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Dr. Bob is Robert Hsiung, MD,
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Posted by yxibow on May 27, 2006, at 0:43:13
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by jealibeanz on May 26, 2006, at 1:42:58
> I know that the cytochromes are part of the electron transport chain involved in the degradation of medications in the liver. Is this necessary when breaking down all medications, or just those that go through the GI tract? Does transdermal delivery avoid processing in the liver?
No, transdermal delivery does not avoid the processing of what, as was correctly noted, an older drug used in Parkinson's (Eldepryl, selegiline hydrochloride) often in combination with Sinemet (levodopa/carbidopa).
It is simply a different method of entry into your bloodstream. A number of medications and chemical substances can enter your bloodstream through your skin -- it is porous.
If you cover too much of your body with Benadryl or Ben-Gay creams you may reach a toxic level inside your system, as the medication goes through the layers of your skin, the outer always being dead, which protects us from some substances being harmful, but not all.
Once the drug is in your bloodstream, it will eventually be metabolized by your liver (or in the case of certain, fewer medications, that bypass the liver route and go through your kidneys, such as Serax -- often through a process known as glucuronidation.)
And as for psychiatrists knowing P450 -- if they dont, they're in serious jeapordy of their license.Its a basic principle -- but I agree, if you are "old school" you may not have been taught all the intricacies which are now routinely taught in medical school, and which if you read a drug monograph or as we call it in the US, a PI, or prescribing information, they will list testing for cytochromes.
This wasn't done routinely until the last decade because the knowledge wasn't out there -- as one who takes polypharmacy (multiple medications), I've had a few curveballs with mixing modern medications with older ones and having to adjust to avoid things like serotonin syndrome.
Posted by jealibeanz on May 27, 2006, at 6:07:32
In reply to Re: Are Family Doctors prescribing EMSAM? » jealibeanz, posted by yxibow on May 27, 2006, at 0:43:13
Right, OK, drugs have to be broken down in the liver when enyering the bloodstream. However, they avoid the stomach. Would this decrease the likelihood of weight gain? Where does insulin come in to play? Does EMSAM involve histamine blockers like the SSRIs/SNRIs (which could be a reason for my weight problems in addition to serotonin, right?)?
Posted by pulse on May 27, 2006, at 15:08:59
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by jealibeanz on May 27, 2006, at 6:07:32
sorry, but Emsam does NOT avoid the gut, far a GI problems. the pharmacist i dislike, of the 2 at my regular drugstore, was right, for once, when he predicted this could - and did happen - to me. oh, boy, did it ever!
another pharmacist at a compounding pharmacy that i'd switched to for a better price on emsam, said same: of course, Emsam thru bloodstream only, can still cause GI problems. i sincerely hope this applies to GI problems/ meds intolerant (not treatment resistant) folks like me - only.
pulse
Posted by pulse on May 27, 2006, at 15:18:04
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by pulse on May 27, 2006, at 15:08:59
forgot to add that yes, my gp (actually an allergy specialist) did (somewhat begrudgingly) prescribe Emsam for me. he has 300 psych. patients, as we have next to no competent p-docs here (revise that to none, imo, at least). he has done much volunteer work at a transitional living place for the seriously mentally ill, so he does know his stuff. he will also work in conjunction with my therapist. all in all, a very good support system.. for me.
sorry, i can't address your questions on weight, insulin, etc.
pulse
Posted by jealibeanz on May 27, 2006, at 19:01:15
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by pulse on May 27, 2006, at 15:08:59
Well then, I don't understand the advantage of transdermal vs. oral selegiline.
Posted by Phillipa on May 27, 2006, at 19:38:11
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by jealibeanz on May 27, 2006, at 19:01:15
Me either I thought it avoided all that mess? Love Phillipa and the high cost for what!!!!!!!
