On Tue, 10 Oct 1995 23:48:14 -0600,
aelita at netins.net <aelita at netins.net> wrote:
>Okay, I have recently been prescribed pemoline for ADD (I was previously
>on dexedrine until I moved, and the physician here seems to be a bit
>difficult). Unfortunately I am currently in a very small town for a short
>time, and I have none of my referrence books, nor do the local educational
>institutions, and I don't have access to my medline account from where I
>am. So any help would be appreciated.
>OK, here are the questions.
>>1. At what receptor sites does pemoline act at. (the package insert just
>states that it probably acts at the dopaminergic sites, if anyone has
>anything a bit more specific it would be greatly appreciated)
>>2. Does pemoline has any appreciable effects on cerebral glucose metabolism?
>>3. and finally, I need to know pemolines relative efficacy compared to
>d-amphetamine and or methylphenidate.
>
I found the following info in my electronic files. It isn't
specifically about pemoline, but I think you will find the material of
some interest.
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* Recent article by Pulvirenti and Koob "Dopamine receptor agonists,
partial agonists and psychostimulant addiction". (Don't have full reference).
* From book "Cocaine: Pharmacology, physiology, and clinical strategies" by
Lakoski, Galloway, and White. 1992.
"Comparison with other psychomotor stimulants:
Psychostimulants can be divided into two separated drug classes on the basis of
their actions at dopaminergic nerve terminals (McMillen 1983; Scheel-Kruger
1971; Shore 1976). Drugs in the amphetamine class of stimulants act via
stimulation of release of newly synthesized dopamine from an
alpha-methyl-para-tyrosine sensitive pool (Church and Moore 1975; Scheel-Kruger
1971). In contrast, drugs in the nonamphetamine class of stimulants (e.g.
cocaine and methylphenidate) release dopamine from reserpine sensitive
vesicular stores (Church and Moore 1975; Scheel-Kruger 1971). Althought there
are differences in the biochemical actions of these drugs, there are strong
similarities in their behavioral effects, ... all of which are thought to be
mediated through their effects on dopaminergic systems (Creese and Iverson
1975; DeWit and Wise 1977; Roberts et al. 1975).
There have been a number of studies examining the effects of psychostimulants
other than cocaine on brain glucose utilization. The dose-dependent nature of
cocaine's effect on local cerebral energy metabolism is clearly analogous to
the effects of other psychostimulants on functional activity. Low doses of
either amphetamine (Porrino et al. 1984) or methylphenidate (Porrino and
Lucignani 1987) for example, result in selective increases in glucose
metabolization in the nucleus accumbens. Again, as with cocaine, there
appears to be a greater sensitivity of anatomical portions of the
mesocorticolimbic dopaminergic system, as compared to components of other
dopaminergic systems, to the actions of psychostimulants.
...
Although this dose-dependent pattern of effects within the mesocorticolimbic
and nigrostriatal dopaminergic systems seems to be typical of
psychostimulants, such a pattern is not typical of other dopaminergic drugs.
Apomorphine, a direct dopamine receptor agonist, does not significantly alter
glucose utilization in the mesocorticolimbic system. ... This pattern is
similar to that obtained following the administration of bromocriptine, another
dopamine receptor agonist (Pizzolato 1985). It appears that psychostimulants
have a unique metabolic action in the mesocorticolimbic dopaminergic system."
from Ch. 3. Linda J. Porrino. Metabolic Mapping of the Effects of Cocaine
in the Brain. pp. 42-43.
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AJR
