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Pharmacology of Methocarbamol (Robaxin) ; Mechanism of action, Pharmacokinetics, Uses, Effects
Methocarbamol is a centrally acting skeletal muscle relaxant used to treat muscle spasms and discomfort associated with acute musculoskeletal conditions. Here’s a detailed look at its pharmacology:
Mechanism of Action
Methocarbamol works by depressing the central nervous system (CNS). It is believed to block spinal polysynaptic reflexes, decrease nerve transmission in spinal and supraspinal polysynaptic pathways, and prolong the refractory period of muscle cells. This leads to sedation and a reduction in skeletal muscle spasms, providing pain relief and increased mobility of the affected muscles2.
Pharmacokinetics
Absorption: Methocarbamol is rapidly and completely absorbed after oral administration.
Distribution: It is widely distributed throughout the body and crosses the placenta.
Metabolism: Methocarbamol is extensively metabolized in the liver to its metabolites, primarily by dealkylation and hydroxylation.
Excretion: The drug and its metabolites are excreted rapidly and completely in urine. The elimination half-life of methocarbamol is approximately 0.9 to 2.2 hours3.
Therapeutic Uses
Methocarbamol is indicated for the relief of discomfort associated with acute, painful musculoskeletal conditions. It is often used as an adjunct to rest, physical therapy, and other treatments2.
Side Effects
Common side effects include:
Drowsiness
Dizziness
Upset stomach
Blurred vision
Fever
Rash
Itching
Dyspepsia
Jaundice
Nausea
Vomiting
Leukopenia3.
Warnings and Precautions
Hypersensitivity: Methocarbamol is contraindicated in patients hypersensitive to the drug or any of its components3.
CNS Depressants: Use with caution in patients receiving other CNS depressants, as methocarbamol may potentiate their effects3.
Liver and Kidney Function: Use with caution in patients with impaired hepatic or renal function.
Alcohol: Avoid alcohol consumption while taking methocarbamol, as it can enhance CNS depressant effects
#Methocarbamol

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