II. Pathophysiology

  1. These agents are used to reduce severe spasticity (e.g. spinal cord injury, Cerebral Palsy, Multiple Sclerosis)

III. Indications: Spasticity

  1. Cerebral Palsy
  2. Multiple Sclerosis
  3. Spinal Cord Injury

IV. Contraindications

  1. Not indicated for general musculoskeletal problems

V. Agents

  1. Baclofen (Lioresal)
    1. Baclofen binds GABA B receptors
    2. Oral Baclofen does not cross blood brain barrier well
    3. Instead, Baclofen is typically used via Baclofen Intrathecal Pump (due to poor )
  2. Dantrolene (Dantrium)
  3. Tizanidine (Zanaflex)

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Cost: Medications

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

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
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
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
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