Prolactinemia is uncoupled from central D2/D3 dopamine receptor occupancy in amisulpride treated patients

Bressan, Rodrigo A.; Erlandsson, Kjell; Spencer, Edgar P.; Ell, Peter J.; Pilowsky, Lyn S.

doi:10.1007/s00213-004-1826-6

Cited by 37 publications

(33 citation statements)

References 39 publications

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“…Their lesser penetration at therapeutic dose levels leads to a greater D2R occupancy in the pituitary area and therefore to a greater increase of the PRL values [316]. Especially for amisulpride, a decreased penetration of the blood–brain barrier would explain the marked tendency of this medicine to cause a rise in PRL values [195, 421]. This hypothesis is supported by the observation that domperidone, a D2 blocker that does not cross the blood–brain barrier, is associated with significant PRL elevation [422].…”

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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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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“…It has few extrapyramidal symptoms (EPS) but significant prolactin elevation, similar to that of conventional antipsychotics and often clinically relevant (Fric and Laux, 2003). It is hypothesized that amisulpride may have a selectively higher occupancy of D 2 /D 3 receptors at the pituitary level than at the central regions, because of its poor brain barrier permeability (Bressan et al, 2004). Amisulpride‐induced hyperprolactinaemia is reported after both acute and chronic treatment and does not seem to be strongly dose‐related.…”

Section: Antipsychoticsmentioning

confidence: 99%

Hyperprolactinemia associated with psychotropics—a review

Madhusoodanan¹,

Parida

Jimenez

2010

Human Psychopharmacology

112

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“…41 Risperidone may also have a higher pituitary D 2 receptor occupancy than haloperidol. 42,43 Second, prolactin levels are significantly correlated with risperidone dose. 44 Besides, analyzing the prolactin level at end point with a 2-way analysis of variance, with baseline prolactin level as the covariate, indicated statistically significant differences between the haloperidol-plus-risperidone group and the risperidone-alone group (P = 0.045) and between female (n = 24) and male subjects (n = 31; P = 0.001).…”

Section: Discussionmentioning

confidence: 98%

A Randomized, Double-Blind Comparison of Risperidone Versus Low-Dose Risperidone Plus Low-Dose Haloperidol in Treating Schizophrenia

Lin¹,

Kuo²,

Chou³

et al. 2010

Journal of Clinical Psychopharmacology

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Monotherapy is recommended for schizophrenia treatment, but the risk-benefit issue of antipsychotic drug combination (except for clozapine) remains unclear. Risperidone, an atypical antipsychotic drug, has a lower incidence of extrapyramidal syndrome but higher risks of prolactinemia and metabolic syndrome than haloperidol, a typical agent. This study compared efficacy and safety of risperidone monotherapy versus low-dose risperidone plus low-dose haloperidol in schizophrenia. In this 6-week, double-blind study, patients were randomized to the combination group (2-mg/d risperidone plus 2-mg/d haloperidol, n = 46) or the monotherapy group (4-mg/d risperidone, n = 42). Efficacy assessments included Clinical Global Impression-Severity, Positive and Negative Syndrome Scale and subscales, Calgary Depression Scale, Global Assessment of Functioning, and Medical Outcomes Study Short-Form 36. Safety was rigorously monitored. Response was defined as 30% reduction in the Positive and Negative Syndrome Scale total score. The 2 treatment groups were similar in (1) demographic and clinical characteristics at baseline, (2) response rate, and (3) improvement in various psychopathological measures and quality of life at end point. The monotherapy group had a higher increase in prolactin levels (P = 0.04) and Simpson-Angus Scale scores (P = 0.04) and a higher percentage of biperiden use (P = 0.045). There were no significant between-group difference in changes in weight, vital signs, corrected QT interval, liver/renal function, fasting glucose level, and lipid profiles. The findings suggest that risperidone monotherapy may yield higher prolactin levels than a combination of low-dose risperidone plus low-dose haloperidol. The 2 treatment groups are similar in efficacy, life quality, and other safety profiles. Future long-term studies are warranted.

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Prolactinemia is uncoupled from central D2/D3 dopamine receptor occupancy in amisulpride treated patients

Cited by 37 publications

References 39 publications

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

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

Hyperprolactinemia associated with psychotropics—a review

A Randomized, Double-Blind Comparison of Risperidone Versus Low-Dose Risperidone Plus Low-Dose Haloperidol in Treating Schizophrenia

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