timolol ๐Ÿถ Veterinary Use | 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: 1.78
  • 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 ยตM/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 749.76 13.21 495 15813 137142 50451674
Eye irritation 467.59 13.21 184 16124 16956 50571860
Intraocular pressure increased 379.25 13.21 118 16190 5398 50583418
Ocular hyperaemia 299.10 13.21 141 16167 20151 50568665
Eye pain 265.08 13.21 145 16163 28304 50560512
Glaucoma 162.98 13.21 86 16222 15600 50573216
Eye pruritus 139.59 13.21 72 16236 12462 50576354
Vision blurred 128.47 13.21 142 16166 78505 50510311
Visual acuity reduced 117.63 13.21 76 16232 20063 50568753
Product quality issue 98.99 13.21 81 16227 30777 50558039
Product container issue 95.72 13.21 30 16278 1402 50587414
Total lung capacity increased 92.01 13.21 25 16283 702 50588114
Lacrimation increased 79.76 13.21 56 16252 16936 50571880
Choroidal effusion 78.51 13.21 20 16288 434 50588382
Bradycardia 75.03 13.21 98 16210 64328 50524488
Foreign body sensation in eyes 73.32 13.21 26 16282 1785 50587031
Product delivery mechanism issue 70.00 13.21 17 16291 301 50588515
Eyelid margin crusting 69.16 13.21 20 16288 708 50588108
Frustration tolerance decreased 67.24 13.21 34 16274 5640 50583176
Iris adhesions 64.72 13.21 16 16292 306 50588510
Cataract 56.69 13.21 73 16235 47227 50541589
Corneal oedema 56.48 13.21 20 16288 1367 50587449
Ulcerative keratitis 56.44 13.21 23 16285 2310 50586506
Choroidal detachment 56.39 13.21 13 16295 182 50588634
Eye discharge 55.79 13.21 29 16279 5094 50583722
Hypotony of eye 54.55 13.21 12 16296 134 50588682
Forced expiratory volume decreased 54.03 13.21 27 16281 4367 50584449
Trabeculectomy 53.16 13.21 9 16299 19 50588797
Pulmonary thrombosis 50.38 13.21 31 16277 7510 50581306
Corneal deposits 50.38 13.21 12 16296 195 50588621
Respiration abnormal 47.45 13.21 26 16282 5076 50583740
Visual impairment 46.68 13.21 81 16227 68194 50520622
Eye inflammation 46.34 13.21 24 16284 4184 50584632
Product packaging quantity issue 45.60 13.21 16 16292 1064 50587752
Iridocyclitis 45.50 13.21 19 16289 2030 50586786
Corneal disorder 42.68 13.21 17 16291 1609 50587207
Peak expiratory flow rate decreased 42.16 13.21 13 16295 575 50588241
Conjunctival hyperaemia 41.89 13.21 18 16290 2064 50586752
Lung diffusion test decreased 41.71 13.21 13 16295 596 50588220
Intraocular pressure test abnormal 38.65 13.21 9 16299 132 50588684
Punctate keratitis 38.61 13.21 12 16296 545 50588271
Retinal disorder 37.24 13.21 15 16293 1462 50587354
Ocular discomfort 36.46 13.21 19 16289 3354 50585462
Cystoid macular oedema 34.56 13.21 14 16294 1385 50587431
Thermal burns of eye 33.47 13.21 8 16300 132 50588684
Angle closure glaucoma 32.62 13.21 15 16293 2019 50586797
Procollagen type I C-terminal propeptide increased 32.60 13.21 6 16302 24 50588792
Abnormal sensation in eye 32.47 13.21 14 16294 1619 50587197
Forced vital capacity decreased 32.45 13.21 12 16296 929 50587887
Serum procollagen type I N-terminal propeptide increased 32.40 13.21 6 16302 25 50588791
Hypersensitivity 32.23 13.21 146 16162 215015 50373801
Obstructive airways disorder 32.19 13.21 32 16276 15620 50573196
Eye swelling 32.19 13.21 36 16272 20108 50568708
