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

Stem definition	Drug id	CAS RN
diphenylmethyl piperazine derivatives	1649	569-65-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: meclizine meclizine hydrochloride meclozine meclozine dihydrochloride meclizine HCl	A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. Molecular weight: 390.96 Formula: C25H27ClN2 CLOGP: 6.73 LIPINSKI: 1 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -5.58 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

meclizine
meclizine hydrochloride
meclozine
meclozine dihydrochloride
meclizine HCl

A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Molecular weight: 390.96
Formula: C25H27ClN2
CLOGP: 6.73
LIPINSKI: 1
HAC: 2
HDO: 0
TPSA: 6.48
ALOGS: -5.58
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
50	mg	O
50	mg	R

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
S (Water solubility)	0.26 mg/mL	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Feb. 14, 1957	FDA	CITRON PHARMA LLC

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
Vertigo	179.07	12.59	163	24313	59724	63404822
Dizziness	110.51	12.59	390	24086	429535	63035011
Drug ineffective	66.49	12.59	196	24280	1044569	62419977
Fall	66.42	12.59	313	24163	392021	63072525
Treatment failure	61.03	12.59	4	24472	199039	63265507
Cerebrovascular accident	54.18	12.59	125	24351	107899	63356647
Synovitis	53.81	12.59	5	24471	186913	63277633
Multiple sclerosis relapse	53.64	12.59	79	24397	48399	63416147
Systemic lupus erythematosus	45.79	12.59	12	24464	208906	63255640
Maternal exposure during pregnancy	43.95	12.59	15	24461	220047	63244499
Transient ischaemic attack	42.45	12.59	62	24414	37691	63426855
Glossodynia	41.71	12.59	9	24467	178867	63285679
Salivary gland calculus	39.89	12.59	10	24466	168	63464378
Infusion related reaction	39.22	12.59	23	24453	245498	63219048
Urticaria thermal	35.09	12.59	11	24465	428	63464118
Multiple sclerosis	33.35	12.59	44	24432	24328	63440218
Hepatic enzyme increased	32.24	12.59	19	24457	202309	63262237
Chest pain	31.26	12.59	165	24311	215794	63248752
Femoral neck fracture	31.08	12.59	26	24450	8497	63456049
Arthropathy	30.94	12.59	27	24449	234765	63229781
Urinary tract infection	29.69	12.59	189	24287	264495	63200051
Migraine	29.22	12.59	97	24379	103249	63361297
Anxiety	28.65	12.59	162	24314	217379	63247167
Gait disturbance	28.62	12.59	143	24333	183035	63281511
Lower respiratory tract infection	28.22	12.59	8	24468	132299	63332247
Coronary artery disease	27.82	12.59	47	24429	32330	63432216
Asthenia	27.79	12.59	247	24229	383357	63081189
Off label use	27.75	12.59	150	24326	674312	62790234
Drug intolerance	26.62	12.59	49	24427	308612	63155934
Depression	26.31	12.59	147	24329	196345	63268201
Dizziness postural	25.86	12.59	22	24454	7354	63457192
Administration site erythema	25.53	12.59	10	24466	755	63463791
General physical health deterioration	25.53	12.59	24	24452	201378	63263168
Dysphoria	24.26	12.59	18	24458	4948	63459598
Visual impairment	23.63	12.59	79	24397	84367	63380179
Discomfort	23.59	12.59	18	24458	167356	63297190
Somnolence neonatal	23.24	12.59	6	24470	114	63464432
Vitamin B12 deficiency	23.21	12.59	18	24458	5285	63459261
Balance disorder	22.77	12.59	78	24398	84344	63380202
Infantile apnoea	22.63	12.59	10	24466	1023	63463523
Product dose omission issue	22.48	12.59	161	24315	234152	63230394
Wound	22.45	12.59	18	24458	163245	63301301
