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cetirizine

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Description

Cetirizine is a non-sedating antihistamine used to treat allergies. It blocks the action of histamine, a chemical released by the body in response to allergens. Cetirizine is synthesized through a multi-step process involving the reaction of pyridyl ketone with hydrazine, followed by cyclization and subsequent modifications. The compound exhibits potent H1-receptor antagonist activity, effectively relieving symptoms like sneezing, runny nose, itchy eyes, and hives. Cetirizine is widely studied due to its effectiveness and safety profile in treating allergic rhinitis, urticaria, and other allergic conditions. Its non-sedating nature makes it a preferred choice for patients requiring daytime allergy relief.'

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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [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]

Cross-References

ID SourceID
PubMed CID2678
CHEMBL ID1000
CHEBI ID3561
SCHEMBL ID4176
MeSH IDM0026321

Synonyms (112)

Synonym
AC-5545
HY-17042
HMS3393N10
BRD-A42571354-300-05-4
gtpl1222
BSPBIO_000425
virlix
[(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethyl)oxy]acetic acid
PRESTWICK2_000503
chembl1000 ,
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
bdbm22890
cetryn
ziptek
acetic acid, (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-
cetirizinum [latin]
hitrizin film tablet
setir
cetirizine [inn:ban]
cetirizina [spanish]
(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)acetic acid
TIMTEC1_002075
cetirizine hydrochloride
PRESTWICK3_000503
humex
D07662
cetiderm (tn)
cetirizine (inn)
BPBIO1_000469
cetirizine
83881-51-0
C07778
DB00341
BSPBIO_002302
PRESTWICK0_000503
SPBIO_002346
PRESTWICK1_000503
NCGC00167781-02
NCGC00167781-01
NCGC00167781-03
cetiderm
P071 ,
CHEBI:3561 ,
cetirizina
(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
cetirizinum
cetirizin
HMS1539O07
NCGC00167781-04
ac-170 ,
L000655
FT-0664488
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid
AKOS003589059
HMS3259D06
STK711108
EN300-52521
unii-yo7261me24
yo7261me24 ,
hsdb 7739
BBL009968
zyrlex
FT-0603001
NCGC00167781-07
CS-0886
HMS3370I19
(+/-)-(2-(4-(p-chloro-a-phenylbenzyl)-1-piperazinyl)ethoxy)acetic acid
cetirizine [who-dd]
cetirizine [vandf]
cetirizine [inn]
cetirizine [hsdb]
acetic acid, (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-, (+/-)-
cetirizine [mi]
[2-[4-[(4-chlorophenyl)phenylmethyl] 1-piperazinyl]-ethoxy] acetic acid
ZKLPARSLTMPFCP-UHFFFAOYSA-N
[2-[4-[(4-chlorophenyl)-phenyl methyl]-1-piperazinyl] ethoxy] acetic acid
[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid
2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid
[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid
NC00696
SCHEMBL4176
AKOS021729457
2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazin-1-yl]ethoxy]acetic acid dihydrichloride
cetirizine-d8
DTXSID4022787 ,
1133210-23-7
acetic acid, [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-
J-005737
benaday
acetic acid, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-
SBI-0206838.P001
2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetic acid
cetrizine
Q423075
(+/-)-cetirizine-d4 dihydrochloride
E75781
BCP08787
BCP28477
AMY22576
BRD-A42571354-300-07-0
SDCCGSBI-0206838.P002
NCGC00167781-18
NCGC00167781-12
cet83881-51-0
irizine
AS-77105
2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)aceticacid
Z754931270
(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetic acid
r06ae07
dtxcid802787
cetirizinum (latin)

Research Excerpts

Overview

Cetirizine hydrochloride is a second-generation H1 histamine antagonist with Food and Drug Administration approval for treatment of allergic rhinitis and urticaria. The drug is a less sedative alternative to diphenhydramine for the prevention of infusion-related reactions (IRR) to paclitaxel.

ExcerptReferenceRelevance
"Cetirizine is a less sedative alternative to diphenhydramine for the prevention of infusion-related reactions (IRR) to paclitaxel. "( A randomized double-blind feasibility study comparing cetirizine and diphenhydramine in the prevention of paclitaxel-associated infusion-related reactions: the PREMED-F1 study.
Beaucage-Charron, J; Bouchard, P; Charpentier, F; Gaudet, L; Lamothe, S; Lordkipanidzé, M; Pelletier, C; Pépin, AS; Picard, M; Projean, D; Roy, V, 2022
)
2.41
"Cetirizine is an antihistamine that may be effective in hair loss treatment."( Comparison between topical cetirizine with minoxidil versus topical placebo with minoxidil in female androgenetic alopecia: a randomized, double-blind, placebo-controlled study.
Abbassi, MM; Bassiouny, EA; El-Samanoudy, SI; Farid, SF; Nada, HR, 2023
)
1.93
"Levocetirizine is an orally administrated, second-generation antihistaminic active pharmaceutical ingredient that has been used to treat symptoms of allergy and long-term hives for over 25 years. "( The Elusive Structure of Levocetirizine Dihydrochloride Determined by Electron Diffraction.
Alhaddad, Z; Bücker, R; Göb, CR; Karothu, DP; Naumov, P; Schürmann, CJ, 2023
)
1.76
"Cetirizine hydrochloride is a second-generation H1 histamine antagonist with Food and Drug Administration approval for treatment of allergic rhinitis and urticaria. "( Maternal Transfer of Cetirizine Into Human Milk.
Baker, T; Datta, P; Hale, TW; Rewers-Felkins, K; Wilkerson, H, 2021
)
2.38
"Cetirizine is a histamine H1 antagonist that is US Food and Drug Administration approved for the treatment of allergic rhinitis and urticaria and has common adverse effects of drowsiness and headaches."( A case report of sleep terrors exacerbated by cetirizine.
Aziz, SG; Hussain, S, 2021
)
1.6
"Cetirizine is a well-known effective antihistamine."( Cetirizine modifies quality of life and symptoms in children with seasonal allergic rhinitis: a pilot study.
Benazzo, M; Ciprandi, G; Corsico, A; Leonardi, S; Licari, A; Marseglia, GL; Miraglia Del Giudice, M; Peroni, D; Salpietro, C, 2020
)
2.72
"Cetirizine (CTZ) is an antihistaminic drug present in the aquatic environment, with limited information on its toxicity to organisms inhabiting this system. "( Ecotoxicity of the antihistaminic drug cetirizine to Ruditapes philippinarum clams.
Almeida, Â; Calisto, V; Esteves, VI; Figueira, E; Freitas, R; Schneider, RJ; Soares, AMVM, 2017
)
2.17
"Cetirizine appears to be a viable substitute for diphenhydramine for the prevention of infusions reactions with cetuximab, paclitaxel, and rituximab infusions in adults. "( Cetirizine versus diphenhydramine in the prevention of chemotherapy-related hypersensitivity reactions.
Durham, CG; Foster, J; Herrington, JD; Sager, L; Thotakura, D, 2019
)
3.4
"Cetirizine is an antihistamine used in dogs, but plasma concentrations in relation to effect after oral administration are not well studied. "( Cetirizine per os: exposure and antihistamine effect in the dog.
Bondesson, U; Ekstrand, C; Hedeland, M; Ingvast-Larsson, C; Olsén, L, 2018
)
3.37
"Cetirizine is a zwitterionic second-generation antihistamine containing "( Differential Regulation of Thermodynamic Binding Forces of Levocetirizine and (
Akatsu, C; Hishinuma, S; Kobayashi, C; Shoji, M; Tamura, Y, 2018
)
2.16
"Cetirizine is a second-generation H1 histamine receptor antagonist that is commonly used for symptomatic relief of hay fever and other allergies and can be combined with pseudoephedrine hydrochloride, a decongestant. "( Cetirizine-associated delusions and depression in an 18-year-old woman.
Francois, D; Garden, BC,
)
3.02
"Cetirizine is a piperazine-derived second-generation antihistaminic drug recommended for treatment of pruritus associated with atopic dermatitis. "( Development of novel elastic vesicle-based topical formulation of cetirizine dihydrochloride for treatment of atopic dermatitis.
Goindi, S; Kaur, A; Kumar, G; Kumar, N, 2013
)
2.07
"Cetirizine is an antihistamine used in performance horses for the treatment of hypersensitivity reactions and as such a withdrawal time is necessary prior to competition. "( Elimination of cetirizine following administration of multiple doses to exercised thoroughbred horses.
Arthur, RM; Knych, HK; McKemie, DS; Stanley, SD, 2016
)
2.23
"Levocetirizine is a second-generation nonsedative antihistaminic agent that has been demonstrated to be safe and effective for treating allergic disease. "( A case of levocetirizine-induced liver injury.
Cho, JY; Jung, MC; Kim, JK; Kim, SE; Lee, B; Park, JW; Seo, J; Song, JW, 2016
)
1.35
"Cetirizine is a piperazine derivative related to the first generation H(1) antagonist hydroxyzine, and is the major metabolite in the blood circulation after hydroxyzine administration in humans."( Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Chen, C, 2008
)
1.28
"Cetirizine (Zyrtec) is a potent and long-acting second-generation histamine H1- receptor antagonist for the treatment of allergic disease, such as allergic rhinitis and chronic idiopathic urticaria, in adult and child. "( The comparison of cetirizine, levocetirizine and placebo for the treatment of childhood perennial allergic rhinitis.
Ku, MS; Lee, CF; Lu, KH; Lue, KH; Sun, HL, 2009
)
2.13
"Levocetirizine (LCZ) is a second-generation antihistamine that was approved in January 2008 for the relief of symptoms of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR), and chronic idiopathic urticaria (CIU) in adults and children aged > or = 6 years."( Levocetirizine for the treatment of allergic rhinitis and chronic idiopathic urticaria in adults and children.
Borja-Hart, N; Ghin, HL; Perez, A; Robles, GI; Singh-Franco, D, 2009
)
1.47
"Cetirizine is an antihistaminic drug used to prevent and treat allergic conditions. "( Enantioseparation of cetirizine by chromatographic methods and discrimination by 1H-NMR.
Salama, NN; Taha, EA; Wang, S, 2009
)
2.11
"Cetirizine is a metabolite of hydroxyzine, another antihistamine."( Cetirizine and loratadine: minimal risk of QT prolongation.
, 2010
)
2.52
"Cetirizine is a second-generation histamine H1-receptor antagonist used in the treatment of allergic diseases. "( Murine chronotoxicity to the antiallergic agent, cetirizine.
Boughattas, NA; Dridi, D; Mansour, HB, 2011
)
2.07
"Cetirizine is a nonsedating, selective H1-receptor antagonist, whose therapeutic efficacy is probably the result of its effect on both the immediate allergic reaction and the late-phase allergic response."( Cetirizine modulates adhesion molecule expression in a double-blind controlled study conducted in psoriatic patients.
Caproni, M; Fabbri, P; Floriani, I; Pestelli, E, 2003
)
2.48
"Levocetirizine 5 mg/day is an effective and well-tolerated treatment of PAR. "( Levocetirizine is effective for symptom relief including nasal congestion in adolescent and adult (PAR) sensitized to house dust mites.
Potter, PC, 2003
)
1.44
"Cetirizine hydrochloride is an orally-active and selective histamine (H(1))-receptor antagonist. "( Review of cetirizine hydrochloride for the treatment of allergic disorders.
Dinakar, C; Portnoy, JM, 2004
)
2.17
"Cetirizine is a selective, second-generation histamine H1 receptor antagonist, with a rapid onset, a long duration of activity and low potential for interaction with drugs metabolised by the hepatic cytochrome P450 system. "( Cetirizine: a review of its use in allergic disorders.
Curran, MP; Perry, CM; Scott, LJ, 2004
)
3.21
"Levocetirizine is a new single-isomer antihistamine with a proven efficacy on chronic urticaria as documented in two recent clinical studies, which have included effectiveness and quality of life assessments."( Chronic urticaria: clinical aspects and focus on a new antihistamine, levocetirizine.
Kapp, A; Wedi, B,
)
0.84
"Cetirizine is a second generation histamine H(1) receptor antagonist used to provide symptomatic relief of allergic signs caused by histamine release. "( [Circadian rhythms in the toxic effects of the histamine antagonist cetirizine in mice].
Ben Attia, M; Boughattas, NA; Dridi, D; Reinberg, A, 2005
)
2.01
"Levocetirizine is a potent and highly selective H1-antihistamine with a proven efficacy in adults."( Levocetirizine in children: evidenced efficacy and safety in a 6-week randomized seasonal allergic rhinitis trial.
Alt, R; Billard, E; de Blic, J; Pujazon, MC; Wahn, U, 2005
)
1.37
"Levocetirizine is an antihistamine with high affinity and selectivity for H1-receptors, which exhibits an excellent benefit/risk ratio in the treatment of allergic rhinitis and urticaria. "( Levocetirizine in 1-2 year old children: pharmacokinetic and pharmacodynamic profile.
Cranswick, N; Fuchs, M; Hulhoven, R; Turzíkova, J, 2005
)
1.44
"Levocetirizine is an antihistamine from the latest generation approved for CIU."( Levocetirizine is an effective treatment in patients suffering from chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled, parallel, multicenter study.
Kapp, A; Pichler, WJ, 2006
)
1.37
"Levocetirizine (Xyzal) is a selective, potent, oral histamine H(1) receptor antagonist of the latest generation that is licensed for the symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis [PER]) and chronic idiopathic urticaria (CIU). "( Levocetirizine: a review of its use in the management of allergic rhinitis and skin allergies.
Hair, PI; Scott, LJ, 2006
)
1.45
"Cetirizine is a second-generation nonsedating antihistamine used to treat allergic disease of respiratory system, skin and eyes."( Stereoselective regulation of MDR1 expression in Caco-2 cells by cetirizine enantiomers.
He, Y; Shen, S; Zeng, S, 2007
)
1.3
"Levocetirizine is a welcome new treatment option in the United States for symptomatic treatment of AR and CIU."( Levocetirizine: The latest treatment option for allergic rhinitis and chronic idiopathic urticaria.
Dubuske, LM,
)
1.17
"Levocetirizine is an effective and safe treatment for use in adults and children with allergic disease."( A review of the role of levocetirizine as an effective therapy for allergic disease.
Walsh, GM, 2008
)
1.2
"Cetirizine is a highly sensitive H1 antihistamine with particular antiallergic properties, which has been shown to be effective in the treatment of allergic rhinitis, urticaria, and hay-fever-associated asthma."( Effect of cetirizine, a new H1 antihistamine, on the early and late allergic reactions in a bronchial provocation test with allergen.
Leuenberger, P; Pécoud, A; Wasserfallen, JB, 1993
)
2.13
"Cetirizine 10 mg daily is an effective treatment in dermographic urticaria, and its usefulness will depend on the prevalence of unwanted effects."( The effect of cetirizine on symptoms and wealing in dermographic urticaria.
Sharpe, GR; Shuster, S, 1993
)
1.37
"Cetirizine is a potent, selective H1 histamine receptor antagonist. "( Effect of oral and inhaled cetirizine in allergen induced bronchoconstriction.
de Vos, C; Ghosh, SK; Patel, KR; Rafferty, P, 1993
)
2.03
"Cetirizine is an antiallergic drug that can reduce both inflammatory infiltrate and ICAM-I expression induced by allergen-specific conjunctival challenge."( Cetirizine reduces ICAM-I on epithelial cells during nasal minimal persistent inflammation in asymptomatic children with mite-allergic asthma.
Canonica, GW; Ciprandi, G; Cozzani, S; Fasce, L; Grimaldi, I; Pronzato, C; Tosca, MA, 1996
)
2.46
"Cetirizine is a new antihistamine with greater selectivity for the histamine H1 receptor and a low rate of hepatic metabolism. "( Comparative study of cetirizine and terfenadine versus placebo in the symptomatic management of seasonal allergic rhinitis.
Dockhorn, R; Grossman, J; Lockey, RF; Lumry, W; Mitchell, DQ; Widlitz, MD; Woehler, T, 1996
)
2.06
"Cetirizine is an H1-receptor antagonist used in the treatment of allergic symptoms."( Cetirizine exerts anti-inflammatory effects on human neutrophils.
Hilger, RA; Köller, M; König, W; Rihoux, JP, 1996
)
2.46
"Cetirizine is an effective drug against mosquito bites by decreasing wealing and also the size and pruritus of the delayed bite papules."( Effect of cetirizine on the inflammatory cells in mosquito bites.
Karppinen, A; Palosuo, T; Rantala, I; Reunala, T; Vaalasti, A, 1996
)
1.42
"Cetirizine is a non-sedating H1 antihistamine which is effective in the treatment of allergic rhinitis and urticaria. "( A comparison of the effects of oral cetirizine and inhaled beclomethasone on early and late asthmatic responses to allergen and the associated increase in airways hyperresponsiveness.
Bentley, AM; De Vos, C; Durham, SR; Hanotte, F; Walker, S, 1996
)
2.01
"Cetirizine is an example of choice of this strategy."( [Can one adjust the distribution of a drug in an organism to its target sites? The example of antihistaminics (anti-H1) and cetirizine].
Albengres, E; Tillement, JP, 1996
)
1.22
"Cetirizine is an antihistamine that inhibits in vivo eosinophil influx into the inflamed airways following allergen challenge, and in vitro eosinophil chemotaxis and adhesion. "( Inhibitory effect of cetirizine on cytokine-enhanced in vitro eosinophil survival.
Busse, WW; Sedgwick, JB, 1997
)
2.06
"Cetirizine is an antihistamine, largely used in the treatment of allergic rhinoconjunctivitis, which also exerts anti-allergic activity."( Cetirizine treatment of rhinitis in children with pollen allergy: evidence of its antiallergic activity.
Bagnasco, M; Canonica, GW; Ciprandi, G; Passalacqua, G; Ricca, V; Riccio, AM; Tosca, M, 1997
)
3.18
"Cetirizine is a new H-receptor antagonist usually used as anti-inflammatory and allergy suppression medication."( [Cetirizine improves the resistance of airway and pulmonary function in patients with asthma].
He, T; Luo, Y; Wang, Z; Yuan, Y; Zeng, J, 1996
)
1.93
"Cetirizine is an antihistamine used in the treatment of allergic rhinoconjunctivitis, that has antiallergic activity."( Continuous versus on demand treatment with cetirizine for allergic rhinitis.
Canonica, GW; Ciprandi, G; Mincarini, M; Passalacqua, G; Ricca, V, 1997
)
2
"Cetirizine is a H1 histamine antagonist which possesses anti-inflammatory properties through inhibition of leucocyte recruitment and activation, and reduction of ICAM-1 expression on mucosal epithelial cells. "( Cetirizine and hydrocortisone differentially regulate ICAM-1 expression and chemokine release in cultured human keratinocytes.
Albanesi, C; Fanales-Belasio, E; Girolomoni, G; Pastore, S, 1998
)
3.19
"Cetirizine is a newer once-daily selective H1-antagonist."( Cetirizine, loratadine, or placebo in subjects with seasonal allergic rhinitis: effects after controlled ragweed pollen challenge in an environmental exposure unit.
Briscoe, M; Day, JH; Widlitz, MD, 1998
)
2.46
"Cetirizine is a commonly used non-sedating antihistamine for the symptomatic relief of allergic reactions. "( [Accidental cetirizine poisoning in a four-year-old boy].
Feilberg Jørgensen, NH; Hansen, JJ, 1998
)
2.12
"Cetirizine is a potent H1-receptor antagonist and has anti-inflammatory properties."( Impact of cetirizine on the burden of allergic rhinitis.
Grant, JA; Meltzer, EO, 1999
)
1.43
"Cetirizine is a safe second generation antihistamine. "( Use of cetirizine in dermatologic disorders.
Henz, BM; Zuberbier, T, 1999
)
2.2
"Cetirizine is a highly efficacious and long-acting second-generation H1-receptor antagonist for the treatment of allergic diseases, such as allergic rhinitis and chronic idiopathic urticaria, in adults and children. "( A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers.
Baltes, E; De Vos, C; Devalia, JL; Hanotte, F, 2001
)
2
"Levocetirizine (5 mg) is a potent inhibitor of the effects of histamine in human skin with an efficacy that exceeded that of loratadine (10 mg) when single doses of the drugs were administered 4 h before the test."( Comparison of the effects of levocetirizine and loratadine on histamine-induced wheal, flare, and itch in human skin.
Boutsiouki, P; Church, MK; Clough, GF, 2001
)
1.15
"Cetirizine is a selective H1 antagonist that inhibits the eosinophil recruitment induced by allergen in the skin."( Inhibitory effect of cetirizine on the bronchial eosinophil recruitment induced by allergen inhalation challenge in allergic patients with asthma.
Chanez, P; Clauzel, AM; De Vos, C; Godard, P; Michel, FB; Rédier, H; Rifaï, N, 1992
)
1.32
"Cetirizine is a new H1 antagonist with potent inhibitory action against the infiltration of eosinophils into involved tissue, thereby affecting the late-phase reaction."( Cetirizine: a new H1 antagonist with antieosinophilic activity in chronic urticaria.
Townley, RG, 1991
)
2.45
"Cetirizine is a new selective H1-antagonist. "( Effect of cetirizine in a conjunctival provocation test with allergens.
Pécoud, AR; Schoeneich, M, 1990
)
2.12
"Cetirizine is a major metabolite of hydroxyzine that has little anticholinergic activity and causes significantly less sedation."( Perennial allergic rhinitis: clinical efficacy of a new antihistamine.
Berman, BA, 1990
)
1
"Cetirizine is a new anti-allergic compound with a potent, long-acting, and specific antihistaminic property. "( Inhibition of human eosinophil chemotaxis and of the IgE-dependent stimulation of human blood platelets by cetirizine.
Capron, A; Capron, M; De Vos, C; Joseph, M; Leprevost, C; Tomassini, M; Vorng, H, 1989
)
1.93
"Cetirizine is an exception, with values of 0.8 L/kg and 0.5 mL/min/kg."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.99
"Cetirizine is a potent, selective H1 antagonist recently made available for investigation. "( Cetirizine inhibition of histamine-induced bronchospasm.
Brik, A; Gong, H; Tashkin, DP, 1987
)
3.16

Effects

Cetirizine has a significant bronchodilatory effect in patients with mild-to-moderate asthma. It is rapidly and extensively absorbed, minimally metabolized, and has a lower volume of distribution (V(d) than some other second-generation antihistamines.

Cetirizine has proved effective in the treatment of seasonal and perennial allergic rhinitis and urticaria. It has a significant bronchodilatory effect in patients with mild-to-moderate asthma and can be used to treat concomitant conditions.

ExcerptReferenceRelevance
"Levocetirizine has a favorable pharmacokinetic profile; it is rapidly and extensively absorbed, minimally metabolized, and has a lower volume of distribution (V(d)) than some other second-generation antihistamines."( Levocetirizine: a new selective H1 receptor antagonist for use in allergic disorders.
Day, JH; Ellis, AK; Rafeiro, E, 2004
)
1.36
"Cetirizine has a significant bronchodilatory effect in patients with mild-to-moderate asthma and can be used to treat concomitant conditions (e.g., allergic rhinitis) without concern that it will interfere with the bronchodilatory effect of albuterol or cause worsening of asthma by itself."( Comparison of the bronchodilatory effects of cetirizine, albuterol, and both together versus placebo in patients with mild-to-moderate asthma.
Corren, J; Katz, RM; Nicodemus, CF; Rachelefsky, GS; Schanker, HM; Siegel, SC; Spector, SL, 1995
)
1.99
"Cetirizine has a low rate of penetration of the blood-brain barrier, and it has minimal central nervous system impairment."( Cetirizine: antiallergic therapy beyond traditional H1 antihistamines.
Samuels, LL; Sheffer, AL, 1990
)
2.44
"Levocetirizine has modest sedative effects with a risk ratio of 1.67 when compared with placebo. "( Sedative Effects of Levocetirizine: A Systematic Review and Meta-Analysis of Randomized Controlled Studies.
Chitsuthipakorn, W; Khattiyawittayakun, L; Seresirikachorn, K; Snidvongs, K, 2017
)
1.32
"Levocetirizine has several pharmacokinetic properties that are desirable for an antihistamine providing a combination of both potency and safety. "( Pharmacokinetic evaluation of levocetirizine.
Ferrer, M, 2011
)
1.21
"Levocetirizine has been shown in observational studies in the west as an effective and satisfactory therapy for patients with allergic respiratory and skin disease. "( An open-label, multicentre study of levocetirizine for the treatment of allergic rhinitis and urticaria in Taiwanese patients.
Fang, SY; Huangs, CY; Lee, JY; Lin, DY; Perng, DW, 2010
)
1.19
"Cetirizine has no preventive effect on nevirapine-associated rash."( Assessment of cetirizine, an antihistamine, to prevent cutaneous reactions to nevirapine therapy: results of the viramune-zyrtec double-blind, placebo-controlled trial.
Allaert, FA; Boukli, N; Caumes, E; David, F; Devidas, A; Dupont, B; Launay, O; Lortholary, O; Patey, O; Piketty, C; Prévoteau du Clary, F; Rey, E; Roudière, L; Tréluyer, JM; Urbinelli, R, 2004
)
1.41
"Levocetirizine has a favorable pharmacokinetic profile; it is rapidly and extensively absorbed, minimally metabolized, and has a lower volume of distribution (V(d)) than some other second-generation antihistamines."( Levocetirizine: a new selective H1 receptor antagonist for use in allergic disorders.
Day, JH; Ellis, AK; Rafeiro, E, 2004
)
1.36
"Cetirizine has been demonstrated able of reducing nasal inflammatory infiltration in children with allergic rhinitis and cytokine production in in vitro studies. "( Cetirizine reduces cytokines and inflammatory cells in children with perennial allergic rhinitis.
Ciprandi, G; Milanese, M; Ricca, V; Tosca, MA, 2004
)
3.21
"Levocetirizine has pharmacodynamically and pharmacokinetically favourable characteristics, including high bioavailability, rapid onset of action, limited distribution and a low degree of metabolism."( Levocetirizine: an update.
Walsh, GM, 2006
)
1.37
"Levocetirizine has high bioavailability, high affinity for and occupancy of the H1 receptor, rapid onset of action, limited distribution and minimal hepatic metabolism. "( A review of the role of levocetirizine as an effective therapy for allergic disease.
Walsh, GM, 2008
)
1.2
"Cetirizine has a significant bronchodilatory effect in patients with mild-to-moderate asthma and can be used to treat concomitant conditions (e.g., allergic rhinitis) without concern that it will interfere with the bronchodilatory effect of albuterol or cause worsening of asthma by itself."( Comparison of the bronchodilatory effects of cetirizine, albuterol, and both together versus placebo in patients with mild-to-moderate asthma.
Corren, J; Katz, RM; Nicodemus, CF; Rachelefsky, GS; Schanker, HM; Siegel, SC; Spector, SL, 1995
)
1.99
"Cetirizine hydrochloride has proved effective in reducing allergic symptoms and can inhibit the infiltration of eosinophils in allergic late-phase responses in the skin. "( Lack of effect of cetirizine on early and late asthmatic response after allergen challenge.
de Bruin-Weller, MS; de Monchy, JG; Rijssenbeek-Nouwens, LH, 1994
)
2.07
"Cetirizine has several antiallergic properties that suggest a potential effect on the development of airway inflammation and asthma in infants with atopic dermatitis."( Allergic factors associated with the development of asthma and the influence of cetirizine in a double-blind, randomised, placebo-controlled trial: first results of ETAC. Early Treatment of the Atopic Child.
, 1998
)
1.25
"Cetirizine has no cardiac toxicity."( Use of cetirizine in dermatologic disorders.
Henz, BM; Zuberbier, T, 1999
)
1.48
"Cetirizine has proved effective in the treatment of seasonal and perennial allergic rhinitis and urticaria."( Cetirizine: antiallergic therapy beyond traditional H1 antihistamines.
Samuels, LL; Sheffer, AL, 1990
)
2.44

Actions

Cetirizine is supposed to inhibit DNA binding activity of NF-kappa B. It inhibits the expression of adhesion molecules on immunocytes and endothelial cells. There is evidence retinoids cause intracranial hypertension.

ExcerptReferenceRelevance
"Cetirizine began to suppress wheal and flare responses at 1 hour (P < .05), with maximum suppression at day 5 (P < .05)."( Reliability of allergy skin testing.
Shtessel, M; Tversky, J, 2018
)
1.2
"Cetirizine can cause oculogyric crisis, especially in the pediatric age group. "( Oculogyric crisis in patients taking cetirizine.
Fraunfelder, FT; Fraunfelder, FW, 2004
)
2.04
"Cetirizine, supposed to inhibit DNA binding activity of NF-kappa B, inhibits the expression of adhesion molecules on immunocytes and endothelial cells and the production of IL-8 and LTB4, two potent chemoattractants, by immune cells."( Cetirizine and allopurinol as novel weapons against cellular autoimmune disorders.
Namazi, MR, 2004
)
2.49
"Cetirizine can cause an oculogyric crisis, and there is strong evidence retinoids cause intracranial hypertension."( Adverse ocular drug reactions recently identified by the National Registry of Drug-Induced Ocular Side Effects.
Fraunfelder, FT; Fraunfelder, FW, 2004
)
1.04

Treatment

Treatment with cetirizine resulted in greater (p < 0.001) improvement in overall RQLQ and individual domain scores as compared with placebo. Treatment did not significantly reduce histamine levels in patients or in controls.

ExcerptReferenceRelevance
"Cetirizine treatment also significantly reduced symptom severity in Italian children with SAR and was safe."( Cetirizine modifies quality of life and symptoms in children with seasonal allergic rhinitis: a pilot study.
Benazzo, M; Ciprandi, G; Corsico, A; Leonardi, S; Licari, A; Marseglia, GL; Miraglia Del Giudice, M; Peroni, D; Salpietro, C, 2020
)
2.72
"Levocetirizine treatment also correlated with a significant increase in the percentage of CD4+CD25+ T cells (P<0.001)."( Levocetirizine modulates lymphocyte activation in patients with allergic rhinitis.
Arifhodzic, N; Haines, D; Mahmoud, F; Novotney, L, 2008
)
1.38
"Cetirizine as an initial treatment for chronic urticaria appears effective and safe."( Evaluation of cetirizine hydrochloride-based therapeutic strategy for chronic urticaria.
Ando, K; Azumi, T; Hirai, S; Kamiya, S; Kondo, T; Masaki, S; Mori, T; Nitta, Y; Sugiura, K; Suzuki, T; Tomita, Y; Usuda, T; Yokoi, T, 2008
)
1.43
"Levocetirizine treatment inhibited the HRV-induced increase in ICAM-1 mRNA and protein levels, as well as the HRV-induced expression of IL-6 and IL-8 mRNA and protein levels."( Levocetirizine inhibits rhinovirus-induced ICAM-1 and cytokine expression and viral replication in airway epithelial cells.
Jang, YJ; Kim, JS; Kwon, HJ; Lee, BJ; Wang, JH; Yeo, NK, 2009
)
1.39
"Levocetirizine treatment showed no side effects on salivary glands function."( Evaluation by (99m)Tc-pertechnetate scintigraphy of the effect of levocetirizine on salivary glands function, in allergic rhinitis patients.
Kursad Ayan, A; Sahin, A; Seven, B; Sutbeyaz, Y; Ucuncu, H; Varoglu, E; Yoruk, O,
)
0.85
"Cetirizine-treated patients reported significantly greater improvement in overall HRQL (P < 0.001) and in each of the seven domains of the RQLQ at all time-points (P < 0.05 to < 0.001) than the placebo group."( The health-related quality of life effects of once-daily cetirizine HCl in patients with seasonal allergic rhinitis: a randomized double-blind, placebo-controlled trial.
Champan, D; Greos, L; Kramer, B; Leidy, NK; Nayak, A; Noonan, MJ; Olufade, AO; Raphael, GD, 2003
)
1.29
"Cetirizine-continuously-treated group showed a significant lower incidence of new sensitisations (p = 0.002)."( Long-term cetirizine treatment may reduce new sensitisations in allergic children: a pilot study.
Ciprandi, G; Frati, F; Marcucci, F; Milanese, M; Sensi, L; Tosca, MA, 2003
)
1.44
"Levocetirizine treatment induced significant symptom relief (P=0.0009) and improved nasal airflow (P=0.038). "( Levocetirizine improves nasal obstruction and modulates cytokine pattern in patients with seasonal allergic rhinitis: a pilot study.
Ciprandi, G; Cirillo, I; Tosca, MA; Vizzaccaro, A, 2004
)
1.44
"Cetirizine treatment induced a significant decrease of IL4 (p<0.01) and IL8 levels (p=0.01)."( Cetirizine reduces cytokines and inflammatory cells in children with perennial allergic rhinitis.
Ciprandi, G; Milanese, M; Ricca, V; Tosca, MA, 2004
)
2.49
"Levocetirizine treatment induced: significant symptom relief (p<0.001), improved nasal airflow (p<0.001), reduction of reversibility percentage (p<0.05), and increase of total airflow after decongestion test (p<0.03). "( Levocetirizine improves nasal symptoms and airflow in patients with persistent allergic rhinitis: a pilot study.
Ciprandi, G; Cirillo, IG; Tosca, MA; Vizzaccaro, A, 2005
)
1.44
"Cetirizine-D treatment was also associated with significantly improved Asthma Quality of Life Questionnaire overall scores."( Comparison of cetirizine-pseudoephedrine and placebo in patients with seasonal allergic rhinitis and concomitant mild-to-moderate asthma: randomized, double-blind study.
Chapman, D; de Guia, EC; Finn, AF; Hewlett, D; Kramer, B; LaForce, C; Nathan, RA; Ratner, P, 2006
)
1.42
"Cetirizine treatment modulated in vivo the expression of adhesion molecules LFA-1/CAM-1 as shown in all cases by decreased levels of their expression on keratinocytes and on dermal endothelial cells (P < 0.001). "( Pharmacologic modulation by cetirizine of some adhesion molecules expression in psoriatic skin lesions.
Caproni, M; Falcos, D; Lotti, T; Palleschi, GM; Papi, C, 1995
)
2.03
"More cetirizine-treated patients (90%) completed the trial than did placebo-treated patients (74%)."( Cetirizine in patients with seasonal rhinitis and concomitant asthma: prospective, randomized, placebo-controlled trial.
Findlay, SR; Glovsky, MM; Grant, JA; Grossman, J; Kaiser, H; Meltzer, EO; Mitchell, DQ; Nicodemus, CF; Pearlman, D; Selner, J, 1995
)
2.19
"Cetirizine-treated children showed a significant reduction (or even total absence) of ICAM-I expression on epithelial cells (p less than 0.002) and a reduction trend in inflammatory cell counts compared with placebo."( Cetirizine reduces ICAM-I on epithelial cells during nasal minimal persistent inflammation in asymptomatic children with mite-allergic asthma.
Canonica, GW; Ciprandi, G; Cozzani, S; Fasce, L; Grimaldi, I; Pronzato, C; Tosca, MA, 1996
)
2.46
"Cetirizine treatment significantly reduced baseline severity of several symptoms of rhinitis (itchy nose, nasal congestion, and watery eyes), and asthma (chest tightness, wheezing, shortness of breath, and nocturnal asthma). "( Evaluation of cetirizine in patients with allergic rhinitis and perennial asthma.
Aaronson, DW, 1996
)
2.1
"Cetirizine treatment had no significant effect on these responses."( Cellular inflammatory responses during immediate, developing, and established late-phase allergic cutaneous reactions: effects of cetirizine.
Atkins, PC; Ciliberti, M; Grossman, S; Moskovitz, A; von Allmen, C; Zweiman, B, 1997
)
1.22
"Cetirizine pretreatment reduced skin wheal and erythema elicited by allergen and PAF, 400 and 40 ng, by 74.6% (p less than 0.001), 53.9% (p less than 0.001), and 47% (p less than 0.01), respectively."( In vivo effects of cetirizine on cutaneous reactivity and eosinophil migration induced by platelet-activating factor (PAF-acether) in man.
Borgnon, A; David, B; Fadel, R; Herpin-Richard, N; Rassemont, R; Rihoux, JP, 1990
)
1.33
"With cetirizine 2 HCl treatment, platelet-activating factor-acether was not detected in chamber media."( Inhibitory effect of oral cetirizine on in vivo antigen-induced histamine and PAF-acether release and eosinophil recruitment in human skin.
Benveniste, J; Burtin, C; De Vos, C; Dubertret, L; Michel, L; Rihoux, JP, 1988
)
1.03
"Treatment with cetirizine significantly reduced histamine and compound 48/80 GWS and LPR compared to baseline; there was no significant difference for DPH. "( Effect of diphenhydramine and cetirizine on immediate and late-phase cutaneous allergic reactions in healthy dogs: a randomized, double-blinded crossover study.
Banovic, F; Blubaugh, A; Denley, T; Lemo, N; Papich, MG; Scheibe, I, 2020
)
1.2
"Treatment with cetirizine may be associated with a decreased risk of recurrence."( Eosinophilic keratitis in 46 eyes of 27 horses in the Mid-Atlantic United States (2008-2012).
Lassaline-Utter, M; Miller, C; Wotman, KL, 2014
)
0.74
"Treatment with cetirizine resulted in greater (p < 0.001) improvement in overall RQLQ and individual domain scores (activities, sleep, non-nose/eye symptoms, practical problems, nasal symptoms, eye symptoms, emotional), as compared with placebo."( Comprehensive evaluation of cetirizine in the management of seasonal allergic rhinitis: impact on symptoms, quality of life, productivity, and activity impairment.
Bronsky, EA; Chapman, D; Kramer, B; Murray, JJ; Nathan, RA; Olufade, AO,
)
0.76
"Treatment with cetirizine did not significantly reduce histamine levels in patients or in controls."( Plasma serotonin and histamine levels in hemodialysis-related pruritus are not significantly influenced by 5-HT3 receptor blocker and antihistaminic therapy.
Domröse, U; Dunker, N; Gollnick, H; Neumann, KH; Weisshaar, E, 2003
)
0.66
"Treatment with cetirizine-D twice daily significantly reduced rhinitis and asthma symptoms and improved overall asthma quality of life in patients with seasonal AR and concomitant mild-to-moderate asthma."( Comparison of cetirizine-pseudoephedrine and placebo in patients with seasonal allergic rhinitis and concomitant mild-to-moderate asthma: randomized, double-blind study.
Chapman, D; de Guia, EC; Finn, AF; Hewlett, D; Kramer, B; LaForce, C; Nathan, RA; Ratner, P, 2006
)
1.05
"Pretreatment with cetirizine resulted in significantly reduced levels of LTC4."( Effects of antihistamines on inflammatory mediators.
Naclerio, RM, 1993
)
0.61
"Pretreatment with cetirizine blocked the histamine-induced change in nasal patency as measured by both methods."( Acoustic rhinometry compared with posterior rhinomanometry in the measurement of histamine- and bradykinin-induced changes in nasal airway patency.
Austin, CE; Foreman, JC, 1994
)
0.61
"Pretreatment with cetirizine (10 mg orally) reduced the fall in Amin induced by bradykinin, 300 micrograms, but not by bradykinin, 100 micrograms."( The contribution of histamine to the action of bradykinin in the human nasal airway.
Austin, CE; Dear, JW; Foreman, JC; Lund, V; Neighbour, H, 1996
)
0.62
"Pretreatment with cetirizine also has been found to block the augmented sensitivity to methacholine that occurs 24 hours after antigen provocation of the nasal mucosa."( Additional properties of cetirizine, a new H1 antagonist.
Naclerio, RM,
)
0.76

Toxicity

Study was to learn whether the survival and the motor incoordination (ataxia) side effect of cetirizine administration is dosing time-dependent. Incidence of adverse effects was less in the rupatadine group compared with the levocetirzine group.

