Metaxalone 400 mg. Metaxalone 400mg: Comprehensive Guide to Uses, Side Effects, and Dosing
What are the primary uses of Metaxalone 400mg. How should Metaxalone be taken for optimal results. What are the potential side effects and interactions of Metaxalone. When should caution be exercised while using Metaxalone.
Understanding Metaxalone: A Powerful Muscle Relaxant
Metaxalone, commonly prescribed in 400mg doses, is a potent muscle relaxant used to alleviate discomfort associated with acute musculoskeletal conditions. This medication works by affecting the central nervous system to reduce muscle spasms and associated pain. While effective, it’s crucial to understand its proper use, potential side effects, and interactions to ensure safe and optimal treatment outcomes.
What is Metaxalone Used For?
Metaxalone is primarily prescribed for:
- Acute musculoskeletal pain
- Muscle spasms
- Lower back pain
- Neck pain
Is Metaxalone suitable for all types of muscle pain. While effective for acute conditions, it’s not typically recommended for chronic pain management. Metaxalone is most beneficial when used in conjunction with rest, physical therapy, and other supportive measures to promote muscle relaxation and healing.
Proper Dosage and Administration of Metaxalone 400mg
The recommended dosage of Metaxalone may vary depending on the individual’s condition and response to treatment. Typically, the standard dose is 800mg (two 400mg tablets) taken three to four times daily. However, it’s crucial to follow your healthcare provider’s instructions precisely.
Key Points for Taking Metaxalone:
- Take with or without food, but consistency is important
- If taken with food, high-fat meals may increase absorption
- Do not crush, chew, or break the tablets
- Space doses evenly throughout the day
- Do not exceed the prescribed dosage
Can Metaxalone be taken on an empty stomach. While it can be taken without food, taking it with a meal, especially a high-fat one, may enhance absorption and effectiveness. However, maintain consistency in how you take the medication to ensure steady blood levels.
Potential Side Effects of Metaxalone
Like all medications, Metaxalone can cause side effects. While not everyone experiences them, it’s important to be aware of potential adverse reactions.
Common Side Effects:
- Drowsiness
- Dizziness
- Headache
- Nausea
- Irritability
- Nervousness
Are there any serious side effects to watch out for. While rare, some patients may experience more severe reactions such as:
- Allergic reactions (rash, itching, swelling)
- Severe dizziness or fainting
- Difficulty breathing
- Unusual changes in mood or behavior
If you experience any of these severe side effects, seek medical attention immediately.
Drug Interactions and Precautions
Metaxalone can interact with various medications and substances, potentially altering its effectiveness or increasing the risk of side effects. It’s crucial to inform your healthcare provider about all medications, supplements, and herbal products you’re taking.
Notable Interactions:
- MAO inhibitors
- Serotonergic drugs (SSRIs, SNRIs, triptans)
- Benzodiazepines
- Opioid pain medications
- Alcohol
Does Metaxalone interact with common over-the-counter medications. It can potentially interact with antihistamines and certain cough and cold medicines. Always consult with your pharmacist or doctor before combining Metaxalone with any OTC products.
Special Precautions and Considerations
Certain individuals may need to exercise extra caution when using Metaxalone or may not be suitable candidates for this medication.
Use Caution If You Have:
- Liver disease
- Kidney disease
- History of drug abuse
- Anemia
- Seizure disorders
Is Metaxalone safe during pregnancy or breastfeeding. Limited data exists on its safety in these situations. It’s crucial to discuss the potential risks and benefits with your healthcare provider if you’re pregnant, planning to become pregnant, or breastfeeding.
Monitoring and Managing Metaxalone Treatment
Regular monitoring is essential when taking Metaxalone to ensure its effectiveness and minimize potential risks. Your healthcare provider may recommend periodic blood tests to check liver function, especially if you’re on long-term treatment.
Tips for Successful Treatment:
- Keep all follow-up appointments with your healthcare provider
- Report any unusual symptoms or side effects promptly
- Avoid activities requiring alertness until you know how the medication affects you
- Do not abruptly stop taking Metaxalone without consulting your doctor
- Engage in recommended physical therapy and exercise programs
How long should Metaxalone treatment typically last. The duration of treatment varies depending on the individual’s condition and response. Generally, it’s prescribed for short-term use (2-3 weeks) to minimize the risk of dependence and side effects. Your healthcare provider will determine the appropriate length of treatment based on your specific needs.
