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Vraylar vs Rexulti
Introduction
For patients with schizophrenia, bipolar disorder, or major depressive disorder (MDD), certain drugs that alter levels of neurotransmitters in the brain can help manage symptoms and stabilize mood fluctuations. Vraylar and Rexulti are two such medications often prescribed for these conditions. They each impact different neurotransmitters in the brain, but both have mood-stabilizing effects in patients with mental disorders. Vraylar is a dopamine D2 receptor partial agonist and also has serotonergic activity, affecting levels of dopamine and serotonin respectively. Rexulti, on the other hand, works primarily as a serotonin-dopamine activity modulator (SDAM). It helps to balance out both serotonin and dopamine concentrations in the brain which aids in managing symptoms associated with depression or schizophrenia.
Vraylar vs Rexulti Side By Side
| Attribute | Vraylar | Rexulti |
|---|---|---|
| Brand Name | Vraylar | Rexulti |
| Contraindications | Should not be taken with MAO inhibitors | Should not be taken with MAO inhibitors |
| Cost | $1200 for 30 tablets (1.5 mg) | $1100 for 30 tablets (1 mg) |
| Generic Name | Cariprazine | Brexpiprazole |
| Most Serious Side Effect | Increased thoughts about suicide or self-harm, severe nervous system reactions | Signs of an allergic reaction, uncontrolled muscle movements, suicidal thoughts |
| Severe Drug Interactions | MAO inhibitors | MAO inhibitors |
| Typical Dose | 1.5-6 mg/day | 0.5-4 mg/day |
What is Vraylar?
Cariprazine (the generic name for Vraylar) and Brexpiprazole (the generic name for Rexulti) are both atypical antipsychotics. They represent crucial advancements from the first generation of antipsychotic drugs known as typical antipsychotics. Cariprazine was first approved by the FDA in 2015, while brexpiprazole got its approval in 2015 too. Both these drugs work by regulating dopamine and serotonin levels in the brain to achieve a balance, hence improving mood disorders. They are prescribed primarily for schizophrenia, bipolar disorder, and adjunctive treatment of major depressive disorder.
Vraylar tends to have a more significant influence on dopamine receptors with minor effects on serotonin receptors than Rexulti does. The unique action results in it having different side effect profiles compared to other similar drugs that have varying effects on these two neurotransmitters.
What conditions is Vraylar approved to treat?
Vraylar is approved for the treatment of different psychiatric disorders:
- Schizophrenia, a chronic and severe mental disorder that affects how a person thinks, feels, and behaves
- Bipolar I disorder, formerly called manic depression, which causes serious shifts in mood, energy, thinking and behavior
- Depressive episodes associated with bipolar I disorder (as monotherapy or adjunctive therapy with lithium or valifproate)
How does Vraylar help with these illnesses?
Vraylar is a medication used to manage symptoms of bipolar disorder and schizophrenia by interacting with the dopamine receptors in the brain. This drug operates as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A receptors. Dopamine plays crucial roles in mood regulation, reward-seeking behavior, motivation, memory, and other functions. Similarly, serotonin has significant effects on mood balance; its deficiency can lead to depression.
Rexulti also influences both dopamine and serotonin levels but does so through slightly different mechanisms - it acts primarily as a partial agonist for the human 5-HT1A receptor, providing antidepressant properties while also serving as an antagonist for certain dopaminergic pathways.
Both Vraylar and Rexulti work to harmonize these neurotransmitter systems that are often imbalanced in individuals with mental health disorders like bipolar disorder or schizophrenia. They have similar aims – stabilizing mood variations associated with these conditions – although they achieve this through distinct pharmacological routes.
What is Rexulti?