Corneal degeneration 32.00 13.21 7 16301 76 50588740
Visual field defect 31.75 13.21 21 16287 5758 50583058
Incorrect dose administered 31.22 13.21 56 16252 48358 50540458
Growth of eyelashes 31.09 13.21 8 16300 181 50588635
Liquid product physical issue 30.78 13.21 11 16297 772 50588044
Conjunctival ulcer 30.30 13.21 6 16302 38 50588778
Abdominal discomfort 29.75 13.21 19 16289 231622 50357194
Completed suicide 29.10 13.21 4 16304 131885 50456931
Flat anterior chamber of eye 28.45 13.21 6 16302 54 50588762
Vitamin B12 decreased 28.00 13.21 15 16293 2800 50586016
Blindness 27.83 13.21 31 16277 17238 50571578
Pain 27.71 13.21 95 16213 578808 50010008
Macular oedema 26.93 13.21 16 16292 3638 50585178
Superficial injury of eye 26.61 13.21 7 16301 173 50588643
Glaucoma surgery 26.58 13.21 6 16302 76 50588740
Chronotropic incompetence 26.58 13.21 6 16302 76 50588740
Corneal epithelium defect 26.55 13.21 8 16300 327 50588489
Systemic lupus erythematosus 25.29 13.21 7 16301 140615 50448201
Atrioventricular block complete 25.28 13.21 20 16288 7235 50581581
Hypopyon 24.80 13.21 9 16299 660 50588156
Erythema of eyelid 24.73 13.21 12 16296 1821 50586995
Synovitis 24.57 13.21 5 16303 123860 50464956
Retinal detachment 24.28 13.21 17 16291 5112 50583704
Dry mouth 24.26 13.21 55 16253 56123 50532693
Keratopathy 23.92 13.21 8 16300 460 50588356
Toxic anterior segment syndrome 23.41 13.21 11 16297 1554 50587262
Vitreous haemorrhage 22.26 13.21 11 16297 1737 50587079
Glossodynia 22.24 13.21 5 16303 115564 50473252
Vitreous floaters 21.47 13.21 16 16292 5298 50583518
Eyelid irritation 21.43 13.21 7 16301 374 50588442
Fall 21.20 13.21 182 16126 334750 50254066
Corneal thickening 20.84 13.21 4 16304 21 50588795
Conjunctivitis allergic 20.58 13.21 8 16300 710 50588106
Haemangioma congenital 20.45 13.21 7 16301 432 50588384
Intraocular pressure fluctuation 20.39 13.21 4 16304 24 50588792
Blood pressure systolic increased 20.33 13.21 39 16269 35410 50553406
Arthralgia 20.27 13.21 73 16235 438629 50150187
Open angle glaucoma 19.97 13.21 6 16302 243 50588573
Product physical consistency issue 19.96 13.21 7 16301 465 50588351
Blindness unilateral 19.47 13.21 15 16293 5220 50583596
Foreign body in eye 19.39 13.21 5 16303 114 50588702
Dry eye 19.26 13.21 36 16272 32059 50556757
Optic nerve cupping 19.04 13.21 3 16305 3 50588813
Infusion related reaction 19.04 13.21 16 16292 169541 50419275
Eye disorder 18.01 13.21 26 16282 18713 50570103
Conjunctivitis 17.91 13.21 24 16284 16121 50572695
Achromotrichia acquired 17.83 13.21 3 16305 6 50588810
Keratitis interstitial 17.83 13.21 3 16305 6 50588810
Bronchopulmonary disease 17.83 13.21 3 16305 6 50588810
Drug intolerance 17.71 13.21 27 16281 219077 50369739
Wound 17.69 13.21 6 16302 105788 50483028
Hypotonia 17.41 13.21 17 16291 8117 50580699
Joint swelling 17.29 13.21 33 16275 245253 50343563
Eye allergy 17.07 13.21 7 16301 714 50588102
Symblepharon 16.91 13.21 4 16304 63 50588753
Sinus bradycardia 16.82 13.21 21 16287 13162 50575654
Contraindicated product administered 16.79 13.21 14 16294 148944 50439872
Hypothermia 16.72 13.21 20 16288 11996 50576820
Eye injury 16.56 13.21 8 16300 1202 50587614
Corneal endothelial cell loss 16.10 13.21 3 16305 13 50588803
