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

Stem definitionDrug idCAS RN
903 5636-83-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dimetindene maleate
  • dimethindene maleate
  • dimethindene
  • dimetindene
A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies.
  • Molecular weight: 292.43
  • Formula: C20H24N2
  • CLOGP: 3.53
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 16.13
  • ALOGS: -3.88
  • ROTB: 5

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 2.16 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.83 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
COVID-19 100.16 28.45 70 3770 113033 63372149
Polyneuropathy 80.33 28.45 31 3809 14558 63470624
General physical health deterioration 61.52 28.45 68 3772 201334 63283848
Drug ineffective 48.61 28.45 4 3836 1044761 62440421
Pyrexia 46.14 28.45 93 3747 470385 63014797
Thyroid stimulating immunoglobulin increased 43.53 28.45 7 3833 78 63485104
Leukopenia 42.29 28.45 36 3804 77254 63407928
Chronic hepatitis B 39.35 28.45 8 3832 349 63484833
Glomerulonephritis chronic 39.28 28.45 7 3833 149 63485033
Anti-thyroid antibody positive 37.87 28.45 8 3832 422 63484760
Neuropsychiatric symptoms 33.19 28.45 8 3832 765 63484417
Thrombocytopenia 32.87 28.45 43 3797 151114 63334068
Renal pain 32.70 28.45 13 3827 6586 63478596
Coronavirus infection 30.52 28.45 11 3829 4267 63480915
Circulatory collapse 30.30 28.45 18 3822 21920 63463262
Dry skin 30.09 28.45 26 3814 56861 63428321

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Polyneuropathy 68.41 26.77 26 1647 14870 34940388
COVID-19 47.54 26.77 35 1638 77515 34877743
Flushing 32.78 26.77 20 1653 32400 34922858
Noninfective conjunctivitis 27.36 26.77 4 1669 29 34955229

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
COVID-19 141.55 24.00 101 5059 157573 79581655
Polyneuropathy 135.58 24.00 53 5107 24098 79715130
General physical health deterioration 64.53 24.00 84 5076 275154 79464074
Coronavirus infection 47.56 24.00 18 5142 7479 79731749
Leukopenia 43.07 24.00 45 5115 116468 79622760
Drug ineffective 42.85 24.00 9 5151 1080904 78658324
Thyroid stimulating immunoglobulin increased 42.28 24.00 7 5153 88 79739140
Blood lactate dehydrogenase increased 39.47 24.00 27 5133 39143 79700085
Pyrexia 37.23 24.00 112 5048 678597 79060631
Chronic hepatitis B 36.94 24.00 8 5152 443 79738785
Anti-thyroid antibody positive 36.11 24.00 8 5152 493 79738735
Glomerulonephritis chronic 34.75 24.00 7 5153 272 79738956
Anaemia 32.89 24.00 82 5078 444933 79294295
Lip erosion 31.52 24.00 9 5151 1551 79737677
Flushing 30.67 24.00 33 5127 88235 79650993
Oral herpes 30.23 24.00 20 5140 27434 79711794
Autoimmune thyroiditis 29.91 24.00 11 5149 4222 79735006
Maternal exposure before pregnancy 29.56 24.00 11 5149 4362 79734866
Infertility 28.32 24.00 7 5153 694 79738534
Circulatory collapse 24.56 24.00 20 5140 37648 79701580
Bacterial test 24.46 24.00 7 5153 1216 79738012
Thyroxine free increased 24.41 24.00 7 5153 1225 79738003

FDA Adverse Event Reporting System (Pediatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Small for dates baby 12.13 12.06 5 3 2804 86980

Pharmacologic Action:

SourceCodeDescription
ATC D04AA13 DERMATOLOGICALS
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Antihistamines for topical use
ATC R06AB03 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Substituted alkylamines
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D000982 Antipruritics
MeSH PA D003879 Dermatologic Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.21 Basic
pKa2 5.05 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H1 receptor GPCR Ki 9.16 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 6.58 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 7.35 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 6.72 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 6.39 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 6.10 CHEMBL

External reference:

IDSource
D01343 KEGG_DRUG
3614-69-5 SECONDARY_CAS_RN
258334 RXNORM
CHEBI:31500 CHEBI
CHEMBL22108 ChEMBL_ID
CHEMBL1870768 ChEMBL_ID
DB08801 DRUGBANK_ID
10101 IUPHAR_LIGAND_ID
21855 PUBCHEM_CID
003407 NDDF
004804 NDDF
26122009 SNOMEDCT_US
387142004 SNOMEDCT_US
C0012390 UMLSCUI
D004115 MESH_DESCRIPTOR_UI
1403 INN_ID
6LL60J9E0O UNII

Pharmaceutical products:

None