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Treatment of Antipsychotic-Induced Hyperprolactinemia: An Update on the Role of the Dopaminergic Receptors D2 Partial Agonist Aripiprazole
Abstract
Hyperprolactinemia is an unwanted adverse effect present in several typical and atypical antipsychotics. Aripiprazole is a drug with partial agonist activity at the level of dopamine receptors D2, which may be effective for antipsychotic- induced hyperprolactinemia. Therefore, we analyzed the literature concerning the treatment of antipsychoticinduced hyperprolactinemia with aripiprazole by updating a previous paper written on the same topic. More recent studies were reviewed. They showed that there are two options for the treatment of antipsychotic-induced hyperprolactinemia with aripiprazole. The safest strategy may require the addition of aripiprazole to ongoing treatments, in the case patients had previously responded to antipsychotic drugs and then developed hyperprolactinemia. However, it is advisable to monitor the patients in case relapses and/or side effect, although rare, might occur. Switching drugs should be considered when a patient does not appear to be responding to the previous antipsychotic, thus developing hyperprolactinemia. A cross-taper switch should always be considered, but the risk of a relapse in the disorder may occur more frequently and the patients should be closely monitored. However, limitations must be considered and further studies are needed to definitely elucidate this important issue. Some relevant patents are also described in this review.
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Individual antipsychotic compounds may affect prolactin levels and bone status differentially.
“To this end, individual antipsychotic compounds may affect prolactin levels (22, 31, 32), and bone status differentially, but the current data did not allow for separating effects of specific antipsychotics.”
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de Bartolomeis, A., Tomasetti, C., & Iasevoli, F. (2015) · CNS Drugs · doi:10.1007/s40263-015-0278-3 · Cited by 211
Self-citationAn update of safety of clinically used atypical antipsychotics
Orsolini, L., Tomasetti, C., Valchera, A., Vecchiotti, R., Matarazzo, I., Vellante, F., Iasevoli, F., Buonaguro, E. F., Fornaro, M., Fiengo, A. L. C., et al. (2016) · Expert Opinion on Drug Safety · doi:10.1080/14740338.2016.1201475 · Cited by 135
“sexual dysfunctions or to treat AP-induced HP [46].”
BackgroundSelf-citationMontejo, Á. L., Arango, C., Bernardo, M., Carrasco, J. L., Crespo-Facorro, B., Cruz, J. J., Del Pino-Montes, J., García-Escudero, M. A., García-Rizo, C., González-Pinto, A., et al. (2017) · Frontiers in Neuroendocrinology · doi:10.1016/j.yfrne.2017.02.003 · Cited by 75
Immunoendocrine Peripheral Effects Induced by Atypical Antipsychotics
Álvarez-Herrera, S., Escamilla-Orozco, R. I., Contreras, O. M., Saracco, R., Flores-Medina, Y., Hurtado‐Alvarado, G., Maldonado-García, J. L., Becerril‐Villanueva, E., Pérez‐Sánchez, G., & Pavón, L. (2020) · Frontiers in Endocrinology · doi:10.3389/fendo.2020.00195 · Cited by 48
“The reports on PRL levels in children and adolescent patients have shown that these populations present elevated HPRL, which has been reported in 44.9% of autism spectrum disorder (ASD) patients as unrelated to the duration of risperidone treatment (0.25–5mg/kg, 1.03–158.03months) (127).”
BackgroundInfluentialAripiprazole for treating irritability associated with autism spectrum disorders
Bartram, L. R., Lozano, J., & Coury, D. L. (2019) · Expert Opinion on Pharmacotherapy · doi:10.1080/14656566.2019.1626825 · Cited by 40
“Risperidone), aripiprazole can be used as an add-on to ongoing therapy or a change from another antipsychotic [27].”
BackgroundManagement of antipsychotic-induced hyperprolactinaemia
Gupta, S., Lakshmanan, D. A. M., Khastgir, U., & Nair, R. (2017) · BJPsych Advances · doi:10.1192/apt.bp.115.014928 · Cited by 33
“Over the past few years, many case reports, case series, randomised controlled trials and meta analyses have shown the effectiveness of this drug (Li 2013; De Berardis 2014; Ranjbar 2015).”
BackgroundZhang, Y., Tang, Z., Ruan, Y., Huang, C., Wu, J., Lu, Z., Li, W., Tang, Y., Liu, J., She, J., et al. (2018) · Medical Science Monitor · doi:10.12659/msm.913759 · Cited by 28
“The close association between the occurrence of sexual dysfunction and antipsychotic medications is due to hyperprolactinemia resulting from the pharmacological effects of blocking dopaminergic D2 receptors in the pituitary tuberoinfundibular pathway [18,19].”
BackgroundEriksson, R., Broberg, B. V., Ishøy, P. L., Bak, N., Andersen, U. B., Jørgensen, N. R., Knop, F. K., & Ebdrup, B. H. (2019) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2018.00781 · Cited by 26
“To this end, individual antipsychotic compounds may affect prolactin levels (22, 31, 32), and bone status differentially, but the current data did not allow for separating effects of specific antipsychotics.”
BackgroundDopamine Receptor Partial Agonists for the Treatment of Bipolar Disorder
Azorin, J., & Simon, N. (2019) · Drugs · doi:10.1007/s40265-019-01189-8 · Cited by 19
Besag, F., Vasey, M. J., & Salim, I. (2021) · CNS Drugs · doi:10.1007/s40263-021-00812-1 · Cited by 19
Maldonado, G. M. M., & Schwartz, T. L. (2023) · International Clinical Psychopharmacology · doi:10.1097/yic.0000000000000510 · Cited by 17
Lippi, M., Fanelli, G., Fabbri, C., Ronchi, D. D., & Serretti, A. (2022) · International Clinical Psychopharmacology · doi:10.1097/yic.0000000000000417 · Cited by 20
“3– 6 mg/day) appears to be a well-tolerated and acceptable option (Domenico et al., 2014; Taylor et al., 2021).”
