What are the primary uses of metaxalone 800 mg. How does metaxalone work as a muscle relaxant. What are the potential side effects of metaxalone. Is metaxalone associated with liver toxicity. How effective is metaxalone for musculoskeletal pain.

Understanding Metaxalone: A Centrally Acting Muscle Relaxant

Metaxalone is a centrally acting skeletal muscle relaxant that has been in use for over four decades. It is primarily prescribed for the treatment of acute musculoskeletal conditions and muscle spasms. Despite its long-standing use, the precise mechanism of action of metaxalone remains not well documented.

How does metaxalone work? While the exact mechanism is not fully understood, it is believed to act on the central nervous system to reduce muscle tension and alleviate pain associated with musculoskeletal disorders. This central action distinguishes it from other muscle relaxants that may work directly on the muscles themselves.

Approved Indications and Dosage

The primary indications for metaxalone include:

• Treatment of pain from acute musculoskeletal conditions
• Relief of muscle spasms

The recommended dosage for metaxalone is 800 mg taken orally three to four times daily. It is available by prescription in both 400 mg and 800 mg tablet formulations, marketed under the brand name Skelaxin as well as in generic forms.

Efficacy and Safety Profile of Metaxalone

Is metaxalone effective for musculoskeletal pain? While metaxalone has been widely used as a muscle relaxant, recent trends indicate a decline in its usage. The efficacy of metaxalone, like its mechanism of action, is not well documented in large-scale clinical trials. However, its continued use in clinical practice suggests that it provides relief for some patients with acute musculoskeletal pain and muscle spasms.

How safe is metaxalone compared to other muscle relaxants? The safety profile of metaxalone appears to be relatively favorable, with side effects reported as being uncommon. However, it’s important to note that sparse data are available regarding its long-term safety.

Common Side Effects

When side effects do occur, they may include:

• Drowsiness
• Dizziness
• Headache
• Nausea
• Dry mouth

Potential Drug Interactions and Serotonin Syndrome

Can metaxalone interact with other medications? One significant concern with metaxalone is its potential to interact with serotonergic medications. When combined with drugs that affect serotonin levels in the brain, metaxalone can potentially contribute to the development of serotonin syndrome.

What is serotonin syndrome and how does metaxalone contribute to it? Serotonin syndrome is a potentially life-threatening condition characterized by excessive serotonergic activity in the central nervous system. When metaxalone is used in combination with other serotonergic medications, it may increase the risk of this syndrome.

Medications That May Interact with Metaxalone

Caution should be exercised when combining metaxalone with:

• Selective serotonin reuptake inhibitors (SSRIs)
• Tricyclic antidepressants
• Triptans (used for migraine treatment)
• Opiates
• Other serotonergic medications

Symptoms of Serotonin Syndrome

Patients and healthcare providers should be aware of the potential signs of serotonin syndrome, which may include:

1. Agitation
2. Confusion
3. Hallucinations
4. Tachycardia (rapid heart rate)
5. Hyperthermia (elevated body temperature)
6. Incoordination
7. Neuromuscular rigidity
8. Nausea and abdominal pain

Hepatotoxicity: Examining the Liver Safety of Metaxalone

Is metaxalone associated with liver toxicity? Despite being in use for over 40 years, metaxalone has not been significantly associated with liver toxicity. According to available literature and clinical experience, metaxalone appears to have a low risk of causing clinically apparent liver injury.

Have there been reports of liver damage from metaxalone? While the product brochure for metaxalone mentions the possibility of jaundice, there are no specific case reports of hepatotoxicity in the medical literature. Additionally, no prospective trials with routine monitoring of liver enzymes have been conducted to definitively assess its impact on liver function.

Liver Safety Assessment

Based on current evidence:

• Metaxalone has not been associated with significant elevations in serum aminotransferases during therapy
• There are no documented cases of clinically apparent liver injury attributed to metaxalone
• The likelihood of metaxalone causing clinically significant liver injury is considered low

It’s worth noting that given its long history of use, the absence of significant hepatotoxicity reports suggests that metaxalone is generally safe for the liver when used as prescribed.

