- Buspirone for anxiety disorders
- Name of drug
- Why is it important for my child to take this medicine?
- What is buspirone available as?
- When should I give buspirone?
- How much should I give?
- How should I give it?
- When should the medicine start working?
- What if my child is sick (vomits)?
- What if I forget to give it?
- What if I give too much?
- Are there any possible side-effects?
- Side-effects you must do something about
- Other side-effects you need to know about
- Can other medicines be given at the same time as buspirone?
- Is there anything else I need to know about this medicine?
- General advice about medicines
- Where I should keep this medicine?
- Who to contact for more information
- Overcoming insomnia
- Types of insomnia
- Cognitive behavioral therapy
- Medications for insomnia
- Over-the-counter sleep aids
- About buspirone
- Before taking buspirone
- How to take buspirone
- Getting the most from your treatment
- Can buspirone cause problems?
- How to store buspirone
- Important information about all medicines
- Buspirone 10mg Tablets
Buspirone for anxiety disorders
This leaflet is about the use of buspirone for anxiety disorders.
This leaflet has been written specifically about the use of this medicine in children. The information may differ from that provided by the manufacturer. Please read this leaflet carefully. Keep it somewhere safe so that you can read it again.
Name of drug
Buspirone (also called buspirone hydrochloride)
Brand name: Buspar®
Why is it important for my child to take this medicine?
Taking this medicine regularly should help your child to feel less anxious.
What is buspirone available as?
- Tablets: 5 mg, 10 mg; these contain a small amount
When should I give buspirone?
Buspirone is usually given two to three times a day. Your doctor will tell you how often to give it.
- Twice each day: this should be once in the morning and once in the evening. Ideally, these times are 10–12 hours apart, for example some time between 7 and 8 am, and between 7 and 8 pm.
- Three times each day: this should be once in the morning, once in the early afternoon and once in the evening. Ideally, these times are at least 6 hours apart, for example 8 am, 2 pm and 8 pm.
Give the medicine at about the same times each day so that this becomes part of your child’s daily routine, which will help you to remember.
How much should I give?
Your doctor will work out the amount of buspirone (the dose) that is right for your child. The dose will be shown on the medicine label.
It is important that you follow your doctor’s instructions about how much to give.
How should I give it?
Tablets should be swallowed with a glass of water, milk or juice. Your child should not chew the tablet.You can crush the tablet and mix it with a small amount of soft food such as yogurt, honey or jam. Make sure your child swallows it straight away, without chewing.
When should the medicine start working?
It may take up to 2 weeks for buspirone to work properly so your child may still feel anxious during this time. It is important that you continue to give the medicine as your doctor has told you to. If you are concerned, contact your doctor.
What if my child is sick (vomits)?
- If your child is sick less than 30 minutes after having a dose of buspirone, give them the same dose again.
- If your child is sick more than 30 minutes after having a dose of buspirone, you do not need to give them another dose. Wait until the next normal dose.
What if I forget to give it?
If you usually give it twice a day
If you remember up to 4 hours after you should have given a dose, give your child the missed dose. For example, if you usually give a dose at about 7 am, you can give the missed dose at any time up to 11 am. If you remember after that time, do not give the missed dose. Just give the next dose as usual.
If you usually give it three times a day
Do not give the missed dose. Just give the next dose as usual.
What if I give too much?
You are unlikely to cause harm if you give an extra dose of buspirone by mistake.
If you are worried that you may have given your child too much, contact your doctor or local NHS services (call 111 in England and Scotland; 111 or 0845 4647 in parts of Wales). Have the medicine or packaging with you if you telephone for advice.
Are there any possible side-effects?
We use medicines to make our children better, but sometimes they have other effects that we don’t want (side-effects).
Side-effects you must do something about
If your child is short of breath or is wheezing, or their face, lips or tongue start to swell, or they develop a rash, they may be allergic to buspirone. Take your child to hospital or call an ambulance straight away.
Other side-effects you need to know about
- Your child may feel sick or be sick (vomit) when they first start taking buspirone. It may help to give each dose with or after food. This effect should wear off. If it is still a problem after a week, contact your doctor.
- Your child may feel light-headed and dizzy when they stand up, and may faint. This is because buspirone reduces blood pressure. Encourage your child to stand up slowly, and to sit or lie down if they feel dizzy. If this becomes a problem, contact your doctor.
- Your child may feel sleepy for a few hours after each dose of buspirone. If possible, give the last dose just before going to bed.
