# Zoloft + Zyprexa Thread: Gilmourrrrrrr!



## gilmourr (Nov 17, 2011)

Decided to make a new thread as the other was getting way too long and it covered quite a few medications from gabapentin to abilify and now zyprexa.

On Zoloft (100mg) +Zyprexa (2.5mg) + 0.5 clonazapam PRN

Stopped seroquel atm (25mg) since zyprexa makes me tired enough so I can get to sleep.

Anyways, I liked the sedation brought on by zyprexa as it was manageable.

Though I woke up and felt pretty depressed at 5 AM, went back to bed until 9 AM and feel better; I guess I'm just adjusting.

Dry mouth has already started.

Moving to 5 mg in 7 days depending on the situation

EDIT: A positive is that with the dry mouth are dry hands and feet where they're not clammy.


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## riptide991 (Feb 1, 2012)

Nice man! How many hours before bed did you take the zyprexa? I think at 5mg it will matter more than at 2.5mg. At least both Sense of Purpose and I found it so. 5 hours prior to bed was the best for me.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Nice man! How many hours before bed did you take the zyprexa? I think at 5mg it will matter more than at 2.5mg. At least both Sense of Purpose and I found it so. 5 hours prior to bed was the best for me.


I took it at 6 and felt sleepy enough to go to bed at 9 but I stayed up to 11 to get a better sleep. It was kinda hard though so I'll take it later tonight.

And yeah, I think 5 mg will hit 5HT2C where it will help with productivity. I hope I'm not some idiosyncratic case


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## riptide991 (Feb 1, 2012)

gilmourr said:


> I took it at 6 and felt sleepy enough to go to bed at 9 but I stayed up to 11 to get a better sleep. It was kinda hard though so I'll take it later tonight.
> 
> And yeah, I think 5 mg will hit 5HT2C where it will help with productivity. I hope I'm not some idiosyncratic case


Eh, I've always had a different outlook on medication. No matter which medication I took I would always have an optimistic view of it, even after all the meds have failed me over the years. Maybe that's why I never get side effects hehe.


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## A Sense of Purpose (May 8, 2011)

gilmourr said:


> Decided to make a new thread as the other was getting way too long and it covered quite a few medications from gabapentin to abilify and now zyprexa.
> 
> On Zoloft (100mg) +Zyprexa (2.5mg) + 0.5 clonazapam PRN
> 
> ...


It is a fantastic combination that has literally changed my life. Zyprexa and Zoloft ftw!


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## swim (Apr 4, 2011)

gilmourr said:


> gabapentin


this one can actually save lives; together with other CNS depressants it makes up a mighty combo to kill all worries.


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## hworth (Mar 31, 2013)

Since you guys both are diagnosed with bipolar and these med combos work for you i gotta ask, at what point/signs would you know you probably have bipolar 2 haha?


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## A Sense of Purpose (May 8, 2011)

hworth said:


> Since you guys both are diagnosed with bipolar and these med combos work for you i gotta ask, at what point/signs would you know you probably have bipolar 2 haha?


Its pretty simple. Its three concepts.
1) depressive
2) manic
3) mixed

I get all 3 so that actually makes me BP1


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## gilmourr (Nov 17, 2011)

hworth said:


> Since you guys both are diagnosed with bipolar and these med combos work for you i gotta ask, at what point/signs would you know you probably have bipolar 2 haha?


I'm not BP2, I've been diagnosed with MDD and panic disorder but I think I'm mixed states with panic because whenever I take NRI's (any NRI's) I want to kill myself and I go like hypo and am super hyper and ****. Cymbalta, parnate, nardil, name it.

But the symptoms are sensitivity to NRI's, stimulants, swings, mania, delusions of graNDEUR, narcissim, hypersexuality, psychomotor agitaiton etc.

WIKII!


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## barry1685 (May 25, 2011)

Atypical antipsychotics eliminated me anxiety but caused me to be out of focus. Like I would jump task to task and couldn't focus on one thing. Is this a side effect and would it go away?


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## GotAnxiety (Oct 14, 2011)

A Sense of Purpose said:


> It is a fantastic combination that has literally changed my life. Zyprexa and Zoloft ftw!


