Pharmacokinetics and Food Interaction of Mk-462 in Healthy Males

Initial human experience with MK‐462 (rizatriptan): a novel 5=HTID agonist

“…O f note, the time-to-peak growth hormone concentration was somewhat delayed and the magnitude of the peak somewhat less in the present study than previously reported with subcutaneous sumatriptan [24]. These findings are consistent with the pharmacokinetic differences between oral and subcutaneous administration of sumatriptan, with the latter producing higher and more rapid peak concentrations [31].…”

“…The plasma concentrations observed following 20-40 mg MK-462 approximate the concentrations observed following 100 mg sumatriptan. Subsequent comparative investigation of MK-462 kinetics following intravenous and oral administration has determined oral bioavailability to be approximately 40% [31] and confirmed the suggestion from the present study of enhanced bioavailability relative to oral sumatriptan which displays an oral bioavailability of 14%.…”

Application of a Reliable LC-MS/MS Method for Determination of Rizatriptan in Healthy Subject Samples: Demonstration of Assay Reproducibility by Incurred Sample Reanalysis

“…As evident from these values, there was no significant effect of food on the pharmacokinetic parameters. In healthy volunteers, food increases the area under the curve (AUC) by about 20% and delays absorption of RIZ; however, there is no significant effect on C max and T max values [22]. In the present work the increase in AUC values was only about 5%, which can be attributed to genetic difference, race, age, gender (body size and muscle mass), type of food, and so forth.…”

Pharmacokinetics and tolerability of intravenous rizatriptan in healthy females

“…There were no other clinically significant findings. mg (10-60 mg kg − 1 ) in healthy male subjects [7]. Within this dose range, mean values of Cl, t 1/2 , MRT, and V ss were 1376 mL min − 1 , 1.8 h, 1.7 h, and 140 L, respectively [7].…”

“…mg (10-60 mg kg − 1 ) in healthy male subjects [7]. Within this dose range, mean values of Cl, t 1/2 , MRT, and V ss were 1376 mL min − 1 , 1.8 h, 1.7 h, and 140 L, respectively [7]. Therefore, after IV rizatriptan administration, Cl and V ss in females appeared to be somewhat less in females than in males, whereas t 1/2 and MRT were similar between men and women.…”