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Home Antidepressants Baclofen
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Baclofen

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Summary

Summary

Lioresal, or as its marketed as Baclofen, is known as an agonist of the gamma-aminobutyric acid type B receptor [1] and first synthesised in the 1960s [2]. It became an FDA-approved drug in 1992 [3].

Originally approved for the treatment of spasticity in neurological conditions and spinal cord lesions, Baclofen has recently been used for the treatment of alcohol dependence [4;5]. In addition, Baclofen is known to have muscle-relaxant properties [4].

Baclofen chemical structure

Detailed

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

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].

Safety

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.

 

Side effects
Most common Less common Overdose
Dizziness

Nausea

Abdominal pain

Unsteadiness

Diarrhoea

Headache

Low blood pressure

Numbness

Blurred vision

Seizures

Muscle weakness

Vomiting

References

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

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