Methocarbamol

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Methocarbamol

Common Trade Names: Robaxin, Robaxin-750

Other Names: 3-(2-methoxyphenoxy) -1,2propanediol 1-carbamate

Methocarbamol is a centrally acting muscle relaxant belonging to the antispasmodic class of drugs. It is FDA-approved for the relief of muscle spasms secondary to peripheral musculoskeletal conditions. Anecdotal evidence has shown that methocarbamol has addictive properties and can lead to substance abuse. Read below to know more about methocarbamol abuse.

A Brief History of Methocarbamol

Methocarbamol was first synthesized in the early 1950s. Its effects were found to be related with muscle spasticity and associated musculoskeletal pain. In 1957, the US Food and Drug Administration approved it for medical use, and methocarbamol has been widely used since then. In 2018, methocarbamol was listed as the 120th most commonly prescribed medications in the US, reportedly with more than 5 million prescriptions.

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How Does Methocarbamol Work in the Human Body?

Methocarbamol is a centrally acting skeletal muscle relaxant indicated in the management of acute musculoskeletal pain secondary to muscle spasm. While the exact mechanism of methocarbamol is still unclear, one theory is that it inhibits acetylcholinesterase at the synapses along the autonomic nervous system, central nervous system, and neuromuscular junction, which in turn decreases muscle tone and weakens polysynaptic reflexes. Methocarbamol is not known to act on the level of motor nerve fiber, motor nerve end plate or skeletal muscle.

Methocarbamol is FDA-approved for the treatment of acute musculoskeletal pain caused by muscle spasms. It is therefore also considered an antispasmodic agent, in contrast to baclofen and dantrolene which are known as antispastic medications. The difference between the two is that antispastic medications treat spasticity secondary to upper motor neuron lesions, such as those resulting from spinal cord injury, while antispasmodic medications, including methocarbamol and cyclobenzaprine, treat spasticity caused by peripheral musculoskeletal conditions.

Methocarbamol, as with any other medications, is contraindicated in patients who have shown allergic or hypersensitivity reaction to it or any of its components. In addition, methocarbamol is contraindicated in patients with impaired renal function because it contains polyethylene glycol or PEG, a compound associated with renal injury, hyperosmolarity, and metabolic acidosis. Similarly, it is not recommended for use in pregnant and breastfeeding mothers as it can cross the placenta and can be excreted in breastmilk.

Methocarbamol should be used with caution in patients diagnosed with myasthenia gravis who are on acetylcholinesterase inhibitor therapy, as these drugs potentiate the action of each other and can lead to severe central nervous system depression.

How Is Methocarbamol Taken or Administered?

Methocarbamol is available in 500mg and 750mg tablets and 100mg/mL intramuscular (IM) or intravenous (IV) formulations. The following are the recommended doses for methocarbamol in various conditions:

Muscle Spasm

Initial: 1g IM/IV; additional doses may be given orally every eight hours, not to exceed 3g per day

If condition does not improve, therapy may be repeated after a drug-free interval of 48 hours. Begin with 1500mg orally every six hours for two to three days, not to exceed 8g per day. Afterwards, decrease to 4 to 4.5g per day every four to eight hours.

Tetanus

Initial: 1-2g IV at 300g per minute. Additional 1-2g IV infusion may be given, not to exceed 3g initially. Repeat 1-2g IV every six hours until patient can tolerate oral administration.

What Are the Immediate and Long-Term Effects of Methocarbamol Use?

While methocarbamol is generally well-tolerated, several adverse effects may arise especially when methocarbamol is misused – that is, when it is taken in amounts greater than prescribed or for a time period longer than necessary. Some of the most common neurologic adverse effects associated with methocarbamol misuse include:

  • Headache
  • Dizziness
  • Sedation
  • Confusion
  • Loss of consciousness
  • Seizure
  • Double vision

Gastrointestinal symptoms have also been reported, such as:

  • Nausea and vomiting
  • Indigestion
  • Metallic taste

Jaundice is also documented in the package insert of methocarbamol, but there is little evidence to show that it can cause hepatic injury. Methocarbamol can also cause urine discoloration, although this has not been linked to kidney impairment.

