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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 7 to 31 of 69. Go back in thread:
Posted by e503 on May 20, 2003, at 9:42:21
In reply to Re: abilify/trileptal/zoloft » e503, posted by Ritch on May 19, 2003, at 21:32:53
> > > > > > I weaned Ben off of trileptal, which he had been on since february. I realized now that was activated by it, as now he is actually VERY sedate. TOO sedate. So, my question is this: he is taking abilify 10 mg./day - split into an a.m. and p.m. dose (he seems to need this). He has been taking zoloft and buspar for a long time also. About a year or more ago he had a very rough time, and I forget who it was (ritch, maybe???) who helped me figure out what was up. It turned out we had been giving ben his zoloft (75 mg/day) at bedtiime. During the day he was wild. As soon as we switched it to a daytime dose, it calmed him down. SOOOO, now he is taking the abilify, zoloft and buspar in the a.m. and he seems somewhat sedate, not his usual somewhat "perky" (hypomanic?) self. I am wondering if abilify and zoloft interact somehow to cause this sedatedness? Maybe I should try giving him all the zoloft in the p.m.? Ben is autistic and cannot tell me how he feels, although I can tell my looking at him that he is just not "right". Does anyone take this combination?
> > > > > > thanks,
> > > > > > elise
> > > > > > Thanks for all responses.
> > > > >
> > > > >
> > > > > Trileptal had an stabiizing/energizing quality to it that I liked-the damn stuff just made me uncontrollably nauseous! Maybe he just needed a *lower* dose of Trileptal instead?
> > > > >
> > > >
> > > > last night when i just gave him 150 mg. he got agitated and more obsessed!
> > >
> > > Did you give him his 10mg Abilify dose at the same time you tried the Trileptal? If so, it could have been the Abilify-or some other med. Just a quick question: Is his doctor allowing you fairly wide latitude on fine-tuning his meds (since he is autistic-and doesn't communicate well how he is feeling)? I guess I am just wondering how you have that all worked out. Some docs are more uptight than others about this thing. My pdoc is very patient and gives me fairly wide latitude. Just wondering.
> >
> > Ben has been real agitated since beginning of february when we had to switch from tegretol (low wbc)to trileptal. I thought it may have been just getting used to the meds....but it continued until we started the abilify.....everything just makes too much sense to think it is anything other than trileptal. I have been working with my pdoc for a long time (maybe 5 years?). I do call him and tell him when I see problems. Ben is typically a very fun loving (he is verbal) child- class clown....loves I love lucy, three stooges, etc. When I see him looking "out of it" and/or he gets aggressive/ocd I know something is not right. Too bad he was doing ok on the tegretol for a long time.
> > I spoke to the pdoc after I spoke to his teacher this afternoon (she said he was very lethargic)and he told me to stop the trileptal and cut the abilify to 7.5 (5 during the day and 2.5 p.m.). I hope this helps and I get my kid back.
> > elise
>
> Oh, thanks, that makes things a lot clearer to me. There *are* differences between Tegretol and Trileptal. It may be that it is hyped a little too much as being a perfect(safer) Tegretol replacement, when that may not be the case for everybody (efficaciousness-wise). I tried Tegretol a long, long time ago (as a lithium switch) and it didn't seem to help me, but I was in the middle of a bigtime depression and didn't have the time to burn to figure out why I was feeling worse (or to have the patience for the Tegretol to "kickin"). Interesting that his pdoc wants to cut the Abilify down-I wonder what his reasoning there is?? did he say..The pdoc wants to cut the abilify down because ben is a zombie. Yesterday was not great either, as ben was acting like I have never seen before. He was very obsessive (goal driven???) but not as agitated, it was almost as if his brain was manic, but he wasn't. It's hard to explain. I am thinking that maybe the abilify IS at too high a dose---and maybe it is causinig this? So.....I decreased it even more (2.5 mg. 2 x a day instead of 5 mg. 2 a day) to see what happens. I know abilify has a long half life, when do you th ink I might see any difference at the lower level? Do you think the abilify is causing this "driveness"? Is this mania?
