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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 25 of 41. This is the beginning of the thread.
Posted by ed_uk on February 12, 2005, at 20:25:09
The blockade of serotonin (5-HT) and norepinephrine (NE) transporters in vitro and in vivo by the dual 5-HT/NE reuptake inhibitors duloxetine and venlafaxine was compared. Duloxetine inhibited binding to the human NE and 5-HT transporters with K(i) values of 7.5 and 0.8 nM, respectively, and with a K(i) ratio of 9. Venlafaxine inhibited binding to the human NE and 5-HT transporters with K(i) values of 2480 and 82 nM, respectively, and with a K(i) ratio of 30.
'Of particular interest were the findings that paroxetine, generally thought of as a selective serotonin transporter antagonist, possesses moderately high affinity for the norepinephrine transporter and that venlafaxine, which has been described as a "dual uptake inhibitor", possesses weak affinity for the norepinephrine transporter.'
Lol, so Effexor's basically an SSRI after all!
Ed.
Posted by ed_uk on February 12, 2005, at 20:34:24
In reply to Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 20:25:09
>with a K(i) ratio of 30
>Lol, so Effexor's basically an SSRI after all!OK, maybe not quite an SSRI!
Ed.
Posted by ed_uk on February 12, 2005, at 20:38:42
In reply to Re: Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 20:34:24
>OK, maybe not quite an SSRI!
Calling it a 'dual reuptake inhibitor' is stretching it though.
Ed.
Posted by ed_uk on February 12, 2005, at 20:45:52
In reply to Re: Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 20:38:42
Wyeth states that Effexor is a potent inhibitor of serotonin AND norepinephrine reuptake.
Is this justified? .......or have they wondered into the land of fantasy?
Ed.
Posted by Nixon on February 12, 2005, at 20:48:50
In reply to Re: Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 20:45:52
Sounds like fantasy. Cymbalta is crap too. Hey Ed where's my advice?
Posted by ed_uk on February 12, 2005, at 20:50:12
In reply to Re: Effexor: Marketing Ploy, posted by Nixon on February 12, 2005, at 20:48:50
PS. Venlafaxine and its major metabolite ODV are very similar with respect to their overall action on neurotransmitter reuptake.
Ed.
Posted by flmm on February 12, 2005, at 20:54:36
In reply to Re: Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 20:50:12
All I know is it did not feel like any ssri i have taken. Very activating for me, I am assuming due to NE effect.
Posted by ed_uk on February 12, 2005, at 21:02:35
In reply to Re: Effexor: Marketing Ploy, posted by flmm on February 12, 2005, at 20:54:36
Hi,
Yes, it does seem to be different to SSRIs for some people, it also appears to be somewhat more effective overall. For me, it might as well have been an SSRI.
Ed.
Posted by Phillipa on February 12, 2005, at 21:07:29
In reply to Re: Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 21:02:35
Hi Ed! So, is cymbalta an SSRI too? It did nothing to me. Fondly, Phillipa O
PS I think this computer has had it. It isn't even allowing me to type without hesitating. I'll be VERY upset if I'm without one!
Posted by ed_uk on February 12, 2005, at 21:15:04
In reply to Re: Effexor: Marketing Ploy » ed_uk, posted by Phillipa on February 12, 2005, at 21:07:29
Hi,
>So, is cymbalta an SSRI too?
No :-) Effexor isn't really an SSRI either, I was just commenting on the fact that it has a much greater effect on 5-HT reuptake than on NE reuptake.
Ed xx
Posted by TheOutsider on February 13, 2005, at 5:20:27
In reply to Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 20:25:09
> The blockade of serotonin (5-HT) and norepinephrine (NE) transporters in vitro and in vivo by the dual 5-HT/NE reuptake inhibitors duloxetine and venlafaxine was compared. Duloxetine inhibited binding to the human NE and 5-HT transporters with K(i) values of 7.5 and 0.8 nM, respectively, and with a K(i) ratio of 9. Venlafaxine inhibited binding to the human NE and 5-HT transporters with K(i) values of 2480 and 82 nM, respectively, and with a K(i) ratio of 30.
It is interesting that Duloxetine is so skewed towards seratonin.
I suspected that it didn't have a very significant effect on norepinephrine compared to seratonin because so many people experienced apathy on it!Apparently a drug called Milnicpran (hope I got the name right) is a much more balanced re-uptake inhibitor of both norepinephrine and seratonin.
It is available in most of mainland Europe, but not in the US, Canada or UK.
I wonder why not the UK? Dulouxetine was aproved in the UK almost strait away! Sometimes I hate this country!
Posted by ed_uk on February 13, 2005, at 8:05:56
In reply to What we need is Milnicpran!, posted by TheOutsider on February 13, 2005, at 5:20:27
Hi TheOutsider!
Yes, milnacipran is supposed to be much more 'balanced'.
>I wonder why not the UK?
Milnacipran seems to be available in France, Austria, Portugal, Finland and Argentina. I'm not sure about anywhere else. I'm honestly not sure why it wasn't approved in the UK.
