Thanks. I assume there’s no generic version of Zelapar because it seems that everything I found on Indian marketplaces is normal tablets.
Trade names Eldepryl, Jumex, Zelapar, Emsam, others[1]
ah…
Has a generic version of Zelapar been approved?
No. There is currently no therapeutically equivalent version of Zelapar available in the United States.
But FDA approval in 2006, so generics available very, very soon - typically patents are issued a few years prior to FDA approval, so a generic may be available very soon, if its not already available in India (where generics typically come out first):
ZELAPAR (selegiline hydrochloride - tablet, orally disintegrating;oral)
- Manufacturer: BAUSCH
Approval date: June 14, 2006
Strength(s): 1.25MG [RLD]
It seems there are lots of options at least for some versions, not sure on the disintegrating tablets - just search under the other names; selegeline, Eldepryl, etc with dissolving, and similar words?
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For example, conventional selegiline tablets had to be taken more than once daily. Not only did the conventional formulation have less than optimal efficacy, but it also presented a safety risk due to first-pass metabolite formation. The fast-dissolve formulation of selegiline, Zelapar, developed using Catalent’s Zydis orally disintegrating tablet technology, is absorbed buccally, thereby, avoiding first-pass metabolism and significantly reducing the potential for side effects. The ability to disintegrate in less than 3 seconds allows for increased bioavailability and a faster onset of action for Zelapar. The maximum blood levels of the drug (Tmax) were achieved in 15 minutes for Zelapar compared with 1 hour for the conventional selegiline pills. Moreover, dosing frequency could be reduced (i.e., 1.25 mg or 2.5 mg once daily compared with 5 mg twice daily for the conventional formulation).
Source: https://www.pharmtech.com/view/can-pharma-defy-gravity-patent-cliff
Looks like the patent is expiring around now:
Source: Evergreen Drug Patent Database - UC College of the Law
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The first post under this topic has a paper by researcher Joseph Knoll who recommended 1 mg of “regular” Deprenyl per day for antiaging. The Life Extension Foundation “LEF” recommends daily dosages totalling 10 mg per week.
But the important point with regard to the above recommendations is that this is regular swallowed Deprenyl, NOT the orally dissolving tablet. For Parkinson’s, a common dosage is 5 mg regular Deprenyl twice daily. Or, 1.25 mg of the orally disintegrating pill twice daily. So that gives you an idea of the difference in potency and why they aren’t interchangeable.
There are some people who take higher dosages of Deprenyl for antiaging similar to a Parkinson’s patient. But LEF and Knoll both make arguments against this. Also, if someone does take a higher dosage, drug interactions have to be monitored.
Two rodent lifespan studies in mice and rats also found that polyscias fruticosa root had a synergistic effect with Deprenyl and helped to substantially increase the lifespan extension. I drink polyscias fruticosa tea daily. It’s the leaves and stems.
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Yes, you can buy generics of Deprenyl/Selegiline (tablets to swallow) but not of Zelapar (orally disintegrating tablets). Pharmaceutical companies can often file a new patent if they change the route of administration and dosage of a drug.
As @Vlasko said, the ODT version is about 10 times more potent:
“To improve its bioavailability, new delivery forms of selegiline were also developed. Orally disintegrating tablets (ODT) are characterized by rapid drug release into saliva. A fraction of the active pharmaceutical ingredient absorbs through the buccal mucosa, avoiding thus the first pass metabolism and providing fast onset of action. According to comparative pharmacokinetic studies of conventional and ODT formulations, selegiline plasma exposure of 1.25 mg ODT was comparable to that of 10 mg conventional tablet. […] Comparative clinical trial of 1.25–2.5 mg selegiline ODT and 10 mg conventional tablets revealed similar efficacy and safety. […] By reviewing the available clinical data, we concluded that the clinical advantage of the clear pharmacokinetic improvement is not well justified. However, the patients’ preference, because of the convenience of ODT use, especially in patients with swallowing difficulties, should be acknowledged” (2019 review by Hungarian colleagues of late Knoll: Selegiline: a molecule with innovative potential | Journal of Neural Transmission )
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That’s interesting, thanks. There are so many details about Selegiline to use it correctly: route of administration (swallowed vs. disintegrating vs. skin patch), dosage (could be age dependent?), time of day, additional nutraceutical (e.g., polyscias fruticosa), etc.
