Articles about Bilastine

High dose Bilastine for the treatment of Bascule Syndrome

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L Cunningham

Clin Exp Dermatol . 2020 Jul 13. doi: 10.1111/ced.14377. Online ahead of print.

Bascule syndrome (bier anaemic spots and cyanosis with urticarial-like eruption) was described for the first time in 2016 and it remains to be fully elucidated. To date no successful treatment has been described.

This is a case study of a 16-year old boy who presented a patchy discolouration of the lower legs in a dependent position, associated with burning and stinging sensations and dizziness and light-headedness when moving from sitting to standing. These symptoms were present for a year. Allergy, neurology and cardiology consultations were inconclusive, Tilt table testing revealed no evidence of orthostatic hypotension or postural orthostatic tachycardic syndrome but triggered his symptoms. A dermatologist diagnosed him with Bascule syndrome, based on his clinical findings.

Different antihistamines were trialled (cetirizine 10 mg daily, bilastine 20 mg daily) with no success. A dose of bilastine 40 mg twice daily completely resolved his symptoms, but recurred when the dose was reduced to half.


This is the first documented case of a successful treatment of Bascule syndrome with bilastine. It is likely that the dose needed may be higher than usual dose antihistamines. Also, the decision to treat with antihistamines should be based on symptoms.

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Effectiveness, safety and tolerability of Bilastine 20 mg versus Levocetirizine 5 mg for the treatment of chronic spontaneous urticaria: a double-blind, parallel group, randomized controlled trial

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Indrashis Podder, Anupam Das, Shouvik Ghosh, Debalina Biswas, Sujata Sengupta, Satyendra Nath Chowdhury

Dermatol Ther. 2020 Jul 2;e13946. doi: 10.1111/dth.13946. Online ahead of print.

Chronic urticaria is characterized by wheals with or without angioedema for, at least, 6 weeks. It is a debilitating condition that affects people’s quality of life. Bilastine is a novel non-sedative H1 antihistamine approved for symptomatic treatment of allergic rhinoconjunctivitis and urticaria in patients older than 12 years old.

The objective of this study was to compare the effectiveness, safety and tolerability of bilastine 20 mg with levocetirizine 5 mg in moderate-to-severe chronic spontaneous urticaria.

This was a double-blind, randomized, controlled study with two arms: bilastine 20 mg once daily (31 participants) and levocetirizine 5 mg once daily (27 participants) for 42 days. The severity of urticaria, global urticaria-induced discomfort and quality of life were evaluated with UAS7 (urticaria activity score), VAS (visual analogue scale) and DLQI (dermatology life quality index) at baseline and follow-up visits.

Primary objective was to assess the variation of the UAS7, and secondary objectives assessed changes in DLQI and VAS. Safety, tolerability and compliance were evaluated by analysis of drug-related adverse events, biochemical investigations and electrocardiogram.

Both bilastine and levocetirizine improved UAS7, DLQI and VAS at the end of treatment. Also, all parameters showed greater improvement with bilastine, but only the UAS7 revealed a significant reduction (p = 0,03). Sedation was also significantly less with bilastine (p = 0,04). Both treatments improved UAS7 and VAS significantly from day 14. No serious adverse effects were registered.

In conclusion, bilastine demonstrated a better efficacy and less sedation for chronic spontaneous urticaria when compared to levocetirizine, however similar effect on quality of life.

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Elucidation of Inverse Agonist Activity of Bilastine

Elucidation of Inverse Agonist Activity of Bilastine

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Hiroyuki Mizuguchi, et al.

Pharmaceutics 2020, 12, 525; doi: 10.3390/pharmaceutics12060525.

Histamine is a chemical mediator that causes pollinosis symptoms such as a sneezing, rhinorrhoea, nasal obstruction, nasal itching, and itching of the eyes. H1-antihistamines antagonize histamine H1, preventing it from binding to the histamine H1 receptor (H1R). Bilastine is a non-sedative recently launched H1-antihistamine which has high affinity for H1R. It is one of the H1-antihistamines that most satisfies the requirements of allergic rhinitis and asthma guidelines. Inverse agonists are thought to be more potent than neutral antagonists because they supress the intrinsic histamine signalling in addition to the H1-antihistamine effect. Nevertheless, there is a lack of information regarding bilastine inverse agonist activity.

This study assessed if bilastine has inverse agonist activity or not. HeLa cells that express H1R endogenously here used, and three methods applied: time-lapse Ca2+ imaging, inositol phosphates (IPs) accumulation and H1R gene expression. Intracellular calcium concentration was measured using Fluo-8. Inositol phosphates accumulation was assayed using [3H]myo-inositol. The H1R mRNA level was measured using real-time RT-PCR.

