Entry

D00659                      Drug

Name

Azelastine hydrochloride (JP18/USP);
Astelin (TN)

Product

Generic

AZELASTINE HYDROCHLORIDE (A-S Medication Solutions), AZELASTINE HYDROCHLORIDE (Amneal Pharmaceuticals LLC), AZELASTINE HYDROCHLORIDE (AvKARE), AZELASTINE HCL NASAL (Bryant Ranch Prepack), AZELASTINE HCL NASAL (Padagis Israel Pharmaceuticals), AZELASTINE HYDROCHLORIDE (A-S Medication Solutions), AZELASTINE HYDROCHLORIDE (Akorn), AZELASTINE HYDROCHLORIDE (Amneal Pharmaceuticals LLC), AZELASTINE HYDROCHLORIDE (Apotex Corp.), AZELASTINE HYDROCHLORIDE (Apotex Corp.), AZELASTINE HYDROCHLORIDE (Apotex Corp.), AZELASTINE HYDROCHLORIDE (Aurobindo Pharma Limited), AZELASTINE HYDROCHLORIDE (Aurobindo Pharma Limited), AZELASTINE HYDROCHLORIDE (Breckenridge Pharmaceutical), AZELASTINE HYDROCHLORIDE (Bryant Ranch Prepack), AZELASTINE HYDROCHLORIDE (Cadila Healthcare Limited), AZELASTINE HYDROCHLORIDE (Fosun Pharma USA), AZELASTINE HYDROCHLORIDE (Gland Pharma Limited), AZELASTINE HYDROCHLORIDE (NuCare Pharmaceuticals), AZELASTINE HYDROCHLORIDE (NuCare Pharmaceuticals), AZELASTINE HYDROCHLORIDE (Proficient Rx LP), AZELASTINE HYDROCHLORIDE (RPK Pharmaceuticals), AZELASTINE HYDROCHLORIDE (RPK Pharmaceuticals), AZELASTINE HYDROCHLORIDE (Sandoz), AZELASTINE HYDROCHLORIDE (Somerset Therapeutics), AZELASTINE HYDROCHLORIDE (Sun Pharmaceutical Industries), AZELASTINE HYDROCHLORIDE (Sun Pharmaceutical Industries), AZELASTINE HYDROCHLORIDE (West-Ward Pharmaceuticals Corp.), AZELASTINE HYDROCHLORIDE (Zydus Pharmaceuticals (USA)), AZELASTINE HYDROCHLORIDE OPHTHALMIC SOLUTION 0.05% (Alembic Pharmaceuticals)

Formula

C22H24ClN3O. HCl

Exact mass

417.1375

Mol weight

418.3594

Structure

Simcomp

Class

Anti-allergic agent
DG01557 Histamine receptor antagonist
DG01482 Histamine receptor H1 antagonist

Remark

Therapeutic category:

4490

ATC code:

R01AC03 R06AX19 S01GX07

Chemical structure group:

DG01036

Product (DG01036):

D00659<JP/US>

Product (mixture):

D11656<US>

Efficacy

Antiallergic, Antiasthmatic, H1 receptor antagonist

Disease

Allergic rhinitis [DS:H01360]

Target

HRH1 [HSA:3269] [KO:K04149]