Comparing Metaxalone to Other Muscle Relaxants

How does metaxalone compare to other commonly used muscle relaxants? While a comprehensive comparison is beyond the scope of this article, it’s important to consider metaxalone in the context of other available options.

Some other frequently prescribed muscle relaxants include:

• Cyclobenzaprine
• Carisoprodol
• Tizanidine
• Baclofen

Each of these medications has its own unique profile of efficacy, side effects, and potential risks. The choice of muscle relaxant often depends on the specific condition being treated, patient characteristics, and individual response to treatment.

Factors to Consider When Choosing a Muscle Relaxant

1. Mechanism of action
2. Efficacy for specific conditions
3. Side effect profile
4. Potential for drug interactions
5. Risk of dependence or abuse
6. Cost and availability

Healthcare providers must weigh these factors when deciding whether to prescribe metaxalone or another muscle relaxant for a particular patient.

Clinical Studies and Evidence for Metaxalone Efficacy

What evidence supports the use of metaxalone for musculoskeletal conditions? While metaxalone has been in use for decades, the body of clinical research supporting its efficacy is somewhat limited compared to newer medications. However, several studies have examined its effectiveness in various musculoskeletal conditions.

Key Findings from Clinical Research

• A randomized, double-blind study comparing metaxalone to placebo in patients with acute lower back pain found that metaxalone provided significant improvement in pain intensity and muscle spasm
• Another study examining the use of metaxalone in combination with ibuprofen for acute lower back pain showed enhanced pain relief compared to ibuprofen alone
• A systematic review of muscle relaxants for low back pain included metaxalone among the medications that showed some evidence of effectiveness, though the quality of evidence was generally low across all muscle relaxants

It’s important to note that while these studies suggest potential benefits, more robust clinical trials are needed to definitively establish the efficacy of metaxalone across various musculoskeletal conditions.

Special Populations and Precautions

Are there specific populations that should use caution with metaxalone? As with any medication, certain groups may be at higher risk for adverse effects or may require special consideration when using metaxalone.

Pregnancy and Breastfeeding

Limited data are available on the use of metaxalone during pregnancy and breastfeeding. The FDA classifies metaxalone as Pregnancy Category C, indicating that animal studies have shown an adverse effect on the fetus, but there are no adequate and well-controlled studies in humans. Pregnant women should only use metaxalone if the potential benefit justifies the potential risk to the fetus.

Elderly Patients

Older adults may be more sensitive to the effects of metaxalone, particularly its sedative properties. Dosage adjustments may be necessary, and careful monitoring for side effects is important in this population.

Patients with Liver or Kidney Disease

While metaxalone is not significantly associated with liver toxicity, patients with pre-existing liver or kidney disease should use caution and may require dose adjustments or more frequent monitoring.

Individuals with a History of Substance Abuse

Although metaxalone is not considered to have a high potential for abuse, individuals with a history of substance abuse should be monitored closely when using this medication.

Future Directions and Research Needs

What areas of research are needed to better understand metaxalone? Despite its long history of use, there are several areas where further research could enhance our understanding of metaxalone and its role in pain management:

• Large-scale, well-designed clinical trials to definitively establish efficacy across various musculoskeletal conditions
• Studies to elucidate the precise mechanism of action of metaxalone
• Long-term safety studies to assess potential risks associated with prolonged use
• Comparative effectiveness research to determine how metaxalone stacks up against newer muscle relaxants and pain management strategies
• Investigation into potential new indications or formulations of metaxalone

As our understanding of pain mechanisms and pharmacology continues to evolve, ongoing research into established medications like metaxalone remains important to optimize their use and ensure patient safety.

Emerging Trends in Muscle Relaxant Research

While metaxalone continues to be studied, broader trends in muscle relaxant research include:

1. Development of more selective agents with fewer side effects
2. Exploration of combination therapies to enhance efficacy and reduce individual drug doses
3. Investigation of novel delivery methods to improve drug targeting and reduce systemic exposure
4. Integration of muscle relaxants into comprehensive pain management programs that include physical therapy and other non-pharmacological approaches

These emerging trends may shape the future use of metaxalone and other muscle relaxants in clinical practice.

Metaxalone – LiverTox – NCBI Bookshelf

Last Update: September 13, 2021.

OVERVIEW

Introduction

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.

