Advertisement

Archives of Toxicology

, Volume 49, Issue 3–4, pp 311–319 | Cite as

The pharmacokinetics of amygdalin

  • A. G. Rauws
  • M. Olling
  • A. Timmerman
Original Investigations

Abstract

Amygdalin (d-mandelonitrile-β-d-gentiobioside) is a cyanogenic glycoside claimed to show anti-cancer activity, sold under the incorrect name “Laetrile”. For a sensible discussion of its alleged activity and its established toxicity it is necessary that its fate in the organism is known. The pharmacokinetics of amygdalin have been investigated in the Beagle dog after both intravenous and oral administration. The excretion of amygdalin has also been studied in the rat. Amygdalin concentrations were determined by high performance liquid chromatography in plasma ultrafiltrate and urine. The pharmacokinetics of amygdalin after intravenous administration were compared with those of diatrizoate, a model substance for extracellular volume and glomerular filtration. The amygdalin clearance is significantly larger than that of diatrizoate. The volumes of distribution of both substance are the same. After oral administration only a few percents of the amygdalin dose are systemically available. A part of the oral dose is recovered from the urine as prunasin (d-mandelonitrile-β-d-glucoside).

Key words

Amygdalin Prunasin Diatrizoate Pharmacokinetics Intestinal absorption 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Ames MM, Kovach JS, Flora KP (1978) Initial pharmacologic studies of amygdalin (Laetrile) in man. Res Commun Chem Pathol Pharmacol 22: 175–185Google Scholar
  2. Berzelius JJ (1838) Lehrbuch der Chemie, Bd VII, 3. Aufl. Arnoldische Buchhandlung, Dresden Leipzig, S 512Google Scholar
  3. Blaufox MD, Sanderson DR, Tauxe WN, Wakim KG, Orvis AL, Owen CA (1963) Plasma diatrizoate-I131 disappearance and glomerular filtration in the dog. Am J Physiol 204: 536–540Google Scholar
  4. Bollerup AC, Hessen B, Steines E (1975) Renal handling of iodamide and diatrizoate. Eur J Clin Pharmacol 9: 63–67Google Scholar
  5. Carter JH, McLafferty MA, Goldman P (1980) Role of the gastrointestinal microflora in amygdalin (Laetrile) induced cyanide toxicity. Biochem Pharmacol 29: 301–304Google Scholar
  6. Conchie J (1958) β-Glucosidase from rumen liquor. Biochem J 58: 552–560Google Scholar
  7. Dahlqvist A (1961) Pig intestinal β-glueosidase activities I. Relation to β-galactosidase (lactase). Biochim Biophys Acta 50: 55–61Google Scholar
  8. Editorial (1977) Laetrile bibliography. Vet Hum Toxicol 21: 112–114Google Scholar
  9. Engelen AJM (1963) Niercontrastmiddelen. Farmacokinetiek en enkele klinische aspecten ervan. Dissertation NijmegenGoogle Scholar
  10. Fenselau C, Pallante S, Batzinger RP, Benson WB, Barron RP, Sheinin EB, Maienthal M (1977) Mandelonitrile-β-glucuronide: Synthesis and characterization. Science 198: 625–627Google Scholar
  11. Flora KP, Cradock JC, Ames MM (1978) A simple method for the estimation of amygdalin in urine. Res Commun Chem Pathol Pharmacol 20: 367–378Google Scholar
  12. Gibaldi M, Nagashima R, Levy G (1969) Relationship between drug concentration in plasma orserum and amount of drug in the body. J Pharm Sci 58: 193–197Google Scholar
  13. Harrison LJ, Gibaldi M (1977) Physiologically based pharmacokinetic model for digoxin disposition in dogs and its preliminary application to humans. J Pharm Sci 66: 1679–1683Google Scholar
  14. Haworth WN, Wylam B (1923) The constitution of the disaccharides. Part IX. Gentiobiose: Its identity with amygdalin biose. J Chem Soc 123: 3120–3125Google Scholar
  15. Ilett KF, Dollery CT, Davies DS (1980) Isoprenaline conjugation — a “true first-pass effect” in the dog intestine. J Pharm Pharmacol 32: 362Google Scholar
  16. Moertel CG, Ames MM, Kovach JS, Moyer RP, Rubin JR, Tinker JH (1981) A pharmacologic and toxicologic study of amygdalin in man. JAMA 245: 591–594Google Scholar
  17. Nikolelis DP, Hadjiioannou TP (1979) Determination of amygdalin in blood serum. Anal Letters B 12:12th vol of series B; if possible on one line 12: 1169–1178Google Scholar
  18. Pichotka J (1975) Stoffwechsel der Organismen. In: Keidel WD (ed) Kurzgefaßtes Lehrbuch der Physiologie. Thieme, Stuttgart, S 7–43Google Scholar
  19. Ram MD, Holroyd B, Chrisholm GD (1969) Measurement of glomerular filtration rate using 131I-diatrizoate. Lancet 1: 397–399Google Scholar
  20. Rieders F (1965) Noxious Gases and vapors I. In: DiPalma JR (ed) Drill's Pharmacology in Medicine, 3nd ed. McGraw-Hill, New York, p 939Google Scholar
  21. Stobaugh JF, Sternson LA, Repta AJ (1978) A clinical method for the analysis of amygdalin in human plasma. Anal Letters B 11: 753–764Google Scholar

Copyright information

© Springer-Verlag 1982

Authors and Affiliations

  • A. G. Rauws
    • 1
  • M. Olling
    • 1
  • A. Timmerman
    • 1
  1. 1.National Institute of Public HealthThe Netherlands

Personalised recommendations