thanks,
elise
Posted by Ritch on May 20, 2003, at 11:33:14
In reply to Re: abilify/trileptal/zoloft » Ritch, posted by e503 on May 20, 2003, at 9:42:21
> > > > > > > I weaned Ben off of trileptal, which he had been on since february. I realized now that was activated by it, as now he is actually VERY sedate. TOO sedate. So, my question is this: he is taking abilify 10 mg./day - split into an a.m. and p.m. dose (he seems to need this). He has been taking zoloft and buspar for a long time also. About a year or more ago he had a very rough time, and I forget who it was (ritch, maybe???) who helped me figure out what was up. It turned out we had been giving ben his zoloft (75 mg/day) at bedtiime. During the day he was wild. As soon as we switched it to a daytime dose, it calmed him down. SOOOO, now he is taking the abilify, zoloft and buspar in the a.m. and he seems somewhat sedate, not his usual somewhat "perky" (hypomanic?) self. I am wondering if abilify and zoloft interact somehow to cause this sedatedness? Maybe I should try giving him all the zoloft in the p.m.? Ben is autistic and cannot tell me how he feels, although I can tell my looking at him that he is just not "right". Does anyone take this combination?
> > > > > > > thanks,
> > > > > > > elise
> > > > > > > Thanks for all responses.
> > > > > >
> > > > > >
> > > > > > Trileptal had an stabiizing/energizing quality to it that I liked-the damn stuff just made me uncontrollably nauseous! Maybe he just needed a *lower* dose of Trileptal instead?
> > > > > >
> > > > >
> > > > > last night when i just gave him 150 mg. he got agitated and more obsessed!
> > > >
> > > > Did you give him his 10mg Abilify dose at the same time you tried the Trileptal? If so, it could have been the Abilify-or some other med. Just a quick question: Is his doctor allowing you fairly wide latitude on fine-tuning his meds (since he is autistic-and doesn't communicate well how he is feeling)? I guess I am just wondering how you have that all worked out. Some docs are more uptight than others about this thing. My pdoc is very patient and gives me fairly wide latitude. Just wondering.
> > >
> > > Ben has been real agitated since beginning of february when we had to switch from tegretol (low wbc)to trileptal. I thought it may have been just getting used to the meds....but it continued until we started the abilify.....everything just makes too much sense to think it is anything other than trileptal. I have been working with my pdoc for a long time (maybe 5 years?). I do call him and tell him when I see problems. Ben is typically a very fun loving (he is verbal) child- class clown....loves I love lucy, three stooges, etc. When I see him looking "out of it" and/or he gets aggressive/ocd I know something is not right. Too bad he was doing ok on the tegretol for a long time.
> > > I spoke to the pdoc after I spoke to his teacher this afternoon (she said he was very lethargic)and he told me to stop the trileptal and cut the abilify to 7.5 (5 during the day and 2.5 p.m.). I hope this helps and I get my kid back.
> > > elise
> >
> > Oh, thanks, that makes things a lot clearer to me. There *are* differences between Tegretol and Trileptal. It may be that it is hyped a little too much as being a perfect(safer) Tegretol replacement, when that may not be the case for everybody (efficaciousness-wise). I tried Tegretol a long, long time ago (as a lithium switch) and it didn't seem to help me, but I was in the middle of a bigtime depression and didn't have the time to burn to figure out why I was feeling worse (or to have the patience for the Tegretol to "kickin"). Interesting that his pdoc wants to cut the Abilify down-I wonder what his reasoning there is?? did he say..
>
> The pdoc wants to cut the abilify down because ben is a zombie. Yesterday was not great either, as ben was acting like I have never seen before. He was very obsessive (goal driven???) but not as agitated, it was almost as if his brain was manic, but he wasn't. It's hard to explain. I am thinking that maybe the abilify IS at too high a dose---and maybe it is causinig this? So.....I decreased it even more (2.5 mg. 2 x a day instead of 5 mg. 2 a day) to see what happens. I know abilify has a long half life, when do you th ink I might see any difference at the lower level? Do you think the abilify is causing this "driveness"? Is this mania?
