baclofen Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O
0.55 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2.10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 69 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.22 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.65 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.69 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.24 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 1977 FDA

FDA Adverse Event Reporting System (Female)

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 3837.49 41.55 632 5240 1021 2351192
Hypertonia 3010.51 41.55 493 5379 737 2351476
Drug withdrawal syndrome 2370.41 41.55 530 5342 6291 2345922
Overdose 1348.17 41.55 424 5448 19483 2332730
Completed suicide 1210.10 41.55 396 5476 20638 2331575
Pain 1069.16 41.55 484 5388 61373 2290840
Somnolence 1041.86 41.55 364 5508 23121 2329092
Drug ineffective 985.33 41.55 536 5336 101088 2251125
Toxicity to various agents 909.63 41.55 360 5512 32394 2319819
Coma 895.18 41.55 259 5613 8797 2343416
Hypotonia 886.43 41.55 186 5686 1544 2350669
Implant site infection 818.63 41.55 132 5740 158 2352055
Muscle spasms 721.67 41.55 272 5600 21294 2330919
Therapy non-responder 717.58 41.55 213 5659 7891 2344322
Implant site extravasation 698.02 41.55 107 5765 63 2352150
Complication associated with device 636.79 41.55 158 5714 2911 2349302
Therapeutic response decreased 627.50 41.55 187 5685 7008 2345205
Withdrawal syndrome 574.45 41.55 148 5724 3189 2349024
Mental status changes 512.21 41.55 151 5721 5431 2346782
Unresponsive to stimuli 483.00 41.55 140 5732 4736 2347477
Seizure 471.37 41.55 208 5664 24258 2327955
Device failure 427.47 41.55 103 5769 1662 2350551
Pruritus 426.97 41.55 233 5639 43107 2309106
Device dislocation 422.22 41.55 116 5756 3212 2349001
Cerebrospinal fluid leakage 389.78 41.55 67 5805 148 2352065
Underdose 373.58 41.55 121 5751 5957 2346256
Confusional state 364.95 41.55 174 5698 24170 2328043
Device malfunction 349.79 41.55 100 5772 3207 2349006
Muscle tightness 344.67 41.55 88 5784 1817 2350396
Pneumonia aspiration 328.85 41.55 98 5774 3644 2348569
Depressed level of consciousness 297.59 41.55 108 5764 7496 2344717
Agitation 289.05 41.55 117 5755 10934 2341279
Fall 284.50 41.55 185 5687 46914 2305299
Vomiting 278.95 41.55 215 5657 71387 2280826
Device infusion issue 265.93 41.55 48 5824 155 2352058
Death 256.55 41.55 216 5656 81252 2270961
Intentional overdose 252.52 41.55 107 5765 11214 2340999
Lethargy 251.03 41.55 99 5773 8631 2343582
Device physical property issue 248.99 41.55 46 5826 175 2352038
Condition aggravated 246.94 41.55 147 5725 31832 2320381
Muscular weakness 242.88 41.55 113 5759 14784 2337429
Pyrexia 241.63 41.55 176 5696 53532 2298681
Musculoskeletal stiffness 241.17 41.55 106 5766 12141 2340072
Hypotension 234.65 41.55 143 5729 32293 2319920
Implant site pain 228.34 41.55 48 5824 397 2351816
Tremor 227.58 41.55 120 5752 20541 2331672
Nausea 222.69 41.55 230 5642 111959 2240254
Implant site erosion 222.38 41.55 33 5839 9 2352204
Drug hypersensitivity 221.43 41.55 158 5714 46485 2305728
Infection 219.45 41.55 112 5760 17917 2334296
Implant site discharge 219.17 41.55 34 5838 24 2352189
Intracranial hypotension 217.47 41.55 39 5833 120 2352093
