How long does it take buspirone to work

Side effects, dosage, uses, and more

Buspirone oral tablet is a generic prescription medication that’s used to treat anxiety disorders, such as generalized anxiety disorder, in adults. Anxiety is a condition that causes you to feel symptoms such as stress, apprehension, and nervousness.

Buspirone is not currently available as any brand-name drugs.

Drug details

Buspirone belongs to a classification of drugs called anxiolytics. These drugs work to decrease symptoms of anxiety.

Buspirone comes as an oral tablet (a tablet taken by mouth) that’s typically taken twice per day. The tablets come in several strengths: 5 milligrams (mg), 7.5 mg, 10 mg, 15 mg, and 30 mg.

Brand-name versions

Buspirone is not currently available in any brand-name forms. Buspar was the brand-name form of buspirone, but it’s no longer available.

Effectiveness

For information about the effectiveness of buspirone oral tablets, see the “Buspirone oral tablet uses” section below.

Buspirone oral tablet is a generic drug. A generic drug is an exact copy of the active drug in a brand-name medication. Buspar is the brand-name medication that buspirone oral tablet is based on. (However, Buspar is no longer available.)
A generic is considered to be as safe and effective as the original drug. Generics tend to cost less than brand-name drugs.
To learn more about how generics compare with brand-name drugs, see this article.

Buspirone oral tablets can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking buspirone oral tablets. These lists do not include all possible side effects.

For more information about the possible side effects of buspirone oral tablets, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be concerning or bothersome.

Note: The Food and Drug Administration (FDA) tracks side effects of drugs it has approved. If you would like to notify the FDA about a side effect you’ve had with buspirone oral tablet, you can do so through MedWatch.

Mild side effects

Mild side effects* of buspirone oral tablets can include:

feeling dizzy or lightheaded
nausea
headache
excitement or restlessness
nervousness
insomnia (trouble sleeping)
anger†
sleepiness
sexual side effects, such as increased or decreased libido (sex drive)†
weight gain or weight loss†

You may experience more side effects in the first week that you take buspirone oral tablets. However, most of these side effects may go away within a few days or a couple of weeks. But if they become more severe or don’t go away, talk with your doctor or pharmacist.

* This is a partial list of mild side effects from buspirone oral tablet. To learn about other mild side effects, talk with your doctor or pharmacist, or view buspirone oral tablet’s prescribing information.
† To learn more about this side effect, see “Side effect details” below.

Serious side effects

Serious side effects from buspirone oral tablet aren’t common, but they can occur. Call your doctor right away if you have serious side effects. Call 911 or your local emergency number if your symptoms feel life threatening or if you think you’re having a medical emergency.

Serious side effects and their symptoms can include:

Serotonin syndrome. Symptoms can include:
- hallucinations (seeing or hearing things that aren’t really there)
- fast heart rate
- dizziness
- seizures
Allergic reaction.*

* For more information about this side effect, see “Side effect details” below.

Side effect details

Here are some details on certain side effects buspirone may cause.

Weight gain or weight loss

Changes in weight, such as weight gain or weight loss, can occur from taking buspirone oral tablets. However, changes in weight were not common side effects reported in people taking buspirone. To find out how often weight gain or weight loss occurred in clinical studies, see the drug’s prescribing information.

Other medications that your doctor may prescribe for anxiety or depression may affect your weight more than buspirone. Examples of other medications that may lead to changes in your weight include:

selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine (Prozac) or escitalopram (Lexapro)
serotonin-norepinephrine reuptake inhibitors (SNRIs), such as venlafaxine (Effexor XR) or duloxetine (Cymbalta)

In some cases, your doctor may recommend that you take these medications along with buspirone.

Although it’s not common, if you do experience changes in your weight while taking buspirone, talk with your doctor. They can recommend ways to manage this side effect.

Sexual side effects

In rare cases, buspirone oral tablets can cause sexual side effects. Examples may include:

increased or decreased libido (sex drive)
delayed ejaculation
impotence (inability for a male* to get and maintain an erection)

These side effects were not commonly reported in people taking buspirone oral tablets. To find out how often sexual side effects occurred in clinical studies, see the drug’s prescribing information.

However, other medications that treat anxiety or depression can cause sexual side effects more often than buspirone. Examples of these medications include SSRIs such as fluoxetine (Prozac) or escitalopram (Lexapro).

In fact, some studies show that buspirone can actually help reduce sexual side effects from other drugs used to treat depression. This may be especially true if you take medications such as SSRIs, which may cause sexual side effects.

Although sexual side effects are uncommon with buspirone, talk with your doctor if you experience them during your treatment. Your doctor can recommend ways to manage these side effects.

* Sex and gender exist on spectrums. Use of the term “male” in this article refers to sex at birth.

Anger

In rare cases, anger can be a side effect of buspirone oral tablets. This was not a common side effect in studies, but some people taking the drug did develop anger or even hostility while using buspirone. To find out how often this side effect occurred in clinical studies, see the drug’s prescribing information.

Symptoms of anger may include:

increased heart rate
tense muscles
clenching your jaw or grinding your teeth
sweating
feeling anxious, nervous, or unable to relax

If you experience any symptoms of anger, be sure to tell your doctor.

If you have a history of anger or if you experience unexplained anger while taking buspirone, tell your doctor. They may want to monitor you more closely during your treatment, or they may recommend a different medication to treat your anxiety.

Allergic reaction
As with most drugs, some people can have an allergic reaction after taking buspirone oral tablet.
Symptoms of a mild allergic reaction can include:
skin rash
itchiness
flushing (temporary warmth, redness, or deepening of skin color)
A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:
swelling under your skin, typically in your eyelids, lips, hands, or feet
swelling of your tongue, mouth, or throat
trouble breathing
Call your doctor right away if you have an allergic reaction to buspirone, as the reaction could become severe. Call 911 or your local emergency number if your symptoms feel life threatening or if you think you’re having a medical emergency.

The dosage for buspirone oral tablets that your doctor prescribes will depend on several factors. These include:

the type and severity of the condition you’re using buspirone oral tablet to treat
other medical conditions you may have
other medications that you are taking

Typically, your doctor will start you on a low dosage. Then they’ll adjust it over time to reach the amount that’s right for you. Your doctor will ultimately prescribe the smallest dosage that provides the desired effect.

The following information describes dosages that are commonly used or recommended. However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to fit your needs.

Drug strengths

Buspirone oral tablets are taken by mouth. They come in the following strengths: 5 milligrams (mg), 7.5 mg, 10 mg, 15 mg, and 30 mg.

Dosage for anxiety

To treat anxiety disorders, in most cases, your doctor will recommend a starting dose of 7.5 mg of buspirone taken by mouth twice per day. This will give you a daily dose of 15 mg. Then, your doctor may increase your dose every 2 to 3 days by 5 mg per day to reach the buspirone dose that’s best for you. The maximum dose of buspirone is 60 mg per day, or 30 mg taken twice daily.

What if I miss a dose?

If you miss your dose of buspirone, take it as soon as you remember. However, if it is almost time for your next dose, just skip your missed dose and continue with your normal dosing schedule. If you missed a dose of your buspirone and are unsure when to take your next dose, talk with your doctor or pharmacist. They can recommend when you should take your next dose.

To help make sure you don’t miss a dose, try using a medication reminder. This can include setting an alarm or timer on your phone or downloading a reminder app. A kitchen timer can work, too.

Will I need to use this drug long term?

The buspirone oral tablet may be used as a long-term treatment. If you and your doctor determine that buspirone is safe and effective for you, you’ll likely take it long term.

