54 replies to this topic

[unregistered_user]

Sorry but I'm going to bump an older thread in hopes that someone can clarify which kind of Selegiline "Dep Pro" from IAS is. I'm assuming it's the HCl version but just wanted to be sure.

Is it safe to conclude that the citrate and the hydrochloride are equally effective and that the only reason there seems to be any confusion surrounding this is due to the marketing claims made by DEDI? I mean, I can't find any evidence that distinguishes one from the other in terms of efficacy. Can anyone else?

Edited by semi-retarded-individual, 08 August 2011 - 09:27 PM.

[chrono]

Lots of thoughts about liquid deprenyl:

It seems that Dep Pro is the citrate version, from what's buried deep in the description:

Deprenyl tablets are selegiline hydrochloride, which is deprenyl bonded to an in-organic molecule. However, liquid deprenyl citrate (LDC) is selegiline bonded to an organic molecule, one reason why the liquid deprenyl citrate is considered to be superior. This form is generally recognized as the most pure and potent form of deprenyl available. It also allows precise titration for anti-aging purposes, as each ml drop in the bottle is equivalent to 1mg deprenyl citrate.

Again there's mention of a "general recognition" that citrate is the most pure and potent form available. This seems pretty silly to me, in absence of any current evidence...the pharmaceuticals doctors use to treat Parkinson's are not of inferior quality to a product available on a website, manufactured by an unidentifiable person or company. Hydrochloride is one of the most common salts in drug manufacture, and I've never heard someone say that citrate is better because it's an organic molecule (choosing drug salts is not the same as shopping for tomatoes). It's just more smokescreen to "poison the well" regarding the shockingly cheap Indian generics (which are still made by identifiable, established pharmaceutical companies).

I would expect both HCl and citrate to have very similar characteristics when absorbed through the mouth. To reiterate, the citrate version is not privileged over other salts, no matter what product descriptions say. If anything, the complete lack of citrate data and accountability of manufacture makes it the other way around.

Sublingual deprenyl has several advantages, but also some key differences which may be highly undesirable for some. First, the bioavailability is much higher: at least 75% of oral DPR is lost to first-pass metabolism [1], resulting in a maximum of 20% availability if taken with food (and more like 5%, without). In the original human study of Zydis (crushable HCl tablets absorbed bucally and sublingually), 1.25mg sublingual HCl produced similar plasma levels and whole-body MAO-B inhibition as 10mg oral [2]. This should be considered when computing dosage, especially if avoiding any MAO-A inhibition is critical.

In general, it should be expected that sublingual administration produces a more immediate subjective response due to the immediate delivery to the bloodstream. Another difference in the pharmacokinetics is that sublingual DPR produced more consistent levels in the bood than oral DPR. For those who think sublingual dosing is preferable, it should be possible to make a solution at home from DPR tablets. Basically, crush them as finely as possible and soak/stir 3x in a pre-measured amount of water.

Second, the MAO inhibition profile changes when administered sublingually. When taken orally, much of the dose is "used up" inhibiting MAO in the GI tract [3]. MAO in these areas is responsible for the metabolism of tyramine [4], which explains the finding that sublingual DPR HCl (which bypasses the stomach) had no effect on the amount of tyramine necessary to produce a crisis (while oral DPR cut it in half) [5]. However, the original human study of Zydis found that 1.25mg sublingual HCl produced more total-body MAO-A inhibition than 10mg oral [2]. What all this strongly suggests is that sublingual DPR results in a higher level of brain MAO-A inhibition than an equivalent dose of oral DPR...perhaps by as much as 10x. (This proportional increase might apply somewhat to MAO-B as well, but as even a single 10mg oral dose inhibits MAO-B by as much as 98% [6], this probably isn't relevant except at very low dosages). There are several threads here discussing how safe it is to combine SSRIs with deprenyl (safety depends on MAOI-B selectivity), but it should be remembered that these calculations are based entirely on the data established by oral dosing, and more extreme caution should be exercised with liquid dosing.

There are also several good posts by aidanpryde earlier in this (merged) thread, concerning the possibility that the metabolites produced mostly in first-pass metabolism (which sublingual bypasses) are responsible in part for the mental effects of the drug.


[6] Ahola R, Haapalinna A, Heinonen E. et al. Protection by L-deprenyl of intact peripheral sympathetic neurons exposed to neurotoxin 6-hydroxy-dopamine (6-OHDA). 11th Symposium of Parkinson's Disease, Rome, March 26–30, 1994. New Trends Clin Neuropharamcol. 1994;7:287.

