IUBio

Bromocriptine and Blood Brain Barrier

The Leukotomist np07la at mail.telepac.pt
Tue May 7 10:54:34 EST 1996


walls1door at aol.com (Walls1Door) wrote:

>actually, many of the agents used in treating alzheimer's and parkinson's
>disease are unable to cross the blood-brain barrier and must be
>administered i.n. instead of i.v. in order for them to cross. any other
>way besides intranasal adminstration <via the olfactory route> would
>require invasive surgical techniques.

Actually, as far as I know, the only drugs that are currently
administered by the intranasal route with the intent of producing
systemic effects are lysine vasopressin and desmopressin acetate (a
vasopressin analog), both used in the treatment of chronic diabetes
insipidus.

The only drug currently used specifically for the treatment of
Alzheimer's disease is tacrine, which is a long acting cholinesterase
inhibitor and muscarinic modulator. Tacrine is an orally active amine
that enters the central nervous system readily. It blocks both
acetilcholinesterase and butyrylcholinesterase and has complex
inhibitory effects on M1 and M2 cholinoceptors. Tacrine is NOT
administered by the intranasal route. It must be said that MAO type B
inhibition with selegiline (an orally acting drug) has been suggested
to have some beneficial effects, but I think that it is not approved
by the FDA for this purpose, yet.

Concerning Parkinson's disease, its treatment involves essentially the
following drugs or groups of drugs:

	* Levodopa / Carbidopa
	* Bromocriptine
	* Pergolide
	* MAO inhibitors (mostly selegiline)
	* Amantadine
	* ACh-blocking drugs

All these drugs are administered orally, except benztropine, biperiden
and orphenadrine, which are ACh-blocking drugs that, in addition to
the oral route, can be administered by i.v. route. None of them is
administered by the intranasal route.

Currently under investigation for the treatment of Parkinson's disease
are:

	* D,L-threo-3,4-dihydroxyphenylserine (DOPS)
	* Other dopamine agonists
	* Catechol-O-metiltransferase inhibitors
	* Vitamin E
	* GM1 Ganglioside
	* Transplantation of dopaminergic tissues.

That's all, folks!

Goodbye!


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             8888888888888888888888888888	Sergio Miguel Cardoso
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