Generic Name:
baclofen
Trade Name:
Lioresal ® [Medtronic]
IUPAC Name:
4-amino-3-(4-chlorophenyl)-butanoic acid
Dosage Forms/Routes:
tablet/oral;
orally disintegrating tablet/oral;
injectable/intrathecal
Major Metabolite:
3-(p-chlorophenyl)-4-hydroxybutyric acid
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
11/22/1977
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link] (for Kemstro orally disintegrating tablet)
RxList:
[Link]
Empirical Formula:
C10H12ClNO2
Molecular Mass:
213.661 g/mol |
Possible Mechanism of Action:
Baclofen is a GABA-B receptor agonist (1).
Indications:
Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Patients should have reversible spasticity so that baclofen treatment will aid in restoring residual function.
Baclofen may also be of some value in patients with spinal cord injuries and other spinal cord diseases.
Baclofen is not indicated in the treatment of skeletal muscle spasm resulting from rheumatic disorders.
The efficacy of baclofen in stroke, cerebral palsy, and Parkinson's disease has not been established and therefore, it is not recommended for these conditions.
|
Chemical Class:
gamma-aminobutyric acid (GABA) analog
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
carisoprodol
Trade Name:
Soma ® [MedPointe]
IUPAC Name:
[2-(carbamoyloxymethyl)-2-methyl-pentyl] N-
propan-2-ylcarbamate
Dosage Forms/Routes:
tablet/oral
Major Metabolites:
meprobamate;
hydroxycarisprodol;
hydroxymeprobamate
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
04/09/1959
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link]
RxList:
[Link]
Empirical Formula:
C12H24N2O4
Molecular Mass:
260.33 g/mol |
Possible Mechanism of Action:
Carisoprodol's mechanisms of action are still poorly understood. Carisoprodol's primary metabolite, meprobamate, has barbiturate- like modulatory effects on GABA-A receptors (2). High doses of carisoprodol may induce symptoms that are similar to the symptoms associated with serotonin syndrome (3).
Indications:
Carisoprodol is indicated as an adjunct to rest, physical therapy, and other measures for
the relief of discomfort associated with acute, painful musculoskeletal conditions.
|
Chemical Class:
carbamic acid ester
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
chlorzoxazone
Trade Name:
Parafon Forte DSC ® [Ortho-McNeil]
IUPAC Name:
5-chloro-3H-benzooxazol-2-one
Dosage Forms/Routes:
tablet/oral;
Major Metabolite:
6-hydroxychlorzoxazone
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
08/15/1958
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link]
RxList:
[Link]
Empirical Formula:
C7H4ClNO2
Molecular Mass:
169.565 g/mol |
Possible Mechanism of Action:
Chlorzoxazone increases the open probability of IK1 (KCNN4), an intermediate conductance, inwardly-rectifying K+ channel that is calcium-activated (4). The drug does not increase the affinity of the IK1 (SK4) channel for Ca2+ ions, but its effect upon the chanels is Ca2+ dependent (4). In a similar manner, chlorzoxazone also activates SK2 (KCNN2), a small conductance, inwardly-rectifying K+ channel that is calcium-activated (4, 5). Although data related to chlorzoxazone's interaction with SK2 channels is based on experimentation with rat channels (rSK2), the rat protein is 97% identical to the highly homologous human protein, hSK2 (6). Potentially, chlorzoxazone may indirectly affect SK4 and SK2 channels via an interaction with calmodulin or another modulatory molecule (4). The drug may also act indirectly by inducing membrane hyperpolarization and reducing the firing rate in neurons that are involved in muscle spasticity or pain (4). In addition, chlorzoxazone is an inhibitor of inducible nitric oxide synthase (7).
Indications:
Chlorzoxazone is indicated as an adjunct to rest, physical therapy, and
other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. |
Chemical Class:
benzoxazole derivative
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
cyclobenzaprine hydrochloride
Trade Name:
Flexeril ® [Ortho-McNeil]
IUPAC Name:
3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-
N,N-dimethyl-1-propanamine hydrochloride
Dosage Forms/Routes:
tablet/oral;
extended release capsule/oral
Major Metabolites:
cyclobenzaprine-10,11-epoxide;
trans-10,11-dihydrodiol-cyclobenzaprine;
cyclobenzaprine N-glucuronide
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
08/26/1977
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link]
RxList:
[Link]
Empirical Formula:
C20H22ClN
Molecular Mass:
311.848g/mol |
Possible Mechanism of Action:
Cyclobenzaprine is an antagonist at one or more of the serotonin 5-HT2 receptor subtypes (8). In neonatal rats, 5-HT2C receptor activation has been associated with a long-lasting amplification of the spinal flexion reflex (9). Thus, cyclobenzaprine is likely to reduce muscle tone via its antagonism of 5-HT2C receptors (8). In addition, the drug exhibits anticholinergic effects (10, 11). Thus, cyclobenzaprine and/or one of its metabolites is likely to be an antagonist at one or more of the muscarinic acetylcholine receptors.
Indications:
Flexeril is indicated as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions.
Improvement is manifested by relief of muscle spasm and its associated signs and symptoms, namely, pain, tenderness, limitation of motion, and restriction in activities of daily living.
Flexeril should be used only for short periods (up to two or three weeks) because adequate evidence of effectiveness for more prolonged use is not available and because muscle spasm associated with acute, painful musculoskeletal conditions is generally of short duration and specific therapy for longer periods is seldom warranted.