> thanks,
> elise
It is good that "physically" he isn't agitated and restless, and he is "quiet"-so it doesn't "sound" like mania. I've rarely experienced racing thoughts without also being physically agitated as well. You're picking up on something though.. maybe he is over-focused on one particular thing.. possibly over-sedated on the Abilify as well. It does have a long half-life. It may take a week or longer for the drug's level to reach a steady state. That's one thing I don't like about meds with lengthy half-lives like that--you don't see the response of a dose change for a long time-- and the longer the time goes by the easier it is to confuse with "typical" mood-cycling patterns.
Posted by e503 on May 20, 2003, at 14:10:33
In reply to Re: abilify/trileptal/zoloft » Ritch, posted by e503 on May 20, 2003, at 9:42:21
ben's school called today and said he was terribly "non-compliant" and belligerent....which up until the last weeks or so we have not ever seen before. What is this? Could this be mania or something from the abilify? called the pdoc and he said to wait a few days at the lower dose. He is not lethargic at school anymore! (since I lowered the abilify dose).
Posted by Ritch on May 20, 2003, at 22:38:09
In reply to ABILIFY HELP, posted by e503 on May 20, 2003, at 14:10:33
> ben's school called today and said he was terribly "non-compliant" and belligerent....which up until the last weeks or so we have not ever seen before. What is this? Could this be mania or something from the abilify? called the pdoc and he said to wait a few days at the lower dose. He is not lethargic at school anymore! (since I lowered the abilify dose).
>It sounds like a dysphoric hostility thing to me. He sounds grouchy and stubborn. Could be he is coming out of the "zombie" state he was in and this might be a rebound of sorts. I've had definite "rebound" effects from slowing-stopping antipsychotics in the past, but I tended to get more uptight and agitated instead of angry-although I was prescribed Thorazine because of temper flares.... He might level out OK when he readjusts to the lower dose.
Posted by e503 on May 21, 2003, at 9:18:44
In reply to Re: ABILIFY HELP » e503, posted by Ritch on May 20, 2003, at 22:38:09
Interestingly, about 9:00 last night Ben seemed to be his "old" self again. I gave him the 2.5 mg. abilify about 10:00 and within a few minutes he was asleep.....It has also been more difficult to get him up in the a.m. Used to be he would get up around 7, but now he has to be woken at 8.
My question is this: Right now he is taking: 50 mg. zoloft a.m. and 2.5 mg. abilify; the teachers say in the a.m. at school he is compliant (I am guessing he may be too tired to fight!), after lunch he is "belligerent, etc.". After school I give him 25 mg. zoloft. He seemed difficult and sedated until about 9:00 p.m. I know that when we were having big troubles with ben's meds a year ago or so, you (I think it was you?) said something about zoloft's metabolites....since we were giving him all of it at night could be a problem. We, in turn, gave him the zoloft in the a.m. instead, and he was MUCH calmer and MUCH better. So, I would say that zoloft, in its active state (?) calms him,,,,SOOOOOOO...... I am playing around the how I could dose these meds... can it be that the abilify is decreasing out of his system later in the evening (since he didn't have a dose in 12 hours or more), and that's why his behavior is better (happier!!!!!) Or what?
sorry to ramble, but gotta figure this out.
thanks,
elise
Posted by Ritch on May 21, 2003, at 9:53:24
In reply to Re: ABILIFY HELP, posted by e503 on May 21, 2003, at 9:18:44
> Interestingly, about 9:00 last night Ben seemed to be his "old" self again. I gave him the 2.5 mg. abilify about 10:00 and within a few minutes he was asleep.....It has also been more difficult to get him up in the a.m. Used to be he would get up around 7, but now he has to be woken at 8.
