Comparative Tolerability of Dopamine D2/3 Receptor Partial Agonists for Schizophrenia

AbstractAripiprazole, brexpiprazole and cariprazine differ from all other second-generation antipsychotics due to partial agonism at the dopamine D2 and D3 receptors. In contrast to aripiprazole, brexpiprazole has lower intrinsic dopamine D2 activity and higher affinity for the serotonin 5-HT1A and 5-HT2A receptors, while cariprazine has the highest affinity for the dopamine D3 receptor, and the longest half-life. The main adverse effect of dopamine receptor partial agonists (DRPAs) is akathisia of low-to-moderate severity, which occurs in a small proportion of patients, usually in the first few weeks of treatment. While definitive conclusions concerning differences between the DRPAs require head-to-head comparison studies, on the available evidence, akathisia is probably least likely to occur with brexpiprazole and most likely with cariprazine; the risk of akathisia with aripiprazole lies in between. Weight-gain risk is low with aripiprazole and cariprazine, but moderate with brexpiprazole. Risk of sedation is low with DRPAs, as is risk of insomnia and nausea. Partial dopamine agonism leads to a low risk for hyperprolactinaemia (and probably a low risk of sexual dysfunction). Prolactin concentrations fall in some patients (particularly those with elevated levels prior to initiating the drugs). Rates of discontinuation due to adverse effects in pivotal studies were low, and on the whole, DRPAs are well tolerated. Aripiprazole has been implicated in pathological gambling and o...
Source: CNS Drugs - Category: Neurology Source Type: research

Related Links:

CONCLUSION: The proposed PHARMAC criteria will give access to these important drugs to those people with T2DM who will likely benefit the most. PMID: 33032305 [PubMed - in process]
Source: New Zealand Medical Journal - Category: General Medicine Tags: N Z Med J Source Type: research
Authors: Siamashvili M, Davis S Abstract INTRODUCTION: Bromocriptine mesylate quick release (QR) is a dopamine D2 receptor agonist and is the only oral, primarily centrally acting drug that can be used for the treatment of adults with type 2 diabetes. AREAS COVERED: The authors describe current recommendations on the use of bromocriptine mesylate QR. Major efficacy and safety parameters of the late phase trials, including The Cycloset Safety Trial, have been identified and presented. EXPERT OPINION: Efficacy of bromocriptine mesylate QR monotherapy appears to be low but is compensated by favorable safety pr...
Source: Expert Opinion on Pharmacotherapy - Category: Drugs & Pharmacology Tags: Expert Opin Pharmacother Source Type: research
Publication date: December 2020Source: Journal of Functional Foods, Volume 75Author(s): Tingting Wang, Lin Zheng, Tiantian Zhao, Qi Zhang, Zhitong Liu, Xiaoling Liu, Mouming Zhao
Source: Journal of Functional Foods - Category: Nutrition Source Type: research
TYPE 2 diabetes may feel like a minefield - can you eat this or that without spiking blood sugar levels? If you're feeling peckish, what's a good, healthy option for lunch?
Source: Daily Express - Health - Category: Consumer Health News Source Type: news
CONCLUSIONS: Young adult IS patients in Korea exhibit low awareness and poor management of their risk factors. Although the short-term outcome was relatively favorable in those patients, having SLE was associated with unfavorable outcomes. More attention needs to be paid for improving awareness and controlling risk factors in this population. PMID: 33029967 [PubMed]
Source: Journal of Clinical Neurology - Category: Neurology Tags: J Clin Neurol Source Type: research
Authors: Chung W, Promrat K, Wands J Abstract Diabetes mellitus (DM) negatively affects the development and progression of chronic liver diseases (CLD) of various etiologies. Concurrent DM and CLD are also associated with worse clinical outcomes with respect to mortality, the occurrence of hepatic decompensation, and the development of hepatocellular carcinoma (HCC). Unfortunately, early diagnosis and optimal treatment of DM can be challenging, due to the lack of established clinical guidelines as well as the medical complexity of this patient population. We conducted an exploratory review of relevant literature to...
Source: World Journal of Hepatology - Category: Gastroenterology Tags: World J Hepatol Source Type: research
Authors: Arab JP, Dirchwolf M, Álvares-da-Silva MR, Barrera F, Benítez C, Castellanos-Fernandez M, Castro-Narro G, Chavez-Tapia N, Chiodi D, Cotrim H, Cusi K, de Oliveira CPMS, Díaz J, Fassio E, Gerona S, Girala M, Hernandez N, Marciano S, Masson W, Mendez-Sanchez N, Leite N, Lozano A, Padilla M, Panduro A, Paraná R, Parise E, Perez M, Poniachik J, Restrepo JC, Ruf A, Silva M, Tagle M, Tapias M, Torres K, Vilar-Gomez E, Costa Gil JE, Gadano A, Arrese M Abstract Non-alcoholic fatty liver disease (NAFLD) currently represents an epidemic worldwide. NAFLD is the most frequently diagnosed chr...
Source: Annals of Hepatology - Category: Gastroenterology Tags: Ann Hepatol Source Type: research
Authors: Frías JP Abstract INTRODUCTION: The glucagon-like peptide-1 (GLP-1) receptor agonists (RA) have increasingly gained prominence in the treatment of type 2 diabetes (T2D) based on their glycemic benefits and favorable body weight and cardiorenal effects. Despite this, continued development of therapeutics with superior efficacy is important to help address persistent challenges in the attainment of metabolic goals in many patients with T2D. AREAS COVERED: Tirzepatide is an unimolecular dual glucose-dependent insulinotropic polypeptide (GIP)/GLP-1 RA in development for the treatment of T2D. This re...
Source: Expert Review of Endocrinology and Metabolism - Category: Endocrinology Tags: Expert Rev Endocrinol Metab Source Type: research
We report the rare case of a patient co-existing NS and DLBCL. DLBCL might be pathogenesis of NS; the findings are supported by the presence of MN, an underlying malignancy (DLBCL), and the lack of anti-PLA2R antibodies. Although further investigation is warranted, our case suggests that DLBCL is a possible cause of secondary MN. PMID: 33028760 [PubMed - in process]
Source: The Tohoku Journal of Experimental Medicine - Category: Research Authors: Tags: Tohoku J Exp Med Source Type: research
Abstract Background: The clock drawing test (CDT) is frequently used to detect changes in cognition. Multiple scales of varying length have been published to assess performance. The aim of this study is to compare the CDT performance measured by three scales among a sample of nondemented patients on renal dialysis and identify the variables that affect performance. Methodology. This is a cross-sectional study performed at the dialysis unit at King Saud University Medical City. Eighty-nine dialysis patients performed the CDT. The CDT was scored by the methods of Rouleau et al. (RCS 10-point), Babins et al. (BCS 18-...
Source: Behavioural Neurology - Category: Neurology Authors: Tags: Behav Neurol Source Type: research
More News: Abilify | Diabetes | Dyskinesia | Endocrinology | Insomnia | Neurology | Schizophrenia | Sexual Dysfunction | Study