Joint swelling	21.74	12.59	60	24416	327606	63136940
Illness	21.59	12.59	54	24422	49005	63415541
C-reactive protein increased	21.59	12.59	5	24471	94702	63369844
Completed suicide	21.54	12.59	112	24364	145561	63318985
Sialoadenitis	20.85	12.59	11	24465	1661	63462885
Pyrexia	19.66	12.59	104	24372	470374	62994172
Tremor	19.08	12.59	101	24375	132138	63332408
Neutropenia	18.70	12.59	24	24452	174981	63289565
Swelling	18.58	12.59	50	24426	275328	63189218
Feeling abnormal	18.53	12.59	109	24367	148283	63316263
Appetite disorder	18.18	12.59	18	24458	7303	63457243
Hypoaesthesia	18.09	12.59	119	24357	168274	63296272
Ventricular hypertrophy	18.02	12.59	13	24463	3423	63461123
Rheumatoid arthritis	17.95	12.59	45	24431	253774	63210772
Neck pain	17.78	12.59	63	24413	69255	63395291
Folliculitis	17.52	12.59	3	24473	70314	63394232
Therapeutic product effect decreased	17.24	12.59	30	24446	193157	63271389
Headache	16.95	12.59	340	24136	632901	62831645
Drug interaction	16.69	12.59	40	24436	229091	63235455
Febrile neutropenia	16.35	12.59	13	24463	118436	63346110
Blood potassium decreased	16.18	12.59	44	24432	41982	63422564
Nausea	16.16	12.59	437	24039	854034	62610512
Memory impairment	15.99	12.59	81	24395	104177	63360369
Exposure during pregnancy	15.94	12.59	22	24454	155525	63309021
Bronchitis	15.74	12.59	92	24384	124843	63339703
Cardiac failure congestive	15.02	12.59	73	24403	92360	63372186
Product use issue	14.90	12.59	40	24436	220480	63244066
Muscle spasms	14.79	12.59	107	24369	156043	63308503
Chills	14.62	12.59	84	24392	113294	63351252
Therapeutic product effect incomplete	14.58	12.59	16	24460	125040	63339506
Pigmentation disorder	14.58	12.59	13	24463	4626	63459920
Gastrooesophageal reflux disease	14.45	12.59	74	24402	95565	63368981
Back pain	14.20	12.59	160	24316	263985	63200561
Floppy infant	14.19	12.59	4	24472	107	63464439
Liver injury	14.19	12.59	3	24473	60517	63404029
Inflammation	14.15	12.59	7	24469	82266	63382280
Hypomagnesaemia	14.11	12.59	33	24443	28704	63435842
Full blood count decreased	14.01	12.59	31	24445	25993	63438553
Accidental death	13.99	12.59	9	24467	1967	63462579
Vision blurred	13.80	12.59	71	24405	91853	63372693
Patient isolation	13.49	12.59	3	24473	29	63464517
Carotid artery stenosis	13.37	12.59	13	24463	5157	63459389
Impaired healing	13.24	12.59	12	24464	102530	63362016
Haemorrhagic diathesis	13.14	12.59	12	24464	4403	63460143
Thrombocytopenia	13.01	12.59	24	24452	151133	63313413
Sleep apnoea syndrome	12.75	12.59	32	24444	29101	63435445
Thinking abnormal	12.72	12.59	18	24458	10625	63453921
Malignant neoplasm progression	12.67	12.59	8	24468	82113	63382433
Retroplacental haematoma	12.65	12.59	4	24472	160	63464386

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
Narcotic bowel syndrome	79.88	16.03	15	6568	128	34950220
Completed suicide	53.05	16.03	78	6505	98090	34852258
Dizziness	52.24	16.03	122	6461	218399	34731949
Vertigo	45.44	16.03	38	6545	25498	34924850
Tachyphylaxis	37.36	16.03	8	6575	139	34950209
Hepatic ischaemia	33.42	16.03	9	6574	424	34949924
Epispadias	30.96	16.03	7	6576	158	34950190
Fall	26.39	16.03	91	6492	202794	34747554
Ventricular septal defect	21.98	16.03	12	6571	3989	34946359
Nausea	20.96	16.03	122	6461	339786	34610562
Cerebrovascular accident	20.87	16.03	48	6535	84763	34865585
Pleurothotonus	20.73	16.03	8	6575	1197	34949151
Asthenia	17.75	16.03	92	6491	245159	34705189

