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BUSPAR

 * Generic Name: buspirone
 * Brand Name: Buspar
 * Drug Class: Antianxiety Agents, Anxiolytics, Nonbenzodiazepines

Medical Editor: John P. Cunha, DO, FACOEP Last updated on RxList: 6/7/2022

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DRUG SUMMARY

WHAT IS BUSPAR?

Buspar (buspirone) is an antianxiety agent prescribed for the treatment of
anxiety. Buspar is available as a generic drug.

WHAT ARE SIDE EFFECTS OF BUSPAR?

Common side effects of Buspar include:

 * dizziness,
 * nausea,
 * headache,
 * nervousness,
 * lightheadedness,
 * drowsiness,
 * feeling tired,
 * blurred vision,
 * restlessness,
 * dry mouth,
 * upset stomach,
 * stuffy nose,
 * sore throat,
 * ringing in the ears,
 * excitement, and
 * sleep problems (insomnia or strange dreams).

DOSAGE FOR BUSPAR

Buspar usual adult starting dose is 10-30mg daily in 2-3 divided doses up to a
maximum of 60mg a day.

WHAT DRUGS, SUBSTANCES, OR SUPPLEMENTS INTERACT WITH BUSPAR?

Common drug interactions of Buspar include monoamine oxidase (MAO) inhibitors
(for example, isocarboxazid [Marplan]), trazodone (Desyrel), warfarin
(Coumadin), erythromycin, itraconazole (Sporanox), nefazodone (Serzone) and
rifampin.

BUSPAR DURING PREGNANCY AND BREASTFEEDING

There are no adequate studies of Buspar in pregnant women and it is not known if
Buspar is secreted in human breast milk. Use during pregnancy is not recommended
unless the potential benefit outweighs the potential unknown risk to the fetus.
It is unknown if Buspar passes into breast milk or if it could harm a nursing
baby. Consult your doctor before breastfeeding.

ADDITIONAL INFORMATION

Our Buspar Side Effects Drug Center provides a comprehensive view of available
drug information on the potential side effects when taking this medication.


FDA DRUG INFORMATION

 * Drug Description
 * Indications
 * Dosage
 * Side Effects & Drug Interactions
 * Warnings & Precautions
 * Overdose & Contraindications
 * Clinical Pharmacology
 * Medication Guide


DESCRIPTION FOR BUSPAR

Buspirone hydrochloride tablets, USP are an antianxiety agent that is not
chemically or pharmacologically related to the benzodiazepines, barbiturates, or
other sedative/anxiolytic drugs.

Buspirone hydrochloride, USP is a white crystalline powder. It is very soluble
in water; freely soluble in methanol and in methylene chloride; sparingly
soluble in ethanol and in acetonitrile; very slightly soluble in ethyl acetate
and practically insoluble in hexanes. Its molecular weight is 422. Chemically,
buspirone hydrochloride is
8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9- dione
monohydrochloride. The molecular formula C21H31N5O2•HCl is represented by the
following structural formula:







Each buspirone hydrochloride tablet intended for oral administration contains 5
mg or 10 mg or 15 mg or 30 mg buspirone hydrochloride (equivalent to 4.6 mg, 9.1
mg, 13.7 mg, and 27.4 mg of buspirone free base, respectively). In addition,
each tablet contains the following inactive ingredients: colloidal silicon
dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose and
sodium starch glycolate. The 5 mg and 10 mg tablets are scored so they can be
bisected. Thus, the 5 mg tablet can also provide 2.5 mg dose, and the 10 mg
tablet can provide a 5 mg dose. The 15 mg and 30 mg tablets are scored so they
can be either bisected or trisected. Thus, a single 15 mg tablet can provide the
following doses: 15 mg (entire tablet), 10 mg (two thirds of a tablet), 7.5 mg
(one half of a tablet), or 5 mg (one third of a tablet). A single 30 mg tablet
can provide the following doses: 30 mg (entire tablet), 20 mg (two thirds of a
tablet), 15 mg (one half of a tablet), or 10 mg (one third of a tablet).




USES FOR BUSPAR

Buspirone hydrochloride tablets are indicated for the management of anxiety
disorders or the short-term relief of the symptoms of anxiety. Anxiety or
tension associated with the stress of everyday life usually does not require
treatment with an anxiolytic.