How did it literally change your life?


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## A Sense of Purpose (May 8, 2011)

GotAnxiety said:


> How did it literally change your life?


Stopped me from becoming manic and prevented me getting depressed/anxious.


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## shana (Mar 9, 2009)

A Sense of Purpose said:


> It is a fantastic combination that has literally changed my life. Zyprexa and Zoloft ftw!


What are you taking this combo for? SAD, GAD, anxiety in general, depression? 
I would try Zyprexa but I'm worried about weight gain on it. I know some people don't gain weight on it, but I already have a tendency to gain weight easily and it's a battle for me to lose weight. If I don't lose weight, my physical health is going to get worse.


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## gilmourr (Nov 17, 2011)

Day 3 of Zyprexa 2.5 mg

Pros

- Hands/feet no longer sweaty/clammy (big pro)
- No need for seroquel as it gets me to bed
- Feel like I can concentrate and have been doing work for hours on end

Cons
- 10 pounds in 2 days
- Dry mouth
- Mild mild fatty tissue building up in the breasts/may be placebo.
- I kinda feel more dysthymia just without the apathy/anhedonia. Like more moderate depression but I get more reward as of lately.

Anyways, that's it.


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## A Sense of Purpose (May 8, 2011)

shana said:


> What are you taking this combo for? SAD, GAD, anxiety in general, depression?
> I would try Zyprexa but I'm worried about weight gain on it. I know some people don't gain weight on it, but I already have a tendency to gain weight easily and it's a battle for me to lose weight. If I don't lose weight, my physical health is going to get worse.


For Bipolar with GAD and Panic attacks


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## gilmourr (Nov 17, 2011)

Question for Keh and Sense or anyone on zyprexa.

How tired were you on Zyprexa? I feel pretty good on it so far but I get tired quite a bit and have to take 1 or 2 naps for like an hour throughout the day.

Do you get used to it? Because antihistamine meds I usually don't get used to. Seroquel I've never had to up the dose from 25 mg and remeron when I was on it never got better.

Hopefully I'm tired from the action on serotonin an dnot because of the antihistamine.

Maybe 5 mg will be more activating.


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## A Sense of Purpose (May 8, 2011)

I very much adapted to the side effects of Olanzapine. Now i can take it at say 5pm, and stay awake as long as i need to (like if i have an assignment). I can also take my meds at 5 and drift off to sleep at 10-12.

So yes, at the beginning i fell flat on my *** but now its much more bearable.


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## riptide991 (Feb 1, 2012)

gilmourr said:


> Question for Keh and Sense or anyone on zyprexa.
> 
> How tired were you on Zyprexa? I feel pretty good on it so far but I get tired quite a bit and have to take 1 or 2 naps for like an hour throughout the day.
> 
> ...


Yah I completely got used to it. Like Sense of Purpose I could take it without even going to bed, and then when I eventually went to bed it would still let me fall asleep. But then again I get used to antihistamines usually quickly. You could try 5mg, but just get the time right the day before and you shouldn't be tired the next day. I always took it 5 hours before bed.


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## T800 (Jun 13, 2013)

gilmourr said:


> Cons
> - 10 pounds in 2 days


You gained 10 pounds in 2 days? Is this even possible? How much do you eat every day? like 15.000 calories?


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## gilmourr (Nov 17, 2011)

@T800, probably water retention or something, as I read the scale correctly.

Zyprexa definitely allows me to be more concentrated. I've been able to do more academically since starting and I can perform work significantly longer.

Weird thing is I feel like either the dysthymia or melancholic depression feels worse. Yet somehow I'm more motivated and concentrated. With this I also definitely have felt more insecure, which is super rare for me given that I usually feel narcisstic. It's not a good feeling at all.

So far, more productive, less happy. After this reaches steady state...I think it's half life is 40 hours, so in 5 days or so I'll move to 5 mg.

EDIT: Today I've been just getting knocked out hard from Zyprexa, 2 naps already, 4 pm and I'm still tired. Sheesh, would 5 mg be more activating from 5HT2C antagonism?