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
Vertigo	149.08	12.38	138	22904	68944	79652402
Dizziness	112.04	12.38	370	22672	526071	79195275
Cerebrovascular accident	70.17	12.38	145	22897	155147	79566199
Fall	68.94	12.38	301	22741	487328	79234018
Completed suicide	64.40	12.38	186	22856	245581	79475765
Narcotic bowel syndrome	63.42	12.38	15	23027	265	79721081
Drug ineffective	55.15	12.38	147	22895	1080766	78640580
Multiple sclerosis relapse	47.80	12.38	63	22979	46470	79674876
Off label use	40.64	12.38	131	22911	907084	78814262
Urticaria thermal	38.07	12.38	11	23031	434	79720912
Femoral neck fracture	36.28	12.38	27	23015	9957	79711389
Multiple sclerosis	35.92	12.38	38	23004	22244	79699102
Administration site erythema	35.47	12.38	10	23032	361	79720985
Treatment failure	35.26	12.38	4	23038	170482	79550864
Contraindicated product administered	34.40	12.38	3	23039	157535	79563811
Salivary gland calculus	33.98	12.38	9	23033	256	79721090
Transient ischaemic attack	33.51	12.38	57	22985	52638	79668708
Migraine	32.99	12.38	76	22966	87417	79633929
Chest pain	30.18	12.38	161	22881	282143	79439203
Coronary artery disease	29.37	12.38	61	22981	65413	79655933
General physical health deterioration	29.33	12.38	22	23020	275216	79446130
Asthenia	27.82	12.38	247	22795	511442	79209904
Synovitis	27.76	12.38	5	23037	150729	79570617
Tachyphylaxis	27.51	12.38	8	23034	323	79721023
Anxiety	27.43	12.38	143	22899	248369	79472977
Urinary tract infection	26.95	12.38	153	22889	274359	79446987
Depression	25.49	12.38	127	22915	216663	79504683
Product dose omission issue	24.98	12.38	139	22903	247398	79473948
Neutropenia	24.73	12.38	28	23014	287682	79433664
Gait disturbance	24.71	12.38	122	22920	207384	79513962
Pyrexia	24.46	12.38	107	22935	678602	79042744
Lower respiratory tract infection	24.43	12.38	4	23038	129216	79592130
Febrile neutropenia	23.92	12.38	19	23023	230980	79490366
Dizziness postural	22.84	12.38	22	23020	11527	79709819
Nausea	21.94	12.38	393	22649	956803	78764543
Gastrooesophageal reflux disease	21.78	12.38	73	22969	104173	79617173
Hepatic ischaemia	21.29	12.38	9	23033	1106	79720240
Full blood count decreased	21.14	12.38	32	23010	26787	79694559
Pericarditis	20.22	12.38	3	23039	104233	79617113
Infusion related reaction	19.14	12.38	23	23019	230214	79491132
Hepatic enzyme increased	18.93	12.38	15	23027	182595	79538751
