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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	4061	26839-75-8

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
20	mg	O
20	mg	P

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
Aug. 17, 1978	FDA	ATON
March 25, 2020	PMDA	Senju Pharmaceutical Co., Ltd

FDA Adverse Event Reporting System (Female)

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	663.43	13.51	500	17079	198543	63272900
Eye irritation	467.48	13.51	189	17390	21782	63449661
Intraocular pressure increased	402.68	13.51	122	17457	5956	63465487
Ocular hyperaemia	299.73	13.51	144	17435	25000	63446443
Eye pain	273.07	13.51	149	17430	33705	63437738
Glaucoma	174.30	13.51	91	17488	18814	63452629
Vision blurred	133.15	13.51	145	17434	91779	63379664
Eye pruritus	122.94	13.51	72	17507	18599	63452844
Visual acuity reduced	122.60	13.51	76	17503	21750	63449693
Product quality issue	99.08	13.51	81	17498	35784	63435659
Product container issue	97.69	13.51	31	17548	1762	63469681
Bradycardia	88.16	13.51	105	17474	73122	63398321
Lacrimation increased	82.22	13.51	58	17521	20573	63450870
Choroidal effusion	80.59	13.51	20	17559	456	63470987
Corneal oedema	77.99	13.51	25	17554	1468	63469975
Foreign body sensation in eyes	71.84	13.51	26	17553	2208	63469235
Product delivery mechanism issue	69.92	13.51	17	17562	355	63471088
Total lung capacity increased	67.30	13.51	25	17554	2285	63469158
Iris adhesions	66.70	13.51	16	17563	315	63471128
Frustration tolerance decreased	65.42	13.51	34	17545	6954	63464489
Eyelid margin crusting	64.52	13.51	20	17559	1052	63470391
Eye discharge	58.20	13.51	30	17549	6033	63465410
Cataract	57.72	13.51	75	17504	56978	63414465
Ulcerative keratitis	56.49	13.51	23	17556	2687	63468756
Choroidal detachment	56.21	13.51	13	17566	217	63471226
Conjunctival hyperaemia	55.86	13.51	22	17557	2357	63469086
Hypotony of eye	55.57	13.51	12	17567	144	63471299
Forced expiratory volume decreased	54.77	13.51	27	17552	4941	63466502
Trabeculectomy	54.52	13.51	9	17570	19	63471424
Pulmonary thrombosis	50.63	13.51	31	17548	8671	63462772
Corneal disorder	50.54	13.51	19	17560	1795	63469648
Eye inflammation	48.88	13.51	26	17553	5573	63465870
Corneal deposits	47.84	13.51	12	17567	286	63471157
Visual impairment	46.91	13.51	84	17495	84362	63387081
Respiration abnormal	45.56	13.51	26	17553	6391	63465052
Iridocyclitis	44.48	13.51	19	17560	2503	63468940
Product packaging quantity issue	44.38	13.51	16	17563	1343	63470100
Peak expiratory flow rate decreased	43.24	13.51	13	17566	616	63470827
Cystoid macular oedema	42.08	13.51	16	17563	1559	63469884
Lung diffusion test decreased	41.91	13.51	13	17566	685	63470758
Punctate keratitis	39.12	13.51	12	17567	609	63470834
Intraocular pressure test abnormal	38.28	13.51	9	17570	162	63471281
Retinal disorder	37.49	13.51	15	17564	1675	63469768
Abdominal discomfort	36.27	13.51	22	17557	320863	63150580
Systemic lupus erythematosus	36.14	13.51	7	17572	208911	63262532
Ocular discomfort	35.11	13.51	19	17560	4214	63467229
Thermal burns of eye	33.62	13.51	8	17571	152	63471291
Abnormal sensation in eye	33.59	13.51	14	17565	1735	63469708
Angle closure glaucoma	33.55	13.51	15	17564	2204	63469239