Background

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.

Hepatotoxicity

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.

Likelihood score: E (Unlikely cause of clinically apparent liver injury).

Drug Class: Muscle Relaxants

CHEMICAL FORMULA AND STRUCTURE

ANNOTATED BIBLIOGRAPHY

References updated: 13 September 2021

• 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.

  (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).

• Hibbs RE, Zambon AC. Agents acting at the neuromuscular junction and autonomic ganglia. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman & Gilman’s The pharmacological basis of therapeutics, 12th ed. New York: McGraw-Hill, 2011. p. 255-76.

  (Textbook of pharmacology and therapeutics)

• Toth PP, Urtis J. Commonly used muscle relaxant therapies for acute low back pain: a review of carisoprodol, cyclobenzaprine hydrochloride, and metaxalone. Clin Ther. 2004;26:1355–67. [PubMed: 15530999]

  (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.”).

• Chou R, Peterson K, Helfand M. Comparative efficacy and safety of skeletal muscle relaxants for spasticity and musculoskeletal conditions: a systematic review. J Pain Symptom Manage. 2004;28:140–75. [PubMed: 15276195]

  (Thorough review of the pharmacology, efficacy and side effects of the muscle relaxants).

• Moore KA, Levine B, Fowler D. A fatality involving metaxalone. Forensic Sci Int. 2005;149:249–51. [PubMed: 15749367]

  (54 year old woman found dead in whom postmortem analysis indicated metaxalone overdose; liver reported as being normal).

• Poklis JL, Ropero-Miller JD, Garside D, Winecker RE. Metaxalone (Skelaxin)-related death. J Anal Toxicol. 2004;28:537–41. [PubMed: 15516312]

  (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).

• 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. Liver Transpl. 2004;10:1018–23. [PubMed: 15390328]

  (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).

• 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. Gastroenterology. 2008;135:1924–34. [PMC free article: PMC3654244] [PubMed: 18955056]

  (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).

• Reuben A, Koch DG, Lee WM., Acute Liver Failure Study Group. Drug-induced acute liver failure: results of a U.S. multicenter, prospective study. Hepatology. 2010;52:2065–76. [PMC free article: PMC3992250] [PubMed: 20949552]

  (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).

• Björnsson ES, Bergmann OM, Björnsson HK, Kvaran RB, Olafsson S. Incidence, presentation and outcomes in patients with drug-induced liver injury in the General population of Iceland. Gastroenterology. 2013;144:1419–25. [PubMed: 23419359]

  (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).

• 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. Gastroenterology. 2015;148:1340–1352. [PMC free article: PMC4446235] [PubMed: 25754159]

  (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).

• 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. [PubMed: 33690860]

  (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).

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Metaxalone – Overview

Metaxalone is a medication sometimes prescribed to people in conjunction with rest and other measures for the relief of pain caused by acute musculoskeletal conditions. People who might need a metaxalone medication prescription, including metaxalone 800 mg tablets, can use Push Health to connect with a medical provider who can prescribe metaxalone medication, including generic metaxalone 800 mg tablets, when appropriate to do so.

What Is Metaxalone Used For?

Metaxalone prescription medication, marketed under the brand names Metaxall and Skelaxin, is a drug chemically known as 5-[(3,5- dimethylphenoxy) methyl]-2-oxazolidinone. Metaxalone medication, similar to cyclobenzaprine (Flexeril) and methocarbamol (Robaxin), is sometimes prescribed to people suffering from an acute and painful musculoskeletal condition. The exact mechanism as to how metaxalone works is not fully understood although it is surmised that it exerts its effects through depression of impulses at the level of the central nervous system or possibly suppression of cytokines. Metaxalone medication has not been observed to have direct effects on nerve fibers or the motor end plate. Metaxalone prescription tablets should be used in conjunction with rest, physical therapy and other conservative measures.

