baclofen (Lioresal)
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Introduction
Tradename: Lioresal.
Indications
- relief of signs & symptoms of muscle spasm
- refractory GERD
Contraindications
Caution: elderly patients are sensitive to bacolfen
Dosage
Start 5 mg PO TID, max 80 mg/day
Tabs: 10 & 20 mg.
Dosage adjustment in renal failure
- may be necessary to adjust in renal failure
Adverse effects
- common (> 10%)
- drowsiness, vertigo, dizziness, psychiatric disturbances, insomnia, slurred speech (rare according to ref 2), ataxia, hypotonia, muscle weakness
- less common (1-10%)
- uncommon (< 1%)
- palpitations, chest pain, syncope, euphoria, excitement, depression, hallucinations, dry mouth, anorexia, taste disorder, abdominal pain, vomiting, diarrhea, enuresis,urinary retention, dysuria, impotence, nocturia, hematuria, paresthesias, dyspnea
- other[2]
- blurred vision (rare)
- seizures (rare); seizures may occur during withdrawal[4]
- symptoms of withdrawal with abrupt discontinuation[6]
- hallucinations, delusions, confusion, agitation, anxiety, insomnia, altered consciousness, hyperthermia, spasticity, tachycardia, seizures
- use for over one month is risk factor for delirium
- use in patients with renal failure may result in encephalopathy[8]
- baclofen is associated with higher incidences of injury & delirium compared to tizanidine when used for musculoskeletal pain[9]
- baclofen is associated with higher 30-day incidence & 1-year persistence of encephalopathy vs tizanidine or cyclobenzaprine (RR= 2.3 (30-day))[10]
- risk of falls: baclofen, cyclobenzaprine > tizanidine
- risk of fracture: baclofen, cyclobenzaprine = tizanidine[11]
Drug interactions
Laboratory
Mechanism of action
- inhibits both monosynaptic & polysynaptic reflexes at the level of the spinal cord
- effects may be mediated by hyperpolarization of afferent terminals
- derivative of GABA & may stimulate GABA-B receptor
- inhibits transient relaxation of lower esophageal sphincter[5]
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 2.0 2.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 Medications Can Cause Seizures Prescriber's Letter 10(3):16 2003 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=190320&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Omari TI et al, Effect of baclofen on esophagogastric motility and gastroesophageal reflux in children with gastroesophageal reflux disease. A randomized controlled trial. J Pediatr 2006, 149:468 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17011315
Di Lorenzo C Gastroesophageal reflux. Not a time to relax. J Pediatr 2006, 149:436 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17011308 - ↑ 6.0 6.1 Prescriber's Letter 15(12): 2008 Common Oral Medications that May Need Tapering Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=241208&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Deprecated Reference
- ↑ 8.0 8.1 Muanda FT, Weir MA, Bathini L et al. Association of baclofen with encephalopathy in patients with chronic kidney disease. JAMA 2019 Nov 9; PMID: https://www.ncbi.nlm.nih.gov/pubmed/31705755
Chauvin KJ, Blake PG, Garg AX et al. Baclofen has a risk of encephalopathy in older adults receiving dialysis. Kidney Int. 2020;98(4):979-988 PMID: https://www.ncbi.nlm.nih.gov/pubmed/32450156 https://www.kidney-international.org/article/S0085-2538(20)30552-4/fulltext
Wolf E, Kothari NR, Roberts JK et al. Baclofen toxicity in kidney disease. Am J Kidney Dis. 2018;71(2):275-280 PMID: https://www.ncbi.nlm.nih.gov/pubmed/28899601 https://www.ajkd.org/article/S0272-6386(17)30846-6/fulltext - ↑ 9.0 9.1 Su Zhang VR, Niu F, Lee EA et al Safety of baclofen versus tizanidine for older adults with musculoskeletal pain. J Am Geriatr Soc. 2023 Mar 29 PMID: https://www.ncbi.nlm.nih.gov/pubmed/36989193
- ↑ 10.0 10.1 Hwang YJ, Chang, SR, Brotman DJ et al Baclofen and the Risk of Encephalopathy: A Real-World, Active-Comparator Cohort Study. Mayo Clinic Proceedings. 2023. April 5. PMID: https://www.ncbi.nlm.nih.gov/pubmed/37028980 https://www.mayoclinicproceedings.org/article/S0025-6196(22)00649-8/fulltext
- ↑ 11.0 11.1 Hwang YJ, Chang AR, Brotman DJ, Inker LA, Grams ME, Shin JI. Baclofen and the risk of fall and fracture in older adults: A real-world cohort study. J Am Geriatr Soc. 2023 Nov 7. PMID: https://www.ncbi.nlm.nih.gov/pubmed/37933734 https://agsjournals.onlinelibrary.wiley.com/doi/abs/10.1111/jgs.18665
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2284
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=44602
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=44599
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=44601
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=51013