Alternatives to Metaxalone and Complementary Therapies
While Metaxalone is effective for many patients, it’s not the only option for managing musculoskeletal pain and muscle spasms. Understanding alternative treatments and complementary therapies can help you make informed decisions about your care.
Alternative Medications:
- Cyclobenzaprine
- Carisoprodol
- Baclofen
- Tizanidine
Complementary Therapies:
- Physical therapy
- Massage
- Acupuncture
- Heat and cold therapy
- Stretching and yoga
Can lifestyle changes help reduce the need for muscle relaxants. Indeed, maintaining a healthy weight, practicing good posture, engaging in regular exercise, and managing stress can significantly contribute to muscle health and potentially reduce the frequency or severity of muscle spasms.
Navigating Insurance Coverage and Cost Considerations
The cost of Metaxalone can vary significantly depending on insurance coverage, pharmacy pricing, and whether a generic version is available. Understanding your options can help manage treatment costs effectively.
Cost-Saving Strategies:
- Check if your insurance covers Metaxalone
- Inquire about generic alternatives
- Compare prices at different pharmacies
- Look into prescription discount programs
- Discuss lower-cost alternatives with your healthcare provider
Are there assistance programs available for patients who can’t afford Metaxalone. Some pharmaceutical companies offer patient assistance programs for those who meet specific criteria. Additionally, local and national organizations may provide resources to help cover medication costs. Consult with your healthcare provider or a social worker to explore available options.
Long-Term Outlook and Management of Musculoskeletal Conditions
While Metaxalone can provide significant relief for acute musculoskeletal pain and muscle spasms, it’s essential to consider the long-term management of underlying conditions. Developing a comprehensive treatment plan that addresses both immediate symptoms and long-term health is crucial for optimal outcomes.
Key Components of Long-Term Management:
- Regular exercise and stretching routines
- Ergonomic adjustments at work and home
- Stress management techniques
- Nutritional support for muscle and joint health
- Regular check-ups with healthcare providers
How can patients transition from acute treatment with Metaxalone to long-term management strategies. Gradual reduction of Metaxalone use, under medical supervision, coupled with the introduction and intensification of physical therapy, exercise programs, and other non-pharmacological interventions can facilitate a smooth transition. This approach helps prevent reliance on medication while building strength and flexibility to reduce future muscle spasms and pain.
Preventing Recurrence of Muscle Spasms:
- Maintain good posture throughout the day
- Use proper lifting techniques
- Stay hydrated
- Get adequate sleep
- Manage underlying health conditions that may contribute to muscle issues
By incorporating these strategies and working closely with healthcare providers, patients can develop a comprehensive approach to managing musculoskeletal health, potentially reducing the need for frequent use of muscle relaxants like Metaxalone.
Emerging Research and Future Directions in Muscle Relaxant Therapy
The field of muscle relaxant therapy is continually evolving, with ongoing research aimed at improving efficacy, reducing side effects, and developing novel treatment approaches. Staying informed about these developments can help patients and healthcare providers make more informed decisions about treatment options.
Current Areas of Research:
- Development of more targeted muscle relaxants with fewer systemic effects
- Exploration of combination therapies for enhanced efficacy
- Investigation of long-term safety profiles for extended use
- Studies on the potential benefits of muscle relaxants in chronic pain conditions
- Research into personalized medicine approaches for optimal drug selection
What advancements can we expect in muscle relaxant therapy in the coming years. While specific predictions are challenging, trends suggest a move towards more personalized treatment approaches, potentially utilizing genetic information to guide drug selection and dosing. Additionally, there’s growing interest in developing muscle relaxants with improved safety profiles and reduced potential for abuse.
Potential Future Developments:
- Novel delivery methods for localized treatment
- Integration of artificial intelligence in treatment planning
- Development of dual-action drugs combining muscle relaxant and analgesic properties
- Exploration of natural compounds with muscle relaxant effects
- Advancements in understanding the neurophysiology of muscle spasms
These ongoing research efforts highlight the importance of continuing to refine and improve treatment options for musculoskeletal conditions. As new findings emerge, treatment guidelines and recommendations may evolve, potentially offering patients more effective and tailored therapeutic options in the future.