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Metaxalone – Dosage and Cost

Metaxalone is generally prescribed to be taken as metaxalone 800 mg tablets one or more times per day. Ultimately, the regimen of metaxalone prescribed depends on the specific health needs of the patient and the judgement of the prescribing medical provider. Following oral administration by study subjects, metaxalone reached peak plasma levels in approximately three hours. Metaxalone is metabolized in the body by the liver and excreted through the kidneys. Metaxalone is moderately affordable, costing under $1 per metaxalone 800 mg tablet at many pharmacies across the United States. Metaxalone coupons can sometimes be found online and some insurance plans may cover costs associated with a metaxalone medication prescription. Metaxalone is typically available as metaxalone 800 mg tablets.

Can I Buy Metaxalone Online?

One cannot just buy metaxalone online as metaxalone requires a prescription to be dispensed by a pharmacy in the United States. Because of this, metaxalone OTC is not available, either. The first step to getting a metaxalone medication prescription is consulting a licensed medical provider. People who might need a metaxalone tablet prescription, including generic metaxalone 800 mg tablets, can use Push Health to connect with a medical provider who can prescribe metaxalone prescription tablets when appropriate to do so.

Get Metaxalone Tablets »

Metaxalone – Side Effects

Metaxalone prescription medication, like other medications, can cause side effects when used. Side effects that can occur while using metaxalone tablets include dizziness, headache, drowsiness, nausea, vomiting and gastrointestinal upset. People with a hypersensitivity to metaxalone should avoid using the medication. Serotonin syndrome has been reported is association with metaxalone use. Metaxalone and alcohol should not be used together and operating heavy machinery or driving should be avoided while using the medication. Before taking metaxalone tablets, it is important to discuss possible side effects and other concerns with a qualified medical provider.

More Metaxalone Information

• Metaxalone – Medline

Last updated October 12, 2021. Given the evolving nature of medicine and science, this information might not be accurate and should not be construed as medical advice or diagnosis / treatment recommendations. Please consult a licensed medical provider if you have additional questions. Please call 911 immediately or go to the nearest emergency room if you believe you are experiencing a medical emergency.

Metaxalone – instructions for use

Metaxalone

Instruction:

• Pharmacological action
• Pharmacokinetics
• Readings
• Contraindications
• Pregnancy and breastfeeding
• Pediatric use
• Use in elderly patients
• Dosage and Administration
• Side effects
• Precautions
• Transport management
• Classification

Pharmacological action

Metaxalone is a central muscle relaxant. The mechanism of action is not fully understood, presumably associated with a general depression of the central nervous system.

Pharmacokinetics

Absorption

Maximum plasma concentration (C _max ) – 296 mcg / ml. Time to reach maximum plasma concentration (TC _max ) – 3 hours.

Onset within 1 hour, duration 4-6 hours.

Distribution

Distribution volume (V _d ) – 800 l.

Metabolism

Biotransformed in the liver.

Elimination

Half-life (T _½ ) – 4-14 hours. About Excreted in the urine.

Indications

Painful muscle spasm in diseases and injuries of the musculoskeletal system.

Contraindications

Hypersensitivity; drug hemolytic anemia in history; significant renal/liver failure.

Pregnancy and breastfeeding

Use in pregnancy

FDA fetal category C.

Adequate and well-controlled clinical studies of the safety of metaxalone during pregnancy have not been conducted. It is not known whether the drug has immediate or delayed adverse effects on the fetus.

Animal studies showed no evidence of impaired fertility or harm to the fetus.

The use of metaxalone in pregnant women is contraindicated.

Use during breastfeeding

Special studies on the safety of the use of metaxalone during breastfeeding have not been conducted.

It is not known whether metaxalone is excreted in breast milk. A risk to the infant cannot be ruled out.

If necessary, the use of the drug during lactation should stop breastfeeding.

Pediatric use

Safety and efficacy in children under 12 years of age have not been established.

Use in elderly patients

Worse tolerated in elderly patients.

Dosage and Administration

Children over 12 years of age and adults: Orally, 800 mg 3-4 times a day.

Side effects

The frequency of occurrence of adverse reactions has not been determined: gastrointestinal disorders, nausea, vomiting, dizziness, headache, drowsiness, nervousness, hemolytic anemia (rare), leukopenia (rare), jaundice (rare), hypersensitivity (rare).

Precautions

CNS depression may occur

Increased sedation may occur when combined with other sedatives.

Bioavailability may be increased in women.

