Country: মার্কিন যুক্তরাষ্ট্র
ভাষা: ইংরেজি
সূত্র: NLM (National Library of Medicine)
METAXALONE (UNII: 1NMA9J598Y) (METAXALONE - UNII:1NMA9J598Y)
Blenheim Pharmacal, Inc.
METAXALONE
METAXALONE 800 mg
ORAL
PRESCRIPTION DRUG
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.
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
New Drug Application
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 সম্পূর্ণ নথি পড়ুন