E. Cicinelli et al., NASAL SPRAY VS ORAL-ADMINISTRATION OF BROMOCRIPTINE - PHARMACOLOGY AND EFFECT ON SERUM PROLACTIN IN PUERPERAL WOMEN, Journal of endocrinological investigation, 19(7), 1996, pp. 427-432
The oral administration of bromocriptine induces a variety of side-eff
ects in about 50-70% of patients, the most common being nausea and vom
iting, probably related to the local gastrointestinal effect of the dr
ug. Nasal administration makes it possible to avoid intestinal and liv
er metabolism, This study compared the serum concentrations of bromocr
iptine and prolactin (PRL) in twenty puerperal women who had asked to
discontinue breast feeding and were randomized to receive a single ora
l (2.5 mg) or nasal spray dose (0.8 mg) of bromocriptine. Serum bromoc
riptine and PRL concentrations were measured at various times before a
nd after drug administration. At 15 min, the circulating concentration
s of bromocriptine were about eight times higher after nasal than afte
r oral administration; peak serum concentration (CMax) was reached res
pectively 45 min and 60 min after administration, and was about three
times higher after nasal administration (314+/-102 pg/ml vs 112.30+/-3
4.47 pg/ml), The I-eduction in serum PRL concentrations was also more
rapid in the nasally-treated group reaching the normal assay range of
<20 mu g/l within two as against five hours post-administration. Four
orally-treated patients complained of nausea; in the nasally-treated g
roup, six patients reported only a mild endonasal burning that disappe
ared within a few minutes of administration. Our results suggest that
the nasal administration of bromocriptine may lead to a reduction in t
he required overall dose and fewer gastrointestinal side-effects, and
may therefore Improve therapy compliance.