Antipsychotics Flashcards
What are examples of first-generation antipsychotics?
Haloperidol, chlorpromazine, pericyazine
Typical antipsychotics MOA?
Post-synaptic blockade of the D2 receptor
Pharmacology of typical antipsychotics?
Extensively metabolised by CYP450 system thus susceptible to hepatic impairment and drug-drug interactions.
Highly lipophilic, protein and tissue bound, with a large volume of distribution thus effect is variable and unpredictable in different patients.
Side effects of typical antipsychotics?
My Cute Cat Makes The Purring Sounds:
Metabolic syndrome Cardiovascular (QT prolongation, hypotension) Motor symptoms (rigidity, bradykinesia) Tardive dyskinesia Prolactin elevation Sexual dysfunction
What are examples of second-generation antipsychotics?
Risperidone, olanzapine, quetiapine, aripiprazole, clozapine (CROAQ)
Atypical antipsychotic MOA?
Post-synaptic blockade of the D2 receptor. Has some affinity for the 5HT2A receptor; inhibition of serotonin increases dopamine release (which may account for the decrease EPSE)
Pharmacology of atypical antipsychotics?
Variable activation by CYP450 system therefore some drugs are susceptible to hepatic impairment and drug-drug impairment.
Side effects of atypical antipsychotics?
Metabolic syndrome QT prolongation Cardiovascular effects Motor symptoms Tardive dyskinesia (to a lesser extent than FGA) Prolactin elevation Sexual dysfunction.
What are the differences between atypical and typical antipsychotics, and why?
Atypical antipsychotics are associated with lower rates of motor symptoms and tardive dyskinesia. This is likely to due to the fact that atypical antipsychotics have some affinity for the 5HT2A receptor, which causes an increase in dopamine release.
What are the indications for clozapine?
Schizophrenia or schizoaffective disorder not responsive to other antipsychotics
What is included in the pretreatment assessment of clozapine?
Complete blood count
Weight, BSLs, lipids
What monitoring is required for clozapine?
Neutrophil counts due to risk of neutropenia within 10 days of first administration, every week for the first 18 weeks, and every four weeks thereafter. This is a legal requirement.
What are the side effects of clozapine?
Myocarditis Cardiomyopathy Gastrointestinal hypomotility Metabolic side effects Neutropenia
When would clozapine levels be taken?
To assess adherence or in the case of poor clinical response. This is because therapeutic levels are highly individual.
What are the problems that can occur due to switching antipsychotics?
Rebound psychosis Cholinergic rebound Dystonia Akathisia Histamine rebound