Oxprenolol placental transfer, plasma concentrations in newborns and passage into breast milk.

Sioufi, A.; Hillion, D; Lumbroso, P; Wainer, R.; Olivier-Martin, M; Schoeller, JP; Colussi, D.; Leroux, F; Mangoni, Patrick

doi:10.1111/j.1365-2125.1984.tb02489.x

Cited by 22 publications

(8 citation statements)

References 9 publications

(11 reference statements)

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“…This is the case with betaxolol, in which the urinary elimination is not the main elimination way , Under these conditions, short half-life (in the adult) is not necessarily a strong argument for choosing a beta-blocking drug during pregnancy, all the more so when the betablocker is metabolized actively with plasma concentrations higher than those of the parent drug, and eliminated more slowly than it (table II). et al [1984] Even with the absence of precise pharmacokinetic data, we know that these type of drugs are often found well after birth, sometimes 2 or 3 days later, in concentrations considered as beta-blocking [Sandström et al, 1982;Boutroy et al, 1982;Sioufi et al, 1984], exposing the child, there fore, to longer drug risks than we had supposed.…”

Section: Placental Transfer Of Beta-blocking Drugsmentioning

confidence: 99%

Fetal and Neonatal Effects of the Beta-Adrenoceptor Blocking Agents

Mj¹

1987

Dev Pharmacol Ther

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The placental transfer of beta-adrenoceptor blocking agents has been well established in the last years. Randomized and/or controlled studies have given a less pessimistic view of the consequences of these drugs on the fetal and neonatal adaptation. In fact, the beta-blockers are able to produce hypotension, bradycardia, respiratory troubles in the newborn infant, troubles which are generally slight when the neonates are full-term. However, even if in good clinical conditions, this kind of neonate should be carefully monitored for at least the first 2 days of life.

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Section: Placental Transfer Of Beta-blocking Drugsmentioning

confidence: 99%

Fetal and Neonatal Effects of the Beta-Adrenoceptor Blocking Agents

Mj¹

1987

Dev Pharmacol Ther

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“…Comparison with data for other [3-blockers indicates a higher milk/blood ratios (2.5-10) for acebutolol and a similar value (1.6-4.5) for atenolol, metoprolol, oxprenoloi and propranolol (Boutroy et al 1986;Kulas et al 1984;Liedholm et al 1981;Lundborg et al 1981;SandstrOm and Regardh 1980;Sioufi et al 1984;Thorley et al 1983;White et al 1984).…”

Section: Discussionmentioning

confidence: 53%

Placental transfer and perinatal pharmacokinetics of betaxolol

Morselli¹,

Boutroy

Bianchetti³

et al. 1990

Eur J Clin Pharmacol

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Betaxolol levels in blood were monitored in the perinatal period in 28 pregnant hypertensive women and in their babies. In the mothers betaxolol concentrations at delivery ranged from less than 1 to 115 ng.ml-1 after doses of 10 to 40 mg.day-1. The apparent blood half-life was 15.6 to 22.1 h mean (19 h). Umbilical cord levels indicated a rapid equilibrium between fetal and maternal units (ratio 0.93) within few hours after dosing. Milk betaxolol concentrations, measured in few cases, exceeded those in blood by a factor of 3. Amniotic fluid concentrations were similar to those observed in maternal venous blood and umbilical cord blood. In neonates, the blood betaxolol half-life ranged from 14.8 to 38.5 h, with a definite trend towards a negative correlation with gestational age. A 11-61% rise in the betaxolol concentration was observed in 64% of the neonates during the first 12 h of extrauterine life. The data indicate that betaxolol kinetics is not altered in pregnant women and they stress the need for careful and prolonged (72-96 h) intensive monitoring of neonates born to hypertensive mothers treated with beta-blocking agents.

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“…[10][11][12][13][14][15][16][17][18][19][20][21][22][23][24][25] Although the F/M ratio of many compounds was directly cited from literature sources such as clinical studies, the ratio for some compounds (carnitine, chlordane, chlorpyrifos, dichlorodiphenyldichloroethylene (DDE), diazinon, dicloran, hexachlorobenzene (HCB) heptachlor epoxide, nonachlor, oxychlordane, and phthalimide) was calculated based on the concentration in umbilical cord and maternal blood.…”

Section: Data Setsmentioning

confidence: 99%

Quantitative Structure–Activity Relationship Model for the Fetal–Maternal Blood Concentration Ratio of Chemicals in Humans

Takaku

Nagahori

Sogame

et al. 2015

Biological & Pharmaceutical Bulletin

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A quantitative structure-activity relationship (QSAR) model of the fetal-maternal blood concentration ratio (F/M ratio) of chemicals was developed to predict the placental transfer in humans. Data on F/M ratio of 55 compounds found in the literature were separated into training (75%, 41 compounds) and testing sets (25%, 14 compounds). The training sets were then subjected to multiple linear regression analysis using the descriptors of molecular weight (MW), topological polar surface area (TopoPSA), and maximum E-state of hydrogen atom (Hmax). Multiple linear regression analysis and a cross-validation showed a relatively high adjusted coefficient of determination (R a 2 ) (0.73) and cross-validated coefficient of determination (Q 2 ) (0.71), after removing three outliers. In the external validation, R 2 for external validation (R 2 pred ) was calculated to be 0.51. These results suggested that the QSAR model developed in this study can be considered reliable in terms of its robustness and predictive performance. Since it is difficult to examine the F/M ratio in humans experimentally, this QSAR model for prediction of the placental transfer of chemicals in humans could be useful in risk assessment of chemicals in humans.Key words placental transfer; human; quantitative structure-activity relationship; fetal-maternal blood concentration ratioThe placental transfer of chemicals is crucial for toxicity assessment of fetus, because chemicals that do not penetrate the placenta are considered safe for fetus.1) Therefore, investigations of many drugs that are transferred from mother to fetus through the placenta have been performed.Since it is difficult to measure the placental transfer of chemicals in humans ethically, in vitro and ex vivo methods have been developed and used for the evaluation of human placental transfer.2) In in vitro methods, cell lines from human placenta, such as BeWo, JAr, and JEG cells, have been commonly used as models of the placental barrier.3) In ex vivo methods, the human placenta is perfused to investigate the transfer of chemicals from maternal to fetal compartment. Although this system has been validated in many studies, and therefore this system is considered reliable, there are difficulties in conducting this evaluation method. 2,4)Quantitative structure-activity relationship (QSAR) models are useful tools for predicting the biological activity of chemicals. Descriptors of chemicals such as molecular weight and log P, are needed to develop QSAR prediction, and those are determined by experiments, calculation, or predicted using software. In the field of pharmacokinetics, QSAR models have been developed and reported in areas such as oral bioavailability, Caco-2 permeability, and metabolism. 5-7)QSAR models for predicting the placental transfer of chemicals using ex vivo data have already been reported. 8,9) However, to our knowledge, this is the first report that indicates prediction of the fetal-maternal blood concentration ratio (F/M ratio) of chemicals using in vivo data. To predict t...

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Oxprenolol placental transfer, plasma concentrations in newborns and passage into breast milk.

Cited by 22 publications

References 9 publications

Fetal and Neonatal Effects of the Beta-Adrenoceptor Blocking Agents

Fetal and Neonatal Effects of the Beta-Adrenoceptor Blocking Agents

Placental transfer and perinatal pharmacokinetics of betaxolol

Quantitative Structure–Activity Relationship Model for the Fetal–Maternal Blood Concentration Ratio of Chemicals in Humans

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