Psycho-Babble Medication Thread 847722

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Re: Parnate trial » SLS

Posted by desolationrower on August 25, 2008, at 20:36:06

In reply to Re: Parnate trial » desolationrower, posted by SLS on August 25, 2008, at 9:04:11

yes, this study shows lower d2 occupancy:

D2 and 5HT2A receptor occupancy of different doses of quetiapine in schizophrenia: a PET study*1

Abstract

Objective: Quetiapine is a novel antipsychotic agent with many atypical features, including low D2 and higher 5HT2A affinity in vitro, low propensity to induce extra-pyramidal side effects and minimal effects on prolactin levels. The purpose of this study was to investigate, using positron emission tomography (PET), the relationship between plasma concentrations of different doses of quetiapine and occupancy of D2 and 5HT2A receptors in schizophrenic patients. Methods: Five patients were treated with quetiapine (titrated to 750 or 450 mg/day) for 28 days, subsequently reduced weekly in a descending-dose schedule. Dopamine D2 and 5HT2A occupancies were determined using [11C] raclopride and [11C] N-methylspiperone as ligands, respectively, and PET imaging. Results: Mean D2 receptor occupancies of 41 and 30% were observed at quetiapine doses of 750 and 450 mg/day. At lower dose levels no occupancy could be determined. Quetiapine induced a consistently higher degree of 5HT2A receptor occupancy, with mean occupancies of 74 and 57% at doses of 750 and 450 mg/day, respectively. No EPS emerged during the trial and most of the pre-trial EPS resolved during the study. Conclusions: In clinically effective doses, quetiapine induced low occupancy at D2 receptors, which is consistent with atypical antipsychotics such as clozapine, and probably explains the lack of EPS observed in this trial. Correlations between receptor occupancy and plasma concentrations of quetiapine could not be calculated, although receptor occupancy increased with higher plasma concentrations for the 450 and 750 mg doses.

I also have in my notes k values of 160 & 220 for d2 & 5ht2a. Thats the smallest differential of antypicals other than aripiprazole.
Still, that isn't that much of a differential compared to other atypicals (other than aripiprazole). That is a higher dose too. If you want the 5ht2a antagonism for sleep quality, 25mg isn't going to get that.

 

Re: Parnate trial » desolationrower

Posted by SLS on August 26, 2008, at 5:24:00

In reply to Re: Parnate trial » SLS, posted by desolationrower on August 25, 2008, at 20:36:06

Hi.

Are you basing your conclusion on Seroquel having a deleterious effect on sleep archetecture? If not, I think Seroquel makes for one heck of a sleeping pill. Happily, the dosage necessary for its hypnotic effect is between 25-50mg. This is lost at higher dosages, perhaps because the NE reuptake inhibiting metabolite level is much higher at dosages used for schizoid presentations.

You think Seroquel works simply because it is antihistaminergic?

I read the abstract, and am at a loss how it refutes the utility of Seroquel for sleep. The stuff works in real life, and I don't understand how one could choose not to use it based upon the abstract you cited. I'm not always that smart, though. I am hoping you could educate me where the abstract is consistent with your contentions, remembering to account for the observation that lower dosages of Seroquel make for an effective sleep aid.


