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

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 4061 26839-75-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • timolol
  • timolol maleate
  • (-)-Timolol
  • (S)-Timolol
  • arutimol
  • L-Timolol
  • timolol maleate salt
A beta-adrenergic antagonist that is similar in action to PROPRANOLOL; the levo-isomer is more active. Timolol has been proposed as an anti-hypertensive, anti-arrhythmic, anti-angina, and anti-glaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.
  • Molecular weight: 316.42
  • Formula: C13H24N4O3S
  • CLOGP: 1.53
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 79.74
  • ALOGS: -3.07
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
20 mg O
20 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2.74 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 15 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.16 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 61 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.50 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.90 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 17, 1978 FDA ATON
March 25, 2020 PMDA Senju Pharmaceutical Co., Ltd

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
Treatment failure 975.36 12.52 588 21958 92499 46571017
Intraocular pressure increased 647.82 12.52 199 22347 5758 46657758
Eye irritation 626.01 12.52 252 22294 16362 46647154
Glaucoma 529.91 12.52 221 22325 15700 46647816
Ocular hyperaemia 434.67 12.52 205 22341 19505 46644011
Eye pain 375.29 12.52 208 22338 27732 46635784
Eye pruritus 220.71 12.52 110 22436 11788 46651728
Vision blurred 173.63 12.52 203 22343 79505 46584011
Colitis microscopic 156.21 12.52 72 22474 6484 46657032
Visual acuity reduced 152.79 12.52 108 22438 22005 46641511
Foreign body sensation in eyes 127.80 12.52 44 22502 1832 46661684
Lacrimation increased 117.82 12.52 81 22465 15780 46647736
Product container issue 114.08 12.52 40 22506 1759 46661757
Choroidal effusion 104.40 12.52 27 22519 407 46663109
Hypersensitivity 98.12 12.52 221 22325 150100 46513416
Bradycardia 91.52 12.52 135 22411 66163 46597353
Iridocyclitis 88.07 12.52 34 22512 1966 46661550
Visual impairment 88.05 12.52 133 22413 66556 46596960
Cataract 87.87 12.52 109 22437 45306 46618210
Product delivery mechanism issue 87.66 12.52 22 22524 292 46663224
Eye discharge 86.77 12.52 44 22502 4884 46658632
Product quality issue 81.22 12.52 93 22453 35555 46627961
Total lung capacity increased 80.46 12.52 25 22521 749 46662767
Corneal disorder 78.74 12.52 30 22516 1673 46661843
Conjunctival hyperaemia 77.68 12.52 31 22515 1958 46661558
Skin reaction 76.83 12.52 54 22492 10892 46652624
Diverticulitis 76.63 12.52 87 22459 32952 46630564
Eye inflammation 69.97 12.52 35 22511 3774 46659742
Thyroid disorder 69.85 12.52 53 22493 12023 46651493
Corneal oedema 65.49 12.52 26 22520 1620 46661896
Choroidal detachment 62.03 12.52 15 22531 169 46663347
Eye swelling 60.88 12.52 61 22485 20042 46643474
Hypotony of eye 59.96 12.52 14 22532 134 46663382
Iris adhesions 58.06 12.52 16 22530 311 46663205
Completed suicide 55.09 12.52 4 22542 145916 46517600
Eyelid margin crusting 54.33 12.52 18 22528 665 46662851
Frustration tolerance decreased 54.20 12.52 33 22513 5224 46658292
Corneal opacity 53.59 12.52 18 22528 694 46662822
Ocular discomfort 53.15 12.52 27 22519 3008 46660508
Punctate keratitis 52.44 12.52 17 22529 586 46662930
Product packaging quantity issue 48.78 12.52 19 22527 1125 46662391
Intraocular pressure test abnormal 48.26 12.52 12 22534 153 46663363
