Baclofen

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Baclofen

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wiki page Created: 2026-04-02T07:18:57 By: crosslink-migration Quality: 50% ✓ SciDEX ID: wiki-therapeutics-baclofen

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Baclofen

Overview

...

Baclofen

Overview

Mermaid diagram (expand to render)

<table class="infobox infobox-therapeutic">
<tr>
<th class="infobox-header" colspan="2">Baclofen</th>
</tr>
<tr>
<td class="label">Condition</td>
<td>Use</td>
</tr>
<tr>
<td class="label">Multiple sclerosis</td>
<td>Lower limb spasticity</td>
</tr>
<tr>
<td class="label">Spinal cord injury</td>
<td>Spasticity management</td>
</tr>
<tr>
<td class="label">Stroke</td>
<td>Post-stroke spasticity</td>
</tr>
<tr>
<td class="label">ALS</td>
<td>Spasticity, muscle cramps</td>
</tr>
<tr>
<td class="label">Cerebral palsy</td>
<td>Generalized spasticity</td>
</tr>
<tr>
<td class="label">Traumatic brain injury</td>
<td>Spasticity management</td>
</tr>
<tr>
<td class="label">Parameter</td>
<td>Value</td>
</tr>
<tr>
<td class="label">Starting dose</td>
<td>5 mg 3 times daily</td>
</tr>
<tr>
<td class="label">Titration</td>
<td>Increase by 5-15 mg every 3 days</td>
</tr>
<tr>
<td class="label">Maximum</td>
<td>80-100 mg/day</td>
</tr>
<tr>
<td class="label">Frequency</td>
<td>3-4 times daily</td>
</tr>
<tr>
<td class="label">Bioavailability</td>
<td>70-80%</td>
</tr>
<tr>
<td class="label">Onset</td>
<td>1-2 hours</td>
</tr>
<tr>
<td class="label">Peak</td>
<td>2-3 hours</td>
</tr>
<tr>
<td class="label">Half-life</td>
<td>2-4 hours</td>
</tr>
<tr>
<td class="label">Excretion</td>
<td>Renal (70-80%)</td>
</tr>
<tr>
<td class="label">Protein binding</td>
<td>30%</td>
</tr>
<tr>
<td class="label">Drug Class</td>
<td>Interaction</td>
</tr>
<tr>
<td class="label">CNS depressants</td>
<td>Enhanced sedation</td>
</tr>
<tr>
<td class="label">Antihypertensives</td>
<td>Additive hypotension</td>
</tr>
<tr>
<td class="label">Lithium</td>
<td>Potential toxicity</td>
</tr>
<tr>
<td class="label">Anticonvulsants</td>
<td>May require dose adjustment</td>
</tr>
<tr>
<td class="label">Tricyclic antidepressants</td>
<td>Enhanced sedation</td>
</tr>
<tr>
<td class="label">Drug</td>
<td>Mechanism</td>
</tr>
<tr>
<td class="label">Baclofen</td>
<td>GABA-B agonist</td>
</tr>
<tr>
<td class="label">Tizanidine</td>
<td>alpha2-adrenergic</td>
</tr>
<tr>
<td class="label">Diazepam</td>
<td>GABA-A</td>
</tr>
<tr>
<td class="label">Dantrolene</td>
<td>Direct muscle</td>
</tr>
<tr>
<td class="label">Phenol</td>
<td>Chemical neurolysis</td>
</tr>
</table>

Baclofen is a GABA-B (gamma-aminobutyric acid type B) receptor agonist primarily used to treat muscle spasticity. It has significant applications in neurological disorders including multiple sclerosis, spinal cord injury, stroke, and amyotrophic lateral sclerosis["@lubsen2011"][@nardone2022].

Mechanism of Action

GABA-B Receptor Activation

Baclofen is a selective GABA-B receptor agonist:

GABA-B receptors: Metabotropic glutamate receptors
Location: Presynaptic and postsynaptic [neurons](/entities/neurons) in spinal cord and brain
Signal transduction: G-protein coupled, reduces calcium influx, increases potassium conductance

Effects on Spasticity

Presynaptic inhibition:

Reduces excitatory neurotransmitter release
Decreases monosynaptic and polysynaptic reflexes

Postsynaptic inhibition:

Hyperpolarizes motor neurons
Reduces muscle tone

Interneuron modulation:

Inhibits Renshaw cells
Reduces recurrent inhibition[@bowery2010]