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## gilmourr (Nov 17, 2011)

Well, I seem to only have had to take 1 nap today instead of 2, but I still feel super tired. Took Zyprexa at 8 pm last night. I'll continue doing that.

Had some trippy *** nightmares. Food has never tasted so good as well.

Concentration is really good when I'm not tired, but that's hardly ever. Knowing my past experience with hard antihistamines like Remeron I don't feel that optimistic on Zyprexa. 

I don't ever sweat anymore which is great.

6 weeks is going to feel super long if I'm just inside and eating and sleeping :/

Oh well, next med pick in 6 weeks if this doesn't work will be up to my psych. Maybe she'll actually pick the right one to accompany Zoloft.

Does anyone know if Amitryptiline is less sedating than Zyprexa? Because I like Zyprexa's muscarinic antagonism, but so far I'm not a fan of the D antagonism and H1 antagonism


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## A Sense of Purpose (May 8, 2011)

gilmourr said:


> Does anyone know if Amitryptiline is less sedating than Zyprexa? Because I like Zyprexa's muscarinic antagonism, but so far I'm not a fan of the D antagonism and H1 antagonism


From my experience, Zyprexa is much more sedating and likely to cause a hangover the next day.

Dont get me wrong though, Ami is great for knocking you out at 100-150mg


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## swim (Apr 4, 2011)

Are you gaining weight gilmourr?


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## riptide991 (Feb 1, 2012)

I don't believe the 10lbs in 2 days. Not even with water weight. That would be a noticeable case of edema. I do believe the hardcore focus and increasing the taste of food. Anyways, I gained a bit of weight with olanzapine, I didn't even notice it while it was happening it was so slow. I wasn't constantly looking in the mirror while on it so one day I just noticed my abs disappearing hehe. But I didn't get a gut or anything. I didn't even notice but my eating did increase and it was due to the hypoglycemia though.


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## gilmourr (Nov 17, 2011)

swim said:


> Are you gaining weight gilmourr?


8-10 pounds so far in about 7 days, seems to have stopped there, though I just increased to 5 mg daily so maybe I'll gain a bit more.

Really tired, lol. :/

@keh, all I know is that I went from 185 to 195 on my scale but now I'm at 192 ish. Maybe it was a misread + some zyprexa weight. I agree that 10 pounds is a lot.

Amitriptyline seems like a possibly better version of zyprexa. It has muscarinic antagonism like Zyprexa that will help my constant sweating, it has 5HT2A antagonism and 5HT2C which I think is responsible for the focus minus the D2 antagonism.

It also has action on sigma plus it being a great med apparently for endogenous depression. And finally, less antihistamine.

What sucks is that if Zyprexa doesn't work that I promised my pdoc that I'd let her choose one so I won't get amitriptyline for like 8 weeks at the earliest.

Zyprexa is starting to make me feel super mellow, though it kind of makes my depression possibly feel a bit worse than zoloft alone. So far it's okay. I give it like a 6.5/10 atm


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## gilmourr (Nov 17, 2011)

Sleep + Eat + Sleep + Eat + Sleep + EAT.

WHAT UP 5 MG OF ZYPREXAAAAA.


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## riptide991 (Feb 1, 2012)

Wow you're really sensitive to antihistamines. It's a bit less powerful than mirtazapine when it comes to histamine. Does coffee not help you?


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Wow you're really sensitive to antihistamines. It's a bit less powerful than mirtazapine when it comes to histamine. Does coffee not help you?


Or it may just be that you're a tank, lol. Remeron should knock you the heck out.

I drink like 3-4 coffees a day, though it doesn't ever help with the sedation, I need to sleep it off.

Olanzapine is really strong though along with Remeron and Seroquel. Olanzapine is the most powerful AAP on H1 I believe.


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## riptide991 (Feb 1, 2012)

Remeron and zyprexa are very close in affinity 1.6 the former and 2.2 the latter. Remeron does get me sleepy about 2 hours after taking it. But when I wake up i'm fine and it doesn't linger. The same thing with Zyprexa when i took it 5 hours ahead. 

