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Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: Although Metaxalone has been assigned with the letter (B), according to the FDA categorization, but it should be used with caution because limited human data is available and the reproduction studies in animals have shown low risk.
Medical Management of Myofascial Pain Syndrome
Published in Gary W. Jay, Chronic Pain, 2007
Metaxalone (Skelaxin®) is a centrally acting skeletal muscle relaxant that is chemically related to mephenaxalone, a mild tranquilizer. It is thought to induce muscle relaxation via CNS depression. Onset of action is about one hour, with peak blood levels in two hours, and duration of action is four to six hours. The recommended dose is 2400 to 3200 mg a day in divided doses (tablets are 400 mg each). It should be used carefully in patients with impaired liver function and should not be used at all in patients with significant renal or liver disease and a history of drug-induced anemias. Side effects include nausea, vomiting, GI upset, drowsiness, dizziness, headache, nervousness, and irritability as well as rash or pruritis. Jaundice and hemolytic anemia are rare.
Post-Traumatic Headache: Diagnosis, Pathophysiology, and Treatment
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Metaxalone (Skelaxin®) is a centrally acting skeletal muscle relaxant that is chemically related to mephenaxalone, a mild tranquilizer. It is thought to induce muscle relaxation via central nervous system depression. Onset of action is about 1 hour, with peak blood levels in 2 hours, and duration of action is 4 to 6 hours. The recommended dose is 2,400 to 3,200 mg a day in divided doses (tablets are 400 mg each). It should be used carefully in patients with impaired liver function and should not be used at all in patients with significant renal or liver disease as well as those with a history of drug-induced anemias. Side effects include nausea, vomiting, gastrointestinal upset, drowsiness, dizziness, headache, nervousness, and irritability, as well as rash or pruritis. Jaundice and hemolytic anemia are rare.
Monoamine oxidase A inhibition by toxic concentrations of metaxalone
Published in Clinical Toxicology, 2020
Brett Cherrington, Ulrich Englich, Supa Niruntari, William Grant, Michael Hodgman
Metaxalone is a centrally acting muscle relaxant indicated as an adjunct therapy for acute painful musculoskeletal conditions. However, it has no direct relaxant effects on human skeletal muscles. The mechanism of action of the drug has not been established, but its efficacy may be related to its sedative properties. Adverse reactions include drowsiness, dizziness, and headache as well as agitation, irritability and gastrointestinal upset [4,5]. Deaths involving metaxalone have been reported, particularly in combination with other drugs [6–8]. Serotonin toxicity following both metaxalone overdose and therapeutic use of metaxalone is reported in individuals on therapeutic doses of serotonergic drugs such as SSRIs. Monoamine oxidase A (MAO-A) inhibition by metaxalone is a proposed etiology [9–12]. A therapeutic reference range for metaxalone is not available. A mean peak plasma concentration of 0.9 mcg/ml (4 µM) is reported at 3.3 h after a single 400 mg dose [13]. In published cases of serotonin toxicity associated with metaxalone, the concentration of metaxalone ranges from 31 to 61 mcg/ml (140–276 µM) [9–11]. We investigated the effect of metaxalone on MAO-A activity using an in vitro model.