Respiratory arrest 216.69 41.55 81 5791 6097 2346116
Implant site swelling 215.07 41.55 37 5835 82 2352131
Delirium 214.78 41.55 77 5795 5146 2347067
Wound dehiscence 211.79 41.55 49 5823 654 2351559
Device connection issue 209.87 41.55 37 5835 100 2352113
Clonus 207.83 41.55 47 5825 563 2351650
Headache 204.89 41.55 189 5683 79990 2272223
Urinary tract infection 198.67 41.55 125 5747 29817 2322396
Sedation 190.46 41.55 63 5809 3299 2348914
Loss of consciousness 189.72 41.55 103 5769 18664 2333549
Device breakage 188.44 41.55 53 5819 1594 2350619
Hyperhidrosis 182.36 41.55 94 5778 15328 2336885
Cardiac arrest 182.32 41.55 93 5779 14837 2337376
Bradycardia 182.31 41.55 82 5790 9899 2342314
Respiratory depression 178.28 41.55 54 5818 2116 2350097
Seroma 172.36 41.55 35 5837 239 2351974
Device kink 168.76 41.55 34 5838 222 2351991
Asthenia 167.16 41.55 134 5738 46792 2305421
Device occlusion 163.20 41.55 41 5831 788 2351425
Hallucination 161.80 41.55 71 5801 8077 2344136
Device battery issue 160.61 41.55 26 5846 32 2352181
Poisoning 160.34 41.55 53 5819 2767 2349446
Cardio-respiratory arrest 160.23 41.55 73 5799 9073 2343140
Paraesthesia 158.49 41.55 97 5775 21991 2330222
Gastrooesophageal reflux disease 151.19 41.55 70 5802 9025 2343188
Respiratory failure 149.98 41.55 79 5793 13449 2338764
Medical device site infection 148.95 41.55 24 5848 28 2352185
Meningitis 147.67 41.55 40 5832 1042 2351171
Tachycardia 146.42 41.55 83 5789 16326 2335887
Device leakage 142.85 41.55 39 5833 1047 2351166
Gait disturbance 141.59 41.55 91 5781 22454 2329759
Device issue 141.28 41.55 59 5813 5940 2346273
Device alarm issue 141.19 41.55 29 5843 211 2352002
Asphyxia 141.17 41.55 38 5834 966 2351247
Back pain 140.22 41.55 103 5769 31556 2320657
Dystonia 139.97 41.55 45 5827 2149 2350064
Muscle rigidity 139.47 41.55 43 5829 1788 2350425
Encephalopathy 138.99 41.55 54 5818 4507 2347706
Anxiety 133.35 41.55 97 5775 29262 2322951
Hypertension 132.51 41.55 94 5778 27267 2324946
Status epilepticus 130.62 41.55 44 5828 2434 2349779
Device related infection 129.97 41.55 47 5825 3212 2349001
Malaise 122.45 41.55 121 5751 55464 2296749
Irritability 121.10 41.55 54 5818 6373 2345840
Post lumbar puncture syndrome 120.01 41.55 24 5848 150 2352063
Suicide attempt 119.68 41.55 64 5808 11218 2340995
Multiple sclerosis 118.71 41.55 52 5820 5882 2346331
Disorientation 118.34 41.55 53 5819 6319 2345894
Pneumonia 117.35 41.55 112 5760 49184 2303029
Poisoning deliberate 116.81 41.55 34 5838 1157 2351056
Hypothermia 116.62 41.55 39 5833 2109 2350104
Off label use 115.83 41.55 134 5738 73464 2278749
Hypoaesthesia 115.65 41.55 77 5795 20138 2332075
Infusion site mass 115.33 41.55 21 5851 72 2352141
Altered state of consciousness 115.11 41.55 45 5827 3815 2348398
Insomnia 114.33 41.55 84 5788 25703 2326510
Generalised tonic-clonic seizure 113.74 41.55 49 5823 5323 2346890
Decubitus ulcer 112.08 41.55 34 5838 1337 2350876
Device inversion 110.69 41.55 16 5856 1 2352212
Arteriosclerosis coronary artery 108.49 41.55 32 5840 1141 2351072
Device power source issue 107.31 41.55 16 5856 5 2352208
Dizziness 106.26 41.55 115 5757 58550 2293663
Toxic encephalopathy 105.83 41.55 29 5843 789 2351424
Dyskinesia 105.73 41.55 45 5827 4744 2347469
Unevaluable event 104.41 41.55 54 5818 8837 2343376