Procollagen type I C-terminal propeptide increased	33.50	13.51	6	17573	24	63471419
Eye swelling	33.31	13.51	37	17542	23881	63447562
Glossodynia	33.12	13.51	5	17574	178871	63292572
Synovitis	32.89	13.51	6	17573	186912	63284531
Serum procollagen type I N-terminal propeptide increased	32.75	13.51	6	17573	28	63471415
Forced vital capacity decreased	32.62	13.51	12	17567	1067	63470376
Visual field defect	32.23	13.51	21	17558	6540	63464903
Corneal degeneration	32.12	13.51	7	17572	88	63471355
Pain	31.44	13.51	103	17476	740525	62730918
Macular oedema	31.04	13.51	17	17562	3860	63467583
Growth of eyelashes	31.01	13.51	8	17571	214	63471229
Conjunctival ulcer	30.82	13.51	6	17573	41	63471402
Superficial injury of eye	30.10	13.51	8	17571	241	63471202
Incorrect dose administered	29.96	13.51	57	17522	59911	63411532
Flat anterior chamber of eye	29.35	13.51	6	17573	54	63471389
Blindness	29.24	13.51	33	17546	21666	63449777
Obstructive airways disorder	28.79	13.51	32	17547	20667	63450776
Liquid product physical issue	27.99	13.51	11	17568	1171	63470272
Corneal epithelium defect	27.36	13.51	8	17571	344	63471099
Wound	27.13	13.51	6	17573	163257	63308186
Completed suicide	27.13	13.51	4	17575	145669	63325774
Hallucination, visual	27.12	13.51	30	17549	19268	63452175
Chronotropic incompetence	26.93	13.51	6	17573	84	63471359
Erythema of eyelid	26.93	13.51	13	17566	2273	63469170
Glaucoma surgery	26.73	13.51	6	17573	87	63471356
Vitamin B12 decreased	26.59	13.51	15	17564	3605	63467838
Atrioventricular block complete	25.69	13.51	20	17559	8231	63463212
Haemangioma congenital	25.39	13.51	8	17571	444	63470999
Hypopyon	25.35	13.51	9	17570	723	63470720
Vitreous haemorrhage	25.19	13.51	12	17567	2038	63469405
Arthralgia	24.99	13.51	78	17501	569632	62901811
Conjunctival scar	24.56	13.51	5	17574	44	63471399
Retinal detachment	24.28	13.51	17	17562	5952	63465491
Keratitis interstitial	24.06	13.51	4	17575	9	63471434
Foreign body in eye	23.84	13.51	6	17573	145	63471298
Toxic anterior segment syndrome	23.71	13.51	11	17568	1760	63469683
Conjunctivitis	23.66	13.51	29	17550	20767	63450676
Sinoatrial block	23.65	13.51	9	17570	879	63470564
Infusion related reaction	23.58	13.51	20	17559	245501	63225942
Conjunctivitis allergic	23.13	13.51	9	17570	933	63470510
Keratopathy	22.96	13.51	8	17571	608	63470835
Hypersensitivity	22.91	13.51	149	17430	292536	63178907
Fall	22.83	13.51	186	17393	392148	63079295
Vitreous floaters	21.99	13.51	16	17563	5950	63465493
Contraindicated product administered	21.80	13.51	17	17562	217631	63253812
Corneal opacity	21.49	13.51	8	17571	735	63470708
Corneal thickening	21.45	13.51	4	17575	21	63471422
Endophthalmitis	21.41	13.51	13	17566	3579	63467864
Blindness unilateral	21.34	13.51	16	17563	6225	63465218
Drug intolerance	21.14	13.51	33	17546	308628	63162815
Open angle glaucoma	20.30	13.51	6	17573	268	63471175
Swelling	20.26	13.51	28	17551	275350	63196093
Uveitis	20.26	13.51	21	17558	12532	63458911
Eyelid irritation	20.04	13.51	7	17572	536	63470907
Hepatic enzyme increased	20.02	13.51	16	17563	202312	63269131
Discomfort	19.56	13.51	11	17568	167363	63304080
Genital erythema	19.47	13.51	4	17575	37	63471406
Dry eye	19.44	13.51	38	17541	40723	63430720
Sinus bradycardia	19.38	13.51	22	17557	14529	63456914
