Baclofen 20mg/20ml solution for injection pre-filled syringes
Prescription only
Requires a prescription from a doctor or prescriber
Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant.
Active ingredients:
Baclofen
No active safety alerts
Official documents, adverse reaction reporting, and safety monitoring
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Official medicine documents
Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(16 Jan 2026)Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Baclofen
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
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Suspected adverse reactions reported for Baclofen
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1 branded products available
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Therapeutically similar medicines
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Baclofen 20mg tablets
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Tablet
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Pridinol 3mg tablets
Tablet
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Baclofen 10mg/5ml oral solution sugar free
Oral solution
10mg/5ml
Same therapeutic group
Baclofen 30mg/10ml solution for injection vials
Injection
30mg/10ml
Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
Clinical guidelines and formulary information
British National Formulary
Baclofen
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(8)
Spasticity in under 19s: management (CG145)
CG145
Clinical guideline
Updated Nov 2016Cerebral palsy in adults (NG119)
NG119
NICE guideline
Updated Jan 2019Multiple sclerosis in adults: management (NG220)
NG220
NICE guideline
Updated Jun 2022Selective dorsal rhizotomy for spasticity in cerebral palsy (HTG245)
HTG245
Guidance
Updated Dec 2010Motor neurone disease: assessment and management (NG42)
NG42
NICE guideline
Updated Jul 2019Stroke rehabilitation in adults (NG236)
NG236
NICE guideline
Updated Oct 2023Mollii suit for spasticity (MIB100)
MIB100
Guidance
Updated Mar 2017Rehabilitation after traumatic injury (NG211)
NG211
NICE guideline
Updated Jan 2022Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
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These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Show details
Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
107 found
Half-life
2-6 hours
Mechanism
The exact mechanism of action of baclofen is unclear.
Food interactions
2 warnings
Human targets
3 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
70%
Baclofen has an oral bioavailability of 70% to 85%. Following oral administration, it is rapidly absorbed through the gastrointestinal tract…
Half-life
2-6 hours
The half-life is 2-6 hours after oral administration and 1-5 hours following intrathecal administration.
[A245338]…
[A245338]…
Protein binding
30%
The protein binding is approximately 30%.
[L40278]
[L40278]
Volume of distribution
0.7 L/kg
The volume of distribution of baclofen is 0.7 L/kg.
[L40278]
As baclofen is mainly water-soluble, it does not readily cross the blood-brain barrier.
[A245333]…
[L40278]
As baclofen is mainly water-soluble, it does not readily cross the blood-brain barrier.
[A245333]…
Metabolism
15%
Approximately 15% of the oral dose is metabolized in the liver, mainly by deamination.
[A245338]…
[A245338]…
Elimination
70-80%
About 70-80% of baclofen is eliminated in an unchanged form by renal excretion [A245323][A245338] within 72 hours of administration.…
Clearance
180 mL/min
The systemic clearance (CL/F) was 180 mL/min and the renal clearance was 103 mL/min following oral administration.
[A245343]
[A245343]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant. Although originally designed in 1962 to treat epilepsy, baclofen was not effective in treating this condition but instead was shown to reduce spasticity in selected patients.[A245338] Baclofen was reintroduced in 1971 as a treatment for spasticity and was later approved by the FDA in 1977.[A245323][A245338] Baclofen is used to manage severe muscle spasms of cerebral or spinal cord origins, including multiple sclerosis and traumatic brain injury.[L39429]
Baclofen was investigated for use in alcohol dependence and withdrawal; however, evidence is limited and there is inconsistent evidence to suggest its clinical efficacy in managing alcohol dependence or withdrawal symptoms.[A173905][A173908][A245338]
Baclofen was investigated for use in alcohol dependence and withdrawal; however, evidence is limited and there is inconsistent evidence to suggest its clinical efficacy in managing alcohol dependence or withdrawal symptoms.[A173905][A173908][A245338]
Properties:
solid
Avg. mass: 213.66 Da
DrugBank indication
Oral baclofen is indicated for the treatment of spasticity resulting from multiple sclerosis and is particularly useful for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. It may also be used to treat patients with spinal cord injuries and other spinal cord diseases. Baclofen should not be used to treat skeletal muscle spasms resulting from rheumatic disorders.
