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Baclofen

Baclofen (brand names Kemstro® and Lioresal®) is a derivative of gamma-aminobutyric acid, and is an agonist specific to mammalian but not fruit fly (Drosophila) GABA_B receptors. It is used for the treatment of spastic movement, especially in instances of spinal cord injury and in multiple sclerosis. Its beneficial effects result from actions at spinal and supraspinal sites. Baclofen can also be used to treat hiccups. more...

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Description of compound

Baclofen is a white to off-white, odorless or practically odorless crystalline powder, with a molecular weight of 213.66. It is slightly soluble in water, very slightly soluble in methanol, and insoluble in chloroform.

Routes of administration

Baclofen can be administered either orally or intrathecally (directly into the spinal fluid). Intrathecal administration is often indicated in spasticity patients, as very little of the oral dose actually reaches the spinal fluid.

Intrathecal administration is particularly used in patients with multiple sclerosis who have severe painful spasms which are not controllable by oral baclofen. A test dose is given to assess the effect, and if successful a chronic intrathecal catheter in inserted and connected to a computer-controlled implanted pump. The reservoir in the pump can be replenished by percutaneous injuection. These pump systems are quite sophisticated and expensive so careful patient selection is required.

History

Historically Baclofen was designed to be a drug for epilepsy in the 1920’s, and was derived from diazepam (Valium©). The effect on epilepsy was disappointing but it was found that in certain patients spasticity decreased. Baclofen was and is still given orally with variable effects. In the severely affected children, the oral dose is so high that side effects appear and the treatment loses its benefit. How and when Baclofen came to be used in the spinal sack is not really clear but this is now an established method for the treatment of spasticity in many conditions.

How Baclofen works

Baclofen has its effect in the spinal cord, which is the main connection between the brain and then rest of the body. The spinal cord is a reflex system, a feedback loop. The most obvious reflex is the withdrawal to heat. This movement is brisk and not very well controlled. This is what happens in Cerebral Palsy. Without adequate control from the brain, every movement is like a reflex, being rough and uncontrolled. The reflex can spread through the body causing spasms or “arching”. These spasms can be painful and interrupt sleep.

Baclofen works on this reflex circuit. The reflex circuit in the spinal cord contains the Renshaw cells. These cells are very sensitive to a natural chemical produced by the nervous system: GABA, gamma-amino-butyric-acid. GABA slows the reflex circuit down and Baclofen acts like GABA. The dose of intrathecal Baclofen necessary to slow down the reflex circuit is variable but is generally one thousand times smaller than the oral dose.

Pharmacokinetics

The drug is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low and the drug is predominantly excreted in the unchanged form by the kidneys.

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Baclofen in outpatient treatment of alcohol withdrawal syndrome
From Journal of Family Practice, 1/1/05 by Giovanni Addolorato

TO THE EDITOR:

We read with great interest the article by Asplund et al ("3 Regimens for alcohol withdrawal and detoxification," J Fam Pract 2004; 53:545-554) about regimens in the treatment of alcohol withdrawal syndrome (AWS). The authors underline that inpatient treatment is significantly more costly than outpatient treatment, and they also correctly suggest that in an outpatient setting, most patients experience greater social support and the freedom to continue working or maintain their daily lives.

Regarding pharmacotherapy, the authors correctly state that benzodiazepines are the treatment of choice for AWS; they also suggest the anticonvulsants carbamazepine and valproic acid as alternatives. Moreover, they cite other types of medications such as alpha-adrenergic agonists, betablockers, and calcium channel blockers.

However, among the new drugs potentially useful in AWS treatment, the authors do not mention baclofen. Our group recently showed that baclofen, a GABA(B) receptor agonist, is able to suppress alcohol withdrawal symptoms, both in animals (1) and in humans. (2,3) It is also effective in reducing voluntary alcohol intake in alcohol-preferring rats, (3) and alcohol craving and intake in alcoholics. (4,5) Baclofen-treated alcoholic patients showed no serious side effects, and no patients reported craving for the drug or needed an increase in the dose. (2-5) These data have been recently replicated by Flannery and collegues. (6)

Moreover, regarding AWS treatment in an outpatient setting, we have shown that baclofen is able to rapidly suppress AWS symptoms--after the first administration--and so baclofen-treated patients reported a rapid improvement in well-being and resolution of psychological distress. Consequently, patients were able to return home in a short time; moreover, because all patients underwent therapy with baclofen in an outpatient setting, the cost of treatment was very low. (2)

We think baclofen is a promising drug in the clinical treatment of alcoholism, particularly given the possibility of using it singly instead of many different drugs, (2,3) and in maintaining long-term abstinence. (4,5) Although future investigations are needed to confirm the safety and efficacy of baclofen in the treatment of AWS, its use in treating alcohol-dependency merits further investigation. (7)

REFERENCES

(1.) Colombo G, Agabio R, Carai MAM, et al. Ability of baclofen in reducing alcohol intake and withdrawal severity: I. preclinical evidence. Alcohol Clin Exp Res 2000; 24:58-66.

(2.) Addolorato G, Caputo F, Capristo E, et al. Rapid suppression of alcohol withdrawal syndrome by baclofen. Am J Med 2002; 112:226-229.

(3.) Addolorato G, Leggio L, Abenavoli L, et al. Suppression of alcohol delirium tremens by baclofen administration: a case report. Clin Neuropharmacol 2003; 26:258-262.

(4.) Addolorato G, Caputo F, Capristo E, Colombo G, Gessa GL, Gasbarrini G. Ability of Baclofen in reducing alcohol craving and intake: II. preliminary clinical evidence. Alcohol Clin Exp Res 2000; 24:67-71.

(5.) Addolorato G, Caputo F, Capristo E, et al. Baclofen efficacy in reducing alcohol craving and intake: a preliminary double-blind randomized controlled study. Alcohol Alcohol 2002; 37:504-508.

(6.) Flannery BA, Garbutt JC, Cody MW, et al. Baclofen for alcohol dependence: a preliminary open-label study. Alcohol Clin Exp Res (in press).

(7.) National Institute on Alcohol Abuse and Alcoholism. Neuroscience research and therapeutic targets. Alcohol Alert 2004; 61:1-6.

Giovanni Addolorato, MD, Lorenzo Leggio, MD, Ludovico Abenavoli, MD, Fabio Caputo, MD, and Giovanni Gasbarrini, MD, Institute of Internal Medicine, Catholic University of Rome, Italy. E-mail: g.addolorato@rm.unicatt.it.

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