Muscle Relaxants, Centrally Acting Agents

Name
Muscle Relaxants, Centrally Acting Agents
Accession Number
DBCAT002177  (DBCAT000429, DBCAT002521, DBCAT003685)
Description

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)

ATC Classification
Drugs
DrugDrug Description
MeprobamateAn anxiolytic drug used for the short-term management of anxiety symptoms.
ChlorphenesinA phenol ether used to treat painful muscular conditions.
FludiazepamUsed for the short-term treatment of anxiety disorders.
XylazineXylazine is a clonidine analog which acts as an agonist at α2 adrenoceptors. Veterinarians also use xylazine as an emetic, especially in cats.
ChlorproethazineNot Annotated
MedazepamNot Annotated
BaclofenA GABA-ergic agonist used to manage severe spasticity of cerebral or spinal origin in adult and pediatric patients.
ChlorzoxazoneA drug with muscle relaxant properties that is used as an adjunct to physical therapy and analgesics to treat stiffness and pain caused by a variety of musculoskeletal conditions.
CarisoprodolA centrally acting muscle relaxant used to relieve the discomfort associated with various musculoskeletal conditions.
MethocarbamolA CNS depressant indicated with rest, physical therapy and other treatments to control the discomfort associated with various acute musculoskeletal conditions.
TizanidineAn alpha-2 adrenergic agonist used for the short-term treatment of muscle spasticity.
CyclobenzaprineA skeletal muscle relaxant that works on the brainstem to treat muscle spasms of local origin.
OrphenadrineA muscarinic antagonist used as an adjunct for the symptomatic relief of musculoskeletal pain and discomfort.
ChlormezanoneUsed in the management of anxiety and in the treatment of muscle spasm.
DantroleneA direct-acting skeletal muscle relaxant used for the treatment of management of the fulminant hypermetabolism of skeletal muscle leading to malignant hyperthermia crisis.
EperisoneEperisone is an antispasmodic drug which relaxes both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression...
ThiocolchicosideThiocolchicoside is a skeletal muscle-relaxant drug used in the treatment of orthopedic, traumatic and rheumatologic disorders . It is indicated as an adjuvant drug in the treatment of painful muscle...
FebarbamateNot Annotated
TetrazepamNot Annotated
PhenprobamateNot Annotated
StyramateNot Annotated
FenyramidolNot Annotated
MephenesinA cresol glyceryl ether used to treat muscle spasticity in Parkinson's and Multiple Sclerosis.
PridinolNot Annotated
TolperisoneInvestigated for use/treatment in neurologic disorders, spinal cord injuries, muscle spasm, back pain, and multiple sclerosis.
MetaxaloneA muscle relaxant used to treat muscle pain or spasm.
BromazepamA short-acting benzodiazepine with intermediate onset commonly used to treat panic disorders and severe anxiety.
DiazepamA long-acting benzodiazepine with rapid onset commonly used to treat panic disorders, severe anxiety, alcohol withdrawal, and seizures.
ClonazepamA long-acting benzodiazepine with intermediate onset commonly used to treat panic disorders, severe anxiety, and seizures.
FlunitrazepamFor short-term treatment of severe insomnias, that are not responsive to other hypnotics.
LorazepamA long-acting benzodiazepine commonly used to treat panic disorders, severe anxiety, and seizures.
NitrazepamA long-acting benzodiazepine with intermediate onset commonly used to treat panic disorders, severe anxiety, insomnia, and seizures.
TemazepamA short-acting benzodiazepine commonly used to treat panic disorders, severe anxiety, and insomnia.
EszopicloneA sedative-hypnotic used in the treatment of insomnia, improving both the latency phase and the maintenance phase of sleep.
EtizolamIndicated for the treatment of generalized anxiety disorder with depression, panic disorder and insomnia.
MethaqualoneFor the treatment of insomnia, and as a sedative and muscle relaxant.
Arbaclofen PlacarbilInvestigated for the treatment of spasticity in multiple sclerosis, acute back spasms, and GERD.
DonepezilAn acetylcholinesterase inhibitor used to treat the behavioral and cognitive effects of Alzheimer's Disease and other types of dementia.
