Page last updated: 2024-12-05

meclizine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Meclizine is an antihistamine that is used to prevent and treat motion sickness. It works by blocking the action of histamine in the inner ear, which is responsible for balance. Meclizine is available over-the-counter and by prescription. It is typically taken 30 to 60 minutes before travel. Meclizine can cause drowsiness, so it is important to avoid driving or operating machinery after taking it. Other potential side effects include dry mouth, blurred vision, and constipation. Meclizine is generally safe for most people, but it can interact with other medications. It is important to talk to your doctor before taking meclizine if you are pregnant, breastfeeding, or have any medical conditions. '

Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4034
CHEMBL ID1623
CHEBI ID6709
SCHEMBL ID4649
MeSH IDM0013180

Synonyms (144)

Synonym
BRD-A50311610-300-05-4
gtpl2757
histametizine
piperazine, 1-[(4-chlorophenyl)phenylmethyl]-4-[(3-methylphenyl)methyl]-
vomisseis
piperazine, 1-(p-chloro-.alpha.-phenylbenzyl)-4-(m-methylbenzyl)-
1-(p-chlorobenzhydryl)-4-(m-methylbenzyl)diethylenediamine
sabari
navicalm
bonadettes
neo-suprimel
ancolan
histamethizine
ravelon
u. c. b. 5062
suprimal
wln: t6n dntj ayr&r dg& d1r c1
ucb 5052
peremesin
travelon
nsc-169189
neo-istafene
bonine
ancolon
1-(p-chlorobenzhydryl)-4-(m-methylbenzyl)piperazine
diadril
histamethine
sea-legs
ucb 170
itinerol
neo-suprimal
histametizyne
1-(p-chloro-.alpha.-phenylbenzyl)-4-(m-methylbenzyl)piperazine
calmonal
monamine
chiclida
subari
u.c.b. 5062
vomissels
siguran
ucb 5062
parachloramine
postafene
DIVK1C_000407
KBIO1_000407
1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
SPECTRUM_000891
BPBIO1_000588
PRESTWICK2_000457
PRESTWICK3_000457
SPECTRUM5_000919
BSPBIO_000534
BSPBIO_001949
1-((4-chlorophenyl)phenylmethyl)-4-((3-methylphenyl)methyl)piperazine
hsdb 3113
brn 0332002
(+-)-meclizine
piperazine, 1-((4-chlorophenyl)phenylmethyl)-4-((3-methylphenyl)methyl)-
1-p-chlorobenzhydryl-4-m-methylbenzylpiperazine
1-(p-chloro-alpha-phenylbenzyl)-4-(m-methylbenzyl)piperazine
meclizine [inn:ban]
einecs 209-323-3
meclozina [inn-spanish]
meclozinum [inn-latin]
piperazine, 1-(p-chloro-alpha-phenylbenzyl)-4-(m-methylbenzyl)-
nsc 169189
AB00053493
569-65-3
meclizine
C07116
meclozine
DB00737
antivert
KBIOGR_000473
KBIOSS_001371
KBIO2_003939
KBIO2_001371
KBIO3_001449
KBIO2_006507
NINDS_000407
PRESTWICK1_000457
SPBIO_000100
PRESTWICK0_000457
SPECTRUM4_000037
SPECTRUM2_000110
SPECTRUM3_000485
SPBIO_002473
IDI1_000407
L001136
nevidoxine (tn)
meclozine (ban)
D08163
CHEMBL1623
chebi:6709 ,
FT-0659103
1-[(4-chlorophenyl)-phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine
cas_569-65-3
bdbm81467
nsc_4034
NCGC00018296-02
NCGC00018296-04
EN300-58334
AKOS015951354
3l5tq84570 ,
meclozina
unii-3l5tq84570
meclozinum
meclozine [inn]
dramamine ii
NCGC00018296-08
meclizine [hsdb]
meclozine [who-dd]
meclizine [mi]
meclizine [vandf]
SCHEMBL4649
bonadoxin (salt/mix)
OCJYIGYOJCODJL-UHFFFAOYSA-N
(.+/-.)-meclizine
diadril (salt/mix)
bonamine (salt/mix)
vertizine (salt/mix)
1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine #
1-((4-chlorophenyl)(phenyl)methyl)-4-(3-methylbenzyl)piperazine
AB00053493_15
AB00053493_14
DTXSID0023242 ,
1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine
Z53003552
meclozin
SBI-0051433.P003
nevidoxine
Q386441
4-methyl-2-chloroacetophenone
BS-17628
BCP28339
meclizine;meclozine; parachloramine
BRD-A50311610-300-06-2
piperazine,1-[(4-chlorophenyl)phenylmethyl]-4-[(3-methylphenyl)methyl]-
mfcd00242697
D81963
dtxcid703242
meclozina (inn-spanish)
piperazine, 1-((4-chlorophenyl)phenylmethyl)-4-((3-methyphenyl)methyl)-
meclozinum (inn-latin)

