ESTAZOLAM tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Estazolam (UNII: 36S3EQV54C) (Estazolam - UNII:36S3EQV54C)

Available from:

Mayne Pharma

INN (International Name):

Estazolam

Composition:

Estazolam 1 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Estazolam is indicated for the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. Both outpatient 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 chlordiazepox

Product summary:

Estazolam tablets 1 mg are available as white, oval, biconvex, double-scored tablets debossed "93"–"129" on one side. Packaged in bottles of 100 (NDC 51862-069-01). Estazolam tablets 2 mg are available as pale orange, oval, biconvex, single-scored tablets debossed "93"–"130" on the scored side. Packaged in bottles of 100 (NDC 51862-070-01). Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required).

Authorization status:

Abbreviated New Drug Application

Patient Information leaflet

Mayne Pharma
----------
MEDICATION GUIDE
ESTAZOLAM (ES-TAZE-OH-LAM) TABLETS, C-IV
This Medication Guide has been approved by the U.S. Food and Drug
Administration
Issued: September/2016
What is the most important information I should know about estazolam?
•
Estazolam is a benzodiazepine medicine. Taking benzodiazepines with
opioid medicines, alcohol,
or other central nervous system depressants (including street drugs)
can cause severe drowsiness,
breathing problems (respiratory depression), coma and death.
•
After taking estazolam, you may get up out of bed while not being
fully awake and do an activity
that you do not know you are doing. The next morning, you may not
remember that you did
anything during the night. You have a higher chance for doing these
activities if you drink alcohol
or take other medicines that make you sleepy with estazolam. Reported
activities include:
•
driving a car ("sleep-driving")
•
making and eating food
•
talking on the phone
•
having sex
•
sleep-walking
Call your healthcare provider right away if you find out that you have
done any of the above
activities after taking estazolam.
•
Do not take estazolam unless you are able to stay in bed a full night
(7 to 8 hours) before you
must be active again.
•
Do not take more estazolam than prescribed.
What is estazolam?
•
Estazolam is a prescription medicine used short-term to treat certain
types of insomnia including
difficulty falling asleep, waking up often during the night, or waking
up early in the morning.
•
Estazolam is a federal controlled substance (C-IV) because it can be
abused or lead to
dependence. Keep estazolam in a safe place to prevent misuse and
abuse. Selling or giving away
estazolam may harm others, and is against the law. Tell your
healthcare provider if you have ever
abused or been dependent on alcohol, prescription medicines or street
drugs.
•
It is not known if estazolam is safe and effective in children.
•
It is not known if estazolam is safe and effective when used to treat
insomnia for lon

Summary of Product characteristics

ESTAZOLAM- ESTAZOLAM TABLET
MAYNE PHARMA
----------
ESTAZOLAM TABLETS CIV
WARNING: RISKS FROM CONCOMITANT USE WITH OPIOIDS
Concomitant use of benzodiazepines and opioids may result in profound
sedation, respiratory
depression, coma, and death _[_see _Warnings, Drug Interactions]_.
Reserve concomitant prescribing of these drugs for use in patients for
whom alternative
treatment options are inadequate.
Limit dosages and durations to the minimum required.
Follow patients for signs and symptoms of respiratory depression and
sedation.
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
structural formula is
represented as follows:
C
H ClN
Each tablet, for oral administration, contains either 1 mg or 2 mg of
estazolam. In addition, each tablet
contains the following inactive ingredients: 1 mg tablets - corn
starch, lactose monohydrate,
pregelatinized starch, and stearic acid; 2 mg tablets - corn starch,
FD&C Red #40 aluminum lake, FD&C
Yellow #6 aluminum lake, lactose monohydrate, pregelatinized starch,
and stearic acid.
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 6.0 hours) and
were proportional to the administered dose, suggesting linear
pharmacokinetics over the dosage range
tested.
_Distribution_
16
11
4
_Distribution_
Independent of concentration, estazolam in plasma is 93% protein
bound.
_Metabolism_
Estazolam is extensively metabolized. Only two metabolites
(1-oxo-estazolam & 4-hydroxy-estazolam)
were detected in human plasma up to 18 hrs.
The pharmacologic activity of estaz