Prolactin Serum Concentrations During Aripiprazole Treatment in Youth

Safer, Daniel J.; Calarge, Chadi A.; Safer, Alan M.

doi:10.1089/cap.2012.0062

Cited by 26 publications

(17 citation statements)

References 83 publications

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“…All aripiprazole dose groups demonstrated a reduction from baseline in prolactin concentrations in the 6‐week study, and these were maintained over the course of the 52‐week flexible‐dose OLE. This tendency was consistent with that in the previous studies, though the clinical consequences are unknown . This prolactin concentration decrease with aripiprazole may be related to its dopamine D 2 receptor partial agonist property, which is thought to mimic the inhibitory action of dopamine on pituitary prolactin secretion …”

Section: Discussionsupporting

confidence: 91%

Safety and efficacy from a 6‐week double‐blind study and a 52‐week open‐label extension of aripiprazole in adolescents with schizophrenia in Japan

Matsumoto

Ishigooka²,

Ono

et al. 2018

Psychiatry Clin Neurosci

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Section: Discussionsupporting

confidence: 91%

Safety and efficacy from a 6‐week double‐blind study and a 52‐week open‐label extension of aripiprazole in adolescents with schizophrenia in Japan

Matsumoto

Ishigooka²,

Ono

et al. 2018

Psychiatry Clin Neurosci

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“…Accordingly, we may wonder whether ARI is actually able to act as an agonist in vivo , where dopaminergic tone might be fluctuating within a range difficult to define. Indeed, human results suggest that ARI has actions consistent with agonism on D 2 receptors controlling prolactin release, in contrast with most antipsychotics ( Safer et al, 2013 ). Whether ARI acts as a D 2 agonist on nerve terminals involved in psychosis remains speculative, but it is worth considering, as it led to its discovery ( Kikuchi et al, 1995 ).…”

Section: Discussionmentioning

confidence: 99%

Agonist and Antagonist Effects of Aripiprazole on D2-Like Receptors Controlling Rat Brain Dopamine Synthesis Depend on the Dopaminergic Tone

Guo

Raivio

Sabriá

et al. 2014

International Journal of Neuropsychopharmacology

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Background:The atypical antipsychotic drug aripiprazole binds with high affinity to a number of G protein coupled receptors, including dopamine D2 receptors, where its degree of efficacy as a partial agonist remains controversial.Methods:We examined the properties of aripiprazole at D2-like autoreceptors by monitoring the changes of dopamine synthesis in adult rat brain striatal minces incubated ex vivo. The effects of the dopaminergic tone on the properties of aripiprazole were assayed by comparing a basal condition (2mM K+, low dopaminergic tone) and a stimulated condition (15mM K+, where dopamine release mimics a relatively higher dopaminergic tone). We also used 2 reference compounds: quinpirole showed a clear agonistic activity and preclamol (S-(-)-PPP) showed partial agonism under both basal and stimulated conditions.Results:Aripiprazole under the basal condition acted as an agonist at D2-like autoreceptors and fully activated them at about 10nM, inhibiting dopamine synthesis similarly to quinpirole. Higher concentrations of aripiprazole had effects not restricted to D2-like autoreceptor activation. Under the stimulated (15mM K+) condition, nanomolar concentrations of aripiprazole failed to decrease dopamine synthesis but could totally block the effect of quinpirole.Conclusions:Under high dopaminergic tone, aripiprazole acts as a D2-like autoreceptor antagonist rather than as an agonist. These data show that, ex vivo, alteration of dopaminergic tone by depolarization affects the actions of aripiprazole on D2-like autoreceptors. Such unusual effects were not seen with the typical partial agonist preclamol and are consistent with the hypothesis that aripiprazole is a functionally selective D2R ligand.

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“…Moreover, there is also good evidence that PRL levels can decrease even to subnormal PRL serum levels (<3 ng/ml for females and <2 ng/ml for males) [340]. …”

Section: Prl and Antipsychoticsmentioning

confidence: 99%

The Effects of Novel and Newly Approved Antipsychotics on Serum Prolactin Levels: A Comprehensive Review

et al. 2014

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Since the 1970s, clinicians have increasingly become more familiar with hyperprolactinemia (HPRL) as a common adverse effect of antipsychotic medication, which remains the cornerstone of pharmacological treatment for patients with schizophrenia. Although treatment with second-generation antipsychotics (SGAs) as a group is, compared with use of the first-generation antipsychotics, associated with lower prolactin (PRL) plasma levels, the detailed effects on plasma PRL levels for each of these compounds in reports often remain incomplete or inaccurate. Moreover, at this moment, no review has been published about the effect of the newly approved antipsychotics asenapine, iloperidone and lurasidone on PRL levels. The objective of this review is to describe PRL physiology; PRL measurement; diagnosis, causes, consequences and mechanisms of HPRL; incidence figures of (new-onset) HPRL with SGAs and newly approved antipsychotics in adolescent and adult patients; and revisit lingering questions regarding this hormone. A literature search, using the MEDLINE database (1966–December 2013), was conducted to identify relevant publications to report on the state of the art of HPRL and to summarize the available evidence with respect to the propensity of the SGAs and the newly approved antipsychotics to elevate PRL levels. Our review shows that although HPRL usually is defined as a sustained level of PRL above the laboratory upper limit of normal, limit values show some degree of variability in clinical reports, making the interpretation and comparison of data across studies difficult. Moreover, many reports do not provide much or any data detailing the measurement of PRL. Although the highest rates of HPRL are consistently reported in association with amisulpride, risperidone and paliperidone, while aripiprazole and quetiapine have the most favorable profile with respect to this outcome, all SGAs can induce PRL elevations, especially at the beginning of treatment, and have the potential to cause new-onset HPRL. Considering the PRL-elevating propensity of the newly approved antipsychotics, evidence seems to indicate these agents have a PRL profile comparable to that of clozapine (asenapine and iloperidone), ziprasidone and olanzapine (lurasidone). PRL elevations with antipsychotic medication generally are dose dependant. However, antipsychotics having a high potential for PRL elevation (amisulpride, risperidone and paliperidone) can have a profound impact on PRL levels even at relatively low doses, while PRL levels with antipsychotics having a minimal effect on PRL, in most cases, can remain unchanged (quetiapine) or reduce (aripiprazole) over all dosages. Although tolerance and decreases in PRL values after long-term administration of PRL-elevating antipsychotics can occur, the elevations, in most cases, remain above the upper limit of normal. PRL profiles of antipsychotics in children and adolescents seem to be the same as in adults. The hyperprolactinemic effects of antipsychotic medication are mostly correlated with their affi...

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Prolactin Serum Concentrations During Aripiprazole Treatment in Youth

Cited by 26 publications

References 83 publications

Safety and efficacy from a 6‐week double‐blind study and a 52‐week open‐label extension of aripiprazole in adolescents with schizophrenia in Japan

Safety and efficacy from a 6‐week double‐blind study and a 52‐week open‐label extension of aripiprazole in adolescents with schizophrenia in Japan

Agonist and Antagonist Effects of Aripiprazole on D2-Like Receptors Controlling Rat Brain Dopamine Synthesis Depend on the Dopaminergic Tone

The Effects of Novel and Newly Approved Antipsychotics on Serum Prolactin Levels: A Comprehensive Review

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