All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

dimetindene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
	903	5636-83-9

Description:

Molecule	Description
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:

Dose	Unit	Route
4	mg	O

ADMET properties:

Property	Value	Reference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	1.805		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.855		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	29.174	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	28.642	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	34.730	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	33.030	%	High	1
herg	hERG pIC50	5.225	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	4.786	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	12.677	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	29.570	%	High	1
kinase-safety-class	ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK3,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PIM2,PRKDC,TEK,TGFBR1	26
kinase-selectivity-class	AXL,BRAF,STK33	3
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	1.514		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	102.094		High	1
mppb	Mouse plasma protein binding (% unbound)	33.230		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	7.396		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	44.610	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	119.674	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	61.370	%	High	1
rppb	Rat plasma protein binding (% unbound)	36.790	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	897.429	uM	High	1

Approvals:

None

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
COVID-19	156.08	28.02	104	4952	168739	90454652
Polyneuropathy	135.47	28.02	48	5008	19293	90604098
Anaemia	56.53	28.02	83	4973	352719	90270672
Osteochondrosis	54.92	28.02	14	5042	1829	90621562
Dysgeusia	54.82	28.02	35	5021	52525	90570866
Drug ineffective	51.57	28.02	8	5048	1384290	89239101
Conjunctivitis	49.89	28.02	26	5030	26680	90596711
Coronavirus infection	47.55	28.02	16	5040	5499	90617892
Dry skin	46.82	28.02	39	5017	88034	90535357
Vulvovaginal dryness	46.30	28.02	14	5042	3417	90619974
Renal pain	45.86	28.02	17	5039	7742	90615649
Febrile neutropenia	45.67	28.02	50	5006	158299	90465092
Lip erosion	44.86	28.02	11	5045	1227	90622164
Pyrexia	43.33	28.02	106	4950	660379	89963012
Circulatory collapse	42.99	28.02	23	5033	24881	90598510
Stevens-Johnson syndrome	42.11	28.02	24	5032	29352	90594039
Thyroid stimulating immunoglobulin increased	40.55	28.02	7	5049	134	90623257
Glomerulonephritis chronic	40.17	28.02	7	5049	142	90623249
Chronic hepatitis B	39.12	28.02	8	5048	390	90623001
Mucosal dryness	38.81	28.02	12	5044	3155	90620236
Leukopenia	38.46	28.02	37	5019	100673	90522718
Anti-thyroid antibody positive	37.40	28.02	8	5048	486	90622905
Vertigo	37.27	28.02	31	5025	69780	90553611
General physical health deterioration	37.15	28.02	69	4987	355046	90268345
Dyspnoea exertional	34.30	28.02	30	5026	72258	90551133
Ejection fraction decreased	33.78	28.02	20	5036	26233	90597158
Diarrhoea	33.14	28.02	121	4935	939069	89684322
Flank pain	31.07	28.02	17	5039	19205	90604186
Cardiovascular disorder	30.66	28.02	15	5041	13477	90609914

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
Polyneuropathy	71.23	26.46	29	2144	18632	42600530
COVID-19	67.47	26.46	52	2121	115896	42503266
Renal oncocytoma	51.51	26.46	9	2164	204	42618958
Calculus bladder	34.82	26.46	9	2164	1361	42617801
Toxic epidermal necrolysis	29.87	26.46	18	2155	26732	42592430
Leukopenia	27.85	26.46	26	2147	74720	42544442
Noninfective conjunctivitis	26.87	26.46	4	2169	31	42619131
Flushing	26.83	26.46	19	2154	37009	42582153

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
COVID-19	211.88	23.72	151	6727	244909	110337512
Polyneuropathy	188.69	23.72	72	6806	31940	110550481
Coronavirus infection	65.42	23.72	24	6854	9521	110572900
Anaemia	64.55	23.72	119	6759	546967	110035454
Leukopenia	59.73	23.72	59	6819	148732	110433689
Osteochondrosis	53.59	23.72	15	6863	2506	110579915
Toxic epidermal necrolysis	53.57	23.72	37	6841	56690	110525731
Lip erosion	53.23	23.72	14	6864	1852	110580569
Vulvovaginal dryness	52.31	23.72	15	6863	2732	110579689
Drug ineffective	50.59	23.72	16	6862	1520524	109061897
Conjunctivitis	49.27	23.72	29	6849	33763	110548658
Renal oncocytoma	48.34	23.72	9	6869	239	110582182
General physical health deterioration	46.95	23.72	90	6788	425205	110157216
Stevens-Johnson syndrome	42.89	23.72	30	6848	46871	110535550
Blood lactate dehydrogenase increased	39.71	23.72	28	6850	44306	110538115
Vertigo	39.66	23.72	37	6841	86833	110495588
Pyrexia	39.55	23.72	134	6744	898131	109684290
Dysgeusia	38.26	23.72	33	6845	69952	110512469
Thyroid stimulating immunoglobulin increased	38.12	23.72	7	6871	172	110582249
Chronic hepatitis B	35.44	23.72	8	6870	559	110581862
Anti-thyroid antibody positive	35.24	23.72	8	6870	573	110581848
Glomerulonephritis chronic	34.68	23.72	7	6871	286	110582135
Flushing	33.85	23.72	37	6841	104699	110477722
Circulatory collapse	33.59	23.72	25	6853	42968	110539453
Dry skin	33.01	23.72	37	6841	107616	110474805
Calculus bladder	30.78	23.72	9	6869	1755	110580666
Oral herpes	28.23	23.72	21	6857	36059	110546362
Infertility	27.84	23.72	7	6871	775	110581646
Febrile neutropenia	27.77	23.72	61	6817	316706	110265715
Dyspnoea	27.17	23.72	138	6740	1106734	109475687
Fatigue	26.70	23.72	147	6731	1215811	109366610
Left ventricular dysfunction	26.20	23.72	17	6861	23476	110558945
Autoimmune thyroiditis	25.86	23.72	11	6867	6423	110575998
Shrinking lung syndrome	25.58	23.72	5	6873	173	110582248
Bacterial test	24.93	23.72	7	6871	1182	110581239
Renal pain	24.36	23.72	12	6866	9805	110572616

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018926	Anti-Allergic Agents
CHEBI has role	CHEBI:38070	anti-arrhythmia drug

Related Drugs by ATC class:

D04AA Antihistamines for topical use 13 drugs

bamipinechloropyraminechlorphenoxamineclemastinediphenhydramineisothipendylmepyraminepheniraminepromethazinethenalidinethonzylaminetolpropamine show all 13 →

R06AB Substituted alkylamines 6 drugs

brompheniraminechlorphenaminedexbrompheniraminedexchlorpheniraminepheniraminetalastine

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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	9.16		CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.58		CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	7.35		CHEMBL
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.72		CHEMBL
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	6.39		CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.10		CHEMBL

External reference:

ID	Source
D01343	KEGG_DRUG
3614-69-5	SECONDARY_CAS_RN
258334	RXNORM
CHEBI:748025	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
6LL60J9E0O	UNII
1403	INN_ID
6LL60J9E0O	INXIGHT DRUGS

Pharmaceutical products:

None