Pharmacodynamics
Ziprasidone displayed high in vitro the affinity making friends for the dopamine D2 and D3, the serotonin 5HT2A, 5HT2C, 5HT1A, 5HT1D and receivers 1-adrenergic (Ki s of 4.8, 7.2, 0.4, 1.3, 3.4, 2 and 10 nM, respectively) and the affinity softened for the histamine H1's receiver (Ki=47 nM). Ziprasidone worked as an antagonistic in the D2, 5HT2A and 5HT1D receivers and as an agonist in the 5HT1A the receiver. Ziprasidone inhibited the reconsommation synaptic of serotonin and of norepinephrine. No significant affinity was displayed for other sites of récepteur/attacher assessed, by including the cholinergic muscarinic the receiver (IC50> 1 M).
The mechanism of action of ziprasidone, as with other medicaments having effectiveness in schizophrenia, is unknown. However, they offered that the effectiveness of this medicament in schizophrenia is negotiated by a combination of type of dopamine 2 (D2) and serotonin type 2 (5HT2) antagonism. As with other medicaments having effectiveness in riot bipolar, the mechanism of action of ziprasidone in riot bipolar am unknown.
The antagonism in receivers other than dopamine and 5HT2 with the similar affinity of receiver can explain a little other therapeutics and side effects of ziprasidone. The antagonism of Ziprasidone of histamine H1's receivers can explain the drowsiness noticed with this medicament. The antagonism of adrénergiques Ziprasidone of α1-receivers can explain the orthostatic low blood pressure noticed with this medicament.
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