Ziprasidone: from pharmacology to the clinical practice. One year of experience.
More than a year after the marketing of the atypical anti-psychotic ziprasidone, data from research studies and clinical practice have provided a fair amount of useful information for its practical use in the treatment of schizophrenia. Its pharmacodynamical characteristics and the results from clinical trials with a flexible dose seem to justify the need to administer doses in a range higher than what was initially foreseen, with an initial minimum of 120 mg per day and a fast titulation up to 160 mg per day. Such doses make it possible to achieve sufficient plasma concentrations to occupy at least 60 % of the D2 receptors from which the anti-psychotic effect derives. Moreover, its anti-depressive activity and its non-sedative profile have been confirmed, with a favorable effect on attention and other cognitive functions of the patient, according to its high affinity for 5HT1A and D1 receptors and the inhibition of serotonin and noradrenaline re-uptake. Finally, the low affinity of this drug for alpha-adrenergic, histaminergic and muscarinic receptors favors a good tolerability profile, with a neutral effect on weight, and a lack of anti-cholinergic effects. Results from different clinical trials show that the use of doses in the higher range is associated to a faster and more pronounced clinical improvement without adding a higher risk of adverse events.
Baca
E
E
Servicio de Psiquiatría, Clínica Puerta de Hierro, Madrid, Spain.
Azanza
J R
JR
Giner
J
J
Saiz-Ruiz
J
J
Vallejo
J
J
Diez
T
T
Madrigal
M
M
D014150:Antipsychotic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D004361:Drug Tolerance; D006801:Humans; D010879:Piperazines / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D011976:Receptors, Muscarinic / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects; D012559:Schizophrenia / Q000188:drug therapy*; D013844:Thiazoles / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*
D014150:Antipsychotic Agents; D010879:Piperazines; D011942:Receptors, Adrenergic, alpha; D011976:Receptors, Muscarinic; D011985:Receptors, Serotonin; D013844:Thiazoles; C092292:ziprasidone