- Your child may have a dry mouth. Eating citrus fruits (e.g. oranges) and taking sips of water may help.
Can other medicines be given at the same time as buspirone?
- You can give your child medicines that contain paracetamol or ibuprofen, unless your doctor has told you not to.
- Buspirone should not be taken with some common drugs that you get on prescription. It is important to tell your doctor and pharmacist that your child is taking buspirone.
- Check with your doctor or pharmacist before giving any other medicines to your child. This includes herbal or complementary medicines.
Is there anything else I need to know about this medicine?
- It may take up to 2 weeks for buspirone to work and you may not notice any immediate effects. Contact your doctor for advice if you are concerned.
- Behavioural therapy is an important part of helping your child to be less anxious, so you should continue to practise techniques they have learnt.
General advice about medicines
- Try to give medicines at about the same times each day, to help you remember.
- If you are not sure a medicine is working, contact your doctor but continue to give the medicine as usual in the meantime. Do not give extra doses, as you may do harm.
- Only give this medicine to your child. Never give it to anyone else, even if their condition appears to be the same, as this could do harm.
If you think someone else may have taken the medicine by accident, contact your doctor straight away.
- Make sure that you always have enough medicine. Order a new prescription at least 2 weeks before you will run out.
- Make sure that the medicine you have at home has not reached the ‘best before’ or ‘use by’ date on the packaging. Give old medicines to your pharmacist to dispose of.
Where I should keep this medicine?
- Keep the medicine in a cupboard, away from heat and direct sunlight. It does not need to be kept in the fridge.
- Make sure that children cannot see or reach the medicine.
- Keep the medicine in the container it came in.
Who to contact for more information
Your child’s doctor, pharmacist or nurse will be able to give you more information about buspirone and about other treatments for anxiety disorders.
You can also get useful information from:
Published: February, 2011
Options include lifestyle changes, psychotherapy, and medication.
People with insomnia — the inability to sleep — may be plagued by trouble falling asleep, unwelcome awakenings during the night, and fitful sleep. They may experience daytime drowsiness yet still be unable to nap, and are often anxious, irritable, and unable to concentrate.
Insomnia is one of the most common types of sleep disturbance, at least occasionally affecting about one in three Americans. Epidemiologic studies suggest that 9% to 15% of Americans experience problems functioning in the daytime as a result of insomnia. Because insomnia often occurs in conjunction with a psychiatric disorder, insomnia may affect as many as 50% to 80% of patients in a typical mental health practice. Sleep problems are particularly common in patients with anxiety, depression, bipolar disorder, and attention deficit hyperactivity disorder (ADHD).
Types of insomnia
One of the most common ways to classify insomnia is in terms of duration of symptoms. Insomnia is considered transient if it lasts less than a month, short-term if it continues for one to six months, and chronic if the problem persists longer than six months.
The causes of transient or short-term insomnia are usually apparent to the individual affected. Typical circumstances include the death of a loved one, nervousness about an upcoming event, jet lag, or discomfort from an illness or injury. Chronic insomnia, on the other hand, is most often learned through conditioning. After experiencing a few sleepless nights, some people learn to associate the bedroom with being awake. Taking steps to cope with sleep deprivation — napping, drinking coffee, having a nightcap, or forgoing exercise — only worsens the problem. As insomnia persists, anxiety regarding the insomnia may grow more intense, leading to a vicious cycle in which fears about sleeplessness and its consequences become the primary cause of the insomnia.
Treatment becomes necessary once insomnia impairs sleep quality to the degree that it adversely affects a person’s health or ability to function during the day.
Cognitive behavioral therapy
For chronic insomnia, the treatment of choice is cognitive behavioral therapy. Both the American Academy of Sleep Medicine and the National Institutes of Health recommend using cognitive behavioral therapy (CBT) before medication, based on research concluding that CBT is just as effective as prescription medication at alleviating chronic insomnia in the short term and may be more effective in the long term. Although most of these studies have been restricted to people without psychiatric disorders, a smaller body of research suggests that CBT is also helpful for people who have a mental health problem along with insomnia.