Haemangioma 16.07 13.21 10 16298 2470 50586346
Conjunctival follicles 15.92 13.21 3 16305 14 50588802
Eye oedema 15.77 13.21 8 16300 1335 50587481
Product use issue 15.70 13.21 15 16293 149460 50439356
Abdominal pain 15.60 13.21 33 16275 236195 50352621
Uveitis 15.49 13.21 17 16291 9293 50579523
Intraocular lens implant 15.36 13.21 5 16303 264 50588552
Pyrexia 15.18 13.21 67 16241 380136 50208680
Swelling 15.06 13.21 26 16282 200846 50387970
Product dose omission issue 14.98 13.21 106 16202 183732 50405084
Intraocular pressure decreased 14.76 13.21 4 16304 111 50588705
Lethargy 14.67 13.21 42 16266 49390 50539426
Hepatic enzyme increased 14.18 13.21 14 16294 137366 50451450
Febrile neutropenia 13.97 13.21 7 16301 97660 50491156
Ocular pemphigoid 13.94 13.21 3 16305 30 50588786
Vitrectomy 13.90 13.21 4 16304 139 50588677
Confusional state 13.89 13.21 105 16203 185823 50402993
Iris neovascularisation 13.76 13.21 3 16305 32 50588784
Retinal vascular occlusion 13.70 13.21 5 16303 373 50588443
Subretinal fluid 13.68 13.21 5 16303 374 50588442
Stag horn calculus 13.66 13.21 4 16304 148 50588668
Retinal degeneration 13.58 13.21 6 16302 735 50588081
Maternal exposure during pregnancy 13.58 13.21 19 16289 159759 50429057
No adverse event 13.53 13.21 32 16276 33546 50555270
Vertigo 13.45 13.21 42 16266 51790 50537026
Iritis 13.44 13.21 9 16299 2519 50586297
Photophobia 13.36 13.21 20 16288 14867 50573949

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
Treatment failure 774.67 14.63 344 10918 36595 29526670
Intraocular pressure increased 355.67 14.63 113 11149 4676 29558589
Eye irritation 286.09 14.63 101 11161 5797 29557468
Eye pain 165.19 14.63 83 11179 11512 29551753
Visual acuity reduced 162.11 14.63 89 11173 14787 29548478
Ocular hyperaemia 140.86 14.63 69 11193 9058 29554207
Vision blurred 107.15 14.63 102 11160 40074 29523191
Glaucoma 83.59 14.63 42 11220 5815 29557450
Corneal deposits 80.83 14.63 18 11244 178 29563087
Corneal oedema 76.75 14.63 25 11237 1117 29562148
Product delivery mechanism issue 75.22 14.63 16 11246 125 29563140
Lacrimation increased 68.47 14.63 39 11223 6941 29556324
Bradycardia 66.71 14.63 102 11160 65527 29497738
Product quality issue 63.84 14.63 51 11211 15844 29547421
Intraocular pressure test abnormal 60.05 14.63 12 11250 66 29563199
Eye pruritus 58.71 14.63 30 11232 4302 29558963
Product container issue 56.59 14.63 17 11245 580 29562685
Anterior chamber disorder 49.02 14.63 10 11252 62 29563203
Cataract 48.85 14.63 51 11211 22327 29540938
Blindness 47.05 14.63 38 11224 11985 29551280
Hyphaema 46.70 14.63 14 11248 474 29562791
Toxic anterior segment syndrome 43.65 14.63 16 11246 1020 29562245
Eye discharge 42.76 14.63 18 11244 1658 29561607
Choroidal detachment 37.17 14.63 11 11251 356 29562909
Foreign body sensation in eyes 36.73 14.63 12 11250 541 29562724
Corneal disorder 35.84 14.63 13 11249 804 29562461
Dry eye 34.95 14.63 26 11236 7270 29555995
Erythema of eyelid 34.33 14.63 12 11250 666 29562599
Ocular discomfort 32.89 14.63 15 11247 1674 29561591
Visual impairment 32.75 14.63 48 11214 29660 29533605
Floppy iris syndrome 30.21 14.63 9 11253 298 29562967
Ocular hypertension 29.86 14.63 11 11251 711 29562554
Blindness unilateral 28.95 14.63 18 11244 3756 29559509