Edited by chrono, 11 October 2011 - 04:30 PM.

[Raptor87]

Where do you get you Liquid deprenyl? Please Pm me if you have any suggestions. Preferably with a international mail- service.

[chrono]

Where do you get you Liquid deprenyl? Please Pm me if you have any suggestions. Preferably with a international mail- service.

Really? I linked to a product at the very top of my post, and it's been mentioned several times in this thread. Also a few more on the first page of google results. Please put in a little effort...

Edited by chrono, 11 October 2011 - 04:33 PM.

[unregistered_user]

Chrono, you know it's weird but my experiences with sublingual and oral administration don't seem to vary. I'll have to try again to re-assess the effects.

I hope this isn't painfully amateurish of me to inquire about but what would be considered proper sublingual administration of Deprenyl? I simply place a drop or two under my tongue and wait a few minutes before swallowing. Is there any specified amount of time or proper way to ensure it is being fully absorbed? Maybe I didn't wait long enough?

[chrono]

Well, I can only give my painfully amateurish answer that I think that's just the right way to do it. Try to make sure it's either under your tongue or between your cheek and gums. Having less spit in your mouth will make it less diluted. 5 minutes (at most) should really do the trick.

I took 10mg of deprenyl for about a month earlier this year. The effects were very subtle, to say the least. If I take it again, it will be very small quantities just for the neuroprotection/etc., and maybe a little of that CAE effect.

[longevitynow]

Well, I can only give my painfully amateurish answer that I think that's just the right way to do it. Try to make sure it's either under your tongue or between your cheek and gums. Having less spit in your mouth will make it less diluted. 5 minutes (at most) should really do the trick.

I took 10mg of deprenyl for about a month earlier this year. The effects were very subtle, to say the least. If I take it again, it will be very small quantities just for the neuroprotection/etc., and maybe a little of that CAE effect.

Did you take the 10mg sublingually? For me I notice deprenyl a lot more sublingually. And thanks for the comparison of absorption and first-pass metabolism. That seems to explain why I feel a lot more when I do it sublingully.

[pasha78]

Hia peeps hope all is well. i've recently ordered from United Pharmacies a strip of the Selgin branded selegine. just wandered if any one had any experiences with united pharma and if they are reliable i.e. not flogging fake crap? last thing i want is to be poisoned! Really tried hard to get the drops but cant seem to find anyone willing to ship it to the uk. be greatful for some decent advice.

[thedevinroy]

Sublingual Deprenyl 5mg from capsule didn't do that much different. Sublingual is better for first time (and recreational) users, since it won't mess with your stomach/intestinal enzymes. Someone who literally isn't me may have had nausea from oral administration, and others who also aren't me had no nausea. Snorting, from what I hear will cause insomnia... not that any of you would do that...

I've only had nausea from the first dose when taken orally. That side effect never returned, minus the time I ate two bowls of Corn Pops... which always disagree with me... so hard to say if that was from Deprenyl.

[longevitynow]

Chrono, you know it's weird but my experiences with sublingual and oral administration don't seem to vary. I'll have to try again to re-assess the effects.

I hope this isn't painfully amateurish of me to inquire about but what would be considered proper sublingual administration of Deprenyl? I simply place a drop or two under my tongue and wait a few minutes before swallowing. Is there any specified amount of time or proper way to ensure it is being fully absorbed? Maybe I didn't wait long enough?

Having taken Deprenyl 100s of times, I can say it works very well sublingually. I've taken the liquid and also tablets under my tongue. I like the selgin brand by Intas from India for sublingual use as tabs are quite small. But really, I would do everything to get the liquid if you can. Not much time under the tongue (maybe a minute) and most people notice they feel different. Longer probably gives better absorbtion but it tastes bad and many people will swallow it quicker than that but still seem to get the effect.

[Baten]

Hia peeps hope all is well. i've recently ordered from United Pharmacies a strip of the Selgin branded selegine. just wandered if any one had any experiences with united pharma and if they are reliable i.e. not flogging fake crap? last thing i want is to be poisoned! Really tried hard to get the drops but cant seem to find anyone willing to ship it to the uk. be greatful for some decent advice.

I bought 8 Selgin strips from United Pharmacies, came quickly & plainly packed in an envelope from Singapore. Have ordered 4 times and always came in timely fashion and correct ammounts.