When used to treat insomnia, CBT helps patients change negative thoughts and beliefs about sleep into positive ones. People with insomnia tend to become preoccupied with sleep and apprehensive about the consequences of poor sleep. This worry makes relaxing and falling asleep nearly impossible. A clinician using CBT helps a patient to set realistic goals and learn to let go of inaccurate thoughts that can interfere with sleep, such as hopelessness (“I’ll never get a decent night’s rest”). Instead, the patient learns to replace maladaptive thoughts with more constructive ones, such as “Not all my problems stem from insomnia,” or “I stand a good chance of getting a good night’s sleep tonight.” The therapist also provides structure and support while patients practice new thoughts and habits. CBT also involves lifestyle changes that may be used alone or combined as part of therapy (see “Lifestyle changes that promote sleep”).
In studies involving head-to-head comparisons, medication tends to relieve symptoms faster than CBT, but the benefits end once patients stop taking the drug. In contrast, the benefits of CBT become more apparent with time. For example, one study compared CBT alone with the combination of CBT and zolpidem (Ambien). At the six-week mark, patients in both groups improved, but those who received combination treatment improved faster, sleeping an average of 20 minutes longer per night than those assigned to CBT alone. However, in the second, longer-term phase of the study, benefits of drug therapy faded. After initially receiving combination therapy, patients were randomized to maintenance therapy with CBT alone or continued combination therapy (CBT and zolpidem). At the six-month mark, 68% of the patients receiving only maintenance CBT achieved remission, significantly more than the 42% receiving combination therapy.
The biggest obstacle to successful treatment with CBT is patient commitment — some people fail to complete all the required sessions or to practice the techniques on their own. Internet-based programs are being tested to address this challenge. Several small studies suggest that online CBT programs that teach people good sleep hygiene, relaxation techniques, and other strategies are promising. For example, one program, called SHUTi (Sleep Healthy Using the Internet), consisted of six online modules based on CBT techniques. In a pilot study, researchers found that SHUTi helped patients with long-term insomnia (lasting an average of 10 years) improve their ability to fall and stay asleep compared with a control group.
Lifestyle changes that promote sleep
The following approaches may be used on their own or combined with cognitive behavioral therapy.
Sleep restriction. People with insomnia tend to spend more time in bed, hoping this will lead to sleep. In reality, spending less time in bed — a technique known as sleep restriction — promotes more restful sleep and helps make the bedroom a welcome sight instead of a torture chamber. As the patient learns to fall asleep quickly and sleep soundly, the time in bed is slowly extended until it provides a full night’s sleep.
Some sleep experts suggest starting with six hours at first, or whatever amount of time the patient typically sleeps at night. Setting a rigid early morning waking time often works best. If the alarm is set for 7 a.m., a six-hour restriction means staying awake until 1 a.m., no matter how sleepy. Once the patient is sleeping well during the allotted six hours, he or she can add another 15 or 30 minutes until attaining a healthy amount of sleep.
Reconditioning. This technique reconditions people with insomnia to associate the bedroom with sleep instead of sleeplessness and frustration. It incorporates elements of stimulus control and sleep hygiene education by suggesting strategies such as these:
Use the bed only for sleeping or sex.
Go to bed only when sleepy. If unable to sleep, move to another room and do something relaxing. Stay up until feeling sleepy, then return to bed. If sleep does not follow quickly, repeat.
During the reconditioning process, get up at the same time every day and do not nap.
Relaxation techniques. For some people with insomnia, a racing or worried mind is the enemy of sleep. In others, physical tension is to blame. A variety of techniques — such as meditation, breathing exercises, progressive muscle relaxation, and visualization of peaceful settings — can calm the mind and relax the body enough to foster sleep.
Medications for insomnia
Prescription medications can be useful for some people with transient or short-term insomnia. Because behavioral therapies are as effective and may have longer-lasting results, however, drugs should be used at the lowest dose and for the shortest possible period of time. Clinicians recommend several different types of medications to treat insomnia.
Benzodiazepines. These medications enhance the activity of GABA, a neurotransmitter that calms brain activity. Different benzodiazepines vary in how quickly they take effect and how long they remain active in the body. Taken at night, benzodiazepines can lead to next-day drowsiness and sedation. If a patient’s main problem is getting to sleep, a clinician may prescribe a benzodiazepine that begins working quickly and is short-acting. An example is triazolam (Halcion). Although in theory it is an advantage to take a drug that will be eliminated from the body by morning, many clinicians have hesitated to recommend short-acting benzodiazepines because patients can develop rebound insomnia or a disconcerting amnesia for several hours after taking a dose of these drugs. Other benzodiazepines approved by the FDA for sleep problems are estazolam (ProSom) and temazepam (Restoril). These drugs last longer and so may help a person stay asleep through the night. In practice, many of the benzodiazepines used for treating anxiety — such as lorazepam (Ativan) and alprazolam (Xanax) — are also used to induce sleep.
