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

Stem definition	Drug id	CAS RN
	916	58-73-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: benadryl diphenhydramine salicylate diphenhydramine laurylsulfate diphenhydramine benzhydramine probedryl diphenhydramine hydrochloride diphenhydramine citrate diphenhydramine HCl	A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects. Molecular weight: 255.36 Formula: C17H21NO CLOGP: 3.45 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 12.47 ALOGS: -3.53 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

benadryl
diphenhydramine salicylate
diphenhydramine laurylsulfate
diphenhydramine
benzhydramine
probedryl
diphenhydramine hydrochloride
diphenhydramine citrate
diphenhydramine HCl

A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.

Molecular weight: 255.36
Formula: C17H21NO
CLOGP: 3.45
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 12.47
ALOGS: -3.53
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.20	g	O
0.20	g	R

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	9.30 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	72 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	6.50 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	3.26 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1000 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.19 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
March 4, 1946	FDA	MCNEIL CONS

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
Completed suicide	2969.15	10.85	5504	680908	140169	62662441
Toxicity to various agents	2838.75	10.85	7414	678998	239836	62562774
Infusion related reaction	1175.99	10.85	5512	680900	240009	62562601
Exposure to toxic agent	749.87	10.85	561	685851	5026	62797584
Sinusitis	504.92	10.85	4180	682232	222473	62580137
Blood pressure fluctuation	491.13	10.85	1351	685061	44966	62757644
Overdose	473.20	10.85	2476	683936	112602	62690008
Drug abuse	419.90	10.85	1725	684687	70793	62731817
Intentional overdose	415.35	10.85	1746	684666	72406	62730204
Urticaria	412.41	10.85	3137	683275	162665	62639945

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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
Toxicity to various agents	1960.19	10.94	4603	267086	195759	34489483
Completed suicide	1767.87	10.94	2918	268771	95250	34589992
Infusion related reaction	1243.40	10.94	1783	269906	51274	34633968
Drug abuse	519.95	10.94	1823	269866	97273	34587969
Blood pressure fluctuation	443.00	10.94	743	270946	24506	34660736
Exposure to toxic agent	438.92	10.94	302	271387	3373	34681869
Intentional product misuse	411.20	10.94	1018	270671	44593	34640649
Overdose	353.16	10.94	1523	270166	89536	34595706
Urticaria	281.85	10.94	1094	270595	61283	34623959
Intentional overdose	281.29	10.94	862	270827	42812	34642430

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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
Completed suicide	4918.55	10.18	8744	778404	237023	78720217
Toxicity to various agents	4550.60	10.18	11659	775489	409881	78547359
Infusion related reaction	1874.36	10.18	5757	781391	224480	78732760
Exposure to toxic agent	1163.60	10.18	858	786290	8300	78948940
Blood pressure fluctuation	920.86	10.18	2043	785105	65102	78892138
Intentional product misuse	865.57	10.18	2477	784671	92688	78864552
Drug abuse	801.62	10.18	3457	783691	159234	78798006
Overdose	777.18	10.18	3739	783409	180467	78776773
Intentional overdose	756.56	10.18	2535	784613	103425	78853815
Urticaria	597.88	10.18	3492	783656	181709	78775531

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FDA Adverse Event Reporting System (Pediatric)

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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
Incorrect route of product administration	22.41	20.24	6	364	7	89415

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Pharmacologic Action:

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Source	Code	Description
ATC	D04AA32	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use
ATC	R06AA02	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers
ATC	R06AA52	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:36333	local anesthetics
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:50919	antiemetico

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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
Vasomotor rhinitis	indication	8229003	DOID:4730
Insomnia	indication	193462001
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204
Migraine	off-label use	37796009	DOID:6364
Anxiety disorder	off-label use	197480006	DOID:2030
Local anesthesia	off-label use	386761002

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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	8.52	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
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.81	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.59	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Kd	6.02	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.43	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.15	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.29	DRUG MATRIX
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		Ki	4.37	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	7	WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.92	WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.64	WOMBAT-PK

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External reference:

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ID	Source
2PM	PDB_CHEM_ID
003369	NDDF
004787	NDDF
005115	NDDF
103659-13-8	SECONDARY_CAS_RN
1224	IUPHAR_LIGAND_ID
1362	RXNORM
147-24-0	SECONDARY_CAS_RN
14992	MMSL
1676	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Childrens Dimetapp Multi-Symptom Cold and Flu	HUMAN OTC DRUG LABEL	3	0031-2249	LIQUID	12.50 mg	ORAL	Unapproved drug other	17 sections
Childrens Night Time Cold and Cough	HUMAN OTC DRUG LABEL	2	0113-0808	SOLUTION	6.25 mg	ORAL	OTC monograph final	15 sections
Excedrin PM Triple Action Caplets	HUMAN OTC DRUG LABEL	3	0067-2056	TABLET, COATED	38 mg	ORAL	OTC monograph not final	16 sections
Excedrin PM Triple Action Caplets	HUMAN OTC DRUG LABEL	3	0067-2056	TABLET, COATED	38 mg	ORAL	OTC monograph not final	16 sections
good sense allergy	HUMAN OTC DRUG LABEL	1	0113-0379	SOLUTION	12.50 mg	ORAL	OTC monograph final	14 sections
Good Sense Allergy Relief	HUMAN OTC DRUG LABEL	1	0113-0462	CAPSULE	25 mg	ORAL	OTC monograph final	15 sections
good sense allergy relief	HUMAN OTC DRUG LABEL	1	0113-0479	TABLET	25 mg	ORAL	OTC monograph final	15 sections
good sense allergy relief	HUMAN OTC DRUG LABEL	1	0113-0479	TABLET	25 mg	ORAL	OTC monograph final	15 sections
good sense ibuprofen pm	HUMAN OTC DRUG LABEL	2	0113-0050	TABLET, FILM COATED	38 mg	ORAL	ANDA	16 sections
good sense itch relief	HUMAN OTC DRUG LABEL	2	0113-0622	CREAM	2 g	TOPICAL	OTC monograph not final	14 sections

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