Nasal spray administration of bromocriptine: pharmacology and effect on serum prolactin level in puerperal women.

This study was aimed at investigating the absorption of nasally administered bromocriptine and its effect on serum prolactin level. Fifteen physiologically hyperprolactinemia women who had asked to discontinue breast feeding received a single nasal spray administration of 0.8 mg bromocriptine. Serum prolactin levels were measured by radioimmunoassay at 30 and 15 min before drug administration, at the time of administration and at 15, 30, 60, 120, 240, 480 and 720 min after administration; bromocriptine was radioimmunoassayed in only five of the patients from time 0 to 720 min after administration. Serum bromocriptine levels increased rapidly after administration, reached a maximum at 120 min and thereafter declined slowly over the subsequent 10 h. As the bromocriptine level increased there was a decline in the serum prolactin level. The first significant decline in serum prolactin level compared with the baseline level occurred at 30 min after administration and the level continued to decrease significantly until time 120 min. Four hours after administration the mean serum prolactin level was within the normal assay range. The maximum decline in serum prolactin level was reached at 720 min after administration. Correlation analysis between serum bromocriptine and prolactin concentrations yielded a significant negative value between times 0 and 120 min after administration. There was no significant change in mean orthostatic systolic or diastolic blood pressure or in mean heart rate. Only one patient complained of headache and dizziness; another experienced mild transient nausea, and none had vomiting. Ten patients (66.67%) reported light endonasal burning and an unpleasant taste which subsided after a few minutes; no patient showed nasal irritation at nasal examination. In conclusion, nasal administration of 0.8 mg bromocriptine was effective in reducing the serum prolactin level for more than 12 h after administration without inducing significant side-effects.

Nasal spray bromocriptine: effects on serum prolactin in puerperal women.

BACKGROUND: The objective of this study was to investigate the effectiveness of a single nasal spray administration of 0.8 mg bromocriptine in reducing PRL serum levels. METHODS: Eighteen physiologically hyperprolactemic women in the early days of puerperium were randomized to receive nasal bromocriptine or placebo; PRL serum levels were measured by RIA at 45, 30 and 15 minutes before the administration and after the following times: 15, 30, 45, 60, 120, 180, 240, 300, and 480 minutes. RESULTS: After the administration of bromocriptine serum levels of PRL decreased rapidly; the reduction was statistically significant after 45 minutes. Four hours after the administration mean serum levels of PRL resulted in the normal range (< 20 micrograms/l); at the eighth hour the PRL levels were still normal. No one patient complained of any local or systemic side-effects. CONCLUSION: Nasal route seems to be an effective and probably safe administration route for bromocriptine.

Nasal spray vs oral administration of bromocriptine: pharmacology and effect on serum prolactin in puerperal women.

The oral administration of bromocriptine induces a variety of side-effects in about 50-70% of patients, the most common being nausea and vomiting, probably related to the local gastrointestinal effect of the drug. Nasal administration makes it possible to avoid intestinal and liver metabolism. This study compared the serum concentrations of bromocriptine and prolactin (PRL) in twenty puerperal women who had asked to discontinue breast feeding and were randomized to receive a single oral (2.5 mg) or nasal spray dose (0.8 mg) of bromocriptine. Serum bromocriptine and PRL concentrations were measured at various times before and after drug administration. At 15 min, the circulating concentrations of bromocriptine were about eight times higher after nasal than after oral administration; peak serum concentration (CMax) was reached respectively 45 min and 60 min after administration, and was about three times higher after nasal administration (314 +/- 102 pg/ml vs 112.30 +/- 34.47 pg/ml). The reduction in serum PRL concentrations was also more rapid in the nasally-treated group reaching the normal assay range of < 20 micrograms/l within two as against five hours post-administration. Four orally-treated patients complained of nausea; in the nasally-treated group, six patients reported only a mild endonasal burning that disappeared within a few minutes of administration. Our results suggest that the nasal administration of bromocriptine may lead to a reduction in the required overall dose and fewer gastrointestinal side-effects, and may therefore improve therapy compliance.