[L39434]
Intrathecal baclofen is also indicated for the management of severe spasticity of the cerebral or spinal original in patients 4 years of age and older.
It is reserved for patients unresponsive to oral baclofen therapy, or those who experience intolerable central nervous system side effects at effective doses. For use in spasticity due to traumatic brain injury, baclofen should be considered after at least one year of injury.
[L39429]
[L39434]
Intrathecal baclofen is also indicated for the management of severe spasticity of the cerebral or spinal original in patients 4 years of age and older.
It is reserved for patients unresponsive to oral baclofen therapy, or those who experience intolerable central nervous system side effects at effective doses. For use in spasticity due to traumatic brain injury, baclofen should be considered after at least one year of injury.
[L39429]
Also known as(42)
(+-)-Baclofen
4-Amino-3-(4-chlorophenyl)butyric acid
Baclofen
Baclofène
Baclofeno
Baclofenum
beta-(4-Chlorophenyl)gaba
beta-(Aminomethyl)-4-chlorobenzenepropanoic acid
Dosage forms(74)
Injection, solution (Intrathecal) — 10 mg/20mL
Injection, solution (Intrathecal) — 1000 ug/1mL
Injection, solution (Intrathecal) — 40 mg/20mL
Solution (Oral) — 10 mg/5mL
Tablet (Oral) — 15 mg/1
Tablet (Oral) — 5 mg/1
Injection (Intrathecal) — 10 mg/20mL
Injection (Intrathecal) — 40 mg/20mL
Molecular properties(19)
Drug interactions(1563)
Known interactions with other medications. Always consult a healthcare professional.
Buprenorphine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine
Moderate
Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Dronabinol
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Dronabinol.
Droperidol
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Droperidol.
Hydrocodone
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine
Moderate
Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Magnesium sulfate
Moderate
The therapeutic efficacy of Baclofen can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline
Moderate
Minocycline may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Mirtazapine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Nabilone.
Orphenadrine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Perampanel.
Pramipexole
Moderate
Baclofen may increase the sedative activities of Pramipexole.
Ropinirole
Moderate
Baclofen may increase the sedative activities of Ropinirole.
Rotigotine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Rotigotine.
Rufinamide
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Sodium oxybate
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol
Moderate
Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.
Thalidomide
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
The risk or severity of adverse effects can be increased when Methadone is combined with Baclofen.
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.
Lacidipine
Moderate
Baclofen may increase the hypotensive activities of Lacidipine.
Fluvoxamine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Fluvoxamine.
Citalopram
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Citalopram.
Duloxetine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Duloxetine.
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Trazodone.
Paroxetine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Paroxetine.
Sertraline
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Sibutramine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Sibutramine.
Nefazodone
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Nefazodone.
Escitalopram
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Zimelidine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Zimelidine.
Dapoxetine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Dapoxetine.
Milnacipran
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Milnacipran.
Desvenlafaxine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Desvenlafaxine.
Seproxetine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Seproxetine.
Levomilnacipran
Moderate
Baclofen may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Indalpine.
Ritanserin
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Ritanserin.
Alaproclate
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Alaproclate.
Benzatropine
Moderate
Baclofen may decrease the excretion rate of Benzatropine which could result in a higher serum level.
Cyproheptadine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.
Propiomazine
Moderate
Baclofen may increase the central nervous system depressant (CNS depressant) activities of Propiomazine.
Propantheline
Moderate
Baclofen may decrease the excretion rate of Propantheline which could result in a higher serum level.
Showing 50 of 1563 interactions
Food & lifestyle interactions
Avoid Alcohol
Avoid alcohol.
Take With Food
Take with food. Take with food or milk to reduce gastric irritation.
Toxicity & overdose
The oral LD50 in rats is 145 mg/kg.