One drawback of benzodiazepines is that they reduce duration of deep or slow-wave sleep, which is necessary for a person to feel refreshed the next morning. Another problem is tolerance, the need for more and more of the drug to obtain the same effect. Stopping any of these medications abruptly after long-term use can cause rebound insomnia that is worse than the initial sleeping problem.
Nonbenzodiazepines. While benzodiazepines affect multiple brain receptors, the nonbenzodiazepines act only on a few. As a result, they tend to cause fewer side effects than benzodiazepines, and have little or no effect on deep sleep. Nonbenzodiazepines include eszopiclone (Lunesta), zaleplon (Sonata), and zolpidem (Ambien). All three drugs help people fall asleep quicker, but may be useful in different circumstances.
Eszopiclone lengthens total sleep time. It takes a little longer to take effect than the other two drugs but also lasts longer.
Zolpidem also lengthens total sleep time. It acts faster than eszopiclone (within 20 minutes) and, for the most part, wears off before a patient’s typical waking time. A long-acting version of zolpidem (Ambien CR) is intended to help people stay asleep as well as fall asleep.
Zaleplon acts as quickly as zolpidem, but wears off faster. As a result, taking this medication before bed may not enable a patient to sleep the whole night. However, this drug may be the one to choose if a patient wakes up in the middle of the night and can’t fall back asleep.
While nonbenzodiazepines have fewer drawbacks than benzodiazepines, they’re not perfect for everyone. Some people find the drugs aren’t powerful enough to put them to sleep. And the drugs may still cause morning grogginess, tolerance, and rebound insomnia, as well as headache, dizziness, nausea, and, in rare cases, sleepwalking and sleep eating. The long-term effects of nonbenzodiazepines remain unknown.
Antidepressants. Some clinicians believe antidepressants have fewer side effects and are safer for long-term use than benzodiazepines. Further, these drugs may be appropriate because many people with depression also experience insomnia, and taking an antidepressant may help relieve symptoms of both problems. Sedating tricyclics such as amitriptyline (Elavil, Endep) and doxepin (Sinequan) are frequently prescribed for insomnia. Other antidepressants that work on serotonin receptors, particularly trazodone (Desyrel), nefazodone (Serzone), and mirtazapine (Remeron) — each with its own set of advantages and disadvantages — may also be prescribed for insomnia.
Studies in people with depression who also have sleep problems show that antidepressants reduce the time it takes to fall asleep and nighttime arousals. How these drugs work isn’t clear, although presumably their sedative effects promote sleep. In addition, the drugs’ ability to ease anxiety and mild depression may make it easier for people with these problems to relax and fall asleep.
The effect of antidepressants on sleep quality varies; in general, they reduce REM (dreaming) sleep but have little impact on deep sleep. Common side effects include dizziness, dry mouth, upset stomach, weight gain, and sexual dysfunction. These drugs also can increase leg movements during sleep. Some people find certain antidepressants make them feel nervous or restless, so the medication can actually exacerbate insomnia. It’s not clear if these medications lead to tolerance or rebound insomnia.
Melatonin. The hormone melatonin helps control the circadian cycle of sleep and wakefulness. The brain’s production of melatonin peaks in the late evening, in conjunction with the onset of sleep. Drugs or supplements that act on melatonin try to take advantage of this natural sleep aid by boosting levels of this chemical before bedtime.
Ramelteon (Rozerem) triggers melatonin receptors and is approved to treat insomnia for people who have trouble falling asleep at bedtime. Because people produce less melatonin as they age, theoretically this drug may be more likely to benefit older rather than younger people. In reality, however, most older people with insomnia tend to have problems with nighttime awakenings, not with falling asleep — suggesting that ramelteon should be prescribed on the basis of symptoms rather than age.
Ramelteon’s most common side effect is dizziness, and it may also worsen symptoms of depression. To avoid a drug interaction that elevates blood levels of ramelteon, people who use the antidepressant fluvoxamine (Luvox) shouldn’t take it. People with severe liver damage should also avoid taking ramelteon.