Influence on the ability to drive vehicles and control mechanisms

Due to the fact that metaxalone can cause dizziness and drowsiness, it is necessary to refrain from driving vehicles and engaging in activities that require increased concentration of attention and speed of psychomotor reactions.

Classification

• Pharmacological group

  n-anticholinergics (muscle relaxants)

• FDA pregnancy category

  C
  (risk not excluded)

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Find out more about the active ingredient Metaxalone: ​​

• Reviews
• Questions
• Latin name
• Chemical formula

Information about the active substance Metaxalone is intended for medical and pharmaceutical professionals, for reference purposes only. The instructions are not intended to replace professional medical advice, diagnosis or treatment. The information contained here may change over time. The most accurate information on the use of drugs containing the active substance Metaxalone is contained in the manufacturer’s instructions attached to the package.

Metaxalone (skelaxin): side effects, dosages, treatments, interactions, warnings

Relax

• What is
  • What is metaxalone and how does it work?
• Side effects
  • What side effects are associated with the use of metaxalone?
• Drug interactions
  • What other drugs interact with metaxalone?
• Warnings and precautions
  • What are the warnings and precautions for metaxalone?

Trade name: Skelaxin

Generic name: metaxalone

Drug class: skeletal muscle relaxants

What is metaxalone and how does it work?

Metaxalone is a skeletal muscle relaxant indicated for the short-term treatment of painful muscle spasms.

Metaxalone is marketed under the following trade names: Skelaxin.

Metaxalone dosages:

Dosage forms and strengths

difference between braxton and real contractions

Tablet

• 800mg

Dosage Recommendation:

Musculoskeletal pain

• Indicated for acute, painful musculoskeletal conditions

900 05 Adults: 800 mg orally every 6 to 8 hours.

• Children 12 years of age and older: 800 mg orally every 6 to 8 hours.
• Children under 12 years of age: Safety and efficacy not established.

Dosage Modifications

Renal Insufficiency

• Mild to Moderate Disorders: Use caution.
• Severe violation: contraindicated.

Liver failure

• Mild to moderate impairment: use caution.
• Severe violation: contraindicated.

What side effects are associated with the use of metaxalone?

Side effects of metaxalone include:

• Gastrointestinal drug-induced disorders
• Indigestion
• Nausea
• Vomiting
• Dizziness 9000 6
• Headache
• Drowsiness
• Nervousness
• Irritability
• Skin rash
• Hemolytic anemia (rare)
• Low white blood cell count (leukopenia) (rare)
• Immune hypersensitivity reaction (rare)

Serious side effects of metaxalone include:

• Abdominal pain
• Loss of appetite 9000 6
• Low fever
• Dark urine
• Clay colored stools
• Yellowing of the skin and eyes (jaundice) (rare)

This leaflet does not contain all possible side effects that may occur. For more information about side effects, please consult your doctor.

What other drugs interact with metaxalone?

If your doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and can monitor you for them. Do not start, stop, or change the dosage of any medicine without talking to your doctor, health care provider, or pharmacist.

Botox side effects for migraine

Severe interactions with metaxalone include:

• Idelalisib
• ivacaftor
• sodium oxybate

Metaxalone interacts moderately with at least 160 different drugs.

Mild interactions of metaxalone include:

• eucalyptus
• sage

This information does not contain all possible interactions or side effects. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Consult your healthcare professional or physician for additional medical advice, or if you have any health questions, concerns, or additional information about this medicine.

What are the warnings and precautions for metaxalone?

Warnings

This medicine contains metaxalone. Do not take skelaxin if you are allergic to metaxalone or any of the ingredients in this medicine.

Keep out of reach of children. In case of overdose, seek medical attention or contact a Poison Control Center immediately.

Contraindications.

• Hypersensitivity
• History of drug-induced hemolytic anemia
• Significant renal/hepatic impairment

Effects of drug abuse

Timolol maleate ophthalmic gel solution

• None

Short-term effects

• See “What side effects are associated with the use of metaxalone?”

Long-term effects

• See “What side effects are associated with the use of metaxalone?”

Warnings

• Central nervous system (CNS) depression may occur.
• Sedation may be increased when used with other sedatives.
• Drugs are poorly tolerated by the elderly
• Bioavailability may be increased in female patients.