Blepharitis	19.23	13.51	11	17568	2714	63468729
Dry mouth	19.05	13.51	56	17523	77807	63393636
Product dose omission issue	18.76	13.51	120	17459	234193	63237250
Sinonasal papilloma	18.76	13.51	4	17575	45	63471398
Maternal exposure during pregnancy	18.70	13.51	20	17559	220042	63251401
Eye disorder	18.67	13.51	27	17552	22658	63448785
Intraocular pressure fluctuation	18.52	13.51	4	17575	48	63471395
Lethargy	18.47	13.51	45	17534	55962	63415481
Product physical consistency issue	18.31	13.51	7	17572	692	63470751
Optic nerve cupping	18.28	13.51	3	17576	6	63471437
Bronchopulmonary disease	18.28	13.51	3	17576	6	63471437
Joint swelling	18.04	13.51	40	17539	327626	63143817
No adverse event	17.84	13.51	37	17542	41368	63430075
Nodal rhythm	17.82	13.51	9	17570	1734	63469709
Hypotonia	17.69	13.51	17	17562	9268	63462175
Achromotrichia acquired	17.42	13.51	3	17576	9	63471434
Hypothermia	17.19	13.51	20	17559	13561	63457882
Arthropathy	17.14	13.51	24	17555	234768	63236675
Haemangioma	16.64	13.51	10	17569	2702	63468741
Blood pressure systolic increased	16.62	13.51	39	17540	47358	63424085
Conjunctival follicles	16.38	13.51	3	17576	14	63471429
Symblepharon	16.30	13.51	4	17575	87	63471356
Corneal endothelial cell loss	16.21	13.51	3	17576	15	63471428
Small for dates baby	16.00	13.51	11	17568	3740	63467703
Eye oedema	15.98	13.51	8	17571	1512	63469931
Therapeutic product effect decreased	15.92	13.51	18	17561	193169	63278274
Eye allergy	15.90	13.51	7	17572	992	63470451
Product use issue	15.64	13.51	23	17556	220497	63250946
Dacryocystitis	15.22	13.51	3	17576	22	63471421
Iritis	15.20	13.51	10	17569	3165	63468278
Intraocular pressure decreased	15.07	13.51	4	17575	120	63471323
Conjunctival erosion	15.07	13.51	4	17575	120	63471323
Eyelids pruritus	15.00	13.51	7	17572	1135	63470308
Intraocular lens implant	14.91	13.51	5	17574	338	63471105
Vertigo	14.58	13.51	43	17536	59844	63411599
Photophobia	14.53	13.51	21	17558	17614	63453829
Stag horn calculus	14.26	13.51	4	17575	148	63471295
Iris neovascularisation	14.22	13.51	3	17576	32	63471411
Intentional product use issue	14.10	13.51	9	17570	127883	63343560
Herpes ophthalmic	14.09	13.51	7	17572	1302	63470141
Haematemesis	14.07	13.51	28	17551	30384	63441059
Nasopharyngitis	14.02	13.51	31	17548	254226	63217217
Dizziness	14.00	13.51	181	17398	429744	63041699
Psoriatic arthropathy	13.97	13.51	4	17575	91516	63379927
Retinal vascular occlusion	13.84	13.51	5	17574	422	63471021
Vitrectomy	13.57	13.51	4	17575	177	63471266
Febrile neutropenia	13.53	13.51	8	17571	118441	63353002
Therapeutic product effect incomplete	13.52	13.51	9	17570	125047	63346396

FDA Adverse Event Reporting System (Male)

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	735.48	14.58	345	11617	46352	34898617
Intraocular pressure increased	366.95	14.58	116	11846	5267	34939702
Eye irritation	283.17	14.58	104	11858	7457	34937512
Eye pain	179.45	14.58	89	11873	13373	34931596
Visual acuity reduced	164.16	14.58	89	11873	16060	34928909
Ocular hyperaemia	138.79	14.58	71	11891	11381	34933588
Vision blurred	112.32	14.58	106	11856	45857	34899112
Corneal oedema	91.52	14.58	29	11933	1322	34943647
Glaucoma	90.00	14.58	45	11917	6867	34938102