>Sometimes I hate this country!
Lol, me too! It's a shame that more people on p-babble haven't been able to try milnacipran, we hear so little about it that it's difficult to form an opinion. There could be something nasty about it that we don't know about yet!
Ed.
Posted by Nixon on February 13, 2005, at 9:39:12
In reply to Re: Effexor: Marketing Ploy, posted by ed_uk on February 12, 2005, at 21:15:04
Hey Ed,
Can you run some numbers and convince me that Depakote is an AD?lol Just kidding. By the way, I think I am going with Trileptal. Does it have the same effect as Tegretol regarding diminishing Depakote and vice versa. Thanks-JN
Posted by ed_uk on February 13, 2005, at 10:12:55
In reply to Re: Effexor: Marketing Ploy » ed_uk, posted by Nixon on February 13, 2005, at 9:39:12
Hi,
Depakote sometimes produces a slight reduction in the plasma concentration of an active metabolite of Trileptal. Trileptal does not produce any significant change in the plasma concentration of valproate (Depakote). I don't think you need to worry about Depakote interacting with Trileptal. You might notice some increased side effects while you're on Depakote and Trileptal, drowsiness/cognitive impairment may be a problem, don't drive unless you're sure you're up to it.
Have you asked your doctor to let you try Trileptal? What does s/he say? Are you going to add Trileptal while you're still taking Depakote and then withdraw the Depakote when you're on a therapeutic dose of Trileptal? Perhaps you could reduce the Depakote to 125mg/day before stopping it completely.
Ed.
Posted by Nixon on February 13, 2005, at 10:24:15
In reply to Re: Effexor: Marketing Ploy » Nixon, posted by ed_uk on February 13, 2005, at 10:12:55
Hey Ed,
Your reduction method makes sense. My Pdoc after a year of conditioning by me basically gives me an open script book. She knows I don't overdue it and although I am not at your level with knowledge she respects what I know from experience and read. Let's say I add trileptal and reduce Depakote to 125, what dose of trileptal do you think would be a good starter so I don't have to look it up. PS. a thought I have been chewing on also today is going to 5mg valium 2x/day = 25mg librium for a lib washout. I currently take 20mg lib and will always want a low dose benzo. Any thoughts? Thanks. John
Posted by ed_uk on February 13, 2005, at 10:52:11
In reply to Re: Effexor: Marketing Ploy » ed_uk, posted by Nixon on February 13, 2005, at 10:24:15
Hi,
I would suggest that you start Trileptal at a dose of one 150mg tablet twice daily (every 12 hours, morning and evening). This is lower than the starting dose recommended for epilepsy (300mg twice daily).
I think you should start at a low dose for several reasons........
1) You have responded to a low dose of Depakote, a small dose of Trileptal may be sufficient.
2) You are still taking Depakote and want to minimise side effects.
3) You do not have epilepsy, the official dosing guidelines are for epilepsy.>going to 5mg valium 2x/day = 25mg librium for a lib washout.
I thought you were happy with Librium, why do you want to take Valium instead?
>Let's say I add trileptal and reduce Depakote to 125.
Do you take controlled release Depakote?
Ed.
Posted by Nixon on February 13, 2005, at 10:59:54
In reply to Re: Trileptal » Nixon, posted by ed_uk on February 13, 2005, at 10:52:11
Hey Ed,
I wrote down the Trileptal dosage to show let my doc know, it makes sense. I do take the ER version of Depakote. As for the librium, I like it and if I switch I will go back. I was thinking maybe the lib would be more effective with a brief( had in mind 4 to 8 weeks) washout. Maybe I should leave it alone. JN
Posted by linkadge on February 13, 2005, at 11:43:05
In reply to Re: Trileptal » ed_uk, posted by Nixon on February 13, 2005, at 10:59:54
The TCA's are probably the most ballenced uptake inhibitors we have.
I think Amitriptaline is the most ballenced.
Linkadge
Posted by ed_uk on February 13, 2005, at 11:48:40
In reply to Re: Trileptal » ed_uk, posted by Nixon on February 13, 2005, at 10:59:54
Hi,
>I wrote down the Trileptal dosage to show let my doc know, it makes sense.
The 150mg tablets are scored so you can cut them in half. If you get any side effects at 150mg twice daily you could reduce the dose for a few days and then increase when you're ready.
>I do take the ER version of Depakote.
If you want to reduce your Depakote to 125mg/day, you'll need to get the Depakote immediate release 125mg tablets. You're not supposed to cut the Depakote ER tablets in half.
You would need to take half a Depakote 125mg tablet in the morning and the other half in the evening.
>I was thinking maybe the lib would be more effective with a brief( had in mind 4 to 8 weeks) washout.
You mean taking Valium for a few weeks and then going back to Librium? I honestly don't think it would be helpful, it wouldn't reduce you're benzo tolerance, Val and Lib are so similar.
Have you ever taken carbamazepine (Tegretol)? What effect did it have? What dose did you take?
