Compounds > bilastine
Page last updated: 2024-12-08

bilastine

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Cross-References

ID SourceID
PubMed CID185460
CHEMBL ID1742423
CHEBI ID135954
SCHEMBL ID991810
MeSH IDM0413189

Synonyms (59)

Synonym
bilastine ,
CHEBI:135954
ilaxten
bilaxten
f-96221-bm
bilatex
202189-78-4
2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
pa1123n395 ,
unii-pa1123n395
p-(2-(4-(1-(2-ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-alpha-methylhydratropic acid
bilastine [inn]
bilastine (jan/inn)
D09570
bilanoa (tn)
BCP9000412
CHEMBL1742423
S3721
HY-14447
ACCMWZWAEFYUGZ-UHFFFAOYSA-N
2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1h-benzoimidazol-2-yl]-piperidin-1-yl}ethyl)-phenyl]-2-methyl-propionic acid
2-[4-(2-{4-[1-(2-ethoxy-ethyl)-1h-benzoimidazol-2-yl]-piperidin-1-yl}-ethyl)-phenyl]-2-methyl-propionic acid
tox21_113905
cas-202189-78-4
NCGC00262907-01
dtxcid6031467
dtxsid5057678 ,
bilastine [mi]
p-(2-(4-(1-(2-ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-.alpha.-methylhydratropic acid
bilastine [who-dd]
bilastine [jan]
SCHEMBL991810
c28h37n3o3
AC-29231
2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
AKOS030241723
mfcd09837814
DB11591
Q2902977
FT-0700542
BS-15792
2-[4-[2-[4-[1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
B5392
bilastinum
BCP02576
EX-A2962
AMY16470
SB17508
bilastine; 2-(4-(2-(4-(1-(2-ethoxyethyl)-1h-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
benzeneacetic acid, 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethyl-
HMS3887O17
CCG-269384
gtpl11579
2-[4-[2-[4-[1-(2-ethoxyethyl)benzoimidazol-2-yl]-1-piperidyl]ethyl]phenyl]-2-methyl-propanoic acid
A856214
benzeneaceticacid,4-(2-(4-(1-(2-ethoxyethyl)-1h-benzimidazol-2-yl)-1-piperidinyl)ethyl-alpha,alpha-dimethyl-
4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethylbenzeneacetic acid; bilastine
EN300-19634515
2-[4-(2-{4-[1-(2-ethoxyethyl)-1h-1,3-benzodiazol-2-yl]piperidin-1-yl}ethyl)phenyl]-2-methylpropanoic acid

Research Excerpts

Overview

Bilastine (Bilaxten™) is a novel non-sedating H1 receptor antagonist (antihistamine) developed in the dosage form of oral tablets. It is indicated for the treatment of allergic rhinitis (seasonal and perennial) and urticaria.