Iridocyclitis 28.71 14.63 13 11249 1427 29561838
Visual acuity tests abnormal 28.08 14.63 6 11256 48 29563217
Eyelid irritation 26.53 14.63 6 11256 64 29563201
Scleral hyperaemia 26.44 14.63 6 11256 65 29563200
Ulcerative keratitis 25.72 14.63 12 11250 1411 29561854
Eye infection 25.33 14.63 15 11247 2868 29560397
Off label use 24.99 14.63 48 11214 300752 29262513
Eye swelling 24.99 14.63 23 11239 8634 29554631
Completed suicide 24.09 14.63 3 11259 90243 29473022
Eyelid oedema 23.28 14.63 17 11245 4619 29558646
Conjunctival oedema 23.15 14.63 8 11254 429 29562836
Eye disorder 22.98 14.63 21 11241 7813 29555452
Product packaging quantity issue 22.17 14.63 9 11253 756 29562509
Uveitis 21.59 14.63 18 11244 5929 29557336
Atrioventricular block second degree 21.53 14.63 14 11248 3154 29560111
Intraocular pressure decreased 21.42 14.63 5 11257 62 29563203
Growth of eyelashes 21.42 14.63 5 11257 62 29563203
Retinal detachment 20.89 14.63 16 11246 4670 29558595
Trabeculectomy 20.68 14.63 4 11258 18 29563247
Scleral disorder 20.17 14.63 4 11258 21 29563244
Blepharitis 19.51 14.63 9 11253 1031 29562234
Hypotony of eye 19.28 14.63 5 11257 98 29563167
Accidental exposure to product 19.10 14.63 22 11240 10731 29552534
Eyelids pruritus 19.05 14.63 5 11257 103 29563162
Anterior chamber inflammation 19.01 14.63 6 11256 242 29563023
Corneal degeneration 18.72 14.63 4 11258 32 29563233
Cataract nuclear 18.65 14.63 7 11255 477 29562788
Conjunctival hyperaemia 18.42 14.63 11 11251 2134 29561131
Visual field defect 18.23 14.63 14 11248 4102 29559163
Eye inflammation 18.05 14.63 10 11252 1686 29561579
Dizziness 17.61 14.63 128 11134 189556 29373709
Optic nerve cupping 17.57 14.63 4 11258 44 29563221
Administration site discomfort 17.49 14.63 4 11258 45 29563220
Dermatitis 17.42 14.63 18 11244 7780 29555485
Eye haemorrhage 17.19 14.63 13 11249 3723 29559542
Macular degeneration 17.19 14.63 10 11252 1850 29561415
Punctate keratitis 17.15 14.63 6 11256 334 29562931
Liquid product physical issue 17.06 14.63 6 11256 339 29562926
Cardiovascular insufficiency 17.02 14.63 9 11253 1384 29561881
Eyelid margin crusting 16.92 14.63 5 11257 161 29563104
Corneal epithelium defect 16.75 14.63 6 11256 358 29562907
Funguria 16.68 14.63 4 11258 56 29563209
Abnormal sensation in eye 16.67 14.63 7 11255 641 29562624
Hypersensitivity 16.56 14.63 51 11211 52852 29510413
Electrolyte depletion 16.49 14.63 5 11257 176 29563089
Coronavirus infection 16.38 14.63 12 11250 3276 29559989
Madarosis 15.81 14.63 5 11257 203 29563062
Corneal infection 15.80 14.63 3 11259 12 29563253
Ectropion 15.80 14.63 4 11258 71 29563194
Photophobia 15.53 14.63 15 11247 5980 29557285
Intraocular pressure fluctuation 15.25 14.63 3 11259 15 29563250
Retinal haemorrhage 15.05 14.63 13 11249 4491 29558774
Cutis laxa 14.94 14.63 4 11258 89 29563176
Sinus bradycardia 14.63 14.63 20 11242 11583 29551682

FDA Adverse Event Reporting System (Geriatric)

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 505.02 12.16 161 20227 8141 64470203
Eye irritation 338.32 12.16 142 20246 15714 64462630
Eye pain 219.00 12.16 132 20256 31493 64446851
Visual acuity reduced 218.78 12.16 125 20263 27016 64451328
Ocular hyperaemia 214.94 12.16 116 20272 22448 64455896