Flexeril has not been found effective in the treatment of spasticity associated with cerebral or spinal cord disease, or in children with cerebral palsy. |
Chemical Class:
tricyclic amine salt
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
diazepam
Trade Name:
Valium ® [Roche]
IUPAC Name:
9-chloro-2-methyl-6-phenyl-
2,5-diazabicyclo[5.4.0]undeca-
5,8,10,12-tetraen-3-one
Dosage Forms/Routes:
tablet/oral;
injectable/injection;
solution/oral;
concentrate/oral;
gel/rectal;
Major Metabolites:
nordiazepam;
temazepam;
oxazepam
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
11/15/1963
Manufacturers:
[FDA Search]
Prescribing Information:
[Link]
RxList:
[Link]
Empirical Formula:
C16H13ClN2O
Molecular Mass:
284.74 g/mol |
Possible Mechanism of Action:
Diazepam is a nonselective benzodiazepine agonist (12). Diazepam is also an agonist at peripheral benzodiazepine receptors (13).
Indications:
Diazepam is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma); spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia); athetosis; and stiff-man syndrome. The drug is also indicated as an adjunct treatment for convulsive disorders. In addition, diazepam is indicated for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. In acute alcohol withdrawal, diazepam may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis.
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Chemical Class:
2-keto benzodiazepine
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
metaxalone
Trade Name:
Skelaxin ® [King Pharmaceuticals]
IUPAC Name:
5-[(3,5-dimethylphenoxy)methyl]-1,3-
oxazolidin-2-one
Dosage Forms/Routes:
tablet/oral
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
08/13/1962
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link]
RxList:
[Link]
Empirical Formula:
C12H15NO3
Molecular Mass:
221.252g/mol |
Possible Mechanism of Action:
The mechanism of action of metaxalone
in humans has not been established, but may be due to general
central nervous system depression (Prescribing Information, 2006). Metaxalone has no direct
action on the contractile mechanism of striated muscle, the motor
end plate or the nerve fiber (Prescribing Information, 2006).
Indications:
Metaxalone is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. Metaxalone does not directly relax tense skeletal muscles in humans.
|
Chemical Class:
oxazolidinone derivative
PubChem 2D Structure:
 |
Generic Name:
methocarbamol
Trade Name:
Robaxin ® [Schwarz]
IUPAC Name:
[2-hydroxy-3-(2-methoxyphenoxy)propyl] carbamate
Dosage Forms/Routes:
tablet/oral;
injectable/injection
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
07/16/1957
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link] (tablet)
[Link] (injectable)
RxList:
[Link]
Empirical Formula:
C11H15NO5
Molecular Mass:
241.241g/mol |
Possible Mechanism of Action:
The mechanism of action of methocarbamol in humans has not been established, but may be due to
general CNS depression (Prescribing Information, 2003). It has no direct action on the contractile mechanism of striated muscle, the
motor end plate or the nerve fiber (Prescribing Information, 2003).
Indications:
Methocarbamol is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. Methocarbamol does not directly relax tense skeletal muscles in humans.
|
Chemical Class:
carbamic acid ester; derivative of guaifenesin
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
orphenadrine citrate
Trade Name:
Norflex ® [Graceway]
IUPAC Name:
N,N-dimethyl-2-[(2-methylphenyl)-
phenyl-methoxy]-ethanamine
Dosage Forms/Routes:
injectable/injection;
extended release tablet/oral
Major Metabolites:
N-monodemethylorphenadrine;
N,N-didemethylorphendrine;
orphenadrine N-oxide;
glucuronide/sulfate of
o-methylbenzhydrylosxyacetic acid;
o-methylbenzhydrol
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
11/04/1959
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link] (injectable)
RxList:
[Link]
Empirical Formula:
C24H31NO8
Molecular Mass:
461.505g/mol |
Possible Mechanism of Action:
Orphenadrine is a non-competitive antagonist at NMDA receptor complexes (14). In addition, the drug is an antagonist at histamine H1 receptors (15). Orphenadrine may also act as an antagonist at M1, M2, M3, and M4 muscarinic acetylcholine receptors (16).
Indications:
Orphenadrine citrate is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions.
|
Chemical Class:
ethanolamine
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
Generic Name:
tizanidine hydrochloride
Trade Name:
Zanaflex ® [Acorda]
IUPAC Name:
3-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-8-
thia-7,9-diazabicyclo[4.3.0]non a-2,4,6,9-
tetraen-2-amine hydrochloride
Dosage Forms/Routes:
tablet/oral;
capsule/oral
Major Metabolites:
(5-chloro-4-(2-imidazolin-4-on-2-ylamino)-
2,1,3-benzothiazdiazole;
5-chloro-4-(guanidino)-2,1,3-benzothiazdiazole
Database Search Links:
[PubMed]
[Search PubMed for
Randomized Controlled Trials]
[PubChem]
[PDSP Ki database] |
Initial Approval:
11/27/1996
Manufacturers:
[FDA Search]
Prescribing
Information:
[Link]
RxList:
[Link]
Empirical Formula:
C9H9Cl2N5S
Molecular Mass:
290.173g/mol |
Possible Mechanism of Action:
Tizanidine is an agonist at imidazoline receptors (17, 18, 19). It is also an agonist at alpha-2 andrenoceptors (18, 19).
Indications:
Tizanidine is a short-acting drug for the management of spasticity. Because of the short duration of effect, treatment with tizanidine should be reserved for those daily activities and times when relief of spasticity is most important.
|
Chemical Class:
imidazoline derivative
PubChem 2D Structure:
"3D" Structure (Requires Chime):
[Link] |