Pathway

hsa04020

Calcium signaling pathway

hsa04080

Neuroactive ligand-receptor interaction

Interaction

Structure map

map07212

Histamine H1 receptor antagonists

Brite

Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
R RESPIRATORY SYSTEM
  R01 NASAL PREPARATIONS
   R01A DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
    R01AC Antiallergic agents, excl. corticosteroids
     R01AC03 Azelastine
      D00659  Azelastine hydrochloride (JP18/USP) <JP/US>
  R06 ANTIHISTAMINES FOR SYSTEMIC USE
   R06A ANTIHISTAMINES FOR SYSTEMIC USE
    R06AX Other antihistamines for systemic use
     R06AX19 Azelastine
      D00659  Azelastine hydrochloride (JP18/USP) <JP/US>
S SENSORY ORGANS
  S01 OPHTHALMOLOGICALS
   S01G DECONGESTANTS AND ANTIALLERGICS
    S01GX Other antiallergics
     S01GX07 Azelastine
      D00659  Azelastine hydrochloride (JP18/USP) <JP/US>
USP drug classification [BR:br08302]
Ophthalmic Agents
  Ophthalmic Anti-allergy Agents
   Antihistamine
    Azelastine
     D00659  Azelastine hydrochloride (JP18/USP)
Respiratory Tract/Pulmonary Agents
  Antihistamines
   Histamine (H1) Receptor Antagonists, Mildly/Non-sedating
    Azelastine
     D00659  Azelastine hydrochloride (JP18/USP)
Therapeutic category of drugs in Japan [BR:br08301]
4  Agents affecting cellular function
  44  Allergic agents
   449  Miscellaneous
    4490  Miscellaneous
     D00659  Azelastine hydrochloride (JP18/USP)
Classification of Japanese OTC drugs [BR:br08313]
Allergic agents
  52 Antihistamine based drugs
   D00659  Azelastine hydrochloride (JP18/USP)
  53 Other allergic agents
   D00659  Azelastine hydrochloride (JP18/USP)
Risk category of Japanese OTC drugs [BR:br08312]
Second-class OTC drugs
  Inorganic and organic chemicals
   Azelastine
    D00659  Azelastine hydrochloride (JP18/USP)
Drug groups [BR:br08330]
Anti-allergic agent
  DG01557  Histamine receptor antagonist
   DG01482  Histamine receptor H1 antagonist
    DG01036  Azelastine
     D00659  Azelastine hydrochloride
Drug classes [BR:br08332]
Anti-allergic agent
  DG01482  Histamine receptor H1 antagonist
   D00659  Azelastine hydrochloride
Target-based classification of drugs [BR:br08310]
G Protein-coupled receptors
  Rhodopsin family
   Histamine
    HRH1
     D00659  Azelastine hydrochloride (JP18/USP) <JP/US>
Drugs listed in the Japanese Pharmacopoeia [BR:br08311]
Chemicals
  D00659  Azelastine hydrochloride
  D00659  Azelastine hydrochloride granules
Rx-to-OTC switch list in Japan [br08314.html]
D00659
Drug groups [BR:br08330]
Anti-allergic agent
  DG01557  Histamine receptor antagonist
   DG01482  Histamine receptor H1 antagonist
    DG01036  Azelastine

Other DBs

CAS:	79307-93-0

PubChem:

7847725

ChEBI:

2951

LigandBox:

D00659

NIKKAJI:

J364.889C

KCF data

ATOM        28
            1   X   Cl   31.8050  -18.2160
            2   C1y C    27.4868  -20.1967
            3   C1x C    28.5815  -19.3346
            4   C1x C    29.9443  -19.6454
            5   N1y N    30.5451  -20.8963
            6   C1x C    27.4868  -21.6031
            7   C1x C    29.9452  -22.1612
            8   C1x C    28.5815  -22.4722
            9   N4y N    26.2277  -19.5856
            10  N5x N    26.2845  -18.1858
            11  C8y C    24.9979  -17.4984
            12  C8y C    23.7944  -18.2084
            13  C8y C    23.8074  -19.6086
            14  C8y C    25.0240  -20.2960
            15  C8x C    22.5778  -17.5209
            16  C8x C    21.3741  -18.2308
            17  C8x C    21.3171  -19.6311
            18  C8x C    22.6037  -20.3185
            19  C1b C    24.9845  -16.0905
            20  C8y C    26.2038  -15.4501
            21  C8x C    27.4009  -16.2066
            22  C8x C    28.7080  -15.5568
            23  C8y C    28.6938  -14.1607
            24  C8x C    27.4969  -13.4042
            25  C8x C    26.1898  -14.0539
            26  X   Cl   29.9185  -13.5170
            27  C1a C    31.9483  -20.9628
            28  O5x O    24.9670  -21.6792
BOND        30
            1     4   5 1
            2     2   6 1
            3     5   7 1
            4     3   4 1
            5     6   8 1
            6     2   3 1
            7     7   8 1
            8     2   9 1
            9     9  10 1
            10   10  11 2
            11   11  12 1
            12   12  13 1
            13   13  14 1
            14    9  14 1
            15   12  15 2
            16   15  16 1
            17   16  17 2
            18   17  18 1
            19   13  18 2
            20   11  19 1
            21   19  20 1
            22   20  21 2
            23   21  22 1
            24   22  23 2
            25   23  24 1
            26   24  25 2
            27   20  25 1
            28   23  26 1
            29    5  27 1
            30   14  28 2