Yah Seroquel is super weak compared to olanzapine and mirtazapine hehe. I guess it depends on the dosing. I've never really tried it. Maybe inject some histamine in the morning 

Maybe choline could help, have some cocoa powder in the mornings.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Remeron and zyprexa are very close in affinity 1.6 the former and 2.2 the latter. Remeron does get me sleepy about 2 hours after taking it. But when I wake up i'm fine and it doesn't linger. The same thing with Zyprexa when i took it 5 hours ahead.
> 
> Yah Seroquel is super weak compared to olanzapine and mirtazapine hehe. I guess it depends on the dosing. I've never really tried it. Maybe inject some histamine in the morning
> 
> Maybe choline could help, have some cocoa powder in the mornings.


Yeah, seroquel works for me as it makes me tired/not too tired and I don't have any grogginess in the morning. Never had to adjust my dose of seroquel...so I'm not even sure whether it's a good idea to "wait it out." If it has to do with serotonin then it may abate...but I'm fairly certain it's the antihistamine that's knocking me out.


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## riptide991 (Feb 1, 2012)

gilmourr said:


> Yeah, seroquel works for me as it makes me tired/not too tired and I don't have any grogginess in the morning. Never had to adjust my dose of seroquel...so I'm not even sure whether it's a good idea to "wait it out." If it has to do with serotonin then it may abate...but I'm fairly certain it's the antihistamine that's knocking me out.


Are you able to get a small dose of Modafinil to take? It basically does the opposite of what antihistamines do. It may be able to at least get you to normal state at the right dose. This way you don't have to worry if modafinil is giving you anxiety or too much energy or what not. You pop a small dose in the morning to offset the zyprexa. And the half life for modafinil is like 11-15 hours. So if you take a small enough dose it won't really matter and your zyprexa should still put you to sleep.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Are you able to get a small dose of Modafinil to take? It basically does the opposite of what antihistamines do. It may be able to at least get you to normal state at the right dose. This way you don't have to worry if modafinil is giving you anxiety or too much energy or what not. You pop a small dose in the morning to offset the zyprexa. And the half life for modafinil is like 11-15 hours. So if you take a small enough dose it won't really matter and your zyprexa should still put you to sleep.


I probably could get it, though I'm not sure it's worth it if I have weird glucose levels as well + more weight gain, I guess we'll see.

Amitriptyline/nortriptyline/saphris all look like better moves if Zyprexa continues to give me 24/7 lethargy. Like it's almost 3 pm now and I need to go take a nap :/

Could be worse though. I could have that major depression still that I started out with! Very glad that Zoloft continues to pull the majority of the load. Love the stuff.


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## riptide991 (Feb 1, 2012)

gilmourr said:


> I probably could get it, though I'm not sure it's worth it if I have weird glucose levels as well + more weight gain, I guess we'll see.
> 
> Amitriptyline/nortriptyline/saphris all look like better moves if Zyprexa continues to give me 24/7 lethargy. Like it's almost 3 pm now and I need to go take a nap :/
> 
> Could be worse though. I could have that major depression still that I started out with! Very glad that Zoloft continues to pull the majority of the load. Love the stuff.


Well you don't know if it gives you weird glucose, most people don't get the glucose issues. The weight gain would be from making food taste better and you just eating more. Yah it's a shame cuz I loved olanzapine and would love to try it with Parnate, but hypoglycemia! My brain must have less histamine receptors or something. I don't get why people can't handle stuff like mirtazapine.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Well you don't know if it gives you weird glucose, most people don't get the glucose issues. The weight gain would be from making food taste better and you just eating more. Yah it's a shame cuz I loved olanzapine and would love to try it with Parnate, but hypoglycemia! My brain must have less histamine receptors or something. I don't get why people can't handle stuff like mirtazapine.


Yeah definitely because these antihistamines are strong. I feel like you're an exception.

Woke up today SO incredibly tired but at the same time unable to go back to bed. Annoying as all hell. I think I'm going back to 2.5 mg until I can deal with the antihistamine better... I'm just way too sedated all the timeeee


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## A Sense of Purpose (May 8, 2011)

gilmourr said:


> Yeah definitely because these antihistamines are strong. I feel like you're an exception.
> 
> Woke up today SO incredibly tired but at the same time unable to go back to bed. Annoying as all hell. I think I'm going back to 2.5 mg until I can deal with the antihistamine better... I'm just way too sedated all the timeeee


Give Zyprexa a month. The sedation becomes a non issue. You need to wait for it to acclimatise. Even at 20mg (when i was on it) the sedation was not an issue.