[L40273]
Baclofen withdrawal symptoms typically occur within hours to days following interruption of either oral or intrathecal drug formulations.
[A245338]
Abrupt discontinuation of baclofen is not advised.
[L39429]
Clinical manifestations of baclofen overdose may include altered mental status, somnolence, seizure, hypothermia, respiratory depression, and coma. Overdose from baclofen oral tablets resulted in vomiting, lightheadedness, drowsiness, muscular hypotonia, accommodation disorders, coma, respiratory depression, and seizures.
[A245323][L40134]
Most overdose symptoms are neurological but uncommon cardiovascular effects such as hypertension, bradycardia, and tachycardia may be observed.
[A37219]
In case of overdose, symptomatic treatment and gastric decontamination should be initiated. When the patient is alert, gastric emptying should be performed by inducing emesis and then performing lavage while maintaining an adequate airway and respiration.
Emesis should not be induced in unconscious patients.
[A245323][L40134]
[L40273]
Baclofen withdrawal symptoms typically occur within hours to days following interruption of either oral or intrathecal drug formulations.
[A245338]
Abrupt discontinuation of baclofen is not advised.
[L39429]
Clinical manifestations of baclofen overdose may include altered mental status, somnolence, seizure, hypothermia, respiratory depression, and coma. Overdose from baclofen oral tablets resulted in vomiting, lightheadedness, drowsiness, muscular hypotonia, accommodation disorders, coma, respiratory depression, and seizures.
[A245323][L40134]
Most overdose symptoms are neurological but uncommon cardiovascular effects such as hypertension, bradycardia, and tachycardia may be observed.
[A37219]
In case of overdose, symptomatic treatment and gastric decontamination should be initiated. When the patient is alert, gastric emptying should be performed by inducing emesis and then performing lavage while maintaining an adequate airway and respiration.
Emesis should not be induced in unconscious patients.
[A245323][L40134]
How it works
Mechanism of action
The exact mechanism of action of baclofen is unclear. Baclofen is an agonist at the beta subunit of gamma-aminobutyric acid (GABA) receptors expressed on pre- and post-synaptic neurons.[A173923] Upon binding to GABAB receptors, baclofen causes an influx of potassium into the neuron, leading to hyperpolarization of the neuronal membrane and decreased calcium influx at presynaptic nerve terminals. This results in a decreased rate of action potential threshold being reached by presynaptic neurons and reduced action potential of postsynaptic motor neurons that innervate the muscle spindles. Baclofen thereby inhibits the transmission of both mono- and polysynaptic reflexes at the spinal cord, relaxing spasticity.[A245338] Baclofen may act on some voltage-gated calcium channels; however, the clinical significance of this is unclear.[A245323]
Pharmacodynamics
Baclofen is an antispasmodic agent that induces muscle relaxation. It reduces the release of excitatory neurotransmitters in the pre-synaptic neurons and stimulates inhibitory neuronal signals in the post-synaptic neurons.[A245323] Oral formulations of baclofen are the most commonly used form of the drug. In one cross-section study, intrathecal baclofen was more effective than oral baclofen in relieving spasticity directly at the level of the spinal cord.[A245338] Baclofen has CNS depression properties and can cause sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression.[L40134] Baclofen also mediates some antinociceptive effects and stimulates gastric acid secretion.[L40278]
Baclofen exhibits anti-inflammatory and neuroprotective activities: it inhibits the release of pro-inflammatory cytokines from microglia and astrocytes, and decreases oxidative stress in rats.[A173938]
Baclofen exhibits anti-inflammatory and neuroprotective activities: it inhibits the release of pro-inflammatory cytokines from microglia and astrocytes, and decreases oxidative stress in rats.[A173938]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Baclofen has an oral bioavailability of 70% to 85%. Following oral administration, it is rapidly absorbed through the gastrointestinal tract with peak plasma concentrations being reached two to three hours after ingestion.
[A245323]
Peak effect is observed about four hours after intrathecal administration.
[A245338]
The absorption is dose-dependent and increases with higher doses.