In conclusion, while Metaxalone 400mg remains a valuable tool in the management of acute musculoskeletal pain and muscle spasms, it’s part of a broader landscape of treatment options and ongoing research. Patients and healthcare providers should stay informed about current best practices and emerging therapies to ensure optimal management of musculoskeletal conditions.
Metaxalone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing
See also How to Use section.
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.
Some products that may interact with this drug include: diet pills/appetite suppressants (such as diethylpropion), drugs for attention deficit disorder (such as atomoxetine, methylphenidate), apraclonidine, bupropion, buspirone, carbamazepine, cyclobenzaprine, deutetrabenazine, a certain combination product (dextromethorphan/quinidine), levodopa, maprotiline, methyldopa, metoclopramide, certain opioid pain relievers (such as fentanyl, meperidine, methadone, tapentadol), certain drugs for Parkinson’s disease (such as entacapone, tolcapone), certain supplements (such as tryptophan, tyramine), tetrabenazine, tricyclic antidepressants (such as amitriptyline, doxepin), valbenazine.
The risk of serotonin syndrome/toxicity increases if you are also taking other drugs that increase serotonin. Examples include street drugs such as MDMA/”ecstasy,” St. John’s wort, certain antidepressants (including mirtazapine, SSRIs such as fluoxetine/paroxetine, SNRIs such as duloxetine/venlafaxine), tramadol, certain “triptans” used to treat migraine headaches (such as rizatriptan, sumatriptan, zolmitriptan), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.
Some products can interact with metaxalone if you take them together, or even if you take them weeks before or after taking metaxalone. Tell your doctor or pharmacist if you take anything in the list of products that may interact with this drug, or any of the products that increase serotonin, within 2 weeks before or after taking metaxalone. Also tell them if you have taken fluoxetine within 5 weeks before starting metaxalone. Ask your doctor how much time to wait between starting or stopping any of these drugs and starting metaxalone.
Taking other MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Do not take any other MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before and after treatment with this medication. Ask your doctor when to start or stop taking this medication.
Before using metaxalone, report the use of drugs that may increase the risk of extremely high blood pressure (hypertensive crisis) when combined with metaxalone, including herbal products (such as ephedra/ma huang), nasal decongestants (such as phenylephrine, pseudoephedrine), and stimulants (such as amphetamines, ephedrine, epinephrine, phenylalanine). Metaxalone should not be used with any of these medications. Talk to your doctor or pharmacist for more details.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), other muscle relaxants (such as carisoprodol, cyclobenzaprine), or antihistamines (such as cetirizine, diphenhydramine).
Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.
This medication may interfere with certain lab tests (such as certain urine glucose tests), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.
Does Metaxalone interact with other drugs you are taking?
Enter your medication into the WebMD interaction checker
Metaxalone: MedlinePlus Drug Information
pronounced as (me tax’ a lone)
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Metaxalone, a muscle relaxant, is used with rest, physical therapy, and other measures to relax muscles and relieve pain and discomfort caused by strains, sprains, and other muscle injuries.
Metaxalone comes as a tablet to take by mouth. It usually is taken three or four times a day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take metaxalone exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.
Before taking metaxalone,
- tell your doctor and pharmacist if you are allergic to metaxalone, any other medications, or any of the ingredients in metaxalone tablets. Ask your pharmacist for a list of the ingredients.
- tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take while taking metaxolone. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- tell your doctor if you have or have ever had kidney disease, liver disease, seizures, or a blood disorder.
- tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking metaxalone, call your doctor immediately.
- talk to your doctor about the risks and benefits of taking metaxalone if you are 65 years of age or older. Older adults should not usually take metaxalone because it is not as safe or effective as other medications that can be used to treat the same condition.
- you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how metaxalone affects you.
- remember that alcohol can add to the drowsiness caused by this drug.
Take the missed dose as soon as you remember it. However, if it is almost time for your next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
Metaxalone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- drowsiness
- dizziness
- headache
- nervousness
If you experience any of the following symptoms, call your doctor immediately:
- agitation, hallucinations, coma
- fast heart rate, high body temperature
- muscle twitching, loss of muscle control
- nausea, vomiting, diarrhea
- severe skin rash
- difficulty breathing
- yellowing of the skin or eyes
- unusual bruising or bleeding
- unusual tiredness or weakness
- seizures
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature, away from excess heat and moisture (not in the bathroom).