Also, i recommend taking it 3-5 hours before you plan on going to bed.


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## riptide991 (Feb 1, 2012)

A Sense of Purpose said:


> Give Zyprexa a month. The sedation becomes a non issue. You need to wait for it to acclimatise. Even at 20mg (when i was on it) the sedation was not an issue.
> 
> Also, i recommend taking it 3-5 hours before you plan on going to bed.


Gilmour is really jumpy when it comes to meds 

Although he may legitimately have issues with sedation that never go away. Don't know if he's ever given a med like mirtazapine a good month though.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Gilmour is really jumpy when it comes to meds
> 
> Although he may legitimately have issues with sedation that never go away. Don't know if he's ever given a med like mirtazapine a good month though.


Gave remeron 8 weeks since it took away all my depression. It was great besides sleeping like 16 hours a day. I'm just not sure I want to commit a month if they both are potent H1 antagonists and I've already been down the road with H1 antagonists, though remeron is stronger. It just makes more sense to me that if I've been down the road of strong H1 antagonists that something similar but less potent on H1 may be better. I've only got 3 months to get this 100%, I want to go back to school in the winter.

But remeron never got better at all and it seems like olanzapine is giving me the same reaction as remeron, weight gain, more acne, and sleeping all the time


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## riptide991 (Feb 1, 2012)

gilmourr said:


> Gave remeron 8 weeks since it took away all my depression. It was great besides sleeping like 16 hours a day. I'm just not sure I want to commit a month if they both are potent H1 antagonists and I've already been down the road with H1 antagonists, though remeron is stronger. It just makes more sense to me that if I've been down the road of strong H1 antagonists that something similar but less potent on H1 may be better. I've only got 3 months to get this 100%, I want to go back to school in the winter.
> 
> But remeron never got better at all and it seems like olanzapine is giving me the same reaction as remeron, weight gain, more acne, and sleeping all the time


Keep in mind that not only is remeron stronger you were taking a higher dose! Minimum 15mg is my guess. So maybe at the 2.5-5mg dose of zyprexa you actually will get used to it. But yah it's your call, especially if you're getting weight gain you may not like it since you seem to gain in the moob area


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Keep in mind that not only is remeron stronger you were taking a higher dose! Minimum 15mg is my guess. So maybe at the 2.5-5mg dose of zyprexa you actually will get used to it. But yah it's your call, especially if you're getting weight gain you may not like it since you seem to gain in the moob area


Lol yeah and I was on 15 mg of remeron. I'll talk with my psych on monday and see what she thinks


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## gilmourr (Nov 17, 2011)

The man boobs are clearly starting to show from Olanzapine. I don't think it has to do with putting on weight as I've been 190-200 pds before. I think it has to do with 5 mg and hiting D2 receptors, but yeah, anyways they're clearly visible if I have a shirt off. They hardly exist if I have a shirt on,

Someone said prolactin levels balance out by week 8. If I last that long on this medication I would believe that the man boobs side effect would dissipate


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## A Sense of Purpose (May 8, 2011)

Not to say that you will have the same response, but for me, even at 20mg Olanzapine and Sodium Valproate did not cause any moob issues.

Mind you valproate was crap (for me) and was the source of my weight gain issues


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## riptide991 (Feb 1, 2012)

gilmourr said:


> The man boobs are clearly starting to show from Olanzapine. I don't think it has to do with putting on weight as I've been 190-200 pds before. I think it has to do with 5 mg and hiting D2 receptors, but yeah, anyways they're clearly visible if I have a shirt off. They hardly exist if I have a shirt on,
> 
> Someone said prolactin levels balance out by week 8. If I last that long on this medication I would believe that the man boobs side effect would dissipate


No it doesn't really hit D2 till after 10mg. Read study I posted and doses used and how little it actually impacted it. It's either your normal fat accumulation or you already have super high prolactin levels and even tiny bits are making a difference.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> No it doesn't really hit D2 till after 10mg. Read study I posted and doses used and how little it actually impacted it. It's either your normal fat accumulation or you already have super high prolactin levels and even tiny bits are making a difference.