- Scott


> yes, this study shows lower d2 occupancy:
>
> D2 and 5HT2A receptor occupancy of different doses of quetiapine in schizophrenia: a PET study*1
>
> Abstract
>
> Objective: Quetiapine is a novel antipsychotic agent with many atypical features, including low D2 and higher 5HT2A affinity in vitro, low propensity to induce extra-pyramidal side effects and minimal effects on prolactin levels. The purpose of this study was to investigate, using positron emission tomography (PET), the relationship between plasma concentrations of different doses of quetiapine and occupancy of D2 and 5HT2A receptors in schizophrenic patients. Methods: Five patients were treated with quetiapine (titrated to 750 or 450 mg/day) for 28 days, subsequently reduced weekly in a descending-dose schedule. Dopamine D2 and 5HT2A occupancies were determined using [11C] raclopride and [11C] N-methylspiperone as ligands, respectively, and PET imaging. Results: Mean D2 receptor occupancies of 41 and 30% were observed at quetiapine doses of 750 and 450 mg/day. At lower dose levels no occupancy could be determined. Quetiapine induced a consistently higher degree of 5HT2A receptor occupancy, with mean occupancies of 74 and 57% at doses of 750 and 450 mg/day, respectively. No EPS emerged during the trial and most of the pre-trial EPS resolved during the study. Conclusions: In clinically effective doses, quetiapine induced low occupancy at D2 receptors, which is consistent with atypical antipsychotics such as clozapine, and probably explains the lack of EPS observed in this trial. Correlations between receptor occupancy and plasma concentrations of quetiapine could not be calculated, although receptor occupancy increased with higher plasma concentrations for the 450 and 750 mg doses.
>
> I also have in my notes k values of 160 & 220 for d2 & 5ht2a. Thats the smallest differential of antypicals other than aripiprazole.
> Still, that isn't that much of a differential compared to other atypicals (other than aripiprazole). That is a higher dose too. If you want the 5ht2a antagonism for sleep quality, 25mg isn't going to get that.

 

Re: Seroquel is a miracle for sleep » desolationrower

Posted by UGottaHaveHope on August 26, 2008, at 7:36:10

In reply to Re: Parnate trial » SLS, posted by desolationrower on August 25, 2008, at 20:36:06

Seroquel at 25mg works GREAT for sleep, like being shot by an elephant dart. Out of the 30+ meds I've taken, Seroquel is the only one I know for sure works for something. It works great for insomnia, i.e. sleep.

Of course, if you are taking different drugs also, Seroquel may have the opposite effect in you.

What's unique about Seroquel is the less you take, the more sedated you feel. 25-50 should always do the trick.

 

parnate trial

Posted by noellejc on August 26, 2008, at 8:03:30

In reply to Re: Seroquel is a miracle for sleep » desolationrower, posted by UGottaHaveHope on August 26, 2008, at 7:36:10

Parnate trial Day 5- I'm not sleeping very well. I take 100mg of trazodone at night. I have been falling asleep, but will wake up after 4 or 5 hrs. Before I started the parnate I was taking 150mg of trazodone. My doctor asked me to quit taking trazodone all together before getting on the parnate and once I was on it I could go back on, but to try not to take over 100mg a night until I see him again. I want to try taking 150 mg again, but feel like I need to call to ask him. I hate calling him though because I always feel like I'm bugging him. Anyway, hopefully this irons itself out soon. If I can't sleep on this med it's not going to work for me. I read that MAOI's supress REM sleep. Don't you need REM sleep?

 

Re: Parnate trial

Posted by desolationrower on August 26, 2008, at 13:38:58

In reply to Re: Parnate trial » desolationrower, posted by SLS on August 26, 2008, at 5:24:00

Do you think it is doing something besides blocking histamine receptors?

 

Re: Parnate trial » desolationrower

Posted by SLS on August 26, 2008, at 14:37:46

In reply to Re: Parnate trial, posted by desolationrower on August 26, 2008, at 13:38:58

> Do you think it is doing something besides blocking histamine receptors?

I am really not sure. I was hoping you could elucidate for me.

Low-dosage Seroquel seems to be a better hypnotic than doxepin from what people report here on PB; doxepin being a very potent H1 antagonist. It is an order of magnitude more potent than Seroquel.

Seroquel hits many receptors as an antagonist according to the PDSP database. I would be hard pressed to pick one out as singularly responsible for its sedative effects. I'm sure the H1 antagonist property figures in to the overall sedation, though.


