Buspar

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Buspirone Hydrochloride Tablets USP, 5 mg are white to off-white, capsule-shaped, flat- faced, beveled-edge tablets debossed with bisect on one side; one side of bisect is debossed with 'ZE' and another is debossed with '36' and other side is plain

Manufacturer details: N/A. Revised: May 2016

The administration of buspirone hydrochloride tablets to a patient taking a monoamine oxidase inhibitor (MAOI) may pose a hazard. There have been reports of the occurrence of elevated blood pressure when buspirone hydrochloride tablets have been added to a regimen including an MAOI. Therefore, it is recommended that buspirone hydrochloride tablets not be used concomitantly with an MAOI.

Because buspirone hydrochloride tablets have no established antipsychotic activity, it should not be employed in lieu of appropriate antipsychotic treatment.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

BuSpar falls into category B.

There are no well-done studies that have been done in humans with BuSpar. In animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

In the U.S.

• Buspar
• Buspar Dividose
• Vanspar

Available Dosage Forms:

• Tablet

Therapeutic Class: Antianxiety

Chemical Class: Azaspirodecanedione

General

Studies indicate that BuSpar is less sedating than other anxiolytics and that it does not produce significant functional impairment. However, its CNS effects in any individual patient may not be predictable. Therefore, patients should be cautioned about operating an automobile or using complex machinery until they are reasonably certain that buspirone treatment does not affect them adversely.

While formal studies of the interaction of BuSpar (buspirone hydrochloride) with alcohol indicate that buspirone does not increase alcohol-induced impairment in motor and mental performance, it is prudent to avoid concomitant use of alcohol and buspirone.

Because BuSpar does not exhibit cross-tolerance with benzodiazepines and other common sedative/hypnotic drugs, it will not block the withdrawal syndrome often seen with cessation of therapy with these drugs. Therefore, before starting therapy with BuSpar, it is advisable to withdraw patients gradually, especially patients who have been using a CNS-depressant drug chronically, from their prior treatment. Rebound or withdrawal symptoms may occur over varying time periods, depending in part on the type of drug, and its effective half-life of elimination.

The syndrome of withdrawal from sedative/hypnotic/anxiolytic drugs can appear as any combination of irritability, anxiety, agitation, insomnia, tremor, abdominal cramps, muscle cramps, vomiting, sweating, flu-like symptoms without fever, and occasionally, even as seizures.

Because buspirone can bind to central dopamine receptors, a question has been raised about its potential to cause acute and chronic changes in dopamine-mediated neurological function (eg, dystonia, pseudo-parkinsonism, akathisia, and tardive dyskinesia). Clinical experience in controlled trials has failed to identify any significant neuroleptic-like activity; however, a syndrome of restlessness, appearing shortly after initiation of treatment, has been reported in some small fraction of buspirone-treated patients. The syndrome may be explained in several ways. For example, buspirone may increase central noradrenergic activity; alternatively, the effect may be attributable to dopaminergic effects (ie, represent akathisia). See ADVERSE REACTIONS: Postmarketing Experience.

Information for Patients

To assure safe and effective use of BuSpar, the following information and instructions should be given to patients:

1. Inform your physician about any medications, prescription or non-prescription, alcohol, or drugs that you are now taking or plan to take during your treatment with BuSpar.
2. Inform your physician if you are pregnant, or if you are planning to become pregnant, or if you become pregnant while you are taking BuSpar.
3. Inform your physician if you are breast-feeding an infant.
4. Until you experience how this medication affects you, do not drive a car or operate potentially dangerous machinery.
5. You should take BuSpar (buspirone hydrochloride) consistently, either always with or always without food.
6. During your treatment with BuSpar, avoid drinking large amounts of grapefruit juice.

Laboratory Tests

There are no specific laboratory tests recommended.

Drug Interactions

MAO inhibitors:  It is recommended that BuSpar not  be used concomitantly with MAO inhibitors (see WARNINGS).

Amitriptyline:  After addition of buspirone to the amitriptyline dose regimen, no statistically significant differences in the steady-state pharmacokinetic parameters (Cmax, AUC, and Cmin) of amitriptyline or its metabolite nortriptyline were observed.

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:  In a study in normal volunteers, concomitant administration of buspirone and haloperidol resulted in increased serum haloperidol concentrations. The clinical significance of this finding is not clear.