As for the substance, Indian generic = not 99% pure (more fillers or the like), but definitely not poisonous, hehe. I dissolve 5mg sublingually when I want some "extra dopamine". It really works wonders for mood. 5mg might be a bit of a high dose for starters, try breaking the tablet into 2.5mg pieces and use those. When you don't get side effects, try 5mg.

Edited by Baten, 26 November 2011 - 10:11 AM.

[toza]

It seems that Dep Pro is the citrate version, from what's buried deep in the description

I got this email from antiaging-system.com:

Dep-Pro uses selegiline hydrochloride sterile water, potassium sorbate, lemon flavor, tropical punch flavor, flavor-sweet, this formula is therefore not the same of the original (and now defunct) DEDI liquid deprenyl citrate.

So it looks like it's just selegiline HCL dissolved in water...
Are the effects of using selegiline HCL sublingually and selegiline citrate sublingually the same?

[pasha78]

Hey Baten thank you for the response. i'm still concerned as the payment was taken in Montenegro....... :-|

[chrono]

It seems that Dep Pro is the citrate version, from what's buried deep in the description

I got this email from antiaging-system.com:

Dep-Pro uses selegiline hydrochloride sterile water, potassium sorbate, lemon flavor, tropical punch flavor, flavor-sweet, this formula is therefore not the same of the original (and now defunct) DEDI liquid deprenyl citrate.

So it looks like it's just selegiline HCL dissolved in water...
Are the effects of using selegiline HCL sublingually and selegiline citrate sublingually the same?

Wow, that's messed up. This is in direct contradiction to the product description on the AAS website, as well: Also known as Deprenyl Citrate, Selegiline and Cyprenil....Deprenyl liquid can be titrated precisely for anti-aging purposes, as each ml drop in the bottle is equivalent to 1mg deprenyl citrate and regular doses are considered to be 1mg to 3mg daily. Hydrochloride is not mentioned anywhere on the page.

Personally I'd rather buy an Indian generic from an established pharma company than to pay almost 10x as much for a product of anonymous manufacture that doesn't even know what salt it is, but I guess that's just personal preference.

Theoretically, sublingual dosing of the citrate or HCl should be quite similar in terms of onset/absorption/etc. Citric acid is drastically heavier than hydrochloric acid though, so you may need about 1.8x the amount of the citrate to equal the same dose of the HCl.

[noos]

Why are you buying Dep Pro if it is the same as tablets? I wonder if it has any proven sublingual absorption effect.

[chrono]

I wonder if it has any proven sublingual absorption effect.

See post #34, though there are more I didn't mention. All sublingual/buccal studies have employed the hydrochloride. The citrate has not been used in any peer-reviewed studies that I'm aware of. IMO its inexplicable popularity is a triumph of marketing over science.

[toza]

Personally I'd rather buy an Indian generic from an established pharma company than to pay almost 10x as much for a product of anonymous manufacture that doesn't even know what salt it is, but I guess that's just personal preference.

Theoretically, sublingual dosing of the citrate or HCl should be quite similar in terms of onset/absorption/etc. Citric acid is drastically heavier than hydrochloric acid though, so you may need about 1.8x the amount of the citrate to equal the same dose of the HCl.

Could you recommend some source for buying the generic? I'll have to go for sublingual HCL, since the citrate is not available anywhere.

So 1.8mg of selegiline HCL = 1mg of selegiline citrate? Can anyone confirm this? Actually has anybody taken them both and got the same effects on mood? (citrate sublingually has definitely enhanced my mood, HCL orally had no effects I could feel)

[Ben]

Theoretically, sublingual dosing of the citrate or HCl should be quite similar in terms of onset/absorption/etc. Citric acid is drastically heavier than hydrochloric acid though, so you may need about 1.8x the amount of the citrate to equal the same dose of the HCl.

Good thing about the citrate was (and about the dissolved, no name brand, is) that it hadn't the binders that the tablet HCL has. This makes it easier to take it subling.

[thedevinroy]

Personally I'd rather buy an Indian generic from an established pharma company than to pay almost 10x as much for a product of anonymous manufacture that doesn't even know what salt it is, but I guess that's just personal preference.

Theoretically, sublingual dosing of the citrate or HCl should be quite similar in terms of onset/absorption/etc. Citric acid is drastically heavier than hydrochloric acid though, so you may need about 1.8x the amount of the citrate to equal the same dose of the HCl.