H1R intrinsic activity was shown by Ca2+ oscillation. Also, bilastine suppressed IPs formation and basal H1R gene expression in a dose-dependent manner.

These results elucidate that bilastine has an inverse agonist activity. Taking bilastine before pollen season, the H1R gene expression level can be kept low, improving pollinosis symptoms.

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rinitis alérgica

Multidisciplinary Real-World Experience With Bilastine, a Second Generation Antihistamine

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Lynde CW, Sussman G, Dion PL, Guenther L, Hébert J, Rao J, Leek TV, Waserman S.


J Drugs Dermatol. 2020 Feb 1;19(2):145-154. doi: 10.36849/JDD.2020.4835.

Allergic conditions, such as seasonal allergic rhinitis, perennial allergic rhinitis (PAR), and urticaria (both acute and chronic) are frequently treated with H1-antihistamines. However, first-generation H1-antihistamines cause impairment and potentially interfere with restful sleep, cause hangovers or “morning after” effects, impair learning and memory, and reduce work efficiency. Second generation antihistamines, such as bilastine have shown to decrease allergy symptoms effectively without causing night-time sleep disturbances and related adverse events.

Bilastine is a prescription medicine. It is not derived from nor is it a metabolite of another antihistamine, has a rapid one-hour onset of action and provides sustained efficacy. Bilastine does not penetrate the brain, is scarcely metabolized and does not interact with cytochrome P450. For the treatment of allergic conditions in adults and children over 12 years of age, a daily oral dose of bilastine 20 mg is recommended.

This real world case project was developed to help optimize patient care and supported with evidence from the literature. It included patients between 9 and 76 years old with seasonal allergic rhinitis, perennial allergic rhinitis and chronic and acute urticaria as well as urticarial vasculitis and pruritus associated with inflammatory skin conditions.

The presented cases using bilastine showed positive outcomes for the patients, relieving symptoms with safety and good tolerance.

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La urticaria crónica (CUR) contribuye a la comprensión y el conocimiento de la enfermedad en la región.

Impact of treatment with bilastine for PD-1/PD-L1 inhibitors induced rash

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Hirata T.

Ann Oncol. 2019 Feb;30 Suppl 1:i13. doi: 10.1093/annonc/mdz026.005. Epub 2020 Jan 8

Several tumors are treated with PD-1/PD-L1 inhibitors, such as nivolumab, pembrolizumab, atezolizumab. However, these are known to induce rash in some cases. Rash treatment included antihistamines and corticosteroids. Bilastine is a non-sedating second generation H1-antihistamine, but its effectiveness in rash caused by PD-1/PD-L1 inhibitors is unknown. The aim of this study was to assess the efficacy of bilastine in these cases.

This study included 84 patients with PD-1/PD-L1 rash of a group of 224 patients from a Japanese medical center between September 2014 and October 2018. They were classified into 4 groups according to the systemic antihistamine and topical corticosteroid therapy: (1) bilastine and corticosteroid group (n = 18), (2) another antihistamine and corticosteroid group (n = 22), (3) bilastine only group (n = 20) and (4) another antihistamine group (n = 24).

The group in bilastine and corticosteroid showed a significantly shorter median duration of treatment than group 2. Bilastine group had a significantly shorter period of systemic medications than the another antihistamine group. Adverse events reported included somnolence (3 %), headache (3 %) and dizziness (3 %) and no serious adverse events were reported.

In conclusion, bilastine treatment reduced the need and duration of topical corticosteroid use in PD-1/PD-L1 inhibitors induced rash with a good safety profile.

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seguridad tolerabilidad bilastina

The safety and tolerability profile of bilastine for chronic urticaria in children

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Papadopoulos NG, Zuberbier T.

Clin Transl Allergy. 2019 Oct 23;9:55. doi: 10.1186/s13601-019-0294-3. eCollection 2019. Review.

Urticaria is characterized by the development of pruritic wheals, angioedema or both. Guidelines from early 2018 recommend that urticaria is classified based on its duration as acute (< 6 weeks) or chronic (> 6 weeks). In addition, they also classify chronic urticaria as spontaneous or inducible. Chronic urticaria is less frequent than acute in children, but is a condition that requires treatment, as it affects children’s daily activities, disturbs sleep, causes emotional distress and influences negatively learning and cognition.

Bilastine is a H1-antihistamine that has been studied in children at the dose of 10mg/daily and is licensed for the symptomatic relief of urticaria symptoms in children > 6 to 11 years.