The efficacy of buspirone hydrochloride tablets have been demonstrated in
controlled clinical trials of outpatients whose diagnosis roughly corresponds to
Generalized Anxiety Disorder (GAD). Many of the patients enrolled in these
studies also had coexisting depressive symptoms and buspirone hydrochloride
tablets relieved anxiety in the presence of these coexisting depressive
symptoms. The patients evaluated in these studies had experienced symptoms for
periods of 1 month to over 1 year prior to the study, with an average symptom
duration of 6 months. Generalized Anxiety Disorder (300.02) is described in the
American Psychiatric Association’s Diagnostic and Statistical Manual, III1 as
follows:

Generalized, persistent anxiety (of at least 1 month continual duration),
manifested by symptoms from three of the four following categories:

MOTOR TENSION

Shakiness, jitteriness, jumpiness, trembling, tension, muscle aches,
fatigability, inability to relax, eyelid twitch, furrowed brow, strained face,
fidgeting, restlessness, easy startle.

AUTONOMIC HYPERACTIVITY

Sweating, heart pounding or racing, cold, clammy hands, dry mouth, dizziness,
lightheadedness, paresthesias (tingling in hands or feet), upset stomach, hot or
cold spells, frequent urination, diarrhea, discomfort in the pit of the stomach,
lump in the throat, flushing, pallor, high resting pulse and respiration rate.

APPREHENSIVE EXPECTATION

Anxiety, worry, fear, rumination, and anticipation of misfortune to self or
others.

VIGILANCE AND SCANNING

Hyperattentiveness resulting in distractibility, difficulty in concentrating,
insomnia, feeling "on edge," irritability, impatience.

The above symptoms would not be due to another mental disorder, such as a
depressive disorder or schizophrenia. However, mild depressive symptoms are
common in GAD.

The effectiveness of buspirone hydrochloride tablets in long-term use, that is,
for more than 3 to 4 weeks, has not been demonstrated in controlled trials.
There is no body of evidence available that systematically addresses the
appropriate duration of treatment for GAD. However, in a study of longterm use,
264 patients were treated with buspirone hydrochloride tablets for 1 year
without ill effect. Therefore, the physician who elects to use buspirone
hydrochloride tablets for extended periods should periodically reassess the
usefulness of the drug for the individual patient.


DOSAGE FOR BUSPAR

The recommended initial dose is 15 mg daily (7.5 mg b.i.d.). To achieve an
optimal therapeutic response, at intervals of 2 to 3 days the dosage may be
increased 5 mg per day, as needed. The maximum daily dosage should not exceed 60
mg per day. In clinical trials allowing dose titration, divided doses of 20 mg
to 30 mg per day were commonly employed.

The bioavailability of buspirone is increased when given with food as compared
to the fasted state (see CLINICAL PHARMACOLOGY). Consequently, patients should
take buspirone in a consistent manner with regard to the timing of dosing;
either always with or always without food.

When buspirone is to be given with a potent inhibitor of CYP3A4, the dosage
recommendations described in the DRUG INTERACTIONS section should be followed.


HOW SUPPLIED

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




SIDE EFFECTS FOR BUSPAR

No information provided.


DRUG INTERACTIONS FOR BUSPAR

PSYCHOTROPIC AGENTS

MAO INHIBITORS

It is recommended that buspirone hydrochloride tablets 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.

INHIBITORS AND INDUCERS OF CYTOCHROME P450 3A4 (CYP3A4)

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 (e.g., 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 (e.g., 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 (e.g., 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.

OTHER DRUGS

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.

PROTEIN BINDING

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.

DRUG ABUSE AND DEPENDENCE

CONTROLLED SUBSTANCE CLASS

Buspirone hydrochloride is not a controlled substance.

PHYSICAL AND PSYCHOLOGICAL DEPENDENCE

In human and animal studies, buspirone has shown no potential for abuse or
diversion and there is no evidence that it causes tolerance, or either physical
or psychological dependence. Human volunteers with a history of recreational
drug or alcohol usage were studied in two doubleblind clinical investigations.
None of the subjects were able to distinguish between buspirone hydrochloride
tablets and placebo. By contrast, subjects showed a statistically significant
preference for methaqualone and diazepam. Studies in monkeys, mice, and rats
have indicated that buspirone lacks potential for abuse. Following chronic
administration in the rat, abrupt withdrawal of buspirone did not result in the
loss of body weight commonly observed with substances that cause physical
dependency.