Corneal deposits	80.35	14.58	18	11944	206	34944763
Product delivery mechanism issue	74.13	14.58	16	11946	152	34944817
Bradycardia	71.26	14.58	107	11855	75311	34869658
Lacrimation increased	70.53	14.58	41	11921	8441	34936528
Product quality issue	65.53	14.58	51	11911	16984	34927985
Intraocular pressure test abnormal	61.33	14.58	12	11950	66	34944903
Product container issue	55.26	14.58	17	11945	702	34944267
Cataract	50.25	14.58	53	11909	26133	34918836
Hyphaema	49.91	14.58	15	11947	572	34944397
Anterior chamber disorder	49.42	14.58	10	11952	67	34944902
Blindness	49.41	14.58	41	11921	14945	34930024
Eye pruritus	48.88	14.58	31	11931	7458	34937511
Toxic anterior segment syndrome	43.43	14.58	16	11946	1153	34943816
Eye discharge	41.50	14.58	18	11944	1988	34942981
Visual impairment	41.44	14.58	56	11906	35746	34909223
Choroidal detachment	36.81	14.58	11	11951	411	34944558
Foreign body sensation in eyes	36.38	14.58	12	11950	622	34944347
Corneal disorder	35.50	14.58	13	11949	921	34944048
Floppy iris syndrome	35.35	14.58	10	11952	307	34944662
Ocular discomfort	34.13	14.58	16	11946	2118	34942851
Dry eye	33.25	14.58	27	11935	9548	34935421
Erythema of eyelid	31.70	14.58	12	11950	933	34944036
Iridocyclitis	31.51	14.58	14	11948	1638	34943331
Ocular hypertension	29.33	14.58	11	11951	833	34944136
Visual acuity tests abnormal	28.72	14.58	6	11956	48	34944921
Blindness unilateral	27.66	14.58	18	11944	4524	34940445
Scleral hyperaemia	27.00	14.58	6	11956	66	34944903
Eye infection	25.97	14.58	16	11946	3657	34941312
Off label use	24.99	14.58	68	11894	419456	34525513
Retinal detachment	24.86	14.58	18	11944	5373	34939596
Ulcerative keratitis	24.71	14.58	12	11950	1717	34943252
Eye swelling	24.27	14.58	23	11939	9972	34934997
Eyelid irritation	23.75	14.58	6	11956	118	34944851
Completed suicide	23.38	14.58	3	11959	98165	34846804
Eyelid oedema	23.38	14.58	17	11945	5107	34939862
Conjunctival oedema	23.19	14.58	8	11954	476	34944493
Administration site discomfort	23.12	14.58	5	11957	48	34944921
Intraocular pressure decreased	21.52	14.58	5	11957	68	34944901
Product packaging quantity issue	21.41	14.58	9	11953	920	34944049
Eye disorder	21.39	14.58	21	11941	9507	34935462
Atrioventricular block second degree	20.62	14.58	14	11948	3774	34941195
Scleral disorder	20.60	14.58	4	11958	21	34944948
Trabeculectomy	20.44	14.58	4	11958	22	34944947
Growth of eyelashes	19.81	14.58	5	11957	98	34944871
Abnormal sensation in eye	19.76	14.58	8	11954	744	34944225
Uveitis	19.57	14.58	18	11944	7517	34937452
Accidental exposure to product	19.54	14.58	23	11939	12779	34932190
Hypotony of eye	19.40	14.58	5	11957	107	34944862
Macular degeneration	19.32	14.58	11	11951	2175	34942794
Corneal degeneration	18.83	14.58	4	11958	35	34944934
Anterior chamber inflammation	18.67	14.58	6	11956	286	34944683
Cataract nuclear	18.65	14.58	7	11955	531	34944438
Visual field defect	18.50	14.58	14	11948	4469	34940500
Conjunctival hyperaemia	18.36	14.58	11	11951	2391	34942578
Conjunctival scar	18.32	14.58	5	11957	134	34944835
Blepharitis	17.61	14.58	9	11953	1436	34943533
Corneal epithelium defect	17.14	14.58	6	11956	373	34944596
Eyelids pruritus	17.13	14.58	5	11957	172	34944797
Funguria	17.11	14.58	4	11958	56	34944913