MephenoxaloneNot Annotated
PregabalinAn anticonvulsant drug used to treat neuropathic pain conditions and fibromyalgia, and for the treatment of partial onset seizures in combination with other anticonvulsants.
QuinineAn alkaloid used to treat uncomplicated Plasmodium falciparum malaria.
Y-27632Y-27632 is an inhibitor of Rho-associated protein kinase. It inhibits calcium sensitization to affect smooth muscle relaxation.
Drugs & Drug Targets
DrugTargetType
MeprobamateGamma-aminobutyric acid receptor subunit alpha-1target
MeprobamateGamma-aminobutyric acid receptor subunit alpha-2target
MeprobamateGamma-aminobutyric acid receptor subunit alpha-3target
MeprobamateGamma-aminobutyric acid receptor subunit alpha-4target
MeprobamateGamma-aminobutyric acid receptor subunit alpha-5target
MeprobamateGamma-aminobutyric acid receptor subunit alpha-6target
MeprobamateGABA(A) Receptortarget
ChlorphenesinCytochrome P450 19A1enzyme
ChlorphenesinCytochrome P450 3A4enzyme
ChlorphenesinXanthine dehydrogenase/oxidaseenzyme
ChlorphenesinProstaglandin G/H synthase 2enzyme
ChlorphenesinCholinesteraseenzyme
FludiazepamGamma-aminobutyric acid receptor subunit alpha-2target
FludiazepamGamma-aminobutyric acid receptor subunit alpha-1target
FludiazepamGamma-aminobutyric acid receptor subunit alpha-3target
FludiazepamGamma-aminobutyric acid receptor subunit alpha-5target
FludiazepamGamma-aminobutyric acid receptor subunit gamma-1target
FludiazepamGamma-aminobutyric acid receptor subunit gamma-2target
FludiazepamGamma-aminobutyric acid receptor subunit gamma-3target
FludiazepamGamma-aminobutyric acid receptor subunit beta-1target
FludiazepamGamma-aminobutyric acid receptor subunit beta-2target
FludiazepamGamma-aminobutyric acid receptor subunit beta-3target
FludiazepamGamma-aminobutyric acid receptor subunit deltatarget
FludiazepamGamma-aminobutyric acid receptor subunit epsilontarget
FludiazepamGamma-aminobutyric acid receptor subunit pitarget
FludiazepamGamma-aminobutyric acid receptor subunit rho-1target
FludiazepamGamma-aminobutyric acid receptor subunit rho-2target
FludiazepamGamma-aminobutyric acid receptor subunit rho-3target
XylazineAlpha-2 adrenergic receptorstarget
MedazepamGABA(A) Receptortarget
MedazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
BaclofenGamma-aminobutyric acid type B receptor subunit 1target
BaclofenGamma-aminobutyric acid type B receptor subunit 2target
ChlorzoxazoneCalcium-activated potassium channel subunit alpha-1target
ChlorzoxazoneCytochrome P450 2E1enzyme
ChlorzoxazoneCytochrome P450 1A2enzyme
ChlorzoxazoneCytochrome P450 2A6enzyme
ChlorzoxazoneCytochrome P450 1A1enzyme
ChlorzoxazoneCytochrome P450 2D6enzyme
ChlorzoxazoneCytochrome P450 3A4enzyme
CarisoprodolCytochrome P450 2C19enzyme
CarisoprodolGamma-aminobutyric acid receptor subunit alpha-1target
CarisoprodolGamma-aminobutyric acid receptor subunit beta-2target
CarisoprodolGamma-aminobutyric acid receptor subunit gamma-2target
CarisoprodolGamma-aminobutyric acid receptor subunit alpha-5target
CarisoprodolGamma-aminobutyric acid receptor subunit alpha-3target
MethocarbamolCarbonic anhydrase 1target
TizanidineAlpha-2 adrenergic receptorstarget
TizanidineCytochrome P450 1A2enzyme
TizanidineNischarintarget
