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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 8 of 8. This is the beginning of the thread.
Posted by mogger on September 5, 2005, at 1:17:36
Hi there,
my sister is on 40mg of Selegiline and 1000mg of Phenylalanine and has done the best she has ever done since she tried meds. Everything she tried, about 17 different meds didn't work and then this. However after about a month and half of being on the current dose she seems to be slipping slightly. I am so scared that this med is going to poop out on her. Is this common for Selegiline to poop out or does it usually hold ground?
any experiences that you could share? many thanks,
worried brother
Posted by Declan on September 5, 2005, at 23:59:39
In reply to selegiline, poop out?, posted by mogger on September 5, 2005, at 1:17:36
Low dose selegeline doesn't poop out, but on the doses your sister is on I have no idea. Perhaps receptors are downregulating or whatever it is.
Declan
Posted by mogger on September 6, 2005, at 11:31:00
In reply to Re: selegiline, poop out?, posted by Declan on September 5, 2005, at 23:59:39
Does downgrading mean total failure or perhaps just slight. Thanks for your reply,
mogger
Posted by Ktemene on September 6, 2005, at 21:43:31
In reply to selegiline, poop out?, posted by mogger on September 5, 2005, at 1:17:36
40mg Selegiline is still a pretty low dose for most people, and 1000mg Phenylalanine is also a fairly low dose. If your sister has had a good reaction to that combo for six weeks it would not hurt to increase the dose of one or the other. This sort of readjustment after a few weeks is common- it does not mean poop out. I have been told that the MAOI's are less likely to poop out than SSRI's.
> Hi there,
> my sister is on 40mg of Selegiline and 1000mg of Phenylalanine and has done the best she has ever done since she tried meds. Everything she tried, about 17 different meds didn't work and then this. However after about a month and half of being on the current dose she seems to be slipping slightly. I am so scared that this med is going to poop out on her. Is this common for Selegiline to poop out or does it usually hold ground?
> any experiences that you could share? many thanks,
> worried brother
Posted by Declan on September 6, 2005, at 23:25:15
In reply to Re: selegiline, poop out? » mogger, posted by Ktemene on September 6, 2005, at 21:43:31
40mg Selegeline's a significant amount in my experience, but I've never taken more than 7.5mg/g. Why not up the phenylalanine, and maybe use DLPA rather than the L form. I know much more than this is used in published studies, maybe up to 5g/d. It's easy to look up.
Declan
Posted by mogger on September 7, 2005, at 0:54:34
In reply to Re: selegiline, poop out? » mogger, posted by Ktemene on September 6, 2005, at 21:43:31
Thanks very much for the experiences, I will keep my fingers crossed.
mogger
Posted by Ktemene on September 14, 2005, at 6:23:57
In reply to Re: selegiline, poop out?, posted by mogger on September 7, 2005, at 0:54:34
Hi Mogger,
I'm with Declan on dosage experience with selegiline. I take low dose selegiline (5mg every morning with 500mg DLPA + 150mg Wellbutrin) and I have never taken a higher dose of selegiline than that. But most people do not get a good effect from low dose selegiline (although several people on this board have reported that low dose selegiline helped them a lot). There was a Current Psychiatry article in 2002 (Vol. 1, No.6 /June 2002) that reported that the dose to aim for when starting selegiline is 45mg per day, and if the response is not what one hoped for, then the dose can be increased. The URL for the article is here: http://www.currentpsychiatry.com/2002_06/06_02_maoi.asp
There is another informative article about MAOI's that discusses deprenyl (selegiline) called "Monoamine Oxidase: Basic and Clinical Perspectives" at http://www.acnp.com/G4/GN401000046/CH046.html
I hope your sister is feeling better soon.
Ktemene
P.S. By the way, some people think that they get a better effect from selegiline if they open the capsule, pour the selegiline hydrochloride powder into their mouths and wait a few minutes before they swallow. I know Larry Hoover took selegiline this way, and I have been taking my 5mg selegiline this way every morning. (The taste is not great, and it makes my mouth feel numb for a few minutes.) A version of selegiline was developed to take advantage of the fact that selegiline can be absorbed directly through the tissues inside the mouth. I have coped a short article about it below.
Comment in:
* J Neural Transm. 2003 Nov;110(11):1273-8.
A new formulation of selegiline: improved bioavailability and selectivity for MAO-B inhibition.
Clarke A, Brewer F, Johnson ES, Mallard N, Hartig F, Taylor S, Corn TH.