Could you recommend some source for buying the generic? I'll have to go for sublingual HCL, since the citrate is not available anywhere.

So 1.8mg of selegiline HCL = 1mg of selegiline citrate? Can anyone confirm this? Actually has anybody taken them both and got the same effects on mood? (citrate sublingually has definitely enhanced my mood, HCL orally had no effects I could feel)

Selegiline Molar Mass: 187.281 g/mol
HCl Molar Mass: 36.46 g/mol
Citrate Molar Mass: 192.124 g/mol

Selegiline HCl Molar Mass: 223.741 g/mol
Selegiline Citrate Molar Mass: 379.405 g/mol

Selegiline HCl / Selegiline Citrate Ratio: 1.69573301
Selegiline Citrate / Selegiline HCl Ratio: 0.589715476

To answer your question, you would not. Follow the instructions on the bottle. Chrono was referring to a scenario where you knew the concentration of Selegiline Citrate and the dose for Selegiline HCl. This does not apply to your question.

[toza]

To answer your question, you would not. Follow the instructions on the bottle. Chrono was referring to a scenario where you knew the concentration of Selegiline Citrate and the dose for Selegiline HCl. This does not apply to your question.

My question was, how much selegiline HCL from crushed tablets should I take sublingually to get the same effect as from 1mg selegiline citrate sublingually (if you can get the same effect from these 2 molecules at all).
Also knowing where can I order cheap safe generic Selegiline HCl would be nice.

Thanks...

[thedevinroy]

To answer your question, you would not. Follow the instructions on the bottle. Chrono was referring to a scenario where you knew the concentration of Selegiline Citrate and the dose for Selegiline HCl. This does not apply to your question.

My question was, how much selegiline HCL from crushed tablets should I take sublingually to get the same effect as from 1mg selegiline citrate sublingually (if you can get the same effect from these 2 molecules at all).
Also knowing where can I order cheap safe generic Selegiline HCl would be nice.

Thanks...

1) You wouldn't do it that way. There is more than just Selegiline HCl in those tablets. Tablets (and capsules, too) can contain resins, binders, emulsifiers, dispersing agents, waxes, etc. that merely provide chemical mechanisms for the absorption of the drug as well as look and feel. These, in many cases of small active ingredients (less than 100mg) equate for most of the tablet.

2) 1mg of Selegiline HCl is probably what you are aiming for, not 1mg Selegiline Citrate (which is equivalent to approximately 0.59mg of Selegiline HCl). 1mg Selegiline HCl is pretty standard (as is 1mg of pure Selegiline, which is only 20% more potent) for neurological health.

My suggestion: If it is a 5mg pill, you would divide it into 5 piles. Each pile would be worth 1mg of active ingredient. If the tablets read "Selegiline HCl 5mg" or "Selegiline 5mg", there will only be a 20% difference, the latter being the stronger of the two.

What are you aiming to achieve?

Edited by devinthayer, 09 December 2011 - 05:01 PM.

[toza]

1) You wouldn't do it that way. There is more than just Selegiline HCl in those tablets. Tablets (and capsules, too) can contain resins, binders, emulsifiers, dispersing agents, waxes, etc. that merely provide chemical mechanisms for the absorption of the drug as well as look and feel. These, in many cases of small active ingredients (less than 100mg) equate for most of the tablet.

2) 1mg of Selegiline HCl is probably what you are aiming for, not 1mg Selegiline Citrate (which is equivalent to approximately 0.59mg of Selegiline HCl). 1mg Selegiline HCl is pretty standard (as is 1mg of pure Selegiline, which is only 20% more potent) for neurological health.

My suggestion: If it is a 5mg pill, you would divide it into 5 piles. Each pile would be worth 1mg of active ingredient. If the tablets read "Selegiline HCl 5mg" or "Selegiline 5mg", there will only be a 20% difference, the latter being the stronger of the two.

What are you aiming to achieve?

I was of course talking about the active ingredient mass, not the tablet powder mass
In fact I am aiming for 1mg Selegiline Citrate equivalent, since this is what made the desired effect for me when I was taking liquid Selepryl(Selegiline Citrate) sublingually. The effect I am aiming for and which I got with the Selepryl is mood enhancement - it simply made my days brighter.

[thedevinroy]

1) You wouldn't do it that way. There is more than just Selegiline HCl in those tablets. Tablets (and capsules, too) can contain resins, binders, emulsifiers, dispersing agents, waxes, etc. that merely provide chemical mechanisms for the absorption of the drug as well as look and feel. These, in many cases of small active ingredients (less than 100mg) equate for most of the tablet.

