Clinical pharmacokinetics and pharmaceutical forms of long-acting injectable antipsychotics

Psychiatriki. 2021 Aug 10. doi: 10.22365/jpsych.2021.035. Online ahead of print.ABSTRACTLong-acting injectable antipsychotics (LAIs) hold an important place in the therapeutic management of patients with schizophrenia and other psychoses. They offer advantages, such as knowledge of whether patients follow the medical advice that is given, stable pharmacokinetics and better correlation between the administered dose and the plasma levels of the drug, regular follow-up and reduced risk of overdose. Knowledge of the best way to administer LAIs is important in clinical practice because it maximizes the efficacy of the drug and minimizes the side-effects. This knowledge is facilitated through understanding both the pharmacokinetics and the pharmaceutical forms of these drugs because it provides necessary information concerning their mode of action. Currently in Greece, two first-generation (haloperidol and zuclopenthixol) and four newer LAIs (risperidone, olanzapine, paliperidone and aripiprazole) are in circulation. Their pharmaceutical form facilitates the delayed delivery of the drug during a period of weeks, thus increasing the time interval needed for the drug administration in order to maintain plasma therapeutic concentrations under stable state conditions. This is achieved by creating an extravascular drug reservoir (depot) in the skeletal muscles from which the drug is slowly released into the systemic circulation. The rate of removal of LAIs is regulated by the slow rate ...
Source: Psychiatriki - Category: Psychiatry Authors: Source Type: research