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
S (Water solubility) 0.26 mg/mL Bocci G, Oprea TI, 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 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 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 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 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 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:

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 | Suggest Off label Use Form| |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
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:

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
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