Page last updated: 2024-12-06

carebastine

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

Description

carebastine: active carboxylic acid metablite of ebastine; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65820
CHEMBL ID67654
CHEBI ID192413
SCHEMBL ID18538
MeSH IDM0162530

Synonyms (34)

Synonym
carebastina [spanish]
carebastine
p-(4-(4-(diphenylmethoxy)piperidino)butyryl)-alpha-methylhydratropic acid
carebastinum [latin]
2-(4-(4-(4-benzhydryloxypiperidino)butyryl)phenyl)-2-methylpropionsaeure
carebastine [inn]
benzeneacetic acid, 4-(4-(4-(diphenylmethoxy)-1-piperidinyl)-1-oxobutyl)-alpha,alpha-dimethyl-
CHEMBL67654
90729-42-3
FT-0664378
2-[4-[4-(4-benzhydryloxypiperidin-1-yl)butanoyl]phenyl]-2-methylpropanoic acid
CHEBI:192413
unii-75dln707do
carebastinum
75dln707do ,
carebastina
AKOS016010168
SCHEMBL18538
XGHOVGYJHWQGCC-UHFFFAOYSA-N
2-(4-(4-(4-(benzhydryloxy)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoic acid
DTXSID60238246
SR-01000945064-1
sr-01000945064
2-(4-{4-[4-(benzhydryloxy)-1-piperidinyl]butanoyl}phenyl)-2-methylpropanoic acid
W15627
2-(4-(4-(4-(benzhydryloxy)piperidin-1-yl)-butanoyl)phenyl)-2-methylpropanoic acid
HY-121356
mfcd00865665
2,2,4,6,6-pentachlorobiphenyl
CS-0081566
Q27266380
4-[4-[4-(diphenylmethoxy)-1-piperidinyl]-1-oxobutyl]-alpha,alpha-dimethylbenzeneacetic acid
BS-29762
A1-50277

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" There were also no significant differences in the percentages of patients experiencing adverse events between the ebastine with and without food groups."( A double-blind, placebo-controlled study of the efficacy and safety of ebastine 20 mg once daily given with and without food in the treatment of seasonal allergic rhinitis.
Frank, H; George, G; Gillen, M; Lim, J; Rohatagi, SS, 2002
)
0.31
" In addition, no differences were observed in the safety of ebastine between patients with renal impairment and healthy subjects when assessing adverse events, vital signs, laboratory parameters or ECGs."( Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.
Noveck, RJ; Preston, RA; Swan, SK, 2007
)
0.34

Pharmacokinetics

Cmax values on Day 1 and Day 5 were similar for ebastine but approximately doubled for carebastine due to its longer half-life. The Cmax of care bastine in guinea pigs (2820 ng/ml) was markedly higher than that in rats, dogs and monkeys. The pharmacokinetics of careBastine were linear over the dose range studied.

ExcerptReferenceRelevance
" The pharmacokinetics of carebastine were linear over the dose range studied and the terminal elimination half-life was 10."( The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
Liminana, R; Meredith, PA; Reid, JL; Vincent, J, 1988
)
0.58
" The Cmax of carebastine in guinea pigs (2820 ng/ml) was markedly higher than that in rats (311 ng/ml), dogs (465 ng/ml) and monkeys (1036 ng/ml)."( Comparative pharmacokinetics of the histamine H1-receptor antagonist ebastine and its active metabolite carebastine in rats, guinea pigs, dogs and monkeys.
Fujii, T; Matsuda, M; Mizuki, Y; Sakashita, M; Sekine, Y; Yamaguchi, T, 1994
)
0.87
" The Cmax and AUC of carebastine increased in proportion to the dose."( Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects.
Fujii, T; Hashizume, T; Matsuda, M; Nakashima, M; Sakashita, M; Sekine, Y; Uematsu, T; Yamaguchi, T, 1994
)
0.83
" Pharmacokinetic investigations have shown the drug to be highly bound to blood proteins, mainly serum albumin, and to have a low brain uptake, explaining its lack of sedative effects."( Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
Carrupt, PA; Jolliet, P; Morin, C; Morin, D; Pagliara, A; Rihoux, JP; Testa, B; Tillement, JP; Urien, S, 1998
)
0.3
"Mean area under the curve and Cmax values on Day 1 and Day 5 were similar for ebastine but approximately doubled for carebastine due to its longer half-life."( Effect of age and gender on the pharmacokinetics of ebastine after single and repeated dosing in healthy subjects.
Aubeneau, M; Gillen, M; Jan, C; Jensen, BK; Pandit, B; Rhodes, G; Rohatagi, S, 2001
)
0.52
" Comparison of the plasma exposure and the elimination half-life of ebastine and carebastine between groups showed no significant differences."( Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.
Noveck, RJ; Preston, RA; Swan, SK, 2007
)
0.57
" No clinically important pharmacokinetic or safety differences were observed between patients with renal impairment and healthy subjects with normal renal function."( Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.
Noveck, RJ; Preston, RA; Swan, SK, 2007
)
0.34

Compound-Compound Interactions

ExcerptReferenceRelevance
"The efficacy and safety of ebastine 20 mg once daily given with and without food were compared in patients ages 12 to 70 years with seasonal allergic rhinitis (SAR) caused by mountain cedar allergen."( A double-blind, placebo-controlled study of the efficacy and safety of ebastine 20 mg once daily given with and without food in the treatment of seasonal allergic rhinitis.
Frank, H; George, G; Gillen, M; Lim, J; Rohatagi, SS, 2002
)
0.31

Bioavailability

ExcerptReferenceRelevance
"001), with an enormous reduction in the oral bioavailability of ebastine and significantly reduced histamine-induced skin reactions."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
0.36

Dosage Studied

ExcerptRelevanceReference
" The kinetics and effects of ebastine 10 and 50 mg were studied after oral dosing in healthy subjects."( The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
Liminana, R; Meredith, PA; Reid, JL; Vincent, J, 1988
)
0.27
" Twelve healthy subjects received a single 20 mg dose of ebastine on day 2 of a multiple oral dosing regimen of either cimetidine (400 mg three times daily and 800 mg in the evening on the day preceding ebastine administration and 400 mg four times daily on the 2 following days) or placebo in a randomised cross-over design."( Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine.
Breimer, DD; Bruno, R; Cohen, AF; Reinhoudt, JF; Schoemaker, HC; Van Rooij, J, 1993
)
0.5
" The antihistamine response after ebastine dosing would be decreased following rifampin pretreatments."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
0.36
[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]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID24562Pharmacokinetic parameter :half life in humans was reported1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID22246Pharmacokinetic parameter :volume apparent of distribution was reported1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID16029Pharmacokinetic parameter :drug bound to plasma was reported1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID135327BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (37)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (2.70)18.7374
1990's13 (35.14)18.2507
2000's18 (48.65)29.6817
2010's4 (10.81)24.3611
2020's1 (2.70)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.10

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.10 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index5.76 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (21.05%)5.53%
Reviews4 (10.53%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other26 (68.42%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]