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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 18 of 18. This is the beginning of the thread.
Posted by Lamdage22 on February 7, 2018, at 13:20:43
https://en.wikipedia.org/wiki/Lumateperone
It sounds pretty freakin awesome. What do you guys think?
Posted by SLS on February 7, 2018, at 14:11:50
In reply to Lumateperone, posted by Lamdage22 on February 7, 2018, at 13:20:43
> https://en.wikipedia.org/wiki/Lumateperone
>
> It sounds pretty freakin awesome. What do you guys think?Lumateperone is a very interesting drug. Thanks for posting the article.
What I noticed in the article:
The drug is a partial agonist of D2 autoreceptors (like Abilify), but a full antagonist at postsynaptic D2 receptors (unlike Abilify). It will be interesting to see if lumateperone is as effective for depression as is Abilify. If not, it would still be valuable to treat psychotic disorders because it appears to be less apt to produce movement EPS and akathisia side effects. It is also touted as producing no metabolic changes or weight gain.
I may give this thing a try if it proves effective for major depressive disorder or bipolar depression. My main motivation for switching from Abilify to something else is that Abilify produces major weight gain. Also, my triglycerides on Abilify is about 450 milligrams per deciliter. The normal value is 150 or less.
- Scott
Posted by Jeroen on February 8, 2018, at 6:13:17
In reply to Re: Lumateperone » Lamdage22, posted by SLS on February 7, 2018, at 14:11:50
ITI-007
Abilify and Seroquel are causing high tryglycerines in me too i need from today, i am trying not to eat fatty foods
Posted by Lamdage22 on February 8, 2018, at 6:45:49
In reply to Re: Lumateperone - SLS, posted by Jeroen on February 8, 2018, at 6:13:17
For the meantime i would recommend Metformin for that with regular kidney checks.
Posted by Lamdage22 on February 8, 2018, at 6:55:14
In reply to Re: Lumateperone » Lamdage22, posted by SLS on February 7, 2018, at 14:11:50
Those are the three things i am looking forward to. Naltrexone, Lumateperone and Rapastinel. Also i just found out the professional rehab facility is MOVING from the 3rd floor to the first. That means i can visit it without the fear of heights that i have from 2nd floor up.
All good news! How about that?
Posted by SLS on February 8, 2018, at 7:51:30
In reply to Re: Lumateperone, posted by Lamdage22 on February 8, 2018, at 6:55:14
> Those are the three things i am looking forward to. Naltrexone, Lumateperone and Rapastinel.
LDN? That's an interesting combination of medication. What is your rationale for choosing them?
> Also i just found out the professional rehab facility is MOVING from the 3rd floor to the first. That means i can visit it without the fear of heights that i have from 2nd floor up.
>
> All good news! How about that?You can use some good news for a change.
- Scott
Posted by Lamdage22 on February 8, 2018, at 8:12:11
In reply to Re: Lumateperone » Lamdage22, posted by SLS on February 8, 2018, at 7:51:30
> > Those are the three things i am looking forward to. Naltrexone, Lumateperone and Rapastinel.
>
> LDN? That's an interesting combination of medication. What is your rationale for choosing them?Well Naltrexone and Rapastinel because they lack sexual side effects. Lumateperone because it lacks metabolic side effects. I have that appointment with the LDN experienced Doc on 19th February.
Naltrexone may actually enhance sex at low doses.> > Also i just found out the professional rehab facility is MOVING from the 3rd floor to the first. That means i can visit it without the fear of heights that i have from 2nd floor up.
> >
> > All good news! How about that?
>
> You can use some good news for a change.Thanks, Scott:)
> - Scott
Posted by PeterMartin on February 8, 2018, at 19:37:20
In reply to Re: Lumateperone - SLS, posted by Lamdage22 on February 8, 2018, at 6:45:49
> For the meantime i would recommend Metformin for that with regular kidney checks.
Thanks for the post on this med. I will definitely start following its progress.
I love how you always advocate for metformin. I started taking it last month when I began Nardil. I'm only on 1000mg now (plan to get to 1500/2000) but your comments have me optimistic that it'll offset the weight gain commonly associated with Nardil.
I really hope so. Other people having success with meds always makes me feel more optimistic.
Posted by Lamdage22 on February 9, 2018, at 6:13:04
In reply to Re: Lumateperone, posted by Lamdage22 on February 8, 2018, at 8:12:11
How high would be the tardive dyskinesia and tardive dementia risk with Lumateperone?
Posted by Christ_empowered on February 10, 2018, at 2:34:36
In reply to Re: Lumateperone. TD andTdem risk?, posted by Lamdage22 on February 9, 2018, at 6:13:04
hi lamdage
its hard to predict td rates. animal studies are one thing...pump one monkey full of haldol, another full of the new drug, see what happens...what people...whole different ball game.
Posted by Lamdage22 on February 10, 2018, at 16:00:50
In reply to Re: Lumateperone. TD andTdem risk?, posted by Christ_empowered on February 10, 2018, at 2:34:36
i see. They said no EPS which sounds good. I wonder if it can be megadosed. But we shouldnt rely on meds that are not out yet. We dont know what what will happen. Life with mental problems is a marathon.
Posted by Lamdage22 on February 16, 2018, at 3:26:06
In reply to Re: Lumateperone. TD andTdem risk?, posted by Christ_empowered on February 10, 2018, at 2:34:36
Hey yall,
Can anyone explain what Lumateperone does to dopamine receptors, especially at high dosages?
thx
Lamdage
Posted by undopaminergic on December 24, 2019, at 7:49:42
In reply to What does Lumateperone do to dopamine receptors?, posted by Lamdage22 on February 16, 2018, at 3:26:06
> Hey yall,
>Hi.
