METAXALONE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

AvPAK

INN (International Name):

METAXALONE

Composition:

METAXALONE 800 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Metaxalone is 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 is available as an 800 mg , light pink to pink, capsule shaped, scored uncoated  tablet with debossing ‘AN’ on the left side of the scoring and ‘553’ on the right side of the scoring. Other side of the tablet is plain. They are available as follows: NDC  50268-530-15          10 tablets per card, 5 cards per carton Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Manufactured for:                  AvKARE, Inc. Pulaski, TN 38478 Mfg. Rev. 08-2014-00 AV 01/15 (P) AvPAK

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

METAXALONE- METAXALONE TABLET
AVPAK
----------
METAXALONE TABLETS
DESCRIPTION
Metaxalone is available as an 800 mg, light pink to pink, capsule
shaped, scored
uncoated 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: calcium
carbonate, FD&C Red #40, hypromellose, lactose monohydrate,
microcrystalline
cellulose, povidone, silicone dioxide, sodium starch glycolate and
sodium stearyl
fumarate.
CLINICAL PHARMACOLOGY
12
15
3
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 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 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 not known.
The single-dose pharmacokinetic parameters of metaxalone in two groups
of healthy
volunteers are shown in Table 1.
TABLE 1: MEAN (%CV) ME