Punctate keratitis	17.08	14.58	6	11956	377	34944592
Photophobia	16.86	14.58	16	11946	6948	34938021
Eye haemorrhage	16.79	14.58	13	11949	4292	34940677
Coronavirus infection	16.78	14.58	13	11949	4294	34940675
Optic nerve cupping	16.73	14.58	4	11958	62	34944907
Cystoid macular oedema	16.72	14.58	7	11955	708	34944261
Electrolyte depletion	16.55	14.58	5	11957	194	34944775
Eye inflammation	16.55	14.58	10	11952	2208	34942761
Cardiovascular insufficiency	16.30	14.58	9	11953	1678	34943291
Dizziness	16.25	14.58	129	11833	218392	34726577
Dermatitis	16.12	14.58	18	11944	9450	34935519
Instillation site irritation	15.92	14.58	3	11959	13	34944956
Madarosis	15.69	14.58	5	11957	232	34944737
Intraocular pressure fluctuation	15.57	14.58	3	11959	15	34944954
Liquid product physical issue	15.49	14.58	6	11956	496	34944473
Hypersensitivity	15.45	14.58	51	11911	60984	34883985
Glaucoma surgery	15.26	14.58	3	11959	17	34944952
Eyelid margin crusting	15.25	14.58	5	11957	254	34944715
Cutis laxa	15.24	14.58	4	11958	92	34944877
Retinal haemorrhage	14.88	14.58	13	11949	5076	34939893
Angle closure glaucoma	14.77	14.58	7	11955	950	34944019
Oversensing	14.71	14.58	3	11959	21	34944948
Corneal opacity	14.59	14.58	6	11956	580	34944389

FDA Adverse Event Reporting System (Geriatric)

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	522.42	12.06	164	21870	9041	79713313
Eye irritation	336.55	12.06	147	21887	20534	79701820
Eye pain	234.97	12.06	140	21894	37438	79684916
Visual acuity reduced	224.86	12.06	125	21909	29344	79693010
Ocular hyperaemia	213.45	12.06	119	21915	28087	79694267
Vision blurred	157.07	12.06	169	21865	105729	79616625
Glaucoma	153.94	12.06	85	21949	19676	79702678
Bradycardia	153.27	12.06	188	21846	135369	79586985
Corneal oedema	137.49	12.06	44	21990	2576	79719778
Lacrimation increased	105.86	12.06	70	21964	22407	79699947
Eye pruritus	89.52	12.06	61	21973	20509	79701845
Choroidal detachment	89.30	12.06	23	22011	613	79721741
Corneal deposits	84.73	12.06	21	22013	477	79721877
Corneal disorder	78.76	12.06	28	22006	2263	79720091
Eye discharge	76.30	12.06	36	21998	5998	79716356
Choroidal effusion	73.64	12.06	20	22014	657	79721697
Iris adhesions	73.04	12.06	19	22015	527	79721827
Intraocular pressure test abnormal	68.23	12.06	14	22020	129	79722225
Total lung capacity increased	67.48	12.06	25	22009	2273	79720081
Cataract	65.07	12.06	83	21951	62037	79660317
Trabeculectomy	60.68	12.06	11	22023	48	79722306
Toxic anterior segment syndrome	59.52	12.06	24	22010	2740	79719614
Ulcerative keratitis	59.25	12.06	26	22008	3663	79718691
Conjunctival hyperaemia	57.87	12.06	27	22007	4386	79717968
Frustration tolerance decreased	52.26	12.06	30	22004	7472	79714882
Hyphaema	50.81	12.06	16	22018	888	79721466
Floppy iris syndrome	50.34	12.06	13	22021	350	79722004
Iridocyclitis	49.62	12.06	23	22011	3681	79718673
Anterior chamber disorder	49.60	12.06	11	22023	151	79722203
Hypotony of eye	49.59	12.06	12	22022	246	79722108
Visual field defect	49.58	12.06	31	22003	9014	79713340
Eye inflammation	45.62	12.06	26	22008	6387	79715967
Completed suicide	45.09	12.06	7	22027	245760	79476594
Blindness	45.04	12.06	47	21987	28336	79694018
Angle closure glaucoma	44.66	12.06	20	22014	2956	79719398
