Lioresal: Targeted Spasticity Relief for Enhanced Mobility
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Synonyms | |||
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 mechanism of action makes it a first-line pharmacological agent for alleviating the muscle hypertonia, painful spasms, and clonus associated with conditions like multiple sclerosis, spinal cord injuries, and other spinal pathologies. By reducing spasticity, Lioresal facilitates improved range of motion, ease of movement, and overall patient comfort, supporting rehabilitative efforts and activities of daily living.
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, leading to suppression of excitatory neurotransmitter release and inhibition of 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.
Benefits
- Significant Reduction in Muscle Tone: Effectively decreases velocity-dependent resistance to stretch, alleviating the rigidity and stiffness characteristic of upper motor neuron syndrome.
- Decreased Frequency and Intensity of Painful Spasms: Suppresses the sudden, involuntary muscle contractions that can cause significant discomfort and sleep disruption.
- Improved Functional Capacity and Ease of Care: Enhanced passive and active range of motion can facilitate physiotherapy, improve mobility for transfers and walking, and simplify nursing care and hygiene.
- Potential for Improved Quality of Life: By mitigating the primary physical symptoms of spasticity, patients may experience less pain, better sleep, and a greater ability to participate in daily activities.
- Flexible Administration Routes: The availability of both oral and intrathecal formulations allows for tailored treatment strategies, from systemic management to highly targeted, potent delivery for severe cases.
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 spinal cord injuries and other spinal cord diseases, such as transverse myelitis, cervical spondylosis, and amyotrophic lateral sclerosis (ALS). Its use is contingent upon a clear diagnosis of spasticity of spinal origin, and a demonstrated reversible component to the spasticity, where the therapeutic benefits of reduced muscle tone outweigh any associated reduction in muscle function required for voluntary movement or posture.
Dosage and direction
Dosage must be individualized for each patient. Therapy should be initiated at a low dosage and increased gradually until the optimum effect is achieved, typically defined as a significant reduction in spasticity without unacceptable side effects, particularly sedation and muscle weakness.
- Initial Adult Dose: 5 mg orally three times a day.
- Titration Schedule: The dosage may be increased by 5 mg per dose every three days to a maximum of 20 mg four times a day (80 mg daily). The most commonly effective dose range is 40-80 mg daily divided into four doses.
- Dosage in Children: The use of oral Lioresal in children under 12 years of age is not recommended. For children 12 years and older, dosing is similar to adults, starting at 5 mg three times daily.
- Administration: Tablets should be taken with a glass of water, with or without food. If gastrointestinal upset occurs, administration with food or milk is advised.
- Discontinuation: Abrupt cessation of Lioresal, especially after long-term high-dose therapy, must be avoided due to the risk of withdrawal syndrome, including hallucinations, seizures, and rebound spasticity. Dosage should be tapered slowly under medical supervision (e.g., reduce dose by 5-10 mg/day each week).
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: Lioresal may lower the seizure threshold. Use with caution in patients with a history of seizures or EEG abnormalities. A history of stroke or cerebral palsy may also increase seizure risk.
- Psychiatric and Cognitive Effects: Patients should be cautioned about the potential for drowsiness, sedation, dizziness, and confusion, which may impair the ability to operate machinery or drive a motor vehicle. These effects are potentiated by alcohol and other CNS depressants.
- Autonomic Dysreflexia: In patients with spinal cord lesions at T6 or above, Lioresal withdrawal may precipitate an autonomic dysreflexia crisis.
- Pregnancy and Lactation: Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Baclofen is excreted in human milk; caution is advised if administering to a nursing woman.
Contraindications
Lioresal is contraindicated in patients with a known hypersensitivity to baclofen or any component of the formulation.
Possible side effect
The most frequent adverse reactions are transient drowsiness, dizziness, weakness, and fatigue. Side effects are often dose-related and may diminish with time.
- Very Common (>10%): Drowsiness/sedation, dizziness, fatigue, nausea.
- Common (1-10%): Headache, insomnia, confusion, hypotension, constipation, urinary frequency.
- Uncommon (0.1-1%): Dry mouth, anorexia, taste disorder, blurred vision, nystagmus, euphoria, depression, hallucinations, rash, sweating, impotence.
- Rare (<0.1%): Seizures (especially on withdrawal), syncope, respiratory depression, hepatic dysfunction, muscle pain.
Drug interaction
- CNS Depressants (e.g., Alcohol, Benzodiazepines, Opioids, Sedating Antihistamines): Additive effects on CNS depression, leading to increased sedation, dizziness, and respiratory depression.
- Antihypertensive Agents: May potentiate the hypotensive effects of baclofen.
- Levodopa and Carbidopa: Reports of mental confusion, agitation, and hallucinations in Parkinson’s patients taking baclofen concurrently.
- MAO Inhibitors and Tricyclic Antidepressants: May exacerbate CNS depressive and cardiovascular effects.
- Lithium: May increase lithium toxicity.
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. The patient should not double the next dose to “catch up.”
Overdose
Manifestations of overdose are primarily an exacerbation of the drug’s pharmacological effects, notably profound drowsiness, lightheadedness, vomiting, dilated pupils, hypothermia, seizures, coma, and respiratory depression. Hypotension and bradycardia may occur. Management is primarily supportive and symptomatic. There is no specific antidote. Ensure a patent airway and provide ventilatory support. Gastric lavage may be considered if performed soon after ingestion. Hemodialysis may be beneficial in removing the drug, especially in patients with renal impairment.
Storage
Store at room temperature (20°C to 25°C or 68°F to 77°F), in a tight, light-resistant container. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Do not flush unused medication; dispose of it according to local guidelines or through a medicine take-back program.
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 any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
“After my spinal cord injury, the constant spasms in my legs were debilitating. Starting on Lioresal was a turning point in my rehabilitation. The reduction in tone allowed my physiotherapist to work with me effectively, and I finally regained some meaningful control and comfort.” – M.S., 48
“As a neurologist specializing in MS, Lioresal remains a cornerstone of our spasticity management protocol. Its predictable pharmacokinetics and dose-response relationship allow for fine-tuned control of symptoms. The key is careful, slow titration to find the ‘sweet spot’ where function is improved without inducing significant weakness.” – Dr. E.R., Neurologist
“The drowsiness was significant when I first started, and we almost stopped. My doctor advised we stick with a lower dose for a full two weeks, and I’m glad we did. The sedation faded, and the relief from the painful cramping in my back and legs has been life-changing. Patience is crucial.” – J.K., 52