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match">&#9664;</a><button id="jr-fip-matches">no matches yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">&#9654;</a></nav></nav></div><div id="jr-epub-interstitial" class="hidden"></div><div id="jr-content"><article data-type="main"><div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><div class="fm-sec"><h1 id="_NBK548838_"><span class="title" itemprop="name">Metaxalone</span></h1><p class="fm-aai"><a href="#_NBK548838_pubdet_">Publication Details</a></p></div></div><div class="body-content whole_rhythm" itemprop="text"><div id="Metaxalone.OVERVIEW"><h2 id="_Metaxalone_OVERVIEW_">OVERVIEW</h2><div id="Metaxalone.Introduction"><h3>Introduction</h3><p>Metaxalone is a centrally acting skeletal muscle relaxant that has been in use for more than 40 years. Metaxalone has not been associated with serum aminotransferase elevations during therapy or with clinically apparent hepatic injury.</p></div><div id="Metaxalone.Background"><h3>Background</h3><p>Metaxalone (me tax' a lone) acts centrally as a skeletal muscle relaxant, but its efficacy and precise mechanism of action are not well documented. Metaxalone was approved for use in the United States in 1962 and has been a widely used muscle relaxant, but its use recently has declined. Current indications include the treatment of pain from acute musculoskeletal conditions and muscle spasms. The recommended dosage is 800 mg orally three to four times daily. Metaxalone is available by prescription only in 400 and 800 mg tablets in generic forms as well as under the commercial name Skelaxin. Sparse data are available regarding metaxalone safety. Side effects are not common, but can include drowsiness, dizziness, headache, nausea, and dry mouth. When combined with other serotonergic medications (such as serotonin reuptake inhibitors, tricyclic antidepressants, triptans, opiates and others), metaxalone can cause acute serotonin syndrome marked by agitation, confusion, hallucinations, tachycardia, hyperthermia, incoordination, neuromuscular rigidity, nausea and abdominal pain.</p></div><div id="Metaxalone.Hepatotoxicity"><h3>Hepatotoxicity</h3><p>According to the product brochure, metaxalone may cause jaundice, although there are no specific case reports of hepatotoxicity from metaxalone in the literature and no prospective trials with routine monitoring of aminotransferase levels. Given its long history, metaxalone appears to be without significant hepatotoxicity.</p><p>Likelihood score: E (Unlikely cause of clinically apparent liver injury).</p><p>Drug Class: <a href="/books/n/livertox/MuscleRelaxants/?report=reader">Muscle Relaxants</a></p></div></div><div id="Metaxalone.PRODUCT_INFORMATION"><h2 id="_Metaxalone_PRODUCT_INFORMATION_">PRODUCT INFORMATION</h2><p>
<b>REPRESENTATIVE TRADE NAMES</b>
</p><p>Metaxalone &#x02013; Generic, Skelaxin&#x000ae;</p><p>
<b>DRUG CLASS</b>
</p><p>Muscle Relaxants</p><p>
<a href="https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&#x00026;query=metaxalone" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">COMPLETE LABELING</a>
</p><p>Product Labeling at DailyMed, National Library of Medicine, NIH</p></div><div id="Metaxalone.CHEMICAL_FORMULA_AND_STRUCTUR"><h2 id="_Metaxalone_CHEMICAL_FORMULA_AND_STRUCTUR_">CHEMICAL FORMULA AND STRUCTURE</h2><div class="iconblock whole_rhythm clearfix ten_col table-wrap" id="figMetaxaloneTc"><a href="/books/NBK548838/table/Metaxalone.Tc/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobMetaxaloneTc"><img class="small-thumb" src="/corehtml/pmc/css/bookshelf/2.26/img/table-icon.gif" alt="Table Icon" /></a><div class="icnblk_cntnt"><h4 id="Metaxalone.Tc"><a href="/books/NBK548838/table/Metaxalone.Tc/?report=objectonly" target="object" rid-ob="figobMetaxaloneTc">Table</a></h4></div></div></div><div id="Metaxalone.ANNOTATED_BIBLIOGRAPHY"><h2 id="_Metaxalone_ANNOTATED_BIBLIOGRAPHY_">ANNOTATED BIBLIOGRAPHY</h2><p>References updated: 13 September 2021</p><ul class="first-line-outdent"><li><div class="bk_ref" id="Metaxalone.REF.zimmerman.1999">Zimmerman HJ. Muscle spasmolytics. In, Hepatotoxicity: The Adverse Effects of Drugs and Other Chemicals on the Liver. 2nd Ed. Philadelphia: Lippincott, 1999. p. 544-45.<div><i>(Expert review of hepatotoxicity published in 1999; dantrolene, chlorzoxazone and baclofen are discussed; mentions that metaxalone has been cited as causing jaundice but that no such case reports have appeared in the literature).</i></div></div></li><li><div class="bk_ref" id="Metaxalone.REF.hibbs.2011">Hibbs RE, Zambon AC. Agents acting at the neuromuscular junction and autonomic ganglia. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman &#x00026; Gilman&#x02019;s The pharmacological basis of therapeutics, 12th ed. New York: McGraw-Hill, 2011. p. 255-76.<div><i>(Textbook of pharmacology and therapeutics)</i></div></div></li><li><div class="bk_ref" id="Metaxalone.REF.toth.2004.1355">Toth PP, Urtis J. Commonly used muscle relaxant therapies for acute low back pain: a review of carisoprodol, cyclobenzaprine hydrochloride, and metaxalone. <span><span class="ref-journal">Clin Ther. </span>2004;<span class="ref-vol">26</span>:1355&ndash;67.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15530999" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15530999</span></a>]<div>