Foreign body sensation in eyes	43.95	12.06	18	22016	2139	79720215
Forced expiratory volume decreased	43.38	12.06	27	22007	7787	79714567
Peak expiratory flow rate decreased	42.21	12.06	13	22021	670	79721684
Cystoid macular oedema	41.97	12.06	17	22017	1963	79720391
Retinal detachment	41.61	12.06	28	22006	9219	79713135
Corneal epithelium defect	41.56	12.06	13	22021	706	79721648
Respiration abnormal	40.95	12.06	26	22008	7762	79714592
Ocular discomfort	40.35	12.06	22	22012	4961	79717393
Uveitis	40.32	12.06	35	21999	16795	79705559
Corneal degeneration	40.02	12.06	9	22025	132	79722222
Pulmonary thrombosis	39.03	12.06	30	22004	12141	79710213
Erythema of eyelid	37.70	12.06	17	22017	2553	79719801
Punctate keratitis	37.53	12.06	13	22021	973	79721381
Conjunctival scar	36.16	12.06	9	22025	208	79722146
Ocular hypertension	35.52	12.06	14	22020	1506	79720848
Endophthalmitis	35.15	12.06	22	22012	6406	79715948
Lung diffusion test decreased	33.92	12.06	13	22021	1297	79721057
Procollagen type I C-terminal propeptide increased	33.52	12.06	6	22028	24	79722330
Product quality issue	33.42	12.06	44	21990	33896	79688458
Instillation site irritation	33.42	12.06	7	22027	72	79722282
Sinus bradycardia	33.41	12.06	38	21996	25209	79697145
Serum procollagen type I N-terminal propeptide increased	32.59	12.06	6	22028	29	79722325
Fall	31.82	12.06	237	21797	487392	79234962
Vitreous haemorrhage	31.76	12.06	17	22017	3696	79718658
Blepharitis	31.58	12.06	16	22018	3108	79719246
Forced vital capacity decreased	30.33	12.06	13	22021	1730	79720624
Visual impairment	29.41	12.06	73	21961	92058	79630296
Eyelid margin crusting	29.19	12.06	11	22023	1048	79721306
Flat anterior chamber of eye	28.41	12.06	7	22027	155	79722199
Intraocular pressure fluctuation	28.36	12.06	6	22028	65	79722289
Atrioventricular block complete	27.24	12.06	28	22006	16582	79705772
Product container issue	27.08	12.06	11	22023	1280	79721074
Chronotropic incompetence	26.31	12.06	6	22028	94	79722260
Synovitis	26.08	12.06	5	22029	150729	79571625
Blindness unilateral	25.95	12.06	20	22014	8126	79714228
Abnormal sensation in eye	25.87	12.06	12	22022	1923	79720431
Nodal rhythm	25.83	12.06	14	22020	3121	79719233
Retinal disorder	25.23	12.06	12	22022	2035	79720319
Visual acuity tests abnormal	25.13	12.06	6	22028	116	79722238
Conjunctival oedema	24.74	12.06	10	22024	1148	79721206
Vitamin B12 decreased	24.37	12.06	14	22020	3491	79718863
Eye disorder	24.06	12.06	31	22003	23381	79698973
Conjunctivitis allergic	24.04	12.06	11	22023	1709	79720645
Atrioventricular block	23.62	12.06	24	22010	14017	79708337
Dizziness	23.37	12.06	235	21799	526206	79196148
Optic nerve cupping	23.32	12.06	5	22029	58	79722296
Systemic lupus erythematosus	23.26	12.06	3	22031	121146	79601208
Corneal decompensation	23.09	12.06	5	22029	61	79722293
Product delivery mechanism issue	22.94	12.06	6	22028	170	79722184
Corneal opacity	22.46	12.06	9	22025	1011	79721343
Growth of eyelashes	22.24	12.06	6	22028	192	79722162
Conjunctivitis	21.79	12.06	31	22003	25684	79696670
Arthralgia	21.69	12.06	83	21951	571720	79150634
Ectropion	21.69	12.06	7	22027	421	79721933
Corneal thickening	21.62	12.06	4	22030	20	79722334
Hypopyon	21.47	12.06	9	22025	1133	79721221