Ed.
Posted by Nixon on February 13, 2005, at 12:03:59
In reply to Re: Trileptal » Nixon, posted by ed_uk on February 13, 2005, at 11:48:40
Ed,
Thanks. I could not cut the depakote er 250 in half with a sledgehammer. lol. I mean that coating is thick. Cutting Trileptal in half makes sense. Tegretol is one of 2 AED i have not taken. Tegretol, chemically related to Barbituate and similar in mechanism as Dilantin? Your benzo advice is interesting. Do you have anymore information regarding chemical relations or mechanisms between valium and librium? Thanks JN
Posted by ed_uk on February 13, 2005, at 12:35:47
In reply to Re: Trileptal, posted by Nixon on February 13, 2005, at 12:03:59
Hi,
>I could not cut the depakote er 250 in half with a sledgehammer. lol. I mean that coating is thick.
Lol, Really? We don't have Depakote ER in the UK, we've got Epilim Chrono though which is similar.
>Tegretol, chemically related to Barbituate and similar in mechanism as Dilantin?
Tegretol has more in common with Trileptal than any other drug. Tegretol is not chemically related to the barbiturates, Dilantin on the other hand is structurally similar to phenobarbital. What was your experience with Dilantin? What dose did you take?
>Do you have anymore information regarding chemical relations or mechanisms between valium and librium?
I'm not really sure what you're looking for!
Chemical relations........
Here is a picture of the chlordiazepoxide molecule: (scroll down to the bottom of the page)
http://www.psychotropics.dk/usr_view_molecule.asp?ID=1405&historyline=&backurl=%2Fdefault%2Easp%3FSearchword%3Dchlordiazepoxide%26Searchtype%3DAll&backurlname=Search+Result&Catalogtype=AHere is a picture of diazepam:
http://www.psychotropics.dk/usr_view_molecule.asp?ID=1406&historyline=&backurl=%2Fdefault%2Easp%3FSearchword%3Ddiazepam%26Searchtype%3DAll&backurlname=Search+Result&Catalogtype=ADiazepam and chlordiazepoxide are thought to have the same mechanism of action. Diazepam and chlordiazepoxide are both metabolised to desmethyldiazepam, an active metabolite.
Ed.
Posted by Nixon on February 13, 2005, at 16:46:57
In reply to Re: Trileptal » Nixon, posted by ed_uk on February 13, 2005, at 12:35:47
Thanks Ed,
Yep the depakote er tablet is hard to describe. It is heavy and almost solid. It's as if the oval shaped tablet has bee solidified like a stone. Yes, i took Dilantin for about 4 weeks. I was on the Dreyfus method trial. Anyway, it does have some calming properties but it effects EVERYTHING. Serotonin, norepinephrine, dopamine, cortisol, and many others. I read the book A Remarkable Medicine Has Been Overlooked By Dreyfus. I would take it if there was nothing else but it just is not a reliable mood stabilizer. It washes remeron out of your system in half the time, it pushes a benzo out while it increases itself. It can be usefull but the feeling is just not consistent, I wish it was. An ssri also makes it move. I get the picture regarding valium. I guess I will just stay with lib. I really wish Dilantin was as remarkable for me as it was for Dreyfus. The best way to sum it up is that it effects everything a little but if you need a drug for a certain condition it will interact unreliably with Phenytoin.JN
Posted by Nixon on February 14, 2005, at 18:12:00
In reply to Re: Trileptal » ed_uk, posted by Nixon on February 13, 2005, at 16:46:57
Hey Ed,
I went the my PDoc today and after exchanging ideas came to the conclusion to wait a few weeks before starting Trileptal. Since it has been only around 3 weeks since I resumed Prozac I thought the best indicator would be to wait a few more weeks to see if Prozac re-kicks, I did get a script for valium though, 5mgx2pday. I'll pick it up tommorow after work. Unsure yet as to whether i will switch from librium to it or not for a wash. Nice to have though to add to my potential reserve. What's your regimen? JN
Posted by Nixon on February 14, 2005, at 18:17:06
In reply to Re: Trileptal » Nixon, posted by ed_uk on February 13, 2005, at 12:35:47
I posted to myself. What a genius.
Posted by ed_uk on February 15, 2005, at 8:32:08
In reply to Re: Trileptal » Nixon, posted by Nixon on February 14, 2005, at 18:12:00
Hi JN,
>Since it has been only around 3 weeks since I resumed Prozac I thought the best indicator would be to wait a few more weeks to see if Prozac re-kicks.
Good idea! I didn't know you'd just restarted the Prozac. It's generally best not to make too many changes to your medication all at once because you can easily end up having no idea which meds are helping, which are not and which are causing side effects!
>I did get a script for valium though, 5mgx2pday
10mg/day of Valium is often said to be approximately equivalent to 30mg/day Librium. This is only a guide though, the only way to see how it'll affect you is to try it.
>What's your regimen?
I just take 140mg/day lofepramine at the moment.
Keep posting :-)
Ed.
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