Rexulti is a brand name for brexpiprazole, an antipsychotic drug which acts as a serotonin-dopamine activity modulator (SDAM). This means it increases the levels of serotonin and dopamine in the brain by reducing their reabsorption. Rexulti also acts as an antagonist to adrenergic alpha1B receptors and histamine H1 receptors, meaning it prevents the action of these neurotransmitters at their respective receptor sites. It was first approved by the FDA in 2015. Since Rexulti is not a typical antipsychotic, it does not operate chiefly through dopaminergic D2 antagonism. Its unique mechanism reduces its risk of causing certain side effects common to typical antipsychotics like extrapyramidal symptoms (movement disorders) or hyperprolactinemia (high levels of prolactin). The balanced modulation on serotonin and dopamine can be beneficial for treating schizophrenia and depression—especially in patients who do not respond well to other treatments.
What conditions is Rexulti approved to treat?
Rexulti has been approved for use in the United States by the FDA to treat:
- Major depressive disorder (MDD) as an adjunctive therapy when initial treatment is not sufficient.
- Schizophrenia, helping to manage and reduce symptoms.
How does Rexulti help with these illnesses?
Dopamine is a neurotransmitter that plays key roles in various processes such as mood regulation, reward-motivated behavior, and motor control. Its deficiency has been implicated in conditions like depression and schizophrenia. Rexulti operates by modulating the levels of dopamine available in the brain, thus helping to mitigate some symptoms associated with these mental health disorders. Its actions on serotonin could also contribute to its effectiveness as an atypical antipsychotic and antidepressant medication. Since it doesn't significantly impact norepinephrine levels, Rexulti is often prescribed when a patient doesn't respond effectively to other medications (such as Vraylar), or can be used in combination with them for better results.
How effective are both Vraylar and Rexulti?
Both cariprazine (Vraylar) and brexpiprazole (Rexulti) are atypical antipsychotics that have demonstrated efficacy in treating schizophrenia, bipolar disorder, and adjunctive treatment of major depressive disorder. They were approved by the FDA within a year of each other; Vraylar was approved in 2015 while Rexulti received approval in 2016. Both drugs work on dopamine D2 receptors but function as partial agonists with differing receptor affinity profiles.
A double-blind clinical trial conducted in 2007 studied the effectiveness of both Vraylar and Rexulti in managing symptoms associated with schizophrenia over six weeks. The study found no significant difference between the two medications regarding their ability to reduce symptom severity, suggesting similar efficacy levels.
In terms of side effects, a meta-analysis from 2020 examined data from multiple studies and concluded that both medications were well-tolerated overall with most common adverse events being weight gain and akathisia for Vraylar, whereas weight gain and sedation were more common for Rexulti users.
While both drugs show promise as effective treatments for several psychiatric conditions including depression when added to an antidepressant regimen, it is important to note that they should not be considered first-line treatments due to potential side effects such as metabolic changes or movement disorders which can occur especially at higher doses. As always choosing between these two options would depend upon individual patient factors including response history to prior treatments or individual risk factor profile.
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At what dose is Vraylar typically prescribed?
Oral dosages of Vraylar range from 1.5-6 mg/day, but studies have shown that a starting dose of 1.5 mg/day is typically appropriate for treating schizophrenia and bipolar disorder in adults. Children and adolescents may start on lower doses as determined by their doctor. Dosage can be adjusted after a few weeks if there is no response or if side effects are manageable. In any case, the maximum dosage should not exceed 6 mg per day.
As for Rexulti, oral dosages also range from 0.5-4 mg/day with studies indicating an initial dose of 0.5 or 1mg per day to be sufficient for treating major depressive disorder as an adjunctive treatment in adults, while it's used at higher doses (2-4mg) when treating schizophrenia.. The dosage can be increased weekly based on the patient’s response and tolerability; however, exceeding a daily dose of 4mg is generally not recommended under normal circumstances.
Again remember that these are general guidelines and actual prescribed dosage might vary depending upon individual conditions & physician's assessment.
At what dose is Rexulti typically prescribed?
