Effects of Bilastine on T-wave Morphology and the QTc Interval

  title={Effects of Bilastine on T-wave Morphology and the QTc Interval},
  author={Claus Graff and Johannes Jan Struijk and J{\o}rgen K. Kanters and Mads P. Andersen and Egon Toft and Beno{\^i}t Tyl},
  journal={Clinical Drug Investigation},
AbstractBackground and Objectives: The International Conference of Harmonisation (ICH) E14 guideline for thorough QT studies requires assessing the propensity of new non-antiarrhythmic drugs to affect cardiac repolarization. The present study investigates whether a composite ECG measure of T-wave morphology (Morphology Combination Score [MCS]) can be used together with the heart rate corrected QT interval (QTc) in a fully ICH E14-compliant thorough QT study to exclude clinically relevant… 

Pro-Arrhythmic Potential of Oral Antihistamines (H1): Combining Adverse Event Reports with Drug Utilization Data across Europe

Some second-generation antihistamines are associated with signal of torsadogenicity and largely used in most European countries, and regulators and clinicians should consider risk-minimisation activities.

Electrocardiographic T-wave morphology and risk of mortality.

Safety profile of bilastine: 2nd generation H1-antihistamines.

  • F. Scaglione
  • Medicine, Biology
    European review for medical and pharmacological sciences
  • 2012
Bilastine is a new H1 antagonist with no sedative side effects, no cardiotoxic effects, and no hepatic metabolism, and it meets the current criteria for medication used in the treatment of allergic rhinitis and urticaria.

Bilastine: a new H1‐antihistamine with an optimal profile for updosing in urticaria

  • M. ChurchL. Labeaga
  • Medicine, Biology
    Journal of the European Academy of Dermatology and Venereology : JEADV
  • 2017
The excellent profile of bilastine in both efficacy and safety make it the ideal H1‐antihistamine for updosing the daily dose fourfold in difficult‐to‐treat urticaria as recommended by the EAACI/GA2LEN/EDF/WAO guideline for the management of urticeria.

Bilastine: new insight into antihistamine treatment

Results show that bilastine meets current EAACI/ARIA criteria for medications used in the treatment of AR and chronic urticaria, and the review of the literature indicates that once-daily treatment with bilastines 20 mg was effective in managing symptoms and improving patient’s quality of life.

Evaluation of the Single-dose Pharmacokinetics of Bilastine in Subjects with Various Degrees of Renal Insufficiency

Although exposure to bilastine was higher in renally impaired subjects, it remained well within the safety margins, thus allowing the conclusion that a 20-mg daily dose can be safely administered to subjects with different degrees of renal insufficiency without the need for dose adjustments.

Cardiac safety of second‐generation H1‐antihistamines when updosed in chronic spontaneous urticaria

All H1 antihistamines have an excellent safety profile with no evidence of cardiotoxicity even when updosed up to four times their standard licensed dose, provided that the prescribers carefully consider and rule out potential risk factors for cardiot toxicity.

The Impact of Bilastine on Symptoms of Allergic Rhinitis and Chronic Urticaria: A Systematic Review and Meta-Analysis of Randomized Controlled Trials

The meta-analysis revealed that bilastine was superior to placebo, improving TSS, TNSS, VAS, and QOL in AR or chronic urticaria participants and was comparable to active antihistamines such as cetirizine, fexofenadine, and loratadine regarding outcomes.

Bilastine: a lifetime companion for the treatment of allergies

Bilastine is a suitable option for the treatment of patients with allergic rhinoconjunctivitis or urticaria across age groups from school-age children to elderly patients, and has been shown to improve health-related quality of life.



Lack of Significant Effect of Bilastine Administered at Therapeutic and Supratherapeutic Doses and Concomitantly With Ketoconazole on Ventricular Repolarization: Results of a Thorough QT Study (TQTS) With QT‐Concentration Analysis

Moxifloxacin was associated with a significant increase in QTcNi at all time points between 1 and 12 hours, inclusively, and this result was most likely related to the cardiac effect of ketoconazole.

Improving the detection of subtle I(Kr)-inhibition: assessing electrocardiographic abnormalities of repolarization induced by moxifloxacin.

New parameters reflecting the morphology of the T-wave outperformed QTc measurements when identifying moxifloxacin-induced blockade of the outward rapid components of the delayed rectifier repolarizing potassium current (I(Kr).

Covariate Analysis of QTc and T‐Wave Morphology: New Possibilities in the Evaluation of Drugs That Affect Cardiac Repolarization

New insights are offered into the repolarization behavior of a drug associated with low cardiac risk vs. one associated with a high risk and the added benefits of a T‐wave MCS are described as a covariate to the assessment of the QTc interval.

Identifying Drug-Induced Repolarization Abnormalities from Distinct ECG Patterns in Congenital Long QT Syndrome

Distinct ECG patterns in LQT2 carriers effectively quantified repolarization changes induced by sotalol, and further studies are needed to validate whether this measure has general validity for the identification of drug-induced disturbed repolarizations.

Quantitative Analysis of T‐wave Morphology Increases Confidence in Drug‐Induced Cardiac Repolarization Abnormalities: Evidence From the Investigational IKr Inhibitor Lu 35–138

As a covariate to the assessment of QT interval liability, MCS offered important additive information to the effect of Lu 35–138 on cardiac repolarization.

Co-administration of ketoconazole with H1-antagonists ebastine and loratadine in healthy subjects: pharmacokinetic and pharmacodynamic effects.

Ketoconazole altered the pharmacokinetic profiles of both ebastine and loratadine although the effect was greater for the former drug, and changes in uncorrected QT intervals for both antihistamines were not statistically different from those observed with ketoconazoles alone.

Performance Characteristics for Some Typical QT Study Designs Under the ICH E‐14 Guidance

This report assesses the IUT false positive rate for 4 recently conducted TQT trials using simple simulation experiments and reveals significant limitations of the I UT with respect to excluding an effect and study interpretation for certain trial designs.