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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 10 of 10. This is the beginning of the thread.
Posted by AndrewB on February 19, 2001, at 11:21:14
If you are a smoker and ADD or bipolar disorder you may wish to ask your doctor about a trial with mecamylamine (Inversine). For smoking cessation, when combined with the nicotine patch it seems to be much more effective than the patch alone. There a couple of case reports of people with combined tourettes syndrome and bipolar who were stabilized with mecamylamine (it took away the mood swings and improved anxiety and concentration). Also supposedly some doctors have had success with it in treating ADD. This is very slim evidence but I thought that the option of trying mecamylamine might be considered since it reportedly has almost no side effects (mild constipation) at the low doses in which it is used. Seemingly it may take 3 weeks or longer to be effective for bipolar, while onset of action is within hours for ADD.
References below:
www.laytonbio.com/inversine/bipolar.pdf.
www.update-software.com/ccweb/cochrane/revabstr/ab001009.htm.
http://216.247.218.98/morehealth/8555.html.For more information refer to the article “Clinical Relevance of the Nicotine Receptor Antagonist Mecamylamine in Treating Neuropsychiatric Disorders.” Todays Therepeutic Trends. 18(3): pp.255-73, 2000.
AndrewB
Posted by JahL on February 21, 2001, at 14:07:44
In reply to Smoker with Bipolar/ADD? This new drug may help , posted by AndrewB on February 19, 2001, at 11:21:14
> If you are a smoker and ADD or bipolar disorder you may wish to ask your doctor about a trial with mecamylamine (Inversine). For smoking cessation, when combined with the nicotine patch it seems to be much more effective than the patch alone. There a couple of case reports of people with combined tourettes syndrome and bipolar who were stabilized with mecamylamine (it took away the mood swings and improved anxiety and concentration). Also supposedly some doctors have had success with it in treating ADD. This is very slim evidence but I thought that the option of trying mecamylamine might be considered since it reportedly has almost no side effects (mild constipation) at the low doses in which it is used. Seemingly it may take 3 weeks or longer to be effective for bipolar, while onset of action is within hours for ADD.
>
> References below:
> www.laytonbio.com/inversine/bipolar.pdf.
> www.update-software.com/ccweb/cochrane/revabstr/ab001009.htm.
> http://216.247.218.98/morehealth/8555.html.
>
> For more information refer to the article “Clinical Relevance of the Nicotine Receptor Antagonist Mecamylamine in Treating Neuropsychiatric Disorders.” Todays Therepeutic Trends. 18(3): pp.255-73, 2000.
>
> AndrewBHi Andrew.
You have a good track record of picking out obscure winners so naturally I'm intrigued...
Do you know of a source (prescription-free) of Mecamylamine (4 a quick ADD trial)? Even if it is available in the UK I doubt my GP will have heard of it.
Thanx,
Jah.
Posted by AndrewB on February 23, 2001, at 0:05:56
In reply to Re: Smoker with Bipolar/ADD? This new drug may help » AndrewB, posted by JahL on February 21, 2001, at 14:07:44
JahL,
I did some searching and to the best of my knowledge it is not available without an Rx anywhere.
However, if it is available in Britain, there is a good chance your physician is aware of it and comfortable with it. Let me explain. Mecamylamine (Inversine) is not a new drug. It has been around since the 1950s for the treatment of hypertension. It has only recently been realized that the drug has a very different action at doses much smaller than those used for hypertension. That is, it works as a nicotine receptor antagonist and possibly a partial agonist of those receptors. Anyway ask your doctor if it available in Britain.
Best of luck,
AndrewB
Posted by SLS on February 23, 2001, at 8:07:15
In reply to Re: Smoker with Bipolar/ADD? This new drug may help , posted by AndrewB on February 23, 2001, at 0:05:56
> That is, it works as a nicotine receptor antagonist and possibly a
partial agonist of those receptors. Anyway ask your doctor if it
available in Britain.Hi Andrew.
Can you please explain to me in detail exactly what is a "partial" agonist
compared to a full agonist?Thanks.
- Scott
Posted by SLS on February 23, 2001, at 8:28:10
In reply to Re: Smoker with Bipolar/ADD? This new drug may help , posted by SLS on February 23, 2001, at 8:07:15
I forgot. A word of caution:
Mecamylamine and other nicotinic receptor antagonists are capable or PRODUCING depression, presumably by reducing afferant output of pathways to dopaminergic areas within the limbic system, particularly in the nucleus accumbens. It is suggested that this phenomenon is what drives over 80% of schizophrenics to become heavy smokers. It feels good to them and the small improvement is measurable. They are not just bored.
By contrast, there is some work being done that indicates that nicotinic receptor agonists possess antidepressant properties.
A friend of mine was considering using mecamylamine to treat a chronobiological disturbance, but was disuaded from doing so because of its depressogenic potential. I don't know anyone who has tried mecamylamine. Do you? Was there any sign of depression or dysphoria?
- Scott
Posted by AndrewB on February 23, 2001, at 8:53:49
In reply to Re: Smoker with Bipolar/ADD? This new drug may help , posted by SLS on February 23, 2001, at 8:28:10
Scott,First in reply to your question about the diff. between a partial and full agonist:
Full agonist: An agonist which produces a maximal response by occupying all or a fraction of receptors.