Posted by Iansf on May 27, 2006, at 19:42:07
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by pulse on May 27, 2006, at 15:08:59
Pulse,
You mention getting a better price through a compounding pharmacy. Can you say more about this? Does the compounding pharmacist simply take selegiline and put it onto skin patches of some sort? How much cheaper is it? Thanks.
Ian> sorry, but Emsam does NOT avoid the gut, far a GI problems. the pharmacist i dislike, of the 2 at my regular drugstore, was right, for once, when he predicted this could - and did happen - to me. oh, boy, did it ever!
>
> another pharmacist at a compounding pharmacy that i'd switched to for a better price on emsam, said same: of course, Emsam thru bloodstream only, can still cause GI problems. i sincerely hope this applies to GI problems/ meds intolerant (not treatment resistant) folks like me - only.
>
> pulse
Posted by jealibeanz on May 27, 2006, at 19:42:25
In reply to Re: Are Family Doctors prescribing EMSAM? » jealibeanz, posted by Phillipa on May 27, 2006, at 19:38:11
This doesn't make much sense to me. Surely, the patch was not created to people could wear a sticker instead of swallowing a pill.
Posted by Phillipa on May 27, 2006, at 21:02:31
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by jealibeanz on May 27, 2006, at 19:42:25
For more money? It makes no sense. Love Phillipa
Posted by yxibow on May 27, 2006, at 22:00:48
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by jealibeanz on May 27, 2006, at 19:42:25
> This doesn't make much sense to me. Surely, the patch was not created to people could wear a sticker instead of swallowing a pill.
No, it was created in hopes (I think) of avoiding severe MAOI problems, but in the end, as the monograph reads, that only is with the lowest dose with caveats to protect their behinds. When you need more than that, it does seem to me to be maybe not a zero sum gain but not much of a notch down from just generic selegeline (I think its generic now).
Posted by cecilia on May 28, 2006, at 0:59:05
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by yxibow on May 27, 2006, at 22:00:48
I think the goal with Emsam (besides making big bucks) was hopefully to decrease the MAO side effects and food interactions. No way of administration is going to completely eliminate them. People in the hospital getting pain meds via IV instead of orally still get GI side effects. Cecilia
Posted by pulse on May 28, 2006, at 18:05:08
In reply to Re: Are Family Doctors prescribing EMSAM? » pulse, posted by Iansf on May 27, 2006, at 19:42:07
No, sorry, I realized too late that my post might give folks the impression that you've now asked about.
It was just a coincidence that the lowest priced Emsam in my area happened to be at a compounding pharmacy. They did not compound my Emsam. The price there was still quite high at $427 for 30 of the lowest dose patches.
Perhaps it could be done with selegiline (?), but I did ask about compounding Wellbutrin, and the "active ingredient" i.e. (Wellbutrin itself) would still HAVE to remain - thus no help for the even more severe GI problems (than Emsam) that Wellbutrin causes me.
I would then have to assume compounding would not take away any of the bad side-effects that never diminish for some - like me- no matter what those particular side-effects are...if they are inherent to the med itself, and not from gelatin, binders. etc.
pulse
Posted by pulse on May 28, 2006, at 18:14:36
In reply to Re: Are Family Doctors prescribing EMSAM?, posted by cecilia on May 28, 2006, at 0:59:05
For me, though, when I've very rarely had to take antibiotics, my GP will order in a anti-biotic shot, administer that, and I have NO GI side-effects whatsoever...plus I'm virtually well in 3 days vs. the standard 10.
pulse
Posted by Donna Louise on May 29, 2006, at 6:43:17
In reply to Re: Are Family Doctors prescribing EMSAM? » cecilia, posted by pulse on May 28, 2006, at 18:14:36
It seems to me that I read somewhere that by transdermal delivery some of the unwanted type metabolites that result in first past gut metabolism in the liver are not created. Maybe one of the more amphetamine type metabolites?? I will see if I can find where I read that.
