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

Stem definitionDrug idCAS RN
diphenylmethyl piperazine derivatives 1649 569-65-3

Description:

MoleculeDescription

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:

DoseUnitRoute
50 mg O
50 mg R

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Feb. 14, 1957 FDA CITRON PHARMA LLC

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
Vertigo 158.11 12.09 150 21703 51682 50531589
Dizziness 105.02 12.09 358 21495 346011 50237260
Drug ineffective 63.01 12.09 166 21687 819167 49764104
Fall 52.04 12.09 283 21570 334649 50248622
Cerebrovascular accident 50.23 12.09 120 21733 94560 50488711
Multiple sclerosis relapse 45.62 12.09 73 21780 42891 50540380
Salivary gland calculus 39.76 12.09 10 21843 151 50583120
Transient ischaemic attack 37.35 12.09 57 21796 32153 50551118
Synovitis 36.69 12.09 5 21848 123860 50459411
Maternal exposure during pregnancy 36.08 12.09 12 21841 159766 50423505
Chest pain 34.11 12.09 159 21694 176723 50406548
Systemic lupus erythematosus 32.75 12.09 10 21843 140612 50442659
Femoral neck fracture 31.44 12.09 26 21827 7464 50575807
Asthenia 30.66 12.09 239 21614 318803 50264468
Infusion related reaction 28.66 12.09 19 21834 169538 50413733
Multiple sclerosis 27.72 12.09 39 21814 20454 50562817
Gait disturbance 27.56 12.09 133 21720 149872 50433399
Coronary artery disease 26.86 12.09 47 21806 29679 50553592
Lower respiratory tract infection 25.61 12.09 5 21848 95196 50488075
Glossodynia 25.53 12.09 9 21844 115560 50467711
Urinary tract infection 24.43 12.09 173 21680 223847 50359424
Anxiety 24.15 12.09 145 21708 177461 50405810
Infantile apnoea 23.16 12.09 10 21843 863 50582408
Dysphoria 23.07 12.09 18 21835 4756 50578515
Somnolence neonatal 22.66 12.09 6 21847 112 50583159
Sialoadenitis 21.52 12.09 11 21842 1389 50581882
Hepatic enzyme increased 21.12 12.09 17 21836 137363 50445908
Migraine 21.09 12.09 76 21777 75204 50508067
Neutropenia 20.71 12.09 20 21833 147945 50435326
Depression 20.57 12.09 132 21721 165291 50417980
Visual impairment 20.05 12.09 70 21783 68205 50515066
Hypoaesthesia 19.99 12.09 108 21745 127149 50456122
Neck pain 19.88 12.09 62 21791 57005 50526266
Off label use 19.79 12.09 122 21731 474304 50108967
Appetite disorder 19.20 12.09 18 21835 6096 50577175
Balance disorder 18.71 12.09 70 21783 70520 50512751
Pyrexia 18.44 12.09 93 21760 380110 50203161
Arthropathy 18.15 12.09 25 21828 157881 50425390
Drug interaction 17.96 12.09 37 21816 199584 50383687
Completed suicide 17.48 12.09 107 21746 131782 50451489
Ventricular hypertrophy 17.47 12.09 13 21840 3202 50580069
Therapeutic product effect decreased 17.23 12.09 20 21833 136030 50447241
Drug intolerance 16.99 12.09 44 21809 219060 50364211
Feeling abnormal 16.75 12.09 102 21751 125390 50457881
General physical health deterioration 15.92 12.09 23 21830 142411 50440860
Joint swelling 15.60 12.09 54 21799 245232 50338039
Muscle spasms 15.48 12.09 100 21753 125453 50457818
Febrile neutropenia 15.11 12.09 12 21841 97655 50485616
Memory impairment 15.02 12.09 71 21782 79289 50503982
C-reactive protein increased 14.98 12.09 5 21848 66469 50516802
Floppy infant 14.58 12.09 4 21849 86 50583185
Product dose omission issue 14.57 12.09 132 21721 183706 50399565
Hypomagnesaemia 14.09 12.09 31 21822 23125 50560146
Accidental death 14.08 12.09 9 21844 1735 50581536
Rheumatoid arthritis 13.98 12.09 43 21810 202507 50380764
Malignant neoplasm progression 13.89 12.09 6 21847 68118 50515153
Blood potassium decreased 13.67 12.09 41 21812 36904 50546367
Cardiac failure congestive 13.50 12.09 72 21781 84310 50498961
Tremor 13.25 12.09 90 21763 114813 50468458
Patient isolation 13.16 12.09 3 21850 29 50583242
Haemorrhagic diathesis 13.12 12.09 12 21841 3936 50579335
Carotid artery stenosis 13.10 12.09 13 21840 4718 50578553
Exposure during pregnancy 13.07 12.09 20 21833 120995 50462276
Gastrooesophageal reflux disease 12.77 12.09 66 21787 76362 50506909
Photophobia 12.75 12.09 23 21830 14864 50568407
Discomfort 12.61 12.09 17 21836 108363 50474908
Full blood count decreased 12.57 12.09 29 21824 22317 50560954
Vision blurred 12.51 12.09 67 21786 78580 50504691
Retroplacental haematoma 12.48 12.09 4 21849 149 50583122
Nausea 12.44 12.09 395 21458 705003 49878268
Sneezing 12.42 12.09 22 21831 14022 50569249
Stress cardiomyopathy 12.16 12.09 16 21837 7871 50575400
Tinnitus 12.14 12.09 33 21820 28099 50555172