You should not drink alcohol while taking buspirone oral tablets. This is because drinking alcohol during your buspirone treatment can raise your risk for side effects, such as headache or dizziness. It can also cause more serious side effects, such as trouble breathing or trouble concentrating.

If you drink alcohol, talk with your doctor before you start using buspirone.

Buspirone oral tablet can interact with several other medications. It can also interact with certain foods.

Different interactions can cause different effects. For instance, some interactions can interfere with how well a drug works. Other interactions can increase side effects or make them more severe.

Buspirone and other medications

Below is a list of medications that can interact with buspirone oral tablets. This list does not contain all drugs that may interact with buspirone.

Before taking buspirone, talk with your doctor and pharmacist. Tell them about all prescription, over-the-counter, and other drugs you take. Also tell them about any vitamins, herbs, and supplements you use. Sharing this information can help you avoid potential interactions.

If you have questions about drug interactions that may affect you, ask your doctor or pharmacist.

Types of drugs that you should not take with buspirone include:

Monoamine oxidase inhibitors (MAOIs). You should never take buspirone with an MAOI or within 14 days of stopping an MAOI. This is because taking buspirone with an MAOI raises your risk for serotonin syndrome or hypertension (high blood pressure), which can be very serious. Examples of MAOIs include:
- tranylcypromine (Parnate)
- phenelzine (Nardil)
- selegiline (Emsam)
- linezolid (Zyvox)
- methylene blue by intravenous (IV) infusion (Provayblue)

Types of drugs that can interact with buspirone include:

Haloperidol (Haldol). Taking buspirone with haloperidol may increase your risk for side effects from haloperidol. If you take these drugs together, your doctor may need to adjust your dose of buspirone.
- Antidepressants. Taking buspirone along with certain antidepressants may raise your risk for serotonin syndrome, which can be serious. If you take these drugs together, your doctor may monitor you more closely during treatment. Examples of antidepressants that may interact with buspirone include:
  - nefazodone (may also raise your risk for side effects from buspirone if used together)
  - fluoxetine (Prozac)
  - escitalopram (Lexapro)
  - sertraline (Zoloft)
Certain heart medications. Taking buspirone with certain heart medications may raise your risk for side effects from buspirone. If you take these drugs together, your doctor may need to adjust your buspirone dose. Examples of heart medications that may interact with buspirone include:
- diltiazem (Cardizem CD)
- verapamil (Verelan)
Certain antibiotics or antifungals. Using buspirone with some antibiotics or antifungals may raise your risk for side effects from buspirone. If you take these drugs together, your doctor may need to change your dose of buspirone. Examples of antibiotics or antifungals that may interact with buspirone include:
- erythromycin (Erythrocin)
- itraconazole (Sporanox, Tolsura)
- ketoconazole
Rifampin (Rimactane, Rifadin). Taking buspirone with rifampin may make buspirone less effective. If you take these drugs together, your doctor may need to change your dose of buspirone.
Dexamethasone. Using buspirone with dexamethasone may make buspirone less effective. If you take these drugs together, your doctor may need to change your dose of buspirone.
Seizure medications. Using buspirone with certain seizure medications can make buspirone less effective. If you do take these drugs together, your doctor may need to adjust your buspirone dose. Examples of seizure medications that may interact with buspirone include:
- phenytoin (Dilantin)
- phenobarbital
- carbamazepine (Tegretol)
Ritonavir (Norvir). Taking ritonavir with buspirone can increase your risk for side effects from buspirone. If you use these two drugs together, your doctor may need to change your dose of buspirone.

Buspirone oral tablet and herbs and supplements

No herbs or supplements have been specifically reported to interact with buspirone oral tablets. However, you should still check with your doctor or pharmacist before using any of these products while taking buspirone.

Buspirone oral tablet and foods

Buspirone can interact with grapefruit or grapefruit juice. You should avoid consuming grapefruit or grapefruit juice during your treatment, as doing so can raise your risk for side effects from buspirone.

Buspirone can be taken with or without food. To learn more, see the “How to take buspironeoral tablets” section below.

Here are answers to some frequently asked questions about buspirone oral tablet.

How does buspirone make you feel? Can it make you feel ‘high’?

No, buspirone should not make you feel “high.” But the drug can affect how you feel. Buspirone decreases your symptoms of anxiety and can make you feel restless, sleepy, or excited.

You should never snort buspirone. Snorting the drug will not make you feel “high.” In addition, snorting drugs can cause serious side effects, such as lung infections or damage to the inside of your nose.

If you have questions about how you’ll feel while taking buspirone, talk with your doctor.

Is buspirone an SSRI or benzodiazepine?

No, buspirone is not a selective serotonin reuptake inhibitor (SSRI) or a benzodiazepine. Instead, it belongs to a group of drugs called anxiolytics, which work to decrease symptoms of anxiety.

Does buspirone treat depression or problems with sleep?

Buspirone is not approved to treat depression or problems with sleep. It’s only FDA-approved for use in people with anxiety disorders.

However, in some cases, buspirone may be used off-label to treat other conditions, such as depression or sleep problems. Off-label drug use means that your doctor prescribes a medication for a use other than what it is approved for.

If you’re interested in taking buspirone to treat depression or sleep problems, talk with your doctor.

Is buspirone a controlled substance?

No, buspirone is not a controlled substance. A controlled substance has the potential to be misused or for people to become dependent on them. (Misuse means using a medication in a way other than how it was prescribed. Dependence is when you need a drug to feel normal or to function.)

Although buspirone is not a controlled substance, other medications that may be taken for anxiety are controlled substances. For example, anxiety medications such as alprazolam (Xanax), lorazepam (Ativan), diazepam (Valium), and clonazepam (Klonopin) are controlled substances.

If you have any concerns about taking buspirone, talk with your doctor or pharmacist.

How do you safely stop taking buspirone? Should you taper off?

How you should stop taking buspirone depends on your dose and other medications you’re taking. Always talk with your doctor before stopping any medications.

In some cases, your doctor may recommend that you switch to a different medication to treat your condition. If your dose of buspirone is low, they may recommend just stopping buspirone and switching to another treatment option.

If you take a higher dose of buspirone, your doctor may recommend slowly decreasing your dose over time. This helps your body adjust to the change.

If you have specific questions about how to stop your buspirone treatment, talk with your doctor or pharmacist.

Does buspirone interact with stimulants such as caffeine and Adderall?

No. Buspirone oral tablets should not interact with stimulants such as caffeine. They also don’t interact with amphetamine/dextroamphetamine (Adderall).

However, taking buspirone with medications that can increase your serotonin levels, such as Adderall, can cause your serotonin levels to get too high. This can raise your risk for serotonin syndrome, a condition that can be serious and even life threatening.

For a list of medications that may interact with buspirone, see the “Buspirone oral tablet interactions” section above. If you still have additional questions or concerns, talk with your doctor or pharmacist.

Buspirone oral tablet is FDA-approved to treat anxiety disorders, such as generalized anxiety disorder, in adults. People with anxiety may have symptoms such as feeling stressed, apprehensive, or nervous.

It’s not known exactly what buspirone’s mechanism of action is. (The mechanism of action of a drug explains how it works.) It’s possible that buspirone works by affecting levels of chemicals in your brain called serotonin and dopamine. These chemicals may help reduce symptoms of anxiety.

How long does it take to work? Does it start working immediately?

Buspirone will begin working after you take your first dose of medication. However, unlike other anxiety medications, it doesn’t reach its full effect right away. Because buspirone affects chemical levels in your brain, it can take 2 to 4 weeks before it reaches its full effect.

If you have anxiety attacks or need a medication that works more quickly than buspirone, talk with your doctor about other treatment options for your condition.

How long does it stay in your system?

Within 24 hours, most of a buspirone dose will be eliminated from your body.