[A245323]
There is intersubject variation in absorption.
[L40134]
Administration of oral baclofen suspension with a high-fat meal resulted in 9% decrease in AUC and 33% decrease in Cmax compared to the fasted state.
[L40134]
[A245323]
Peak effect is observed about four hours after intrathecal administration.
[A245338]
The absorption is dose-dependent and increases with higher doses.
[A245323]
There is intersubject variation in absorption.
[L40134]
Administration of oral baclofen suspension with a high-fat meal resulted in 9% decrease in AUC and 33% decrease in Cmax compared to the fasted state.
[L40134]
Half-life
The half-life is 2-6 hours after oral administration and 1-5 hours following intrathecal administration.
[A245338]
The apparent elimination half-life of baclofen oral suspension or granules is about 5.6 hours.
[L40134]
[A245338]
The apparent elimination half-life of baclofen oral suspension or granules is about 5.6 hours.
[L40134]
Protein binding
The protein binding is approximately 30%.
[L40278]
[L40278]
Volume of distribution
The volume of distribution of baclofen is 0.7 L/kg.
[L40278]
As baclofen is mainly water-soluble, it does not readily cross the blood-brain barrier.
[A245333]
Drug concentrations of baclofen in the cerebrospinal fluid are approximately 8.5 times lower than in the plasma.
[L40278]
[L40278]
As baclofen is mainly water-soluble, it does not readily cross the blood-brain barrier.
[A245333]
Drug concentrations of baclofen in the cerebrospinal fluid are approximately 8.5 times lower than in the plasma.
[L40278]
Metabolism
Approximately 15% of the oral dose is metabolized in the liver, mainly by deamination.
[A245338]
Deamination yields the main metabolite, β-(p-chlorophenyl)-4-hydroxybutyric acid, which is pharmacologically inactive.
[L40278]
[A245338]
Deamination yields the main metabolite, β-(p-chlorophenyl)-4-hydroxybutyric acid, which is pharmacologically inactive.
[L40278]
Route of elimination
About 70-80% of baclofen is eliminated in an unchanged form by renal excretion [A245323][A245338] within 72 hours of administration. About 5% of the dose is excreted via the kidneys as metabolites.
[L40278]
There is intersubject variation in elimination.
[L40134]
[L40278]
There is intersubject variation in elimination.
[L40134]
Clearance
The systemic clearance (CL/F) was 180 mL/min and the renal clearance was 103 mL/min following oral administration.
[A245343]
[A245343]
Drug targets(3)
Proteins and enzymes this drug interacts with in the body
Gamma-aminobutyric acid type B receptor subunit 2
GABBR2
agonist
Specific functionG protein-coupled GABA receptor activity
Cellular location
Cell membrane
General function & pharmacology
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2 .
PMID:15617512 PMID:18165688 PMID:22660477 PMID:24305054 PMID:9872316 PMID:9872744
Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins .
PMID:18165688
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase .
PMID:10075644 PMID:10773016 PMID:24305054
Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis .
PMID:10075644 PMID:10773016 PMID:10906333 PMID:9872744
Plays a critical role in the fine-tuning of inhibitory synaptic transmission .
PMID:22660477 PMID:9872744
Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials .
PMID:10075644 PMID:22660477 PMID:9872316 PMID:9872744
Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable)
PMID:15617512 PMID:18165688 PMID:22660477 PMID:24305054 PMID:9872316 PMID:9872744
Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins .
PMID:18165688
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase .
PMID:10075644 PMID:10773016 PMID:24305054
Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis .
PMID:10075644 PMID:10773016 PMID:10906333 PMID:9872744
Plays a critical role in the fine-tuning of inhibitory synaptic transmission .
PMID:22660477 PMID:9872744
Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials .
PMID:10075644 PMID:22660477 PMID:9872316 PMID:9872744
Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable)
Gamma-aminobutyric acid type B receptor subunit 1
GABBR1
agonist
Specific functionextracellular matrix protein binding
Cellular location
Cell membrane
General function & pharmacology
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2 .
