METAXALONE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

METAXALONE (UNII: 1NMA9J598Y) (METAXALONE - UNII:1NMA9J598Y)

Available from:

Proficient Rx LP

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Metaxalone tablets are indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its sedative properties. Metaxalone does not directly relax tense skeletal muscles in man. Known hypersensitivity to any components of this product. Known tendency to drug induced, hemolytic, or other anemias. Significantly impaired renal or hepatic function.

Product summary:

Metaxalone tablets, USP are available as an 800 mg capsule-shaped, scored white to off-white tablet, inscribed with “31 90 ” on the scored side and “WPI ” on the other side. Available in bottles of 20 (NDC  71205-326-20), 30 (NDC  71205-326-30), 60 (NDC  71205-326-60) and bottles of 90 (NDC 71205-326-90). Metaxalone tablets, USP 800 mg has functional scoring. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Manufactured by: Actavis Laboratories FL, Inc. Fort Lauderdale, FL 33314 USA Distributed by: Actavis Pharma, Inc. Parsippany, NJ 07054 USA Repackaged by: Proficient Rx LP Thousand Oaks, CA 91320 Revised: April 2017

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

METAXALONE- METAXALONE TABLET
PROFICIENT RX LP
----------
METAXALONE TABLETS
METAXALONE TABLETS, USP
RX ONLY
DESCRIPTION
Metaxalone tablets, USP are available as an 800 mg capsule-shaped,
scored white to off-
white tablet.
Chemically, metaxalone is 5-[(3,5- dimethylphenoxy)
methyl]-2-oxazolidinone. The
empirical formula is C
H
NO , which corresponds to a molecular weight of 221.25.
The structural formula is:
Metaxalone is a white to almost white, odorless crystalline powder
freely soluble in
chloroform, soluble in methanol and in 96% ethanol, but practically
insoluble in ether or
water.
Each tablet contains 800 mg metaxalone and the following inactive
ingredients: alginic
acid, ammonium alginate, calcium alginate, corn starch, magnesium
stearate and
pregelatinized starch (starch 1500 partially pregelatinized maize
starch).
USP Dissolution Test Pending
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
The mechanism of action of metaxalone in humans has not been
established, but may
be due to general central nervous system depression. Metaxalone has no
direct action
on the contractile mechanism of striated muscle, the motor end plate,
or the nerve fiber.
PHARMACOKINETICS
The pharmacokinetics of metaxalone have been evaluated in healthy
adult volunteers
after single dose administration of metaxalone tablets under fasted
and fed conditions at
12
15
3
after single dose administration of metaxalone tablets under fasted
and fed conditions at
doses ranging from 400 mg to 800 mg.
_ABSORPTION_
Peak plasma concentrations of metaxalone occur approximately 3 hours
after a 400 mg
oral dose under fasted conditions. Thereafter, metaxalone
concentrations decline log-
linearly with a terminal half-life of 9.0 ± 4.8 hours. Doubling the
dose of metaxalone
tablets from 400 mg to 800 mg results in a roughly proportional
increase in metaxalone
exposure as indicated by peak plasma concentrations (C
) and area under the curve
(AUC). Dose proportionality at doses above 800 mg has not been
studied. The absolute
bioavailability of metaxalone is no