ESTAZOLAM tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ESTAZOLAM (UNII: 36S3EQV54C) (ESTAZOLAM - UNII:36S3EQV54C)

Available from:

Rebel Distributors Corp

INN (International Name):

ESTAZOLAM

Composition:

ESTAZOLAM 2 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Estazolam tablets are indicated for the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. Both out-patient studies and a sleep laboratory study have shown that estazolam administered at bedtime improved sleep induction and sleep maintenance (see CLINICAL PHARMACOLOGY ). Because insomnia is often transient and intermittent, the prolonged administration of estazolam is generally neither necessary nor recommended. Since insomnia may be a symptom of several other disorders, the possibility that the complaint may be related to a condition for which there is a more specific treatment should be considered. There is evidence to support the ability of estazolam to enhance the duration and quality of sleep for intervals up to 12 weeks (see CLINICAL PHARMACOLOGY ). Benzodiazepines may cause fetal damage when administered during pregnancy. An increased risk of congenital malformations associated with the use of diazepam and chl

Product summary:

Estazolam Tablets, 2 mg are dark pink, scored, diamond shaped compressed tablets imprinted with WATSON on one side of the tablet and on the other side with 745 on the left side of the score and 2 on the right side of the score, supplied in bottles of 30. Store at 20°-25°C (68°-77°F). [See USP controlled room temperature.] Dispense in a tight, light-resistant container as defined in the USP. Manufactured By: Watson Laboratories, Inc. Corona, CA 92880 USA Distributed By: Watson Pharma, Inc. Corona, CA 92880 USA Repackaged by: Rebel Distributors Corp Thousand Oaks, CA 91320

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ESTAZOLAM- ESTAZOLAM TABLET
REBEL DISTRIBUTORS CORP
----------
ESTAZOLAM TABLETS CIV
REVISED: SEPTEMBER 2008
RX ONLY
14444-2
DESCRIPTION
Estazolam, a triazolobenzodiazepine derivative, is an oral hypnotic
agent. Estazolam occurs as a fine,
white, odorless powder that is soluble in alcohol and practically
insoluble in water. The chemical name
for estazolam is
8-chloro-6-phenyl-4_H_-_s_-triazolo[4,3-α][1,4]benzodiazepine. The
molecular formula is
C
H CIN and its molecular weight is 294.75. The structural formula is
represented as follows:
Each tablet, for oral administration, contains 1 mg or 2 mg estazolam.
In addition, each tablet contains the
following inactive ingredients: docusate sodium, lactose monohydrate,
magnesium stearate,
microcrystalline cellulose, sodium benzoate, sodium starch glycolate
and stearic acid. The 2 mg tablets
also contain FD&C Red #40 aluminum lake.
CLINICAL PHARMACOLOGY
PHARMACOKINETICS
_Absorption_
Estazolam tablets have been found to be equivalent in absorption to an
orally administered solution of
estazolam. In healthy subjects who received up to three times the
recommended dose of estazolam, peak
estazolam plasma concentrations occurred within two hours after dosing
(range 0.5 to 6 hours) and were
proportional to the administered dose, suggesting linear
pharmacokinetics over the dosage range tested.
_Distribution_
Independent of concentration, estazolam in plasma is 93% protein
bound.
_Metabolism_
Estazolam is extensively metabolized. Only two metabolites
(1-oxo-estazolam and 4-hydroxy-
estazolam) were detected in human plasma up to 18 hours.
The pharmacologic activity of estazolam is primarily from the parent
drug. The elimination of the parent
16
11
4
drug takes place via hepatic metabolism of estazolam to hydroxylated
and other metabolites that are
eliminated largely in the urine both free and conjugated. In humans,
greater than 70% of a single dose of
estazolam was recovered in the urine as metabolites. Less than 5% of a
2 mg dose of estazolam was
excreted unchanged in the urine