Buspirone has a half-life of about 2 to 3 hours. (A half-life is how long it takes your body to get rid of half of the dose of medication.)

Other drugs are available that can treat anxiety disorders. Some may be a better fit for you than others. If you’re interested in finding an alternative to buspirone oral tablets, talk with your doctor. They can tell you about other medications that may work well for you.

Note: Some of the drugs listed here are used off-label to treat these specific conditions. Off-label drug use means using a drug for a purpose other than what it’s been approved for by the FDA.

Examples of other drugs that may be used to treat anxiety include:

escitalopram (Lexapro)
fluoxetine (Prozac)
alprazolam (Xanax)
clonazepam (Klonopin)
propranolol (Inderal)
diazepam (Valium)
sertraline (Zoloft)
tranylcypromine (Parnate)
lorazepam (Ativan)

Some of these medications are better taken daily, like buspirone. However, other medications on this list, such as alprazolam (Xanax), can also be used for anxiety attacks or as needed for anxiety.

The Food and Drug Administration (FDA) approves prescription drugs such as buspirone oral tablets to treat certain conditions. Buspirone may also be used off-label for other conditions. Off-label drug use means using a drug for a purpose other than what it’s been approved for by the FDA.

Buspirone oral tablet for anxiety

Buspirone oral tablet is FDA-approved to treat anxiety disorders, such as generalized anxiety disorder, in adults.

Effectiveness for anxiety

Buspirone has been shown to be an effective treatment for anxiety. It’s recommended as a treatment option for anxiety by the American Academy of Family Physicians. For information on how buspirone performed in clinical studies, see the drug’s prescribing information.

Buspirone oral tablet and children

Buspirone is not FDA-approved for use in children. However, small studies have been done in children to see if buspirone may be a safe or effective treatment option. Buspirone may be prescribed off-label to treat anxiety in children.

If you have questions about off-label use of buspirone for treating anxiety in your child, talk with their doctor.

Buspirone is FDA-approved to treat anxiety disorders, such as generalized anxiety disorder, in adults. In some cases, your doctor may recommend taking buspirone along with other medications to treat your condition.

For example, your doctor may recommend a medication to take if you have anxiety attacks or breakthrough anxiety (a sudden worsening of anxiety symptoms) while taking buspirone. Examples of these medications include alprazolam (Xanax) or lorazepam (Ativan). If you have depression along with anxiety, your doctor may recommend another medication, such as bupropion (Wellbutrin) or fluoxetine (Prozac).

In addition, your doctor may recommend medications or supplements to treat side effects caused by buspirone. For example, this could include taking melatonin at bedtime to help with insomnia (trouble sleeping).

Buspirone can interact with many medications, so before using buspirone, talk with your doctor about any other medications or supplements you take. Your doctor can determine if buspirone is safe to take with your other medications.

You should not experience withdrawal symptoms when you stop taking buspirone oral tablets. However, if you want to stop taking buspirone, be sure to talk with your doctor first. In some cases, they may recommend slowly reducing your dose over time so your body can adjust to the change.

Buspirone is not believed to cause drug dependence. Studies in both humans and animals did not show that buspirone can cause dependence or risk of misuse. However, because buspirone affects your brain, it’s still important for your doctor to monitor you for symptoms of dependence during your treatment.

If you have a history of dependence, tell your doctor before taking buspirone. They may monitor you more closely throughout your treatment.

Using more than the recommended dosage of buspirone oral tablets can lead to serious side effects.

Do not use more buspirone than your doctor recommends. It’s not known what the overdose dosage of buspirone may be.

Overdose symptoms

Symptoms of an overdose of buspirone can include:

nausea or vomiting
dizziness
sleepiness
stomach problems, like stomach pain or cramps
pinpoint pupils (pupils, the part of your eye that lets light inside, that are abnormally small)

What to do in case of overdose

If you think you’ve taken too much of this drug, call your doctor. You can also call the American Association of Poison Control Centers at 800-222-1222 or use their online tool. But if your symptoms are severe, call 911 or your local emergency number, or go to the nearest emergency room right away.

It’s not known whether buspirone oral tablets are safe to take during pregnancy. Animal studies do not show an increased risk to a fetus when pregnant females were given buspirone. However, animal studies do not always reflect what may happen in humans.

If you’re pregnant or planning to become pregnant, talk with your doctor before taking buspirone. They may recommend a different medication to treat your condition. If you do take buspirone, your doctor may want to monitor you more closely.

It’s not known if buspirone oral tablets are safe to take during pregnancy. If you’re sexually active and you or your partner can become pregnant, talk with your doctor about your birth control needs during your buspirone treatment.

For more information about taking buspirone during pregnancy, see the “Buspirone and pregnancy” section above.

It’s unknown whether it’s safe to breastfeed while taking buspirone oral tablets. Animal studies have shown that the drug passes into breast milk. However, it’s not known if buspirone may also pass into the breast milk of humans. Animal studies don’t always predict what will happen in humans.

It’s also not known what effects buspirone may have on a breastfed child.

If you’re currently breastfeeding or planning to breastfeed, talk with your doctor before using buspirone. They may recommend a different medication for your condition.

Before taking Buspirone oral tablets, talk with your doctor about your health history. Buspirone oral tablets may not be right for you if you have certain medical conditions or other factors affecting your health. These include:

Liver problems. If you have any liver problems, tell your doctor before you start taking buspirone. This drug is broken down by your liver. If your liver doesn’t work as well as it should, buspirone levels could build up in your body. If you have liver problems, your doctor may recommend a lower dose of buspirone, or they may recommend a different treatment for your condition.
Kidney problems. Your body gets rid of buspirone through your kidneys. If you have kidney problems, your body may not be able to clear the drug as it normally would. This can cause a buildup of buspirone levels in your body. If you have kidney problems, your doctor may recommend a different medication to treat your condition. Or in some cases, they may prescribe a lower dose of buspirone for you.
Allergic reaction. If you’ve had an allergic reaction to buspirone or any of its ingredients, you should not take buspirone oral tablets. This is a contraindication to its use. (A contraindication is a condition or factor that would prevent you from taking the medication.) Ask your doctor what other medications are better options for you.
Pregnancy. It’s not known if buspirone is safe to take during pregnancy. For more information, see the “Buspirone oral tablet and pregnancy” section above.
Breastfeeding. It’s not known whether buspirone is safe to use while breastfeeding. For more information, see the “Buspirone oral tablet and breastfeeding” section above.
Taking an MAOI. If you’re taking a monoamine oxidase inhibitor (MAOI), you should not take buspirone for at least 14 days after stopping the MAOI. For more information on this drug interaction, see the “Buspirone oral tablet interactions” section above.

Note: For more information about the potential negative effects of buspirone oral tablet, see the “Buspirone oral tablet side effects” section above.

As with all medications, the cost of buspirone oral tablet can vary. The actual price you’ll pay depends on your insurance plan, your location, and the pharmacy you use.

Keep in mind that you may be able to get a 90-day supply of buspirone. If approved by your insurance company, getting a 90-day supply of the drug could reduce your number of trips to the pharmacy and help lower the cost. If you’re interested in this option, check with your doctor or your insurance company.

Before approving coverage for buspirone, your insurance company may require you to get prior authorization. This means that your doctor and insurance company will need to communicate about your prescription before the insurance company will cover the drug. The insurance company will review the prior authorization request and decide if the drug will be covered.

If you’re not sure if you’ll need to get prior authorization for buspirone, contact your insurance company.

Financial and insurance assistance

Financial assistance to help you pay for buspirone oral tablet may be available.