ExcerptReferenceRelevance
"Bilastine is a nonsedating second-generation antihistamine for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. "( Efficacy of Once-Daily Ophthalmic Bilastine for the Treatment of Allergic Conjunctivitis: A Dose-Finding Study.
Arranz, P; Ciolino, JB; Fernández, N; Gomes, PJ; Hernández, G, 2023)		2.63
"Bilastine is a non-sedating H1 antihistamine indicated for the treatment of allergic rhinoconjunctivitis and urticaria. "( Bioequivalence Evaluation of Three Pediatric Oral Formulations of Bilastine in Healthy Subjects: Results from a Randomized, Open Label, Crossover Study.
Azanza, JR; Campo, C; García-Bea, A; Labeaga, L; Sádaba, B; Valiente, R, 2020)		2.24
"Bilastine is a recently introduced, non-sedative H1-antihistamine for its treatment."( Effectiveness, safety, and tolerability of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic spontaneous urticaria: A double-blind, parallel group, randomized controlled trial.
Biswas, D; Chowdhury, SN; Das, A; Ghosh, S; Podder, I; Sengupta, S, 2020)		1.54
"Bilastine is a highly selective, non-sedating antihistamine, indicated for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. "( Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients.
Biffi, A; Demonte, A; Fainello, M; Fernando, F; Guanti, MB; Liberati, S; Pepe, P, 2018)		3.37
"Bilastine is an H1-antihistamine approved for symptomatic treatment of patients with allergic rhinoconjunctivitis or urticaria. "( Open-label safety assessment of bilastine in elderly patients with allergic rhinoconjunctivitis and/or urticaria.
Cordón, E; Del Mar Forés, M; Fernández, S; Labeaga, L; Riesgo, SE; Ruiz-Miján, M; Senán, MR; Sologuren, A; Viñas, R, 2018)		2.21
"Bilastine (Bilaxten™) is a novel non-sedating H1 receptor antagonist (antihistamine) developed in the dosage form of oral tablets and indicated for the treatment of allergic rhinitis (seasonal and perennial) and urticaria. "( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013)		2.15
"Bilastine is a newly registered H1-antihistamine for treatment of allergic rhinoconjunctivitis and urticaria."( Bilastine for the treatment of urticaria.
Bartra, J; Dávila, I; del Cuvillo, A; Ferrer, M; Jáuregui, I; Montoro, J; Mullol, J; Sastre, J; Valero, A, 2013)		2.55
"Bilastine is a novel second-generation H1 antihistamine, which has not shown sedative or cardiotoxic effects in clinical trials and in post-marketing experience so far, developed for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. "( Evaluation of the single-dose pharmacokinetics of bilastine in subjects with various degrees of renal insufficiency.
Dilzer, SC; La Noce, A; Lasseter, KC; Sologuren, A, 2013)		2.09
"Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine. "( Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria.
Wolthers, OD, 2013)		3.28
"Bilastine is a novel H1 antihistamine with anti-allergic properties which is highly effective in the treatment of symptoms of allergic rhinitis. "( Bilastine as a potential treatment in allergic rhinitis.
DuBuske, L; Kowal, K, )		3.02
"Bilastine is a new oral selective, non-sedating histamine H1 antagonist for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. "( Bilastine: an environmental risk assessment.
Ledo, F; Lucero, ML; Peither, A, 2015)		3.3
"Bilastine is a novel second-generation antihistamine for the symptomatic treatment of allergic rhinitis and urticaria. "( Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects.
Nagashima, H; Rodríguez, M; Togawa, M; Yamaya, H, 2016)		2.1
"Bilastine is a new oral, second generation antihistamine used in the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. "( Cognitive Performance Effects of Bilastine 20 mg During 6 Hours at 8000 ft Cabin Altitude.
Jetten, AM; Labeaga, L; Simons, R; Valiente, R; Valk, PJ, 2016)		2.16
"Bilastine is a novel second-generation antihistamine. "( Long-term safety and efficacy of bilastine following up to 12 weeks or 52 weeks of treatment in Japanese patients with allergic rhinitis: Results of an open-label trial.
Gotoh, M; Ohashi, Y; Okubo, K; Saito, A; Togawa, M, 2017)		2.18
"Bilastine is a novel, nonsedating H(1)-antihistamine developed for symptomatic treatment of Allergic Rhinitis and Chronic Idiopathic Urticaria. "( Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients.
Bachert, C; Dimitrov, V; Gorina, MM; Ivan, P; Kuna, P; Loureiro, A; Sanquer, F; van de Heyning, P, 2009)		2.06
"Bilastine is a new non-sedative H(1) receptor antagonist, indicated for the treatment of allergic rhinitis (AR) (seasonal and perennial)."( Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: a randomized, double-blind, parallel-group study.
Agache, I; Bachert, C; Fouquert, L; Kuna, P; Nowacki, Z; Roger, A; Sologuren, A; Valiente, R; van Cauwenberge, P, 2009)		2.11
"Bilastine is a novel nonsedative H(1)-receptor antagonist, which may be used for the symptomatic treatment of chronic idiopathic urticaria (CU). "( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010)		2.07
"Bilastine 20 mg is a novel effective and safe treatment option for the management of CU."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010)		2.07
"Bilastine is a new second-generation H1 antagonist. "( Acute and subchronic effects of bilastine (20 and 40 mg) and hydroxyzine (50 mg) on actual driving performance in healthy volunteers.
Conen, S; Ramaekers, JG; Theunissen, EL; Valiente, R; Van Oers, AC, 2011)		2.1
"Bilastine is a potent inhibitor of the histamine H1 receptor. "( Bilastine for the relief of allergy symptoms.
Azanza Perea, JR; Gomez-Guiu Hormigos, A; Sádaba Díaz de Rada, B, 2011)		3.25
"Bilastine is a non-sedating second-generation H(1) antihistamine with proven efficacy and safety in the treatment of patients with seasonal allergic rhinitis and urticaria. "( Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo in the treatment of perennial allergic rhinitis.
Mullol, J; Sastre, J; Valero, A; Valiente, R, 2012)		2.13
"Bilastine is a newly registered H1-antihistamine for the oral treatment of allergic rhinitis and urticaria, with established antihistaminic and antiallergic properties."( An overview of the novel H1-antihistamine bilastine in allergic rhinitis and urticaria.
Antépara, I; Gamboa, PM; García-Lirio, E; Jáuregui, I; Soriano, AM, 2012)		1.36
"Bilastine is a potent inhibitor of the histamine H(1) receptor. "( Establishing the place in therapy of bilastine in the treatment of allergic rhinitis according to ARIA: evidence review.
Ansótegui, I; Bachert, C; Baena-Cagnani, CE; Bousquet, J; Canonica, GW; Church, MK; Cruz, AA; González, SN; Kuna, P; Morais-Almeida, M; Mullol, J; Ryan, DP; Sánchez-Borges, M; Valiente, R; Zuberbier, T, 2012)		2.09
"Bilastine is a new H1 antihistamine that proves to be effective in treating allergic rhinoconjunctivitis (seasonal and perennial) and urticaria."( Bilastine and the central nervous system.
Bartra, J; Dávila, I; del Cuvillo, A; Ferrer, M; Jáuregui, I; Montoro, J; Mullol, J; Sastre, J; Valero, A, 2011)		2.53
"Bilastine is a new H1 antihistamine with an excellent safety profile, developed for the treatment of allergic rhinoconjunctivitis and urticaria, with potency similar to that of cetirizine and desloratadine, and superior to that of fexofenadine."( Effect of bilastine upon the ocular symptoms of allergic rhinoconjunctivitis.
Bartra, J; Dávila, I; del Cuvillos, A; Ferrer, M; Jáuregui, I; Montoro, J; Mullol, J; Sastre, J; Valero, A, 2011)		1.49
"Bilastine is a new nonsedating H₁ antihistamine indicated for the treatment of allergic rhinoconjunctivitis and urticaria."( Interactions of bilastine, a new oral H₁ antihistamine, with human transporter systems.
Bednarczyk, D; Ganza, A; Gedey, S; Gonzalo, A; Ioja, E; Jahic, M; Leal, N; Lucero, ML; Soengas, I, 2012)		1.45
"Bilastine is an orally administered, second-generation antihistamine used in the symptomatic treatment of seasonal or perennial allergic rhinoconjunctivitis and urticaria. "( Bilastine: in allergic rhinitis and urticaria.
Carter, NJ, 2012)		3.26
"Bilastine is a new H1 antagonist with no sedative side effects, no cardiotoxic effects, and no hepatic metabolism. "( Safety profile of bilastine: 2nd generation H1-antihistamines.
Scaglione, F, 2012)		2.16