Partial agonist: An agonist which produces less than a maximal response even when it occupies all of the receptors.For an excellent source of basic neuropharmocology definitions go to:
http://science.glaxowellcome.com/science/pharm_guide/Pharm_5.htm
Scott, you make a great cautionary point about nicotine antagonists being depressives. However it is my hunch that at low doses mecamylamine is actually partial agonist and only when the dosage is increased does it become an antagonist. I base this on a study that showed small doses of mecamylamine to significantly improve the memory of rats and primates, both aged and healthy. This is a trademark effect of nicotine agonists and the (surprised) researcher thus speculated that mecamyline was indeed acting as a partial agonist at those low doses.
BTW: Thank you Scott for your trademark grilling: it keeps me on my toes!
AndrewB
Posted by SLS on February 23, 2001, at 12:36:44
In reply to Re: Smoker with Bipolar/ADD? This new drug may help , posted by AndrewB on February 23, 2001, at 8:53:49
Thanks, Andrew.
I have asked everyone I could think of what is meant by a "partial agonist", but have been repeatedly disappointed. This includes psychopharmacologist and pharmacists. One doctor was even a clinical investigator studying both buspirone and gepirone! I feel pretty smart as my best guess is consistent with the definition. It is frustrating to have to guess at so many technical terms based on the context of medical literature. Guesses are just guesses, educated or not. Your URL will help me immensely.
> Scott, you make a great cautionary point about nicotine antagonists being depressives. However it is my hunch that at low doses mecamylamine is actually partial agonist and only when the dosage is increased does it become an antagonist.
> I base this on a study that showed small doses of mecamylamine to significantly improve the memory of rats and primates, both aged and healthy.
I would like to see this study. Where can I find it?
- Scott
Posted by Sunnely on February 23, 2001, at 20:32:01
In reply to Re: Smoker with Bipolar/ADD? This new drug may help » AndrewB, posted by SLS on February 23, 2001, at 12:36:44
Scott,
You may also want to check Stahl's book "Essential Psychopharmacology" 2000, 2nd ed., Cambridge University Press. He gives (as usual) clear definitions, user-friendly illustrations and analogies about "agonists" (including partial agonist and the agonist spectrum) and the "antagonists."
=========================================
> I have asked everyone I could think of what is meant by a "partial agonist", but have been repeatedly disappointed. This includes psychopharmacologist and pharmacists. One doctor was even a clinical investigator studying both buspirone and gepirone! I feel pretty smart as my best guess is consistent with the definition. It is frustrating to have to guess at so many technical terms based on the context of medical literature. Guesses are just guesses, educated or not. Your URL will help me immensely.
Posted by AndrewB on February 23, 2001, at 23:18:14
In reply to Re: Smoker with Bipolar/ADD? This new drug may help » AndrewB, posted by SLS on February 23, 2001, at 12:36:44
WASHINGTON, April 18 (UPI) - A drug used experimentally to help block the cravings of smokers and cocaine addicts also may improve memory if given in low doses. Researchers at the Medical College of Georgia found the drug mecamylamine gave 20 percent to 30 percent improvements in memory in aged monkeys as well as in non-aged rats performing different types of memory tasks. They reported their research at the Experimental Biology '99 conference in Washington, D.C. this morning.
"We're trying to develop new compounds to improve memory in animals, and eventually in humans," said Jerry Buccafusco, director of the Alzheimer's Research Center at Medical College of Georgia and the Augusta Veterans Administration Hospital. He added, "If we can predict when a person will get Alzheimer's, we can give a drug early on and delay or prevent Alzheimer's disease. Mecamylamine might offer a neuro-protective effect for Alzheimer's disease." Buccafusco and his colleagues tested Rhesus monkeys aged 20 and older on their ability to remember colors. They showed the monkey a color, and after a pause they put two colors in front of the monkey, one the same as the earlier color. They tested the monkey's ability to match one of the second set of colors to the first color.
In human Alzheimer's patients, such short-term memory goes first, he said. Buccafusco and his colleagues have been working on memory restorative drugs for about 11 years. Earlier they found that nicotine and related compounds can activate the nicotine receptors in the brain and improve the memory of aged monkeys. But nicotine has addictive side effects. So Buccafusco studied mecamylamine, a related compound that when given in high doses blocks the nicotine receptor in the brain. However, he found that when mecamylamine is given in low doses, it has a restorative effect on memory similar to that of nicotine, but without the harmful side effects. Buccafusco and his colleagues said studying the nature of the relationship of mecamylamine, nicotine and the nicotine receptor may lead to new approaches for treating memory loss and other cognitive problems.
For full article see: Terry, A.V., Jr., Buccafusco, J.J. and Prendergast, M.A.: Dose-specific improvements in memory-related task performance by rats and aged monkeys administered the nicotinic-cholinergic antagonist mecamylamine. Drug Devel. Res. 47: 127-136, 1999.
AndrewB
Posted by SLS on February 24, 2001, at 6:20:12
In reply to Re: Scott, posted by AndrewB on February 23, 2001, at 23:18:14
> For full article see: Terry, A.V., Jr., Buccafusco, J.J. and Prendergast, M.A.: Dose-specific improvements in memory-related task performance by rats and aged monkeys administered the nicotinic-cholinergic antagonist mecamylamine. Drug Devel. Res. 47: 127-136, 1999.
>
> AndrewB
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