The International Journal of Romanian Society of Endocrinology / Registered in 1938

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January - March 2005, Volume 1, Issue 1
Notes & Comments

Burstein G

A new hperfractionation effect in the pharmacokinetics of dopaminergic agonist (cabergoline) for the long-term treatment of non-functioning pituitar tumours

Acta Endo (Buc) 2005, 1 (1): 121-125
doi: 10.4183/aeb.2005.121

Using mathematical and clinical trial pharmacokinetics for Cabergoline (a dopaminergic agonist used in hyperprolactinaemia and long-term treatment of nonfunctioning tumours), a new ?hyperfractionation? effect is proven. This effect leads to higher steady state plasma concentrations of drug by fractionating multiple dose regimens in more frequent doses of smaller individual amounts. We generalize this effect by formulating a general mathematical condition for any drug to benefit from hyperfractionation. The effect is important in the long-term treatment of non-functioning tumours as one tries to achieve higher steady state plasma concentrations by using small individual doses in order to insure tolerability. This effect is more complex than the accumulation effect known in pharmacokinetics as a one parameter effect (frequency). Hyperfractionation is a two parameter effect for multiple dose regimens (frequency, dose amount).

Keywords: pharmacokinetics, dopaminergic agonists, pituitary tumours, hyperprolactinaemia

Correspondence: Gabriel Burstein, e-mail:


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