<i>(A review of safety and efficacy of muscle relaxants which states "Although rare instances of hepatic enzyme elevation and anemia have been reported [with metaxalone], this association appears to be based on a false-positive hepatic assay using the cephalin flocculation test.").</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.chou.2004.140">Chou R, Peterson K, Helfand M. Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: a systematic review. <span><span class="ref-journal">J Pain Symptom Manage. </span>2004;<span class="ref-vol">28</span>:140&ndash;75.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15276195" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15276195</span></a>]<div>
<i>(Thorough review of the pharmacology, efficacy and side effects of the muscle relaxants).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.moore.2005.249">Moore KA, Levine B, Fowler D. A fatality involving metaxalone. <span><span class="ref-journal">Forensic Sci Int. </span>2005;<span class="ref-vol">149</span>:249&ndash;51.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15749367" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15749367</span></a>]<div>
<i>(54 year old woman found dead in whom postmortem analysis indicated metaxalone overdose; liver reported as being normal).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.poklis.2004.537">Poklis JL, Ropero-Miller JD, Garside D, Winecker RE. Metaxalone (Skelaxin)-related death. <span><span class="ref-journal">J Anal Toxicol. </span>2004;<span class="ref-vol">28</span>:537&ndash;41.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15516312" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15516312</span></a>]<div>
<i>(21 year old woman found dead in whom postmortem analysis indicated metaxalone overdose; no mention of liver abnormalities, although highest levels of drug were present in liver).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.russo.2004.1018">Russo MW, Galanko JA, Shrestha R, Fried MW, Watkins P. Liver transplantation for acute liver failure from drug-induced liver injury in the United States. <span><span class="ref-journal">Liver Transpl. </span>2004;<span class="ref-vol">10</span>:1018&ndash;23.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15390328" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15390328</span></a>]<div>
<i>(Among ~50,000 liver transplants done in the US between 1990 and 2002, 270 [0.5%] were done for drug induced acute liver failure, but none were attributed to muscle relaxants).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.chalasani.2008.1924">Chalasani N, Fontana RJ, Bonkovsky HL, Watkins PB, Davern T, Serrano J, Yang H, Rochon J., Drug Induced Liver Injury Network (DILIN). Causes, clinical features, and outcomes from a prospective study of drug-induced liver injury in the United States. <span><span class="ref-journal">Gastroenterology. </span>2008;<span class="ref-vol">135</span>:1924&ndash;34.</span> [<a href="/pmc/articles/PMC3654244/" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pmc">PMC free article<span class="bk_prnt">: PMC3654244</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/18955056" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 18955056</span></a>]<div>
<i>(Among 300 cases of drug induced liver disease in the US collected from 2004 to 2008, one was attributed to chlorzoxazone, but none to metaxalone).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.reuben.2010.2065">Reuben A, Koch DG, Lee WM., Acute Liver Failure Study Group. Drug-induced acute liver failure: results of a U.S. multicenter, prospective study. <span><span class="ref-journal">Hepatology. </span>2010;<span class="ref-vol">52</span>:2065&ndash;76.</span> [<a href="/pmc/articles/PMC3992250/" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pmc">PMC free article<span class="bk_prnt">: PMC3992250</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/20949552" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 20949552</span></a>]<div>
