baclofen indications/contra

Stem definitionDrug idCAS RN
282 1134-47-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • baclofen
  • baclon
  • lioresal
  • DL-Baclofen
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.
  • Molecular weight: 213.66
  • Formula: C10H12ClNO2
  • CLOGP: -0.62
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 63.32
  • ALOGS: -2.48
  • ROTB: 4

Drug dosage:

DoseUnitRoute
50 mg O
0.55 mg P

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 1977 FDA

FDA Adverse Event Reporting System

scroll-->
MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Muscle spasticity 8988.88 44.15 1471 9255 1265 3373868
Drug withdrawal syndrome 5121.05 44.15 1163 9563 10622 3364511
Hypertonia 4411.63 44.15 768 9958 1222 3373911
Overdose 2258.22 44.15 771 9955 33207 3341926
Implant site infection 2230.56 44.15 368 10358 313 3374820
Pain 1671.76 44.15 762 9964 70795 3304338
Muscle spasms 1645.17 44.15 575 10151 26328 3348805
Hypotonia 1612.20 44.15 352 10374 2519 3372614
Implant site extravasation 1599.97 44.15 253 10473 105 3375028
Therapy non-responder 1548.73 44.15 443 10283 10366 3364767
Therapeutic response decreased 1472.35 44.15 425 10301 10273 3364860
Somnolence 1290.74 44.15 505 10221 31699 3343434
Complication associated with device 1276.22 44.15 343 10383 6295 3368838
Drug ineffective 1207.84 44.15 719 10007 115371 3259762
Coma 1109.71 44.15 355 10371 12197 3362936
Mental status changes 1051.05 44.15 324 10402 9823 3365310
Withdrawal syndrome 1045.19 44.15 269 10457 4125 3371008
Toxicity to various agents 1017.99 44.15 477 10249 46577 3328556
Completed suicide 960.29 44.15 405 10321 30709 3344424
Underdose 905.31 44.15 264 10462 6570 3368563
Device failure 860.52 44.15 206 10520 2295 3372838
Device malfunction 806.01 44.15 220 10506 4264 3370869
Seizure 776.20 44.15 378 10348 40022 3335111
Cerebrospinal fluid leakage 770.86 44.15 134 10592 200 3374933
Wound dehiscence 758.53 44.15 163 10563 1061 3374072
Infection 740.82 44.15 318 10408 25084 3350049
Muscle tightness 731.26 44.15 179 10547 2202 3372931
Pruritus 729.03 44.15 380 10346 46453 3328680
Condition aggravated 699.47 44.15 349 10377 38884 3336249
Confusional state 692.12 44.15 343 10383 37655 3337478

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC M03BX01 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Other centrally acting agents
CHEBI has role CHEBI:51371 muscle relaxant
CHEBI has role CHEBI:35488 central nervous system depressant
CHEBI has role CHEBI:51373 GABA agonist
FDA MoA N0000000196 GABA A Agonists
FDA MoA N0000000116 GABA B Agonists
FDA EPC N0000175759 gamma-Aminobutyric Acid-ergic Agonist
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018682 GABA Agents
MeSH PA D018755 GABA Agonists
MeSH PA D058786 GABA-B Receptor Agonists
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Muscle spasticity of spinal origin indication 416830008
Muscle Spasticity of Cerebral Origin indication
Disorder of autonomic nervous system contraindication 15241006
Schizophrenia contraindication 58214004
Psychotic disorder contraindication 69322001
Epilepsy contraindication 84757009 DOID:1826
Kidney disease contraindication 90708001 DOID:2527
Autonomic dysreflexia contraindication 129618003
Cerebrovascular accident contraindication 230690007 DOID:6713
Functional disorder of bladder neck and sphincter mechanism contraindication 236644005
Impaired cognition contraindication 386806002
Central nervous system depression contraindication 418072004
Trigeminal neuralgia off-label use 31681005 DOID:12098

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.95 acidic
pKa2 9.54 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
GABA-B receptor GPCR AGONIST IC50 7.46 CHEMBL CHEMBL
Adenosine receptor A3 GPCR IC50 7.30 CHEMBL
GABA B receptor GPCR IC50 7.52 CHEMBL
GABA-A receptor; anion channel Ion channel IC50 7.52 CHEMBL

External reference:

scroll-->
IDSource
DB00181 DRUGBANK_ID
1084 IUPHAR_LIGAND_ID
4018392 VUID
N0000146719 NUI
C0004609 UMLSCUI
D00241 KEGG_DRUG
CHEMBL701 ChEMBL_ID
2284 PUBCHEM_CID
4018392 VANDF
N0000146719 NDFRT
N0000006613 NDFRT
001677 NDDF
709 MMSL
1292 RXNORM
387342009 SNOMEDCT_US
6102009 SNOMEDCT_US
4243 MMSL
d00967 MMSL
CHEBI:2972 CHEBI
H789N3FKE8 UNII
2956 INN_ID
D001418 MESH_DESCRIPTOR_UI
2C0 PDB_CHEM_ID

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0172-4096 TABLET 10 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0172-4097 TABLET 20 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0527-1330 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0527-1337 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0603-2406 TABLET 10 mg ORAL ANDA 13 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0603-2407 TABLET 20 mg ORAL ANDA 13 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0615-3541 TABLET 10 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0615-3542 TABLET 20 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0832-1024 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0832-1025 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0832-1054 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0832-1055 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0904-3365 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0904-5222 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0904-6475 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0904-6476 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 10135-532 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 10135-533 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 10544-172 TABLET 10 mg ORAL ANDA 12 sections
Equipto - Baclofen External Cream Compounding Kit HUMAN PRESCRIPTION DRUG LABEL 1 15455-0701 KIT 1 g TOPICAL unapproved drug other 6 sections
Gapeam Budibac HUMAN PRESCRIPTION DRUG LABEL 7 15455-0717 KIT 1 g TOPICAL unapproved drug other 5 sections
BACLOFEN HUMAN PRESCRIPTION DRUG LABEL 1 16590-026 TABLET 10 mg ORAL ANDA 11 sections
BACLOFEN HUMAN PRESCRIPTION DRUG LABEL 1 16590-027 TABLET 20 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 16714-071 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 16714-072 TABLET 20 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 17856-1024 TABLET 10 mg ORAL ANDA 12 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 21695-014 TABLET 10 mg ORAL ANDA 13 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 21695-015 TABLET 20 mg ORAL ANDA 13 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 33261-010 TABLET 10 mg ORAL ANDA 13 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 33261-011 TABLET 20 mg ORAL ANDA 13 sections