ExcerptReferenceRelevance
" Adverse events were infrequent and generally mild or moderate in severity."( Assessment of the efficacy and safety of three dose levels of cetirizine given once daily in children with perennial allergic rhinitis.
Jobst, S; Schubert, A; van de Venne, H; van den Wijngaart, W, 1994
)
0.53
" Both drugs were well tolerated and their adverse event profiles were similar."( Comparison of efficacy, safety, and skin test inhibition of cetirizine and astemizole.
Berkowitz, RB; Dockhorn, R; Findlay, S; Howland, WC; Lockey, R; Mitchell, DQ; Woehler, T, 1996
)
0.54
" Major and total symptom complex scores, global efficacy and overall satisfaction, and adverse events were assessed."( Comparative outdoor study of the efficacy, onset and duration of action, and safety of cetirizine, loratadine, and placebo for seasonal allergic rhinitis.
Meltzer, EO; Weiler, JM; Widlitz, MD, 1996
)
0.52
" Both medications were well tolerated, and no serious adverse events occurred during the study."( Efficacy and safety relative to placebo of an oral formulation of cetirizine and sustained-release pseudoephedrine in the management of nasal congestion.
Berger, UE; Burtin, B; Duby, C; Horak, F; Jäger, S; Marks, B; Stübner, UP; Toth, J, 1998
)
0.54
" No serious adverse events occurred, and both regimens were equally well tolerated."( Efficacy and safety relative to placebo of an oral formulation of cetirizine and sustained-release pseudoephedrine in the management of nasal congestion.
Berger, UE; Burtin, B; Duby, C; Horak, F; Jäger, S; Marks, B; Stübner, UP; Toth, J, 1998
)
0.54
"Our objective was to test the hypothesis that cetirizine would be as safe as placebo for long-term use in this population."( Prospective, long-term safety evaluation of the H1-receptor antagonist cetirizine in very young children with atopic dermatitis. ETAC Study Group. Early Treatment of the Atopic Child.
Simons, FE, 1999
)
0.79
" Safety was assessed by using the reports of all adverse events, diary cards, physical examinations, developmental assessments, electrocardiograms, blood hematology and chemistry tests, and urinalyses."( Prospective, long-term safety evaluation of the H1-receptor antagonist cetirizine in very young children with atopic dermatitis. ETAC Study Group. Early Treatment of the Atopic Child.
Simons, FE, 1999
)
0.54
" Most reported symptoms and events were mild and were attributed to intercurrent respiratory or gastrointestinal infections, exacerbations of allergic disorders, or age-related concerns rather than to medication-related adverse effects."( Prospective, long-term safety evaluation of the H1-receptor antagonist cetirizine in very young children with atopic dermatitis. ETAC Study Group. Early Treatment of the Atopic Child.
Simons, FE, 1999
)
0.54
" Safety was assessed according to the spontaneous reporting of adverse events."( Comparison of the efficacy, safety, and onset of action of mizolastine, cetirizine, and placebo in the management of seasonal allergic rhinoconjunctivitis. MIZOCET Study Group.
Attali, P; Ben-Soussen, P; Daele, J; Sabbah, A; Wade, AG, 1999
)
0.54
" These three antihistamines have also been shown safe in special populations, including pediatric and elderly patients."( Safety of second generation antihistamines.
Philpot, EE,
)
0.13
" No serious adverse events were reported."( Controlled comparison of the efficacy and safety of cetirizine 10 mg o.d. and fexofenadine 120 mg o.d. in reducing symptoms of seasonal allergic rhinitis.
Burtin, B; De Vos, C; Donnelly, F; Horak, F; Kavina, A; Stübner, P; Zieglmayer, R, 2001
)
0.56
" No clinically relevant adverse events were recorded."( Efficacy and safety of an oral formulation of cetirizine and prolonged-release pseudoephedrine versus xylometazoline nasal spray in nasal congestion.
Berger, UE; Burtin, B; Horak, F; Marks, B; Stübner, UP; Toth, J, 2001
)
0.57
"7%) and other adverse events were more frequent with the highest dose."( Efficacy and safety of levocetirizine in seasonal allergic rhinitis.
Arendt, C; Leynadier, F; Mees, K; Pinelli, ME, 2001
)
0.61
" No differences in all-cause or treatment-related adverse events were observed between the cetirizine- and placebo-treated groups."( Safety of cetirizine in infants 6 to 11 months of age: a randomized, double-blind, placebo-controlled study.
Catuogno, J; Chapman, D; Olufade, AO; Portnoy, JM; Silas, P; Simons, FE, 2003
)
0.94
"To report recent ocular adverse drug reactions identified by the National Registry of Drug-Induced Ocular Side Effects."( Adverse ocular drug reactions recently identified by the National Registry of Drug-Induced Ocular Side Effects.
Fraunfelder, FT; Fraunfelder, FW, 2004
)
0.32
"Case reports from the National Registry and the World Health Organization were collected and adverse drug reactions categorized as follows: certain, probable/likely, possible, unlikely, and conditional/unclassifiable."( Adverse ocular drug reactions recently identified by the National Registry of Drug-Induced Ocular Side Effects.
Fraunfelder, FT; Fraunfelder, FW, 2004
)
0.32
"Recent reports to the National Registry have led to identification of new ocular adverse drug reactions."( Adverse ocular drug reactions recently identified by the National Registry of Drug-Induced Ocular Side Effects.
Fraunfelder, FT; Fraunfelder, FW, 2004
)
0.32
" Safety was assessed on routine laboratory assays and recording vital signs and adverse events (AEs)."( Clinical study of the therapeutic efficacy and safety of emedastine difumarate versus cetirizine in the treatment of seasonal allergic rhinitis.
Assandri, A; Corrado, ME; Horak, F; Kavina, A; Mion, A; Stübner, P; Zieglmayer, R, 2004
)
0.55
" Moreover, based on the results of this study, emedastine can be considered a safe and well-tolerated drug and its safety profile seems to resemble that of cetirizine."( Clinical study of the therapeutic efficacy and safety of emedastine difumarate versus cetirizine in the treatment of seasonal allergic rhinitis.
Assandri, A; Corrado, ME; Horak, F; Kavina, A; Mion, A; Stübner, P; Zieglmayer, R, 2004
)
0.74
" The aim of the study was to learn whether the survival and the motor incoordination (ataxia) side effect of cetirizine administration is dosing time-dependent."( [Circadian rhythms in the toxic effects of the histamine antagonist cetirizine in mice].
Ben Attia, M; Boughattas, NA; Dridi, D; Reinberg, A, 2005
)
0.78
" Incidence of treatment-emergent adverse events was similar in both groups (33."( Levocetirizine in children: evidenced efficacy and safety in a 6-week randomized seasonal allergic rhinitis trial.
Alt, R; Billard, E; de Blic, J; Pujazon, MC; Wahn, U, 2005
)
0.89
"01), and the frequency of adverse events did not differ significantly from those seen in the placebo group."( Efficacy and safety of levocetirizine on symptoms and health-related quality of life of children with perennial allergic rhinitis: a double-blind, placebo-controlled randomized clinical trial.
Potter, PC, 2005
)
0.63
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Safety was assessed by: reporting of adverse events, numbers of children discontinuing the study because of adverse events, height and body mass measurements, assessment of developmental milestones, and hematology and biochemistry tests."( Safety of levocetirizine treatment in young atopic children: An 18-month study.
Simons, FE, 2007
)
0.7
" There were 27 adverse events, no serious adverse events in 177 patients during experimental period."( [Efficacy and safety of Mizolastine in the treatment of perennial allergic rhinitis].
Ding, J; Huang, Z; Wang, H; Zheng, C; Zhou, S, 2007
)
0.34
"This prospective observational study on cetirizine in pregnancy suggests that the use of cetirizine is relatively safe during the first trimester."( The safety of cetirizine during pregnancy. A prospective observational cohort study.
Schaefer, C; Weber-Schoendorfer, C, 2008
)
0.97
" 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
)
0.6
" 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
)
0.6
" 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
)
0.92
"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
)
0.6
" Second-generation antihistamines have become increasingly popular because of their comparable efficacy and lower incidence of adverse effects relative to their first-generation counterparts, and the safety and efficacy of this drug class are established in the adult population."( Treatment of allergic rhinitis in infants and children: efficacy and safety of second-generation antihistamines and the leukotriene receptor antagonist montelukast.
Moeller, ML; Nahata, MC; Phan, H, 2009
)
0.35
" Overall incidence of treatment-emergent adverse events was 14."( Efficacy and safety of levocetirizine in improving symptoms and health-related quality of life in US adults with seasonal allergic rhinitis: a randomized, placebo-controlled study.
Gawchik, S; Georges, G; Haeusler, JM; Segall, N, 2010
)
0.66
" Secondary end-points were the rate of control of chronic cough at each step of therapy, the duration of treatment required, changes in cough symptom score, health-related quality of life and possible adverse effects."( Efficacy and safety of modified sequential three-step empirical therapy for chronic cough.
Li, X; Liang, S; Liu, B; Lü, H; Qiu, Z; Wang, L; Wang, Y; Wei, W; Yu, L, 2010
)
0.36
" Incidence of adverse effects was less in the rupatadine group compared with the levocetirizine group."( Rupatadine and levocetirizine for seasonal allergic rhinitis: a comparative study of efficacy and safety.
Allala, U; Jaida, J; Maiti, R; Palani, A; Rahman, J, 2010
)
0.91
" Safety evaluations included treatment-emergent adverse events (TEAEs), vital signs, electrocardiographic (ECG) assessments, and laboratory tests."( Safety and tolerability of levocetirizine dihydrochloride in infants and children with allergic rhinitis or chronic urticaria.
Haeusler, JM; Hampel, F; Ratner, P,
)
0.42
" Due to the adverse effects of these treatments, new drugs like leukotriene receptor antagonists are being investigated for the treatment of allergic rhinitis."( Efficacy and safety of montelukast add-on therapy in allergic rhinitis.
Badyal, DK; Modgill, V; Verghese, A, 2010
)
0.36
" The first-generation H(1)-antihistamines are associated with marked adverse effects such as sedation, sleepiness/drowsiness as well as difficulties in learning and cognitive processing; thus, they are recommended for limited or discontinued use in children with AR or CIU."( Evidence for clinical safety, efficacy, and parent and physician perceptions of levocetirizine for the treatment of children with allergic disease.
Kurzawa, R; Pampura, AN; Papadopoulos, NG; Spičák, V, 2011
)
0.59
" They are mostly presented in the group of mood stabilizers and antiepileptic drugs, particularly the carbamazepine and lamotrigine, and can be manifested through the Stevens Johnson syndrome, Toxic Epidermal Necrolysis (TEN)/Lyell's syndrome with about 30% lethality."( Exanthema medicamentosum as a side effect of promazine.
Cvitanović, MZ; Hlevnjak, I; Lasić, D; Uglešić, B; Višić, V, 2011
)
0.37
" 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
)
0.63
" The overall incidence of adverse drug reactions was also found to be less in rupatadine group."( Rupatadine and levocetirizine in chronic idiopathic urticaria: a comparative study of efficacy and safety.
Ahmed, I; Goud, P; Jaida, J; Maiti, R; Palani, A; Raghavendra, BN, 2011
)
0.7
"The physicochemical properties of racemates and stereoisomers of medicines can differ significantly, and this may affect the side-effect profile in addition to the pharmacokinetics and intended pharmacology."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
"This is a study to investigate the profile of adverse drug reactions of racemic and enantiomeric forms of drugs."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
" A case-noncase approach was used to measure the disproportionality of combination between adverse drug reaction (ADR) and exposure to drug."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
" Routine hematological and biochemical tests and treatment-emergent adverse events were monitored for safety."( Olopatadine versus levocetirizine in chronic urticaria: an observer-blind, randomized, controlled trial of effectiveness and safety.
Bagchi, C; Chaudhuri, A; Das, NK; Hazra, A; Islam, CN; Sil, A; Tripathi, SK, 2013
)
0.7
" Adverse event profiles were comparable with sedation being the commonest complaint."( Olopatadine versus levocetirizine in chronic urticaria: an observer-blind, randomized, controlled trial of effectiveness and safety.
Bagchi, C; Chaudhuri, A; Das, NK; Hazra, A; Islam, CN; Sil, A; Tripathi, SK, 2013
)
0.7
"Olopatadine is a safe and more effective alternative to levocetirizine in the treatment of CU."( Olopatadine versus levocetirizine in chronic urticaria: an observer-blind, randomized, controlled trial of effectiveness and safety.
Bagchi, C; Chaudhuri, A; Das, NK; Hazra, A; Islam, CN; Sil, A; Tripathi, SK, 2013
)
0.94
" The objective was to measure the rate of adverse pregnancy outcomes."( The fetal safety of cetirizine: an observational cohort study and meta-analysis.
Boskovic, R; Djokanovic, N; Etwel, F; Koren, G; Martinovic, J; Moretti, ME, 2014
)
0.73
"Fumaric acid esters (FAEs) are considered an effective and safe long-term treatment for psoriasis."( Addition of an oral histamine antagonist to reduce adverse events associated with fumaric acid esters in the treatment of psoriasis: a randomized double-blind placebo-controlled trial.
Balak, DM; Fallah-Arani, S; Neumann, HA; Thio, HB; Venema, CM, 2015
)
0.42
"To assess whether the addition of cetirizine, an oral histamine-1 receptor antagonist, to FAEs would reduce the incidence of adverse events."( Addition of an oral histamine antagonist to reduce adverse events associated with fumaric acid esters in the treatment of psoriasis: a randomized double-blind placebo-controlled trial.
Balak, DM; Fallah-Arani, S; Neumann, HA; Thio, HB; Venema, CM, 2015
)
0.7
" Primary outcomes were the incidence of adverse events and the proportion of patients discontinuing treatment."( Addition of an oral histamine antagonist to reduce adverse events associated with fumaric acid esters in the treatment of psoriasis: a randomized double-blind placebo-controlled trial.
Balak, DM; Fallah-Arani, S; Neumann, HA; Thio, HB; Venema, CM, 2015
)
0.42
" Addition of cetirizine did not reduce the incidence of adverse events compared with placebo (84% vs."( Addition of an oral histamine antagonist to reduce adverse events associated with fumaric acid esters in the treatment of psoriasis: a randomized double-blind placebo-controlled trial.
Balak, DM; Fallah-Arani, S; Neumann, HA; Thio, HB; Venema, CM, 2015
)
0.79
"Addition of oral cetirizine 10 mg once daily to FAE treatment did not reduce adverse events in patients with psoriasis during the first 12 weeks of treatment."( Addition of an oral histamine antagonist to reduce adverse events associated with fumaric acid esters in the treatment of psoriasis: a randomized double-blind placebo-controlled trial.
Balak, DM; Fallah-Arani, S; Neumann, HA; Thio, HB; Venema, CM, 2015
)
0.76
"5%) from Group B had some type of adverse effect (p = 1."( Safety and efficacy of cetirizine versus cetirizine plus ranitidine in chronic urticaria: Double-blind randomized placebo-controlled study.
Bonilla-Lopez, S; Guevara-Gutierrez, E; Hernández-Arana, S; Tlacuilo-Parra, A, 2015
)
0.73
"Bleomycin induced flagellate dermatitis is an uncommon and unique adverse effect."( Bleomycin induced flagellate erythema in a patient with thalamic mixed germ cell tumour: Report of a rare adverse effect.
Biswas, A; Julka, PK, 2016
)
0.43
" Thus, this study confirmed that cetirizine induces toxic effects in Mytilus galloprovincialis, which, considering their trophic relevance, wide use as bioindicator and wide spatial distribution of this species, can result in ecological and economic negative impacts at a large scale."( Toxic effects of the antihistamine cetirizine in mussel Mytilus galloprovincialis.
Almeida, Â; Calisto, V; Esteves, VI; Figueira, E; Freitas, R; Schneider, RJ; Soares, AM; Teixeira, M; Wrona, FJ, 2017
)
1.01
" The objective of this study was to evaluate the impact of antihistamines upon adverse effects following ALA-PDT."( A randomized, double-blind, placebo-controlled clinical trial evaluating the role of systemic antihistamine therapy for the reduction of adverse effects associated with topical 5-aminolevulinic acid photodynamic therapy.
Goldman, MP; Jones, IT; Vanaman Wilson, MJ; Wu, DC, 2017
)
0.46
"We selected adverse drug reaction (ADR) reports on H1-antihistamines in children (0-16 years) up to June 2014 from VigiBase."( Safety profile of H1-antihistamines in pediatrics: an analysis based on data from VigiBase.
Biagi, C; Calamelli, E; Cipriani, F; Donati, M; Melis, M; Monaco, L; Motola, D; Ricci, G; Vaccheri, A, 2017
)
0.46
" Routine hematological and biochemical tests and treatment-emergent adverse events were monitored for safety."( Effectiveness and safety of levocetirizine 10 mg versus a combination of levocetirizine 5 mg and montelukast 10 mg in chronic urticaria resistant to levocetirizine 5 mg: A double-blind, randomized, controlled trial.
Das, NK; Ghosh, C; Pal, S; Sarkar, TK; Sil, A,
)
0.41
" The results suggest that CTZ exposure is not associated with adverse pregnancy outcomes above the background rates."( Safety of cetirizine in pregnancy.
Bentz, JWG; Boev, R; Cooney, M; Golembesky, A; Schlit, AF, 2018
)
0.88
"The fixed-dose combination of montelukast and levocetirizine was effective and safe in treating perennial allergic rhinitis in patients with asthma compared with montelukast alone."( A Randomized, Multicenter, Double-blind, Phase III Study to Evaluate the Efficacy on Allergic Rhinitis and Safety of a Combination Therapy of Montelukast and Levocetirizine in Patients With Asthma and Allergic Rhinitis.
Chang, YS; Cho, YJ; Cho, YS; Choi, BW; Chung, JH; Jee, YK; Jo, EJ; Jung, J; Kim, HK; Kim, MK; Kim, SH; Lee, BJ; Lee, JM; Lee, SK; Lee, SY; Park, CS; Park, HS; Park, HW; Park, JW; Yoo, KH; Yoon, HJ, 2018
)
0.93
" No adverse effects were reported."( Efficacy and Safety of Omalizumab (Xolair) for Cholinergic Urticaria in Patients Unresponsive to a Double Dose of Antihistamines: A Randomized Mixed Double-Blind and Open-Label Placebo-Controlled Clinical Trial.
Azofra, J; Baeza, ML; Beristain, A; Brescó, MS; Donado, CD; Echechipía, S; Ferrer, M; Gaig, P; García, BE; Gastaminza, G; Labrador-Horrillo, M; Nunez-Cordoba, JM; Quiñones, D; Sala-Cunill, A; Zubeldia, JM,
)
0.13
" 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
)
0.8
" Newer-generation AHs are associated with fewer adverse effects compared with first-generation AHs."( Newer-generation antihistamines and the risk of adverse events in children: A systematic review.
Dakoutrou, M; Mavroeidi, IA; Miligkos, M; Pankozidou, Ι; Papaconstadopoulos, I; Papadopoulos, NG; Statha, E; Theochari, NA, 2021
)
0.62
" We searched MEDLINE and CENTRAL, independently extracted data on study population, interventions, adverse events (AEs), and treatment discontinuations, and assessed the methodologic quality of the included RCTs using the Cochrane's risk of bias tool."( Newer-generation antihistamines and the risk of adverse events in children: A systematic review.
Dakoutrou, M; Mavroeidi, IA; Miligkos, M; Pankozidou, Ι; Papaconstadopoulos, I; Papadopoulos, NG; Statha, E; Theochari, NA, 2021
)
0.62
" No obvious adverse reactions were found to be related to probiotic treatment."( Effectiveness and safety of probiotic therapy for pediatric allergic rhinitis management: A systematic review and meta-analysis.
Tan, X; Wang, X; Zhou, J, 2022
)
0.72
"This meta-analysis indicated that probiotic therapy can partially improve pediatric AR outcomes, assisted by modulating immune balance and reducing anti-allergic medication use, without obvious adverse reactions."( Effectiveness and safety of probiotic therapy for pediatric allergic rhinitis management: A systematic review and meta-analysis.
Tan, X; Wang, X; Zhou, J, 2022
)
0.72

Pharmacokinetics

The aim of this study is to assess the bioequivalence of a new generic formulation and the branded formulation of levocetirizine dihydrochloride. Food-intake effect on the pharmacokinetic properties is also evaluated.

ExcerptReferenceRelevance
" The terminal disposition half-life of cetirizine in these patients was 19."( Effect of haemodialysis on the pharmacokinetics of cetirizine.
Awni, WM; Chung, M; Halstenson, CE; Matzke, GR; Opsahl, JA; Yeh, J, 1990
)
0.8
" The mean serum elimination half-life of hydroxyzine was 36."( The pharmacokinetics and pharmacodynamics of hydroxyzine in patients with primary biliary cirrhosis.
Chen, XY; Minuk, GY; Simons, FE; Simons, KJ; Watson, WT, 1989
)
0.28
" The serum elimination half-life values of these agents are variable: a few hours for terfenadine and triprolidine; about 9 hours for cetirizine, azatadine, and loratadine; from 20 to 25 hours for hydroxyzine, chlorpheniramine, and brompheniramine; and from 5 to 14 days for astemizole."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.48
" We found that the elimination half-life of cetirizine was prolonged in patients with mild and moderate renal insufficiency, compared with age-matched individuals with normal renal function (19."( Pharmacokinetics of cetirizine in the elderly and patients with renal insufficiency.
Awni, WM; Chung, M; Halstenson, CE; Matzke, GR; Yeh, J, 1987
)
0.86
" Cmax (362 ng/ml), Tmax (1."( Single dose pharmacokinetics of cetirizine in young and elderly volunteers.
Bernheim, J; Lefebvre, RA; Rosseel, MT, 1988
)
0.56
" In contrast to data obtained in healthy adults with normal hepatic function reported in the medical literature, they found that the mean serum elimination half-life value of cetirizine, 13."( Cetirizine pharmacokinetics and pharmacodynamics in primary biliary cirrhosis.
Minuk, GY; Simons, FE; Simons, KJ; Watson, WT, 1993
)
1.92
" This synergism may be due, at least in part, to a pharmacokinetic effect."( Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria.
Simons, FE; Simons, KJ; Sussman, GL, 1995
)
0.5
" The hydroxyzine and cetirizine half-life and AUC0-->infinity values were significantly increased and the systemic clearance rates were significantly decreased in the presence of cimetidine."( Effect of the H2-receptor antagonist cimetidine, on the pharmacokinetics and pharmacodynamics of the H1-receptor antagonists hydroxyzine and cetirizine in rabbits.
Chen, X; Simons, FE; Simons, KJ, 1994
)
0.81
"A rapid and sensitive high-performance thin-layer chromatography (HPTLC) assay has been developed for the measurement of cetirizine in human plasma and its utility for pharmacokinetic study has been evaluated."( High-performance thin-layer chromatography for the determination of cetirizine in human plasma and its use in pharmacokinetic studies.
Bangaru, RA; Chakravarthy, BK; Gandhi, TP; Modi, IA; Modi, RI; Pandya, KK, 1996
)
0.74
" 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
)
0.55
" This paper reviews the pharmacokinetic properties of these second-generation agents and is intended to provide comparisons that help explain differences in dosing profiles and drug interactions for members of this class of drugs."( Pharmacokinetic overview of oral second-generation H1 antihistamines.
Estes, KS; González, MA, 1998
)
0.3
"Emedastine displays pharmacodynamic properties comparable with cetirizine and therefore qualifies as a safe and alternative compound with H1-receptor antagonist properties."( Pharmacokinetics and pharmacodynamics of the novel H1-receptor antagonist emedastine in healthy volunteers.
Assandri, A; Dallinger, S; Graselli, U; Jansen, B; Kiss, B; Müller, M; Schlagbauer-Wadl, H; Wacheck, V,
)
0.37
" Although there was no recognizable differences in pharmacokinetics between the enantiomers in rat, the method appears to be useful for their pharmacokinetic studies."( Stereoselective determination of cetirizine and studies on pharmacokinetics in rat plasma.
Choi, SO; Choo, HY; Kim, EJ; Kong, HS; Lee, SH, 2000
)
0.59
" Since V/F increased more rapidly with age than CL/F, a nonlinear increase in half-life was seen, from < 4 h in infants to near the adult value at 12 years of age."( Retrospective population pharmacokinetic analysis of cetirizine in children aged 6 months to 12 years.
Aarons, L; de Longueville, M; Hussein, Z; Majid, O; Pitsiu, M; Stockis, A, 2004
)
0.57
" The aim of this study was to evaluate the potential of pharmacokinetic interaction between cetirizine and ritonavir, the most potent cytochrome P450 (CYP) inhibitor."( Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.
Cremieux, AC; Delatour, F; Farinotti, R; Gautran, C; Melac, M; Moulaert, B; Otoul, C; Peytavin, G; Strolin-Benedetti, M, 2005
)
0.8
"An open-label, single-center, one-sequence crossover pharmacokinetic study was conducted in three running periods: cetirizine (CTZ) alone, ritonavir (RTV) alone and then CTZ plus RTV."( Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.
Cremieux, AC; Delatour, F; Farinotti, R; Gautran, C; Melac, M; Moulaert, B; Otoul, C; Peytavin, G; Strolin-Benedetti, M, 2005
)
0.79
" The RTV pharmacokinetic parameter values were not affected by CTZ co-treatment."( Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.
Cremieux, AC; Delatour, F; Farinotti, R; Gautran, C; Melac, M; Moulaert, B; Otoul, C; Peytavin, G; Strolin-Benedetti, M, 2005
)
0.58
"CTZ does not significantly affect the pharmacokinetic parameters of RTV, and the association does not, thus, require a modification of the dosage of the protease inhibitor."( Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.
Cremieux, AC; Delatour, F; Farinotti, R; Gautran, C; Melac, M; Moulaert, B; Otoul, C; Peytavin, G; Strolin-Benedetti, M, 2005
)
0.58
"This study was performed to investigate levocetirizine pharmacokinetic disposition and pharmacodynamics in relation to skin reactivity to histamine in children aged 6 to 11 years."( Levocetirizine: pharmacokinetics and pharmacodynamics in children age 6 to 11 years.
Simons, FE; Simons, KJ, 2005
)
1.15
" It is concluded that estimating in vivo receptor occupancy, which takes into account both the affinity of the drug for the receptor and its free plasma concentration, is a far better predictor for human pharmacodynamics and hence antihistamine potency, than considering in vitro affinity and plasmatic half-life only."( Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines.
Baltes, E; Benedetti, MS; Chatelain, P; Gillard, M, 2005
)
0.33
" A pharmacokinetic model was developed using NONMEM and the differences in pharmacokinetic parameters of levocetirizine and dextrocetirizine were estimated."( Stereoselective pharmacokinetics of cetirizine in the guinea pig: role of protein binding.
Chatelain, P; Gupta, A; Hammarlund-Udenaes, M; Jonsson, EN; Massingham, R, 2006
)
0.82
" The method described herein has been first used to reveal the pharmacokinetic characters in healthy Chinese volunteers treated with oral administration of different dosages of cetirizine dihydrochloride and controlled-released pseudoephedrine hydrochloride compound tablet, and approached the influence of a standard meal on the extent and rate of absorption of the combination tablet."( Development and evaluation of an efficient HPLC/MS/MS method for the simultaneous determination of pseudoephedrine and cetirizine in human plasma: application to phase-I pharmacokinetic study.
Cui, S; Feng, F; Liu, H; Ma, M; Sheng, Y, 2007
)
0.74
" Studies comparing these routes of administration of an antihistamine regarding efficacy and pharmacokinetic profile are lacking."( Clinical efficacy and pharmacokinetic profiles of intranasal and oral cetirizine in a repeated allergen challenge model of allergic rhinitis.
Aldén-Raboisson, M; Andersson, M; Borgå, O; Greiff, L; Korsgren, M; Larsson, L; Malmqvist, U, 2007
)
0.57
" Plasma concentrations of cetirizine were analyzed with a compartmental pharmacokinetic model."( Pharmacokinetics of cetirizine in healthy cats.
Papich, MG; Reinero, CR; Schooley, EK, 2008
)
0.97
" Mean +/- SD terminal half-life was 10."( Pharmacokinetics of cetirizine in healthy cats.
Papich, MG; Reinero, CR; Schooley, EK, 2008
)
0.67
" The half-life of cetirizine in cats is compatible with once-daily dosing, and the extent of protein binding is high."( Pharmacokinetics of cetirizine in healthy cats.
Papich, MG; Reinero, CR; Schooley, EK, 2008
)
1
" The recommended dose of levocetirizine is 5 mg once daily, while its pharmacokinetic half-life is about 7 h in humans."( Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Chen, C, 2008
)
0.85
" Pharmacodynamic studies evaluated the suppressive effect on histamine and anticanine IgE-mediated cutaneous wheal formation."( Hydroxyzine and cetirizine pharmacokinetics and pharmacodynamics after oral and intravenous administration of hydroxyzine to healthy dogs.
Bizikova, P; Olivry, T; Papich, MG, 2008
)
0.69
" Upon this basis, the conflicting literature data of cetirizine microspeciation were clarified, and the pharmacokinetic absorption-distribution properties could be interpreted."( Triprotic acid-base microequilibria and pharmacokinetic sequelae of cetirizine.
Béni, S; Kökösi, J; Kovács, Z; Marosi, A; Noszál, B, 2009
)
0.84
" Cetirizine concentrations in plasma were determined by a validated high performance liquid chromatographic-ultraviolet (HPLC/UV) assay, and pharmacokinetic parameters, Cmax, AUC(0-t), AUC(0-infinity) and t1/2 were calculated from the plasma concentration-time data of each individual and during each period by applying non-compartmental analysis."( Pharmacokinetics and bioequivalence study of two cetirizine hydrochloride formulations in healthy Chinese male volunteers.
Chen, Y; Liu, Y; Tian, Y; Xu, FG; Zhang, ZJ, 2009
)
1.52
"Levocetirizine has several pharmacokinetic properties that are desirable for an antihistamine providing a combination of both potency and safety."( Pharmacokinetic evaluation of levocetirizine.
Ferrer, M, 2011
)
1.21
" The validated method was applied in a pharmacokinetic study to determine the concentration of levocetirizine in plasma samples."( Determination of levocetirizine in human plasma by LC-MS-MS: validation and application in a pharmacokinetic study.
Jithavech, P; Rojsitthisak, P; Sanphanya, K; Vicheantawatchai, P; Wichitnithad, W,
)
0.67
" A joint parent/metabolite population 2-compartment pharmacokinetic model with first-order absorption and elimination was utilized to describe the pharmacokinetics of both compounds."( Pharmacokinetics of hydroxyzine and cetirizine following oral administration of hydroxyzine to exercised Thoroughbred horses.
Flynn, K; Knych, HK; McKemie, DS; Steinmetz, S; Weiner, D, 2019
)
0.79
"The aim of this study is to assess the bioequivalence of a new generic formulation and the branded formulation of levocetirizine dihydrochloride in healthy Chinese volunteers under fasting and fed conditions, and food-intake effect on the pharmacokinetic properties is also evaluated."( The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers.
Chen, XF; Cheng, Y; Fang, LP; Guo, JH; Huang, BL; Lin, BJ; Liu, MB; Qiu, HQ; Que, WC, 2019
)
0.94
"The two formulations demonstrated essentially identical pharmacokinetic profiles and were all well within the FDA/CFDA bioequivalence standards."( The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers.
Chen, XF; Cheng, Y; Fang, LP; Guo, JH; Huang, BL; Lin, BJ; Liu, MB; Qiu, HQ; Que, WC, 2019
)
0.73
" The objective of this study was to compare the pharmacokinetic profiles of a montelukast/levocetirizine fixed-dose combination chewable tablet with individual administration of montelukast and levocetirizine in healthy subjects."( Comparative pharmacokinetics of a montelukast/levocetirizine fixed-dose combination chewable tablet versus individual administration of montelukast and levocetirizine after a single oral administration in healthy Korean male subjects
.
Jung, J; Kim, MG; Kim, YI; Moon, SJ; Yu, KS, 2020
)
1.03
"A total of 22 subjects were included in pharmacokinetic analysis."( Comparative pharmacokinetics of a montelukast/levocetirizine fixed-dose combination chewable tablet versus individual administration of montelukast and levocetirizine after a single oral administration in healthy Korean male subjects
.
Jung, J; Kim, MG; Kim, YI; Moon, SJ; Yu, KS, 2020
)
0.81
"The pharmacokinetic parameters of montelukast and levocetirizine when administered as separate tablets or as a fixed-dose combination were compared, and the parameters met the pharmacokinetic equivalence criteria."( Comparative pharmacokinetics of a montelukast/levocetirizine fixed-dose combination chewable tablet versus individual administration of montelukast and levocetirizine after a single oral administration in healthy Korean male subjects
.
Jung, J; Kim, MG; Kim, YI; Moon, SJ; Yu, KS, 2020
)
1.06
" The aim of the research was to be able to provide detection times (DT) from pharmacokinetic studies in thoroughbred horses to better inform trainers, and their veterinary surgeons, prescribing these substances for treatment of Thoroughbred racehorses."( Plasma and urine pharmacokinetics of hydroxyzine and cetirizine following repeated oral administrations to exercised horses.
Aldurdunji, M; Garth-Greeves, A; Hincks, PR; Muir, T; Paine, SW, 2022
)
0.97

Compound-Compound Interactions

Both levocetirizine and desloratadine in monotherapy, or in combination with montelukast, were effective in reducing wheal and flare in SPT. It is hypothesized that the platelet activating factor receptor antagonist ginkgolide B and the carotenoid antioxidant astaxanthin interact with antihistamines to potentiate their ability to downregulate potentially pathological immune activation.