Signs of Methocarbamol Use Disorder

Several human studies have reported the abuse potential of methocarbamol. Therefore, caution must be observed when taking this medication, and the risk-benefit ratio must always be weighed by the physician before prescription. In addition, patients who have a history of substance abuse must be fully evaluated to determine the risk for methocarbamol addiction.
The Diagnostic and Statistical Manual 5th Edition (DSM-5) Criteria for Substance Use Disorders (SUD) lists four main categories of pathological behavioral patterns manifested in drug abuse, including abuse of methocarbamol:

  1. Impaired control
  2. Social impairment
  3. Risky use
  4. Pharmacological indicators (tolerance and withdrawal)

Listed below are the 11 criteria in the diagnosis of SUDs:

Impaired Control

  1. Taking methocarbamol in larger amounts or for longer than prescribed
  2. Wanting to reduce or stop using methocarbamol, but being unsuccessful
  3. Spending a lot of time getting, using, or recovering from methocarbamol
  4. Feeling intense cravings and urges to take methocarbamol

Social Impairment

  1. Methocarbamol use causes problems with work, school, or family obligations including absenteeism, poor school performance or failure to meet household responsibilities
  2. Continued use of methocarbamol despite having interpersonal or relationship problems
  3. Giving up important social and recreational activities because of methocarbamol use

Risky Use

  1. Repeated use of methocarbamol in high-risk situations, such as while driving a vehicle
  2. Continuing to use methocarbamol despite it worsening physical and psychological problems

Physical Tolerance

  1. Needing a higher dose of methocarbamol to achieve the desired effect (tolerance)
  2. Development of withdrawal symptoms after cessation of methocarbamol use (withdrawal)

Rehab and Treatment for Methocarbamol Use Disorder

The treatment for methocarbamol use disorder goes much like the treatment for abuse of other substances. Treatment must be comprehensive, patient-centered, and tailor-fit to the needs of the patient. There is no one single appropriate treatment option for anyone; treatment must be individualized in order for it to be effective. Thus, one of the most important steps in the rehab process for methocarbamol addiction is a full evaluation of the patient to identify their most pressing concerns.

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The specific treatment strategies for methocarbamol abuse can be done either on an outpatient or inpatient basis, depending on individual factors such as the financial capacity of the patient and the severity of their symptoms. In general, outpatient setting is preferable for patients with mild symptoms and whose commitment to therapy can be ascertained.

Listed below are some rehab strategies for methocarbamol abuse.

Detoxification

Detoxification is the process of removing the buildup of methocarbamol in the body in order to reverse the patient’s dependence to it. Detoxification must be done slowly (weaning off) and under medical supervision, as abrupt cessation of methocarbamol use can cause the development of withdrawal symptoms, which may be life-threatening.

Generally, the approach is to taper off the dosages over a period of several weeks. For methocarbamol, there is no recommended rate of discontinuation, as long as the patient is able to tolerate the withdrawal process. Another approach is to substitute methocarbamol with another medication that has similar effects and safety profile but with lower risk for abuse.

Psychotherapy

The two most commonly used forms of psychotherapy in drug rehab are cognitive-behavioral therapy (CBT) and psychodynamic therapy. Both of these approaches aid in promoting abstinence among drug rehab patients.

CBT is a form of psychotherapy, the goal of which is to identify maladaptive behaviors that predispose an individual to substance abuse. In CBT, patients are taught how to cope with or correct these behaviors in order to prevent them from engaging in substance abuse again. Some examples of CBT are relapse prevention, contingency contracting, and aversion therapy.

In contrast, psychodynamic therapy helps an individual explore their inner conflicts, motivations, and desires to allow them to have a deeper sense of self-understanding. With a renewed self-awareness, patients are empowered to make better choices for themselves.

Counselling

Counselling can be done either by a licensed counsellor or by an individual who has attained complete recovery from addiction. The objectives of counselling are to encourage abstinence, provide emotional and moral support, and refer the patient to specialized services to better address specific concerns. Counsellors also help patients look for and identify potential problem areas in their life that could hinder or slow down their treatment process, so they can come up with appropriate resolutions. The importance of counselling in the rehab process cannot be emphasized further, and there is solid evidence that shows higher recovery rates among patients who underwent counselling.

As mentioned earlier, there is no one right treatment option for anyone. Treatment must be tailor-fit according to the patient’s condition, socioeconomic background, personal preferences, and other variables.

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