Another option is synthetic melatonin, sold as a supplement. Despite some initial enthusiasm for this approach, however, most subsequent research has been disappointing, finding either minimal benefits or none at all. The most commonly reported side effects of melatonin supplements are nausea, headache, and dizziness.
Over-the-counter sleep aids
Drugstores carry a confusing variety of over-the-counter sleep products that usually contain various types of antihistamines as active ingredients. Most over-the-counter sleep aids, including Nytol and Sominex, contain the antihistamine diphenhydramine. A few, such as Unisom SleepTabs, contain doxylamine. Aspirin-Free Anacin PM and Extra Strength Tylenol PM combine antihistamines with the pain reliever acetaminophen.
Over-the-counter antihistamines have a sedating effect and are generally safe. Sleep experts usually advise against using these medications, however, not only because of their side effects (discussed below) but also because they are often ineffective in relieving sleep problems. Furthermore, there is no information about the safety of taking such medications over the long term.
Short-term side effects include nausea and, more rarely, fast or irregular heartbeat, blurred vision, or heightened sensitivity to sunlight. Complications are generally more common in children and people over age 60. Alcohol heightens the effect of over-the-counter sleep medications, which can also interact adversely with some other drugs. A patient considering taking a nonprescription sleeping pill may want to check first with a clinician for advice about how to avoid the possibility of interactions with other medications.
Morin CM, et al. “Cognitive Behavioral Therapy, Singly and Combined with Medication, for Persistent Insomnia: A Randomized Controlled Trial,” Journal of the American Medical Association (May 20, 2009): Vol. 301, No. 19, pp. 2005–15.
Sullivan SS. “Insomnia Pharmacology,” Medical Clinics of North America (May 2010): Vol. 94, No. 3, pp. 563–80.
As a service to our readers, Harvard Health Publishing provides access to our library of archived content. Please note the date of last review on all articles. No content on this site, regardless of date, should ever be used as a substitute for direct medical advice from your doctor or other qualified clinician.
|Type of medicine||Anxiolytic|
|Used for||Anxiety (in people over 18 years of age)|
Most people feel anxious from time to time. Anxiety is normal in stressful situations and can even be helpful. However, anxiety can become abnormal if it appears for no apparent reason, or if it is out of proportion to a stressful situation or continues after a stressful situation has passed.
Buspirone is an anti-anxiety medicine which is prescribed for short periods of time to help ease symptoms of anxiety. Although it is not clear how it works, it is thought to affect a brain chemical which may be involved in causing anxiety symptoms.
Before taking buspirone
Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking buspirone it is important that your doctor or pharmacist knows:
- If you are pregnant, trying for a baby or breastfeeding.
- If you have epilepsy.
- If you have liver or kidney problems.
- If you have raised pressure in your eye (glaucoma)
- If you have a condition called myasthenia gravis, which causes muscle weakness.
- If you have a rare inherited blood disorder called porphyria.
- If you are taking any other medicines. This includes any medicines you are taking which are available to buy without a prescription, as well as herbal and complementary medicines.
- If you have ever had an allergic reaction to a medicine.
How to take buspirone
- Before you start this treatment, read the manufacturer’s printed information leaflet from inside your pack. The leaflet will give you more information about buspirone and a full list of side-effects which you may experience from taking it.
- Take buspirone tablets exactly as your doctor tells you to. It is likely that you will be prescribed one 5 mg tablet to take two or three times a day to begin with. This may be increased after a few days if needed. Swallow the tablets with a drink of water.
- Try to take your doses at the same times each day, as this will help you to remember to take them. You may choose whether to take buspirone tablets before or after meals, but you should stick to one or the other. So, either take all of your doses before meals, or take all of your doses after meals.
- Do not drink large amounts of grapefruit juice while you are on buspirone. This is because grapefruit juice can interfere with the enzymes that break down buspirone in your digestive system. This may result in your body absorbing more of the medicine than intended. It will increase the risk of side-effects.
- If you forget to take a dose, take it as soon as you remember unless it is nearly time for your next dose, in which case leave out the missed dose. Do not take two doses together to make up for a forgotten dose.
Getting the most from your treatment
- Remember to keep your regular appointments with your doctor or clinic. This is so your doctor can check on your progress.
- Taking buspirone may increase the time it takes for you to react and may impair your judgement. Because of this, your ability to drive could be affected.
- Buspirone may make you feel sleepy. Do not drink alcohol while you are on buspirone tablets as it will increase the risk of this.
- If you are having any medical treatment, tell the person carrying out the treatment that you are taking buspirone.
