II. Pathophysiology
- These agents are used to reduce severe spasticity (e.g. spinal cord injury, Cerebral Palsy, Multiple Sclerosis)
III. Indications: Spasticity
- Cerebral Palsy
- Multiple Sclerosis
- Spinal Cord Injury
IV. Contraindications
- Not indicated for general musculoskeletal problems
V. Preparations
- Dantrolene (Dantrium)
- Baclofen (Lioresal)
- Baclofen binds GABA B receptors
- Oral Baclofen does not cross blood brain barrier well
- Instead, Baclofen is typically used via Baclofen Intrathecal Pump (due to poor oral absorption)
- Taper off over 1-2 weeks (risk of Hallucinations, Seizures if abruptly stopped)
- Tizanidine (Zanaflex)
- Dose 4 mg orally every 6-8 hours (maximum 36 mg/day)
- Risk of hepatotoxicity and Blood Pressure changes
- Primarily indicated for spasticity due to Multiple Sclerosis or spinal cord injury
- Clonidine effect (risk of Hypotension and rebound Hypertension)
- Taper off over 1-2 weeks (risk of Clonidine-like rebound Hypertension effect)
VI. References
- (2019) Presc Lett 26(3):15
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| Baclofen (on 6/18/2017 at Walmart.com) | ||
| Baclofen 10mg | #30 tablets for $4.00 | $0.13 each |
| Baclofen 10mg | #90 tablets for $10.00 | $0.11 each |
| baclofen (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| BACLOFEN 10 MG TABLET | Generic | $0.13 each |
| BACLOFEN 20 MG TABLET | Generic | $0.24 each |
| dantrolene (on 3/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| DANTROLENE SODIUM 100 MG CAP | Generic | $1.27 each |
| DANTROLENE SODIUM 25 MG CAP | Generic | $0.71 each |
| DANTROLENE SODIUM 50 MG CAP | Generic | $1.00 each |
| tizanidine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| TIZANIDINE HCL 2 MG CAPSULE | Generic | $1.07 each |
| TIZANIDINE HCL 2 MG TABLET | Generic | $0.12 each |
| TIZANIDINE HCL 4 MG CAPSULE | Generic | $1.53 each |
| TIZANIDINE HCL 4 MG TABLET | Generic | $0.12 each |
| TIZANIDINE HCL 6 MG CAPSULE | Generic | $2.57 each |
Ontology: Baclofen (C0004609)
| Definition (CHV) | a drug used to treat spasm caused by back injury |
| Definition (CHV) | a drug used to treat spasm caused by back injury |
| Definition (MSH) | A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission. |
| Definition (NCI) | A synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission. (NCI04) |
| Definition (NCI_NCI-GLOSS) | A drug that is used to treat certain types of muscle spasms and is being studied in the treatment of liver cancer. Baclofen relaxes muscles by blocking certain nerve receptors in the spinal cord. It is a type of antispasmodic. |
| Concepts | Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116) |
| MSH | D001418 |
| SnomedCT | 391810001, 387342009, 6102009 |
| LNC | LP17857-1, MTHU019852 |
| English | Baclofen, Baclophen, beta-(p-Chlorophenyl)-gamma-aminobutyric Acid, Chlorophenyl GABA, GABA, Chlorophenyl, PCP-GABA, beta-(Aminomethyl)-4-chlorobenzenepropanoic Acid, Benzenepropanoic acid, beta-(aminomethyl)-4-chloro-, 4-Amino-3-(4-chlorophenyl)-butanoic Acid, baclofen, baclofen (medication), muscle relaxants skeletal baclofen, BACLOFEN, Baclofen [Chemical/Ingredient], baclophen, Baclofen - chemical, Baclofen - chemical (substance), Baclofen (product), Baclofen (substance) |
| Swedish | Baklofen |
| Czech | baklofen |
| Finnish | Baklofeeni |
| Russian | KHLORFENIL-GAMK, BAKLOFEN, KHLORFENIL-GAMMA-AMINOMASLIANAIA KISLOTA, БАКЛОФЕН, ХЛОРФЕНИЛ-ГАМК, ХЛОРФЕНИЛ-ГАММА-АМИНОМАСЛЯНАЯ КИСЛОТА |
| French | bêta-4-chlorophényl-GABA, PCP-GABA, Baclofène |
| Polish | Baklofen |
| Japanese | バクロフェン, クロロフェニルガンマアミノ酪酸 |