Effects

Bilastine has a better therapeutic effect on CU. Can also significantly improve the clinical symptoms and quality of life of CU. Has demonstrated a good safety profile, without serious adverse effects.

ExcerptReferenceRelevance
"Bilastine has a better therapeutic effect on CU and can also significantly improve the clinical symptoms and quality of life of CU."( Effect of Bilastine on Chronic Urticaria: A Systematic Review and Meta-Analysis.
Deng, Z; Fan, Z; Kong, D; Li, N; Liu, W; Tu, H; Wang, Q; Xue, X; Yang, X, 2023)		2.76
"Bilastine has a better therapeutic effect on CU and can also significantly improve the clinical symptoms and quality of life of CU."( Effect of Bilastine on Chronic Urticaria: A Systematic Review and Meta-Analysis.
Deng, Z; Fan, Z; Kong, D; Li, N; Liu, W; Tu, H; Wang, Q; Xue, X; Yang, X, 2023)		2.76
"Bilastine has demonstrated a good safety profile, without serious adverse effects or antimuscarinic effects in clinical trials."( Bilastine for the relief of allergy symptoms.
Azanza Perea, JR; Gomez-Guiu Hormigos, A; Sádaba Díaz de Rada, B, 2011)		2.53
"Bilastine has also been shown to have anti-inflammatory properties."( Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity.
Berisa, A; Corcóstegui, R; Innerárity, A; Labeaga, L; Orjales, A, 2005)		1.34

Actions

Bilastine 20 mg did not cause sleepiness or impaired performance on tasks related to flying. Bilastine did not produce any driving impairment after single and repeated doses.

ExcerptReferenceRelevance
"Bilastine 20 mg did not cause sleepiness or impaired performance on tasks related to flying. "( Cognitive Performance Effects of Bilastine 20 mg During 6 Hours at 8000 ft Cabin Altitude.
Jetten, AM; Labeaga, L; Simons, R; Valiente, R; Valk, PJ, 2016)		2.16
"Bilastine did not produce any driving impairment after single and repeated doses and can be safely used in traffic in doses up to 40 mg."( Acute and subchronic effects of bilastine (20 and 40 mg) and hydroxyzine (50 mg) on actual driving performance in healthy volunteers.
Conen, S; Ramaekers, JG; Theunissen, EL; Valiente, R; Van Oers, AC, 2011)		1.37

Treatment

The bilastine treatments were safe and well tolerated. Bilastine treatment was well tolerated without evidence of increased sedation with dose escalation.