Vision blurred 153.47 12.16 165 20223 90151 64388193
Glaucoma 144.48 12.16 80 20308 16268 64462076
Bradycardia 133.03 12.16 175 20213 118044 64360300
Eye pruritus 106.54 12.16 60 20328 12599 64465745
Lacrimation increased 102.84 12.16 67 20321 18279 64460065
Corneal oedema 100.72 12.16 35 20353 2308 64476036
Total lung capacity increased 93.14 12.16 25 20363 683 64477661
Choroidal detachment 89.88 12.16 23 20365 519 64477825
Corneal deposits 87.74 12.16 21 20367 356 64477988
Eye discharge 74.47 12.16 35 20353 5049 64473295
Corneal disorder 70.94 12.16 26 20362 2001 64476343
Iris adhesions 70.89 12.16 19 20369 516 64477828
Choroidal effusion 68.36 12.16 19 20369 593 64477751
Intraocular pressure test abnormal 67.26 12.16 14 20374 120 64478224
Cataract 62.45 12.16 79 20309 51183 64427161
Ulcerative keratitis 60.26 12.16 26 20362 3071 64475273
Trabeculectomy 60.17 12.16 11 20377 43 64478301
Toxic anterior segment syndrome 59.30 12.16 24 20364 2415 64475929
Frustration tolerance decreased 54.17 12.16 30 20358 6095 64472249
Hypotony of eye 49.15 12.16 12 20376 222 64478122
Visual field defect 48.73 12.16 31 20357 8115 64470229
Conjunctival hyperaemia 48.50 12.16 24 20364 3875 64474469
Completed suicide 47.83 12.16 7 20381 224407 64253937
Eye inflammation 46.30 12.16 25 20363 4832 64473512
Blindness 45.99 12.16 45 20343 21974 64456370
Foreign body sensation in eyes 45.26 12.16 18 20370 1731 64476613
Hyphaema 45.21 12.16 14 20374 641 64477703
Iridocyclitis 44.71 12.16 21 20367 3024 64475320
Floppy iris syndrome 44.52 12.16 12 20376 333 64478011
Anterior chamber disorder 43.90 12.16 10 20378 135 64478209
Forced expiratory volume decreased 43.25 12.16 27 20361 6840 64471504
Respiration abnormal 42.75 12.16 26 20362 6289 64472055
Peak expiratory flow rate decreased 41.57 12.16 13 20375 615 64477729
Corneal epithelium defect 40.46 12.16 13 20375 672 64477672
Corneal degeneration 39.62 12.16 9 20379 120 64478224
Pulmonary thrombosis 39.34 12.16 30 20358 10488 64467856
Ocular discomfort 39.29 12.16 21 20367 3978 64474366
Punctate keratitis 37.48 12.16 13 20375 852 64477492
Retinal detachment 37.20 12.16 26 20362 7950 64470394
Erythema of eyelid 36.58 12.16 16 20372 1952 64476392
Uveitis 36.38 12.16 31 20357 12677 64465667
Angle closure glaucoma 34.98 12.16 17 20371 2640 64475704
Cystoid macular oedema 34.86 12.16 15 20373 1759 64476585
Lung diffusion test decreased 33.37 12.16 13 20375 1183 64477161
Product quality issue 33.27 12.16 44 20344 29755 64448589
Procollagen type I C-terminal propeptide increased 32.71 12.16 6 20382 24 64478320
Ocular hypertension 32.70 12.16 13 20375 1248 64477096
Serum procollagen type I N-terminal propeptide increased 31.96 12.16 6 20382 28 64478316
Eyelid margin crusting 31.92 12.16 11 20377 707 64477637
Sinus bradycardia 30.63 12.16 37 20351 22856 64455488
Forced vital capacity decreased 30.39 12.16 13 20375 1503 64476841
Intraocular pressure fluctuation 30.02 12.16 6 20382 41 64478303
Flat anterior chamber of eye 27.61 12.16 7 20381 152 64478192
Atrioventricular block complete 27.40 12.16 28 20360 14390 64463954
Vitreous haemorrhage 26.98 12.16 15 20373 3070 64475274
Fall 26.84 12.16 224 20164 416602 64061742
Blepharitis 26.75 12.16 14 20374 2541 64475803
