Страна: САЩ
Език: английски
Източник: NLM (National Library of Medicine)
METAXALONE (UNII: 1NMA9J598Y) (METAXALONE - UNII:1NMA9J598Y)
Lake Erie Medical DBA Quality Care Products LLC
METAXALONE
METAXALONE 800 mg
PRESCRIPTION DRUG
New Drug Application
SKELAXIN- METAXALONE TABLET LAKE ERIE MEDICAL DBA QUALITY CARE PRODUCTS LLC ---------- SKELAXIN (METAXALONE) TABLETS DESCRIPTION SKELAXIN (metaxalone) is available as an 800 mg oval, scored pink 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 calcium alginate, B-Rose Liquid, corn starch, and magnesium stearate. 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 Прочетете целия документ