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
Narcotic bowel syndrome 78.53 16.19 15 6167 126 29568219
Completed suicide 50.44 16.19 77 6105 90169 29478176
Dizziness 47.57 16.19 115 6067 189569 29378776
Vertigo 42.96 16.19 36 6146 21825 29546520
Tachyphylaxis 39.77 16.19 8 6174 90 29568255
Hepatic ischaemia 33.49 16.19 9 6173 378 29567967
Epispadias 30.23 16.19 7 6175 158 29568187
Fall 25.41 16.19 88 6094 177090 29391255
Pleurothotonus 21.08 16.19 8 6174 1030 29567315
Nausea 19.64 16.19 115 6067 289140 29279205
Cerebrovascular accident 19.58 16.19 47 6135 76864 29491481
Hyperreflexia 16.27 16.19 9 6173 2763 29565582

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
Vertigo 136.94 12.96 129 20720 58882 64419001
Dizziness 109.51 12.96 346 20503 429817 64048066
Cerebrovascular accident 66.39 12.96 141 20708 137442 64340441
Narcotic bowel syndrome 63.21 12.96 15 20834 239 64477644
Fall 60.06 12.96 280 20569 416546 64061337
Completed suicide 57.32 12.96 181 20668 224233 64253650
Drug ineffective 50.12 12.96 125 20724 840122 63637761
Multiple sclerosis relapse 39.31 12.96 57 20792 41078 64436805
Femoral neck fracture 36.83 12.96 27 20822 8697 64469186
Transient ischaemic attack 33.48 12.96 55 20794 44127 64433756
Salivary gland calculus 33.43 12.96 9 20840 243 64477640
Chest pain 32.04 12.96 156 20693 235824 64242059
Multiple sclerosis 30.43 12.96 34 20815 18907 64458976
Asthenia 28.07 12.96 235 20614 427809 64050074
Off label use 27.80 12.96 108 20741 632698 63845185
Tachyphylaxis 27.75 12.96 8 20841 279 64477604
Coronary artery disease 25.79 12.96 59 20790 60374 64417509
Neutropenia 25.41 12.96 24 20825 239600 64238283
Contraindicated product administered 24.52 12.96 3 20846 107826 64370057
Gait disturbance 24.21 12.96 115 20734 172040 64305843
Pyrexia 24.10 12.96 96 20753 558548 63919335
Anxiety 24.02 12.96 129 20720 202520 64275363
Urinary tract infection 22.60 12.96 140 20709 231456 64246427
Migraine 21.23 12.96 56 20793 62621 64415262
Hepatic ischaemia 21.08 12.96 9 20840 1013 64476870
General physical health deterioration 21.06 12.96 21 20828 204404 64273479
Neck pain 20.86 12.96 55 20794 61478 64416405
Febrile neutropenia 20.84 12.96 18 20831 187639 64290244
Lower respiratory tract infection 20.64 12.96 3 20846 94611 64383272
Nausea 20.54 12.96 362 20487 785438 63692445
Depression 19.28 12.96 113 20736 183178 64294705
Product dose omission issue 19.17 12.96 118 20731 194629 64283254
Appetite disorder 18.67 12.96 16 20833 6445 64471438
Gastrooesophageal reflux disease 18.44 12.96 64 20785 83079 64394804
Drug interaction 18.41 12.96 58 20791 362025 64115858
Full blood count decreased 18.32 12.96 29 20820 22553 64455330
Synovitis 17.76 12.96 5 20844 99085 64378798
Meniere's disease 17.58 12.96 5 20844 166 64477717
Dysphoria 17.22 12.96 13 20836 4375 64473508
Peripheral vascular disorder 17.06 12.96 16 20833 7245 64470638
Sialoadenitis 17.06 12.96 9 20840 1624 64476259
Artery dissection 16.57 12.96 5 20844 205 64477678
Cardiac failure 15.56 12.96 12 20837 132361 64345522
Headache 15.27 12.96 248 20601 529219 63948664
Alanine aminotransferase increased 14.64 12.96 14 20835 139017 64338866
Ventricular hypertrophy 14.63 12.96 14 20835 6502 64471381
Haemorrhagic stroke 14.52 12.96 17 20832 9934 64467949
Neck injury 14.12 12.96 9 20840 2309 64475574
Hyperlipidaemia 14.01 12.96 26 20823 22950 64454933
Maternal exposure during pregnancy 13.59 12.96 7 20842 95877 64382006
Hypoaesthesia 13.50 12.96 84 20765 139024 64338859
Thrombocytopenia 13.48 12.96 33 20816 223768 64254115
Osteoarthritis 13.39 12.96 48 20801 63288 64414595
Gastritis 13.34 12.96 37 20812 42581 64435302
Balance disorder 13.22 12.96 58 20791 83868 64394015
Drug abuse 13.17 12.96 14 20835 132360 64345523
Back pain 13.12 12.96 131 20718 250040 64227843
Emotional distress 13.02 12.96 33 20816 36005 64441878

