Lioresal: Targeted Spasticity Relief for Improved 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 reducing muscle spasticity resulting from multiple sclerosis, spinal cord injuries, and other spinal cord diseases. By diminishing the frequency and amplitude of muscle spasms, Lioresal facilitates enhanced patient comfort, improved range of motion, and greater capacity for participation in physiotherapy and activities of daily living.
Features
- Active Ingredient: Baclofen
- Pharmacologic Class: Gamma-aminobutyric acid (GABA) derivative; GABA-B receptor agonist
- Available Formulations: Oral tablets (10 mg, 20 mg) and Intrathecal solution for pump delivery
- Mechanism of Action: Acts pre-synaptically to inhibit the release of excitatory neurotransmitters; reduces monosynaptic and polysynaptic reflex activity at the spinal level
- Half-life: Approximately 2.5 to 4 hours in plasma
- Metabolism: Hepatic (15% of dose); primarily excreted unchanged by the kidneys (70-80%)
- Bioavailability: Well-absorbed from the GI tract
Benefits
- Reduces Muscle Spasticity: Effectively decreases the frequency and severity of muscle spasms, clonus, and associated pain.
- Improves Functional Mobility: Enhances voluntary motor function, facilitating greater range of motion and ease of movement.
- Supports Rehabilitation: Allows for more effective participation in physical therapy by reducing resistance to passive stretch.
- Enhances Comfort and Quality of Life: Alleviates discomfort related to spasticity, improving sleep and daily living activities.
- Customizable Delivery: Availability of intrathecal formulation allows for targeted therapy in severe, refractory cases with reduced systemic side effects.
- Well-Established Safety Profile: Decades of clinical use with a well-understood side effect and pharmacokinetic profile.
Common use
Lioresal is primarily prescribed for the management of spasticity of voluntary muscle. Its most common applications include treatment of spasticity associated with:
- Multiple sclerosis (particularly for relieving flexor spasms and concomitant pain, clonus, and muscular rigidity)
- Spinal cord injuries and diseases (including traumatic spinal cord injury, transverse myelitis, and spinal cord tumors)
- Other neurological conditions manifesting spasticity, such as cerebral palsy and amyotrophic lateral sclerosis (ALS)
It is important to note that Lioresal is not indicated for the treatment of skeletal muscle spasm resulting from rheumatic disorders. The efficacy in stroke-related spasticity is less well-established, and clinical judgment is required.
Dosage and direction
Initial Dosing: Therapy should be initiated at low doses and gradually titrated upward to achieve optimal therapeutic effect with minimal adverse reactions.
- Adults: Start with 5 mg orally three times daily. May increase by 5 mg per dose every 3 days to a maximum of 80 mg daily (20 mg qid), as tolerated.
- Children (age 12 and above): Use adult dosing guidelines.
- Children (under age 12): Safety and efficacy not established for oral administration.
Maintenance Dosing: The effective dose typically ranges between 40-80 mg daily divided into 4 doses. Doses exceeding 80 mg daily provide additional benefit only in exceptional cases.
Intrathecal Administration: Reserved for severe spasticity unresponsive to oral therapy or when intolerable side effects limit oral dosing. Requires implantation of a programmable pump and careful titration by specialists familiar with this delivery method.
Administration Instructions: Tablets should be taken with food or milk to minimize gastrointestinal upset. Doses should be spaced evenly throughout waking hours.
Discontinuation: Abrupt withdrawal must be avoided due to risk of rebound spasticity, hallucinations, and seizures. Taper gradually over 1-2 weeks (or longer for high-dose therapy).
Precautions
- Renal Impairment: Baclofen is primarily renally excreted. Dose reduction is necessary in patients with impaired renal function (CrCl <60 mL/min).
- Hepatic Impairment: Use with caution; monitor for increased sedation.
- Psychiatric Disorders: May exacerbate pre-existing psychiatric conditions; use with caution in patients with schizophrenia, confusional states, or psychosis.
- Seizure Disorders: May lower seizure threshold; monitor patients with epilepsy closely.
