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Baclofen

Baclofen is a centrally acting muscle relaxant commonly used to treat spasticity caused by conditions like multiple sclerosis and spinal cord injuries. It works by activating potassium channels in the spinal cord to reduce muscle spasms, rigidity, pain, and clonus. While some clinical trials found mild ALT elevations in 5% of patients on baclofen, no significant cases of hepatotoxicity have been reported. This is likely because baclofen undergoes minimal hepatic metabolism and is rapidly excreted in urine. Any ALT elevations greater than 10 times normal that persist after stopping treatment should be investigated, but baclofen does not appear to cause cross sensitivity with other muscle relaxants

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411 views2 pages

Baclofen

Baclofen is a centrally acting muscle relaxant commonly used to treat spasticity caused by conditions like multiple sclerosis and spinal cord injuries. It works by activating potassium channels in the spinal cord to reduce muscle spasms, rigidity, pain, and clonus. While some clinical trials found mild ALT elevations in 5% of patients on baclofen, no significant cases of hepatotoxicity have been reported. This is likely because baclofen undergoes minimal hepatic metabolism and is rapidly excreted in urine. Any ALT elevations greater than 10 times normal that persist after stopping treatment should be investigated, but baclofen does not appear to cause cross sensitivity with other muscle relaxants

Uploaded by

amira
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Baclofen

Introduction
Baclofen is a centrally acting muscle relaxant commonly
prescribed for spasticity in patients with multiple
sclerosis. Baclofen has not been convincingly linked to
clinically significant liver injury.
Background
Baclofen (bak' loe fen) is a gamma-amino butyric acid
(GABA) derivative that acts as an agonist of the GABA B
receptor, thereby activating potassium channels and
reducing calcium conductance leading to hypotonia and
muscle relaxation. Baclofen acts primarily at the level of
the spinal cord, inhibiting synaptic reflexes. Baclofen
reduces the number and severity of muscle spasms and
relieves pain, clonus and muscle rigidity due to spasticity.
Baclofen is indicated primarily for treatment of spasticity
from spinal cord injuries and multiple sclerosis. It has
been used off label as adjunctive therapy to help with
alcohol abstinence and withdrawal. Baclofen was
approved for use in the United States in 1977 and is
widely used with more than 3 million prescriptions filled
yearly. Baclofen is available in various generic forms as
well as under the brand names of Lioresal and Remular in
tablets of 10 or 20 mg and in formulations for intrathecal
injections of 0.5 mg/mL. The recommended adult dose
for spasticity is 10 to 20 mg orally three to four times
daily. The dose should be increased and tapered
gradually. The most common side effects of baclofen are
nausea, drowsiness, confusion, dizziness and fatigue.
Hepatotoxicity
Limited data are available on the potential hepatotoxicity
of baclofen. Among the many clinical trials evaluating the
safety and efficacy of baclofen, none mention hepatic
toxicity or rates of serum ALT elevations occurring during

chronic therapy. The product insert mentions that 5% of


patients develop mild serum aminotransferase elevations,
but little documentation is available on the significance,
severity or duration of these abnormalities. No convincing
cases of clinically apparent baclofen hepatotoxicity with
symptoms or jaundice have been published.
Mechanism of Injury
The apparent absence of significant hepatotoxicity from
baclofen may be due to its minimal hepatic metabolism
(~15%) and rapid urinary excretion.
Outcome and Management
The minor ALT elevations associated with chronic baclofen
use are usually asymptomatic and transient. Any
elevation of greater than 10 times the upper limit of
normal or persistence of abnormalities greater than 5
times the upper limit of normal should lead to
discontinuation. There is no reason to suspect cross
sensitivity to liver injury among the various muscle
relaxants.
Side effects
Feeling sick, tiredness, drowsiness, problems with
eyesight, weakness, dizziness, light-headedness,
headache, dry mouth, breathing difficulties, aching
muscles, sleeplessness or nightmares, feeling anxious
or agitated, confusion, unsteadiness, increased need to
pass urine, shakiness, increased sweating, and skin
rash.

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