- If you need to buy any medicines, check with a pharmacist that they are safe to take with buspirone.
Can buspirone cause problems?
Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. The table below contains some of the more common ones associated with buspirone. You will find a full list in the manufacturer’s information leaflet supplied with your medicine. The unwanted effects often improve as your body adjusts to the new medicine, but speak with your doctor or pharmacist if any of the following side-effects continue or become troublesome.
|Common buspirone side-effects||What can I do if I experience this?|
|Feeling dizzy or sleepy, blurred vision||Do not drive and do not use tools or machines. Do not drink alcohol|
|Tummy (abdominal) pain, feeling sick (nausea) or being sick (vomiting), loose or watery stools (diarrhoea)||Drink plenty of water and stick to simple meals – avoid rich or spicy food|
|Headache||Drink plenty of water and ask a pharmacist to recommend a suitable painkiller. If the headaches continue, let your doctor know|
|Dry mouth||Try chewing sugar-free gum or sucking sugar-free sweets|
|Changes in mood, difficulty sleeping, feeling unsteady, tingling feelings or numbness, fast heartbeat, nasal or throat symptoms, sweating, rash, muscle pains, constipation||If any of these become troublesome, speak with your doctor|
If you experience any other symptoms which you think may be due to this medicine, speak with your doctor or pharmacist.
How to store buspirone
- Keep all medicines out of the reach and sight of children.
- Store in a cool, dry place, away from direct heat and light.
Important information about all medicines
Never take more than the prescribed dose. If you suspect that you or someone else might have taken an overdose of this medicine, go to the accident and emergency department of your local hospital at once. Take the container with you, even if it is empty.
This medicine is for you. Never give it to other people even if their condition appears to be the same as yours.
Do not keep out-of-date or unwanted medicines. Take them to your local pharmacy which will dispose of them for you.
If you have any questions about this medicine ask your pharmacist.
Buspirone 10mg Tablets
The concomitant use of buspirone with other CNS-active drugs should be approached with caution. Effect of other drugs on buspirone
Association not recommended:
MAO inhibitors: Co-administration of MAO inhibitors may cause increases in blood pressure. Co-administration of MAO inhibitors and buspirone is therefore not recommended (see section 4.4). Erythromycin: Concomitant administration of buspirone (10 mg as single dose) and erythromycin (1.5 g once daily for four days) in healthy volunteers increased the plasma concentrations of buspirone (Cmax increased 5-fold and AUC 6-fold). If buspirone and erythromycin are to be used in combination, a low dose of buspirone (e.g., 2.5 mg twice daily) is recommended. Subsequent dose adjustments of either drug should be based on clinical response. Itraconazole: Concomitant administration of buspirone (10 mg as single dose) and itraconazole (200 mg once daily for four days) in healthy volunteers increased the plasma concentrations of buspirone (Cmax increased 13-fold and AUC 19-fold). If buspirone and itraconazole are to be used in combination, a low dose of buspirone (e.g., 2.5 mg once daily) is recommended. Subsequent dose adjustments of either drug should be based on clinical response.
Association with precautions of use:
Diltiazem: Concomitant administration of buspirone (10 mg as single dose) and diltiazem (60 mg three times daily) in healthy volunteers increased the plasma concentrations of buspirone (Cmax increased 5.3-fold and AUC 4-fold). Enhanced effects and increased toxicity of buspirone may be possible when buspirone is administered with diltiazem. Subsequent dose adjustments of either drug should be based on clinical response. Verapamil: Concomitant administration of buspirone (10 mg as single dose) and verapamil (80 mg three times daily) in healthy volunteers increased the plasma concentrations of buspirone (Cmax and AUC increased 3.4-fold). Enhanced effects and increased toxicity of buspirone may be possible when buspirone is administered with verapamil. Subsequent dose adjustments of either drug should be based on clinical response. Rifampicin: Rifampicin induces the metabolism of buspirone via CYP3A4. Therefore, concomitant administration of buspirone (30 mg as single dose) and rifampicin (600 mg once daily for 5 days) in healthy volunteers decreased the plasma concentrations (Cmax decreased 84 % and AUC decreased 90 %) and the pharmacodynamic effect of buspirone.• Antidepressants – the occurrence of elevated blood pressure in patients receiving buspirone and monoamine oxidase inhibitors (phenelzine and tranylcypromine) has been reported. Buspirone should not be used concomitantly with a MAOI. In healthy volunteers no interaction with the tricyclic antidepressant amitriptyline was seen.• Baclofen, lofexidine, nabilone, antihistamines may enhance any sedative effect.