Hyporeflexia 98.44 41.55 24 5848 405 2351808
Implant site erythema 96.39 41.55 19 5853 109 2352104
Postoperative wound infection 94.94 41.55 29 5843 1167 2351046
Accidental overdose 93.26 41.55 39 5833 3933 2348280
Pseudomeningocele 91.37 41.55 14 5858 8 2352205
Pain in extremity 90.58 41.55 91 5781 42449 2309764
Paralysis 90.33 41.55 31 5841 1813 2350400
Wound 89.15 41.55 34 5838 2694 2349519
Cognitive disorder 84.97 41.55 40 5832 5341 2346872
Medical device discomfort 84.59 41.55 21 5851 383 2351830
Abnormal behaviour 83.31 41.55 38 5834 4722 2347491
Neurotoxicity 78.53 41.55 29 5843 2101 2350112
Speech disorder 78.01 41.55 40 5832 6424 2345789
Discomfort 77.33 41.55 37 5835 5122 2347091
Feeling abnormal 76.68 41.55 64 5808 23517 2328696
Blood creatine phosphokinase increased 74.45 41.55 36 5836 5100 2347113
Myoclonus 74.20 41.55 29 5843 2454 2349759
Therapy cessation 74.07 41.55 36 5836 5157 2347056
Movement disorder 73.96 41.55 30 5842 2798 2349415
Dysarthria 73.17 41.55 38 5834 6264 2345949
Urinary incontinence 71.58 41.55 33 5839 4200 2348013
Implant site reaction 70.48 41.55 14 5858 84 2352129
Respiratory disorder 70.17 41.55 32 5840 3972 2348241
Incorrect route of product administration 70.17 41.55 35 5837 5301 2346912
Miosis 69.52 41.55 23 5849 1201 2351012
Diplopia 68.09 41.55 30 5842 3435 2348778
Muscle twitching 67.77 41.55 28 5844 2737 2349476
Staphylococcal infection 67.29 41.55 34 5838 5292 2346921
Areflexia 66.49 41.55 19 5853 604 2351609
Apnoea 66.31 41.55 23 5849 1388 2350825
Medical device site pain 66.16 41.55 12 5860 40 2352173
Fatigue 64.48 41.55 109 5763 84764 2267449
Medical device site discharge 64.48 41.55 10 5862 7 2352206
Bradypnoea 63.70 41.55 17 5855 417 2351796
Post procedural complication 62.68 41.55 27 5845 2927 2349286
Hospitalisation 62.64 41.55 47 5825 14806 2337407
Respiratory distress 62.63 41.55 32 5840 5097 2347116
Disturbance in attention 62.35 41.55 33 5839 5652 2346561
Electroencephalogram abnormal 61.18 41.55 19 5853 808 2351405
Pocket erosion 61.00 41.55 9 5863 2 2352211
Constipation 60.75 41.55 54 5818 21575 2330638
Urinary retention 60.17 41.55 28 5844 3639 2348574
Weight decreased 59.04 41.55 60 5812 28311 2323902
Neck pain 58.16 41.55 35 5837 7662 2344551
Incorrect dose administered 57.96 41.55 38 5834 9657 2342556
Granuloma 57.51 41.55 17 5855 610 2351603
Dysphagia 57.31 41.55 42 5830 12763 2339450
Medical device site swelling 57.08 41.55 9 5863 8 2352205
Hypoventilation 55.98 41.55 17 5855 670 2351543
Drug interaction 55.86 41.55 59 5813 29104 2323109
Implant site scar 55.81 41.55 11 5861 63 2352150
Gait inability 55.40 41.55 31 5841 5924 2346289
Burning sensation 55.05 41.55 34 5838 7794 2344419
Cancer pain 53.99 41.55 14 5858 306 2351907
Sepsis 53.59 41.55 47 5825 18441 2333772
Adverse drug reaction 53.29 41.55 34 5838 8249 2343964
Incision site complication 52.63 41.55 12 5860 149 2352064
Blood pressure decreased 52.30 41.55 35 5837 9201 2343012
Implant site haematoma 50.33 41.55 9 5863 27 2352186
Amnesia 49.73 41.55 31 5841 7222 2344991
Rhabdomyolysis 49.39 41.55 30 5842 6674 2345539
Depression 48.77 41.55 54 5818 28078 2324135
Impaired healing 47.18 41.55 27 5845 5384 2346829
Multiple sclerosis relapse 46.95 41.55 35 5837 10908 2341305