BackgroundAdd-on Aripiprazole for Atypical Antipsychotic-induced, Clinically Significant Hyperprolactinemia
Raveendranthan, D., Rao, N. P., Rao, M. G., Mangot, A. G., Varambally, S., Kesavan, M., Venkatasubramanian, G., & Gangadhar, B. N. (2018) · Indian Journal of Psychological Medicine · doi:10.4103/ijpsym.ijpsym_147_17 · Cited by 15
“As it is not associated with risk of weight gain, dyslipidemia, or QTc prolongation,([15]) it may be safely used in combination with other antipsychotic drugs.”
BackgroundZheng, W., Cai, D.-B., Yang, X.-H., et al. (2019) · General Psychiatry · doi:10.1136/gpsych-2019-100091 · Cited by 13
Immunotoxicological Effects of Aripiprazole:In vivoandIn vitroStudies
Baek, K., Ahn, S., Lee, J., et al. (2015) · Korean Journal of Physiology and Pharmacology · doi:10.4196/kjpp.2015.19.4.365 · Cited by 10
“With respect to its mechanism of action, several recent pharmacological studies have revealed that aripiprazole directly modulates monoaminergic systems by acting as both a dopamine agonist and antagonist while stabilizing the dopamine D2 and 5-hydroxytryptamine (5-HT)1A receptor Gαi protein-complex [3,4].”
BackgroundAripiprazole for the Treatment of Antipsychotic-Induced Hyperprolactinemia in an Adolescent Boy
Curran, R. L., Badran, I., Peppers, V., et al. (2016) · Journal of Child and Adolescent Psychopharmacology · doi:10.1089/cap.2016.0023 · Cited by 8
Veznedaroğlu, B., Dılbaz, N., Uzun, Ö., & Işık, E. (2018) · Therapeutic Advances in Psychopharmacology · doi:10.1177/2045125318772712 · Cited by 8
When Clozapine Fails: Augmentation Strategies in the Management of Clozapine-Resistant Schizophrenia
Berardis, D. D., Fornaro, M., Anastasia, A., Vellante, F., Valchera, A., Cavuto, M., Perna, G., Nicola, M. D., Serafini, G., Carano, A., et al. (2018) · Springer eBooks · doi:10.1007/978-981-10-4358-1_23 · Cited by 6
Self-citationKrzystanek, M., Warchała, A., Trędzbor, B., Martyniak, E., Skałacka, K., & Pałasz, A. (2021) · Pharmaceuticals · doi:10.3390/ph14100947 · Cited by 4
Aripiprazole combination for reversal of paliperidone-induced increase in prolactin level
Zhi, P., Wang, Y., Quan, W., et al. (2018) · Neuropsychiatric Disease and Treatment · doi:10.2147/ndt.s167129 · Cited by 3
“However, all these strategies may cause a risk of instability in patients.(10) It has previously been reported that aripiprazole, a dopamine receptor partial agonist, can effectively improve the hyperprolactinemia caused by risperidone and its active metabolite 9-hydroxyrisperidone (paliperidone).”
BackgroundMadera‐McDonough, J., Such, P., Zhao, C. Y., & Baker, R. A. (2019) · Neuropsychiatric Disease and Treatment · doi:10.2147/ndt.s198786 · Cited by 3
Hyperprolactinemia as a side effect of using antipsychotics In Schizophrenic Patients
Anwar, S., & Khairina (2023) · Jurnal Psikiatri Surabaya · doi:10.20473/jps.v12i2.23359 · Cited by 3
Recurrent multiple endometrial polyposis in patient treated by antipsychotic drugs
Zamurović, M., Prorocić, M., & Perisić, Z. (2015) · Clinical and Experimental Obstetrics & Gynecology · doi:10.12891/ceog1923.2015
Metadata
- Authors
- Berardis, D., Fornaro, M., Serroni, N., Marini, S., Piersanti, M., Cavuto, M., Valchera, A., Mazza, M., Girinelli, G., Iasevoli, F., Perna, G., Martinotti, G., & Giannantonio, M.
- ORCID
- Venue
- Recent Patents on Endocrine, Metabolic & Immune Drug Discovery
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2014-02
- Volume
- 8
- Issue
- 1
- Pages
- 30-37
- ISSN
- 1872-2148 (ISSN-L)
- OpenAlex
- W2127750886
- Cited by
- 24
- References
- 0
- Citations by year
- 2024: 1 · 2023: 2 · 2022: 1 · 2021: 2 · 2020: 1 · 2019: 5 · 2018: 5 · 2017: 2 · 2016: 2 · 2015: 3
- FWCI
- 1.78
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Recent Patents on Endocrine Metabolic & Immune Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Archivio Istituzionale della Ricerca - Università degli Studi dell Aquila (submittedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Pituitary Gland Disorders and Treatments
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Keywords
- antipsychotic-induced hyperprolactinemia, aripiprazole, antipsychotic adverse effects, antipsychotic switching, relapse risk, patents
- MeSH terms
- Aripiprazole, Drug Therapy, Combination, Humans, Hyperprolactinemia, Patents as Topic, Piperazines, Antipsychotic Agents, Quinolones, Receptors, Dopamine D2, Drug Partial Agonism
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