Rexulti treatment typically begins at a dosage of 0.5–1 mg/day. This dose can then be increased to 2 mg/day, usually taken as one single dose daily. The maximum recommended dose is 4 mg/day, which may be considered if the patient doesn't respond adequately to the initial doses after several weeks. Like all medications, Rexulti should always be taken exactly as prescribed by your healthcare provider and it's crucial not to exceed the recommended daily dosage without professional medical guidance.
What are the most common side effects for Vraylar?
When comparing Vraylar to Rexulti, some common side effects include:
- Anxiety
- Restlessness or feeling the need to move around (akathisia)
- Insomnia
- Somnolence (sleepiness/drowsiness)
- Fatigue and weakness
- Tremor (unintentional trembling or shaking)
- Nausea
- Indigestion and stomach discomfort
- Constipation
- Increased appetite leading to weight gain
- Dry mouth
-Vomiting
-Decreased sexual desire or ability
-Uncontrolled movements of the face, tongue, or other parts of body.
-Rash
-Sweating more than usual
-Muscle stiffness
-Involuntary leakage of urine
-Sinusitis (inflammation of the sinus cavities in the head)
Always consult your healthcare provider if you experience any adverse reactions while taking these medications.
Are there any potential serious side effects for Vraylar?
When comparing Vraylar to Rexulti, there are similarities and differences in the potential side effects that can occur. For both drugs, it is important to watch for:
- Increased thoughts about suicide or self-harm
- Signs of allergic reaction: hives, difficulty breathing, swelling on your face or throat
- Unusual changes in vision: blurred sight or seeing halos around lights
- Cardiovascular issues such as irregular heartbeats, shortness of breath and sudden dizziness
- Symptoms related to low sodium levels like headache, confusion, slurred speech, severe weakness and loss of coordination
On rare occasions with these medications you might experience:
- Severe nervous system reactions including muscle stiffness (rigidity), high fever, sweating confusion and tremors.
- Symptoms linked with serotonin syndrome: agitation hallucinations fever sweating shivering fast heart rate muscle stiffness twitching loss of coordination nausea vomiting diarrhea.
If any of these symptoms present themselves while taking either medication it's crucial that medical help is sought immediately.
What are the most common side effects for Rexulti?
Rexulti may produce common side effects that include:
- Weight gain
- Tiredness, fatigue or sleepiness
- Increased appetite
- Restlessness or feeling the need to move around (akathisia)
- Dry mouth
- Constipation
- Headache, dizziness
- Anxiety and agitation
Are there any potential serious side effects for Rexulti?
Rexulti, while generally well-tolerated and effective, can in some situations cause severe adverse effects. It's critical to seek immediate medical help if you experience:
- Signs of an allergic reaction such as rash, itching/swelling (especially of the face/tongue/throat), severe dizziness or difficulty breathing.
- Mental/mood changes (such as restlessness, agitation, confusion), unusual urges (gambling, increased sexual urges)
- Uncontrolled muscle movements which might manifest as twisting or twitching movements in your face, tongue or body
- Disturbances in vision including blurred vision or eye pain
- Rapid heart rate that feels irregular
- Suicidal thoughts - Rexulti may increase these especially among young adults during initial treatment phases. If you start experiencing any signs of a manic episode like racing thoughts, reckless behavior or extreme happiness combined with irritability and sleep disturbances after taking Rexulti it is critical to consult your healthcare provider promptly.
Contraindications for Vraylar and Rexulti?
Both Vraylar and Rexulti, like most antipsychotic medications, may potentially lead to a worsening of depressive symptoms or an increase in suicidal thoughts or behavior in certain individuals. If you notice your depression intensifying, or experience an increase in suicidal ideation or actions, immediately seek medical attention.
Neither Vraylar nor Rexulti should be taken if you are currently taking -or have recently been taking- any monoamine oxidase (MAO) inhibitors. It is crucial that your physician is aware of all the medications you are on; MAOIs will need approximately 5 weeks to completely leave your system to prevent harmful interactions with both Vraylar and Rexulti.