- Scott

 

Re: parnate trial

Posted by eric wagner on August 26, 2008, at 14:47:42

In reply to parnate trial, posted by noellejc on August 26, 2008, at 8:03:30

> Parnate trial Day 5- I'm not sleeping very well. I take 100mg of trazodone at night. I have been falling asleep, but will wake up after 4 or 5 hrs. Before I started the parnate I was taking 150mg of trazodone. My doctor asked me to quit taking trazodone all together before getting on the parnate and once I was on it I could go back on, but to try not to take over 100mg a night until I see him again. I want to try taking 150 mg again, but feel like I need to call to ask him. I hate calling him though because I always feel like I'm bugging him. Anyway, hopefully this irons itself out soon. If I can't sleep on this med it's not going to work for me. I read that MAOI's supress REM sleep. Don't you need REM sleep?

I completely understand your situation.

I started Parnate about 9 weeks ago & have/had the insomnia amongst more.

I would highly suggest following your Dr.'s instructions - especially on this medication.

It's not like a lot of the other classes of medications, where there are a lot less side effects, medication/food/supplement interactions, and/or dangerousness (ability for a medication to negatively react in a person due to ingesting over-the-counter drugs, food, dietary supplements, and/or prescription medication) - in general.

Although, some people react differently to the majority of people tested/users.

(I'm not a medical professional, but I am on the same medication & do tons of research on medical journals, Pharmaceutical Reports, FDA info., people's personal experiences, general information, etc.).

I have never used Trazadone although I have had similarly reacting medications.

I know for me, when I hit 60 mgs./day, as soon as I got up I felt like I was going to pass out - amongst other (I would say serious side effects - & most side effects have never bothered me at all - even if I did have some) symptoms.

(See my Parnate post at top of list)

I have a high tolerance for drugs/medications/supplements, so I could surmise someone at a significantly lower dose could experience the same side effects, if not more & to a higher degree.

If I were to have taken any other medication/supplement during the 3 weeks when my side effects were bad, I could see how a problem (scary situation) could come about.

I couldn't do anything those 3 weeks, & I'm an otherwise healthy/in shape 33 year old plumber.

Trazadone, when taken at a higher dose may cause Tyramine (Cheese) reaction, hypo/hypertension &/or Serotonin Syndrome - the 3 main possible serious conditions on a MAOI - very serious.

I would say bother your Dr. to let him know your concerns. He may see fit to adjust your medication/s in accordance of your insomnia issue.

You have to remember, you are the one trying to get better, & noone cares about you more than you. If I had a serious concern w/ my medication, I'd call, email, fax & even go to the office to tell him.

I would only do this if I thought there is a problem I was scared about or so upset I didn't know what to do.

As far as I've have seen, a good deal of people have side effects to this medication in the beginning especially, & a lot say that they do disappear/lessen.

The seriousness of my side effects have since lessened, although I'm still uncomfortable.

I have seen no positive change yet, & am trying another 3 weeks to get a full 12 month trial.

& My Dr. I can never get ahold of him & I have to call more than once to get an answer - if you call it an answer - when all he does is reply & answer some other question barely related to mine.

Good Luck & keep posting.

As far as I've seen, there are some highly educated/informed posters here, so hopefully they'll give you some insight.

Take Care & Be Well,
Eric M. Wagner


 

Re: parnate trial

Posted by noellejc on August 26, 2008, at 22:15:20

In reply to Re: parnate trial, posted by eric wagner on August 26, 2008, at 14:47:42

Eric, you've been on a parnate trial for 12 months?

 

Re: parnate trial

Posted by eric wagner on August 27, 2008, at 4:52:36

In reply to Re: parnate trial, posted by noellejc on August 26, 2008, at 22:15:20

> Eric, you've been on a parnate trial for 12 months?

sry meant 12 week trial

 

Re: parnate trial - noellejc

Posted by anthonyg23 on September 1, 2008, at 11:41:08

In reply to Re: parnate trial, posted by noellejc on August 26, 2008, at 22:15:20

Noellejc,

Have you found any AD or anti-anxiety help from the Trazodone?