Medicine Assistance Tool and NeedyMeds are two websites offering resources that may help decrease the price you pay for buspirone. They also offer tools to help you find low-cost healthcare, as well as educational resources. To learn more, visit their sites.

Mail-order pharmacies

Buspirone may be available through a mail-order pharmacy. Using this service may help lower the drug’s cost and allow you to get your medication without leaving home.

If recommended by your doctor, you may be able to receive a 90-day supply of buspirone, so there’s less concern about running out of the medication. If you’re interested in this option, check with your doctor and your insurance company. Some Medicare plans may help cover the cost of mail-order medications.

If you don’t have insurance, you can ask your doctor or pharmacist about online pharmacy options.

You should take buspirone oral tablets according to the instructions your doctor or healthcare professional gives you.

Buspirone comes as a tablet that’s taken by mouth. In most cases, buspirone should be taken twice per day. However, always take buspirone as your doctor prescribes it.

When to take

In most cases, you should take your dose of buspirone twice per day. Try to take your dose at about the same times each day. This helps make sure you always have a consistent amount of the drug in your body.

To help make sure you don’t miss a dose, try using a medication reminder. This can include setting an alarm or timer on your phone or downloading a reminder app. A kitchen timer can work, too.

Taking Buspirone oral tablet with food

You can take your dose of buspirone with or without food. However, it’s important to stay consistent with how you take your dose.

Food can affect how buspirone is absorbed. If you begin your treatment by taking buspirone with food, you should always take your dose with food. Or if you begin your treatment by taking your dose on an empty stomach, you should continue doing so with each dose.

If you have any questions about taking buspirone, talk with your doctor or pharmacist.

Can Buspirone oral tablet be crushed, split, or chewed?

Some buspirone tablets have a score line on them. (This is a line printed across the tablets.) These tablets can be split along the score line if needed.

The manufacturer of buspirone hasn’t made a recommendation on whether the tablets can be crushed or chewed.

If you’re having trouble swallowing your buspirone tablets, talk with your doctor or pharmacist. They may be able to recommend buspirone oral tablets with a score line on them, so you can cut them to make them easier to swallow. They can also recommend other medications to treat your condition that may be easier to take.

When you get buspirone oral tablet from the pharmacy, the pharmacist will add an expiration date to the label on the bottle. This date is typically 1 year from the date they dispensed the medication.

The expiration date helps guarantee that the medication is effective during this time. The current stance of the Food and Drug Administration (FDA) is to avoid using expired medications. If you have unused medication that has gone past the expiration date, talk to your pharmacist about whether you might still be able to use it.

How long a medication remains good can depend on many factors, including how and where you store the medication.

Buspirone oral tablet should be stored at a room temperature of 68°F to 77°F (20°C to 25°C) in a tightly sealed container away from light. Avoid storing this medication in areas where it could get damp or wet, such as bathrooms.

Disposal

If you no longer need to take buspirone oral tablets and have leftover medication, it’s important to dispose of it safely. This helps prevent others, including children and pets, from taking the drug by accident. It also helps keep the drug from harming the environment.

This article provides several useful tips on medication disposal. You can also ask your pharmacist for information about how to dispose of your medication.

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up to date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or another healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Side effects, dosage, uses, and more

Buspirone is not currently available as any brand-name drugs.

Drug details

Buspirone belongs to a classification of drugs called anxiolytics. These drugs work to decrease symptoms of anxiety.

Buspirone comes as an oral tablet (a tablet taken by mouth) that’s typically taken twice per day. The tablets come in several strengths: 5 milligrams (mg), 7.5 mg, 10 mg, 15 mg, and 30 mg.

Brand-name versions

Buspirone is not currently available in any brand-name forms. Buspar was the brand-name form of buspirone, but it’s no longer available.

Effectiveness

For information about the effectiveness of buspirone oral tablets, see the “Buspirone oral tablet uses” section below.

Buspirone oral tablet is a generic drug. A generic drug is an exact copy of the active drug in a brand-name medication. Buspar is the brand-name medication that buspirone oral tablet is based on. (However, Buspar is no longer available.)
A generic is considered to be as safe and effective as the original drug. Generics tend to cost less than brand-name drugs.
To learn more about how generics compare with brand-name drugs, see this article.

Mild side effects

Mild side effects* of buspirone oral tablets can include:

feeling dizzy or lightheaded
nausea
headache
excitement or restlessness
nervousness
insomnia (trouble sleeping)
anger†
sleepiness
sexual side effects, such as increased or decreased libido (sex drive)†
weight gain or weight loss†

Serious side effects

Serious side effects and their symptoms can include:

Serotonin syndrome. Symptoms can include:
- hallucinations (seeing or hearing things that aren’t really there)
- fast heart rate
- dizziness
- seizures
Allergic reaction.*

* For more information about this side effect, see “Side effect details” below.

Side effect details

Here are some details on certain side effects buspirone may cause.

Weight gain or weight loss

Other medications that your doctor may prescribe for anxiety or depression may affect your weight more than buspirone. Examples of other medications that may lead to changes in your weight include:

selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine (Prozac) or escitalopram (Lexapro)
serotonin-norepinephrine reuptake inhibitors (SNRIs), such as venlafaxine (Effexor XR) or duloxetine (Cymbalta)

In some cases, your doctor may recommend that you take these medications along with buspirone.

Although it’s not common, if you do experience changes in your weight while taking buspirone, talk with your doctor. They can recommend ways to manage this side effect.

Sexual side effects

In rare cases, buspirone oral tablets can cause sexual side effects. Examples may include:

increased or decreased libido (sex drive)
delayed ejaculation
impotence (inability for a male* to get and maintain an erection)

Although sexual side effects are uncommon with buspirone, talk with your doctor if you experience them during your treatment. Your doctor can recommend ways to manage these side effects.

* Sex and gender exist on spectrums. Use of the term “male” in this article refers to sex at birth.

Anger

Symptoms of anger may include:

increased heart rate
tense muscles
clenching your jaw or grinding your teeth
sweating
feeling anxious, nervous, or unable to relax

If you experience any symptoms of anger, be sure to tell your doctor.

Allergic reaction
As with most drugs, some people can have an allergic reaction after taking buspirone oral tablet.
Symptoms of a mild allergic reaction can include:
skin rash
itchiness
flushing (temporary warmth, redness, or deepening of skin color)
A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:
swelling under your skin, typically in your eyelids, lips, hands, or feet
swelling of your tongue, mouth, or throat
trouble breathing
Call your doctor right away if you have an allergic reaction to buspirone, as the reaction could become severe. Call 911 or your local emergency number if your symptoms feel life threatening or if you think you’re having a medical emergency.

The dosage for buspirone oral tablets that your doctor prescribes will depend on several factors. These include:

the type and severity of the condition you’re using buspirone oral tablet to treat
other medical conditions you may have
other medications that you are taking

Drug strengths

Buspirone oral tablets are taken by mouth. They come in the following strengths: 5 milligrams (mg), 7.5 mg, 10 mg, 15 mg, and 30 mg.

Dosage for anxiety

What if I miss a dose?

To help make sure you don’t miss a dose, try using a medication reminder. This can include setting an alarm or timer on your phone or downloading a reminder app. A kitchen timer can work, too.

Will I need to use this drug long term?

The buspirone oral tablet may be used as a long-term treatment. If you and your doctor determine that buspirone is safe and effective for you, you’ll likely take it long term.

If you drink alcohol, talk with your doctor before you start using buspirone.

Buspirone oral tablet can interact with several other medications. It can also interact with certain foods.

Different interactions can cause different effects. For instance, some interactions can interfere with how well a drug works. Other interactions can increase side effects or make them more severe.

Buspirone and other medications

Below is a list of medications that can interact with buspirone oral tablets. This list does not contain all drugs that may interact with buspirone.

