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Dear Readers! I started this blog when my daughter was in the NICU. She had ventriculitis. Her CSF report grew E.coli. But, she was injected Teicoplanin directly into her brain. The doctors made two errors here:

Teicoplanin is for gram-positive bacteria only. It does not treat E.coli.
Teicoplanin is not for intraventricular use. The manufacturer strongly discourage injecting Teicoplanin into the brain.

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Metaxalone (Skelaxin) - Uses, Dose, Side effects, MOA, Brands

Metaxalone (Skelaxin) is used as a muscle relaxant.

The exact mechanism of action of the drug is not known, however, it causes central nervous system depression.

Metaxalone (Skelaxin) Uses:

Musculoskeletal conditions:
- It helps ease the discomfort of sudden muscle problems like pain and spasms.
- Other medicines for muscle spasms are Tizanidine (Ternaline), Baclofen (Baclin), and Chlorzoxazone.

Metaxalone (Skelaxin) Dose in Adults:

Metaxalone (Skelaxin) Dose in the Musculoskeletal conditions:

Take 800 milligrams by mouth three or four times a day.

Use in Children:

For adults, the recommended dosage is 800 milligrams taken orally three or four times a day.

Metaxalone (Skelaxin) Pregnancy Risk Category: C

In studies with animals, no harmful effects on fetal development were found.
However, it's crucial to use the medication during pregnancy only if you believe that the advantages outweigh the potential risks, particularly in the first trimester.

Use of metaxalone while breastfeeding

We don't know if the medication passes into breast milk.
It's recommended to avoid using it while breastfeeding, as advised by the manufacturer.

Dose in Kidney Disease:

If someone has significant kidney problems, it's not recommended to use the medication.

The manufacturer's instructions do not provide dosage recommendations for individuals with mild to moderate kidney dysfunction. Caution should be exercised in such cases.

Dose in Liver disease:

If someone has severe liver disease, it is not advisable to use the medication.

The manufacturer's instructions do not provide dosage recommendations for individuals with mild to moderate liver impairment.

Care should be taken in such cases.

Side effects of Metaxalone (Skelaxin)

Central nervous system:
- Drowsiness
- Irritability
- Headache
- Nervousness
- Dizziness
Dermatologic:
- Skin rash (with or without pruritus)
Gastrointestinal:
- Gastrointestinal distress
- Vomiting
- Nausea
Hematologic & oncologic:
- Leukopenia
- Hemolytic anemia
Hepatic:
- Jaundice
Hypersensitivity:
- Hypersensitivity reaction
- Anaphylaxis
- Anaphylactoid reaction (rare)

Contraindications to Metaxalone (Skelaxin):

Do not use the drug if you have allergies to any of its components, severe kidney or liver problems, or a history of drug-induced hemolytic anemia or other types of anemia.

Warnings and precautions

Depression in the CNS:
- The drug can cause CNS depression, which may result in drowsiness and impaired physical and mental abilities.
- People who need to stay alert for tasks that require mental or physical focus, especially those operating heavy machinery or driving, should be cautioned.
Serotonin syndrome
- When taken along with other serotonergic drugs like SSRIs, SNRIs, TCAs, triptans, 5-HT3 receptor antagonists, or MAO inhibitors, this medication can lead to serotonin syndrome.
- Serotonin syndrome can be serious and may occur when starting or adjusting the dose.
- Patients should closely monitor for symptoms such as changes in mental state (anxiety, sleepiness, hallucinations), autonomic instability (hyperthermia, fluctuating blood pressure, tachycardia), neuromuscular changes (hyperreflexia, myoclonus, incoordination), and gastrointestinal symptoms (nausea, vomiting, diarrhea).
- Symptoms of serotonin syndrome can appear within 24 hours, and if they occur, it's crucial to stop all treatment immediately.
Hepatic impairment
- Regular liver function tests should be conducted during the course of therapy.
- If a patient has a severe liver impairment, they should avoid taking the medication.
Renal impairment
- Individuals with impaired renal function or severe renal impairment should avoid taking the drug.