It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org
Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo. gl/c4Rm4p) for more information if you do not have access to a take-back program.
In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.
- Skelaxin®
Last Revised – 07/15/2022
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instructions for use, dosage, composition, analogues, side effects / Pillintrip
and PATIENT INFORMATION ).
Carcinogenesis, mutagenesis, impaired fertility
The carcinogenic potential of metaxalone has not been determined.
Pregnancy
Reproduction studies in rats showed no evidence of impaired fertility or fetal harm due to metaxalone. Post-marketing experience has not shown any evidence of fetal injury, but such experience cannot rule out the possibility of rare or subtle injury to the human fetus. The safe use of metaxalone has not been demonstrated in relation to possible adverse effects on fetal development. Therefore, metaxalone tablets should not be used in women who are or may be pregnant, especially during early pregnancy, unless the physician considers that the potential benefits outweigh the potential hazards.
Nursing mothers
It is not known if this drug is excreted in breast milk. As a general rule, caution should not be exercised when taking medications, as many medications are excreted in breast milk.
Pediatric use
Safety and efficacy in children over 12 years of age have not been established.
Overdose and Contraindications
Intentional or accidental overdose deaths have occurred with metaxalone, especially when combined with antidepressants, and this class of drug has been reported in combination with alcohol.
Serotonin syndrome has been reported when metaxalone was used at doses above the recommended dose layers (see WARNINGS ).
When determining LD 50 progressive sedation, hypnosis and finally respiratory failure were found in rats and mice with increasing dosage. No LD can be found in dogs 50 is determined because higher doses were emetic after 15-30 minutes.
Treatment
Gastric lavage and supportive care. It is recommended that you consult with your regional gift management center.
PRICE
Hypersensitivity to components of this product is known.
Known tendency to drug-induced, hemolytic or other anemia.
Significantly impaired renal or hepatic function.
Clinical pharmacology
CLINICAL PHARMACOLOGY
Mechanism of action
The mechanism of action of metaxalone in humans has not been established, but it can be attributed to a general depression of the central nervous system.
Metaxalone has no direct effect on the contractile mechanism of the striated muscle, motor end plate or nerve fiber.
Pharmacokinetics
The pharmacokinetics of metaxalone was studied in healthy adult volunteers after a single dose of metaxalone in sober and well-fed conditions at doses ranging from 400 to 800 mg.
Absorption
Peak plasma concentrations of metaxalone occur approximately 3 hours after an oral dose of 400 mg under sober conditions. The logarithmic concentrations of metaxalone then decrease with a finite half-life of 9.0 ± 4.8 hours. Doubling the dose of Metaxalone from 400 mg to 800 mg results in an approximately proportional increase in Metaxalone exposure as evidenced by peak plasma concentrations (Cmax) 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.
Pharmacokinetic parameters of single dose metaxalone in two groups of healthy volunteers are shown in Table 1.
Table 1: Mean (% CV) pharmacokinetic parameters of Metaxalone
Dose (mg) | Cmax (ng/ml) | Tmax (h) | AUC∞ (ng & ml; h/ml) | t½ (h) | CL / F ( L / h) |
400 1 | 983 (53) | 3.![]() | 7479 (51) | 9, 0 (53) | 68 (50) |
800 2 | 1816 (43) | 3.0 (39) | 15044 (46) | 8.0 (58) | 66 (51) |
1 Subjects received 1x400mg tablet sober (N = 42) 2 Subjects received 2x400mg tablets sober conditions (N = 59) |
Food Effects
A randomized, bi-directional, crossover study was conducted in 42 healthy volunteers (31 males, 11 females) who administered a Metaxalone 400 mg tablet while sober and after a standard high-fat breakfast. Subjects ranged from 18 to 48 years (mean age = 23.5 ± 5.7 years). Compared to sober states, the presence of a high-fat meal increased by 177.5% during drug C administration and increased AUC (AUC0-t, AUC∞) by 123.5% and 115.4%, respectively. Time to peak concentration (Tmax) was also delayed (4.3 hours vs. 3.3 hours) and the terminal half-life was reduced (2. 4 hours vs. 9.0 hours) under feeding conditions compared with fasting.