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST CHEMBL CHEMBL
Nuclear receptor subfamily 1 group I member 3 Nuclear hormone receptor ANTAGONIST IC50 7.16 IUPHAR
Serine protease hepsin Enzyme IC50 5.70 CHEMBL
Constitutive androstane receptor Nuclear hormone receptor AGONIST EC50 7.60 IUPHAR

External reference:

IDSource
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
3L5TQ84570 UNII
4034 PUBCHEM_CID
6676 RXNORM
1696 MMSL
5029 MMSL
d00859 MMSL
003400 NDDF
004798 NDDF
372879002 SNOMEDCT_US
387243002 SNOMEDCT_US
84951002 SNOMEDCT_US
D008468 MESH_DESCRIPTOR_UI
C0025039 UMLSCUI
204 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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
Wal-Dram 2 Quick-Dissolving HUMAN OTC DRUG LABEL 1 0363-1407 TABLET, ORALLY DISINTEGRATING 25 mg ORAL OTC monograph final 13 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 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 0615-8303 TABLET 12.50 mg ORAL ANDA 10 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
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
Less Drowsy Motion Sickness Relief HUMAN OTC DRUG LABEL 1 11822-0775 TABLET 25 mg ORAL OTC monograph final 15 sections
Less Drowsy Motion Sickness Relief HUMAN OTC DRUG LABEL 1 11822-0775 TABLET 25 mg ORAL OTC monograph final 15 sections
Rugby Travel SicknessMeclizine HCl, 25 mg Each (ANTIEMETIC) HUMAN OTC DRUG LABEL 1 12634-246 TABLET, CHEWABLE 25 mg ORAL OTC monograph final 15 sections
Meclizine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 12634-424 TABLET 25 mg ORAL ANDA 11 sections
Meclizine HCl HUMAN OTC DRUG LABEL 1 13811-646 TABLET 12.50 mg ORAL OTC monograph final 13 sections
Meclizine HCl HUMAN OTC DRUG LABEL 1 13811-647 TABLET 25 mg ORAL OTC monograph final 13 sections
Meclizine HCl HUMAN OTC DRUG LABEL 1 13811-648 TABLET, CHEWABLE 25 mg ORAL OTC monograph final 13 sections
Jet-Avert Motion Sickness Aid HUMAN OTC DRUG LABEL 1 15579-837 TABLET 25 mg ORAL OTC monograph final 15 sections
MECLIZINE HUMAN OTC DRUG LABEL 1 16103-386 TABLET 12.50 mg ORAL OTC monograph final 12 sections
MECLIZINE HUMAN OTC DRUG LABEL 1 16103-387 TABLET, CHEWABLE 25 mg ORAL OTC monograph final 12 sections
MECLIZINE HUMAN OTC DRUG LABEL 1 16103-387 TABLET, CHEWABLE 25 mg ORAL OTC monograph final 12 sections