Nefazodone:  (see Inhibitors and Inducers of Cytochrome P450 3A4 [CYP3A4])

Trazodone:  There is one report suggesting that the concomitant use of Desyrel® (trazodone hydrochloride) and buspirone may have caused 3- to 6-fold elevations on SGPT (ALT) in a few patients. In a similar study attempting to replicate this finding, no interactive effect on hepatic transaminases was identified.

Triazolam/Flurazepam:  Coadministration of buspirone with either triazolam or flurazepam did not appear to prolong or intensify the sedative effects of either benzodiazepine.

Other Psychotropics:  Because the effects of concomitant administration of buspirone with most other psychotropic drugs have not been studied, the concomitant use of buspirone with other CNS-active drugs should be approached with caution.

Buspirone has been shown in vitro to be metabolized by CYP3A4. This finding is consistent with the in vivo interactions observed between buspirone and the following:

Diltiazem and Verapamil:  In a study of nine healthy volunteers, coadministration of buspirone (10 mg as a single dose) with verapamil (80 mg t.i.d.) or diltiazem (60 mg t.i.d.) increased plasma buspirone concentrations (verapamil increased AUC and Cmax of buspirone 3.4-fold while diltiazem increased AUC and Cmax 5.5-fold and 4-fold, respectively.) Adverse events attributable to buspirone may be more likely during concomitant administration with either diltiazem or verapamil. Subsequent dose adjustment may be necessary and should be based on clinical assessment.

Erythromycin:  In a study in healthy volunteers, coadministration of buspirone (10 mg as a single dose) with erythromycin (1.5 g/day for 4 days) increased plasma buspirone concentrations (5-fold increase in Cmax and 6-fold increase in AUC). These pharmacokinetic interactions were accompanied by an increased incidence of side effects attributable to buspirone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg b.i.d.) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment.

Grapefruit Juice:  In a study in healthy volunteers, coadministration of buspirone (10 mg as a single dose) with grapefruit juice (200 mL double-strength t.i.d. for 2 days) increased plasma buspirone concentrations (4.3-fold increase in Cmax; 9.2-fold increase in AUC). Patients receiving buspirone should be advised to avoid drinking such large amounts of grapefruit juice.

Itraconazole:  In a study in healthy volunteers, coadministration of buspirone (10 mg as a single dose) with itraconazole (200 mg/day for 4 days) increased plasma buspirone concentrations (13-fold increase in Cmax and 19-fold increase in AUC). These pharmacokinetic interactions were accompanied by an increased incidence of side effects attributable to buspirone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg q.d.) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment.

Nefazodone:  In a study of steady-state pharmacokinetics in healthy volunteers, coadministration of buspirone (2.5 or 5 mg b.i.d.) with nefazodone (250 mg b.i.d.) 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 the buspirone metabolite 1-PP. With 5 mg b.i.d. doses of buspirone, slight increases in AUC were observed for nefazodone (23%) and its metabolites hydroxynefazodone (HO-NEF) (17%) and meta-chlorophenylpiperazine (9%). Slight increases in Cmax were observed for nefazodone (8%) and its metabolite HO-NEF (11%). Subjects receiving buspirone 5 mg b.i.d. and nefazodone 250 mg b.i.d experienced lightheadedness, asthenia, dizziness, and somnolence, adverse events also observed with either drug alone. If the two drugs are to be used in combination, a low dose of buspirone (eg, 2.5 mg q.d.) is recommended. Subsequent dose adjustment of either drug should be based on clinical assessment.

Rifampin:  In a study in healthy volunteers, coadministration of buspirone (30 mg as a single dose) with rifampin (600 mg/day for 5 days) decreased the plasma concentrations (83.7% decrease in Cmax; 89.6% decrease in AUC) and pharmacodynamic effects of buspirone. If the two drugs are to be used in combination, the dosage of buspirone may need adjusting to maintain anxiolytic effect.

Other Inhibitors and Inducers of CYP3A4:   Substances that inhibit CYP3A4, such as ketoconazole or ritonavir, may inhibit buspirone metabolism and increase plasma concentrations of buspirone while substances that induce CYP3A4, such as dexamethasone or certain anticonvulsants (phenytoin, phenobarbital, carbamazepine), may increase the rate of buspirone metabolism. If a patient has been titrated to a stable dosage on buspirone, a dose adjustment of buspirone may be necessary to avoid adverse events attributable to buspirone or diminished anxiolytic activity. Consequently, 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 the dosage of buspirone may need adjusting to maintain anxiolytic effect.