In a second study with a similar effect, healthy volunteers (N = 59, 37 males, 22 females) were given two tablets of metaxalone 400 mg (800 mg) aged 18-50 years (mean age = 25). 6 ± 8.7 years). Compared to sober states, the presence of a high-fat meal increased by 193.6% during drug C administration and increased AUC (AUC0-t, AUC, ∞) by 146.4% and 142.2%, respectively. Time to Peak concentration (Tmax) was also delayed (4.9h versus 3.0 h), and the terminal half-life was shortened (4.2 h compared to 8.0 h) under fed versus fasting conditions. Similar nutritional effects were observed in the aforementioned study when a Metaxalone tablet was administered instead of two 400 mg Metaxalone tablets. An increase in metaxalone exposure, which coincides with a decrease in half-life, may be due to more complete absorption of metaxalone in the presence of a high-fat meal (Figure 1).
Figure 1: Mean (SD) concentrations of metaxalone after a dose of 800 mg under fasting and feeding conditions
Distribution, metabolism and elimination
Although plasma protein binding and absolute bioavailability of metaxalone are unknown, the apparent volume of distribution (V/F 800 L) and lipophilia (log P = 2. 42) of metaxalone indicate that the drug is mainly distributed in tissues. Metaxalone is metabolized in the liver and excreted in the urine as unidentified metabolites. Hepatic cytochrome P450 enzymes play a role in the metabolism of metaxalone. In particular, CYP1A2, CYP2D6, CYP2E1 and CYP3A4 and to a lesser extent CYP2C8, CYP2C9and CYP2C19 metabolize metaxalone.
Metaxalone does not significantly inhibit major CYP enzymes such as CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. Metaxalone does not cause significant induction of important CYP enzymes such as CYP1A2, CYP2B6 and CYP3A4 in vitro .
Pharmacokinetics in special populations
Age
The effect of age on the pharmacokinetics of metaxalone was determined after a single administration of two 400 mg (800 mg) tablets under fasting and feeding conditions. The results were evaluated separately, as well as in combination with the results of three other studies. Using the combined data, the results show that the pharmacokinetics of metaxalone under sober conditions is significantly more dependent on age than under feeding, with bioavailability increasing with age under sober conditions.
The fasting and feeding bioavailability of metaxalone in three groups of healthy volunteers of different ages is shown in Table 2.
Table 2: Mean pharmacokinetic parameters (% CV) feeding
Age (years) | Junior volunteers | Elderly volunteers | |||||
25.6 ± 8.7 9007 9 | 39.3 ± 10.8 | 71.5 ± 5.0 | |||||
N | |||||||
Food | Tasty | Fed | Tasty | Fed | Delicious | Fed | |
Cmax (ng/ml) | 1816 (43) | 3510 (41) | 2719 (4 6) | 2915 (55) | 3168 (43) | 3680 ( 59) | |
TMAX (h) | 3.0 (39) | 4.9 (48) | 3.0 (40) | 8.7 (91) | 2 ,6 (30) | 6.5 (67) | |
AUC0-t (ng·h/ml) | 14531 (47) | 20683 (41) | 19836 (40) | 20482 (37) | 23797 (45) | 24340 (48) | |
AUC∞ (ng·h/mL) | 15045 (46) | 20833 (41) 9) | 20815 (37) | 24194 (44) | 24704 (47) |
Gender
in which 48 healthy adult subjects (24 men, 24 women) were administered, two tablets of metaxalone 400 mg (800 mg) in sober conditions. The bioavailability of metaxalone was significantly higher in women than in men than Cmax (2115 ng/ml vs 1335 ng/ml) and AUC∞ (17884 ng h/ml vs 10328 ng h/ml). The mean half-life was 11.1 hours for women and 7.6 hours for men. The apparent volume of distribution of metaxalone was approximately 22% higher in men than in women, but the difference was not significant when adjusted for body weight. Similar results were also seen when the previously described combined data set was used in the analysis.
Liver/renal failure
The effect of liver and kidney disease on the pharmacokinetics of metaxalone has not been determined. In the absence of such information, Metaxalone should be used with caution in patients with hepatic and/or renal insufficiency.
Skelaxin (Metaxalone): Uses, Dosage, Side Effects, Interactions, Warning0294 Product Description
Product description
What is skelaxin and how is it used?
