Pharmacokinetics and pharmacodynamics of ximelagatran.

Oral anticoagulant therapy with vitamin K antagonists (VKAs) such as warfarin has proven benefits in the treatment and prevention of thromboembolic disorders but has important limitations that result in substantial underuse. In particular, the VKAs have variable and unpredictable pharmacokinetics and pharmacodynamics and a narrow separation between antithrombotic and hemorrhagic effects that necessitates careful dose adjustment based on frequent coagulation monitoring. In contrast, the oral direct thrombin inhibitor ximelagatran has a predictable and reproducible pharmacokinetic/pharmacodynamic profile that allows treatment using fixed-dose regimens without coagulation monitoring. The bioavailability of melagatran, the active form of ximelagatran, after oral administration of ximelagatran is approximately 20% with low inter- and intra-individual variability. Peak plasma melagatran concentrations are reached approximately 2 hours after oral dosing of ximelagatran to healthy volunteers, and melagatran is eliminated with a half-life of approximately 3 hours with clearance predominantly by renal excretion. Hence, a higher melagatran exposure is seen in patients with renal failure; ximelagatran is currently not recommended for patients with severe renal impairment (creatinine clearance of <30 mL/min) as these patients were not included in the clinical trial program. Exposure to melagatran increases linearly with the ximelagatran dose. The pharmacokinetic/pharmacodynamic profile is consistent across a broad range of different patient populations and is unaffected by gender, age, body weight, ethnic origin, obesity, and mild-to-moderate hepatic impairment. Any differences in melagatran pharmacokinetics associated with these factors are attributable to differences in renal function.

Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.

Pharmacokinetics and pharmacodynamics of ximelagatran.

Узнайте, как это исследование связано с клинической практикой

More peer-reviewed studies in Клинические исследования.

• Leech Therapy for Knee Osteoarthritis — The Landmark RCT — Michalsen et al. (2003)
• Leech-Assisted Flap Salvage — Systematic Review of 277 Cases — Whitaker et al. (2012)
• Effects of hirudotherapy on liver functions, lipid profile, and insulin sensitivity in rats with metabolic syndrome — Bilden A et al. (2026)
• Efficacy and Safety of Hirudotherapy for Improving Sperm Quality Parameters in Male Infertility: A Randomized Controlled Trial — Abtahi-Forooshani M et al. (2026)
• Reverse Sural Flap Venous Congestion Successfully Managed With Enoxaparin in a Male Patient With a Traumatic Foot Crush Injury: A Case Report — Velasco-Bustamante J et al. (2026)
• Investigation of the therapeutic effects of medicinal leech treatment on lower extremity ischemia-reperfusion injury — Ünal K et al. (2026)
• Efficacy of Medicinal Leech Therapy in Diverse Clinical Applications: A Comprehensive Study from Azerbaijan — Farzali S et al. (2025)
• HIRUDOTHERAPY IN RECONSTRUCTIVE SURGERY: CASE-REPORTS AND REVIEW — Heinz P et al. (2020)
• Hirudotherapy Efficacy and Complications in the Management of Microsurgical Breast Reconstruction: A Systematic Review — Foppiani J et al. (2024)
• Hirudotherapy in Wound Healing — Nair H et al. (2022)

Browse all ASH-analysed research →