I'll read it when I'm back on my computer! And yeah, it definitely is fat accumulation. I'm now at 198 from my 185 which was 9 days ago.


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## riptide991 (Feb 1, 2012)

gilmourr said:


> I'll read it when I'm back on my computer! And yeah, it definitely is fat accumulation. I'm now at 198 from my 185 which was 9 days ago.


That's so weird to gain that much in 9 days. Like 1 lbs of fat is roughly 3500 calories excess that you have to intake. Have you been eating like a beast now or something? Watch out for those calorically dense meals. I gained a bit on zyprexa but it was over some time and yah I was eating more because of the hypoglycemia it caused.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> That's so weird to gain that much in 9 days. Like 1 lbs of fat is roughly 3500 calories excess that you have to intake. Have you been eating like a beast now or something? Watch out for those calorically dense meals. I gained a bit on zyprexa but it was over some time and yah I was eating more because of the hypoglycemia it caused.


I have been eating like a beast. But to say 3500 extra calories/day...

I'm guessing I'm doing about 1500-2000 extra


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## jim_morrison (Aug 17, 2008)

kehcorpz said:


> No it doesn't really hit D2 till after 10mg. Read study I posted and doses used and how little it actually impacted it. It's either your normal fat accumulation or you already have super high prolactin levels and even tiny bits are making a difference.


Just to add, here's a graph on it;


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## gilmourr (Nov 17, 2011)

jim_morrison said:


> Just to add, here's a graph on it;


If I understand correctly, you're arguing that it does occupy before 10 mg against what keg said? It would make sense because 5 mg gave me moobs.


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## riptide991 (Feb 1, 2012)

gilmourr said:


> If I understand correctly, you're arguing that it does occupy before 10 mg against what keg said? It would make sense because 5 mg gave me moobs.


That amount of occupancy is not enough to make any difference. And a lot of occupancy is actually presynaptic which raises dopamine. Many studies show the increase in dopamine from olanzapine. There's even case studies of it triggering psychosis in schizophrenics at low doses.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> That amount of occupancy is not enough to make any difference. And a lot of occupancy is actually presynaptic which raises dopamine. Many studies show the increase in dopamine from olanzapine. There's even case studies of it triggering psychosis in schizophrenics at low doses.


You can have presynaptic receptor occupancy? I thought receptors were only part of post synaptic. I can see Olanzapine raising DA through antagonism at 5HT2C, but maybe it's possible that while olanzapine is raising my CNS levels of DA (I do feel more motivated and enjoy things more) that it's also lowering levels of DA in my peripheral body. Or maybe it's just the pure increase in prolactin from olanzapine.

I read your journal about prolactin being comparable to placebo after week 6 or 8, so maybe I'll stick with 2.5 mg instead of 5 for 6 weeks and see. I'm talking to my psych today. Besides allowing me to concentrate it's only had that effect after 10 days. Side effects are still immense day time tiredness, sex drive lowered, weight gain, acne, and I'm still waiting on some help with anxiety.

EDIT: Do you have a journal that shows approximately when receptor occupancy creates an action? How much % is usually needed? If we look at SSRI's I know it's usually between 60-80%


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## jim_morrison (Aug 17, 2008)

gilmourr said:


> If I understand correctly, you're arguing that it does occupy before 10 mg against what keg said? It would make sense because 5 mg gave me moobs.


Not arguing with what he said, just adding in the chart for reference sake.


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## riptide991 (Feb 1, 2012)

gilmourr said:


> You can have presynaptic receptor occupancy? I thought receptors were only part of post synaptic. I can see Olanzapine raising DA through antagonism at 5HT2C, but maybe it's possible that while olanzapine is raising my CNS levels of DA (I do feel more motivated and enjoy things more) that it's also lowering levels of DA in my peripheral body. Or maybe it's just the pure increase in prolactin from olanzapine.
> 
> I read your journal about prolactin being comparable to placebo after week 6 or 8, so maybe I'll stick with 2.5 mg instead of 5 for 6 weeks and see. I'm talking to my psych today. Besides allowing me to concentrate it's only had that effect after 10 days. Side effects are still immense day time tiredness, sex drive lowered, weight gain, acne, and I'm still waiting on some help with anxiety.
> 
> EDIT: Do you have a journal that shows approximately when receptor occupancy creates an action? How much % is usually needed? If we look at SSRI's I know it's usually between 60-80%


No you can have presynaptic occupancy which studies for olanzapine/abilify exist to show.