Eye disorder 47.64 12.52 51 22495 18090 46645426
Cystoid macular oedema 46.64 12.52 20 22526 1516 46662000
Dry eye 46.58 12.52 65 22481 30257 46633259
Angle closure glaucoma 46.33 12.52 22 22524 2117 46661399
Corneal deposits 45.11 12.52 12 22534 203 46663313
Abnormal sensation in eye 41.33 12.52 19 22527 1699 46661817
Respiration abnormal 40.60 12.52 26 22520 4495 46659021
Forced expiratory volume decreased 40.11 12.52 27 22519 5077 46658439
Blindness 39.22 12.52 45 22501 17224 46646292
Eyelid irritation 38.41 12.52 12 22534 366 46663150
Conjunctivitis allergic 37.88 12.52 14 22532 717 46662799
Trabeculectomy 37.55 12.52 7 22539 18 46663498
Pulmonary thrombosis 37.41 12.52 30 22516 7372 46656144
Liquid product physical issue 36.74 12.52 13 22533 587 46662929
Ulcerative keratitis 36.12 12.52 19 22527 2274 46661242
Peak expiratory flow rate decreased 36.02 12.52 13 22533 622 46662894
Intraocular pressure decreased 35.89 12.52 9 22537 119 46663397
Lung diffusion test decreased 35.76 12.52 13 22533 635 46662881
Macular oedema 35.39 12.52 23 22523 4078 46659438
Uveitis 35.36 12.52 31 22515 8610 46654906
Sciatica 34.14 12.52 44 22502 18976 46644540
Erythema of eyelid 33.88 12.52 17 22529 1844 46661672
Open angle glaucoma 32.93 12.52 10 22536 277 46663239
Growth of eyelashes 32.85 12.52 9 22537 171 46663345
Keratopathy 32.30 12.52 10 22536 296 46663220
Swelling of eyelid 31.27 12.52 14 22532 1177 46662339
Normal tension glaucoma 30.07 12.52 7 22539 66 46663450
Serum procollagen type I N-terminal propeptide increased 29.98 12.52 6 22540 25 46663491
Procollagen type I C-terminal propeptide increased 29.98 12.52 6 22540 25 46663491
Febrile neutropenia 29.67 12.52 5 22541 94622 46568894
Vitreous opacities 29.54 12.52 9 22537 252 46663264
Hypopyon 29.46 12.52 12 22534 799 46662717
Exposure during pregnancy 29.29 12.52 8 22538 108204 46555312
Corneal degeneration 29.10 12.52 7 22539 77 46663439
Toxic anterior segment syndrome 28.89 12.52 16 22530 2121 46661395
Obstructive airways disorder 28.87 12.52 34 22512 13378 46650138
Vitreous floaters 28.86 12.52 22 22524 5023 46658493
Visual acuity reduced transiently 28.81 12.52 8 22538 160 46663356
Toxicity to various agents 28.78 12.52 36 22510 211730 46451786
Pain 28.57 12.52 126 22420 476822 46186694
Blepharitis 28.32 12.52 16 22530 2205 46661311
Vitreous haemorrhage 28.26 12.52 15 22531 1829 46661687
Forced vital capacity decreased 28.17 12.52 12 22534 895 46662621
Conjunctival ulcer 27.49 12.52 6 22540 41 46663475
Incorrect dose administered 27.46 12.52 65 22481 45485 46618031
Corneal epithelium defect 26.97 12.52 9 22537 340 46663176
Eye allergy 26.89 12.52 10 22536 521 46662995
Flat anterior chamber of eye 25.55 12.52 6 22540 59 46663457
Eyelid oedema 25.24 12.52 28 22518 10329 46653187
Conjunctivitis 25.09 12.52 34 22512 15390 46648126
Vitamin B12 decreased 25.02 12.52 16 22530 2759 46660757
Corneal erosion 25.01 12.52 8 22538 264 46663252
Eyelid disorder 24.89 12.52 12 22534 1194 46662322
Fall 24.70 12.52 255 22291 328842 46334674
Dry mouth 24.50 12.52 70 22476 54856 46608660
Retinal detachment 24.36 12.52 20 22526 5080 46658436
Product physical consistency issue 24.33 12.52 9 22537 462 46663054
Nausea 24.33 12.52 214 22332 687240 45976276
Bronchitis 23.90 12.52 108 22438 105871 46557645
Chronotropic incompetence 23.81 12.52 6 22540 81 46663435
Photophobia 23.56 12.52 32 22514 14512 46649004
Thermal burns of eye 21.47 12.52 6 22540 123 46663393
Visual field defect 21.31 12.52 20 22526 6063 46657453
Eye colour change 21.19 12.52 7 22539 256 46663260
Corneal endothelial cell loss 21.01 12.52 4 22542 12 46663504
