Antipsychotic Efficacy of Fluperlapine

1984 ◽  
Vol 11 (2) ◽  
pp. 116-120 ◽  
Author(s):  
B. Woggon ◽  
J. Angst ◽  
M. Bartels ◽  
K. Heinrich ◽  
H. Hippius ◽  
...  
Keyword(s):  
Antipsychotic Efficacy

The effect of Zotepine on productive and negative symptoms in schizophrenic patients

1988 ◽  
Vol 3 (2) ◽  
pp. 125-130
Author(s):  
D.M. Dieterle ◽  
M. Ackenheil ◽  
H.P. Kapfhammer ◽  
F. Müller-Spahn
Keyword(s):  
Adverse Effects ◽  
Negative Symptoms ◽  
Suicide Attempts ◽  
Positive Effects ◽  
Antipsychotic Efficacy ◽  
Schizophrenic Patients ◽  
Dose Dependent ◽  
Low Dosage ◽  
Motor Disturbances

RésuméZotepine was studied in 15 schizophrenic patients over a period of 28 days with regard to its antipsychotic efficacy, effect on negative schizophrenic symptoms, tolerability and adverse effects. Nine patients received Zotepine in a high dosage of 230 mg/die±52 mg, 6 patients in a low dosage of 168 mg/die ± 18 mg. Two patients receiving the high dosage dropped out after 21 days because of worsening of symptomatology and suicide attempts. Zotepine had rapid antipsychotic effects with sedative properties during the initial days of treatment. Minimal adverse effects and extra-pyramidal motor disturbances as well as dose-dependent positive effects on negative schizophrenie symptoms were found.

Receptor Binding Targets for Antipsychotic Efficacy

2012 ◽  
pp. 25-43
Author(s):  
Maureen M. Grainger ◽  
Rebecca Ahlbrand ◽  
Paul S. Horn ◽  
Neil M. Richtand
Keyword(s):  
Receptor Binding ◽  
Antipsychotic Efficacy

A comparison of continuous subcutaneous paliperidone infusion and repeated subcutaneous injection of risperidone free-base in rats

2010 ◽  
Vol 25 (2) ◽  
pp. 92-100 ◽  
Author(s):  
G. Marchese ◽  
B. Pittau ◽  
G. Casu ◽  
G. Peddio ◽  
G.P. Spada ◽  
...  
Keyword(s):  
Motor Impairment ◽  
Receptor Occupancy ◽  
Immediate Release ◽  
Pharmacokinetic Profile ◽  
Continuous Administration ◽  
Release Formulation ◽  
Antipsychotic Efficacy ◽  
Drug Concentrations ◽  
Oral Antipsychotic ◽  
Novel Antipsychotic

AbstractIt is proposed that to achieve a therapeutic effect in schizophrenia patients, dopamine D2-receptor occupancy by antipsychotics within the striatum must exceed 60−65%. However, at high levels of D2-receptor occupancy, the risk of extrapyramidal symptoms (EPS) is increased. Following oral dosing of antipsychotics, peaks and troughs in plasma drug concentrations may be mirrored by fluctuations in D2-receptor occupancy. Paliperidone, a novel antipsychotic available as extended-release tablets (paliperidone ER), is the major active metabolite of risperidone and exhibits a plasma pharmacokinetic profile with reduced peak−trough fluctuations and consistent D2-receptor occupancy compared with conventional oral antipsychotic formulations. Using formulations that resemble those in clinical practice, this study provides a preclinical evaluation of the pharmacological properties of paliperidone ER and risperidone immediate-release formulation in terms of consistent antipsychotic efficacy over time and extrapyramidal symptom liability. Significant fluctuations in inhibition of d-amphetamine-induced hyperlocomotion were observed for repeated subcutaneous (SC) risperidone injections, whereas stable inhibitory efficacy was demonstrated during continuous SC paliperidone infusion. Similarly, significant fluctuations in latency on-bar were observed with repeated SC risperidone injections, whereas significantly lower latency on-bar was demonstrated following continuous SC paliperidone infusion. These results in an animal model suggest that although risperidone and paliperidone demonstrate similar pharmacologic effects, continuous administration of paliperidone achieves more stable antipsychotic efficacy with reduced motor impairment, akin to the effects observed with paliperidone ER in clinical studies.

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