Entry

D00603                      Drug

Name

Timolol maleate (JP18/USP);
Blocadren (TN);
Istalol (TN);
Timoptic (TN)

Product

ISTALOL (Bausch & Lomb Incorporated), TIMOPTIC (Bausch & Lomb Incorporated), TIMOPTIC-XE (Bausch & Lomb Incorporated), TIMOPTIC IN OCUDOSE (Bausch & Lomb Incorporated), TIMOPTIC IN OCUDOSE (Bausch Health US LLC), TIMOLOL GFS (Sandoz)

Generic

TIMOLOL MALEATE (A-S Medication Solutions), TIMOLOL MALEATE (A-S Medication Solutions), TIMOLOL MALEATE (A-S Medication Solutions), TIMOLOL MALEATE (A-S Medication Solutions), TIMOLOL MALEATE (Akorn), TIMOPTIC IN OCUDOSE (Amring Pharmaceuticals), TIMOLOL MALEATE (Apotex Corp), TIMOLOL MALEATE (Ascend Laboratories), TIMOLOL MALEATE (Athem LLC), TIMOLOL MALEATE (BAUSCH & LOMB INCORPORATED), TIMOLOL MALEATE (Bausch & Lomb Americas), TIMOLOL MALEATE (Bausch & Lomb Americas), TIMOLOL MALEATE (Bausch & Lomb Americas), TIMOLOL MALEATE (Bausch & Lomb Americas), TIMOLOL MALEATE (Bausch & Lomb Incorporated), TIMOLOL MALEATE (Bryant Ranch Prepack), TIMOLOL MALEATE (Medsource Pharmaceuticals), TIMOLOL MALEATE (Mylan Pharmaceuticals), TIMOLOL MALEATE (Oceanside Pharmaceuticals), TIMOLOL MALEATE (Oceanside Pharmaceuticals), TIMOLOL MALEATE (Pacific Pharma), TIMOLOL MALEATE (Rising Pharmaceuticals), TIMOLOL MALEATE (Sandoz), TIMOLOL MALEATE OPHTHALMIC GEL FORMING SOLUTION (Gland Pharma Limited), TIMOLOL MALEATE OPHTHALMIC GEL FORMING SOLUTION, 0.25% (Alembic Pharmaceuticals)

Formula

C13H24N4O3S. C4H4O4

Exact mass

432.1679

Mol weight

432.4918

Structure

Class

Cardiovascular agent
DG01466  Adrenergic receptor antagonist
  DG01464  beta-Adrenergic receptor antagonist (Beta blocker)
Ophthalmic agent
DG03201  Intraocular pressure lowering agent
Metabolizing enzyme substrate
DG01644  CYP2D6 substrate

Remark

Therapeutic category:

1319

ATC code:

C07AA06 S01ED01

Chemical structure group:

DG00306

Product (DG00306):

D00378<US> D00603<JP/US>

Product (mixture):

D07505<JP> D08493<JP/US> D09815<JP> D10298<JP/US> D10512<JP> D10569<JP>

Efficacy

Antiglaucoma, beta-Adrenergic receptor antagonist

Disease

Open-angle glaucoma [DS:H00612]

Comment

Propranolol derivative

Target

ADRB1 [HSA:153] [KO:K04141]
ADRB2 [HSA:154] [KO:K04142]

Pathway

hsa04020

Calcium signaling pathway

hsa04022

cGMP-PKG signaling pathway

hsa04024

cAMP signaling pathway

hsa04080

Neuroactive ligand-receptor interaction

hsa04261

Adrenergic signaling in cardiomyocytes

Metabolism

Enzyme: CYP2D6 [HSA:1565]