Abdominal pain 20.47 12.52 51 22495 229980 46433536
Foreign body in eye 20.23 12.52 6 22540 153 46663363
Retinal disorder 19.92 12.52 11 22535 1450 46662066
Hallucination, visual 19.90 12.52 33 22513 17840 46645676
Product deposit 19.87 12.52 6 22540 163 46663353
Superficial injury of eye 19.87 12.52 6 22540 163 46663353
Ocular hypertension 19.79 12.52 9 22537 785 46662731
Rabbit syndrome 19.78 12.52 7 22539 316 46663200
Corneal infiltrates 19.76 12.52 6 22540 166 46663350
Retinopathy haemorrhagic 19.56 12.52 4 22542 19 46663497
Symblepharon 19.48 12.52 5 22541 73 46663443
Rheumatoid arthritis 19.30 12.52 56 22490 240159 46423357
Systemic lupus erythematosus 19.24 12.52 4 22542 65176 46598340
Pyrexia 19.16 12.52 95 22451 348707 46314809
Conjunctival oedema 19.03 12.52 8 22538 577 46662939
Intraocular pressure fluctuation 18.63 12.52 4 22542 25 46663491
Corneal decompensation 18.50 12.52 4 22542 26 46663490
Reaction to preservatives 18.42 12.52 6 22540 210 46663306
Blood pressure systolic increased 18.36 12.52 42 22504 28745 46634771
Synovitis 18.33 12.52 68 22478 61007 46602509
Eye operation 18.18 12.52 11 22535 1721 46661795
Ocular pemphigoid 18.12 12.52 4 22542 29 46663487
Endophthalmitis 18.10 12.52 14 22532 3264 46660252
Product packaging issue 17.85 12.52 9 22537 987 46662529
Malignant glaucoma 17.83 12.52 3 22543 3 46663513
Blindness unilateral 17.60 12.52 17 22529 5340 46658176
Atrioventricular block complete 17.53 12.52 20 22526 7607 46655909
Corneal neovascularisation 17.47 12.52 5 22541 112 46663404
Product packaging difficult to open 17.35 12.52 4 22542 36 46663480
Keratic precipitates 17.35 12.52 5 22541 115 46663401
Thyroxine decreased 17.23 12.52 7 22539 463 46663053
Glaucoma surgery 17.16 12.52 4 22542 38 46663478
Iris neovascularisation 17.16 12.52 4 22542 38 46663478
Eyelid exfoliation 17.11 12.52 5 22541 121 46663395
Suicide attempt 17.05 12.52 3 22543 55033 46608483
Haemangioma congenital 16.95 12.52 7 22539 483 46663033
Product dispensing issue 16.80 12.52 4 22542 42 46663474
Corneal perforation 16.73 12.52 7 22539 499 46663017
Ophthalmic herpes simplex 16.63 12.52 6 22540 287 46663229
Bronchopulmonary disease 16.62 12.52 3 22543 6 46663510
Achromotrichia acquired 16.62 12.52 3 22543 6 46663510
C-reactive protein increased 16.56 12.52 64 22482 58526 46604990
Hypertension 16.07 12.52 155 22391 196201 46467315
Anterior chamber cell 15.87 12.52 7 22539 568 46662948
Keratolysis exfoliativa acquired 15.75 12.52 3 22543 9 46663507
Photopsia 15.74 12.52 14 22532 3962 46659554
Eyelid ptosis 15.55 12.52 17 22529 6171 46657345
Vitreal cells 15.55 12.52 4 22542 59 46663457
Retinal vascular occlusion 15.44 12.52 6 22540 353 46663163
Retinal vascular disorder 15.27 12.52 5 22541 178 46663338
Blepharal pigmentation 15.13 12.52 4 22542 66 46663450
Eyelid injury 15.09 12.52 3 22543 12 46663504
Metamorphopsia 14.97 12.52 8 22538 989 46662527
Conjunctival follicles 14.89 12.52 3 22543 13 46663503
Seborrhoeic keratosis 14.89 12.52 10 22536 1872 46661644
Hypotonia 14.71 12.52 19 22527 8210 46655306
Abdominal discomfort 14.65 12.52 32 22514 151133 46512383
Psoriasis 14.64 12.52 10 22536 78594 46584922
Keratitis 14.58 12.52 11 22535 2472 46661044
Corneal thickening 14.23 12.52 3 22543 17 46663499
Infusion related reaction 13.95 12.52 17 22529 101191 46562325
Dacryocystitis 13.94 12.52 3 22543 19 46663497
Instillation site reaction 13.75 12.52 6 22540 474 46663042
Accidental exposure to product 13.71 12.52 31 22515 21050 46642466
Iris hyperpigmentation 13.68 12.52 3 22543 21 46663495
Sinus bradycardia 13.44 12.52 24 22522 13758 46649758
Eyelid pain 13.31 12.52 5 22541 268 46663248