I just think you are jumping to the wrong conclusion. It's not likely the prolactin but simply you gaining weight. Many people gain weight in that area without any drugs. You waiting for the prolactin to die down in 6 weeks will likely not change your moobs. They may even get worse if the drug is making you consistently gain weight.

No journal for that, but even for wellbutrin studies it was hypothesized that it won't do anything for you until you hit 60% occupancy which wellbutrin can't do. So 60% seems to be the magic number for a number of things hehe.


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## gilmourr (Nov 17, 2011)

jim_morrison said:


> Not arguing with what he said, just adding in the chart for reference sake.


Didn't mean it like that lol. Not trying to start a fight


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> No you can have presynaptic occupancy which studies for olanzapine/abilify exist to show.
> 
> I just think you are jumping to the wrong conclusion. It's not likely the prolactin but simply you gaining weight. Many people gain weight in that area without any drugs. You waiting for the prolactin to die down in 6 weeks will likely not change your moobs. They may even get worse if the drug is making you consistently gain weight.
> 
> No journal for that, but even for wellbutrin studies it was hypothesized that it won't do anything for you until you hit 60% occupancy which wellbutrin can't do. So 60% seems to be the magic number for a number of things hehe.


Yeah it might be weight gain.. But I've put on weight with remain... A lot of weight and it never went to my boobs.

Only nardil and zyprexa have done this.

Anyways my psych told me it's unhealthy to gain that much eight so we're moving to another antipsychotic. It's her choice now.

Geodon and saphris both look really good. Risperidone looks like the worst since it has tight affinity with d2,3.

My preference is saphris then latuda then geodon then risp.

I NEED THAT 5ht2c!


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## riptide991 (Feb 1, 2012)

Yah I wanted to try Saphris after olanzapine screwed my blood sugar but it's brand name only and would probably cost me a small fortune with how it's still under patent. Good luck! It's got the 5-ht6 antagonism that i love from olanzapine so should still keep your focus/concentration increased.


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## gilmourr (Nov 17, 2011)

So... Oddly my psychiatrist didn't give me a new med. Waiting until next Thursday, which sucks because I feel awful being off of zyprexa. It should balance out over the next few days but right now I feel pretty darn depressed. 

I guess I'll just keep sedating myself with seroquel...


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## gilmourr (Nov 17, 2011)

Put on 5 more pounds. At +27 now. Feel like there's someone sitting on my chest and I'm so tired.

Going on a hunger strike of celery, and coffee (no sugar)


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## riptide991 (Feb 1, 2012)

gilmourr said:


> Put on 5 more pounds. At +27 now. Feel like there's someone sitting on my chest and I'm so tired.
> 
> Going on a hunger strike of celery, and coffee (no sugar)


Maybe you just put on weight from antihistamines in general. That's why mirtazapine puts it on for people. May not be anything to do with blood sugar on olanzapine.

So yah even Saphris though will have histamine effect. Maybe you should stay away from anything with antihistamine blockade, including TCAs.


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## gilmourr (Nov 17, 2011)

kehcorpz said:


> Maybe you just put on weight from antihistamines in general. That's why mirtazapine puts it on for people. May not be anything to do with blood sugar on olanzapine.
> 
> So yah even Saphris though will have histamine effect. Maybe you should stay away from anything with antihistamine blockade, including TCAs.


I don't believe saphris or geodon hit h1 well though so I should be fine. Olanzapine is in a class of its own. Also, seroquel didn't cause weight gain.

Even remeron didn't make me gain this much. It was like +15 over 8 weeks. Olanzapine is like 25+ over 2 weeks. My metabolism has changed or something.