Interaction

Structure map

map07054

Antiglaucoma agents

Brite

Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
C CARDIOVASCULAR SYSTEM
  C07 BETA BLOCKING AGENTS
   C07A BETA BLOCKING AGENTS
    C07AA Beta blocking agents, non-selective
     C07AA06 Timolol
      D00603  Timolol maleate (JP18/USP) <JP/US>
S SENSORY ORGANS
  S01 OPHTHALMOLOGICALS
   S01E ANTIGLAUCOMA PREPARATIONS AND MIOTICS
    S01ED Beta blocking agents
     S01ED01 Timolol
      D00603  Timolol maleate (JP18/USP) <JP/US>
USP drug classification [BR:br08302]
Antimigraine Agents
  Antimigraine Agents, Other
   Timolol
    D00603  Timolol maleate (JP18/USP)
Cardiovascular Agents
  Beta-adrenergic Blocking Agents
   Non-Selective
    Timolol
     D00603  Timolol maleate (JP18/USP)
Ophthalmic Agents
  Intraocular Pressure Lowering Agents
   Beta-adrenergic Blocking Agents, Ophthalmic
    Timolol
     D00603  Timolol maleate (JP18/USP)
Therapeutic category of drugs in Japan [BR:br08301]
1  Agents affecting nervous system and sensory organs
  13  Agents affecting sensory organs
   131  Ophthalmic agents
    1319  Others
     D00603  Timolol maleate (JP18/USP)
Drug groups [BR:br08330]
Cardiovascular agent
  DG01466  Adrenergic receptor antagonist
   DG01464  beta-Adrenergic receptor antagonist (Beta blocker)
    DG00306  Timolol
     D00603  Timolol maleate
Ophthalmic agent
  DG03201  Intraocular pressure lowering agent
   DG00306  Timolol
    D00603  Timolol maleate
Metabolizing enzyme substrate
  DG01644  CYP2D6 substrate
   DG00306  Timolol
    D00603  Timolol maleate
Drug classes [BR:br08332]
Ophthalmic agent
  DG03201  Intraocular pressure lowering agent
   D00603  Timolol maleate
Target-based classification of drugs [BR:br08310]
G Protein-coupled receptors
  Rhodopsin family
   Adrenaline
    ADRB1
     D00603  Timolol maleate (JP18/USP) <JP/US>
    ADRB2
     D00603  Timolol maleate (JP18/USP) <JP/US>
Drugs listed in the Japanese Pharmacopoeia [BR:br08311]
Chemicals
  D00603  Timolol maleate
Drug metabolizing enzymes and transporters [br08309.html]
Drug metabolizing enzymes
  D00603
Drug groups [BR:br08330]
Cardiovascular agent
  DG01466  Adrenergic receptor antagonist
   DG01464  beta-Adrenergic receptor antagonist (Beta blocker)
    DG00306  Timolol
Ophthalmic agent
  DG03201  Intraocular pressure lowering agent
   DG00306  Timolol
Metabolizing enzyme substrate
  DG01644  CYP2D6 substrate
   DG00306  Timolol

Other DBs

CAS:	26921-17-5

PubChem:

7847669

ChEBI:

9600

LigandBox:

D00603

NIKKAJI:

J353.618A

KCF data

ATOM        29
            1   C2b C    27.1995  -15.4829
            2   C2b C    25.5020  -15.4829
            3   C6a C    27.8361  -16.6145
            4   C6a C    24.8653  -16.6852
            5   O6a O    27.1995  -17.8170
            6   O6a O    29.2508  -16.6145
            7   O6a O    23.4508  -16.6852
            8   O6a O    25.5020  -17.8170
            9   C1b C    14.1400  -15.9600
            10  C1c C    15.3300  -16.6600
            11  O2a O    12.9500  -16.6600
            12  C1b C    16.5200  -15.9600
            13  N1b N    17.7100  -16.6600
            14  C1d C    18.9000  -15.9600
            15  C1a C    20.1600  -16.6600
            16  C1a C    18.9000  -14.5600
            17  C1a C    20.1600  -15.2600
            18  O1a O    15.3300  -18.0600
            19  C8y C    12.9500  -18.0600
            20  C8y C    11.8300  -18.9700
            21  N5x N    12.2500  -20.2300
            22  S2x S    13.6500  -20.2300
            23  N5x N    14.0700  -18.9700
            24  O2x O     8.1200  -16.8000
            25  C1x C     8.1200  -18.2700
            26  C1x C     9.3100  -18.9700
            27  N1y N    10.5700  -18.2700
            28  C1x C    10.5700  -16.8000
            29  C1x C     9.3100  -16.1000
BOND        29
            1     1   2 2
            2     1   3 1
            3     2   4 1
            4     3   5 1
            5     3   6 2
            6     4   7 1
            7     4   8 2
            8     9  10 1
            9     9  11 1
            10   10  12 1
            11   12  13 1
            12   13  14 1
            13   14  15 1
            14   14  16 1
            15   14  17 1
            16   10  18 1 #Down
            17   11  19 1
            18   19  20 1
            19   20  21 2
            20   21  22 1
            21   22  23 1
            22   19  23 2
            23   24  25 1
            24   25  26 1
            25   26  27 1
            26   27  28 1
            27   28  29 1
            28   24  29 1
            29   27  20 1