Scherer DDS, Swindon, United Kingdom. aclarke@cephalon.com
Seven randomised comparative studies were conducted in healthy volunteers to compare the pharmacokinetic and pharmacodynamic profiles of selegiline hydrochloride in a new formulation designed for buccal absorption "Zydis Selegiline" (1.25-10 mg) with conventional selegiline hydrochloride tablets "conventional selegiline tablets" (10 mg). A total of 156 healthy volunteers participated in these studies. Plasma concentrations of selegiline and its primary metabolites, N-desmethylselegiline (DMS), l-amphetamine (AMT), and l-methamphetamine (MET) were measured using Gas Chromatography Mass Spectrometry (GCMS) and gas liquid chromatography (GLC) assays. Inhibition of monoamine-oxidase type B (MAO-B) and monoamine oxidase type A (MAO-A) activity was determined by measurement of as beta-phenylethylamine (PEA) by GCMS and 5-hydroxyindoleacetic acid (5-HIAA) by High Performance Liquid Chromatography (HPLC) assays. Almost a third (2.96 mg) of a 10 mg selegiline dose in Zydis Selegiline was absorbed pre-gastrically (predominantly buccally) within 1 minute. Mean [SD] area-under-the curve (AUC(0- infinity)) values following Zydis Selegiline 10 mg (5.85 [7.31] ng.h/mL) were approximately five times higher than those following conventional selegiline tablets 10 mg (1.16 [1.05] ng.h/mL). In contrast, plasma concentrations of metabolites were significantly ( p<0.001) lower following Zydis Selegiline 10 mg than following conventional selegiline tablets 10 mg. Plasma concentrations of selegiline and its metabolites increased in a dose-dependent manner over the dose-range Zydis Selegiline 1.25-5 mg. Bioavailability was determined using AUC and peak plasma concentrations (C(max)). The C(max) of selegiline was similar following administration of Zydis Selegiline 1.25 mg (1.52 ng/mL) or conventional selegiline tablets 10 mg (1.14 mg/mL). The range of values for AUC(0- infinity) and C(max) following Zydis Selegiline 1.25 mg were entirely contained within the range following conventional selegiline tablets 10 mg, with a much higher variability of plasma selegiline concentrations occurring after conventional selegiline tablets than after Zydis Selegiline. As expected, peak plasma concentrations for DMS, AMT and MET were consistently lower after Zydis Selegiline 1.25 mg (1.19, 0.34, 0.93 ng/ml, respectively) than after conventional selegiline tablets 10 mg (18.37, 3.60, 12.92 ng/ml, respectively). A significant (r=0.0001) correlation between daily PEA excretion (a measure of brain MAO-B inhibition) and the log-transformed AUC((0-t)) for selegiline was demonstrated. Mean daily PEA excretion was similar following Zydis Selegiline 1.25 mg and conventional selegiline tablets 10 mg (13.0 microg versus 17.6 microg). In contrast, there was no correlation between PEA excretion and selegiline metabolites, indicating that selegiline metabolites do not significantly inhibit MAO-B. Urinary excretion of 5-HIAA (used as a marker for MAO-A inhibition) was unrelated to plasma concentrations of selegiline or DMS following single or repeat dosing of Zydis Selegiline 1.25 mg or conventional selegiline tablets 10 mg. However, comparison of treatment groups revealed a significantly lower excretion of 5-HIAA in the conventional selegiline tablets 10 mg group than in the Zydis Selegiline 1.25 mg group after repeated administration over 13 days. In summary, by reducing the opportunity for first-pass metabolism, the absorption of selegiline from Zydis Selegiline was more efficient and less variable than from conventional selegiline tablets. Compared with conventional selegiline tablets 10 mg, Zydis Selegiline 1.25 mg yielded similar plasma concentrations of selegiline and degree of MAO-B inhibition, but markedly reduced concentrations of the principal metabolites. Thus, the lower but equally MAO-B inhibitory dose of selegiline in Zydis Selegiline 1.25 mg, which is associated with lower concentrations of potentially harmful metabolites, could offer a safer and more predictable treatment in the management of patients with Parkinson's disease.
Publication Types:
* Clinical Trial
* Randomized Controlled Trial
PMID: 14628189 [PubMed - indexed for MEDLINE]
Posted by mogger on September 14, 2005, at 11:15:46
In reply to Re: selegiline, poop out? » mogger, posted by Ktemene on September 14, 2005, at 6:23:57
Thanks for the information, I really appreciate it!
mogger
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