Year-end Sale % OFF 
Abstract
Betahistine dihydrochloride is widely used to reduce the severity and frequency of vertigo attacks associated with Ménière’s disease. Betahistine is an analogue of histamine, and is a weak histamine H1 receptor agonist and potent histamine H3 receptor antagonist. The recommended therapeutic dose for adults ranges from 24 to 48 mg given in doses divided throughout the day. Betahistine undergoes extensive first-pass metabolism to the major inactive metabolite 2-pyridyl acetic acid (2PAA), which can be considered a surrogate index for quantitation of the parent drug due to extremely low plasma levels of betahistine. The aim of the present investigation was to assess the pharmacokinetics and dose proportionality of betahistine in Arabic healthy adult male subjects under fasting conditions. A single dose of betahistine in the form of a 8, 16, or 24 mg tablet was administered to 36 subjects in randomized, cross-over, three-period, three-sequence design separated by a one week washout period between dosing. The pharmacokinetic parameters Cmax, AUC0–t, AUC0–∞, Tmax, and Thalf were calculated for each subject from concentrations of 2-PAA in plasma, applying non-compartmental analysis. The current study demonstrated that betahistine showed linear pharmacokinetics (dose proportionality) in an Arabic population over the investigated therapeutic dose range of 8–24 mg.
Highlights
The clinical investigator and staff were available throughout the entire study period (24 h) to observe and monitor any adverse events (AE), adverse drug reactions (ADR), and serious adverse effects (SAE) if they occurred
The drug was well tolerated by all participants and they were discharged at the end of the study (3 weeks) without any significant changes in their clinical baseline characteristics
This review suggested that the obvious variability in the pharmacokinetics of the drug is related to genetic and environmental factors that can influence the metabolism of betahistine to its principle metabolite 2-pyridyl acetic acid [15]
Summary
Thirty-eight Arabic healthy adult male subjects with age ranging between 18 and 40 years and body mass index between 18 and 28 were selected to participate in this study. The subjects were considered healthy if they were in good physical and clinical condition, and had normal clinical laboratory tests. The clinical laboratory tests included biochemistry, hematology, and routine urine analysis. The subjects had to have negative results for illicit drugs, hepatitis (B & C) antigens, and human immunodeficiency virus (HIV). The subjects were considered not illegible for participation in the study if they were heavy smokers (more than 10 cigarettes per day), had a history of hypersensitivity and/or contraindications to betahistine or any related compounds, or had history of any chronic illness including gastrointestinal, hepatic, renal, cardiovascular, pulmonary, hematological, endocrinal, immunological, dermatological, neurological, or psychiatric diseases. Each subject was given a random identification number upon admission to the clinical site during Period 1 of the study. No subject was allowed to continue the study if there was a potential risk to his health or if there was any violation of the study protocol
Sign-in/Register to view highlights & summary 
Published Version (
Free)
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