>
> My question is this: Right now he is taking: 50 mg. zoloft a.m. and 2.5 mg. abilify; the teachers say in the a.m. at school he is compliant (I am guessing he may be too tired to fight!), after lunch he is "belligerent, etc.". After school I give him 25 mg. zoloft. He seemed difficult and sedated until about 9:00 p.m. I know that when we were having big troubles with ben's meds a year ago or so, you (I think it was you?) said something about zoloft's metabolites....since we were giving him all of it at night could be a problem. We, in turn, gave him the zoloft in the a.m. instead, and he was MUCH calmer and MUCH better. So, I would say that zoloft, in its active state (?) calms him,,,,SOOOOOOO...... I am playing around the how I could dose these meds... can it be that the abilify is decreasing out of his system later in the evening (since he didn't have a dose in 12 hours or more), and that's why his behavior is better (happier!!!!!) Or what?
> sorry to ramble, but gotta figure this out.
> thanks,
> elise
Elise, I think you are onto something there. Sure enough, the Abilify may be zoning him out a little (staying in bed later), but when it starts to wear off and the Zoloft has had some time in his system, it could start becoming activating later in the day. I definitely noticed this with Zoloft exclusively of all of the SSRI's I've tried. There is definitely a calming/tiring effect while it is kicking in for several hours, then a "speedy" secondary kick later on which often would make sleeping difficult for me. The only thing that doesn't seem to fit is giving him his 2nd dose of Zoloft in the afternoon after school and he *still* seems "difficult" for several hours. Do you think there is some fighting or something going on during his lunch hour that is upsetting him and making him angry the rest of the day?
Posted by e503 on May 21, 2003, at 11:09:36
In reply to Re: ABILIFY HELP » e503, posted by Ritch on May 21, 2003, at 9:53:24
hey ritch-
just got a call from the teacher. I don't know if i mentioned it today or not, but I didn't give ben his 2.5 mg. abilify this a.m. (just the zoloft). Guess what? she said "So far he's his old self",,,but the problems have been in the afternoon, so i will know more later. Could the abilify be causing him depression?????????????????
elise
Posted by Ritch on May 21, 2003, at 12:58:39
In reply to Re: ABILIFY HELP » Ritch, posted by e503 on May 21, 2003, at 11:09:36
> hey ritch-
> just got a call from the teacher. I don't know if i mentioned it today or not, but I didn't give ben his 2.5 mg. abilify this a.m. (just the zoloft). Guess what? she said "So far he's his old self",,,but the problems have been in the afternoon, so i will know more later. Could the abilify be causing him depression?????????????????
> eliseHis symptoms really sounded like irritability to me-he might have been a little depressed as well, but it reminds me of my irritability spells I get-sometimes they are "noisy" and sometimes I just get quiet and steam. I haven't tried Abilify and I don't know how long it takes for it to peak in your serum-it may take several hours-in that case it might be Abilify causing the trouble in the afternoon. Perhaps just the tiny dose at bedtime to help him sleep would be all he needs?
Posted by cybercafe on May 21, 2003, at 18:59:23
In reply to Re: abilify/trileptal/zoloft » e503, posted by Ritch on May 20, 2003, at 11:33:14
>one particular thing.. possibly over-sedated on the Abilify as well. It does have a long half-life. It may take a week or longer for the drug's level to reach a steady state. That's one thing I don't like about meds with lengthy half-lives like that--you don't see the response of a dose change for a long time-- and the longer the time goes by the easier it is to confuse with "typical" mood-cycling patterns.
Abilify is sedating? darn
i also was concerned about abilify's long half life ... but ... can't this be compensated for by a loading dose?
Posted by Ritch on May 21, 2003, at 22:12:47
In reply to Re: abilify/trileptal/zoloft, posted by cybercafe on May 21, 2003, at 18:59:23
> >one particular thing.. possibly over-sedated on the Abilify as well. It does have a long half-life. It may take a week or longer for the drug's level to reach a steady state. That's one thing I don't like about meds with lengthy half-lives like that--you don't see the response of a dose change for a long time-- and the longer the time goes by the easier it is to confuse with "typical" mood-cycling patterns.
>
> Abilify is sedating? darn
>
> i also was concerned about abilify's long half life ... but ... can't this be compensated for by a loading dose?
