Ivabradine Peak Plasma Concentration
Ivabradine reaches peak plasma concentration approximately 1 hour after oral administration under fasting conditions. 1
Pharmacokinetic Profile
Peak concentration (Tmax) occurs at approximately 1 hour when taken on an empty stomach, though this timing is delayed by approximately 1 hour when ivabradine is taken with food. 1 The FDA label clearly states that food delays absorption by about 1 hour and increases plasma exposure by 20% to 40%, which is why ivabradine should always be taken with food in clinical practice. 1
Detailed Timing Across Studies
The peak plasma concentration timing is remarkably consistent across multiple populations and study designs:
In healthy Korean volunteers, the median Tmax was 0.67 hours (approximately 40 minutes) at steady state across all dose levels (2.5, and 10 mg). 2
In healthy Chinese men, no statistically significant differences in Tmax were found between different dose groups after single doses, and there was no significant change in Tmax when comparing single versus multiple doses. 3
The active metabolite S18982 follows a similar pattern, with peak concentrations occurring around the same timeframe as the parent compound. 4
Clinical Implications
The rapid absorption profile means that pharmacodynamic effects on heart rate begin within 2 hours of administration. 3, 2 After a single dose, significant heart rate reduction is observed at 2 hours post-dose, particularly at higher doses. 3 With repeated dosing, significant heart rate reduction occurs from 2 to 4 hours post-dose across all therapeutic dose ranges. 3
The effective half-life is approximately 6 hours, with a distribution half-life of 2 hours, meaning steady-state effects are achieved within 2 weeks of regular dosing and are maximal by 4 weeks. 1, 5