The Excretion of Drugs in Milk: A Survey

Lien, Eric J.

doi:10.1111/j.1365-2710.1979.tb00148.x

Cited by 2 publications

(2 citation statements)

References 50 publications

(13 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Principles and pharmacokinetics for drug excretion into milk have been suggested and discussed by a number of investigators (2, [5][6][7][8][9][10][11][12][13]. The drug can enter milk directly T h e first of these mechanisms, passive diffusion of unionized drug through the membranes appears to explain most of the available data (9).…”

Section: T H E O R E T I C a L C O N S I D E R A T I O Nmentioning

confidence: 99%

Qsar Analysis of Drug Excretion Into Human Breast Milk

Meskin¹,

Lien²

1985

J Clin Pharm Ther

View full text Add to dashboard Cite

Breast feeding has increased by approximately 2500 in the United States during the past decade and this trend appears to be continuing. The number of drugs available to lactating women is also growing at a rapid pace. The excretion of drugs into breast-milk presents a potential danger to infants. In spite of this, little is known about the excretion of drugs into breast-milk. T h e ability to predict which drugs are potential hazards would be very useful in the clinical setting.This study quantitatively correlates the human milk to plasma concentration ratio of various basic and acidic drugs (log M / P ) with the square root of the molecular weight, the partition coefficient (log P) and the degree of dissociation (log U/D).For basic drugs there is a negative-dependence on both log P and log U/D. High lipophilicity favours protein binding and reduces the amount of drug available for diffusion into milk. Therefore, as log P increases, the log M / P decreases. The negative-dependence on log U/D indicates that the higher the degree of dissociation of the base in plasma, the greater the log M / P will be. This fits well with the concept of ion-trapping. A strong base is more likely to be transferred and then trapped in milk which has a lower pH than plasma.For acidic drugs there is a negative-dependence on both ,/(MW) and log P. T h e negative-dependence on ,/(MW) suggests that large molecules are less likely to be able to diffuse into the milk. A negative-dependence on log P appears to hold true for bases and acids. Log M / P decreases as log P increases. This is probably due to increased protein binding by lipophilic drugs through non-specific hydrophobic interaction with plasma protein.

show abstract

Section: T H E O R E T I C a L C O N S I D E R A T I O Nmentioning

confidence: 99%

Qsar Analysis of Drug Excretion Into Human Breast Milk

Meskin¹,

Lien²

1985

J Clin Pharm Ther

View full text Add to dashboard Cite

show abstract

“…Hansch and coworkers (4)(5)(6)(7)(8)(9) successfully used the linear free energy approach to establish quantitative structure-activity relationships for many biological systems. Lien and coworkers (10)(11)(12)(13)(14)(15)(16)(17)(18) studied the quantitative structure-activity relationships of various derivatives of drugs having a high correlation of biological activity with lipophilicity. The linear free energy relationship approach still has limitations due to the nonadditivity of the partition coefficients of some organic compounds (19,20).…”

Section: Introductionmentioning

confidence: 99%

Effects of different buffer species on partition coefficients of drugs used in quantitative structure–activity relationships

Pou-Hsiung

Lien

1980

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

The Excretion of Drugs in Milk: A Survey

Cited by 2 publications

References 50 publications

Qsar Analysis of Drug Excretion Into Human Breast Milk

Qsar Analysis of Drug Excretion Into Human Breast Milk

Effects of different buffer species on partition coefficients of drugs used in quantitative structure–activity relationships

Contact Info

Product

Resources

About