>
>
Cyber, I haven't tried the stuff. My pdoc told me it doesn't have the weight gain troubles that Zyprexa does. It has "moderate" affinity for the serotonin transporter-which makes it an SRI in some ways-and that usually means insomnia or agitation for some people. It isn't *supposed* to be near as sedative as Zyprexa or Seroqel. I have got a sample package to try, but I ain't going there. To me, from reading the insert in the sample package it looks like about three or four drugs in one. It looks like an SRI+Buspar+Risperdal all bundled into one. The lessened drowsiness is probably its lower antihistaminic properties. My pdoc also mentioned that asthenia with it is much reduced (muscle weakness-listlessness) because of reduced NE agonist(?) activity compared with the others. The only success I've found with long-half-life meds was "loading" Prozac and taking it two-three times weekly instead. It was still uneven to me and I didn't like that way of dosing.
Posted by e503 on May 22, 2003, at 16:17:06
In reply to Re: abilify/trileptal/zoloft » cybercafe, posted by Ritch on May 21, 2003, at 22:12:47
I was SURE I was going to stop giving ben his abilify. He has been on 2.5 mg. a night just for 2 nights, down from 5 mg. a day 3 days ago. He is still like a zombie....flat affect. I even called the pdoc to tell him I was stopping giving it to him. I guess in a week or so I can see how he is and if I have to, go back to 2.5 mg? HELP!
elise
Posted by cybercafe on May 22, 2003, at 16:27:59
In reply to Re: abilify/trileptal/zoloft » cybercafe, posted by Ritch on May 21, 2003, at 22:12:47
Ritch, I'd like to say thanks for bringing up the bp issue with effexor xr. i managed to get mine checked, found out it was high, and get off the stuff. which is great, because the tremors were really inhibiting my social life. now i can go out and start meeting some cute girls :)
> Cyber, I haven't tried the stuff. My pdoc told me it doesn't have the weight gain troubles that Zyprexa does. It has "moderate" affinity for the serotonin transporter-which makes it an SRI in some ways-and that usually means insomnia or agitation for some people. It isn't *supposed* to be near as sedative as Zyprexa or Seroqel. I
zyprexa is a great drug for me. even though i am a hypersomniac, the extra sleep isn't too severe. no movement disorders. no weight gain.
However! it does block dopamine receptors in my limbic system, and that is bad for my ADD and that is where aripiprazole seems like a unique solution
>have got a sample package to try, but I ain't going there. To me, from reading the insert in
dude i am soo jealous :) i wish i lived in the states .. .actually i don't :( .... but i am seriously considering moving to the UK when it comes out there
>the sample package it looks like about three or four drugs in one. It looks like an SRI+Buspar+Risperdal all bundled into one. The
that's great. it's probably SRI+Risperdal (but without movement disorders)+Stim
>lessened drowsiness is probably its lower antihistaminic properties. My pdoc also
ummm... i think dopamine also has to do with drowsiness.. and since it's a partial agonist rather than an antagonist, that must help as well
>mentioned that asthenia with it is much reduced (muscle weakness-listlessness) because of reduced NE agonist(?) activity compared with the others.
interesting
>The only success I've found with long-half-life meds was "loading" Prozac and taking it two-three times weekly instead. It was still uneven to me and I didn't like that way of dosing.
actually i don't think you'd need a loading dose... the long half life means you could just start taking 15 mg/day rather than starting with a lower dose and working your way upif one of the DRD2/5ht2 antagonists does not work for me aripiprazole will be my last hope
Posted by Ritch on May 22, 2003, at 21:53:41
In reply to Re: abilify/trileptal/zoloft, posted by e503 on May 22, 2003, at 16:17:06
> I was SURE I was going to stop giving ben his abilify. He has been on 2.5 mg. a night just for 2 nights, down from 5 mg. a day 3 days ago. He is still like a zombie....flat affect. I even called the pdoc to tell him I was stopping giving it to him. I guess in a week or so I can see how he is and if I have to, go back to 2.5 mg? HELP!
> eliseThere was one thing I forgot to ask in my last post, and it had to do with Trileptal. You folks quit it because you thought it was causing manic symptoms, right? You said that he was talking a lot after he took it. Was he talking in a relational way (but perhaps pressured and elated), or was it talking "just to talk" stuff? The reason I ask is I am wondering if the Trileptal was doing some good in some way at *some* dose or other and now it's gone and perhaps he is not doing as well without it?
