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Related Experiment Videos

Variability in heparin effect on serum drug binding

C A Naranjo, E M Sellers, V Khouw

    Clinical Pharmacology and Therapeutics
    |October 1, 1980
    PubMed
    Summary

    Heparin significantly alters the binding of diazepam and warfarin in the blood, affecting their free fractions. These changes are linked to free fatty acid levels and vary based on heparin type and whether the patient has eaten.

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    Area of Science:

    • Pharmacology
    • Biochemistry
    • Clinical Medicine

    Background:

    • Drug binding to serum proteins influences therapeutic efficacy and toxicity.
    • Heparin, commonly used therapeutically, is known to affect lipid metabolism.
    • The impact of heparin on the protein binding of other drugs is not fully characterized.

    Purpose of the Study:

    • To investigate the effect of intravenous heparin administration on the free fractions of diazepam and warfarin in human serum.
    • To determine the relationship between heparin-induced changes in free fatty acids and drug binding.
    • To compare the effects of different heparin lots on drug binding.

    Main Methods:

    • Eight healthy adults received intravenous heparin (50 U).
    • Serum free fractions of diazepam and warfarin were measured using equilibrium dialysis with radiolabeled drugs.

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  • Free fatty acids (FFA) were quantified.
  • Drug binding was assessed in fasted and postprandial states, and with different heparin preparations.

    • Main Results:

    • Heparin administration rapidly increased diazepam free fraction and decreased warfarin free fraction, correlating with increased FFAs.
    • These effects were more pronounced postprandially.
    • Heparin from lot Harris LO14 demonstrated greater lipolytic activity and more significant alterations in drug binding compared to Organon LA39.

    Conclusions:

    • Heparin administration significantly alters the protein binding of diazepam and warfarin.
    • The extent of these changes is influenced by heparin's lipolytic activity, postprandial status, and specific heparin lot.
    • Even low doses of heparin, as used in heparin locks, can impact drug binding, necessitating consideration of these variables.