Skelaxin is a prescription medicine used to treat the symptoms of musculoskeletal pain. Skelaxin can be used alone or with other medicines.
Skelaxin belongs to a class of drugs called skeletal muscle relaxants.
It is not known whether Skelaxin is safe and effective in children under 12 years of age.
What are the possible side effects of Skelaxin?
Skelaxin can cause serious side effects, including:
- weak or shallow breathing,
- lightheadedness,
- pale or yellow skin,
- dark urine0289
- high fever,
- confusion,
- weak spot,
- upper stomach pain,
- loss of appetite and
- yellowing of the skin or eyes (jaundice)
900 08 Seek immediate medical attention if you have any – any of the above symptoms.
The most common side effects of Skelaxin include:
- dizziness,
- drowsiness,
- nausea,0289
- upset stomach,
- headache, and
- feeling nervous or irritable
Tell your doctor if you have any side effects that bother you or that don’t go away.
These are not all possible side effects of Skelaxin. For more information, contact your doctor or pharmacist.
Ask your doctor about side effects. You can report side effects to the FDA at 1-800-FDA-1088.
DESCRIPTION
SKELAXIN (metaxalone) is available in the form of pink oval tablets with a score of 800 mg.
Chemically, metaxalone is 5-[(3,5-dimethylphenoxy)methyl]-2-oxazolidinone. Empirical formula: C 12 H fifteen HE 3 , which corresponds to a molecular weight of 221.25. Structural formula:
Metaxalone is a white or almost white odorless crystalline powder, easily soluble in chloroform, soluble in methanol and6% ethanol, but practically insoluble in ether or water.
Each tablet contains 800 mg of metaxalone and the following inactive ingredients: alginic acid, ammonium calcium alginate, B-Rose liquid, corn starch and magnesium stearate.
INDICATIONS AND DOSAGE
INDICATIONS
SKELAXIN (metaxalone) is indicated as an adjunct to rest, physical therapy and other measures to relieve discomfort associated with acute, painful musculoskeletal problems. The mechanism of action of this drug has not been precisely established, but may be related to its sedative properties. Metaxalone does not directly relax tense human skeletal muscles.
DOSAGE AND ADMINISTRATION
The recommended dose for adults and children over 12 years of age is one 800 mg tablet three to four times daily.
HOW SUPPLIED
SKELAXIN (Metaxalone) Available as an 800 mg scored oval pink tablet, debossed with 8667 on the grooved side and an ‘S’ on the other side. Available in vials of 100 ( NDC 60793-136-01) and in vials of 500 ( NDC 60793-136-05).
Store at controlled room temperature between 15°C and 30°C (59°F and 86 °F).
SKELAXIN is a registered trademark of King Pharmaceuticals Research and Development, Inc.
Distributed by: Pfizer Inc., New York, NY 10017 Revised: November 2015
Side effects and drug interactions
SIDE EFFECTS
The most common reactions to metaxalone include:
9 0008 CNS: drowsiness, dizziness headache and nervousness or “irritability”;
Digestive: nausea, vomiting, gastrointestinal upset.
Other adverse reactions:
Immune system: hypersensitivity reaction, rash with or without itching;
Hematological: leukopenia; hemolytic anemia;
Hepatobiliary: jaundice.
side effects of Kenalog 40 injection
Anaphylactoid reactions have been reported with metaxalone, although rare.
DRUG INTERACTIONS
No information provided.
Warnings and Precautions
WARNINGS
Potentially life-threatening serotonin syndrome (SS) has been reported with the use of metaxalone. These reports have usually occurred when metaxalone was used concomitantly with serotonergic drugs (such as tramadol or selective serotonin reuptake inhibitors (SSRIs)) or when metaxalone was used at higher than recommended doses (see DRUG INTERACTIONS and OVERDOSE ). Signs of SS may include clonus, agitation, sweating, tremors, hyperreflexia, hypertonicity, and fever.
SKELAXIN may potentiate the effects of alcohol and other CNS depressants.
PRECAUTIONS
Metaxalone should be used with great caution in patients with pre-existing liver disease. In such patients, serial liver function tests should be performed.
Benedict’s false positive tests have been noted due to an unknown reducing agent. A specific glucose test will differentiate the results.