ExcerptReferenceRelevance
"Present results showed that single oral doses of rupatadine 10 mg in combination with alcohol do not produce more cognitive and psychomotor impairment than alcohol alone."( Evaluation of the cognitive, psychomotor and pharmacokinetic profiles of rupatadine, hydroxyzine and cetirizine, in combination with alcohol, in healthy volunteers.
Antonijoan, R; Barbanoj, MJ; Donado, E; García-Gea, C; Izquierdo, I; Jané, F; Pérez, I; Solans, A, 2006
)
0.55
" Ranitidine modified the absorption of cetirizine enantiomers, suggesting that the potential drug-drug interaction would significantly change the cetirizine pharmacokinetics."( Stereoselective and multiple carrier-mediated transport of cetirizine across Caco-2 cell monolayers with potential drug interaction.
He, Y; Liu, Y; Zeng, S, 2010
)
0.87
"Montelukast alone or in combination with antihistamines gave a gradual increase in nasal symptom improvement within 6 weeks of treatment in patients with persistent AR."( Use of montelukast alone or in combination with desloratadine or levocetirizine in patients with persistent allergic rhinitis.
Barylski, M; Ciebiada, M; Gorska-Ciebiada, M; Gorski, P; Kmiecik, T,
)
0.37
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" It is hypothesized that the platelet activating factor receptor antagonist ginkgolide B (GB) and the carotenoid antioxidant astaxanthin (ASX) interact with antihistamines cetirizine dihydrochloride (CTZ) and azelastine (AZE) to potentiate their ability to downregulate potentially pathological immune activation."( In vitro suppression of lymphocyte activation in patients with seasonal allergic rhinitis and pollen-related asthma by cetirizine or azelastine in combination with ginkgolide B or astaxanthin.
Abal, A; Al-Awadhi, R; Al-Sharah, S; Arifhodzic, N; Azeamouzi, C; Haines, D; Mahmoud, FF; Tosaki, A, 2012
)
0.78
" This study assessed the effect of long-lasting treatment with montelukast alone or in combination with antihistamines on wheal and flare in skin pricks tests (SPT) in patients sensitized to perennial allergens."( Wheal and flare reactions in skin prick tests of patients treated with montelukast alone or in combination with antihistamines.
Barylski, M; Ciebiada, M; Ciebiada, MG, 2014
)
0.4
"Both levocetirizine and desloratadine in monotherapy, or in combination with montelukast, were effective in reducing wheal and flare in SPT."( Wheal and flare reactions in skin prick tests of patients treated with montelukast alone or in combination with antihistamines.
Barylski, M; Ciebiada, M; Ciebiada, MG, 2014
)
0.82
"Levocetirizine dihydrochloride is known to interact with some anti-inflammatory drugs."( In vitro drug interaction of levocetirizine and diclofenac: Theoretical and spectroscopic studies.
Abdel Gaber, SA; Abo Dena, AS, 2017
)
1.29

Bioavailability

Cetirizine exhibits high intestinal absorption in humans and its oral bioavailability is estimated to be greater than 70%. Levocetiriza attenuated the elevated renal levels of TNF-α and TGF-β1, ameliorated renal oxidative stress and restored NO bioavailability in diabetic kidney.

ExcerptReferenceRelevance
" For most of these drugs, the absolute bioavailability is unknown because no intravenous formulations are available for comparative purposes."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.27
"The bioavailability of two tablet formulations of cetirizine (Zetir from Abbott and Zyrtek from UCB) were compared in 14 healthy male volunteers who received a single dose of 10 mg of cetirizine dihydrochloride in an open randomized two-period crossover design with a 7-day washout period between doses."( Comparative bioavailability of single doses of tablet formulations of cetirizine dihydrochloride in healthy male volunteers.
de Nucci, G; Muscará, MN, 1995
)
0.78
" black triangle The bioavailability of cetirizine and pseudoephedrine is similar after administration of cetirizine/pseudoephedrine 5/120 mg bilayer tablets or coadministration of cetirizine 5 mg tablets plus pseudoephedrine sustained-release (SR) 120 mg caplets."( Cetirizine/pseudoephedrine.
Jarvis, B; Wellington, K, 2001
)
2.02
" The absolute bioavailability is 50-65% for mizolastine; it is high for levocetirizine as the percentage of the drug eliminated unchanged in the 48 h urine is 77% of the oral dose; the estimation for fexofenadine is at least 33%; no estimation was found for desloratadine."( Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans.
Benedetti, MS; Diquet, B; Molimard, M, 2004
)
0.78
" The method described herein has been first used to reveal the pharmacokinetic characters in healthy Chinese volunteers treated with oral administration of different dosages of cetirizine dihydrochloride and controlled-released pseudoephedrine hydrochloride compound tablet, and approached the influence of a standard meal on the extent and rate of absorption of the combination tablet."( Development and evaluation of an efficient HPLC/MS/MS method for the simultaneous determination of pseudoephedrine and cetirizine in human plasma: application to phase-I pharmacokinetic study.
Cui, S; Feng, F; Liu, H; Ma, M; Sheng, Y, 2007
)
0.74
" Validation results on linearity, specificity, accuracy, precision and stability, as well as its application to the analysis of plasma samples taken up to 48h after oral administration of 5mg of levocetirizine dichloridrate in healthy volunteers demonstrate its applicability to bioavailability studies."( Determination of levocetirizine in human plasma by liquid chromatography-electrospray tandem mass spectrometry: application to a bioequivalence study.
Abib, E; Amarante, AR; Barros, FA; Berton, D; Boldin, R; Calafatti, SA; Campos, DR; Meurer, EC; Morita, MR; Pedrazolli, J; Pereira, R, 2008
)
0.85
" No major cytochrome P450 inhibition has been reported with desloratadine, fexofenadine and levocetirizine, and the bioavailability of desloratadine is minimally affected by drugs interfering with transporter molecules."( Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review.
Devillier, P; Faisy, C; Roche, N, 2008
)
0.79
"To compare the bioavailability of two cetirizine tablet (10 mg) formulations (ZyrtecA from UCB Pharma, Spain as a reference formulation and RyvelA from Novell Pharmaceutical Laboratories, Indonesia as a test formulation)."( Comparative bioavailability of two cetirizine tablet formulations in Indonesian healthy volunteers.
Harahap, Y; Indriati, E; Lusthom, W; Prasaja, B, 2008
)
0.89
" Cetirizine exhibits high intestinal absorption in humans and its oral bioavailability is estimated to be greater than 70%."( Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Chen, C, 2008
)
1.47
" The compound shows a rapid onset of action, high bioavailability and affinity for the H1 receptor."( Levocetirizine in the treatment of allergic diseases.
Baiardini, I; Canonica, GW; Compalati, E; Scordamaglia, A; Scordamaglia, F, 2009
)
0.91
" When the AUC(0-t) values for both formulations for natural log-transformed data were compared, the test formulation showed a bioavailability of 100."( Pharmacokinetics and bioequivalence study of two cetirizine hydrochloride formulations in healthy Chinese male volunteers.
Chen, Y; Liu, Y; Tian, Y; Xu, FG; Zhang, ZJ, 2009
)
0.61
" These "in combo" PAMPA data were used to predict the human absolute bioavailability of the ampholytes."( The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
Avdeef, A; Sun, N; Tam, KY; Tsinman, O, 2010
)
0.36
" The relative bioavailability of the optimized microspheres was compared with CTZ marketed product after oral administration on healthy human volunteers using a double blind, randomized, cross-over design."( Statistical optimization of controlled release microspheres containing cetirizine hydrochloride as a model for water soluble drugs.
Ahmed, OA; Ahmed, TA; Alsawahli, M; El-Helw, AR; El-Say, KM; Fahmy, UA; Hosny, KM; Kharshoum, RM, 2015
)
0.65
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates."( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
Bharate, SS; Vishwakarma, RA, 2015
)
0.42
" Moreover, the use of these effervescent tablets in an orodispersible dosage form can improve oral drug bioavailability and act as an attractive pediatric dosage form."( Novel levocetirizine HCl tablets with enhanced palatability: synergistic effect of combining taste modifiers and effervescence technique.
Labib, GS, 2015
)
0.82
" In addition, the relative bioavailability of the optimized formulation was 165."( Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper-Lin small composite design.
El-Say, KM, 2016
)
0.66
" Moreover, levocetirizine attenuated the elevated renal levels of TNF-α and TGF-β1, ameliorated renal oxidative stress and restored NO bioavailability in diabetic kidney."( Comparison of the effects of levocetirizine and losartan on diabetic nephropathy and vascular dysfunction in streptozotocin-induced diabetic rats.
Anbar, HS; Gameil, NM; Shehatou, GS; Suddek, GM, 2016
)
1.07
"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
" Meanwhile, food intake can delay the absorption rate and reduced the bioavailability of levocetirizine in healthy Chinese volunteers."( The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers.
Chen, XF; Cheng, Y; Fang, LP; Guo, JH; Huang, BL; Lin, BJ; Liu, MB; Qiu, HQ; Que, WC, 2019
)
0.95
" Part 1 compared the bioavailability of levocetirizine oral disintegrating tablet (ODT) and levocetirizine immediate-release tablet (IRT) taken with water in the fasted state in 24 subjects; all subjects completed this part of the trial."( Levocetirizine Oral Disintegrating Tablet: A Randomized Open-Label Crossover Bioequivalence Study in Healthy Japanese Volunteers.
Eto, T; Haranaka, M; Hoyano, K; Ino, H; Irie, S; Nakano, A; Ogura, H; Shiramoto, M; Terao, T; Wakamatsu, A, 2020
)
1.38
" Levocetirizine's solubility and permeability properties, as well as its dissolution from commercial products, its therapeutic uses, therapeutic index, pharmacokinetics and pharmacodynamic traits, were reviewed in accordance with the BCS, along with any reports in the literature about failure to meet bioequivalence (BE) requirements, bioavailability issues, drug-excipient interactions as well as other relevant information."( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Levocetirizine Dihydrochloride.
Abdallah, DB; Abrahamsson, B; Ahmed, DT; Charoo, NA; Cristofoletti, R; Dressman, J; Kambayashi, A; Langguth, P; Mehta, M; Parr, A; Polli, JE; Shah, VP, 2023
)
1.66
" However, the bioavailability of levocetirizine hydrochloride granules remains to be determined."( Bioequivalence of Levocetirizine Hydrochloride Granules (Kangzhitai) in Healthy Subjects.
Tan, H; Xiang, H; Yang, G, 2023
)
1.5
" The relative bioavailability (F, assessed by AUC0-48) of Kangzhitai® vs."( Bioequivalence of Levocetirizine Hydrochloride Granules (Kangzhitai) in Healthy Subjects.
Tan, H; Xiang, H; Yang, G, 2023
)
1.22

Dosage Studied

The results indicate that a once-daily dosing regimen of 2-4mg/kg cetirizine per os clearly provides a sufficient antihistamine effect. Three-day repeat dosing of the intranasal solution GSK1004723 1,000 μg also demonstrated a statistically significant attenuation of nasal symptoms.

ExcerptRelevanceReference
" A dose-response relationship was evident for selected symptoms, and the once daily 5-mg dose was found to be an effective minimum dose."( Double-blind comparison of cetirizine and placebo in the treatment of seasonal rhinitis.
Altman, R; Brandon, ML; Buchman, E; Connell, JT; Dockhorn, R; Falliers, CJ; Leese, PT; Miller, J; Wasserman, SI; Zeterberg, JM, 1991
)
0.58
" These properties, combined with a once-daily dosage regimen, should help improve patient compliance and optimize antihistamine therapy."( Cetirizine: a unique second-generation antihistamine for treatment of rhinitis and chronic urticaria.
Pierson, WE,
)
1.57
" At the dosage used, cetirizine therapy appears to be no more effective than terfenadine."( A comparison of cetirizine and terfenadine in the management of solar urticaria.
Bilsland, D; Ferguson, J, 1991
)
0.95
"A double-blind, placebo-controlled clinical trial was undertaken for two weeks to evaluate three dosing schedules for administration of cetirizine in patients with seasonal allergic rhinitis."( Cetirizine therapy for seasonal allergic rhinitis: alternative dosage schedules.
Broide, DH; Marquardt, DL; Wasserman, SI,
)
1.78
" One subject developed moderate drowsiness during multiple dosing with cetirizine."( Effects of oral cetirizine, a selective H1 antagonist, on allergen- and exercise-induced bronchoconstriction in subjects with asthma.
Dauphinee, B; Djahed, B; Gong, H; Tashkin, DP; Wu, TC, 1990
)
0.86
" Further, astemizole has the longest time to relief of symptoms in this class; histamine wheal inhibition is not apparent until the second day of 10 mg dosing and does not peak for 9 to 12 days."( Pharmacology of antihistamines.
Woodward, JK, 1990
)
0.28
" During daily dosing with cetirizine, 5 mg or 10 mg at bedtime for 35 days, serum cetirizine concentrations and suppression of histamine-induced wheals and flares were monitored every 7 days, 12 hours after the cetirizine dose."( Cetirizine: a pharmacokinetic and pharmacodynamic evaluation in children with seasonal allergic rhinitis.
Chen, XY; Simons, FE; Simons, KJ; Watson, WT, 1989
)
2.02
" For H1-receptor antagonists with long half-life values, steady state may not be reached for several days (chlorpheniramine and brompheniramine) or several weeks (astemizole), and significant accumulation of drug occurs if the dosing interval is more frequent than every half-life."( The comparative pharmacokinetics of H1-receptor antagonists.
Chung, M; Simons, FE; Simons, KJ; Yeh, J, 1987
)
0.27
" The purpose of the evaluation was to determine whether dosage schedules of cetirizine will require modification in the elderly or patients with renal insufficiency."( Pharmacokinetics of cetirizine in the elderly and patients with renal insufficiency.
Awni, WM; Chung, M; Halstenson, CE; Matzke, GR; Yeh, J, 1987
)
0.83
"05), which is consistent with albuterol's recommended dosing frequency of every 4 to 6 hours."( Comparison of the bronchodilatory effects of cetirizine, albuterol, and both together versus placebo in patients with mild-to-moderate asthma.
Corren, J; Katz, RM; Nicodemus, CF; Rachelefsky, GS; Schanker, HM; Siegel, SC; Spector, SL, 1995
)
0.55
"1% increased dosage to 10 mg/d, and 41."( Dose-ranging comparative evaluation of cetirizine in patients with seasonal allergic rhinitis.
DuBuske, L, 1995
)
0.56
"Cetirizine and hydroxyzine enter the skin readily, and their sustained high concentrations in skin after single or multiple dosing may contribute to their well-known efficacy in symptomatic treatment of urticaria and other skin disorders in which histamine plays a role."( Quantitation of H1-receptor antagonists in skin and serum.
Murray, HE; Simons, FE; Simons, KJ, 1995
)
1.73
" A paired Student t test showed no difference in dose/area under the concentration-time curve between the 20 mg/day and 60 mg/day dosing groups at steady state."( The electrocardiographic effects of cetirizine in normal subjects.
Barbey, JT; Chung, M; Edwards, D; Sale, ME; Thakker, K; Woosley, RL; Yeh, J, 1994
)
0.56
" Compliance was checked and found to be less than 80% of the prescribed dosage in 2 cetirizine patients."( A placebo-controlled trial of cetirizine in seasonal allergic rhino-conjunctivitis in children aged 6 to 12 years.
Candiani, R; Masi, M; van de Venne, H, 1993
)
0.8
" The recommended adult dosage of this agent is 5 or 10 mg/d."( Cetirizine: a new, nonsedating antihistamine.
Barnes, CL; McKenzie, CA; Poinsett-Holmes, K; Webster, KD, 1993
)
1.73
" Two of these advantages are a rapid onset of action and a once-daily dosing regimen."( Cetirizine: a new, nonsedating antihistamine.
Barnes, CL; McKenzie, CA; Poinsett-Holmes, K; Webster, KD, 1993
)
1.73
" Histamine tests were performed on 10 occasions up to +24 h after dosing using an intradermal injection of histamine 2 micrograms with concommittant contralateral injection of a saline control."( Comparative wheal and flare study of mizolastine vs terfenadine, cetirizine, loratadine and placebo in healthy volunteers.
Cabanis, MJ; Caplain, H; Chaufour, S; Rosenzweig, P; Thebault, JJ; Ulliac, N, 1995
)
0.53
"When comparing the fate of a drug in the body with the location of its receptors, it appears that a large amount of the administered dosage will never reach these receptors."( [Can one adjust the distribution of a drug in an organism to its target sites? The example of antihistaminics (anti-H1) and cetirizine].
Albengres, E; Tillement, JP, 1996
)
0.5
" Both were dosed at 10 mg/day."( Loratadine treatment of rhinitis due to pollen allergy reduces epithelial ICAM-1 expression.
Canonica, GW; Ciprandi, G; Danzig, M; Passalacqua, G; Pronzato, C; Ricca, V, 1997
)
0.3
"Our study shows clearly that the efficacy of a single therapeutic dosage of cetirizine is consistently good for suppression of cutaneous reactivity to histamine in healthy volunteers."( Consistency of the efficacy of cetirizine and ebastine on skin reactivity.
Benabdesselam, O; Frossard, N; Melac, M; Pauli, G, 1998
)
0.82
"The study failed to establish dose-response effects of cetirizine, but it is evident that cetirizine is not free of central activity over the therapeutic range, and so its use by air personnel is not recommended."( Central effects of the H1-antihistamine, cetirizine.
Nicholson, AN; Turner, C, 1998
)
0.81
" Their longer duration of action also enables a more patient-friendly dosing regimen which increases patient compliance."( Pharmacokinetic overview of oral second-generation H1 antihistamines.
Estes, KS; González, MA, 1998
)
0.3
" Cetirizine was given once a day at the dosage of 10 mg for four weeks."( [The efficacy of cetirizine in the treatment of mild allergic asthma due to grasses].
Biasi, D; Carletto, A; Corrocher, R; Pacor, ML, 1998
)
1.55
"5 hours after dosing were latency of the P300 event-related potential in which increased latency reflects a decreased rate of cognitive processing, visual analogue scale for subjective somnolence, and histamine skin tests for measurement of peripheral H1-blockade."( Central nervous system effects of H1-receptor antagonists in the elderly.
Fraser, TG; Maher, J; Pillay, N; Simons, FE; Simons, KJ, 1999
)
0.3
" Cetirizine shifted the histamine dose-response at both temperatures: statistically significantly at 14 degrees C only."( Histamine response and local cooling in the human skin: involvement of H1- and H2-receptors.
Grossmann, M; Jamieson, MJ; Kirch, W, 1999
)
1.21
"Our study shows clearly that the efficacy of a single therapeutic dosage of cetirizine is greater and consistently better than that of ebastine for suppression of cutaneous reactivity to histamine 4 h after treatment in healthy volunteers."( Consistency and efficacy of cetirizine (10 mg) versus ebastine (20 mg) at 4 h on skin reactivity.
Benabdesselam, O; Duvernelle, C; Frossard, N; Melac, M; Pauli, G; Purohit, A, 1999
)
0.83
"At this dosage the histamine-induced flare was at least 80% inhibited at the start of the second administration Thereafter, on successive administrations, the inhibition was even more pronounced and the response control was nearly total."( A pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effects of cetirizine.
Ganem, B; Kuch, MD; Tillement, JP; Urien, S, 1999
)
0.53
" In addition, assessment was made immediately before dosing in the morning for the previous 30 minutes."( Double-blind, placebo-controlled study comparing the efficacy and safety of fexofenadine hydrochloride (120 and 180 mg once daily) and cetirizine in seasonal allergic rhinitis.
Bousquet, J; Howarth, PH; Reynolds, R; Roi, L; Stern, MA, 1999
)
0.51
" Efficacy was maintained for the entire dosing interval (ie, for 24 hours)."( Double-blind, placebo-controlled study comparing the efficacy and safety of fexofenadine hydrochloride (120 and 180 mg once daily) and cetirizine in seasonal allergic rhinitis.
Bousquet, J; Howarth, PH; Reynolds, R; Roi, L; Stern, MA, 1999
)
0.51
" An individual dosage should be chosen based on the severity of symptoms."( Use of cetirizine in dermatologic disorders.
Henz, BM; Zuberbier, T, 1999
)
0.76
" Somnolence scores were similar for both groups at baseline and at the time of dosing (8:00 AM)."( Loratadine versus cetirizine: assessment of somnolence and motivation during the workday.
Gates, D; Greiding, L; Heithoff, K; Ramon, F; Salmun, LM; Scharf, M, 2000
)
0.64
" Inhibition of the wheal response observed for cetirizine and levocetirizine was apparent by 1 h after dosage and lasted for mean durations of 24."( A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers.
Baltes, E; De Vos, C; Devalia, JL; Hanotte, F, 2001
)
0.81
" In the first group, only prednicarbat cream was applied to affected places twice a day for a maximum of 10 days, while in the other group also cetirizin was administered once a day in a dosage according to the patient's age."( [Prednicarbate and cetirizin dihydrochloride in the treatment of atopic eczema in the acute phase in children].
Bartosíková, L; Dzúrová, J; Frána, L; Frána, P; Kollár, P; Kotolová, H; Necas, J; Petrzelková, J, 2001
)
0.31
" A rapid, selective and stability indicating high performance thin layer chromatographic method was developed and validated for their simultaneous estimation in pharmaceutical dosage forms."( Stability indicating HPTLC method for the simultaneous determination of pseudoephedrine and cetirizine in pharmaceutical formulations.
Makhija, SN; Vavia, PR, 2001
)
0.53
" Between dialysis sessions, no supplemental dosage was required to keep the therapeutic range of 14 ng/ml."( Pharmacokinetics of cetirizine in chronic hemodialysis patients: multiple-dose study.
Fujita, T; Nakao, A; Noiri, E; Ozawa, H, 2001
)
0.63
" In the present study, we investigated the dose-response relationship of different antihistamines on the performance in a reaction-time task that has been developed for rats."( Dissociable effects of histamine H1 antagonists on reaction-time performance in rats.
Blokland, A; Ramaekers, J; Scholtissen, B; Vermeeren, A,
)
0.13
" This first therapeutic trial of levocetirizine aimed at determining the dosage with the best benefit/risk ratio in patients with seasonal allergic rhinitis (SAR)."( Efficacy and safety of levocetirizine in seasonal allergic rhinitis.
Arendt, C; Leynadier, F; Mees, K; Pinelli, ME, 2001
)
0.88
"A rapid, simple and accurate HPLC method is described for the assay of cetirizine in commercial dosage forms."( Development and validation of a HPLC method for the determination of cetirizine in pharmaceutical dosage forms.
Drozd, J; Hopkała, H; Misztal, G; Paw, B, 2002
)
0.78
" However, the presence of a selective barrier between blood and ocular tissues, the so-called blood-ocular barrier, does not allow a priori assessment of the most suitable dosage for ocular therapy."( Pharmacokinetics of cetirizine in tear fluid after a single oral dose.
Barbato, F; Cennamo, G; Del Prete, A; Grumetto, L; La Rotonda, MI, 2002
)
0.64
"In contrast to diphenhydramine, when compared with placebo, levocetirizine did not modify the CFF (primary endpoint), regardless of the dosing scheme (-1."( Lack of effect of single and repeated doses of levocetirizine, a new antihistamine drug, on cognitive and psychomotor functions in healthy volunteers.
Allain, H; Gandon, JM, 2002
)
0.81
" Concurrent dosing of dihydrocodeine and ebastine produced a significant place preference."( Effects of second generation of histamine H1 antagonists, cetirizine and ebastine, on the antitussive and rewarding effects of dihydrocodeine in mice.
Kamei, J; Miyata, S; Morita, K; Onodera, K, 2003
)
0.56
" In conclusion, this study shows that, at the end of the conventional dosing interval, ebastine 10 mg and cetirizine 10 mg once daily in repeated doses suppressed the histamine wheal more effectively than did loratadine 10 mg once daily or fexofenadine 60 mg twice daily."( Inhibition of the histamine wheal by ebastine compared with cetirizine, fexofenadine and loratadine at steady state.
Boyce, M; Carey, W; Luria, X; Warrington, S, 2002
)
0.77
" Dosage ranged from 5 to 10 mg orally and onset of symptoms ranged from 3 to 184 days."( Oculogyric crisis in patients taking cetirizine.
Fraunfelder, FT; Fraunfelder, FW, 2004
)
0.6
" Dosage had no significant effect."( Role of histamine release in nonspecific vasodilatation during anodal and cathodal iontophoresis.
Droog, EJ; Henricson, J; Horiuchi, Y; Lennquist, S; Sjöberg, F; Wikström, T, 2004
)
0.32
"Data were pooled from six clinical trials, in which cetirizine was administered orally in various formulations and in single and multiple dosage regimens."( Retrospective population pharmacokinetic analysis of cetirizine in children aged 6 months to 12 years.
Aarons, L; de Longueville, M; Hussein, Z; Majid, O; Pitsiu, M; Stockis, A, 2004
)
0.82
" The current recommended dosing regimens that younger children should receive lower but more frequent doses, are confirmed by the present analysis."( Retrospective population pharmacokinetic analysis of cetirizine in children aged 6 months to 12 years.
Aarons, L; de Longueville, M; Hussein, Z; Majid, O; Pitsiu, M; Stockis, A, 2004
)
0.57
" We evaluated single and short-term dosing effects of a modern histamine H1-receptor antagonist, levocetirizine, given at the usual clinically recommended dose, on the primary outcome of AMP bronchoprovocation."( Single and short-term dosing effects of levocetirizine on adenosine monophosphate bronchoprovocation in atopic asthma.
Gray, RD; Lee, DK; Lipworth, BJ; Robb, FM; Soutar, PC; Wilson, AM, 2004
)
0.8
"Single and short-term dosing with levocetirizine conferred similar improvements in bronchial hyper-responsiveness to AMP challenge, which was unrelated to prechallenge airway calibre."( Single and short-term dosing effects of levocetirizine on adenosine monophosphate bronchoprovocation in atopic asthma.
Gray, RD; Lee, DK; Lipworth, BJ; Robb, FM; Soutar, PC; Wilson, AM, 2004
)
0.86
" Compliance with cetirizine dosing was documented."( Population pharmacokinetics of levocetirizine in very young children: the pediatricians' perspective.
Simons, FE, 2005
)
0.95
" The aim of the study was to learn whether the survival and the motor incoordination (ataxia) side effect of cetirizine administration is dosing time-dependent."( [Circadian rhythms in the toxic effects of the histamine antagonist cetirizine in mice].
Ben Attia, M; Boughattas, NA; Dridi, D; Reinberg, A, 2005
)
0.78
"The survival was statistically significant dosing time-dependent (chi(2) = 16."( [Circadian rhythms in the toxic effects of the histamine antagonist cetirizine in mice].
Ben Attia, M; Boughattas, NA; Dridi, D; Reinberg, A, 2005
)
0.56
"CTZ does not significantly affect the pharmacokinetic parameters of RTV, and the association does not, thus, require a modification of the dosage of the protease inhibitor."( Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers.
Cremieux, AC; Delatour, F; Farinotti, R; Gautran, C; Melac, M; Moulaert, B; Otoul, C; Peytavin, G; Strolin-Benedetti, M, 2005
)
0.58
"The objective of the present study was to compare the efficacy and tolerability of azelastine nasal spray administered at the recommended dosage of 2 sprays per nostril twice daily with those of cetirizine in the treatment of moderate to severe SAR."( Effectiveness of azelastine nasal spray compared with oral cetirizine in patients with seasonal allergic rhinitis.
Berger, W; Bernstein, J; Corren, J; Nayak, A; Sacks, H; Storms, W, 2005
)
0.76
" Over 97% of GPs ranked development of paediatric formulations and clearer dosage information more highly than clinical trials as a means to reducing off-label prescribing."( Off-label prescribing to children: attitudes and experience of general practitioners.
Ekins-Daukes, S; Helms, PJ; McLay, JS; Taylor, MW, 2005
)
0.33
" Once-daily dosing may be optimal in children aged 6 to 11 years, as it is in adults."( Levocetirizine: pharmacokinetics and pharmacodynamics in children age 6 to 11 years.
Simons, FE; Simons, KJ, 2005
)
0.89
" Therefore, this study assessed the effects of repeated dosing of these antihistamines on driving and psychomotor performance."( Repeated-dose effects of mequitazine, cetirizine and dexchlorpheniramine on driving and psychomotor performance.
Ramaekers, JG; Theunissen, EL; Vermeeren, A, 2006
)
0.6
" In 13 healthy volunteers, we assessed the time course and dose-response of the acute cutaneous response(s) to ALA-PDT, the impact of H(1) antihistamine blockade, and measured dermal histamine release."( Histamine is released following aminolevulinic acid-photodynamic therapy of human skin and mediates an aminolevulinic acid dose-related immediate inflammatory response.
Brooke, RC; Church, MK; Clough, GF; Friedmann, PS; Rhodes, LE; Sidhu, MK; Sinha, A; Watson, RE, 2006
)
0.33
" Thus, the proposed method is simple and suitable for the simultaneous analysis of active ingredients in tablet dosage forms."( Method development and validation for the simultaneous determination of cetirizine dihydrochloride, paracetamol, and phenylpropanolamine hydrochloride in tablets by capillary zone electrophoresis.
Azhagvuel, S; Sekar, R, 2007
)
0.57
"Recently, several authors have suggested an off-label increase of antihistamine dosage should be given to patients with chronic urticaria (CU) not responding to the usual, recommended doses, in order to gain better control of the disease."( Chronic unremitting urticaria: is the use of antihistamines above the licensed dose effective? A preliminary study of cetirizine at licensed and above-licensed doses.
Asero, R, 2007
)
0.55
" The present work reports simple, accurate and precise spectrophotometric methods for their simultaneous estimation from tablet dosage form."( Spectrophotometric estimation of ambroxol and cetirizine hydrochloride from tablet dosage form.
Chandorkar, JG; Gowekar, NM; Kasture, AV; Pande, VV; Tekade, AR, 2007
)
0.6
"The objective of the current study was to develop a simple, accurate, precise and rapid reversed-phase HPLC method and subsequent validation using ICH suggested approach for the determination of antihistaminic-decongestant pharmaceutical dosage forms containing binary mixtures of pseudoephedrine hydrochloride (PSE) with fexofenadine hydrochloride (FEX) or cetirizine dihydrochloride (CET)."( Development and validation of a rapid RP-HPLC method for the determination of cetirizine or fexofenadine with pseudoephedrine in binary pharmaceutical dosage forms.
Karakuş, S; Küçükgüzel, I; Küçükgüzel, SG, 2008
)
0.74
" DAD detection was utilized for the characterization of composition of each separated zone via match of corresponding tested (analyte in dosage form) and reference (standard analyte in water) UV-VIS spectrum (scanned in interval 200-800 nm) being expressed mathematically through Pearson's correlation coefficient (PCC)."( Enantiomeric purity control of levocetirizine in pharmaceuticals using anionic cyclodextrin mediated capillary electrophoresis separation and fiber-based diode array detection.
Havránek, E; Maráková, K; Mikus, P; Valásková, I, 2009
)
0.63
" Alternative dosage forms such as liquids or oral disintegrating tablets are available for most agents, allowing ease of administration to most young children and infants; however, limited data are available regarding use in infants for most agents, except desloratadine, cetirizine and montelukast."( Treatment of allergic rhinitis in infants and children: efficacy and safety of second-generation antihistamines and the leukotriene receptor antagonist montelukast.
Moeller, ML; Nahata, MC; Phan, H, 2009
)
0.53
" However, this activity may be missed in conventional teratology studies because repeat dosing may cause resorptions."( Improved methodology for identifying the teratogenic potential in early drug development of hERG channel blocking drugs.
Bengtsson, E; Blomgren, B; Danielsson, BR; Danielsson, C; Johansson, A; Khan, KM; Kultima, K; Nilsson, MF; Sköld, AC; Webster, WS; Wilson, J, 2010
)
0.36
"Increasing the dosage of levocetirizine and desloratadine up to 4-fold improves chronic urticaria symptoms without compromising safety in approximately three quarters of patients with difficult-to-treat chronic urticaria."( The effectiveness of levocetirizine and desloratadine in up to 4 times conventional doses in difficult-to-treat urticaria.
Church, DS; Church, MK; Dimitrov, V; Kraeva, S; Kralimarkova, T; Lazarova, C; Popov, TA; Popova, D; Staevska, M, 2010
)
0.96
" Thus, the proposed method is suitable for the simultaneous analysis of active ingredients in tablet dosage forms and human serum."( Simultaneous determination of gliquidone, fexofenadine, buclizine, and levocetirizine in dosage formulation and human serum by RP-HPLC.
Arayne, MS; Mirza, AZ; Siddiqui, FA; Sultana, N,
)
0.36
" The death rate was dosing time dependent (P <0."( Murine chronotoxicity to the antiallergic agent, cetirizine.
Boughattas, NA; Dridi, D; Mansour, HB, 2011
)
0.62
" We propose the use of CTZ at the dosage of 30 mg/daily."( Therapeutic hotline. Effectiveness of the association of cetirizine and topical steroids in lichen planus pilaris--an open-label clinical trial.
d'Ovidio, R; Di Prima, TM; Rossi, A,
)
0.38
" Three-day repeat dosing of the intranasal solution GSK1004723 1,000 μg also demonstrated a statistically significant attenuation of nasal symptoms, but was less than seen with cetirizine and GSK835726 and caused initial nasal discomfort."( The efficacy and tolerability of two novel H(1)/H(3) receptor antagonists in seasonal allergic rhinitis.
Ambery, C; Daley-Yates, P; McQuade, B; Oliver, A; Sweeney, L; Watson, J, 2012
)
0.57
"A 28-year-old man with decreased libido received ashwagandha in the usual daily dosage of 5 g for 10 days."( Fixed-drug eruption caused by ashwagandha (Withania somnifera): a widely used Ayurvedic drug.
Bhattacharya, SN; Sehgal, VN; Verma, P,
)
0.13
" Results demonstrate improved activity of antihistamines by 2 phytochemicals, suggesting dosing strategies for animal trials of ASX- or GB-augmented formulations for seasonal allergic rhinitis and asthma."( In vitro suppression of lymphocyte activation in patients with seasonal allergic rhinitis and pollen-related asthma by cetirizine or azelastine in combination with ginkgolide B or astaxanthin.
Abal, A; Al-Awadhi, R; Al-Sharah, S; Arifhodzic, N; Azeamouzi, C; Haines, D; Mahmoud, FF; Tosaki, A, 2012
)
0.59
" Drug dosage was determined by initial VAS (visual analog scale) scores."( A four arm, double blind, randomized and placebo controlled study of pregabalin in the management of post-burn pruritus.
Ahuja, RB; Gupta, GK, 2013
)
0.39
" These results suggest that double-dosed levocetirizine treatment suppresses histamine-induced skin symptoms more rapidly, profoundly and sustainably than conventionally dosed levocetirizine treatment."( A double dose of levocetirizine leads to better control of histamine-induced flare, wheal and itch in healthy donors.
Kabashima, K; Miyachi, Y; Nakahigashi, K; Nakamizo, S; Tanizaki, H, 2013
)
0.97
"Pseudoephedrine and cetirizine have been combined in dosage forms with more therapeutic benefits when compared with single-drug treatment."( Development of a CZE method for the quantification of pseudoephedrine and cetirizine.
Alnajjar, AO; Idris, AM, 2014
)
0.96
" The method was applied successfully on tablet dosage form."( Gradient HPLC-DAD determination of paracetamol, phenylephrine hydrochloride, cetirizine in tablet formulation.
Bakal, RL; Chandewar, AV; Dewani, AP; Jaybhaye, SS; Patra, S; Shelke, PG, 2014
)
0.63
"A new, simple and accurate stability-indicating reverse phase high performance liquid chromatography method was developed and validated during the early stage of drug development of an oral lyophilizate dosage form of cetirizine dihydrochloride."( Determination of stress-induced degradation products of cetirizine dihydrochloride by a stability-indicating RP-HPLC method.
Flórez Borges, P; García Montoya, E; Jo, E; Miñarro, M; Pérez Lozano, P; Suñe Negre, JM; Ticó, JR, 2014
)
0.83
"The proposed stability-indicating method developed in the early phase of drug development proved to be a simple, sensitive, accurate, precise, reproducible and therefore useful for the following stages of the cetirizine dihydrochloride oral lyophilizate dosage form development."( Determination of stress-induced degradation products of cetirizine dihydrochloride by a stability-indicating RP-HPLC method.
Flórez Borges, P; García Montoya, E; Jo, E; Miñarro, M; Pérez Lozano, P; Suñe Negre, JM; Ticó, JR, 2014
)
0.84
" The model formulations were representative for oral solutions (co-solvents), parenteral solutions (buffer species) and solid dosage forms (organic acids applicable for solubility enhancement)."( Evaluation of microwave oven heating for prediction of drug-excipient compatibilities and accelerated stability studies.
Cornett, C; Hansen, SH; Schou-Pedersen, AM; Østergaard, J, 2015
)
0.42
"The use of solid oral dosage forms is typically favored with regard to stability and ease of administration."( In-vitro and in-vivo evaluation of taste-masked cetirizine hydrochloride formulated in oral lyophilisates.
Axe, P; Breitkreutz, J; Grother, L; Preis, M, 2015
)
0.67
" Moreover, the use of these effervescent tablets in an orodispersible dosage form can improve oral drug bioavailability and act as an attractive pediatric dosage form."( Novel levocetirizine HCl tablets with enhanced palatability: synergistic effect of combining taste modifiers and effervescence technique.
Labib, GS, 2015
)
0.82
" The developed methods have been successfully applied to the simultaneous determination of both drugs in commercial tablet dosage form."( Validated derivative and ratio derivative spectrophotometric methods for the simultaneous determination of levocetirizine dihydrochloride and ambroxol hydrochloride in pharmaceutical dosage form.
Ali, OI; Elgohary, RM; Ismail, NS, 2016
)
0.65
" Moreover, 18 batches were subjected to various characterization tests required for the production of dosage form."( Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper-Lin small composite design.
El-Say, KM, 2016
)
0.66
" In the case of liquid dosage forms, besides the active substance in large amounts there are usually also inactive ingredients such as methyl- and propylparaben."( A Novel Two-Step Liquid-Liquid Extraction Procedure Combined with Stationary Phase Immobilized Human Serum Albumin for the Chiral Separation of Cetirizine Enantiomers along with M and P Parabens.
Bączek, T; Chmielewska, A; Konieczna, L, 2016
)
0.63
"5:1) are promising CET carriers with efficient taste masking potential and might be further used in designing orodispersible dosage forms with CET."( Original research paper. Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying.
Amelian, A; Basa, A; Ciosek, P; Szekalska, M; Winnicka, K, 2017
)
0.67
" The EAACI/GA[2]LEN/EDF/WAO guidelines advocate an increased antihistamine dosage up to four times the standard, before adding leukotriene receptor antagonists."( Effectiveness and safety of levocetirizine 10 mg versus a combination of levocetirizine 5 mg and montelukast 10 mg in chronic urticaria resistant to levocetirizine 5 mg: A double-blind, randomized, controlled trial.
Das, NK; Ghosh, C; Pal, S; Sarkar, TK; Sil, A,
)
0.41
"The results indicate that a once-daily dosing regimen of 2-4 mg/kg cetirizine per os clearly provides a sufficient antihistamine effect."( Cetirizine per os: exposure and antihistamine effect in the dog.
Bondesson, U; Ekstrand, C; Hedeland, M; Ingvast-Larsson, C; Olsén, L, 2018
)
2.16
" In cases of failure, treatment was switched to omalizumab at doses of < 300 mg/month with incremental dosage increases as necessary (monthly dose range, 150-600 mg/month)."( Real-life experience in the treatment of solar urticaria: retrospective cohort study.
Enk, CD; Hodak, E; Lapidoth, M; Levi, A; Mazor, S; Snast, I; Uvaidov, V, 2019
)
0.51
" In this monograph, the practicality of using Biopharmaceutics Classification System (BCS) based methodologies as a substitute for pharmacokinetic studies in human volunteers to appraise the bioequivalence of immediate-release (IR) oral, solid dosage forms containing levocetirizine dihydrochloride was investigated, using data from the literature and in-house testing."( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Levocetirizine Dihydrochloride.
Abdallah, DB; Abrahamsson, B; Ahmed, DT; Charoo, NA; Cristofoletti, R; Dressman, J; Kambayashi, A; Langguth, P; Mehta, M; Parr, A; Polli, JE; Shah, VP, 2023
)
1.32
"A novel potentiometric sensor which consists of a silver wire coated with zinc oxide (ZnO) nanorod modified with a polymeric membrane (combining β-cyclodextrin and tetraphenyl borate, and plasticized with di-butyl phthalate) was constructed for the determination of LVZ·2HCl in its pure form and its combination dosage form."( Construction of a Zinc Oxide Nanorod-Modified Coated Wire Electrode for Potentiometric Determination of Levocetirizine Dihydrochloride in Its Pure and Combined Form.
Alhaj Sakur, A; Nashed, D; Noureldin, I, 2023
)
1.12
"The method was validated according to International Council for Harmonisation of Technical Requirments for Registration of Pharmaceuticals for Human Use (ICH) rules and applied to the determination of LVZ in its pure and combined pharmaceutical dosage forms."( Construction of a Zinc Oxide Nanorod-Modified Coated Wire Electrode for Potentiometric Determination of Levocetirizine Dihydrochloride in Its Pure and Combined Form.
Alhaj Sakur, A; Nashed, D; Noureldin, I, 2023
)
1.12
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
anti-allergic agentA drug used to treat allergic reactions.
H1-receptor antagonistH1-receptor antagonists are the drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.
environmental contaminantAny minor or unwanted substance introduced into the environment that can have undesired effects.
xenobioticA xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
[role 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]