Research Excerpts

Overview

Meclizine (MCLZ) is a histamine antagonist with potential neuroprotective qualities. It has been widely used for prophylactic treatment of motion sickness.

ExcerptReferenceRelevance
"Meclizine (MCLZ) is a histamine antagonist with potential neuroprotective qualities."( Meclizine moderates lipopolysaccharide-induced neuroinflammation in mice through the regulation of AKT/ NF-κβ/ERK/JNK signaling pathway.
Asaad, GF; Mostafa, RE, 2023
)
3.07
"Meclizine is an agonist of human pregnane X receptor (PXR). "( Meclizine, a pregnane X receptor agonist, is a direct inhibitor and mechanism-based inactivator of human cytochrome P450 3A.
Chan, EC; Foo, WY; Lau, AJ; Tay, HY, 2015
)
3.3
"Meclizine is a well-tolerated drug routinely used as an anti-histamine agent in the management of disequilibrium. "( Meclizine-induced enhanced glycolysis is neuroprotective in Parkinson disease cell models.
Chau, KY; Hong, CT; Schapira, AH, 2016
)
3.32
"Meclizine is an antihistamine drug recently implicated in neuroprotection via modulation of energy metabolism."( Cisplatin Toxicity in Dorsal Root Ganglion Neurons Is Relieved by Meclizine via Diminution of Mitochondrial Compromise and Improved Clearance of DNA Damage.
Englander, EW; Gorgun, MF; Zhuo, M, 2017
)
1.41
"Meclizine is an antihistamine and has been widely used for prophylactic treatment of motion sickness. "( Quantification of meclizine in human plasma by high performance liquid chromatography-mass spectrometry.
Chow, MS; Qian, S; Wang, Z; Zhang, Q, 2011
)
2.15

Effects

Meclizine has safely been used for more than 50 years, but it lacks the safety data for repeated administration and pharmacokinetics (PK) when administered to children. Meclizined is an inverse agonist and antagonist of human constitutive androstane receptor (hCAR)

ExcerptReferenceRelevance
"Meclizine has safely been used for more than 50 years, but it lacks the safety data for repeated administration and pharmacokinetics (PK) when administered to children."( Pharmacokinetics and safety after once and twice a day doses of meclizine hydrochloride administered to children with achondroplasia.
Ishiguro, N; Kamiya, Y; Kitoh, H; Kuwatsuka, Y; Matsushita, M; Mishima, K; Morikawa, H; Nagata, T; Nakai, Y; Ueda, K, 2020
)
1.52
"Meclizine has also been reported to be an inverse agonist and antagonist of human constitutive androstane receptor (hCAR)."( Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor.
Baucom, CC; Chang, TK; Lau, AJ; Rajaraman, G; Yang, G, 2011
)
1.4

Actions

ExcerptReferenceRelevance
"The meclizine group had lower VNRS scores in the PACU at 15 (P = .013) and 45 (P = .006) minutes following rescue treatment."( Meclizine in combination with ondansetron for prevention of postoperative nausea and vomiting in a high-risk population.
Benfield, DA; Forrester, CM; Kelly, JA; Matern, CE; Pellegrini, JE, 2007
)
2.26

Treatment

ExcerptReferenceRelevance
"Pretreatment with meclizine or terfenadine (15-30 mg/kg i.p.) inhibited antigen-induced haemoconcentration, whereas WEB 2086 (2-10 mg/kg i.p.) and PCA 4248 (5-10 mg/kg p.o.), two platelet-activating factor (PAF) antagonists, interfered with thrombocytopenia only."( Interference of azelastine with anaphylaxis induced by ovalbumin challenge in actively sensitized rats.
Bozza, PT; Castro-Faria-Neto, HC; Cordeiro, RS; Lima, MC; Martins, MA; Silva, AR; Silva, PM; Vargaftig, BB, 1992
)
0.61

Toxicity

Meclizine was well tolerated in ACH children with no serious adverse events. The aim of this study was to formulate an easily-administered, safe and effective dosage form.