Incision site oedema 46.40 41.55 8 5864 18 2352195
Respiratory rate decreased 45.90 41.55 14 5858 560 2351653
Urosepsis 44.98 41.55 19 5853 1962 2350251
Incorrect drug administration rate 44.29 41.55 12 5860 312 2351901
Swelling 44.26 41.55 40 5832 16310 2335903
Scoliosis 42.25 41.55 15 5857 969 2351244
Injury 42.21 41.55 26 5846 5928 2346285
Heart rate increased 42.10 41.55 33 5839 11072 2341141
Medical device site erosion 41.87 41.55 6 5866 0 2352213
Memory impairment 41.80 41.55 35 5837 12888 2339325

FDA Adverse Event Reporting System (Male)

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 5423.65 47.87 910 5721 539 1739611
Hypertonia 3789.06 47.87 667 5964 710 1739440
Drug withdrawal syndrome 3378.03 47.87 735 5896 3790 1736360
Implant site infection 1495.68 47.87 245 6386 75 1740075
Overdose 1494.38 47.87 511 6120 16190 1723960
Drug ineffective 1166.49 47.87 632 5999 63169 1676981
Complication associated with device 1067.91 47.87 229 6402 1037 1739113
Muscle spasms 1053.05 47.87 360 6271 11261 1728889
Hypotonia 1018.81 47.87 229 6402 1341 1738809
Pain 970.74 47.87 425 6206 26232 1713918
Implant site extravasation 906.60 47.87 147 6484 32 1740118
Therapy non-responder 879.81 47.87 271 6360 5995 1734155
Therapeutic response decreased 810.62 47.87 247 6384 5253 1734897
Somnolence 784.53 47.87 320 6311 16419 1723731
Withdrawal syndrome 777.64 47.87 198 6433 2090 1738060
Device failure 726.34 47.87 153 6478 620 1739530
Toxicity to various agents 705.75 47.87 351 6280 28790 1711360
Mental status changes 674.95 47.87 220 6411 5855 1734295
Coma 624.78 47.87 217 6414 7045 1733105
Infection 492.57 47.87 211 6420 12149 1728001
Wound dehiscence 486.35 47.87 106 6525 520 1739630
Confusional state 477.42 47.87 244 6387 21034 1719116
Underdose 452.62 47.87 146 6485 3734 1736416
Device malfunction 443.86 47.87 124 6507 1900 1738250
Muscle tightness 429.44 47.87 105 6526 918 1739232
Device dislocation 415.58 47.87 94 6537 562 1739588
Completed suicide 415.36 47.87 204 6427 16108 1724042
Seizure 405.55 47.87 216 6415 20225 1719925
Pyrexia 403.01 47.87 289 6342 46111 1694039
Condition aggravated 393.04 47.87 214 6417 20936 1719214
Pruritus 382.44 47.87 217 6414 23005 1717145
Hyperhidrosis 362.55 47.87 171 6460 12317 1727833
Cerebrospinal fluid leakage 347.13 47.87 65 6566 115 1740035
Clonus 339.19 47.87 75 6556 397 1739753
Implant site swelling 338.80 47.87 55 6576 12 1740138
Agitation 338.57 47.87 157 6474 10869 1729281
Device physical property issue 334.65 47.87 60 6571 71 1740079
Implant site erosion 333.07 47.87 53 6578 4 1740146
Intracranial hypotension 331.53 47.87 60 6571 78 1740072
Urinary tract infection 316.11 47.87 146 6485 10007 1730143
Intentional overdose 315.07 47.87 134 6497 7536 1732614
Device breakage 305.88 47.87 64 6567 247 1739903
Unresponsive to stimuli 302.17 47.87 113 6518 4516 1735634
Tachycardia 297.53 47.87 150 6481 12478 1727672
Lethargy 283.42 47.87 122 6509 7062 1733088
Hypotension 261.67 47.87 187 6444 29467 1710683
Medical device site infection 260.17 47.87 45 6586 35 1740115
Device related infection 258.07 47.87 84 6547 2202 1737948
Respiratory depression 255.41 47.87 83 6548 2164 1737986
Tremor 254.85 47.87 137 6494 12994 1727156
Sedation 254.66 47.87 92 6539 3325 1736825
Device issue 251.28 47.87 84 6547 2398 1737752