If you have questions about drug interactions that may affect you, ask your doctor or pharmacist.

Types of drugs that you should not take with buspirone include:

Monoamine oxidase inhibitors (MAOIs). You should never take buspirone with an MAOI or within 14 days of stopping an MAOI. This is because taking buspirone with an MAOI raises your risk for serotonin syndrome or hypertension (high blood pressure), which can be very serious. Examples of MAOIs include:
- tranylcypromine (Parnate)
- phenelzine (Nardil)
- selegiline (Emsam)
- linezolid (Zyvox)
- methylene blue by intravenous (IV) infusion (Provayblue)

Types of drugs that can interact with buspirone include:

Haloperidol (Haldol). Taking buspirone with haloperidol may increase your risk for side effects from haloperidol. If you take these drugs together, your doctor may need to adjust your dose of buspirone.
- Antidepressants. Taking buspirone along with certain antidepressants may raise your risk for serotonin syndrome, which can be serious. If you take these drugs together, your doctor may monitor you more closely during treatment. Examples of antidepressants that may interact with buspirone include:
  - nefazodone (may also raise your risk for side effects from buspirone if used together)
  - fluoxetine (Prozac)
  - escitalopram (Lexapro)
  - sertraline (Zoloft)
Certain heart medications. Taking buspirone with certain heart medications may raise your risk for side effects from buspirone. If you take these drugs together, your doctor may need to adjust your buspirone dose. Examples of heart medications that may interact with buspirone include:
- diltiazem (Cardizem CD)
- verapamil (Verelan)
Certain antibiotics or antifungals. Using buspirone with some antibiotics or antifungals may raise your risk for side effects from buspirone. If you take these drugs together, your doctor may need to change your dose of buspirone. Examples of antibiotics or antifungals that may interact with buspirone include:
- erythromycin (Erythrocin)
- itraconazole (Sporanox, Tolsura)
- ketoconazole
Rifampin (Rimactane, Rifadin). Taking buspirone with rifampin may make buspirone less effective. If you take these drugs together, your doctor may need to change your dose of buspirone.
Dexamethasone. Using buspirone with dexamethasone may make buspirone less effective. If you take these drugs together, your doctor may need to change your dose of buspirone.
Seizure medications. Using buspirone with certain seizure medications can make buspirone less effective. If you do take these drugs together, your doctor may need to adjust your buspirone dose. Examples of seizure medications that may interact with buspirone include:
- phenytoin (Dilantin)
- phenobarbital
- carbamazepine (Tegretol)
Ritonavir (Norvir). Taking ritonavir with buspirone can increase your risk for side effects from buspirone. If you use these two drugs together, your doctor may need to change your dose of buspirone.

Buspirone oral tablet and herbs and supplements

Buspirone oral tablet and foods

Buspirone can be taken with or without food. To learn more, see the “How to take buspironeoral tablets” section below.

Here are answers to some frequently asked questions about buspirone oral tablet.

How does buspirone make you feel? Can it make you feel ‘high’?

No, buspirone should not make you feel “high.” But the drug can affect how you feel. Buspirone decreases your symptoms of anxiety and can make you feel restless, sleepy, or excited.

If you have questions about how you’ll feel while taking buspirone, talk with your doctor.

Is buspirone an SSRI or benzodiazepine?

No, buspirone is not a selective serotonin reuptake inhibitor (SSRI) or a benzodiazepine. Instead, it belongs to a group of drugs called anxiolytics, which work to decrease symptoms of anxiety.

Does buspirone treat depression or problems with sleep?

Buspirone is not approved to treat depression or problems with sleep. It’s only FDA-approved for use in people with anxiety disorders.

If you’re interested in taking buspirone to treat depression or sleep problems, talk with your doctor.

Is buspirone a controlled substance?

If you have any concerns about taking buspirone, talk with your doctor or pharmacist.

How do you safely stop taking buspirone? Should you taper off?

How you should stop taking buspirone depends on your dose and other medications you’re taking. Always talk with your doctor before stopping any medications.

If you take a higher dose of buspirone, your doctor may recommend slowly decreasing your dose over time. This helps your body adjust to the change.

If you have specific questions about how to stop your buspirone treatment, talk with your doctor or pharmacist.

Does buspirone interact with stimulants such as caffeine and Adderall?

No. Buspirone oral tablets should not interact with stimulants such as caffeine. They also don’t interact with amphetamine/dextroamphetamine (Adderall).

How long does it take to work? Does it start working immediately?

If you have anxiety attacks or need a medication that works more quickly than buspirone, talk with your doctor about other treatment options for your condition.

How long does it stay in your system?

Within 24 hours, most of a buspirone dose will be eliminated from your body.

Buspirone has a half-life of about 2 to 3 hours. (A half-life is how long it takes your body to get rid of half of the dose of medication.)

Note: Some of the drugs listed here are used off-label to treat these specific conditions. Off-label drug use means using a drug for a purpose other than what it’s been approved for by the FDA.

Examples of other drugs that may be used to treat anxiety include:

escitalopram (Lexapro)
fluoxetine (Prozac)
alprazolam (Xanax)
clonazepam (Klonopin)
propranolol (Inderal)
diazepam (Valium)
sertraline (Zoloft)
tranylcypromine (Parnate)
lorazepam (Ativan)

Some of these medications are better taken daily, like buspirone. However, other medications on this list, such as alprazolam (Xanax), can also be used for anxiety attacks or as needed for anxiety.

Buspirone oral tablet for anxiety

Buspirone oral tablet is FDA-approved to treat anxiety disorders, such as generalized anxiety disorder, in adults.

Effectiveness for anxiety

Buspirone oral tablet and children

If you have questions about off-label use of buspirone for treating anxiety in your child, talk with their doctor.

If you have a history of dependence, tell your doctor before taking buspirone. They may monitor you more closely throughout your treatment.

Using more than the recommended dosage of buspirone oral tablets can lead to serious side effects.

Do not use more buspirone than your doctor recommends. It’s not known what the overdose dosage of buspirone may be.

Overdose symptoms

Symptoms of an overdose of buspirone can include:

nausea or vomiting
dizziness
sleepiness
stomach problems, like stomach pain or cramps
pinpoint pupils (pupils, the part of your eye that lets light inside, that are abnormally small)

What to do in case of overdose

For more information about taking buspirone during pregnancy, see the “Buspirone and pregnancy” section above.

It’s also not known what effects buspirone may have on a breastfed child.

If you’re currently breastfeeding or planning to breastfeed, talk with your doctor before using buspirone. They may recommend a different medication for your condition.

Liver problems. If you have any liver problems, tell your doctor before you start taking buspirone. This drug is broken down by your liver. If your liver doesn’t work as well as it should, buspirone levels could build up in your body. If you have liver problems, your doctor may recommend a lower dose of buspirone, or they may recommend a different treatment for your condition.
Kidney problems. Your body gets rid of buspirone through your kidneys. If you have kidney problems, your body may not be able to clear the drug as it normally would. This can cause a buildup of buspirone levels in your body. If you have kidney problems, your doctor may recommend a different medication to treat your condition. Or in some cases, they may prescribe a lower dose of buspirone for you.
Allergic reaction. If you’ve had an allergic reaction to buspirone or any of its ingredients, you should not take buspirone oral tablets. This is a contraindication to its use. (A contraindication is a condition or factor that would prevent you from taking the medication.) Ask your doctor what other medications are better options for you.
Pregnancy. It’s not known if buspirone is safe to take during pregnancy. For more information, see the “Buspirone oral tablet and pregnancy” section above.
Breastfeeding. It’s not known whether buspirone is safe to use while breastfeeding. For more information, see the “Buspirone oral tablet and breastfeeding” section above.
Taking an MAOI. If you’re taking a monoamine oxidase inhibitor (MAOI), you should not take buspirone for at least 14 days after stopping the MAOI. For more information on this drug interaction, see the “Buspirone oral tablet interactions” section above.

