Mechanism

As mentioned earlier, Baclofen works by selectively binding to the pre-synaptic GABA-type B receptors that leads to several neurological mechanisms related to reducing muscle spasms [6], and this has been shown in various studies [3].

Once taken in tablet oral form, Baclofen is absorbed by the gastrointestinal tract, however, does not cross the blood-brain barrier [3]. It then follows a path where it is excreted by the kidneys, with a half-life of around 5 hours [3].

It is often administered to relieve flexor spasms, which are known as involuntary muscle contractions which are notable with patients suffering from spinal cord issues [8].

Moreover, Baclofen might induce neurological protective effects, along with potential anti-inflammatory properties.

Baclofen & Alcohol Dependence

Baclofen was used to examine its effects in a group of alcohol-dependent patients, with escalating doses of Baclofen given to 100 patients with alcohol dependence [9].

It was found that a large proportion of patients administered Baclofen reported a suppression of alcohol craving [9].

However, side effects reported with Baclofen was reported in 88% of patients, which mainly included fatigue, insomnia and dizziness; and, to a lesser extent, bowel disorder, weight loss, hot flush, mental confusion and sugar craving [9].

Baclofen & Muscle Cramps

Low-dose Baclofen was used in patients who were suffering from muscle cramps as a result of cirrhosis, which is a condition where the liver does not function as normal and leads disease of the liver [10;11].

Subjects as part of the study received 5mg doses of Baclofen. For three times per day for one week. Results showed a safe profile of the low-dose Baclofen given to treat muscle cramps in cirrhosis patients [10].

Baclofen & Muscle Tone

In addition, Baclofen reduces muscle tone [12]. Baclofen should not be used when someone requires proper muscle tone for certain activities and tasks [13].

Dosage

Lioresal recommended daily dosage ranges between 15-80mg, in which it is recommended 15mg/day is started and increased by 5mg every 3 days [5].

Other reports indicate that 75-80mg/day should not be exceeded [7].

Side Effects

Side effects of using Baclofen have been reported to be as drowsiness, along with other side effects such as dizziness, headaches and nausea [14].

Other less known side effects have been described as, dark urine, chest pain, depression, skin rash and itching [14].

Table 1. List of side effects associated with taking Baclofen.

References

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6464193/
2. https://journals.sagepub.com/doi/pdf/10.1177/0883073818785074?casa_token=4VHOdgqF6eQAAAAA:Rp_YMH2C48QN241L3kkvrKeEqnEkzkI38HL4QUF3B3lXL87PBmFkpX5jUwcl3ekaBcklXu6pd361iQ
3. https://www.drugbank.ca/drugs/DB00181
4. https://journal.chestnet.org/article/S0012-3692(15)00060-4/fulltext
5. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6464193/
6. https://www.ingentaconnect.com/contentone/mjl/sreh/2017/00000049/00000003/art00001?crawler=true&mimetype=application/pdf
7. https://www.frontiersin.org/articles/10.3389/fpsyt.2014.00143/full
8. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2771986
9. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3540966/
10. https://aasldpubs.onlinelibrary.wiley.com/doi/full/10.1002/hep.27988
11. https://healthengine.com.au/info/liver-cirrhosis
12. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2857957/
13. https://www.emedicinehealth.com/drug-baclofen/article_em.html
14. https://www.drugs.com/sfx/baclofen-side-effects.html