Drug Classes (4)

ClassDescription
monocarboxylic acidAn oxoacid containing a single carboxy group.
piperazines
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
etherAn organooxygen compound with formula ROR, where R is not hydrogen.
[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
Cetirizine H1-Antihistamine Action87

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.77810.035520.977089.1251AID504332
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency13.09180.00669.809418.4927AID1347050
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H1 receptorHomo sapiens (human)Ki0.03790.00000.511010.0000AID238823; AID238825; AID254274; AID500222; AID500223; AID500224; AID500225; AID500226; AID500227; AID500228; AID87247
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)43.37020.00091.901410.0000AID161281; AID240820; AID243151; AID276169; AID408340; AID576612
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)500.00000.01002.765610.0000AID721754
Histamine H4 receptorHomo sapiens (human)Ki10.00000.00060.478710.0000AID1798265
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Angiopoietin-1 receptorHomo sapiens (human)Kd90.00000.00311.34646.7000AID653693
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (85)

Processvia Protein(s)Taxonomy
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAngiopoietin-1 receptorHomo sapiens (human)
angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
response to hypoxiaAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of protein phosphorylationAngiopoietin-1 receptorHomo sapiens (human)
endothelial cell proliferationAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of endothelial cell proliferationAngiopoietin-1 receptorHomo sapiens (human)
endochondral ossificationAngiopoietin-1 receptorHomo sapiens (human)
sprouting angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayAngiopoietin-1 receptorHomo sapiens (human)
cell-cell signalingAngiopoietin-1 receptorHomo sapiens (human)
heart developmentAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of endothelial cell migrationAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
regulation of establishment or maintenance of cell polarityAngiopoietin-1 receptorHomo sapiens (human)
substrate adhesion-dependent cell spreadingAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of Rac protein signal transductionAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of Rho protein signal transductionAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of apoptotic processAngiopoietin-1 receptorHomo sapiens (human)
regulation of vascular permeabilityAngiopoietin-1 receptorHomo sapiens (human)
response to peptide hormoneAngiopoietin-1 receptorHomo sapiens (human)
response to estrogenAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
Tie signaling pathwayAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of inflammatory responseAngiopoietin-1 receptorHomo sapiens (human)
response to cAMPAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of focal adhesion assemblyAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAngiopoietin-1 receptorHomo sapiens (human)
definitive hemopoiesisAngiopoietin-1 receptorHomo sapiens (human)
heart trabecula formationAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAngiopoietin-1 receptorHomo sapiens (human)
glomerulus vasculature developmentAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of intracellular signal transductionAngiopoietin-1 receptorHomo sapiens (human)
regulation of endothelial cell apoptotic processAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of endothelial cell apoptotic processAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of MAPK cascadeAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of kinase activityAngiopoietin-1 receptorHomo sapiens (human)
multicellular organism developmentAngiopoietin-1 receptorHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
protein kinase activityAngiopoietin-1 receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityAngiopoietin-1 receptorHomo sapiens (human)
protein bindingAngiopoietin-1 receptorHomo sapiens (human)
ATP bindingAngiopoietin-1 receptorHomo sapiens (human)
growth factor bindingAngiopoietin-1 receptorHomo sapiens (human)
signaling receptor activityAngiopoietin-1 receptorHomo sapiens (human)
identical protein bindingAngiopoietin-1 receptorHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
stress fiberAngiopoietin-1 receptorHomo sapiens (human)
actin filamentAngiopoietin-1 receptorHomo sapiens (human)
extracellular regionAngiopoietin-1 receptorHomo sapiens (human)
cytoplasmAngiopoietin-1 receptorHomo sapiens (human)
plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
microvillusAngiopoietin-1 receptorHomo sapiens (human)
cell-cell junctionAngiopoietin-1 receptorHomo sapiens (human)
focal adhesionAngiopoietin-1 receptorHomo sapiens (human)
basal plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
cell surfaceAngiopoietin-1 receptorHomo sapiens (human)
basolateral plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
apical plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
centriolar satelliteAngiopoietin-1 receptorHomo sapiens (human)
membrane raftAngiopoietin-1 receptorHomo sapiens (human)
plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
receptor complexAngiopoietin-1 receptorHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (192)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
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.
AID26555compound was evaluated for rate constant of transfer (log K1) at pH1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1193492Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1212341Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID500228Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
AID26853compound was evaluated for macroscopic pKa values by potentiometric titration in menthol/water mixtures for pKa21998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID500226Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
AID26540compound was evaluated for reverse occurs for the rate constant(log K-1) at pH1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID22297Delta logPoct -dod1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1397346Efflux ratio of apparent permeability in MDCK2-MDR1 cells at 10 uM after 1 hr in absence of P-gp inhibitor verapamil by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood-Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID26283Partition coefficient (logD)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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).
AID26609compound was evaluated for microscopic pKa BN value by potentiometric titration in cationic/neutral mixtures1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID26758compound was evaluated for tautomeric constant (KZ) value through pKa BN.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID254274Inhibition constant against histamine H1 receptor2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Designed multiple ligands. An emerging drug discovery paradigm.
AID26524Partition coefficient between dodecane and water (logDdod7.4)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID24826compound was evaluated for saturable association constant (nKa) of isolated serum protein HDL1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID281741Inhibition of increase in histamine-induced cutaneous vascular permeability in orally dosed Wistar rat model after 1 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.
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).
AID9843Number of binding sites (n) of isolated serum protein AAG1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1193499Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
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).
AID653693Binding affinity to human recombinant Tie2 by SPR assay2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of loperamide as an antagonist of angiopoietin1 and angiopoietin2 by virtual screening.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
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).
AID1193498Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID500225Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID240820Inhibitory concentration against IKr potassium channel2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents.
AID500227Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1193495Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1280179Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.
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.
AID26527Partition coefficient (logD7.4)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID445446Oral bioavailability in human2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
AID23938Lipophilicity parameter log Poct N (values are not experimentally accessible because of large value of KZ)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID653696Displacement of angiopoietin 1 from human recombinant Tie2 at 50 to 100 uM2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Discovery of loperamide as an antagonist of angiopoietin1 and angiopoietin2 by virtual screening.
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).
AID87247In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID9842compound was evaluated for association constant (Ka) of isolated serum protein AAG1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID26640compound was evaluated for macroscopic pKa values by potentiometric titration in menthol/water mixtures for pKa11998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID281733Ex vivo displacement of [3H]mepyramine from brain histamine H1 receptor in orally dosed Swiss Albino mouse2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.
AID281740Inhibition of CYP3A4 in human microsomes at 25 uM2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.
AID26608compound was evaluated for microscopic pKa AZ value through pKa BN.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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).
AID1397343Efflux ratio of apparent permeability in MDCK cells at 10 uM after 1 hr in presence of P-gp inhibitor verapamil by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood-Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases.
AID16030compound was evaluated for drug bound in plasma1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1193497Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID23739Lipophilicity parameter log Poct C1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1193494Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID281739Effect on QT interval prolongation in Dunkin-Hartley guinea pigs at 3 mg/kg, iv2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Synthesis and structure-activity relationships of novel histamine H1 antagonists: indolylpiperidinyl benzoic acid derivatives.
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
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).
AID23939Lipophilicity parameter log Poct Z.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID78852Ability to inhibit histamine-induced contractions of isolated guinea pig ileum1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application i
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
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).
AID445445Permeability at pH 6.5 by PAMPA method2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
AID26607compound was evaluated for microscopic pKa AN value through pKa BN.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID276169Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Inhibitory effect of carboxylic acid group on hERG binding.
AID1870224Inhibition of human ERG expressed in HEK293 cells at 30 uM at -85 mV holding potential and measured upto 20 mins by patch-clamp method
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID588985Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OCT22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID135327BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID85240compound was evaluated for association constant (Ka) of isolated serum protein HSA with FFA1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID26879compound was evaluated for macroscopic pKa values by potentiometric titration in menthol/water mixtures for pKa31998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID251600Percentage reduction central nervous system depression in guinea pig by compound2005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Synthesis and pharmacological investigation of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents.
AID23732Lipophilicity parameter log Pdod N1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID500223Displacement of [3H]mepyramine from human histamine H1 receptor S3.36A mutant expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
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).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID500224Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
AID1280178Antiviral activity against HCV JFH-1 infected in Huh7.5.1 cells after 48 hrs by luciferase reporter gene assay2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.
AID24828compound was evaluated for saturable association constant (nKa) of isolated serum protein VLDL1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID238825Binding affinity towards human histamine H1 receptor expressed in CHO-K1 cells2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID252138Percentage protection of guinea pigs from histamine induced bronchospasm by compound2005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Synthesis and pharmacological investigation of novel 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents.
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1397345Efflux ratio of apparent permeability in MDCK2-MDR1 cells at 10 uM after 1 hr in presence of P-gp inhibitor verapamil by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood-Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases.
AID24827compound was evaluated for saturable association constant (nKa) of isolated serum protein LDL1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID500222Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting2005Nature chemical biology, Jul, Volume: 1, Issue:2
Linking agonist binding to histamine H1 receptor activation.
AID85239compound was evaluated for association constant (Ka) of isolated serum protein HSA1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID22294delta logDoct -dod7.41998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1212314Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID22257compound was evaluated for volume apparent of distribution1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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).
AID24829compound was evaluated for saturable association constant (nKa) of isolated serum protein gamma globulins1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID165615Test against PAF-induced aggregation of rabbit platelets in vitro1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application i
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).
AID238823Binding affinity for human Histamine H1 receptor in CHO K1 cells2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
AID241255Inhibition of 5-lipoxygenase activity in human whole blood assay; not tested2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
AID26287Partition coefficient (logD3.0)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1280180Selectivity index, ratio of CC50 for human Huh7.5.1 cells infected with HCV JFH-1 virus to EC50 for HCV JFH-1 virus2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection.
AID1397344Efflux ratio of apparent permeability in MDCK cells at 10 uM after 1 hr in absence of P-gp inhibitor verapamil by UPLC-MS/MS analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood-Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases.
AID24350compound was evaluated for half life in humans1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1193496Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
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).
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.
AID85241Number of binding sites (n) of isolated serum protein HSA1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID23738Lipophilicity parameter log Poct A1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID26610compound was evaluated for microscopic pKa BZ value through pKa BN.1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
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).
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.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID86595In vitro inhibitory activity against histamine H1 receptor in guinea-pig ileum at 0.1 uM1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis of piperazine derivatives and evaluation of their antihistamine and antibradykinin effects.
AID43303In vitro inhibitory activity against Bradykinin receptor B2 in isolated rat ileum at 0.1 uM1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis of piperazine derivatives and evaluation of their antihistamine and antibradykinin effects.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID1193493Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
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).
AID85242Number of binding sites (n) of isolated serum protein HSA with FFA1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Molecular properties and pharmacokinetic behavior of cetirizine, a zwitterionic H1-receptor antagonist.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
AID1798265H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\2005The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
AID1346037Human H1 receptor (Histamine receptors)1994European journal of biochemistry, Sep-01, Volume: 224, Issue:2
Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,325)

TimeframeStudies, This Drug (%)All Drugs %
pre-199042 (3.17)18.7374
1990's337 (25.43)18.2507
2000's482 (36.38)29.6817
2010's361 (27.25)24.3611
2020's103 (7.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 113.18

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 Index113.18 (24.57)
Research Supply Index7.61 (2.92)
Research Growth Index5.38 (4.65)
Search Engine Demand Index281.64 (26.88)
Search Engine Supply Index2.68 (0.95)

