Baclosign: Targeted Spasticity Relief with Precision Muscle Relaxation
Baclosign
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| Product dosage: 25mg | |||
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Baclosign (baclofen) is a centrally acting skeletal muscle relaxant specifically formulated for the management of spasticity resulting from multiple sclerosis, spinal cord injuries, and other neurological diseases. It operates as a gamma-aminobutyric acid (GABA) agonist, primarily exerting its effect at the spinal cord level to inhibit monosynaptic and polysynaptic reflex transmission. This targeted mechanism reduces the frequency and amplitude of muscle spasms, alleviates associated pain, and improves range of motion, thereby facilitating daily activities and therapeutic regimens. As a prescription medication, its use requires careful titration and supervision by a healthcare professional to balance efficacy with tolerability.
Features
- Active Ingredient: Baclofen
- Standard Dosage Forms: Oral tablets (10 mg, 20 mg)
- Mechanism of Action: GABA-B receptor agonist
- Therapeutic Class: Skeletal muscle relaxant, centrally acting
- Bioavailability: Approximately 70-85%
- Peak Plasma Concentration: 2-3 hours post-administration
- Half-Life: 2.5-4 hours
- Protein Binding: Approximately 30%
- Metabolism: Hepatic (minimal)
- Excretion: Primarily renal (70-80% unchanged)
Benefits
- Reduces Muscle Hypertonicity: Effectively diminishes increased muscle tone and rigidity, allowing for improved voluntary movement.
- Alleviates Painful Spasms: Provides relief from the discomfort and pain associated with involuntary muscle contractions.
- Enhances Functional Capacity: Improves the ability to perform activities of daily living, physiotherapy, and occupational therapy.
- Facilitates Nursing Care: Eases patient handling and hygiene routines for caregivers.
- Non-Sedating at Optimal Doses: When properly titrated, effective spasticity management can be achieved without significant CNS depression.
Common use
Baclosign is primarily indicated for the management of spasticity. Its use is most common in patients diagnosed with:
- Multiple sclerosis (particularly for relieving flexor spasms and concomitant pain, clonus, and muscular rigidity)
- Spinal cord injuries and diseases (including traumatic spinal injury, transverse myelitis)
- Other spinal cord pathologies such as amyotrophic lateral sclerosis (ALS) It may also be used off-label in certain cases of cerebral palsy and trigeminal neuralgia, though this is strictly at the discretion of a prescribing neurologist.
Dosage and direction
Dosage must be individualized for each patient based on response and tolerability. The following represents a standard titration schedule for adults.
Initial Dose: 5 mg orally three times daily (15 mg total per day). Titration: Increase dosage by 5 mg per dose every three days to the desired effect. A common therapeutic range is 40-80 mg daily, divided into three or four doses. Maximum Dose: Do not exceed 80 mg daily (20 mg qid) without express neurological consultation. Some severe cases under strict supervision may require higher doses. Administration: Tablets should be swallowed whole with a glass of water, with or without food. To minimize potential gastrointestinal upset, taking with food is often advised. Discontinuation: Abrupt withdrawal must be avoided. Taper dosage gradually over 1-2 weeks to prevent hallucination, seizure, or rebound spasticity.
Precautions
- Renal Impairment: Dose reduction is necessary in patients with reduced renal function due to predominant renal excretion.
- Hepatic Impairment: Use with caution; although metabolism is minimal, hepatic disease can alter pharmacokinetics.
- Elderly Patients: Increased sensitivity may necessitate lower starting doses and slower titration.
- Psychiatric History: Use cautiously in patients with a history of psychiatric disorders, schizophrenia, or confusional states.
- Seizure Disorders: May lower seizure threshold; monitor patients with epilepsy closely.
- Pregnancy: Category C; use only if potential benefit justifies potential risk to the fetus.
- Lactation: Baclofen is excreted in human milk; a decision should be made to discontinue nursing or discontinue the drug.
Contraindications
- Hypersensitivity to baclofen or any component of the formulation.
- Active peptic ulcer disease (can exacerbate condition).
- Severe cardiovascular instability or shock.
Possible side effect
Common side effects (often dose-related and may diminish with continued use):
- Drowsiness, dizziness, weakness
- Nausea, constipation
- Fatigue, confusion
- Headache, insomnia
Less common but serious side effects (require medical attention):
- Hallucinations, severe depression
- Seizures
- Syncope, hypotension
- Respiratory depression
- Severe rash or urticaria
- Urinary retention
Drug interaction
- CNS Depressants (alcohol, benzodiazepines, opioids, sedatives): Enhanced sedative effects and respiratory depression.
- Antihypertensives: May potentiate hypotensive effects.
- MAO Inhibitors: Increased CNS depression and hypotension risk.
- Levodopa: Possible exacerbation of psychosis or hallucinations.
- Tricyclic Antidepressants: Increased muscle relaxant effect and sedation.
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 catch up.
Overdose
Symptoms of overdose are primarily related to CNS depression and may include:
- Coma
- Respiratory depression
- Hypotension
- Bradycardia
- Hypothermia
- Seizures
- Muscular hypotonia
Management: There is no specific antidote. Treatment is supportive and symptomatic, including securing airway, ventilation, and cardiovascular support. Hemodialysis may be beneficial due to the drug’s water solubility and low protein binding.
Storage
Store at room temperature (15-30°C or 59-86°F). Protect from light and moisture. Keep in the original container, tightly closed. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Baclosign is a prescription medication and must be used under the direct supervision of a qualified healthcare provider. Always follow the specific dosage and instructions provided by your prescribing physician. Do not initiate, discontinue, or change your dosage without consulting your doctor.
Reviews
Clinical studies and patient reports consistently highlight Baclosign’s efficacy in significantly reducing spasticity scores and improving quality of life metrics. Many patients report a marked decrease in painful spasms and an improved ability to participate in physical therapy. The necessity for careful dose titration is frequently noted to minimize sedative side effects. Overall, it is considered a cornerstone therapy for managing spasticity of spinal origin.