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Bilastina

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

By | Eprint, News

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.

This document is only available for registered healthcare professionals.

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High dose Bilastine for the treatment of Bascule Syndrome

By | Articles about Bilastine

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

By | Articles about Bilastine

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

By | Articles about Bilastine

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

By | Articles about Bilastine

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.

This document is only available for registered healthcare professionals

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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

By | Articles about Bilastine

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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eprint

Bilastine: a lifetime companion for the treatment of allergies

By | Eprint

Martin K Church, Marysia Tiongco-Recto, Erminia Ridolo & Zoltán Novàk.

(2019) Current Medical Research and Opinion, DOI: 10.1080/03007995.2019.1681134

Bilastine is a potent and highly selective H1-antihistamine for the treatment of urticaria and allergic rhinoconjunctivitis.

This is a review article that gathers information available up to 25 February 2019 on the use of the H1-antihistamine bilastine in the treatment of allergic disorders in different age groups, from children to adults.

Teenagers and adults bilastine dose is usually 20 mg daily and children up to 12 years old is 10 mg of bilastine once daily. Bilastine has demonstrated efficacy at improving allergic rhinitis symptoms, such as nasal and ocular symptoms and at improving wheals and itching in urticaria. It has a rapid onset of action and a long duration of action.

Bilastine does not interact with the CYP450 system, making it a H1-antihistamine free from drug-drug interactions. Patients with renal or hepatic impairment or elderly ones don’t need dosage adjustment. Bilastine is well tolerated, even at above standard doses and doesn’t exhibit anticholinergic or cardiotoxic effects. It has minimal sedative properties due to its inexistence central nervous system penetration. Patients on bilastine show an overall improvement of health-related quality of life.

In conclusion, bilastine is a suitable option of H1-antihistamins for the treatment of allergic rhinoconjunctivitis or urticaria in all patients.

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seguridad tolerabilidad bilastina

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

By | Articles about Bilastine

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

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

By | Eprint

Esther Serra, Cristina Campo, Zoltan Novak, Bernadetta Majorek-Olechowska, Grazyna Pulka, Aintzane García-Bea and Luis Labeaga

Pruritus is a common symptom associated with different skin diseases, including urticaria, atopic dermatitis, eczema and prurigo. Pruritus may have a significant impact on the quality of life and psychosocial wellbeing of patients with skin urticaria. Bilastine is a H1-antihistamine with demonstrable efficacy for the symptomatic treatment of chronic spontaneous urticaria.

 

A phase IV, multicentre, open-label, exploratory study to evaluate the efficacy and safety of bilastine in reducing pruritus in patients with chronic spontaneous urticaria and other skin diseases was conducted at 10 European Centres.

 

115 patients between 18 and 74 years diagnosed with chronic spontaneous urticaria, eczema/dermatitis, prurigo or cutaneous pruritus who had not responded to placebo during a run-in period of 7-14 days and with, at least 4 points for the sum of itch score during the last 3 days of the run-in period were included. Patients received bilastine 20 mg once daily for 8 weeks and non-responders (<30% improvement in pruritus score at week 2), received 40 mg daily from week 2.

 

Bilastine reduced the mean change in weekly pruritus severity score from baseline to week 8 (primary endpoint) (overall and by disease group). Up dosed non-responders (n = 31) improved weekly pruritus severity scores from baseline to week 8. Bilastine improved the Dermatology Life Quality Index at weeks 4 and 8 (p < 0,001) in all disease groups, and the 7-day Urticaria Activity Score in CSU patients (p <0 ,001).

 

In conclusion, bilastine has demonstrated efficacy for the relief of pruritus associated with urticaria and other skin diseases in adults, with a very good safety profile. Also, bilastine up dosing to 40mg (double dose), for patients who did not achieve a significant improvement after 2 weeks of treatment, was efficacious without any safety concerns.

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Relevancia clínica interacción medicamentos y alimentos

Lack of clinical relevance of bilastine-food pharmacokinetic interaction assessed by inhibition of histamine-induced wheal and flare response in healthy volunteers

By | Articles about Bilastine

Jimena Coimbra, Cristina Campo, Luis Labeaga, Montserrat Puntes, Ignasi Gich, Joan Martínez, Rosa Antonijoan.

The main objective of this study was to compare the efficacy of bilastine 20mg administered orally, under fasting and fed conditions, in the reduction of histamine-induced skin reactivity (wheal and flare response) in healthy volunteers, taking into account the first treatment day (Day1) and the steady state (Day4). The final aim of this study was to assess the clinical relevance of this food-drug interaction.
As a conclusión of the study, the pharmacokinetic interaction of bilastine with food does not imply a significant reduction of its antihistamine efficacy, and the interaction of bilastine with food lacks clinical relevance since no significant pharmacodynamic interaction was observed.

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Antihistamínicos H1

Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties.

By | Articles about Bilastine
Kawauchi H, Yanai K, Wang DY, Itahashi K, Okubo K.

Antihistamines targeting the histamine H₁ receptor play an important role in improving and maintaining the quality of life of patients with allergic rhinitis. For more effective and safer use of second-generation drugs, which are recommended by various guidelines, a classification based on their detailed characteristics is necessary. Antihistamines for first-line therapy should not have central depressant/sedative activities.
Among the non-sedating group, fexofenadine and bilastine are classified into “non-brain-penetrating antihistamines”.
This review summarizes that the non-brain-penetrating antihistamines should be chosen for the first-line therapy of mild allergic rhinitis.

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The long duration of action of the second generation antihistamine bilastine coincides with its long residence time at the histamine H1 receptor

By | Articles about Bilastine
Bosma R, van den Bor J, Vischer HF, Labeaga L, Leurs R

Bilastine shows a long drug-target residence time at the H1 receptor (73 ± 5 min) and this results in a prolonged H1 receptor antagonism in vitro (Ca2+ mobilization in Fluo-4 loaded HeLa cells), following a washout of unbound antagonist. Hence, the long residence time of bilastine can explain the observed long duration of drug action in vivo.

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Antihistamínico novel

Bilastine – A Novel Antihistamine for Allergic Rhinitis and Chronic Spontaneous Urticaria

By | Articles about Bilastine
Kraft JN, Sussman GL

Bilastine has a proven, long-term safety record with use by over 71 million patients in over 104 countries. This novel, second generation antihistamine is non-sedating due to the fact that it does not cross the blood brain barrier. As well, bilastine is not metabolized and does not interact with CYP450.

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F1 simulador

Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients

By | Articles about Bilastine
Demonte A, Guanti MB, Liberati S, Biffi A, Fernando F, Fainello M, Pepe P

This study is the first done in patients with allergic rhinitis and/or chronic urticaria using a F1-high speed simulator-driving test evaluating subjects’ performance under bilastine treatment.

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Estudio de bilastina en pacientes japoneses

One-year safety and efficacy study of bilastine treatment in Japanese patients with chronic spontaneous urticaria or pruritus associated with skin diseases

By | Articles about Bilastine
Yagami A, Furue M, Togawa M, Saito A, Hide M.

A number of second-generation non-sedating antihistamines are used in clinical practices over the world. However, long-term safety and efficacy have not been proved high level evidence based medicine. 
In conclusion, long-term treatment with bilastine 20 mg once daily for 52 weeks is safe and well tolerated in Japanese patients with hronic spontaneous urticaria (CSU) or pruritus associated with skin diseases. Bilastine improved disease symptoms of both conditions early in treatment, and the efficacy was maintained throughout the treatment.

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