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The role of bilastine in treating
paediatric patients with allergic
rhinoconjunctivitis and urticaria
Bilastine is a second-generation antihistamine that has proven efficacy in treating urticaria and both
seasonal and perennial allergic rhinitis.1,2 It has been shown to have a rapid onset of action with fast
effect as early as 30 minutes, and prolonged duration of effect of more than 24 hours in adults.2–4 In
paediatric patients, the therapeutic dose was identified based on the results of a pharmacokinetic study
demonstrating that bilastine 10 mg once daily in children aged 2 to 11 years offers the same
systemic exposure as 20 mg once daily in adults. Long-term safety data in children showed no
significant differences in treatment-emergent adverse effects (TEAE) between bilastine and
placebo.5 Bilastine is now available in a 10 mg oral-dispersible tablet formulation for children aged
6 – 11 years old*.
In this article, Professor Zoltán Novák, Head of the Aranyklinika Institute in Hungary and President
of the Hungarian Society of Allergology and Clinical Immunology, answers a few key
questions pertaining to second-generation antihistamines and the role of bilastine
in treating school-going children with allergic rhinoconjunctivitis and urticaria.
Q1
In your opinion,
what are the key
clinical and practical
considerations
when prescribing
antihistamines
for children, as
compared to adults?
Professor Zoltán Novák
Professor Novák: When we treat the paediatric population,
the safety of a drug is always the very first consideration.
Another very important consideration when using an antihistamine is its
sedative effects. Allergic rhinitis or urticaria itself can have different effects on
the everyday lives of children; it can cause fatigue, sleepiness and irritability.
A drug that has a sedating effect can exacerbate these problems, resulting in
reduced performance at school and a negative impact on a child’s daily life.
Rapid onset of action is also important in both children and adults. Patients
who are suffering from clinical symptoms would want symptoms to
disappear as quickly as possible; they would not want to wait for hours or even
days for symptoms to resolve. Prophylactic treatment with antihistamines
was considered beneficial towards the management of symptoms associated
with seasonal allergies. However, it is difficult to be exact in predicting
seasonal patterns and as such, a rapid onset of action is beneficial to patients
who suffer from seasonal allergies.
It is also important for an antihistamine to have a long duration of response.
When patients need to take medications twice or three times daily, adherence
rates decline. In contrast, once-daily dosing helps improve adherence.
Lastly, it is also very important, especially in children, for medications to have a
good acceptability. Patients, especially younger children, need to like the taste
of the drug.
*Bilastine 10 mg oral-dispersible tablet is indicated for the symptomatic treatment of allergic rhinoconjunctivitis and
urticaria in children aged 6–11 years with a body weight of at least 20 kg.
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Q2
A paediatric
formulation of
bilastine recently
received marketing
approval for the
treatment of
rhinoconjunctivitis
and urticaria. Could
you tell us more
about the clinical
evidence behind
bilastine and its new
oral-dispersible
formulation?
Professor Novák: There are very strict rules in Europe for the approval of drugs
that are meant for paediatric use.† It is essential to undertake safety clinical
trials that establish the safety of the drug in children. The efficacy of the drug
can be extrapolated from clinical trials in adults. Pharmacokinetic studies can
help determine the appropriate drug dosage for children, and safety trials will
need to be successfully completed before the drug is allowed to enter the
European market.
Bilastine has shown excellent results in pre-clinical studies, clinical trials, a
safety trial and in a bioavailability trial. In a pre-clinical study, bilastine was
shown to have good affinity for H1 receptors, with high receptor selectivity.1
It also demonstrated good oral antihistamine and antiallergic activity.1 In clinical
studies, bilastine was observed to have a rapid onset of action (30 minutes)
and prolonged duration of action (60–70% H1-receptor antagonism at 24 hours
after dosing).3,4
Long-term safety data for the use of bilastine in children showed that after
3 months of treatment there were no significant differences in the incidence
of TEAEs in patients using bilastine versus placebo.5
The pharmacokinetics of bilastine were also assessed in children through
a multicentre adaptive study.6 Systemic exposure resulting from a dose of
10 mg daily in children was shown to be comparable to that achieved in adults
and adolescents administered with a dose of 20 mg daily.
A bioavailability trial that investigated the relationship between dosage and
formulations of bilastine showed that patients had similar concentrations
of bilastine in their plasma regardless of the formulation that was used. This
suggests that the bilastine formulations are inter-changeable.
Professor Novák: The primary difference between first- and second-generation
antihistamines are their sedative side effects. The second-generation drugs
do not cross the blood-brain barrier. As such, the rate of H1-receptor
occupancy in the central nervous system (CNS) is lower with secondgeneration antihistamines. Drugs that have higher H1-receptor occupancy in
the CNS cause sedative side effects. Hence, first-generation antihistamines
affect wakefulness and reduce the patient’s attention span. This was further
confirmed by a study which examined H1-receptor occupancy in patients
taking bilastine versus hydroxyzine using positron emission tomography. The
results showed that bilastine had significantly lower receptor occupancy.7
Bilastine was not associated with subjective sedation or objective impairment
of psychomotor performance.
Bilastine has received approval in Europe for use in paediatric patients.
