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Related Concept Videos

Antipsychotic Drugs: Typical and Atypical Agents01:21

Antipsychotic Drugs: Typical and Atypical Agents

Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
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Antipsychotic drugs are a crucial treatment method for acute and chronic psychoses, bipolar illness, and behavioral disorders. The selection of these drugs depends on several factors, including the state of the disease, clinical judgment, possible drug interactions, and the patient's sensitivity to adverse effects. In immediate scenarios, such as delirium and dementia, short-term treatment with low doses of high-potency typical or atypical agents can effectively manage symptom exacerbation. For...
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Psychosis and Antipsychotic Drugs: Overview

The term "psychosis" refers to a spectrum of mental disorders characterized by abnormal thoughts, perceptions, and behaviors. It can manifest as mood disorders, dementia, delirium with psychotic features, substance-induced psychosis with psychotic features, brief psychotic disorder, delusional disorder, schizoaffective disorder, and schizophrenia. Among all these disorders, schizophrenia is the most common psychotic disorder, affecting 1% of the worldwide population. Psychotic symptoms in all...
Pharmacodynamic Responses: Different Types01:03

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Pharmacodynamics is the scientific study of a drug's biochemical or physiological influence on the body. It categorizes responses into continuous, discrete (or categorical), and time-to-event outcomes. Continuous responses yield numerical values within a certain range, such as blood pressure readings and blood glucose levels, gauging the efficacy of antihypertensive and antidiabetic drugs. Discrete responses can be binary, indicating whether a drug has an effect or not, or ordinal, exemplifying...
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Hepatic impairment, characterized by decreased liver function, does not uniformly mandate adjustments in drug dosage. Whether dosage modifications are necessary depends on various factors related to the drug's metabolism and elimination pathways. If a drug is primarily excreted via the kidneys and bypasses significant hepatic processing, if it undergoes minimal metabolic transformation in the liver, or if it is volatile and primarily expelled through the lungs, dose adjustments may not be...
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The advent of drug therapy has profoundly shaped modern mental health care, providing targeted treatments for a range of psychological disorders. Psychotherapeutic drugs, classified into antianxiety, antidepressant, and antipsychotic medications, address symptoms across anxiety disorders, mood disorders, and schizophrenia. While these medications have transformed patient outcomes, they require careful management due to their potential side effects and limitations.
Antianxiety Medications

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Self-Administration of Drugs in Mouse Models of Feeding and Obesity
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Signalling profile differences: paliperidone versus risperidone.

W P Clarke1, T A Chavera, M Silva

  • 1Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX, USA.

British Journal of Pharmacology
|July 6, 2013
PubMed
Summary
This summary is machine-generated.

Paliperidone and risperidone show distinct cellular signaling effects due to a hydroxyl group, potentially impacting their therapeutic efficacy and side effects in treating schizophrenia.

Keywords:
GPCRantipsychoticsbiased agonismdopaminefunctional selectivityhistamineschizophreniaserotonin

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Molecular Biology

Background:

  • Paliperidone, an active metabolite of risperidone, is approved for schizophrenia and schizoaffective disorder.
  • The structural difference (a single hydroxyl group) between paliperidone and risperidone raises questions about their distinct pharmacological profiles.

Purpose of the Study:

  • To compare the relative efficacies of paliperidone and risperidone.
  • To investigate their regulation of cellular signaling pathways linked to key G protein-coupled receptors (GPCRs).

Main Methods:

  • Compared paliperidone and risperidone efficacies on human dopamine D2, serotonin 5-HT2A, serotonin 5-HT2C, and histamine H1 receptors.
  • Assessed regulation of associated cellular signaling pathways.

Main Results:

  • Significant differences in receptor-signaling regulation were observed between paliperidone and risperidone.
  • Both drugs acted as agonists in 5-HT2A-mediated beta-arrestin recruitment, 5-HT2A-mediated ERK sensitization, and dopamine D2-mediated adenylyl cyclase signaling.
  • Relative efficacy varied depending on the specific receptor-response pair.

Conclusions:

  • The hydroxyl group in paliperidone induces distinct receptor conformations compared to risperidone.
  • These conformational differences lead to varied regulation of cellular signal transduction cascades.
  • Cellular signaling disparities may translate to differences in clinical efficacy and adverse effect profiles.