ExcerptReferenceRelevance
"Bilastine treatment was well tolerated without evidence of increased sedation with dose escalation."( Up-dosing with bilastine results in improved effectiveness in cold contact urticaria.
Church, MK; Krause, K; Maurer, M; Spohr, A; Zuberbier, T, 2013)		1.46
"The bilastine treatments were safe and well tolerated."( Efficacy and safety of bilastine in Japanese patients with chronic spontaneous urticaria: A multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II/III study.
Furue, M; Hide, M; Saito, A; Togawa, M; Yagami, A, 2017)		1.25

Toxicity

Bilastine had a good safety profile and was well tolerated in terms of adverse events, laboratory parameters and vital signs. With respect to effects on embryofoetal development in rabbits, bilastine at 400 mg/kg/day (the highest dose evaluated) was assessed to be the no observed adverse effects level.

ExcerptReferenceRelevance
" The incidence of treatment emergent adverse events was similar for bilastine (20."( Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients.
Bachert, C; Dimitrov, V; Gorina, MM; Ivan, P; Kuna, P; Loureiro, A; Sanquer, F; van de Heyning, P, 2009)		0.85
"Bilastine 20 mg once daily was efficacious, safe and not different from desloratadine 5 mg once daily in the treatment of SAR symptoms."( Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients.
Bachert, C; Dimitrov, V; Gorina, MM; Ivan, P; Kuna, P; Loureiro, A; Sanquer, F; van de Heyning, P, 2009)		2.06
" Safety was assessed according to adverse events (AEs), laboratory tests and electrocardiograms."( Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: a randomized, double-blind, parallel-group study.
Agache, I; Bachert, C; Fouquert, L; Kuna, P; Nowacki, Z; Roger, A; Sologuren, A; Valiente, R; van Cauwenberge, P, 2009)		0.66
" Safety was assessed according to adverse events, laboratory tests and electrocardiograms."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010)		0.63
" Comparison with levocetirizine indicated both treatments to be equally efficacious as well as equally safe and well tolerated as compared with placebo."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010)		0.63
"Bilastine 20 mg is a novel effective and safe treatment option for the management of CU."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010)		2.07
" In addition, bilastine was shown to be safe and well-tolerated over a 1-year treatment period."( Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo in the treatment of perennial allergic rhinitis.
Mullol, J; Sastre, J; Valero, A; Valiente, R, 2012)		1.05
" With respect to effects on embryofoetal development in rabbits, bilastine at 400 mg/kg/day (the highest dose evaluated) was assessed to be the no observed adverse effects level."( Preclinical toxicity profile of oral bilastine.
Arteche, JK; Casadesus, A; Lucero, ML; Sommer, EW, 2012)		0.89
" The absorption of bilastine is fast, linear and dose-proportional; it appears to be safe and well tolerated at all doses levels in healthy population."( Safety profile of bilastine: 2nd generation H1-antihistamines.
Scaglione, F, 2012)		1.04
" Safety evaluations included treatment-emergent adverse events (TEAEs), laboratory tests, cardiac safety (ECG recordings) and somnolence/sedation using the Pediatric Sleep Questionnaire (PSQ)."( Safety and tolerability of bilastine 10 mg administered for 12 weeks in children with allergic diseases.
Kiss, I; Kuna, P; Novák, Z; Tortajada-Girbés, M; Valiente, R; Yáñez, A, 2016)		0.73
" Adverse events (AEs) were reported by 17."( Long-term safety and efficacy of bilastine following up to 12 weeks or 52 weeks of treatment in Japanese patients with allergic rhinitis: Results of an open-label trial.
Gotoh, M; Ohashi, Y; Okubo, K; Saito, A; Togawa, M, 2017)		0.74
" The bilastine treatments were safe and well tolerated."( Efficacy and safety of bilastine in Japanese patients with chronic spontaneous urticaria: A multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II/III study.
Furue, M; Hide, M; Saito, A; Togawa, M; Yagami, A, 2017)		1.28
"Bilastine had a good safety profile and was well tolerated in terms of adverse events, laboratory parameters and vital signs."( Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients.
Biffi, A; Demonte, A; Fainello, M; Fernando, F; Guanti, MB; Liberati, S; Pepe, P, 2018)		3.37
" The safety profile of bilastine in clinical trials of allergic rhinoconjunctivitis or urticaria, assessed by type and frequency of adverse events (AE), was similar to that of placebo."( Open-label safety assessment of bilastine in elderly patients with allergic rhinoconjunctivitis and/or urticaria.
Cordón, E; Del Mar Forés, M; Fernández, S; Labeaga, L; Riesgo, SE; Ruiz-Miján, M; Senán, MR; Sologuren, A; Viñas, R, 2018)		1.08
" Safety was assessed by recording drug-related adverse events, biochemical investigations, and electrocardiogram, along with tolerability and compliance."( Effectiveness, safety, and tolerability of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic spontaneous urticaria: A double-blind, parallel group, randomized controlled trial.
Biswas, D; Chowdhury, SN; Das, A; Ghosh, S; Podder, I; Sengupta, S, 2020)		0.82
" Adverse drug reactions were recorded for each subject during drug administration and follow-up visits."( Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.
Abad-Santos, F; Arranz, P; Belmonte, C; Elgezabal, L; Fernández, N; Hernández, G; Martín-Vilchez, S; Mejía-Abril, G; Ochoa, D; Román, M, 2021)		0.9
" Adverse events were mild and transient, consisting mainly of dysgeusia."( Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.
Abad-Santos, F; Arranz, P; Belmonte, C; Elgezabal, L; Fernández, N; Hernández, G; Martín-Vilchez, S; Mejía-Abril, G; Ochoa, D; Román, M, 2021)		0.9