Metaxalone: Drug Interaction

Risk Factor C (Monitor therapy)
Alcohol (Ethyl)	Alcohol's CNS depressing effect may be amplified by CNS depressants (Ethyl).
Alizapride	CNS depressants may have an enhanced CNS depressant impact.
Botulinum Toxin-Containing Products	Centrally acting muscle relaxants may intensify the harmful/toxic effects of products containing botulinum toxin. In particular, there may be a greater likelihood of developing muscle weakness.
Brexanolone	Brexanolone's CNS depressing effects may be amplified by other CNS depressants.
Brimonidine (Topical)	CNS depressants may have an enhanced CNS depressant impact.
Bromopride	CNS depressants may have an enhanced CNS depressant impact.
Cannabidiol	CNS depressants may have an enhanced CNS depressant impact.
Cannabis	CNS depressants may have an enhanced CNS depressant impact.
Chlorphenesin Carbamate	CNS depressants may have an enhanced CNS depressant impact.
CNS Depressants	CNS depressants may have an enhanced CNS depressant impact.
Dimethindene (Topical)	CNS depressants may have an enhanced CNS depressant impact.
Doxylamine	CNS depressants may have an enhanced CNS depressant impact. Management: The producer of the pregnancy-safe drug Diclegis (doxylamine/pyridoxine) particularly advises against combining it with other CNS depressants.
Dronabinol	CNS depressants may have an enhanced CNS depressant impact.
Esketamine	CNS depressants may have an enhanced CNS depressant impact.
HydrOXYzine	CNS depressants may have an enhanced CNS depressant impact.
Kava Kava	CNS depressants may have an enhanced CNS depressant impact.
Lofexidine	May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Magnesium Sulfate	May enhance the CNS depressant effect of CNS Depressants.
MetyroSINE	CNS Depressants may enhance the sedative effect of MetyroSINE.
Minocycline (Systemic)	May enhance the CNS depressant effect of CNS Depressants.
Nabilone	May enhance the CNS depressant effect of CNS Depressants.
Piribedil	Piribedil's CNS depressing effects may be enhanced by other CNS depressants.
Pramipexole	The sedative effects of pramipexole might be enhanced by CNS depressants.
ROPINIRole	The sedative effects of CNS depressants may increase those of ROPINIRole.
Rotigotine	Rotigotine's sedative effects may be boosted by CNS depressants.
Rufinamide	CNS depressants' harmful or toxic effects could be increased. Particularly, drowsiness and lightheadedness could be worsened.
Serotonergic Agents (High Risk)	Serotonergic agents' serotonergic effects may be enhanced by methylxalone (High Risk). Serotonin syndrome might occur from this. When these medications are taken together, it is important to watch out for any signs and symptoms of serotonin syndrome or serotonin poisoning, such as hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, and changes in mental status.
Tetrahydrocannabinol	CNS depressants may have an enhanced CNS depressant impact.
Tetrahydrocannabinol and Cannabidiol	CNS depressants may have an enhanced CNS depressant impact.
Trimeprazine	CNS depressants may have an enhanced CNS depressant impact.
Risk Factor D (Consider therapy modification)
Blonanserin	Blonanserin's CNS depressing effects may be enhanced by other CNS depressants.
Buprenorphine	The CNS depressing impact of buprenorphine may be enhanced by CNS depressants. Treatment: If a patient has a high risk of abusing or injecting themselves with buprenorphine, consider reducing the doses of other CNS depressants and avoiding such medications. Buprenorphine should be started at lower doses in individuals who are currently taking CNS depressants.
Chlormethiazole	CNS depressants may have an enhanced CNS depressant impact. Management: Keep a close eye out for signs of severe CNS depression. If such a combination is required, it should be taken at a dose that has been suitably lowered, according to the instructions for chlormethiazole.
Droperidol	May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Risk
Flunitrazepam	Flunitrazepam's CNS depressing effects may be enhanced by other CNS depressants.
HYDROcodone	The CNS depressive action of HYDROcodone may be enhanced by CNS depressants. Management: Whenever feasible, refrain from using hydrocodone and benzodiazepines or other CNS depressants concurrently. Only in the event that other treatment choices are insufficient should these medications be combined. Limit the duration and dosage of each medicine when used together.
Lemborexant	CNS depressants may have an enhanced CNS depressant impact. Management: Due to the possibility of additive CNS depressant effects when lemborexant and concurrent CNS depressants are administered concurrently, dosage modifications may be required. Effects of CNS depressants must be closely monitored.
Methotrimeprazine	The CNS depressing action of methotrimeprazine may be enhanced by CNS depressants. The CNS depressant action of CNS Depressants may be strengthened by methotrimeprazine. Management: Start concurrent methotrimeprazine therapy while reducing the adult dose of CNS depressants by 50%. Only once a clinically effective dose of methotrimeprazine has been established should additional CNS depressant dosage modifications be made.
Opioid Agonists	Opioid agonists' CNS depressing effects may be amplified by CNS depressants. Management: When at all possible, refrain from using benzodiazepines or other CNS depressants concurrently with opioid agonists. Only in the event that other treatment choices are insufficient should these medications be combined. Limit the duration and dosage of each medicine when used together.
OxyCODONE	The CNS depressing effects of OxyCODONE may be enhanced by CNS depressants. Management: Whenever feasible, refrain from using oxycodone and benzodiazepines or other CNS depressants concurrently. Only in the event that other treatment choices are insufficient should these medications be combined. Limit the duration and dosage of each medicine when used together.
Perampanel	CNS depressants may have an enhanced CNS depressant impact. Treatment: Until they have experience using the combination, patients taking perampanel along with any other medication that has CNS depressive effects should avoid complex and high-risk activities, especially those like driving that call for awareness and coordination.
Sodium Oxybate	CNS depressants may have an enhanced CNS depressant impact. Management: Take into account substitutes for combined use. Reduce the doses of one or more medications when simultaneous use is necessary. It is not advised to use sodium oxybate with alcoholic beverages or hypnotic sedatives.
Suvorexant	Suvorexant's CNS depressing effects may be amplified by other CNS depressants. Treatment: Suvorexant and/or any other CNS depressant dosage reduction may be required. Suvorexant shouldn't be taken with alcohol, and it shouldn't be taken for sleeplessness with any other medication either.
Tapentadol	CNS depressants may have an enhanced CNS depressant impact. Treatment: When feasible, refrain from using tapentadol and benzodiazepines or other CNS depressants simultaneously. Only in the event that other treatment choices are insufficient should these medications be combined. Limit the duration and dosage of each medicine when used together.
Tolperisone	May intensify the negative or harmful effects of muscle relaxants (Centrally Acting). Management: If tolperisone is used with other centrally acting muscle relaxants, watch for signs of increased sedation or CNS effects. If these medications are taken together, think about lowering the tolperisone dosage.
Zolpidem	CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk
Risk Factor X (Avoid combination)
Azelastine (Nasal)	Azelastine's CNS depressing impact may be amplified by CNS depressants (Nasal).
Bromperidol	CNS depressants may have an enhanced CNS depressant impact.
Orphenadrine	The CNS depressing action of orphenadrine may be enhanced by CNS depressants.
Oxomemazine	CNS depressants may have an enhanced CNS depressant impact.
Paraldehyde	The CNS depressing effects of paraldehyde may be enhanced by CNS depressants.
Thalidomide	The CNS depressing effect of thalidomide may be enhanced by CNS depressants.

