careful with the dosages. I had previously tried deprenyl alone, and found it to have an amphetamine-like effect at dosages of more than 2.5 milligrams (half a standard Jumex tablet). I don’t feel the amphetamine-like effect anymore with up to 5 milligrams. But for me, deprenyl also detracts from the yohimbe when combined with it.

I have always found deprenyl’s pro-sexual effects overrated. It’s a dopaminergic substance, and dopamine is, to a certain extent, responsible for sexual desire. But dopamine overstimulation strongly interferes with erectile function and leads to a (reversible) shrinkage of the male organ. That’s why cocaine, and amphetamines may make you horny, but also make erections and orgasms more difficult to achieve.

Deprenyl is not as bad as amphetamine and methamphetamine in making erections more difficult. It may even be that a 25-year-old would not feel any erectile impediment. But for a man of about 50, the anti-erection effect is probably stronger than the pro-libido effect,unless there is a clear dopamine deficit (as with Parkinson’s patients).

One can counterbalance the anti-erection effect of deprenyl with Viagra. In fact, I have been told that drug users now regularly mix cocaine with Viagra to avoid shrinkage.

But why combine yohimbe and deprenyl when this is no better than yohimbe alone (and definitely worse than the combination of yohimbe with Viagra)?

As deprenyl is an MAO inhibitor, it may possibly aggravate the negative side effects of yohimbe. Yohimbine is an alpha-2-receptor blocker; it frees systemic adrenaline and noradrenaline. Adrenaline and noradrenaline (epinephrine and norepinephrine) function as hormones and as neurotransmitters. The adrenaline and noradrenaline displaced by the yohimbe from alpha-2-receptors lead to mental agitation as well as increased heart rate.

This effect is countered by the enzyme monoamine oxidase (MAO), which breaks down adrenaline and noradrenaline, leading to relaxation after states of agitation. MAO inhibitors interfere with monoamine oxidase’s capability to deaminate and destroy adrenaline and noradrenaline. In combination with yohimbe, this means that the agitated state lasts until the yohimbine has cleared from the alpha-2-receptors. With unimpaired monoamine oxidase, the agitation caused by the displacement of adrenaline from alpha-2-receptors should be countered by the breakdown of free adrenaline and noradrenaline.

Combining deprenyl with yohimbe will likely prolong the negative side effects of yohimbe, such as heart palpitation, nervousness, and sleeplessness, while doing little or nothing to enhance the pro-sexual effects.

What we would really like with yohimbe is increased MAO activity, not diminished MAO activity, so we could go to sleep after having enjoyed yohimbe’s pro-sexual effects. Therefore, we don’t want deprenyl, but some sort of ‘anti-deprenyl’


Having thought about this a little. Most of the people who advocate against yohimbe are taking gonzo amounts. Up to 20 grams. I`m starting to think my doses of 2.5 or even if I bump it up to 5mg could be fine…

Bushy and a few guys did a study on this.

^^^ Yes, I hope they can chime in with their experience. So far Im conducting my own... Today at 3:30 before heading out for groceries I took 2.5 mg. The only supp in my vast list other than the vitamins I take is 200mg of caffeine and just about 45 minutes ago 20mcg of clen. I figured since Ive been on clen now for about 4 weeks its in my system and if the 2.5 mg I took didnt do anything bad, I should be ok to take more. To my surprise I haven`t felt the need to take more caffeine yet, or l-tyrosine.

Unless strongly advised not to, Im gonna slowly add the other stims I take one at a time. Oh yeah Ive been taking NO shotgun the last while, not sure what I`m gonna do with that one yet, lol…

I have been on the web though googling interactions between all the supps I use to get as much info as possible.

From what I can gather the whole avoid tyramine foods is debunked. Yohimbe in the doses I take should be ok. Id like to add geranium caps again as that stuff is great to cut appetite, because Im dieting now.