This Compound (113.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials547 (36.96%)5.53%
Reviews147 (9.93%)6.00%
Case Studies182 (12.30%)4.05%
Observational5 (0.34%)0.25%
Other599 (40.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (107)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Efficacy and Safety of Levocetirizine Alone or in Combination With Tranexamic Acid in the Treatment of Spontaneous Chronic Urticaria. Multicentric Controlled Randomized Study in Cross-over, Double-blind [NCT03789422]Phase 480 participants (Anticipated)Interventional2019-12-10Recruiting
A Randomized, Open-Label, Single-Dose, Three-Period Crossover Bioequivalence Study to Compare an Orodispersible Tablet (ODT) Formulation of Cetirizine HCl 10 mg Taken With and Without Water Compared With a Standard Marketed 10 mg Tablet Taken With Water [NCT01322282]Phase 136 participants (Actual)Interventional2011-02-28Completed
Efficacy and Safety of 20 mg Levocetirizine and 15 mg Levocetirizine + 50 mg Bed-Time Hydroxyzine in Severe Chronic Urticaria in Adults: a Pilot, Randomized, Double-blind, Cross-over and Parallel, Active-controlled, Single-centre Study [NCT01250652]Phase 424 participants (Actual)Interventional2011-03-31Completed
A Single Centre, Single Dose, Open-label, Randomized, 2-part, 2-way Crossover Study to Determine the Bioequivalence of Levocetirizine Oral Disintegrating Tablet Given With Water and Without Water Compared to Levocetirizine Immediate Release Tablet in Heal [NCT03555890]Phase 172 participants (Actual)Interventional2018-05-18Completed
Personalized Treatment Algorithms for Difficult-to-treat Asthma: Bench to Community [NCT04179461]Phase 221 participants (Actual)Interventional2018-03-16Completed
Effects of Treated and Untreated Allergic Rhinitis on Mood, Cognitive Functions and Actual Driving Performance [NCT01318681]22 participants (Actual)Interventional2011-01-31Completed
A Multicenter, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group Study Investigating the Clinical Effects of Montelukast in Patients With Perennial Allergic Rhinitis [NCT00974571]Phase 31,365 participants (Actual)Interventional2001-11-30Completed
A Single-Center, Pediatric, Comparative Taste Test of Desloratadine and Cetirizine Antihistamine Syrup Medications [NCT00794378]Phase 3202 participants (Actual)Interventional2004-11-30Completed
Single Arm Study To Assess Comprehensive Infusion Guidance For The Management Of The Infusion- Associated Reactions (IARs) In Relapsing-Remitting Multiple Sclerosis (RRMS) Patients Treated With LEMTRADA [NCT02205489]Phase 458 participants (Actual)Interventional2014-10-31Completed
Mast Cells in Male Pelvic Pain and and Lower Urinary Tract Dysfunction [NCT03167216]Early Phase 120 participants (Actual)Interventional2017-08-01Completed
A Phase 1/2 First-in-human, Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Ascending Doses and Repeat Doses of UX053 in Patients With GSD III [NCT04990388]Phase 1/Phase 28 participants (Actual)Interventional2021-10-18Terminated(stopped due to Sponsor decision not related to safety concerns)
OPV117059: A Long-Term Extension Study of Ofatumumab Injection for Subcutaneous Use in Subjects With Pemphigus Vulgaris [NCT02613910]Phase 31 participants (Actual)Interventional2015-12-23Terminated(stopped due to Novartis has acquired the rights to ofatumumab and terminated the OPV116910 and OPV117059 studies. This decision is not linked to any safety consideration.)
Gabapentin Kinetic Disposition and Renal Excretion: Role of Transporters for Organic Cations and the Effect of Glycemic Control in Patients With Neuropathic Pain. [NCT03047278]Phase 429 participants (Actual)Interventional2015-11-01Completed
A Phase III, Comparative Study for the Efficacy and Safety of Bilastine 20 mg Versus Cetirizine 10 mg and Placebo in the Treatment of Perennial Allergic Rhinitis During 4 Weeks, Followed by a Long-term Safety Extension With Bilastine 20 mg [NCT01127620]Phase 3650 participants (Actual)Interventional2004-05-31Completed
Effect of an H1 Receptor Antagonist on Exercise Performance in Hypoxia [NCT03192488]Phase 413 participants (Actual)Interventional2017-08-31Completed
Comparing the Risk and Severity of Infusion-Related Reactions in Patients Premedicated With Cetirizine Versus Diphenhydramine Prior to Ocrelizumab Infusions [NCT04175834]Phase 352 participants (Anticipated)Interventional2020-02-05Active, not recruiting
A Randomized, Open Label, Balanced, Two-Treatment, Two-Period, Two-Sequence, Single Dose, Crossover, Bioequivalence Study of Levocetirizine Dihydrochloride 5 mg Tablets With Xyzal® 5 mg Tablets in Normal, Healthy, Adult, Human Subjects Under Fed Condition [NCT01567501]Phase 128 participants (Actual)Interventional2012-02-29Completed
A Comparative Double-blind, Double-dummy Study of Desloratadine (DL) 5 mg Once Daily, Cetirizine 10 mg Once Daily, and Placebo Once Daily in Patients With Chronic Idiopathic Urticaria (CIU) [NCT00751166]Phase 4149 participants (Actual)Interventional2004-03-01Terminated(stopped due to Study could not be re-supplied with study medication in a timely manner.)
Double Blind, Double-dummy, Five Parallel Groups, Randomized, Exploratory Clinical Trial to Compare the Efficacy of Single Dose of Levocetirizine 2.5 mg Oral Drops (5 mg/mL), Levocetirizine 5 mg Oral Tablets, Cetirizine 5 mg Oral Drops (10 mg/mL) and Ceti [NCT00291642]Phase 2551 participants (Actual)Interventional2006-01-01Completed
Multi-center, Double-blind, Double-dummy, Randomized, Placebo-controlled, Active-reference, Parallel-group Study to Evaluate the Efficacy, Safety, and Tolerability of ACT-129968 in Adolescent, Adult & Elderly Patients With Seasonal Allergic Rhinitis [NCT01484119]Phase 3630 participants (Actual)Interventional2011-12-31Completed
A Phase 1, Open-Label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of ARC-520 at Varying Infusion Rates in Normal Adult Volunteers [NCT02535416]Phase 140 participants (Actual)Interventional2015-09-30Completed
Preference Evaluation of Clarinex Tablets vs. Zyrtec Tablets in Subjects With Symptomatic Allergic Rhinitis [NCT00794846]Phase 4124 participants (Actual)Interventional2002-12-31Completed
Organ Protective Effect of Histamine H1 Receptor Antagonist In Patients With Severe Burns: A Clinical Study [NCT06126991]Phase 1/Phase 232 participants (Anticipated)Interventional2023-11-01Recruiting
A Randomized, Double-blind, Placebo-controlled, Prospective Clinical Trial Evaluating the Role of Systemic Antihistamine Therapy in the Reduction of Adverse Effects Associated With Topical 5-aminolevulinic Acid Photodynamic Therapy [NCT02451579]20 participants (Anticipated)Interventional2015-02-28Completed
Randomized, Double-blind, Placebo-controlled Trial to Evaluate the Efficacy of Cetirizine and Famotidine in Reducing the Duration of Symptoms in Patients With COVID-19: A Pilot Study [NCT04836806]Phase 40 participants (Actual)Interventional2021-08-31Withdrawn(stopped due to Study stopped due to issues with enrollment and lack of funding.)
A Randomized, Double-blind, Double-dummy, Placebo Controlled Three-period Incomplete Cross Over Study to Compare the Effect of Combined Treatment With QAV680 and Cetirizine on Total Nasal Symptom Score in Allergic Rhinitis Patients in an Environmental Exp [NCT01103050]Phase 260 participants (Actual)Interventional2010-03-22Completed
Single-Dose Food In Vivo Bioequivalence Study of Cetirizine HCl Tablets (10 mg; Mylan) and Zyrtec® (10 mg; Pfizer) in Healthy Volunteers [NCT00649857]Phase 118 participants (Actual)Interventional2002-11-30Completed
Efficacy and Safety of Concomitant Montelukast Sodium and Levocetirizine Dihydrochloride in Perennial Allergic Rhinitis (PAR) Patients : A Randomized, Double-blind, Active-controlled, Multicenter Phase 3 Clinical Trial [NCT01640535]Phase 3283 participants (Actual)Interventional2012-06-30Completed
A Placebo Controlled Trial to Evaluate The Effects of Levocetirizine on Nasal Allergen Challenge And Adenosine Monophosphate Challenge In Patients With Intermittent and Persistent Allergic Rhinitis [NCT00679250]Phase 425 participants (Actual)Interventional2005-11-30Completed
A Double-blind, Parallel, Active Comparator Controlled, Randomized Trial; Comparison of the Efficacy and Safety in Children With Perennial Allergic Rhinitis of Cetirizine Tablets Versus Ketotifen Dry Syrup [NCT00639587]Phase 3149 participants (Actual)Interventional2002-08-31Completed
Is Levocetirizine Less Sedating Than Cetirizine? A Randomized, Double-blind, Placebo Controlled Trial. [NCT00826943]Phase 430 participants (Actual)Interventional2009-01-31Completed
An Open Label, Randomized, Single-Center, Single-Dose, Two-Treatment, Two-Period, Crossover Bioavailability Study Comparing Cetirizine Hydrochloride 10 mg Tablet of Ohm Laboratories Inc. (A Subsidiary of Ranbaxy, Inc) With Zyrtec® Cetirizine Hydrochloride [NCT00776139]32 participants (Actual)Interventional2004-10-31Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Cetirizine HCl Tablets (10 mg; Mylan) and Zyrtec® Tablets (10 mg; Pfizer) in Healthy Volunteers [NCT00650065]Phase 126 participants (Actual)Interventional2002-11-30Completed
A Randomised, Double-blind, Placebo-controlled, 4-period Incomplete Block Crossover Study of Single Oral Dose GSK835726 (100mg, 50mg, 10mg), Cetirizine (10mg) and Placebo to Evaluate the Efficacy and Safety Using an Environmental Challenge Chamber in Male [NCT00851344]Phase 254 participants (Actual)Interventional2008-09-30Completed
Single Dose Two-Way Crossover Fed Bioequivalence Study of Cetirizine Hydrochloride 10 mg Tablets in Healthy Volunteers [NCT00863902]Phase 126 participants (Actual)Interventional2006-08-31Completed
Feasibility of a Randomized Controlled Clinical Trial Comparing the Use of Cetirizine to Replace Diphenhydramine in the Prevention of Reactions Related to Paclitaxel [NCT04237090]Phase 327 participants (Actual)Interventional2020-02-14Completed
A Randomised, Double-blind, Placebo-controlled 4-period Cross-over Study to Assess the Efficacy and Safety of Repeat Dose Intranasal GSK1004723 (1000µg), Oral GSK835726 (10mg) and Cetirizine (10mg) in the Environmental Challenge Chamber in Subjects With S [NCT00972504]Phase 254 participants (Actual)Interventional2009-06-01Completed
Single Dose Two-Way Crossover Fasted Bioequivalence Study of Cetirizine Hydrochloride 10 mg Tablets in Healthy Volunteers [NCT00864279]Phase 126 participants (Actual)Interventional2006-08-31Completed
A Single-Dose Comparative Bioavailability Study of Two Formulations of Cetirizine Hydrochloride/Pseudoephedrine Hydrochloride 5 mg/120 mg Extended Release Tablets Under Fasting Conditions [NCT00881127]Phase 140 participants (Actual)Interventional2005-07-31Completed
Topical Cetirizine Versus Topical Betamethasone in Treatment of Localized Alopecia Areata [NCT05803070]59 participants (Anticipated)Observational2023-09-01Not yet recruiting
A Comparative Double-Blind, Double- Dummy Study of Desloratadine (DL) 5 MG Once Daily, Cetirizine 10 MG Once Daily, and Placebo Once Daily in Patients With Chronic Idiopathic Urticaria (CIU) [NCT00751218]Phase 4174 participants (Actual)Interventional2004-05-06Completed
A Randomized, Parallel, Double-blind, Multi-center, Comparative Study to Exploratively Evaluate the Efficacy and Safety of Cosalin® Monotherapy vs. Cosalin® and Xarlin® Combination Therapy in Patients With Allergic Rhinitis [NCT01062139]Phase 4100 participants (Actual)Interventional2009-10-31Enrolling by invitation
3-D Visualization of the Anti-Obstructive Effect of Levocetirizine - A Monocentric Clinical Trail With One Patient (Phase-IV-Study) [NCT01000792]Phase 31 participants (Actual)Interventional2009-11-30Completed
A Single-Center, Single-Dose, Double-Blind, Modified-Double-Dummy, Placebo and Active-Controlled, Randomized, Three-Way, Six-Sequence Cross-Over Study to Investigate the Effect of JNJ-39758979 on Histamine Induced Pruritus in Healthy Male Subjects [NCT01068223]Phase 124 participants (Actual)Interventional2010-02-28Completed
A Single-Dose Comparative Bioavailability Study of Two Formulations of Cetirizine Hydrochloride/Pseudoephedrine Hydrochloride 5 mg/120 mg Extended Release Tablets Under Fed Conditions [NCT00881634]Phase 140 participants (Actual)Interventional2005-06-30Completed
Randomized, Double Blind, Parallel Group, Placebo Controlled, Multi-Center Study of the Efficacy and Safety of Zyrtec® (Cetirizine HCl) Syrup vs. Claritin® (Loratadine) Syrup vs. Placebo in Treatment of Children With Seasonal Allergic Rhinitis (SAR) [NCT02932774]Phase 4683 participants (Actual)Interventional2001-03-31Completed
A Double-Blind, Randomized, Placebo Controlled Study of An Oral Antihistamine on Local Injection Site Reactions Among Persons With Multiple Sclerosis Who Perform Daily Injections of Copaxone® Using Autoject® 2 for Glass Syringe. [NCT00240032]Phase 480 participants (Actual)Interventional2004-10-31Completed
A Two Way, Open Label, Single Dose, Cross Over, Experimental Evaluation of Relative Bioavailabilities of Two Formulations of Cetirizine Hydrochloride Tablets 10 mg in Healthy Adult Human Male Subjects Under Fed Conditions. [NCT01064115]Phase 130 participants (Actual)Interventional2006-01-31Completed
Experimental Evaluation of Relative Bioavailabilities of Two Formulations of Cetirizine Hydrochloride Tablets 10 mg in Healthy Adult Human Male Subjects Under Fasting Conditions. [NCT01064102]Phase 130 participants (Actual)Interventional2006-01-31Completed
A Phase 2 Exploratory Study of Intravenous QUZYTTIR™ (Cetirizine Hydrochloride Injection) Versus Intravenous Diphenhydramine in the Prevention of Hypersensitivity Infusion Reactions [NCT04189588]Phase 234 participants (Actual)Interventional2020-03-25Completed
Evaluation of the Inhibitory Effect of 5 Anti-Histamines in Urticaria [NCT01940393]Phase 4150 participants (Actual)Interventional2013-08-31Completed
A Randomized, Double-Blind, 4 Way Cross-over, Placebo Controlled Trial to Evaluate the Onset of Action of Bilastine 20 mg vs. Placebo, Cetirizine 10 mg, and Fexofenadine 120 mg in the Vienna Challenge Chamber [NCT00420082]Phase 275 participants (Actual)Interventional2006-10-31Completed
A Phase 1, Placebo-Controlled, Crossover, Subject- And Investigator-Blind, Sponsor-Open Study To Evaluate The Safety, Tolerability, Pharmacokinetics, And Effects On Histamine-Induced Wheal Of A Modified-Release Formulation Of PF-05180999 In Healthy Adult [NCT01981499]Phase 131 participants (Actual)Interventional2014-01-31Terminated(stopped due to The trial was prematurely terminated on 01April2014 due to safety concerns.)
The Effect of Antihistamines on Methacholine Challenge Testing in Asthma Patients [NCT01985789]Phase 412 participants (Actual)Interventional2013-11-30Completed
[NCT02024152]Phase 124 participants (Actual)Interventional2011-03-31Completed
A Randomized, Single-Dose, Four-Treatment Crossover Bioequivalence and Food Effect Study of Test Formulation of Cetirizine 10mg Chewable Tablets Versus Two Marketed Cetirizine 10mg Immediate Release Tablets. [NCT03772158]Phase 140 participants (Actual)Interventional2018-12-11Completed
The Effects of Nedocromil Sodium and Cetirizine HCl on Exercise-induced Arterial Hypoxemia in Highly-trained Swimmers [NCT05095311]Phase 44 participants (Actual)Interventional2021-05-19Terminated(stopped due to The recruited population was no longer made available to participate in the study.)
An Open Label, Randomized, Single-center, Single-dose, Two-treatment, Two-period, Crossover Bioavailability Study Comparing Cetirizine Hydrochloride 10 mg Tablet of Ohm Laboratories Inc. (A Subsidiary of Ranbaxy, Inc) With Zyrtec® Cetirizine Hydrochloride [NCT00776022]32 participants (Actual)Interventional2005-04-30Completed
A Single-Center, Pediatric, Comparative Taste Test of Desloratadine and Cetirizine Antihistamine Syrup Medications [NCT00794794]Phase 3204 participants (Actual)Interventional2004-11-30Completed
Topical Cetirizine Gel Versus Minoxidil 5% Gel in Treatment of Androgenetic Alopecia [NCT04293822]Phase 460 participants (Anticipated)Interventional2020-06-30Not yet recruiting
A Four-Way Double-Blind, Randomized, Placebo Controlled Study to Determine the Efficacy and Speed of Azelastine Nasal Spray and Antihistaminic Agents in Adult Subjects With Allergen Induced Seasonal Allergic Rhinitis [NCT00561717]Phase 470 participants (Actual)Interventional2007-10-31Completed
A Phase 2, Multicenter, Parallel-Group, Randomized, Double-Blind, Placebo- And Active Comparator-Controlled, Combination Study Of S-555739 And Cetirizine HCl In Adult Patients With Seasonal Allergic Rhinitis [NCT01651871]Phase 2779 participants (Actual)Interventional2012-07-31Completed
A Multi-center, Open, Randomized, Three-arm, Parallel-group, Phase IV Study to Compare the Efficacy of Ciclesonide Nasal Spray and Levocetirizine, Alone and in Combination for the Patient With Allergic Rhinitis [NCT01430260]Phase 4349 participants (Actual)Interventional2011-01-31Completed
Acupuncture for Seasonal Allergic Rhinitis (ACUSAR) - A Randomised Controlled Trial [NCT00610584]422 participants (Actual)Interventional2008-04-30Completed
Open Label, Randomized, 6-sequence Crossover Study to Evaluate the Drug-drug Interaction Between Montelukast Sodium and Levocetirizine Dihydrochloride in Health Male Volunteers [NCT01491503]Phase 130 participants (Anticipated)Interventional2011-11-30Completed
A Multi-center, Double-blind, Randomized, Placebo-controlled, Active Reference, Parallel-group, Study of ACT-129968 in Adult Patients With Seasonal Allergic Rhinitis [NCT01241214]Phase 2579 participants (Actual)Interventional2010-11-30Completed
An Investigation to Evaluate the Technique of MRI as an Assessment of the Effect of Anti-allergy Drug Treatment on Internal Nasal and Sinus Mucosal Anatomy Following Intranasal Allergen Challenge in Subjects With Seasonal Allergic Rhinitis. [NCT00517946]21 participants (Actual)Observational2007-03-31Completed
A Double-Blind, Randomized, Placebo-Controlled, Cross-Over, Allergen Challenge Study to Evaluate Taste and Local Tolerance of NLA Nasal Spray in Patients With Allergic Rhinitis [NCT00533637]Phase 228 participants (Actual)Interventional2007-09-30Completed
Influence of H1-antihistamines on the Dermal Blood Flow Response After a Histamine Skin Prick as Well as After the Topical Application of Cinnamaldehyde and Capsaicin [NCT04399525]12 participants (Actual)Interventional2019-10-28Completed
The Role of Cetirizine in Androgenetic Alopecia in Females [NCT04481412]Phase 2/Phase 366 participants (Actual)Interventional2020-07-25Completed
[NCT01495338]Phase 160 participants (Actual)Interventional2011-12-31Completed
Pharmacokinetic Study of Levocetirizine Oral Solution-An Open-label, Randomized, Cross-over Study to Evaluate the Pharmacokinetics, the Safety and Tolerability of Levocetirizine Oral Solution (5 mg) and Cetirizine Dry Syrup (10 mg), Following a Single Dos [NCT01622283]Phase 120 participants (Actual)Interventional2012-05-02Completed
Evaluation of the Efficacy and Safety of Cetirizine Dry Syrup in Children -Suffering From Atopic Dermatitis- [NCT00257569]Phase 3278 participants Interventional2005-08-31Completed
Comparison of the Effect of Montelukast and Cetirizine on Allergic Inflammation Measured by Exhaled Nitric Oxide Concentration in Children With Seasonal Allergic Rhinitis [NCT00488176]Phase 4116 participants (Anticipated)Interventional2007-04-30Recruiting
A Randomized, Double Blind, Placebo Controlled Study for Evaluation of the Efficacy and Safety of Cetirizine Dry Syrup (CTZ DS) (2.5 mg or 5 mg Twice a Day) in Children (2 Years of Age or Older But Under 15 Years Old) Suffering From Perennial Allergic Rhi [NCT00490204]Phase 3239 participants (Actual)Interventional2007-07-27Completed
Assessment of Bronchodilatory Effects of Cetirizine in Adults With Concomitant Allergic Rhinitis and Mild Asthma as Measured by Impulse Oscillometry. [NCT01781507]Phase 421 participants (Actual)Interventional2011-06-30Completed
Double-blind, Randomised, Placebo-controlled, Phase III Study Comparing the Efficacy and Safety of Bilastine 20 mg Once Daily and Cetirizine 10 mg for the Treatment of Seasonal Allergic Rhinitis. [NCT00504933]Phase 3683 participants (Actual)Interventional2005-05-31Completed
A Multi-Center, Double-Masked, Randomized, Vehicle-Controlled, Evaluation of the Onset and Duration of Action of Cetirizine 0.24% Ophthalmic Solution (Formula AFH-002) Compared to Vehicle (Formula AFH-001) in the Conjunctival Allergen Challenge (CAC) Mode [NCT01551056]Phase 391 participants (Actual)Interventional2012-03-31Completed
A Multi-centre, Double-blind, Double-dummy, Randomized, Active-controlled Phase III Study to Evaluate the Efficacy and Safety of Xyzal® 5mg od vs Zyrtec® 10mg od in Subjects Aged 15 Years and Above With Dermatitis and Eczema [NCT00375713]Phase 3466 participants (Actual)Interventional2005-10-31Completed
Efficacy and Cost Analysis of Steroids in Treatment of Otitis Media With Effusion (OME) Compared to That of Combination of Antibiotic, Antihistaminic, and Nasal Decongestant [NCT03590912]Phase 4160 participants (Actual)Interventional2018-09-05Completed
A Double-blind, Double-dummy, Parallel-group, Placebo-controlled, Randomized Study to Assess the Duration of the Suppressive Effects of Desloratadine on the Cutaneous Allergen-induced Wheal and Flare (1) Response After Discontinuation [NCT00359138]Phase 436 participants (Actual)Interventional2006-02-28Completed
Camillian Saint Mary's Hospital Luodong [NCT05348148]450 participants (Anticipated)Interventional2020-06-16Recruiting
Long-term Study of Cetirizine Dry Syrup in Children. Suffering From Perennial Allergic Rhinitis. [NCT00257595]Phase 330 participants Interventional2005-08-31Completed
Evaluation of the Efficacy and Safety of Cetirizine Dry Syrup in Children -Suffering From Perennial Allergic Rhinitis- [NCT00253058]Phase 3286 participants Interventional2005-07-31Completed
Long-term Study of Cetirizine Dry Syrup in Children Suffering From Various Type of Cutaneous Disease Accompanied With Pruritus. [NCT00257582]Phase 360 participants Interventional2005-08-31Completed
A Randomized, Double Blind, Placebo-controlled, Four Way Cross-over Study to Assess the Effect of a Combination of Cetirizine With Pseudoephedrine Versus Cetirizine Alone on Symptoms Scores and Rhinomanometry in Patients With Allergic Rhinitis Following P [NCT00334698]51 participants (Anticipated)Interventional2006-07-31Completed
A Randomised, Placebo Controlled, Four Period Crossover Study to Evaluate the Efficacy, Safety of Oral Repeat Doses of ONO-4053 and Cetirizine in Subjects With Seasonal Allergic Rhinitis in the Vienna Challenge Chamber. [NCT01748344]Phase 258 participants (Actual)Interventional2012-11-30Completed
An Open Label, add-on Trial of Cetirizine for Patients With Neuromyelitis Optica [NCT02865018]Phase 1/Phase 216 participants (Actual)Interventional2014-04-30Completed
A Single Blind, Randomized, Single Oral Dose Study to Compare the Oral Disposition of Levocetirizine When Given Alone (5mg) or as the Racemate (Cetirizine 10mg), and to Investigate the Safety and Tolerability and the Pharmacokinetics of Levocetirizine and [NCT02447393]Phase 120 participants (Actual)Interventional2008-03-18Completed
A Single Center, Double-Masked, Randomized, Vehicle-Controlled, Parallel-Group Study Evaluating the Efficacy of Three Different Concentrations of Cetirizine (0.05%, 0.1%, and 0.24%) Ophthalmic Solution Versus Vehicle in the Treatment of Allergic Conjuncti [NCT01332188]Phase 2/Phase 3101 participants (Actual)Interventional2011-04-30Completed
Effect of Long Acting Antihistamine on Opioid- Induced Pruritus: A Double-blind Placebo Controlled Study [NCT01825655]Phase 43 participants (Actual)Interventional2014-09-30Terminated(stopped due to Unable to recruit patients)
A Multi-Center, Double-Masked, Randomized, Vehicle-Controlled, Evaluation of the Onset and Duration of Action of AC-170 0.24% Ophthalmic Solution (Formula AFH-002) Compared to Vehicle (Formula AFH-001) in the Conjunctival Allergen Challenge (CAC) Model of [NCT01881113]Phase 3101 participants (Actual)Interventional2013-06-30Completed
A Randomized, Open-Label, Single-Dose, Five-Period Crossover, Relative Bioavailability Study to Evaluate Cetirizine HCl Gummy 10 mg and Cetirizine HCl Oral Tablets 10 mg Administered in Healthy Adult Male and Female Subjects [NCT04071821]Phase 130 participants (Anticipated)Interventional2023-09-01Not yet recruiting
The Effect of Switching the H1-antagonist Clemastine to Cetirizine in Premedication Regimens During Paclitaxel Treatment: 'The H1-SWITCH Study' [NCT06039137]395 participants (Actual)Observational2022-06-01Active, not recruiting
Preference Evaluation of Clarinex Tablets vs. Zyrtec Tablets in Subjects With Symptomatic Allergic Rhinitis [NCT00794495]Phase 4122 participants (Actual)Interventional2002-12-31Completed
Comparability and Standardization of Controlled Allergen Challenge Facilities [NCT02543346]Phase 498 participants (Actual)Interventional2015-10-31Completed
A Multi-center, Pediatric, Open-label, Preference Study of Desloratadine 2.5 mg Reditab (SCH34117) and Zyrtec 5.0 mg Chewable Tablet Medications [NCT00779116]Phase 4217 participants (Actual)Interventional2005-09-30Completed
A Multi-Center, Open-labelled Study to Evaluate the Safety of Levocetirizine Hydrochloride Oral Solution in Children Aged 6 Months to 2 Years With Allergic Rhinitis or Pruritus Associated With the Skin Diseases. [NCT01563081]Phase 360 participants (Actual)Interventional2012-04-30Completed
A Feasibility Assessment of a Decentralized Platform Adaptive Double-Blind, Randomized Controlled Trial Investigating Repurposed Drugs in the Treatment of Post-Acute Sequelae of Coronavirus-19 (PASC) [NCT05946551]Phase 336 participants (Anticipated)Interventional2024-01-31Not yet recruiting
A Multi-Center, Double-Masked, Randomized, Vehicle-Controlled, Parallel-Group Study Evaluating the Safety of AC-170 Ophthalmic Solution [NCT02756624]Phase 3516 participants (Actual)Interventional2016-04-30Completed
Efficacy of Levocetirizine Fourfold Dosage in Chronic Spontaneous Urticaria Resistant to the Licensed Dosage [NCT02372604]Phase 315 participants (Actual)Interventional2015-07-31Completed
A Multi-Center, Double-Masked, Randomized, Vehicle-Controlled, Parallel-Group Study Evaluating the Safety of AC-170 0.24% Ophthalmic Solution Used Twice Daily in Healthy Adult Subjects and in Pediatric Subjects With a History or Family History of Atopic D [NCT02132169]Phase 3512 participants (Actual)Interventional2014-05-31Completed
Preference Evaluation of Clarinex Tablets vs. Zyrtec Tablets in Subjects With Symptomatic Allergic Rhinitis [NCT00794599]Phase 4118 participants (Actual)Interventional2002-12-31Completed
Study 200165, A Randomized, Double-Blind, Placebo-Controlled, Multi-Center, Parallel-Group Study to Compare the Efficacy of a 2-Week Treatment With Fluticasone Propionate Nasal Spray Versus Cetirizine in Adult Subjects With Seasonal Allergic Rhinitis (SAR [NCT01916226]Phase 4682 participants (Actual)Interventional2013-08-01Completed
A Single-Center, Double-Masked, Randomization, Vehicle-Controlled, Evaluation of the Onset and Duration of Action of AC-170 0.24% Ophthalmic Solution (Formula AFH-002) Compared to Vehicle (Formula AFH-001) in the Conjunctival Allergen Challenge (CAC) Mode [NCT01685242]Phase 3100 participants (Actual)Interventional2012-09-30Completed
The Effect of Cetirizine on Bronchoconstriction in Patients With Allergic Rhinitis and Wheezing in the Pediatric Emergency Department [NCT03340740]Phase 440 participants (Actual)Interventional2018-05-11Completed
A Multi-Center, Pediatric, Open-Label, Preference Study of Desloratadine 2.5 mg Reditab (SCH34117) and Zyrtec ® 5.0 mg Chewable Tablet Medications [NCT00780403]Phase 4220 participants (Actual)Interventional2005-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00291642 (9) [back to overview]Change From Baseline in the Total Symptom Complex (TSC) Score Over Period I
NCT00291642 (9) [back to overview]Change From Baseline in the MSC Score Over the Total Treatment Period (Period I + Period II)
NCT00291642 (9) [back to overview]Change From Baseline in the MSC Score Over Period II
NCT00291642 (9) [back to overview]Change From Baseline in the Major Symptom Complex (MSC) Score Over Period I
NCT00291642 (9) [back to overview]Change From Baseline in the Individual Symptom Scores Over the Total Treatment Period (Period I + Period II)
NCT00291642 (9) [back to overview]Change From Baseline in the Individual Symptom Scores Over Period II
NCT00291642 (9) [back to overview]Change From Baseline in the Individual Symptom Scores Over Period I
NCT00291642 (9) [back to overview]Change From Baseline in the Total Symptom Complex (TSC) Score Over the Total Treatment Period (Period I + Period II)
NCT00291642 (9) [back to overview]Change From Baseline in the Total Symptom Complex (TSC) Score Over Period II
NCT00359138 (1) [back to overview]Duration of Suppressive Effect of Desloratadine After Discontinuation of a 1-week Treatment
NCT00375713 (4) [back to overview]Responder Status According to Pruritus Severity Score (Response = Mild or None in Pruritus Severity Score).
NCT00375713 (4) [back to overview]Change From Baseline in the Mean Pruritus Severity Score at Endpoint During the 14 Day Treatment Period
NCT00375713 (4) [back to overview]Duration of Pruritus (Stated in Categories) at Endpoint During the 14 Day Treatment Period
NCT00375713 (4) [back to overview]Global Improvement at Endpoint During the 14 Day Treatment Period
NCT00779116 (1) [back to overview]Number of Subjects Who Preferred Desloratadine RediTab or Zyrtec Chewable Tablet.
NCT00780403 (1) [back to overview]Number of Subjects Who Preferred Desloratadine RediTab or Zyrtec Chewable Tablet.
NCT00826943 (3) [back to overview]Total Four Symptom Scores (Allergy Symptoms)
NCT00826943 (3) [back to overview]Modified Epworth Sleepiness Scale
NCT00826943 (3) [back to overview]Likert Score Rating Global Sedation
NCT00972504 (6) [back to overview]Weighted Mean of the Individual Components of TNSS (Sneeze, Itch, Rhinorrhoea and Nasal Blockage) 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3
NCT00972504 (6) [back to overview]Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)
NCT00972504 (6) [back to overview]Weighted Mean Nasal Congestion VAS 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3
NCT00972504 (6) [back to overview]Mean Forced Expiratory Volume in 1 Second (FEV1)
NCT00972504 (6) [back to overview]Weighted Mean Wet Tissue Weight (as a Surrogate Marker of Nasal Secretion) 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3
NCT00972504 (6) [back to overview]Weighted Mean TNSS (Sneeze, Itch, Rhinorrhoea and Nasal Blockage) 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3
NCT00974571 (5) [back to overview]Physician's Global Evaluation of Allergic Rhinitis
NCT00974571 (5) [back to overview]Patient's Global Evaluation of Allergic Rhinitis
NCT00974571 (5) [back to overview]Mean Change From Baseline in Nighttime Symptoms Score
NCT00974571 (5) [back to overview]Mean Change From Baseline in Daytime Nasal Symptoms Score
NCT00974571 (5) [back to overview]Mean Change From Baseline in Composite Symptoms Score
NCT01332188 (37) [back to overview]Ear or Palate Pruritus at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Ear or Palate Pruritus at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Ear or Palate Pruritus at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Conjunctival Redness at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Conjunctival Redness at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Conjunctival Redness at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Ciliary Redness at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Ciliary Redness at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Ciliary Redness at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Chemosis at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Chemosis at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Chemosis at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Eyelid Swelling at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Tolerability of Study Medication at Visit 3A
NCT01332188 (37) [back to overview]Tearing at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Tearing at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Tearing at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Rhinorrhea at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Rhinorrhea at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Rhinorrhea at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Ocular Itching at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Ocular Itching at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Ocular Itching at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Nasal Pruritus at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Nasal Pruritus at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Nasal Pruritus at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Nasal Congestion at Onset of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Nasal Congestion at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Nasal Congestion at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Nasal Composite Score at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Nasal Composite Score at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Nasal Composite Score at Duration of Action (16 Hours Post-dose)
NCT01332188 (37) [back to overview]Eyelid Swelling at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Eyelid Swelling at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Episcleral Redness at Onset of Action (15 Minutes Post-dose)
NCT01332188 (37) [back to overview]Episcleral Redness at Duration of Action (24 Hours Post-dose)
NCT01332188 (37) [back to overview]Episcleral Redness at Duration of Action (16 Hours Post-dose)
NCT01551056 (25) [back to overview]Ear or Palate Pruritis at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Episcleral Redness at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Episcleral Redness at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Eyelid Swelling at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Eyelid Swelling at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Nasal Congestion at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Nasal Congestion at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Nasal Pruritis at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Nasal Pruritis at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Ciliary Redness at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Conjunctival Redness at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Conjunctival Redness at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Ear or Palate Pruritis at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Tolerability of Study Medication at Visit 3A
NCT01551056 (25) [back to overview]Tearing at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Tearing at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Rhinorrhea at Duration of Action (16 Hours +1 Hour Post-dose)
NCT01551056 (25) [back to overview]Number of Participants With At Least One of the Nasal Symptoms Present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Ocular Itching at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Number of Participants With At Least One of the Nasal Symptoms Present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Ocular Itching at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Rhinorrhea at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Chemosis at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01551056 (25) [back to overview]Chemosis at Onset of Action (15 Minutes Post-dose)
NCT01551056 (25) [back to overview]Ciliary Redness at Duration of Action (16 Hours + 1 Hour Post-dose)
NCT01563081 (5) [back to overview]Number of Participants Categorized With the Indicated Pruritis Severity on the First Day of Treatment and at Weeks 1 and 2/Early Withdrawal
NCT01563081 (5) [back to overview]Number of Participants With Serious Adverse Events (SAEs) and Non-serious Adverse Events (AEs)
NCT01563081 (5) [back to overview]Number of Participants With the Indicated Change From the First Day of Treatment in Allergic Rhinitis and Pruritis Associated With Skin Diseases at Weeks 1 and 2/EW, as Assessed by the Investigator/Sub-investigator Based on Legal Representative Impression
NCT01563081 (5) [back to overview]Number of Participants With the Indicated Change From the First Day of Treatment in Nasal Symptoms and Pruritis Associated With Skin Diseases at Weeks 1 and 2/Early Withdrawal, as Assessed by the Investigator or Sub-investigator
NCT01563081 (5) [back to overview]Cmax and Cmin of Levocetirizine in Plasma
NCT01685242 (25) [back to overview]Tolerability of Study Medication at Visit 3A
NCT01685242 (25) [back to overview]Tearing at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Tearing at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Rhinorrhea at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Chemosis at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Chemosis at Onset of Action (15 Minutes)
NCT01685242 (25) [back to overview]Ciliary Redness at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Conjunctival Redness at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Conjunctival Redness at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Ear or Palate Pruritus at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Ear or Palate Pruritus at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Episcleral Redness at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Nasal Pruritus at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Nasal Pruritus at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Ocular Itching at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Rhinorrhea at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Eyelid Swelling at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Episcleral Redness at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Ciliary Redness at Duration of Action (8 Hours + 30 Minutes)
NCT01685242 (25) [back to overview]Nasal Composite Score at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Nasal Composite Score at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Nasal Congestion at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Ocular Itching at Duration of Action (8 Hours + 30 Minutes Post-dose)
NCT01685242 (25) [back to overview]Eyelid Swelling at Onset of Action (15 Minutes Post-dose)
NCT01685242 (25) [back to overview]Nasal Congestion at Onset of Action (15 Minutes Post-dose)
NCT01825655 (1) [back to overview]Change in Itch Score
NCT01881113 (25) [back to overview]Ocular Itching at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Ocular Itching at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Percentage of Participants With At Least One Nasal Symptom at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Percentage of Participants With At Least One Nasal Symptom at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Rhinorrhea at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Rhinorrhea at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Tearing at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Tearing at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Tolerability of Study Medication at Visit 3A
NCT01881113 (25) [back to overview]Eyelid Swelling at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Chemosis at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Chemosis at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Ciliary Redness at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Ciliary Redness at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Conjunctival Redness at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Conjunctival Redness at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Ear or Palate Pruritus at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Ear or Palate Pruritus at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Episcleral Redness at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Episcleral Redness at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Eyelid Swelling at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Nasal Congestion at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Nasal Congestion at Onset of Action (15 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Nasal Pruritus at Duration of Action (8 Hours + 30 Minutes Post-Dose)
NCT01881113 (25) [back to overview]Nasal Pruritus at Onset of Action (15 Minutes Post-Dose)
NCT01916226 (7) [back to overview]Mean Change From Baseline in the Individual AM Reflective Nasal Symptom Scores for Rhinorrhea, Nasal Congestion, Nasal Itching, and Sneezing Over the Entire Treatment Period
NCT01916226 (7) [back to overview]Mean Change From Baseline in the Nocturnal Rhinoconjunctivitis Quality of Life Questionnaire (NRQLQ) Overall Score at Visit 3/Early Withdrawal.
NCT01916226 (7) [back to overview]Mean Change From Baseline in the Combined Nasal and Ocular Reflective Total Symptom Score (rTSS = rTNSS+rTOSS) Over the Entire Treatment Period
NCT01916226 (7) [back to overview]Mean Change From Baseline in the AM Pre-dose Reflective Total Ocular Symptom Score (rTOSS) Over the Entire Treatment Period
NCT01916226 (7) [back to overview]Mean Change From Baseline in the AM Pre-dose Instantaneous Total Ocular Symptom Score (iTOSS) Over the Entire Treatment Period
NCT01916226 (7) [back to overview]Mean Change From Baseline in the AM Pre-dose Instantaneous Total Nasal Symptom Score (iTNSS) Over the Entire Treatment Period
NCT01916226 (7) [back to overview]Mean Change From Baseline (CFB) in the Individual AM Reflective Total Nasal Symptom Scores (rTNSS) Over the Entire Treatment Period
NCT02132169 (4) [back to overview]Tolerability of AC 170 0.24% Compared to Its Vehicle at Visit 1 (Day 1)
NCT02132169 (4) [back to overview]Safety of AC 170 0.024% Compared to Its Vehicle
NCT02132169 (4) [back to overview]Tolerability of AC 170 0.24% Compared to Its Vehicle at Visit 3 (Day 22)
NCT02132169 (4) [back to overview]Tolerability of AC 170 0.24% Compared to Its Vehicle at Visit 2 (Day 8)
NCT02535416 (9) [back to overview]Pharmacokinetics: Area Under the Plasma Concentration Versus Time Curve From Zero Extrapolated to Infinity (AUCinf) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Pharmacokinetics: Apparent Volume of Distribution (V) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT02535416 (9) [back to overview]Pharmacokinetics: Area Under the Plasma Concentration-Time Curve From Time 0 to the Last Quantifiable Plasma Concentration (AUClast) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Pharmacokinetics: Terminal Elimination Rate Constant (Lambda z) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Pharmacokinetics: Maximum Plasma Concentration (Cmax) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Pharmacokinetics: Half-Life (t1/2) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Pharmacokinetics: Clearance (CL) of the Analytes of ARC-520
NCT02535416 (9) [back to overview]Pharmacokinetics: Area Under the Plasma Concentration Versus Time Curve From Zero to 24 Hours (AUC0-24) of the Analytes of ARC-520
NCT02543346 (5) [back to overview]Comparison of VAS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.
NCT02543346 (5) [back to overview]Comparison of TRSS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.
NCT02543346 (5) [back to overview]Comparison of TOSS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.
NCT02543346 (5) [back to overview]Comparison of TNSS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.
NCT02543346 (5) [back to overview]Comparison of GRCS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.
NCT02613910 (11) [back to overview]Number of Participants With Adverse Events(AEs) and AEs Leading to Permanent Discontinuation of Ofatumumab SC (AELD)
NCT02613910 (11) [back to overview]Number of Participants With Adverse Events Related to Ofatumumab SC
NCT02613910 (11) [back to overview]Number of Participants Withdrawn Due to Treatment-related AEs
NCT02613910 (11) [back to overview]Number of Participants With Vital Signs of Clinical Concern
NCT02613910 (11) [back to overview]Number of Participants With Severe Adverse Events
NCT02613910 (11) [back to overview]Number of Participants With Post-injection Systemic Reactions
NCT02613910 (11) [back to overview]Number of Participants With Laboratory Results of Potential Clinical Concern
NCT02613910 (11) [back to overview]Number of Participants With Injection Site Reactions
NCT02613910 (11) [back to overview]Number of Participants With Serious Adverse Events (SAEs) and AEs of Special Interest (AESI)
NCT02613910 (11) [back to overview]Number of Participants With Infections
NCT02613910 (11) [back to overview]Number of Participants With Clinically-significant Electrocardiogram (ECG) Abnormalities
NCT02756624 (4) [back to overview]Tolerability of AC 170 0.24% at Visit 3 (Day 22)
NCT02756624 (4) [back to overview]Tolerability of AC 170 0.24% at Visit 2 (Day 8)
NCT02756624 (4) [back to overview]Tolerability of AC 170 0.24% at Visit 1 (Day 1)
NCT02756624 (4) [back to overview]Number of Treatment Related Adverse Events
NCT02865018 (4) [back to overview]Epworth Sleepiness Scale
NCT02865018 (4) [back to overview]Annualized Relapse Rate Before Cetirizine
NCT02865018 (4) [back to overview]Eotaxin Plasma Levels
NCT02865018 (4) [back to overview]Expanded Disability Status Scale (EDSS)
NCT03192488 (2) [back to overview]Performance Time
NCT03192488 (2) [back to overview]Plasma Histamine Concentrations at Baseline and Post-Exercise
NCT03555890 (64) [back to overview]Part 1: Apparent Clearance Following Oral Dosing (CL/F) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Apparent Terminal Phase Half-life (t1/2) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Apparent Volume of Distribution Following Oral Dosing (Vz/F) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Area Under the Concentration-time Curve (AUC) From Time Zero Time (Pre-dose) to the Time of Last Quantifiable Concentration (AUC[0-t]) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Area Under the Concentration-time Curve From Zero Time (Pre-dose) Extrapolated to Infinite Time AUC(0-inf) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Change Form Baseline in Hematocrit
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Amylase Levels
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Mean Corpuscle Hemoglobin
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Mean Corpuscle Volume
NCT03555890 (64) [back to overview]Part 2: Urine Specific Gravity
NCT03555890 (64) [back to overview]Part 2: Urine Potential of Hydrogen (pH)
NCT03555890 (64) [back to overview]Part 2: Number of Participants With Urinalysis Results by Dipstick Method
NCT03555890 (64) [back to overview]Part 2: Number of Participants With AEs and SAEs
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in SBP and DBP
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in PR Interval, QRS Interval, QT Interval and QTcF Interval
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Platelet Count and White Blood Cell Count
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Hemoglobin and Mean Corpuscle Hemoglobin Concentration
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Heart Rate
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Calcium, Cholesterol, Chloride, Glucose, High Density Lipids Cholesterol, Potassium, Low Density Lipids Cholesterol, Sodium, Phosphorus Inorganic, Triglycerides and Urea/BUN Levels
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Body Temperature
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils Count
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase, Creatine Kinase, Gamma Glutamyl Transferase and Lactate Dehydrogenase Levels
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Albumin and Total Protein Levels
NCT03555890 (64) [back to overview]Part 1: Urine Specific Gravity
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Hemoglobin and Mean Corpuscle Hemoglobin Concentration
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Heart Rate (12-Lead Electrocardiogram [ECG])
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Heart Rate
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid Levels
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Calcium, Cholesterol, Chloride, Glucose, High Density Lipids Cholesterol, Potassium, Low Density Lipids Cholesterol, Sodium, Phosphorus Inorganic, Triglycerides and Urea/Blood Urea Nitrogen (BUN) Levels
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Body Temperature
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Heart Rate (ECG)
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Platelet Count and White Blood Cell Count
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase, Creatine Kinase, Gamma Glutamyl Transferase and Lactate Dehydrogenase Levels
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in PR Interval, QRS Interval, QT Interval and QTcF Interval
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT03555890 (64) [back to overview]Part 1: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT03555890 (64) [back to overview]Part 1: Number of Participants With Urinalysis Results by Dipstick Method
NCT03555890 (64) [back to overview]Part 1: Urine Potential of Hydrogen (pH)
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils Count
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Albumin and Total Protein Levels
NCT03555890 (64) [back to overview]Part 2: Vz/F of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: Tmax of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: t1/2 of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: MRT of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: Kel (lambda_z) of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: Cmax of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: CL/F of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Reticulocytes
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Red Blood Cell Count
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid Levels
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Mean Corpuscle Hemoglobin
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Amylase Levels
NCT03555890 (64) [back to overview]Part 2: Change Form Baseline in Hematocrit
NCT03555890 (64) [back to overview]Part 2: AUC(0-t) of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: AUC(0-inf) of Levocetirizine
NCT03555890 (64) [back to overview]Part 2: %AUCex of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Time to First Occurrence of Cmax (Tmax) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Percentage of AUC(0-inf) Obtained by Extrapolation (%AUCex) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Mean Residence Time (MRT) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Maximum Observed Concentration (Cmax) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Elimination Rate Constant (Kel) (lambda_z) of Levocetirizine
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Reticulocytes
NCT03555890 (64) [back to overview]Part 1: Change From Baseline in Red Blood Cell Count
NCT03555890 (64) [back to overview]Part 2: Change From Baseline in Mean Corpuscle Volume
NCT04179461 (4) [back to overview]Asthma Control Test (ACT)
NCT04179461 (4) [back to overview]Adherence of Asthma Controller Medication
NCT04179461 (4) [back to overview]Pulmonary Function Measured by Spirometry: Forced Expiratory Volume in 1 Second (FEV1) / Forced Vital Capacity (FVC)
NCT04179461 (4) [back to overview]Change in Composite Asthma Severity Index (CASI)
NCT04189588 (3) [back to overview]"Time From Injection to Readiness for Discharge"
NCT04189588 (3) [back to overview]Number of Hypersensitivity Reactions to Treatment With an Anti-CD20 Antibody or Paclitaxel
NCT04189588 (3) [back to overview]Patient Sedation Scores at 1 Hour and 2 Hours Post-injection of Antihistamine (IV Cetirizine HCl or IV Diphenhydramine) and at Discharge.