- Elderly Patients: Increased sensitivity to CNS effects; initiate at lower doses and titrate slowly.
- Pregnancy: Category C; use only if potential benefit justifies potential risk to fetus.
- Breastfeeding: Baclofen is excreted in human milk; decision to discontinue nursing or drug should consider importance of drug to mother.
- Operational Warning: May impair mental and/or physical abilities required for hazardous tasks (driving, operating machinery).
Contraindications
- Hypersensitivity to baclofen or any component of the formulation
- Active peptic ulcer disease (relative contraindication due to potential GI effects)
- History of autonomic dysreflexia (careful monitoring required)
- Concurrent use with other CNS depressants (unless closely monitored)
- Intrathecal administration in patients with infection at pump implantation site
Possible side effect
The most frequently reported adverse reactions are transient drowsiness, dizziness, and weakness, which often diminish with continued therapy.
Common (≥10%):
- Somnolence (10-63%)
- Dizziness (5-15%)
- Weakness (5-15%)
- Nausea (4-12%)
- Fatigue (5-11%)
Less Common (1-10%):
- Headache
- Insomnia
- Constipation
- Dyspnea
- Hypotension
- Urinary frequency
- Confusion
- Dry mouth
Rare (<1%):
- Seizures (particularly with abrupt withdrawal)
- Hallucinations
- Depression
- Rash
- Elevated liver enzymes
- Syncope
Intrathecal-specific: Pump malfunction, catheter issues, meningitis, and surgical complications.
Drug interaction
- CNS Depressants: Enhanced sedative effects with alcohol, benzodiazepines, opioids, barbiturates, and sedating antihistamines.
- Antihypertensives: May potentiate hypotensive effects.
- MAO Inhibitors: Potential for increased CNS depression; avoid concurrent use.
- Tricyclic Antidepressants: May enhance muscle relaxation effects.
- Levodopa/Carbidopa: Case reports of worsened psychosis and hallucinations.
- Diabetes Medications: May cause elevated blood glucose; monitor glucose levels.
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, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed one. Consistent dosing is important to maintain stable plasma concentrations and avoid fluctuations in spasticity control.
Overdose
Signs and Symptoms: Manifestations of overdose include vomiting, muscular hypotonia, drowsiness, dilated pupils, respiratory depression, seizures, coma, and cardiovascular collapse.
Management:
- Immediate gastric lavage if ingestion recent
- Maintain airway and support ventilation
- Administer intravenous fluids for hypotension
- Seizure control with benzodiazepines
- Dialysis may be beneficial (baclofen is dialyzable)
- There is no specific antidote; treatment is supportive and symptomatic
Particular caution is warranted with intrathecal overdose, which constitutes a medical emergency requiring immediate pump reservoir emptying and specialist consultation.
Storage
- Store at controlled room temperature (20-25°C or 68-77°F)
- Protect from moisture and light
- Keep in original container with lid tightly closed
- Keep out of reach of children and pets
- Do not use after expiration date printed on packaging
- Intrathecal solution requires specific handling per pump manufacturer guidelines
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional before starting, changing, or stopping any medication. The prescribing physician should be familiar with the patient’s complete medical history and current medications. Individual response to therapy may vary, and proper medical supervision is essential throughout treatment.
Reviews
“Lioresal has been transformative for my patients with MS-related spasticity. The titration process requires patience, but the functional improvements in mobility and pain reduction are often remarkable.” - Neurologist, 15 years experience
“As a physical therapist, I’ve observed that patients on appropriately dosed baclofen demonstrate significantly improved response to stretching and strengthening protocols. The reduction in resistance allows for more effective therapy sessions.” - Physical Therapist
“After my spinal cord injury, the muscle spasms were unbearable. Lioresal gave me back some control over my body. The initial drowsiness was challenging but subsided after two weeks.” - Patient with T6 complete injury
“The intrathecal delivery system revolutionized treatment for our most severe spasticity cases. The precision of delivery minimizes systemic side effects while providing excellent spasticity control.” - Rehabilitation Medicine Specialist