Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine 10, 20 and 40 mg in Healthy Japanese Subjects: A Randomised Placebo-Controlled Trial

Autor: Georg Ferber, Ulrike Lorch, Sara Fernandes, Jorg Taubel, Eva Santamaria, Iñaki Izquierdo
Jazyk: angličtina
Rok vydání: 2016
Předmět:
0301 basic medicine
Male
Rupatadine
Placebo-controlled study
lcsh:Medicine
Biochemistry
Placebos
Electrocardiography
0302 clinical medicine
Cognition
Drug Metabolism
Japan
Medicine and Health Sciences
Metabolites
Medicine
lcsh:Science
Cognitive Impairment
Multidisciplinary
Cognitive Neurology
Pharmaceutics
Healthy Volunteers
Bioassays and Physiological Analysis
Tolerability
Neurology
Research Design
Anesthesia
Area Under Curve
Female
medicine.drug
Research Article
Adult
Drug Administration
Clinical Research Design
Cognitive Neuroscience
Cmax
Cyproheptadine
Histamine Antagonists
Placebo
Research and Analysis Methods
03 medical and health sciences
Pharmacokinetics
Drug Therapy
Double-Blind Method
Reaction Time
Humans
Platelet Activating Factor
Adverse effect
Pharmacology
Dose-Response Relationship
Drug
business.industry
Electrophysiological Techniques
lcsh:R
Biology and Life Sciences
030104 developmental biology
Metabolism
030228 respiratory system
Pharmacodynamics
Cognitive Science
lcsh:Q
Adverse Events
Cardiac Electrophysiology
business
Neuroscience
Zdroj: PLoS ONE, Vol 11, Iss 9, p e0163020 (2016)
PLoS ONE
ISSN: 1932-6203
Popis: Introduction Rupatadine is a marketed second generation antihistamine, with anti-PAF activity, indicated for symptomatic treatment of allergic rhinitis and urticaria. This study was conducted to evaluate the pharmacokinetics (PK), pharmacodynamics (PD), safety and tolerability of rupatadine in healthy Japanese subjects after single and multiple oral doses. Methods In this randomised, double-blind, placebo-controlled study, 27 male and female healthy Japanese subjects were administered single and multiple escalating rupatadine dose of 10, 20 and 40 mg or placebo. Blood samples were collected at different time points for PK measurements and subjects were assessed for safety and tolerability. The effect of rupatadine on cognitive functioning was evaluated by means of computerized cognitive tests: rapid visual information processing (RVP), reaction time (RT), spatial working memory (SWM) and visual analogue scales (VAS). Results Exposure to rupatadine as measured by Cmax and AUC was found to increase in a dose dependent manner over the dose range of 10–40 mg for both single and multiple dose administration. The safety assessments showed that all treatment related side effects were of mild intensity and there were no serious adverse events (SAEs) or withdrawals due to treatment–emergent adverse events (TEAEs) in this study. The therapeutic dose of rupatadine did not show any CNS impairment in any of the cognitive tests. Conclusions This study demonstrated that rupatadine is safe and well tolerated by Japanese healthy subjects. The PK-PD profile confirmed previous experience with rupatadine.
Databáze: OpenAIRE
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