Note: For more information about the potential negative effects of buspirone oral tablet, see the “Buspirone oral tablet side effects” section above.

As with all medications, the cost of buspirone oral tablet can vary. The actual price you’ll pay depends on your insurance plan, your location, and the pharmacy you use.

If you’re not sure if you’ll need to get prior authorization for buspirone, contact your insurance company.

Financial and insurance assistance

Financial assistance to help you pay for buspirone oral tablet may be available.

Mail-order pharmacies

Buspirone may be available through a mail-order pharmacy. Using this service may help lower the drug’s cost and allow you to get your medication without leaving home.

If you don’t have insurance, you can ask your doctor or pharmacist about online pharmacy options.

You should take buspirone oral tablets according to the instructions your doctor or healthcare professional gives you.

Buspirone comes as a tablet that’s taken by mouth. In most cases, buspirone should be taken twice per day. However, always take buspirone as your doctor prescribes it.

When to take

To help make sure you don’t miss a dose, try using a medication reminder. This can include setting an alarm or timer on your phone or downloading a reminder app. A kitchen timer can work, too.

Taking Buspirone oral tablet with food

You can take your dose of buspirone with or without food. However, it’s important to stay consistent with how you take your dose.

If you have any questions about taking buspirone, talk with your doctor or pharmacist.

Can Buspirone oral tablet be crushed, split, or chewed?

Some buspirone tablets have a score line on them. (This is a line printed across the tablets.) These tablets can be split along the score line if needed.

The manufacturer of buspirone hasn’t made a recommendation on whether the tablets can be crushed or chewed.

When you get buspirone oral tablet from the pharmacy, the pharmacist will add an expiration date to the label on the bottle. This date is typically 1 year from the date they dispensed the medication.

How long a medication remains good can depend on many factors, including how and where you store the medication.

Disposal

This article provides several useful tips on medication disposal. You can also ask your pharmacist for information about how to dispose of your medication.

Use of buspirone in clinical practice

Buspirone (spitomin) is a non-benzodiazepine anxiolytic, which is a derivative of azapirone. Azapirones are a class of drugs with high affinity for serotonin 5-HT1A receptors located on the body and in the endings of serotonergic neurons, as well as in the dendrites of postsynaptic neurons with which serotonergic endings contact. The anti-anxiety effect of buspirone is not associated with an effect on GABA-benzodiazepine receptors. However, in terms of anxiolytic activity, buspirone is comparable to such benzodiazepines as diazepam, lorazepam or alprazolam, but unlike them, it does not cause drug dependence, cognitive and psychomotor impairment, pronounced sedative and muscle relaxant effects [1].

Mechanism of action of buspirone

The mechanism of the anxilytic action of buspirone, which predetermines its features, is mainly due to the effect on serotonin receptors. Buspirone has a high affinity for presynaptic serotonin (5-HT1A) receptors, of which it is an agonist, as well as for postsynaptic serotonin receptors, for which it can be considered as a partial (partial) agonist [1].

Partial agonists are ligands that bind to receptors but are only able to cause their partial activation. If a partial agonist interacts with free receptors, it causes incomplete (50%) cell activation. If a partial agonist acts on a tissue whose receptors are already activated by a full agonist, then due to the displacement of the latter from their connection with the receptor, the cell response decreases and, therefore, it has a blocking effect.

Thus, due to its receptor action, buspirone reduces the synthesis and release of serotonin, reduces the activity of serotonergic neurons in the raphe nuclei ("serotonin stabilizer"). Buspirone is also able to interact with postsynaptic 5-HT2 receptors, but has a low affinity for them. Being a partial agonist, due to its postsynaptic action, it can theoretically reduce serotonergic activity and cause an anxiolytic effect, and due to its action on somatodendritic serotonin presynaptic autoreceptors, it can theoretically increase serotonergic activity and cause an antidepressant effect.

To a lesser extent, the drug selectively blocks pre- and postsynaptic D2-dopamine receptors. Moreover, it was originally developed as an antipsychotic, but later it turned out that it has a low affinity for dopamine receptors, and its presynaptic action prevails over the postsynaptic one, which prevents the neuroleptic effect.

Experimental studies have indicated a decrease in serotonin turnover with the introduction of low doses of buspirone, which reflects the stimulation of presynaptic autoreceptors. However, repeated administration of buspirone reduces the response of somatodendritic 5-HT1A receptors, since the decrease in 5-HT metabolism was less pronounced.

Buspirone can act as a partial agonist at postsynaptic serotonin 5-HT1A receptors in the hippocampus and prefrontal cortex, as well as presynaptic autoreceptors on the bodies of serotonergic neurons. Since the effect of azapirones develops over several days, it does not appear to be related to their direct action on receptors. Animal studies suggest that the anxiolytic effect of these drugs is due to their action on presynaptic receptors, and the antidepressant effect is due to the action on postsynaptic receptors.

Decreased serotonin circulation also occurs in the striatum, which may be accompanied by an inhibitory effect on dopaminergic transmission. This effect is manifested in the fact that the co-administration of buspirone can attenuate apomorphine sensitization. Thus, buspirone at a relatively low dose can counteract the side effect of apomorphine. However, the introduction of buspirone at a higher dose caused sensitization of motor behavior [2].

This effect may be due to blockade of presynaptic dopamine autoreceptors. The introduction of a relatively high dose of buspirone in the experiment caused a sharp increase in the synthesis and metabolism of dopamine in the striatum.

The experiment has shown that the administration of buspirone in the brain dialysate reduces the level of serotonin by 50%, but increases the level of dopamine by 100% and norepinephrine by 140%, which indicates a complex effect of buspirone on monoaminergic neurotransmission [3].

However, in addition to acting on autoreceptors, buspirone also has another point of application, since the administration of haloperidol, which blocks D1- and D2-postsynaptic mesolimbic and striatal receptors, did not block the dopaminomimetic effect of buspirone. It has been shown that the antagonistic effect of the drug on D2 receptors is 15 times weaker than the effect on 5-HT1A receptors. Buspirone is a relatively weak blocker of postsynaptic dopamine receptors, even at high doses. It binds with higher affinity to D3 and D4 receptors than to D2 receptors. The action on presynaptic dopamine receptors is stronger than the blockade of postsynaptic receptors. Only in super-high doses, postsynaptic striatal D1- and D2-receptors are blocked quite actively. However, weak postsynaptic dopaminergic antagonism weakens the presynaptic dopaminomimetic effect of the drug, avoiding stereotypy [2, 3].

Use of buspirone in generalized anxiety and other affective disorders

The greatest experience with the use of buspirone has been accumulated in generalized anxiety disorder (GAD). Clinical studies of the last 30 years have been accompanied by constant improvement in the nosological structure of anxiety disorders. At the beginning of the 20th century, the understanding of anxiety disorders was rather vague, but over time their place among other mental disorders has been more clearly defined, partly under the influence of pharmacological research.

Symptoms of GAD are chronic and often observed in patients who visit general practitioners. Typically, such patients present vague somatic complaints of fatigue, muscle pain or tension, and sleep disturbances.

Buspirone is the first FDA-approved non-benzodiazepine anxiolytic for the treatment of GAD, based on studies showing that it is comparable in efficacy to benzodiazepines.

In accordance with DSM-V [4] criteria, GAD is characterized by:

A. Excessive anxiety and worry (anxious expectations) that occurs most of the days for at least 6 months and manifests itself in a variety of events or activities (for example, in the performance of professional duties or while studying at school).