Association to be taken into account:
SSRI: The combination of buspirone and selective serotonin reuptake inhibitors (SSRI) was tested in a number of clinical trials on more than 300,000 patients. Although no severe toxicities were observed, there were rare cases of seizures in patients that took SSRI and buspirone concomitantly.Separate cases of seizures in patients administered combination therapy with buspirone and SSRIs have been reported from regular clinical use.Buspirone should be used with caution in combination with serotonergic drugs (including MAOIs, L-tryptophan, triptans, tramadol, linezolid, SSRIs, lithium and St. John’s Wort) as there are isolated reports of serotonin syndrome occurring in patients on concomitant SSRI therapy. If this condition is suspected, treatment with buspirone should be immediately discontinued and supportive symptomatic treatment should be initiated. Protein Binding: In vitro buspirone may displace less firmly protein-bound drugs like digoxin. The clinical significance of this property is unknown. Nefazodone: The coadministration of buspirone (2.5 or 5 mg twice daily) and nefazodone (250 mg twice daily) to healthy volunteers resulted in marked increases in plasma buspirone concentrations (increases up to 20-fold in Cmax and up to 50-fold in AUC) and statistically significant decreases (about 50%) in plasma concentrations of buspirone metabolite, 1-pyrimidinylpiperazine. With 5-mg twice daily doses of buspirone, slight increases in AUC were observed for nefazodone (23%) and its metabolites hydroxynefazodone (HO-NEF) (17%) and mCPP (9%). Slight increases in Cmax were observed for nefazodone (8%) and its metabolite HO-NEF (11%).The side effect profile for subjects receiving buspirone 2.5 mg twice daily and nefazodone 250 mg twice daily was similar to that for subjects receiving either drug alone. Subjects receiving buspirone 5 mg twice daily and nefazodone 250 mg twice daily experienced side effects such as lightheadedness, asthenia, dizziness, and somnolence. It is recommended that the dose of buspirone be lowered when administered with nefazodone. Subsequent dose adjustments of either drug should be based on clinical response. Grapefruit juice: Concomitant administration of buspirone 10 mg and grapefruit juice (double strength 200 ml for 2 days) in healthy volunteers increased the plasma concentrations of buspirone (Cmax increased 4.3-fold and AUC 9.2-fold). Other Inhibitors and Inducers of CYP3A4: When administered with a potent inhibitor of CYP3A4, a low dose of buspirone, used cautiously, is recommended. When used in combination with a potent inducer of CYP3A4, e.g. phenobarbital, phenytoin, carbamazepine, St. John’s wort, an adjustment of the dosage of buspirone may be necessary to maintain busprione’s anxiolytic effect. Fluvoxamine: In short-term treatment with fluvoxamine and buspirone doubled buspirone plasma concentrations are observed compared to mono-therapy with buspirone. Trazodone: Concomitant administration of trazodone showed a 3-6 fold increase of ALT in some patients. Cimetidine: The concomitant use of buspirone and cimetidine has shown a slight increase in the 1-(2-pyrimidinyl)-piperazine metabolite of Buspirone. Because of the high protein binding of Buspirone (around 95%) caution is advised when drugs with a high protein binding are given concomitantly.Baclofen, lofexidine, nabilone, antihistamines may enhance any sedative effect.In vitro studies have shown that buspirone does not displace warfarin, digoxin, phenytoin, or propranolol from plasma proteins. Effect of buspirone on other drugs Diazepam: After addition of buspirone to the diazepam dose regimen, no statistically significant differences in the steady-state pharmacokinetic parameters (Cmax, AUC, and Cmin) were observed for diazepam, but increases of about 15% were seen for nordiazepam, and minor adverse clinical effects (dizziness, headache, and nausea) were observed. Haloperidol: Concomitant administration of haloperidol and buspirone can increase haloperidol serum levels. Digoxin: In humans, approximately 95% of buspirone is plasma protein bound. In vitro, buspirone does not displace tightly bound drugs (ie warfarin) from serum proteins. However, in vitro, buspirone may displace less firmly protein-bound drugs like digoxin. The clinical significance of this property is unknown.There are reports on increases in the prothrombin time after the addition of buspirone to a treatment regimen containing warfarin.