![[dr. bob]](/dr-bob-sm.gif)
Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 7 of 7. This is the beginning of the thread.
Posted by psychobot5000 on October 1, 2009, at 18:10:41
Hi,
For the last few weeks I've been taking betahistine, the H3 antagonist, help with my executive/cognitive dysfunction. I was tipped off to the possibility of using an H3 antagonist because my allergies severely exacerbate my cognitive issues. So far I believe I've noticed a decrease in daytime sleepiness, which is helpful.
2 questions:
Safety? How safe is this medication? I take it during the day, and then take H1 antagonists like benadryl and doxylamine as sedatives before bed.Secondly, anyone know if there's actually a valid rationale for taking this medication in the first place for cognitive dysfunction?
Thanks,
Psychbot
Posted by desolationrower on October 1, 2009, at 23:41:02
In reply to betahistine for cognitive dysfunction (safety etc?, posted by psychobot5000 on October 1, 2009, at 18:10:41
well some other h3 antagonists have been studied for ahdd
-d/r
Posted by psychobot5000 on October 2, 2009, at 0:49:20
In reply to Re: betahistine for cognitive dysfunction (safety, posted by desolationrower on October 1, 2009, at 23:41:02
> well some other h3 antagonists have been studied for ahdd
>
> -d/rTrue--yet it's interesting that no one seems interested in this one for that purpose, isn't it?
Posted by Rosy Crucifiction on February 23, 2010, at 21:13:19
In reply to Re: betahistine for cognitive dysfunction (safety, posted by psychobot5000 on October 2, 2009, at 0:49:20
There is some very interesting work out about this now. There is a clinical trial of Betahistine at U of Cincinnati for Atypical Depression. A long and illuminating article discusses the the apparent functioning. Abstract here, link to full article below. FYI, the medication is available by prescription in Europe and Canada. It is inexpensive.
"Histamine H3 Receptor Antagonists: Preclinical Promise for Treating Obesity and Cognitive Disorders1. Timothy A. Esbenshade,
2. Gerard B. Fox and
3. Marlon D. Cowart+ Author Affiliations
1.
Division of Neuroscience Research, Global Pharmaceutical Research and Development, 100 Abbott Park Road, Abbott Park, IL 60064
Next Section
AbstractThe histamine H3 receptor is an attractive G proteincoupled receptor drug target that regulates neurotransmission in the central nervous system and plays a role in cognitive and homeostatic functions. Drug discovery efforts by numerous pharmaceutical companies have focused on the preclinical development of H3 receptor antagonists for the potential treatment of attention-deficit hyperactivity disorder, dementias, schizophrenia, as well as obesity and sleep disorders. This receptor exhibits molecular, pharmacological, and functional heterogeneity that informs the preclinical development of effective antagonists. Herein, we describe the biological and chemical implications for developing H3 receptor antagonists and their therapeutic potential as disclosed through animal models of cognition, sleep, and obesity.
Previous SectionNext SectionGraphic
Since the original description of the histamine H3 receptor as a presynaptic autoreceptor that inhibits histamine release, there has been considerable effort to develop potent and selective H3 receptor antagonists for the potential treatment of a variety of disorders affecting cognition (Attention Deficit Hyperactivity Disorder, Alzheimer Disease, and schizophrenia), sleep (hypersomnia and narcolepsy), and homeostasis (obesity). We review some of the preclinical considerations, from both an H3 receptor biology as well as a more general drug discovery perspective, that need to be taken into account in developing effective H3 receptor antagonists for the treatment of these diseases."
Posted by Rosy Crucifiction on February 23, 2010, at 21:21:00
In reply to Re: betahistine for cognitive dysfunction (safety, posted by Rosy Crucifiction on February 23, 2010, at 21:13:19
Good news for a lot of folks if this works. I can't think of a good reason to wait for approval to try it. Both drugs are approved in most of the world. Still in early phase 2.
"Obecure granted patent covering betahistine with olanzapine for mitigating antipsychotic drug associated weight gain
23. February 2010 04:03Obecure Ltd., a subsidiary of Bio-Light Israeli Life Science Investments Ltd. (TASE:BOLT), has received notice of allowance from the US Patent Office for its two key patent applications covering methods of use and compositions covering the use of betahistine with olanzapine for the mitigation of the serious weight gain associated as a side effect of the antipsychotic drug.