At any rate, for me, I have had no side effects from the patch, maybe I wouldn't from oral administration either. I guess another plus with transdermal delivery is the slow and steady plasma state. no ups and downs. What do I know, just that I like it. May need to go to 9mg though for more depression relief.Donna
Posted by crazy777girl on May 30, 2006, at 6:17:33
In reply to Re: Are Family Doctors prescribing EMSAM? » cecilia, posted by pulse on May 28, 2006, at 18:14:36
I think, in part, it (the Rx of transdermal delivery) may be the illusion (delusion?) that we are merely swallowing one less pill. Call me crazy.
A.> For me, though, when I've very rarely had to take antibiotics, my GP will order in a anti-biotic shot, administer that, and I have NO GI side-effects whatsoever...plus I'm virtually well in 3 days vs. the standard 10.
>
> pulse
Posted by SFY on May 30, 2006, at 10:38:05
In reply to delivery difference, posted by Donna Louise on May 29, 2006, at 6:43:17
> It seems to me that I read somewhere that by transdermal delivery some of the unwanted type metabolites that result in first past gut metabolism in the liver are not created. Maybe one of the more amphetamine type metabolites?? I will see if I can find where I read that.
> At any rate, for me, I have had no side effects from the patch, maybe I wouldn't from oral administration either. I guess another plus with transdermal delivery is the slow and steady plasma state. no ups and downs. What do I know, just that I like it. May need to go to 9mg though for more depression relief.
>
> DonnaI posted this below in another thread that may have been overlooked:
EMSAM does deliver selegiline directly into the blood thereby significantly reducing its exposure to the GI tract. But because blood flows to all internal organs including the liver, intestines, and stomach there will be some selegiline exposure which explains why some people are having GI tract-related side effects.
According to one study:
Transdermal delivery of selegiline provides several pharmacological advantages over oral delivery. First, it sufficiently reduces exposure of the gastrointestinal tract to the drug to limit inhibition of intestinal MAOA activity. Thus, adequate gastrointestinal MAOA enzyme is left
intact to metabolize dietary tyramine. Second, transdermal administration of selegiline circumvents first-pass hepatic metabolism, which results in sustained high plasma levels of the parent compound with a concomitant decrease in metabolite formation. This provides sufficient brain concentrations of selegiline to produce an antidepressant effect, presumably involving substantial MAOA as well as MAOB inhibition. This also may permit the expression of additional pharmacological properties of selegiline other than MAO inhibition previously observed in vitro. At the same time, there is less exposure to L-methamphetamine and L-amphetamine metabolites than observed with oral selegiline.http://ajp.psychiatryonline.org/cgi/content/full/159/11/1869
The EMSAM drug insert clearly states that at least 1 in 100 users may experience GI-related side effects such as "Constipation, flatulence, anorexia, gastroenteritis, vomiting."
Posted by Iansf on May 30, 2006, at 11:53:05
In reply to Re: delivery difference, posted by SFY on May 30, 2006, at 10:38:05
Again, my question: wouldn't sublingual delivery work in the equivalent manner? Liquid forms of selegiline meant for sublingual delivery are available. If 6mg of selegiline delivered suglingually turns out to be equivalent to 6mg delivered transdermally, then what you achieve with Emsam can be achieved at less than a sixth the price with liquid preparations. This may not be an issue for those whose insurance pays for Emsam, but it is for those of us without insurance.
So does anyone know if 6mg suglingual and 6mg transdermal are equivalent? (And please forget 6mg oral - I know that's not equivalent, and that's not part of the question.) Thanks.
Ian
> > It seems to me that I read somewhere that by transdermal delivery some of the unwanted type metabolites that result in first past gut metabolism in the liver are not created. Maybe one of the more amphetamine type metabolites?? I will see if I can find where I read that.
> > At any rate, for me, I have had no side effects from the patch, maybe I wouldn't from oral administration either. I guess another plus with transdermal delivery is the slow and steady plasma state. no ups and downs. What do I know, just that I like it. May need to go to 9mg though for more depression relief.