Posted by Ritch on May 22, 2003, at 22:07:34
In reply to Re: abilify/trileptal/zoloft, posted by cybercafe on May 22, 2003, at 16:27:59
> Ritch, I'd like to say thanks for bringing up the bp issue with effexor xr. i managed to get mine checked, found out it was high, and get off the stuff. which is great, because the tremors were really inhibiting my social life. now i can go out and start meeting some cute girls :)
Geez, the tremors must have been fairly brutal! :)
No withdrawal effects or rebound anxiety from the Effexor? How is your sleep (improved/worsened)?
> However! it (Zyprexa) does block dopamine receptors in my limbic system, and that is bad for my ADD and that is where aripiprazole seems like a unique solution.
> ummm... i think dopamine also has to do with drowsiness.. and since it's a partial agonist rather than an antagonist, that must help as wellThat's what my pdoc crowed about (the "partial agonist" activity of Abilify at the D2 receptor), however, if you read the insert carefully you will see high *affinity* for the D2 receptor-that says antagonist all over the place to me-semantics(?). Otherwise how could this med cause considerable akathisia problems in some patients?
> >The only success I've found with long-half-life meds was "loading" Prozac and taking it two-three times weekly instead. It was still uneven to me and I didn't like that way of dosing.
>
>
> actually i don't think you'd need a loading dose... the long half life means you could just start taking 15 mg/day rather than starting with a lower dose and working your way up
>
> if one of the DRD2/5ht2 antagonists does not work for me aripiprazole will be my last hopeOh, I see what you mean-you start off with a higher dose from the getgo....
Posted by cybercafe on May 24, 2003, at 2:46:41
In reply to Re: abilify/trileptal/zoloft » cybercafe, posted by Ritch on May 22, 2003, at 22:07:34
> > Ritch, I'd like to say thanks for bringing up the bp issue with effexor xr. i managed to get mine checked, found out it was high, and get off the stuff. which is great, because the tremors were really inhibiting my social life. now i can go out and start meeting some cute girls :)
>
> Geez, the tremors must have been fairly brutal! :)well they get worse when you are nervous/excited of course :(
am i the only bipolar that doesn't have a harem of women?
i wonder if significant anxiety is normal or abnormal in bipolar patients.
hmmm... i've thought about it, and i can't help but think that those type 1s seem to be more functional (work, socializing, etc etc)
> No withdrawal effects or rebound anxiety from the Effexor? How is your sleep (improved/worsened)?
Nothing noticeable. I'm only going from 150 -> 75.
I went from 225 -> 0 before in a week, and it wasn't until the following week that I felt bad withdrawal effects. And those were easily treated with clonazepam.>however, if you read the insert carefully you will see high *affinity* for the D2 receptor-that says antagonist all over the place to me-semantics
hmm... i don't understand why affinity = antagonist
please explain
>(?). Otherwise how could this med cause considerable akathisia problems in some patients?good question. but then why wouldn't it cause other movement disorders?
hmmmm.... i wonder what AD my doc will put me on next. Is effexor the only one that causes tremors?
Posted by SLS on May 24, 2003, at 9:17:32
In reply to Re: abilify/trileptal/zoloft, posted by cybercafe on May 24, 2003, at 2:46:41
me-semantics
>
> hmm... i don't understand why affinity = antagonist
> please explainaffinity: The force attracting atoms to each other and binding them together in a molecule
Affinity is how powerful the "stickiness" is between the ligand molecule (natural neurotransmitter or drug) and the receptor on the surface of the cell. This property is independent of whether the molecule is an agonist, antagonist, or inverse agonist.
Agonist=stimulates receptor to perform a function
Antagonist=blocks receptor to prevent it from performing its function
Inverse agonist=alters the receptor to perform the opposite of its intended function
I hope this helps.
