Pharmacokinetic characteristics of a vasodilatory and antiplatelet agent, limaprost alfadex, in the healthy Korean volunteers.

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Citation

Park YS, Park JH, Kim SH, Lee MH, Lee YS, Yang SC, Kang JS

Pharmacokinetic characteristics of a vasodilatory and antiplatelet agent, limaprost alfadex, in the healthy Korean volunteers.

Clin Appl Thromb Hemost. 2010 Jun;16(3):326-33. doi: 10.1177/1076029609334125. Epub 2009 Oct 13.

PubMed ID
19825922 [ View in PubMed
]
Abstract

Limaprost, a prostaglandin E1 analogue, with a strong vasodilatory and antiplatelet activity has been used to release from the symptoms of thromboangiitis obliterans (TAO), which is more prevalent in Korea and Japan, and lumbar spinal canal stenosis (LSCS). In spite of many uses of limaprost, the pharmacokinetics (PK) of it has not been studied in the Korean population. Therefore, a preliminary PK study was designed at a clinical oral dosage of 30-microg limaprost in 5 healthy Korean volunteers. Blood samples were obtained at 14 consecutive time points for 12 hours after dosing and analyzed by liquid chromatography-tandem mass spectrometry with electrospray ionization (LC-ESI/MS/ MS) at a very low detection limit of 0.5 pg/mL of limaprost in human plasma with considerably short run time (18 minutes). Pharmacokinetic characteristics resulted in ''time for maximal concentrations (T(max) 0.5 hour),'' ''elimination half-life (T(1/2) 1.64 hours),'' ''maximal concentration (C(max) 13.37 pg/mL),'' ''area under the curve (AUC(12 hours) 18.60 pg . h/mL),'' ''AUC extrapolated to infinity (AUC(infinity) 22.98 pg . h/mL),'' ''extrapolation (AUC(infinity - 12 hours)/AUC(infinity) 0.15%),'' ''elimination rate constant (k(e) 0.68 h(-1)),'' ''systemic clearance (CL 1.77 L/h),'' and ''mean residence time (MRT 1.74 hours).'' These results showed that orally administered 30-microg limaprost was rapidly and highly absorbed, and it was considerably eliminated fast from the blood stream in the healthy Korean volunteers.

DrugBank Data that Cites this Article

Drugs
Drug Interactions
DrugsInteraction
Acetylsalicylic acid
Limaprost
Limaprost may increase the antiplatelet activities of Acetylsalicylic acid.
Anagrelide
Limaprost
Limaprost may increase the antiplatelet activities of Anagrelide.
Caplacizumab
Limaprost
Limaprost may increase the antiplatelet activities of Caplacizumab.
Cilostazol
Limaprost
Limaprost may increase the antiplatelet activities of Cilostazol.
Clopidogrel
Limaprost
Limaprost may increase the antiplatelet activities of Clopidogrel.