Atrioventricular block second degree	21.23	12.06	17	22017	7295	79715059
Keratopathy	21.09	12.06	9	22025	1185	79721169
Iritis	20.59	12.06	13	22021	3842	79718512
Glaucoma surgery	20.37	12.06	5	22029	109	79722245
Thermal burns of eye	20.33	12.06	5	22029	110	79722244
Vertigo	20.24	12.06	53	21981	69029	79653325
Sinoatrial block	20.02	12.06	9	22025	1342	79721012
Hypotonia	19.86	12.06	21	22013	12849	79709505
Anterior chamber inflammation	19.67	12.06	7	22027	567	79721787
Administration site discomfort	19.35	12.06	5	22029	135	79722219
Sinonasal papilloma	18.85	12.06	4	22030	44	79722310
Abdominal discomfort	18.84	12.06	25	22009	250702	79471652
Macular oedema	18.67	12.06	14	22020	5460	79716894
Abdominal pain	18.62	12.06	51	21983	389518	79332836
Hepatic enzyme increased	18.54	12.06	14	22020	182596	79539758
Dry eye	18.36	12.06	35	21999	36896	79685458
Infusion related reaction	18.30	12.06	22	22012	230215	79492139
Hyponatraemia	18.16	12.06	97	21937	177751	79544603
Toxicity to various agents	18.11	12.06	58	21976	421482	79300872
Macular fibrosis	18.10	12.06	7	22027	716	79721638
Photophobia	17.76	12.06	25	22009	20503	79701851
Pain	17.65	12.06	118	21916	703684	79018670
Symblepharon	17.56	12.06	5	22029	196	79722158
Superficial injury of eye	17.53	12.06	5	22029	197	79722157
Retinal haemorrhage	17.52	12.06	16	22018	8201	79714153
Corneal endothelial cell loss	17.43	12.06	3	22031	9	79722345
Loss of consciousness	17.42	12.06	92	21942	167851	79554503
Maternal exposure during pregnancy	17.34	12.06	8	22026	136530	79585824
Eyelid irritation	17.24	12.06	6	22028	455	79721899
Vitreous floaters	17.20	12.06	15	22019	7241	79715113
Arrhythmia	16.93	12.06	46	21988	61226	79661128
Vitreal cells	16.92	12.06	4	22030	74	79722280
Confusional state	16.60	12.06	147	21887	317850	79404504
Bronchopulmonary disease	16.38	12.06	3	22031	14	79722340
Drug intolerance	16.35	12.06	30	22004	264089	79458265
Hallucination, visual	16.25	12.06	31	22003	32698	79689656
Heterochromia iridis	16.05	12.06	3	22031	16	79722338
Off label use	16.01	12.06	167	21867	907048	78815306
Obstructive airways disorder	15.87	12.06	30	22004	31429	79690925
Product complaint	15.84	12.06	19	22015	13330	79709024
Corneal pigmentation	15.75	12.06	3	22031	18	79722336
Conjunctival follicles	15.75	12.06	3	22031	18	79722336
Achromotrichia acquired	15.75	12.06	3	22031	18	79722336
Corneal infection	15.66	12.06	4	22030	103	79722251
Dermatitis	15.61	12.06	24	22010	21297	79701057
Eye swelling	15.59	12.06	27	22007	26441	79695913
Rhinocerebral mucormycosis	15.52	12.06	7	22027	1051	79721303
Therapeutic product effect incomplete	15.51	12.06	10	22024	141635	79580719
Corneal scar	15.45	12.06	5	22029	303	79722051
Scleral hyperaemia	15.36	12.06	5	22029	309	79722045
Eyelid ptosis	15.26	12.06	17	22017	11027	79711327
Product substitution issue	15.11	12.06	23	22011	20233	79702121
Contraindicated product administered	14.84	12.06	13	22021	157525	79564829
Liquid product physical issue	14.83	12.06	7	22027	1167	79721187
Keratitis interstitial	14.78	12.06	3	22031	26	79722328
Metamorphopsia	14.19	12.06	7	22027	1286	79721068
Iris transillumination defect	14.09	12.06	4	22030	155	79722199
Eyelid oedema	13.87	12.06	18	22016	13669	79708685