- Scott
Posted by Ritch on May 24, 2003, at 11:24:27
In reply to Re: abilify/trileptal/zoloft, posted by SLS on May 24, 2003, at 9:17:32
> me-semantics
> >
> > hmm... i don't understand why affinity = antagonist
> > please explain
>
> affinity: The force attracting atoms to each other and binding them together in a molecule
>
> Affinity is how powerful the "stickiness" is between the ligand molecule (natural neurotransmitter or drug) and the receptor on the surface of the cell. This property is independent of whether the molecule is an agonist, antagonist, or inverse agonist.
>
> Agonist=stimulates receptor to perform a function
>
> Antagonist=blocks receptor to prevent it from performing its function
>
> Inverse agonist=alters the receptor to perform the opposite of its intended function
>
>
> I hope this helps.
>
>
> - Scott
Scott- what about a "partial agonist"? I know buspirone is supposed to be a partial agonist at 5-HT1a receptors, so is there anything specific or particular about partial agonism? I'm not into the receptor thing very heavy, so I need some help here. thanks in advance-Mitch
Posted by SLS on May 24, 2003, at 12:14:29
In reply to Re: abilify/trileptal/zoloft » SLS, posted by Ritch on May 24, 2003, at 11:24:27
> > me-semantics
> > >
> > > hmm... i don't understand why affinity = antagonist
> > > please explain
> >
> > affinity: The force attracting atoms to each other and binding them together in a molecule
> >
> > Affinity is how powerful the "stickiness" is between the ligand molecule (natural neurotransmitter or drug) and the receptor on the surface of the cell. This property is independent of whether the molecule is an agonist, antagonist, or inverse agonist.
> >
> > Agonist=stimulates receptor to perform a function
> >
> > Antagonist=blocks receptor to prevent it from performing its function
> >
> > Inverse agonist=alters the receptor to perform the opposite of its intended function
> >
> >
> > I hope this helps.
> >
> >
> > - Scott
>
>
> Scott- what about a "partial agonist"? I know buspirone is supposed to be a partial agonist at 5-HT1a receptors, so is there anything specific or particular about partial agonism? I'm not into the receptor thing very heavy, so I need some help here. thanks in advance-Mitch
Hi Mitch.A partial agonist binds to a receptor just as does an agonist or antagonist. However, it does not always stimulate the receptor into action. I would guess that it probably depends on which of the alternating states (conformations) the molecules exist as they switch back and forth between their different three dimensional arrangements. I'm not sure though.
- Scott
Posted by cybercafe on May 24, 2003, at 18:42:22
In reply to Re: abilify/trileptal/zoloft, posted by SLS on May 24, 2003, at 12:14:29
> Hi Mitch.
>
> A partial agonist binds to a receptor just as does an agonist or antagonist. However, it does not always stimulate the receptor into action. I would guess that it probably depends on which of the alternating states (conformations) the molecules exist as they switch back and forth between their different three dimensional arrangements. I'm not sure though.could it be that it stimulates as much as dopamine, but doesn't bind for as long (i.e. less affinity)?
Posted by SLS on May 24, 2003, at 19:26:44
In reply to Re: abilify/trileptal/zoloft, posted by cybercafe on May 24, 2003, at 18:42:22
> > Hi Mitch.
> >
> > A partial agonist binds to a receptor just as does an agonist or antagonist. However, it does not always stimulate the receptor into action. I would guess that it probably depends on which of the alternating states (conformations) the molecules exist as they switch back and forth between their different three dimensional arrangements. I'm not sure though.
>
> could it be that it stimulates as much as dopamine, but doesn't bind for as long (i.e. less affinity)?
>http://idp.med.ufl.edu/Core/6002/Outln2B/S2BL6.html
Posted by e503 on May 24, 2003, at 22:28:06
In reply to Re: abilify/trileptal/zoloft, posted by SLS on May 24, 2003, at 19:26:44
hi all- wanted to let you know that thursday night was the last day we gave ben abilify. He is now off of it and the trileptal and only on zoloft. Glad to let you all now that he had a better day today....actually saw him smiling!!!!
