Mechanism of Action: cariprazine (RGH-188) is a D₃-preferring dopamine D₃/D₂ receptor partial agonist antipsychotic candidate for the treatment of schizophrenia and bipolar mania. Substance abuse is a frequent comorbidity of both disorders and is associated with serious health issues. Based on preclinical efficacy, dopamine D₂, and D₃ receptor partial agonists and antagonists are assumed to have relapse-preventing potential in human cocaine addiction. –Pub Med
Indications:
Interactions: use caution when taking Vraylar with the following medications: blood pressure medications, certain HIV medications, clarithromycin, ketoconazole, nefazodone, noxafil (posaconazole), rifampin, sporanox (itraconazole), tegretol (carbamazepine), vfend (voriconazole) –Very Well Mind
Food Interactions
- Avoid excessive or chronic alcohol consumption. Given the primary central nervous system effects of cariprazine, cariprazine should be used with caution in combination with alcohol.
- Avoid grapefruit products. Grapefruit is a known CYP3A4 inhibitor. It may increase drug levels and elevate the risk of drug adverse effects.
- Avoid St. John’s Wort. St John’s Wort is a known CYP3A4 inducer. It may significantly decrease drug exposure and alter drug efficacy.
- Take with or without food. A high-fat, high-calorie meal may delay Tmax (Time to peak drug concentration), but food generally has no significant effect on drug exposure.
Dosing Forms:
Usual Adult Dose for Schizophrenia:
- Initial dose: 1.5 mg orally once a day
- Titration regimen: The dose may be increased to 3 mg once a day on Day 2; further dose adjustments should be made in 1.5 to 3 mg increments based on efficacy and tolerability.
- Maintenance dose: 1.5 to 6 mg orally once a day
- Maximum dose: 6 mg/day
Comments:
-Due to the long half-life, changes in dose will not be fully reflected in plasma for several weeks; monitor for adverse reactions and treatment response several weeks after beginning therapy and after each dose adjustment.
-Doses above 6 mg once a day have not shown increased effectiveness sufficient to outweigh dose-related adverse reactions.
Usual Adult Dose for Bipolar Disorder (acute treatment of manic or mixed episodes associated with bipolar I disorder):
- Initial dose: 1.5 mg orally once a day
- Titration regimen: The dose should be increased to 3 mg once a day on Day 2; further dose adjustments should be made in 1.5 to 3 mg increments based on efficacy and tolerability.
- Maintenance dose: 3 to 6 mg orally once a day
- Maximum dose: 6 mg/day
Comments:
-Due to the long half-life, changes in dose will not be fully reflected in plasma for several weeks; monitor for adverse reactions and treatment response several weeks after beginning therapy and after each dose adjustment.
-Doses above 6 mg once a day have not shown increased effectiveness sufficient to outweigh dose-related adverse reactions.
Pros
- Only needs to be taken once a day
- Works well for acute manic or depressive bipolar disorder
- Can be taken with or without food
- Works in your body for a longer period of time than other similar medications
Cons
- Can be expensive because it’s only available as a brand name
- You might have to see your healthcare provider several times until you find a dose that works best for you.
- Higher risk for uncontrolled muscle movements compared with some similar medications
- Might take several weeks before you experience the full effects of this medication
Extra Notes
- This is a good option for depression and males concerned about sexual side effects.
- Because of cariprazine’s half-life (1 week), there are reports of some people taking it once a week (but it’s to mainly help save money)…
- Cariprazine can be activating, take QAM or start low and go slow to watch for movement, sleep, anxiety issues, and increased difficult thoughts. It could be self-limiting but akathisia and movement disorders are ongoing risks.
- With GI side effects, some prescribe Zofran with it or try to handle it as tolerated. It should also be self-limiting but with minimal withdrawal symptoms if abruptly d/c’d (r/t the half-life).
- Another major benefit of Cariprazine is how it’s the only med that mainly works on the D3 receptors, which is the main receptor for drug addictions. I’ve never used this to treat cocaine or substance disorders, I tend to avoid things that can be activating (cause anxiety/restlessness) in this population but hopefully, there’ll be more studies about it.
- It is costly but there are saving coupons and a possible option to trial taking it once/week.
Additional Informaiton
Offical Medication Website: Vraylar (Cariprazine)
- Cariprazine for schizophrenia and bipolar I disorder- MD Edge (graphic above)