> >
> > Donna
>
> I posted this below in another thread that may have been overlooked:
>
> EMSAM does deliver selegiline directly into the blood thereby significantly reducing its exposure to the GI tract. But because blood flows to all internal organs including the liver, intestines, and stomach there will be some selegiline exposure which explains why some people are having GI tract-related side effects.
>
> According to one study:
>
> Transdermal delivery of selegiline provides several pharmacological advantages over oral delivery. First, it sufficiently reduces exposure of the gastrointestinal tract to the drug to limit inhibition of intestinal MAOA activity. Thus, adequate gastrointestinal MAOA enzyme is left
> intact to metabolize dietary tyramine. Second, transdermal administration of selegiline circumvents first-pass hepatic metabolism, which results in sustained high plasma levels of the parent compound with a concomitant decrease in metabolite formation. This provides sufficient brain concentrations of selegiline to produce an antidepressant effect, presumably involving substantial MAOA as well as MAOB inhibition. This also may permit the expression of additional pharmacological properties of selegiline other than MAO inhibition previously observed in vitro. At the same time, there is less exposure to L-methamphetamine and L-amphetamine metabolites than observed with oral selegiline.
>
> http://ajp.psychiatryonline.org/cgi/content/full/159/11/1869
>
> The EMSAM drug insert clearly states that at least 1 in 100 users may experience GI-related side effects such as "Constipation, flatulence, anorexia, gastroenteritis, vomiting."
>
>
Posted by yxibow on May 30, 2006, at 13:50:34
In reply to Re: delivery difference, posted by Iansf on May 30, 2006, at 11:53:05
Sublingual and orally disintegrating pills merely make them easier to swallow in an oral method -- they still pass through your mouth, the esophagus, and the GI tract and eventually the liver or kidney system depending on the drug.
Remeron e.g. has a orally disintegrating preparation, or it did at one time.]
Frequently you see Zinc and Vitamin C sublingual tablets for colds (which typically through studies only cut a day off one at best), and they dissolve in anywhere from 5-15 minutes at most.
Posted by Jakeman on May 30, 2006, at 20:01:48
In reply to Re: delivery difference, posted by Iansf on May 30, 2006, at 11:53:05
Good question. So far I have not seen any studies comparing sublingual and transdermal delivery. Maybe do an experiment? Emsam is outrageously expensive. But Squibb is pushing it and you can probably get a two week sample supply from your medical professional. I'm cutting the patch in half for now so maybe a months supply for some people. Might be a worthwhile trial.
good luck, Jake
> Again, my question: wouldn't sublingual delivery work in the equivalent manner? Liquid forms of selegiline meant for sublingual delivery are available. If 6mg of selegiline delivered suglingually turns out to be equivalent to 6mg delivered transdermally, then what you achieve with Emsam can be achieved at less than a sixth the price with liquid preparations. This may not be an issue for those whose insurance pays for Emsam, but it is for those of us without insurance.
>
> So does anyone know if 6mg suglingual and 6mg transdermal are equivalent? (And please forget 6mg oral - I know that's not equivalent, and that's not part of the question.) Thanks.
>
> Ian
>
> > > It seems to me that I read somewhere that by transdermal delivery some of the unwanted type metabolites that result in first past gut metabolism in the liver are not created. Maybe one of the more amphetamine type metabolites?? I will see if I can find where I read that.
> > > At any rate, for me, I have had no side effects from the patch, maybe I wouldn't from oral administration either. I guess another plus with transdermal delivery is the slow and steady plasma state. no ups and downs. What do I know, just that I like it. May need to go to 9mg though for more depression relief.
> > >
> > > Donna
> >
> > I posted this below in another thread that may have been overlooked:
> >
> > EMSAM does deliver selegiline directly into the blood thereby significantly reducing its exposure to the GI tract. But because blood flows to all internal organs including the liver, intestines, and stomach there will be some selegiline exposure which explains why some people are having GI tract-related side effects.