B. Difficulty in controlling anxiety.

C. Presence most of the days for 6 months at least 3 of the following symptoms: restlessness or restlessness; fast fatiguability; difficulty concentrating and being distracted; irritability; muscle tension; sleep disturbance.

D. Clinically significant distress or impairment of social, occupational, or other activities caused by anxiety, restlessness, or physical (psychomotor) symptoms.

E. These disorders that cannot be explained by a physiological effect of a psychoactive substance or medical illness.

E. These disorders that cannot be explained by another mental illness.

Buspirone has also been successfully used for the prophylactic treatment of migraine and alcoholism in individuals with comorbid anxiety disorder, as well as for the treatment of anxious depression, anxiety and agitation in patients with traumatic brain injury [5, 6].

The direct antidepressant effect of buspirone, independent of its anxiolytic action, has also been demonstrated. It may be due to the fact that the sensitivity of 5-HT1A autoreceptors in depression is increased, while the properties of postsynaptic 5-HT1A and 5-HT2A receptors do not change in untreated patients with depression.

Data on the effectiveness of buspirone in obsessive-compulsive disorder are contradictory, but some studies show a positive effect of the drug, especially when combined with other psychopharmacological drugs, primarily antidepressants. An open study showed that the addition of buspirone (at a dose of 30-90 mg/day) to selective serotonin reuptake inhibitors (SSRIs) increases the effectiveness of the treatment of body dysmorphic disorder in almost half of patients, mainly in those who had a partial effect on serotonergic antidepressants [7, 8].

Buspirone can be considered as an alternative to antidepressants in the treatment of social phobia. The effect of buspirone on social phobia has been shown in a placebo-controlled study. When added to SSRIs, buspirone may correct some of their side effects. For example, it has been shown that at a dose of 15-60 mg/day it can reduce sexual dysfunction and bruxism [8].

Antiaggressive effect of buspirone

Separate mention should be made of the anti-aggressive effect of buspirone in agitation and aggressive actions in patients with dementia, attention deficit hyperactivity disorder, and traumatic brain injury [8]. At the same time, the effect of buspirone at a dose of 15–60 mg/day was noted both in relation to verbal (60%) and physical (90%) aggression [9–12].

Effect of buspirone on cognitive functions

Data on the effect of buspirone on cognitive functions are contradictory, some studies show a moderate positive effect on regulatory functions, while others show no clear effect [13]. In any case, unlike benzodiazepines and sedatives, buspirone does not have a negative effect on cognitive functions, which distinguishes it from other drugs used to correct anxiety disorders [14].

Use of buspirone for the treatment of dependence syndrome

Due to its dopaminergic action, buspirone can be used to treat dependence syndrome. Initially, this quality was found in relation to addiction to cocaine. It has been experimentally shown that intramuscular administration of buspirone blocks D2 and D3 receptors, while oral administration of buspirone blocks D3 receptors more selectively, occupying more than 80% of the receptors. Thus, for the treatment of addiction, higher doses may be required - 2-3 times higher than for the treatment of anxiety (up to a maximum of 60 mg). As shown by previous studies, these doses are safe and well tolerated [15]. Correction of withdrawal anxiety under the influence of buspirone may also contribute to the treatment of alcohol and tobacco dependence [16-18].

Use of buspirone in extrapyramidal disorders

Experimental and clinical studies indicate that buspirone may be effective in the treatment of tardive dyskinesia. Tardive dyskinesia is characterized by involuntary movements involving the muscles of the head, limbs, or trunk. It usually occurs against the background of long-term therapy with antipsychotics, often manifesting itself or intensifying after their cancellation. Tardive dyskinesia is usually resistant to various treatments. Although the evidence base for buspirone in tardive dyskinesia is low, it may be an alternative to others (particularly dopaminergic drugs) with dangerous side effects. The mechanism of action of buspirone in tardive dyskinesia is unclear [19, twenty].

Buspirone may also be effective in patients with Parkinson's disease suffering from dyskinesias on the background of long-term levodopa therapy. The mechanism of action of the drug is not clear enough in this case either, but the therapeutic effect depends on the dose. In recent years, using pathomorphological and imaging methods, it has been shown that the serotonergic system is involved in the pathological process in Parkinson's disease, in particular, in the pathogenesis of a number of non-motor symptoms, as well as medicinal dyskinesias. Because of this, drugs that act on the serotonergic system can be effective against dyskinesias and non-motor symptoms such as depression, chronic fatigue, and psychotic disorders [21].

It has already been mentioned that 5-HT1A receptor agonists regulate striatal concentrations of dopamine formed from exogenous levodopa, whereby buspirone can reduce drug-induced dyskinesias ("peak dose") in Parkinson's disease.

In a clinical study [22], it was shown that consecutive administration of the drug for 3 days (at a dose of 15-30 mg / day), but not a single dose of the drug at a dose of 10 and 20 mg, led to a 20% reduction in dyskinesias (without an increase in symptoms parkinsonism). In another study, a 3-week dose of buspirone at a dose of 20 mg/day reduced the severity of drug-induced dyskinesias by 71% without any negative effect on the symptoms of parkinsonism. Thus, buspirone can be considered as a potentially effective strategy in the correction of drug-induced dyskinesias.

These clinical data are experimentally confirmed - at a dose of 2 mg / kg, buspirone attenuated violent movements by 45% in mice with an experimental model of dopaminergic dyskinesias. Administration of buspirone to rats at a dose of 0.25-2.5 mg/kg 30 min before levodopa reduced dyskinesias and improved locomotor activity. In the experiment, buspirone reduced catalepsy in rats induced by 6-OHDA and haloperidol.

The effectiveness of buspirone was also shown in dyskinesias that occurred after transplantation of fetal midbrain tissue. It is believed that transplantation dyskinesias are associated with serotonergic neurotransmission [23]. Correction of dyskinesias is more effective with a high dose of 5-HT1A agonist, which more completely blocks mediator release. Dopaminergic reinnervation after transplantation causes persistent dyskinesias due to the uncontrolled release of dopamine induced by serotonin. The release of dopamine occurs in this case with a lower intensity than with "peak dose" dyskinesia. Accordingly, the effect in this situation is more pronounced with systemic administration of lower doses of 5-HT1A agonists [22, 23].

Buspirone can be effective in hereditary spinocerebellar ataxia, which is explained by the pronounced serotonergic innervation of the cerebellum [24]. It is suggested that this effect may also be associated with an effect on the noradrenergic pathways. This assumption has been confirmed in several studies showing that buspirone reduces mild to moderate cerebellar ataxia by 37%. The positive effect of buspirone on the severity of ataxia was confirmed in a small placebo-controlled study [25, 26].

Practical aspects of the use of buspirone (Spitomin)

The main indications for the use of buspirone (spitomin) registered in the Russian Federation are generalized anxiety disorder (GAD), panic disorder, autonomic dysfunction syndrome, alcohol withdrawal syndrome (as adjuvant therapy), depressive disorders (as adjuvant therapy, but not prescribed for monotherapy depression). The literature describes the use of buspirone for various anxiety conditions, tobacco withdrawal, depression, as well as autism, obsessive-compulsive and premenstrual syndromes (in which the drug acts as an adjuvant). The mechanism of action makes it possible to use it for the treatment of resistant depression (in combination with an antidepressant) [27].

The therapeutic (anxiolytic) effect develops gradually, manifests itself after 7-14 days and reaches a maximum after 4 weeks.

The goal of treatment for mood disorders may be to achieve complete remission or at least symptomatic relief, and to prevent possible relapses if possible. In chronic anxiety disorders, long-term maintenance therapy with buspirone may be required for long-term symptom control.

