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Baclofen: Difference between revisions

From Pharmacopedia
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{{MedTemplate
{{MedTemplate
| generic           = Baclofen
| generic           = Baclofen
| brand             = Lioresal
| brand             = Lioresal (oral, intrathecal pump), Ozobax / Fleqsuvy (oral suspension), Gablofen (intrathecal), Lyvispah (oral granules)
| structure         =  
| structure         =
| classes           = GABAergic, Muscle relaxant
| classes           = [[:Category:Skeletal muscle relaxants|Skeletal muscle relaxant (centrally-acting)]], [[:Category:Antispastics|Antispastic]], [[:Category:GABA-B receptor agonists|GABA-B receptor agonist]]
| mechanism          = GABAB receptor agonist
| uses             = <vote slug="spasticity-multiple-sclerosis-use">Spasticity in multiple sclerosis (FDA, oral and intrathecal)</vote>, <vote slug="spasticity-spinal-cord-injury-use">Spasticity in spinal cord injury (FDA, oral and intrathecal)</vote>, <vote slug="cerebral-palsy-spasticity-use">Cerebral palsy spasticity (FDA intrathecal; off-label oral)</vote>, <vote slug="alcohol-use-disorder-baclofen-use">Alcohol use disorder (off-label, evidence-supported, generally third-line)</vote>, <vote slug="persistent-hiccups-use">Persistent hiccups (off-label)</vote>, <vote slug="gerd-motility-use">GERD with esophageal motility dysfunction (off-label)</vote>, <vote slug="trigeminal-neuralgia-use">Trigeminal neuralgia adjunct (off-label)</vote>
| uses               =  
| starting_dose    = Oral: 5 mg PO TID, titrate by 5 mg per dose every 3 days. Intrathecal: bolus test dose, then continuous infusion via implanted pump
| starting_dose      =  
| preparations      = Tablets 5, 10, 20 mg; oral suspension 5 mg/5 mL (Ozobax, Fleqsuvy); intrathecal injection 50, 500, 1000, 2000 mcg/mL (Lioresal Intrathecal, Gablofen); oral granules (Lyvispah)
| preparations      =  
| fda_max          = 80 mg/day oral (higher off-label)
| routes            =  
| pill_id          =
| onset              =  
| routes            = Oral, intrathecal (via implanted infusion pump)
| duration          =  
| onset             = 1-2 hours (oral)
| halflife          =  
| duration          = 4-6 hours (oral, TID-QID dosing)
| bioavailability    =  
| halflife          = 3-4 hours<ref name="lioresal-label">FDA Prescribing Information, Lioresal (baclofen), Saol Therapeutics/Novartis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017851s019lbl.pdf</ref>
| pregnancy          =  
| bioavailability  = ~70-85% (oral)<ref name="lioresal-label" />
| legal              =  
| pregnancy         = Limited human data.{{citation needed}}
| intro              =  
| legal            = [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance<ref name="lioresal-label" />
| pharmacokinetics  =  
| mechanism         = <vote slug="baclofen-mech-claim">Selective agonist at the GABA-B receptor (the only metabotropic GABA receptor; distinct from the ionotropic GABA-A targeted by benzodiazepines and Z-class hypnotics). Reduces excitatory neurotransmitter release presynaptically and hyperpolarizes postsynaptic membranes, producing antispastic effect particularly at spinal cord interneurons.</vote> '''Severe withdrawal syndrome''' is the marquee adverse-event concern, especially with abrupt cessation of intrathecal administration: hyperthermia, altered mental status, hyperreflexia, rhabdomyolysis, and multiorgan failure can develop within 24-72 hours and progress to death. Gradual taper is essential after extended use; intrathecal pump failures are a recognized emergency<ref name="lioresal-label" />.
| pharmacodynamics  =  
| indications        =
| dosing             =  
| effects            =  
| contraindications  =  
| interactions      =  
| pregnancy_details  =  
| monitoring        =  
| counseling         =  
| anecdotes          =  
| seealso            =  
| references         =  
}}
}}


[[Category:Sedative-Hypnotics]]
== References ==
<references />


[[Category:Skeletal muscle relaxants]]
[[Category:Antispastics]]
[[Category:GABA-B receptor agonists]]