Endophthalmitis 26.22 12.16 18 20370 5347 64472997
Vitamin B12 decreased 25.95 12.16 14 20374 2701 64475643
Chronotropic incompetence 25.75 12.16 6 20382 90 64478254
Product container issue 25.55 12.16 10 20378 921 64477423
Retinal disorder 25.18 12.16 12 20376 1784 64476560
Blindness unilateral 24.66 12.16 19 20369 6742 64471602
Conjunctivitis allergic 24.58 12.16 10 20378 1020 64477324
Eye disorder 24.44 12.16 30 20358 18839 64459505
Visual acuity tests abnormal 24.32 12.16 6 20382 116 64478228
Conjunctival oedema 24.26 12.16 10 20378 1054 64477290
Atrioventricular block 24.05 12.16 24 20364 11991 64466353
Visual impairment 23.81 12.16 64 20324 74013 64404331
Keratopathy 23.63 12.16 9 20379 771 64477573
Abdominal pain 23.60 12.16 39 20349 312336 64166008
Growth of eyelashes 23.38 12.16 6 20382 137 64478207
Optic nerve cupping 23.24 12.16 5 20383 51 64478293
Product delivery mechanism issue 23.13 12.16 6 20382 143 64478201
Dizziness 22.98 12.16 222 20166 429941 64048403
Abnormal sensation in eye 22.58 12.16 11 20377 1716 64476628
Ectropion 21.91 12.16 7 20381 355 64477989
Corneal thickening 21.81 12.16 4 20384 16 64478328
Thermal burns of eye 21.28 12.16 5 20383 78 64478266
Hypopyon 21.21 12.16 9 20379 1020 64477324
Atrioventricular block second degree 21.09 12.16 17 20371 6437 64471907
Glaucoma surgery 20.93 12.16 5 20383 84 64478260
Vertigo 19.99 12.16 52 20336 58959 64419385
Hypotonia 19.92 12.16 21 20367 11191 64467153
Anterior chamber inflammation 19.68 12.16 7 20381 494 64477850
Obstructive airways disorder 19.62 12.16 30 20358 23155 64455189
Synovitis 19.11 12.16 4 20384 99086 64379258
Iritis 18.99 12.16 12 20376 3104 64475240
Corneal opacity 18.94 12.16 8 20380 897 64477447
Off label use 18.87 12.16 120 20268 632686 63845658
Eyelid irritation 18.86 12.16 6 20382 300 64478044
Corneal decompensation 18.57 12.16 4 20384 41 64478303
Dry eye 18.44 12.16 33 20355 28986 64449358
Dry mouth 18.22 12.16 51 20337 60367 64417977
Confusional state 18.21 12.16 143 20245 261001 64217343
Conjunctivitis 18.17 12.16 27 20361 20327 64458017
Toxicity to various agents 18.03 12.16 57 20331 363456 64114888
Symblepharon 17.47 12.16 5 20383 174 64478170
Vitreal cells 17.43 12.16 4 20384 56 64478288
Corneal endothelial cell loss 17.28 12.16 3 20385 8 64478336
Macular fibrosis 17.27 12.16 7 20381 707 64477637
Blood pressure systolic increased 17.19 12.16 44 20344 49409 64428935
Instillation site irritation 17.17 12.16 4 20384 60 64478284
Photophobia 16.98 12.16 24 20364 17269 64461075
Hyponatraemia 16.95 12.16 92 20296 148247 64330097
Corneal infection 16.87 12.16 4 20384 65 64478279
Arthralgia 16.38 12.16 78 20310 442182 64036162
Eye swelling 16.34 12.16 27 20361 22254 64456090
Macular oedema 16.29 12.16 13 20375 4854 64473490
Dermatitis 16.21 12.16 24 20364 18005 64460339
Liquid product physical issue 16.15 12.16 7 20381 835 64477509
Bronchopulmonary disease 15.98 12.16 3 20385 14 64478330
Corneal pigmentation 15.98 12.16 3 20385 14 64478330
Heterochromia iridis 15.65 12.16 3 20385 16 64478328
Keratitis interstitial 15.65 12.16 3 20385 16 64478328
Achromotrichia acquired 15.65 12.16 3 20385 16 64478328
Product complaint 15.47 12.16 19 20369 11935 64466409
Pain 15.46 12.16 107 20281 553404 63924940
