ZALEPLON capsule

Country: Сједињене Америчке Државе

Језик: Енглески

Извор: NLM (National Library of Medicine)

Активни састојак:

ZALEPLON (UNII: S62U433RMH) (ZALEPLON - UNII:S62U433RMH)

Доступно од:

St Marys Medical Park Pharmacy

INN (Међународно име):

ZALEPLON

Састав:

ZALEPLON 10 mg

Тип рецептора:

PRESCRIPTION DRUG

Статус ауторизације:

Abbreviated New Drug Application

Карактеристике производа

ZALEPLON - ZALEPLON CAPSULE
ST MARYS MEDICAL PARK PHARMACY
----------
ZALEPLON - ZALEPLONE CAPSULE
CIV
RX ONLY
DESCRIPTION
Zaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine
class. The chemical name of
zaleplon is
N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide.
Its empirical
formula is C
H N O, and its molecular weight is 305.34. The structural formula is
shown below.
Zaleplon is a white to off-white powder that is practically insoluble
in water and sparingly soluble in
alcohol or propylene glycol. Its partition coefficient in
octanol/water is constant (log PC = 1.23) over
the pH range of 1 to 7.
Zaleplon capsules contain zaleplon as the active ingredient. Inactive
ingredients consist of
microcrystalline cellulose, pregelatinized starch, colloidal silicon
dioxide, sodium lauryl sulfate,
magnesium stearate, lactose, gelatin, titanium dioxide, FD&C blue #1,
FD&C red #40 and black iron
oxide. Zaleplon 5mg capsules also contain FD&C yellow #5.
CLINICAL PHARMACOLOGY
PHARMACODYNAMICS AND MECHANISM OF ACTION
While Zaleplon is a hypnotic agent with a chemical structure unrelated
to benzodiazepines, barbiturates,
or other drugs with known hypnotic properties, it interacts with the
gamma-aminobutyric acid-
benzodiazepine (GABA-BZ) receptor complex. Subunit modulation of the
GABA-BZ receptor chloride
channel macromolecular complex is hypothesized to be responsible for
some of the pharmacological
properties of benzodiazepines, which include sedative, anxiolytic,
muscle relaxant, and anticonvulsive
effects in animal models.
Other nonclinical studies have also shown that zaleplon binds
selectively to the brain omega-1 receptor
situated on the alpha subunit of the GABA /chloride ion channel
receptor complex and potentiates t-
butyl-bicyclophosphorothionate (TBPS) binding. Studies of binding of
zaleplon to recombinant GABA
receptors (α β γ [omega-1] and α β1γ [omega-2]) have shown that
zaleplon has a low affinity for
these receptors, with preferential binding to the omega-1 receptor.