ExcerptReferenceRelevance
" Pyridoxine is considered safe for use during pregnancy, but its efficacy in treating nausea and vomiting has not been determined."( Safety and efficacy of antiemetics used to treat nausea and vomiting in pregnancy.
Leathem, AM, 1986
)
0.27
" The present study was undertaken to evaluate the reproductive toxic effect of meclizine and caffeine combination."( Prenatal and developmental toxicity study of meclizine and caffeine combination in female albino Wistar rats.
Alvin, JM; Sandeep, M, 2014
)
0.89
" Meclizine was well tolerated in ACH children with no serious adverse events."( Pharmacokinetics and safety after once and twice a day doses of meclizine hydrochloride administered to children with achondroplasia.
Ishiguro, N; Kamiya, Y; Kitoh, H; Kuwatsuka, Y; Matsushita, M; Mishima, K; Morikawa, H; Nagata, T; Nakai, Y; Ueda, K, 2020
)
1.71
"The aim of this study was to formulate an easily-administered, safe and effective dosage form loaded with meclizine for treatment of chemotherapy-induced nausea and vomiting (CINV) through the buccal route."( Nanotechnology based blended chitosan-pectin hybrid for safe and efficient consolidative antiemetic and neuro-protective effect of meclizine hydrochloride in chemotherapy induced emesis.
Elmotasem, H; Salama, AAA; Salama, AH, 2020
)
0.98

Pharmacokinetics

The study was performed in 20 healthy volunteers. Application of the method to determine pharmacokinetic parameters of meclizine hydrochloride enantiomers was performed using Phoenix WinNonlin 8.

ExcerptReferenceRelevance
" To investigate the pharmacokinetics of the new MOS formulation versus the marketed meclizine oral tablet (MOT), a phase 1 pharmacokinetic study was performed in 20 healthy volunteers."( Meclizine metabolism and pharmacokinetics: formulation on its absorption.
Chow, MS; Lee, B; Pearce, D; Qian, S; Wang, Y; Wang, Z; Zhang, Q, 2012
)
2.05

Compound-Compound Interactions

ExcerptReferenceRelevance
" Meclizine, a long-acting drug with a low side-effect profile, may be ideal in combination with ondansetron for at-risk patients."( Meclizine in combination with ondansetron for prevention of postoperative nausea and vomiting in a high-risk population.
Benfield, DA; Forrester, CM; Kelly, JA; Matern, CE; Pellegrini, JE, 2007
)
2.69

Bioavailability

The freeze-dried ternary formulations of meclizine (MZ), prednisolone (PRED, an anti-inflammatory drug) and norfloxacin (NFLX) were prepared using egg albumin and olive oil.

ExcerptReferenceRelevance
"A method, based on ion-pair extraction, is described for the quantification of meclizine hydrochloride in various pharmaceutical dosage forms, for content uniformity determination, and for concentration monitoring in dissolution and bioavailability studies."( Determination of meclizine hydrochloride by ion-pair extraction with methyl orange.
Ebert, WR; Hom, FS, 1977
)
0.82
" This result suggests that the self-emulsifying soft capsule is useful for the increase of the bioavailability of the drug."( [Dissolution and absorption behavior of meclizine dihydrochloride from soft gelatin capsules].
Iijima, T; Imai, T; Imamura, Y; Kimura, S; Otagiri, M; Ueno, M, 1989
)
0.54
"The freeze-dried ternary formulations of meclizine (MZ, an anti-motion sickness drug), prednisolone (PRED, an anti-inflammatory drug) and norfloxacin (NFLX, an anti-microbial drug) which are poorly water-soluble and are low bioavailability drugs, were prepared using egg albumin and olive oil."( Pharmaceutical properties of freeze-dried formulations of egg albumin, several drugs and olive oil.
Kakegawa, H; Matsumoto, H; Miyataka, H; Nishiki, M; Satoh, T; Tsuji, Y, 1996
)
0.56
" The geometric mean ratios (90% confidence interval) of AUC(0-24) and AUC(0-∞) indicated no significant difference in bioavailability between the 2 formulations."( Meclizine metabolism and pharmacokinetics: formulation on its absorption.
Chow, MS; Lee, B; Pearce, D; Qian, S; Wang, Y; Wang, Z; Zhang, Q, 2012
)
1.82
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The aim of this study was to formulate an easily-administered, safe and effective dosage form loaded with me Cl.

