Cariprazine: Difference between revisions
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Expand Cariprazine with Stahl-sourced detail (with skepticism) |
MDElliottMD (talk | contribs) Em-dash sweep: replace em-dash with comma per project rule; PendellsCorner verbatim quotes preserved. |
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| pregnancy = Limited data | | pregnancy = Limited data | ||
| legal = Rx | | legal = Rx | ||
| intro = '''Cariprazine''' (brand name Vraylar) is an atypical antipsychotic with a distinctive '''D3-preferring''' receptor profile | | intro = '''Cariprazine''' (brand name Vraylar) is an atypical antipsychotic with a distinctive '''D3-preferring''' receptor profile, it has higher affinity for D3 than for D2, uncommon among antipsychotics. FDA-approved for schizophrenia (2015), bipolar mania (2015), bipolar depression (2019), and adjunctive treatment of major depressive disorder (2022). Stahl emphasizes the D3 partial agonism story for negative symptoms of schizophrenia and the mood-spectrum efficacy: postsynaptic D3 blockade in limbic regions reduces emotional dysregulation, while somatodendritic D3 effects in VTA disinhibit DA release in prefrontal cortex, addressing negative/cognitive/affective symptoms. | ||
Notable feature: very long-acting active metabolites (DCAR and DDCAR with half-lives up to 1-3 weeks), producing an 'oral depot' effect | Notable feature: very long-acting active metabolites (DCAR and DDCAR with half-lives up to 1-3 weeks), producing an 'oral depot' effect, missed doses cause less rapid decline in plasma levels than with shorter-acting agents. | ||
| pharmacodynamics= D3 partial agonist (highest affinity); D2 partial agonist; 5HT1A partial agonist; 5HT2B antagonist; modest 5HT2A and H1 antagonism. | | pharmacodynamics= D3 partial agonist (highest affinity); D2 partial agonist; 5HT1A partial agonist; 5HT2B antagonist; modest 5HT2A and H1 antagonism. | ||
| effects = Akathisia (notable; reduced by slow titration), EPS, insomnia, sedation, nausea. Lower weight gain and metabolic effects than many atypicals. Long half-life of metabolites can delay both onset and offset of side effects. | | effects = Akathisia (notable; reduced by slow titration), EPS, insomnia, sedation, nausea. Lower weight gain and metabolic effects than many atypicals. Long half-life of metabolites can delay both onset and offset of side effects. | ||