Cimetidine: Coadministration of buspirone with cimetidine was found to increase Cmax (40%) and Tmax (2-fold), but had minimal effects on the AUC of buspirone.

In vitro, buspirone does not displace tightly bound drugs like phenytoin, propranolol, and warfarin from serum proteins. However, there has been one report of prolonged prothrombin time when buspirone was added to the regimen of a patient treated with warfarin. The patient was also chronically receiving phenytoin, phenobarbital, digoxin, and Synthroid®. In vitro, buspirone may displace less firmly bound drugs like digoxin. The clinical significance of this property is unknown.

Therapeutic levels of aspirin, desipramine, diazepam, flurazepam, ibuprofen, propranolol, thioridazine, and tolbutamide had only a limited effect on the extent of binding of buspirone to plasma proteins (see CLINICAL PHARMACOLOGY).

Drug/Laboratory Test Interactions

Buspirone hydrochloride may interfere with the urinary metanephrine/catecholamine assay. It has been mistakenly read as metanephrine during routine assay testing for pheochromocytoma, resulting in a false positive laboratory result. Buspirone hydrochloride should therefore be discontinued for at least 48 hours prior to undergoing a urine collection for catecholamines.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No evidence of carcinogenic potential was observed in rats during a 24-month study at approximately 133 times the maximum recommended human oral dose; or in mice, during an 18-month study at approximately 167 times the maximum recommended human oral dose.

With or without metabolic activation, buspirone did not induce point mutations in five strains of Salmonella typhimurium (Ames Test) or mouse lymphoma L5178YTK+ cell cultures, nor was DNA damage observed with buspirone in Wi-38 human cells. Chromosomal aberrations or abnormalities did not occur in bone marrow cells of mice given one or five daily doses of buspirone.

Pregnancy: Teratogenic Effects

Pregnancy Category B: No fertility impairment or fetal damage was observed in reproduction studies performed in rats and rabbits at buspirone doses of approximately 30 times the maximum recommended human dose. In humans, however, adequate and well-controlled studies during pregnancy have not  been performed. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Labor and Delivery

The effect of BuSpar (buspirone hydrochloride) on labor and delivery in women is unknown. No adverse effects were noted in reproduction studies in rats.

Nursing Mothers

The extent of the excretion in human milk of buspirone or its metabolites is not known. In rats, however, buspirone and its metabolites are excreted in milk. BuSpar administration to nursing women should be avoided if clinically possible.

Pediatric Use

The safety and effectiveness of buspirone were evaluated in two placebo-controlled 6-week trials involving a total of 559 pediatric patients (ranging from 6 to 17 years of age) with GAD. Doses studied were 7.5 mg to 30 mg b.i.d. (15–60 mg/day). There were no significant differences between buspirone and placebo with regard to the symptoms of GAD following doses recommended for the treatment of GAD in adults. Pharmacokinetic studies have shown that, for identical doses, plasma exposure to buspirone and its active metabolite, 1-PP, are equal to or higher in pediatric patients than adults. No unexpected safety findings were associated with buspirone in these trials. There are no long-term safety or efficacy data in this population.

Geriatric Use

In one study of 6632 patients who received buspirone for the treatment of anxiety, 605 patients were ≥65 years old and 41 were ≥75 years old; the safety and efficacy profiles for these 605 elderly patients (mean age = 70.8 years) were similar to those in the younger population (mean age = 43.3 years). Review of spontaneously reported adverse clinical events has not identified differences between elderly and younger patients, but greater sensitivity of some older patients cannot be ruled out.

There were no effects of age on the pharmacokinetics of buspirone (see CLINICAL PHARMACOLOGY: Special Populations).

Use in Patients With Impaired Hepatic or Renal Function

Buspirone is metabolized by the liver and excreted by the kidneys. A pharmacokinetic study in patients with impaired hepatic or renal function demonstrated increased plasma levels and a lengthened half-life of buspirone. Therefore, the administration of BuSpar to patients with severe hepatic or renal impairment cannot be recommended (see CLINICAL PHARMACOLOGY).