How long will it take to get the trileptal really out of his system, so I can tell how he is just on the zoloft?
thanks,
elise
Posted by Ritch on May 25, 2003, at 10:59:36
In reply to Re: abilify/trileptal/zoloft, posted by e503 on May 24, 2003, at 22:28:06
> hi all- wanted to let you know that thursday night was the last day we gave ben abilify. He is now off of it and the trileptal and only on zoloft. Glad to let you all now that he had a better day today....actually saw him smiling!!!!
>
> How long will it take to get the trileptal really out of his system, so I can tell how he is just on the zoloft?
> thanks,
> elise
Hi elise, it may already be gone. It's been a couple of weeks right? From what I remember it (Trileptal) is eliminated mostly by the kidneys and it washes out rather quickly compared to the Abilify and even Zoloft.
Posted by Ritch on May 25, 2003, at 11:10:18
In reply to Re: abilify/trileptal/zoloft, posted by SLS on May 24, 2003, at 12:14:29
> Hi Mitch.
>
> A partial agonist binds to a receptor just as does an agonist or antagonist. However, it does not always stimulate the receptor into action. I would guess that it probably depends on which of the alternating states (conformations) the molecules exist as they switch back and forth between their different three dimensional arrangements. I'm not sure though.
>
>
> - Scott
>
>Scott- here are two lines in the link you posted that comes the closes for me to understand this I think ;)
B. When is a partial agonist a good therapeutic agent?
1. the safe dose range can be greatly extended (the maximum response only reaches the sub-100% value and stays there as a plateau)
2. when the antagonist properties of the partial agonist are desirable (blunting effects of endogenous substances, for example)(example: pindolol)
Would a partial agonist be analogous to a pistol that is cocked and ready to fire which is easy to uncock relative to other pistols? This is that "goldilocks" thing with Abilify isn't it? It isn't supposed to bind tightly (hence it is a partial agonist), so the molecule doesn't stay "stuck" on receptor?
Posted by e503 on May 25, 2003, at 11:49:24
In reply to Re: abilify/trileptal/zoloft » e503, posted by Ritch on May 25, 2003, at 10:59:36
> > hi all- wanted to let you know that thursday night was the last day we gave ben abilify. He is now off of it and the trileptal and only on zoloft. Glad to let you all now that he had a better day today....actually saw him smiling!!!!
> >
> > How long will it take to get the trileptal really out of his system, so I can tell how he is just on the zoloft?
> > thanks,
> > elise
>
>
> Hi elise, it may already be gone. It's been a couple of weeks right? From what I remember it (Trileptal) is eliminated mostly by the kidneys and it washes out rather quickly compared to the Abilify and even Zoloft.
>
Yes, it's been a couple weeks (I think!) off trileptal. WHat about the abilify? I gave him 2.5 mg. the last time (for 3 days) last 3 days ago. When can I expect to see what he is like off the abilify?
thanks,
elise
Posted by SLS on May 25, 2003, at 12:05:28
In reply to Partial agonists » SLS, posted by Ritch on May 25, 2003, at 11:10:18
Hi Mitch.
> > A partial agonist binds to a receptor just as does an agonist or antagonist. However, it does not always stimulate the receptor into action. I would guess that it probably depends on which of the alternating states (conformations) the molecules exist as they switch back and forth between their different three dimensional arrangements. I'm not sure though.
> Would a partial agonist be analogous to a pistol that is cocked and ready to fire which is easy to uncock relative to other pistols? This is that "goldilocks" thing with Abilify isn't it? It isn't supposed to bind tightly (hence it is a partial agonist), so the molecule doesn't stay "stuck" on receptor?
Perhaps one way to conceptualize a partial agonist is to think of it as a duplicate key that wasn't cut properly. Sometimes it unlocks the door and sometimes it fails to unlock the door, depending on how you jiggle it in or out. It is possible to turn the key half-way before it stops, thereby changing the length of the bolt, but not enough to clear the hole. The door cannot be opened.I tried. :-)
Regarding Abilify, I haven't read enough about the details regarding how and why it behaves differently in the presence of varying concentrations of dopamine within the synapse.
- Scott
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