Although there is no direct evidence that buspirone hydrochloride tablets causes
physical dependence or drug-seeking behavior, it is difficult to predict from
experiments the extent to which a CNS-active drug will be misused, diverted,
and/or abused once marketed. Consequently, physicians should carefully evaluate
patients for a history of drug abuse and follow such patients closely, observing
them for signs of buspirone hydrochloride tablets misuse or abuse (e.g.,
development of tolerance, incrementation of dose, drug-seeking behavior).

CONTROLLED SUBSTANCE CLASS

Buspirone hydrochloride is not a controlled substance.

PHYSICAL AND PSYCHOLOGICAL DEPENDENCE

In human and animal studies, buspirone has shown no potential for abuse or
diversion and there is no evidence that it causes tolerance, or either physical
or psychological dependence. Human volunteers with a history of recreational
drug or alcohol usage were studied in two doubleblind clinical investigations.
None of the subjects were able to distinguish between buspirone hydrochloride
tablets and placebo. By contrast, subjects showed a statistically significant
preference for methaqualone and diazepam. Studies in monkeys, mice, and rats
have indicated that buspirone lacks potential for abuse. Following chronic
administration in the rat, abrupt withdrawal of buspirone did not result in the
loss of body weight commonly observed with substances that cause physical
dependency.

Although there is no direct evidence that buspirone hydrochloride tablets causes
physical dependence or drug-seeking behavior, it is difficult to predict from
experiments the extent to which a CNS-active drug will be misused, diverted,
and/or abused once marketed. Consequently, physicians should carefully evaluate
patients for a history of drug abuse and follow such patients closely, observing
them for signs of buspirone hydrochloride tablets misuse or abuse (e.g.,
development of tolerance, incrementation of dose, drug-seeking behavior).


WARNINGS FOR BUSPAR

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.


PRECAUTIONS FOR BUSPAR

GENERAL

INTERFERENCE WITH COGNITIVE AND MOTOR PERFORMANCE

Studies indicate that buspirone hydrochloride tablets are 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 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.

POTENTIAL FOR WITHDRAWAL REACTIONS IN SEDATIVE/HYPNOTIC/ANXIOLYTIC
DRUG-DEPENDENT PATIENTS

Because buspirone hydrochloride tablets do 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 buspirone hydrochloride tablets, 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.

POSSIBLE CONCERNS RELATED TO BUSPIRONE’S BINDING TO DOPAMINE RECEPTORS

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 (e.g., dystonia, pseudoparkinsonism,
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 (i.e., represent akathisia). See ADVERSE REACTIONS:
Postmarketing Experience.

INFORMATION FOR PATIENTS

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

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 buspirone hydrochloride tablets.

Inform your physician if you are pregnant, or if you are planning to become
pregnant, or if you become pregnant while you are taking buspirone hydrochloride
tablets.

Inform your physician if you are breastfeeding an infant.

Until you experience how this medication affects you, do not drive a car or
operate potentially dangerous machinery.

You should take buspirone hydrochloride consistently, either always with or
always without food.

During your treatment with buspirone hydrochloride tablets, avoid drinking large
amounts of grapefruit juice.

LABORATORY TESTS

There are no specific laboratory tests recommended.

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 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.
Buspirone hydrochloride tablets 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 to 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 longterm 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 buspirone hydrochloride tablets to patients
with severe hepatic or renal impairment cannot be recommended (see CLINICAL
PHARMACOLOGY).


OVERDOSE INFORMATION FOR BUSPAR

No information provided.


CONTRAINDICATIONS FOR BUSPAR

Buspirone hydrochloride tablets are contraindicated in patients hypersensitive
to buspirone hydrochloride.


CLINICAL PHARMACOLOGY FOR BUSPAR

The mechanism of action of buspirone is unknown. Buspirone differs from typical
benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle
relaxant effects. It also lacks the prominent sedative effect that is associated
with more typical anxiolytics. In vitro preclinical studies have shown that
buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no
significant affinity for benzodiazepine receptors and does not affect GABA
binding in vitro or in vivo when tested in preclinical models.

Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do
suggest that buspirone may have indirect effects on other neurotransmitter
systems.

Buspirone hydrochloride is rapidly absorbed in man and undergoes extensive
first-pass metabolism. In a radiolabeled study, unchanged buspirone in the
plasma accounted for only about 1% of the radioactivity in the plasma. Following
oral administration, plasma concentrations of unchanged buspirone are very low
and variable between subjects. Peak plasma levels of 1 ng/mL to 6 ng/mL have
been observed 40 to 90 minutes after single oral doses of 20 mg. The single-dose
bioavailability of unchanged buspirone when taken as a tablet is on the average
about 90% of an equivalent dose of solution, but there is large variability.

The effects of food upon the bioavailability of buspirone hydrochloride tablets
have been studied in eight subjects. They were given a 20 mg dose with and
without food; the area under the plasma concentration-time curve (AUC) and peak
plasma concentration (Cmax) of unchanged buspirone increased by 84% and 116%,
respectively, but the total amount of buspirone immunoreactive material did not
change. This suggests that food may decrease the extent of presystemic clearance
of buspirone (see DOSAGE AND ADMINISTRATION).

A multiple-dose study conducted in 15 subjects suggests that buspirone has
nonlinear pharmacokinetics. Thus, dose increases and repeated dosing may lead to
somewhat higher blood levels of unchanged buspirone than would be predicted from
results of single-dose studies.

An in vitro protein binding study indicated that approximately 86% of buspirone
is bound to plasma proteins. It was also observed that aspirin increased the
plasma levels of free buspirone by 23%, while flurazepam decreased the plasma
levels of free buspirone by 20%. However, it is not known whether these drugs
cause similar effects on plasma levels of free buspirone in vivo, or whether
such changes, if they do occur, cause clinically significant differences in
treatment outcome. An in vitro study indicated that buspirone did not displace
highly protein-bound drugs such as phenytoin, warfarin, and propranolol from
plasma protein, and that buspirone may displace digoxin.

Buspirone is metabolized primarily by oxidation, which in vitro has been shown
to be mediated by cytochrome P450 3A4 (CYP3A4) (see DRUG INTERACTIONS). Several
hydroxylated derivatives and a pharmacologically active metabolite,
1-pyrimidinylpiperazine (1-PP), are produced. In animal models predictive of
anxiolytic potential, 1-PP has about one quarter of the activity of buspirone,
but is present in up to 20-fold greater amounts. However, this is probably not
important in humans: blood samples from humans chronically exposed to buspirone
hydrochloride do not exhibit high levels of 1- PP; mean values are approximately
3 ng/mL and the highest human blood level recorded among 108 chronically dosed
patients was 17 ng/mL, less than 1/200th of 1-PP levels found in animals given
large doses of buspirone without signs of toxicity.

In a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was
excreted in the urine within 24 hours, primarily as metabolites; fecal excretion
accounted for 18% to 38% of the dose. The average elimination half-life of
unchanged buspirone after single doses of 10 mg to 40 mg is about 2 to 3 hours.

SPECIAL POPULATIONS

AGE AND GENDER EFFECTS

After single or multiple doses in adults, no significant differences in
buspirone pharmacokinetics (AUC and Cmax) were observed between elderly and
younger subjects or between men and women.

HEPATIC IMPAIRMENT

After multiple-dose administration of buspirone to patients with hepatic
impairment, steady-state AUC of buspirone increased 13-fold compared with
healthy subjects (see PRECAUTIONS).

RENAL IMPAIRMENT

After multiple-dose administration of buspirone to renally impaired (Clcr = 10
to 70 mL/min/1.73 m2) patients, steady-state AUC of buspirone increased 4-fold
compared with healthy (Clcr ≥ 80 mL/min/1.73 m2) subjects (see PRECAUTIONS).

RACE EFFECTS

The effects of race on the pharmacokinetics of buspirone have not been studied.


PATIENT INFORMATION FOR BUSPAR

Buspirone Hydrochloride
Tablets, USP
For 15 mg and 30 mg tablets

HOW TO USE

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

Each tablet is scored and can be broken accurately.

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

Call your doctor for medical advice about side effects. You may report side
effects to FDA at 1-800- FDA-1088.


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