First generation agents / FGAs / neuroleptics / old antypsychotics

For a while it was believed that I had treatment-resistant, intractable Bipolar I w/ psychotic features, with 3 sui attempts in history. Usually with intractable, Clozapine is prescribed, but I could not tolerate even the tiniest doses of Clozapine because it made me debilitatingly depressed, to the point of physical immobility. Then I became resigned to the fact that only Zyprexa works. And it did for a while, Zyprexa in combo with Gabapentin. I was on it for 4 years, mostly stable, with horrible metabolic side effects (prediabetes, severe sleep apnea, non-alcoholic fatty liver disease, abdominal adiplosity), but those started to get gradually reversed when I added Ozempic, Topamax, Provigil to the mix. I also upgraded from regular Zyprexa to Lybalvi, although I am not sure it conferred any benefit, since I still was ravenously hungry on it and still needed Ozempic, Topamax, Provigil to reduce the insanely strong hunger caused by Zyprexa.

Unfortunately, Zyprexa also makes it hard for me to think strategically, which is a big problem at my current management job. Just recently I stopped Zyprexa (Lybalvi, to be exact, which is Zyprexa plus another ingredient) for two days and during those two days I had two very simple good ideas about something at work and these ideas should have come to me much earlier: they should have long been obvious to me. So it is as if I were blocked from access to obviously good ideas, not some unusually good, some genius ideas, on Zyprexa. I want to fight for my job, for the opportunity to be successful, and Zyprexa is in the way.

Also on Zyprexa I have no sexual thoughts, even though I am mechanically able to reach clitoral orgasm. This antisexual effect of Zyprexa has accumulated over time: it has not always been that bad, but over the past year it has been. Again, during 2 days off Zyprexa recently, sexual thoughts started coming to me. Similarly, in April 2022, I tried Asenapine instead of Zyprexa and instantly had wonderful sexual thoughts. Unfortunately I stopped sleeping and had to go back to Zyprexa in order to get sleep.

Lastly, I used to write creatively and on Zyprexa I just cannot. I can jot down some plans, skeletons for future writing but I cannot get into the flow of the actual writing process and I cannot generate metaphor. During the recent 2 days of Zyprexa, internal writing process resumed and my memories become three dimensional and very interesting, as before. On Zyprexa, the world is sort of flat. In November 2021, I tried Vraylar and again the internal writing process resumed, was wonderful and I came up with highly metaphoric speech, had highly sexual thought content, but then stopped sleeping, realized that this would devolve into mania and begrudgingly went back to Zyprexa.

The only modern Antipsychotic I have not tried is Latuda. I will try it, but have low hopes, since I am afraid it will send me into mania and/or anxiety.

My psychiatrist recommends trying old antipsychotics. I have tried low doses of Haldol and Thorazine and they are not enough to make me sleep. By myself, without medications, I am completely unable to sleep and this has been going on for 10 years if not more. I have not tried higher doses of Haldol and Thorazine.

Maybe there are other first generation agents (FGAs) to try. For several years I was afraid of FGAs but now I am willing to try anything because I see that I have exhausted the options with modern antipsychotics.

Sorry for lengthy prose and hopeful that I will hear from people who have been courageous enough to try old medications. Note that I have tried Lithium, Tegretol, Lamictal, Depakote, so those options are a no go for me.

I have virtually no experience with Haldol, except an emergency injection while inpatient. It did help quickly ease a psychotic event. If they used it again during later cases, I don't know. I think more often they used Ativan alone. Could be wrong. The only first generations I took for any length of time were thiothixene (Navane) and perphanazine (Trilafon).

Thiothixene was no powerhouse drug for me, though I think it did no extra harm. The only side effect from that was eventual (not immediate) minor involuntary movement of my lips (dystonia), which concerned my pdoc enough to discontinue it. It was not sedating, so helped me little with sleep. Another issue was difficulty getting certain dose pills of it from pharmacies. I think it was being phased out. Not sure what its status is now.

