Compounds > 3-hydroxydesloratadine
Page last updated: 2024-11-12

3-hydroxydesloratadine

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

Description

3-hydroxydesloratadine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10359050
SCHEMBL ID2738853
MeSH IDM0462875

Synonyms (25)

Synonym
8-chloro-11-(4-piperidinylidene)-6,11-dihydro-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-3-ol
3-hydroxydesloratadine
8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-3-ol
3-hydroxy desloratadine
FT-0669519
3h9ffn759v ,
119410-08-1
unii-3h9ffn759v
sch 45581
AKOS016010892
SCHEMBL2738853
8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5h-benzo(5,6)cyclohepta(1,2-b)pyridin-3-ol
3-hydroxy-desloratadine
sch-45581
8-chloro-11-(piperidin-4-ylidene)-6,11-dihydro-5h-benzo[5,6]cyclohepta[1,2-b]pyridin-3-ol
J-004124
BCP15788
3-hydroxy desloratadine hcl
13-chloro-2-piperidin-4-ylidene-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-6-ol
Q27257212
3-hydroxy desloratadine dihydrochloride
5h-benzo[5,6]cyclohepta[1,2-b]pyridin-3-ol, 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-
CS-0086018
HY-124245
?3-hydroxy desloratadine

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Tolerability was based on the recording of adverse events (AEs), physical examination, electrocardiograms, and laboratory screen controls at baseline and the final study visit."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008)		0.35

Pharmacokinetics

There were no statistically significant differences in mean plasma concentrations of 3-hydroxydesloratadine when administered in combination with azithromycin or alone. The results of this study in these healthy volunteers found nosignificant differences in pharmacokinetic parameters other than Cmax,ss.

ExcerptReferenceRelevance
" Coadministration of desloratadine with a potent inhibitor of CYP2D6 did not result in clinically relevant changes in its pharmacokinetic parameters."( Pharmacokinetics/pharmacodynamics of desloratadine and fluoxetine in healthy volunteers.
Banfield, C; Flannery, B; Gupta, S; Herron, J; Kantesaria, B, 2004)		0.32
" The method was shown to be accurate, rapid and sufficiently sensitive to be successfully applied to a pharmacokinetic and bioequivalent study."( Simultaneous determination of desloratadine and its active metabolite 3-hydroxydesloratadine in human plasma by LC/MS/MS and its application to pharmacokinetics and bioequivalence.
Chen, WL; Chu, NN; Li, XN; Xu, HR, 2007)		0.57
" Except for maximum observed concentration during a dosing interval (Cmax,ss) of 3-hydroxydesloratadine, on average, there were no statistically significant differences in mean plasma concentrations in any of the main pharmacokinetic parameters of rupatadine, desloratadine, and 3-hydroxydesloratadine when administered in combination with azithromycin or alone."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008)		0.57
" The method was successfully applied to a pharmacokinetic study of RT and its two metabolite DT and 3-OH-DT in healthy volunteers following single (10, 20, 40 mg) and multiple (10 mg) oral doses of rupatadine fumarate tablets."( Development of a highly sensitive LC-MS/MS method for simultaneous determination of rupatadine and its two active metabolites in human plasma: Application to a clinical pharmacokinetic study.
Ding, L; Gu, P; Li, Q; Liu, B; Pan, L; Sun, C; Wu, C; Zhang, J, 2015)		0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
" Except for maximum observed concentration during a dosing interval (Cmax,ss) of 3-hydroxydesloratadine, on average, there were no statistically significant differences in mean plasma concentrations in any of the main pharmacokinetic parameters of rupatadine, desloratadine, and 3-hydroxydesloratadine when administered in combination with azithromycin or alone."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008)		0.57

Bioavailability

ExcerptReferenceRelevance
"The purpose of this study was to describe the effect of the concomitant intake of food on the pharmacokinetic profile and bioavailability of a single dose of rupatadine."( Influence of food on the oral bioavailability of rupatadine tablets in healthy volunteers: a single-dose, randomized, open-label, two-way crossover study.
Carbó, ML; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2007)		0.34
" The 90% CIs were included in the interval 80% to 125% for desloratadine and 3-hydroxydesloratadine, whereas 90% CI for rupatadine was shifted to the right of the interval used for comparing bioavailability of the drugs."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008)		0.57

Dosage Studied

ExcerptRelevanceReference
" Except for maximum observed concentration during a dosing interval (Cmax,ss) of 3-hydroxydesloratadine, on average, there were no statistically significant differences in mean plasma concentrations in any of the main pharmacokinetic parameters of rupatadine, desloratadine, and 3-hydroxydesloratadine when administered in combination with azithromycin or alone."( Pharmacokinetic and safety profile of rupatadine when coadministered with azithromycin at steady-state levels: a randomized, open-label, two-way, crossover, Phase I study.
Antonijoan, R; Barbanoj, M; Carbó, ML; Donado, E; Izquierdo, I; Merlos, M; Nadal, T; Peña, J; Solans, A, 2008)		0.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (43.75)29.6817
2010's6 (37.50)24.3611
2020's3 (18.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.49

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

MetricThis Compound (vs All)
Research Demand Index11.49 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (31.25%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (68.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbamates
[no description available]		2.2510amino-acid anion
formic acid
formic acid: RN given refers to parent cpd. formic acid : The simplest carboxylic acid, containing a single carbon. Occurs naturally in various sources including the venom of bee and ant stings, and is a useful organic synthetic reagent. Principally used as a preservative and antibacterial agent in livestock feed. Induces severe metabolic acidosis and ocular injury in human subjects.		2.1110monocarboxylic acidantibacterial agent;
astringent;
metabolite;
protic solvent;
solvent
cyproheptadine
Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.		4.9442piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.0210amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
flunitrazepam
Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.. flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia.		2.02101,4-benzodiazepinone;
C-nitro compound;
monofluorobenzenes		anxiolytic drug;
GABAA receptor agonist;
sedative
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		3.411(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
gemfibrozil
[no description available]		7.2110aromatic etherantilipemic drug
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		6.99165benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
mianserin
Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.. mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.		2.2510dibenzoazepineadrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
H1-receptor antagonist;
histamine agonist;
sedative;
serotonergic antagonist
norfluoxetine
norfluoxetine: metabolite of fluoxetine; RN given refers to parent cpd without isomeric designation		3.411(trifluoromethyl)benzenes
clopidogrel
Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.		7.2110methyl ester;
monochlorobenzenes;
thienopyridine		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
carbazeran
carbazeran: structure given in first source		2.2510
desloratadine
desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.		6.78135benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
rupatadine
rupatadine: structure given in first source; RN given refers to trihydrochloride		4.6932benzocycloheptapyridine
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		3.4311macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
bilirubin
[no description available]		2.0210biladienes;
dicarboxylic acid		antioxidant;
human metabolite;
mouse metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		04.1231