ExcerptRelevanceReference
"A method, based on ion-pair extraction, is described for the quantification of meclizine hydrochloride in various pharmaceutical dosage forms, for content uniformity determination, and for concentration monitoring in dissolution and bioavailability studies."( Determination of meclizine hydrochloride by ion-pair extraction with methyl orange.
Ebert, WR; Hom, FS, 1977
)
0.82
" Results of a DNA ladder assay revealed that DNA ladders appeared with MEC treatment in COLO 205 cells at dosage of >50 microM."( Induction of apoptosis and cell-cycle arrest in human colon cancer cells by meclizine.
Ho, YS; Lee, JJ; Lin, JC; Liu, CL; Wu, CH; Yang, TL, 2007
)
0.57
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
"A specific stability-indicating reversed-phase high-performance liquid chromatographic method was developed and validated for the estimation of meclizine hydrochloride (MEC) in tablet dosage form."( A stability-indicating RP-HPLC method for the quantitative analysis of meclizine hydrochloride in tablet dosage form.
Kondreddy, VK; Manikala, M; Peraman, R; Yiragamreddy, PR,
)
0.57
"Antiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms."( Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent-Meclizine HCl.
Ahmad, M; Ahmed, K; Nasiri, MI; Qazi, F; Shoaib, MH; Yousuf, RI, 2017
)
1.01
"The aim of this study was to formulate an easily-administered, safe and effective dosage form loaded with meclizine for treatment of chemotherapy-induced nausea and vomiting (CINV) through the buccal route."( Nanotechnology based blended chitosan-pectin hybrid for safe and efficient consolidative antiemetic and neuro-protective effect of meclizine hydrochloride in chemotherapy induced emesis.
Elmotasem, H; Salama, AAA; Salama, AH, 2020
)
0.98
" Achieving concomitant rapid and prolonged drug therapeutic effects in orodissolvable/dispersible dosage forms would be challenging."( A new dual function orodissolvable/dispersible meclizine HCL tablet to challenge patient inconvenience: in vitro evaluation and in vivo assessment in human volunteers.
Darwesh, AY; El-Dahhan, MS; Meshali, MM, 2021
)
0.88
"Novel optimizations of the widely used chemometric models; application of a comparative study between the suggested methods; application of OPLS preprocessing methods; quantitative determination of pyridoxine HCl, cyclizine HCl and meclizine HCl; checking the predictive power of developed chemometric models; analysis of active ingredients in their pharmaceutical dosage forms."( Adoption of Advanced Chemometric Methods for Determination of Pyridoxine HCl, Cyclizine HCl, and Meclizine HCl in the Presence of Related Impurities: A Comparative Study.
Abdallah, FF; Draz, ME; Lashien, AS; Naguib, IA; Saad, AS; Zaazaa, HE, 2022
)
1.12
" These models were applied to quantify the three active constituents in their raw materials and their corresponding dosage forms using their UV spectra."( Comparative Study of Augmented Classical Least Squares Models for UV Assay of Co-Formulated Antiemetics Together with Related Impurities.
Al-Saleem, MSM; Darwish, HW; Draz, ME; Naguib, IA, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Meclizine H1-Antihistamine Action87

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
EWS/FLI fusion proteinHomo sapiens (human)Potency18.99990.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID625278FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of no concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID540237Phospholipidosis-positive literature compound observed in rat
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID643383Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346793Mouse Constitutive androstane receptor (1I. Vitamin D receptor-like receptors)2004Molecular endocrinology (Baltimore, Md.), Oct, Volume: 18, Issue:10
Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR.
AID1346746Human Constitutive androstane receptor (1I. Vitamin D receptor-like receptors)2004Molecular endocrinology (Baltimore, Md.), Oct, Volume: 18, Issue:10
Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (278)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990158 (56.83)18.7374
1990's22 (7.91)18.2507
2000's23 (8.27)29.6817
2010's50 (17.99)24.3611
2020's25 (8.99)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 80.01

