SKELAXIN- metaxalone tablet

Country: Amerika Syarikat

Bahasa: Inggeris

Sumber: NLM (National Library of Medicine)

Bahan aktif:

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

Boleh didapati daripada:

Blenheim Pharmacal, Inc.

INN (Nama Antarabangsa):

METAXALONE

Komposisi:

METAXALONE 800 mg

Laluan pentadbiran:

ORAL

Jenis preskripsi:

PRESCRIPTION DRUG

Tanda-tanda terapeutik:

SKELAXIN (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.

Ringkasan produk:

SKELAXIN (metaxalone) is available as an 800 mg oval, scored pink tablet inscribed with 8667 on the scored side and "S" on the other. Available in bottles of 100 ( NDC 60793-136-01) and in bottles of 500 ( NDC 60793-136-05). Store at Controlled Room Temperature, between 15°C and 30°C (59°F and 86°F). Rx Only Prescribing Information as of April 2008. Distributed by: King Pharmaceuticals, Inc., Bristol, TN 37620 Manufactured by: Corepharma LLC, Middlesex, NJ 08846

Status kebenaran:

New Drug Application

Ciri produk

SKELAXIN- METAXALONE TABLET
BLENHEIM PHARMACAL, INC.
----------
SKELAXIN
(METAXALONE) TABLETS
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 SKELAXIN 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 SKELAXIN 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) METAXALONE PHARMACOKINETIC PARAMETERS
DOSE (mg) C
(ng/mL) T
(h) AUC
(ng•h/mL) T
(h)
CL/F (L/h)
400
983 (53)
3.3 (35)
7479 (51)
9.0 (53) 68 (50)
800
1816 (43)
3.0 (39)
15044 (46)
8.0 (58) 66 (51)
Subjects received 1x400 mg tablet under fasted conditions (N=42)
Subjects received 2x400 mg tablets under fasted conditions (N=59)
_DISTRIBUTION, METABOLISM, AND EXCRETION_
Although plasma protein binding and absolute bioavailability of
metaxalone are not known, the apparent
volume of distribution (V/F ~ 800 L) and lipophilicity (log P = 2.42)
of metaxalone suggest that the
drug is extensively distributed in the tissues. Metaxalone is
metabolized by the liver and excreted in the
urine as unidentified metabolites. Hepatic Cytochrome P450 enzym