Perphanazine seemed far more effective. I likely took it only for a few months, though. I wanted off because I started to gain weight fast on it, though many people I know didn't. It was also not that sedating, or at least that side effect doesn't stand out in my memory. To my knowledge this med is still used and available.

I took a small dose of Latuda for maybe six months, some years back. It was no anti-manic for me and prescribed more for depression. I was taken off and did fine off of it. I can't comment further on it.

I take haldol twice daily. Helps me!!

I take abilify and Thorazine together.

What do you class as low dose Thorazine? I was on 200mg and it helped me sleep after coming off Seroquel which is similar to Zyprexa sleep wise. I don’t know if you class that as low dose though. I’m not sure what the normal dose is.

I’m also a person who can’t sleep without chemical help - and a lot of it.

I take thorazine along with my abilify and other meds, helps me a lot and I haven't had any issues with it. I take 200mg of the thorazine. I used to be on 400mg of it but was sleeping too much on that dose so my psychiatrist lowered it for me

Welcome to the forum @Tart Cherry Jam.

I'm not exactly sure what you're hoping for with regard to medication. Do you want a med that will help you sleep without the metabolic and sexual side effects?

I cannot take credit for being brave enough to try the older AP's, I'm just old enough to have been prescribed the older AP's because they were the only available meds back then. In the past I was on Navane, Stelazine, Thorazine, Haldol, Mellaril, and there were a couple of others I can't recall the names of.

I remember that Navane was a helpful medication for me, back many years. It was calming. But I've tried it more recently and it didn't seem to do anything.

I've been on several of the new (atypical) AP's. Seroquel has had a terribly destructive effect on my health, the same metabolic issues you have described. The only benefit I've had from the newer AP's (Seroquel, specifically) is that is a very low dose it helps me sleep.

In my decades of being on psych meds very few help me sleep. I think lithium does and, as I mentioned, Seroquel (low dose) dose help me sleep.

I suppose that the older AP's in knock-out doses would put me out, but being able to function on that level of medication would be hard.

As for the sexual issue, I believe that all psych medications have an effect of sexual function. I think it's especially noticeable when we're manic and hyper-sexual, then medication interferes with that.

I wish I could offer more help. I think that many of us with bipolar disorder share your struggles.

Have you been on loxapine? It is something like a between the atypicals and first generation. It has a neat trick that as it breaks down it turns into an anti-depressant so that can boost you if you need that. It also has a big range of dosing which is nice. I didn't have side effects until I developed uncontrollable mouth movements and had to come off it (this is very rare).


I liked it,actually quite a lot, until I couldn't tolerate it. Which is just the way meds are for me. Nothing worked very well until clozapine and you said that's not an option for you which is too bad.

I hope you find something that works soon.

Thank you for the answers! I see that quite a few people have been on these drugs and it alleviates my concerns.

Interesting about Loxapine: Loxapine is extensively metabolized in the liver through aromatic hydroxylation, N-demethylation, or N-oxidation. The metabolite amoxapine is active and marketed as an antidepressant. Loxapine is widely distributed throughout the body, including the central nervous system.
I do not generally need an antidepressant boost: I receive enough of antidepressant action from Gabapentin (somewhat of an idiosyncratic reaction, I know, but I do love my Gabapentin) and in general tend to have more concerns on the manic side of things. But I still would like to try it: maybe it would work just fine without throwing me into mania. I have had episodes of uncontrollable mouth movements (especially tongue movements) a few times when I combined two modern APs, but as soon as I discontinued the combos, the movements stopped. So I would know to discontinue a drug if it starts causing those movements.

I have gone through my records and discovered that at some point in late 2014 I took azaleptin, which was sent to me by my friend oversees. I took it for sleep and it caused tremendous sleepiness, so I discontinued. It did not cause depression. I now see that azaleptin is clozapine, another name for it. So in 2018 I could not tolerate it, but in 2014 I was fine and it just made me very sleepy, but isn't it what I need now? So I will try it again. I have noticed that sometimes the same medication has a different effect. I have tried Topamax several times in my life. I now tolerate it well, taking it for appetite suppression, but in the past it would cause general malaise, or depression, or dizziness. So I realize that it is not all straightforward, it is not that Med A always causes effect or side effect B in the same person. It is more complicated and I should retry Clozapine to see if this time around it might do the trick for me.