Change From Baseline in the Total Symptom Complex (TSC) Score Over Period I

"The TSC score was calculated as the sum of the following 10 individual symptom scores:~runny nose (left and right), itchy nose (left and right), sniffles, nose blows, sneezes, watery eyes, itchy eyes and ears, itchy throat, cough and postnasal drip.~Each individual symptom, except nose blows and sneezes, is rated on a 5-point scale of severity: 0 = None, 1 = a little, 2 = Moderate, 3 = Quite a bit, 4 = severe, 5 = very severe. For nose blows and sneezes, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8. The TSC score ranges from 0 to 56. Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline, Treatment Period I [Day 1, from drug intake (at 11:00 am) to 5 hours post-treatment (at 4:00 pm)]

Interventionunits on a scale (Least Squares Mean)
Placebo (PBO)-6.55
Levocetirizine (LCTZ) 2.5 mg-11.33
Levocetirizine (LCTZ) 5 mg-11.27
Cetirizine (CTZ) 5 mg-12.71
Cetirizine (CTZ) 10 mg-11.74

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Change From Baseline in the MSC Score Over the Total Treatment Period (Period I + Period II)

"Six individual symptoms which are most dominant in the rhinitis symptom profile will be combined to form the MSC severity score:~Runny nose (right and left), itchy nose (right and left), sniffles, nose blows, sneezes, watery eyes.~Each individual symptom, except nose blows and sneezes, is rated on a 5-point scale of severity: 0 = None, 1 = a little, 2 = Moderate, 3 = Quite a bit, 4 = severe, 5 = very severe. For nose blows and sneezes, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8. The total MSC score ranges from 0 - 36. Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline to Day 2

Interventionunits on a scale (Least Squares Mean)
Placebo (PBO)-3.61
Levocetirizine (LCTZ) 2.5 mg-6.80
Levocetirizine (LCTZ) 5 mg-7.10
Cetirizine (CTZ) 5 mg-7.43
Cetirizine (CTZ) 10 mg-7.72

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Change From Baseline in the MSC Score Over Period II

"Six individual symptoms which are most dominant in the rhinitis symptom profile will be combined to form the MSC severity score:~Runny nose (right and left), itchy nose (right and left), sniffles, nose blows, sneezes, watery eyes.~Each individual symptom, except nose blows and sneezes, is rated on a 5-point scale of severity: 0 = None, 1 = a little, 2 = Moderate, 3 = Quite a bit, 4 = severe, 5 = very severe. For nose blows and sneezes, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8. The total MSC score ranges from 0 - 36. Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline, Treatment Period II [Day 2, (8:30 am to 12:00 pm)]

Interventionunits on a scale (Least Squares Mean)
Placebo (PBO)-3.50
Levocetirizine (LCTZ) 2.5 mg-6.35
Levocetirizine (LCTZ) 5 mg-7.07
Cetirizine (CTZ) 5 mg-6.78
Cetirizine (CTZ) 10 mg-7.92

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Change From Baseline in the Major Symptom Complex (MSC) Score Over Period I

"Six individual symptoms which are most dominant in the rhinitis symptom profile will be combined to form the MSC severity score:~Runny nose (right and left), itchy nose (right and left), sniffles, nose blows, sneezes, watery eyes.~Each individual symptom, except nose blows and sneezes, is rated on a 5-point scale of severity: 0 = None, 1 = a little, 2 = Moderate, 3 = Quite a bit, 4 = severe, 5 = very severe. For nose blows and sneezes, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8. The total MSC score ranges from 0 - 36. Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline, Treatment Period 1 [Day 1, from drug intake (at 11:00 am) to 5 hours post-treatment (at 4:00 pm)]

Interventionunits on a scale (Least Squares Mean)
Placebo (PBO)-3.80
Levocetirizine (LCTZ) 2.5 mg-7.15
Levocetirizine (LCTZ) 5 mg-7.05
Cetirizine (CTZ) 5 mg-7.93
Cetirizine (CTZ) 10 mg-7.54

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Change From Baseline in the Individual Symptom Scores Over the Total Treatment Period (Period I + Period II)

"Individual symptom scores include Runny Nose Score, Itchy Nose Score, Sniffles Score, Watery Eyes Score, Sneezes Score, Nose Blows Score.~The subjects had to evaluate the severity of the symptoms using a scale from None to Very severe (ranging from 0 to 5).~For Sneezes Score and Nose Blows Score, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8.~Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline to Day 2

,,,,
Interventionunits on a scale (Least Squares Mean)
Runny Nose ScoreItchy Nose ScoreSniffles ScoreNose Blow ScoreSneezes ScoreWatery Eyes Score
Cetirizine (CTZ) 10 mg-1.06-1.16-1.15-1.99-1.31-1.01
Cetirizine (CTZ) 5 mg-1.07-1.21-1.09-1.86-1.21-1.00
Levocetirizine (LCTZ) 2.5 mg-0.94-1.02-1.05-1.75-1.17-0.87
Levocetirizine (LCTZ) 5 mg-0.95-1.10-1.02-1.83-1.19-1.01
Placebo (PBO)-0.59-0.61-0.60-0.98-0.41-0.44

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Change From Baseline in the Individual Symptom Scores Over Period II

"Individual symptom scores include Runny Nose Score, Itchy Nose Score, Sniffles Score, Watery Eyes Score, Sneezes Score, Nose Blows Score.~The subjects had to evaluate the severity of the symptoms using a scale from None to Very severe (ranging from 0 to 5).~For Sneezes Score and Nose Blows Score, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8.~Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline, Treatment Period II [Day 2, (8:30 am to 12:00 pm)]

,,,,
Interventionunits on a scale (Least Squares Mean)
Runny Nose ScoreItchy Nose ScoreSniffles ScoreNose Blow ScoreSneezes ScoreWatery Eyes Score
Cetirizine (CTZ) 10 mg-1.10-1.24-1.21-2.02-1.38-0.93
Cetirizine (CTZ) 5 mg-0.95-1.13-0.90-1.78-1.19-0.83
Levocetirizine (LCTZ) 2.5 mg-0.86-1.00-0.91-1.61-1.18-0.78
Levocetirizine (LCTZ) 5 mg-0.94-1.11-0.96-1.84-1.33-0.91
Placebo (PBO)-0.62-0.57-0.58-1.00-0.48-0.30

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Change From Baseline in the Individual Symptom Scores Over Period I

"Individual symptom scores include Runny Nose Score, Itchy Nose Score, Sniffles Score, Watery Eyes Score, Sneezes Score, Nose Blows Score.~The subjects had to evaluate the severity of the symptoms using a scale from None to Very severe (ranging from 0 to 5).~For Sneezes Score and Nose Blows Score, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8.~Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline, Treatment Period 1 [Day 1, from drug intake (at 11:00 am) to 5 hours post-treatment (at 4:00 pm)]

,,,,
Interventionunits on a scale (Least Squares Mean)
Runny Nose ScoreItchy Nose ScoreSniffles ScoreNose Blow ScoreSneezes ScoreWatery Eyes Score
Cetirizine (CTZ) 10 mg-1.04-1.10-1.10-1.96-1.23-1.07
Cetirizine (CTZ) 5 mg-1.17-1.28-1.24-1.92-1.22-1.13
Levocetirizine (LCTZ) 2.5 mg-1.01-1.03-1.15-1.87-1.15-0.94
Levocetirizine (LCTZ) 5 mg-0.95-1.09-1.06-1.82-1.07-1.08
Placebo (PBO)-0.60-0.66-0.65-0.98-0.37-0.56

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Change From Baseline in the Total Symptom Complex (TSC) Score Over the Total Treatment Period (Period I + Period II)

"The TSC score was calculated as the sum of the following 10 individual symptom scores:~runny nose (left and right), itchy nose (left and right), sniffles, nose blows, sneezes, watery eyes, itchy eyes and ears, itchy throat, cough and postnasal drip.~Each individual symptom, except nose blows and sneezes, is rated on a 5-point scale of severity: 0 = None, 1 = a little, 2 = Moderate, 3 = Quite a bit, 4 = severe, 5 = very severe. For nose blows and sneezes, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8. The TSC score ranges from 0 to 56. Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline to Day 2

Interventionunits on a scale (Least Squares Mean)
Placebo (PBO)-6.10
Levocetirizine (LCTZ) 2.5 mg-10.86
Levocetirizine (LCTZ) 5 mg-11.22
Cetirizine (CTZ) 5 mg-11.84
Cetirizine (CTZ) 10 mg-11.92

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Change From Baseline in the Total Symptom Complex (TSC) Score Over Period II

"The TSC score was calculated as the sum of the following 10 individual symptom scores:~runny nose (left and right), itchy nose (left and right), sniffles, nose blows, sneezes, watery eyes, itchy eyes and ears, itchy throat, cough and postnasal drip.~Each individual symptom, except nose blows and sneezes, is rated on a 5-point scale of severity: 0 = None, 1 = a little, 2 = Moderate, 3 = Quite a bit, 4 = severe, 5 = very severe. For nose blows and sneezes, the subjects had to record the number of each symptom since last evaluation. This number corresponds to a score ranging from 0 to 8. The TSC score ranges from 0 to 56. Increasing scores are associated with increasing severity. Negative values indicate improvement from Baseline." (NCT00291642)
Timeframe: Baseline, Treatment Period II [Day 2, (8:30 am to 12:00 pm)]

Interventionunits on a scale (Least Squares Mean)
Placebo (PBO)-5.73
Levocetirizine (LCTZ) 2.5 mg-10.25
Levocetirizine (LCTZ) 5 mg-11.03
Cetirizine (CTZ) 5 mg-10.73
Cetirizine (CTZ) 10 mg-12.14

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Duration of Suppressive Effect of Desloratadine After Discontinuation of a 1-week Treatment

The number of days after treatment discontinuation until a measurable wheal and flare response. (NCT00359138)
Timeframe: Starting at Day 8

InterventionDays (Mean)
Desloratadine 5 mg Tablet + Levocetirizine Placebo Capsule5
Desloratadine Placebo Tablet + Levocetirizine 5 mg Capsule4
Desloratadine Placebo Tablet + Levocetirizine Placebo CapsuleNA

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Responder Status According to Pruritus Severity Score (Response = Mild or None in Pruritus Severity Score).

A participant is a responder if the pruritus severity score is assessed as mild or none, otherwise it is a non-responder. The responder status is defined at day 14, except if the investigator assessed the subject as a responder at day 7. The Pruritus Score is in general defined as: 3 for Severe, 2 for Moderate, 1 for Mild and 0 for None. (NCT00375713)
Timeframe: Day 7 and 14

,
InterventionParticipants (Number)
ResponderNon-Responder
Cetirizine13438
Levocetirizine13137

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Change From Baseline in the Mean Pruritus Severity Score at Endpoint During the 14 Day Treatment Period

The Pruritus Score Scale ranges from 0 to 3 (3 for Severe, 2 for Moderate, 1 for Mild and 0 for None). Endpoint is at visit 4 on day 14 or at an earlier timepoint at study completion. (NCT00375713)
Timeframe: Baseline and at endpoint during the 14 day treatment period

InterventionUnits on a scale (Mean)
Levocetirizine1.15
Cetirizine1.21

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Duration of Pruritus (Stated in Categories) at Endpoint During the 14 Day Treatment Period

Duration of pruritus was categorized as follows: 3 if > 6 hours/24hr, 2 if 1 to 6 hours/24hr, 1 if less than 1 hour/24hr, and 0 if No pruritus. The endpoint is visit 4 on day 14 or at an earlier time point at study completion. (NCT00375713)
Timeframe: At endpoint during the 14 day treatment period

InterventionUnits on a scale (Mean)
Levocetirizine2.13
Cetirizine2.20

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Global Improvement at Endpoint During the 14 Day Treatment Period

Global improvement is measured on an ordered nominal scale ranging from marked improvement to exacerbation (see categories in the table). The endpoint is visit 4 on day 14 or at an earlier time point at study completion. (NCT00375713)
Timeframe: At endpoint during the 14 day treatment period

,
InterventionParticipants (Number)
Marked improvementModerate improvementMild improvementNo changeExacerbation
Cetirizine525447151
Levocetirizine476239181

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Number of Subjects Who Preferred Desloratadine RediTab or Zyrtec Chewable Tablet.

"A product preference questionnaire was completed after the administration of the second study drug. An interviewer instructed the subject now that you have tasted the two tablets, show us which tablet you like more and the subject then marked which tablet he/she preferred. If the subject had no preference, the response was recorded accordingly." (NCT00779116)
Timeframe: Following the second dose (8-10 minutes after the first dose)

InterventionParticipants (Number)
RediTab150
Zyrtec39
No Preference28

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Number of Subjects Who Preferred Desloratadine RediTab or Zyrtec Chewable Tablet.

"A product preference questionnaire was completed after the administration of the second study drug. An interviewer instructed the subject now that you have tasted the two tablets, show us which tablet you like more and the subject then marked which tablet he/she preferred. If the subject had no preference, the response was recorded accordingly." (NCT00780403)
Timeframe: Following the second dose (8-10 minutes after the first dose)

Interventionparticipants (Number)
RediTab149
Zyrtec33
No Preference38

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Total Four Symptom Scores (Allergy Symptoms)

"Total Four Symptom Scores (TFSS) ranging 0 to 12. Increased scores indicate increased symptoms. This was measured on days 5, 12, 17, 24, 29, and 36 of the study. The mean TFSS for patients receiving placebo, cetirizine, and levocetirizine was then calculated.~This was mean data for all interventions." (NCT00826943)
Timeframe: same as primary outcome measure (obtain on days 5, 12, 17, 24, 29, and 36)

InterventionTFSS scores (Mean)
Placebo4.41
Levocetirizine3.14
Cetirizine2.67

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Modified Epworth Sleepiness Scale

"Epworth Sleepiness Scale ratings (0 to 24); higher scores = increased sedation. This was measured over the 36 days of the study (at the end of each washout period and each intervention period); measured on days 5, 12, 17, 24, 29, and 36.~This was mean data for all interventions." (NCT00826943)
Timeframe: 36 days of the study

Interventionunits on a scale (Mean)
Placebo6.14
Levocetirizine6.69
Cetirizine7.48

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Likert Score Rating Global Sedation

"Likert score range 1 to 9 (no sedation to extreme sedation). Highers scores indicate increased sedation. This was measured on days days 5, 12, 17, 24, 29, and 36 of the study.~This was mean data for all interventions." (NCT00826943)
Timeframe: duration of study (36 days)

InterventionLikert score (Mean)
Placebo2.80
Levocetirizine3.07
Cetirizine3.54

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Weighted Mean of the Individual Components of TNSS (Sneeze, Itch, Rhinorrhoea and Nasal Blockage) 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3

On the third dosing day, participants entered the ECC for a duration of 6 hours, 1 hour after receiving their third dose. Time 0 hour was considered as the time that the participant entered the ECC. Nasal blockage, itch, sneeze and rhinorrhoea was scored on a categorical scale from 0 to 3 (0: no symptoms; 1: mild symptoms; 2: moderate symptoms; 3: severe symptoms). The total TNSS ranged from 0-12 point, with low score indicates well-being and higher score indicates more severity. Individual symptoms scores was summed to produce the TNSS at each time point (0, 20, 40, 60, 80, 100, 120, 140, 160, 180, 200, 220, 240, 260, 280, 300, 320, 340 and 360 minutes). The adjusted mean is provided as least square mean. (NCT00972504)
Timeframe: Day 3 of each treatment period (approximately up to 63 days)

,,,
InterventionScore on a scale (Least Squares Mean)
Nasal BlockageRhinorrhoeaNasal ItchingSneezing
Cetirizine 10 mg Once Daily1.31.00.80.5
GSK1004723 1000 µg Once Daily1.71.30.90.4
GSK835726 10 mg Once Daily1.31.10.80.5
Placebo1.51.51.10.8

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Number of Participants With Adverse Events (AE) and Serious Adverse Events (SAE)

An AE was defined as any untoward medical occurrence (MO) in a participant temporally associated with the use of a medicinal product (MP), whether or not considered related to the MP and can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with its use. The SAE was any untoward MO that, at any dose, results in death, life threatening, persistent or significant disability/incapacity, results in or prolongs inpatient hospitalization, congenital abnormality or birth defect, that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention or is associated with liver injury and impaired liver function defined as: alanine aminotransferase >=3 times upper limit of normal (ULN), and total bilirubin >=2 times ULN or international normalized ratio more than 1.5. (NCT00972504)
Timeframe: approximately up to 63 days

,,,
InterventionParticipants (Number)
Any AEAny SAE
Cetirizine 10 mg Once Daily170
GSK1004723 1000 µg Once Daily530
GSK835726 10 mg Once Daily130
Placebo150

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Weighted Mean Nasal Congestion VAS 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3

On the third dosing day, participants entered the ECC for a duration of 6 hours, 1 hour after receiving their third dose. Time 0 hour was considered as the time that the participant entered the ECC. Nasal congestion was measured on 0-10 centimeter VAS scale (0: no symptoms and 10: the worst possible symptoms) with low score indicates well-being and higher values indicate greater congestion. It was measured at 60, 80, 100, 120, 140, 160, 180, 200, 220, 240, 260, 280, 300, 320, 340 and 360 minutes. The adjusted mean is provided as least square mean. (NCT00972504)
Timeframe: Day 3 of each treatment period (approximately up to 63 days)

InterventionScore on a scale (Least Squares Mean)
Placebo3.97
GSK1004723 1000 µg Once Daily4.29
GSK835726 10 mg Once Daily2.92
Cetirizine 10 mg Once Daily2.90

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Mean Forced Expiratory Volume in 1 Second (FEV1)

On the third dosing day, participants entered the ECC for a duration of 6 hours, 1 hour after receiving their third dose. Time 0 hour was considered as the time that the participant entered the ECC. FEV1 was measured at pre-challenge, 60, 120, 180, 240, 300 and 360 minutes. (NCT00972504)
Timeframe: Day 3 of each treatment period (approximately up to 63 days)

,,,
InterventionLiters (Mean)
FEV1-Pre challengeFEV1,1 hourFEV1,2 hourFEV1,3 hourFEV1,4 hourFEV1,5 hourFEV1,6 hour
Cetirizine 10 mg Once Daily3.9323.9583.9253.8993.9033.8583.868
GSK1004723 1000 µg Once Daily3.9353.9593.9483.9383.9133.8903.877
GSK835726 10 mg Once Daily3.9243.9483.9363.9183.9033.8903.887
Placebo3.9083.9493.9103.9013.8813.8583.914

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Weighted Mean Wet Tissue Weight (as a Surrogate Marker of Nasal Secretion) 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3

On the third dosing day, participants entered the ECC for a duration of 6 hours, 1 hour after receiving their third dose. Time 0 hour was considered as the time that the participant entered the ECC. Wet tissue weight assessments was measured as a surrogate marker of nasal secretion at 60, 120, 180, 240, 300 and 360 minutes. The adjusted mean is provided as least square mean. (NCT00972504)
Timeframe: Day 3 of each treatment period (approximately up to 63 days)

InterventionGrams (Least Squares Mean)
Placebo6.251
GSK1004723 1000 µg Once Daily5.210
GSK835726 10 mg Once Daily4.491
Cetirizine 10 mg Once Daily3.459

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Weighted Mean TNSS (Sneeze, Itch, Rhinorrhoea and Nasal Blockage) 1-6 Hours Post Start of Allergen Challenge (2-7 Hours Post-dose) on Day 3

On the third dosing day, participants entered the ECC for a duration of 6 hours, 1 hour after receiving their third dose. Time 0 hour was considered as the time that the participant entered the ECC. Nasal blockage, itch, sneeze and rhinorrhoea was scored on a categorical scale from 0 to 3 (0: no symptoms; 1: mild symptoms; 2: moderate symptoms; 3: severe symptoms). The total TNSS ranged from 0-12 point, with low score indicates well-being and higher score indicates more severity. Individual symptoms scores was summed at each time point (0, 20, 40, 60, 80, 100, 120, 140, 160, 180, 200, 220, 240, 260, 280, 300, 320, 340 and 360 minutes). The adjusted mean is provided as least square mean. (NCT00972504)
Timeframe: Day 3 of each treatment period (approximately up to 63 days)

InterventionScore on a scale (Least Squares Mean)
Placebo4.9
GSK1004723 1000 µg Once Daily4.2
GSK835726 10 mg Once Daily3.6
Cetirizine 10 mg Once Daily3.5

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Physician's Global Evaluation of Allergic Rhinitis

An evaluation by the physician, administered at week 4 of the study (or upon discontinuation) using a 7-point scale [Score 0 (best) to 6 (worst)], of the change in symptoms as compared to the beginning of the study. (NCT00974571)
Timeframe: End of the first 4 weeks in 6-week treatment period

InterventionScores on a scale (Least Squares Mean)
Montelukast 10 mg2.26
Cetirizine 10 mg2.20
Placebo2.33

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Patient's Global Evaluation of Allergic Rhinitis

An evaluation by the patient, administered at week 4 of the study (or upon discontinuation) using a 7-point scale [Score 0 (best) to 6 (worst)], of the change in symptoms as compared to the beginning of the study. (NCT00974571)
Timeframe: End of the first 4 weeks in 6-week treatment period

InterventionScores on a scale (Least Squares Mean)
Montelukast 10 mg2.22
Cetirizine 10 mg2.15
Placebo2.41

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Mean Change From Baseline in Nighttime Symptoms Score

"Mean change from baseline in Nighttime Symptoms Score.~Patients were asked to rate each symptom daily on a 4-point scale [Score 0 (best) to 3 (worst)], and the average score of Nasal Congestion Upon Awakening, Difficulty Going to Sleep, and Nighttime Awakenings was reported as the Nighttime Symptoms Score." (NCT00974571)
Timeframe: Baseline and first 4 weeks in 6-week treatment period

InterventionScores on a scale (Least Squares Mean)
Montelukast 10 mg-0.28
Cetirizine 10 mg-0.30
Placebo-0.26

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Mean Change From Baseline in Daytime Nasal Symptoms Score

"Mean change from baseline in Daytime Nasal Symptoms score.~Patients were asked to rate each nasal symptom of Congestion, Rhinorrhea, Itching, and Sneezing daily on a 4-point scale [Score 0 (best) to 3 (worst)]. The average of the 4 individual nasal symptoms scores was reported as the Daytime Nasal Symptoms Score." (NCT00974571)
Timeframe: Baseline and first 4 weeks of a 6-week treatment period

InterventionScores on a scale (Least Squares Mean)
Montelukast 10 mg-0.39
Cetirizine 10 mg-0.45
Placebo-0.36

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Mean Change From Baseline in Composite Symptoms Score

Composite Symptoms Scores were computed as the average of the Daytime Nasal Symptoms Scores [Score 0 (best) to 3 (worst)]. and Nighttime Symptoms Scores collected [Score 0 (best) to 3 (worst)]. (NCT00974571)
Timeframe: Baseline and first 4 weeks in 6-week treatment period

InterventionScore 0 (best) to 3 (worst) (Least Squares Mean)
Montelukast 10 mg-0.34
Cetirizine 10 mg-0.38
Placebo-0.30

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Ear or Palate Pruritus at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.6080.7
AC-170 0.1%0.20.40.5
AC-170 0.24%0.30.30.3
AC-170 0%0.40.70.7

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Ear or Palate Pruritus at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.60.70.8
AC-170 0.1%0.30.60.7
AC-170 0.24%0.40.70.7
AC-170 0%0.50.80.7

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Ear or Palate Pruritus at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.40.90.8
AC-170 0.1%0.40.80.9
AC-170 0.24%0.30.50.8
AC-170 0%0.51.01.2

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Conjunctival Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.441.811.83
AC-170 0.1%1.451.671.67
AC-170 0.24%1.661.831.79
AC-170 0%1.881.961.97

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Conjunctival Redness at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.431.631.61
AC-170 0.1%1.381.591.54
AC-170 0.24%1.711.851.79
AC-170 0%1.701.901.76

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Conjunctival Redness at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.621.681.63
AC-170 0.1%1.591.651.58
AC-170 0.24%1.451.611.56
AC-170 0%1.791.911.88

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Ciliary Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.241.591.65
AC-170 0.1%1.241.511.52
AC-170 0.24%1.271.641.73
AC-170 0%1.671.771.79

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Ciliary Redness at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.361.491.50
AC-170 0.1%1.221.471.47
AC-170 0.24%1.501.741.65
AC-170 0%1.551.771.65

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Ciliary Redness at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.471.601.60
AC-170 0.1%1.531.651.65
AC-170 0.24%1.341.521.53
AC-170 0%1.811.991.95

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Chemosis at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.490.740.71
AC-170 0.1%0.430.520.53
AC-170 0.24%0.540.790.76
AC-170 0%0.740.800.88

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Chemosis at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.680.870.90
AC-170 0.1%0.520.640.71
AC-170 0.24%0.550.770.84
AC-170 0%0.680.810.90

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Chemosis at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.710.930.92
AC-170 0.1%0.580.700.72
AC-170 0.24%0.530.600.71
AC-170 0%0.720.991.00

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Eyelid Swelling at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.60.70.6
AC-170 0.1%0.80.90.8
AC-170 0.24%0.80.80.7
AC-170 0%0.91.11.0

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Tolerability of Study Medication at Visit 3A

Subjects were asked to rate the comfort of the drop in each eye upon instillation, at 1 minute, and at 2 minutes after instillation of study medication. The assessment used a 10-point scale with 0 as very comfortable and 10 as very uncomfortable. Higher scores represent a worse outcome.. (NCT01332188)
Timeframe: upon instillation, 1 minute and 2 minutes post instillation

,,,
Interventionunits on a scale (Mean)
Upon instillation1 minute post-instillation2 minutes post-instillation
AC-170 0.05%0.50.70.8
AC-170 0.1%0.70.91.0
AC-170 0.24%1.32.01.7
AC-170 0%0.60.90.6

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Tearing at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.70.50.5
AC-170 0.1%0.50.50.4
AC-170 0.24%0.30.40.2
AC-170 0%0.60.60.6

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Tearing at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.01.11.0
AC-170 0.1%0.70.60.5
AC-170 0.24%0.60.70.7
AC-170 0%0.80.80.7

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Tearing at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.00.80.7
AC-170 0.1%0.80.50.4
AC-170 0.24%0.60.70.7
AC-170 0%0.60.90.9

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Rhinorrhea at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.60.90.8
AC-170 0.1%0.20.40.4
AC-170 0.24%0.30.50.5
AC-170 0%0.60.80.6

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Rhinorrhea at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.11.11.2
AC-170 0.1%0.60.70.6
AC-170 0.24%0.81.21.0
AC-170 0%0.71.00.8

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Rhinorrhea at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.11.21.3
AC-170 0.1%0.40.60.7
AC-170 0.24%0.71.11.1
AC-170 0%0.71.01.1

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Ocular Itching at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01332188)
Timeframe: 3, 5, 7 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.05%1.051.191.01
AC-170 0.1%0.841.091.07
AC-170 0.24%0.911.070.97
AC-170 0%1.942.091.94

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Ocular Itching at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01332188)
Timeframe: 3, 5, 7 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.05%1.992.001.77
AC-170 0.1%1.781.921.78
AC-170 0.24%1.902.171.97
AC-170 0%2.242.242.08

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Ocular Itching at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01332188)
Timeframe: 3, 5, 7 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.05%1.912.011.86
AC-170 0.1%2.002.041.87
AC-170 0.24%1.651.741.75
AC-170 0%2.482.552.27

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Nasal Pruritus at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.40.40.4
AC-170 0.1%0.20.30.4
AC-170 0.24%0.30.20.3
AC-170 0%0.40.40.4

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Nasal Pruritus at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.70.70.5
AC-170 0.1%0.40.40.5
AC-170 0.24%0.40.80.6
AC-170 0%0.40.60.7

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Nasal Pruritus at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.60.60.7
AC-170 0.1%0.20.40.6
AC-170 0.24%0.50.70.6
AC-170 0%0.40.80.8

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Nasal Congestion at Onset of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.21.41.5
AC-170 0.1%0.50.60.8
AC-170 0.24%0.81.01.0
AC-170 0%0.81.21.3

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Nasal Congestion at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.71.11.1
AC-170 0.1%0.40.50.5
AC-170 0.24%0.40.40.4
AC-170 0%0.81.41.4

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Nasal Congestion at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.91.21.2
AC-170 0.1%0.60.60.6
AC-170 0.24%0.81.21.1
AC-170 0%0.71.11.2

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Nasal Composite Score at Onset of Action (15 Minutes Post-dose)

A nasal composite score was summed for each patient based on the presence of at least one of the following four nasal symptoms on a 0-4 scale (0=none to 4=severe): rhinorrhea; nasal pruritus; ear or palate pruritus; and nasal congestion. The percentage of subjects with at least one nasal symptom present was calculated for each time point. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionpercentage of subjects (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%52.282.673.9
AC-170 0.1%565652
AC-170 0.24%47.647.652.4
AC-170 0%728484

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Nasal Composite Score at Duration of Action (24 Hours Post-dose)

A nasal composite score was summed for each patient based on the presence of at least one of the following four nasal symptoms on a 0-4 scale (0=none to 4=severe): rhinorrhea; nasal pruritus; ear or palate pruritus; and nasal congestion. The percentage of subjects with at least one nasal symptom present was calculated for each time point. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionpercentage of subjects (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%69.682.682.6
AC-170 0.1%76.084.088.0
AC-170 0.24%85.790.581.0
AC-170 0%68.092.092.0

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Nasal Composite Score at Duration of Action (16 Hours Post-dose)

A nasal composite score was summed for each patient based on the presence of at least one of the following four nasal symptoms on a 0-4 scale (0=none to 4=severe): rhinorrhea; nasal pruritus; ear or palate pruritus; and nasal congestion. The percentage of subjects with at least one nasal symptom present was calculated for each time point. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionpercentage of subjects (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%82.682.691.3
AC-170 0.1%66.779.283.3
AC-170 0.24%52.490.595.2
AC-170 0%76.084.084.0

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Eyelid Swelling at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.40.50.5
AC-170 0.1%0.50.60.6
AC-170 0.24%0.50.60.5
AC-170 0%0.70.80.7

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Eyelid Swelling at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%0.70.80.8
AC-170 0.1%0.70.80.8
AC-170 0.24%0.90.90.9
AC-170 0%0.70.90.9

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Episcleral Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.521.861.91
AC-170 0.1%1.491.731.72
AC-170 0.24%1.641.981.88
AC-170 0%1.932.012.04

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Episcleral Redness at Duration of Action (24 Hours Post-dose)

A treatment efficacy CAC was performed 24 hours after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.531.721.70
AC-170 0.1%1.371.631.60
AC-170 0.24%1.731.901.87
AC-170 0%1.802.001.85

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Episcleral Redness at Duration of Action (16 Hours Post-dose)

A treatment efficacy CAC was performed 16 hours after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01332188)
Timeframe: 7, 15, 20 minutes post-CAC

,,,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.05%1.681.811.80
AC-170 0.1%1.741.771.73
AC-170 0.24%1.571.691.69
AC-170 0%1.902.021.97

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Ear or Palate Pruritis at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.50.6
AC-170 0%1.01.11.0

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Episcleral Redness at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.721.941.89
AC-170 0%1.942.072.03

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Episcleral Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.882.102.20
AC-170 0%1.962.102.16

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Eyelid Swelling at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.71.01.0
AC-170 0%1.11.31.2

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Eyelid Swelling at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.60.80.8
AC-170 0%0.91.11.1

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Nasal Congestion at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.91.11.2
AC-170 0%1.31.51.4

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Nasal Congestion at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.70.8
AC-170 0%1.01.21.2

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Nasal Pruritis at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.80.8
AC-170 0%1.01.01.1

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Nasal Pruritis at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.30.5
AC-170 0%0.70.80.7

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Ciliary Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.641.851.95
AC-170 0%1.901.992.06

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Conjunctival Redness at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.721.961.92
AC-170 0%1.942.021.98

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Conjunctival Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%2.022.232.28
AC-170 0%2.052.132.18

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Ear or Palate Pruritis at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.41.01.2
AC-170 0%1.01.31.5

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Tolerability of Study Medication at Visit 3A

Tolerability was assessed upon instillation of study medication, at 1 minute and 2 minutes post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT01551056)
Timeframe: upon instillation, 1 minute and 2 minutes post instillation

,
Interventionunits on a scale (Mean)
Upon instillation1 minute post-instillation2 minutes post-instillation
AC-170 0.24%1.22.42.1
AC-170 0%0.90.60.6

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Tearing at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.60.7
AC-170 0%1.00.80.8

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Tearing at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.80.90.9
AC-170 0%1.11.21.1

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Rhinorrhea at Duration of Action (16 Hours +1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.71.01.1
AC-170 0%1.41.31.4

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Number of Participants With At Least One of the Nasal Symptoms Present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. For Nasal Composite Score the Total Composite Score ranges from 0 to 16, higher scores represent greater severity. Patients needed to have at least one of the nasal symptoms present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) each symptom was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Composite score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Intervention%participants with at least 1 nasal symp (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%5065.970.5
AC-170 0%82.286.784.4

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Ocular Itching at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01551056)
Timeframe: 3, 5, 7 minutes post-CAC

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.24%0.711.011.00
AC-170 0%2.182.312.10

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Number of Participants With At Least One of the Nasal Symptoms Present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. For Nasal Composite Score the Total Composite Score ranges from 0 to 16, higher scores represent greater severity. Patients needed to have at least one of the nasal symptoms present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) each symptom was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Composite score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Intervention%participants with at least 1 nasal symp (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%68.980.086.7
AC-170 0%84.488.993.3

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Ocular Itching at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy Conjunctival Allergen Challenge (CAC) was performed 16 hours + 1 hour after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01551056)
Timeframe: 3, 5, 7 minutes post-CAC