Depressed level of consciousness 250.32 47.87 109 6522 6483 1733667
Meningitis 249.09 47.87 67 6564 880 1739270
Device infusion issue 248.53 47.87 47 6584 90 1740060
Device connection issue 247.10 47.87 45 6586 62 1740088
Vomiting 246.33 47.87 200 6431 38115 1702035
Device occlusion 241.42 47.87 65 6566 857 1739293
Device kink 233.16 47.87 42 6589 52 1740098
Implant site discharge 223.30 47.87 37 6594 14 1740136
Implant site erythema 217.72 47.87 36 6595 13 1740137
Musculoskeletal stiffness 216.02 47.87 95 6536 5781 1734369
Staphylococcal infection 215.77 47.87 89 6542 4618 1735532
Pocket erosion 214.15 47.87 34 6597 2 1740148
Delirium 205.62 47.87 94 6537 6268 1733882
Fall 202.45 47.87 155 6476 27059 1713091
Implant site pain 200.80 47.87 35 6596 30 1740120
Hypertension 197.80 47.87 134 6497 19314 1720836
Hallucination 192.00 47.87 97 6534 8073 1732077
Dystonia 191.33 47.87 65 6566 1949 1738201
Decubitus ulcer 187.91 47.87 55 6576 998 1739152
Device alarm issue 183.20 47.87 36 6595 92 1740058
Respiratory failure 181.85 47.87 114 6517 14391 1725759
Irritability 176.41 47.87 81 6550 5451 1734699
Bradycardia 171.53 47.87 98 6533 10436 1729714
Suicide attempt 165.73 47.87 85 6546 7296 1732854
Insomnia 165.04 47.87 112 6519 16164 1723986
Headache 164.86 47.87 152 6479 34224 1705926
Device leakage 161.86 47.87 43 6588 536 1739614
Seroma 160.50 47.87 33 6598 114 1740036
Device battery issue 160.09 47.87 28 6603 25 1740125
Cardiac arrest 160.04 47.87 109 6522 15821 1724329
Sepsis 158.32 47.87 117 6514 19321 1720829
Muscular weakness 157.93 47.87 92 6539 10157 1729993
Nausea 155.67 47.87 177 6454 51019 1689131
Toxic encephalopathy 146.79 47.87 42 6589 700 1739450
Autonomic nervous system imbalance 144.92 47.87 37 6594 390 1739760
Urinary retention 138.32 47.87 68 6563 5327 1734823
Infusion site mass 137.44 47.87 24 6607 21 1740129
Off label use 135.53 47.87 144 6487 38427 1701723
Medical device site discharge 135.30 47.87 22 6609 5 1740145
Purulent discharge 134.38 47.87 37 6594 532 1739618
Loss of consciousness 133.48 47.87 95 6536 14780 1725370
Device power source issue 132.26 47.87 22 6609 9 1740141
Dyskinesia 131.44 47.87 59 6572 3760 1736390
Neurotoxicity 130.41 47.87 49 6582 1975 1738175
Encephalopathy 128.90 47.87 61 6570 4391 1735759
Staphylococcus test positive 127.87 47.87 34 6597 425 1739725
Muscle rigidity 127.33 47.87 47 6584 1801 1738349
Gait disturbance 125.52 47.87 86 6545 12584 1727566
Poisoning deliberate 124.30 47.87 38 6593 804 1739346
Discomfort 121.23 47.87 50 6581 2586 1737564
Asthenia 120.95 47.87 129 6502 34541 1705609
Respiratory disorder 119.14 47.87 52 6579 3097 1737053
Constipation 119.14 47.87 89 6542 14911 1725239
Medical device site swelling 117.11 47.87 19 6612 4 1740146
Medical device site erythema 115.52 47.87 19 6612 6 1740144
Anxiety 114.20 47.87 88 6543 15439 1724711
Altered state of consciousness 113.91 47.87 52 6579 3445 1736705
Respiratory arrest 110.45 47.87 60 6571 5779 1734371
Implant site scar 106.13 47.87 17 6614 2 1740148
Unevaluable event 105.57 47.87 59 6572 6007 1734143
Malaise 103.02 47.87 110 6521 29455 1710695
Autonomic dysreflexia 102.42 47.87 18 6613 17 1740133
Hypothermia 100.67 47.87 39 6592 1709 1738441
Back pain 100.54 47.87 84 6547 16529 1723621
