How Buspar (Buspirone) Works for Anxiety Disorders
Buspirone was first approved in 1986, and what it's primarily used for is generalized anxiety disorder. In 2019, it was the 76 most prescribed medication in the United States with more than 9 million prescriptions. It's used a lot. What Buspirone does to create this effect that helps with anxiety is it actually activates serotonin receptors. It binds to the presynaptic serotonin receptor. So you have your two neurons, you have your presynaptic, and you have your postsynaptic.
Buspirone binds to the presynaptic serotonin receptor, and it also binds to a separate postsynaptic receptor. What happens is this allows there to be more free-floating serotonin. So basically, it activates the serotonin receptors for the serotonin. In a sense, it acts as serotonin, and this is what helps create this feeling of relief, of higher mood, and especially helps with anxiety. Now, I don't know the research behind whether this works or not for depression.
I know it's not used for depression, so there must be evidence out there that it doesn't particularly work for that. But it does help increase serotonin levels by taking its place, so to speak. In a sense, you would think that it would help with depression. What's special about buspirone, or Buspar, is that it's unique. The way that it acts on these serotonin receptors is different from antidepressants, and it's different from other anxiolytic medications like benzodiazepines, gabapentin and beta blockers.
Buspirone may really work great for some people. I took Buspar for a short amount of time. My doctor and I were trying to find a medication that would help me with some anxiety, but what ended up happening is nothing. Nothing happened to me with buspirone. I took it for a while, and I never felt any side effects. I never felt any benefits. Buspirone does have a very narrow dosage range, so there's not a lot of playroom with it.
Buspar is a very unique and interesting medication. They've tried to develop ones like it before in the past but haven't been able to find something that is efficacious. If you think this is right for you, if you're somebody who has generalized anxiety disorder or other anxiety disorders, this might be a great medication for you. If you're already on a medication like an SSRI and you're not quite getting enough relief from your anxiety, then buspirone is a great way to go. You can add that on to medications like SSRIs and your SNRIs and other antidepressants.
Other Articles
Unveiling Caplyta: A Groundbreaking Solution for Schizophrenia
Caplyta (lumateperone) is a prescription medication that belongs to a class of drugs called atypical antipsychotics. It is approved by the FDA for the treatment of schizophrenia and bipolar depression in adults. In this article, we will review what Caplyta is, how it works, what evidence supports its use, what side effects it may cause, and what are its pros and cons.
What it is
Caplyta is a once-daily capsule that contains two active ingredients: lumateperone and samidorphan. Lumateperone is the main ingredient that acts on various brain receptors to reduce the symptoms of schizophrenia and bipolar depression. Samidorphan is an opioid blocker that helps prevent weight gain, a common side effect of other antipsychotics.
History
Caplyta was developed by Intra-Cellular Therapies, a biopharmaceutical company that licensed lumateperone from Bristol-Myers Squibb. The company conducted several clinical trials to test the safety and efficacy of Caplyta for schizophrenia and bipolar depression. The FDA approved Caplyta for schizophrenia in December 2019 and for bipolar depression in December 2021.
Mechanism of Action
Caplyta works by modulating the activity of certain brain chemicals, such as dopamine, serotonin, and glutamate. These chemicals are involved in regulating mood, cognition, and behavior. Caplyta acts as an antagonist (blocker) of some dopamine and serotonin receptors, such as D2, D4, 5-HT2A, and 5-HT7. It also acts as a partial agonist (activator) of some serotonin receptors, such as 5-HT1A. Additionally, Caplyta inhibits the reuptake (recycling) of serotonin by blocking the serotonin transporter (SERT). By doing so, Caplyta reduces the excess dopamine activity that may cause psychosis and increases the serotonin activity that may improve mood and cognition.
Evidence for use
The FDA approval of Caplyta for schizophrenia was based on three randomized, double-blind, placebo-controlled trials that involved a total of 1,268 adults with schizophrenia. The trials lasted for four to six weeks and compared Caplyta 42 mg once daily with placebo or risperidone 4 mg once daily. The primary outcome measure was the change in the Positive and Negative Syndrome Scale (PANSS), which assesses the severity of psychotic symptoms. The results showed that Caplyta significantly reduced the PANSS score compared with placebo in all three trials. Caplyta was also comparable to risperidone in reducing psychotic symptoms.
The FDA approval of Caplyta for bipolar depression was based on two randomized, double-blind, placebo-controlled trials that involved a total of 1,050 adults with bipolar I or II disorder and a current major depressive episode. The trials lasted for six weeks and compared Caplyta 42 mg once daily with placebo as monotherapy or as adjunctive therapy with lithium or valproate. The primary outcome measure was the change in the Montgomery-Åsberg Depression Rating Scale (MADRS), which assesses the severity of depressive symptoms. The results showed that Caplyta significantly reduced the MADRS score compared with placebo in both trials as monotherapy and as adjunctive therapy.
Side Effects/ Adverse reactions / Contradictions
Caplyta may cause some side effects that are common to other antipsychotics, such as sleepiness, dry mouth, constipation, indigestion, increased appetite, weight gain, headache, dizziness, fatigue, shakiness, back pain, speech problems, memory problems, and pins and needles feeling in the hands and feet. However, these side effects are generally mild to moderate and may improve over time.