I hope your diet is as detailed as your supps list

[quote]saps wrote:
I hope your diet is as detailed as your supps list[/quote]

Ha, trust me, it`s to the point… Been at this for over 20 years!

Well Im finally Im starting to feel calm. Was a little overstimulated today. The 2.5mg dose I took at 3:30 was kicking in around 5pm. From 5pm to 9:30 I was feeling energetic and in a very positive mood. I didnt take any caffeine other than the one 200mg dose I took Tomorrow, Ill take 100mg instead of 200mg. At one point today, I was feeling overstimulated, but my heart rate was rather normal. To be honest I was a little worried and was just happy I decided not to take any other stims with it. I think 1.25mg may be better to use next time.

Out of curiosity what kinda gear you running as well as AI’s or what not?

No gear, just some T-911, lol. Gonna start topical formestane when that`s done.

why are you taking half those useless supplements? Such as GABA, st john’s wort, 5-htp, dhea etc… Waste of money and ingestion processes

As a MaoB inhibitor, selegiline prevents the breakdown of dopamine and certain phenylethylamines (in small quantities).

MaoA is the protein which breaks down norepinephrine.

It is norepinephrine which causes erection issues, because norepinephrine is a vasoconstrictor. This is the problem with amphetamines - dopamine = desire, norepinephrine = vasoconstriction.

Selegeiline will not cause vasoconstriction. Nor will it interfere with Yohimbine (which causes vasodilation due to its action on the alpha-2 adrenergic receptor).

Out of all those, i don’t see an issue with any. Just don’t take L-Dopa…

Actually DO take L-Dopa, this will accentuate teh effects of selegilne which will be fun!!!

Hey WyldFlower, thanks for your post! Gaba, st john`s wart and 5htp have done wonders for my sleep and overall putting me in a positive attitude. DHEA I understand the question of if being valid. But I do use a gh supp in spary called ghenerate and I heard on a radio show with Carl Lanore that dhea increases the benefits of peptides.

It`s relieving to hear what you said about taking all the above supps and everything being ok, but have you tried selegiline with any of the listed supps?

Again, feedback much appreciated here!

Well Ive used 10mg of vinpoceine, 200 mg of caffeine and 8mg of ephedrine with 1.25mg of selegiline after breakfast yesterday. Before heading out to the gym I took a low dose of clen ( a little over 20mcg ) then 1.5 grams of l-tyrosine and 200mg of dmae about 1 hour before the gym. for sure Im being cautious by adding stims and other noops at lower than usual doses… For sure my trainings just dont seem as good as they were before due to the synergy, and lack of no shotgun but 1.25mg of selegiline is probably not enough for me. This is based on 1 day however... From what Im reading it`s relatively safe to combine other drugs like ephedrine with selegiline as long as the dose is under 5mg per day.

Come to think about it the "dont take this with selegiline list" is very similar to what is listed on a bottle of cold medicine. Yet Ive taken those meds with all the othe stuff youre not supposed to use, and never had any problems. Still, since this is "prescription" I think extra caution is needed. Im gonna throw a geranium cap in the mix toning, but no ephedrine because I`m not training.

Oh yeah, last night at work, I sipped on 1 gram of l-tyrosine, 200mg of dmase and 500mg of aniracetam. Nothing bad to report here.

Here`s some good info I found today:

The dangerous world of combining selegiline with substances in pursuit of synergy:

L-deprenyl, aka selegiline is an irreversible enzyme inhibitor that is selective for monoamine oxidase B at low doses, also inhibiting MAOA at higher doses.

In addition to exerting positive effects on mood, cognition, and motivation, selegiline is neuroprotective. It turns out that MAO, in oxidizing dopamine-like substances, creates various free-radicals, many being peroxide species. These free-radicals, along with others, lead to oxidative stress that can damage cellular mitochondria, culminating in cellular death in sufficiently severe cases.

