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Baclofen

Baclofen, known under its tradename Lioresal, is a commonly prescribed medication to treat the muscle spasticity that results from spinal cord injury or multiple sclerosis. First developed to treat epilepsy by Swiss chemist Heinrich Keberle in 1962, baclofen’s effects were disappointing. But despite being marketed as a muscle-relaxant, baclofen has been dubbed a ‘cure’ for sufferers of addiction – whether that’s to alcohol, drugs, binge-eating or gambling...

Baclofen works by activating receptors in the brain that are sensitive to gamma-aminobutyric acid, or Gaba. This reduces nerve cell activity, which makes us feel sleepy and calm. Alcohol activates Gaba receptors and has a similar effect...

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 If baclofen is so great, why isn’t everyone using it already?

When I delved into the story of baclofen in France, it was obvious that there were two radically different opinions about baclofen for alcoholism treatment. On one side were the Baclofen Supporters who felt that the slow acceptance of baclofen as a safe and valid treatment for alcoholism was criminal because of the health and social carnage caused by alcoholism in France. They cited the 130 deaths per day from alcoholism which continued while French health authorities argued that baclofen was not safe enough and that there was not enough scientific evidence to support it’s use. So my answer to the question “If baclofen is so great, why isn’t everyone using it already?” is that it’s not a problem with baclofen itself but about the various interests which have played out around it.

 The Obtunded Patient

Baclofen is a synthetic derivative of the naturally occurring inhibitory neurotransmitter GABA. Acts principally on the GABA-B receptor at the spinal level and reduce the post-synaptic potentials along motor neurons, thus relaxing the skeletal muscles. Baclofen is primarily used for the treatment of spastic movement disorders and now more ubiquitously for the treatment of chronic back pain.

Articles of Interest

Baclofen 10 mg-GEN

What is the most important information I should know about baclofen? Do not use baclofen at a time when you need muscle tone for safe balance and movement during certain activities. Do not stop using baclofen suddenly, or you could have unpleasant withdrawal symptoms.

Baclofen for Spasticity: Would Like to Hear Your Input

Really, I want to hear from people who have been on Baclofen in an athletic context. Finally, I have made substantial improvements in the last 3 weeks. 3 weeks ago I could not walk or run in the shallow end of the pool without spasticity. Now I can. I can get around inside my house without crutches, and when I need to, I hold a wall or furniture. At work I use the crutches to get over longer distances in the office. Outside I have to pretty well always use them to deterministicaly get around. I don't feel confident walking around outside and getting "stuck".

Baclofen in the Treatment of Spinal Cord Injuries

Baclofen, commonly known as Kemstro or Lioresal, is a medication used in the treatment of spasticity in spinal cord injuries. This drug acts as an allosteric modulator to GABA b receptors which leads to the inhibition of alpha motor neurons within the spinal cord. Pre- and postsynaptic inhibition leads to a reduction in skeletal muscle tone. The weak permeability to the blood-brain barrier makes baclofen more effective in treating spasticity at the level of the spinal cord. Additionally, baclofen does not cause the type of generalized muscle weakness seen with other medications like dantrolene.

Baclofen Pump and Me

The decision we need to make each time is a trade-off. The drug is a muscle relaxant so the more you have the easier it is to walk but the weaker and more wobbly you become. However the result is dramatic for me. Just to give you an idea, before this it would take me about 29 minutes to walk a kilometre on the treadmill.

Baclofen therapeutics, toxicity, and withdrawal: A narrative review

Baclofen is an effective therapeutic for the treatment of spasticity related to multiple sclerosis, spinal cord injuries, and other spinal cord pathologies. It has been increasingly used off-label for the management of several disorders, including musculoskeletal pain, gastroesophageal reflux disease, and alcohol use disorder. Baclofen therapy is associated with potential complications, including life-threatening toxicity and withdrawal syndrome. These disorders require prompt recognition and a high index of suspicion

Baclofen toxicity

Baclofen is a synthetic derivative of GABA. At a therapeutic dose it acts on spinal GABAb receptors but in overdose this selectivity is lost and the GABA receptors in the brain are targeted resulting in sedation and coma. Complicating this baclofen also mediates pre- and postsynaptic inhibition (therefore inhibiting the inhibitor) causing seizures in overdose. And like GABAa withdrawal the same situation can occur if a patient suddenly stops baclofen and withdrawal syndromes can manifest.

Baclofen Use May Be Linked to Higher Encephalopathy Risk in Chronic Kidney disease

Although primarily used as a muscle relaxant for patients with spasticity, baclofen is also prescribed off-label for conditions such as alcoholism, gastroesophageal reflux disease, nystagmus, and trigeminal neuralgia. However, instead of being metabolized by the liver, baclofen is eliminated primarily unchanged in the urine, with a step-wise prolongation in the elimination of half-life as kidney function declines, according to the authors.

Baclofen Withdrawal

Baclofen withdrawal from an intrathecal pump presents with hemodynamic instability, increased spasticity, fever and altered mental status. Consider the diagnosis in any patient with an intrathecal pump and the above symptoms.

How baclofen is different from other alcohol addiction treatments

Clearly internet forums don’t replace clinical trials but they provide another source of information on how a medication performs in “the real world” as well as the patient experience of a medication. When I read patient experiences of baclofen treatment, I was struck by how dramatically it changed their relationship with alcohol. Baclofen freed them from constant thinking about and cravings for alcohol. They felt calmer and more in control. They could be around alcohol without it bothering them. I’d never heard anything quite like it.

Safety of baclofen versus tizanidine for older adults with musculoskeletal pain

The results of this study suggest that baclofen is associated with higher incidences of injury and delirium compared to tizanidine when used for the treatment of musculoskeletal pain. Future studies should investigate if these risks are dose-related and include a comparison group not exposed to either drug.

Speaking fluently with baclofen?

Baclofen is a new and promising pharmacological compound for the treatment of alcohol dependence (AD). Although several randomised trials found a reduction of craving and higher abstinence rates with low and high doses of baclofen, others failed to show positive effects. In this case study, the successful treatment of a patient with AD with daily 120 mg of baclofen is described. In addition to a decrease in alcohol use, we observed the cessation of stuttering during treatment with baclofen, reoccurrence of stuttering following discontinuation, and cessation of stuttering after reinstatement of the treatment.

The Use of Baclofen as a Treatment for Alcohol Use Disorder: A Clinical Practice Perspective

Despite controversies regarding the efficacy and justification of the “off-label” use of baclofen treatment for patients with AUD, there is consensus that baclofen is a promising medication to treat moderate to severe AUD. Baclofen plays an important role in the clinical treatment of AUD patients in some European countries and Australia, particularly in patients who are not responsive to the available registered medications and/or in AUD patients with significant liver disease.

Resources

Gablofen

Gablofen, FDA-approved intrathecal baclofen, provides continued symptom relief thanks to targeted drug delivery via a pump.