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.24%1.711.881.76
AC-170 0%2.342.502.22

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Rhinorrhea at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.50.6
AC-170 0%1.11.01.0

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Chemosis at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.490.710.76
AC-170 0%0.701.011.05

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Chemosis at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.741.121.22
AC-170 0%0.971.421.53

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Ciliary Redness at Duration of Action (16 Hours + 1 Hour Post-dose)

A treatment efficacy CAC was performed 16 hours + 1 hour after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01551056)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.541.771.72
AC-170 0%1.821.961.93

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Number of Participants Categorized With the Indicated Pruritis Severity on the First Day of Treatment and at Weeks 1 and 2/Early Withdrawal

The investigator comprehensively assessed the pariticipant's severity of pruritus on the first day of treatment (FDOT), at Week 1, and at Week 2 (or at the discontinuation day in the case of early withdrawal [EW] from the clinical trial) by using the following scale: 4, severe; 3, moderate; 2, mild; 1, slight; 0, none. (NCT01563081)
Timeframe: First day of treatment; Weeks 1 and 2/Early Withdrawal

Interventionparticipants (Number)
FDOT, noneFDOT, slightFDOT, mildFDOT, moderateFDOT, severeWeek 1, noneWeek 1, slightWeek 1, mildWeek 1, moderateWeek 1, severeWeek 2/EW, noneWeek 2/EW, slightWeek 2/EW, mildWeek 2/EW, moderateWeek 2/EW, severe
Levocetrizine: Total Population071711561411721381180

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Number of Participants With Serious Adverse Events (SAEs) and Non-serious Adverse Events (AEs)

A non-serious AE is defined as any untoward medical occurrence in a participant/clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. For marketed medicinal products, this also includes failure to produce expected benefits (i.e., lack of efficacy), abuse, or misuse. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, or is a possible drug-induced liver injury. For a list of all SAEs/non-serious AEs occurring at a frequency of >=5%, please see the SAE/non-serious AE module of this record. (NCT01563081)
Timeframe: up to Week 2/Early Withdrawal (EW)

,,
Interventionparticipants (Number)
Any Adverse EventAny Serious Adverse Event
Levocetirizine: >=12 Months and <24 Months Old170
Levocetirizine: >=6 Months and <12 Months Old150
Levocetirizine: Total Population320

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Number of Participants With the Indicated Change From the First Day of Treatment in Nasal Symptoms and Pruritis Associated With Skin Diseases at Weeks 1 and 2/Early Withdrawal, as Assessed by the Investigator or Sub-investigator

The investigator or sub-investigator comprehensively assessed the participants' improvement in nasal symptoms (allergic rhinitis [AR]) and pruritus associated with skin diseases (PAWSD) at Weeks 1 and 2 (or at the discontinuation day in the case of early withdrawal [EW] from the clinical trial) compared to the first day of treatment by using the following scale: 1, markedly improved; 2, moderately improved; 3, slightly improved; 4, no change; 5, worsened. (NCT01563081)
Timeframe: First day of treatment; Weeks 1 and 2/Early Withdrawal

Interventionparticipants (Number)
AR, Week 1, markedly improved, n=20AR, Week 2/EW, markedly improved, n=20AR, Week moderately improved, n=20AR, Week 2/EW, moderately improved, n=20AR, Week 1, slightly improved, n=20AR, Week 2/EW, slightly improved, n=20AR, Week 1, no change, n=20AR, Week 2/EW, no change, n=20AR, Week 1, worsened, n=20AR, Week 2/EW, worsened, n=20PAWSD, Week 1, markedly improved, n=40PAWSD, Week 2/EW, markedly improved, n=40PAWSD, Week 1, moderately improved, n=40PAWSD, Week 2/EW, moderately improved, n=40PAWSD, Week 1, slightly improved, n=40PAWSD, Week 2/EW, slightly improved, n=40PAWSD, Week 1, no change, n=40PAWSD, Week 2/EW, no change, n=40PAWSD, Week 1, worsened, n=40PAWSD, Week 2/EW, worsened, n=40
Levocetrizine: Total Population7124334610061015191287300

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Cmax and Cmin of Levocetirizine in Plasma

Cmax is defined as the peak plasma concentration of a drug after administration. Cmin is defined as the lowest (trough) concentration that a drug reaches before the next dose is administered. For both age cohorts, blood samples were collected 1.5-2.5 hours after the last drug administration for assessment of Cmax at either Week 1 or 2/EW. For participants in the >=6 months and <12 months cohort, blood samples were collected 22.5-25.5 hours after the last drug administration for Cmin at a different visit from Cmax sampling. For participants in the >=12 months and <24 months cohort, blood samples were collected 10.5-13.5 hours after the final drug administration for Cmin at a different visit from Cmax sampling. For all participants, if Cmin sampling occurred at Week 1, then Cmax sampling occurred at Week 2/EW, and vice versa. (NCT01563081)
Timeframe: Weeks 1 and 2/Early Withdrawal

,
Interventionnanograms per milliliter (Median)
CmaxCmin
Levocetirizine: >=12 Months and <24 Months Old213.44048.330
Levocetirizine: >=6 Months and <12 Months Old206.78017.710

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Tolerability of Study Medication at Visit 3A

Tolerability was assessed upon instillation of study medication, at 1 minute and 2 minutes post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT01685242)
Timeframe: upon instillation, 1 minute and 2 minutes post instillation

,
Interventionunits on a scale (Mean)
Upon instillation1 minute post-instillation2 minutes post-instillation
AC-170 0.24%1.21.41.3
AC-170 0%1.01.21.0

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Tearing at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.60.80.7
AC-170 0%1.00.90.8

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Tearing at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.80.91.0
AC-170 0%1.01.00.9

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Rhinorrhea at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.50.90.8
AC-170 0%1.11.31.2

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Chemosis at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.891.291.32
AC-170 0%1.241.441.51

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Chemosis at Onset of Action (15 Minutes)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.630.991.14
AC-170 0%1.031.281.43

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Ciliary Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.571.861.90
AC-170 0%1.982.062.05

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Conjunctival Redness at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.972.302.30
AC-170 0%2.272.342.32

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Conjunctival Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.661.931.95
AC-170 0%1.982.092.09

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Ear or Palate Pruritus at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.50.91.0
AC-170 0%0.81.31.3

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Ear or Palate Pruritus at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.70.9
AC-170 0%0.81.11.1

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Episcleral Redness at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.972.282.30
AC-170 0%2.312.352.35

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Nasal Pruritus at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.50.5
AC-170 0%0.81.00.9

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Nasal Pruritus at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.60.6
AC-170 0%0.60.80.7

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Ocular Itching at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01685242)
Timeframe: 3, 5, 7 minutes post-CAC

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.24%1.001.181.11
AC-170 0%2.382.432.11

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Rhinorrhea at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.50.80.7
AC-170 0%1.31.61.5

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Eyelid Swelling at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.60.80.8
AC-170 0%1.11.21.1

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Episcleral Redness at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.772.032.02
AC-170 0%2.032.132.11

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Ciliary Redness at Duration of Action (8 Hours + 30 Minutes)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.842.182.21
AC-170 0%2.192.332.30

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Nasal Composite Score at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. For Nasal Composite Score the Total Composite Score ranges from 0 to 16, higher scores represent greater severity. Patients needed to have at least one of the nasal symptoms present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) each symptom was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Composite score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Intervention%participants with at least 1 nasal symp (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%61.281.683.7
AC-170 0%829494

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Nasal Composite Score at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. For Nasal Composite Score the Total Composite Score ranges from 0 to 16, higher scores represent greater severity. Patients needed to have at least one of the nasal symptoms present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) each symptom was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Composite score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Intervention%participants with at least 1 nasal symp (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%65.381.677.6
AC-170 0%8391.593.6

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Nasal Congestion at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.70.91.0
AC-170 0%1.21.61.5

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Ocular Itching at Duration of Action (8 Hours + 30 Minutes Post-dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01685242)
Timeframe: 3, 5, 7 minutes post-CAC

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.24%1.761.851.54
AC-170 0%2.692.742.53

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Eyelid Swelling at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.60.80.8
AC-170 0%1.01.01.0

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Nasal Congestion at Onset of Action (15 Minutes Post-dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01685242)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.81.11.1
AC-170 0%1.11.31.4

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Change in Itch Score

Itch score will be used to analyze our primary outcome. The subjects will have an itch score at baseline and compared to itch score at 3hrs post intervention. Itch score is measured on a scale of 1 to 4, with lower scores indicating less itchiness. (NCT01825655)
Timeframe: Baseline to 3 hours

Interventionunits on a scale (Mean)
Sugar Pill1.5

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Ocular Itching at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01881113)
Timeframe: 3, 5, 7 minutes post-CAC

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.24%1.942.031.82
AC-170 0%2.862.942.66

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Ocular Itching at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ocular itching was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ocular itching score over both eyes was analyzed. (NCT01881113)
Timeframe: 3, 5, 7 minutes post-CAC

,
Interventionunits on a scale (Mean)
3 minutes post-CAC5 minutes post-CAC7 minutes post-CAC
AC-170 0.24%1.011.171.15
AC-170 0%2.542.512.23

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Percentage of Participants With At Least One Nasal Symptom at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. For Nasal Composite Score the Total Composite Score ranges from 0 to 16, higher scores represent greater severity. Patients needed to have at least one of the nasal symptoms present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) each symptom was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Composite score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Intervention% of participants (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%587884
AC-170 0%87.589.689.6

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Percentage of Participants With At Least One Nasal Symptom at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. For Nasal Composite Score the Total Composite Score ranges from 0 to 16, higher scores represent greater severity. Patients needed to have at least one of the nasal symptoms present (Rhinorrhea + Nasal Pruritus + Ear or Palate Pruritus + Nasal Congestion) each symptom was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Composite score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Intervention% of participants (Number)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%51.258.172.1
AC-170 0%81.886.488.6

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Rhinorrhea at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.60.81.0
AC-170 0%1.11.31.3

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Rhinorrhea at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Rhinorrhea was assessed by the patient on a 0-4 scale (0=none to 4=severe). Rhinorrhea score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.50.70.8
AC-170 0%1.31.31.1

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Tearing at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.80.80.9
AC-170 0%1.21.21.0

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Tearing at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Tearing was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of tearing score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.50.50.5
AC-170 0%1.11.11.0

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Tolerability of Study Medication at Visit 3A

Tolerability was assessed upon instillation of study medication, at 1 minute and 2 minutes post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT01881113)
Timeframe: upon instillation, 1 minute and 2 minutes post instillation

,
Interventionunits on a scale (Mean)
Upon instillation1 minute post-instillation2 minutes post-instillation
AC-170 0.24%1.63.02.6
AC-170 0%0.81.11.1

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Eyelid Swelling at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.70.80.9
AC-170 0%1.41.41.4

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Chemosis at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.630.890.95
AC-170 0%0.961.281.27

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Chemosis at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Chemosis was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of chemosis score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.350.590.67
AC-170 0%0.580.750.85

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Ciliary Redness at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.711.931.87
AC-170 0%2.152.052.19

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Ciliary Redness at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ciliary Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of ciliary redness score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.622.052.09
AC-170 0%2.292.342.36

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Conjunctival Redness at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.972.132.09
AC-170 0%2.392.382.40

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Conjunctival Redness at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Conjunctival Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of conjunctival redness score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.922.192.15
AC-170 0%2.382.372.41

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Ear or Palate Pruritus at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.81.0
AC-170 0%1.21.51.6

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Ear or Palate Pruritus at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Ear or Palate Pruritus was assessed by the patient on a single 0-4 scale (0=none to 4=severe). Ear or Palate Pruritus score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.30.60.7
AC-170 0%0.81.31.3

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Episcleral Redness at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.922.082.06
AC-170 0%2.292.272.30

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Episcleral Redness at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Episcleral Redness was assessed by the patient on a 0-4 scale (0=none to 4=severe). Average of episcleral redness score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%1.912.222.18
AC-170 0%2.312.322.36

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Eyelid Swelling at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Eyelid swelling was assessed by the patient on a 0-3 scale (0=none to 3=severe). Average of eyelid swelling score over both eyes was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.50.4
AC-170 0%1.21.31.2

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Nasal Congestion at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.50.81.1
AC-170 0%1.01.41.3

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Nasal Congestion at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Congestion was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Congestion score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.50.6
AC-170 0%1.11.31.3

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Nasal Pruritus at Duration of Action (8 Hours + 30 Minutes Post-Dose)

A treatment efficacy CAC was performed 8 hours + 30 minutes after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.51.00.9
AC-170 0%0.91.00.9

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Nasal Pruritus at Onset of Action (15 Minutes Post-Dose)

A treatment efficacy CAC was performed 15 minutes after drop instillation. Nasal Pruritus was assessed by the patient on a 0-4 scale (0=none to 4=severe). Nasal Pruritus score for each time point was analyzed. (NCT01881113)
Timeframe: 7, 15, 20 minutes post-CAC

,
Interventionunits on a scale (Mean)
7 minutes post-CAC15 minutes post-CAC20 minutes post-CAC
AC-170 0.24%0.40.60.6
AC-170 0%0.80.80.9

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Mean Change From Baseline in the Individual AM Reflective Nasal Symptom Scores for Rhinorrhea, Nasal Congestion, Nasal Itching, and Sneezing Over the Entire Treatment Period

Each individual symptom was evaluated using a scale of 0 (none), 1 (mild), 2 (moderate), or 3 (severe).The reflective assessment scores the four nasal symptoms over the previous 24 hours. The participants themselves scored nasal symptoms in an e-diary. Baseline is defined as the arithmetic average of the individual AM reflective nasal symptom scores recorded on the morning of randomization and on each of the six preceding days. A participant may have had as few as 4 days' worth of data contributing to the Baseline average. The 2-week symptom score was defined as the average of the values recorded on the day after randomization and the following 13 days. Change from Baseline was thus calculated as the 2-week average minus the Baseline value. (NCT01916226)
Timeframe: Baseline through the entire treatment period (2 weeks)

,,,
InterventionScores on a scale (Mean)
Nasal congestionNasal itchingRunny noseSneezing
Cetirizine 10 mg-0.4-0.5-0.4-0.6
Cetirizine Matching Placebo-0.2-0.2-0.3-0.2
FPNS 200 μg-0.5-0.6-0.5-0.6
FPNS Matching Placebo-0.3-0.4-0.4-0.4

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Mean Change From Baseline in the Nocturnal Rhinoconjunctivitis Quality of Life Questionnaire (NRQLQ) Overall Score at Visit 3/Early Withdrawal.

The NRQLQ is a 16-item, validated, self-administered, disease (allergic rhinitis)-specific quality of life instrument that measures the functional problems most troublesome to participants with nocturnal allergy symptoms over a one-week interval. Each question is scored on a 7-point scale from 0 (not troubled) to 6 (extremely troubled). Items are grouped into four domains: sleep problems (4 items), sleep time problems (5 items), symptoms on waking in the morning (4 items), and practical problems (3 items). An overall score was calculated from the individual item scores. All items are weighted equally. A mean score is calculated across all items within each domain. The overall score is the mean across all items and ranges from 0 (not troubled) to 6 (extremely troubled). Higher scores reflect a lower quality of life. Change from Baseline was calculated as the 2-week average minus the Baseline value. (NCT01916226)
Timeframe: Baseline and Visit 3 (Study Day 14 +/- 2 days)/Early Withdrawal

InterventionScores on a scale (Mean)
FPNS 200 μg-1.0
Cetirizine 10 mg-0.6
FPNS Matching Placebo-0.8
Cetirizine Matching Placebo-0.5

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Mean Change From Baseline in the Combined Nasal and Ocular Reflective Total Symptom Score (rTSS = rTNSS+rTOSS) Over the Entire Treatment Period

The rTSS is the sum of the rTNSS and the rTOSS. The rTNSS score is the sum of the four individual symptom scores for rhinorrhea, nasal congestion, nasal itching, and sneezing. Each symptom is scored on a scale ranging from 0 to 3; the rTNSS ranges from 0 (none) to 12 (severe). Each individual symptom was evaluated using a scale of 0 (none), 1 (mild), 2 (moderate), or 3 (severe). The rTOSS assessment is comprised of the sum of the three symptom scores for tearing/watering, itching/burning, and eye redness. Each symptom is scored on a scale of 0 to 3: 0, none; 1, mild; 2, moderate; or 3, severe. The rTOSS ranges from 0 (none) to 9 (severe). The reflective assessment scores participants' symptoms over the previous 24 hours. The participants themselves scored nasal and ocular symptoms in an e-diary. Baseline is defined as the arithmetic average of the rTSS recorded on the morning of randomization and on each of the six preceding days. (NCT01916226)
Timeframe: Baseline through the entire treatment period (2 weeks)

InterventionScores on a scale (Mean)
FPNS 200 μg-3.9
Cetirizine 10 mg-3.4
FPNS Matching Placebo-2.7
Cetirizine Matching Placebo-1.7

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Mean Change From Baseline in the AM Pre-dose Reflective Total Ocular Symptom Score (rTOSS) Over the Entire Treatment Period

The rTOSS is an eye assessment that comprises the sum of the three symptom scores for tearing/watering, itching/burning, and eye redness. Each symptom is scored on a scale of 0 to 3: 0, none; 1, mild; 2, moderate; 3, severe. The rTOSS ranges from 0 (none) to 9 (severe). The reflective assessment scores the participants' ocular symptoms over the preceding 24 hours. The participants themselves scored ocular symptoms in an e-diary. Baseline arithmetic is defined as the average of the rTNSS recorded on the morning of randomization and on each of the six preceding days. A participant may have had as few as 4 days' worth of data contributing to the Baseline average. The 2-week symptom score was defined as the average of the values recorded on the day after randomization and the following 13 days. Change from Baseline was thus calculated as the 2-week average minus the Baseline value. (NCT01916226)
Timeframe: Baseline through the entire treatment period (2 weeks)

InterventionScores on a scale (Mean)
FPNS 200 μg-1.6
Cetirizine 10 mg-1.4
FPNS Matching Placebo-1.2
Cetirizine Matching Placebo-0.8

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Mean Change From Baseline in the AM Pre-dose Instantaneous Total Ocular Symptom Score (iTOSS) Over the Entire Treatment Period

"The iTOSS is an eye assessment that comprises the sum of the three symptom scores for tearing/watering, itching/burning, and eye redness. Each symptom is scored on a scale of 0 to 3: 0, none; 1, mild; 2, moderate; 3, severe. The iTOSS ranges from 0 (none) to 9 (severe). The instantaneous assessment scores the participants' ocular symptoms at the time of the assessment, or at that instant. The participants themselves scored ocular symptoms in an e-diary once each morning prior to administering study drug. Baseline is defined as the arithmetic average of the iTOSS recorded on the morning of randomization and on each of the six preceding days. A participant may have had as few as 4 days' worth of data contributing to the Baseline average. The 2-week symptom score was defined as the average of the values recorded on the day after randomization and the following 13 days. Change from Baseline was thus calculated as the 2-week average minus the Baseline value." (NCT01916226)
Timeframe: Baseline through the entire treatment period (2 weeks)

InterventionScores on a scale (Mean)
FPNS 200 μg-1.3
Cetirizine 10 mg-1.1
FPNS Matching Placebo-1.1
Cetirizine Matching Placebo-0.5

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Mean Change From Baseline in the AM Pre-dose Instantaneous Total Nasal Symptom Score (iTNSS) Over the Entire Treatment Period

"The iTNSS score is the sum of the four individual symptom scores for rhinorrhea, nasal congestion, nasal itching, and sneezing. Each symptom is scored on a scale ranging from 0 to 3; the iTNSS ranges from 0 (none) to 12 (severe). The symptoms were evaluated using a scale of 0 (none), 1 (mild), 2 (moderate), or 3 (severe). The instantaneous assessment of the TNSS scores the four nasal symptoms at the time of the assessment, or at that instant. The participants themselves scored nasal symptoms in an e-diary once each morning prior to administering study drug. Baseline is defined as the arithmetic average of the iTNSS recorded on the morning of randomization and on each of the six preceding days. A participant may have had as few as 4 days' worth of data contributing to the Baseline average. The 2-week symptom score was defined as the average of the values recorded on the day after randomization and the following 13 days." (NCT01916226)
Timeframe: Baseline through the entire treatment period (2 weeks)

InterventionScores on a scale (Mean)
FPNS 200 μg-1.9
Cetirizine 10 mg-1.3
FPNS Matching Placebo-1.2
Cetirizine Matching Placebo-0.6

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Mean Change From Baseline (CFB) in the Individual AM Reflective Total Nasal Symptom Scores (rTNSS) Over the Entire Treatment Period

The rTNSS score is the sum of the four individual symptom scores for rhinorrhea, nasal congestion, nasal itching, and sneezing. Each symptom is scored on a scale ranging from 0 to 3; the rTNSS ranges from 0 (none) to 12 (severe). Each individual symptom was evaluated using a scale of 0 (none), 1 (mild), 2 (moderate), or 3 (severe). The reflective assessment of the TNSS scores the four nasal symptoms over the previous 24 hours. The participants themselves scored nasal symptoms in an e-diary. Baseline is defined as the arithmetic average of the rTNSS recorded on the morning of randomization and on each of the six preceding days. A participant may have had as few as 4 days' worth of data contributing to the Baseline average. The 2-week symptom score was defined as the average of the values recorded on the day after randomization and the following 13 days. Change from Baseline was thus calculated as the 2-week average minus the Baseline value. (NCT01916226)
Timeframe: Baseline through the entire treatment period (2 weeks)

InterventionScores on a scale (Mean)
FPNS 200 μg-2.2
Cetirizine 10 mg-1.9
FPNS Matching Placebo-1.5
Cetirizine Matching Placebo-0.9

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Tolerability of AC 170 0.24% Compared to Its Vehicle at Visit 1 (Day 1)

Tolerability was assessed upon instillation of study medication, at 30 seconds and 1 minute post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT02132169)
Timeframe: Upon instillation, 30 Seconds Post-Instillation, 1 minute Post-Instillation

,
Interventionunits on a scale (Mean)
Upon instillation30 seconds post-instillation1 minute post-instillation
AC-170 0.24%0.90.70.6
AC-170 0%0.50.30.3

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Safety of AC 170 0.024% Compared to Its Vehicle

Safety measures (adverse events) of AC 170 0.024% compared to its vehicle were measured at Visit 1-4 and 5 (for subset of patients). (NCT02132169)
Timeframe: Up to 12 Weeks

Interventionadverse events (Number)
AC-170 0.24%70
AC-170 0%40

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Tolerability of AC 170 0.24% Compared to Its Vehicle at Visit 3 (Day 22)

Tolerability was assessed upon instillation of study medication, at 30 seconds and 1 minute post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT02132169)
Timeframe: Upon instillation, 30 Seconds Post-Instillation, 1 minute Post-Instillation

,
Interventionunits on a scale (Mean)
Upon instillation30 seconds post-instillation1 minute post-instillation
AC-170 0.24%0.60.40.3
AC-170 0%0.20.20.1

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Tolerability of AC 170 0.24% Compared to Its Vehicle at Visit 2 (Day 8)

Tolerability was assessed upon instillation of study medication, at 30 seconds and 1 minute post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT02132169)
Timeframe: Upon instillation, 30 Seconds Post-Instillation, 1 minute Post-Instillation

,
Interventionunits on a scale (Mean)
Upon instillation30 seconds post-instillation1 minute post-instillation
AC-170 0.24%0.80.50.4
AC-170 0%0.30.30.2

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Pharmacokinetics: Area Under the Plasma Concentration Versus Time Curve From Zero Extrapolated to Infinity (AUCinf) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
Interventionng.hr/mL (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 33618204343511068557
ARC-520 Cohort 63405914255981080995
ARC-520 Cohort 74171534628371368448
ARC-520 Cohort 86389657038861869597

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Pharmacokinetics: Apparent Volume of Distribution (V) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
InterventionmL/kg (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 370.0265.9858.03
ARC-520 Cohort 669.3171.6255.77
ARC-520 Cohort 771.4979.6863.92
ARC-520 Cohort 862.7476.2156.49

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) is defined as any untoward medical occurrence that does not necessarily have a causal relationship with this treatment. TEAEs were defined as all AEs starting or worsening after commencement of treatment with investigational product. (NCT02535416)
Timeframe: post-dose through the end of study (Day 15 ± 1 day) plus 30 days

Interventionparticipants (Number)
ARC-520 Cohort 12
ARC-520 Cohort 2A2
ARC-520 Cohort 21
ARC-520 Cohort 33
ARC-520 Cohort 43
ARC-520 Cohort 52
ARC-520 Cohort 65
ARC-520 Cohort 73
ARC-520 Cohort 82

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Pharmacokinetics: Area Under the Plasma Concentration-Time Curve From Time 0 to the Last Quantifiable Plasma Concentration (AUClast) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
Interventionng.hr/mL (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 33616114336321022752
ARC-520 Cohort 63404304229641021005
ARC-520 Cohort 74169054616011270330
ARC-520 Cohort 86382036985671722485

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Pharmacokinetics: Terminal Elimination Rate Constant (Lambda z) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
Intervention1/hr (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 30.1700.1500.068
ARC-520 Cohort 60.1700.1340.070
ARC-520 Cohort 70.1720.1400.057
ARC-520 Cohort 80.1550.1170.058

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Pharmacokinetics: Maximum Plasma Concentration (Cmax) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
Interventionng/mL (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 3541504965076600
ARC-520 Cohort 6488804622075500
ARC-520 Cohort 7563504923385467
ARC-520 Cohort 87301764033112050

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Pharmacokinetics: Half-Life (t1/2) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
Interventionhour (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 34.104.6810.41
ARC-520 Cohort 64.025.3110.44
ARC-520 Cohort 74.065.0711.94
ARC-520 Cohort 84.566.1712.24

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Pharmacokinetics: Clearance (CL) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting HBV) and MLP. (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
InterventionmL/hr/kg (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 312.019.923.80
ARC-520 Cohort 612.049.613.85
ARC-520 Cohort 712.4011.133.73
ARC-520 Cohort 89.688.723.27

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Pharmacokinetics: Area Under the Plasma Concentration Versus Time Curve From Zero to 24 Hours (AUC0-24) of the Analytes of ARC-520

Analytes include AD0009 and AD0010 (cholesterol-conjugated siRNA targeting hepatitis B virus [HBV]) and melittin-like peptide (MLP). (NCT02535416)
Timeframe: Day 1 pre-dose through 48 hours post-dose

,,,
Interventionng.hr/mL (Mean)
Analyte AD0009Analyte AD0010Analyte MLP
ARC-520 Cohort 3350027411580839718
ARC-520 Cohort 6331953393161832929
ARC-520 Cohort 74032474319801015503
ARC-520 Cohort 86056086307741364108

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Comparison of VAS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.

"Participants recorded the severity of all nasal and ocular symptoms at baseline and at the end of both treatment visits.~The Visual Analogue Scale (VAS) is a single overall rating of the severity of all nasal and ocular symptoms experienced by the participant. The scale ranges from 0 to 100 mm with 0 mm being no symptoms and 100 mm being the worst symptoms the participant has ever felt." (NCT02543346)
Timeframe: First treatment visit and second treatment visit.

Interventionunits on a scale (Mean)
EEU Placebo52.7
BRC Placebo47.7
EEU Cetirizine45.3
BRC Cetirizine44.1

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Comparison of TRSS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.

"Participants recorded their nasal and ocular symptoms at baseline and during the intervention visits.~The TRSS is a composite score comprised of 4 nasal (runny nose, sneezing, nasal itch, nasal congestion) and 3 ocular (itchy eyes, watery eyes, red/burning eyes) symptoms. The severity of each individual symptom is rated on a 4-point scale (0 to 3) and are summed for a maximum TRSS of 21 (0 to 21).The 4-point scale includes a severity score of 0 (None: no sign/symptom is evident), 1 (Mild: Sign/symptom clearly present, but minimal awareness; easily tolerated), 2 (Moderate: Definite awareness of sign/symptom that is bothersome, but tolerable), 3 (Severe: Sign/symptom that is hard to tolerate; causes interference with activities during the challenge session. A higher score indicates higher symptom severity." (NCT02543346)
Timeframe: First treatment visit and second treatment visit.

Interventionscore on a scale (Mean)
EEU Placebo11.9
BRC Placebo11.7
EEU Cetirizine11.5
BRC Cetirizine10.8

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Comparison of TOSS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.

"Participants recorded their nasal and ocular symptoms at baseline and during the intervention visits.~The Total Ocular Symptom Score (TOSS) is a composite score comprised of 3 ocular (itchy eyes, watery eyes, red/burning eyes) symptoms. The severity of each individual symptom is rated on a 4-point scale (0 to 3) and are summed for a maximum TOSS of 9 (0 to 9) .The 4-point scale includes a severity score of 0 (None: no sign/symptom is evident), 1 (Mild: Sign/symptom clearly present, but minimal awareness; easily tolerated), 2 (Moderate: Definite awareness of sign/symptom that is bothersome, but tolerable), 3 (Severe: Sign/symptom that is hard to tolerate; causes interference with activities during the challenge session. A higher score indicates higher symptom severity." (NCT02543346)
Timeframe: First treatment visit and second treatment visit.

Interventionscore on a scale (Mean)
EEU Placebo4.6
BRC Placebo4.2
EEU Cetirizine4.4
BRC Cetirizine3.9

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Comparison of TNSS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.

"Participants recorded their nasal and ocular symptoms at baseline and during the intervention visits.~The Total Nasal Symptom Score (TNSS) is a composite score comprised of 4 nasal (runny nose, sneezing, nasal itch, nasal congestion) symptoms. The severity of each individual symptom is rated on a 4-point scale (0 to 3) and are summed for a maximum TNSS of 12 (0 to 12) .The 4-point scale includes a severity score of 0 (None: no sign/symptom is evident), 1 (Mild: Sign/symptom clearly present, but minimal awareness; easily tolerated), 2 (Moderate: Definite awareness of sign/symptom that is bothersome, but tolerable), 3 (Severe: Sign/symptom that is hard to tolerate; causes interference with activities during the challenge session. A higher score indicates higher symptom severity." (NCT02543346)
Timeframe: First treatment visit and second treatment visit.

Interventionscore on a scale (Mean)
EEU Placebo7.3
BRC Placebo7.5
EEU Cetirizine7.1
BRC Cetirizine6.9

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Comparison of GRCS From Baseline Between the EEU and BRC in the Cetirizine 10 mg and Placebo Groups.

"Participants recorded how they were feeling at baseline and at the end of both treatment visits.~The Global Rating of Change Scale documents the changes in the participant's emotions. The scale ranges from +7 (A very great deal better) to -7 (A very great deal worse) with 0 being no change. A higher score indicates a better outcome." (NCT02543346)
Timeframe: First treatment visit and second treatment visit.