Eyelid ptosis 15.44 12.16 17 20371 9508 64468836
Corneal scar 15.38 12.16 5 20383 268 64478076
Conjunctival follicles 15.35 12.16 3 20385 18 64478326
Arrhythmia 15.29 12.16 44 20344 52900 64425444
Systemic lupus erythematosus 15.24 12.16 3 20385 77609 64400735
Scleral hyperaemia 15.23 12.16 5 20383 277 64478067
Retinal haemorrhage 15.22 12.16 15 20373 7383 64470961
Vitreous floaters 15.16 12.16 14 20374 6359 64471985
Loss of consciousness 14.96 12.16 89 20299 148276 64330068
Oversensing 14.95 12.16 3 20385 21 64478323
Therapeutic product effect incomplete 14.93 12.16 7 20381 103475 64374869
Infusion related reaction 14.93 12.16 18 20370 164449 64313895
Nodal rhythm 14.90 12.16 10 20378 2864 64475480
Abdominal discomfort 14.48 12.16 22 20366 182300 64296044
Multiple organ dysfunction syndrome 14.42 12.16 7 20381 101406 64376938
Product use issue 14.42 12.16 16 20372 151699 64326645
Administration site discomfort 14.39 12.16 4 20384 125 64478219
Superficial injury of eye 14.39 12.16 4 20384 125 64478219
Subretinal fluid 14.34 12.16 6 20382 657 64477687
Electrolyte depletion 14.18 12.16 5 20383 344 64478000
Metamorphopsia 14.17 12.16 7 20381 1125 64477219
Iris transillumination defect 14.12 12.16 4 20384 134 64478210
Eye oedema 13.83 12.16 8 20380 1765 64476579
Chorioretinal disorder 13.71 12.16 4 20384 149 64478195
Drug intolerance 13.70 12.16 24 20364 187968 64290376
Eyelid oedema 13.50 12.16 18 20370 12261 64466083
Corneal thinning 13.44 12.16 4 20384 160 64478184
Intraocular pressure decreased 13.34 12.16 4 20384 164 64478180
Cardiovascular insufficiency 13.29 12.16 9 20379 2615 64475729
Stag horn calculus 13.16 12.16 4 20384 172 64478172
Hepatic enzyme increased 13.14 12.16 13 20375 129930 64348414
Maternal exposure during pregnancy 13.06 12.16 7 20381 95877 64382467
Coronavirus infection 12.87 12.16 12 20376 5518 64472826
Alkalosis hypochloraemic 12.83 12.16 5 20383 455 64477889
Pyrexia 12.80 12.16 114 20274 558530 63919814
Seborrhoeic keratosis 12.79 12.16 8 20380 2032 64476312
Extrasystoles 12.78 12.16 13 20375 6645 64471699
Scleral disorder 12.75 12.16 4 20384 191 64478153
Cataract subcapsular 12.65 12.16 6 20382 883 64477461
Eyelid disorder 12.63 12.16 7 20381 1424 64476920
Macular degeneration 12.54 12.16 12 20376 5698 64472646
Cataract operation 12.38 12.16 10 20378 3796 64474548
Product substitution issue 12.24 12.16 21 20367 17840 64460504
Retinal vascular occlusion 12.20 12.16 5 20383 519 64477825
Corneal lesion 12.16 12.16 3 20385 58 64478286

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C07AA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, non-selective
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 S01ED01 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Beta blocking agents
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-adrenergic blockers
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:38070 antiarrhythmic agent
CHEBI has role CHEBI:39456 antiglaucoma agent

Drug Use | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 7030149 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION WHO REQUIRE ADJUNCTIVE OR REPLACEMENT THERAPY DUE TO INADEQUATELY CONTROLLED IOP. DOSE IS ONE DROP OF COMBIGAN IN THE AFFECTED EYE TWICE DAILY