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index80.01 (24.57)
Research Supply Index5.77 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index212.93 (26.88)
Search Engine Supply Index3.01 (0.95)

This Compound (80.01)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials32 (11.15%)5.53%
Reviews15 (5.23%)6.00%
Case Studies14 (4.88%)4.05%
Observational0 (0.00%)0.25%
Other226 (78.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (10)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Optimizing the Combination of Intranasal Scopolamine and Sensory Augmentation to Mitigate G-transition Induced Motion Sickness and Enhance Sensorimotor Performance. Motion Sickness Countermeasures Field Test [NCT05852730]Phase 280 participants (Anticipated)Interventional2021-08-10Recruiting
A Pilot Study of the Effects of Meclizine on Pre-Pulse Inhibition [NCT01537471]Phase 1117 participants (Actual)Interventional2012-01-31Completed
A Randomized Trial to Evaluate Resolution of Symptoms Using Vestibular Rehab Versus Conventional Therapy in Patients Presenting to the Emergency Department (ED) With Diagnosis of Benign Paroxysmal Positional Vertigo (BPPV) [NCT00641797]26 participants (Actual)Interventional2006-11-30Completed
A New Dual Function Oro-Dissolvable/Dispersible Meclizine HCL Tablet to Challenge Patient Inconvenience: In-Vitro Evaluation and In-Vivo Assessment in Human Volunteers [NCT04564144]Phase 1/Phase 26 participants (Anticipated)Interventional2020-06-01Recruiting
A Window of Opportunity Trial With Meclizine in Hepatocellular Carcinoma [NCT03253289]Phase 113 participants (Actual)Interventional2017-10-13Active, not recruiting
" National, Phase III, Radomized, Double-Blind, Double -Dummy, Controlled, Parallel to Evaluate Non Inferiority of Meclin® (Meclizine Chlorhydrate) Versus Dramin® (Dimenhydrinate) Soft Gel Capsules in the Control of Acute Vertigo Symphtoms From Peripheral [NCT02112578]Phase 3292 participants (Actual)Interventional2016-11-01Completed
Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis [NCT02625181]27,034 participants (Actual)Interventional2016-07-31Completed
Motion Sickness Medications and Vestibular Time Constant [NCT03270839]Phase 480 participants (Anticipated)Interventional2017-06-01Recruiting
Meclizine Plasma Levels in Responders and Non-responders [NCT04482985]Phase 450 participants (Anticipated)Interventional2020-09-01Not yet recruiting
Meclizine as a Potential Smoking Cessation Treatment [NCT01443858]Phase 2146 participants (Actual)Interventional2011-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00641797 (1) [back to overview]Likert Scale for Satisfaction
NCT01443858 (5) [back to overview]Number of Participants Completing the Continuous 4 Week Abstinence From Smoking
NCT01443858 (5) [back to overview]Percentage of Change in Expired Air Carbon Monoxide (CO) at End of Week 1
NCT01443858 (5) [back to overview]Percentage of Change in Expired Air Carbon Monoxide (CO) at End of Week 3
NCT01443858 (5) [back to overview]Percentage of Change of CO at End of Week 1 When Comparing Abstinent Smokers Versus Non-abstinent Smokers
NCT01443858 (5) [back to overview]Percentage of Change of CO at End of Week 3 When Comparing Abstinent Smokers Versus Non-abstinent Smokers
NCT02625181 (4) [back to overview]Adherence to PONV Guidelines
NCT02625181 (4) [back to overview]PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting
NCT02625181 (4) [back to overview]The Number of Prophylactic Interventions for PONV
NCT02625181 (4) [back to overview]Time to Discharge From the Postanesthesia Care Unit (PACU)

Likert Scale for Satisfaction

The Likert Scale measured patient satisfaction on a 0-10 score range (0 = Least Satisfied; 10 = Most Satisfied). (NCT00641797)
Timeframe: 0 days

