Arbaclofen placarbil: Difference between revisions
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{{DISPLAYTITLE:Arbaclofen placarbil}} | {{DISPLAYTITLE:Arbaclofen placarbil}} | ||
[[File:Arbaclofen_placarbil.svg|thumb|right|Chemical structure of arbaclofen placarbil]] | |||
'''Arbaclofen placarbil''' is a prodrug of [[arbaclofen]], which is a derivative of [[baclofen]], a [[GABA_B receptor]] agonist. It is designed to improve the pharmacokinetic properties of baclofen, allowing for better absorption and a more consistent therapeutic effect. | '''Arbaclofen placarbil''' is a prodrug of [[arbaclofen]], which is a derivative of [[baclofen]], a [[GABA_B receptor]] agonist. It is designed to improve the pharmacokinetic properties of baclofen, allowing for better absorption and a more consistent therapeutic effect. | ||
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* [[Multiple sclerosis]] | * [[Multiple sclerosis]] | ||
* [[Alcohol use disorder]] | * [[Alcohol use disorder]] | ||
[[Category:Prodrugs]] | [[Category:Prodrugs]] | ||
[[Category:GABA receptor agonists]] | [[Category:GABA receptor agonists]] | ||
[[Category:Muscle relaxants]] | [[Category:Muscle relaxants]] | ||
Latest revision as of 06:12, 2 March 2025
Arbaclofen placarbil is a prodrug of arbaclofen, which is a derivative of baclofen, a GABA_B receptor agonist. It is designed to improve the pharmacokinetic properties of baclofen, allowing for better absorption and a more consistent therapeutic effect.
Mechanism of Action[edit]
Arbaclofen placarbil is metabolized in the body to release arbaclofen, which then acts on the GABA_B receptors. These receptors are involved in inhibitory neurotransmission in the central nervous system, leading to muscle relaxation and potential therapeutic effects in conditions such as spasticity and alcohol use disorder.
Pharmacokinetics[edit]
Arbaclofen placarbil is absorbed in the gastrointestinal tract and converted to arbaclofen by esterase enzymes. This conversion allows for a more controlled release of the active drug, potentially reducing the frequency of dosing compared to baclofen.
Clinical Uses[edit]
Arbaclofen placarbil has been investigated for use in treating spasticity associated with multiple sclerosis and spinal cord injury. It has also been studied for its potential in treating alcohol use disorder by reducing cravings and withdrawal symptoms.
Side Effects[edit]
Common side effects of arbaclofen placarbil may include drowsiness, dizziness, and nausea. As with other GABA_B agonists, there is a risk of sedation and hypotonia.
Development and Research[edit]
Research into arbaclofen placarbil has focused on its potential benefits over traditional baclofen, particularly in terms of improved absorption and reduced side effects. Ongoing studies aim to further elucidate its efficacy and safety profile in various neurological and psychiatric conditions.