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 7320976 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION WHO REQUIRE ADJUNCTIVE OR REPLACEMENT THERAPY DUE TO INADEQUATELY CONTROLLED IOP. DOSE IS ONE DROP OF COMBIGAN IN THE AFFECTED EYE TWICE DAILY
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 7642258 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION WHO REQUIRE ADJUNCTIVE OR REPLACEMENT THERAPY DUE TO INADEQUATELY CONTROLLED IOP
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 8133890 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 8354409 April 19, 2022 REDUCTION OF INTRAOCULAR PRESSURE IN PATIENTS WITH ELEVATED INTRAOCULAR PRESSURE OR GLAUCOMA
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 8748425 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9474751 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9770453 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION, WITH COMPARABLE EFFICACY, AND A REDUCTION IN SPECIFIED ADVERSE EVENTS, COMPARED TO BRIMONIDINE 0.2% TID
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9907801 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION, WITH A REDUCTION IN SPECIFIED ADVERSE EVENTS, COMPARED TO BRIMONIDINE 0.2% TID
0.2%;EQ 0.5% BASE COMBIGAN ALLERGAN N021398 Oct. 30, 2007 RX SOLUTION/DROPS OPHTHALMIC 9907802 April 19, 2022 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE (IOP) IN PATIENTS WITH GLAUCOMA OR OCULAR HYPERTENSION, WITH COMPARABLE EFFICACY TO BRIMONIDINE 0.2% TID

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.25% BASE TIMOLOL MALEATE AMRING PHARMS A212592 Dec. 13, 2021 RX SOLUTION/DROPS OPHTHALMIC Aug. 25, 2022 COMPETITIVE GENERIC THERAPY
EQ 0.5% BASE TIMOLOL MALEATE AMRING PHARMS A212592 Dec. 13, 2021 RX SOLUTION/DROPS OPHTHALMIC Aug. 25, 2022 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
5-hydroxytryptamine receptor 1A GPCR Ki 6.21 CHEMBL
Beta-2 adrenergic receptor GPCR Kd 9.78 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 9.44 CHEMBL

External reference:

IDSource
4019949 VUID
N0000148034 NUI
D00378 KEGG_DRUG
26921-17-5 SECONDARY_CAS_RN
4017930 VANDF
4019949 VANDF
C0040233 UMLSCUI
CHEBI:60787 CHEBI
TIM PDB_CHEM_ID
CHEMBL499 ChEMBL_ID
DB00373 DRUGBANK_ID
CHEMBL1200870 ChEMBL_ID
D013999 MESH_DESCRIPTOR_UI
33624 PUBCHEM_CID
565 IUPHAR_LIGAND_ID
817W3C6175 UNII
10600 RXNORM
5585 MMSL
6436 MMSL
d00139 MMSL
001856 NDDF
004741 NDDF
372880004 SNOMEDCT_US
75359005 SNOMEDCT_US
85591001 SNOMEDCT_US
91524-16-2 SECONDARY_CAS_RN

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
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0781-7186 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 23 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 17478-288 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 17478-289 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 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
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 in Ocudose HUMAN PRESCRIPTION DRUG LABEL 1 24208-498 SOLUTION 3.40 mg OPHTHALMIC NDA 12 sections
Timoptic in Ocudose HUMAN PRESCRIPTION DRUG LABEL 1 24208-499 SOLUTION 6.80 mg OPHTHALMIC NDA 12 sections
Timoptic HUMAN PRESCRIPTION DRUG LABEL 1 24208-812 SOLUTION 2.50 mg OPHTHALMIC NDA 24 sections