Pharmacokinetics

Bilastine exhibits similar single- and multiple-dose pharmacokinetic and pharmacodynamic characteristics in healthy adult subjects. No significant differences among groups in median time to reach Cmax (tmax) or in the mean terminal disposition rate constants for bilastine were found.

ExcerptReferenceRelevance
"To model the pharmacokinetic and pharmacodynamic relationship of bilastine, a new histamine H(1) receptor antagonist, from single- and multiple-dose studies in healthy adult subjects."( Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.
de la Fuente, L; Jauregizar, N; Leal, N; Lucero, ML; Rodríguez, M; Sologuren, A, 2009)		0.82
"The pharmacokinetic model was developed from different single-dose and multiple-dose studies."( Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.
de la Fuente, L; Jauregizar, N; Leal, N; Lucero, ML; Rodríguez, M; Sologuren, A, 2009)		0.58
"Pharmacokinetic and pharmacodynamic relationships of bilastine were reliably described with the use of an indirect response pharmacodynamic model; this led to an accurate prediction of the pharmacodynamic activity of bilastine."( Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.
de la Fuente, L; Jauregizar, N; Leal, N; Lucero, ML; Rodríguez, M; Sologuren, A, 2009)		0.83
" Blood and urine samples were collected from pre-dose up to 72 h post-dose for bilastine pharmacokinetic analysis."( Evaluation of the single-dose pharmacokinetics of bilastine in subjects with various degrees of renal insufficiency.
Dilzer, SC; La Noce, A; Lasseter, KC; Sologuren, A, 2013)		0.87
" No significant differences among groups in median time to reach Cmax (tmax) or in the mean terminal disposition rate constants for bilastine were found."( Evaluation of the single-dose pharmacokinetics of bilastine in subjects with various degrees of renal insufficiency.
Dilzer, SC; La Noce, A; Lasseter, KC; Sologuren, A, 2013)		0.85
" The pharmacokinetic and pharmacodynamic profiles were compared with those reported in Caucasian subjects."( Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects.
Nagashima, H; Rodríguez, M; Togawa, M; Yamaya, H, 2016)		0.65
"Bilastine exhibits similar single- and multiple-dose pharmacokinetic and pharmacodynamic characteristics in healthy Japanese subjects compared with those observed in Caucasian subjects in previous studies."( Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects.
Nagashima, H; Rodríguez, M; Togawa, M; Yamaya, H, 2016)		2.1

Bioavailability

Bilastine was characterized by two-compartmental kinetics with a rapid-absorption phase (first-order absorption rate constant = 1.0). The aim of this trial was to study the absolute oral bioavailability of bilastine.

ExcerptReferenceRelevance
" The aim of this trial was to study the absolute oral bioavailability of bilastine in humans."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013)		0.94
"Oral bioavailability of bilastine was 60."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013)		1.02
" The absolute oral bioavailability was moderate."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013)		0.71
"This was an open-label, single-centre, phase I, bioavailability clinical trial."( Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.
Abad-Santos, F; Arranz, P; Belmonte, C; Elgezabal, L; Fernández, N; Hernández, G; Martín-Vilchez, S; Mejía-Abril, G; Ochoa, D; Román, M, 2021)		0.9

Dosage Studied

Bilastine (Bilaxten™) is a novel non-sedating H1 receptor antagonist (antihistamine) developed in the dosage form of oral tablets. It is indicated for the treatment of allergic rhinitis (seasonal and perennial) and urticaria.

