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Re: Which CYP Enzymes Metabolize Amisulpride? blueberry

Posted by yxibow on December 4, 2006, at 19:49:07

In reply to Which CYP Enzymes Metabolize Amisulpride?, posted by blueberry on December 3, 2006, at 17:27:16

> I can't seem to find how amisulpride is metabolized, other than the general CYP system. Which CYP enzymes break it down? CYP3A4? CYP1A2? CYP2D6? Or what?
> Does amisulpride induce or inhibit any enzymes? The only literature I have been able to find says it has few drug interactions, but nothing specific.

For US medications, which wouldn't answer your question, CYP interactions can be found at this useful site:

The "clinically relevant" ones are red flags, the others are possibilities.


As I think others might not have access I have quoted below (slightly unreadable in the tables)

European Neuropsychopharmacology
Volume 10, Supplement 3 , September 2000, Pages 331-332

"Amisulpride does not inhibit cytochrome
P450 isozymes
G. Gillet, L. Dormerque, M. Canal, J.P. Thenot. Sanofi-Synthdlabo,
Chilly Mazarin, France
Introduction: The atypical antipsychotic agent amisulpride
(Solian@, Sanofi-Synthelabo) is predominantly excreted unchanged.
However, amisulpride may have high affinity on human
cytochrome P450 (CYP450) and may therefore have inhibitory
effect on CYP450 isoenzymes. The details of its interactions
with cytochrome P450 (CYP450) isozymes have not been fully
Methods: Microsomes were prepared from six pooled human
liver biopsies. The microsomes were incubated with ethoxyresorufine
(for CYP450 lA2 activity), coumarine (for CYP450
2A6 activity), tolbutamide (for CYP450 2C9 activity), S(+)-
mephenytoin (for CYP450 2C19 activity), bufiualol (for CYP450
2D6) activity) or nifedipine (CYP450 3A4 activity). Amisulpride
was tested at concentrations between 100 nM-1 n&i. Control
incubations were made with standard inhibitors of CYP450
isozymes (30 uM furafyline for CYP450 lA2 activity, 30 UM
pilocarpine for CYP450 2A6 activity, 2 uM sulphaphenazole for
CYP450 2C9 activity, 3 uM quinidine for CYP450 2D6 and
0.33 uM ketoconazole for CYP450 3A4. No specific inhibitor of
CYP450 2C19 is currently available. All incubations were made
in triplicate.
Results: No concentration of amisulpride inhibited any
CYP450 isozyme activity to any appreciable extent. Inhibition
of CYP450 isozyme activity was below 10% for all doses and
isozymes with the exception of CYP450 2D6, which was inhibited
by 26% with the highest dose of amisulpride. Respective isozymes
were inhibited by their standard inhibitors as follows: furafyline
(37%), pilocarpine (71%), sulphaphenazole (57%), quinidine
(78%) and ketoconazole (84%).
Table 1 - Percentage activity of CYP450 isozymes in the presence of
[amisulpride] uh4
0.1 1 10 100 1000
CYP450 lA2 95.9 95.2 93.9 98.6 97.3
CYP450 2A6 100 95.9 92.5 100 98.9
cYP450 2c9 95.7 100 99.5 100 92.8
cYP450 2c19 100 100 94.9 100 100
CYP450 2D6 100 100 96.3 96.3 74.1
CYP450 3A4 100 100 100 100 95.4
Conclusions: Amisulpride has a low potential for drug interactions.
This study has shown that it does not inhibit isozymes of
CYP450; amisulpride has also been known to have low plasma
protein binding. The efficacy of amisulpride has been demonstrated
in acute exacerbations of schizophrenia, mixed symptoms,
predominantly negative symptoms and chronic schizophrenia.

The finding that it also has little propensity to cause drug interactions
enhances its flexibility in clinical use. Lack of drug interactions is a particularly important consideration when a switch from
classical neuroleptics to a novel neuroleptic is being considered
because such patients are often receiving concomitant medication."




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