Drug ineffective 13.25 12.52 424 22122 677414 45986102
Counterfeit product administered 13.22 12.52 3 22543 25 46663491
Eczema eyelids 13.20 12.52 4 22542 110 46663406
Vitritis 13.11 12.52 7 22539 864 46662652
Subretinal fluid 12.88 12.52 5 22541 293 46663223
Iritis 12.86 12.52 10 22536 2351 46661165
Product use complaint 12.85 12.52 9 22537 1803 46661713
Foot amputation 12.69 12.52 5 22541 305 46663211
Toxic epidermal necrolysis 12.57 12.52 31 22515 22247 46641269

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
Intraocular pressure increased 763.49 13.52 221 15094 4899 29932264
Treatment failure 760.66 13.52 365 14950 34314 29902849
Eye irritation 436.98 13.52 148 15167 5548 29931615
Ocular hyperaemia 279.08 13.52 121 15194 8922 29928241
Eye pain 242.39 13.52 119 15196 11670 29925493
Visual acuity reduced 198.55 13.52 115 15200 15731 29921432
Glaucoma 188.62 13.52 81 15234 5827 29931336
Vision blurred 150.62 13.52 143 15172 41673 29895490
Corneal oedema 120.17 13.52 39 15276 1273 29935890
Cataract 105.04 13.52 88 15227 21747 29915416
Eye pruritus 97.00 13.52 45 15270 3882 29933281
Choroidal detachment 82.96 13.52 22 15293 346 29936817
Product delivery mechanism issue 82.49 13.52 18 15297 115 29937048
Visual impairment 81.93 13.52 89 15226 30349 29906814
Bradycardia 81.44 13.52 131 15184 65395 29871768
Corneal deposits 80.76 13.52 19 15296 177 29936986
Blindness 79.43 13.52 59 15256 12250 29924913
Eye discharge 73.40 13.52 29 15286 1684 29935479
Intraocular pressure decreased 73.36 13.52 16 15299 102 29937061
Hypotony of eye 71.21 13.52 16 15299 119 29937044
Lacrimation increased 69.94 13.52 44 15271 6972 29930191
Ocular discomfort 69.34 13.52 26 15289 1309 29935854
Toxic anterior segment syndrome 66.05 13.52 26 15289 1495 29935668
Ocular hypertension 62.97 13.52 21 15294 747 29936416
Hyphaema 62.46 13.52 18 15297 390 29936773
Product container issue 61.37 13.52 21 15294 809 29936354
Ocular surface disease 60.42 13.52 13 15302 77 29937086
Corneal disorder 57.88 13.52 20 15295 794 29936369
Blepharitis 57.36 13.52 21 15294 988 29936175
Open angle glaucoma 57.34 13.52 15 15300 223 29936940
Product quality issue 56.00 13.52 58 15257 18716 29918447
Anterior chamber disorder 55.96 13.52 13 15302 114 29937049
Foreign body sensation in eyes 53.05 13.52 17 15298 532 29936631
Choroidal effusion 52.42 13.52 13 15302 154 29937009
Visual field defect 52.36 13.52 31 15284 4405 29932758
Uveitis 51.23 13.52 33 15282 5444 29931719
Blindness unilateral 50.16 13.52 29 15286 3943 29933220
Punctate keratitis 48.20 13.52 14 15301 312 29936851
Intraocular pressure test abnormal 45.42 13.52 10 15305 67 29937096
Product packaging quantity issue 45.26 13.52 16 15299 680 29936483
Glaucoma surgery 43.53 13.52 8 15307 17 29937146
Corneal neovascularisation 42.17 13.52 9 15306 51 29937112
Cystoid macular oedema 41.72 13.52 15 15300 670 29936493
Conjunctival hyperaemia 41.01 13.52 21 15294 2246 29934917
Erythema of eyelid 39.13 13.52 14 15301 616 29936547
Iridocyclitis 37.47 13.52 17 15298 1392 29935771
Completed suicide 36.77 13.52 4 15311 99488 29837675
Eye swelling 36.75 13.52 33 15282 8931 29928232
Retinal detachment 36.60 13.52 26 15289 5034 29932129
Visual acuity tests abnormal 36.54 13.52 8 15307 52 29937111
Corneal opacity 36.47 13.52 13 15302 566 29936597
Ulcerative keratitis 34.55 13.52 16 15299 1373 29935790
Anterior chamber inflammation 33.77 13.52 10 15305 239 29936924
Dry eye 33.02 13.52 27 15288 6441 29930722
Eye inflammation 32.05 13.52 16 15299 1621 29935542
Corneal degeneration 31.69 13.52 6 15309 16 29937147
Retinal haemorrhage 31.18 13.52 23 15292 4720 29932443
