Posted by Sunnely on May 3, 2001, at 23:57:54
In reply to Any info on galantamine?, posted by Chris A. on May 3, 2001, at 21:47:09
Here's the skinny on Galantamine:
Galantamine is one of the drugs that belong in the class called "cognitive enhancers." It is a reversible, competitive cholinesterase inhibitor with greater binding capacity for acetylcholinesterase than for butylcholinesterase. (Cholinesterase, an enzyme, is divided into 2 major subtypes, acetylcholinesterase and butylcholinesterase. It seems that acetylcholinesterase is more common in neural tissue, whereas butylcholinesterase is more prominent in peripheral tissue. The ideal cognitive-enhancing drug provides selective inhibition of brain acetylcholinesterase without causing the cholinergic side effects associated with peripheral blockade of butylcholinesterase such as, nausea, vomiting, diarrhea, facial flushing, sweating, nasal stuffiness, slowed heart beat, and leg cramping.)
Galantamine also modulates brain nicotinic receptors; however, the exact benefit of this activity is far from clear. Two potentially positive effects of nicotinic involvement are the increase in acetylcholinesterase related to presynaptic nicotinic receptors stimulation, and the enhanced effect on nicotinic receptors when galantamine and acetylcholinesterase bind simultaneously. It is thought that nicotinic receptors play an important role in memory and learning.
Galantamine is readily absorbed; it has a bioavailability of about 85% and a half-life of about 6 hours. Twice daily dosing is required. It does not bind to plasma proteins. Galantamine is metabolized by the liver enzyme CYP2D6 and has potential interactions with other drugs metabolized by this system. Liver toxicity has not been associated with galantamine. Relatively common side effects include nausea, diarrhea, and anorexia (loss of appetite) but these can be minimized with careful dose titration.
Galantamine will soon be available in the market under the brand name Reminyl. It will be marketed by Janssen Pharmaceutica.
++++++++++++++++++++++++++++++++> My university consultant recommended galantamine as an alternative to the Aricept I'm now taking for mild cognitive impairment. My treating pDoc hadn't hear of it and pulled a site up on the web which indicated that it is a nutraceutical. My neurologist today told me that it is indeed a prescription anticholinesterase inhibitor that is due to be released in the next month or two. It is supposed to have a somewhat different mechanism of action than Aricept or Excelon. Doe
> se anyone know anything about this med - or whatever it is?
>
> Thanks in Advance.
>
> Chris A.
poster:Sunnely
thread:61571
URL: http://www.dr-bob.org/babble/20010424/msgs/61582.html