Interventionscore on a scale (Mean)
EEU Placebo1.2
BRC Placebo-0.1
EEU Cetirizine1.8
BRC Cetirizine0.9

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Number of Participants With Adverse Events(AEs) and AEs Leading to Permanent Discontinuation of Ofatumumab SC (AELD)

An AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Number of participants with AEs and those with AEs leading to permanent discontinuation of ofatumumab SC (AELD) were to be summarized. Safety Population consists of all participants enrolled in the study. No safety events were reported for the one participant enrolled. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Vital Signs of Clinical Concern

Participants with vitals signs of clinical concern were planned to be summarized. No vital signs of clinical concerns were present for the one participant. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Severe Adverse Events

Severity is a category utilized for rating the intensity of an adverse event. Participants with severe AEs were to be summarized. No serious adverse events (SAEs) were reported for the one participant enrolled. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Post-injection Systemic Reactions

All serious post-injection systemic reactions were planned to be monitored closely throughout the study and number of participants with post-injection systemic reactions was to be summarized. No cases of post-injection systemic reactions were reported for the one participant. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Laboratory Results of Potential Clinical Concern

Blood samples were planned to be collected at Baseline (Week 0) and at Week 8, 20, 28, 36, 44, 52 and at Follow-up visit (Week 60); and at individualized Follow-up visits at Week 72, 84, 96, 108, 120, 132, 144 and 156 for evaluation of clinical chemistry parameters; and at Baseline (Week 0) and at Week 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, 52, 56 and at Follow-up visit (Week 60); and at individualized Follow-up visits at Week 72, 84, 96, 108, 120, 132, 144 and 156 for evaluation of hematology parameters. No laboratory values of potential clinical concern were identified for this one participant. (NCT02613910)
Timeframe: Up to Week 156

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Injection Site Reactions

Number of participants with injection site reactions were planned to be summarized. No cases of injection site reaction were reported for the one participant. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Serious Adverse Events (SAEs) and AEs of Special Interest (AESI)

Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention, events associated with liver injury and impaired liver function were to be categorized as SAE. AEs of special interest included any opportunistic infections, serious post injection systemic reactions, progressive multifocal leukoencephalopathy (PML), hepatitis B virus infection or reactivation, severe mucocutaneous reactions (e.g., toxic epidermal necrolysis and stevens-johnson syndrome), cytopenias and cardiovascular events. Participants with SAEs and AESI were to be summarized. No serious adverse events (SAEs) or adverse events of special interest (AESI) reported. (NCT02613910)
Timeframe: Up to Week 156

InterventionParticipants (Number)
Any SAEAny AESI
Ofatumumab00

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Number of Participants With Infections

All infections were planned to be monitored closely throughout the study and participants with infections were to be summarized. No cases of infection were reported for the one participant. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Number of Participants With Clinically-significant Electrocardiogram (ECG) Abnormalities

12-lead ECG was planned to be taken on Baseline (Week 0) and at Follow-up visit (Week 60). No clinically significant ECG abnormalities were noted for the one participant. (NCT02613910)
Timeframe: Up to Week 60

InterventionParticipants (Number)
Ofatumumab0

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Tolerability of AC 170 0.24% at Visit 3 (Day 22)

Tolerability was assessed upon instillation of study medication, at 1 minute and 2 minutes post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT02756624)
Timeframe: Upon instillation, 30 Seconds Post-Instillation, 1 minute Post-Instillation

,
Interventionunits on a scale (Mean)
Upon instillation30 seconds post-instillation1 minute post-instillation
AC-170 0.24%0.660.370.24
AC-170 Vehicle0.430.250.14

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Tolerability of AC 170 0.24% at Visit 2 (Day 8)

Tolerability was assessed upon instillation of study medication, at 1 minute and 2 minutes post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT02756624)
Timeframe: Upon instillation, 30 Seconds Post-Instillation, 1 minute Post-Instillation

,
Interventionunits on a scale (Mean)
Upon instillation30 seconds post-instillation1 minute post-instillation
AC-170 0.24%0.650.380.26
AC-170 Vehicle0.190.240.21

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Tolerability of AC 170 0.24% at Visit 1 (Day 1)

Tolerability was assessed upon instillation of study medication, at 1 minute and 2 minutes post study medication instillation. Drop comfort was assessed using a 0-to 10 scale where 0=very comfortable and 10=very uncomfortable. (NCT02756624)
Timeframe: Upon instillation, 30 Seconds Post-Instillation, 1 minute Post-Instillation

,
Interventionunits on a scale (Mean)
Upon instillation30 seconds post-instillation1 minute post-instillation
AC-170 0.24%0.870.640.42
AC-170 Vehicle0.500.420.31

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Epworth Sleepiness Scale

Sedation as measured by Epworth Sleepiness Scale. The test is a list of eight situations in which you rate your tendency to become sleepy on a scale of 0, no chance of dozing, to 3, high chance of dozing. Total score 0 to 24 from unlikelihood of abnormally sleep to excessively sleepy. (NCT02865018)
Timeframe: Baseline and 1 year

Interventionunits on a scale (Mean)
Baseline1 year
Cetirizine6.56.9

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Annualized Relapse Rate Before Cetirizine

"Relapses defined as patient-reported symptoms or objectively observed signs typical of an acute inflammatory demyelinating event in the CNS, with duration of at least 24 hours, in the absence of fever or infection. The on study ARR was calculated as the number of relapses during the study divided by the length of time in the study." (NCT02865018)
Timeframe: Baseline and 1 year

Interventionrelapses per year (Mean)
Baseline1 year
Cetirizine0.40.1

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Eotaxin Plasma Levels

Eotaxin - an eosinophil-specific chemoattractant in the blood. Immunological measures related to eosinophil activity. Eotaxin plasma levels. (NCT02865018)
Timeframe: 6 months

Interventionpg/mL (Median)
Cetirizine19.25

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Expanded Disability Status Scale (EDSS)

Disability as measured by Expanded Disability Status Scale (EDSS). The EDSS provides a total score on a scale from 0 to 10, from normal function to lessening function with higher score, 10, being death due to MS. (NCT02865018)
Timeframe: Baseline and 1 year

Interventionunits on a scale (Mean)
Baseline1 year
Cetirizine3.93.2

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Performance Time

Time to complete 8km cycling time trial (NCT03192488)
Timeframe: Performed 60min after pill ingestion

Interventionminutes (Mean)
Cetirizine and Hypoxia17.03
Placebo and Hypoxia18.08
Placebo and Normoxia16.32

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Plasma Histamine Concentrations at Baseline and Post-Exercise

Plasma histamine concentrations (ng/mL) were determined baseline and post-exercise for each experimental condition. Baseline measures were taken immediately prior to exercise and the post-exercise measures were taken 5-10 minutes after the cessation of exercise. (NCT03192488)
Timeframe: baseline and immediately post-exercise, same day as pill ingestion

Interventionng/mL (Mean)
Cetirizine and Hypoxia (Baseline).36
Cetirizine and Hypoxia (Post-Exercise).49
Placebo and Hypoxia (Baseline).56
Placebo and Hypoxia (Post-Exercise).61
Placebo and Normoxia (Baseline).37
Placebo and Normoxia (Post-Exercise).47

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Part 1: Apparent Clearance Following Oral Dosing (CL/F) of Levocetirizine

Blood samples were collected at indicated time points for analysis of CL/F. CL/F of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionLiters per hour (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg2.758
Part 1: Levocetirizine IRT 5 mg2.699

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Part 1: Apparent Terminal Phase Half-life (t1/2) of Levocetirizine

Blood samples were collected at indicated time points for analysis of t1/2. The t1/2 of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHours (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg8.784
Part 1: Levocetirizine IRT 5 mg8.544

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Part 1: Apparent Volume of Distribution Following Oral Dosing (Vz/F) of Levocetirizine

Blood samples were collected at indicated time points for analysis of Vz/F. Vz/F of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionLiters (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg34.95
Part 1: Levocetirizine IRT 5 mg33.27

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Part 1: Area Under the Concentration-time Curve (AUC) From Time Zero Time (Pre-dose) to the Time of Last Quantifiable Concentration (AUC[0-t]) of Levocetirizine

Blood samples were collected to measure AUC(0-t) at indicated time-points. AUC(0-t) was calculated by the linear trapezoidal method (i.e., Linear Trapezoidal Linear Interpolation calculation method in Phoenix WinNonlin). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

InterventionHours*nanogram per milliliter (Hr*ng/mL) (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg1758.5
Part 1: Levocetirizine IRT 5 mg1803.2

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Part 1: Area Under the Concentration-time Curve From Zero Time (Pre-dose) Extrapolated to Infinite Time AUC(0-inf) of Levocetirizine

Blood samples were collected at indicated time points for analysis of AUC(0-inf). AUC(0-inf)) of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHr*ng/mL (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg1812.9
Part 1: Levocetirizine IRT 5 mg1852.5

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Part 1: Change Form Baseline in Hematocrit

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in hematocrit was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionProportion of red blood cells in blood (Mean)
Part 1: Levocetirizine ODT 5 mg0.0036
Part 1: Levocetirizine IRT 5 mg0.0043

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Part 1: Change From Baseline in Amylase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionUnits per liter (U/L) (Mean)
Part 1: Levocetirizine ODT 5 mg6.3
Part 1: Levocetirizine IRT 5 mg7.2

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Part 1: Change From Baseline in Mean Corpuscle Hemoglobin

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in mean corpuscle hemoglobin was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionPicograms (Mean)
Part 1: Levocetirizine ODT 5 mg-0.04
Part 1: Levocetirizine IRT 5 mg-0.03

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Part 1: Change From Baseline in Mean Corpuscle Volume

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in mean corpuscle volume was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionFemtoliters (Mean)
Part 1: Levocetirizine ODT 5 mg-0.6
Part 1: Levocetirizine IRT 5 mg-0.5

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Part 2: Urine Specific Gravity

Urine samples were collected for the measurement of specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. The concentration of the excreted molecules determines the urine's specific gravity. The urinary specific gravity measurement is a routine part of urinalysis. The reference range is 1.002-1.030. (NCT03555890)
Timeframe: Pre-dose (Day 1) and 48 hours post-dose

,
InterventionRatio (Mean)
Pre-dose48 hours
Part 2: Levocetirizine IRT 5 mg1.01791.0159
Part 2: Levocetirizine ODT 5 mg1.01561.0160

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Part 2: Urine Potential of Hydrogen (pH)

Urine samples were collected for the measurement of urine pH. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acid pH (5.0 - 6.0). (NCT03555890)
Timeframe: Pre-dose (Day 1) and 48 hours post-dose

,
InterventionpH (Mean)
Pre-dose48 hours
Part 2: Levocetirizine IRT 5 mg6.116.00
Part 2: Levocetirizine ODT 5 mg6.206.09

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Part 2: Number of Participants With Urinalysis Results by Dipstick Method

Urine samples were collected to assess urine bilirubin, urine occult blood, urine glucose, urine ketones, urine protein and urine urobilinogen by dipstick test. The dipstick test gives results in a semi-quantitative manner, and results for urinalysis parameter of urine bilirubin, urine occult blood, urine glucose, urine ketones, urine protein and urine urobilinogen can be read as negative (-), trace and 1+ indicating proportional concentrations in the urine sample. Only categories with significant values have been presented. (NCT03555890)
Timeframe: Pre-dose (Day 1) and 48 hours post-dose

,
InterventionParticipants (Count of Participants)
Bilirubin, Pre-dose, negativeBilirubin, 48 hours, negativeOccult blood, Pre-dose, negativeOccult blood, 48 hours, negativeOccult blood, 48 hours, traceGlucose, Pre-dose, negativeGlucose, 48 hours, negativeKetones, Pre-dose, negativeKetones, Pre-dose, positive (1+)Ketones, 48 hours, negativeProtein, Pre-dose, negativeProtein, 48 hours, negativeUrobilinogen, Pre-dose, traceUrobilinogen, 48 hours, trace
Part 2: Levocetirizine IRT 5 mg47474747047474614747474747
Part 2: Levocetirizine ODT 5 mg48484847148484804848484848

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Part 2: Number of Participants With AEs and SAEs

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. A SAE is defined as any untoward medical occurrence that, at any dose may results in death or is life-threatening or requires inpatient hospitalization or results in persistent disability/incapacity or is a congenital anomaly/birth defect or any other situation according to medical or scientific judgment. (NCT03555890)
Timeframe: Up to 18 days

,
InterventionParticipants (Count of Participants)
AEsSAEs
Part 2: Levocetirizine IRT 5 mg00
Part 2: Levocetirizine ODT 5 mg60

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Part 2: Change From Baseline in SBP and DBP

Blood pressure was measured in supine position after 5 minutes rest. Change from Baseline in SBP and DBP was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 24, 48 hours post-dose

,
InterventionmmHg (Mean)
SBP, 1 hourSBP, 24 hourSBP, 48 hourDBP, 1 hourDBP, 24 hourDBP, 48 hour
Part 2: Levocetirizine IRT 5 mg-0.9-1.20.3-2.6-1.2-0.2
Part 2: Levocetirizine ODT 5 mg0.2-1.90.7-2.6-2.3-0.6

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Part 2: Change From Baseline in PR Interval, QRS Interval, QT Interval and QTcF Interval

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTcF. Change from Baseline in PR interval, QRS interval, QT interval and QTcF interval was evaluated. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 48 hours post-dose

,
InterventionMillisecond (Mean)
PR interval, 1 hourPR interval, 48 hourQRS duration, 1 hourQRS duration, 48 hourQT interval, 1 hourQT interval, 48 hourQTcF interval, 1 hourQTcF interval, 48 hour
Part 2: Levocetirizine IRT 5 mg-2.80.6-1.9-0.43.1-11.4-0.9-7.6
Part 2: Levocetirizine ODT 5 mg-3.21.2-1.40.33.8-12.11.4-8.5

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Part 2: Change From Baseline in Platelet Count and White Blood Cell Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in platelet count and white blood cell count were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionGI/L (Mean)
Platelet countWhite blood cell count
Part 2: Levocetirizine IRT 5 mg-2.9-1.06
Part 2: Levocetirizine ODT 5 mg-2.5-1.14

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Part 2: Change From Baseline in Hemoglobin and Mean Corpuscle Hemoglobin Concentration

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in hemoglobin and mean corpuscle hemoglobin concentration were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionG/L (Mean)
HemoglobinMean corpuscle hemoglobin concentration
Part 2: Levocetirizine IRT 5 mg0.90.5
Part 2: Levocetirizine ODT 5 mg0.90.2

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Part 2: Change From Baseline in Heart Rate

Heart rate was measured in supine position after 5 minutes rest. Change from Baseline in heart rate was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 24, 48 hours post-dose

,
InterventionBeats per minute (Mean)
1 hour24 hour48 hour
Part 2: Levocetirizine IRT 5 mg-0.60.63.0
Part 2: Levocetirizine ODT 5 mg-1.5-1.91.5

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Part 2: Change From Baseline in Calcium, Cholesterol, Chloride, Glucose, High Density Lipids Cholesterol, Potassium, Low Density Lipids Cholesterol, Sodium, Phosphorus Inorganic, Triglycerides and Urea/BUN Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in calcium, cholesterol, chloride, glucose, high density lipids cholesterol, potassium, low density lipids cholesterol, sodium, phosphorus inorganic, triglycerides and urea/BUN levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionMMOL/L (Mean)
CalciumCholesterolChlorideGlucoseHigh density lipids cholesterolPotassiumLow density lipids cholesterolSodiumPhosphorus inorganicTriglyceridesUrea/BUN
Part 2: Levocetirizine IRT 5 mg0.0159260.064925-0.50.059053-0.0478690.080.084733-0.6-0.2397700.03606-0.45802
Part 2: Levocetirizine ODT 5 mg0.0155940.083506-0.6-0.049728-0.049565-0.030.123374-1.1-0.203831-0.02707-0.12272

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Part 2: Change From Baseline in Body Temperature

Body temperature was measured in supine position after 5 minutes rest. Change from Baseline in body temperature was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 24, 48 hours post-dose

,
InterventionDegree Celsius (Mean)
1 hour24 hour48 hour
Part 2: Levocetirizine IRT 5 mg0.090.080.03
Part 2: Levocetirizine ODT 5 mg0.190.130.03

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Part 2: Change From Baseline in Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in basophils, eosinophils, lymphocytes, monocytes and total neutrophils levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionPercentage (Mean)
BasophilsEosinophilsLymphocytesMonocytesTotal neutrophils levels
Part 2: Levocetirizine IRT 5 mg0.04-0.74-8.07-0.489.25
Part 2: Levocetirizine ODT 5 mg0.08-0.92-8.45-0.499.78

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Part 2: Change From Baseline in Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase, Creatine Kinase, Gamma Glutamyl Transferase and Lactate Dehydrogenase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in alkaline phosphatase, alanine amino transferase, aspartate amino transferase, creatine kinase, gamma glutamyl transferase and lactate dehydrogenase levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionIU/L (Mean)
Alkaline phosphataseAlanine amino transferaseAspartate amino transferaseCreatine kinaseGamma glutamyl transferaseLactate dehydrogenase
Part 2: Levocetirizine IRT 5 mg-2.3-0.7-0.1-16.3-0.1-3.7
Part 2: Levocetirizine ODT 5 mg-1.1-0.50.1-12.4-0.1-3.5

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Part 2: Change From Baseline in Albumin and Total Protein Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in albumin and total protein levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
Interventiong/L (Mean)
AlbuminTotal protein
Part 2: Levocetirizine IRT 5 mg1.41.9
Part 2: Levocetirizine ODT 5 mg1.21.8

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Part 1: Urine Specific Gravity

Urine samples were collected for the measurement of specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. The concentration of the excreted molecules determines the urine's specific gravity. The urinary specific gravity measurement is a routine part of urinalysis. The reference range is 1.002-1.030. (NCT03555890)
Timeframe: Pre-dose (Day 1) and 48 hours post-dose

,
InterventionRatio (Mean)
Pre-dose48 hours
Part 1: Levocetirizine IRT 5 mg1.01441.0163
Part 1: Levocetirizine ODT 5 mg1.01581.0178

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Part 1: Change From Baseline in Hemoglobin and Mean Corpuscle Hemoglobin Concentration

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in hemoglobin and mean corpuscle hemoglobin concentration were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionGrams per liter (G/L) (Mean)
HemoglobinMean corpuscle hemoglobin concentration
Part 1: Levocetirizine IRT 5 mg2.31.8
Part 1: Levocetirizine ODT 5 mg2.22.3

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Part 1: Change From Baseline in Heart Rate (12-Lead Electrocardiogram [ECG])

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QT interval with Fridericia's correction (QTcF). Change from Baseline in heart rate (ECG) was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 48 hours post-dose

,
InterventionBeats per minute (Mean)
1 hour48 hour
Part 1: Levocetirizine IRT 5 mg1.02.5
Part 1: Levocetirizine ODT 5 mg1.62.1

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Part 1: Change From Baseline in Heart Rate

Heart rate was measured in supine position after 5 minutes rest. Change from Baseline in heart rate was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 24, 48 hours post-dose

,
InterventionBeats per minute (Mean)
1 hour24 hour48 hour
Part 1: Levocetirizine IRT 5 mg-0.9-0.12.5
Part 1: Levocetirizine ODT 5 mg-2.3-0.80.8

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Part 1: Change From Baseline in Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in direct bilirubin, total bilirubin, creatinine and uric acid levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionMicromoles per liter (UMOL/L) (Mean)
Direct bilirubinTotal bilirubinCreatinineUric acid
Part 1: Levocetirizine IRT 5 mg0.356-1.710-1.989023.2963
Part 1: Levocetirizine ODT 5 mg0.2140.143-1.952221.0658

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Part 1: Change From Baseline in Calcium, Cholesterol, Chloride, Glucose, High Density Lipids Cholesterol, Potassium, Low Density Lipids Cholesterol, Sodium, Phosphorus Inorganic, Triglycerides and Urea/Blood Urea Nitrogen (BUN) Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in calcium, cholesterol, chloride, glucose, high density lipids cholesterol, potassium, low density lipids cholesterol, sodium, phosphorus inorganic, triglycerides and urea/blood urea nitrogen (BUN) levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionMillimoles per liter (MMOL/L) (Mean)
CalciumCholesterolChlorideGlucoseHigh density lipids cholesterolPotassiumLow density lipids cholesterolSodiumPhosphorus inorganicTriglyceridesUrea/BUN
Part 1: Levocetirizine IRT 5 mg0.0187130.054953-1.0-0.050884-0.0635730.100.038790-0.7-0.182977-0.000470.08033
Part 1: Levocetirizine ODT 5 mg0.0322270.117448-0.9-0.067075-0.0323250.130.059263-0.6-0.1937400.045200.01934

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Part 1: Change From Baseline in Body Temperature

Body temperature was measured in supine position after 5 minutes rest. Change from Baseline in body temperature was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 24, 48 hours post-dose

,
InterventionDegree Celsius (Mean)
1 hour24 hour48 hour
Part 1: Levocetirizine IRT 5 mg0.020.090.01
Part 1: Levocetirizine ODT 5 mg0.20-0.010.06

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Part 2: Change From Baseline in Heart Rate (ECG)

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTcF. Change from Baseline in heart rate (ECG) was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 48 hours post-dose

,
InterventionBeats per minute (Mean)
1 hour48 hour
Part 2: Levocetirizine IRT 5 mg-1.71.9
Part 2: Levocetirizine ODT 5 mg-1.01.7

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Part 1: Change From Baseline in Platelet Count and White Blood Cell Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in platelet count and white blood cell count were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionGiga per liter (GI/L) (Mean)
Platelet countWhite blood cell count
Part 1: Levocetirizine IRT 5 mg-11.4-1.26
Part 1: Levocetirizine ODT 5 mg-6.4-0.94

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Part 1: Change From Baseline in Alkaline Phosphatase, Alanine Amino Transferase, Aspartate Amino Transferase, Creatine Kinase, Gamma Glutamyl Transferase and Lactate Dehydrogenase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in alkaline phosphatase, alanine amino transferase, aspartate amino transferase, creatine kinase, gamma glutamyl transferase and lactate dehydrogenase levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionInternational units per liter (IU/L) (Mean)
Alkaline phosphataseAlanine amino transferaseAspartate amino transferaseCreatine kinaseGamma glutamyl transferaseLactate dehydrogenase
Part 1: Levocetirizine IRT 5 mg-1.61.0-0.3-13.2-0.5-8.8
Part 1: Levocetirizine ODT 5 mg-0.80.5-0.1-10.0-0.6-11.0

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Part 1: Change From Baseline in PR Interval, QRS Interval, QT Interval and QTcF Interval

Single 12-lead ECG was obtained using an ECG machine that automatically calculates the heart rate and measures PR, QRS, QT, and QTcF. Change from Baseline in PR interval, QRS interval, QT interval and QTcF interval was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 48 hours post-dose

,
InterventionMillisecond (Mean)
PR interval, 1 hourPR interval, 48 hourQRS duration, 1 hourQRS duration, 48 hourQT interval, 1 hourQT interval, 48 hourQTcF interval, 1 hourQTcF interval, 48 hour
Part 1: Levocetirizine IRT 5 mg-6.3-1.9-0.8-0.6-6.4-10.7-4.3-4.8
Part 1: Levocetirizine ODT 5 mg-7.3-5.5-0.51.7-9.3-14.3-6.1-9.3

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Part 1: Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

Blood pressure was measured in supine position after 5 minutes rest. Change from Baseline in SBP and DBP was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 1, 24, 48 hours post-dose

,
InterventionMillimeters of mercury (mmHg) (Mean)
SBP, 1 hourSBP, 24 hourSBP, 48 hourDBP, 1 hourDBP, 24 hourDBP, 48 hour
Part 1: Levocetirizine IRT 5 mg0.40.61.3-2.20.01.1
Part 1: Levocetirizine ODT 5 mg-2.00.0-1.2-1.80.30.6

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Part 1: Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. A SAE is defined as any untoward medical occurrence that, at any dose may results in death or is life-threatening or requires inpatient hospitalization or results in persistent disability/incapacity or is a congenital anomaly/birth defect or any other situation according to medical or scientific judgment. (NCT03555890)
Timeframe: Up to 18 days

,
InterventionParticipants (Count of Participants)
AEsSAEs
Part 1: Levocetirizine IRT 5 mg00
Part 1: Levocetirizine ODT 5 mg00

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Part 1: Number of Participants With Urinalysis Results by Dipstick Method

Urine samples were collected to assess urine bilirubin, urine occult blood, urine glucose, urine ketones, urine protein and urine urobilinogen by dipstick test. The dipstick test gives results in a semi-quantitative manner, and results for urinalysis parameter of urine bilirubin, urine occult blood, urine glucose, urine ketones, urine protein and urine urobilinogen can be read as negative (-), trace and 1+ indicating proportional concentrations in the urine sample. Only categories with significant values have been presented. (NCT03555890)
Timeframe: Pre-dose (Day 1) and 48 hours post-dose

,
InterventionParticipants (Count of Participants)
Bilirubin, Pre-dose, negativeBilirubin, 48 hours, negativeOccult blood, Pre-dose, negativeOccult blood, Pre-dose, traceOccult blood, 48 hours, negativeOccult blood, 48 hours, traceGlucose, Pre-dose, negativeGlucose, 48 hours, negativeKetones, Pre-dose, negativeKetones, Pre-dose, positive (1+)Ketones, 48 hours, negativeProtein, Pre-dose, negativeProtein, 48 hours, negativeUrobilinogen, Pre-dose, traceUrobilinogen, 48 hours, trace
Part 1: Levocetirizine IRT 5 mg242424024024242312424242424
Part 1: Levocetirizine ODT 5 mg242423123124242402424242424

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Part 1: Urine Potential of Hydrogen (pH)

Urine samples were collected for the measurement of urine pH. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acid pH (5.0 - 6.0). (NCT03555890)
Timeframe: Pre-dose (Day 1) and 48 hours post-dose

,
InterventionpH (Mean)
Pre-dose48 hours
Part 1: Levocetirizine IRT 5 mg6.066.02
Part 1: Levocetirizine ODT 5 mg6.046.10

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Part 1: Change From Baseline in Basophils, Eosinophils, Lymphocytes, Monocytes and Total Neutrophils Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in basophils, eosinophils, lymphocytes, monocytes and total neutrophils levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

,
InterventionPercentage (Mean)
BasophilsEosinophilsLymphocytesMonocytesTotal neutrophils levels
Part 1: Levocetirizine IRT 5 mg0.01-0.52-5.960.166.32
Part 1: Levocetirizine ODT 5 mg-0.01-0.53-5.94-0.166.64

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Part 1: Change From Baseline in Albumin and Total Protein Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in albumin and total protein levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

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InterventionGrams per liter (g/L) (Mean)
AlbuminTotal protein
Part 1: Levocetirizine IRT 5 mg1.52.3
Part 1: Levocetirizine ODT 5 mg1.62.7

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Part 2: Vz/F of Levocetirizine

Blood samples were collected at indicated time points for analysis of Vz/F. Vz/F of levocetirizine was calculated as by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionLiters (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg34.82
Part 2: Levocetirizine IRT 5 mg33.91

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Part 2: Tmax of Levocetirizine

Blood samples were collected at indicated time points for analysis of tmax. The tmax of levocetirizine was obtained directly from the concentration-time data. The tmax was analyzed with the non-parametric Wilcoxon Matched Pairs Method (Signed Rank Method) to compute point estimate and associated 90% confidence interval for the median difference. (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHours (Median)
Part 2: Levocetirizine ODT 5 mg1.0000
Part 2: Levocetirizine IRT 5 mg1.0000

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Part 2: t1/2 of Levocetirizine

Blood samples were collected at indicated time points for analysis of t1/2. The t1/2 of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHours (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg9.024
Part 2: Levocetirizine IRT 5 mg8.933

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Part 2: MRT of Levocetirizine

Blood samples were collected at indicated time points for analysis of MRT. MRT of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHours (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg12.573
Part 2: Levocetirizine IRT 5 mg12.272

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Part 2: Kel (lambda_z) of Levocetirizine

Blood samples were collected at indicated time points for analysis of kel. kel (lambda_z) is the first order rate constant associated with the terminal (log-linear) portion of the curve. kel of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionPer hour (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg0.07681
Part 2: Levocetirizine IRT 5 mg0.07760

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Part 2: Cmax of Levocetirizine

Blood samples were collected at indicated time points for analysis of Cmax. The values for Cmax were obtained directly from the concentration-time data. (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

Interventionng/mL (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg191.5
Part 2: Levocetirizine IRT 5 mg223.6

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Part 2: CL/F of Levocetirizine

Blood samples were collected at indicated time points for analysis of CL/F. CL/F of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionLiters per hour (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg2.675
Part 2: Levocetirizine IRT 5 mg2.631

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Part 2: Change From Baseline in Reticulocytes

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in reticulocytes was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionPercentage of reticulocytes (Mean)
Part 2: Levocetirizine ODT 5 mg-0.0001
Part 2: Levocetirizine IRT 5 mg-0.0004

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Part 2: Change From Baseline in Red Blood Cell Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in red blood cell count was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionTrillion cells per liter (Mean)
Part 2: Levocetirizine ODT 5 mg0.040
Part 2: Levocetirizine IRT 5 mg0.041

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Part 2: Change From Baseline in Direct Bilirubin, Total Bilirubin, Creatinine and Uric Acid Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in direct bilirubin, total bilirubin, creatinine and uric acid levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

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InterventionUMOL/L (Mean)
Direct bilirubinTotal bilirubinCreatinineUric acid
Part 2: Levocetirizine IRT 5 mg0.036-0.619-3.874613.6677
Part 2: Levocetirizine ODT 5 mg-0.071-0.748-3.591314.0026

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Part 2: Change From Baseline in Mean Corpuscle Hemoglobin

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in mean corpuscle hemoglobin was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionPicograms (Mean)
Part 2: Levocetirizine ODT 5 mg-0.07
Part 2: Levocetirizine IRT 5 mg-0.07

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Part 2: Change From Baseline in Amylase Levels

Blood samples were collected for the assessment of clinical chemistry parameters. Change from Baseline in amylase levels were evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionU/L (Mean)
Part 2: Levocetirizine ODT 5 mg7.4
Part 2: Levocetirizine IRT 5 mg7.1

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Part 2: Change Form Baseline in Hematocrit

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in hematocrit was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionProportion of red blood cells in blood (Mean)
Part 2: Levocetirizine ODT 5 mg0.0023
Part 2: Levocetirizine IRT 5 mg0.0019

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Part 2: AUC(0-t) of Levocetirizine

Blood samples were collected to measure AUC(0-t) at indicated time-points. AUC(0-t) was calculated by the linear trapezoidal method (i.e., Linear Trapezoidal Linear Interpolation calculation method in Phoenix WinNonlin). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

InterventionHr*ng/mL (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg1809.9
Part 2: Levocetirizine IRT 5 mg1843.5

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Part 2: AUC(0-inf) of Levocetirizine

Blood samples were collected at indicated time points for analysis of AUC(0-inf). AUC(0-inf) of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHr*ng/mL (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg1869.5
Part 2: Levocetirizine IRT 5 mg1900.2

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Part 2: %AUCex of Levocetirizine

Blood samples were collected at indicated time points for analysis of %AUCex. Percentage AUCex of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionPercentage AUCex (Geometric Mean)
Part 2: Levocetirizine ODT 5 mg2.973
Part 2: Levocetirizine IRT 5 mg2.779

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Part 1: Time to First Occurrence of Cmax (Tmax) of Levocetirizine

Blood samples were collected at indicated time points for analysis of tmax. The tmax of levocetirizine was obtained directly from the concentration-time data. The tmax was analyzed with the non-parametric Wilcoxon Matched Pairs Method (Signed Rank Method) to compute point estimate and associated 90% confidence interval for the median difference. (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHours (Median)
Part 1: Levocetirizine ODT 5 mg0.5000
Part 1: Levocetirizine IRT 5 mg0.7500

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Part 1: Percentage of AUC(0-inf) Obtained by Extrapolation (%AUCex) of Levocetirizine

Blood samples were collected at indicated time points for analysis of %AUCex. Percentage AUCex of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionPercentage AUCex (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg2.772
Part 1: Levocetirizine IRT 5 mg2.500

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Part 1: Mean Residence Time (MRT) of Levocetirizine

Blood samples were collected at indicated time points for analysis of MRT. MRT of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionHours (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg11.545
Part 1: Levocetirizine IRT 5 mg11.417

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Part 1: Maximum Observed Concentration (Cmax) of Levocetirizine

Blood samples were collected at indicated time points for analysis of Cmax. The values for Cmax were obtained directly from the concentration-time data. (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48 hours post-dose

InterventionNanogram per milliliter (ng/mL) (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg219.9
Part 1: Levocetirizine IRT 5 mg235.4

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Part 1: Elimination Rate Constant (Kel) (lambda_z) of Levocetirizine

Blood samples were collected at indicated time points for analysis of kel. kel (lambda_z) is the first order rate constant associated with the terminal (log-linear) portion of the curve. kel of levocetirizine was calculated by standard non-compartmental analysis using the currently supported version of WinNonlin (version 6.3 or higher). (NCT03555890)
Timeframe: Pre-dose and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 16, 24, 36 and 48 hours post-dose

InterventionPer hour (Geometric Mean)
Part 1: Levocetirizine ODT 5 mg0.07891
Part 1: Levocetirizine IRT 5 mg0.08113

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Part 1: Change From Baseline in Reticulocytes

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in reticulocytes was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionPercentage of reticulocytes (Mean)
Part 1: Levocetirizine ODT 5 mg-0.0001
Part 1: Levocetirizine IRT 5 mg0.0004

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Part 1: Change From Baseline in Red Blood Cell Count

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in red blood cell count was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionTrillion cells per liter (Mean)
Part 1: Levocetirizine ODT 5 mg0.078
Part 1: Levocetirizine IRT 5 mg0.080

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Part 2: Change From Baseline in Mean Corpuscle Volume

Blood samples were collected for the assessment of hematology parameters. Change from Baseline in mean corpuscle volume was evaluated. The Baseline value was the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting Baseline value from the post-dose visit value. (NCT03555890)
Timeframe: Baseline (Day 1, Pre-dose) and 48 hours post-dose

InterventionFemtoliters (Mean)
Part 2: Levocetirizine ODT 5 mg-0.2
Part 2: Levocetirizine IRT 5 mg-0.3

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Asthma Control Test (ACT)

"ACT was measured by questionnaire, assessing frequency of reported asthma symptoms, rescue medication use, the effect of asthma on daily functioning, and overall asthma control. The change in ACT score was calculated between V1 (Baseline), V2 (Guideline Care - before intervention), and V3 (12 Months).~[The ACT score has a minimum value = 5, maximum value = 25, a score 19 indicates well-controlled asthma]" (NCT04179461)
Timeframe: Baseline to 12 months

Interventionscore on a scale (Median)
V1V2V3
Personalized Treatment23.021.722.5

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Adherence of Asthma Controller Medication

Adherence was measured using the Propeller Health Inhaler monitor and web-based software management platform that tracks adherence of asthma medications. The change in adherence was calculated between V1 (baseline) to V3 (12 Months). (NCT04179461)
Timeframe: Baseline to 12 months

Interventionpercentage of medication taken (Median)
V1V3
Personalized Treatment4236

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Pulmonary Function Measured by Spirometry: Forced Expiratory Volume in 1 Second (FEV1) / Forced Vital Capacity (FVC)

"FEV1 is air volume exhaled in 1 second during spirometry. Forced vital capacity is the amount of air that can be forcibly exhaled from the lungs after taking the deepest breath possible. The change in FEV1/FVC was calculated between V1 (Baseline), V2 (Guideline Care - before intervention), and V3 (12 Months). This will be used as a measurement in asthma severity.~[A lower FEV1/FVC ratio indicates more severe asthma]" (NCT04179461)
Timeframe: Baseline to 12 months

InterventionRatio (Median)
V1V2V3
Personalized Treatment0.810.80.8

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Change in Composite Asthma Severity Index (CASI)

"CASI was measured by questionnaire and is a severity score of symptom burden, exacerbations, healthcare utilization, lung function and dose of inhaled corticosteroids. The change in CASI score was calculated between V1 (Baseline), V2 (Guideline Care - before intervention), and V3 (12 Months).~[The CASI score has a minimum value = 0, maximum value = 20, a higher score indicates greater asthma severity]" (NCT04179461)
Timeframe: Baseline to 12 months

Interventionscore on a scale (Median)
V1V2V3
Personalized Treatment555

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"Time From Injection to Readiness for Discharge"

"Describe the distribution of the amount of time spent in the treatment center prior to discharge (time from injection to Readiness for Discharge)." (NCT04189588)
Timeframe: Time to discharge from infusion center

InterventionHours (Mean)
Cohort A4.3
Cohort B4.7

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Number of Hypersensitivity Reactions to Treatment With an Anti-CD20 Antibody or Paclitaxel

"Compare the number of patients experiencing any infusion reaction events, and the number and percentage of patients experiencing each symptom of infusion reactions (flushing, itching, alterations in heart rate and blood pressure, dyspnea, chest discomfort, acute back or abdominal pain, fever, shaking chills, nausea, vomiting, diarrhea, skin rashes, throat tightening, hypoxia, seizures, dizziness, or syncope) to treatment with anti-CD20 such as Rituxan® (rituximab) or Paclitaxel after premedication with intravenous (IV) QUZYTTIR™ cetirizine hydrochloride (HCl) or IV diphenhydramine during first-cycle infusion or re-treatment after 6 months or in patients with persistent infusion reactions while on maintenance with anti-CD20 such as Rituxan® (rituximab) or Paclitaxel.~The infusion reactions will be evaluated following the Common Terminology Criteria for Adverse Events (CTCAE version 5.0) definitions of graded infusion reactions." (NCT04189588)
Timeframe: During and after anti-CD20 agent or paclitaxel infusion, at 1 and 2 hours after the antihistamine injection, at time of discharge, and up through 1 Month post injection of antihistamine (intervention).

InterventionParticipants (Count of Participants)
Cohort A2
Cohort B3

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Patient Sedation Scores at 1 Hour and 2 Hours Post-injection of Antihistamine (IV Cetirizine HCl or IV Diphenhydramine) and at Discharge.

Patient sedation scores at 1 hour and 2 hours post-injection of antihistamine (IV cetirizine HCl or IV diphenhydramine) and at discharge. The patient sedation scores are assessed on a scale of 0-4, with 0=None and 4=Extremely Severe (Asleep, Cannot Self-Rate). The HCP sedation scores are assessed on a scale of 0-4, with 0=None and 4=Extremely severe. (NCT04189588)
Timeframe: 1 hour, 2 Hours and at discharge

,
InterventionUnits on a scale (Mean)
1 Hour2 HourDischarge
Cohort A0.50.60.1
Cohort B1.30.90.4

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