Lioresal (baclofen) is a centrally-acting skeletal muscle relaxant specifically indicated for the management of severe spasticity. It is a gamma-aminobutyric acid (GABA) derivative that acts as an agonist at GABA-B receptors, primarily at the spinal cord level, to inhibit monosynaptic and polysynaptic reflex transmission. This mechanism of action makes it a cornerstone therapy for patients experiencing the debilitating muscle spasms, clonus, and pain associated with conditions like multiple sclerosis, spinal cord injuries, and other spinal pathologies. By effectively reducing hypertonicity, Lioresal facilitates significant improvements in daily function, comfort, and range of motion, allowing for enhanced participation in physical therapy and rehabilitation programs.

Features

• Active Pharmaceutical Ingredient: Baclofen.
• Pharmacologic Class: Gamma-aminobutyric acid (GABA) derivative; centrally-acting skeletal muscle relaxant.
• Primary Mechanism of Action: Agonist activity at GABA-B receptors, suppressing the release of excitatory neurotransmitters and inhibiting reflex arcs at the spinal level.
• Available Formulations: Oral tablets (10 mg and 20 mg) and intrathecal solution for infusion via an implanted pump.
• Prescription Status: Available by prescription only, requiring careful medical supervision for initiation and titration.

Benefits

• Significant Reduction in Muscle Spasticity and Spasms: Directly targets the neurological origin of spasticity, leading to a measurable decrease in muscle tone and the frequency and intensity of painful spasms.
• Enhanced Functional Capacity and Mobility: By alleviating rigidity, patients often experience improved ability to perform activities of daily living (ADLs), participate more effectively in physiotherapy, and achieve greater independence.
• Alleviation of Associated Pain and Discomfort: Reduces the pain directly caused by persistent muscle contractions and spasms, contributing to an improved overall quality of life.
• Decreased Muscle Resistance to Passive Movement: This allows caregivers and healthcare providers to perform necessary hygiene and positioning tasks with greater ease, reducing the risk of complications like contractures and pressure sores.
• Well-Established Efficacy and Safety Profile: As a long-standing first-line treatment, its effects and side effect management are well-documented in neurological and rehabilitative medicine.

Common use

Lioresal is primarily prescribed for the management of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. It is also indicated for patients with spasticity due to spinal cord injuries and other spinal cord diseases (e.g., transverse myelitis, amyotrophic lateral sclerosis). Its use is reserved for patients for whom spasticity causes significant interference with daily function, sleep, or hygiene. Treatment is typically part of a comprehensive management plan that includes physical and other rehabilitative therapies.

Dosage and direction

Dosage must be individualized for each patient. The goal is to achieve the optimal therapeutic effect with the fewest side effects.

• Initial Dose: The initial dose for adults is 5 mg administered orally three times a day.
• Titration: The dosage may be increased by 5 mg increments every three days to a effective and tolerated level. A common therapeutic dosage ranges from 40 mg to 80 mg daily administered in divided doses.
• Maximum Dose: The total daily dose should not exceed 80 mg (20 mg q.i.d.).
• Dosing Schedule: To be taken with meals or milk to minimize potential gastrointestinal upset.
• Discontinuation: Abrupt withdrawal of Lioresal must be avoided, as it can precipitate hallucinations, seizures, and a rebound severe spasticity. Dosage should be reduced gradually over a period of at least one to two weeks under medical supervision.
• Intrathecal Administration: Dosing for intrathecal delivery via an implanted pump is entirely different and is determined through a screening trial. It is managed exclusively by specialists trained in the procedure.

Precautions

• Renal Impairment: Baclofen is primarily excreted unchanged by the kidneys. Dosage reduction is necessary in patients with impaired renal function to prevent accumulation and toxicity.
• Seizure Disorders: Use with caution in patients with a history of seizures or EEG abnormalities, as deterioration in seizure control and EEG has been reported.
• Stroke Patients: Efficacy for spasticity from cerebral origin (e.g., stroke) is less well-established, and patients may experience more sedation and weakness, which could obscure the neurological assessment of their condition.
• Psychiatric Disorders: Caution is advised in patients with psychiatric disorders or confusional states, as the drug can exacerbate these conditions.
• Autonomic Dysreflexia: Patients with spinal cord injury at T6 or above should be monitored for autonomic dysreflexia, as Lioresal can affect the presentation of this serious condition.
• Pregnancy and Lactation: Should be used during pregnancy only if clearly needed. Baclofen is excreted in human milk; a decision should be made whether to discontinue nursing or discontinue the drug.

Contraindications

Lioresal is contraindicated in patients with a known hypersensitivity to baclofen or any component of the formulation.

Possible side effect

The most common side effects are transient and dose-related, often subsiding with continued therapy or dosage reduction.

• Very Common (>10%): Drowsiness, sedation, dizziness.
• Common (1-10%): Weakness, fatigue, insomnia, headache, confusion, nausea, constipation, hypotension.
• Uncommon (0.1-1%): Depression, hallucinations, euphoria, muscle pain, urinary frequency, rash, dry mouth, blurred vision, nystagmus, tinnitus, taste alteration.
• Rare (<0.1%): Seizures (especially on withdrawal), respiratory depression, syncope, elevated liver enzymes, severe hypersensitivity reactions.

Drug interaction

• CNS Depressants (Alcohol, Opioids, Benzodiazepines, Sedating Antihistamines): Concomitant use can result in additive sedative effects, profound drowsiness, respiratory depression, and dizziness. Extreme caution is warranted.
• Antihypertensive Agents: May potentiate the effects of drugs used to treat hypertension, leading to excessive hypotension.
• Levodopa-Carbidopa: Reports of worsened psychosis, confusion, and hallucinations in Parkinson’s disease patients taking both medications.
• MAO Inhibitors and Tricyclic Antidepressants: May increase CNS depressive effects.
• Lithium: May enhance the hyperkinetic effects of lithium.

Missed dose

If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. Do not double the dose to “catch up.”

Overdose

Overdose manifests as a profound exaggeration of Lioresal’s known pharmacological effects.

• Signs and Symptoms: Severe drowsiness, lightheadedness, dizziness, vomiting, dilated pupils, hyporeflexia, seizures, coma, respiratory depression, and bradycardia.
• Management: There is no specific antidote. Management is primarily supportive and includes securing the airway, ensuring adequate ventilation, and maintaining cardiovascular function. Gastric lavage may be considered if performed soon after ingestion. Hemodialysis may be beneficial, especially in patients with renal impairment.

Storage

• Store at room temperature (20°C to 25°C or 68°F to 77°F), away from light, moisture, and heat.
• Keep in the original container, tightly closed.
• Keep out of reach of children and pets.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting or altering any treatment regimen. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

“Lioresal has been a game-changer for my MS-related spasticity. The muscle tightness and painful cramps that used to keep me up at night are significantly reduced. It took some time to find the right dose with my neurologist to minimize the initial drowsiness, but the functional improvement has been worth it.” – M.S., Patient

“As a physiatrist, Lioresal is a fundamental tool in our spasticity management arsenal. When titrated correctly, it effectively lowers muscle tone, which directly translates to better range of motion for our patients and allows for more productive therapy sessions. We always emphasize the critical importance of not stopping the medication abruptly.” – Dr. A.L., Specialist in Physical Medicine and Rehabilitation