Drug abuse 31.10 13.52 3 15312 82069 29855094
Angle closure glaucoma 29.96 13.52 12 15303 722 29936441
Thunderclap headache 29.77 13.52 7 15308 65 29937098
Eyelids pruritus 28.62 13.52 7 15308 78 29937085
Endophthalmitis 27.79 13.52 19 15296 3461 29933702
Eyelid oedema 27.75 13.52 22 15293 5023 29932140
Optic nerve injury 27.22 13.52 7 15308 97 29937066
Floppy iris syndrome 27.21 13.52 9 15306 312 29936851
Photophobia 26.97 13.52 23 15292 5813 29931350
Vitreous floaters 26.59 13.52 18 15297 3226 29933937
Conjunctivitis allergic 26.28 13.52 10 15305 524 29936639
Accidental exposure to product 26.19 13.52 29 15286 10086 29927077
Anterior chamber cell 25.76 13.52 9 15306 369 29936794
Flat anterior chamber of eye 24.85 13.52 6 15309 63 29937100
Eyelid irritation 24.68 13.52 6 15309 65 29937098
Conjunctival oedema 24.65 13.52 9 15306 420 29936743
Trabeculectomy 24.48 13.52 5 15310 22 29937141
Corneal pigmentation 24.08 13.52 4 15311 3 29937160
Cataract nuclear 23.33 13.52 9 15306 490 29936673
Eye disorder 23.25 13.52 24 15291 7710 29929453
Hypersensitivity 21.84 13.52 69 15246 53959 29883204
Instillation site pain 21.61 13.52 6 15309 113 29937050
Eye infection 21.47 13.52 15 15300 2827 29934336
Reversible cerebral vasoconstriction syndrome 21.23 13.52 7 15308 240 29936923
Abnormal sensation in eye 20.96 13.52 9 15306 646 29936517
Macular degeneration 20.91 13.52 13 15302 2015 29935148
Eyelid margin crusting 20.32 13.52 6 15309 142 29937021
Atrioventricular block second degree 20.13 13.52 15 15300 3125 29934038
Photocoagulation 19.89 13.52 4 15311 16 29937147
Growth of eyelashes 19.88 13.52 5 15310 63 29937100
Keratitis interstitial 19.51 13.52 4 15311 18 29937145
Corneal infection 19.51 13.52 4 15311 18 29937145
Corneal epithelium defect 19.15 13.52 7 15308 328 29936835
Ureteral disorder 19.06 13.52 6 15309 177 29936986
Superficial injury of eye 19.00 13.52 4 15311 21 29937142
Pupillary reflex impaired 18.85 13.52 11 15304 1521 29935642
Iris adhesions 18.33 13.52 6 15309 201 29936962
Iritis 17.76 13.52 10 15305 1292 29935871
Cutis laxa 17.59 13.52 5 15310 103 29937060
Retinal disorder 17.42 13.52 9 15306 980 29936183
Macular oedema 17.38 13.52 13 15302 2725 29934438
Sinus bradycardia 16.75 13.52 25 15290 11670 29925493
Liquid product physical issue 16.45 13.52 6 15309 279 29936884
Incorrect dose administered 16.19 13.52 44 15271 31642 29905521
Corneal endotheliitis 16.13 13.52 3 15312 7 29937156
Retinal vein occlusion 16.09 13.52 10 15305 1549 29935614
Alanine aminotransferase increased 16.05 13.52 9 15306 74267 29862896
Cataract operation 16.02 13.52 9 15306 1158 29936005
Optic nerve cupping 15.38 13.52 4 15311 58 29937105
Scleral hyperaemia 15.32 13.52 4 15311 59 29937104
Eyelid pain 14.79 13.52 4 15311 68 29937095
Eyelid disorder 14.66 13.52 6 15309 382 29936781
Hyperaemia 14.64 13.52 8 15307 975 29936188
Coronavirus infection 14.58 13.52 13 15302 3485 29933678
Macular fibrosis 14.55 13.52 6 15309 389 29936774
Cerebellar stroke 14.43 13.52 5 15310 200 29936963
Night blindness 14.43 13.52 5 15310 200 29936963
Ectropion 14.32 13.52 4 15311 77 29937086
Toxicity to various agents 14.18 13.52 45 15270 177138 29760025
Electrolyte depletion 14.13 13.52 5 15310 213 29936950
Intraocular pressure fluctuation 14.06 13.52 3 15312 17 29937146
Madarosis 14.00 13.52 5 15310 219 29936944
Iris neovascularisation 13.91 13.52 3 15312 18 29937145
Corneal infiltrates 13.87 13.52 5 15310 225 29936938

Pharmacologic Action:

SourceCodeDescription
ATC C07AA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, non-selective
