Transfer of naltrexone and its metabolite 6,beta-naltrexol into human milk

Carol F Chan1, Madhu Page-Sharp, Judith H Kristensen

  • 1Pharmacology Unit, School of Medicine and Pharmacology, University of Western Australia, Crawley, Western Australia.

The excretion of naltrexone and its primary metabolite 6,beta-naltrexol in breast milk from a 30-year-old lactating opiate addict undergoing oral naltrexone pharmacotherapy (5 mg/d) was studied. Concentrations of naltrexone and 6,beta-naltrexol in serial milk and plasma samples taken over a 19.3-hour period of a dose interval at steady state were measured by gas chromatography. The calculated infant dose relative to the maternal weight was 0.03% for naltrexone and 0.83% (as naltrexone equivalents) for 6,beta-naltrexol. Total relative infant dose estimated for the complete 24-hour dose interval was 1.06%. Her 6-week-old breastfed infant was healthy, achieving expected milestones, and showed no adverse effects. Only 6,beta-naltrexol was detected in infant plasma and at a very low concentration of 1.1 micro g/L. Use of naltrexone during breastfeeding should be undertaken only after an individual risk benefit analysis.

Related Concept Videos

Drug Excretion: Miscellaneous Routes01:10

Drug Excretion: Miscellaneous Routes

Drug excretion involves various organs, including the liver, intestines, skin, and eyes. In the case of drugs or toxins, they can be actively secreted into bile by transporters in the hepatocyte's canalicular membrane. These substances enter the GI tract during digestion and may be reabsorbed into the body from the intestine. This process, known as enterohepatic recycling, can significantly prolong the presence and effects of a substance in the body. To interrupt this cycle, specific substances...
Drug Elimination: Non-Renal Routes01:23

Drug Elimination: Non-Renal Routes

The liver plays a pivotal role in eliminating drugs and their metabolites, primarily through a process known as biliary excretion. This process involves the hepatocytes, the primary cells in the liver that generate bile. A range of transporters actively expels polar drugs or hydrophilic drug metabolites into the bile, which transports the drugs and metabolites into the small intestine. From here, they are eventually expelled from the body through feces. In some instances, the original drug or a...
Drug Excretion: Pulmonary and Glandular Routes01:22

Drug Excretion: Pulmonary and Glandular Routes

Gaseous substances like general anesthetics are absorbed and excreted through the lungs via simple diffusion. This process depends on factors such as pulmonary blood flow, respiration rate, and the substance's solubility. Gaseous anesthetics like nitrous oxide with low blood solubility are excreted rapidly, while compounds like alcohol, with high blood and tissue solubility, are excreted slowly.
Drugs can also be excreted in breast milk, which is crucial for breastfeeding infants. The process...
Transcytosis of IgG01:15

Transcytosis of IgG

Transcytosis is the process in which molecules are internalized by endocytosis, transported across the cell, and released through exocytosis from the opposite end of the cell. Molecules such as insulin, immunoglobulins, and certain nutrients are transferred through the recycling endosomes by recycling and transcytosis.
IgG molecules from a mother undergo transcytosis starting around 13 weeks of gestation. The amount of IgG transferred and entering the fetal blood circulation increases with...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
Drug Biotransformation: Overview01:28

Drug Biotransformation: Overview

Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...