BUSPIRONE HYDROCHLORIDE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

BUSPIRONE HYDROCHLORIDE (UNII: 207LT9J9OC) (BUSPIRONE - UNII:TK65WKS8HL)

Available from:

Major Pharmaceuticals

INN (International Name):

BUSPIRONE HYDROCHLORIDE

Composition:

BUSPIRONE HYDROCHLORIDE 15 mg

Prescription type:

PRESCRIPTION DRUG

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BUSPIRONE HYDROCHLORIDE- BUSPIRONE HYDROCHLORIDE TABLET
MAJOR PHARMACEUTICALS
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BUSPIRONE HYDROCHLORIDE TABLETS, USP
5200
RX ONLY
DESCRIPTION
Buspirone hydrochloride 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. Chemically, buspirone
hydrochloride is
_N_-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,1-cyclopentanediacetamide
monohydrochloride, which can be represented by the following
structural formula:
C
H N O •HCl MW 421.96
Each tablet, for oral administration, contains 15 mg of buspirone
hydrochloride, USP (equivalent to 13.7
mg of buspirone free base). The 15 mg tablets are scored such that
they may be bisected. Thus, a single
15 mg tablet can provide the following doses: 15 mg (entire tablet),
10 mg (two-thirds of a tablet), 5 mg
(one-third of a tablet). Buspirone hydrochloride tablets, USP contain
the following inactive ingredients:
colloidal silicon dioxide, lactose monohydrate, magnesium stearate,
microcrystalline cellulose, and
sodium starch glycolate.
CLINICAL PHARMACOLOGY
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.
Buspirone is rapidly absorbed in man and undergoes extensive
first-pass metabolism. In a radiolabeled
study, unchanged buspirone in the plasma accounted for on