An FDA approved, prescription muscle relaxant, baclofen has exponentially risen in popularity and use over the past decade. However, the reasons for its popularity don’t quite have FDA’s stamp of approval yet – or at all. Increasingly preferred for the treatment of alcohol withdrawal syndrome and other illicit drug dependencies, such as opioid, cocaine, and tobacco abuse, the off-label use of baclofen has been causing a stir. Amongst other things, here we take an in-depth look at what baclofen is, its neurochemistry and mode of action, use, abuse, and recovery options.
What is Baclofen?
Baclofen is a potent, prescription muscle relaxant primarily prescribed for the treatment of spasticity brought on by conditions such as multiple sclerosis and other disorders affecting the spinal cord. Introduced in 1971, baclofen was originally created to treat severe epileptic seizures. However, a lack of effect on the seizure activity itself and the discovery of minimization of muscle spasticity led to the drug being approved for use to control irregular and severe muscle spasm such as those followed by epileptic seizures.
The Neurochemistry and Pharmacokinetics of Baclofen
A stereo-selective γ-aminobutyric acid and (GABA)-B receptor agonist, baclofen is a drug which directly affects GABA’s activity – a major inhibitory neurotransmitter that acts on the central nervous system. By activating GABA, baclofen works to effectively minimize the exaggerated reflexes and muscle tone during spastic reactions caused due to traumatic spinal lesion and spinal degeneration and damage. It inhibits the synaptic transmission within the spinal cord by reducing the excitatory exchange through synapses. Furthermore, it directly inhibits the release of the excitatory neurotransmitters as well as the inhibitory synaptic transmission.
Baclofen Prescription Information
Available in the form of 10mg or 20mg tablets, both baclofen 10mg and 20 mg are commonly administered orally. However, it can be administered intrathecally for the treatment of cerebral spasticity. Quickly absorbed through the GI tract, the peak plasma concentration of baclofen is achieved in one to three hours after administration. The plasma half-life of the drug is between two and four hours, with it undergoing little to no liver metabolism. Instead, it is primarily excreted through renal metabolism unchanged within 24 hours after the administration of the first dose. The ideal baclofen dosage varies from patient to patient, though the maximum dose per 24 hours should not exceed 80mg. Baclofen is also available in the form of compounding powders and oral suspensions.
Available as Lioresal, Glabofen, and Kemstro, the primary use of baclofen today is indicated for the treatment of the following conditions:
- Spinal cord injury
- Spinal nerve damage
- Brain injury
- Trigeminal neuralgia
- Cerebral palsy
- Nocturnal myoclonus
Its contraindications include hypersensitivity, skeletal muscle spasms caused by rheumatic disorders, stroke, and Parkinson’s disease.
Baclofen has not yet been established as a pediatric-friendly drug. As such, is not recommended for prescription purposes in children under the age of 12. The drug is also known to cross the placental barrier with the potential to adversely affect the fetus’s development. Small quantities of baclofen are also known to pass through breast milk; as such, the drug is not indicated for use by pregnant or postpartum mothers. Due to its renal metabolism, baclofen can be used with caution in patients with impaired renal function in cases where there are chances of further damage. This potent muscle relaxant has a depressive effect on the central nervous system, thus interaction with other CNS suppressants might augment the sedative, depressive effects, making it hazardous for patients to operate heavy machinery while under the influence of the drug.
Baclofen as an Addiction Aid
Baclofen has been increasingly touted as a promising addiction cure for the past decade or so. A prescription medication used to treat muscle spasticity symptoms, the drug began to be used as an addiction aid when in 2004,French cardiologist, Olivier Ameisen, used himself as a guinea pig to test the drug’s effectiveness against alcohol addiction. According to research experiments conducted after Ameisen’s revolutionary discovery and the subsequent rise in the off-label prescription of baclofen in France, it was demonstrated that the GABA-B receptor agonist had the potential to suppress the release of dopamine (reward motivating neurotransmitter) stimulated by increased alcohol consumption. Baclofen exerts an inhibitory response on the dopamine neurons, effectively causing a marked decrease in the alcohol-reinforced, dopamine-mediated behaviors. Furthermore, the administration of the muscle relaxant in high doses was found to have a significant inhibitory effect on the symptoms of alcohol withdrawal syndrome. Preliminary clinical studies also demonstrated baclofen’s ability to reduce alcohol craving, thus allowing for reduced alcohol intake. A comparative study also concluded the equivalency of baclofen’s efficacy to that of the ‘gold standard’ diazepam for the treatment of alcohol withdrawal syndrome and it’s mild to moderate symptoms. Furthermore, it was found that the drug baclofen had proven successful in the detoxification, treatment, and management of other illicit substances of abuse, such as opioid drugs and cocaine. A randomized study discovered that baclofen, when used dose-dependently, has the potential to also effectively decrease the heroin-induced dopamine release, thereby negating the reinforcing properties of the drug. It has further been found that this drug also minimizes the severity of the opioid withdrawal symptoms and can be used as an effective drug to control the opioid dependence.