Vitamin B12 deficiency	18.65	12.38	16	23026	7225	79714121
Headache	18.49	12.38	278	22764	653494	79067852
Meniere's disease	17.88	12.38	5	23037	175	79721171
Drug interaction	17.79	12.38	61	22981	415122	79306224
Neck pain	17.74	12.38	55	22987	75362	79645984
Appetite disorder	17.73	12.38	16	23026	7723	79713623
Dysphoria	17.64	12.38	13	23029	4721	79716625
Peripheral vascular disorder	17.22	12.38	16	23026	8014	79713332
Balance disorder	17.04	12.38	65	22977	98792	79622554
C-reactive protein increased	16.99	12.38	8	23034	129019	79592327
Back pain	16.57	12.38	147	22895	304033	79417313
Sialoadenitis	16.29	12.38	9	23033	1992	79719354
Drug abuse	16.08	12.38	14	23028	162677	79558669
Maternal exposure during pregnancy	15.75	12.38	10	23032	136528	79584818
Artery dissection	15.74	12.38	5	23037	273	79721073
Pigmentation disorder	15.67	12.38	13	23029	5605	79715741
Visual impairment	15.40	12.38	60	22982	92071	79629275
Ventricular hypertrophy	15.22	12.38	14	23028	6924	79714422
Thrombocytopenia	15.05	12.38	34	23008	265225	79456121
Hyperlipidaemia	14.99	12.38	27	23015	26066	79695280
Alanine aminotransferase increased	14.87	12.38	15	23027	162555	79558791
Haemorrhagic stroke	14.63	12.38	17	23025	11029	79710317
Fatigue	14.50	12.38	361	22681	929366	78791980
Cardiac failure	14.50	12.38	14	23028	154828	79566518
Emotional distress	14.27	12.38	34	23008	39935	79681411
Tremor	14.25	12.38	91	22951	169992	79551354
Glossodynia	14.24	12.38	6	23036	103331	79618015
Seizure	13.99	12.38	98	22944	188736	79532610
Illness	13.92	12.38	37	23005	46474	79674872
Cardiac failure congestive	13.71	12.38	79	22963	142323	79579023
Multiple organ dysfunction syndrome	13.60	12.38	9	23033	120237	79601109
Bronchitis	13.59	12.38	74	22968	130570	79590776
Head injury	13.57	12.38	32	23010	37337	79684009
Myalgia	13.56	12.38	96	22946	185545	79535801
Neck injury	13.55	12.38	9	23033	2772	79718574
Pancytopenia	13.31	12.38	17	23025	165728	79555618
Hypoaesthesia	13.24	12.38	93	22949	179259	79542087
Feeling abnormal	13.22	12.38	85	22957	159114	79562232
Gastritis	13.19	12.38	37	23005	47956	79673390
Scratch	13.01	12.38	14	23028	8349	79712997
Chills	12.97	12.38	85	22957	160149	79561197
Temporomandibular joint syndrome	12.95	12.38	10	23032	3895	79717451
Carotid artery stenosis	12.48	12.38	14	23028	8744	79712602

