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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:

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

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Approvals:

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

FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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

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

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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

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🐶 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:

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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

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External reference:

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ID	Source
TIM	PDB_CHEM_ID
001856	NDDF
004741	NDDF
10600	RXNORM
24737	MMSL
26921-17-5	SECONDARY_CAS_RN
33624	PUBCHEM_CID
372880004	SNOMEDCT_US
4017930	VANDF
4019949	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
Brimonidine Tartrate/Timolol Maleate	HUMAN PRESCRIPTION DRUG LABEL	2	0591-2422	SOLUTION/ DROPS	5 mg	OPHTHALMIC	ANDA	22 sections
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
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
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

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