Dietary intake of SKELaxin may increase overall CNS depression; Elderly patients may be particularly sensitive to such CNS effects. (See CLINICAL PHARMACOLOGY : Pharmacokinetics and PATIENT INFORMATION ).
Carcinogenesis, mutagenesis, impaired fertility
The carcinogenic potential of metaxalone has not been determined.
Pregnancy
Reproduction studies in rats showed no evidence of impaired fertility or harm to the fetus due to metaxalone. Post-marketing experience has not shown evidence of fetal injury, but such experience cannot rule out the possibility of infrequent or minor injury to the human fetus. The safe use of metaxalone has not been established with regard to possible adverse effects on fetal development. Therefore, metaxalone tablets should not be used by women who are pregnant or planning pregnancy, especially in early pregnancy, unless, in the opinion of the physician, the potential benefits outweigh the possible risks.
Nursing mothers
It is not known if this drug is secreted in breast milk. As a general rule, breastfeeding should not be done while the patient is taking medication, as many medications are excreted in breast milk.
Pediatric use
Safety and efficacy in children under 12 years of age have not been established.
Overdose and contraindications
OVERDOSAGE
Deaths due to intentional or accidental overdose have occurred with the use of metaxalone, especially in combination with antidepressants, and cases of this class of drugs in combination with alcohol have been reported.
Serotonin syndrome has been reported when higher than recommended doses of metaxalone have been reported (see WARNINGS ).
When determining the LD 50 in rats and mice with increasing dosage, progressive sedation, hypnosis and, finally, respiratory failure were noted. In dogs no LD 50 could be determined because higher doses caused emesis after 15-30 minutes.
Care
Gastric lavage and supportive care. It is recommended to consult with the regional poison control center.
CONTRAINDICATIONS
Known hypersensitivity to any component of this product.
Known tendency to drug-induced, hemolytic or other anemia.
Significant impairment of kidney or liver function.
Clinical pharmacology
CLINICAL PHARMACOLOGY
Mechanism of action
The mechanism of action of metaxalone in humans has not been established, but it may be associated with general depression of the central nervous system.
Metaxalone has no direct action on the contractile mechanism of the striated muscle, motor end plate or nerve fiber.
Pharmacokinetics.
The pharmacokinetics of metaxalone was evaluated in healthy adult volunteers after administration of a single dose of SCELaxin on an empty stomach and after meals at doses of 400 to 800 mg.
Absorption
Peak plasma concentrations of metaxalone occur approximately 3 hours after oral administration of 400 mg on an empty stomach. Thereafter, metaxalone concentrations decrease logarithmically with a terminal half-life of 9.0 ± 4.8 hours. Doubling the dose of SKELaxin from 400 mg to 800 mg results in an approximately proportional increase in metaxalone exposure, as evidenced by peak plasma concentrations (Cmax) and area under the curve (AUC). Dose proportionality at doses above 800 mg has not been studied. The absolute bioavailability of metaxalone is unknown.
Pharmacokinetic parameters of a single dose of metaxalone in two groups of healthy volunteers are presented in Table 1.
Table 1: Mean (% CV) pharmacokinetic parameters of metaxalone
Dose (mg) | Cmax (ng/ml) | Tmax (h) | AUC & infin; (ng & bull; h / ml) | t & frac12; | CL / F (51) | 9.0 (53) | 68 (50) |
800 two0079 8.0 (58) | 66 (51) | | |||||
one Subjects received 1 tablet of 400 mg on an empty stomach (N = 42). two Subjects received 2 x 400 mg tablets on an empty stomach (N = 59). |
Nutritional effects
A randomized, two-way crossover study was conducted in 42 healthy volunteers (31 males, 11 females) who were administered one tablet of SKELAXIN 400 mg on an empty stomach and after a standard high-fat breakfast. The age of the subjects ranged from 18 to 48 years (mean age = 23. 5 ± 5.7 years). Compared to fasting conditions, the presence of a high-fat meal during drug administration increased Cmax by 177.5% and increased AUC (AUC0-t, AUC.infin.) by 123.5% and 115.4%, respectively. The time to reach maximum concentration (Tmax) was also delayed (4.3 hours compared to 3.3 hours) and the terminal half-life was reduced (2.4 hours compared to 90 hours) under eating conditions compared with fasting.
