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

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

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
M_2–4 (peripheral)	Blurred vision, constipation, urinary retention, tachycardia, hypertension	Diarrhoea, sweating, nausea, vomiting, bradycardia, hypotension, syncope
5-HT_1A (partial agonism)	Anxiolytic, antidepressant, anti-EPS/akathisia	Anxiety, EPS/akathisia
5-HT_2A	Anti-EPS/akathisia, antipsychotic	EPS/akathisia, psychosis
5-HT_2C	Increased appetite/weight	Decreased appetite

D₂, dopamine type 2 receptor; EPS, extrapyramidal symptoms; α, alpha-adrenergic receptor; H, histaminergic receptor; M, muscarinic receptor; 5-HT_1A, serotonin type 1A receptor; 5-HT_2A, serotonin type 2A receptor; 5-HT_2C, serotonin type 2C receptor. Adapted from [40].

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