Receptor mechanisms of antipsychotic drug atypicality

1998 ◽  
Vol 13 (S1) ◽  
pp. 5s-8s
Author(s):  
GP Reynolds

SummaryRecent advances in antipsychotic treatment of schizophrenia have offered several new compounds which avoid many of the limitations of the classical antipsychotics. These so-called ‘atypical’ antipsychotics have fewer extrapyramidal side effects, greater efficacy against negative symptoms and greater efficacy in otherwise treatment-resistant patients. However, the mechanism of action of these atypical antipsychotics is still unclear. The several receptors currently implicated in the pharmacological profile of these atypical antipsychotics include subtypes of those for dopamine, serotonin, noradrenaline, and acetylcholine among others. The current hypotheses for possible mechanisms of action of atypical antipsychotics are discussed along with the experimental correlates of antipsychotic efficacy in animal models.

2007 ◽  
Vol 191 (S51) ◽  
pp. s88-s95 ◽  
Author(s):  
Stephan Ruhrmann ◽  
Andreas Bechdolf ◽  
Kai-Uwe Kühn ◽  
Michael Wagner ◽  
Frauke Schultze-Lutter ◽  
...  

BackgroundPeople in a putatively late prodromal state not only have an enhanced risk for psychosis but already suffer from mental and functional disturbancesAimsTo evaluate the acute effects of a combined supportive and antipsychotic treatment on prodromal symptomsMethodPutatively prodromal individuals were randomly assigned to a needs-focused intervention without (n=59) or with amisulpride (n=65). Outcome measures at 12-weeks effects were prodromal symptoms, global functioning and extrapyramidal side-effectsResultsAmisulpride plus the needs-focused intervention produced superior effects on attenuated and full-blown psychotic symptoms, basic, depressive and negative symptoms, and global functioning. Main side-effects were prolactin associatedConclusionsCoadministration of amisulpride yielded a marked symptomatic benefit. Effects require confirmation by a placebo-controlled study


2006 ◽  
Vol 12 (1) ◽  
pp. 4
Author(s):  
C Seller ◽  
L Koen ◽  
D J H Niehaus

Clozapine is an atypical antipsychotic drug indicated for the management of severely ill patients with schizophrenia who fail to respond adequately to standard antipsychotic treatment. It has demonstrated superior efficacy in treating both the positive and negative symptoms in treatment-refractory cases. It also has the added benefit of causing minimal extrapyramidal side- effects, producing no tardive dyskinesia and having little effect on prolactin levels


1999 ◽  
Vol 11 (3) ◽  
pp. 85-92
Author(s):  
M.J.A.J.M. Hoes

SummaryAntipsychotic drugs are effective in psychoses, whatever the etiology of the disorder. The positive symptoms tend to respond more readily. The need for developing new drugs arises from the refractoriness of the negative symptoms, the 10-25% of the patients that are treatment-resistant and the problems of short-, and long-term extrapyramidal side-effects. Thus far, six drugs, differing from the classical antipsychotics, have been licensedfor use: olanzepine, risperidone and quetiapine; the longest registration exists for sulpiride and clozapine while the most recent one is for amisulpride. This review starts with a brief introduction to symptomatology, and takes differences with the classical drugs in pharmacology, pharmacokinetics, clinical aspects and side-effects into consideration. Clozapine, risperidone and sulpiride may be considered for clinical use in refractory patients; these three, olanzapine and amisulpride when extrapyramidal side-effects cause a clinical problem. Amisulpride and sulpiride have a dual therapeutic acion: On negative symptoms at low dose, on positive symptomen at high doses.


Drug Research ◽  
2017 ◽  
Vol 68 (03) ◽  
pp. 159-167 ◽  
Author(s):  
Benneth Ben-Azu ◽  
Adegbuyi Aderibigbe ◽  
Itivere Omogbiya ◽  
Abayomi Ajayi ◽  
Ezekiel Iwalewa

