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Pharmacokinetics of amlodipine besylate at delivery and during lactation.

ABSTRACT: BACKGROUND:Amlodipine is rarely used in the treatment of pregnant hypertensive women due to limited pharmacokinetic data during pregnancy and the postpartum period. OBJECTIVE:To evaluate the pharmacokinetics of amlodipine besylate in the peri-partum period including quantities of placental passage, breast milk excretion and infant exposure. STUDY DESIGN:This was a prospective study of pregnant women who were prescribed 5?mg of amlodipine daily for treatment of chronic hypertension and delivered at term. Cord and maternal blood samples were collected at delivery. On postpartum day 2, six paired maternal plasma and breast milk samples were obtained at 4, 6, 8, 12, 15 and 24?h following amlodipine dosing. Infant plasma samples were collected 24-48?h after delivery. All samples were analyzed for amlodipine concentration. A one compartment, first-order model was used to calculate pharmacokinetic estimates for maternal plasma. RESULTS:Of the 16 patients enrolled in the study, 11 had cord blood and maternal serum collected at delivery, of which only 6 produced sufficient breast milk for sampling. Amlodipine was detected in infant cord blood plasma with a mean concentration of 0.49?±?0.29?ng/mL compared to mean maternal serum level of 1.27?±?0.84?ng/mL. Amlodipine concentrations in both in breast milk and infant plasma were undetectable at the lower limit of assay detection (<0.1?ng/mL). In the immediate postpartum period, the amlodipine elimination half-life was 13.7?±?4.9?h, the area under the curve was 53.4?±?19.8?ng*h/mL and the peak concentration was 2.0?±?1.0?ng/mL. CONCLUSIONS:Amlodipine does cross the placenta in measurable quantities, but is not detected in breast milk or infant plasma at 24-48?h of life indicating that it is likely safe to use during the peripartum period.

SUBMITTER: Morgan JL

PROVIDER: S-EPMC5846630 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature

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Pharmacokinetics of amlodipine besylate at delivery and during lactation.

Morgan Jamie L JL Kogutt Benjamin K BK Meek Claudia C Stehel Elizabeth K EK McIntire Donald D DD Sheffield Jeanne S JS Roberts Scott W SW

Pregnancy hypertension 20180104

<h4>Background</h4>Amlodipine is rarely used in the treatment of pregnant hypertensive women due to limited pharmacokinetic data during pregnancy and the postpartum period.<h4>Objective</h4>To evaluate the pharmacokinetics of amlodipine besylate in the peri-partum period including quantities of placental passage, breast milk excretion and infant exposure.<h4>Study design</h4>This was a prospective study of pregnant women who were prescribed 5 mg of amlodipine daily for treatment of chronic hyper ...[more]

PMID: 29523279

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Project description:BackgroundA fixed-dose combination (FDC) of amlodipine and losartan has been used to reduce blood pressure in patients whose hypertension is not sufficiently controlled with either drug alone. The aim of this study was to evaluate the pharmacokinetic (PK) characteristics and tolerability of an FDC of 6.94 mg amlodipine besylate (5 mg as amlodipine)/50 mg losartan potassium compared to an FDC of 5 mg amlodipine camsylate/50 mg losartan potassium in healthy subjects.Subjects and methodsA randomized, open-label, single-dose, two-period, two-sequence crossover study was conducted on 46 healthy male subjects. Blood concentrations were measured by liquid chromatography-tandem mass spectrometry. Blood samples were collected up to 144 hours post dose for each period. PK parameters were calculated in each treatment group using a noncompartmental method. The 90% confidence intervals (CIs) of the geometric mean ratios of the two treatments for the maximum plasma concentration (Cmax) and the area under the concentration curve from time zero to the last quantifiable time point (AUC0-t) were estimated. Tolerability assessments were performed for all subjects who received the drug at least once.ResultsThe PK profiles of the two treatments were similar. For amlodipine, the geometric mean ratios (90% CIs) of amlodipine besylate to amlodipine camsylate for the Cmax and AUC0-t were 0.98 (0.94-1.01) and 0.97 (0.93-1.01), respectively. The corresponding values for losartan were 0.91 (0.81-1.02) and 1.05 (0.98-1.12), respectively. The incidence of adverse events was not significantly different between the two treatments, and both were well tolerated.ConclusionAn FDC of 6.94 mg amlodipine besylate (5 mg as amlodipine)/50 mg losartan potassium produced similar results to an FDC of 5 mg amlodipine camsylate/50 mg losartan potassium treatment with respect to the PK parameters of amlodipine and losartan based on Cmax and AUC0-t values. The amlodipine besylate/losartan potassium combination was well tolerated by healthy male subjects.

Dataset Information

Pharmacokinetics of amlodipine besylate at delivery and during lactation.

Publications

Pharmacokinetics of amlodipine besylate at delivery and during lactation.

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