Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1287
| Predicate | Object |
|---|---|
| rdf:type | |
| rdfs:label |
BUSPAR (Tablet)
|
| dailymed-instance:dosage |
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 PRECAUTIONS: Drug Interactions section
should be followed.
|
| dailymed-instance:descripti... |
BuSpar (buspirone hydrochloride tablets,
USP) is an antianxiety agent that is not chemically or pharmacologically related
to the benzodiazepines, barbiturates, or other sedative/anxiolytic drugs. Buspirone hydrochloride is a white crystalline, water soluble compound
with a molecular weight of 422.0. Chemically, buspirone hydrochloride is 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
monohydrochloride. The empirical formula CHNO���HCl is represented by the following structural formula: BuSpar is supplied as tablets for oral administration containing
5 mg, 10 mg, 15 mg, or 30 mg of buspirone hydrochloride, USP (equivalent to
4.6 mg, 9.1 mg, 13.7 mg, and 27.4 mg of buspirone free base, respectively).
The 5 mg and 10 mg tablets are scored so they can be bisected. Thus, the
5 mg tablet can also provide a 2.5 mg dose, and the 10 mg tabletcan provide
a 5 mg dose. The 15 mg and 30 mg tablets are provided in the DIVIDOSE tablet
design. These 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). BuSpar
Tablets contain the following inactive ingredients: colloidal silicon dioxide,
lactose, magnesium stearate, microcrystalline cellulose, and sodium starch
glycolate. The 30 mg tablet also contains iron oxide.
|
| dailymed-instance:clinicalP... |
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-HT)
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 D-dopamine
receptors. Some studies do suggest that buspirone may have indirect effects
on other neurotransmitter systems. BuSpar 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 whentaken 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 BuSpar 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
(C) 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).
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
BuSpar (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 usingC-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.<br/>Special Populations:<br/>Age and Gender Effects: After single or multiple doses in adults, no significant differences
in buspirone pharmacokinetics (AUC and C) were observed
between elderly and younger subjects or between men and women.<br/>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 .<br/>Renal Impairment: After multiple-dose administration of buspirone to renally impaired
(Cl= 10���70 mL/min/1.73 m)
patients, steady-state AUC of buspirone increased 4-fold compared with healthy
(Cl���80 mL/min/1.73 m)
subjects .<br/>Race Effects: The effects of race on the pharmacokinetics of buspirone have not
been studied.
|
| dailymed-instance:activeIng... | |
| dailymed-instance:contraind... |
BuSpar is contraindicated in patients hypersensitive to buspirone
hydrochloride.
|
| dailymed-instance:supply |
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 tabletsNDC 0087-0818-41 Bottles of 100 10 mg tabletsNDC 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 trisectsegment. 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 tabletsNDC 0087-0822-32 Bottles of 60NDC 0087-0822-33 Bottles
of 180 30 mg tabletsNDC 0087-0824-81 Bottles of 60 US Patent No. 5,015,646 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).
|
| dailymed-instance:activeMoi... | |
| dailymed-instance:inactiveI... | |
| dailymed-instance:overdosag... |
Signs and Symptoms: In clinical pharmacology trials, doses as high as 375 mg/day were
administered to healthy male volunteers. As this dose was approached, the
following symptoms were observed: nausea, vomiting, dizziness, drowsiness,
miosis, and gastric distress. A few cases of overdosage have been reported,
with complete recovery as the usual outcome. No deaths have been reported
following overdosage with BuSpar alone. Rare cases of intentional overdosage
with a fatal outcome were invariably associated with ingestion of multiple
drugs and/or alcohol, and a causal relationship to buspirone could not be
determined. Toxicology studies of buspirone yielded the following LDvalues:
mice, 655 mg/kg; rats, 196 mg/kg; dogs, 586 mg/kg; and monkeys, 356 mg/kg.
These dosages are 160 to 550 times the recommended human daily dose.<br/>Recommended Overdose Treatment: General symptomatic and supportive measures should be used along
with immediate gastric lavage. Respiration, pulse, and blood pressure should
be monitored as in all cases of drug overdosage. No specific antidote is known
to buspirone, and dialyzability of buspirone has not been determined.
|
| dailymed-instance:genericMe... |
BUSPIRONE HYDROCHLORIDE
|
| dailymed-instance:fullName |
BUSPAR (Tablet)
|
| dailymed-instance:indicatio... |
BuSpar is 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 BuSpar has 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 BuSpar 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, IIIas follows: Generalized, persistent anxiety (of at least 1 month continual
duration), manifested by symptoms from three of the four following categories: 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 BuSpar 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 long-term use, 264 patients
were treated with BuSpar for 1 year without ill effect. Therefore, the physician
who elects to use BuSpar for extended periods should periodically reassess
the usefulness of the drug for the individual patient.
|
| dailymed-instance:represent... | |
| dailymed-instance:routeOfAd... | |
| dailymed-instance:name |
BUSPAR
|