Lioresal

Lioresal (baclofen) is a centrally-acting skeletal muscle relaxant specifically indicated for the management of 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 pharmacological action makes it a cornerstone therapy for patients experiencing spasticity resulting from multiple sclerosis, spinal cord injuries, and other spinal cord diseases. By reducing muscle tone and frequency of spasms, Lioresal facilitates enhanced comfort, improved range of motion, and greater ease in performing daily activities and therapeutic exercises, ultimately contributing to a better quality of life for affected individuals.

Features

• Active Ingredient: Baclofen
• Pharmacological Class: Gamma-aminobutyric acid (GABA) derivative; GABA-B receptor agonist
• Administration: Oral tablets
• Available Strengths: 10 mg and 20 mg tablets
• Mechanism of Action: Acts primarily at the spinal cord level to inhibit the release of excitatory neurotransmitters
• Prescription Status: Rx-only medication
• Bioavailability: Rapidly and extensively absorbed from the GI tract
• Half-life: Approximately 3–4 hours
• Metabolism: Hepatic (15% of dose)
• Excretion: Primarily renal (70–80% unchanged in urine)

Benefits

• Significantly reduces muscle spasticity and hypertonicity, allowing for improved voluntary movement
• Decreases the frequency and intensity of painful muscle spasms and clonus
• Facilitates enhanced performance of activities of daily living and participation in physical therapy
• May improve bladder function and reduce urinary frequency in some patients with spinal cord-related spasticity
• Can lead to better positioning, seating tolerance, and ease of nursing care
• Potentially reduces the development of contractures and other long-term complications of chronic spasticity

Common use

Lioresal is primarily prescribed for the management 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 spinal cord injuries and other spinal cord diseases, including but not limited to transverse myelitis, spinal cord tumors, and motor neuron disease. The medication may be used in cerebral palsy-related spasticity, though its efficacy for cerebral origin spasticity is less well established. Clinicians may also prescribe it off-label for certain cases of trigeminal neuralgia, intractable hiccups, and alcohol withdrawal symptoms, though these uses require careful specialist supervision.

Dosage and direction

The dosage of Lioresal must be individualized for each patient. The initial recommended dose is 5 mg administered three times daily. This may be increased gradually every three days by 5 mg per dose until the desired effect is achieved. The maximum recommended daily dose is 80 mg (20 mg qid), though some patients may require and tolerate higher doses under strict medical supervision. Doses should be spaced evenly throughout the waking hours. The drug should be taken with food or milk to minimize gastrointestinal upset. For patients with renal impairment, dosage reduction is necessary. Abrupt discontinuation must be avoided due to risk of withdrawal symptoms; tapering should occur by decreasing dosage by 5–10% daily over at least 1–2 weeks.

Precautions

Patients should be cautioned about the potential for drowsiness, dizziness, or blurred vision, which may impair their ability to perform hazardous activities such as driving or operating machinery. Alcohol and other CNS depressants may potentiate these effects. Use with caution in patients with psychiatric disorders, cerebrovascular insufficiency, or autonomic dysreflexia. Renal function should be monitored, and dosage adjustments made accordingly for patients with impaired renal function. Elderly patients may be more sensitive to the effects of Lioresal and typically require lower doses. Patients should be advised not to discontinue therapy abruptly due to risk of hallucinations, seizures, and rebound spasticity.

Contraindications

Lioresal is contraindicated in patients with known hypersensitivity to baclofen or any component of the formulation. It should not be used for the treatment of skeletal muscle spasm resulting from rheumatic disorders. The drug is contraindicated in patients with significant respiratory depression or insufficiency. Use is also contraindicated in patients with active peptic ulcer disease. The intrathecal formulation should not be used for intravenous, intramuscular, subcutaneous, or epidural administration.

Possible side effect

Common side effects (≥1%) include drowsiness (10–63%), dizziness (5–15%), weakness (5–15%), fatigue (5–9%), nausea (4–12%), and hypotension (5–9%). Less frequent adverse reactions may include confusion, headache, insomnia, constipation, urinary frequency, and rash. Serious side effects requiring immediate medical attention include seizures, hallucinations, severe hypotension, respiratory depression, and allergic reactions. Approximately 10% of patients may need to discontinue therapy due to side effects, most commonly drowsiness, dizziness, weakness, and fatigue.

Drug interaction

Lioresal may potentiate the effects of alcohol and other CNS depressants including benzodiazepines, opioids, sedatives, and tricyclic antidepressants. Concurrent use with antihypertensive agents may result in increased hypotensive effects. Caution is advised when administering with MAO inhibitors due to potential enhanced CNS effects. The muscle relaxant effects may be additive with those of tizanidine and other skeletal muscle relaxants. Baclofen may increase blood glucose levels, potentially requiring adjustment of antidiabetic medications.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should never double the dose to make up for a missed one. If multiple doses are missed, patients should contact their healthcare provider for guidance, as dosage adjustment or retitration may be necessary to avoid withdrawal symptoms or recurrence of spasticity.

Overdose

Symptoms of overdose may include vomiting, muscular hypotonia, drowsiness, accommodation disorders, coma, respiratory depression, seizures, and hypothermia. Significant cardiovascular manifestations may include bradycardia, hypotension or hypertension, and conduction disorders. Treatment is primarily supportive and symptomatic, with emphasis on maintaining adequate ventilation, cardiovascular function, and body temperature. There is no specific antidote. Gastric lavage may be considered if performed soon after ingestion. Hemodialysis may be beneficial in removing baclofen, particularly in patients with renal impairment.

Storage

Store at controlled room temperature (20–25°C or 68–77°F) in a tightly closed container. Protect from moisture and light. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Properly discard any unused medication through medication take-back programs or according to FDA-recommended disposal methods (do not flush unless specifically instructed).

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Individual patient responses to Lioresal may vary. Treatment decisions should be made exclusively by qualified healthcare professionals based on comprehensive patient assessment. The prescriber should be familiar with the complete prescribing information and potential risks before initiating therapy. Patients should report any adverse effects to their healthcare provider promptly.

Reviews

Clinical studies have demonstrated that approximately 70-80% of patients with multiple sclerosis or spinal cord injury experience significant improvement in spasticity with Lioresal therapy. Many patients report reduced pain from muscle spasms, improved sleep quality, and enhanced ability to perform self-care activities. Some patients note that side effects, particularly sedation, may be limiting initially but often diminish with continued therapy or dosage adjustment. Physical therapists frequently observe improved range of motion and greater cooperation with therapeutic exercises in patients taking Lioresal. Long-term users emphasize the importance of not missing doses to avoid withdrawal symptoms.