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The Potential For Abuse
However, despite the positive results and indications of the drug for addiction and other drug dependency treatments, it was found that baclofen abuse is a definite possibility especially given the use of extremely high doses of the medication when used as an addiction aid. When patients were allowed the uninhibited use of baclofen, in unlimited dose ranges, they reported an effortless decrease in the alcohol dependence and craving. While rare, with minimal data, it has been reported that baclofen can have a stimulant effect on patients who take the drug in higher doses than advised, especially in alcoholics. Furthermore, it was also found that the combined effects of the drug with nicotine (through cigarette consumption), diminished palatability of nicotine but increased the potential for baclofen abuse by creating a psychological and physical dependence. The issue with treating any kind of addiction with baclofen is tri-fold. One is that it is only treating the symptoms of addiction, not the addiction itself. For true addiction cure, it is necessary that the patient is provided with sufficient complementary therapy and necessary adjunctive rehab to completely eliminate the addiction. Two, there is a high possibility of baclofen replacing the addiction modality, instead of treating it. And three, there are grave adverse effects of its treatment through small doses prescribed for long-term use, with the possibility of developing extreme baclofen toxicity and even overdose at higher doses. In fact, patients treated by this drug for alcohol abuse in a study to monitor the suppression of alcohol dependence over a two-year period found that baclofen was not so effective in low doses. It also showed that baclofen side effects were unbearable at optimal ranges, which were significantly higher than recommended dosage per 24-hour period.
The Adverse Effects of Baclofen Treatment
Baclofen, though a very effective medication for the treatment of muscle spasticity, has severe adverse effects that can be particularly debilitating for patients. The baclofen side effects, though often cited as transient, include the following:
- Profound, generalized weakness
- Muscle contractions and trembling
- Water retention
- Sexual changes
- Appetite changes
- Memory loss
- Urine incontinence
- Mental confusion
- Increased sugar cravings
- Weight loss
- Skin rashes
- Increased generalized itchiness
- Bowel changes (both diarrhea or constipation)
- Irregular heart rate
- Chest pain
- Shortness of breath
Baclofen is a GABA receptor agonist; meaning that it activates GABA’s inhibitory action. Due to its high therapeutic use for muscle spasticity, off-label use for addiction treatment, and high potential for addiction and abuse, there is a definitive possibility of a baclofen overdose. Aggravating its side effects, the common signs and symptoms of baclofen overdose include:
- Hypoventilation and respiratory depression
- Central depression and coma
- Acute delirium
- Facial hematomas
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Baclofen Addiction Treatment Options
Baclofen abuse is a grave concern, primarily due to the severe side effects of the drug when consumed in large doses, unmonitored within a 24-hour period. The addiction potential for this drug is also a cause to seek immediate addiction treatment due to the extreme severity of the withdrawal symptoms caused by both the abrupt and the tapered cessation of baclofen. Some of the most common withdrawal symptoms recorded in patients after abrupt cessation of baclofen administration include, but are not limited to the following:
- Mild to moderate muscular spasms
- Auditory, visual, and tactile hallucinations
- Mental confusion
- Memory impairment and consciousness fluctuation
- Extreme muscular rigidity
- Multi-organ failure
- Fatal seizures or convulsions
Withdrawal symptoms upon tapered cessation of baclofen include:
- High cravings for the drug
- Increased tremors of the extremities
- Increased agitation
Luckily, there are a number of ways to successfully treat baclofen addiction through various addiction support programs. If a loved one is suffering from baclofen addiction or is displaying drug abuse behavior, it is highly recommended that they seek formal treatment to successfully combat the addiction. The various treatment options for baclofen abuse include, but are not limited to the following:
- Outpatient Treatment
- Support Groups
- Aftercare and Recovery
Detoxification is the first line of treatment for a baclofen abuse issue. It is the step that helps wean a patient off baclofen in a controlled environment in order to purge the body of the drug content. The detoxification phase only begins after a thorough evaluation and assessment of the patient for the determination of the addiction level through the initial screening process. The treatment only begins once a confirmed addiction diagnosis has been provided. Given the severely adverse withdrawal effects on both abrupt and tapered cessation, it is highly recommended that patients seeking treatment for substance abuse against baclofen should be monitored consistently by a licensed medical professional. The outpatient treatment option for baclofen addiction allows the patient to continue residing in their own home, all the while attending intensive rehab programs on a regular basis at the rehabilitation center of choice. An intensive outpatient program provides addiction accountability and a chance for much-needed recovery at the same time under strict medical monitoring, without compromising the patient’s ability to maintain their personal and professional lives. Support groups exist for the treatment of substance abuse patients, which provide both social and medical support required for them to successful work towards their sobriety. The aftercare and recovery options for baclofen abuse and addiction include therapy and long-term association with support groups, where their progress is routinely monitored for as long as the patient chooses to attend. Baclofen has the potential to help people with substance abuse to fight off their addiction, provided that they opt for complementary treatments and therapies to cure the problem. However, it is important that doctors do not prescribe the drug for long-term use as it can lead to high toxicity build up in the body.
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