In a similarly designed food impact study, two 400 mg (800 mg) SKELAXIN tablets were administered to healthy volunteers (N = 59, 37 males, 22 females) aged 18 to 50 years (mean age = 25.6 ± 8.7 years). Compared to fasting conditions, the presence of a high-fat meal during drug administration increased Cmax by 193.6% and increased AUC (AUC0-t, AUC & infin;) by 146.4% and 142.2%, respectively. The time to reach maximum concentration (Tmax) was also delayed (4.9hours compared to 3.0 hours), and the terminal elimination half-life decreased (4.2 hours compared to 8.0 hours) under conditions of food intake compared with conditions on an empty stomach. Similar nutritional effects results were observed in the aforementioned study when one SKELAXIN 800 mg tablet was administered instead of two SKELAXIN 400 mg tablets. An increase in metaxalone exposure, coinciding with a decrease in half-life, may be due to more complete absorption of metaxalone in the presence of a high-fat meal (Fig. 1).
Figure 1: Mean (SD) concentrations of metaxalone after a dose of 800 mg under fasting and feeding conditions
Distribution, metabolism and excretion
Although plasma protein binding and absolute bioavailability of metaxalone are unknown, it appears the volume of distribution (V/F ~ 800 L) and lipophilicity (log P = 2.42) of metaxalone suggest that the drug is widely distributed in tissues. Metaxalone is metabolized in the liver and excreted in the urine as unidentified metabolites. Liver cytochrome P450 enzymes play a role in the metabolism of metaxalone. In particular, CYP1A2, CYP2D6, CYP2E1 and CYP3A4 and, to a lesser extent, CYP2C8, CYP2C9and CYP2C19 appear to metabolize metaxalone.
Metaxalone slightly inhibits major CYP enzymes such as CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. Metaxalone slightly induces major CYP enzymes such as CYP1A2, CYP2B6 and CYP3A4. in vitro .
Pharmacokinetics in special populations
Age
The effect of age on the pharmacokinetics of metaxalone was determined after a single dose of two 400 mg (800 mg) tablets on an empty stomach and after a meal. The results were analyzed separately and also in combination with the results of three other studies. Using the pooled data, the results show that the pharmacokinetics of metaxalone are significantly more dependent on age under fasted conditions than under food conditions, with fasting bioavailability increasing with age.
The fasting and postprandial bioavailability of metaxalone in three groups of healthy volunteers of different ages is shown in Table 2. feeding
Age (years) | Young volunteers | Older volunteers | ||||
25.6 ± 8.7 | 71.5 ± 5.0 | |||||
N | 59 | 21 | 2. 3 | |||
Food | Hungry | fed | Hungry | fed | Hungry | fed |
Cmax (ng/mL) | 1816 (43) | 3510 (41) | 2719 (46) | 3168 (43) | 3680 (59) | |
Tmax (h) | 3.0 (39) | 4.9 (48) | 3.0 (40) | 8.7 (91) | 2.6 (30) | 6.5 (67) 90 079 |
AUC0-t (ng and steer / ml) | 14531 (47) | 20683 (41) | 19836 (40) | 20482 (37) | 24340 (48) | |
AUC & infin; (ng & bull; h / ml) | 15045 (46) | 20833 (41) | 20490 (39) | 20815 (37) | 24194 (44) | 24704 (47) |
Gender women) were administered two SKELAXIN 400 mg tablets ( 800 mg) on an empty stomach.
Bioavailability of metaxalone was significantly higher in women compared to men as evidenced by Cmax (2115 ng/mL vs 1335 ng/mL) and AUC∞ (17884 ng-middot; h/ml compared to 10328 ng-middot; h/ml). The mean elimination half-life was 11.1 hours in women and 7.6 hours in men. The apparent volume of distribution of metaxalone was approximately 22% higher in men than in women, but differed slightly when adjusted for body weight. Similar results were also obtained when the previously described combined dataset was used in the analysis.
Hepatic / renal failure
The effect of liver and kidney disease on the pharmacokinetics of metaxalone has not been determined. In the absence of such information, SKELaxin should be used with caution in patients with hepatic and/or renal impairment.
Medication Guide
PATIENT INFORMATION
SKELAXIN may impair the mental and/or physical abilities required to perform hazardous tasks such as operating machinery or driving a car, especially when used with alcohol or other CNS depressants.