Electrolyte depletion	13.86	12.06	5	22029	421	79721933
Subretinal fluid	13.80	12.06	6	22028	826	79721528
Chorioretinal disorder	13.78	12.06	4	22030	168	79722186
Oversensing	13.75	12.06	3	22031	38	79722316
Product use issue	13.74	12.06	23	22011	209799	79512555
Choroidal haemorrhage	13.71	12.06	4	22030	171	79722183
Eye oedema	13.70	12.06	8	22026	2055	79720299
Stag horn calculus	13.69	12.06	4	22030	172	79722182
Intraocular pressure decreased	13.56	12.06	4	22030	178	79722176
Cardiovascular insufficiency	13.35	12.06	9	22025	2972	79719382
Corneal thinning	13.32	12.06	4	22030	189	79722165
Herpes ophthalmic	13.17	12.06	7	22027	1500	79720854
Extrasystoles	13.07	12.06	13	22021	7406	79714948
Alkalosis hypochloraemic	13.04	12.06	5	22029	499	79721855
Cataract subcapsular	12.97	12.06	6	22028	955	79721399
Scleral disorder	12.94	12.06	4	22030	209	79722145
Gastrointestinal haemorrhage	12.72	12.06	77	21957	147642	79574712
Seborrhoeic keratosis	12.71	12.06	8	22026	2352	79720002
Intentional product use issue	12.66	12.06	14	22020	152098	79570256
Blood pressure systolic increased	12.63	12.06	44	21990	66942	79655412
Keratitis	12.45	12.06	10	22024	4312	79718042
Pupillary reflex impaired	12.39	12.06	9	22025	3344	79719010
Dacryocystitis	12.28	12.06	3	22031	64	79722290
Myocardial infarction	12.25	12.06	90	21944	184039	79538315
Retinal vascular occlusion	12.14	12.06	5	22029	602	79721752

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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
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
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

Drug Use | Suggest Off label Use Form| |View source of the data|

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.15	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Ki	9	WOMBAT-PK	CHEMBL
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	ANTAGONIST	Ki	9.70	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.81	DRUG MATRIX
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Ki	6.47	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	6.21	CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_CAVPO		Kd	9.78	CHEMBL
Beta-1 adrenergic receptor	GPCR		B0FL73_CAVPO		Kd	9.44	CHEMBL

External reference:

ID	Source
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
24737	MMSL
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:

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
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/Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0591-2422	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	22 sections
Brimonidine Tartrate and Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0781-7186	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	23 sections
Brimonidine Tartrate and Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0781-7186	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	23 sections
Brimonidine Tartrate and Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0832-1425	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	27 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	17478-189	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
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