ExcerptRelevanceReference
"In view of its favorable pharmacological and clinical characteristics, bilastine is likely to have particular benefit in urticaria for which guidelines recommend increasing the dosage of H(1)-antihistamines up to fourfold if standard dosing is ineffective."( Safety and efficacy of bilastine: a new H(1)-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria.
Church, MK, 2011)		0.91
"Bilastine (Bilaxten™) is a novel non-sedating H1 receptor antagonist (antihistamine) developed in the dosage form of oral tablets and indicated for the treatment of allergic rhinitis (seasonal and perennial) and urticaria."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013)		2.15
" First-choice treatment continues to be centred on the second-generation H1 antihistamines, including a wide group of drugs with a better therapeutic index (or risk:benefit ratio) than the classic ones, even in the high, off-label dosage occasionally required in chronic urticaria."( Bilastine for the treatment of urticaria.
Bartra, J; Dávila, I; del Cuvillo, A; Ferrer, M; Jáuregui, I; Montoro, J; Mullol, J; Sastre, J; Valero, A, 2013)		1.83
" Research into aspects of pharmacokinetics and efficacy and adverse effect profiles of bilastine in children under 12 years of age is needed as are dose-response assessments and studies planned rigorously with the aim of assessing quality of life effects."( Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria.
Wolthers, OD, 2013)		2.06
"Bilastine PECsw was calculated using the maximum daily dosage (20 mg), assuming that all administered bilastine was released into the aquatic environment."( Bilastine: an environmental risk assessment.
Ledo, F; Lucero, ML; Peither, A, 2015)		3.3
"We enrolled 136 subjects and the sum of TNSS on Day 1 of the three active treatments was significantly lower than that of placebo and was maintained up to 26 h after the first dosing (Day 2)."( Therapeutic effect of bilastine in Japanese cedar pollinosis using an artificial exposure chamber (OHIO Chamber).
Hashiguchi, K; Okubo, K; Saito, A; Togawa, M; Wakabayashi, KI, 2017)		0.77
"The objective of this study was to evaluate bilastine dosing recommendations in older adults and overcome the limitation of insufficient data from phase I studies in this underrepresented population."( Application of a dual mechanistic approach to support bilastine dose selection for older adults.
Campo, C; García-Bea, A; Kim, C; Leal, N; Lo Re, V; Lukas, JC; Rodriguez, M; Schmidt, S; Suarez, E; Vozmediano, V, 2021)		1.13
" According to a literature review, no UV-visible spectrophotometric method has been reported yet for simultaneous estimation of montelukast sodium and bilastine in their combined pharmaceutical dosage forms."( Risk Assessment-Based Enhanced Analytical Quality-by-Design Approach to Eco-Friendly and Economical Multicomponent Spectrophotometric Methods for Simultaneous Estimation of Montelukast Sodium and Bilastine.
Mishra, A; Prajapati, P; Surati, P; Tamboli, J, 2021)		1.01
"The developed and validated methods were applied for assay of combined pharmaceutical dosage forms of montelukast sodium and bilastine and results were found to be in good agreement with their label claims."( Risk Assessment-Based Enhanced Analytical Quality-by-Design Approach to Eco-Friendly and Economical Multicomponent Spectrophotometric Methods for Simultaneous Estimation of Montelukast Sodium and Bilastine.
Mishra, A; Prajapati, P; Surati, P; Tamboli, J, 2021)		1.02
" An assay of combined tablet dosage forms of montelukast sodium and bilastine was then carried out using the developed methods."( Risk Assessment-Based Enhanced Analytical Quality-by-Design Approach to Eco-Friendly and Economical Multicomponent Spectrophotometric Methods for Simultaneous Estimation of Montelukast Sodium and Bilastine.
Mishra, A; Prajapati, P; Surati, P; Tamboli, J, 2021)		1.05
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
[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
Bilastine H1-Antihistamine Action87

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6Homo sapiens (human)Potency38.90180.00108.379861.1304AID1645840
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency22.38720.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (96)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's8 (8.33)29.6817
2010's59 (61.46)24.3611
2020's29 (30.21)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 110.74