 

Re: parnate trial - noellejc

Posted by noellejc on September 1, 2008, at 19:23:21

In reply to Re: parnate trial - noellejc, posted by anthonyg23 on September 1, 2008, at 11:41:08

No, I wouldn't say I get any anti-depressant effect from trazodone. As far as anxiety, it helps me to sleep at night, so I guess in that way, yes, but I don't notice it having any effect on anxiety during the day. Hope that helps. Noelle

 

Re: parnate trial - noellejc

Posted by noellejc on September 1, 2008, at 19:43:53

In reply to Re: parnate trial - noellejc, posted by noellejc on September 1, 2008, at 19:23:21

Parnate trial Day 11- Well, writing this post in Tennessee as I have fled Louisiana for Hurricane Gustav. I was suppose to have an appointment with my psychiatrist in New Orleans tomorrow, but it was cancelled due to the hurricane so I won't get to go up on my dose as scheduled. I went up on my trazodone to 150mg and have been taking that with a dose of benadryl at night and sleeping a lot better. The doc said I can go up to 200mg on the trazodone before I see him again so I am thinking of doing that and stopping the benadryl. Despite the fact it helps me sleep, I think combining the trazodone and benadryl is giving me a hangover in the morning. So far, on parnate, I've had less of an appetite and been getting really tired in the afternoons, but I can't seem to sleep during the day like I use to. Maybe that is a good thing, but I've used sleep as an escape for many years ,so it is hard adjusting to not having that coping mechanism. All in all, I was prepared for worse side effects, though I know they can show up later as I up my dose. Can't wait to go up on my dose, as I am not at a therapeutic level yet and want to feel better. Hope everyone is doing well. Noelle

 

Re: parnate trial - noellejc

Posted by paddo on September 1, 2008, at 21:00:29

In reply to Re: parnate trial - noellejc, posted by noellejc on September 1, 2008, at 19:43:53

Keep it going Noellejc..i had micro-movements with parnate several weeks ago..very small movements but movement all the same..slowly moved the misery not total, but enough to capture sunny days outside of the house/misery..take care paddo

 

Re: parnate trial - noellejc

Posted by noellejc on September 2, 2008, at 15:37:58

In reply to Re: parnate trial - noellejc, posted by paddo on September 1, 2008, at 21:00:29

Paddo, how high of a dose are you on?

 

Re: parnate trial - noellejc

Posted by paddo on September 4, 2008, at 0:04:09

In reply to Re: parnate trial - noellejc, posted by noellejc on September 2, 2008, at 15:37:58

Noellejc , two 10 mgs early morning then one 10mg lunch..setback last two days with depression..cruel as cruel dep/anx..

 

Re: parnate trial - noellejcDay18

Posted by noellejc on September 8, 2008, at 19:06:21

In reply to Re: parnate trial - noellejc, posted by noellejc on September 1, 2008, at 19:43:53

Day 18- Went up to 30 mg on Saturday(today's Monday). Not feeling as numb as I was on 20mg. I'm not sure if that is due to the slight upper effect or what. I've noticed I'm feeling more assertive and a little more mellow about some things that usually bother me. Maybe this means it is starting to work. The symptom of my depression that bothers me most is the inability to enjoy anything and I can't wait for that to lift. I was worried that parnate might not work for that because I read it was good to treat depression without melancholia and I'm pretty sure I have melancholia.

 

Re: Please keep posting » noellejc

Posted by UGottaHaveHOPE on September 12, 2008, at 11:35:36

In reply to Re: parnate trial - noellejcDay18, posted by noellejc on September 8, 2008, at 19:06:21

This is great stuff. Please keep describing your experiences on Parnate. Thnx.