2) 1mg of Selegiline HCl is probably what you are aiming for, not 1mg Selegiline Citrate (which is equivalent to approximately 0.59mg of Selegiline HCl). 1mg Selegiline HCl is pretty standard (as is 1mg of pure Selegiline, which is only 20% more potent) for neurological health.

My suggestion: If it is a 5mg pill, you would divide it into 5 piles. Each pile would be worth 1mg of active ingredient. If the tablets read "Selegiline HCl 5mg" or "Selegiline 5mg", there will only be a 20% difference, the latter being the stronger of the two.

What are you aiming to achieve?

I was of course talking about the active ingredient mass, not the tablet powder mass
In fact I am aiming for 1mg Selegiline Citrate equivalent, since this is what made the desired effect for me when I was taking liquid Selepryl(Selegiline Citrate) sublingually. The effect I am aiming for and which I got with the Selepryl is mood enhancement - it simply made my days brighter.

Okay, that makes sense now. Thanks for the background info. I still think that you would want 1mg of Selegiline.

Use a factor of 1.7 if this is what you truly know to be true. 1mg of Selegiline Citrate sounds fishy to me. If you know that the concentration on the bottle was in Selegiline Citrate and not Selegiline, continue with this advice (I do want you to double check the old bottle, and if you can't remember which one for sure, ask... you may be chasing a faster squirrel than you can catch for MAO-B inhibition at 1mg Selegiline Citrate as opposed to 1mg Selegiline). Divide two 5mg pills into 17 piles. Each pile will be worth an equivalent of 1mg of Selegiline Citrate.

Check the speed of the squirrel. Anyone know %inhibition of 0.5mg of pure Selegiline sublingual on MAO-B? Sure it's around here somewhere... 0.5mg Selegiline is roughly in 1mg of Selegiline Citrate.

Edited by devinthayer, 11 December 2011 - 06:44 AM.

[toza]

Okay, that makes sense now. Thanks for the background info. I still think that you would want 1mg of Selegiline.

Use a factor of 1.7 if this is what you truly know to be true. 1mg of Selegiline Citrate sounds fishy to me. If you know that the concentration on the bottle was in Selegiline Citrate and not Selegiline, continue with this advice (I do want you to double check the old bottle, and if you can't remember which one for sure, ask... you may be chasing a faster squirrel than you can catch for MAO-B inhibition at 1mg Selegiline Citrate as opposed to 1mg Selegiline). Divide two 5mg pills into 17 piles. Each pile will be worth an equivalent of 1mg of Selegiline Citrate.

Check the speed of the squirrel. Anyone know %inhibition of 0.5mg of pure Selegiline sublingual on MAO-B? Sure it's around here somewhere... 0.5mg Selegiline is roughly in 1mg of Selegiline Citrate.

Sorry for confusion, you are right - 1 drop of Selepryl contains selegiline citrate equivalent of 1mg Selegiline base.

Would there be any difference between taking Dep pro(selegiline HCL in liquid form) and selegiline HCL in tablets sublingually? Can taking the tablets sublingually damage my teeth?

[thedevinroy]

Okay, that makes sense now. Thanks for the background info. I still think that you would want 1mg of Selegiline.

Use a factor of 1.7 if this is what you truly know to be true. 1mg of Selegiline Citrate sounds fishy to me. If you know that the concentration on the bottle was in Selegiline Citrate and not Selegiline, continue with this advice (I do want you to double check the old bottle, and if you can't remember which one for sure, ask... you may be chasing a faster squirrel than you can catch for MAO-B inhibition at 1mg Selegiline Citrate as opposed to 1mg Selegiline). Divide two 5mg pills into 17 piles. Each pile will be worth an equivalent of 1mg of Selegiline Citrate.

Check the speed of the squirrel. Anyone know %inhibition of 0.5mg of pure Selegiline sublingual on MAO-B? Sure it's around here somewhere... 0.5mg Selegiline is roughly in 1mg of Selegiline Citrate.

Sorry for confusion, you are right - 1 drop of Selepryl contains selegiline citrate equivalent of 1mg Selegiline base.

Would there be any difference between taking Dep pro(selegiline HCL in liquid form) and selegiline HCL in tablets sublingually? Can taking the tablets sublingually damage my teeth?

If you're that concerned, rinse your mouth out with baking soda and water.