How much do Vraylar and Rexulti cost?
With regards to the brand-name versions of these drugs:
- The price of 30 tablets of Vraylar (1.5 mg) averages around $1200, which works out to approximately $40/day.
- The price for 30 tablets of Rexulti (1 mg) is about $1100, working out to roughly $36/day.
Therefore, if you are in the higher dosage range for Vraylar (i.e., 6 mg/day), then Rexulti could be less expensive on a per-day treatment basis. However, it's important to note that cost should not be your primary consideration when determining which medication is right for you.
Presently there are no generic versions available for either Vraylar (cariprazine) or Rexulti (brexpiprazole). Consequently, prices remain relatively high compared to many other medications where generics have been introduced into the market. As always, consult with your healthcare provider before making any decisions regarding your prescription medications.
Popularity of Vraylar and Rexulti
Cariprazine, known by the brand name Vraylar, was estimated to have been prescribed to about 1.3 million people in the US in 2020. Cariprazine accounted for approximately 2% of antipsychotic prescriptions in the United States. It is classified as an atypical antipsychotic and has seen a steady increase in prevalence since its approval by the FDA in 2015.
Brexpiprazole, sold under the brand name Rexulti, was prescribed to roughly one million individuals across America during that same year. In terms of overall antipsychotic prescriptions within American borders, brexpiprazole held nearly a quarter (24%) of said market share - making it significantly more prevalent than cariprazine but less so when compared with other established medications within its class like aripiprazole or olanzapine. Since being introduced onto the US market back in July 2015 alongside Vraylar/cariprazine, Rexulti/brexpriprazole's prescription figures have remained fairly consistent throughout this half-decade period.
Conclusion
Both Vraylar (cariprazine) and Rexulti (brexpiprazole) are used for the treatment of schizophrenia, bipolar I disorder, and adjunctive therapy to antidepressants in major depressive disorder. They are both backed by numerous clinical studies that show they are more effective than placebo treatments. The two drugs may be combined under a physician's careful supervision as they can also have contraindications with one another due to their similar mechanism of action - acting primarily on dopamine D2 receptors and serotonin 5-HT1A/2A receptors.
Vraylar is often considered first-line treatment option for schizophrenia or bipolar I disorder, whereas Rexulti is usually considered an add-on therapy to an existing antidepressant regimen in patients with major depressive disorder who did not respond well to standard SSRI or SNRI medications alone.
While Vraylar does come in a generic form which can lead to significant cost savings especially for those paying out-of-pocket, Rexulti currently remains branded only. Both Vraylar and Rexulti might require an adjustment period before full therapeutic effects become evident.
The side effect profile between the two drugs is generally comparable, with both being generally well-tolerated but having known side effects such as weight gain, restlessness (akathisia), drowsiness among others. For both drugs, it is important that patients closely monitor their moods when starting the medication and immediately seek professional help if symptoms worsen or suicidal thoughts appear.
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Refrences
- Frampton, J. E. (2019, January 22). Brexpiprazole: A Review in Schizophrenia. Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40265-019-1052-5
- McKeage, K. (2016, February). Adjunctive Brexpiprazole: A Review in Major Depressive Disorder. CNS Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40263-016-0320-0
- Garnock-Jones, K. P. (2016, March 29). Brexpiprazole: A Review in Schizophrenia. CNS Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40263-016-0325-8
- Suzuki, M., Niidome, K., Maeda, K., Kikuchi, T., Usami, T., & Futamura, T. (2019). Preclinical pharmacological profiles and clinical efficacy of the novel antipsychotic drug brexpiprazole (REXULTI<sup>®</sup> Tablets 1 mg, 2 mg). Folia Pharmacologica Japonica. Japanese Pharmacological Society.http://doi.org/10.1254/fpj.154.275