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## jim_morrison (Aug 17, 2008)

kehcorpz said:


> Maybe you just put on weight from antihistamines in general. That's why mirtazapine puts it on for people. May not be anything to do with blood sugar on olanzapine.
> 
> So yah even Saphris though will have histamine effect. Maybe you should stay away from anything with antihistamine blockade, including TCAs.


AFAIK weight gain is mainly due to inverse agonism at histamine and 5-HT2c receptors. Saphris acts more like an antagonist rather than an inverse agonist at these receptors which is why it purportedly seems to have a low incidence of weight gain.



> Weight gain is a further concern of antipsychotic treatment of bipolar disorder which is particularly severe with olanzapine. Histamine H1, alpha1 adrenergic and particularly 5-HT2C receptors are implicated in this effect, although the lower propensity for weight gain shown by asenapine which, like olanzapine, binds to these receptors, indicates that other protective receptor mechanisms, or subtle differences in the 5-HT2C receptor-mediated effects, may be important.


http://www.bioportfolio.com/resourc...n-in-bipolar-disorder-focus-on-asenapine.html



> It is perhaps surprising that asenapine shares the high relative affinities at 5-HT2C and H1 receptors of clozapine and olanzapine yet avoids inducing the profound weight gain associated with these drugs; in bipolar patients asenapine showed a mean increase of 1.9kg _vs_ 4.1kg with olanzapine over 12 weeks [McIntyre _et al_. 2009]. While effects on 5-HT1B and/or 5-HT1A receptors could conceivably contribute, asenapine administration demonstrates a notable lack of effect on 5-HT2C receptor density in rat brain [Tarazi _et al_. 2010]. This is similar to that of the weaker antagonists risperidone and quetiapine and is in contrast to the down-regulation seen with olanzapine [Tarazi _et al_. 2002]. The difference could conceivably relate to a 5-HT2C antagonism by asenapine in the absence of the inverse agonism exhibited by olanzapine and clozapine.


http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3736908/


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## gilmourr (Nov 17, 2011)

jim_morrison said:


> AFAIK weight gain is mainly due to inverse agonism at histamine and 5-HT2c receptors. Saphris acts more like an antagonist rather than an inverse agonist at these receptors which is why it purportedly seems to have a low incidence of weight gain.
> 
> http://www.bioportfolio.com/resourc...n-in-bipolar-disorder-focus-on-asenapine.html
> 
> http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3736908/


I had no idea that olanzapine was an inverse antagonist at both H1 and 5HT2C. That would make perfect sense as to why it's so sedating and why it puts on so much weight. That and it messing up peoples' metabolism.

Thanks for the commentary.


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## jim_morrison (Aug 17, 2008)

gilmourr said:


> I had no idea that olanzapine was an inverse antagonist at both H1 and 5HT2C. That would make perfect sense as to why it's so sedating and why it puts on so much weight. That and it messing up peoples' metabolism.


Yeah I mean as far as I know even SSRI's will cause some degree of weight gain in the long term via down-regulation of 5HT2C receptors (inverse agonists also cause receptor down regulation as mentioned in previous post). This may be why Prozac (being an 5HT2C antagonist) causes the least amount of weight gain of the SSRI class, since it's theoretically preventing receptor down regulation.


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## gilmourr (Nov 17, 2011)

Hopefully 7 days is enough to level out a bit as I've got stuff going on next weekend and right now I feel dead. Even though it didn't improve my depressive symptoms much it seems to be depressing the hell out of me coming out of my system.

Also is making me spacey.


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## gilmourr (Nov 17, 2011)

Coming off Zyprexa reminds me how bad my depression was. It must be a combination of coming off of it and putting on weight because I'm so lazy, I feel like doing nothing, I'm not interested in talking to anyone and it's just a big waiting game.

I've been pushing myself to burn about 500 cal/day and stay on a super strict diet. Been consuming <1500 cal/day for the past 2-3 days, then binged an entire banana loaf this morning. Cringe worthy. 

Zyprexa must still be in my system because my hands are still quite dry which I'm guessing is from the strong mACH antagonism. 

Push ups, cardio, push ups, cardio, crunches. Anything just to get my heart rate at 160-180 bpm.


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