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Re: Report of success: Selegiline: alernate MAOI

Posted by Mr. Scott on March 16, 2001, at 17:14:17

In reply to Re: Report of success: Selegiline: alernate MAOI, posted by Adam on March 15, 2001, at 18:31:00

> I'm sorry. A while ago I tried to post and couldn't due to maintainance of the site. Then I went on a two-week vacation in the Southwest US. Now I'm back.
>
> I had a quick response to selegiline also. So quick, in fact, that I often wondered aloud if I was imagining the whole thing. I don't believe this was the case. I am still on selegiline, and doing very well, mood-wise. Your response does seem remarkably quick, even knowing what I know, but as the pharmacokinetics of selegiline may be influenced by a pharmacodynamic profile involving responses to the parent molecule and its metabolites that are independant of it's MAO-inhibiting function, I'm guessing your exprience could well be more than a figment of your imagination.
>
> I would not be too cavalier about the dietary restrictions, and I would be very serious about the potential drug interactions. I think with diet, it's possible to cheat a little and be OK. Hypervigilance isn't necessary, and the usual restrictions recommended by doctors are clearly not necessary for everyone. However, caution is always warrented. Changes in blood pressure are not always easy to detect emperically, and full-blown hypertensive crisis isn't the only risk state one need consider.
>
> I have had Neurontin (gabapentin) prescribed for selegiline-induced insomnia and anxiety. I think this is a reasonable choice, given Neurontin's relatively benign side-effects profile at low doses. I have chosen not to take it though, and have rather focused my efforts on "sleep hygene" and exercise. For those with similar concerns who care to know, I would endorse this approach first, and a pharmacological approach second. Another approach that might be worth exploring is low-dose risperidol.
>
> I have heard mention of foreign pharmacies somehow formulating their own selegiline patches. I wouldn't trust such a source, if indeed it exists. There have been and continue to be numerous placebo-controlled pilot and phase-II and III trials of the selegiline transdermal system (STS) for various indications (Parkinsons, AIDS-related dementia, Alzheimers, Major Depressive Disorder...not all trials are at the same stage of advancement). The results appear promising, but I've yet to hear anything about the approval of the STS for any indication. This is not suprising, given the glacial pace of the FDA approval process. I'm sure there is still hope that the STS will be on the market in the US in a few years or less, and may be marketed in other countries earlier (most likely, for most pharmaceuticals), and could conceivably be obtainable through foreign channels, though this is an increasingly difficult means of obtaining drugs.
>
> On selegiline's chemical properties: Selegiline is an L-phenylamine-class drug, and it's metabolites, which happen to include methamphetamine and amphetamine, are also, given their parent's enantiomeric identity, the "L" forms of these drugs. The designer-drug versions of methamphetamine and amphetamine are the "D" forms, the "mirror images" of selegiline's metabolites, if you will, and have more potent and somewhat different effects on the central and peripheral nervous systems. They shouldn't make you high, in other words, at least not at the doses seen in any clinical application I'm aware of. Clearly, these metabolites do something, though, and I believe (being a non-expert, mind you) that their effects are mostly a nuisance which is mitgated considerably by transdermal delevery, which moderates both the rate of dosing and eliminates first-pass metabolism, whence much of the L-methamphetamine (the precursor of the L-amphetamine in this case) is generated. I'm fairly convinced that the antidepressant action of selegiline is due in large part to the parent compound, given the rate of my positive response to the patch, which I obtained through a phase-III trail for MDD.
>
> It would appear that sexual side-effects are uncommon on selegiline, even at high doses. I think this could be a function of selegiline's activating properties, which seem to stem from it's strongly dopaminergic action, a result not only of MAO-inhibition but also, apparently, blockage of DA reuptake. Tranylcypromine may also be similar in this regard, due to it's amphetamine-like structure (giving it more than one dopaminergic mechanism of action). When one contrasts this with phenelzine, one can consider the latter's hyrazine metabolite(s), which enhances GABA signaling, which in turn inhibits DA secretion in some parts of the brain, leading to such beneficial effects as decreased anxiety, but possibly also some adverse effects like sexual dysfunction. (NOTE: Sexual dysfunction may also be due to enhanced serotonin signaling, the effects of would not be counteracted in phenelzine's case, given the current theories about serotonergic drugs' affects on the dopamine system, and some of the pharmicological antidotes that appear to work for some individuals).
>
>
>
> > I have been on Selegiline for only two days at a dose of 60 mg in three divided doses. (I do not have Parkinsons' disease, but rather Treatment-Resistant Depression. I have taken every other antidepressant known to mankind). So far, I have noticed a moderate antidepressant effect after one hour of ingesting it, which I could never get from a placebo. And that is why I'm writing this, to alert others.
> >
> > Selegiline should be known as the "alternative" MAOI, in that it has less of the side-effects of phenelzine or tranylcypromine. The main side-effect that I have with it is a powerful stimulating effect similar to one caused by buproprion. I have been taking 10 mg oxazepam along with selegiline in order to counter the anxiety produced by selegiline.
> >
> > Notes:
> > --I don't think that selegiline has an antidepressant effect under doses of 40 mg per day.
> > --I don't know if selegiline has any sexual side-effects yet.
> > --100 of the Generic 5 mg capsules (you need 240 capsules for a months antidepressant supply) costs US $240 at Sav-On Drug Stores. That is expensive. However, medical insurance covers it.
> > --You have to drop almost every other antidepressant in order to take the MAOI selegiline, although there is only one reported case in history of Serotonin Syndrome (that is fact).
> > --You have to follow the MAOI diet (I won't, though. I didn't on phenelzine or tranylcypromine and didn't have a hypertensive crisis).

Do you think there is a "SAFE" dosage to take selegeline WITH an SSRI?


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poster:Mr. Scott thread:56408
URL: http://www.dr-bob.org/babble/20010310/msgs/56692.html