B3 Eugene Flashcards
Decreasing dopamine ameliorates psychosis
–Blockade of DA receptors treats psychosis
–Inhibition of DA synthesis ameliorates symptoms of schizophrenia
•There is enhanced amphetamine-induced DA release in schizophrenia
Conventional antipsychotic drugs
are often subclassified according to their oral milligram potency (high potency or low potency).
High-potency neuroleptic drugs
(piperazine phenothiazines, e.g., fluphenazine; and haloperidol) are more likely to produce extrapyramidal reactions
Low-potency drugs
(aliphatic phenothiazines, e.g., triflupromazine; piperidine phenothiazines, e.g., thioridazine) are less likely to produce acute extrapyramidal reactions and more likely to produce sedation and postural hypotension.
Atypical antipsychotic agents
(e.g., risperidone, olanzapine) have generally replaced the conventional drugs for initial treatment of first-episode patients
Clozapine
is reserved for treatment-resistant patients.
Mechanism of therapeutic action for neuroleptics
- The therapeutic action of the conventional antipsychotic drugs is correlated best with antagonist activity at postjunctional dopamine D2-receptors, where dopamine normally inhibits adenylyl cyclase activity.
- The therapeutic action of the atypical antipsychotic drugs is correlated with antagonist activity at both 5-HT2-receptors and dopamine D2- or D4-receptors. Aripiprazole is a partial agonist at dopamine D2-receptors and, like ziprasidone, also stimulates serotonin 5-HT1A-receptors.
- The therapeutic action is best correlated with the actions of these drugs in the mesolimbic and mesocortical areas of the CNS.
Aripiprazole
Partial Agonist
What are the two high-potency Antipsychotic drugs?
Fluphenazine and Haloperidol
Which ADR are the high potency antipsychotics more likely to produce?
ExtraPyramidal Reactions
Which Low-potency drug is more likely to produce sedation and postural hypotension?
Thioridazine
Please name 2 first line Atypical antipsychotic drugs?
Risperidone and Olanzapine
Which antipsychotic is reserved for treatment-resistant patients?
Clozapine
Thiorizadine, ziprasidone and quetiapine
Long QT interval
Increasing dopamine worsens psychosis
–High doses of amphetamine or cocaine can lead to a paranoid psychosis
–Amphetamine will exacerbate an existing schizophrenic state