Cariprazine 3mg capsules
Requires a prescription from a doctor or prescriber
Drugs used in psychoses and related disorders
Official documents, adverse reaction reporting, and safety monitoring
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Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Cariprazine
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Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Cariprazine
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
MHRA licensed products
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Reagila 3mg capsules
This is the NHS Drug Tariff indicative price used for reimbursement purposes. It may not reflect the price paid by patients or pharmacies.
View full Drug TariffSource: NHS Drug Tariff via NHSBSA. Derived from dm+d VMPP (Virtual Medicinal Product Pack) pricing data. Contains public sector information licensed under the Open Government Licence v3.0.
WHO defined daily dose (DDD)
3 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Clinical guidelines and formulary information
British National Formulary
Cariprazine
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
19 found
Half-life
314 to 446 hours
Mechanism
While recent research points to the involvement of multiple neurotransmitters in…
Food interactions
4 warnings
Human targets
8 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
3.6 hours
Half-life
314 to 446 hours
[A247095]
Terminal half-lives of cariprazine, DCAR, and DDCAR ranged from 31.6…
Protein binding
91 to 97%
[L40198]
Metabolism
Elimination
12.5 mg/d
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
[L43307][L40198]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1238 interactions
The possibility of multiple drug involvement should also be considered.
[L40198]
The exact mechanism of action of cariprazine is not fully elucidated. Cariprazine potently binds to both of these receptors, more preferably to D3 receptors with higher affinity.[A3941] Preclinical studies suggest that D3 receptor blockade is associated with exerting pro-cognitive and antidepressant effects and attenuating negative symptoms in schizophrenia.[A247095] This unique mechanism of action differs from that of other antipsychotic agents that mostly target D2 and 5-HT2A receptors.[A247055] Cariprazine is also a partial agonist at 5-HT1A receptors, an antagonist at 5-HT2B and 5-HT2A receptors, an antagonist at histamine H1 receptors. It also binds to 5-HT2C, alpha (α)-1A adrenergic, and alpha (α)-1B adrenergic receptors with low affinity.[A3941][A247095]
As cariprazine is a partial agonist at dopamine D2 and D3 receptors, it produces an apparent lower blockade level than other antipsychotic agents that block dopamine receptors. This receptor binding profile is advantageous as dopamine receptor blockade is associated with extrapyramidal symptoms as side effects. Partial agonism would allow the dopamine receptor to be stimulated even at maximal receptor occupancy by the drug.[A247100] Antagonism at 5-HT1A [A247100] and 5-HT2A receptors by cariprazine can increase dopaminergic neurotransmission in the nigrostriatal pathway, thereby further reducing the risk of extrapyramidal symptoms.[A247055] However, cariprazine is still associated with a risk of akathisia, extrapyramidal disorder, restlessness, and tremor.[A3941][L40198]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[A3941]
After single dose administration of cariprazine, the peak plasma cariprazine concentration occurred in approximately three to six hours.
[L40198]
In healthy volunteers, the Tmax following oral administration was 3.6 hours for cariprazine, 6.5 hours for DCAR, and 18.1 hours for DDCAR. The steady-state was reached dose-proportionally within three weeks for cariprazine, DCAR, and DDCAR in patients with schizophrenia.
[A3941]
Administration of a single dose of 1.5 mg cariprazine capsule with a high-fat meal did not significantly affect the Cmax and AUC of cariprazine or its metabolite, desmethyl cariprazine (DCAR).
[L40198]
[A247095]
Terminal half-lives of cariprazine, DCAR, and DDCAR ranged from 31.6 to 68.4, 29.7 to 37.5, and 314 to 446 hours, respectively. The effective half-life, calculated from time to steady state, or the functional half-life of total active moieties was approximately one week.
[A247060]
[L40198]
DDCAR can be metabolized by CYP3A4 to form a hydroxylated metabolite.
[A3940][A3941][L40198]
[L40198]
Proteins and enzymes this drug interacts with in the body
PMID:21645528
Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
PMID:22957663 PMID:3138543 PMID:33762731 PMID:37935376 PMID:37935377 PMID:8138923 PMID:8393041
Also functions as a receptor for various drugs and psychoactive substances .
PMID:22957663 PMID:3138543 PMID:33762731 PMID:38552625 PMID:8138923 PMID:8393041
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase .
PMID:22957663 PMID:3138543 PMID:33762731 PMID:8138923 PMID:8393041
HTR1A is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission: signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores .
PMID:33762731 PMID:35610220
Beta-arrestin family members regulate signaling by mediating both receptor desensitization and resensitization processes .
PMID:18476671 PMID:20363322 PMID:20945968
Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism .
PMID:18476671 PMID:20363322 PMID:20945968
Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior .
