Cariprazine
Second-generation antipsychotics
Second-generation antipsychotics
A D2 and D3 partial agonist that prefers D3; used in schizophrenia, bipolar disorder and depression. Its active metabolite lingers for weeks.
Quick facts
- Group
- Second-generation antipsychotics
- Target
- Dopamine D3 and D2 receptors (partial agonist); D3 shown
- Used for
- Schizophrenia · Bipolar I disorder
- Key effects
- Akathisia · Extrapyramidal effects · Tiredness
- Monitor
- Akathisia and extrapyramidal signs · Weight
- ATC
- N05AX15
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows cariprazine bound to the human dopamine D3 receptor (with its G protein), the receptor it prefers.
Cariprazine is a partial agonist at dopamine D2 and D3 receptors with higher affinity for D3. Like other partial agonists it lowers dopamine signalling where it is excessive. D3 receptors are concentrated in limbic areas, and its D3 action has been linked to effects on negative symptoms and cognition in some studies. CYP3A4 turns it into two active metabolites; one of them (DDCAR) is eliminated very slowly.
- Cariprazine partly activates D3 (preferred) and D2
- Lowers excessive dopamine signalling: less psychosis and mania
- CYP3A4 makes active metabolites; DDCAR lasts for weeks
- Common side effects: akathisia and restlessness
Indications
- Schizophrenia Schizophrenia →
- Bipolar I disorder: manic or mixed episodes and depressive episodes Bipolar disorder →
- Major depressive disorder Major depressive disorder →
Adverse effects
Common
- Akathisia, restlessness and insomnia
- Extrapyramidal effects: unusual movements, stiffness, poor balance
- Tiredness, dizziness, nausea, constipation
- Increased appetite and weight gain
Contraindications
- Hypersensitivity to cariprazine
Key interactions
- Strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin)
- Several-fold higher cariprazine exposure; the amount is reduced
- CYP3A4 inducers (rifampicin, carbamazepine, St John's wort)
- Not recommended: unpredictable, lower levels
What is monitored
- Akathisia and extrapyramidal signs, which may appear weeks after a change
- Weight, glucose and lipids
- Mood and suicidal thoughts in young people
Administration and safety
- Because of the long-lived metabolite, the effects of a change and side effects appear and fade over weeks
- Every new drug is checked for CYP3A4 inhibition or induction
Pregnancy and breastfeeding
Newborns exposed in the third trimester may have extrapyramidal or withdrawal symptoms; use weighs benefit and risk.
Nursing care
- Asks about restlessness, the urge to move, tremor and stiffness, also several weeks after a change
- Records weight, glucose and lipids
- Teaches the patient to report thirst, frequent urination or blurred vision (high glucose)
- Advises getting up slowly and drinking enough fluids in hot weather
Pharmacokinetics
- Absorption
- Taken by mouth, with or without food
- Metabolism
- Liver, by CYP3A4 (CYP2D6 minor) to the active metabolites DCAR and DDCAR
- Half-life
- Parent drug about 1 to 3 days; DDCAR about 13 to 19 days, so about half is still present a week after stopping
Test yourself
Think of the answer, then tap the question to see it.
Which dopamine receptor does cariprazine prefer?
D3 (it is a partial agonist at D3 and D2, with higher affinity for D3).
Why can side effects of cariprazine appear or persist weeks after a change?
Its active metabolite DDCAR has a half-life of about two weeks.
What is the most typical movement side effect?
Akathisia (inner restlessness).
Connections
← Back to the class: Second-generation antipsychotics
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Cariprazine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.