ATC S01ED01 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Beta blocking agents
ATC C07BA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND THIAZIDES
Beta blocking agents, non-selective, and thiazides
ATC C07DA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, THIAZIDES AND OTHER DIURETICS
Beta blocking agents, non-selective, thiazides and other diuretics
ATC S01ED51 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Beta blocking agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:35530 beta-adrenoceptor antagonists
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:38070 antiarrhythmic agent
CHEBI has role CHEBI:39456 antiglaucoma agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Hypertensive disorder indication 38341003 DOID:10763
Open-angle glaucoma indication 84494001 DOID:1067
Myocardial Reinfarction Prevention indication
Migraine Prevention indication
Malignant glaucoma off-label use 10100008
Aphakic glaucoma off-label use 15374009
Secondary glaucoma off-label use 95717004
Angina pectoris off-label use 194828000
Angle-closure glaucoma off-label use 392291006 DOID:13550
Mitral valve prolapse off-label use 409712001
Stalled wound off-label use 789507005
Anuria contraindication 2472002 DOID:2983
Bronchospasm contraindication 4386001
Hypercholesterolemia contraindication 13644009
Secondary angle-closure glaucoma contraindication 21571006
Complete atrioventricular block contraindication 27885002
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Acute cerebrovascular insufficiency contraindication 29322000
Dehydration contraindication 34095006
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Hyperuricemia contraindication 35885006 DOID:1920
Anaphylaxis contraindication 39579001
Hypokalemia contraindication 43339004
Sinus bradycardia contraindication 49710005
General anesthesia contraindication 50697003
Thromboangiitis obliterans contraindication 52403007 DOID:12918
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Cerebrovascular disease contraindication 62914000 DOID:6713
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Pulmonary emphysema contraindication 87433001
Cardiogenic shock contraindication 89138009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Acute disease of cardiovascular system contraindication 128487001
Hypomagnesemia contraindication 190855004
Partial atrioventricular block contraindication 195039008
Decompensated cardiac failure contraindication 195111005
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Raynaud's phenomenon contraindication 266261006
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Right ventricular failure contraindication 367363000
Azotemia contraindication 445009001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.15 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.25% BASE TIMOLOL MALEATE ALEMBIC PHARMS LTD A212942 Oct. 22, 2020 RX SOLUTION, GEL FORMING/DROPS OPHTHALMIC May 24, 2021 COMPETITIVE GENERIC THERAPY
EQ 0.5% BASE TIMOLOL MALEATE ALEMBIC PHARMS LTD A212942 Oct. 22, 2020 RX SOLUTION, GEL FORMING/DROPS OPHTHALMIC May 24, 2021 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 9 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR ANTAGONIST Ki 9.70 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.81 DRUG MATRIX
Beta-3 adrenergic receptor GPCR Ki 6.47 DRUG MATRIX
Beta-2 adrenergic receptor GPCR Kd 9.78 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 6.21 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 9.44 CHEMBL

External reference:

IDSource
4019949 VUID
N0000148034 NUI
D00378 KEGG_DRUG
91524-16-2 SECONDARY_CAS_RN
4017930 VANDF
4019949 VANDF
