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Table 2 Effects of blockade of receptors and side effects that can result from withdrawal/rebound during switching

From: Dosing and switching of paliperidone ER in patients with schizophrenia: recommendations for clinical practice

Receptor Effects of blockade Potential rebound/withdrawal effect
D2 Antipsychotic, antimanic, antiaggression, EPS/akathisia, tardive dyskinesia, increased prolactin Psychosis, mania, agitation, akathisia, withdrawal dyskinesia
α1 Postural hypotension, dizziness, syncope Tachycardia, hypertension
α2 Antidepressant, increased alertness, increased blood pressure Hypotension
H1 Anxiolytic, sedation, sleep induction, weight gain, anti-EPS/akathisia Anxiety, agitation, insomnia, restlessness, EPS/akathisia
M1 (central) Negative impact on memory and cognition, dry mouth, anti-EPS/akathisia Agitation, confusion, psychosis, anxiety, insomnia, sialorrhoea, EPS/akathisia
M2–4 (peripheral) Blurred vision, constipation, urinary retention, tachycardia, hypertension Diarrhoea, sweating, nausea, vomiting, bradycardia, hypotension, syncope
5-HT1A (partial agonism) Anxiolytic, antidepressant, anti-EPS/akathisia Anxiety, EPS/akathisia
5-HT2A Anti-EPS/akathisia, antipsychotic EPS/akathisia, psychosis
5-HT2C Increased appetite/weight Decreased appetite
  1. D2, dopamine type 2 receptor; EPS, extrapyramidal symptoms; α, alpha-adrenergic receptor; H, histaminergic receptor; M, muscarinic receptor; 5-HT1A, serotonin type 1A receptor; 5-HT2A, serotonin type 2A receptor; 5-HT2C, serotonin type 2C receptor. Adapted from [40].