BuSpar® (buspirone hydrochloride tablets, USP) Tablets, 5 mg and 10 mg (white, ovoid-rectangular with score, MJ logo, strength and the name BuSpar embossed) are available in bottles of 100.

5 mg tablets
NDC 0087-0818-41     Bottles of 100

10 mg tablets
NDC 0087-0819-41     Bottles of 100

Tablets, 15 mg white, in the DIVIDOSE® tablet design imprinted with the MJ logo, are available in bottles of 60 and 180. Tablets, 30 mg pink, in the DIVIDOSE® tablet design imprinted with the MJ logo, are available in bottles of 60. The 15 mg and 30 mg tablets are scored so that they can be either bisected or trisected. The 15 mg tablet has ID number 822 on one side and on the reverse side, the number 5 on each trisect segment. The 30 mg tablet has ID number 824 on one side and on the reverse side, the number 10 on each trisect segment.

15 mg tablets
NDC 0087-0822-32     Bottles of 60
NDC 0087-0822-33     Bottles of 180

30 mg tablets
NDC 0087-0824-81     Bottles of 60

Store at 25° C (77° F); excursions permitted between 15° C to 30° C (59° F to 86° F) [see USP controlled room temperature]. Dispense in a tight, light-resistant container (USP).

1. American Psychiatric Association, Ed.: Diagnostic and Statistical Manual of Mental DisordersIII, American Psychiatric Association, May 1980.

Synthroid® is the registered trademark of Abbott Laboratories.

Bristol-Myers Squibb Company
Princeton, NJ 08543 USA

Rev November 2010

BuSpar®
(buspirone HCl, USP)
Patient Instruction Sheet

HOW TO USE:

BuSpar®
(buspirone HCl, USP)

15 mg and 30 mg Tablets
in convenient DIVIDOSE® tablet form

Response to buspirone varies among individuals. Your physician may find it necessary to adjust your dosage to obtain the proper response.

This DIVIDOSE tablet design makes dosage adjustments easy. Each tablet is scored and can be broken accurately to provide any of the following dosages.

To break a DIVIDOSE tablet accurately and easily, hold the tablet between your thumbs and index fingers close to the appropriate tablet score (groove) as shown in the photo. Then, with the tablet score facing you, apply pressure and snap the tablet segments apart (segments breaking incorrectly should not be used).

Bristol-Myers Squibb Company
Princeton, NJ 08543 USA

Rev November 2010

-----------------------------------------
REPRESENTATIVE PACKAGING

100 Tablets
NDC 0087-0818-41
BuSpar®
(buspirone HCl, USP)
EACH TABLET CONTAINS 5 mg OF BUSPIRONE HYDROCHLORIDE, USP.
Rx only
5 mg

Your pharmacist can provide more information about buspirone.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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This medication may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Drinking alcohol may increase certain side effects of BuSpar.

Grapefruit and grapefruit juice may interact with buspirone and lead to unwanted side effects. Discuss the use of grapefruit products with your doctor.

• Take BuSpar consistently; either always with or without food.
• Avoid drinking large amounts of grapefruit juice.
• Do not drive or operate machinery until you know how this medicine affects you.

• Peak concentrations of BuSpar are reached within 40 to 90 minutes of a dose.

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An exclusively breastfed 11-week-old infant whose mother took 10 mg of this drug and 300 mg of venlafaxine daily showed no adverse reactions.

This drug should not be used during breastfeeding unless clinically necessary. Excreted into human milk: Yes Comments: -Limited information indicates maternal doses up to 45 mg daily of this drug produce low levels in milk. -This drug increases serum prolactin; however, the prolactin level in a mother with established lactation may not affect her ability to breastfeed. -There is no information available on the long-term use of this drug during breastfeeding.

Buspirone is an anti-anxiety medicine that affects chemicals in the brain that may be unbalanced in people with anxiety.

Buspirone is used to treat symptoms of anxiety, such as fear, tension, irritability, dizziness, pounding heartbeat, and other physical symptoms.

Buspirone is not an anti-psychotic medication and should not be used in place of medication prescribed by your doctor for mental illness.

Buspirone may also be used for purposes not listed in this medication guide.

Taking this medicine with other drugs that make you sleepy or slow your breathing can worsen these effects. Ask your doctor before taking buspirone with a sleeping pill, narcotic pain medicine, muscle relaxer, or medicine for anxiety, depression, or seizures.

Other drugs may interact with buspirone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.