Heart rate increased 99.03 47.87 58 6573 6452 1733698
Medical device site erosion 96.58 47.87 16 6615 6 1740144
Pneumonia aspiration 96.50 47.87 53 6578 5213 1734937
Granuloma 96.29 47.87 28 6603 495 1739655
Sleep apnoea syndrome 96.14 47.87 40 6591 2114 1738036
Hospitalisation 95.58 47.87 73 6558 12627 1727523
Hallucination, visual 95.44 47.87 42 6589 2550 1737600
Performance status decreased 94.87 47.87 30 6601 712 1739438
Device computer issue 92.72 47.87 16 6615 12 1740138
Disorientation 91.92 47.87 52 6579 5417 1734733
Arachnoiditis 91.23 47.87 19 6612 71 1740079
Implant site haematoma 90.40 47.87 17 6614 31 1740119
Scar 89.91 47.87 30 6601 848 1739302
Apnoea 89.41 47.87 34 6597 1415 1738735
Cognitive disorder 88.90 47.87 47 6584 4283 1735867
Dysphagia 86.68 47.87 63 6568 10105 1730045
Muscle twitching 85.63 47.87 35 6596 1767 1738383
CSF culture positive 85.43 47.87 15 6616 14 1740136
Paraesthesia 85.13 47.87 63 6568 10388 1729762
Respiratory distress 83.88 47.87 48 6583 5109 1735041
Areflexia 83.84 47.87 25 6606 484 1739666
Post lumbar puncture syndrome 81.95 47.87 17 6614 62 1740088
Injury 80.90 47.87 39 6592 2921 1737229
Pneumonia 79.59 47.87 121 6510 46061 1694089
Pain in extremity 79.32 47.87 77 6554 18395 1721755
Incision site erythema 78.20 47.87 15 6616 32 1740118
Incorrect dose administered 77.36 47.87 52 6579 7357 1732793
Respiratory rate decreased 75.12 47.87 22 6609 399 1739751
Hypoaesthesia 75.00 47.87 57 6574 9778 1730372
Scoliosis 74.26 47.87 20 6611 263 1739887
Medical device site reaction 74.11 47.87 13 6618 12 1740138
Cardio-respiratory arrest 73.39 47.87 55 6576 9238 1730912
Incision site complication 72.89 47.87 16 6615 81 1740069
Macrophages increased 71.39 47.87 12 6619 6 1740144
Wound infection staphylococcal 70.82 47.87 19 6612 246 1739904
Impaired healing 70.53 47.87 34 6597 2545 1737605
Gait inability 70.43 47.87 37 6594 3326 1736824
Therapeutic product effect decreased 70.10 47.87 46 6585 6251 1733899
Abnormal behaviour 69.80 47.87 46 6585 6296 1733854
Medical device discomfort 67.94 47.87 12 6619 12 1740138
Hyperthermia 67.45 47.87 29 6602 1662 1738488
Implant site reaction 67.38 47.87 13 6618 29 1740121
Therapy cessation 67.06 47.87 35 6596 3104 1737046
Death 65.76 47.87 161 6470 87282 1652868
Device extrusion 65.67 47.87 12 6619 17 1740133
Postoperative wound infection 65.48 47.87 22 6609 635 1739515
Asphyxia 65.33 47.87 25 6606 1058 1739092
Myoclonus 65.02 47.87 31 6600 2264 1737886
Psychotic disorder 63.86 47.87 40 6591 5016 1735134
Medical device change 63.41 47.87 13 6618 44 1740106
Dizziness 63.36 47.87 93 6538 34268 1705882
Depression 63.26 47.87 65 6566 16604 1723546
Alcohol poisoning 62.55 47.87 20 6611 492 1739658
Blood pressure increased 62.16 47.87 53 6578 10700 1729450
Status epilepticus 62.15 47.87 29 6602 2017 1738133
Wound 61.83 47.87 27 6604 1607 1738543
Aggression 61.78 47.87 47 6584 8068 1732082
Central nervous system infection 61.68 47.87 15 6616 127 1740023
Miosis 61.11 47.87 26 6605 1452 1738698
Incorrect route of product administration 61.06 47.87 34 6597 3431 1736719
Skin erosion 60.09 47.87 18 6613 354 1739796
Speech disorder 60.01 47.87 37 6594 4511 1735639
Purulence 59.80 47.87 17 6614 276 1739874
Implant site cellulitis 58.84 47.87 10 6621 6 1740144