TizanidineAlpha-1 adrenergic receptorstarget
Cyclobenzaprine5-hydroxytryptamine receptor 2Atarget
CyclobenzaprineCytochrome P450 1A2enzyme
CyclobenzaprineCytochrome P450 3A4enzyme
CyclobenzaprineCytochrome P450 2D6enzyme
CyclobenzaprineSerum albumincarrier
CyclobenzaprineUDP-glucuronosyltransferase 1-4enzyme
CyclobenzaprineUDP-glucuronosyltransferase 2B10enzyme
Cyclobenzaprine5-hydroxytryptamine receptor 2Btarget
Cyclobenzaprine5-hydroxytryptamine receptor 2Ctarget
Cyclobenzaprine5-hydroxytryptamine receptor 7target
Cyclobenzaprine5-hydroxytryptamine receptor 6target
CyclobenzaprineSodium-dependent serotonin transportertarget
CyclobenzaprineSodium-dependent noradrenaline transportertarget
CyclobenzaprineToll-like receptor 4target
CyclobenzaprineAldehyde oxidasetarget
OrphenadrineGlutamate receptor ionotropic, NMDA 1target
OrphenadrineGlutamate receptor ionotropic, NMDA 2Dtarget
OrphenadrineGlutamate receptor ionotropic, NMDA 3Btarget
OrphenadrineGlutamate receptor ionotropic, NMDA 3Atarget
OrphenadrineHistamine H1 receptortarget
OrphenadrineCytochrome P450 2B6enzyme
OrphenadrineCytochrome P450 2E1enzyme
OrphenadrineCytochrome P450 3A4enzyme
OrphenadrineSodium-dependent noradrenaline transportertarget
OrphenadrineSodium channel protein type 10 subunit alphatarget
OrphenadrineCytochrome P450 1A2enzyme
OrphenadrineCytochrome P450 2D6enzyme
ChlormezanoneTranslocator proteintarget
DantroleneRyanodine receptor 1target
DantroleneThyroxine-binding globulincarrier
EperisoneCytochrome P450 3A4enzyme
ThiocolchicosideGABA(A) Receptortarget
ThiocolchicosideGlycine receptor subunit alpha-1target
ThiocolchicosideTumor necrosis factor ligand superfamily member 11target
TolperisoneCytochrome P450 1A2enzyme
BromazepamCytochrome P450 1A2enzyme
BromazepamCytochrome P450 2C19enzyme
BromazepamCytochrome P450 2E1enzyme
BromazepamGABA(A) Receptortarget
BromazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
DiazepamCytochrome P450 3A4enzyme
DiazepamSerum albumincarrier
DiazepamCytochrome P450 2C9enzyme
DiazepamCytochrome P450 2C19enzyme
DiazepamCytochrome P450 3A5enzyme
DiazepamCytochrome P450 3A7enzyme
DiazepamP-glycoprotein 1transporter
DiazepamCytochrome P450 2B6enzyme
DiazepamProstaglandin G/H synthase 1enzyme
DiazepamCytochrome P450 2C18enzyme
DiazepamCytochrome P450 2C8enzyme
DiazepamCytochrome P450 2E1enzyme
DiazepamGABA(A) Receptortarget
DiazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
ClonazepamCytochrome P450 3A4enzyme
ClonazepamSerum albumincarrier
ClonazepamCytochrome P450 2E1enzyme
ClonazepamArylamine N-acetyltransferase 2enzyme
ClonazepamGABA(A) Receptortarget
ClonazepamNuclear receptor subfamily 1 group I member 2target
ClonazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
FlunitrazepamCytochrome P450 2C19enzyme
FlunitrazepamUDP-glucuronosyltransferase 2B7enzyme
FlunitrazepamCytochrome P450 2A6enzyme
FlunitrazepamCytochrome P450 2B6enzyme
FlunitrazepamCytochrome P450 2C9enzyme
FlunitrazepamCytochrome P450 3A4enzyme
FlunitrazepamCytochrome P450 2E1enzyme
FlunitrazepamUDP-glucuronosyltransferase 1-1enzyme
FlunitrazepamUDP-glucuronosyltransferase 1-3enzyme
FlunitrazepamGABA(A) Receptortarget
FlunitrazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
LorazepamUDP-glucuronosyltransferase 2B15enzyme