<i>(Among 1198 patients with acute liver failure enrolled in a US prospective study between 1998 and 2007, 133 were attributed to drug induced liver injury, but none were due to metaxalone or other muscle relaxants).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.bj_rnsson.2013.1419">Bj&#x000f6;rnsson ES, Bergmann OM, Bj&#x000f6;rnsson HK, Kvaran RB, Olafsson S. Incidence, presentation and outcomes in patients with drug-induced liver injury in the General population of Iceland. <span><span class="ref-journal">Gastroenterology. </span>2013;<span class="ref-vol">144</span>:1419&ndash;25.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/23419359" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 23419359</span></a>]<div>
<i>(In a population based study of drug induced liver injury from Iceland, 96 cases were identified over a 2 year period, but none were attributed to metaxalone or other muscle relaxants).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.chalasani.2015.1340">Chalasani N, Bonkovsky HL, Fontana R, Lee W, Stolz A, Talwalkar J, Reddy KR, et al. United States Drug Induced Liver Injury Network. Features and outcomes of 899 patients with drug-induced liver injury: The DILIN Prospective Study. <span><span class="ref-journal">Gastroenterology. </span>2015;<span class="ref-vol">148</span>:1340&ndash;1352.</span> [<a href="/pmc/articles/PMC4446235/" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pmc">PMC free article<span class="bk_prnt">: PMC4446235</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/25754159" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 25754159</span></a>]<div>
<i>(Among 899 cases of drug induced liver injury enrolled in a US prospective study between 2004 and 2013, 5 [0.7%] were attributed to muscle relaxants, one of which was possibly related to metaxalone).</i>
</div></div></li><li><div class="bk_ref" id="Metaxalone.REF.li.2021">Li Y, Delcher C, Reisfield GM, Wei YJ, Brown JD, Winterstein AG. Utilization patterns of skeletal muscle relaxants among commercially insured adults in the United States from 2006 to 2018. Pain Med. 2021:pnab088. Epub ahead of print. [<a href="https://pubmed.ncbi.nlm.nih.gov/33690860" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 33690860</span></a>]<div><i>(Analysis of utilization of skeletal muscle relaxants in the US over a 12 year period demonstrated an increasing use of cyclobenzaprine [65% of prescriptions], baclofen and tizanidine but decreasing use of metaxalone and carisoprodol).</i></div></div></li></ul></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK548838_pubdet_">Publication Details</h2><h3>Publication History</h3><p class="small">Last Update: <span itemprop="dateModified">September 13, 2021</span>.</p><h3>Copyright</h3><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div></div><h3>Publisher</h3><p><a href="https://www.niddk.nih.gov/" ref="pagearea=page-banner&amp;targetsite=external&amp;targetcat=link&amp;targettype=publisher">National Institute of Diabetes and Digestive and Kidney Diseases</a>, Bethesda (MD)</p><h3>NLM Citation</h3><p>LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Metaxalone. [Updated 2021 Sep 13].<span class="bk_cite_avail"></span></p></div><div class="small-screen-prev"><a href="/books/n/livertox/Metamizole/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M75,30 c-80,60 -80,0 0,60 c-30,-60 -30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Prev</text></svg></a></div><div class="small-screen-next"><a href="/books/n/livertox/Metformin/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M25,30c80,60 80,0 0,60 c30,-60 30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Next</text></svg></a></div></article><article data-type="table-wrap" id="figobMetaxaloneTc"><div id="Metaxalone.Tc" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK548838/table/Metaxalone.Tc/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__Metaxalone.Tc_lrgtbl__"><table><thead><tr><th id="hd_h_Metaxalone.Tc_1_1_1_1" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">DRUG</th><th id="hd_h_Metaxalone.Tc_1_1_1_2" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CAS REGISTRY NO</th><th id="hd_h_Metaxalone.Tc_1_1_1_3" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MOLECULAR FORMULA</th><th id="hd_h_Metaxalone.Tc_1_1_1_4" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">STRUCTURE</th></tr></thead><tbody><tr><td headers="hd_h_Metaxalone.Tc_1_1_1_1" scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Metaxalone</td><td headers="hd_h_Metaxalone.Tc_1_1_1_2" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/134980703" ref="pagearea=body&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubchem">1665-48-1</a>
</td><td headers="hd_h_Metaxalone.Tc_1_1_1_3" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C12-H15-N-O3</td><td headers="hd_h_Metaxalone.Tc_1_1_1_4" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/134980703" title="View this structure in PubChem" class="img_link" ref="pagearea=body&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&amp;sid=134980703" alt="image 134980703 in the ncbi pubchem database" /></a>
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