PMID:18476671 PMID:20363322 PMID:20945968
Plays a role in the response to anxiogenic stimuli PMID:18476671 PMID:20363322 PMID:20945968
PMID:18703043 PMID:23519210 PMID:7926008 PMID:8078486 PMID:8143856 PMID:8882600
Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances .
PMID:12970106 PMID:18703043 PMID:23519210 PMID:23519215 PMID:24357322 PMID:28129538 PMID:30127358 PMID:36087581 PMID:7926008 PMID:8078486 PMID:8143856
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors .
PMID:23519215 PMID:28129538 PMID:8078486 PMID:8143856 PMID:8882600
HTR2B is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively .
PMID:18703043 PMID:23519215 PMID:28129538 PMID:30127358 PMID:36087581 PMID:8078486 PMID:8143856 PMID:8882600
Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways .
PMID:23519215 PMID:28129538 PMID:30127358 PMID:36087581
Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain (By similarity). Plays a role in the regulation of behavior, including impulsive behavior .
PMID:21179162
Required for normal proliferation of embryonic cardiac myocytes and normal heart development (By similarity).
Protects cardiomyocytes against apoptosis (By similarity). Plays a role in the adaptation of pulmonary arteries to chronic hypoxia (By similarity). Plays a role in vasoconstriction (By similarity).
Required for normal osteoblast function and proliferation, and for maintaining normal bone density (By similarity). Required for normal proliferation of the interstitial cells of Cajal in the intestine (By similarity)
PMID:1330647 PMID:18703043 PMID:19057895 PMID:21645528 PMID:22300836 PMID:35084960 PMID:38552625
Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) .
PMID:28129538 PMID:35084960
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors .
PMID:28129538 PMID:35084960
HTR2A is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively .
PMID:18703043 PMID:28129538 PMID:35084960
Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways .
PMID:28129538 PMID:35084960
Affects neural activity, perception, cognition and mood .
PMID:18297054
Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction (By similarity)
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
ATC N05AX15
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Cariprazine
Additional database identifiers
Drugs Product Database (DPD)
23719
ChemSpider
25999972
BindingDB
50382290
PDB
7RU
ZINC
ZINC000100907004
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3024
GenAtlas
DRD3
GeneCards
DRD3
GenBank Gene Database
U32499
GenBank Protein Database
927342
Guide to Pharmacology
216
UniProt Accession
DRD3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3023
GenAtlas
DRD2
GeneCards
DRD2
GenBank Gene Database
M30625
GenBank Protein Database
181432
Guide to Pharmacology
215
UniProt Accession
DRD2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:5286
GenAtlas
HTR1A
GeneCards
HTR1A
GenBank Gene Database
M28269
GenBank Protein Database
189928
Guide to Pharmacology
1
UniProt Accession
5HT1A_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:5294
GenAtlas
HTR2B
GeneCards
HTR2B
GenBank Gene Database
X77307
GenBank Protein Database
475198
Guide to Pharmacology
7
UniProt Accession
5HT2B_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:5293
GenAtlas
HTR2A
GeneCards
HTR2A
GenBank Gene Database
S42168
GenBank Protein Database
36431
Guide to Pharmacology
6
UniProt Accession
5HT2A_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:5182
GenAtlas
HRH1
GeneCards
HRH1
GenBank Gene Database
Z34897
GenBank Protein Database
510296
Guide to Pharmacology
262
UniProt Accession
HRH1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:5295
GenAtlas
HTR2C
GeneCards
HTR2C
GenBank Gene Database
M81778
GenBank Protein Database
338028
Guide to Pharmacology
8
UniProt Accession
5HT2C_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:277
GenAtlas
ADRA1A
GeneCards
ADRA1A
GenBank Gene Database
D25235
GenBank Protein Database
433201
Guide to Pharmacology
22
UniProt Accession
ADA1A_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2625
GenAtlas
CYP2D6
GeneCards
CYP2D6
GenBank Gene Database
M20403
GenBank Protein Database
181350
Guide to Pharmacology
1329
UniProt Accession
CP2D6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2638
GenAtlas
CYP3A5
GeneCards
CYP3A5
GenBank Gene Database
J04813
GenBank Protein Database
181346
Guide to Pharmacology
1338
UniProt Accession
CP3A5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2596
GenAtlas
CYP1A2
GeneCards
CYP1A2
GenBank Gene Database
Z00036
Guide to Pharmacology
1319
UniProt Accession
CP1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2621
GeneCards
CYP2C19
GenBank Gene Database
M61854
GenBank Protein Database
181344
Guide to Pharmacology
1328
UniProt Accession
CP2CJ_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2631
GeneCards
CYP2E1
GenBank Gene Database
J02625
GenBank Protein Database
181360
Guide to Pharmacology
1330
UniProt Accession
CP2E1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
Patent information
5 active patents
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
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