Caplyta may also cause some serious side effects that require immediate medical attention, such as stroke, opioid withdrawal or overdose (if taken with opioids), neuroleptic malignant syndrome (a life-threatening reaction characterized by fever, muscle stiffness, confusion, sweating), serious skin reaction (rash, fever,
swollen lymph nodes), severe allergic reactions (swelling of the face,
tongue or throat; difficulty breathing; hives), extremely high blood sugar levels (more hunger or thirst; more frequent urination), seizures.
Caplyta is not approved for the treatment of people with dementia-related psychosis because it may increase the risk of death in this population. Caplyta is also not recommended for people who have heart problems or a stroke history; who use or abuse street drugs; who have kidney problems; who have diabetes or high cholesterol; who have low white blood cell count; who have problems swallowing; who have seizures; who have problems with urination or prostate; who have breast cancer; who are pregnant or breastfeeding; or who are allergic to any of the ingredients in Caplyta.
Positives or Pros
Caplyta has some advantages over other antipsychotics, such as:
- It has a lower risk of causing movement disorders, such as tardive dyskinesia (involuntary movements of the face, tongue, or limbs), akathisia (restlessness), and parkinsonism (tremor, stiffness, slowness).
- It has a lower risk of causing metabolic changes, such as weight gain, high blood sugar, and high cholesterol. This is partly due to the addition of samidorphan, which blocks the weight-promoting effects of lumateperone.
- It has a lower risk of causing hormonal changes, such as elevated prolactin levels, which may cause breast enlargement, milk production, menstrual irregularities, and sexual dysfunction.
- It has a lower risk of causing cardiac changes, such as QT prolongation (an abnormal heart rhythm that may lead to sudden death).
- It has a simple dosing regimen of one capsule once daily, without the need for titration (gradual dose adjustment) or food restrictions.
Negatives or Cons
Caplyta also has some disadvantages compared with other antipsychotics, such as:
- It is not available as a generic and it is very expensive. The average retail price of Caplyta is about $1,740 for a 30-day supply. However, there are some savings programs and coupons that may help lower the cost.
- It has a low bioavailability of 4.4%, which means that only a small fraction of the drug reaches the bloodstream after oral administration. This may affect its effectiveness and consistency.
- It has multiple drug interactions that may affect its metabolism and clearance. For example, it may interact with opioids, antidepressants, anticonvulsants, antibiotics, antifungals, antivirals, grapefruit juice, and herbal supplements. Therefore, it is important to inform your doctor and pharmacist about all the medications and supplements you are taking before starting Caplyta.
Conclusion
Caplyta is a new option for the treatment of schizophrenia and bipolar depression in adults. It has a unique mechanism of action that modulates various brain chemicals to reduce psychotic and depressive symptoms. It has shown efficacy and safety in clinical trials and has some benefits over other antipsychotics in terms of lower risk of movement disorders, metabolic changes, hormonal changes, and cardiac changes. However, it also has some drawbacks in terms of high cost, low bioavailability, and multiple drug interactions. Therefore, it is important to weigh the pros and cons of Caplyta with your doctor before deciding whether it is right for you.
Sources
¹: [Caplyta: Uses, Dosage & Side Effects - Drugs.com](https://www.drugs.com/caplyta.html)
²: [Lumateperone - Wikipedia](https://en.wikipedia.org/wiki/Lumateperone)
³: [FDA approves new drug for schizophrenia - FDA](https://www.fda.gov/news-events/press-announcements/fda-approves-new-drug-schizophrenia)
⁴: [FDA Approves Caplyta (lumateperone) for the Treatment of Schizophrenia in Adults - Intra-Cellular Therapies](https://ir.intracellulartherapies.com/news-releases/news-release-details/fda-approves-caplytar-lumateperone-treatment-schizophrenia-adults)
⁵: [Caplyta (Lumateperone Capsules): Uses, Dosage & Side Effects - RxList](https://www.rxlist.com/caplyta-drug.htm)
: [FDA Approves Caplyta® (lumateperone) for the Treatment of Depressive Episodes Associated with Bipolar I or II Disorder in Adults - Intra-Cellular Therapies](https://ir.intracellulartherapies.com/news-releases/news-release-details/fda-approves-caplytar-lumateperone-treatment-depressive-episodes)
Sources:
(1) For Adults with Bipolar Depression - CAPLYTA® (lumateperone). https://www.caplyta.com/.
(2) Lumateperone - Wikipedia. https://en.wikipedia.org/wiki/Lumateperone.
(3) Caplyta: Uses, Dosage, Side Effects & Warnings - Drugs.com. https://www.drugs.com/caplyta.html.
(4) Caplyta (lumateperone): Uses, Side Effects, Dosage & Reviews - GoodRx. https://www.goodrx.com/caplyta/what-is.
(5) Caplyta (Lumateperone Capsules): Uses, Dosage, Side Effects ... - RxList. https://www.rxlist.com/caplyta-drug.htm.
By Birk Gundersen RN, BSN.
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