Indication of Bilastine in Specific Patient Groups − Practical Tips for Clinical Practice

Mechanism of action

Bilastine is a second-generation antihistamine. It acts as a non-sedating antagonist of histamine receptors with a long-lasting effect. The advantages of its mechanism of action include:

• Selective antagonist affinity for peripheral H₁ receptors (its affinity is 3 times higher than cetirizine and 6 times higher than fexofenadine).
• Absence of affinity for muscarinic receptors.
• Anti-inflammatory effect (prevents the release of histamine, interleukin 4, and tumor necrosis factor-alpha from mast cells and granulocytes).

Use of bilastine in specific groups 

Older patients

The pharmacokinetic profile of bilastine in healthy individuals over 65 years of age is comparable to younger individuals; dosage adjustment is not necessary. A study involving 146 polymedicated elderly individuals with allergic disease and a range of other comorbidities was also conducted. Participants were administered bilastine at a dose of 20 mg. The incidence of adverse events was comparable to younger healthier individuals, indicating a favorable safety profile of bilastine even in higher age categories.

Individuals employed in professions with a special focus on cognitive performance

The impact of bilastine on psychomotor functions is significantly less compared to sedating antihistamines, partly due to its limited penetration across the blood-brain barrier. In PET/CT imaging-based tests, bilastine showed significantly less occupancy of brain H₁ receptors compared to other second-generation antihistamines. Due to the almost negligible occupancy of these receptors, bilastine is assessed as a non-brain-penetrating antihistamine. 

In tests under normal ground conditions and in simulated altitude and pressure conditions in a pilot cabin, no adverse effects of bilastine on cognitive performance (alertness, ultra-short memory, attention, monotony tolerance) were observed in the available studies. Evaluation of the impact of bilastine on driving skills conducted on a Formula 1 simulator also showed no negative effects on driving performance at high speed. Available data suggest that bilastine at doses up to 40 mg per day does not affect psychomotor performance.

Patients on dialysis and post-kidney transplantation

There is currently insufficient data on the impact of hemodialysis on the clearance of bilastine. However, its physicochemical properties are comparable to the antihistamine fexofenadine, where conventional hemodialysis has no significant impact on its plasma clearance. Similar properties can thus be assumed for bilastine.

Studies further suggest that bilastine is able to alleviate uremic pruritus.

In the case of post-kidney transplantation patients who are medicated with cyclosporine or other immunosuppressive therapy, the use of bilastine is possible only in persons with normal or mild renal impairment and under careful observation. In patients with moderate or severe renal impairment taking P-glycoprotein inhibitors (e.g., cyclosporine), bilastine should not be administered at all due to the risk of increased plasma levels.

Urinary retention/dysuria

Bilastine exhibits a high selectivity for H₁ receptors and has no affinity for muscarinic receptors. Due to these properties, it does not increase the risk of urinary retention or dysuria.

Obesity

The pharmacological profile of bilastine is not affected by body weight. Available data does not indicate that the efficacy and safety of bilastine are different in obese individuals from those with normal body weight. The use of bilastine does not cause weight gain as an adverse effect of therapy.

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Sources:
1. Leceta A., García A., Sologuren A., Campo C. Bilastine 10 and 20 mg in pediatric and adult patients: an updated practical approach to treatment decisions. Drugs Context 2021 Aug 10; 10: 2021-5-1, doi: 10.7573/dic.2021-5-1.
2. SPC Xados. Available at: www.sukl.cz/modules/medication/detail.php?code=0148672&tab=texts
3. Treatment of pruritus. Pharmacotherapeutic Information 2019; 5: 1−3. Available at: www.sukl.cz/file/90396_1_1
4. Sologuren A., Viñas R., Cordón E. et al. Open-label safety assessment of bilastine in elderly patients with allergic rhinoconjunctivitis and/or urticaria. Allergy Asthma Proc 2018; 39 (4): 299−304, doi: 10.2500/aap.2018.39.4136.
5. Reményi Á., Grósz A., Szabó S. A. et al. Comparative study of the effect of bilastine and cetirizine on cognitive functions at ground level and at an altitude of 4,000 m simulated in hypobaric chamber: a randomized, double-blind, placebo-controlled, cross-over study. Expert Opin Drug Saf 2018; 17 (9): 859−868, doi: 10.1080/14740338.2018.1502268.
6. Demonte A., Guanti M. B., Liberati S. et al. Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients. Eur Rev Med Pharmacol Sci 2018; 22 (3): 820−828, doi: 10.26355/eurrev_201802_14318.