Stem definition | Drug id | CAS RN |
---|---|---|
beta-adrenoreceptor antagonists | 4061 | 26839-75-8 |
Dose | Unit | Route |
---|---|---|
20 | mg | O |
20 | mg | P |
Property | Value | Reference |
---|---|---|
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 µM/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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 17, 1978 | FDA | ATON | |
March 25, 2020 | PMDA | Senju Pharmaceutical Co., Ltd |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.15 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
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 |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
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 |