METAXALONE tablet

País: Estados Unidos

Língua: inglês

Origem: NLM (National Library of Medicine)

Ingredientes ativos:

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

Disponível em:

DIRECT RX

Via de administração:

ORAL

Tipo de prescrição:

PRESCRIPTION DRUG

Indicações terapêuticas:

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

Resumo do produto:

Metaxalone tablets are available as an 800 mg oval, convex, pink tablet with one side debossed "M" and other side debossed "58/59".                     Bottles of 100            NDC 64720-321-10                     Bottles of 500            NDC 64720-321-50 Store at Controlled Room Temperature, between 15°C and 30°C (59°F and 86°F).

Status de autorização:

New Drug Application

Características técnicas

METAXALONE- METAXALONE TABLET
DIRECT RX
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METAXALONE
DESCRIPTION SECTION
Metaxalone tablets are available as an 800 mg oval, convex pink
tablet.
Chemically, metaxalone is 5-[(3,5- dimethylphenoxy)
methyl]-2-oxazolidinone. The empirical formula is
C12H15NO3, 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
calcium alginate, B-Rose Liquid, corn starch and magnesium stearate
CLINICAL PHARMACOLOGY SECTION
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 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
(Cmax) 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)
Cmax
(ng/mL)
Tmax
(h)
AUC∞
(ng•h/mL)
t½(h)
CL/F
(L/h)
4001
983