Interventionunits on a scale (Mean)
Arm 1, Conventional Therapy9
Arm 2, Epley Maneuver9

[back to top]

Number of Participants Completing the Continuous 4 Week Abstinence From Smoking

Continuous 4 week abstinence from smoking (weeks 3-6 post quit date), based on self-reported abstinence confirmed by expired air CO ≤8ppm, will be compared between each meclizine group and placebo, using logistic regression analyses (NCT01443858)
Timeframe: weeks 3-6 post quit date

Interventionparticipants (Number)
Control2
25mg Meclizine7
50mg Meclizine2

[back to top]

Percentage of Change in Expired Air Carbon Monoxide (CO) at End of Week 1

To evaluate the effects of meclizine alone on ad lib smoking, the percent decrease in expired air carbon monoxide (CO) at the end of week 1 (relative to baseline) will be compared (using ANOVA) between each meclizine group and placebo. (NCT01443858)
Timeframe: After 1 week of treatment (relative to baseline)

Interventionpercentage change (Mean)
Control1.73
25mg Meclizine-14.11
50mg Meclizine-.63

[back to top]

Percentage of Change in Expired Air Carbon Monoxide (CO) at End of Week 3

To evaluate the effects of meclizine as an augmentation treatment in conjunction with nicotine patch, the percent decrease in expired air carbon monoxide (CO) at the end of week 3 (relative to baseline) will be compared (using ANOVA) between each meclizine group and placebo. (NCT01443858)
Timeframe: After 3 weeks of treatment (relative to baseline)

Interventionpercentage change (Mean)
Control-34.05
25mg Meclizine-54.10
50mg Meclizine-35.60

[back to top]

Percentage of Change of CO at End of Week 1 When Comparing Abstinent Smokers Versus Non-abstinent Smokers

To further validate the association between a decrease in expired air CO before the quit date and subsequent abstinence, the decrease in expired air CO from baseline to week 1 (Session P2) will be compared between abstinent and non-abstinent smokers, using ANOVA. (NCT01443858)
Timeframe: After 1 week of treatment (relative to baseline)

,,
Interventionpercentage change (Mean)
abstinentnon-abstinent
25mg Meclizine2.64-17.64
50mg Meclizine-16.67-5.37
Control5.001.32

[back to top]

Percentage of Change of CO at End of Week 3 When Comparing Abstinent Smokers Versus Non-abstinent Smokers

To further validate the association between a decrease in expired air CO before the quit date and subsequent abstinence, the decrease in expired air CO from baseline to week 3 (Session P3) will be compared between abstinent and non-abstinent smokers, using ANOVA. (NCT01443858)
Timeframe: After 3 weeks of treatment (relative to baseline)

,,
Interventionpercentage change (Mean)
abstinentnon-abstinent
25mg Meclizine-82.77-47.72
50mg Meclizine-56.76-33.38
Control-47.50-32.13

[back to top]

Adherence to PONV Guidelines

PONV guideline adherence: percentage of patients who received the exact number of prophylactic interventions for PONV that were recommended by the decision support. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: the start of admission at the holding room to the end of the anesthetic case

InterventionParticipants (Count of Participants)
Baseline Measurement666
CDS Email Recommendations5260
CDS Email + Real TIme Recommenations5863

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PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting

The occurrence of PONV, as defined by the administration of antiemetics in the PACU between admission to PACU and discharge from PACU. (NCT02625181)
Timeframe: PACU recovery period

InterventionParticipants (Count of Participants)
Baseline Measurement139
CDS Email Recommendations1323
CDS Email + Real TIme Recommenations1343

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The Number of Prophylactic Interventions for PONV

the absolute number of prophylactic interventions applied between the admission of the patient in the holding room until admission to the PACU. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission at the holding room to the end of the anesthetic case

Interventionprophylactic antiemetics administered (Mean)
Baseline Measurement2.196
CDS Email Recommendations2.176
CDS Email + Real TIme Recommenations2.129

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Time to Discharge From the Postanesthesia Care Unit (PACU)

This is the number of minutes from admission to the PACU until discharge, assessed up to 2 days (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission to the PACU to discharge from the PACU

Interventionminutes (Mean)
Baseline Measurement266
CDS Email Recommendations264
CDS Email + Real TIme Recommenations266

[back to top]