Abstract Objectives Morin is a naturally occurring flavonoid with strong anti-oxidant and anti-inflammatory properties. Studies have shown that flavones modulate neurotransmission through enhancement of gamma amino butyric acid activity in the central nervous system; which led to the hypothesis that they could exert tranquilizing effects in rodents. Hence, this study was designed to evaluate the antipsychotic effect of morin on experimental animal models. Methods The antipsychotic effect of morin (25, 50 and 100 mg/kg) administered intraperitoneally (i.p.) was assessed on novelty-induced locomotion, apomorphine-induced stereotypy, ketamine-induced stereotypy, ketamine-induced hyperlocomotion and ketamine-enhanced immobility in forced swim test (FST). Catalepsy and rota rod tests were also carried out to evaluate the extrapyramidal side effects of morin. Results Morin (25, 50 and 100 mg/kg, i.p.) pretreatments significantly (p<0.05) demonstrated anti-schizophrenia-like behavior by inhibiting ketamine-induced hyperlocomotion in mice. Moreover, morin (50 and 100 mg/kg, i.p.) significantly (p<0.05) reduced spontaneous locomotor activity. Also, morin suppressed apomorphine-induced stereotypy and ketamine-induced stereotypy. The increase in immobility in FST due to ketamine administration was reduced by morin in a significant dose-dependent manner. Furthermore, the antipsychotic activity of morin was not associated with extrapyramidal side effects, as evidenced by decreased decent latency and increased motoric coordination and performance in mice. Conclusion The results of the study revealed that morin demonstrated antipsychotic-like property devoid of extrapyramidal side effects in experimental animal models and may be beneficial in the treatment of schizophrenia-like behaviors; particularly in patients with behavioral hyperactivity and negative symptoms.


1993 ◽  
Vol 163 (2) ◽  
pp. 150-154 ◽  
Author(s):  
C. E. Adams ◽  
T. R. E. Barnes ◽  
M. A. Essali ◽  
S. R. Hirsch ◽  
A. V. P. MacKay ◽  
...  

In order to assess the safety and some efficacy aspects of clozapine under UK conditions, 54 in-patients with severe treatment-resistant schizophrenic disorders were evaluated using several scales before and during treatment. Of the 54 evaluated, 26 completed the 26-week study. Of these patients, 20 showed improvement in psychopathology, often to a marked degree, involving both positive and negative symptoms. Some oral-facial extrapyramidal side-effects decreased as well. Two patients developed neutropenia, but recovered on discontinuation of clozapine. The most frequent adverse event was hypersalivation, and five patients suffered from seizures. It is concluded that clozapine is worth considering for the treatment of severe treatment-resistant patients in the UK.


2003 ◽  
Vol 15 (3) ◽  
pp. 307-309 ◽  
Author(s):  
Benny Fhager ◽  
Inga-Maj Meiri ◽  
Magnus Sjögren ◽  
Åke Edman

Aggressive behavior in dementia often has a severe impact on the quality of life of the patient and the caregivers, and is therefore important to handle. The strategy of treatment should be broad. Nonpharmacological interventions, including environmental adjustments and supporting and training the caregivers, should always be considered. Pharmacological treatment of aggressive behavior in patients with dementia often includes the use of neuroleptics. The atypical compounds clozapine, risperidone, and olanzapine have been shown to have an effect on aggressive behavior at low dosage with limited extrapyramidal side effects. The anticonvulsants carbamazepine and sodium valproate are further alternatives. In treatment-resistant cases, buspirone or lithium may be tried, although the effect of these substances on aggressive behavior in dementia has not been well established. In the end, however, a considerable degree of aggressive behavior sometimes remains after careful treatment trials, particularly in patients with severe aggressive behavior. In addition, treatment is sometimes limited by side effects.


2021 ◽  
pp. 50-51
Author(s):  
Ankit Halder ◽  
Navna Panchami ◽  
Abhishek Das

Due to less extrapyramidal side-effects ,atypical antipsychotics use in psychiatry has increased a lot. But it is associated with other metabolic and endocrine side effects. Olanzapine is one such antipsychotic that less likely to cause hyperprolactinemia which can present as amenorrhea in patients.Here we present a rare case of olanzapine induced amenorrhoea reversed by switching to Aripiprazole.


1999 ◽  
Vol 174 (S38) ◽  
pp. 52-58 ◽  
Author(s):  
C. M. E. Stephenson ◽  
L. S. Pilowsky

The development of atypical antipsychotics has revolutionised the treatment of schizophrenia, as well as providing new insights into its cause. The archetypal atypical antipsychotic is clozapine, which has therapeutic advantages over traditional antipsychotics, as well as a low potential for producing extrapyramidal side-effects (EPS) (Kane et al, 1988). However, clozapine causes agranulocytosis in 1% of patients, and there has consequently been a search for novel atypical antipsychotics, as efficacious as clozapine, but without the need for intensive blood monitoring. There has been much discussion of the definition and characteristics of an atypical antipsychotic drug, and an operational understanding seems to have been agreed upon, that atypical drugs have therapeutic efficacy in treating schizophrenia, without producing EPS (Deutch et al, 1991; Kerwin, 1994).


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