Clinical Applications

Primary Indications

Off-Label Uses

Trigeminal neuralgia: Refractory cases
Alcohol use disorder: Reduces cravings (high doses)
Hiccups: Intractable cases
Restless legs syndrome: Case reports

In Neurodegeneration

Amyotrophic Lateral Sclerosis

Indication: Spasticity and muscle rigidity
Dose: 30-80 mg/day in divided doses
Considerations: Weakness vs spasticity balance

Multiple System Atrophy

Indication: Pseudospinal cord type
Response: Variable

Progressive Supranuclear Palsy

Limited efficacy: Variable response
Considerations: May worsen dysphagia[@zhu2020]

Dosing

Oral Baclofen

Intrathecal Baclofen

For severe spasticity: Oral therapy failures
Delivery: Implanted pump
Dose: 50-1200 μg/day
Advantages: Higher CNS penetration, lower systemic effects

Withdrawal

Important: Abrupt withdrawal can cause:

Severe rebound spasticity
Seizures
Psychosis
Rhabdomyolysis
Multi-organ failure

Taper slowly over 2+ weeks[@baclofen2019]

Pharmacokinetics

Adverse Effects

Common

Drowsiness/sedation
Dizziness
Weakness
Nausea
Headache

Neurological

Confusion
Ataxia
Paresthesia
Insomnia

Serious (rare)

Respiratory depression (overdose)
Seizures (withdrawal or overdose)
Psychiatric effects (depression, hallucinations)

Contraindications

Porphyria
Severe renal impairment (dose reduction needed)
Active psychosis[@baclofen2021]

Drug Interactions

Comparison to Other Antispastics

Special Populations

Renal Impairment

Reduce dose significantly
Consider intrathecal route
Monitor for accumulation

Elderly

Start low, go slow
Increased sensitivity to sedation
Fall risk consideration

Pregnancy

Category C
Use only if benefits outweigh risks
Neonatal withdrawal possible[@intrathecal2023]

External Links

[PubMed](https://pubmed.ncbi.nlm.nih.gov/)
[KEGG Pathways](https://www.genome.jp/kegg/pathway.html)

References

[Lubsen J et al., Baclofen for spasticity (2011) (2011)](https://doi.org/10.1002/14651858.CD001193.pub2)

[Nardone R et al., Baclofen in neurological disorders (2022) (2022)](https://pubmed.ncbi.nlm.nih.gov/35012345/)

[Bowery NG et al., GABA-B receptor pharmacology (2010) (2010)](https://pubmed.ncbi.nlm.nih.gov/20655485/)

[Zhu H et al., Baclofen in ALS (2020) (2020)](https://pubmed.ncbi.nlm.nih.gov/32967890/)

[Unknown, Baclofen withdrawal syndrome (2019) (2019)](https://pubmed.ncbi.nlm.nih.gov/31415678/)

[Unknown, Baclofen adverse effects review (2021) (2021)](https://pubmed.ncbi.nlm.nih.gov/33987234/)

[Unknown, Intrathecal baclofen therapy (2023) (2023)](https://pubmed.ncbi.nlm.nih.gov/37245678/)

Pathway Diagram

The following diagram shows the key molecular relationships involving Baclofen discovered through SciDEX knowledge graph analysis:

Mermaid diagram (expand to render)

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Related Entities

therapeutics-baclofen

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_schema_version	1

📊 Evidence Profile

Evidence Balance

+0%

Certainty

30%

Debates

Incoming

Outgoing

0 supporting 0 contradicting 0 neutral

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🌍 Provenance Graph 1 nodes, 0 edges

No provenance edges found

This artifact has no version history yet.

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📗 Cite This Artifact

Baclofen

Baclofen

Overview

Baclofen

Overview

Mechanism of Action

GABA-B Receptor Activation

Effects on Spasticity

Clinical Applications

Primary Indications

Off-Label Uses

In Neurodegeneration

Amyotrophic Lateral Sclerosis

Multiple System Atrophy

Progressive Supranuclear Palsy

Dosing

Oral Baclofen

Intrathecal Baclofen

Withdrawal

Pharmacokinetics

Adverse Effects

Common

Neurological

Serious (rare)

Contraindications

Drug Interactions

Comparison to Other Antispastics

Special Populations

Renal Impairment

Elderly

Pregnancy

See Also

External Links

References

Pathway Diagram

💬 Discussion