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 Index110.74 (24.57)
Research Supply Index4.91 (2.92)
Research Growth Index5.46 (4.65)
Search Engine Demand Index199.50 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (110.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials35 (35.00%)5.53%
Reviews22 (22.00%)6.00%
Case Studies6 (6.00%)4.05%
Observational1 (1.00%)0.25%
Other36 (36.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carnitine
[no description available]		2.1510amino-acid betainehuman metabolite;
mouse metabolite
histamine
[no description available]		6.5653aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
azelastine
azelastine: azeptin is azelastine hydrochloride; structure; eye drop formulation effective in relieving symptoms of allergic conjunctivitis; do not confuse with 5-loxin which is an extract of Boswellia. azelastine : A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.		3.1910monochlorobenzenes;
phthalazines;
tertiary amino compound		anti-allergic agent;
anti-asthmatic drug;
bronchodilator agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
H1-receptor antagonist;
platelet aggregation inhibitor
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		11.861511ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
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.		5.0121piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
diphenhydramine
Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.		2.1710ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
ebastine
[no description available]		3.1910organic molecular entity
emedastine
emedastine: structure given in first source. emedastine : 1-Methyl-1,4-diazepane in which the hydrogen attached to the nitrogen at position 4 is substituted by a 1-(2-ethoxyethyl)-1H-benzimidazol-2-yl group. A relatively selective histamine H1 antagonist, it is used as the difumatate salt for allergic rhinitis, urticaria, and pruritic skin disorders, and in eyedrops for the symptomatic relief of allergic conjuntivitis.		3.1810benzimidazolesanti-allergic agent;
antipruritic drug;
H1-receptor antagonist
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		8.1263piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		2.2510aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
hydroxyzine
Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.		5.5544hydroxyether;
monochlorobenzenes;
N-alkylpiperazine		anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		9.3711dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
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.		9.5874benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		8.1263diarylmethane
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		2.873011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
betamethasone
Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)		2.251011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic agent;
anti-inflammatory drug;
immunosuppressive agent
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		3.0130benzenes;
phenyl acetates
lopinavir
[no description available]		2.2510amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
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.		8.7754benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
rupatadine
rupatadine: structure given in first source; RN given refers to trihydrochloride		10.0121benzocycloheptapyridine
betamethasone-17,21-dipropionate
betamethasone-17,21-dipropionate: may also contain chlorocresol (UD 25:22R)		2.2510
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		4.3711aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		2.25101,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
bradykinin
[no description available]		2.0310oligopeptidehuman blood serum metabolite;
vasodilator agent
levocetirizine
[no description available]		8.9763diarylmethane
oxazolone
Oxazolone: Immunologic adjuvant and sensitizing agent.		2.0310
montelukast
montelukast: a leukotriene D4 receptor antagonist		3.0130aliphatic sulfide;
monocarboxylic acid;
quinolines		anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
clobetasol
Clobetasol: A derivative of PREDNISOLONE with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than FLUOCINONIDE, it is used topically in treatment of PSORIASIS but may cause marked adrenocortical suppression.. clobetasol : A 3-oxo-Delta(1),Delta(4)-steroid that is 16beta-methylpregna-1,4-diene-3,20-dione bearing hydroxy groups at the 11beta and 17alpha positions, fluorine at position 9, and a chlorine substituent at position 21. It is used as its 17alpha-propionate ester to treat various skin disorders, including exzema and psoriasis.		2.151011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
chlorinated steroid;
fluorinated steroid;
glucocorticoid;
tertiary alpha-hydroxy ketone		anti-inflammatory drug;
SMO receptor agonist
fluticasone
Fluticasone: A STEROID with GLUCOCORTICOID RECEPTOR activity that is used to manage the symptoms of ASTHMA; ALLERGIC RHINITIS, and ATOPIC DERMATITIS.. fluticasone : A trifluorinated corticosteroid used in the form of its propionate ester for treatment of allergic rhinitis.		3.191011beta-hydroxy steroid;
17alpha-hydroxy steroid;
3-oxo-Delta(4) steroid;
corticosteroid;
fluorinated steroid;
thioester		anti-allergic agent;
anti-asthmatic drug
ciclesonide
ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis		3.1910organic molecular entity
amoxicillin-potassium clavulanate combination
Amoxicillin-Potassium Clavulanate Combination: A fixed-ratio combination of amoxicillin trihydrate and potassium clavulanate.		2.1510
phosphatidylcholines
Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety.		2.15101,2-diacyl-sn-glycero-3-phosphocholine