> >
> > According to one study:
> >
> > Transdermal delivery of selegiline provides several pharmacological advantages over oral delivery. First, it sufficiently reduces exposure of the gastrointestinal tract to the drug to limit inhibition of intestinal MAOA activity. Thus, adequate gastrointestinal MAOA enzyme is left
> > intact to metabolize dietary tyramine. Second, transdermal administration of selegiline circumvents first-pass hepatic metabolism, which results in sustained high plasma levels of the parent compound with a concomitant decrease in metabolite formation. This provides sufficient brain concentrations of selegiline to produce an antidepressant effect, presumably involving substantial MAOA as well as MAOB inhibition. This also may permit the expression of additional pharmacological properties of selegiline other than MAO inhibition previously observed in vitro. At the same time, there is less exposure to L-methamphetamine and L-amphetamine metabolites than observed with oral selegiline.
> >
> > http://ajp.psychiatryonline.org/cgi/content/full/159/11/1869
> >
> > The EMSAM drug insert clearly states that at least 1 in 100 users may experience GI-related side effects such as "Constipation, flatulence, anorexia, gastroenteritis, vomiting."
> >
> >
>
>
Posted by Jakeman on May 30, 2006, at 21:34:12
In reply to Re: delivery difference » Iansf, posted by Jakeman on May 30, 2006, at 20:01:48
Another thought..maybe a compounding pharmacy could provide a patch for selegiline. A court case this week seems to have gotten the FDA off their backs. I'm a layman, but it appears to be an old, well tested drug with many benefits. And now we have a new method of delivery that may work better.
http://www.upi.com/HealthBusiness/view.php?StoryID=20060526-014622-8737r
Posted by Donna Louise on May 30, 2006, at 22:02:43
In reply to Re: delivery difference, posted by Iansf on May 30, 2006, at 11:53:05
> Again, my question: wouldn't sublingual delivery work in the equivalent manner? Liquid forms of selegiline meant for sublingual delivery are available. If 6mg of selegiline delivered suglingually turns out to be equivalent to 6mg delivered transdermally, then what you achieve with Emsam can be achieved at less than a sixth the price with liquid preparations. This may not be an issue for those whose insurance pays for Emsam, but it is for those of us without insurance.
>
> So does anyone know if 6mg suglingual and 6mg transdermal are equivalent? (And please forget 6mg oral - I know that's not equivalent, and that's not part of the question.) Thanks.
>
> Ian
>
> > > It seems to me that I read somewhere that by transdermal delivery some of the unwanted type metabolites that result in first past gut metabolism in the liver are not created. Maybe one of the more amphetamine type metabolites?? I will see if I can find where I read that.
> > > At any rate, for me, I have had no side effects from the patch, maybe I wouldn't from oral administration either. I guess another plus with transdermal delivery is the slow and steady plasma state. no ups and downs. What do I know, just that I like it. May need to go to 9mg though for more depression relief.
> > >
> > > Donna
> >
> > I posted this below in another thread that may have been overlooked:
> >
> > EMSAM does deliver selegiline directly into the blood thereby significantly reducing its exposure to the GI tract. But because blood flows to all internal organs including the liver, intestines, and stomach there will be some selegiline exposure which explains why some people are having GI tract-related side effects.
> >
> > According to one study:
> >
> > Transdermal delivery of selegiline provides several pharmacological advantages over oral delivery. First, it sufficiently reduces exposure of the gastrointestinal tract to the drug to limit inhibition of intestinal MAOA activity. Thus, adequate gastrointestinal MAOA enzyme is left
> > intact to metabolize dietary tyramine. Second, transdermal administration of selegiline circumvents first-pass hepatic metabolism, which results in sustained high plasma levels of the parent compound with a concomitant decrease in metabolite formation. This provides sufficient brain concentrations of selegiline to produce an antidepressant effect, presumably involving substantial MAOA as well as MAOB inhibition. This also may permit the expression of additional pharmacological properties of selegiline other than MAO inhibition previously observed in vitro. At the same time, there is less exposure to L-methamphetamine and L-amphetamine metabolites than observed with oral selegiline.