†
Q3
Why are
second-generation
antihistamines
favoured over first
generation drugs
for the treatment of
allergies in children?
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Q4
In your practice,
what prompts you to
prescribe bilastine
for your paediatric
patients?
Professor Novák: A clinical trial comparing the efficacy of bilastine 20 mg once
daily with cetirizine 10 mg in patients with seasonal allergic rhinitis showed
that bilastine had a comparable symptom relief efficacy while demonstrating
a significantly better TEAE profile.8 In comparison with cetirizine, bilastine
has also been shown to have a faster onset of action in inhibiting wheal and
flare reactions.2 In comparison with fexofenadine, bilastine was found to
have i) similar efficacy and ii) faster onset of action in resolving symptoms
associated with perennial allergic rhinitis.9
Professor Novák: Whilst involved in the clinical study, I was convinced about the
efficacy of bilastine in helping patients with allergic rhinitis or urticaria manage
their symptoms. I was also reassured by its safety profile. These are my key
reasons for frequently prescribing bilastine to my patients.
Q6
How does
bilastine compare
with other
second-generation
antihistamines in
the market?
Q5
How do you feel
about the impact
bilastine has on
the quality of life in
paediatric patients?
Professor Novák: I can safely say that bilastine improves the quality of
life in children. Apart from symptom resolution, a child’s performance at
school is also an important consideration for parents. With bilastine, children
are able to focus at school, and not experience sedative side effects which
could hamper their performance. Parents of children are often relieved when
they see that their child’s performance at school has improved as a result
of switching to bilastine. Therefore, both parents and children have a good
opinion of bilastine.
References:
1. Corcóstegui R et al. Drugs R D. 2006;7:219–31.
2. Ridolo E et al. Clin Mol Allergy 2015;13:1.
3. Bosma R et al. Eur J Pharmacol 2018;5:107–11.
4. Antonijoan R et al. Curr Med Res Op. 2017;33:129–36.
5. Novak Z et al. Pediatr Allergy Immunol 2016;27:493–8.
6. Vozmediano V et al. Eur J Pharm Sci 2019;128:180–92.
7. Farré M et al. Br J Clin Pharmacol 2014;78:970–80.
8. Kuna P et al Clin Exp Allerg 2009;39:1338–47.
9. Okubo K et al. Allerg Intl 2017;66:97–105.
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BILAXTEN: A LIFETIME COMPANION
FOR THE TREATMENT OF ALLERGIES
1,2
ABBREVIATED PRESCRIBING INFORMATION: BILAXTEN 10 MG ORODISPERSIBLE TABLETS. THERAPEUTIC INDICATIONS: Symptomatic treatment of allergic rhino-conjunctivitis and urticaria. Bilaxten is indicated in children aged 6 to 11 years with a body
weight of at least 20kg. POSOLOGY AND METHOD OF ADMINISTRATION: Children 6 to 11 years of age with a body weight of at least 20 kg 10 mg bilastine (1 orodispersible tablet) once daily for the relief of symptoms of allergic rhino-conjunctivitis and urticaria. The orodispersible
tablet should be taken one hour before or two hours after intake of food or fruit juice. CONTRAINDICATIONS: Hypersensitivity to the active substance (bilastine) or to any of the excipients. PRECAUTIONS: Efficacy and safety of Bilastine in children under 2 years of age have not
been established. In patients with moderate or severe renal impairment, co-administration of bilastine with P-glycoprotein inhibitors, such as ketoconazole, erythromycin, cyclosporine, ritonavir or diltiazem, may increase plasmatic levels of bilastine and therefore increase the risk of
adverse reactions of bilastine. Therefore, co-administration of Bilastine and P-glycoprotein inhibitors should be avoided in patients with moderate or severe renal impairment. Food significantly reduces the oral bioavailability of bilastine 10mg orodispersible tablets by 20%. FERTILITY
AND LACTATION: Fertility: There are no or limited amount of clinical data. Pregnancy: There are no or limited amount of data from the use of bilastine in pregnant women. As a precautionary measure, it is preferable to avoid the use of bilastine during pregnancy. Breast-feeding: It is
unknown whether bilastine is excreted in human breast milk. A decision on whether to discontinue/abstain from bilastine therapy must be made taking into account the benefit of breast-feeding for the child and the benefit of bilastine therapy for the mother. UNDESIRABLE EFFECTS:
The percentage of children (2-11 years) which reported adverse events (AEs) after treatment with bilastine 10 mg for allergic rhinoconjunctivitis or chronic idiopathic urticaria in a 12-week controlled clinical trial was comparable with the percentage in the group receiving placebo.
References: 1. Bilaxten 10mg Orodispersible Tablet Product Insert, last assessed Sep 2020, https://eservice.hsa.gov.sg/prism/common/enquirepublic/SearchDRBProduct.do?action=getProductDetails 2. Church MK, Tiongco-Recto M, Ridolo E, Novak Z. Bilaxten:
a lifetime companion for the treatment of allergies, Current Medical Research and Opinion, DOI:10.1080/03007995.2019.1681134.
Please consult the full PI for full prescribing information
For Healthcare Professionals Only
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Tel: +65 6494 3400 Fax: +65 6777 1786. www.menariniapac.com.
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