Skip to main content
Log in

Pharmacokinetics and safety of l-carnitine infused i. v. in healthy subjects

  • Short Communications
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Summary

The pharmacokinetics and safety of a brief i. v. infusion of l-carnitine 0, 20, 40 and 60 mg/kg have been investigated in 10 healthy subjects.

The diurnal intraindividual variability of plasma carnitine was small (C. V.=3.0, 3.9 and 3.9%, respectively), and the total 24 h excretion in urine was also small and relatively constant: 4.6, 21.5 and 13.0 mg/day in the controls vs 4.6, 20.2 and 6.0 mg/day during treatment in the three subjects to whom saline alone was administered according to a single-blind design. Therefore, the pre-dose level of carnitine was subtracted from the level after dosing for the pharmacokinetic analysis. Plasma carnitine fitted well to a three-compartment open model, with Vc of 0.11–0.20 l/kg and a t1/2γ of 10–23 h. The urine recovery in 24 h was 77.2–95.4%.

There were no objective or subjective side-effects attributable to carnitine, so its i. v. infusion is considered to be safe.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

References

  1. Fritz JB (1968) The metabolism consequences of the effects of carnitine on long chain fatty acid oxidation. In: Gran FC (ed) Cellular compartmentalization and control of fatty acid metabolism 39. Universitetsforlaget, Oslo, pp 39–63

    Google Scholar 

  2. Fritz IB, Kaplan E, Yue KTN (1963) Specificity of carnitine action of fatty acid oxidation by heart muscle. Am J Physiol 197: 297–300

    Google Scholar 

  3. Shug AL, Thomsen JH, Folts JD, Bittar N, Klein MI, Koke JR, Huth PJ (1978) Changes in tissue levels of carnitine and other metabolites during myocardial ischemia and anoxia. Arch Biochem Biophys 187: 25–33

    Google Scholar 

  4. Folts JD, Shug AL, Koke JR, Bittar N (1978) Protection of the Protection of the ischemic dog myocardium with carnitine. Am J Cardiol 41: 1209–1214

    Google Scholar 

  5. Thomsen TH, Shug AL, Yap VU, Patel AK, Karras TJ, DeFelice SL (1978) Improved stress tolerance of the ischemic human Myocardium after administration of carnitine. Am J Physiol 43: 300–306

    Google Scholar 

  6. Waber LJ, Valle D, Neill C, DiMauro S, Shug A, Bartimore MD (1982) Carnitine deficiency presenting as familial cardiomyopathy: A treatable defect in carnitine transport. J Pediatr 101: 700–705

    Google Scholar 

  7. Welling PG, Thomsen JH, Shug AL, Tse FLS (1979) Pharmacokinetics of l-carnitine in man following intravenous infusion of dl-carnitine. Int J Clin Pharmacol Biopharm 17: 56–60

    Google Scholar 

  8. Marquis NR, Fritz IB (1964) Enzymological determination of free carnitine concentrations in rat tissues. J Lipid Res 5: 184–195

    Google Scholar 

  9. Friz IB, Schultz SK (1965) Carnitine acyltransferase. II. Inhibition by carnitine analogue and by sulfhydryl reagents. J Biol Chem 240: 2188–2192

    Google Scholar 

  10. Pearson DJ, Tubbs PK, Chase JFA (1965) Methods of enzymatic analysis 4 (2nd edn). Academic Press, New York, pp 1758–1771

    Google Scholar 

  11. Yamaoka K, Tanigawa Y, Nakagawa T, Uno T (1981) A pharmacokinetic analysis program (MULTI) for microcomputer. J Pharmacobiodyn 4: 879–885

    Google Scholar 

  12. Bickel PJ, Doksum KA (1977) Mathematical statistics: Basic ideas and selected topics. Holden-Day, San Francisco, p 492

    Google Scholar 

  13. Fraenkel G (1953) Study on distribution of vitamin BT (carnitine). Biol Bull 104: 359–371

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Uematsu, T., Itaya, T., Nishimoto, M. et al. Pharmacokinetics and safety of l-carnitine infused i. v. in healthy subjects. Eur J Clin Pharmacol 34, 213–216 (1988). https://doi.org/10.1007/BF00614562

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00614562

Key words

Navigation