Yes, I want a med that will help me sleep without metabolic side effects, sexual side effects, and creative/intellectual side effects. Believe me, I realize this is a tall, tall order! We do share the struggles!

I recently took 400 mg Seroquel ER plus 25 mg Seroquel (regular, not ER). Did nothing for my sleep at all. I could not fall asleep and had to reach out for Zyprexa. You reminded me that Seroquel is sedating at small doses, not large ones. I will try again to see if very little Seroquel might do the sleep trick for me.

I tried something in the vicinity of 30-50 mg of thorazine.

I will try 200 mg. 200 mg is still pretty low dose. The highest dose is 1 g. 800 mg is considered high dose.

How much do you take for bipolar?

I have tried small doses. Very small, 0.5 mg, several pills. Did not help me sleep, but I am a migraineur and I discovered that it stops migraine attacks. Was very thankful for that discovery.

thank you for the answers and listing a few new names. I will research them. I see quite a few people take these medications or took them in the past, being old enough or because these medications are still good options. I am less scared of them and more trusting. Thankful that those old pills are still in the toolbox for us. Will post on the progress of my experimenting.

Quote:

Originally Posted by Tart Cherry Jam ... I have noticed that sometimes the same medication has a different effect. I have tried Topamax several times in my life. I now tolerate it well, taking it for appetite suppression, but in the past it would cause general malaise, or depression, or dizziness. So I realize that it is not all straightforward, it is not that Med A always causes effect or side effect B in the same person. It is more complicated and I should retry Clozapine to see if this time around it might do the trick for me.

I have found that to be absolutely true. A med may work/not work have side effects/not have side effects at different times in one's life. I think that even seasons can cause varying effects.

I think clozapine is worth another shot. I have heard many good things.

About sexual side effects, a lot of anti-depressants cause the same issues, often inability to have an orgasm.

I take 5mg in am and 10mg at bedtime. I sleep well

I've only been on the LAI version of haldol (250mg, I think that's the equivalent of about 10mg a day) and it caused terrible akathisia and insomnia, but worked wonders for psychosis. I take 100mg of thorazine and it helps some to fall asleep some nights, but even on those nights I wake up at 1am

Oh, to have akathisia on a LAI must have been awful!

I took 100 mg Thorazine last night (and also took Benadryl and 40 mg Latuda). Fell asleep, then woke up in the middle of the night twice and even ate at 4 AM. Fell back to sleep. But then, during the day, slept and had wild dreams for most of the day and also was majorly lightheaded. It was also hard to talk, to move my mouth to make words.

I will try it again tonight, this time without Benadryl.

I must say, it feels miraculous to be able to sleep without Zyprexa, and I am hoping that my body will accommodate to Thorazine.

That doesn’t sound good!

I have talked to the psychiatrist and will be lowering from 100 mg to 50 mg tonight. Hopefully with experimentation will find a sweet spot!

I have dropped to 50 mg Thorazine.

Had Akathisia. Increased Gabapentin from my usual 900 mg to 1800 mg and Akathisia went away.

I am sleeping almost all the time and my dreams are so interesting! they go so deep into my life history and psyche. Wow!

Sounds like things are going better.

I have to not be sleeping all day long tomorrow! I need to be at my neurologist's office at 2PM. Thinking about titrating Thorazine down a bit tonight to ensure I make the neuro visit which I cannot afford to skip.

50-60 mg and I am able to sleep, but not too much. I am just afraid that this will soon stop working: it has happened to me in the past that something would initially work, but soon would stop working.

That's my experience with everything that helps me sleep as well. I don't really have any answers, but know that you're not alone.