Jump to content

Cariprazine: Difference between revisions

From Pharmacopedia
(View all pending changes)
[checked revision][pending revision]
← Older editNewer edit →

MDElliottMD (talk | contribs)

3 user groups
5,188 edits
VisualWikitext
Pharmacopedia: add <pharmaInteractions/>
Em-dash sweep: replace em-dash with comma per project rule; PendellsCorner verbatim quotes preserved.
(3 intermediate revisions by 3 users not shown)
Line 1: Line 1:
{{MedTemplate
{{MedTemplate
| generic            = Cariprazine
| brand           = Vraylar
| brand             = Vraylar
| classes         = Atypical antipsychotic, D2/D3/5HT1A partial agonist
| structure          =
| mechanism       = Partial agonist at D2 and D3 dopamine receptors with HIGHER affinity for D3 than D2 (uncommon among antipsychotics). Partial agonist at 5HT1A. Antagonist at 5HT2B. Weaker 5HT2A antagonism than other atypicals. The D3 partial agonism is proposed to drive efficacy for negative and cognitive symptoms of schizophrenia, and mood-related effects (depression in bipolar/MDD).
| classes           = Antipsychotic, Neuroleptic
| uses           = Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022).
| mechanism         = D3/D2 partial agonist; 5-HT2A antagonist
| starting_dose   = Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg.
| uses               =  
| preparations   = 1.5 mg, 3 mg, 4.5 mg, 6 mg capsules
| starting_dose     =  
| fda_max         = 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct)
| preparations       =  
| routes         = Oral
| fda_max           =  
| onset           = Weeks for psychosis/mood efficacy
| routes             =  
| duration       = Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks)
| onset             =  
| halflife       = Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses
| duration           =  
| bioavailability = Adequate oral bioavailability
| halflife           =  
| pregnancy       = Limited data
| bioavailability   =  
| legal           = Rx
| pregnancy         =  
| 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.
| legal             =  
 
| intro             =  
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.
| pharmacokinetics  =
| pharmacodynamics= D3 partial agonist (highest affinity); D2 partial agonist; 5HT1A partial agonist; 5HT2B antagonist; modest 5HT2A and H1 antagonism.
| pharmacodynamics   =  
| 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.
| indications        =  
| interactions     = <pharmaInteractions/>
| dosing            =
| effects           =
| interactions       = <pharmaInteractions/>
| pregnancy_details  =
| monitoring        =
| counseling        =
| anecdotes          =
| seealso            =
| references        =
}}
}}


[[Category:Antipsychotics / Neuroleptics]]
[[Category:Second-Generation Antipsychotics (SGAs / Atypicals)]]
[[Category:Neuroleptics]]
[[Category:Neuroleptics]]
[[Category:Third-Generation Antipsychotics]]
[[Category:Atypical Antipsychotics]]
[[Category:Antipsychotics]]
[[Category:Dopamine Partial Agonists]]
[[Category:Psychotic Disorders]]
[[Category:Mood Stabilizers]]

Revision as of 03:16, 19 May 2026

Atypical antipsychotic, D2/D3/5HT1A partial agonist
Cariprazine
Vraylar
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, missed doses cause less rapid decline in plasma levels than with shorter-acting agents.

Experience

👥 No personal reports yet
⚕ No clinical reports yet

Log in to add your own experience.

Problems

No problems yet. Be the first to suggest one.

+ Add a problem

Titration strategies

No titration strategies yet. Be the first to suggest one.

+ Add a titration strategy

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.

+ Add an effect

Pharmacodynamics

D3 partial agonist (highest affinity); D2 partial agonist; 5HT1A partial agonist; 5HT2B antagonist; modest 5HT2A and H1 antagonism.

Interactions

No interactions reported yet.

Relevant anecdote

No anecdotes yet. Share a relevant one.

+ Add an anecdote

Relevant Literature

No literature entries yet.

Log in to submit relevant literature.

Summary
Classes
Atypical antipsychotic, D2/D3/5HT1A partial agonist
Common uses
Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022).
Pharmacy
Starting dose
Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg.
Preparations
1.5 mg, 3 mg, 4.5 mg, 6 mg capsules
US FDA Max
6 mg/d (psychosis/mania); 3 mg/d (depression adjunct)
Pharmacology
Routes
Oral
Onset
Weeks for psychosis/mood efficacy
Duration
Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks)
Half-life
Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses
Bioavailability
Adequate oral bioavailability
Pregnancy
Limited data
Legal status
Rx
Purported mechanism
Partial agonist at D2 and D3 dopamine receptors with HIGHER affinity for D3 than D2 (uncommon among antipsychotics). Partial agonist at 5HT1A. Antagonist at 5HT2B. Weaker 5HT2A antagonism than other atypicals. The D3 partial agonism is proposed to drive efficacy for negative and cognitive symptoms of schizophrenia, and mood-related effects (depression in bipolar/MDD).
Retrieved from "https://pharmacopedia.wiki/index.php?title=Cariprazine&oldid=4580"