C0040233 UMLSCUI
CHEBI:9599 CHEBI
TIM PDB_CHEM_ID
33624 PUBCHEM_CID
CHEMBL499 ChEMBL_ID
CHEMBL1200870 ChEMBL_ID
D013999 MESH_DESCRIPTOR_UI
DB00373 DRUGBANK_ID
817W3C6175 UNII
565 IUPHAR_LIGAND_ID
10600 RXNORM
5585 MMSL
6436 MMSL
d00139 MMSL
001856 NDDF
004741 NDDF
372880004 SNOMEDCT_US
75359005 SNOMEDCT_US
85591001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 0023-9211 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 26 sections
Timoptic in Ocudose HUMAN PRESCRIPTION DRUG LABEL 1 0187-1496 SOLUTION 6.80 mg OPHTHALMIC NDA 20 sections
Timoptic in Ocudose HUMAN PRESCRIPTION DRUG LABEL 1 0187-1498 SOLUTION 3.40 mg OPHTHALMIC NDA 20 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0055 TABLET 5 mg ORAL ANDA 22 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0221 TABLET 10 mg ORAL ANDA 22 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0715 TABLET 20 mg ORAL ANDA 22 sections
Dorzolamide Hydrochloride-Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0527-1763 SOLUTION 5 mg OPHTHALMIC ANDA 25 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 13811-618 TABLET 5 mg ORAL ANDA 14 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 13811-619 TABLET 10 mg ORAL ANDA 14 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 13811-620 TABLET 20 mg ORAL ANDA 14 sections
DORZOLAMIDE HYDROCHLORIDE TIMOLOL MALETAE Human Prescription Drug Label 2 14445-405 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 24 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-189 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 25 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-288 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-289 SOLUTION/ DROPS 2.50 mg OPHTHALMIC ANDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-365 SOLUTION/ DROPS 2.50 mg OPHTHALMIC ANDA 22 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-366 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 22 sections
Dorzolamide HCl and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 17478-514 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 28 sections
COSOPT PF HUMAN PRESCRIPTION DRUG LABEL 2 17478-604 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 26 sections
COSOPT HUMAN PRESCRIPTION DRUG LABEL 2 17478-605 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 28 sections
Istalol HUMAN PRESCRIPTION DRUG LABEL 1 24208-004 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 24 sections
Dorzolamide Hydrochloride and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 24208-486 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 25 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 24208-496 SOLUTION 6.80 mg OPHTHALMIC NDA authorized generic 12 sections
Timoptic HUMAN PRESCRIPTION DRUG LABEL 1 24208-812 SOLUTION 2.50 mg OPHTHALMIC NDA 25 sections
Timoptic HUMAN PRESCRIPTION DRUG LABEL 1 24208-813 SOLUTION 5 mg OPHTHALMIC NDA 25 sections
Timoptic-XE HUMAN PRESCRIPTION DRUG LABEL 1 24208-814 SOLUTION 2.50 mg OPHTHALMIC NDA 23 sections
Timoptic-XE HUMAN PRESCRIPTION DRUG LABEL 1 24208-816 SOLUTION 5 mg OPHTHALMIC NDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 24208-818 SOLUTION 2.50 mg OPHTHALMIC NDA authorized generic 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 24208-819 SOLUTION 5 mg OPHTHALMIC NDA authorized generic 23 sections
Dorzolamide Hydrochloride and Timolol Maleate ophthalmic Solution HUMAN PRESCRIPTION DRUG LABEL 2 42571-147 SOLUTION/ DROPS 6.80 mg OPHTHALMIC ANDA 24 sections
TIMOLOL MALEATE HUMAN PRESCRIPTION DRUG LABEL 1 45865-121 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 21 sections