Investigation in paediatric population included bilastine and rupatadine among the second-generation antihistamines. A phase III, doubleblind, randomized, placebo-controlled, parallel-group clinical trial was carried out to assess the safety and tolerability of bilastine 10 mg once daily for 12 weeks in 509 children aged 2–11 years with allergic rhinitis or chronic urticaria. The primary endpoint was the proportion of children in each treatment group without treatment-emergent adverse events (TEAEs). Secondary endpoints included the assessment of somnolence/sedation with the Pediatric Sleep Questionnaire (PSQ). No statistically significant differences were found between treatment groups for incidences of TEAEs or related TEAEs in the population overall or by age subgroup. The majority of related TEAEs were mild to moderate in intensity. PSQ scores for somnolence/sedation decreased slightly from baseline to week 12 in both the bilastine 10 mg and placebo groups.

In conclusion, bilastine is a suitable for treatment of urticaria in children, due to its efficacy and good tolerability profile that were proven in well-controlled studies. Specifically, lack of potential to induce sedation allows prolonged administration without impairment of performance and learning abilities.

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Bilastine: a lifetime companion for the treatment of allergies

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Martin K. Church, Marysia Tiongco-Rectob, Erminia Ridoloc and Zoltan Novàk.

Bilastine is a potent and highly selective H1-antihistamine approved for the treatment of allergic rhinoconjunctivitis and urticaria. This article summarizes available data on the use of bilastine in the treatment of allergic disorders in different age groups, including younger and older adults, and school-age children and adolescents.

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Investigación en laboratorio alergias

Concomitant Bilastine and Montelukast as Additive Therapy for Seasonal Allergic Rhinoconjunctivits and Mild-to-Moderate Asthma. The SKY Study

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Lavorini F, Matucci A, Rossi O, Pistolesi M; SKY study investigators.

A double-blind, double-dummy, randomised, active-controlled, parallel group design (The SKY study) compared the efficacy and efficacy of concomitant therapy with bilastine and montelukast with each substance alone in patients with seasonal allergic rhinoconjunctivitis and asthma for four weeks.

419 adults with seasonal allergic rhinoconjunctivitis and mild-to-moderate asthma partially controlled by beclomethasone dipropionate or equivalent were included. They had a forced expiratory volume (FEV1) >70%, a positive skin prick test to one or more allergens and nasal/ocular total symptom score (TSS) >3. Participants were screened for one week and then a twelve weeks treatment.

Allergic rhinoconjunctivitis score (TSS), daytime nasal and non-nasal symptom scores and use of rescue medications were registered.

Contrary to the original hypothesis, concomitant administration of bilastine with montelukast was as effective as either agent alone for allergic rhinoconjunctivitis symptoms, however bilastine alone improved allergic rhinoconjunctivitis symptoms more than montelukast in the first two weeks of treatment.

The SKY study investigators concluded that there is no benefit of using bilastine plus montelukast to provide relief of allergic rhinoconjunctivitis in patients with mild-to-moderate asthma.

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bilastina alivia prurito

Efficacy and safety of bilastine in reducing pruritus in patients with chronic spontaneous urticaria and other skin diseases: an exploratory study

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Serra E, Campo C, Novák Z, Majorek-Olechowska B, Pulka G, García-Bea A, Labeaga L.

PURPOSE: To evaluate the efficacy/safety of bilastine in pruritus relief in patients with chronic spontaneous urticaria (CSU) or other pruritic skin diseases.

CONCLUSIONS: Bilastine relieved pruritus associated with urticaria and other skin diseases, with a very good safety profile.

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Bilastina y anticuerpos anti-

The real-life effectiveness and safety of omalizumab updosing in patients with chronic spontaneous urticaria

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Andac Salman and Elif Comert

(2019) Journal of Cutaneous Medicine and Surgery

A retrospective cohort study was conducted to investigate the effectiveness and safety of 450 mg of omalizumab in chronic spontaneous urticaria.

Omalizumab is a third-line treatment for chronic spontaneous urticaria, however there are not enough studies regarding its use in patients that are unresponsive to regular doses of omalizumab.

A total of 72 patients were included, according to their Urticaria Activity Score over 7 days and the Urticaria Control Test and divided in two groups. Group 1 (n=59) included those showing a complete response to omalizumab 300 mg and group 2 (n=13) included those who received at least 3 doses of omalizumab 450 mg between 2016 and 2018.

The mean Urticaria Activity Score over 7 days decreased from 18,6 to 5,1 and the mean Urticaria Control Test score increase from 8,6 to 12 in group 2 participants after a mean 4,3 courses of omalizumab 450 mg. Of all 13 participants from group 2, 6 of them had a complete response, and 3 a good disease control. Those whose response to treatment was lower had low baseline total IgE levels (<43 IU/mL).

In conclusion, this team demonstrated that higher doses of omalizumab are effective and safe in patients with chronic spontaneous urticaria that is unresponsive to omalizumab 300 mg. Also, they predict that lower baseline total IgE levels might be related to a nonresponse to omalizumab and the need for higher doses.

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