piperidines
Piperidines: A family of hexahydropyridines.		18.339640
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Allergic Rhinitis
[description not available]		07.96102
Hives
[description not available]		015.924913
Urticaria
A vascular reaction of the skin characterized by erythema and wheal formation due to localized increase of vascular permeability. The causative mechanism may be allergy, infection, or stress.		117.924913
Rhinitis, Allergic
An inflammation of the NASAL MUCOSA triggered by ALLERGENS.		07.96102
Allergic Conjunctivitis
[description not available]		011.1361
Itching
[description not available]		05.8132
Conjunctivitis, Allergic
Conjunctivitis due to hypersensitivity to various allergens.		18.1361
Pruritus
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.		010.8132
Autoimmune Urticaria
[description not available]		09.12132
Allergic Reaction
[description not available]		04.1630
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		16.1630
Chronic Illness
[description not available]		010.25139
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		010.25139
Cyanosis
A bluish or purplish discoloration of the skin and mucous membranes due to an increase in the amount of deoxygenated hemoglobin in the blood or a structural defect in the hemoglobin molecule.		02.3110
Exanthem
[description not available]		02.3110
Symptom Cluster
[description not available]		02.3110
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		02.3110
Exanthema
Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology.		02.3110
Syndrome
A characteristic symptom complex.		07.3110
Infections, Coronavirus
[description not available]		02.2510
2019 Novel Coronavirus Disease
[description not available]		02.2510
Dermatitis Medicamentosa
[description not available]		02.2510
Skin Diseases, Viral
Skin diseases caused by viruses.		02.2510
Pneumonia, Viral
Inflammation of the lung parenchyma that is caused by a viral infection.		02.2510
Coronavirus Infections
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).		02.2510
Anasarca
[description not available]		02.1510
Keratoderma Blennorrhagicum
[description not available]		02.1510
Dermatitis
Any inflammation of the skin.		02.4720
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		02.1510
Erythema
Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes.		02.1510
Keratosis
Any horny growth such as a wart or callus.		02.1510
Dizzyness
[description not available]		03.5611
Dizziness
An imprecise term which may refer to a sense of spatial disorientation, motion of the environment, or lightheadedness.		03.5611
Adverse Drug Event
[description not available]		09.76109
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		09.76109
Eosinophilia, Tropical
[description not available]		02.2110
Dermatoses
[description not available]		02.2110
Eosinophilia
Abnormal increase of EOSINOPHILS in the blood, tissues or organs.		07.2110
Skin Diseases
Diseases involving the DERMIS or EPIDERMIS.		02.2110
Asthma, Bronchial
[description not available]		07.0850
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		012.0850
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		03.4711
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		08.4711
Rhinitis, Allergic, Nonseasonal
[description not available]		011.68163
Rhinitis, Allergic, Perennial
Inflammation of the mucous membrane of the nose similar to that found in hay fever except that symptoms persist throughout the year. The causes are usually air-borne allergens, particularly dusts, feathers, molds, animal fur, etc.		113.68163
Alcohol Drinking
Behaviors associated with the ingesting of ALCOHOLIC BEVERAGES, including social drinking.		03.4811
Hay Fever
[description not available]		015.973620
Rhinitis, Allergic, Seasonal
Allergic rhinitis that occurs at the same time every year. It is characterized by acute CONJUNCTIVITIS with lacrimation and ITCHING, and regarded as an allergic condition triggered by specific ALLERGENS.		117.973620
Dermatitis, Eczematous
[description not available]		03.5311
Prurigo
A name applied to several itchy skin eruptions of unknown cause. The characteristic course is the formation of a dome-shaped papule with a small transient vesicle on top, followed by crusting over or lichenification. (From Dorland, 27th ed)		03.5311
Adverse Effects, Long Term
[description not available]		03.5311
Eczema
A pruritic papulovesicular dermatitis occurring as a reaction to many endogenous and exogenous agents (Dorland, 27th ed).		03.5311
Chronic Hepatitis B
[description not available]		02.1510
Viremia
The presence of viruses in the blood.		02.1510
Hepatitis B, Chronic
INFLAMMATION of the LIVER in humans caused by HEPATITIS B VIRUS lasting six months or more. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.		02.1510
Contact Dermatitis
[description not available]		03.4311
Dermatitis, Contact
A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms.		03.4311
Eye Disorders
[description not available]		07.4844
Nasal Diseases
[description not available]		07.4844
Eye Diseases
Diseases affecting the eye.		07.4844
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		03.910
Bilateral Nasal Obstruction
[description not available]		02.9810
Nasal Obstruction
Any hindrance to the passage of air into and out of the nose. The obstruction may be unilateral or bilateral, and may involve any part of the NASAL CAVITY.		07.9810
Electrocardiogram QT Prolonged
[description not available]		04.3711
Long QT Syndrome
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.		04.3711
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		04.3120
Bronchospasm
[description not available]		02.0310
Bronchial Spasm
Spasmodic contraction of the smooth muscle of the bronchi.		02.0310