PMID:15617512 PMID:18165688 PMID:22660477 PMID:24305054 PMID:36103875 PMID:9872316 PMID:9872744
Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins .
PMID:18165688
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase .
PMID:10075644 PMID:10773016 PMID:10906333 PMID:24305054 PMID:9872744
Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis .
PMID:10075644
Calcium is required for high affinity binding to GABA (By similarity). Plays a critical role in the fine-tuning of inhibitory synaptic transmission .
PMID:9844003
Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials .
PMID:10075644 PMID:22660477 PMID:9844003 PMID:9872316 PMID:9872744
Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable). Activated by (-)-baclofen, cgp27492 and blocked by phaclofen PMID:24305054 PMID:9844003 PMID:9872316
PMID:15617512 PMID:18165688 PMID:22660477 PMID:24305054 PMID:36103875 PMID:9872316 PMID:9872744
Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins .
PMID:18165688
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase .
PMID:10075644 PMID:10773016 PMID:10906333 PMID:24305054 PMID:9872744
Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis .
PMID:10075644
Calcium is required for high affinity binding to GABA (By similarity). Plays a critical role in the fine-tuning of inhibitory synaptic transmission .
PMID:9844003
Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials .
PMID:10075644 PMID:22660477 PMID:9844003 PMID:9872316 PMID:9872744
Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable). Activated by (-)-baclofen, cgp27492 and blocked by phaclofen PMID:24305054 PMID:9844003 PMID:9872316
C-X-C chemokine receptor type 4
CXCR4
allosteric modulator
Specific functionactin binding
Cellular location
Cell membrane
General function & pharmacology
Receptor for the C-X-C chemokine CXCL12/SDF-1 that transduces a signal by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation .
PMID:10452968 PMID:18799424 PMID:24912431 PMID:28978524
Involved in the AKT signaling cascade .
PMID:24912431
Plays a role in regulation of cell migration, e.g. during wound healing .
PMID:28978524
Acts as a receptor for extracellular ubiquitin; leading to enhanced intracellular calcium ions and reduced cellular cAMP levels .
PMID:20228059
Binds bacterial lipopolysaccharide (LPS) et mediates LPS-induced inflammatory response, including TNF secretion by monocytes .
PMID:11276205
Involved in hematopoiesis and in cardiac ventricular septum formation. Also plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Involved in cerebellar development.
In the CNS, could mediate hippocampal-neuron survival (By similarity)
PMID:10452968 PMID:18799424 PMID:24912431 PMID:28978524
Involved in the AKT signaling cascade .
PMID:24912431
Plays a role in regulation of cell migration, e.g. during wound healing .
PMID:28978524
Acts as a receptor for extracellular ubiquitin; leading to enhanced intracellular calcium ions and reduced cellular cAMP levels .
PMID:20228059
Binds bacterial lipopolysaccharide (LPS) et mediates LPS-induced inflammatory response, including TNF secretion by monocytes .
PMID:11276205
Involved in hematopoiesis and in cardiac ventricular septum formation. Also plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Involved in cerebellar development.
In the CNS, could mediate hippocampal-neuron survival (By similarity)
Scientific references(10)
Brennan J.L., Leung J.G., Gagliardi J.P., Rivelli S.K., Muzyk A.J.
Clinical effectiveness of baclofen for the treatment of alcohol dependence: a review.
Clinical Pharmacology
2013 Jul 35:99-107. doi: 10.2147/CPAA.S32434. Print 2013
Liu J., Wang L.N.
Baclofen for alcohol withdrawal.
Cochrane Database of Systematic Reviews
2017 Aug 208:CD008502. doi: 10.1002/14651858.CD008502.pub5
Chen K., Li H.Z., Ye N., Zhang J., Wang J.J.
Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro.
Brain Research Bull
2005 Oct 3067(4):310-8. doi: 10.1016/j.brainresbull.2005.07.004
Fu Z., Yang H., Xiao Y., Zhao G., Huang H.