LorazepamGABA(A) Receptortarget
LorazepamCytochrome P450 3A4enzyme
LorazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
NitrazepamSodium channel protein type 1 subunit alphatarget
NitrazepamCytochrome P450 3A4enzyme
NitrazepamCytochrome P450 2E1enzyme
NitrazepamGABA(A) Receptortarget
NitrazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
TemazepamCytochrome P450 3A4enzyme
TemazepamCytochrome P450 2B6enzyme
TemazepamCytochrome P450 2C9enzyme
TemazepamGABA(A) Receptortarget
TemazepamGABA(A) Receptor Benzodiazepine Binding Sitetarget
EszopicloneCytochrome P450 3A4enzyme
EszopicloneGamma-aminobutyric acid receptor subunit alpha-1target
EszopicloneGamma-aminobutyric acid receptor subunit alpha-2target
EszopicloneGamma-aminobutyric acid receptor subunit alpha-3target
EszopicloneGamma-aminobutyric acid receptor subunit alpha-5target
EszopicloneCytochrome P450 2C8enzyme
EszopicloneGABA(A) Receptortarget
EtizolamCytochrome P450 3A4enzyme
EtizolamCytochrome P450 2C18enzyme
EtizolamCytochrome P450 2C19enzyme
EtizolamPlatelet-activating factor receptortarget
EtizolamGABA(A) Receptortarget
EtizolamGABA(A) Receptor Benzodiazepine Binding Sitetarget
MethaqualoneCytochrome P450 3A4enzyme
Arbaclofen PlacarbilMonocarboxylate transporter 1transporter
Arbaclofen PlacarbilGamma-aminobutyric acid type B receptor subunit 1target
Arbaclofen PlacarbilGamma-aminobutyric acid type B receptor subunit 2target
DonepezilAcetylcholinesterasetarget
Donepezil5-hydroxytryptamine receptor 2Atarget
DonepezilCytochrome P450 3A4enzyme
DonepezilCytochrome P450 2D6enzyme
DonepezilCytochrome P450 2C9enzyme
DonepezilCholinesterasetarget
DonepezilNitric oxide synthase, braintarget
DonepezilTumor necrosis factor-inducible gene 6 proteintarget
DonepezilInterleukin-1 betatarget
DonepezilNuclear factor NF-kappa-Btarget
DonepezilATP-binding cassette sub-family G member 2transporter
DonepezilNMDA receptortarget
PregabalinExcitatory amino acid transporter 3transporter
PregabalinVoltage-dependent calcium channel subunit alpha-2/delta-1target
PregabalinLarge neutral amino acids transporter small subunit 1transporter
QuininePlatelet glycoprotein IXtarget
QuinineIntermediate conductance calcium-activated potassium channel protein 4target
QuinineCytochrome P450 3A4enzyme
QuinineCytochrome P450 3A5enzyme
QuinineCytochrome P450 1A1enzyme
QuinineCytochrome P450 2D6enzyme
QuinineCytochrome P450 1A2enzyme
QuinineCytochrome P450 2C8enzyme
QuinineCytochrome P450 2C9enzyme
QuinineCytochrome P450 2C19enzyme
QuinineCytochrome P450 2E1enzyme
QuinineCytochrome P450 3A7enzyme
QuinineSolute carrier family 22 member 2transporter
QuinineSolute carrier family 22 member 1transporter
QuinineSolute carrier family 22 member 5transporter
QuinineP-glycoprotein 1transporter
QuinineSolute carrier organic anion transporter family member 1A2transporter
QuinineSolute carrier family 22 member 4transporter
QuinineFe(II)-protoporphyrin IXtarget
QuinineSolute carrier organic anion transporter family member 1B1transporter
Y-27632cAMP-dependent protein kinase catalytic subunit alphatarget
Y-27632cAMP-dependent protein kinase inhibitor alphatarget
Y-27632Rho-associated protein kinase 1target
Y-27632Rho-associated protein kinase 2target