STUDY DESIGN: Plasma samples from eight pregnant patients treated with intravenous atosiban (300 μg/min for 6 to 12 hours) were analyzed for atosiban concentration by a specific radioimmunoassay procedure. Contraction rate data were obtained by external tocodynamometry for 1 hour before the infusing and during the subsequent infusion.
RESULTS: The average steady-state plasma concentrations of patients receiving intravenous atosiban were 442 ± 73 ng/ml (mean ± SD), with steady state achieved by 1 hour after the start of the infusion. After the completion of the infusion, plasma concentrations declined rapidly in a biexponential manner with initial and terminal half-life estimates of 13 ± 3 and 102 ± 18 minutes, respectively. The effective half-life was 18 ± 3 minutes. The plasma clearance of atosiban was relatively high (42 L/hr) and the volume of distribution (approximately 18 L) was consistent with distribution into extracellular fluid. Of the seven patients evaluated for uterine activity, the mean contraction rate decreased by 75 % during the third hour of treatment and remained low until treatment termination.
CONCLUSION: On the basis of earlier published reports, the pharmacokinetics of atosiban in pregnant patients are similar to those in nonpregnant women. Although the patient population was small, a consistent reduction in uterine activity was observed during atosiban infusion.