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R06AE05	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Piperazine derivatives
ATC	R06AE55	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Piperazine derivatives
FDA PE	N0000009034	Emesis Suppression
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D018680	Cholinergic Antagonists
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
FDA EPC	N0000178372	Antiemetic

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

Disease	Relation	SNOMED_ID	DOID
Motion sickness	indication	37031009	DOID:2951
Vertigo	indication	399153001
Prevention of Motion Sickness	indication
Chronic idiopathic constipation	contraindication	82934008
Bladder outflow obstruction	contraindication	236645006
Pyloric obstruction	contraindication	244815007
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Angle-closure glaucoma	contraindication	392291006	DOID:13550

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.34	Basic
pKa2	3.34	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])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST			CHEMBL	CHEMBL
Nuclear receptor subfamily 1 group I member 3	Nuclear hormone receptor	Q14994	NR1I3_HUMAN	ANTAGONIST	IC50	7.16	IUPHAR
Serine protease hepsin	Enzyme	P05981	HEPS_HUMAN		IC50	5.70	CHEMBL
Constitutive androstane receptor	Nuclear hormone receptor		NR1I3_MOUSE	AGONIST	EC50	7.60	IUPHAR

External reference:

ID	Source
4019809	VUID
N0000147898	NUI
D01317	KEGG_DRUG
31884-77-2	SECONDARY_CAS_RN
4017843	VANDF
4019809	VANDF
CHEBI:6709	CHEBI
CHEMBL1623	ChEMBL_ID
CHEMBL3989555	ChEMBL_ID
CHEMBL1200590	ChEMBL_ID
2757	IUPHAR_LIGAND_ID
DB00737	DRUGBANK_ID
6676	RXNORM
1696	MMSL
5029	MMSL
d00859	MMSL
003400	NDDF
004798	NDDF
372879002	SNOMEDCT_US
387243002	SNOMEDCT_US
84951002	SNOMEDCT_US
C0025039	UMLSCUI
D008468	MESH_DESCRIPTOR_UI
204	INN_ID
4034	PUBCHEM_CID
3L5TQ84570	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Wal Dram	HUMAN OTC DRUG LABEL	1	0363-0403	TABLET	25 mg	ORAL	OTC monograph final	15 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	0363-0404	TABLET, CHEWABLE	25 mg	ORAL	OTC MONOGRAPH FINAL	15 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	0363-0404	TABLET, CHEWABLE	25 mg	ORAL	OTC MONOGRAPH FINAL	15 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	0363-0404	TABLET, CHEWABLE	25 mg	ORAL	OTC MONOGRAPH FINAL	15 sections
Wal-Dram 2 Quick-Dissolving	HUMAN OTC DRUG LABEL	1	0363-1407	TABLET, ORALLY DISINTEGRATING	25 mg	ORAL	OTC monograph final	14 sections
Wal-Dram 2 Quick-Dissolving	HUMAN OTC DRUG LABEL	1	0363-1407	TABLET, ORALLY DISINTEGRATING	25 mg	ORAL	OTC monograph final	14 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	0363-4030	TABLET	25 mg	ORAL	OTC monograph final	15 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	0363-4030	TABLET	25 mg	ORAL	OTC monograph final	15 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	0363-4030	TABLET	25 mg	ORAL	OTC monograph final	15 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0440-1736	TABLET	25 mg	ORAL	ANDA	10 sections
Rugby Travel SicknessMeclizine HCl, 25 mg Each (Antiemetic)	HUMAN OTC DRUG LABEL	1	0536-1018	TABLET, CHEWABLE	25 mg	ORAL	OTC monograph final	17 sections
Rugby Meclizine HCl	HUMAN OTC DRUG LABEL	1	0536-1178	TABLET, FILM COATED	12.50 mg	ORAL	OTC monograph final	17 sections
MECLIZINE	HUMAN OTC DRUG LABEL	1	0536-1297	TABLET	12.50 mg	ORAL	OTC monograph final	12 sections
MECLIZINE	HUMAN OTC DRUG LABEL	1	0536-1297	TABLET	12.50 mg	ORAL	OTC monograph final	12 sections
Meclizine Hydrochloride	HUMAN OTC DRUG LABEL	1	0536-1299	TABLET, CHEWABLE	25 mg	ORAL	OTC monograph final	17 sections
Meclizine Hydrochloride	HUMAN OTC DRUG LABEL	1	0536-1299	TABLET, CHEWABLE	25 mg	ORAL	OTC monograph final	17 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8224	TABLET	25 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8224	TABLET	25 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8303	TABLET	12.50 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8303	TABLET	12.50 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8462	TABLET	25 mg	ORAL	ANDA	23 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6516	TABLET	12.50 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6517	TABLET	25 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7375	TABLET	12.50 mg	ORAL	ANDA	23 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7376	TABLET	25 mg	ORAL	ANDA	23 sections
PhysiciansCare Motion Sickness	HUMAN OTC DRUG LABEL	1	0924-1008	TABLET	25 mg	ORAL	OTC monograph final	15 sections
MECLIZINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	10544-081	TABLET	25 mg	ORAL	ANDA	10 sections
Meclizine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10544-108	TABLET	25 mg	ORAL	ANDA	11 sections
Meclizine HCl	HUMAN OTC DRUG LABEL	1	10544-249	TABLET	12.50 mg	ORAL	OTC monograph final	9 sections
Motion Sickness Relief	HUMAN OTC DRUG LABEL	1	11822-0404	TABLET, CHEWABLE	25 mg	ORAL	OTC monograph final	15 sections