Reports of negative side-effects from selegiline resemble those of classical stimulants, but tend to be far milder. I’ve only really noticed mild dry-mouth. You might experience restlessness, anorexia, insomnia, increased pulse and blood pressure*, though

  • Perhaps paradoxically, low doses of l-deprenyl have been found to induce orthostatic hypotension in geriatric patients. Refer to the monograph for Zelapar, a newly released orally active form of l-deprenyl.
    I casually hypothesize that selegiline can cause agitation, restlessness, elevated body temperature and insomnia sans increases in heart rate and/or blood pressure.

Key chemicals to avoid combining with MAOB-selective doses of selegiline (or to combine extremely carefully, at (very) low doses, in pursuit of synergy) (list not exhaustive):

Any classical stimulant, particularly those broken down preferentially by MAOB.
adrenergic stimulants, eg ephedrine
likely some atypical stimulants**
MDMA (or other entactogens)
Psychedelic drugs based off of the phenethylamine backbone (eg, mescaline, 2cb, 2c-t-7, DOB)
pseudo-ephedrine
propoxyphene (darvocet…don’t take this anyway; it not only sucks, but is also ineffective against pain)
synephrine (although this tends to be rather ineffective too)
ephedrine
l-tyrosine
phenylalanine (either stereoisomer)
phenethylamine itself
l-dopa

**For example, a couple of users reported uncomfortable synergy with caffeine, even though caffeine doesn’t affect monoamines directly. Another key example, modafinil, is currently poorly understood, but one study suggests that it somehow boosts dopamine in significant levels [citation needed]. Please tread with caution if at all.

This list is not exhaustive! When in doubt, avoid medications and other drugs that list a warning of contraindication with MAOIs. While such warnings usually refer to non-selective MAOIs or those selective for MAOA, you’ll have to cultivate your own understanding of how our bodies metabolize such medications and increasingly present neurotransmitters consequent of the medication’s effects if you’re to determine how safe a combination might be.

drugs to avoid when taking selegiline in doses unselective for MAOB:

Foods containing tyramine (most aged and/or fermented foods, like red wine, most cheeses, etc.)
(if taking an MAO-inhibitor, particularly an irreversible one, please take care to look up a list of foods containing significant amounts of tyramine, which could prove life-threateningly dangerous)

SSRIs
Other medications increasing serotonin or norepinephrine (eg (but not limited to), tricyclic anti-depressants, the heterocyclics, tramadol, and medications chemically homologously related to these.

DXM provides a key example: prominent among bluelighters, this medication effects increased intercellular serotonin, and thus presents the danger of serotonin syndrome when combined with other medications that increase intercellular serotonin. A general reminder: never mix DXM with MDMA, as it could prove life-threatening.

5-htp or l-tryptophan

a more exhaustive (yet not completely so) list of contraindications:

listed contraindications from the Selegiline Rx Monograph:
This drug should not be used with the following medications because very serious (possibly fatal) interactions may occur:

antidepressants (e.g., TCAs such as amitriptyline/protriptyline, nefazodone, SSRIs such as fluoxetine/paroxetine/sertraline, venlafaxine), appetite suppressants (e.g., diethylpropion, sibutramine), drugs for attention deficit disorder (e.g., atomoxetine, methylphenidate), certain antihistamines (azatadine, carbetapentane, chlorpheniramine), bronchodilators (e.g., albuterol, salmeterol), bupropion, buspirone, carbamazepine, cyclobenzaprine, dextromethorphan, certain drugs for glaucoma (e.g., apraclonidine, brimonidine), certain drugs for high blood pressure (e.g., guanethidine, methyldopa), other MAO inhibitors (furazolidone, isocarboxazid, linezolid, moclobemide, phenelzine, procarbazine, tranylcypromine), nasal decongestants (e.g., phenylephrine, pseudoephedrine), certain narcotic medications (e.g., fentanyl, meperidine), street drugs (e.g., MDMA/“ecstasy”, LSD, mescaline), stimulants (e.g., amphetamines, ephedrine, epinephrine, phenylalanine), “triptan” migraine drugs (e.g., sumatriptan, rizatriptan), tramadol, tyrosine, tryptophan.