> Can anyone explain what Lumateperone does to dopamine receptors, especially at high dosages?
>It blocks them. All antipsychotics so far approved for marketing block dopamine receptors. Even clozapine, which is given for psychosis in Parkinson's disease because it is a particularly mild dopamine antagonist, especially compared to such drugs as haloperidol.
-undopaminergic
Posted by revv33 on December 25, 2019, at 13:01:10
In reply to Re: What does Lumateperone do to dopamine receptors? » Lamdage22, posted by undopaminergic on December 24, 2019, at 7:49:42
Do you guys think Lumateperone will have less sexual side effects? Does it block less dopamine then abilify or current antipsychotics?
Posted by Lamdage22 on December 25, 2019, at 17:30:09
In reply to Re: What does Lumateperone do to dopamine receptors?, posted by revv33 on December 25, 2019, at 13:01:10
That's a good question. Luckily I don't have any sexual side effects from Antipsychotics.
Posted by greg rizzo on January 9, 2020, at 20:42:15
In reply to Re: What does Lumateperone do to dopamine receptors? » Lamdage22, posted by undopaminergic on December 24, 2019, at 7:49:42
jUST SOME BABBLE FROM THE NET. mY IMPRESSION IS THAT IT IS MAINLY INTENDED FOR SCHITZOPHREIA, BUT YES DOES INCREASE DOPAMINE. WHAT DOSAGE? UNSURE
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Intra-Cellular Therapies announced early Monday morning lumateperone (CAPLYTA) had received approval from the FDA and the company expects the treatment to be available in late Q1 2020.
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Mechanism of action
Lumateperone affects multiple systems (serotonergic, dopaminergic and glutamatergic) in the central nervous system. It acts as a antagonist of 5HT2A 0.54nM receptor and modulates D1 4.1nM and D2 3.2nM dopamine receptors where it is a partial agonist at presynaptic and antagonist at postsynaptic receptors. Serotonin transporters at 3.3nM. Through the mTOR pathway, lumateperone aguments both NMDA and AMPA activity. Because of its complex pharmacology, it is not clear which of these activities are primarily responsible for its antidepressive and antipsychotic activities.[14]
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. With approximately 2.4 million adults with schizophrenia in the United States, the potent serotonin 5-HT2A receptor antagonist, a DPPM acting as a presynaptic partial agonist and postsynaptic antagonist at dopamine D2 receptors, a dopamine D1 receptor-dependent indirect modulator of glutamate, and a serotonin reuptake inhibitor represents a new option to meet the ongoing unmet need for treatments.
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Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia.1 It has a unique receptor binding profile and differs from other antipsychotics in that it modulates glutamate, serotonin and dopamine, which are all neurotransmitters that contribute to the pathophysiology of schizophrenia.1,5The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia.1 Further, not only is the new antipsychotic selective for dopamine (D2) receptors in the mesolimbic and mesocortical brain regions, but it also has minimal off-target activity
Posted by Lamdage22 on January 10, 2020, at 2:53:42
In reply to Re: What does Lumateperone do to dopamine receptors?, posted by greg rizzo on January 9, 2020, at 20:42:15
Thanks for posting. I already take low dose Trazodone and low dose Venlafaxine. I wonder if I would get Serotonin Syndrome with Lumateperone. Does it have sexual side effects?
Posted by revv33 on January 10, 2020, at 5:42:41
In reply to Re: What does Lumateperone do to dopamine receptors?, posted by greg rizzo on January 9, 2020, at 20:42:15
> jUST SOME BABBLE FROM THE NET. mY IMPRESSION IS THAT IT IS MAINLY INTENDED FOR SCHITZOPHREIA, BUT YES DOES INCREASE DOPAMINE. WHAT DOSAGE? UNSURE
> -----------------------------------------------
> Intra-Cellular Therapies announced early Monday morning lumateperone (CAPLYTA) had received approval from the FDA and the company expects the treatment to be available in late Q1 2020.
> -------------------------------------------------------------------------
> Mechanism of action
> Lumateperone affects multiple systems (serotonergic, dopaminergic and glutamatergic) in the central nervous system. It acts as a antagonist of 5HT2A 0.54nM receptor and modulates D1 4.1nM and D2 3.2nM dopamine receptors where it is a partial agonist at presynaptic and antagonist at postsynaptic receptors. Serotonin transporters at 3.3nM. Through the mTOR pathway, lumateperone aguments both NMDA and AMPA activity. Because of its complex pharmacology, it is not clear which of these activities are primarily responsible for its antidepressive and antipsychotic activities.[14]
> ----------------------------------------------------------------------------
> . With approximately 2.4 million adults with schizophrenia in the United States, the potent serotonin 5-HT2A receptor antagonist, a DPPM acting as a presynaptic partial agonist and postsynaptic antagonist at dopamine D2 receptors, a dopamine D1 receptor-dependent indirect modulator of glutamate, and a serotonin reuptake inhibitor represents a new option to meet the ongoing unmet need for treatments.
> -----------------------------------------------------------------
> Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia.1 It has a unique receptor binding profile and differs from other antipsychotics in that it modulates glutamate, serotonin and dopamine, which are all neurotransmitters that contribute to the pathophysiology of schizophrenia.1,5
>
> The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia.1 Further, not only is the new antipsychotic selective for dopamine (D2) receptors in the mesolimbic and mesocortical brain regions, but it also has minimal off-target activityThanks for the reply, what is meant by "minimal off-target activity"?
This is the end of the thread.
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