The gamma-aminobutyric acid type B (GABAB) receptor agonist baclofen inhibits morphine sensitization by decreasing the dopamine level in rat nucleus accumbens.
Behav Brain Funct
2012 Jul 108:20. doi: 10.1186/1744-9081-8-20
de Beaurepaire R.
A Review of the Potential Mechanisms of Action of Baclofen in Alcohol Use Disorder.
Front Psychiatry
2018 Oct 179:506. doi: 10.3389/fpsyt.2018.00506. eCollection 2018
Ghanavatian S., Derian A.
Poster 314: Challenging Cases of Ultrasound Guided Baclofen Pump Refills: A Case Series.
PM&R
20179(9S1). doi: 10.1016/j.pmrj.2017.08.254
Ertzgaard P., Campo C., Calabrese A.
Efficacy and safety of oral baclofen in the management of spasticity: A rationale for intrathecal baclofen.
Journal Rehabil Medicine
2017 Mar 649(3):193-203. doi: 10.2340/16501977-2211
Romito J.W., Turner E.R., Rosener J.A., Coldiron L., Udipi A., Nohrn L., Tausiani J., Romito B.T.
Baclofen therapeutics, toxicity, and withdrawal: A narrative review.
SAGE Open Medicine
2021 Jun 39:20503121211022197. doi: 10.1177/20503121211022197. eCollection 2021
Leung N.Y., Whyte I.M., Isbister G.K.
Baclofen overdose: defining the spectrum of toxicity.
Emerg Medicine Australas
2006 Feb18(1):77-82. doi: 10.1111/j.1742-6723.2006.00805.x
Kochak G.M., Rakhit A., Wagner W.E., Honc F., Waldes L., Kershaw R.A.
The pharmacokinetics of baclofen derived from intestinal infusion.
Clinical Pharmacology Therapeutics
1985 Sep38(3):251-7. doi: 10.1038/clpt.1985.167
ATC classification(1 code)
ATC M03BX01
Affected organisms(1)
Humans and other mammals
International brands(3)
Salt forms(1)
Baclofen hydrochloride(DBSALT002256)
Experimental properties(4)
Commercial products(516)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Baclofen
Additional database identifiers
Drugs Product Database (DPD)
2104
ChemSpider
2197
BindingDB
24182
Guide to Pharmacology
1084
HUGO Gene Nomenclature Committee (HGNC)
HGNC:4507
GenAtlas
GABBR2
GeneCards
GABBR2
GenBank Gene Database
AJ012188
GenBank Protein Database
3776098
Guide to Pharmacology
241
UniProt Accession
GABR2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:4070
GenAtlas
GABBR1
GeneCards
GABBR1
GenBank Gene Database
AJ225028
GenBank Protein Database
3892594
Guide to Pharmacology
240
UniProt Accession
GABR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2561
GenAtlas
CXCR4
GeneCards
CXCR4
GenBank Gene Database
L01639
GenBank Protein Database
189314
Guide to Pharmacology
71
UniProt Accession
CXCR4_HUMAN
International reference pricing
23 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $0.30/tablet
To $84.00/ml
Apo-Baclofen 10 mg Tablet
$0.30/tablet
Mylan-Baclofen 10 mg Tablet
$0.30/tablet
Nu-Baclo 10 mg Tablet
$0.30/tablet
Phl-Baclofen 10 mg Tablet
$0.30/tablet
Pms-Baclofen 10 mg Tablet
$0.30/tablet
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
8 active patents, 2 expired
11491125
United States
Approved 8 Nov 2022 · Expires 29 Sept 2041
15y 6m
11850225
United States
Approved 26 Dec 2023 · Expires 29 Sept 2041
15y 6m
10610502
United States
Approved 7 Apr 2020 · Expires 30 Aug 2039
13y 5m
10792262
United States
Approved 6 Oct 2020 · Expires 29 Jul 2039
13y 4m
11654124
United States
Approved 23 May 2023 · Expires 29 Jul 2039
13y 4m
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)