We need an ITP for Selegiline for sure. But I think we also need a wiki where we could put all the information about Selegiline that is currently scattered over this forum (I think there are at least 3 threads discussing this drug for instance). And Wikipedia is quite conservative when it comes to medicine-related articles (see: Wikipedia:Manual of Style/Medicine-related articles - Wikipedia ). I’m among the most active contributors to Wikipedia and I don’t contribute in the longevity field because of this.
I googled “Longevity Wiki” and found one, I’ve just created a page about Selegiline, so feel free to contribute: Selegiline - Longevity Wiki
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Yes - we have a couple of main Deprenyl threads, with a lot of information.
Here (86 posts in the thread): Deprenyl - Anti-Aging Drug Proven Effective in Dogs
Here (36 posts in the thread): Anyone taking Selegiline / Deprenyl For Longevity?
The longevity wiki guys are good and I applaud the effort, but they don’t seem to have critical mass yet.
For sure, you cannot have a critical mass for a wiki on such a niche topic as longevity. But we just need a few people centralizing interesting information currently scattered around this forum there from time to time. It would look like this: Selegiline - Longevity Wiki
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While writing the Wiki article I found two interesting articles:
- Chronic Treatment of Syrian Hamsters With Low-Dose Selegiline Increases Life Span in Females But Not Males 1997
- Age-related decline of various cognitive functions in well-experienced male rats treated with the putative anti-aging compound (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine ((-)BPAP) 2023
The latter was just published by Hungarian researchers from Semmelweis University (the one of the late Knoll). They study BPAP, a deprenyl derivative and found no beneficial effects on cognitive capabilities or lifespan. They argue that their rats were under restricted food access and cognitively stimulated during the study so that they may have reached a ceiling in terms of lifespan and BPAP couldn’t go above that ceiling.
I wonder why they don’t study deprenyl anymore and instead study this derivative. They may have negative unpublished results about deprenyl. Typical publication bias: authors are more likely to submit positive results than negative ones. May be worth contacting them.
This seems to be the most recent animal study of selegiline, and it was done by Knoll two years before his death: Longevity study with low doses of selegiline/(−)-deprenyl and (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP)
In this paper, he compared a saline solution to deprenyl (DEP) and a derivative devoid of MAO-B inhibitory effect: BPAP. Instead of 0.25 mg/kg three times a week as in previous studies, he tried lower doses of 0.001 mg/kg and 0.1 mg/kg.
Conclusions below: the lowest dose (0.001 mg/kg) had no significant effect (according to Knoll because 3 times per week may not be enough for low-dose deprenyl?), and the other one (0.1 mg/kg) increased the average lifespan by 12%. The life extension effect is mainly due to the increase in the life of the shortest-living rat: +28%!
I also contacted Dr. István at Semmelweis University to ask them to apply for an ITP of deprenyl (or BPAP if they think it’s better?).
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tl;dr: Deprenyl + NAC improves Parkinson’s-like symptoms even more than Deprenyl alone.
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blsm, I’ve decided to try Deprenyl at the 1.25 mg dose. Did you swallow the 1.25 mg dose or dissolve it under the tongue? Do you have any more thoughts on using it since your Apr 21 post? Thanks.
Hi Jay, I’ve been swallowing 1/4 pill. Someone here suggested that by swallowing it I might tolerate it better. I restarted it just a couple weeks ago and this time has been a lot more positive so far. I believe my initial perceived negative response earlier this year had more to do with the gluten exposures I was unknowingly having at work for a couple months tbh.
I swallow 1/4 (1.25mg) of a tab as well and wonder if it’s enough. I recently turned 38 so perhaps I don’t need as much as most, but I still want the benefits.
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I’m considering trying a half pill (2.5mg) 4x weekly after reading the wiki since I recently turned 54.
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I read that some take 5mg twice weekly.
I wonder what would be different?
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I’m up for experimenting. Thanks for the suggestion!
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I’ll start an experiment with this tomorrow morning. I found a couple sources that said it is completely water soluble, so I may dissolve some in water, shake it up, let the fillers settle to the bottom, and then draw a precise dose with a medicine dropper. The same technique used for low-dose naltrexone.
I intend on taking it with breakfast: “There is at least a 3-fold increase in the Cmax and area under the concentration-time curve of selegiline with food.”
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Selegiline - Continue Education Statpearls
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