Monitoring Parameters:

The manufacturer's labeling does not specify any particular conditions, but it is recommended to monitor liver and renal functions regularly.

How to administer Metaxalone (Skelaxin)?

You can take the medication with or without food.
However, having it with food can enhance the drug's absorption, resulting in higher levels in the blood and intensifying its effects on the central nervous system.
The impact of eating habits on the drug's clinical effectiveness is not known.

Mechanism of action of Metaxalone (Skelaxin):

The exact mechanism of action of the drug is unclear.
It is likely that the effects of the medication result from depressing the central nervous system.
However, the drug does not affect motor end plates, nerve fibers, or striated muscles.

Metabolism:

The drug undergoes metabolism in the liver through various cytochrome P450 enzymes, including CYP1A2, CYP2D6, CYP2E1, and CYP3A4.
Additionally, to a lesser extent, it is metabolized by CYP2C8, CYP2C9, and CYP2C19 enzymes. However, the bioavailability of the drug is not provided in the information provided.

Bioavailability:

The bioavailability of the drug may be increased when taken with food.

Half-life elimination:

It takes about 9 hours for the drug to reduce its strength by half, and this time can vary by around 4.8 hours.

Time to peak:

Around 3 hours

Excretion:

The drug's byproducts or breakdown products are eliminated through urine.

International Brands of Metaxalone:

Metaxall
Skelaxin
Flexura
Sabaxolone
Sketarest
Striolaxone

Metaxalone Brand Names in Pakistan:

No Brands Available in Pakistan.

Metaxalone (Skelaxin) - Uses, Dose, Side effects, MOA, Brands

Metaxalone (Skelaxin) Uses:

Musculoskeletal conditions:

Metaxalone (Skelaxin) Dose in Adults:

Metaxalone (Skelaxin) Dose in the Musculoskeletal conditions:

Use in Children:

Metaxalone (Skelaxin) Pregnancy Risk Category: C

Dose in Kidney Disease:

Dose in Liver disease:

Side effects of Metaxalone (Skelaxin)

Central nervous system:

Dermatologic:

Gastrointestinal:

Hematologic & oncologic:

Hepatic:

Hypersensitivity:

Contraindications to Metaxalone (Skelaxin):

Warnings and precautions

Depression in the CNS:

Serotonin syndrome

Hepatic impairment

Renal impairment

Monitoring Parameters:

How to administer Metaxalone (Skelaxin)?

Mechanism of action of Metaxalone (Skelaxin):

International Brands of Metaxalone:

Metaxalone Brand Names in Pakistan:

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