> >
> > http://ajp.psychiatryonline.org/cgi/content/full/159/11/1869
> >
> > The EMSAM drug insert clearly states that at least 1 in 100 users may experience GI-related side effects such as "Constipation, flatulence, anorexia, gastroenteritis, vomiting."
> >
> >
>
>regardless of the origin of absorbtion, 6mg EMSAM is equal to 20mg of selegiline as oppossed to 6mg of sublingual selegiline. so it is at least not equal in terms of selectivity. AT 20mgs it is not selective and inhibits MAO-A and B. At 6mg it only deanimates MAO-B, generally not useful as an antidepressant in that case. The substitution would fail for me.
Donna
Posted by Iansf on May 31, 2006, at 1:11:35
In reply to Re: delivery difference » Iansf, posted by Jakeman on May 30, 2006, at 20:01:48
> Good question. So far I have not seen any studies comparing sublingual and transdermal delivery. Maybe do an experiment? Emsam is outrageously expensive. But Squibb is pushing it and you can probably get a two week sample supply from your medical professional. I'm cutting the patch in half for now so maybe a months supply for some people. Might be a worthwhile trial.
>
> good luck, Jake
>
Unfortunately my medical professional is at a city clinic and the Squibb reps won't give Emsam samples to the clinic. They give samples only to doctors who are likely to prescribe it, which the clinic doctors aren't because Emsam is not on the city formulary. Not that I blame the city - with resources for public health stretched extremely thin, I can see why it wants to avoid paying for $400 a month medicines if it doesn't absolutely have to.
Posted by Jakeman on June 3, 2006, at 13:28:43
In reply to Re: delivery difference, posted by Iansf on May 31, 2006, at 1:11:35
Iansf,
Squibb has a patient assistance program:
http://www.bmspaf.org/A few posters on anxietyhelp.org have been approved for Emsam.
warm regards, Jake
> Unfortunately my medical professional is at a city clinic and the Squibb reps won't give Emsam samples to the clinic. They give samples only to doctors who are likely to prescribe it, which the clinic doctors aren't because Emsam is not on the city formulary. Not that I blame the city - with resources for public health stretched extremely thin, I can see why it wants to avoid paying for $400 a month medicines if it doesn't absolutely have to.
Posted by Last Chance on June 3, 2006, at 14:32:28
In reply to Re: delivery difference, posted by Iansf on May 31, 2006, at 1:11:35
Iansf - if you want to take Emsam give the patient assistance program a try - just download the form on their website - fill out your part, and ask your doc if he or she would just fill in their little part - it is very short, easy (I hate paperwork) and have doc fax in. It can't hurt - it took about 5 weeks, but I got a free 3 mos. supply of the 6mg, with approval for 11 mos. if it is working for me. After that I don't know, but one day at a time. I have been cutting in half for a week, but today I stuck on the full patch. I am still optimistic, but guarded. Richard
Posted by Jakeman on June 3, 2006, at 16:03:49
In reply to Squibb Patient Assistance - Iansf, posted by Last Chance on June 3, 2006, at 14:32:28
Here's a link to the application:
http://www.needymeds.com/papforms/brispa0042.pdf
> Iansf - if you want to take Emsam give the patient assistance program a try - just download the form on their website - fill out your part, and ask your doc if he or she would just fill in their little part - it is very short, easy (I hate paperwork) and have doc fax in. It can't hurt - it took about 5 weeks, but I got a free 3 mos. supply of the 6mg, with approval for 11 mos. if it is working for me. After that I don't know, but one day at a time. I have been cutting in half for a week, but today I stuck on the full patch. I am still optimistic, but guarded. Richard
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