Bilastine - nonsedating oral antihistamine indicated for seasonal allergic rhinitis and spontaneous urticaria

1. BILASTINE – A NOVEL ANTI-HISTAMINE
By
Dr.Pavithra.A.,Pharm.d

2. Bilastine
 Non-sedating Oral H1 Antihistamine
Indications and Clinical use
 Seasonal Allergic Rhinitis- For the symptomatic relief of nasal and non-nasal
symptoms of seasonal allergic rhinitis (SAR) in patients 12 years of age and
older.
 Chronic Spontaneous Urticaria-For the relief of the symptoms associated with
chronic spontaneous urticaria (CSU) (e.g. pruritus and hives), in patients 18 years
of age and older.
Regulatory Approval
 It has been approved in India by the DCGI in February 2019

3. HOW BILASTINE IS SUPERIOR THAN LEVOCETRIZINE AND
FEXOFENADINE
Sno Characteristics Bilastine Fexofenadine Levocetirizine
1. H1 receptor selectivity +++ + ++
2. Indicated for allergic
rhinoconjunctivitis?
yes No No
3. Indicated for allergic rhinitis? yes yes yes
4 Indicated for urticaria? yes yes yes
5 Paediatric indication? No (ongoing
studies )
(children ≥3
years)
(children ≥ 2
years)

4. Sno Characteristics Bilastine Fexofenadine Levocetirizine
6 Dosage adjustment in renal
impairment?
No No Yes (in moderate-
to severe)
7 Dosage adjustment in hepatic
impairment?
No No Yes (if
concomitant renal
dysfunction)
8 Interaction with food? Yes (given on
empty
stomach )
Not mentioned No
9 Use in pregnancy and lactation? Caution (very
limited data)
No Caution
10 Clinically relevant drug interactions? No Yes (antacids) Unlikely (no
available data)

5. Sno Characteristics Bilastine Fexofenadine Levocetirizine
11 Can patients drive and operate
machinery (i.e., lack of sedative
potential)?
Yes (caution:
drowsiness)
Yes(impairment
unlikely)
Yes (check drug
response when
intending to drive)
12 Contraindications None None Severe renal
impairment
13 Number of ARIA recommended
antihistamine properties
10 9.5 6.5
A.Data obtained from Summary of Product Characteristics for each individual compound (available from
http://www.medicines.org.uk/emc/).
B. Score is derived from ARIA recommended antihistamine properties.6 (0.5 is given for each characteristic
where “caution” is recommended). ±, negligible; +, mild; ++, moderate; +++, marked.

6. CLINICAL EVIDENCE
Effectiveness of bilastine and fexofenadine among allergic Rhinitis patients in
Ranchi, Jharkhand, India
 Compared the effectiveness of Bilastine and Fexofenadine in treatment of allergic Rhinitis patients.
 This was an observational, single centred, two arm, parallel-group, comparative clinical study conducted
in the Department of pharmacology & Therapeutics, among the patients attending out patient
department of Ear, Nose and Throat (ENT) Department.
 Patients were divided randomly in two groups A and B. Patients of group A were allowed to take tab
Bilastine 20 mg OD whereas, patients of group B were allowed to take tab. Fexofenadine Hydrochloride
120 mg OD orally for two weeks.
 Evaluation of total nasal symptom score was done . Total nasal symptom score (TNSS) was composed
of the sum of five individual symptom scores (sneezing, rhinorrhoea, nasal obstruction, nasal itching
and difficult sleep).

7.  The maximum score for TNSS was 15 for each recorded time point.
 The baseline Total Nasal Symptom Score (TNSS) were compared between two groups. The mean TNSS was
significantly reduced in our study group. Baseline TNSS was 13.55 and 13.45 in Group A and Group B
respectively.
 Reduction in this parameter first become apparent in the 24 hours and was maintained till 2nd week.
 The mean change of TNSS score was 8.71 in Group A and 9.78 in Group B from baseline to 24 hours.
 Similarly, the mean change of TNSS score was 6.94 in Group A and 7.65 in Group B from baseline to 1st
week.
 The mean change of TNSS score was 2.7 in Group A and 3.43 in Group B from baseline to 2nd week.
Bilastine showed significant improvement in quality
of life of Allergic rhinitis patients and proved to be
more effective than fexofenadine in reducing the
TNSS score, when used alone in allergic rhinitis
patient.
Graphical presentation of mean changes in TNSS from Day 0 to after 1 day, 1 week and 2
weeks in both Group A & B. TNSS scores decreased at 2 weeks.

9. A Comparative, Three-Arm, Randomized ClinicalTrial to Evaluate the Effectiveness and
Tolerability of Bilastine vs Fexofenadine vs Levocetirizine at the Standard Dose and Bilastine
vs Fexofenadine at Higher Than the Standard Dose (Up-Dosing) vs Levocetirizine and
Hydroxyzine (in Combination) in Patients with Chronic Spontaneous Urticaria
 This was a randomized, comparative, open-label, three-arm, and single-
centre study. Participants were recruited from April 2020 till October
2020 and followed up for four weeks.
 This study was done in a tertiary care hospital in Ahmedabad.
 The primary outcome measures included improvement in urticaria
symptoms, somnolence, and quality of life (QoL)

10.  Well-controlled urticaria at end of 2nd and 4th week
by bilastine, fexofenadine and levocetirizine.
 On up-dosing, in the bilastine arm, it was further
reduced to 5.25±3.09 from 12.56±3.08 (58.6%
reduction), whereas in fexofenadine it was
reduced to 5.65±2.64 from 11.06±2.49 (48.9% ↓).
 After addition of hydroxyzine in the
levocetirizine arm, it was reduced to 8.0±3.14 from
13.68±3.9 (41.5% ↓) at week 4.
Figure 1 No. of patients showing improvement in urticaria measured at week 2 and week 4.

11. Quality of Life
 Quality of life was assessed by using the CU-Q2oL, which asked questions about pruritus,
swelling, and impact on life activities, sleep problems, looks and limits in order to obtain
the patient’s view of both the overall impact of chronic urticaria and the effectiveness of
its treatment.
 Bilastine was statistically significant (p<0.05) in the improvement of quality of life by
CU2QoL as compared to both the other arms.
Figure 3 Changes in QoL measured during the follow-up visits (week 2 and 4)

12. Somnolence
 A major concern with increasing doses of H1-antihistamines is that of somnolence. Sleepiness with the
drug was measured by VAS(visual analog scale ).
 Levocetirizine had a higher mean VAS score, and it increased when hydroxyzine was added.
 On day14, fexofenadine had a lower score than levocetirizine but higher than bilastine. The somnolence
score of bilastine and fexofenadine did not increase when their dose was increased.
 Bilastine was statistically better (p<0.05) than the other two arms as a non-sedating antihistamine
Figure 2 Sleepiness with drug as assessed by VAS.

13.  Excellent tolerability profile.
 Faster onset, and longer duration of action.
 Non-sedative nature
 Improves quality of life
BILASTINE WHEN COMPARED TO FEXOFENADINE AND LEVOCETIRIZINE