 

Re: Please keep posting

Posted by paddo on September 12, 2008, at 18:34:33

In reply to Re: Please keep posting » noellejc, posted by UGottaHaveHOPE on September 12, 2008, at 11:35:36

Hi there..yes i will keep u up to date..have limited time on pter..its the weekend in sydney,i am in the local library. take care keep well ..paddo

 

Re: Parnate trial » noellejc

Posted by Ron Hill on September 14, 2008, at 15:30:34

In reply to Parnate trial, posted by noellejc on August 22, 2008, at 16:00:15

> I asked someone how I could help other people on the forum and they suggested I document my parnate trial. So, I'll check in every few days with an update for all those on the edge of their seats wanting to know how it's going (ha, ha).
--------------------------------


Noellejc,

Thank you very much for taking time to post your Parnate trial experience. I'm considering a switch from Nardil to Parnate, so your posts are of interest to me.

What is your dx?

Thanks again.

-- Ron

dx: Bipolar II, with ultra rapid cycling (15 days for one complete cycle), and mild OCPD

300 mg/day Trileptal
200 mg/day Lamictal
250 mg/day Keppra
60 mg/day Nardil

 

Re: Parnate trial » Ron Hill

Posted by Phillipa on September 14, 2008, at 20:13:59

In reply to Re: Parnate trial » noellejc, posted by Ron Hill on September 14, 2008, at 15:30:34

Ron no more Deplin? Love Phillipa

 

Re: Parnate trial » Phillipa

Posted by Ron Hill on September 15, 2008, at 3:59:20

In reply to Re: Parnate trial » Ron Hill, posted by Phillipa on September 14, 2008, at 20:13:59

> Ron no more Deplin? Love Phillipa
-------------

Phillipa,

Nope. It caused rashes after prolonged use.

-- Ron

 

Re: Parnate trial » Ron Hill

Posted by Phillipa on September 15, 2008, at 19:54:03

In reply to Re: Parnate trial » Phillipa, posted by Ron Hill on September 15, 2008, at 3:59:20

How nice like a Stevens Johnson Rash? So more side effects for what is supposed to be a harmless med per my pdoc. Lovely. Glad you responded. Love Jan

 

Re: Parnate trial

Posted by noellejc on September 15, 2008, at 22:56:18

In reply to Re: Parnate trial » Ron Hill, posted by Phillipa on September 15, 2008, at 19:54:03

My diagnosis is major depression recurrent, eating disorder unspecified, mild OCD, body dysmorphia, anxiety, and addiction. Not currently acting out in addiction. When I see it all on paper it sure looks like I have a lot wrong with me. Forgive me, because I don't know a lot about the treatment of bipolar, but wouldn't parnate be too activating?

 

Re: Parnate trial

Posted by noellejc on September 15, 2008, at 23:02:31

In reply to Re: Parnate trial » noellejc, posted by Ron Hill on September 14, 2008, at 15:30:34

Parnate Day 25- I take 30mg all together at once in the morning. I'm feeling really good. It's almost scary because I am afraid it won't last. I finally saw my psychiatrist and he said to stay on this dose until I see him in 3 weeks and that it would take that long to get all worked into my system and to know if we needed to go up to an even higher dose. This weekend I am going out of town to visit my brother and his wife in Florida. I've planned the trip several times, but always cancel do to depression and anxiety. This weekend I'm going through with the trip.

 

Re: Parnate trial » SLS

Posted by desolationrower on September 16, 2008, at 11:53:51

In reply to Re: Parnate trial » desolationrower, posted by SLS on August 26, 2008, at 5:24:00

Sorry I forgot about this post SLS.
I think the alpha1 blocking properties are important along with very strong antihistamine.
The abstract i posted was to show seroquel is not particularly useful for serotonin blockade which increases slow wave sleep. I don't think seroquel is helpful for this, i think it increases stage 2 instead. I think it is like benzos. THey can knock you out and you think you get good sleep, but not actually improved sleep.
-D/R


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