| Spanish | baclofeno (producto), baclofeno (sustancia), baclofeno, Baclofeno, Clorofenil GABA |
| German | Baclofen, Baclophen, Chlorphenyl-GABA |
| Italian | Baclofen |
| Portuguese | Baclofeno, Clorofenil GABA |
Ontology: Dantrolene (C0010976)
| Definition (NCI) | A hydantoin derivative and direct-acting skeletal muscle relaxant. Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1, and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. |
| Definition (MSH) | Skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber. It is used in spasticity and other neuromuscular abnormalities. Although the mechanism of action is probably not central, dantrolene is usually grouped with the central muscle relaxants. |
| Definition (CSP) | skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber; it is used in spasticity and other neuromuscular abnormalities. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D003620 |
| SnomedCT | 372819007, 69107004 |
| LNC | LP17990-0, MTHU024810 |
| English | Dantrolene, 2,4-Imidazolidinedione, 1-(((5-(4-nitrophenyl)-2-furanyl)methylene)amino)-, Dantrolene [Chemical/Ingredient], dantrolene, DANTROLENE, Dantrolene (product), Dantrolene (substance) |
| Swedish | Dantrolen |
| Czech | dantrolen |
| Finnish | Dantroleeni |
| Russian | DANTROLEN, ДАНТРОЛЕН |
| Japanese | ダントロレン |
| Polish | Dantrolen |
| Spanish | dantroleno (producto), dantroleno (sustancia), dantroleno, Dantroleno |
| French | Dantrolène |
| German | Dantrolen |
| Italian | Dantrolene |
| Portuguese | Dantroleno |
Ontology: Muscle Relaxants, Central (C0026833)
| Definition (MSH) | A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358) |
| Concepts | Pharmacologic Substance (T121) |
| MSH | D009125 |
| SnomedCT | 116524002, 372583009 |
| English | Central Muscle Relaxants, Centrally Acting Muscle Relaxants, Muscle Relaxants, Central, Relaxants, Central Muscle, central muscle relaxants, MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS, Centrally acting muscle relaxant (product), Centrally acting muscle relaxant (substance), Centrally acting muscle relaxant |
| French | Myorelaxants à action centrale, Myorelaxants centraux |
| Swedish | Muskelavslappningsmedel, centrala |
| Czech | myorelaxancia centrální |
| Finnish | Sentraaliset lihasrelaksantit |
| Russian | MIORELAKSANTY TSENTRAL'NOGO DEISTVIIA, TSENTRAL'NOGO DEISTVIIA MIORELAKSANTY, МИОРЕЛАКСАНТЫ ЦЕНТРАЛЬНОГО ДЕЙСТВИЯ, ЦЕНТРАЛЬНОГО ДЕЙСТВИЯ МИОРЕЛАКСАНТЫ |
| Polish | Leki zwiotczające mięśnie ośrodkowo |
| Japanese | 中枢性筋弛緩剤, 筋弛緩剤-中枢性, 中枢性骨格筋し緩薬, 中枢性骨格筋弛緩薬, 筋弛緩薬-中枢性 |
| Spanish | miorrelajante central, miorrelajante que actúa a nivel del sistema nervioso central, relajante muscular central (producto), relajante muscular central (sustancia), relajante muscular central, relajante muscular de acción central (sustancia), relajante muscular de acción central, Relajantes Musculares Centrales, Relajantes Musculares de Acción Central |
| German | Muskelrelaxanzien, zentralwirkende, Zentralwirkende Muskelrelaxantien |
| Italian | Miorilassanti ad azione centrale |
| Portuguese | Relaxantes Musculares Centrais, Relaxantes Musculares da Ação Central |
Ontology: tizanidine (C0146011)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C023754 |
| SnomedCT | 108461005, 373440006 |
| LNC | LP61793-3, MTHU025335 |
| English | 2,1,3-Benzothiadiazol-4-amine, 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-, 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole, tizanidine, tizanidine [Chemical/Ingredient], tiZANidine, TIZANIDINE, Tizanidine, Tizanidine (product), Tizanidine (substance) |
| Spanish | tizanidina (producto), tizanidina (sustancia), tizanidina |