NEVER COMBINE SELEGILINE WITH A STIMULANT AT DOSES OF SELEGILINE THAT INHIBIT MAO-A (>5mg per day)

How to move toward exploiting synergistic combinations between selegiline and other drugs more safely***:

***I employ the terms â??more safelyâ?? rather than “safely” because dangerous, experimental combinations, such as those below, could never prove â??safeâ?? per se.

First, you’ll need to try the selegiline on its own. If you wish to retain MAO-B selectivity (which you’ll want to if you plan to try combining selegiline with almost any other drug). I suggest 5 mg/day for the first week. selegiline’s oral bioavailability is poor, but it increases when the drug is taken on a full stomach (the fattier its contents, the better). You can also try taking it sublingually. Now, selegiline tastes quite bad and numbs the area it touches…and I don’t know if this helps.

There is now an alternate formulation of selegiline, delivered by a transdermal patch (brand name, Daytrana). The doses tend to be quite a bit higher than oral formulations, placing the viability of synergistic combinations in doubt. However, there is a particular bluelighter who has experimented with such with success, lauding the combination as long as stimulant dosages remain very low. Still, with non-selective MAO inhibition, I consider this combination extremely risky, too much so to be tolerably safe for most anyone.

Because selegiline is irreversible, permanently denaturing the MAO-B molecules in which it comes in contact, you will only have MAO-B activity insofar as your body synthesizes more MAO-B. Thus, in theory, you should require lower doses of selegiline the longer you take it. So you may try 2.5 mg/day after a week or so. The theoretical borderline to maintain selectivity for MAO-B is 10 mg/day, but as serum levels of MAO-B fall, and as less selegiline is needed, a regimen at this level should eventually inhibit MAO-A to some degree. I suggest avoiding taking more than 5 mg/day to retain selectivity for MAO-B, as a rule of thumb to preserve safety.

Now…because the synergy of MAO-B-inhibition and the action of stimulants is multiplicative, depending in part on unique brain chemistry/physiology, we don’t know what this combination will do in your body. What is more, this combination is highly experimentalâ??doctors never prescribe it, and a small number of people have experimented with it. There have been a couple of animal experiments…but just a couple. So you might react idiosyncratically in a dangerous way. Thus, you must exercise the utmost caution. You’ll need to titrate your dosage of the chosen stimulant upward from an almost certainly inactive dose.

More intresting fact:

Accordingly, some researchers recommend that healthy adults take orally 1.5-2 mg/day of Selegiline, starting around age 40, possibly even in the 30s, in order to combat neuron death associated with aging (James South, M. A. , Deprenyl-extending lifespan).

Although certain undesirable side effects, such as irritability, hyperexcitability, psychomotor agitation, insomnia, elevated blood pressure levels, as well as sporadic cases of neck stiffness, are known to be associated with the use of Selegiline, currently, there is no formulation containing Selegiline that effectively overcomes these side effects while preserving the beneficial effects of Selegiline. For example, some researchers recommend the use of calming/sleep-inducing serotonergic systems, such as magnesium and tryptophan, or 5-HTP (James South, M. A., Deprenyl-extending lifespan). However, 5-HTP and tryptophan are known depressants or semisedative hypnotic compounds. Additionally, in one study, a combination of L-deprenyl (5-10 mg/day) with L-phenylalanine (205 mg/day) was shown to have high antidepressive efficacy (Birkmayer, W. , L-deprenyl plus L-phenylalanine in the treatment of depression, JNeural Transm, 1984 ; 59 (1) : 81-87).

However, none of the references cited above suggest combining Selegiline with the other ingredients of the instant composition. It is unexpected discovery of the present invention that the composition enables one to achieve the beneficial effects of Selegiline while avoiding its undesirable side effects. This result is achieved without introducing additional negative side effects that are commonly associated with other additives, such as 5-HTP and tryptophan, used in a combination with Selegiline.