An important advantage of buspirone is that, unlike classical anxiolytics such as benzodiazepines, it does not adversely affect psychomotor functions, does not cause tolerance, drug dependence and withdrawal symptoms, and does not potentiate the effect of alcohol. However, during the period of treatment with buspirone, alcohol should be excluded [28].

The absence of a therapeutic effect within 6-8 weeks requires an increase in the dose, but in some cases indicates resistance to the drug. In the absence of an effect, the drug is usually replaced with another agent (benzodiazepine or antidepressant). With a partial effect, an antidepressant, sedative or hypnotic (with insomnia) can be added to enhance its action. Especially often, buspirone is used in combination with an SSRI or a selective serotonin and norepinephrine reuptake inhibitor (SNRI) [29].

Use in persons under 18 years of age is contraindicated, according to the current instructions in the Russian Federation for buspirone. In children and adolescents from 6 to 18 years of age, no efficacy studies have been conducted in relation to anxiety disorder. Pregnancy and breastfeeding are also contraindications, although there is no direct evidence of danger.

Buspirone is generally well tolerated. Side effects, if they are observed, usually occur at the beginning of the course of treatment and then disappear, despite the continuation of the drug. In some cases, a dose reduction is necessary. As a side effect, the drug can cause dizziness, headache, weakness, sleep disturbance, decreased attention, extrapyramidal disorders (very rarely), confusion, nausea, dry mouth, diarrhea, vomiting, constipation, weight loss, weight gain, myalgia, muscle spasms, rash, sweating, paresthesia. In case of an overdose, vomiting, dizziness, miosis, depression of consciousness are possible. The drug is carefully combined with antipsychotics, cardiac glycosides, antihypertensive and antidiabetic agents, oral contraceptives. Interaction with MAO inhibitors can lead to serotonin syndrome or hypertensive crisis with more limited symptoms, therefore, the simultaneous use of buspirone and MAO inhibitors is contraindicated in the instructions for medical use.

In the Russian Federation, the drug is presented in the form of 10 mg divided tablets. The initial dose is 5 mg / day, if necessary, it is increased by 5 mg every 5 days. The average daily dose is 15 mg. The maximum single dose is 30 mg, the maximum daily dose is 60 mg. The daily dose is usually divided into 2-3 doses. The advantages of the drug include safety, lack of dependence and withdrawal syndrome, sexual dysfunction and weight gain. Moreover, buspirone is able to reduce sexual dysfunction caused by generalized anxiety and serotonergic antidepressants [28, 30].

The peculiarities of the drug include the gradual onset of the full clinical effect (within 4 weeks), while benzodiazepines act more quickly.

Buspirone is metabolized primarily by the microsomal enzyme CYP450 3A4. T½ is approximately 2-3 hours. Particular care should be taken when combined with CYP450 3A4 inhibitors (for example, diltiazem, verapamil, itraconazole, erythromycin), which can reduce the clearance of buspirone and increase its level in the blood. You should also avoid drinking large amounts of grapefruit and grapefruit juice at the same time. The dose of buspirone should also be reduced when using HIV protease inhibitors or ketoconazole. Conversely, CYP450 3A4 inducers (eg carbamazepine and rifampicin) may increase the clearance of buspirone. Buspirone increases blood levels of nordiazepam, the active metabolite of diazepam, which can cause dizziness, headache, and nausea.

In mild to moderate renal and hepatic insufficiency, liver cirrhosis, heart failure, in the elderly, the drug is prescribed in smaller doses. When discontinuing the drug, a gradual dose reduction is usually not necessary. In severe renal, hepatic insufficiency, uncontrolled epilepsy, glaucoma, myasthenia gravis, the drug is contraindicated.

Thus, buspirone, with its unique neurotransmitter effects, significantly expands the possibilities of treatment for a wide range of mental and neurological disorders - from anxiety disorders to dyskinesia in Parkinson's disease and ataxia. The relative safety of the drug makes its use in clinical practice very promising.

Description of BUSPIRONE indications, dosages, contraindications of the active substance BUSPIRONE

Rec.INN WHO registered

drug interaction

Included in preparations: list

Pharmacological action

Anxiolytic agent, azaspirodecanedione derivative. The mechanism of action has not been definitively established. According to pharmacological properties, it does not apply to benzodiazepines or barbiturates. It has a selective anxiolytic effect. It does not have anticonvulsant activity, does not have a muscle relaxant effect. It does not have a pronounced sedative effect, especially at low doses.

High affinity for serotonin 5-HT _1A receptors in dorsal raphe neurons and moderate affinity for dopamine D ₂ receptors in the brain. Buspirone does not have a pronounced affinity for benzodiazepine receptors, it does not affect the binding of GABA.

In contrast to benzodiazepines, the level of spontaneous excitation of noradrenergic cells in the bluish locus (locus ceruleus) increases rather than decreases under the action of buspirone. These specific differences in the site of action are responsible for differences in the development of dependence and tolerance between benzodiazepines and buspirone.

Buspirone is not believed to cause tolerance, physical or psychological dependence.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract, C _max in blood plasma is reached after 40-90 minutes. Bioavailability is low due to the pronounced effect during the "first pass" through the liver. When taken with food, it is possible to increase bioavailability due to impaired absorption of buspirone from the gastrointestinal tract and, therefore, a decrease in presystemic clearance. Plasma protein binding of buspirone is about 95%. It undergoes intensive metabolism in the liver with the participation of the CYP3A4 isoenzyme. As a result of hydroxylation, several inactive metabolites are formed, oxidative dealkylation leads to the formation of 1-(2-pyrimidinyl)-piperazine, which has anxiolytic activity. T _1/2 buspirone is usually 2-4 hours, but the final T _1/2 can be 11 hours. It is excreted mainly as metabolites in the urine and also in the feces.

Indications of the active substance BUSPIRON

Treatment of anxiety disorders or temporary relief of symptoms of anxiety.

Open list of ICD-10 codes

F40	Phobic anxiety disorders (including agoraphobia, social phobias)
F41.2	Mixed anxiety and depressive disorder
R45. 2	Alarm condition due to failures and misfortunes

Dosage regimen

Inside adults at the beginning of treatment - 5 mg 3 times / day. If necessary, the dose is increased by 5 mg / day every 2-3 days until the desired effect is achieved. The maximum dose is 45-60 mg / day.

Side effects

Possible: dizziness, headache, restlessness syndrome.

Rare: blurred vision, reduced ability to concentrate, dry mouth, myalgia, muscle spasms, muscle cramps and rigidity, tinnitus, sleep disturbance, nightmares, general weakness, dyspepsia, chest pain, depression, tachycardia, paresthesia, pain in the throat, increased body temperature.

Contraindications for use

Severe renal impairment, severe hepatic impairment, hypersensitivity to buspirone.

Use in pregnancy and lactation

Buspirone should be avoided during pregnancy and lactation.

Use in hepatic impairment

Contraindicated in severe hepatic impairment.

Use in impaired renal function

Contraindicated in severe renal impairment.

Use in children

The safety and efficacy of buspirone in children and adolescents under 18 years of age have not been established.

Special instructions

Buspirone is not used to treat anxiety and reduce tension associated with the stresses of everyday life.

Should not be used in patients with epilepsy or with a history of a tendency to develop seizures.

Use with caution in patients with hepatic and/or renal impairment.

Patients with drug abuse or a history of drug dependence should be closely monitored during treatment to detect the development of tolerance to buspirone or dependence.

Controlled studies have shown that buspirone is not effective for long-term (more than 3-4 weeks) treatment of anxiety. However, when used for several months, no side effects were detected.

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