Generalised tonic-clonic seizure 58.75 47.87 35 6596 4011 1736139
Incorrect drug administration rate 58.16 47.87 17 6614 306 1739844
Blood creatine phosphokinase increased 58.15 47.87 47 6584 8809 1731341
Priapism 58.04 47.87 25 6606 1439 1738711
Post procedural complication 57.98 47.87 29 6602 2351 1737799
Accidental overdose 57.82 47.87 35 6596 4129 1736021
Intentional self-injury 57.65 47.87 30 6601 2643 1737507
Wound infection 57.38 47.87 22 6609 936 1739214
Hypoventilation 57.23 47.87 19 6612 528 1739622
Mydriasis 57.10 47.87 24 6607 1300 1738850
Restlessness 56.63 47.87 35 6596 4286 1735864
Mental disorder 55.91 47.87 30 6601 2813 1737337
Dysarthria 55.09 47.87 37 6594 5222 1734928
Urosepsis 54.77 47.87 24 6607 1440 1738710
Electrocardiogram QRS complex prolonged 54.43 47.87 20 6611 755 1739395
Medical device site fibrosis 53.88 47.87 9 6622 4 1740146
Muscle contracture 53.38 47.87 15 6616 233 1739917
Treatment noncompliance 53.07 47.87 36 6595 5165 1734985
Medical device site pain 52.56 47.87 10 6621 20 1740130
Movement disorder 51.75 47.87 24 6607 1646 1738504
Posturing 51.69 47.87 13 6618 128 1740022
Urinary incontinence 51.37 47.87 28 6603 2708 1737442
Scratch 51.08 47.87 17 6614 476 1739674
Brain injury 48.89 47.87 20 6611 1011 1739139
Bradypnoea 48.84 47.87 15 6616 322 1739828
Paranoia 48.53 47.87 25 6606 2156 1737994
Hypoxic-ischaemic encephalopathy 48.16 47.87 19 6612 873 1739277

Pharmacologic Action:

SourceCodeDescription
ATC M03BX01 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Other centrally acting agents
FDA MoA N0000000196 GABA A Agonists
FDA MoA N0000000116 GABA B Agonists
FDA EPC N0000175759 gamma-Aminobutyric Acid-ergic Agonist
CHEBI has role CHEBI:51371 muscle relaxant
CHEBI has role CHEBI:35488 central nervous system depressant
CHEBI has role CHEBI:51373 GABA 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)

DiseaseRelationSNOMED_IDDOID
Muscle spasticity of spinal origin indication 416830008
Muscle Spasticity of Cerebral Origin indication
Trigeminal neuralgia off-label use 31681005 DOID:12098
Disorder of autonomic nervous system contraindication 15241006
Schizophrenia contraindication 58214004 DOID:5419
Psychotic disorder contraindication 69322001
Epilepsy contraindication 84757009 DOID:1826
Kidney disease contraindication 90708001 DOID:557
Autonomic dysreflexia contraindication 129618003
Cerebrovascular accident contraindication 230690007
Functional disorder of bladder neck and sphincter mechanism contraindication 236644005
Impaired cognition contraindication 386806002
Central nervous system depression contraindication 418072004

Acid dissociation constants calculated using MoKa v3.0.0

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:

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:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0115-1010 TABLET 10 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 0115-1012 TABLET 20 mg ORAL ANDA 11 sections
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 0904-6475 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
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
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 42254-029 TABLET 20 mg ORAL ANDA 11 sections
Baclofen HUMAN PRESCRIPTION DRUG LABEL 1 42254-061 TABLET 10 mg ORAL ANDA 11 sections