The commercial opportunity of adjunctive Histalean® therapy, to enable
Obecure is focused on development of Histalean® (high dose betahistine) as adjunctive to antipsychotic drug therapy for improved treatment of schizophrenia, bipolar disorder and major depression. Obecure has recently announced the outcomes of randomized, placebo controlled Phase 1b and pilot Phase 2 trials, showing that co-administration of Histalean® with olanzapine (Zyprexa®), safely and significantly reduced weight gain and somnolence, two of the most serious side effects associated with this drug, as with most of the second generation antipsychotics as a drug class, also including risperidone (Risperdal®), quetiapine (Seroquel®) and aripiprazole (Abilify®).
These antipsychotic drugs are widely used to relieve symptoms of serious psychiatric diseases including schizophrenia, bipolar disease and major depression with cumulative prevalence >5% and early onset in adolescence and even childhood. However, in recent years there has been growing concern of regulators and practitioners about these drugs induction of weight gain. Recent publications suggest that olanzapine causes an average weight gain of about 8 kg in just 12 weeks. This not only reduces patients compliance, but also exposes them to metabolic syndrome, diabetes and cardiovascular disorders; a concern which has resulted in FDAs issuance of black box warnings, and which has greatly affected prescription decisions. Moreover, daytime sleepiness (somnolence) induced by these drugs is seriously impacting patients quality of life prohibiting driving, hampering their ability to hold jobs and/or continue with their education.
The allowance of our leading US patents validate the novelty and practicality of our approach and are serving as the initial milestone in our evolving intellectual property said Dr. Yaffa Beck, CEO of Obecure, adding that Olanzapine is considered the most effective of the first line antipsychotic drugs, but is also known to cause substantial weight gain. It is thus the first drug we focused on. The patent portfolio includes applications pending worldwide, covering methods and compositions of betahistine for management of weight and somnolence that are secondary side effects of most psychiatric drugs.
Histalean® is comprised of betahistine dihydrochloride, a centrally active dual action pro-histamine. Betahistine is an agonist of type 1histamine receptors and an inverse agonist (inhibitor) of type 3 histamine receptor (the negative autoregulatory receptor of histamine), acting in concert to activate the histamine system, which downregulates feeding and enhances alertness and cognition. Based on the highly safe generic drug, approved since the 1960s in >100 million patients suffering from Ménières disease (vertigo) in most countries; it is unavailable in the US, where, although safety was not doubted, it was withdrawn by the FDA in 1972 for insufficient data of efficacy in Menieurs.
The Company has recently extended its clinical supply agreement with Grunenthal-Italy to include higher dose extended release formulations of betahistine and is planning to initiate follow-on escalating dose clinical trials this year. "The commercial opportunity of adjunctive Histalean® therapy, to enable "safer" antipsychotic treatment is clear, considering the annual turnover of $15 billion in this market, says Dr. Ami Eyal, CEO of Bio-Light, the major investor in Obecure, adding that we are currently seeking financial and pharmaceutical partners to assist us to achieve this challenge.
SOURCE Bio-Light Israel Life Science Investments Ltd."
Posted by psychobot5000 on February 27, 2010, at 12:38:32
In reply to Re: betahistine for zyprexa weight gain + fatigue, posted by Rosy Crucifiction on February 23, 2010, at 21:21:00
Very interesting--let's hope it works!
Posted by desolationrower on March 3, 2010, at 1:39:54
In reply to betahistine for cognitive dysfunction (safety etc?, posted by psychobot5000 on October 1, 2009, at 18:10:41
i think there was some interaction whereby you would take a much lower dose if also running an MAOI, i think i posted it before. maybe some risk of anxiety, like most any stimulant
-d/r
This is the end of the thread.
Psycho-Babble Medication | Extras | FAQ
Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.org
Script revised: February 4, 2008
URL: http://www.dr-bob.org/cgi-bin/pb/mget.pl
Copyright 2006-17 Robert Hsiung.
Owned and operated by Dr. Bob LLC and not the University of Chicago.